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Description.

ZEPAM 0.25 mg Tablets

Generic name: Clonazepam

 

Drug class: Benzodiazepines

 

Dose available: 0.25mg and 0.5mg tablets

General information:

Clonazepam is an Benzodiazepines with prominent anticonvulsant properties indicated for the treatment of panic disorder, with or without agoraphobia.

 

Pharmacokinetics:

Absorption: rapidly and completely absorbed after oral administration

Bioavailability: ~ 90%

Tmax: 1-4 hours

Distribution: 85% bound to plasma protein

Metabolism:  highly metabolized, hepatic metabolism

Elimination: via urine with 2 % unchanged

Half life: 30-40 hours

 

Mechanism of action: The precise mechanism by which clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system resulting in calming effect.

 

Indication:

  • Seizure disorder: Absence seizure with or without Lennox-Gastaut syndrome

Monotherapy or adjunct in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures. In patients with absence seizures (petit mal) who have failed to respond to succinimides, Clonazepam is helpful.

  • Adjuvant in myoclonic seizure
  • Anxiety disorder
  • Panic disorder
  • Bipolar disorder, mixed or maniac episodes
  • REM sleep behavior disorder
  • Tardive dyskinesia

 

 

Dosage and administration:

Seizure disorder (Adults): Initial dose should not exceed 1.5mg/day as TID, dose may be increased from 0.5mg to 1 mg until seizures are adequately controlled.

(Pediatrics): 0.01-0.03 mg/kg/day BD/TID

Panic disorder: 0.25mg OD/BD

 

Dose adjustment:

  • Hepatic impairment: No dose adjustment required
  • Renal impairment: No dose adjustment required

 

Adverse Drug Reaction:

Drowsiness, ataxia, behavioural problems, dizziness, fatigue, constipation, abdominal pain, anorexia, myalgia, blurred vision

Drug-Drug Interaction:

  • Clonazepam may increase the levels/effects of alcohol, CNS depressants, Flunitrazepam,SSRIs, Opioids, Mirtazapine, Pra,ipexole, Ropinirole, Zolpidem
  • The levels/effects of Clonazepam may be increased by Cannabidiol, Doxylamine, Hydroxyzine, Lofexidine, Magnesium sulphate, Mifepristone, Minocycline, Olanzapine, Palbociclib, Tapentadol, Vigabatrin
  • The levels/effects of Clonazepam may be decreased by Phenytoin, Fosphenytoin, Theophylline, Tocilizumab, Siltuximab
  • Concurrent administration of clonazepam and valproate is contraindicated because absence status may be precipitated.

Precaution and warnings:

  • Concomitant administration with Opioids may result in profound sedation, respiratory deression
  • Potentiation of sedation from concomitant use with CNS depressants
  • Patient who are risk of falls
  • Patient with history of drug abuse or alcoholism

Contraindication:  History of hypersensitivity to the drug or its ingredients. Hypersensitivity reactions have included serious dermatological reactions

Pregnancy Category: ‘D

Advantages:

  • Superior safety profile compared to other Benzodiazepines
  • Indicated in patients with Absence seizure (Petil mal) who have failed to respond to succinimides
  • Used in combination with anti-psychotics for the treatment of mania or acute psychosis-induced aggression, when urgent sedation is required
  • Clonazepam has more marked muscle relaxant property compared with other BZDs
  • Clonazepam have more prominent anticonvulsant activity than other BZDs

 

 

 

ZEPAM 0.5

Generic name: Clonazepam

 

Drug class: Benzodiazepines

 

Dose available: 0.25mg and 0.5mg tablets

General information:

Clonazepam is an Benzodiazepines with prominent anticonvulsant properties indicated for the treatment of panic disorder, with or without agoraphobia.

 

Pharmacokinetics:

Absorption: rapidly and completely absorbed after oral administration

Bioavailability: ~ 90%

Tmax: 1-4 hours

Distribution: 85% bound to plasma protein

Metabolism:  highly metabolized, hepatic metabolism

Elimination: via urine with 2 % unchanged

Half life: 30-40 hours

 

Mechanism of action: The precise mechanism by which clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system resulting in calming effect.

 

Indication:

  • Seizure disorder: Absence seizure with or without Lennox-Gastaut syndrome

Monotherapy or adjunct in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures. In patients with absence seizures (petit mal) who have failed to respond to succinimides, Clonazepam is helpful.

  • Adjuvant in myoclonic seizure
  • Anxiety disorder
  • Panic disorder
  • Bipolar disorder, mixed or maniac episodes
  • REM sleep behavior disorder
  • Tardive dyskinesia

 

 

Dosage and administration:

Seizure disorder (Adults): Initial dose should not exceed 1.5mg/day as TID, dose may be increased from 0.5mg to 1 mg until seizures are adequately controlled.

(Pediatrics): 0.01-0.03 mg/kg/day BD/TID

Panic disorder: 0.25mg OD/BD

 

Dose adjustment:

  • Hepatic impairment: No dose adjustment required
  • Renal impairment: No dose adjustment required

 

Adverse Drug Reaction:

Drowsiness, ataxia, behavioural problems, dizziness, fatigue, constipation, abdominal pain, anorexia, myalgia, blurred vision

Drug-Drug Interaction:

  • Clonazepam may increase the levels/effects of alcohol, CNS depressants, Flunitrazepam,SSRIs, Opioids, Mirtazapine, Pra,ipexole, Ropinirole, Zolpidem
  • The levels/effects of Clonazepam may be increased by Cannabidiol, Doxylamine, Hydroxyzine, Lofexidine, Magnesium sulphate, Mifepristone, Minocycline, Olanzapine, Palbociclib, Tapentadol, Vigabatrin
  • The levels/effects of Clonazepam may be decreased by Phenytoin, Fosphenytoin, Theophylline, Tocilizumab, Siltuximab
  • Concurrent administration of clonazepam and valproate is contraindicated because absence status may be precipitated.

Precaution and warnings:

  • Concomitant administration with Opioids may result in profound sedation, respiratory deression
  • Potentiation of sedation from concomitant use with CNS depressants
  • Patient who are risk of falls
  • Patient with history of drug abuse or alcoholism

Contraindication:  History of hypersensitivity to the drug or its ingredients. Hypersensitivity reactions have included serious dermatological reactions

Pregnancy Category: ‘D

Advantages:

  • Superior safety profile compared to other Benzodiazepines
  • Indicated in patients with Absence seizure (Petil mal) who have failed to respond to succinimides
  • Used in combination with anti-psychotics for the treatment of mania or acute psychosis-induced aggression, when urgent sedation is required
  • Clonazepam has more marked muscle relaxant property compared with other BZDs
  • Clonazepam have more prominent anticonvulsant activity than other BZDs

 

 

 

LUCICAINE

Generic composition: Magaldrate 800mg, Simethicone 100mg and Oxetacaine 20mg/10ml

General Introduction

Lucicaine is an antacid that has triple benefits. It provides faster action. It neutralizes the excess acid in the stomach, prevents flatulence as well as makes insensate to pain.

Therapeutic category

  • Anesthetic Antacid

Dosage form available

  • LUCICAINE suspension in 170ml

Base and Flavour

  • In a Peppermint flavoured sorbitol base

Mechanism of Action

Magaldrate: It is a hydrated complex of hydroxy magnesium aluminates which initially reacts with the gastric acid and releases Aluminum Hydroxide and Magnesium Hydroxide.  This will neutralize the excess acid in stomach, increase pH of stomach.

Simethicone: It acts by decreasing the surface tension of gas bubbles, thus facilitating their coalescence and expulsion as flatus or belching also preventing formation and accumulation of mucus-enclosed pockets of gas in digestive tract.

Oxetacaine: It is a local anesthetic which provides faster relief from pain due to ulcers or acidic injury in the stomach. Oxetacaine exerts a local anesthetic effect on the gastric mucosa.

Indications

  • Dyspepsia
  • Esophageal reflux, GERD
  • Epigastric pain
  • Symptomatic relief of Hyperacidity
  • Heartburn
  • Peptic ulcer
  • IBS (Irritable bowel syndrome)
  • Flatulence, abdominal distention, blotting, etc

Dose

For Adults, elderly and children over 12 years of age: 5-20ml three times daily 20 minutes to one hour after meals, and at bedtime, or as required. Not recommended for children below 12 years of age.

Side effects

Chalky taste, Diarrhea, Constipation, Allergic reaction

Precautions

  • Avoid drinking anything immediately after taking this medicine as that can reduce its effectiveness.
  • Do not take antacid medicines half an hour before or after taking this medicine.

Contraindications

  • Hypersensitivity with use of aluminum or magnesium containing antacids

Advantages

  • Oxetacaine containing antacids are being recommended as complementary to PPIs in GERD and related disease
  • The local anesthetic agent helps relieve the pain caused due to hyperacidity and aluminum and magnesium hydroxide
  • Good alternative for quick symptomatic relief
  • The therapeutic spectrum of Anesthetic antacid will increase manifold, if in addition with Anti-flatulent Simethicone
  • Some investigations has reported that Oxetacaine containing antacid produces persistent increase in gastric pH to 3.5 or above
  • The anesthetic component Oxetacaine remains non-ionized at hyperacidic condition and produces a prolonged anesthetic effect (numbing effect) on the walls of the stomach, thereby bordening the therapeutic spectrum of antacids besides the normal process of neutralizing acid

 

Manufactured by:

MERYL BM

Generic composition: Terbutaline + Bromhexine

General introduction:

Terbutaline + Bromhexine is the combination of Bronchodilator and Mucolytic agent, hence the brand name MERYL BM.

Therapeutic category

  • Bronchodilator and mucolytic agent

Dosage form available

  • Each 5ml contains Terbutaline sulphate IP 2.5mg and Bromhexine HCl IP 8mg

 

Mechanism of action:

Terbutaline is a beta-adrenogernic agonist with preferential effects exerting bronchodilating and smooth muscle relaxation effects. Its pharmacologic mechanism is due to the stimulation of adenyl cyclase resulting in increased intracellular level of cyclic AMP. Elevated cAMP triggers relaxation of bronchial smooth muscle and inhibition of release of inflammatory mediators.

Bromhexine is a mucolytic that enhances mucus transport by increasing the amount of thin, watery, bronchial secreation and thereby decreasing viscosity. It increases cilia activity, resulting in enhanced mucociliar clearance, and has a secretolytic and scretomotor effect in the bronchial tract, which aids expectoration and eases cough.

Pharmacokinetics:

Terbutaline

Absorption: Tmax- 0.5h-1.5h, Bioavailability- 14-15%

Distribution: distributed to body tissues and is not highly bound to plasma protein

Metabolism: Metabolite: Sulfate conjugate

Excreation: Fecal (less than 1%), Renal (30-50%), half life- 3.4hr

 

Bromhexine

 

Absorption: absorbed from GIT

Distribution: distributed to body tissues and highly bound to plasma proteins

Metabolism: Metabolite: Sulfate conjugate

Excreation: 85-90% of dose is excreted in urine, half life: upto 12 hours

Crosses Blood brain barrier and small amounts cross the placenta 

Indication:

  • Bronchitis
  • Bronchial asthma
  • COPD
  • Emphysema
  • Bronchospasm

 

Dose: 5-10ml 3-4 times a day

Or As directed by physician.

Adverse effect: Nausea, Indigestion, Bloating, Diarrhea, Dizziness, Headache, Tremor, Sweating, Skin rash, Increased heart rate, Palpitations

Contraindication:

  1. Hypersensitivity to Bromhexine or any symphathomimetic amines or any component of terbutaline sulfate products.

Preacautions:

  1. Stop taking Terbutaline + Bromhexine and inform your doctor if your cough persists for more than 1 week, tends to recur, or is accompanied by a fever, rash or persistent headache.

Pregnancy category: C (Terbutaline), A (Bromhexine)

Advantage:

  • Terbutaline is a bronchodilator which relaxes muscles in your airways and widens the airways.
  • Bromhexine is a mucolytic which thins and loosens mucus (phlegm), making it easier to cough out. Together, they make breathing easier.

 

 

THYLOBIN 1500

THYLOBIN 1500

Generic composition:

Each uncoated tablet contains: Mecobalamin JP 1500mcg

Drug Class: Anti-neuropathic Vitamin B12 Supplement

Description:

THYLOBIN 1500 is Mecobalamin 1500 microgram which is a naturally occuring and pure form of Vitamin B12. It regulates certain vital bodily functions like cell multipication, blood formation, and protein synthesis. It is used to Vitamin B12 deficiency in people with Megaloblastic anemia and Pernicious anemia.

Mechanism of action:

It works by functioning in the production of a compound called myelin, which covers and protect nerve fibres. Mecobalamin rejuvenates the damaged neuron. Without enough Mecobalamin, myelin sheath does not form properly due to which nerve fibres suffers and people experience irreversible nerve damage. An intrinsic factor made in the stomach, must be present in the intestinal tract to allow its proper absorption. People lacking this factor show Vitamin B12 defeiciencies such as Pernicious anemia.

Mecobalamin acts as coenzyme in the synthesis of methionine from homocysteine for various metabolic functions that are essential in cell replication and haematopoiesis. It also promotes nucleic acid and protein synthesis in nerve cells, production of all epithelial cells and maintenance of myelin throughout the nervous system. It causes increased myelination via promotion of lecithin synthesis, increase in nerve fibre excitability, and promotion of maturation and division of erythroblasts.

Pharmacokinetics

Mecobalamin binds with an intrinsic factor and form a complex which is absorbed in distal ileum. Mecobalamin adminstered orally is actively absorbed form the Gastrointestinal tract. Peak plasma concentration is reached in 3 hours as per oral dose. The half life of Mecobalamin is 6 days. It is extensively bound to Transcobalamin, disturbed to every cell of the body. It crosses placenta and enters breast milk. Excreation is occurred via urine.

Indication

  • Peripheral neuropathy
  • Diabetic neuropathy
  • Neuropathic pain
  • Vitamin B12 deficiency
  • Megaloblastic anemia
  • Pernicious anemia
  • Homocysteinemia

 

Dose

The recommended dose is 1500mcg once daily in the morning. May be taken with food or without food or as directed by the physician.

Side effects

Nausea, vomiting, diarrhea, headache, abdominal pain, skin rash, anorexia

Drug interaction

  • Decreased absorption with amino salicyclic acid, Chloramphenicol, Colchicine, H2 Blockers, Neomycin, PPIs
  • Decreased serum concentration with oral contraceptives
  • Impaired therapeutic response with large and continuous doses of folic acid
  • Reduced absorption with alcohol intake

Precautions

Pregnancy and Lactation

Pregnancy Category: ‘C’

Contraindication

Hypersensitivity to Mecobalamin and other derivatives of Vitamin B12.

Advantages

  • Natural form and most active form of Vitamin B12
  • Acts as neuroprotectives and promotes myelination in neurons
  • Significantly effective in peripheral neuropathy in both diabetic and non diabetic patients

 

Alprazolam (Alprazolam 0.25mg)

ALPRALAM (Alprazolam 0.25mg tablets)

Introduction

Alprazolam is a fast-acting tranquilizer of medium duration in the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole rings indicated for the treatment of anxiety and panic disorders.

It is intermediate acting benzodiazepines. It belongs to a class of drugs called Anti-anxiety, Anxiolytics Benzodiazepines. It may be used alone or in combination with medications.

Mechanism of action

Alprazolam binds to Benzodiazepines site of GABA-A receptors in the brain and enhancing the GABA-mediated synaptic inhibition and resulting in calming effect.

Binding of alprazolam to the GABAA receptor, a chloride ion channel opens and enhances the effects of GABA thus chloride enters the cell which makes it more resistant to depolarization. Therefore, alprazolam has a depressant effect on synaptic transmission to reduce anxiety.

Pharmacokinetic

Alprazolam is rapidly absorbed in GI tract, oral bioavailability is 84-91%, alprazolam is 80% protein bound, alprazolam is metabolized via liver (substrate of CYP3A4) , eliminated in the urine, half life is 11.2 hours; in elderly 16.3 hours,  volume of distribution is 0.8-1.3L/kg, crosses the blood brain barrier.

Dose

  • 25mg to 0.5mg three times a day; maximum daily dose is 4mg, dose may be increased at a interval of 3 to 4 days, dose tapering should be done while discontinuing the drug by not more than 0.5 mg every 3 days.

Dose Adjustment:

  • Renal impairment: No specific recommendation
  • Hepatic impairment: 0.25mg 2-3 times a day; increase needed and tolerated
  • Geriatrics: 0.25mg 2-3 times a day; increase needed and tolerated

Indication

Generalized anxiety disorder, anxiety associated with depression, panic disorder with or without agoraphobia.

Off label use in insomnia, premenstrual syndrome and depression.

Side effects

Decrease in appetite (7-28%), increase in appetite (7-33%), constipation, reduced salivation, xerostomia, weight gain, Sedated, Lightheadedness, somnolence, in-coordination, memory impairment, confusion, irritability, feeling anxious early in the morning, reduced libido, fatigue, Seizure due to drug withdrawal

Drug Interactions

  • Use with other CNS
  • Digoxin
  • Imipramine and Despiramine
  • OCPs
  • Fluoxetine, Propoxyphene
  • Drug that inhibit CYP3A enzyme.

Precautions

  • Geriatric patients: Avoid use in elderly patients due to greater BZD sensitivity, esp. in patients with history of falls and fractures, cognitive impairment or dementia and delirium
  • Use caution when driving or operating heavy machinery
  • Risk of seizure recurrence upon rapid discontinuation; slow taper recommended for patients with history of seizures
  • Uricosuric effect
  • Mania/Hypomania reported in patients with depression
  • Suicidal thoughts been reported, increased monitoring recommended with patients with depression
  • Birth defect risk in pregnant mothers, avoid use in first trimester
  • Use in pediatric patients

Contraindications

  • Hypersensitivity to Benzodiazepines
  • Pregnancy
  • Nursing mothers: Excreted in breast milk

Pregnancy category: Category D

Advantages:

  • High potency anxiolytic BZD which in addition has some mood elevating action in mild depression

 

 

 

 

 

 

 

 

FLUVO‌

Generic composition: Fluvoxamine Maleate

 

Introduction

Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor (SSRIs); belonging to the chemical series, the 2-aminoethyl oxime ethers of alkyl ketones. Fluvoxamine is a selective serotonin-reuptake inhibitor majorly used to treat obsessive-compulsive disorder.

 

Therapeutic Category

  • Antidepressants ; Class: SSRIs

 

Dosage forms available

  • FLUVO 50 mg
  • FLUVO 100 mg

 

Mechanism of action

The exact mechanism of action of fluvoxamine has not been fully determined, but appears to be linked to its inhibition of CNS neuronal uptake of serotonin. Fluvoxamine blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. Studies have also demonstrated that fluvoxamine has virtually no affinity for α1– or α2-adrenergic, β-adrenergic, muscarinic, dopamine D2, histamine H1, GABA-benzodiazepine, opiate, 5-HT1, or 5-HT2 receptors, despite having an affinity for binding to σ1 receptors.

 

Pharmacokinetics

Well absorbed, oral bioavailability 53% and not significantly affected by food, half-life 9-28 hours, plasma protein binding is about 80%, metabolized in liver and excreted by urine.

 

Indications

  • Obsessive-compulsive disorder (OCD)
  • Depression
  • Generalized anxiety disorder (GAD)
  • Social Anxiety Disorder (SAD)
  • Post-traumatic Stress Disorder (PTSD)

 

Dose

  • Adult: Initial dose 50 mg orally once a day at bedtime, increased by 50 mg increments every 4 to 7 days, maximum 300mg/day.
  • Pediatric: 25mg orally a day at bedtime, increased by 25mg every 4-7 day, maximum 200mg/day
  • Dose reduction and slow titration recommended in hepatic impairment and elderly

 

Side effects

Possible side effect includes: anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, somnolence, liver toxicity, mania, increase urination, seizures, sweating, tremors, drowsiness, dizziness, (sleep problems) insomnia, abnormal ejaculation, muscle pain, loss of appetite

 

 Interactions

  • Smoking may decrease effectiveness of fluvoxamine
  • Concurrent use with Tricyclic Antidepressants(TCAs) may increase plasma levels of fluvoxamine
  • Decrease metabolism and may increase effects of some beta blockers (propranolol), some benzodiazepines, carbamazepine
  • Increase risk of bleeding with NSAIDS, aspirin, clopidogrel, or warfarin
  • Concentrations of thioridazine and its two active metabolites, mesoridazine and sulforidazine, increased threefold following co administration of fluvoxamine.
  • Reduces the clearance of benzodiazepines metabolized by hepatic oxidation (e.g., alprazolam, diazepam, midazolam, triazolam, etc).
  • Elevated serum levels of clozapine have been reported in patients taking fluvoxamine maleate and clozapine.

 

Precaution

  • Pregnancy category C
  • Gradual withdrawal recommended
  • Patients with history of seizure

 

Contraindication

  • Hypersensitivity to fluvoxamine or other SSRIs or any excipient
  • Concurrent use of MAOIs (or within 14 days of discontinuing fluvoxamine)

 

Tyline

Generic composition: Amytryptyline HCl

General description

Tyline is Amitriptyline HCl, a dibenzocycloheptadiene derivative, is a white, or practically white, odourless, crystalline compound which is freely soluble in water and alcohol. Tyline is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain.

 

Therapeutic Group:

  • Tricyclic Antidepressant(TCA)

 

Dosage forms available

  • TYLINE 10mg Tablets
  • TYLINE 25mg Tablets

 

Uses

  • Endogenous Depression, Anxiety.
  • Offlabel use: Chronic pain management in diabetic nephropathy, peripheral nerve disease, fibromyalgia etc.

 

Dosage

  • 75 mg daily in divided dose or 50-100 mg bedtime; can be increased up to 150mg per day. Maintenance dose of 50-100 mg per day preferably bedtime after satisfactory improvement seen.
  • Not recommended for children under 12 yrs

 

Mechanism of Action

Amitriptyline inhibits the membrane pump mechanism responsible for re-uptake of norepinephrine and serotonin post-synaptic neurons. Pharmacologically, this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity.

 

Pharmacokinetics

Absorption: Rapidly absorbed, bioavailability is 30-60% due to first pass metabolism, peak plasma concentrations are reached 2-12 hours after oral or intramuscular administration

Distribution: Apparent volume of distribution estimated after intravenous administration is 1221 L±280 L; range 769-1702 L (16±3 L/kg), it is found widely distributed throughout the body

Metabolism: metabolism of amitriptyline occurs mainly by demethylation (CYP2C19, CYP3A4) as well as hydroxylation (CYP2D6) followed by conjugation with glucuronic acid. The main active metabolite is the secondary amine, nortriptyline.

Elimination:  Amitriptyline and its metabolites are mainly excreted in the urine

Half-life: elimination half-life of amitriptyline after oral administration is about 25 hours.

 

Adverse effects:

Common side effects include dizziness, headache, weight gain, side effects common to anticholinergics, cognitive effects such as delirium and confusion, mood disturbances such as anxiety and agitation, cardiovascular side effects such as orthostatic hypotension, sinus tachycardia, and QT-interval prolongation, sexual side effects such as loss of libido and impotence, sleep disturbances such as drowsiness, insomnia and nightmares, blurred vision and hepatic failure.

 

Contraindications:

  • In patients who have shown prior hypersensitivity to it.
  • It should not be given concomitantly with Monoamine Oxidase Inhibitors (MAOIs). Hyperpyretic crises, severe convulsions, and deaths have occurred in patients receiving TCAs and MOAIs given simultaneously. A minimum of 14 days interval should be allowed between administrations of two.
  • Should not be given with Cisapride due to the potential for increased QT interval and increased risk for arrhythmia.
  • Not recommended for use during the acute recovery phase following myocardial infarction.

 

 

Precautions:

  • Gradual withdrawal recommended.
  • Pregnancy category C
  • Schizophrenia or manic depression
  • Increase in suicidal tendency
  • Caution in hepatic impairment
  • Reduced dose for elderly patients recommended

 

Drug Interactions:

  • Topiramate
  • Cardiovascular drugs like quinidine, antiarrhythmics like propafenone and flecainide.
  • Caution is indicated in the co-administration of TCAs with any of the SSRIs and also in switching from one class to the other especially with fluoxetine, because of long half-life and active metabolite.
  • Caution when Amitriptyline given with anticholinergic agents or sympathomimetic drugs, including epinephrine combined with local anesthetics; hyperpyrexia has been reported.
  • Concurrent administration with ethchlorvynol: Transient delirium has been reported.
  • Amitriptyline hydrochloride may block the antihypertensive action of guanethidine or similarly acting compounds.
  • Caution in patients with history of seizures.
  • Close supervision is required when Amitriptyline hydrochloride is given to hyperthyroid patients or that receiving thyroid medication.
  • Cimetidine, phenothiazines, carbamazepine; alters metabolism of Amitriptyline.
  • Amitriptyline may enhance the response to alcohol and the effects of barbiturates and other CNS depressants.
  • Delirium has been reported with concurrent administration of Amitriptyline and disulfiram.

 

Advantages:

  • There is evidence that the TCAs (esp Amitriptyline) are more efficacious for severe (melancholic/endogenous) depression than SSRIs and proven analgesic effects
  • The only documented and most widely used prophylactic therapy for chronic tension-type headache
  • Small efficacy advantage over other tricyclic antidepressants
  • Relatively early onset of antidepressive effect
  • Fewer gastrointestinal and sexual side effects than SSRIs.

Trisone T

TRISONE-T

Generic composition: Mometasone furoate 0.1% and Terbinafine 1% cream

General Introduction

Mometasone furoate cream is a synthetic corticosteroid with anti-inflammatory activity which is for topical use.

Terbinafine is a synthetic allylamine antifungal. It is highly lipophilic in nature and tends to accumulate in skin, nails, and fatty tissues.

Therapeutic category

  • Corticosteroids and combinations

Dosage form available

  • TRISONE-T Cream

Mechanism of action

Terbinafine inhibits the enzyme squalene monooxygenase (also called squalene epoxidase), preventing the conversion of squalene to 2, 3-oxydosqualene, a step in the synthesis of ergosterol. This inhibition leads to decreased ergosterol, which would normally be incorporated into the cell wall, and accumulation of squalene, ultimately inhibits growth of fungi.

Mometasone furoate binds to a glucocorticoid receptor; receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Mometasone furoate also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB)

Dosage and administration

Apply a thin layer of the cream to the affected area as instructed by the doctor. Do not apply in larger or smaller quantities than recommended. Do not cover the application area with bandages or other coverings unless specifically instructed by the doctor.

Uses

  • Used for treatment of topical fungal infections associated with redness, swelling, itching.

Side effects

  • Application site reactions (burning, irritation, itching and redness), Skin peeling

Contraindications

  • Known allergy to mometasone, terbinafine

Precautions

  • Pregnancy and Lactating mothers
  • Use with caution in patients with compromised immune systems.
  • Photosensitivity (avoid exposure to sunlight)

Trisone

TRISONE

Generic composition: Mometasone Furoate

General Introduction

Mometasone furoate Cream, 0.1% contains mometasone furoate for topical use. Mometasone furoate is a synthetic corticosteroid with anti-inflammatory activity.

Mometasone Cream is a corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses in patients 2 years of age or older.

Therapeutic category

  • Corticosteroids

Dosage forms available

  • TRISONE 0.1% Cream

Mechanism of action

Like other topical corticosteroids, mometasone furoate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

 

Pharmacokinetics

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle and the integrity of the epidermal barrier. Studies in humans indicate that approximately 0.4% of the applied dose enters the circulation after 8 hours of contact on normal skin without occlusion. Inflammation and/or other disease processes in the skin may increase percutaneous absorption.

 

Uses

  • Atopic and Contact Dermatitis
  • Psoriasis
  • Lichen Planus

Dosage

  • Apply to the affected area once a day twice a day as directed by the doctor.

Side effects

  • Skin rash, itching, redness, dryness, burning, tingling, thinning or softening of skin,

Precautions

  • Pregnancy category: C
  • Topical corticosteroids may increase the risk of posterior sub capsular cataracts and glaucoma.

Contraindications

  • Hypersensitivity to any ingredients of Mometasone.

Mycol

Generic composition: Clotrimazole

General Introduction

Clotrimazole is an imidazole group of anti-fungal agent. Topical application of an antifungal may reduce the risk of transmission.

Therapeutic category

  • Anti-fungal (Topical)

Dosage forms available

  • MYCOL 1% Cream

Mechanism of action

  • Clotrimazole acts primarily by damaging the permeability barrier in the cell membrane of fungi. Clotrimazole causes inhibition of ergosterol biosynthesis, an essential constituent of fungal cell membranes.
  • If ergosterol synthesis is inhibited, the cell is no longer able to function, as ergosterol directly promotes the growth of fungal cells.

Pharmacokinetics

Clotrimazole is 98% protein bound, undergoes hepatic metabolism and eliminiated via hepatic route.

Uses

  • Tinea Infections
  • Candidiasis

Dosage

  • Apply a thin layer over affected area two to three times a day or as directed by dermatologists.

Side effects

  • Nausea, vomiting, unpleasant mouth sensations and pruritus

 Precautions

  • Pregnancy category C
  • Hepatic Impairment
  • For external use only

Contraindications

  • Contraindicated in patients who are hypersensitive to any of its components.

Newfin

General Introduction

Newfin is a synthetic allylamine anti-fungal agent.

Generic composition: Terbinafine

Therapeutic category

  • Anti-fungal

Dosage forms available

  • NEWFIN 1% cream
  • NEWFIN 250mg Tablets

Mechanism of action

Terbinafine inhibits the enzyme squalene monooxygenase (also called squalene epoxidase), preventing the conversion of squalene to 2, 3-oxydosqualene, a step in the synthesis of ergosterol. This inhibition leads to decreased ergosterol, which would normally be incorporated into the cell wall, and accumulation of squalene.

Pharmacokinetics

Absorption: Well absorbed from GI tract,

Distribution: extensively distributed to hair follicle, nails, scalp and face

Elimination: Approximately 80% of dose is eliminated in urine and remainder in feces

Half-life: Oral terbinafine has half life of approximate 36 hours

Uses

  • Athelet’s foot
  • Jock itch
  • Ringworm
  • Candidiasis
  • Onychomycosis

Dosage

  • 1 tablet to be taken once a day
  • Cream to be applied in affected area once or twice a day.

 Side effects

Diarrhea, nausea, skin rash, upset stomach, headache, abnormal liver function test, taste disturbances,

Contraindication

History of allergic reaction to oral terbinafine because of the risk of anaphylaxis.

Pregnancy category: B

Drug Interactions

  • increase or decrease in prothrombin times in patients concomitantly taking oral terbinafine and warfarin.
  • Terbinafine decreases the clearance of caffeine by 19%. Terbinafine increases the clearance of cyclosporine by 15%.

Precautions

Hepatic insufficiency

Lucotin

Generic composition: Luliconazole

General description

Luliconazole is a topical antifungal agent that acts by unknown mechanisms but is postulated to involve altering the synthesis of fungi cell membranes. It is an imidazole antifungal.

Therapeutic category

  • Anti-fungal

Dosage forms available

  • Luliconazole 1% Cream (Topical use)

Mechanism of action

The exact mechanism of action for luliconazole’s anti-fungal activity is still not known, but luliconazole is thought to inhibit the enzyme lanosterol demethylase. Lanosterol demethylase is needed for the synthesis of ergosterol, which is a major component of the fungus cell membranes.

Pharmacokinetics

About 99% plasma protein bound,

Uses

  • Athlete’s foot (Tinea Pedis)
  • Jock itch (Tinea Cruris)
  • Ringworm (Tinea Corporis)
  • Onychomycosis

Direction of use

  • Apply once daily on the affected area for 7 to 14 days; two week for Tinea pedis and one weeks for Tinea corporis, Tinea cruris; treatment may prolong depending upon the clinical condition.

Side effects

Less common: Itchiness, redness and sensitivity around the area of use.

 Precautions

  • Pregnancy and Lactation
  • Luliconazole cream is for external use only. Do not let luliconazole get into your eyes, nose, or mouth, and do not swallow it. Do not use luliconazole cream in the vaginal area. Improper use may cause skin erosion.

Contraindications

Hypersensitivity to Luliconazole or its excipients.

Kerocid

KEROCID

Generic composition: Salicylic acid

General Introduction

Kerocid is salicylic acid, topical ointment. Salicylic acid belongs to a group keratolytics, used in the treatment of scaly skin where the skin becomes thickened, scaly and flaky.

 

Therapeutic category

  • Keratolytic

Dosage forms available

  • KEROCID 40% ointment

 

Mechanism of action

 

It works by softening keratin, a protein that forms part of the skin structure thus, helps to loosen dry scaly skin making it easier to remove.

In acne, topical salicylic acid helps slow down shedding of the cells inside the follicles, preventing clogging. Salicylic acid also helps break down blackheads and whiteheads.

 

 

Uses

  • Psoriasis
  • Corns and calluses
  • Lichen simplex
  • Ichthyosis
  • Chronic atopic dermatitis
  • Viral warts

Dose

Adults, children and the elderly: apply one to two times daily to  affected areas depending upon condition or as directed by the dermatologists.

 

 

Contraindications

  • Hypersensitivity or sensitivity to any other ingredient in the preparation

 

 

Side effects

  • Mild stinging may occur especially on broken skin and when higher concentrations are used
  • Possible sensitivity reactions, drying and irritation

 

 

Precautions

  • Not on broken or inflamed skin
  • Salicylate toxicity when applied over large areas or to skin of neonates

 

 

Simagyl Forte Suspension

Generic composition: Metronidazole 100mg and Diloxanide furoate 125mg/5ml

General Introduction

Metronidazole is a commonly used antibiotic, belonging to the nitroimidazole class of antibiotics. Diloxanide furoate is a luminal amoebicide.

Therapeutic category

  • Anti-protozoal

Dosage forms available

  • SIMAGYL Forte Suspension

Mechanism of action

Unionized metronidazole is readily taken up by anaerobic organisms and cells and reduced to its active form in intracellular. The electron transport proteins necessary for this reaction are found only in anaerobic bacteria. Reduced metronidazole then disrupts DNA’s helical structure, thereby inhibiting bacterial nucleic acid synthesis. This eventually results in bacterial cell death.

Diloxanide furoate destroys the trophozoites of E. histolytica that eventually form into cysts. The cysts are then excreted by persons infected with asymptomatic amoebiasis.

Pharmacokinetics

Metronidazole is rapidly absorbed after oral administration with peak plasma concentrations occur after 20 min to 3 hours, undergoes hepatic metabolism, elimination half-life of metronidazole is 7 – 8 hours.

Diloxanide furoate is hydrolysed into diloxanide and furoic acid under the combined action of bacterial and gut esterases. After absorption, diloxanide is very rapidly conjugated to form a glucuronide. In circulating blood, it is present to about 99% as a glucuronide and 1% as free diloxanide. Diloxanide is predominantly excreted in the urine. It is believed that the unabsorbed diloxanide is the active anti-amoebic substance, up to 10% remaining in the gut, which is subsequently excreted as diloxanide in the faeces.

Uses

  • Amoebiasis and Giardiasis
  • Prevention and treatment of anaerobic infection

 Dosage

  • 5-10 ml three times a day

Side effects

  • Seizures, headache, dizziness, peripheral neuropathy, unpleasant metallic taste, furred tongue, GI disturbances

Precautions

  • The drug should be used with special precaution in renal and hepatic impairment.
  • Alcoholic beverages should be avoided during the course.

Contraindications

  • first trimester pregnancy
  • Lactation
  • Severe hepatic failure
  • Hypersensitivity
  • Active CNS disease, serious neurological disease and seizures

Drug Interactions

  • Disulfiram like reaction with alcohol
  • Acute psychoses with disulfiram
  • Additive or synergistic effect with other antimicrobials
  • Enhances action of coumarin anticoagulants
  • Blood levels increased by cimetidine
  • Effect reduced by phenobarbitone

Vigoran

VIGORAN

Introduction

Nutrition is inevitable for the growth and development of the body. We fulfill the need from the food. Vigoran is a B-complex with Zinc.

Compositions

Each 5ml contains                           

Thiamine HCl BP………………………………………………………..5 mg

Riboflavin Sodium Phosphate BP …….…………………..……..2.5mg

Pyridoxine HCl BP…………………………………………..……….. 1.5 mg

Nicotinamide BP……………………………………………..………… 45 mg

Cyanocobalamin BP…………………………………..…………..…… 5 mcg

Zinc Sulphate BP…………………………………………………………20mg

Dexpanthenol USP…………….………………………….………..…….5 mg

Each Capsule contains

Thiamine mononitrate BP………………………………….………. 10 mg

Riboflavin BP………………………………………………….………… 10 mg

Pyridoxine HCl BP………………………………………………………. 3 mg

Niacinamide BP..…………………………………………………….…. 35 mg

Nicotinic acid BP…………………….…………………………….……..15mg

Calcium Pantothenate BP……………………………………….….12.5mg

Folic acid BP……………………………………………………….………..1mg

Cyanocobalamin BP…………………………………………….…….15 mcg

Zinc Sulphate BP…………………………………………………………60mg

 

 

Thiamine Mononitrate: Thiamine deficiency causes:

  • Lesions of central and peripheral nervous system.
  • Weakens the heart and causes peripheral vasodilatation
  • Gastrointestinal tract disturbances

 

Riboflavin: Normally combines in the tissues to form co enzymes. Riboflavin deficiency frequently occurs in association with thiamine and/or Niacin and causes deficiency syndrome like Pellagra, beriberi, sprue, and kwashiorkor. Deficiency causes:

  • Digestive disturbances
  • Burning sensation of the skin and eyes
  • Cracking at the corners
  • Headache, Mental depression, forgetfulness and so on.

 

Pyridoxine: Pyridoxine functions as a coenzyme for many chemical reactions related to amino acids and protein metabolism. The deficiency may result into

  • Dermatitis
  • Decreased rate of growth
  • Development of fatty liver anaemia
  • Evidence of mental deterioration
  • Rarely causes seizures, dermatitis, and GI disturbances in children

 

Cyanocobalamin: The intrinsic factor (a glycoprotein secreted by the gastric acid forming cells) acts solely as a vehicle for carrying the important extrinsic factor into the body via receptors. Vit B12 is essential for DNA synthesis. Cyanocobalamin deficiency causes:

  • Pernicious anaemia
  • Demyelination of the large nerves fibres of the spinal cord

 

Nicotinamide: Functions in the body as coenzymes in the form of Nicotinamide Adenine Dinucleotide (NAD) and Nicotinamide adenine Dinucleotide Phosphate (NADP). Nicotinamide deficiency may cause:

  • Simple physiologic changes such as muscle weakness and poor glandular secretion may occur. But in severe deficiency actual death of tissue ensues.
  • Pathological lesions appear in many parts of the central nervous system and permanent dementia or many types of psychoses may result.
  • Skin develops cracked, pigmentation in injured areas being unable to repair the tissues.
  • Intestine irritation and inflammation of the mucous membrane of the mouth and other parts of GI tract instituting many digestive abnormalities resulting in gastrointestinal haemorrhage.
  • Pellagra and canine disease called black tongue (This is common who mainly depend on corn food as it is deficient in amino acid.

 

Calcium Pantothenate: Calcium pantothenate supplies calcium and elemental calcium. The role of calcium is well established in the formation of bone, prevention of osteoporosis and its role as bivalent ions for cellular function of heart and blood vessels as well as muscles. Low calcium can cause spontaneous discharge of nerve fibers resulting in tetany.

Pantothenic acid is mainly incorporated in the body into coenzyme A (CoA), which has many metabolic roles in the cells. The deficiency of pantothenic acid can lead to depressed metabolism of both carbohydrates and fats.

Dose

  • 1 capsule once daily
  • 5ml twice daily

Symol

Generic composition: Paracetamol

General Introduction

Symol contains the active ingredient, paracetamol, widely used analgesic and antipyretic

Therapeutic category

  • NSAIDs

Dosage forms available

  • SYMOL Tablets 500mg
  • SYMOL Suspension 125mg/5ml

Mechanism of action

Paracetamol is para-amino phenol derivative that exhibits analgesic and anti-pyretic activity. The mechanism of action is dependent on the inhibition of prostaglandin synthesis.

Pharmacokinetics

It is rapidly absorbed from the gastrointestinal tract, its systemic bioavailability being dose-dependent and ranging from 70 to 90%. Its rate of oral absorption is predominantly dependent on the rate of gastric emptying, being delayed by food. Paracetamol is also well absorbed from the rectum. It distributes rapidly and evenly throughout most tissues and fluids. Paracetamol is extensively metabolised (predominantly in the liver), the major metabolites being the sulphate and glucuronide conjugates and excreted in the urine.

Uses

  • Reduces fever
  • Relief of persistent pain associated with osteoarthritis and muscle aches and pains such as backache.
  • Paracetamol also provides effective, temporary relief of pain and discomfort associated with headache, tension headache, period pain, toothache, pain after dental procedures, and cold & flu.

Dosage

The common adult dose is 500 mg to 1000 mg two to three times a day or depending upon the condition. The recommended maximum daily dose, for adults, is 4000 mg

Contraindications

  • In hypersensitivity to paracetamol or to any of the excipients.

Adverse Effects

  • Dyspepsia, nausea, allergic and haematological reactions although reports of adverse reactions are rare.

Drug Interactions

  • Anticoagulant dosage may require reduction if Paracetamol medication is prolonged.
  • Paracetamol absorption from immediate release preparations is increased by drugs which increase gastric emptying, eg metoclopramide and decreased by drugs which decrease gastric emptying, egpropantheline, However, concurrent administration of metoclopramide may reduce the absorption of paracetamol from this sustained release dosage form, as it accelerates gastric emptying and intestinal transit.
  • Paracetamol may increase chloramphenicol concentrations.
  • The likelihood of paracetamol toxicity may be increased by the concomitant use of enzyme inducing agents such as alcohol or anticonvulsant drugs.

Precautions

  • Should be administered with caution to patients with hepatic or renal dysfunction.

Panoflam

Generic composition

  • For tablet– Ibuprofen 400mg and Paracetamol 500mg Tablets
  • For Suspension: Ibuprofen 100mg and Paracetamol 125mg / 5ml

General Introduction

Inflammation is one of the body’s prime responses to any injury or disease. Of the five classical symptoms of inflammation (redness, heat, pain, edema and functional limitations), the most common would be pain. Since inflammation and pain co-exist in many situations, the scope exists across specialties for the use of a potent anti-inflammatory-analgesic combination.

Therapeutic category

  • Non-steroidal Anti-inflammatory drugs (NSAIDs)

Dosage forms available

  • PANOFLAM Tablets
  • PANOFLAM Suspension

Mode of action

Non-Steroid Anti-inflammatory drugs like Ibuprofen reduce inflammation by inhibition of prostaglandin synthesis at the site of inflammation while Paracetamol acts on the CNS to produce analgesia and anti-pyretic effect; has negligible anti-inflammatory action in therapeutic doses.

Pharmacokinetics

Ibuprofen is rapidly absorbed. The bioavailability of the drug is minimally altered by the presence of food.

Uses

  • Rheumatic conditions such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis.
  • Low back pain.
  • Infective inflammatory conditions such as tonsillitis, pharyngitis, otitis media, pharyngitis, and inflammatory conditions in gynecology, urology
  • Reduce mild to moderate pain associated with migraine, headache, backache, period (menstrual) pain, dental pain

 Dosage

  • Adults and children (12 years and over): One tablet every 8 hourly.
  • Children (under 12 years): Suspension Half measure (5 ml) to one measure (10 ml) thrice daily

Contraindications

Ibuprofen is contraindicated in patients with peptic ulcers, bronchial asthma, recent GI bleeding and in known hypersensitivity to the drug. Paracetamol is contraindicated in patients with hepatic dysfunction.

Adverse Reactions

Ibuprofen: Dyspepsia, heart burn, GI bleeding, rash, asthmatic attacks, thrombocytopenia, drug induced ulcer, drowsiness, hepatic necrosis, diarrhora, headache, dizziness

Paracetamol: In recommended doses, the side effects of paracetamol are mild to non-existent

Drug Interactions

Ibuprofen:

  • Ibuprofen antagonizes the effects of furosemide and thiazides.
  • Aspirin displaces the Ibuprofen from binding sites.
  • Increases risk of GI ulceration and bleeding with anticoagulants.
  • Ibuprofen increases the risk of methotrexate toxicity and lithium toxicity.

Paracetamol:

  • Paracetamol increases the risk of liver damage in chronic alcohlolics.

 Precautions

The drug should be used with special precaution in bronchial asthma,renal orhepatic disorders, bleeding disorders, Patients on anticoagulants, pregnancy and lactation.

Taprol

Generic Composition: Pantoprazole sodium

General Introduction

Taprol contains active ingredient Pantoprazole, proton pump inhibitor compounds. More acid stable and less chances of drug interaction.

Therapeutic category

  • Proton Pump Inhibitors

Dosage forms available

  • TAPROL 40 mg tablets

Mechanism of action

Pantoprazole binds to the sulfhydryl group of H+, K+-ATPase, which is an enzyme implicated in accelerating the final step in the acid secretion pathway. The enzyme is inactivated, inhibiting gastric acid secretion.7 The inhibition of gastric acid secretion is stronger with proton pump inhibitors such as pantoprazole and lasts longer than with the H (2) antagonists. 

Pharmacokinetics

After oral administration, Pantoprazole is well absorbed. It undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%. It has 98% protein binding. It is metabolized in liver and 71% is excreted via urine and 18% is excreted via biliary route. Its half-life is 1 hour.

Uses

  • GERD
  • Esophagitis
  • Eradication of H.pylori in combination with antibiotics
  • Zollinger-Ellison Syndrome
  • Peptic ulcer
  • Heartburn
  • Stress ulcer

Dose

40 mg once daily on empty stomach for up to 8 weeks for GERD, esophagitis and 40 mg twice daily for Zollinger-Ellison syndrome.

Side effects

Fever, pain, fatigue, malaise, abdominal swelling, palpitation, elevated blood pressure, peripheral edema, pancreatitis (some fatal), anorexia, irritable colon, flatulence, fecal discoloration, esophageal candidiasis, mucosal atrophy of the tongue, dry mouth, interstitial nephritis (some with positive rechallenge), urinary tract infection, hypochlorhydria.

Contraindication

Pantoprazole is contraindicated in patients with known hypersensitivity to it and the patients undergoing antiretroviral drug therapy

Precautions

  • Renally and hepatic impaired patients.
  • Pregnant women

Pregnancy category: B

Drug interaction

Risk of drug interaction is minimal.

  • Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with pantoprazole may increase toxicity.
  • Pantoprazole and Warfarin when taken concomitantly, increases in INR and prothrombin time occurs that may lead to abnormal bleeding and even death.
  • Concomitant use of pantoprazole sodium with methotrexate (primarily at high dose) may elevate and prolong serum concentrations of methotrexate and/or its metabolite

Rabizole

Generic composition: Rabiprazole sodium

General Introduction 

Rabezole is rabeprazole, proton pump inhibitor belonging to benzimidazole group same as pantoprazole. It causes fastest acid inhibition.

Therapeutic category

  • Proton pump inhibitors

Dosage forms available

  • RABEZOLE 20mg Tablets

Mechanism of action

Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. 

Pharmacokinetics

Biovaailability is approximately 52%, plasma protein binding is 96.3%, undergoes hepatic metabolism, approximately 90% of the drug was eliminated in the urine, half-life is 1-2 hours

Uses

  • GERD
  • Esophagitis
  • Eradication of H.pylori in combination with antibiotics
  • Zollinger-Ellison Syndrome
  • Peptic ulcer
  • Heartburn
  • Stress ulcer

Dose

  • 20mg once daily before meal for up to 4 to 8 weeks 

Side effects

Bone fracture, hypomagnesimia, cynacobalamin deficiency, erythematosus, 

Contraindication

Patients with known hypersensitivity to rabeprazole

Precautions

Presence of gastric malignancy, acute interstinal nephritis,  erythmatosus, 

Drug Interactions 

With antiretroviral drugs, antirheumatic drug methotrexate, digoxin: increase its toxicity, anticoagulants.

CODIPHEN

Generic composition

  • Acetaminophen 500mg and Codeine 10mg

Therapeutic category

  • Non-steroidal Anti-inflammatory drugs

Dosage forms available

  • CODIPHEN Tablet 

Mechanism of action

  • Codeine binds to mu-opioid receptors, which are involved in the transmission of pain throughout the body and central nervous system; shows analgesic properties
  • Acetaminophen’s exact mechanism of action has not been fully established despite this, it is often categorized alongside NSAIDs (non steroidal anti-inflammatory drugs) due to its ability to inhibit the cyclooxygenase (COX) pathways which exert central actions that ultimately lead to the alleviation of pain symptoms.

Pharmacokinetics

  • Rapidly absorbed from GI tract and distributed. Codeine is not bound to plasma proteins and doesn’t accumulate in body tissues. Metabolized in liver and elimination is via urine.

Uses

  • Headache
  • Muscle ache
  • Back ache
  • Fever
  • Cough
  • Arthritis
  • Toothache

Dose

  • 1-2 tablet every 6 hours; when necessary maximum up to 8 tablets in 24 hours

Side effects

Drowsiness, sedation, nausea, stomach pain, shortness of breath.

Contraindications

  • Hypersensitivity to codeine, acetaminophen and similar compounds.

Precautions

Must be used with caution in patients with increased intracranial pressure, acute abdominal conditions, the elderly, the debilitated, impaired hepatic or renal function, hypothyroidism, Addison’s disease, prostatic hypertrophy and urethral stricture.

Drug Interactions

  • Use with other opoids
  • Anticholinergic drugswhen used concurrently with opioid analgesics including codeine sulfate, may result in increased risk of urinary retention and/or severe constipation

Pregnancy category: A

Sovidone Gargle

Generic composition: Povidone Iodine

General Introduction

Povidone-iodine is a stable chemical complex of polyvinylpyrrolidone (povidone, PVP) and elemental iodine.

Therapeutic category

  • Microbicidal

Dosage forms available

  • SOVIDONE Gargle 1% in 50ml and 100ml

Pharmacodynamics

Povidone iodine is a kind of iodine disinfectant which directly causes in vivo protein denaturation, precipitation of bacteria, and further resulting in the death of pathogenic microorganisms. Therefore, it is effective in disinfection and sterilization.

It can kill viruses, bacteria, spores, fungi, and protozoa with low toxicity to human. Povidone-iodine aqueous solution has strong pharmacological activity against Staphylococcus aureus, Neisseria gonorrhoeae, Pseudomonas aeruginosa, syphilis, hepatitis B virus, HIV, and Trichomonas vaginalis.

Mechanism of action

Povidone-iodine is called iodophore which means povidone acts as a carrier of iodine. Iodine is considered as the active moiety that mediates microbicidal actions. When released from the complex, free iodine penetrates the cell wall of microorganisms quickly, and the lethal effects are believed to result from disruption of protein and nucleic acid structure and synthesis. While the full mechanism of action is not fully elucidated, iodine is thought to inhibit vital bacterial cellular mechanisms and structures, and oxidizes nucleotides fatty or amino acids in bacterial cell membranes. Additionally, free iodine disrupts the function of the cytosolic enzymes involved in the respiratory chain, causing them to become denatured and deactivated.

 Uses

Treatment of acute infections of the lining of the mouth and throat, for example, inflammation of the gums (gingivitis) and mouth ulcers. For cleansing the mouth (oral hygiene) before, during and after dental and mouth surgery.

How to use

  • Dilute with an equal amount of warm water if taste is an issue. Swish part of the solution briefly in the mouth and spit it out. Tilt your head backwards and garglefor a total of 30 seconds via swirling the liquid at the throat.

Contraindications

  • Allergic to povidone-iodine or any of the other ingredients of this medicine.

Sovidone Solution

Generic composition: Povidone Iodine

General Introduction

Povidone-iodine is a stable chemical complex of polyvinylpyrrolidone (povidone, PVP) and elemental iodine.

Therapeutic category

  • Microbicidal

Dosage forms available

  • SOVIDONE Solution 5% and 10%

Pharmacodynamics

Povidone iodine is a kind of iodine disinfectant which directly causes in vivo protein denaturation, precipitation of bacteria, and further resulting in the death of pathogenic microorganisms. Therefore, it is effective in disinfection and sterilization.

It can kill viruses, bacteria, spores, fungi, and protozoa with low toxicity to human. Povidone-iodine aqueous solution has strong pharmacological activity against Staphylococcus aureus, Neisseria gonorrhoeae, Pseudomonas aeruginosa, syphilis, hepatitis B virus, HIV, and Trichomonas vaginalis.

Mechanism of action

Povidone-iodine is called iodophore which means povidone acts as a carrier of iodine. Iodine is considered as the active moiety that mediates microbicidal actions. When released from the complex, free iodine penetrates the cell wall of microorganisms quickly, and the lethal effects are believed to result from disruption of protein and nucleic acid structure and synthesis. While the full mechanism of action is not fully elucidated, iodine is thought to inhibit vital bacterial cellular mechanisms and structures, and oxidizes nucleotides fatty or amino acids in bacterial cell membranes. Additionally, free iodine disrupts the function of the cytosolic enzymes involved in the respiratory chain, causing them to become denatured and deactivated.

 Uses

  • Used as an antiseptic against the wound, injuries, bacterial infections

Dosage application

Apply the solution to the affected area, wound may be covered by a sterile bandage but let the solution dry first.

Precautions

  • For external use only.

Contraindications

  • Allergic to povidone-iodine or any of the other ingredients of this medicine.

Sovidone Ointment

Generic composition: Povidone Iodine

General Introduction

Povidone-iodine is a stable chemical complex of polyvinylpyrrolidone (povidone, PVP) and elemental iodine.

Therapeutic category

  • Microbicidal

Dosage forms available

  • SOVIDONE Ointment 5%

Pharmacodynamics

Povidone iodine is a kind of iodine disinfectant which directly causes in vivo protein denaturation, precipitation of bacteria, and further resulting in the death of pathogenic microorganisms. Therefore, it is effective in disinfection and sterilization.

It can kill viruses, bacteria, spores, fungi, and protozoa with low toxicity to human. Povidone-iodine aqueous solution has strong pharmacological activity against Staphylococcus aureus, Neisseria gonorrhoeae, Pseudomonas aeruginosa, syphilis, hepatitis B virus, HIV, and Trichomonas vaginalis.

Mechanism of action

Povidone-iodine is called iodophore which means povidone acts as a carrier of iodine. Iodine is considered as the active moiety that mediates microbicidal actions. When released from the complex, free iodine penetrates the cell wall of microorganisms quickly, and the lethal effects are believed to result from disruption of protein and nucleic acid structure and synthesis. While the full mechanism of action is not fully elucidated, iodine is thought to inhibit vital bacterial cellular mechanisms and structures, and oxidizes nucleotides fatty or amino acids in bacterial cell membranes. Additionally, free iodine disrupts the function of the cytosolic enzymes involved in the respiratory chain, causing them to become denatured and deactivated.

Uses

  • Used as an antiseptic against the wound, injuries, bacterial infections

Dosage application

  • Apply topically to affected area 1-3 times daily.

Precautions

Povidone-iodine is for external use only. Do not apply over large areas of the body.
Do not ingest topical solution or ointments or gels or apply to eyes.

Contraindications

  • Allergic to povidone-iodine or any of the other ingredients of this medicine.

Chlordine

Generic composition: Chlorhexidine Gluconate

General Introduction

Chlordine mouth wash is Chlorhexidine Gluconate oral solution. Chlorhexidine gluconate product is a near neutral solution (pH range 5-7) and is a salt of Chlorhexidine and gluconic acid. Chlorhexidine has activity against gram-positive and gram-negative organisms, facultative anaerobes, aerobes, and yeast. It is both bacteriostatic and bactericidal, depending on its concentration.

Therapeutic category

  • Microbicidal

 Dosage forms available 

  • CHLORDINE 0.2% oral mouth rinse

Mode of action

  • The bactericidal effect of chlorhexidine is a result of the binding of this cationic molecule to negatively charged bacterial cell walls. At low concentrations, this causes an alteration of bacterial cell osmotic equilibrium and leakage of potassium and phosphorous resulting in a bacteriostatic effect. At high concentrations of chlorhexidine, the cytoplasmic contents of the bacterial cell precipitate and result in cell death.

Pharmacokinetics

  • Pharmacokinetic studies with Chlorhexidine gluconate oral rinse indicate approximately 30% of the active ingredient, Chlorhexidine gluconate, is retained in the oral cavity following rinsing. This retained drug is slowly released into the oral fluids. Studies demonstrate Chlorhexidine gluconate is poorly absorbed from the gastrointestinal tract. The mean plasma level of Chlorhexidine gluconate reached a peak in 30 minutes and detectable levels of Chlorhexidine gluconate were not present in the plasma 12 hours of administration. Excretion of Chlorhexidine gluconate occurred primarily through the feces. 

Uses

  • This medication is used along with regular tooth brushing/flossing to treat gingivitis, a gum disease that causes red, swollen, and easily bleeding gums.
  • Chlorhexidine has also been used in those with weakened immune systems to decrease the formation of mouth sores (mucositis), and used to help prevent pneumonia in hospitalized patients breathing through a ventilator (off-label).

Dosage

  • About 5-15ml (undiluted) orally rinse, generally after brushing, don’t swallow

Side effects

Tooth/tongue staining, increased tartar, mouth/throat irritation, dry mouth, and change in taste of food/drinks may occur.

Contraindications

  • Hypersensitivity to Chlorhexidine gluconate or other formula ingredients

Advantages

  • Chlorhexidine Mouthwash has a broad spectrum of activity and destroys both bacteria and fungi
  • Chlorhexidine Mouthwash offers both anti-plaque and anti-inflammatory properties and acts at a pH level close to neutrality 
  • Chlorhexidine Mouthwash coats all areas of the mouth including tooth surfaces, gums, cheeks and other mouth tissue to ensure a long-lasting anti-plaque and antiseptic effect
  • Chlorhexidine Mouthwash has been shown to work for up to 8 hours

Simfol

SIMFOL

Generic composition: Folic acid

General Introduction

Simfol contains Folic Acid, a complex organic compound present in liver, yeast and other substances, and which may be prepared synthetically. It is given as a supplement to prevent folic acid deficiency in pregnant women, alcoholics, patients with liver disease, and in certain skin diseases.

Therapeutic category

  • Haematinics

Dosage forms available

  • SIMFOL 5mg Tablets

Mechanism of action

Folic acid, as it is biochemically inactive, is converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase (DHFR). These folic acid congeners are transported across cells by receptor-mediated endocytosis where they are needed to maintain normal erythropoiesis, synthesize purine and thymidylate nucleic acids, interconvert amino acids, methylate tRNA, and generate and use formate. Using vitamin B12 as a cofactor, folic acid can normalize high homocysteine levels by remethylation of homocysteine to methionine via methionine synthetase.

Pharmacokinetics

Folic acid is well absorbed, pregnant women may absorb as much as 300-400microgram of folic acid. Normally, 5-20mg of folates is stored in the liver and other tissues. Folates are excreted in the urine and stool. Folic acid deficiency and megaloblastic anemia can develop within 1-6 months after the intake of folic acid stops, depending on the patient’s nutritional status and rate of folate utilization.

Uses

  • Megaloblastic anemia due to a deficiency of folic acid
  • Megaloblastic anemia of infancy
  • Nutritional macrocytic anemia
  • Anemia of pregnancy
  • Prophylaxis in people having kidney dialysis
  • Prevention of anemia in haemolytic conditions, neural tube birth defects.

Dose

  • 1 tablet a day.

Side effects

Allergic sensitization has been reported following both oral and parenteral administration of folic acid.

Warnings

Folic acid alone is improper therapy in the treatment of pernicious anemia and other megaloblastic anaemia where Vitamin B12 is deficient.

 

Safolin-PM

Generic compositions

  1. Iron III Hydroxide Polymaltose complex equivalent to elemental Iron……………………100mg
  2. Folic Acid IP …………………………………………………………………………………………………………….1mg   

General Introduction

 Iron hydroxide poly maltose complex is water soluble oxides of iron. It is used in treatment of iron deficiency anaemia. The iron polymaltose complex has been formulated in such a way that the elemental form is in a nonionic state. This ensures that there is no gastric irritation with iron polymaltose complex. In addition, the high elemental iron content of iron polymaltose complex eliminates the need for frequent dosing and therefore improves compliance.

Folic acid is needed for the production of Red blood cells.

Therapeutic category

  • Haematinics

Dosage forms available

  • SAFOLIN Chewable Tablets

Indications

  • Iron deficiency anaemia
  • Pregnancy and Lactation

Dose

  • Adult: 1-2 tablets to be taken daily or as recommended by the doctor.
  • Children: 1 tablet to be taken daily as recommended by the doctor.

Safolin-C

SAFOLIN -C

Generic compositions

Ferrous Ascorbate equivalent to elemental iron………………………………………………….100mg

Folic Acid IP……………………………………………………………………………………………………1mg

Zinc Sulphate Monohydrate equivalent to elemental Zinc BP………………………………22.5mg

General Introduction

Iron is needed for production of hemoglobin.

Folic acid is needed for the production of Red blood cells.

Ascorbic helps to improve the iron absorption and utilization.

Zinc helps to stimulate the formation of RBC.

Safolin-C prevents spina bifida and other neural tube defects.

Therapeutic category

  • Haematinics

Dosage forms available

  • SAFOLIN-C tablets

Indications

  • Pregnancy – meeting greater demand.
  • Megaloblastic Anaemia
  • Compensation of blood loss occurring due to menstruation, blood donation and use of anti-inflammatory drugs that cause blinding from the gastric mucosa.

Dose

  • 1 tablet to be taken daily or as directed by the physician.

Safolin

SAFOLIN

Generic compositions

Ferrous Fumarate BP………………………………………..300mg

Folic Acid BP…………………………………………..………….1.5mg

Cyanocobalamin BP …………………………………………….15mcg

Pyridoxine HCL BP …………………………………….………….2mg

Zinc Sulphate BP………………………………………….……..15mg

Ascorbic Acid BP…………………………………………………75mg

Docusate Sodium BP …………………………………………50mg

Therapeutic category

  • Haematinics

Dosage forms available

  • SAFOLIN Capsules

General Description

Iron: It helps in formation of hemoglobin, developments of RBC, oxygen carriage. The iron demand is increased in following physiological conditions:

  • During growth spurts of infancy and adolescence
  • During menstrual period
  • During pregnancy
  • During lactation

 

Maternal iron deficiency and iron deficiency anemia may adversely affect the iron status of the fetus and infant, which may in turn lead to deficits in mental and psychomotor development.Infants of iron deficient mothers are at greater risk of developing iron deficiency later in infancy.

Pyridoxine is important for hemoglobin synthesis.

Docusate sodium prevents constipation.

Folic acid helps in RBC production.

Ascorbic acid improves iron utilization.

Cyanocobalamin helps to maintain metabolism and is necessary for DNA synthesis.

Zinc helps to stimulate the formation of RBC.

Dose

  • 1 capsule once a day after a meal or twice a day depending upon condition or as directed by the physician.

 

Meryl Expectorant

Generic composition:  Guaifenesin 100mg/5ml

General Introduction

Guaifenesin is categorized as an expectorant that acts by enhancing the output of phlegm (sputum) and bronchial secretions via decreasing the adhesiveness and surface tension of such material. Guaifenesin is extracted from the bark of Guaiac tree.

Therapeutic category

  • Cough Expectorant

Dosage forms available

  • MERYL Expectorant oral solutions

Mechanism of action

Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. It has been said to aid in the flow of respiratory tract secretions, allowing ciliary movement to carry the loosened secretions upward toward the pharynx.

Pharmacokinetics

  • Guaifenesin is well absorbed from gastrointestinal tract after oral administration.
  • It is metabolized hepatically and largely excreted via urine. Half life of Guaifenesin is approximately 1 hour.

Indications

Cough and chest congestion associated with:

  • Common cold B
  • Bronchitis

Dosage

  • 2 years to 6 years: 2.5ml-5ml four hourly 
  • 6 years to 12 years: 5ml-10ml four hourly 
  • 12 years and older: 5ml-20ml four hourly  

Side effects

  • Dizziness
  • Drowsiness
  • Headache
  • Nausea and vomiting

Contraindications

Hypersensitivity to Guaifenesin or its excipients.

Precautions

  • Lactation 
  • Pregnancy

Cartimin

CARTIMIN

Generic composition: Glucosamine base

General Introduction

Glucosamine is a nutritional supplement for cartilage. Glucosamine is an intermediate substrate in the synthesis of the ground substance (non-collagen portion) of cartilage. It is found in almost all human tissues but is highest in concentration in the liver, kidney, and cartilage.

Therapeutic category

  • Dietary supplement

Dosage forms available

  • CARTIMIN 500mg Tablets

Mechanism of action

Glucosamine is a precursor of glycosylated proteins and lipids. Since glucosamine is a precursor for glycosaminoglycans, and glycosaminoglycans are a major component of joint cartilage, supplemental glucosamine may help to rebuild cartilage and treat arthritis.

Pharmacokinetics

About 90% of glucosamine administered orally gets absorbed from the small intestine. It undergoes significant first pass metabolism.

Uses

  • Treatment and prevention of Osteoarthritis, Rebuild Cartilage, Rheumatic Disorder

Dose

  • A typical dose of glucosamine is 1500 mg per day. It should be taken with full glass water at meal time

Side effects

  • Heartburn, epigastric distress and diarrhea.

 

 

Precautions

  • Dose reduction in renal and hepatic impairment.
  • Diabetic patients
  • Children, pregnancy and lactation.

 

 

Metazyme

Generic composition: Fungal Diastase (1:1200) 50mg and Pepsin (1:3000) 10mg / 5ml

General Introduction

Diastase is the natural pro-digestive enzyme, which catalyses the breakdown of starch into maltose and used in disturbances of GI functions and prevention of malabsorption of food. Pepsin is an enzyme in the stomach that begins the digestion of proteins by splitting them into smaller pieces. Pepsin is secreted in an inactive form, pepsinogen, which is activated by stomach acid. 

Therapeutic category

  • Digestives  

Dosage forms available

  • METAZYME 100ml and 200ml 

Uses

  • Indigestion: as a supplement, or as replacement therapy (e.g., in chronic pancreatitis, cystic fibrosis, cancer of the pancreas, after surgery on the pancreas or gut), dyspepsia, Overeating 

Dose

Adults: 5 ml to be taken immediately after meal.

Children: Half the adult dose.

Contraindications

Metazyme should not be used in case of hypersensitivity to any of its ingredients diastase or pepsin. 

Cinolone-M

Generic compositions: – Triamcinolone Acetonide 0.1% w/w and Miconazole Nitrate 2% w/w 

General Introduction

The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. The steroids in this class include Triamcinolone Acetonide. 

Miconazole is a broad-spectrum azole antifungal with some activity against Gram-positive bacteria as well. It is widely used to treat mucosal yeast infections, including both oral and vaginal infections.

Therapeutic category

  • Corticosteroids 

Dosage forms available

  • CESONE-M Cream 

Mode of action

Corticosteroids like triamcinolone inhibit phospholipase A2 on cell membranes, preventing the breakdown of lysosomal membranes of leukocytes, which in turn prevent the formation of arachidonic acid, which decrease expression of cyclooxygenase and lipoxygenase, inhibiting synthesis of prostaglandins and leukotrienes. 

Miconazole is thought to act through three main mechanisms. The primary mechanism of action is through inhibition of the CYP450 14α-lanosterol demethylase enzyme, which results in altered ergosterol production and impaired cell membrane composition and permeability, which in turn leads to cation, phosphate, and low molecular weight protein leakage.

Pharmacokinetics

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses 

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

Indications

Triamcinolone acetonide cream is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Miconazole is used to treat skin infections such as athlete’s foot, jock itch, ringworm, and other fungal skin infections (candidiasis).

Dosage and administration

  • Apply to affected area two or three times daily. Rub in gently or apply as directed by dermatologists.

Side effects

Burning, itching, irritation, or dryness may occur when this medication is first applied to the skin. This should disappear in a few days as your body adjusts to the medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Cinolone-G

Generic compositions: Triamcinolone Acetonide 0.1% w/w and Gentamycin Sulphate 1% w/w 

General Introduction

The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. The steroids in this class include Triamcinolone Acetonide. Each gram of Triamcinolone Acetonide Cream USP, 0.1% contains 1 mg Triamcinolone Acetonide in a cream base. 

Therapeutic category

  • Corticosteroids 

Dosage forms available

  • CESONE-G Cream 

Mode of action

Corticosteroids like triamcinolone inhibit phospholipase A2 on cell membranes, preventing the breakdown of lysosomal membranes of leukocytes, which in turn prevent the formation of arachidonic acid, which decrease expression of cyclooxygenase and lipoxygenase, inhibiting synthesis of prostaglandins and leukotrienes.

Gentamicin kills bacteria by inhibiting the synthesis of bacterial proteins. Gentamicin irreversibly binds to the 30S ribosomal subunits. This binding interferes with the formation of messenger RNA and the subsequent formation of nonfunctional proteins and the eventual death of susceptible bacteria.

Pharmacokinetics

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses 

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

Indications

Triamcinolone acetonide cream is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. 

Gentamycin is used for minor skin infections (such as impetigo, folliculitis) or minor infections related to some skin conditions (such as eczema, psoriasis, minor burns/cuts/wounds).

Dosage and administration

  • Apply to affected area two or three times daily. Rub in gently or as directed by the doctor.

Side effects

Burning, itching, irritation, or dryness may occur when this medication is first applied to the skin. This should disappear in a few days as your body adjusts to the medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Contraindications

  • Hypersensitivity to traimcinolone or gentamycin.

Cinolone

Generic compositions: Triamcinolone Acetonide 0.1% w/w 

General Introduction

The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. The steroids in this class include Triamcinolone Acetonide. Each gram of Triamcinolone Acetonide Cream USP, 0.1% contains 1 mg Triamcinolone Acetonide in a cream base. 

Therapeutic category

  • Corticosteroids 

Dosage forms available

  • CESONE Cream 

Mode of action

Topical corticosteroids share anti-inflammatory, antipruritic and vasoconstrictive actions.

The mechanism of anti-inflammatory activity of topical corticosteroids is unclear. Corticosteroids like triamcinolone inhibit phospholipase A2 on cell membranes, preventing the breakdown of lysosomal membranes of leukocytes, which in turn prevent the formation of arachidonic acid, which decrease expression of cyclooxygenase and lipoxygenase, inhibiting synthesis of prostaglandins and leukotrienes. 

Pharmacokinetics

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses 

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

Indications

Triamcinolone acetonide cream is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Dosage and administration

  • Apply to affected area two or three times daily. Rub in gently or as directed by your doctor.

Side effects

Burning, itching, irritation, or dryness may occur when this medication is first applied to the skin. This should disappear in a few days as your body adjusts to the medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Precautions

  • Pregnancy Category C
  • It is for external use only. Avoid contact with the eyes.

Cesone

CESONE

Generic composition: Fluticasone Propionate

General Introduction

 Fluticasone is a synthetic fluorinated corticosteroid, for topical dermatologic use. The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents.

Therapeutic category

  • Corticosteroids

Dosage forms available

  • CESONE 0.05% w/w cream

Mechanism of action

The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

Fluticasone propionate is lipophilic and has a strong affinity for the glucocorticoid receptor. It has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors.

Uses

  • Atopic dermatitis
  • Contact dermatitis
  • Poison Ivy
  • Seborrhoeic dermatitis
  • Psoriasis

Dose

  • Apply the cream to the affected area once or twice daily and rub gently or as directed by the dermatologists.

Precautions

For external use only.

Side effects

Burning, pruritus, stinging, skin irritation, dryness,

Contraindications

Patients with a history of hypersensitivity to any of the components of preparations.

 

Simcal

Generic composition: Calcium 500mg and vitamin D3 250 IU 

General Introduction

Simcal; a nutritional supplement contains Calcium and Vit D3. Calcium and Vitamin D3 tablet are much-prescribed mineral and vitamin supplements for various conditions. Simcal contains Oyster Shell 1.250 gm Calcium containing 500 mg of elemental Calcium from Calcium tribasic phosphate and Cholecalciferol (Vit D 3) 250 IU. 

Therapeutic Category

  • Calcium supplements

Dosage forms available

  • SIMCAL Tablets

Pharmacokinetics

Calcium tribasic phosphate: 

Calcium is primarily absorbed in the proximal part of the small intestine. The rate of absorption through the gastro-intestinal way is about 30% of the introduced amount. More than 98% of the filtered Ca2+is reabsorbed from tubules to the circulation.

Vit D3 (Cholecalciferol) 

Vit D3 is absorbed from the small intestine and is transported by proteinic components in blood to the liver and the kidney. Bile is essential for adequate absorption of vitamin D and thus hepatic or biliary dysfunction seriously impairs Vit D absorption. The primary route of excretion of vitamin D is the bile; only a small percentage of an administered dose is found in urine. 

Uses

  • Calcium and Vitamin D3 deficiency and increased needs
  • Calcium supplementation in pregnancy and lactation
  • Osteoporosis, fractures, menopausal women

Dose

  • 1 tablet to be taken two times a day, depending on individual requirement of patients

Side effects

  • Constipation, Flatulence, Nausea, epigastric pain, diarrhea, calciuria, calcemia. 

Contraindications

  • Hypersensitivity to either one of the components , Hypercalcaemia, Hypercalciuria

Drug interactions

  • Digitalis: the oral calcium administration associated with vitamin D increases the toxicity of digitalis (risk of disorders of the rate/rhythm). 
  • Thiazide diuretic: a monitoring of the calcium is recommended (reduction in the urinary elimination of calcium). 
  • Tetracycline: it is recommended to administer at least three hours before/after the administration (possible reduction in the absorption of the tetracycline). 
  • Phenytoin, barbiturates: possible reduction in the effect of the vitamin D3 by inhibition of its metabolism. 
  • Glucocorticoids: possible reduction in the effect of the vitamin D3. 

Precautions

  • Concomitant administration with other calcium containing preparations 
  • Sarcoidosis: The product must be prescribed with precaution among patients with risk of sarcoidosis because of a possible increase in the metabolism of the vitamin D3 in its active form. 
  • Renal insufficiency 
  • Pregnancy: This product can be used during the pregnancy and breast-feeding. However the amount per day should not exceed 1500 calcium mg and 600 i.u. of vitamin D3. 
  • Breast Feeding: Vit D3 and its metabolites pass into the mother’s milk. 
  • The overdose results in a Hypocalciuria and a hypocalcaemia whose symptoms are as follows: nausea, vomiting, polydipsia, polyuria, and constipation. 
  • An overdose in vitamin D3 vitamin can cause vascular calcifications and tissue calcification because of the hypercalcaemia.

 

Meryl Linctus

Generic composition: Dextromethorphan HBr 10mg and Pheniramine Maleate 5mg/5ml

General Introduction

Meryl Linctus contains the active ingredients, Dextromethorphan HBr and Pheniramine Maleate: an effective antitussive agent and anti- allergic agent respectively. 

Therapeutic category

  • Anti-tussive

Dosage forms available

  • MERYL Linctus 50ml and 100ml bottles

Pharmacokinetics

Dextromethorphan: Following oral administration, dextromethorphan is rapidly absorbed from gastrointestinal tract. It crosses the blood-brain barrier. The duration of action after oral administration is approximately 3-8 hrs.

Pheniramine Maleate: Pheniramine maleate is absorbed relatively slowly from the gastrointestinal tract, with peak plasma concentrations occurring about 2.5 to 6 hours after oral administration. Bioavailability is low, values of 25 to 50% having been reported. About 70% of pheniramine in the circulation is bound to plasma proteins. Pheniramine is widely distributed in the body and enters the CNS.

Uses

  • Temporary relief of dry coughs, upper respiratory relief of coughs and upper respiratory symptoms, including nasal congestion, associated with allergy or the common cold

Dose

  • 10 ml to be taken every 6 hourly for adult 
  • 5ml to be taken every 6 hourly for children

Adverse Reactions

Sedation, dryness of mouth, nose and throat, thickening of bronchial secretions, and dizziness. 

Contraindications

  • Hypersensitivity to any of the ingredients. 
  • Not recommended in the treatment of bronchial asthma. 
  • Patients with severe hypertension, severe coronary artery disease, narrow-angle glaucoma, urinary retention, peptic ulcer, and in patients on MAO inhibitor therapy (or for 14 days after stopping MAOI therapy)

Drug Interactions

  • Antihistamines have additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, antianxiety agents, etc.) 
  • The use of phenylephrine with other sympathomimetic amines and MAO inhibitors (or for 14 days after stopping MAOI therapy) may produce an additive elevation of blood pressure. MAO inhibitors (or for 14 days after stopping MAOI therapy) may prolong the anticholinergic effects of antihistamine

Ornazole

Generic composition: Ornidazole 

General Introduction

Ornazole is Ornidazole is a nitroimidazole derivative active against protozoa and anaerobic bacteria. It is effective against anaerobic enteric protozoa.  

Therapeutic category

  • Anti-protozoal

Dosage forms available

  • Ornidazole 500mg Tablets

Mechanism of action

Ornidazole is a bactericidal antibiotic which works by inhibition of protein synthesis by interaction with DNA. The nitro group in Ornidazole is responsible for its antibacterial property. Nitro group is converted to more active amine group and causes destruction of helical DNA structure. This is responsible for bacterial/protozoal cell death due to ornidazole.

Pharmacokinetics

Ornidazole tablets have mean absorption of about 90%. Peak plasma concentrations are reached within three hours. The half-life is about thirteen hours. 85% of a single dose is eliminated within the first five days, most of this being metabolized by liver and excreted in urine (63%) and feces (22%).

Uses

  • Treatment of parasitic infections including amebiasis, trichomoniasis
  • Bacterial vaginosis
  • Giardiasis
  • Anaerobic infections
  • Prophylactic use in surgery

Dose

  • Amoebiasis:   500mg twice daily for 5-10 days(Adult) and 25mg/Kg single daily dose for 5-10 days(pediatric)
  • Amoebic dysentery:  1500 mg single daily dose for 3 days(>60 kg: 1000mg twice daily for 3 days) (Adult) and 40 mg/kg daily(Paediatric)
  • Giardiasis: 1000-1500 mg single daily dose for 1-2 days (adult) and 30-40 mg/kg daily(pediatric)
  • Trichomoniasis: 1500 mg single daily dose or 500 mg twice daily for 5 days and 25 mg/kg single dose(Pediatric)

Dose adjustment is needed in renal and hepatic impairment- supplemental dose may be needed. 

Drug interactions

 Coumarin-type oral anticoagulants (potentiates), Vercuronium bromide (prolongs muscle relaxant action)

Side effects

Common side effects of ornidazole are headaches, nausea, vomiting, dizziness, tremor, rigidity, poor coordination, seizures, tiredness, vertigo, peripheral neuropathy and skin reactions.

Precautions

  • Alcohol: disulfiram type reaction may occur.
  • Pregnancy and lactation
  • Renal and hepatic impairment
  • CNS diseases e.g. epilepsy or multiple sclerosis 

Contraindications

Hypersensitivity with ornidazole or other nitro imidazole derivatives

Mogyl Forte Tablet

Generic composition: Tinidazole 300mg and Diloxanide Fuorate 500mg

General Introduction

Mogyl forte contains Tinidazole and Diloxanide Furoate as an active ingredients and is an antiprotozoal and antiamoebic respectively.

Therapeutic category

  • Anti-protozoal

Dosage forms available 

  • MOGYL Forte Tablets

Mechanism of action

Tinidazole: is anaerobicidal, amoebicidal. It inhibits bacterial nucleic acid formation.

Diloxanide furoate: Luminal amoebicide. It destroys the trophozoites of E. histolytica that eventually form into cysts. The cysts are then excreted by persons infected with asymptomatic amoebiasis.  

Pharmacokinetics

Tinidazole: Rapidly and completely absorbed, 12% plasma protein bound, undergoes hepatic metabolism by oxidation, hydroxylation and conjugation, crosses placental barrier and secreted in milk, excreted by liver and kidneys, plasma half life is 12 to 14 hours

Diloxanide furoate: slowly absorbed from GI tract,hydrolyzed to fuoric acid and diloxanide and metabolized by following glucoronidation, eliminated by renal route(90% as glucoronide metabolite) and 10% in feces, half life is 3 hours

Uses

  • Amoebiasis and Giardiasis
  • Prevention and treatment of anaerobic infection 

Dose

  • One tablet thrice daily for five days. Extended treatment for ten days in refractory cases

Side effects

Seizures, headache, dizziness, peripheral neuropathy, unpleasant metallic taste, furred tongue, GI disturbances

Contraindications

  • first trimester pregnancy 
  • Lactation 
  • Hypersensitivity 
  • Active CNS disease, serious neurological disease and seizure
  • Severe hepatic failure

Precautions

  • The drug should be used with special precaution in renal and hepatic impairment. Alcoholic     beverages should be avoided during the course.

Drug Interactions

  • Acute psychoses with disulfiram
  • Additive or synergistic effect with other antimicrobials 
  • Disulfiram like reaction  with alcohol 
  • Enhances action of coumarin anticoagulants
  • Blood levels increased by cimetidine 
  • Effect reduced by phenobarbitone

Corporate Office

  • Ganabahal, Kathmandu
  • Phone: +977-01 5904868

Factory

  • Byasi Bhaktapur
  • Phone: +977-01 6612742 / 6612716

Email Address