Archives: Products

Description.

Apetone

Generic composition: Cyproheptadine HCl

General Introduction

Apetone syrup contains Cyproheptadine HCl, 2 mg per 5 ml, is primarily an antihistaminic.

Therapeutic category

  • Anti-histamines

Dosage forms available

  • APETONE oral solution 100ml and 200ml

Mode of action

It works by blocking the action of histamine to reduce allergy symptoms. However, because of its appetite stimulating side effect, it is used as an appetite stimulant.

Pharmacokinetics

Apetone is mainly metabolized and passed out through urine.

Uses

Symptomatic relief of perennial and seasonal allergic rhinitis; vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; amelioration of allergic reactions to blood or plasma; mild skin manifestations of uncomplicated urticaria and angioedema; cold urticaria; dermatographism; adjunctive anaphylactic therapy.

Off label uses include appetite stimulation, migraines, nightmares, suppression of vascular headaches.

Dose

  • Adults: 2 teaspoonful 3 times daily Usual dosage, two to five teaspoonful/day; not to exceed 0.5 mg/kg/day.
  • 7years to 14 years: 2 teaspoonful 2 to 3 times daily
  • Children of 2-6 years: 1 teaspoonful 2 to 3 times a day. Total daily dose of 0.25mg/kg.

Contraindications

Newborn or premature infants; breast-feeding mothers; angle-closure glaucoma; stenosing peptic ulcer; symptomatic prostatic hypertrophy; bladder neck obstruction; pyloroduodenal obstruction; elderly, debilitated patients; MAOI therapy; hypersensitivity to cyproheptadine and other drugs of similar structure.

Simtrax

Generic composition: Tranexamic acid

General Introduction
Tranexamic acid is an anti-fibrinolytics drug used in case of severe hemorrhage.

Therapeutic category

  • Anti-fibrinolytics

Dosage forms available

  • SIMTRAX 500mg Tablets

Mechanism of action
Tranexamic acid competitively inhibits activation of plasminogen (via binding to the kringle domain), thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins, including the procoagulant factors V and VIII. Tranexamic acid also directly inhibits plasmin activity, but higher doses are required than are needed to reduce plasmin formation

Pharmacokinetics

  • Absorption: Approximately 30 to 50% of the ingested dose is absorbed; bioavailability is not affected by food intake and is approximately 45%, 3% bound to plasma proteins
  • Distribution: 9 to 12 L
  • Metabolism: small fraction of the tranexamic acid is metabolized (less than 5%)
  • Elimination: eliminated by urinary excretion primarily via glomerular filtration with more than 95% of the dose excreted unchanged
  • Half-life: biological half-life is about 3 hours 

Indications

  • Menorrhagia
  • Tooth extraction
  • Traumatic Injury
  • Epistaxis and tonsillectomy
  • Prostatic surgery
  • Cardio-pulmonary bypass surgery

Dose

  • 2 tablets to be taken three times daily, up to 5 days.
  • Not indicated for pediatric and geriatric use.

Side effects

Common side effects include headache, sinus and nasal symptoms, back pain, abdominal pain, musculoskeletal pain, joint pain, muscle cramps, migraine, anemia, fatigue, allergic skin reactions, visual disturbances, dizziness, 

 Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction); cases have been associated with concomitant use of combination hormonal contraceptives, impaired color vision and other 

Contraindication

  • Hypersensitivity to Tranexamic acid.
  • Thromboembolic risk

Pregnancy category: Category B

Precautions

  • Ocular effects
  • Severe allergic reactions
  • Renal impairment
  • Pregnancy and lactation

Drug Interaction

  • Hormonal Contraceptives (may further exacerbate the increased thrombotic risk)
  • Tissue Plasminogen Activators like: Alteplase, reteplase (decrease the efficacy of both)
  • Anti-inhibitor Coagulant Concentrates (increased risk of thrombosis)

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

Rhinex

RHINEX

Generic composition

For tablet

Phenylephrine HCl: 10mg, Pheniramine Maleate: 7.5mg and Paracetamol: 500mg

For syrup

Phenylephrine HCl 5mg and Pheniramine Maleate 15mg per 5ml

General Introduction

Rhinex is widely used as anti-cold tablets. It contains phenylephrine HCl in addition to pheniramine maleate and paracetamol. This combination medication is used to temporarily relieve symptoms caused by the common cold, flu, allergies, or other breathing illnesses (such as sinusitis, bronchitis). Antihistamines help relieve watery eyes, itchy eyes/nose/throat, runny nose, and sneezing. Decongestants help to relieve stuffy nose and ear congestion symptoms.

Therapeutic category

  • Anti-cold and decongestant

Dosage form available

  • RHINEX Tablets
  • RHINEX Syrup

Mode of action

  • It works by decreasing swelling in the nose and ears, thereby lessening discomfort and making it easier to breathe

Uses

  • Symptomatic relief of cold and flu
  • Temporary relief of stuffy nose, sinus and ear symptoms caused by the common cold, flu, allergies, bronchitis.

Dose

  • Adults: 1-2 tablet to be taken 3-4 times a day depending on condition
  • Children: 5-10 ml three or four times a day or as directed by a physician.

Side effects

Drowsiness, dizziness, sleep disorder, stomach pain, dry mouth, headache, palpitations, blood pressure may rise.

Drug Interaction

Taking MAO inhibitors with this medication may cause a serious drug interaction.

The risk of the hepatotoxic action of paracetamol increases during concurrent use of barbiturates, diphenine, carbamazepine, rifampicin, zidovudine, and other hepatic microsomal enzyme inducers.

Antidepressants, antiparkinsonian agents, antipsychotic agents, and phenothiazine derivatives – increase the risk of developing urinary retention, dry mouth, and constipation. Glucocorticosteroids increase the risk of developing elevated intraocular pressure.

Precautions

  • Do not take with alcohol
  • Do Not exceed the recommended dose
  • Use cautiously in patient with hepatic failure, cardiovascular disease
  • Care must be taken when operating an automobile or other machinery, requiring mental alertness and quick psychomotor reactions.

Contraindications

Hypersensitivity to any of the components of Rhinex.

 

Silvin

SILVIN

Generic composition: Silver Sulfadiazine

General Introduction

Silver sulfadiazine; a sulfonamide used topically to reduce microbial colonization and incidence of infections of wounds from severe burns. Silver sulfadiazine has broad antimicrobial activity. It is bactericidal for many gram-negative and gram-positive bacteria as well as being effective against yeast.

Therapeutic category

  • Anti-bacterial (Topical)

Dosage forms available

  • SILVIN 1% cream in 25g and 200g

Mechanism of action

Silver is a biocide, which binds to a broad range of targets. Silver ions bind to nucleophilic amino acids, as well as sulfhydryl, amino, imidazole, phosphate, and carboxyl groups in proteins, causing protein denaturation and enzyme inhibition. Silver binds to surface membranes and proteins, causing proton leaks in the membrane, leading to cell death.

Sulfadiazine is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.

Pharmacokinetics

While little silver is absorbed, the plasma concentration of sulfadiazine may approach therapeutic levels if a large surface area is involved. Up to about 10% of the sulfadiazine may be absorbed

Uses

Silver sulfadiazine cream, USP 1% is a topical antimicrobial drug indicated as an adjunct for the prevention and treatment of wound sepsis in patients with second and third degree burns.

Dosage and administration

  • The cream should be applied once to twice daily to a thickness of approximately one sixteenth of an inch; burn areas should be covered by cream all the time. Whenever necessary, the cream should be reapplied to any areas from which it has been removed by patient activity,

Adverse effects

  • The infrequent adverse reactions include burning, rash and itching.

Contraindication

  • Contraindicated in patients who are hypersensitive to silver sulfadiazine or any of the other ingredients in the preparation.
  • Silver sulfadiazine cream should not be used on pregnant women approaching or at term, on premature infants, or on newborn infants during the first 2 months of life.

Precautions

  • Hepatic and renal insufficiency
  • Pregnancy Category B

 

Mupiderm 5g/10g

Generic composition: Mupiderm

General Introduction

Mupiderm ointment is 2% mupirocin. Mupirocin is an antibacterial agent obtained by fermentation using Pseudomonas fluorescens. 

Therapeutic category

  • Anti-bacterial (Topical)

Dosage forms available

  • MUPIDERM 5g ointment
  • MUPIDERM 10G ointment

Mechanism of action

Mupirocin specifically and reversibly binds to bacterial isoleucyl transfer-RNA (tRNA) synthetase, which is an enzyme that promotes the conversion of isoleucine and tRNA to isoleucyl-tRNA. Inhibition of this enzyme subsequently leads to the inhibition of the bacterial protein and RNA synthesis. Mupirocin is bacteriostatic at lower concentrations but it exerts bactericidal effects with prolonged exposure, killing 90-99% of susceptible bacteria over a 24 hour period.

Pharmacokinetics

Systemic or percutaneous absorption of mupirocin following dermal application is expected to be minimal in adults and children, protein binding of mupirocin is reported to be over 95%, mupirocin undergoes rapid hepatic metabolism to form the principal metabolite monic acid, which has no antibacterial activity, eliminated by renal excretion.

Uses

  • Topical treatment of impetigo due to S. aureus and S. pyogenes.

Dose

  • 3 times as daily in affected ares for 3-5 days.

Adverse effects

  • Burning, stinging or pain, itching, rash, dry skin, tenderness and contact dermatitis.

Precautions

  • If impetigo has not improved in 3 to 5 days, contact your healthcare practitioner.
  • If a severe reaction suggesting sensitivity or chemical irritation should occur with the use, treatment should be discontinued and appropriate alternative therapy for the infection instituted.
  • As with other antibacterial products, prolonged use may result in overgrowth of nonsusceptible organisms, including fungi, 2% is not formulated for use on mucosal surfaces, nasal use.
  • Pregnancy category: B

Contraindications

  • Hypersentitivity to any constituents

Fulgard

Generic composition: Fusidic acid

General Introduction

Fulgard is fusidic acid, antibiotic belonging to fusidane. It is derived from Fusidium coccineum. It has steroid like structure but does not possess steroidal activity. It has bactericidal activity against Staphylococcus, Streptococcus, and Corynebacterium. It inhibits bacterial replication.

Therapeutic category

  • Topical Anti-bacterial

Dosage forms available

  • FULGARD cream 15g

Mechanism of Action

Fusidic acid works by interfering with bacterial protein synthesis, specifically by preventing the translocation of the elongation factor G (EF-G) from the ribosome. It also can inhibit chloramphenicol acetyltransferase enzymes.

Pharmacokinetics

Fusidic acid is highly protein bound and has good penetration to a number of tissues. Topical application has poor penetration through skin. It is excreted mainly in the bile with little excreted in the urine. Half-life in adult is approximately 5-6 hours,

Uses

  • Soft tissue infections
  • Infected dermatitis, folliculitis, furunculosis
  • Angular cheilitis
  • Abscesses and infected traumatic wounds

Dose

  • Uncovered lesions: apply gently three or four times daily.
  • Covered lesions: less frequent applications may be adequate.

Side effects

Cardiac glycosides

Contraindications

It is contraindicated in patients with known hypersensitivity to fusidic acid or to any of the excipients.

Anerbac Gel

Generic composition: Clindamycin Phosphate

General Introduction

Clindamycin is a lincosamide antibiotic used for the treatment of anaerobic, streptococcal, and staphylococcal infections. Clindamycin gel 1% is for dermatological purpose only.  

Therapeutic category

  • Topical Anti-bacterial

Dosage forms available

  • ANERBAC gel 1%

Mechanism of action

Inhibits bacterial Protein synthesis, It binds with 50s ribosome of bacteria to inhibit bacterial protein synthesis.  It inhibits the first step of protein synthesis i.e. initiation of peptide formation. It is a bacteriostatic antibiotic.

Pharmacokinetics

Absorption of topical preparation is very low: a well tolerated preparation.

Uses

  • Anaerobic infections in skin and soft tissue 
  • Infected acne vulgaris
  • Acne lesions
  • Gardenella Vaginitis
  • MRSA infection in skin and soft tissue

Dosage

Apply twice daily to the affected area, or as directed by a physician, after the affected areas are gently washed, rinsed with warm water and patted dry. Duration of use differs with the acne conditions. Generally improvement is seen after about 6-8 weeks. 

Side effects

  • Burning
  • Itching
  • Scaling
  • Pain
  • Dryness
  • Skin Irritation

Precautions

  1. Hypersensitivity to agent(Allergy)
  2. Don’t apply to either broken or eczematous skin
  3. Don’t share the products with others

Contraindications

Allergic conditions

Paramycetin

 Generic composition: Chloramphenicol

General Introduction

Chloramphenicol is a broad spectrum antibiotic isolated from the cultures of Streptomyces venequelae in 1947 but now manufactured synthetically. It is bacteriostatic in nature.

Therapeutic category

  • Anti-bacterial

Dosage forms available

  • PARAMYCETIN 250mg capsules
  • PARAMYCETIN 500mg capsules
  • PARAMYCETIN Suspension 125mg/5ml

Mechanism of action

Chloramphenicol is lipid-soluble, allowing it to diffuse through the bacterial cell membrane. It then reversibly binds to the L16 protein of the 50S subunit of bacterial ribosomes, where transfer of amino acids to growing peptide chains is prevented (perhaps by suppression of peptidyl transferase activity), thus inhibiting peptide bond formation and subsequent inhibition of bacterial protein synthesis.

Pharmacokinetics

Rapidly and completely absorbed from gastrointestinal tract following oral administration (bioavailability 80%), undergoes hepatic metabolism with 90% conjugated to inactive glucoronide, Half-life in adults with normal hepatic and renal function is 1.5 – 3.5 hours.

Uses

  • Highly active against Salmonella typhi so very useful in typhoid fever.

Dose

  • Adult dose: 250mg-500mg 6 hourly/day
  • Child dose: 25-20mg/kg/day

Drug interactions

Prolongs half life of Warfarin, Phenytoin

Side effects

Hematological toxicity, nausea, vomiting, diarrhea, hypersensitivity reactions.

Precautions

Blood related disorders.

Contraindications

Hypersensitivity with Chloramphenicol or its excipients.

Gramix

Generic composition: Cefixime Trihydrate

General description

It is a third generation cephalosporin highly active against Enterobacteriaceae, H. influenza, Strep. pyrogenes, Strep. pneumonia and is resistant to many ß-lactamases.

Therapeutic category

  • Anti-bacterial – 3rd generation cephalosporins

Dosage forms available

  • GRAMIX DT 100mg
  • GRAMIX 200mg
  • GRAMIX Dry Syrup 50mg/5ml
  • GRAMIX HP 100mg/5ml

Mechanism of Action

  • Like all beta-lactam antibiotics, cefixime binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins

Pharmacokinetics

  • Absorption: About 40%-50% absorbed orally whether administered with or without food,
  • Metabolism: undergoes hepatic metabolism, 
  • Elimination:  Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours.
  • Half-life: 3-4 hours (may range up to 9 hours), in severe renal impairment (5 to 20 mL/min creatinine clearance), the half-life increased to an average of 11.5 hours.

Uses

  • Typhoid
  • Surgical Infections
  • Upper and Lower respiratory tract infection
  • Gynecological Infections
  • Uncomplicated Gonorrhoea
  • Otitis Media

Dose

  • Adult: 400 mg daily as a single dose or in divided dose.
  • Pediatric dose: 8 mg/kg/day of the suspension.

Drug Interaction

  • Carbamazepine (carbamazepine level elevates)
  • Warfarin and anti-coagulants (increased prothrombin time)
  • Increased concentrations of Cefixime when taken with Probenecid.

Side effects

  • GI: Stomach upset/pain, diarrhea, nausea, gas, headache, or dizziness may occur.
  • CNS: headache, dizziness. 
  • Hematologic: thrombocytopenia, eosinophilia etc

Contraindications

  • Allergic to cephalosporin group of anti-biotics.
  • Pegnancy category: B

Precautions

  • Special precautions need to be taken in the case of history of allergy to penicillin, pregnancy, lactation and renal failure. 

Advantages

  • High beta lactamases resistance and cure rate, excellent penetration in tissues,sputum and pleural fluid, safe and well tolerated due to minimum inhibitory concentration.

 

Ciflon

Generic composition: Ciprofloxacin HCl

General Introduction

Ciflon contains the active ingredient, Ciprofloxacin HCL Monohydrate, the most potent first generation fluoroquinolones against a broad range of bacteria. 

Therapeutic category

  • Anti-bacterial

Dosage forms available

  • CIFLON 500mg Tablets

Mechanism of Action

Ciprofloxacin is a broad-spectrum antibiotic active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.

Pharmacokinetics

Ciprofloxacin given as an oral tablet is rapidly and well absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability is approximately 70%, plasma protein binding is 20-40%. After oral administration, ciprofloxacin is widely distributed throughout the body. Ciprofloxacin has also been detected in lung, skin, fat, muscle, cartilage, CSF and bone. Approximately 40 to 50% of an orally administered dose is excreted in the urine as unchanged drug.

Uses

  • Urinary tract infections
  • Gonorrhea
  • Bacterial gastroenterititis
  • Typhoid
  • Bone,softtissue,gynaecological and wound infections
  • Respiratory infections
  • Tuberculosis
  • Gram negative septicaemias
  • Meningitis and Conjunctivitis 

Dose

  • 500mg q12h for upto 7 to 14 days 

Contraindications

  • Ciprofloxacin tablets are contraindicated in persons with a history of hypersensitivity to ciprofloxacin, any member of the quinolone class of antimicrobial agents, or any of the product components.
  • Concomitant administration with tizanidine is contraindicated.

Adverse Reactions

  • Gastrointestinal: nausea, vomiting, bad taste and anorexia
  • CNS: dizziness, headache, restlessness, anxiety, insomnia, confusion and tremor.
  • Skin/hypersensitivity: rash, photosensitivity, urticaria and swelling of lips.
  • Tendonitis and tendon rupture: few cases reported.

Drug Interactions

  • Plasma concentration of theophylline,caffeine and warfarin are increased by ciprofloxacin due to inhibition of metabolism. 
  • NSAIDs may enhance the CNS toxicity of ciprofloxacin.
  • Antacids, sucralfate and iron salts concurrently reduce absorption of Ciprofloxacin. 

Precautions

  • Alteration of the dosage regimen is necessary for patients with impairment of renal function. 
  • Moderate to severe photosensitivity/phototoxicity reactions. Discontinue if phototoxicity occurs
  • Convulsions, increased intracranial pressure, and toxic psychosis have been reported in patients receiving quinolones, including ciprofloxacin. Ciprofloxacin may also cause central nervous system (CNS) events including: dizziness, confusion, tremors, hallucinations, depression, and, rarely, suicidal thoughts or acts. These reactions may occur following the first dose. If these reactions occur in patients receiving ciprofloxacin, the drug should be discontinued and appropriate measures instituted. 

Lucid 170ml

Generic composition: Magaldrate 800mg and Simethicone 100mg

Therapeutic category

  • Antacid

Dosage forms available

  • LUCID gel suspension 

Mechanism of action

These are basic substances, which neutralize gastric acid and raise pH of gastric contents. Peptic activity is indirectly reduced if the pH rises above 4. Antacids do not decrease acid production. Taken with meals antacids may act for at the most 2-3hrs.

Magaldrate is a hydrated complex of hydroxy magnesium aluminates which initially reacts with the gastric acid and releases Aluminium Hydroxide and Magnesium Hydroxide.  

Simethicone is a mixture of polydimethylsiloxane and silica gel. It is an anti-flatulent agent. It reduces surface tension and collapses the froth and allows the lower bubbles of froth collapse into the large bubbles and aids in expulsion. By defoaming the gastric juice, it decreases the incidence of GERD.

Uses

  • Heart Burn
  • Gastro esophageal reflux
  • Dyspepsia
  • Gastric and peptic ulcer

Dose

  • Adults: 10-15ml 2-3 times a day with food
  • Children: Half the adult dose

Side effects

Calcium carbonate antacids cause belching and constipation, magnesium salts can cause Diarrhea. By taking calcium and sodium carbonate together or with milk, there is risk of milk-alkali syndrome leading to headache, anorexia, weakness, abdominal discomfort and renal stones.

Contraindications

  • Hypersensitivity to any component of the formulation

Drug interaction

  • Magaldrate may negatively influence drugs like tetracyclines, benzodiazepines, and indomethacin.
  • High doses or prolonged usage may lead to an increment of defecation and a reduction in feces consistence. 
  • In some cases it can alter the functionality of the gastrointestinal tract, occasionally provoking constipation or diarrhea

Precautions

  • Should be used with caution in renal impairment, pregnancy, lactation, elderly and children.
  • Avoid taking any drug 2 hours before or after antacids to prevent interactions

Nebalin

Nebalin

Pregabalin 50mg / 75mg / 150mg Capsules

Generic composition: Pregabalin

General Introduction

Nebalin is pregabalin, synthetic molecule with a favorable pharmacokinetic profile compared with gabapentin. It falls in the therapeutic category of anticonvulsant and non-opoid analgesics. It is used in the treatment for neuropathic pain.

Therapeutic category

  • Anti-neuropathic drugs

Dosage forms available

  • NEBALIN 50mg capsules
  • NEBALIN 75mg capsules
  • NEBALIN 150mg capsules

Mechanism of action

Pregabalin binds to calcium channel, resulting in reduced depolarization-induced calcium influx at nerve terminals with a consequential reduction in the release of excitatory neurotransmitters.

Pharmacokinetics

Pregabalin is rapidly absorbed, peak blood concentrations within 1 hour; average bioavailability exceeds 90%, half-life 5-7 hour. Pregabalin does not undergo hepatic metabolism and is not bound to plasma proteins. It is renally excreted, and 98% of the absorbed dose is excreted unchanged in the urine.

Uses

  • Neuropathic pain (Diabetic neuropathic pain, fibromyalgia and Post herpetic neuralgia)
  • Chronic pain
  • Complex regional pain syndrome
  • Epilepsy: as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder: treatment of Generalized Anxiety Disorder (GAD) in adults

Dose

150 mg per day in two or three divided dose, increased to 300mg in 3-7 days interval, maximum dose 600mg per day.

*Dose reduction in renal impairment

Side-effects

Dizziness, somnolence, ataxia, peripheral edema, weight gain, visual disturbances

Precautions

  • Gradual withdrawal recommended
  • Pregnancy category C: use with caution in pregnancy and lactation
  • Use with caution in patients with history of angioedema
  • Cardiovascular disease

Contraindications

  • Hypersensitivity to Pregabalin or any of its components

Urimin

Generic composition: Febuxostat

General Introduction:

Urimin is Febuxostat, a selective xanthine oxidase inhibitor. Hyperuricemia is a condition where there is elevated level of uric acid in blood and occurs when the body produces more uric acid than it can eliminate. The uric acid forms crystals in joints (gouty arthritis) and tissues, causing inflammation and pain. Elevated blood uric acid levels also can cause kidney disease and kidney stones.

Therapeutic category

  • Anti-gout

Dosage forms available

  • URIMIN 40mg Tablets
  • URIMIN 80mg Tablets

Mechanism of action

Febuxostat is a non-purine selective inhibitor of xanthine oxidase. It works by non-competitively blocking the molybdenum-pterin center which is the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Febuxostat prevents the production of uric acid by blocking the activity of the enzyme (xanthine oxidase) that converts purines to uric acid.

 Pharmacokinetics

Absorption: about 49%, 99.2% protein bound,

Distribution: apparent volume of distribution (Vss/F) of febuxostat was approximately 50L

Metabolism: metabolized by both conjugations via uridine diphosphate glucuronosyltransferase (UGT) enzymes including UGT1A1, UGT1A3, UGT1A9, and UGT2B7 and oxidation via cytochrome P450 (CYP) enzymes including CYP1A2, 2C8 and 2C9 and non-P450 enzymes.

Elimination: eliminated primarily through both hepatic and renal pathways.

Half-life: about 5-8 hours.

 Uses

  • Chronicgout
  • Hyperuricemia

Dosage

  • 40 mg daily without regard of food; increased to 80mg per day if the target serum level of <6mg/dL is not achieved after 2 weeks, maximum dose upto 120mg.
  • No dose adjustment in elderly and mild-to-moderate hepatic and renal impairment.

 Side effects

Common s/e include: Nausea, Rash, Joint pain, Gout flares, Liver problems

Less common include: stroke, heart attack, anemia, hepatitis, hypersensitivity, weight loss

 Contraindications

  • Hypersensitivity to febuxostat or any other excipient
  • Co-administration of theophylline, azathioprine, didanosine and mercaptopurine

 Precautions

  • High blood uric acid levels caused by a condition other than gout (eg, Lesch-Nyhan syndrome, cancer or treatment of cancer, organ transplant)
  • Caution in use for children under 18 yrs; safety and efficacy not established in children
  • Pregnancy and lactation

Advantages

  • More effective than allopurinol in treating hyperuricemia as it is selective of xanthine oxidase thus does not interfere with other purine metabolism
  • Faster inhibition of uric acid synthesis than allopurinol

Relispas

Generic composition: Drotaverine HCl

General Introduction

Relispas is Drotaverine, an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase-4, and has no anticholinergic effects.

 Therapeutic category

  • Anti-spasmodic

Dosage forms available

  • RELISPAS 40mg Tablets
  • RELISPAS 80mg Tablets

Mechanism of action

Drotaverine inhibits phosphodiesterases-IV, specific for smooth muscle thereby increasing cAMP concentration, decreasing Ca2+ uptake of the smooth muscle cells and changing the distribution of calcium among the cells. Thus, it is a superior smooth muscle relaxant which acts specifically on spastic sites relieving smooth muscle spasm.

Pharmacokinetics

Bioavailability is highly variable, 80-95% plasmas protein binding, plasma half life is 7-12hrs, undergoes hepatic metabolism

 Uses

  • Renal as well as biliary colic
  • Pain and dysfunction due to smooth muscle spasm like biliary spasm, cholangitis, cholecystitis, cholelithiasis,
  • cystitis, ureterolithiasis, nephrolithiasis
  • Spastic dysmennorhoea,
  • Gastric, intestinal or pyloric spasm,
  • Irritable bowel syndrome, spastic constipation

Dosage

Adult: 40-80 mg 3 times/day with or without food

Pediatric: 20 mg 3-4 times a day (1-6 yrs old) and 40 mg 3 times/day for >6yrs

 Side Effects

Porphyria, dizzines, vertigo, headache, nausea, palpitation, constipation, insomnia, dry mouth, hypotension

 Containdications

  • Severe renal, hepatic and cardiac dysfunction.
  • Porphyria

Precautions

Patients with heart/liver/kidney disease, during pregnancy and breastfeeding.

Kecitral

KECITRAL

Generic composition: Potassium citrate 1100mg and citric acid 334mg/5ml

General Introduction

Potassium citrate/citric acid solution is a urinary alkalinizing agent. It neutralizes acidic nature of urine and also reduces the formation of crystals that could become kidney stones or aggravate gout.

Therapeutic category

  • Urinary Alkalizer

Dosage forms available

  • KECITRAL 100/170ml bottle

Mechanism of action

Potassium citrate induces changes in the urine which renders urine less susceptible to the formation of crystals and stones from salts e.g. calcium oxalate, calcium phosphate and uric acid. Citric acid is used as an acidulant to control pH and acts as an anticoagulant by chelating calcium in blood.

Pharmacokinetics

Potassium citrate is absorbed and metabolized to potassium bicarbonate, thus acting as a systemic alkalizer.  The effects are essentially those of chlorides before absorption and those of bicarbonates subsequently.  Oxidation is virtually complete so that less than 5% of the potassium citrate is excreted in the urine unchanged.

Uses

  • Maintenance of alkaline urine like uric acid, urinary tract calculi, urinary tract infection
  • Burning micturation
  • Replacement of potassium due to thiazide medication
  • Reduction of crystaluria during sullphonamide therapy

Dosage

  • 2-3 teaspoonful of solution mixed with water or juice, four times a day after meal.

 

Side effects

Abdominal pain, cramping, black stool, vomiting, heartbeat, muscle weakness, tingling in hands, feet or mouth.

Contraindications

Severe renal impairment with oliguria or azotemia, untreated Addison’s disease, adynamia episodica hereditaria, acute dehydration, heat cramps, anuria, severe myocardial damage, and hyperkalemia from any cause, allergic to the medication.

Precautions

  • Large doses may cause hyperkalemia and alkalosis, especially in the presence of renal disease.
  • Concurrent administration of potassium-containing medication, potassium-sparing diuretics, angiotensin-converting enzyme (ACE) inhibitors, or cardiac glycosides may lead to toxicity.
  • Do not exceed recommended dosage.  Discontinue use if adverse reactions occur.
  • Should be used with caution by patients with low urinary output.

 

Drug Interactions

  • antacids that contain aluminum, aspirin and other salicylates
  • ACE inhibitors such as lisinopril,
  • angiotensin blockers such as losartan)
  • potassium-sparing diuretics such as amiloride, spironolactone, triamterene

 

Mogyl

Generic composition: Tinidazole

 General Introduction

Mogyl contains active ingredient Tinidazole belonging to nitroimidazole group of anti-fungal agents. Tinidazole is active against a wide range of anaerobic bacteria and also protozoa.

Therapeutic category

  • Anti-protozoal

Dosage forms available

  • MOGYL 500mg Tablets

Mechanism of action

In anaerobic microorganisms, tinidazole is converted into an active form by reduction of its nitro group: this binds to DNA and prevents nucleic acid formation; it is bacteriostatic.

Pharmacokinetics

Tinidazole is well absorbed after either oral or rectal administration and distributed to achieve sufficient concentration to eradicate infection in liver, gut wall and pelvic tissues. It is eliminated in the urine, partly unchanged and partly as metabolites.

Uses

  • Postsurgical infection, intra-abdominal infection and septicaemia
  • Pseudomembraneous colitis.
  • Trichomoniasis of the urogenital tract in both sexes.
  • Amoebiasis (Entamoeba histolytica)
  • Giardiasis (Giardia lamblia)
  • Acute ulcerative gingivitis and dental infections (Fusobacterium spp)
  • Anaerobic vaginosis (Gardnerella vaginalis)

Dose

Amoebiasis: 2 gm for 2-3 days or 500 mg twice daily for 5 days.

Giardiasis: 2 gm as single dose or 500 mg O.D for 7 days.

Anaerobic infections: Prophylactic 2 gm single dose before colorectal surgery: Therapeutic 2 gm followed by 0.5 gm BD for 5 days.

Children: 30-50 mg/kg/day.

Side effects

Nausea, vomiting, diarrhea, furred tongue and an unpleasant metallic taste in the mouth, rashes, urticaria and angioedema occur.  Peripheral neuropathy occurs if treatment prolonged and epileptiform seizures if the dose is high.

Precautions

  • Pregnancy
  • Anticoagulants
  • Avoid alcohol intake

Contraindications

  • First trimester of pregnancy
  • Blood dyscrasias
  • Lactation
  • Neurological disorder

Drug Interactions

  • Disulfiram like reaction with alcohol
  • Synergism with ampicillin, doxycycline and co-trimoxazole.

 

Potsim

POTSIM

Generic composition: Potassium Chloride 1.5g equivalent to 20mEq of potassium ion

General Introduction

Potsim is Potassium Chloride solution used as a supplement for potassium loss, either to treat or prevent hypocalcaemia. Each 15 ml of POTSIM solution contains 20 mEq of potassium.

Therapeutic category

  • Potassium supplement

Dosage forms available

  • POTSIM 170ml bottle

Mechanism of Action

Absorption from GI to systemic circulation followed by active ion transport across cell.

Pharmacokinetics

Absorption from GI tract, eliminated via urine, under normal condition the amount of potassium absorbed is equal to the amount excreted in urine.

Uses

  • Used as a potassium supplement during loss of potassium or potassium depletion.

Potassium depletion may be caused by

  • Digitalis intoxication
  • Diuretic therapy (Furosemide/thiazides)
  • Diabetic ketoacidosis
  • Hyper aldosteronism
  • Patients on prolonged parenteral nutrition
  • Starvation
  • Excessive fluid loss- vomiting/diarrhea
  • Corticosteroid therapy
  • Hypochloremic alkalosis

Dose

Treatment of hypokalemia:

  • Adult: Daily dose ranges from 40 to 100 mEq. Give in 2 to 5 divided doses: limit doses to 40 mEq per dose. The total daily dose should not exceed 200 mEq in a 24 hour period. Maintenance or Prophylaxis: Typical dose is 20 mEq per day. Individualize dose based upon serum potassium levels.
  • Pediatric: patients aged birth to 16 years old: 2-4 mEq/kg/day in divided doses; not to exceed 1 mEq/kg as a single dose or 40 mEq. Maintenance dose: typical dose is 1 mEq/kg/day. Do not to exceed 3 mEq/kg/day.

 

Side effects

Hyperkalemia, nausea, vomiting, flatulence, abdominal pain, discomfort, diarrhea.

Drug Interaction

  1. Potassium-Sparing diuretics
  2. Angiotensin-Converting Enzyme Inhibitors
  3. Angiotensin Receptor Blockers

Contraindications

  • Patients with hyperkalaemia are contraindicated to potassium supplements like POTSIM. Increased potassium may results in arrhythmia and ultimately cardiac arrest. Hyperkalemia may complicate chronic renal failure, systemic acidosis such as diabetic acidosis, acute dehydration, and extensive breakdown as in severe burns, adrenal insufficiency, or the administration of a potassium-sparing diuretic.
  • Potassium chloride is contraindicated in patients with metabolic acidosis and hyperchloremia; other salts of potassium should be supplemented in the case.

Advantages

  • The potassium chloride solution for oral use easily replenishes the deficient potassium in the body along with chloride. This will help with lesser side effects and controlled increase of K ions than IV administration

 

Imflanex

Generic composition: Aceclofenac

General Introduction

Imflanex is Aceclofenac, an effective non-steroidal anti-inflammatory drug, which possesses remarkable anti-inflammatory, analgesic and antipyretic properties. It is a potent COX-II blocker and inhibits the synthesis of prostaglandin E2.

Therapeutic category

  • NSAIDs (Non-steroid anti-inflammatory drugs)

Dosage forms available

  • IMFLANEX 100mg Tablets

Mechanism of action

Aceclofenac preferentially inhibits Cyclooxygenase (COX), which is a key enzyme in the inflammation cascade. The inhibition of COX leads to the suppression of pro-inflammatory prostaglandins and cytokines. Thus, NSAIDs act as analgesic, antipyretic by central as well as peripheral action. Because of its safety profile the drug can be continued for long-term management of chronic rheumatic disorders and for acute inflammatory episodes

Pharmacokinetics

Absorption: Rapidly absorbed from GI tract and almost 100% bioavailability, peak plasma levels in 1-3 hours, 99% bound to plasma proteins,

Distribution:  volume of distribution is approximately 25 L

Metabolism: metabolized in liver and excreted via urine.

Elimination: Approximately two thirds of the administered dose is excreted via the urine, mainly as glucuronidated and hydroxylated forms of aceclofenac, about 20% of the dose is excreted into feces.

Half-life: mean plasma elimination half-life is approximately 4 hours

Uses

  • Rheumatoid arthritis
  • Osteoarthritis
  • Ankylosing spondylitis
  • Low back pain

Dose

  • Rheumatoid Arthritis (RA): pain-killing action of aceclofenac 100mg is more prolonged than that of paracetamol (acetaminophen) 650mg
  • Osteoarthritis Arthritis (OA): 100mg twice daily
  • Ankylosing Spondylitis: 100 mg twice daily in adults for symptomatic treatment of pain and inflammation
  • Dysmenorrhea: 100mg once a day is sufficient to reduce primary dysmenorrhoea.
  • Dental Pain Management: 100 mg twice a day
  • Low Back Pain: alone or in combination with Tizanidine

Side effects

Diarrhea, nausea, headache, indigestion, heartburn, abdominal pain, flatulence, feeling sick, dizziness, rash, abdominal bleeding

Contraindications

  • Contraindicated in patients with severe ulcer, gastrointestinal bleeding, and hypersensitivity
  • Pregnancy and lactation
  • History of Asthma

Precautions

  • Aceclofenac must be taken preferably with or after food
  • Elderly: may cause severe bleeding
  • Impaired hepatic and renal function
  • Gastrointestinal disorders of the upper or lower tract, inflammatory bowel disease (ulcerative colitis) and chronic inflammatory bowel disease (Crohn’s disease)
  • Chicken pox occurs
  • Cardiovascular diseases such as porphyria, circulation disorders, heart stroke etc

Drug Interactions

  • Selective serotonin-reuptake inhibitors or lithium
  • Phenytoin
  • Antacids like sucralfate
  • Alcohol: increases risk of GI bleeding
  • Cardiovascular drugs such as digoxin, anti-hypertensive’s, anticoagulants, diuretics
  • Quinolone antibiotics, anti-diabetics or any other NSAID drugs

Fexadine

Generic composition: Fexofenadine HCl

General Introduction

Fexadine contains fexofenadine, a second generation antihistamine. Fexofenadine is H1 receptor antagonist.

Therapeutic category

  • Anti-histamines

Dosage forms available

  • FEXADINE 120mg Tablets
  • FEXADINE 180mg Tablets
  • FEXADINE Suspension 30mg/5ml

Mechanism of action

Fexofenadine is considered an “inverse agonist” of the H1 receptor because it binds to and stabilizes the inactive form of the receptor, preventing its activation and subsequent downstream effects. It has a potent and selective affinity for H1 receptors, and there is no evidence that it carries antidopaminergic, antiserotonergic, anticholinergic, sedative, or adrenergic blocking activity.

Pharmacokinetics

Absorption: Rapidly absorbed from the GI tract following oral administration, peak plasma concentrations achieved in about 2.6 hours, antihistaminic effect occurs within 1–3 hours and persists for about 12 hours, 60–70% plasma protein binding.

Distribution: It is distributed into the small and large intestines, stomach, pancreas, liver, and kidney in animals, does not appear to cross the blood-brain barrier,

Metabolism: Metabolized in the liver and eliminated via feces.

Elimination: very minimally metabolized, with only 5% of an ingested dose undergoing hepatic metabolism.

Half-life: terminal elimination half-life is approximately 11-15 hours.

Uses

  • Allergic rhinitis
  • Chronic urticaria
  • Allergic skin disorders
  • Allergic manifestation of ophthalmic origin

Dose

  • Adults: 120mg OD for allergic rhinitis and 180mg OD for urticaria and other skin diseases.
  • Children:  5 ml every q12 hourly (30mg twice daily)

Side Effects

Headache, upper respiratory tract infection, coughing, nausea, dysmenorrhea, sinusitis, dizziness, drowsiness, dyspepsia, fatigue, headache.

 Precautions

Renal impairment, geriatric patients, pregnancy, lactating infant, rash, urticaria, pruritus, and hypersensitivity reactions (e.g., angioedema, chest tightness, dyspnea, flushing, anaphylaxis) reported rarely.

Advantages

Fexofenadine does not cross the blood-brain barrier and thus is unlikely to cause significant CNS effects.

Esmosim

Generic composition: Esomeprazole

General Introduction

Esomeprazole is an S-enantiomer of omeprazole, claimed to have higher oral bioavailability and produce better control of gastric pH than omeprazole.

Therapeutic category

  • Proton pump inhibitors

Dosage forms available

  • ESMOSIM 20mg Tablets
  • ESMOSIM 40mg Tablets

Mechanism of action

  • Like all other PPIs, it blocks the enzyme H+-K+ATPase in the wall of the stomach thereby suppressing acid production and helps in healing of ulcers.

Pharmacokinetics

  • Absorption: Peak plasma concentration occur at approximately 1.5 hours after oral administration, esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions, 97% plasma protein bound
  • Metabolism: extensively metabolized in liver by cytochrome P450 enzyme
  • Elimination: approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the feces.
  • Half-life: 1-1.5 hours

Uses

  • GERD
  • Dyspepsia
  • Gastritis
  • Peptic ulcer
  • Zollinger-Ellison Syndrome
  • Heartburn

 Dose

  • 1 tablet to be taken once a day in empty stomach
  • 20-40mg once daily for 4-8 weeks for healing erosive esophaigitis, peptic ulcer, 20mg once daily as a maintenance dose,
  • 20mg once daily for up to 4 weeks for GERD and can be additionally taken up to 4 weeks,
  • 10 days of triple therapy with esomeprazole 40 mg once daily, amoxicillin 1g and clarithromycin 500 mg twice daily for eradication of H. Pylori

Side effects

  • The most frequently occurring adverse events were headache, diarrhea, nausea, flatulence, abdominal pain and constipation.

 Contraindications

  • Hypersensitivity to esomeprazole or to substituted benzimidazoles.

Precautions

  • Because treatment with esomeprazole may alleviate symptoms and delay diagnosis, patients on long-term treatment should be kept under regular surveillance.
  • Caution should be exercised in pregnant and nursing mothers.

Drug interaction

  • Atazanavir: Plasma concentrations may be reduced by esomeprazole, decreasing the efficacy.
  • Diazepam: Plasma concentrations may be increased by esomeprazole; however, the increase not likely to be clinically important.
  • Drugs dependent on gastric pH for bioavailability (eg, ampicillin, cyanocobalamin, digoxin, iron salts, ketoconazole) – Absorption of these drugs may be affected.
  • Warfarin: Risk of bleeding may be increased

Cefanol

Generic composition: Cefpodoxime Proxetil

General description

Cefpodoxime is an oral third generation cephalosporin antibiotic with effectiveness against most Gram positive and Gram negative bacteria

Therapeutic category

  • Anti-bacterial (3rd generation Cephalosporin)

Dosage forms available

  • CEFANOL 100mg Tablets
  • CEFANOL 200mg Tablets
  • CEFANOL Dry Syrup 50mg/5ml

Mechanism of action

  • The bactericidal activity of cefpodoxime results from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime binds preferentially to penicillin binding protein 3, which inhibits production of peptidoglycan, the primary constituent of bacterial cell walls.

Pharmacokinetics

  • Absorption: absorbed from GI tract, bioavailability approximately 50%, protein binding is 22 to 33% in serum and from 21 to 29% in plasma.
  • Metabolism: metabolized in liver
  • Elimination: approximately 29 to 33% of the administered cefpodoxime dose was excreted unchanged in the urine in 12 hours.
  • Half-life: 09 to 2.84 hours

Uses

  • ENT Infections
  • Bronchitis
  • UTI
  • Pneumonia
  • Skin and soft tissue infection
  • Acute, uncomplicated urethral and cervical gonorrhea
  • Surgical Infections
  • Typhoid fever

Dose

  • Adult: 100 mg two times a day q12 hourly for Pharyngitis, Tonsillitis, UTI, 200mg two times a day q12 hourly for Pneumonia, ENT infections, Bronchitis,
  • Pediatric: 10ml two times a day 12 hourly

Side effects

Diarrhea, Nausea, headache, abdominal pain, vomiting, skin rash, dyspepsia,

Contraindication

Cefpodoxime is contraindicated in patients with known allergy to the cephalosporin group of   antibiotics.

Drug Interactions

  • Antacids (decreases the extent of absorption of cefanol
  • Renal excretion of cefpodoxime was inhibited by probenecid

Precautions

Dose reduction in case of renal insufficiency. Cefpodoxime, like other cephalosporins, should be administered with caution to patients receiving concurrent treatment with potent diuretics.

Pregnancy category: B

Azocin

General Introduction

Azithromycin is a broad-spectrum macrolide antibiotic.

Therapeutic Category

  • Macrolide antibiotics

Dosage forms available

  • AZOCIN 500mg Tablets

Mechanism of action

  • Azithromycin shows its anti-bacterial properties by binding to the 23S rRNA of the bacterial 50S ribosomal subunit. It stops bacterial protein synthesis by inhibiting the transpeptidation/translocation step of protein synthesis and by inhibiting the assembly of the 50S ribosomal subunit.

Pharmacokinetics

  • Absorption: Absorption not affected by food, oral bioavailability 37%,
  • Distribution: Widely distributed throughout the tissues with apparent volume of distribution of 31.1 L/Kg.
  • Metabolism: metabolized in liver
  • Elimination: excreted via urine, biliary excretion.
  • Half-life: elimination half life is 68 hours

Uses

  • Pharyngitis
  • Sinusitis
  • Tonsillitis
  • Pneumonia
  • Nonspecific urethritis
  • Donovanosis
  • Typhoid in patients allergic to cephalosporins

Dose

  • 500mg tablets once a day for upto 3-5 days maximum upto a week to 10 days

Side effects

  • Anorexia, Constipation, dyspepsia, flatulence, urticaria, edema, fatigue, malaise, anaphylaxis, acute renal failure, hepatic necrosis, hearing disturbances, dizziness, headache

Contraindications

  • Hypersensitivity to azithromycin, any macrolide antibiotic, or erythromycin.

Drug Interactions

Aluminum- and magnesium-containing antacids, Cyclosporine, HMG-CoA reductase inhibitors,

Precautions

  • Patients with impaired hepatic or renal function and during lactation.
  • Safety and efficacy for acute otitis media have not been determined in children less than 6 months of age or for pharyngitis/tonsillitis in children less than 2 years of age.

Pregnancy Category: B

Advantages

  • Azithromycin is highly stable at a low pH, giving it a longer serum half-life and increasing its concentrations in tissues compared to erythromycin.
  • AZOCIN has minimal adverse reaction and superior gastrointestinal tolerability.

Razapine

Generic composition: Mirtazapine

 General Description

Mirtazapine is a tetracyclic piperazino-azepine antidepressant agent

Therapeutic category

  • Atypical Anti-depressant

 Dosage forms available

  • RAZAPINE 7.5mg Tablets
  • RAZAPINE 15mg Tablets
  • RAZAPINE 30mg Tablets

Mechanism of action

Mirtazapine enhances central noradrenergic and serotonergic activity. Mirtazapine acts as an antagonist at

central presynaptic α 2 adrenergic autoreceptors and heteroreceptors, an action that is postulated to increase in

central noradrenergic and serotonergic activity.

Mirtazapine is a potent antagonist of 5-HT2 and 5-HT3 receptors. Mirtazapine has no significant affinity for the 5-HT1A and 5-HT1B receptors.  Mirtazapine is a potent antagonist of histamine (H1) receptors, a property that may explain its prominent sedative effects.

Mirtazapine is a moderate peripheral α1 adrenergic antagonist, a property that may explain the occasional orthostatic hypotension reported in association with its use. Mirtazapine is a moderate antagonist at muscarinic receptors, a property that may explain the relatively low incidence of anticholinergic side effects associated with its use.

 Pharmacokinetics

Absorption: absorption is rapid and complete, bioavailability is 50% due to first pass metabolism, peak concentration reaches after 2 hours of administration, and food has little effect on drug absorption, about 85% protein bound.

Distribution: volume of distribution after an oral steady-state dose was measured to be 107 ± 42L

Metabolism: extensively metabolized in liver by demthylation and hydroxylation, glucuronide conjugation.

Elimination: excreted by kidney; 75% eliminated in the urine and 15% eliminated in the feces.

Half-life: 20-40 hours

Uses

  • Major depressive disorder
  • Mood disorder
  • Anxiety disorder

Dose

  • 15 mg/day, administered in a single dose, preferably in the evening prior to sleep.
  • Initial 15-mg dose may benefit from dose increases up to a maximum of 45 mg/day.
  • The effective dose range was generally 15 to 45 mg/day.

Side effect

Increase in appetite and weight, nausea, drowsiness and sedation are common. Orthostatic hypotension, dry

mouth, constipation, nightmares, confusion, myalgia, anthralgia, tremor, edema.

Contraindications

  • Use with MAO Inhibitors
  • Hypersensivity to Mitrazapine

 Precaution

  • Gradual withdrawal
  • Hyponatremia

Drug interaction

  • MAO Inhibitors, serotonergic drugs
  • Cimetidine
  • Clonidine
  • Alcohol

Pregnancy Category: C

Qtasim

Generic composition: Quetiapine Fumarate

General description

Quetiapine is a second-generation dibenzothiazepine atypical antipsychotic used in schizophrenia, major depression, and bipolar disorder. Quetiapine demonstrates a high level of therapeutic efficacy and low risk of adverse effects during long-term treatment. It is well-tolerated and a suitable option for some patients with high sensitivity to other drugs, such as clozapine and olanzapine.

Therapeutic category

  • Atypical Anti-psychotics

Dosage forms

  • QTASIM 25mg Tablets
  • QTASIM 50mg Tablets
  • QTASIM 100mg Tablets

Indications

  • Schizophrenia
  • Bipolar Disorder
  • Major Depressive Disorder

 Dose

  • 25mg or 50 mg two or three times a day.
  • Dose reduction in elderly and hepatic impairment: initial 25 mg followed by daily increments of 25-50 mg, according to response.

 Mechanism of action:

It is Dopamine (D1 and D2), Serotonin (5-HT2), Histamine (H1), and Adrenergic receptor antagonist. It has been

proposed that the efficacy of Quetiapine in schizophrenia and its mood-stabilizing properties in bipolar

depression and mania are mediated through a combination of D2 and 5-HT2 antagonisms.

Pharmacokinetics     

Absorption: Well absorbed after oral doses, 83% plasma Protein Binding), 1.5 hrs peak plasma concentration

Distribution: distributes throughout body tissues, apparent volume of distribution of this drug is about 10±4 L/kg.

Metabolism: Metabolized in liver by CYP3A4 (sulfoxidation and oxidation).

Elimination: Eliminated primarily via urine (73%) and minor via feces (20%),

Half-life: 6-7 hours

Precautions

Caution in patients receiving antihypertensive, gradual withdrawal is recommended, because of risk of withdrawal symptoms.

Side effects

Common: Somnolence, headache, dizziness, weight gain, particularly during early treatment, rises in plasma-TG and total cholesterol concentration, constipation, dry mouth, dyspepsia, increased appetite, peripheral edema, anxiety.

Rare: Orthostatic hypotension associated with dizziness, tachycardia and syncope, Hyperglycaemia and exacerbation of pre-existing diabetes. Monitoring in such case required.

 Drug Interactions:

  • Central effects of CNS Depressants, including alcohol, are increased.
  • CYP inhibitors like erythromycin, fluconazole, ketoconazole increases plasma concentration. Hence, dose reduction recommended.
  • CYP inducers like carbamazepine, phenytoin decreases concentration. Hence, higher dose recommended.

References

  • Rxlist
  • Drug bank

Oxapine

Generic composition: Oxcarbazepine

 General Description

Oxapine is Oxcarbazepine, anti-epileptic medication primarily used in the treatment of epilepsy. Compared to other anti-epileptic drugs, which are generally metabolized via the cytochrome P450 system, oxcarbazepine has a reduced propensity for involvement in drug-drug interactions owing to its primarily reductive metabolism.

Therapeutic category

  • Antiepileptics

 Dosase forms

  • OXAPINE 150mg Tablets
  • OXAPINE 300mg Tablets

Indications

  • Monotherapy or adjunctive therapy in the treatment of partial seizures in adults
  • Monotherapy in the treatment of partial seizures in children aged 4 years and above with epilepsy,
  • Adjunctive therapy in children aged 2 years and above with epilepsy.
  • Bipolar-disorder (Add-on therapy to intractable cases)
  • Trigeminal Neuralgia
  • Neuropathic Pain
  • Temporal lobe epilepsy in child and adults.

Dose

Adult dose:

Initial dose: 300 mg orally twice a day, increased by 300mg/day every third day as clinically indicated
Maintenance dose: 300-1200mg twice a day

Pediatric dose:

Initial dose: 8-10mg/kg given twice a day, maximum dose 600mg/day, increased by 5mg/kg/day every third day as clinically indicated

 Side effects

Common side effects include nausea, vomiting, dizziness, drowsiness, headache, double vision and trouble with walking

 Contraindications

Known hypersensitivity to oxcarbazepine or to any of its components

Mechanism of action

The precise mechanism by which oxcarbazepine exert their anti-seizure effect is unknown; however, in vitro electrophysiological studies indicate that they block voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and propagation of synaptic impulses. In addition, it also modulates high-voltage activated calcium channels may contribute to the anticonvulsant effects of the drug. Its spectrum of anticonvulsant activity is comparable to carbamazepine, but it has an improved pharmacokinetic profile, is better tolerated and is associated with few clinically significant drug-drug interactions.

 Pharmacokinetics

Absorption: Absorbed following oral administration, rate and extent of absorption of oxcarbazepine is not affected by food intake.

Distribution: apparent volume of distribution of oxcarbazepine is 49 L.

Metabolism: rapidly and extensively metabolized to its primary metabolite, MHD, which is responsible for the bulk of its anti-epileptic activity and exists in much higher concentrations in the plasma than the parent drug.

Elimination: more than 95% of the administered dose of oxcarbazepine is found in the urine. Of this, approximately 49% is MHD glucuronide metabolites, 27% is unchanged MHD, 3% is inactive DHD metabolites, 13% is conjugated oxcarbazepine, and less than 1% is unchanged parent drug. Fecal elimination accounts for only 4% of the administered dose.

Precautions

  • Hyponatremia
  • Serious Dermatological Reactions
  • Suicidal Behavior and Ideation
  • Gradual withdrawal recommended
  • Pregnancy Category C
  • Dose adjustment in renal impairment

 Drug Interactions

  • Anti-epileptic drugs: Phenytoin, phenobarbitone
  • Hormonal contraceptives

 Advantages

  • Better tolerated than Carbamazepine with lesser side effects profile
  • Improved Pharmacokinetic properties

Flumax

Generic composition: Fluoxetine

 General description

Flumax is a second generation anti-depressants which is categorized as a selective serotonin reuptake inhibitor (SSRIs)

 Therapeutic group

  • Anti-depressants

Dosage forms available

  • FLUMAX 10mg capsules
  • FLUMAX 20mg capsules

Uses

  • Major Depressive Disorder (MDD)
  • Obsessive–compulsive disorder(OCD)
  • Bulimia nervosa
  • Panic disorder
  • Premenstrual dysphoric disorder
  • Also been used inpremature ejaculation

 Dose

Condition Adult Pediatric (>8 yrs)
MDD 20 mg/ day initial in morning 10-20 mg/day
OCD 20 mg/ day initial in morning 10 mg/day initial
Bulimia Nervosa 60 mg/day in morning –
Panic Disorder 10 mg/day in morning –

 Adverse effects

Common side effects include insomnia, abnormal dreams, agitation, loss of appetite, dyspepsia, diarrhea, dry mouth, rash, decreased libido, abnormal ejaculation and impotence. Serious side effects include serotonin syndrome, mania, seizures, an increased risk of suicidal behavior in people under 25 years old, and an increased risk of bleeding.

Contraindications

  • Hypersensitivity to fluoxetine or any other excipient.
  • Switching to or from an MAO inhibitor intended to treat psychiatric disorders: Allow 14 days to elapse between discontinuing an MAO inhibitor and initiation of fluoxetine.  Similarly, a 5 weeks interval between discontinuing fluoxetine and initiation of an MAO inhibitor intended to treat psychiatric disorders. -Use with other MAO inhibitors (linezolid or I.V. methylene blue):
  • Concurrent administration of linezolid or I.V. methylene
  • Concurrent administration of thioridazine or pimozide; QT interval prolongation or potential for elevated thioridazine plasma levels.
  • Lactation is not recommended

Mechanism of action

Fluoxetine inhibits the reuptake of serotonin and doesn’t appreciably inhibit norepinephrine and dopamine reuptake at therapeutic doses. It also delays the reuptake of serotonin, resulting in serotonin persisting longer when it is released. It also blocks the uptake of serotonin into human platelets.

 Pharmacokinetics

Absorption: oral bioavailability of fluoxetine is <90%, approximately 94% of fluoxetine is plasma protein bound, fluoxetine is very lipophilic and highly plasma protein bound, allowing the drug and its active metabolite, norfluoxetine, to be distributed to the brain.

Distribution: volume of distribution of fluoxetine and its metabolite varies between 20 to 42 L/kg.

Metabolism: Fluoxetine is metabolized to norfluoxetine by CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5 upon ingestion.

Elimination: Fluoxetine is primarily eliminated in the urine.

Half-life: The half life of fluoxetine is significant with the elimination half-life of the parent drug averaging 1-3 days after acute administration, and 4-6 days after chronic administration

 Precautions

  • Pregnancy category C
  • Gradual withdrawal recommended
  • Clinical worsening and suicidal tendency increased in initial stage of treatment; patient requires close supervision
  • Caution when used with diuretics
  • Caution in patient with seizure/convulsions

Interactions

  • Monoamine Oxidase Inhibitors (MAOI) and other serotonergic drugs.
  • CNS Acting Drugs: Caution should be used when taken in combination with other centrally acting drugs (anti-psychotics, anti-convulsants)
  • Benzodiazepines (e.g. Diazepam) and alprazolam
  • Triptans and tryptophan; Concomitant use with tryptophan is not recommended (5.2, 7.5)
  • NSAIDs and anticoagulants; may potentiate the risk of bleeding

Advantages

  • Fluoxetine has advantages over other SSRIs in patients who are poorly compliantas fluoxetine has a long half-life, so missing a dose is unlikely to cause problems.
  • Safety in overdose, relatively mild toxic effects even in children
  • Mild withdrawal symptoms
  • Low potential for weight gain
  • The only SSRI approved by FDA for use in children 8 years of age and older
  • Associated with the lowest risk of suicide
  • Fluoxetine improves peripheral and hepatic insulin action in type 2 diabetes patients

Durexin

Generic composition: Dosulepin

 General description

Durexin is formerly known as Dothiapen, belongs to Tricyclic antidepressants (TCAs) with anxiolytic effects.

Therapeutic category

  • Tri-cyclic Anti-depressants

Dosage forms available

  • DUREXIN 25mg Tablets

 Mechanism of action

Dosulepin is active in inhibiting the reuptake of noradrenaline, 5- hydroxytryptamine (5-HT) and dopamine. Dosulepin also reduces and/or down regulates central noradrenaline receptor numbers. It inhibits the uptake of 5-HT into the platelets. Dosulepin also has some central and peripheral anti-cholinergic and antihistaminic activity at standard dose levels.

Pharmacokinetics

Dosulepin is readily absorbed from small intestine, peak plasma concentration reaches in 2-3 hours, highly protein-bound, extensively metabolised in the liver and excreted primarily from urine. Dosulepin crosses blood-brain barrier, placenta and excreted in breast milk.

 Uses

  • Major Depressive Disorders
  • Neuropathic pain (Offlabel)

 Dose –

  • Dosulepin to SSRI: gradually reduce the dose to 25mg – 50 mg / day then added SSRI at usual starting dose, and then slowly withdraw the remaining dosulepin over 5 – 7days.
  • Dosulepin 25mg two to three times a day until using the dosulepin, this will reduce chances of side effects while it will be used to the dosulepin
  • Dose start at 25 mg a day and be increased slowly to 75 mg a day for pain relief or preventing migraine.
  • Adults: Initially 75 mg/day in divided doses or as a single dose at night, increasing to 150mg/day
  • Elderly: 50-75mg daily initially.
  • Children: Not recommended

 Side effects

Drowsiness, hyponatremia (esp in elderly), cardiotoxicity, postural hypotension, anticholinergic side effects (blurred vision, urinary retention, constipation), extra pyramidal side effects, arrhythmias, convulsions.

 Contraindications

  • Recent myocardial infarction, any degree of heart block or other cardiac arrhythmias
  • Mania
  • Severe liver disease and hepatic dysfunction
  • Hypersensitivity to dosulepin or to any of the excipients
  • Epileptic patients as dosulepin decreases the seizure threshold
  • Narrow angle glaucoma and prostatic hypertrophy
  • Alcohol consumption due to CNS Depressant activity

Precautions

  • Caution in elderly and patients susceptible for cardiovascular toxicity
  • Suicidal tendency may be increased
  • Caution in patients with history of mania or psychoses
  • Renal impairment
  • Gradual withdrawal recommended
  • Diabetic patients as dosulepin may alter blood sugar levels
  • Pregnancy; should be avoided unless compelling reason to administer.

Pregnancy category: C

Interactions

  • MAOIs and SSRIs; concomitant administration should be avoided.
  • Cardiovascular drugs (eg. quinidine), antiarrhythmics (eg. quinidine), calcium channel blockers (eg. diltiazem, verapamil), antihistamines (eg. astemizole and terfenadine), some antipsychotics (notably pimozide and sertindole), cisapride and sotalol; arrhythmias may precipitate.
  • Antimuscarinic side effects may be enhanced by concurrent use with antimuscarinic drugs.
  • Oral contraceptives may antagonise the antidepressant effect but side effects may be increased due to increased plasma concentrations of tricyclics.
  • Diuretics; increased risk of postural hypotension
  • It is advisable to review all antihypertensive therapy during treatment with tricyclic antidepressants.
  • Anaesthetics given during tricyclic antidepressant therapy may increase the risk of arrhythmias and hypotension. If surgery is necessary, the anaesthetist should be informed that the patient is being so treated.
  • Barbiturates and other enzyme inducers such as rifampicin; may increase the metabolism of tricyclic antidepressants and result in lowered plasma concentrations and reduced antidepressant response.

Advantages

  • Fewer anticholinergic side effects of all TCAs.

Arifil

Generic composition: Aripiprazole

General description

ARIFIL is an  antipsychotic primarily used in the treatment of schizophrenia and bipolar disorder.

Therapeutic category

  • Atypical anti-psychotics

Dosage forms available

  • ARIFIL 10mg Tablets
  • ARIFIL 15mg Tablets

 Uses

  • Schizophrenia
  • Manic and Mixed Episodes associated with Bipolar I Disorder
  • Adjunctive Treatment of Major Depressive Disorder in adults
  • Irritability Associated with Autistic Disorder
  • Tourette’s Disorder

Dose

  • Adult: 10-15mg/day administered on a once-a-day schedule without regard to meals
  • Adolescent: 2mg/day initial dose, increased to 10mg/day, maximum to 30mg/day
  • No dosage adjustment in renal and hepatic impairment

Mechanism of action

Aripiprazole is partial agonist of dopamine receptor and antagonist of Serotonin receptor. Aripiprazole is associated with minimal weight gain in the course of therapy.

 Pharmacokinetics

Absorption: Bioavailability of the oral tablets is about 90%; peak plasma concentration reaches in 3-5 hours

Distribution: Volume of distribution is 404L or 4.9L/kg

Metabolism: undergoes extensive hepatic metabolization by cytochrome P450 (CYP) 3A4 and CYP2D6

Elimination: excreted via feces and urine.

Half-life: half life of aripiprazole is 75 hours and half life of the active metabolite is 94 hours

When dosed daily, brain concentrations of Aripiprazole will increase for a period of 10–14 days, before reaching stable constant levels

Side-effects

Headache, agitation or anxiety, insomnia, orthostatic hypotension, gastro-intestinal effects like nausea and constipation, lightheadedness, sleepiness, increased appetite, and stuffy nose

 Contraindications

Patients with a history of a hypersensitivity reaction to Aripiprazole or any excipients

Precautions

  • Pregnancy category C
  • In patients with Parkinson’s Disease, cardiovascular disease and pneumonia

Interactions

  • Alcohol and other centrally affecting drugs
  • Antihypertensive
  • Interaction of Aripiprazole with inhibitors or inducers of CYP enzymes or other factors like smoking is unlikely

Anzipin MD

Generic composition: Olanzapine

 General description

Anzipin is classified as thiobenzodiazepine that belongs to atypical antipsychotics.  It is available as mouth-dissolving (MD) tablets which mean the tablet rapidly disintegrates and dissolves in the mouth saliva, without the need of water or chewing, normally within 15 seconds to 3 minutes. The advantage of being mouth dissolving formulation means it can be dissolved in everyday solvents like water, curry etc for easy administration to uncooperative patients.

Therapeutic category

  • Atypical Antipsychotics

 Dosage forms available

  • ANZIPIN MD 2.5mg Tablets
  • ANZIPIN MD 5mg Tablets
  • ANZIPIN MD 7.5mg Tablets
  • ANZIPIN MD 10mg Tablets

Uses

  • Schizophrenia
  • Bipolar Disorder (Manic or Mixed phase).

Dosage

 

Condition   Dose
Schizophrenia Adult Initial 5-10 mg once daily, later 10 mg/day
Adolescent Initial 2.5-5 mg once daily, later 10 mg/day
Bipolar Disorder I Adult 10-15 mg once daily, later 10 mg/day
(manic and mixed episode) Adolescent Initial 2.5-5 mg once daily, later 10 mg/day

* Olanzapine is not recommended for use in children and adolescents below 18 years of age due to a lack of data on safety and efficacy.

Mechanism of action

Olanzapine is an antipsychotic, antimanic and mood-stabilising. Olanzapine inhibits dopamine, serotonin, cholinergic and muscarinic receptors. Unlike some other antipsychotic agents, olanzapine increases responding in an “anxiolytic” test.

Pharmacokinetics

Absorption: Well absorbed after oral administration, food does not affect the rate or extent of absorption, peak plasma concentration in around 6 hours, 93% plasma protein bound,

Distribution: extensively distributed throughout the body, volume of distribution is 1000 liters

Metabolism: metabolized by liver and eliminated via urine.

Half-life: Half life is ranging between 21 to 54 hours.

Adverse effects

Dizziness, weight gain, Tardive dyskinesia (irreversible involuntary movements), orthostatic hypotension, agranulocytosis, neutropenia, anticholinergic side effects (dry mouth, blurred vision, urinary retention), hyperglycemia, dyslipidemia, drug-induced Parkinson disease.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients.
  • Patients with known risk of narrow-angle glaucoma
  • Elderly Patients with Dementia-Related Psychosis; increased risk of death and increased incidence of cerebrovascular adverse events (e.g., stroke, transient ischemic attack)
  • Lactation not recommended

Precautions

  • Lower dose (5mg/day) should be considered for those 65 and over, hepatic impairment and renal impairment and dose is to be increased with caution.
  • Increase in suicidal tendency
  • Pregnancy category C
  • A potentially fatal symptom complex referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with administration of antipsychotic drugs, including olanzapine. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis and cardiac dysrhythmia).
  • Patients with diabetes or borderline glucose level.

Interactions

  • Benzodiazepines (e.g. Diazepam) and alcohol; May potentiate orthostatic hypotension
  • Centrally acting drugs such as Carbamazepine, fluvoxamine, lorazepam (IM)
  • Antihypertensive Agents: Enhanced antihypertensive effect
  • Levodopa and Dopamine Agonists: May antagonize levodopa/dopamine agonists

Advantages of olanzapine

  • Used to treat schizophrenia or mania with sedative or anxiolytic action
  • Olanzapine demonstrated superior antipsychotic efficacy compared with haloperidol in acute phase of schizophrenia, and in the treatment of some patients with first-episode or treatment-resistant schizophrenia.
  • Reduced risk of adverse events and therapeutic superiority compared with haloperidol and risperidone in the treatment of negative and depressive symptoms
  • Since it is mouth dissolving, it is ideal in patients with compliance problem or dysphagia (difficulty in swallowing) like children, elderly or mentally disabled patients.

Amisol

Generic composition: Amisulpride

General description

Amisulpride is a substituted benzamide derivative structurally related to sulpiride. It belongs to the second-generation antipsychotic that preferably binds to dopamine D2 /D3 receptors in limbic rather than striatal structures.

 Therapeutic category

  • Atypical Antipsychotics

Dosage forms available

  • AMISOL 50mg Tablets
  • AMISOL 100mg Tablets

Uses

  • Acute and chronic schizophrenic disorders
  • Episodes of mania in bipolar disorder.
  • Tourette syndrome

Dose

  • Acute psychotic episode in schizophrenia: 400-800mg/day in divided doses (BID); maximum recommended daily dose is 1200mg
  • For predominant negative symptoms: oral doses between 50mg/d and 300mg/d; doses should be adjusted individually.
  • Dosage adjustment in renal failure: The dose should be halved if the Creatinine clearance (Cr Cl) is 30-60 mL/min and reduced to one-third for Cr Cl between 10-30 mL/min

Mechanism of action

Amisulpride binds selectively to dopamine D(2) and D(3) receptors in the limbic system. Low doses of amisulpride preferentially block presynaptic D(2)/D(3)-dopamine autoreceptors, thereby enhancing dopaminergic transmission, whereas higher doses block postsynaptic receptors, thus inhibiting dopaminergic hyperactivity. It may also have 5-ht7 antagonistic effect, useful in depression treatment.

 Pharmacokinetics

Absorption: Bioavailability is approximately 36%/48% when given orally; plasma protein binding is 17%,

Half-life: half-life is 12 hours

Metabolism: metabolized in liver

Elimination: excreted unchanged in the urine

Contraindications

  • Concomitant prolactin-dependent tumors e.g. pituitary gland prolactinoma and breast cancer
  • Hypersensitivity to Amisulpride, other benzamide derivatives or any excipients
  • Pregnancy and lactation
  • Amisulpride is not recommended for children up to puberty
  • Levodopa
  • Hepatic impairment
  • Class I and III anti-arrhythmic. Ed. Quinidine, amiodarone, sotalol

Interactions

  • Amisulpride may enhance the CNS effects of hypnotics, tranquilizers, anesthetics, antihistamines, morphine derivatives, barbiturates, benzodiazepines
  • Alcohol: CNS depressant effect may increase
  • Phenytoin, Levodopa, valproate
  • Antihypertensive: may potentiate hypotensive effect

Precautions:

  • Patients with a history of seizures
  • Elderly patients: possible risk of hypotension or sedation
  • Gradual withdrawal recommended
  • Patients with Parkinson’s disease since it may cause worsening of the disease.

Advantages of Amisulpride

  • Minimal extrapyramidal side effects.
  • Lower chances of weight gain and decreased libido.
  • Enhances dopamine transmission.
  • Effective in both Acute Psychoses (short term) and Chronic Psychoses (long term). & Positive results against dysthymia.

Stanil

Generic composition: Sertraline HCl

General description

Sertraline is a popular antidepressant medication commonly known as a selective serotonin reuptake inhibitor (SSRI). Sertraline displays enhanced safety or tolerability than other classes of antidepressants, which frequently cause high levels of drowsiness, dizziness, blurred vision, and other undesirable effects.

Therapeutic group

  • SSRIs Anti-depressants

Dosage forms available

  • STANIL 25mg Tablets
  • STANIL 50mg Tablets

Uses

  • Major Depressive Disorder
  • Post-traumatic Stress Disorder
  • Obsessive-compulsive Disorder
  • Panic Disorder
  • Premenstrual Dysphoric Disorder
  • Social Anxiety Disorder

Dose

  • Initial dose of 25mg to 50mg per day
  • For adults and pediatric patients, subsequent dosages may be increased in case of an inadequate response in 25 to 50 mg per day increments once a week, depending on tolerability, up to a maximum of 200 mg per day.

Mechanism of action

Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, thereby increasing serotonergic activity. These results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. These changes are believed to be responsible for the antidepressant action and beneficial effects in obsessive-compulsive (and other anxiety related disorders).

 Pharmacokinetics

  • Absorption: mean peak plasma concentrations occurred between 4.5 to 8.4 hours after administration, and measured at 20 to 55 μg/L, highly protein bound;about 98%-99%.
  • Distribution: widely distributed, and its volume of distribution is estimated to be more than 20L/kg.
  • Metabolism: heavily metabolized in the liver and has one major active metabolite. It undergoes N-demethylation to form N-desmethylsertraline, which is much less potent in its pharmacological activity than sertraline
  • Elimination: excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces
  • Half-life: elimination half-life of sertraline is approximately 26 hours

Side effects

  • Ejaculation failure, dry mouth, increased sweating, somnolence, dizziness, tremor, diarrhea, nausea, insomnia, fatigue, palpitations, weight loss.
  • Rare: Menstrual irregularities, erythema multiforme and pancreatitis.

Contraindication

  • Use with MAO Inhibitors
  • With known hypersensitivity to sertraline and its excipients
  • Taking pimozide

Drug Interaction

  • The concomitant use of SSRIs with MAOIs increases the risk of serotonin syndrome; eg isocarboxazid, phenelzine, linezolid,
  • Increased plasma concentrations of pimozide, a drug with a narrow therapeutic index, may increase the risk of QTc prolongation and ventricular
  • The concomitant with another drug that is highly bound to plasma protein may increase free concentrations of sertraline or other tightly-bound drugs in plasma eg: Warfarin
  • The concurrent use of an antiplatelet agent or anti-coagulant with ZOLOFT may potentiate the risk of bleeding. Eg aspirin, warfirin.
  • Use with phenytoin increases concentration of phenytoin.
  • Drugs metabolized by CYP2D6 like: flecainide, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, thoridazine, tolterodine, venlafaxine, propafenone as sertraline is CYP2D6 inhibitor

 Precautions

  • Not approved for bipolar depression. May precipitate mixed/manic episode in patients at risk for bipolar disorder.
  • Less frequent dosing or reduced dose is recommended in hepatic impairment patients. While, no such caution is indicated for renal impairment. Gradual dose reduction recommended.
  • Category C drug for Pregnancy. Caution during 3rd trimester of pregnancy due to risk of neonatal complications.

Spen

Generic composition: Risperidone

 General Description

Risperidone is a second-generation antipsychotic medication used in the treatment of a number of mood and mental health conditions including schizophrenia and bipolar disorder. It is one of the most widely used second generation antipsychotics.

Therapeutic group

  • Atypical Anti-psychotics

 Dosage forms available

  • Spen 1mg Tablets
  • Spen 2mg Tablets
  • Spen 3mg Tablets
  • Spen 4mg Tablets

Uses

  • Schizophrenia
  • Bipolar Disorder
  • Irritability associated with autistic disorder
  • Monotherapy or in combination with lithium or valproate in acute mania phase of Bipolar Disorder

Dose

  • Initial 2mg once or twice a day, increments of 1-2mg per day as tolerated to effective dose of 4-8mg per day

     *Dose reduction in hepatic impairment, renal impairment and in elderly

Side effect

Common side effects include movement problems, sleepiness, trouble seeing, constipation, and increased weight, orthostatic hypotension, tardive dyskinesia, neuroleptic malignant syndrome, an increased risk of suicide, and high blood sugar levels.

Contraindications

Hypersensitivity to risperidone or any other excipients

Mechanism of action

It has been proposed that the drug’s therapeutic activity in schizophrenia is mediated through a combination of dopamine Type 2 and serotonin Type 2 receptor antagonism. Dopamine receptor antagonism results in improvement of positive symptoms. Serotonin receptor antagonism provides relief from negative symptoms of schizophrenia.

Pharmacokinetics

Absorption: Rapidly absorbed after oral administration, food does not affect the rate or extent of absorption of risperidone, oral bioavailability is 70%, plasma protein binding is approximately 90%.

Distribution: Volume of distribution is approximately 1 to 2 L/kg.

Metabolism: Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone (paliperidone), which has approximately the same receptor binding affinity as risperidone.

Elimination: Extensively metabolized in liver and excreted via urine.

Half-life: 3 hours in extensive metabolizers and 20 hours in poor metabolisers,

 Drug interaction

  • Carbamazepine and other enzyme inducers: may reduce plasma levels of risperidone
  • SSRIs: may increase plasma levels of risperidone
  • Anti-hypertensives

Precaution

  • Patients on anti-hypertensives
  • Elderly with dementia-related psychosis: increases risk of mortality
  • Alcohol and other centrally acting drugs
  • Patient taking Cimetidine and Ranitidine

References

  • Drugbank
  • Rxlist

Simtoin

Generic composition: Phenytoin sodium

General description

SIMTOIN is Phenytoin, an anti-seizure medication useful in treatment of tonic-clonic seizures, partial seizures, given intravenously or orally. The intravenous form is used for the improving the condition of status epilepticus not prevented through benzodiazepines.

Therapeutic category

  • Anti-epileptics

Dosage forms available

  • SIMTOIN 50mg Capsules
  • SIMTOIN 100mg Capsules

Uses

  • Tonic-clonic seizure
  • Partial seizure
  • Seizures during surgery
  • Status epilepticus: after BZD failed treatment
  • Glossopharyngeal Neuralgia
  • Trigeminal Neuralgia
  • Neuropathic Pain
  • Seizures during or after Neuro Surgery

Doses:

Adults and adolescents over 12 years of age (i.e. with over 50 kg bodyweight): take up to 3 tablets (corresponding to 300 mg phenytoin) single or divided in up to three doses. Dose is adjusted according to clinical requirements.

Children up to 12 years of age: 2 mg phenytoin/kg/day. The daily dose can be increased in 1 mg/day increments every 3 days according to phenytoin plasma concentration.

Maintenance dose: The maintenance dose is determined individually according to seizure control, undesirable effects and phenytoin plasma concentration.

 Contraindications:

  • Patients with a history of hypersensitivity to phenytoin or its inactive ingredients, or other hydantoins.
  • Co administration with delavirdine
  • Cardiovascular disorder like severe damage to the blood cells and bone marrow, arrhythmia, bradycardia and severe hypotension (systolic blood pressure less than 90 mm Hg)

Mechanism of Action

Phenytoin stabilizes neuronal membranes and decreases seizure activity by increasing efflux or decreasing influx of sodium ions across cell membranes in the motor cortex during generation of nerve impulses. Phenytoin reduces the maximal activity of brain stem centers responsible for the tonic phase of tonic-clonic (grand mal) seizures.

Pharmacokinetics

Absorption: nearly complete absorption, half-life is 22 hours, has moderately large volume of distribution, approximately 90% bound to plasma proteins, metabolized in liver and excreted via urine.

Distribution: volume of distribution of phenytoin is approximately 0.75 L/kg.

Metabolism: extensively metabolized in liver and is first transformed into a reactive arene oxide intermediate and arene oxide is metabolized to either a hydroxyphenytoin or phenytoin dihydrodiol metabolite

Elimination: excreted as inactive metabolites in the bile, estimated 1-5% of phenytoin is eliminated unchanged in the urine

Half-life: half-life of phenytoin ranges from 7 to 42 hours, and is 22 hours on average.

*Not indicated for absence seizure alone, might be used in combination with other anti-convulsant.

Side effects:

Common side effects include nausea, stomach pain, loss of appetite, poor coordination, increased hair growth, and enlargement of the gums. Potentially serious side effects include sleepiness, self harm, liver problems, bone marrow suppression, low blood pressure, and toxic epidermal necrolysis.

 Precautions:

  • Hepatic and renal impairment
  • Porphyria and diabetes
  • Pregnancy category D
  • Serious dermatological reactions may occur

 Interactions:

  • Cardiovascular drugs like digoxin, amiodarone, quinidine
  • Anti-epileptic drugs like carbamazepine, oxcarbazepine
  • Antifungal medications and anti-tubercular agents
  • PPIs and antacids
  • Alcohol
  • Oral hormonal contraceptives

Exopram

Generic composition: Escitalopram oxalate

General Description

Escitalopram is a selective serotonin re-uptake inhibitor (SSRI) and the S-enantiomer of racemic citalopram.

Therapeutic category

  • Selective serotonin reuptake inhibitors Antidepressant

Mechanism of action

It increases concentration of serotonin at neuronal synapse by inhibiting pre-synaptic SERT with minimal effects on NE (Nor-epinephrine) or DA (Dopamine) reuptake.

Pharmacokinetics

Absorption: Readily absorbed from GU tract, oral bioavailability is 80%, plasma protein binding is approximately 56%, peak plasma concentration in 5 hours.

Distribution: Volume of distribution is approximately 107 ± 42L

Metabolism: Metabolised in liver by hepatic Cytochrome. P450 (Isoenzymes CYP2C19 and CYP3A4) to active metabolite S-demthylescitalopram (major) and S-didemethylescitalopram (minor)

Elimination: Elimination mainly via liver and minorly from urine

Half-life: 27-32 hours, elimination half-life of escitalopram’s primary metabolite, S-desmethylcitalopram, is approximately 54 hours at steady state

Dosage forms available

  • EXOPRAM 5mg Tablets
  • EXOPRAM 10mg Tablets
  • EXOPRAM 20mg Tablets

Uses

  • Major depressive disorder
  • Generalized anxiety disorder
  • Panic disorder
  • Social anxiety disorder
  • Obsessive compulsive disorder

Dose

  • 10 mg once daily, increased after at least a week, maximum dose 20 mg daily for depression, Generalized anxiety disorder, social anxiety disorder, obsessive compulsive disorder.
  • Initial dose 5 mg, increased to 10 mg at least after a week, maximum dose 20 mg daily for panic disorder
  • *Dose reduction in hepatic impairment, renal impairment and in elderly

Side effect

Insomnia, ejaculation disorder (primarily ejaculatory delay), nausea, constipation, sweating increased, fatigue and somnolence

Contraindications

Contraindicated in bipolar depression due to risk of serotonin syndrome.

Drug interaction

  • MAOIs or other serotonergic medications.
  • Medications that have ability to prolong QT interval such as antimicrobials (Erythromycin, Clarithromycin, Fluconazole, Ketoconazole), antipsychotics, anti-arrhythmics (Dronedarone, Sotalol, Quinidine, Amiodarone, Flecainide) etc.
  • Weak inhibitor of CYP2D6 thus increases the plasma level of aripiprazole, risperidone, tramadol, codeine etc.
  • Caution when taken with cough medicine containing Dextromethorphan; may lead to serotonin syndrome, liver damage and other side effects.

Precaution

  • Hepatic and Renal impairement
  • High caution when taken with Saint John’s Wort; May lead to serotonin syndrome.

Pregnancy category: C

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