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.