Clozapine Pharmacology

Clozapine

About Clozapine

Dibenzodiazepine derivative , Atypical antipsychotic, Tranquilizer, anti-psychotic.

Mechanism of Action of Clozapine

Clozapine binds to dopamine receptors. It has more affinity towards D4 receptor than other Dopamine receptors i.e.D1, D2, D3 &D5 receptors. It exerts its antipsychotic activity by blocking the dopamine projections in the limbic system. It acts as a competitive Dopamine antagonist. Clozapine also produces alpha adrenergic blocking activity, anti-serotonin activity and anticholinergic activity. It also produces moderately potent anticholinergic but paradoxically induce salivation and H1 blocking activity.

Pharmacokinets of Clozapine

Absorption: It is absorbed after oral administration and the bioavailability is about 60 - 70 % due to first pass metabolism. Distribution: It is distributed in the body in protein bound form. Metabolism: It is metabolised in the liver and produce both active and inactive metabolites. Excretion: It is excreted mainly through urine and also through faeces.

Onset of Action for Clozapine

15 minutes.

Duration of Action for Clozapine

4 - 12 hours

Half Life of Clozapine

14 hours

Side Effects of Clozapine

1.Agranulocytosis
2.Leukopenia
3.Seizure
4.Tachycardia
5.Hypotension
6.Nausea
7.Vomiting
8.Constipation
9.Dry mouth
10.Drowsiness
11.Sedation
12.Dizziness
13.Excessive salivation
14.Tremor
15.Weight gain
16.Muscle spasm

Contra-indications of Clozapine

1.Agranulocytosis with prior Clozapine treatment
2.Comatose
3.Bone marrow depression
4.Depression
5.Uncontroled epilepsy

Special Precautions while taking Clozapine

1.Renal impairment
2.Hepatic impairment
3.Cardiovascular disease
4.Angle closure glaucoma
5.Prostatic hyperplasia
6.Slowly withdraw the drug with caution

Pregnancy Related Information

Use with caution.

Old Age Related Information

Use with caution.

Breast Feeding Related Information

Contraindicated

Children Related Information

Contraindicated
NEONATES: Contraindicated

Indications for Clozapine

1.Schizophrenia

Interactions for Clozapine

Anticholinergics: Anticholinergic effects may be potentiated.
Antihypertensives: Hypotensive effects may be potentiated.
CNS drugs: Caution is advised with concomitant use.
Agents that suppress bone marrow function: Avoid concomitant use.

Typical Dosage for Clozapine

Dose is based on clinical response, patient tolerance, monitoring of blood count and adverse reactions
Adult:
Initial dose: 12.5 mg once or twice daily dose can be gradually increased to 300 mg / day after 2 weeks.
Effective dose range: 300 - 450 mg / day
Maximum dose: 900 mg / day

Schedule of Clozapine

Storage Requirements for Clozapine

The drug should be kept at 15-30 degree C in a tightly closed container. Protect from heat and light. Keep out of the reach of children.

Effects of Missed Dosage of Clozapine

Take the missed dose as soon as noticed. If it is the time to take the next dose then take that dose and skip the missed dose. Continue the regular schedule. Do not double the dose.

Effects of Overdose of Clozapine

Give supportive measures and treatment. Gastric lavage can be done to remove the drug from the body. Activated charcoal can be given to reduce the absorption of the drug.

Home Delivery for Clozapine in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including clozapine.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for clozapine and other medicines and health products. Home delivery services for clozapine may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take clozapine only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for clozapine before they complete the sale. You can get this information while placing the order for clozapine with the pharmacy.

Clozapine is a generic medicine name and there are several brands available for it. Some of the brands for clozapine might be better known than clozapine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have clozapine in stock, you can ask for one of the branded alternatives for clozapine.