Clozaril (Clozapine)

Clozaril Review

This medication is used to treat symptoms of a certain type of mental condition (schizophrenia) that is untreatable by other medications

Buy Clozaril in a reliable International Online Pharmacy
Free World Wide Shipping

Clozaril Drug Class and Mechanism

The absorption of clozapine is almost complete, but the oral bioavailability is only 60 to 70% due to first-pass metabolism. The time to peak concentration after oral dosing is about 2.5 hours, and food does not appear to affect the bioavailability of clozapine. The elimination half-life of clozapine is about 14 hours at steady state conditions (varying with daily dose). Clozapine is extensively metabolized in the liver, via the cytochrome P450 system, to polar metabolites suitable for elimination in the urine and faeces. The major metabolite, norclozapine (desmethyl-clozapine), is pharmacologically active. The cytochrome P450 isoenzyme 1A2 is primarily responsible for clozapine metabolism, but 2C, 2D6, 2E1 and 3A3/4 appear to play roles as well. Agents which induce (e.g. cigarette smoke) or inhibit (e.g. theophylline, ciprofloxacin, fluvoxamine) CYP1A2 may increase or decrease, respectively, the metabolism of clozapine.

Clozaril Uses

Clozapine has been shown to be superior in efficacy in treating schizophrenia. Were it not for its side effects it would be first line treatment; however the rare but potentially lethal side effects of agranulocytosis and myocarditis relegate it to third-line use. Furthermore it may rarely lower seizure threshold, cause leukopenia, cause hepatic dysfunction, weight gain and be associated with type II diabetes. More common side effects are predominantly anticholinergic in nature, with dry mouth, sedation and constipation. It is also a strong antagonist at different subtypes of adrenergic, cholinergic, histaminergic and serotonergic receptors. Due to risk of serious side effects, clozapine treatment is commenced at a very low dose (25 mg daily) and increased slowly until a therapeutic dose (300–600 mg daily) is reached.[14] In severely ill and/or younger patients up to 900 mg may be needed. In the elderly, much lower doses may be sufficient (25 to 100 mg). Once the patient is stabilized and the maintenance dose has been determined, the greater part or all of the daily dose may be given at bedtime. This will ameliorate daytime sedation and orthostatic problems; most people benefit from the sedation to get to sleep anyway. Furthermore, compliance on medication taken more frequently than once daily drops off dramatically.

Buy Clozaril in a Reliable International Online Pharmacy
Free International Shipping

Clozaril Side Effects

Clozapine may cause a severe reduction in white blood cell count, a condition known as agranulocytosis, in approximately 1 in 100 patients who take it for at least one year. White blood cells fight infections, and a severe reduction in white blood cells can result in severe infections. If not caught early, agranulocytosis can be fatal. Therefore, the white blood cell count should be measured (with a blood test) prior to starting treatment and regularly (weekly) while patients receive this medication, and for 4 weeks after it is stopped.

Clozaril Pregnancy

Clozaril Overdose

Symptoms of overdose may include nausea, disorientation, unsteadiness, decreased sexual ability, prolonged or painful erection in males, seizures, and loss of consciousness.

Clozaril More Information

Patients should be informed of the significant risk of seizure during CLOZARIL treatment, and they should be advised to avoid driving and any other potentially hazardous activity while taking CLOZARIL.