Quetiapro

Quetiapro 100 is a cream yellow to light yellow to yellow film coated tablet, round, biconvex, plain on both sides.
Quetiapro 200 is a white to off-white film coated tablet, round, biconvex and plain on both sides.
Each film-coated tablet contains: Quetiapine (as fumarate) 25 mg, 100 mg or 200 mg.

Pharmacology: Pharmacodynamics: Quetiapine fumarate is a dibenzothiazepine atypical antipsychotic. It is reported to have affinity for serotonin (5-HT2), dopamine (D2), histamine (H1), and adrenergic (α1 and α2) receptors.
Quetiapine's efficacy on schizophrenia and bipolar disorder is mediated through a combination of dopamine (D2) and serotonin (5-HT2) antagonist.
Pharmacokinetics: Quetiapine is well absorbed following oral administration and widely distributed throughout the body. It is about 83% bound to plasma proteins. Quetiapine is extensively metabolized in the liver by sulfoxidation mediated mainly by the cytochrome P450 isoenzyme CYP3A4 and by oxidation. It is excreted mainly as inactive metabolites, about 73% of a dose appearing in the urine and about 20% in the feces. The elimination half-life has been reported to be about 6 to 7 hours.

Quetiapine is used for the treatment of schizophrenia and of mania associated with bipolar disorder.

The usual initial dose of quetiapine is 25 mg twice a day (every 12 hours) on day one, 50 mg twice daily (every 12 hours) on day two, 100 mg twice daily (every 12 hours) on day three and 150 mg twice daily (every 12 hours) on day four. The dosage is then adjusted to a usual range of 300 mg to 450 mg daily given in 2 divided doses (every 12 hours), or as prescribed by the physician.

In clinical trials, survival has been reported in acute overdoses of up to 30 grams of quetiapine. Most patients who overdosed experience no adverse reactions or recovered fully from the reported reactions. Death has been reported in a clinical trial following an overdose of 13.6 grams of quetiapine alone.
In general, reported signs and symptoms were those resulting from an exaggeration of the drug's known pharmacological effects (i.e., drowsiness and sedation, tachycardia and hypotension). Patients who have pre-existing severe cardiovascular disease may beat an increased risk of the effects of overdose.
Management of overdose: There is no specific antidote to quetiapine. Therefore, appropriate supportive measures should be instituted. In cases of severe signs, the possibility of multiple drug involvement should be considered. In cases where hypotension and circulatory collapse occurs, it should be treated with appropriate measures such as intravenous fluids and/or sympathomimetic agents (epinephrine and dopamine should not be used). In cases of severe extrapyramidal symptoms, anticholinergic medication should be administered. Close medical supervision and monitoring should continue until patient recovers.

Hypersensitivity to the active substance or to any excipient of this product.

Contraindicated in patients with pre-existing CNS depression or coma, bone marrow suppression, pheochromocytoma or prolactin-dependent tumor. It should be used with caution or not at all in patients with impaired liver, kidney, cardiovascular, cerebrovascular and respiratory function and in those with angle-closure glaucoma, history of jaundice, parkinsonism, diabetes mellitus, hypothyroidism, myasthenia gravis, paralytic ileus, prostatic hyperplasia or urinary retention. Care is required in patients with epilepsy or history of seizure.

Pregnancy: Pregnancy Category C.
There are no adequate and well-controlled studies of Quetiapro use in pregnant women. Quetiapine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Quetiapine is excreted into human milk. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother's health.

The most common adverse drug reaction with quetiapine has been somnolence. It has been associated with a low incidence of extrapyramidal symptoms. Other adverse drug reactions have included mild asthenia, anxiety, dizziness, myalgia, rhinitis, dyspepsia, rises in plasma-triglyceride and cholesterol concentrations, and reduced plasma-thyroid hormone concentrations. There have been rare reports of priapism or peripheral edema.

The central effects of other CNS depressants, including alcohol, may be enhanced by quetiapine. Quetiapine should be used with caution in patients also receiving antihypertensives or drugs that prolong the QT interval. Quetiapine may antagonize the actions of dopaminergics such as levodopa.
CYP3A4 is the main isoenzyme responsible for cytochrome P450-mediated metabolism of quetiapine and caution is advised when quetiapine is used with potent inhibitors of CYP3A4 such as erythromycin, fluconazole, itraconazole, and ketoconazole; lower doses of quetiapine should be used when given with such drugs. Conversely, enzyme inducers such as carbamazepine and phenytoin may decrease the plasma concentrations of quetiapine, and higher doses of quetiapine may be necessary. Thioridazine has also been reported to increase the clearance of quetiapine.

Store at temperatures not exceeding 30°C.

Antipsychotics

N05AH04 - quetiapine ; Belongs to the class of diazepines, oxazepines and thiazepines antipsychotics.

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