Quetiapine is a selective decrease in the activity of mesolimbic A10 dopaminergic neurones versus the primobolan depot side effects nigrostriatal neurones involved in motor function. There is no long-term increase prolactin concentration in blood plasma. In clinical studies have shown efficacy against both positive and negative symptoms of schizophrenia. When quetiapine orally is well absorbed from the gastrointestinal tract and is extensively metabolised by the liver. The major metabolites found in the plasma does not possess a pronounced pharmacological activity.
Food intake did not significantly affect the bioavailability of quetiapine. The half-life of about 7 hours. Approximately of quetiapine binds to plasma proteins. The pharmacokinetics of quetiapine linear, differences in pharmacokinetic parameters in men and women is not observed.
The average clearance of quetiapine in elderly patients is less than in patients .
- Manic episodes of moderate to severe in the structure of bipolar disorder.It does not prevent the development of manic and depressive episodes.
- Hypersensitivity to any component of the drug,
- The simultaneous use of inhibitors of cytochrome P450 ZA4 (e.g., HIV protease inhibitors, azole antifungals structure, erythromycin, clarithromycin, nefazodone)
- Children’s age (efficacy and safety have not been established),
- Pregnancy and lactation (effectiveness and safety have been established).Precautions: hypotension, heart failure, cardiac hypertrophy, cardiovascular and cerebrovascular disease, or other conditions predisposing to hypotension, advanced age, liver failure, epilepsy, seizures in history, co-administration of drugs prolonging QT-interval, patients with congenital increase in QT-interval or family history of its increase, hypocalcemia, hypomagnesemia, risk factors for thromboembolism, venous vessels.Dosage and administration
. Inside, 2 times a day, regardless of meals Treatment of schizophrenia The daily dose for the first 4 days of therapy primobolan depot side effects is as follows: Day 1 – 50 mg, 2 nd day – 100 mg, day 3 – 200 mg, day 4 – 300 mg. since the 4th day, the dose is adjusted individually to achieve an effective dosage is typically 300 – 450 mg / day. Depending on the clinical effect, and individual patient tolerance dose can vary from 150 to 750 mg / day. The maximum recommended daily dose is 750 mg. The treatment of manic disorders daily dose for the first 4 days of treatment is as follows: Day 1 – 100 mg, 2 day – 200 mg, 3 day – 300 mg, day 4 – 400 mg. Subsequently, by the 6th day of treatment the daily dose can be increased to 800 mg. The increase in the daily dose should not be more than 200 mg per day. Depending on the clinical effect and individual tolerability, the dose can vary from 200 to 800 mg / day. Typically, the effective dose is from 400 to 800 mg / day. The maximum recommended daily dose is 800 mg / day. Elderly patients in elderly patients the initial dose is 25 mg / day. Daily dose should be increased by 25 – 50 mg to achieve an effective dose which is usually smaller than in younger patients. Renal and / or hepatic impairment is recommended to start treatment with a dose of 25 mg / day. followed by the daily increase of 25 – 50 mg to achieve an effective dose.
very often – more than 10/100, often – more than 1/100 and less than 1/10, rarely – more than 1/1000 and less than 1/100, rarely – more than 1/10000 and less than 1/1000, very rare – less . 1/10000 On the part of the central nervous system: very often – dizziness, drowsiness, headache; often – syncope; rarely – seizures; rarely – tardive dyskinesia; with unknown frequency are found anxiety, hostility primobolan depot side effects, agitation, insomnia, akathisia, tremor, depression, paresthesia, Cardio-vascular system: often – tachycardia, orthostatic hypotension; cases of thromboembolic venous vessels, including pulmonary embolism and deep venous vessels. The respiratory system: pharyngitis, rhinitis, part of the digestive system: often – dry mouth, constipation, dyspepsia; -zheltuha rarely, nausea, vomiting, abdominal pain; very rarely – hepatitis, the part of the blood and lymphatic system: often – leukopenia; -eozinofiliya infrequently; very rarely – neutropenia, Laboratory tests: often – increased activity of serum transaminases (ALT, ACT);rarely – increased activity of gamma-glutamate transaminase; increase in total cholesterol concentration in serum triglycerides; part of the endocrine system: very rarely – hyperglycemia, diabetes Allergic reactions: seldom – hypersensitivity; angioedema, Stevens-Johnson syndrome, a skin rash, the part of the reproductive organs: rarely – priapism; Other: often – moderate fatigue, edema, weight gain, rarely – neuroleptic malignant syndrome, back pain, chest pain, low-grade fever, myalgia, dry skin, impaired vision. during treatment with quetiapine, a slight dose-dependent decrease in thyroid hormone levels, particularly total and free T 4 . The maximum decrease in total and free T 4 were registered during the first 2-4 weeks of therapy with quetiapine, with no further reduction in hormone levels during long-term treatment. There was no evidence of clinically significant changes in the concentration of thyroid stimulating hormone. In almost all cases, the level of total and free T 4 returned to baseline after discontinuation of therapy quetiapine, regardless of the duration of treatment, quetiapine, like other primobolan depot side effects antipsychotics may cause lengthening of the interval QT, but the clinical trials showed no correlation between the reception quetiapine and constant . QT prolongation In the abrupt cancellation of the drug withdrawal syndrome cases have been reported, accompanied by nausea, vomiting; rarely – insomnia.
Overdosing Symptoms: drowsiness and excessive sedation, tachycardia and lowering blood pressure. Treatment: No specific antidote. In cases of severe intoxication – symptomatic treatment (maintenance of respiratory function, cardiovascular system, ensuring adequate oxygenation and ventilation). A careful medical monitoring and observation of the patient is needed to complete recovery.
Interactions with other drugs lekrstvennymi
Cytochrome P450 CYP3A4 is the primobolan depot side effects key enzyme involved in the metabolism of quetiapine. With simultaneous administration of these drugs possessing a strong inhibitory effect on cytochrome P450 CYP3A4 (azole antifungals group and macrolide antibiotics) in the plasma concentration of quetiapine may significantly increase. Thus, while appointing quetiapine and ketoconazole shown to increase the area under the curve (AUC) of quetiapine in 5.8 times. For this reason, the combination of these drugs are contraindicated. Also during treatment Lakvelem not recommended to consume grapefruit juice.
When concomitant administration Lakvelya with drugs that induce liver enzyme system, such as carbamazepine or phenytoin, quetiapine plasma concentration decreases. You should carefully weigh the risks and benefits of co-administration Lakvelya and hepatic enzyme inducers (apart from those mentioned above, barbiturates, rifampicin). You may need to increase the dose Lakvelya, which is carried out progressively; should also consider replacing Lakvelya the drug without inducing microsomal liver enzymes (eg, valproic acid).
The pharmacokinetics of lithium drugs does not change, while the appointment Lakvelya. Simultaneous treatment with antipsychotics risperidone or haloperidol had no significant effect on the pharmacokinetics of quetiapine. However, simultaneous thioridazine leads to increased clearance of quetiapine at about 70%. The pharmacokinetics of quetiapine are not significantly altered, while the application of cimetidine, an inhibitor of P450, and in conjunction with the appointment imipramine or fluoxetine. When concomitant administration of valproic acid and Lakvelya preparations of pharmacokinetic parameters did not change significantly. Drugs that suppress the central nervous system, as well as ethanol increases the risk of side effects.
Caution must be exercised in the appointment of Lakvelya in combination with drugs that prolong the interval QT (neuroleptics, antiarrhythmics, halofantrine, mesoridazine, thioridazine, pimozide, sparfloxacin, gatifloxacin, moxifloxacin, dolasetron mesylate, mefloquine, sertindole, cisapride), as well as drugs that cause electrolyte imbalance (thiazide diuretics).
in the initial period of titration of orthostatic hypotension may occur. In this case, you should go back to the previously received a dose. Particular attention should be given to patients with cardiovascular diseases, cerebrovascular diseases and other conditions predisposing to hypotension.
Antipsychotic drugs (neuroleptics), including quetiapine, contribute to the development of thromboembolic complications in patients with a predisposition to the formation of blood clots. Before initiation of therapy with quetiapine need to identify all possible risk factors for thromboembolism and venous vessels to take appropriate measures for the prevention of thromboembolic complications.
There was no relationship between drug intake in the recommended mode and increased QT-interval. However, an increase in QT-interval in overdose noted. Caution should be exercised in the appointment of quetiapine in conjunction with drugs that prolong the interval of the QT the C , especially in the elderly, in patients primobolan depot side effects with congenital QT-syndrome, heart failure, cardiac hypertrophy, hypocalcaemia or hypomagnesemia, and in the presence of family history to increase QT- interval.
It should be used with caution in combination with other drugs having inhibitory effect on the central nervous system, as well as alcohol. Care should be taken when treating patients with a history of seizures.In the treatment of quetiapine may develop neuroleptic malignant syndrome, the clinical manifestations of which include hyperthermia, altered mental status, muscular rigidity, instability of the autonomic nervous system, increased creatine phosphokinase levels. In such cases, a removal of the drug and appropriate therapy.
It should also consider the possibility of tardive dyskinesia with prolonged use of quetiapine. In this case, you should reduce the dose or consider its abolition. With a sharp lifting treatment with high doses following acute reactions (withdrawal syndrome) can occur – nausea, vomiting, insomnia rarely. It is also possible exacerbation of psychotic symptoms of the disease and the emergence of involuntary movement disorders (akathisia, dystonia, dyskinesia). In this connection, the abolition of the drug is recommended to be made gradually.
Lakvel not intended for the treatment of patients suffering from psychosis, accompanying senile dementia. There is evidence of increased risk of cerebrovascular events in patients primobolan depot side effects with senile dementia during treatment with atypical antipsychotics. Care should be taken when appointing Lakvelya patients with risk factors for stroke. Lakvel The drug contains lactose, so it is not indicated in patients with lactase deficiency or malabsorption of glucose and galactose.
Effects on ability to drive and other mechanisms
The drug can cause drowsiness, so the period of treatment is not recommended for patients: management of vehicles, work with mechanisms, which constitute a danger.