Olanzapine
When ATH:
N05AH03
Characteristic.
Atypical antipsychotic class tienobenzodiazepinov. The yellow crystalline material, practically insoluble in water.
Pharmacological action.
Antipsychotic, neuroleptic.
Application.
Schizophrenia and other. psychotic disorder with marked productive and negative symptoms, affective disorders (treatment exacerbations, maintenance and long-term preventive treatment), acute manic or mixed episodes in bipolar disorder with / without psychotic symptoms, with / without rapid cycling.
Contraindications.
Hypersensitivity, lactation.
Restrictions apply.
Renal and / or hepatic insufficiency, benign prostatic hypertrophy, convulsive status history, Parkinson's disease, cerebrovascular disorders, Alzheimer's disease, diabetes, eozinofilija, myeloproliferative disease, paralytic ileus, zakrыtougolynaya glaucoma, concomitant use of drugs, prolonging the QT interval (especially in the elderly), degidratatsiya, gipovolemiя, myocardial infarction, heart failure, mammary cancer, incl. history, pregnancy, Age to 18 years (Safety and efficacy have not been established).
Pregnancy and breast-feeding.
When pregnancy is with caution, comparing the expected benefit to the mother and the potential risk to the fetus. At the time of treatment should stop breastfeeding.
Side effects.
From the nervous system and sensory organs: dizziness, headache, migraine, weakness, asthenia, drowsiness, insomnia, anxiety, hostility, ažitaciâ, euphoria, amnesia, depersonalization, phobia, obsessive-compulsive symptoms, neuralgia, paresis of the facial nerve, gipesteziya, extrapyramidal disorders, incl. pozdnyaya dyskinesia, ataxia, stiff neck, vellication, tremor, akathisia, dysarthria, zaikanie, syncope, delirium, suicidal tendencies, stupor, coma, subarachnoid hemorrhage, stroke, nistagmo, diplopia, midriaz, pigment deposition in the lens, Cataract, xerophthalmia, bleeding in the eye, ccomodation, amblyopia, glaucoma, corneal, sore eyes, keratokonъyunktyvyt, .Aloe, noise and ear pain, deafness, dysgeusia.
Cardio-vascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, Rituals- and bradycardia, heartbeat, ventricular premature beats, ECG changes, cardiac arrest, cyanosis, vasodilation, transient leukopenia- and neutropenia, eozinofilija, leukocytosis, thrombocytopenia, hemorrhagic syndrome.
From the respiratory system: rhinitis, pharyngitis, laringit, voice alteration, increased cough, dyspnoea, apnea, bronchial asthma, hyperventilation.
From the digestive tract: increased appetite until bulimia, thirst, dry mouth, increased salivation, thrush, gingivitis, glossitis, dysphagia, belching, esophagitis, nausea, vomiting, gastritis, gastroenteritis, enteritis, ground, rectal bleeding, constipation, flatulence, scatacratia, transient increase in liver transaminases, gamma-glutamyl and creatine phosphokinase, hepatitis.
Metabolism: hyperprolactinemia, increase (rarely decrease) body weight, diabetes, giperglikemiâ, diabetic ketoacidosis, diabeticheskaya coma, goiter.
With the genitourinary system: dizurija (incl. polyuria), hematuria, pyuria, albuminuria, urinary incontinence, urinary tract infection, cystitis, decreased libido, impotence, abnormal ejaculation, priapism, gynecomastia, galactorrhea, breast pain, fibrosis matki, premenstrual syndrome, Menno- and metrorrhagia, amenorrhea.
On the part of the musculoskeletal system: arthritis, arthralgia, ʙursit, myasthenia, myopathy, leg cramps, bone pain.
For the skin: photosensitivity, alopecia, girsutizm, xerosis, eczema, seborrhea, contact dermatitis, ulcerative skin lesions, livor, makulopapulleznaya rash.
Allergic reactions: hives.
Other: fever, chills, flu-like symptoms, lymphadenopathy, pain in the chest or abdomen, peripheral edema, withdrawal, possible abuse.
Cooperation.
Activated carbon (1 g) reduces Cmax and AUC of 60%. A single dose of cimetidine (800 mg) aluminum or- and magnesium antacids does not affect the bioavailability of olanzapine. Carbamazepine (400 mg / day) increases in the clearance 50%. Preparations, inducing activity of CYP1A2 and glyukuroniltransferazy (omeprazole, rifampicin and the like.), increase the excretion of olanzapine; ингибиторы CYP1A2 (fluvoxamine et al.) reduce it. Fluoxetine (60 mg once or 60 mg daily for 8 days) increases Cmax of olanzapine 16% and reduces its clearance on 16%. In clinical trials show, that a single administration of olanzapine therapy with imipramine, desipramine, varfarinom, theophylline or diazepam was not accompanied by inhibition of metabolism of these drugs. There was no evidence of drug interactions when combined with lithium or biperidenom. Against the background of the equilibrium concentration of olanzapine did not change the pharmacokinetics of ethanol noted; while taking may increase the pharmacological effects of olanzapine, including sedation. When concomitantly with diazepam, ethanol and antihypertensive drugs increases the risk of orthostatic hypotension. It enhances the effect of anticholinergics. It weakens the effect of levodopa and other dopamine receptor agonists. The probability of elevated liver transaminases increases while admission to hepatotoxic agents. No clinically significant pharmacokinetic interaction between olanzapine and valproate is unlikely.
Overdose.
Symptoms: nausea, Aspiration, excitation, aggressiveness, drowsiness, confusion, speech, extrapyramidal disorder, respiratory insufficiency (depression of the respiratory center), arterial hyper- or hypotension, tachycardia, arrhythmia, cardiac arrest and respiratory, disturbance of consciousness, CNS depression (from sedation to coma), delirium, convulsions, neuroleptic malignant syndrome. Minimum dose for acute fatal overdose was 450 mg, the maximum dose of an overdose of a favorable outcome (survival) - 1500 mg.
Treatment: gastric lavage (artificially induce vomiting is not recommended), administration of activated charcoal, laxatives, ECG monitoring, maintaining vital functions, IVL. No specific antidote. Dialysis nyeeffyektivyen. If necessary, vasopressor therapy should be avoided dopamine, epinephrine and other sympathomimetic (strengthening of hypotension due to summation of the effects of beta-agonists and alpha-adrenoceptor blocking action of olanzapine).
Dosing and Administration.
Inside, regardless of the meal, 1 once a day. Schizophrenia: the initial dose of 5-10 mg/day. May increase dose to 4-5-day treatment up to 15-20 mg/day. Acute mania in bipolar disorder: the initial dose 15 mg / day, doses range is 5-20 mg. For patients with severe renal failure, with liver failure of moderate severity and the elderly initial dose of 5 mg / day.
Precautions.
With the combination of factors, slows metabolism of olanzapine (female patients, senile, non-smokers), It should be used in reduced dose. Careful monitoring of patients with suicidal tendencies, especially at the beginning of treatment. During treatment should regularly monitor the activity of liver transaminases, especially in patients with impaired liver function. Be wary designate drivers of vehicles and people, activities which require high concentration and speed of psychomotor reactions. During treatment excludes alcohol intake. When symptoms of neuroleptic malignant syndrome (fever, muscle tension, akinesia, tachycardia, leukocytosis, increase in creatine phosphokinase) require the immediate withdrawal of the drug. Given the potential for the development of akathisia, when a motor during treatment of anxiety, neusidčivosti, ongoing commitment to the movement to reduce the dose, and the appointment of antiparkinsonian.
