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Melipramin (Imipraminum, Imipramine) - tricyclic antidepressants, derivative dibenzoazepina. Blocks reverse neuronal uptake of monoamines in the brain; reduces motor retardation, improves mood, helps normalize sleep, has a stimulating effect unexpressed. At the beginning of treatment may predominance of sedation, which is less pronounced than that of amitriptyline.
Has m-anticholinergic, antispasmodic myotropic, antihistamine effect. It does not inhibit MAO.
The antidepressant effect develops gradually; optimal therapeutic effect after 1-3 (up to 4) weeks after initiation of therapy.
Depression and depressive states of different etiology, accompanied by motor and ideatornoy retardation: astenodepressivnyh syndrome, depression (endogenous, involutional, climacteric, reactive, alcohol), depression while psychopathy and neurosis, nocturnal enuresis in children, behavioral disorders (activity and attention), panic disorders, chronic pain syndrome (chronic cancer pain, migraine, rheumatic diseases, atypical facial pain, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other. peripheral neuropathy), narcolepsy, accompanied by catalepsy, bulimia nervosa, syndrome `cocaine otmeny` , urinary incontinence (stress and when the urge to urinate), headache, migraine (prevention).
Hypersensitivity, use together with MAO inhibitors and 2 weeks before starting treatment, myocardial infarction (acute and subacute periods); acute intoxication with ethanol, hypnotics, narcotic analgesics, and other drugs, oppressive central nervous system.; angle-closure glaucoma, severe violations of intracardiac conduction (bundle branch block blockade, AV block II st.), lactation, children's age (up to 6 years).
In the appointment of imipramine in patients with epilepsy should be closely monitored state because the drug can provoke in the first days of the treatment of epileptic seizures.
In applying the drug should be noted that the therapeutic effect is not earlier than after 1-3 weeks of treatment, the maintenance dose should be taken at least 3 months. In the initial period of therapy, imipramine need constant medical supervision of patients with suicidal tendencies.
With the sudden cessation of the drug develop withdrawal symptoms (nausea, headache, irritability, insomnia, arrhythmia and extrapyramidal disorders).
Do not use electroconvulsive therapy during use imipramine.
In the case of bipolar depression preparation may provoke a transition of the patient in the manic phase.
In the early days of tricyclic antidepressants in the treatment of panic disorder may paradoxically increased psychomotor restlessness. If this condition is not to be held for 2 weeks, it is advisable the appointment of drugs - benzodiazepines.
Be wary appoint Melipramin patients with a tendency to constipation.
Melipramin should be cautious appoint pheochromocytoma or acute porphyria because of the threat of worsening disease with the development of a crisis.
With care should be prescribed to elderly patients and children, because in these groups of patients may develop serious side effects.
During treatment imipramine recommended systematic blood count, liver function evaluation, monitoring ECG and blood pressure.
The treatment of imipramine can not drink alcoholic beverages.
Effects on ability to drive vehicles and management mechanisms
During the period of imipramine prohibited driving vehicles and perform other potentially dangerous work that requires high concentration and speed of psychomotor reactions.
Inside, during or immediately after a meal (to reduce irritation of the gastric mucosa), individual selection of doses for adults the initial dose - 25-50 mg 3-4 times a day, then increase the daily dose to 25 mg, and bring it to 200-250 mg / day, sometimes - up to 300 mg / day; the duration of treatment in mild forms of depression - 4-6 weeks. Thereafter gradually reduce the dose (25 mg every 2-3 days) and pass to a maintenance therapy dose of 25 mg 1-4 times a day for a further 4-6 weeks. In the elderly the initial dose - 10 mg / day, with a gradual increase to 30-50 mg or more, to obtain the optimum effect. recommended intake after a meal to reduce the irritant effect on the gastric mucosa. For maintenance therapy is often used single dose at night, receiving a fractional reserve in the elderly, adolescents and patients with CVD. Higher doses for adults inside: single - 100 mg daily - 200 mg (patient), 300 mg (in the hospital) and 100 mg of elderly patients. Children, as an antidepressant, the initial dose - 10 mg; for 10 days gradually increase the dose: for children age 6-8 years - 20 mg, 8-14 - 20-25 mg over 14 - 50 mg or more (up to 100 mg), 2 divided doses. If bedwetting at the beginning of treatment a daily dose: For children aged 6-8 years - 25 mg, 9-12 years - 25-50 mg, over 12 years - 50-75 mg, 1 times a day for 1 hour before sleep . If incontinence is manifested in the early hours of the night, the daily dose can be administered in 2 divided doses, one half of the dose received in the middle of the day, and the other - before going to bed. If no effect after 1 week of treatment prescribed higher doses. The daily dose higher than 75 mg are generally not improve results. The highest daily dose for children - 2.5 mg / kg. In severe forms of depression in the hospital can be used combined therapy - in / m and orally. As an antidepressant - 100 mg / day in divided doses. Higher doses for adults: single - 50 mg daily - 300 mg. Children are not recommended for up to 12 years. Too early discontinuation of treatment may lead to a resumption of depression. Cancelling imipramine should be gradual.
From the central and peripheral nervous system: headache, dizziness, excessive sedation, paraesthesia, tremor, seizures, dysarthria, coordination disorders, sleep disorders, hallucinations, agitation, disturbance of accommodation.
From the digestive system: dry mouth, stomatitis, nausea, vomiting, constipation, intestinal obstruction; rarely - hepatitis.
Cardio-vascular system: tachycardia, arrhythmia, orthostatic hypotension.
From the urinary system: urinary retention.
From hemopoiesis system: a leukocytosis, eosinophilia; rarely - leukopenia, thrombocytopenia, agranulocytosis.
From the Endocrine: gynecomastia, galactorrhea, decreased libido, changes in blood glucose levels.
Allergic reactions: urticaria, rash, angioedema.
Concomitant use of imipramine and MAO inhibitors significantly increases the risk of excitation, seizures, blood pressure fluctuations, hyperthermia, coma. After discontinuation of MAO inhibitors is necessary to make a break for 2-3 weeks before the appointment of imipramine (and vice versa).
With simultaneous use of imipramine and m-holinoblokatorov occurs summation of the anticholinergic effect of drugs.
With simultaneous use of imipramine and thyroid hormones is amplified adrenergic effects, which can cause tachyarrhythmias and development of angina attacks.
If concomitant use of imipramine with agonists (epinephrine, norepinephrine, phenylephrine) increases the risk of tachycardia, arrhythmia and hypertension due to inhibition of inactivation of catecholamines imipramine.
With simultaneous use of imipramine with alpha-blockers and stimulants of the central alpha-adrenergic receptors (clonidine, guanethidine, methyldopa), the antihypertensive effect of the latter is reduced, which may be due to inhibition of their binding to presynaptic alpha-adrenergic receptors.
Imipramine reduces the anticonvulsant effect of phenytoin.
Means, depressing the central nervous system, and increases the sedative effect of ethanol imipramine, and benzodiazepines and phenothiazines, sedative and anticholinergic effects of imipramine.
Enzyme inhibitors of microsomal oxidation (cimetidine, methylphenidate, oral contraceptives) slow down the metabolism of imipramine and increase the period of its half-life, and therefore increase the antidepressant efficacy and toxicity of the drug.
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