proviron – tricyclic antidepressant group of non-selective inhibitors of neuronal uptake of monoamines. It possesses strong timoanalepticheskim and sedative effect.
The mechanism of antidepressant action of proviron is associated with inhibition of reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin in the central nervous system.
proviron is an antagonist of muscarinic cholinergic receptors in the CNS and in the periphery, has a peripheral antihistamine (the HI) and antiadrenergicheskim properties. Also of antinevralgicheskoe (central analgesic), anti-ulcer and antibulimicheskoe action effective for bed-wetting.
The antidepressant effect develops within 2-4 weeks. after the start of application.
Bioavailability of proviron for various routes of administration – 30-60%, its active metabolite nortriptyline – 46-70%. Volume of distribution of 5-10 L / kg.
Effective therapeutic blood concentration of proviron – 50-250 ng / ml, nortriptyline (its active metabolite) of 50-150 ng / ml. The maximum plasma concentration (C max ) – 0.04- 0.16 g / ml. Passes through the blood-tissue barriers, including the blood-brain barrier (including nortriptyline).
The concentration of proviron in tissues than in plasma. Communication with plasma proteins 92 -. 96%
is metabolized in the liver (by demethylation, hydroxylation) to form active metabolites – nortriptyline, 10-hydroxy-proviron, and active metabolites.
The half-life from the blood plasma by 10 to 28 hours for proviron and 16 up to 80 hours for nortriptyline. Excreted by the kidneys – 80%, partly with bile. Complete elimination within 7-14 days.
proviron crosses the placental barrier, excreted in breast milk in concentrations similar to plasma.
Indications for use:
- Depression severe. Due to the severity of sedation is particularly effective for anxiety – depressive states.
- Heart failure decompensation.
- Acute and recovery phase of myocardial infarction.
- conduction disorders of the heart muscle.
- Severe hypertension.
- Acute liver and kidney disease with severe dysfunction.
- Peptic ulcer and 12 duodenal ulcer in the acute stage.
- Hypertrophy of the prostate.
- Atony of the bladder.
- Pyloric stenosis, paralytic ileus.
- Simultaneous treatment of MAO inhibitors (See Interactions.).
- Pregnancy, lactation.
- Children under 6 years of age.
- Hypersensitivity to proviron.
proviron should be used with caution in patients suffering from alcoholism, bronchial asthma, manic-depressive psychosis (MDP) and epilepsy (see. Special instructions), with inhibition of bone marrow hematopoiesis, hyperthyroidism, angina and heart failure, angle-closure glaucoma, ocular hypertension, schizophrenia (although his admission usually occurs acute positive symptoms).
Dosing and Administration
Assign intramuscularly or intravenously.
In severe depression resistant to treatment: intramuscularly or intravenously (injected slowly!) Is administered at a dose of 10-20-30 mg up to 4 times a day, an increase in dose should be gradual, the maximum daily dose of 150 mg; 1-2 weeks later, go to the reception of the drug inside.
Children older than 12 years of age and the elderly are administered lower doses and increase them slowly.
If the patient’s condition does not improve within 3-4 weeks of treatment, further treatment is not practical.
Mainly related to the anticholinergic effect of the drug: paresis of accommodation, blurred vision, increased intraocular pressure, dry mouth, constipation, ileus, urinary retention, increase in body temperature.These effects usually disappear after adaptation to the drug or dose reduction.
CNS: headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, confusion, tremor, paresthesia, peripheral neuropathy, changes in the EEG. Rarely – extrapyramidal disorders, convulsions, anxiety.
Cardio-vascular system: tachycardia, arrhythmias, conduction disturbances, labile blood pressure, expansion of the QRS complex on the ECG (violation of intraventricular conduction), symptoms of heart failure, syncope.
On the part of the digestive tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disturbances, dark tongue, epigastric discomfort, gastralgia, increased activity of “liver” transaminases, rarely cholestatic jaundice, diarrhea.
From endocrine system: an increase in the size of the mammary glands in men and women, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), changes in libido, potency. Rarely – hypo- or hyperglycemia, glycosuria, glucose intolerance, swelling of the testicles.
Allergic reactions: skin rash, pruritus, photosensitivity, angioedema, urticaria.
Other: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other changes in the blood, hair loss, swollen lymph nodes, weight gain during prolonged use, sweating, pollakiuria.
With prolonged treatment, especially in high doses, the sudden cessation of treatment may develop withdrawal symptoms: headache, nausea, vomiting, diarrhea, and irritability, sleep disturbance with bright, unusual dreams, irritability.
Drowsiness, disorientation, confusion, depression of consciousness up to coma, dilated pupils, fever, dizziness, dysarthria, agitation, hallucinations, seizures, muscle stiffness, vomiting, arrhythmia, hypotension, heart failure, respiratory depression.
Assistance measures: termination of proviron therapy, infusion fluid, symptomatic therapy, blood pressure and maintaining water and electrolyte balance. Results monitoring cardiovascular activity (ECG) for 5 days, as relapse may occur after 48 hours and later. Hemodialysis and forced diuresis are not effective.
Interaction with other drugs
proviron dampening effect on the central nervous system following medicines: antipsychotics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; exhibits synergism when interacting with other antidepressants.
In a joint application of proviron with neuroleptics, and / or anticholinergic drugs can cause febrile temperature reaction, paralytic ileus.
proviron potentiates the hypertensive effects of catecholamines and other agonists that increases the risk of cardiac arrhythmias, tachycardia, severe hypertension, but it inhibits the effects of drugs that affect noradrenaline release.
proviron may reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect of anticonvulsants.
with the simultaneous use of proviron and anticoagulants – coumarin derivatives may increase the anticoagulant activity of the past.
at the same time reception proviron and cimetidine may increase the plasma concentration of proviron with the possible development of toxic effects.
Inductors of microsomal liver enzymes (barbiturates, carbamazepine) decrease plasma concentrations of proviron.
proviron increases the effects of anti-drugs and other drugs that cause extrapyramidal reactions.
quinidine slows the metabolism of proviron.
Joint the use of proviron with disulfiram and other inhibitors of acetaldehyde dehydrogenase can cause delirium.
estrogensoderjath oral contraceptives may increase the bioavailability of proviron; pimozide probucol and can enhance cardiac arrhythmias.
proviron may enhance the depression caused by corticosteroids; concomitant use with medicinal products for the treatment of hyperthyroidism increases the risk of agranulocytosis. Simultaneous treatment with MAO inhibitors proviron can be fatal. Break in treatment between the intake of MAO inhibitors and tricyclic antidepressants should not be less than 14 days!
proviron in doses above 150 mg / day reduces the threshold for seizure activity, therefore it is necessary to take into account the possibility of seizures in patients with such a history and a category of patients who are predisposed to it due to age or injury. proviron in treatment of the elderly should take place under strict control, with minimal doses and gradually increase them, in order to avoid the development of delirium disorders, hypomania, and other complications. Patients with depressive phase TIR may become manic phase.
During the reception, proviron prohibited from driving vehicles, machinery maintenance and other work requiring high concentration, as well as the reception of alcohol.
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