IMIPRAMINE (Imizinum; synonym: Imipraminum, Melipramin, Tofranil, Deprenil; GFH, joint venture. B) — antidepressant. N-(3-Dimetilaminoironit) - iminodibenzyl a hydrochloride, C 19 H 2 4 N 2 - HCl:
White crystal powder, we will easily dissolve in water and alcohol; pH of water solutions — 3,7 — 4,5.
And. treats group of tricyclic antidepressants. Drug stops or reduces the oppressing effects of Reserpinum, strengthens effects of sympathomimetic substances, has holinoblokiruyushchy effect. Activity of monoamine oxidase does not reduce. Has timoanaleptichesky effect (weakens melancholy, improves mood), reduces motive block, raises a mental and general tone. It is quickly soaked up in blood. The highest concentration of drug are found in a liver, kidneys and lungs. And. and its metabolites communicate blood proteins. Pharmacological an untied part of drug is active. Steady level in blood after administration of drug inside is established approximately in a week after an initiation of treatment. Concentration And. in blood it is quite constant, does not depend on age and the body weight of patients. Drug is emitted with urine of hl. obr. in the form of metabolites, many of which pharmacological are active; 0,5 — 5% of drug are allocated in not changed look.
Mechanism of action And., as well as other tricyclic antidepressants, connect with strengthening of processes serotonin - and adrenergic transfer of nervous impulses in c. N of page generally due to braking of the return transport of noradrenaline and serotonin from a synaptic gap in presynaptic nerve terminations therefore concentration of these mediators in the corresponding receptors of postsynaptic membranes of neurons increases.
Apply And. at depressions and first of all at an endogenous depression (especially at an astheno-depressive and melancholic syndrome), and also at involutional, reactive and organic depressions. The best results receive at motive and ideatorny block. At a neurotic depression And. concedes by efficiency to tranquilizers. And. it is effective at parkinsonism (in this case its holinoblokiruyushchy and dofaminosensibiliziruyushchy action), headaches (migraine, etc. matters), neuralgia, a pain syndrome at onkol, sick, and also at night enuresis at children and teenagers.
Dosage And. it is individual. Usually in the beginning appoint 0,025 — 0,05 g a day, then raise a dose daily on 0,025 g and bring it to 0,15 — 0,2 g a day. At approach of effect stop further increase in a dose. The daily dose is divided into 3 — 4 receptions; in the evening to appoint And. it is not recommended. At achievement of remission the dose is gradually lowered (by 0,025 g every 2 — 3 day) to supporting — 0,025 — 0,075 g a day. At heavy depressions treatment is begun with intramuscular injections in the conditions of a hospital (on 0,025 g, i.e. on 2 ml of 1,25% of solution of 1 — 3 time a day). In the next 4 — 5 days the dose is raised on 0,025 — 0,05 g a day, bringing it to 0,15 — 0,2 g a day. Then gradually pass to administration of drug inside, replacing one injection with reception of two dragees (on 0,025 g).
The highest doses for adults inside: one-time 0,1 g, daily 0,3 g; intramusculary: one-time 0,05 g, daily 0,2 g. Children and patients at advanced age differ in hypersensitivity to And., therefore by it appoint lower doses: since 0,01 g once a day; then the dose is gradually increased (within 10 days), elderly to 0,03 — 0,05 g and more, to children depending on age (from 1 year to 7 years — to 0,02 g, from 8 to 14 years — to 0,02 — 0,05 g, 14 years — to 0,05 g and more in day are more senior).
Treatment is carried out under observation of the doctor. At emergence or strengthening of alarm in the course of treatment And. combine with sedative neuroleptics (levomepromazinum, Promazinum), tranquilizers (chlordiazepoxide, diazepam) or sedative antidepressants (trimeprimin, Insidanum).
And. can cause side effects: dizziness, heartbeat, orthostatic hypotonia, perspiration. Holinoblokiruyushchy action And. it can be shown by dryness in a mouth, disturbance of accommodation, increase in intraocular pressure, a delay of a mocheotdeleniye, locks. Skin allergic reactions and an eosinophilia are sometimes observed.
Drug it is contraindicated at hron, inflammatory processes in a liver and kidneys, coronary atherosclerosis, cardiac arrhythmias and heart failure, at glaucoma, diabetes, diseases of the hemopoietic bodies. It is impossible to appoint And. at the same time or soon after use of monoamine oxidase inhibitors (the break not less than on 2 weeks is necessary).
At to overdose drug there can be a poisoning which is characterized by a loss of consciousness up to a coma, emergence of spasms, disturbance of breath (short wind and an apnoea); cyanosis, a hyperthermia, falling of the ABP (sometimes in an initial stage of poisoning it raises, giving a picture of hypertensive crisis), tachycardia, signs of disturbance of conductivity of heart, expansion of pupils, dryness in a mouth is noted. At poisoning it is necessary to make a gastric lavage, to make a cleansing enema, to appoint salt laxatives. At late detection of poisoning are shown: artificial diuresis or zamenny hemotransfusion, angiotensin and high-speed cardiac glycosides. The drugs braking conductivity of heart (e.g., quinidine), are contraindicated.
Forms of release: dragee on 0,025 g and 1,25% solution in ampoules on 2 ml (25 mg in an ampoule). Store in the cool, protected from light place.
See also Antidepressants .
Bibliography: I. P's wingnuts. Pharmacological characteristic of tofranil, Zhurn, neuropath, and psikhiat., t. 63, century 4 * page 613, 1963; Mashkovsky M. Pharmaceuticals, p.1, M., 1977; Psychotropic drugs in medical practice, under the editorship of G. Ya. Avrutsky, M., 1971.