Hydrochloride (imipraminum)
IMIPRAMIN (Imipraminum).
N - (3-Dimetilaminopropil) - iminodibenzila hydrochloride, or 5 - (dimethyl-3-aminopropyl) -10,11-dihydro-5 H-dibenzo [b, f] - azepina hydrochloride.
Synonyms : Imizin, Melipramin, Antideprin, Deprenil, Deprimin, Deprinol, Depsonil, Dynaprin, Eupramin, Imipramil, Irmin, Melipramin, Surplix, Tofranil and others.
The white crystalline powder. The easily soluble in water and alcohol.
Aqueous solutions have pH 3, 7, 4, 5.
Imipramine is the main representative of typical drugs antidepressants. This is one of the first antidepressants, but because of the high efficiency, it is widely used so far.
In the operation hydrochloride is a reverse takeover inhibitor monoaminov - neyromediatorov. This action is not an election, he had a seizure noradrenalina blocks, something, serotonin and other neyromediatorov and leads to their accumulation in the synaptic junctions and increased their physical activity. In the experiment eliminates or reduces the effects deprimiruyuschie rezerpina, aggravating simpatomimeticheskih substances has holinoliticheskoy activity.
The nature of hydrochloride of the antidepressants associated with stimulant effect.
Applied hydrochloride with the depressed state of various etiology, particularly in astenodepressivnyh state involving motor and ideatornoy inhibition, including endogenous depression involyutsionnoy, menopause depression, reactive depression and depressive state in Psychopathy and the nervousness and others, with alcoholic depression.
The drug reduces sadness, better mood (timoleptichesky effect), a vivacity, reduce engine block, improve mental and general tone the body.
Assign usually inside (after eating), from 0.75-0.1 grams per day, and then gradually increase the dose (daily at 0,025 g) and bring it to 0,2-0,25 grams a day. When the antidepressant effect of increasing the dosage is not recommended. In some cases resistant and no side effects apply to 0.3 grams per day. The duration of treatment on average 4 to 6 weeks, then gradually lower the dose (at 0,025 grams every 2 to 3 days) and then to a supportive therapy (typically 0,025 g of 1 to 4 times a day).
It should be borne in mind that too early termination of treatment can lead to a resumption of depression. Remove hydrochloride should be gradual.
In severe depression in a patient can use combination therapy, intramuscular injections and receiving drugs inside. Started with intramuscular injections of 0,025 grams (2 ml of 1, 25% solution) 1 - 2 - 3 times daily; The 6 th day bringing the daily dose to the city then 0,15-0,2 dose injection beginning reduce and designate drug inside, and every 25 mg drug injection (2 ml of 1, 25% solution) to replace the 50 mg drug in the form of pills. Gradually move to go only into a drug and then to supportive therapy.
Sometimes, beginning with the attack doses : 0.1 - 0.15 g intramuscularly, or 0,2 - 0,25 g inside a day; Then when the antidepressant effect of the dose is gradually reduced.
Dose imipramina be less for children and seniors. Children are designated inwards from 0.01 g 1 per day; Gradually, over a period of 10 days, increasing the dosage for children aged 1 to 7 years to 0.02 g, 8-to 14-years - to 0.02 - 0.05 grams over 14 years up to 0.05 grams or more per day. Those older also appointed from 0.01 g 1 times a day, gradually increasing the dosage to 0,03 - 0,05 g or more (within 10 days), until the optimal dose for the patient.
If necessary (for depression in patients with schizophrenia, involyutsionnoy melanholiey, where alarming azhitatsii etc.) hydrochloride can be combined with Neuroleptics.
Higher doses for adults inside : single 0.1 g, 0.3 g daily; Intramuscularly : single 0.05 grams daily 0.2 g.
Children sometimes designate hydrochloride for the treatment of functional (neurogenic) night minor (incontinence of urine). Mechanism of action is probably due to the fact that sleep admission imipramina becomes less acute. A similar effect may have other antidepressants, which timoleptichesnoe combined with a stimulating effect on the central nervous system. Note that the treatment imipraminom may increase or when insomnia. Therefore, in treating depression, it is recommended to take in the morning (16 to 15 h). Sometimes hydrochloride appointed in narcolepsy.
Treatment imipraminom be conducted under the supervision of a doctor. Please note that in addition to reducing depression and increased activity may increase delirium, anxiety, hallucinations.
Possible side events in the treatment imipraminom include headaches, dizziness, sweating, palpitation. In connection with cholinolytic action may dry mouth, a breach of accommodation, delay urination. Sometimes there allergic skin reactions, eosinophilia and temporary leucocytosis, possible violations of heart rhythm.
When a drug overdose might mark insomnia, agitation.
Imipramine not appoint with MAO inhibitors, or immediately after their admission. The drug can take 1 to 3 weeks after the MAO inhibitors, and should start with low doses (0.025 g / day).
It also appoint hydrochloride with thyroid drugs. Patients who are receiving hydrochloride, tireoidin can cause sharp predserdnuyu paroxysmal tachycardia.
Caution is needed when epilepsy, as hydrochloride can be better prepared to respond convulsant.
There should be appointed hydrochloride in the first three months of pregnancy.
The drug is contraindicated in acute liver, kidneys, blood-forming organs (to radiation and agranulotsitoza), diabetes, cardiovascular decompensation, violations conductivity hearts expressed atherosclerosis, the active phase of pulmonary tuberculosis, infectious diseases, disorders of cerebral circulation, adenoma prostate gland, atony bladder.
In connection with holinoliticheskoy activity imipramina specifically examined the question of admissibility of his application in glaucoma. Imipramine and other antidepressant drugs increase the inner pressure only in the eyes of local anatomical predisposition narrow-angle camera front. In open - glaucoma improve inner pressure is not there.
Nevertheless, these patients treated tricyclic antidepressants should be under regular supervision of an ophthalmologist. Preferably use antidepressants, the non-holinoliticheskoy activity (see Pirazidol, Tetrindol, Azafen etc.). Top holinoliticheskoy active are amitriptyline and Fluacizine.
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