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Active ingredient of medicine – Imipraminum a hydrochloride.
Dragees Melipraminum have the following additional components: titanium dioxide, glitserol 85%, macrogoal 35 000, gelatin, talc, lactoses monohydrate, ferrous oxide red, magnesium stearate, sucrose.
Auxiliary components of solution for intramuscular introduction: sodium pyrosulphite, ascorbic acid, sodium chloride, sodium sulfite anhydrous, water for injections.
Additional elements of tablets, film coated: lactoses monohydrate, krospovidon, magnesium stearate, K-25 povidone. The making covers: gipromelloza, mix of dyes, magnesium stearate, dimetikon E1049 39%.
Medicine is issued in a dragee, in the form of solution for intramuscular introduction, and also in tablets, film coated.
Antidepressant, sedative drug.
Pharmacodynamics and pharmacokinetics
Melipraminum represents tricyclic antidepressant. It not selectively blocks the return capture of neuromediator monoamines because of what they accumulate in a synaptic gap. It leads to strengthening of physiological activity.
Drug also has timoleptichesky effect. It is characterized by the accompanying stimulating activity, raises an organism tone, provokes decrease in motive block. Medicine possesses peripheral and central m-holinoblokiruyushchey, weak antihistaminic, myotropic activity.
At reception orally drug is characterized by good extent of absorption from a gastrointestinal tract. Bioavailability can be ranging from 29% to 77%. The maximum plasma concentration – approximately in 1-2 hours after the use inside and half an hour or hour later at intramuscular injections.
Extent of communication with proteins of plasma – about 85%. Active agent is well distributed in fabrics and is capable to get through GEB. It also selectively accumulates in a brain, a liver and kidneys.
At hit in an organism it biotransformirutsya intensively in a liver. About 40% of Imipraminum of a hydrochloride are removed within a day together with urine in the form of metabolites, and 1-2% – in an invariable look. About 20% of a dosage are excreted with bile. The elimination half-life can be from 4 to 24 hours.
Indications to use
Indications to use of medicine following:
- night enuresis at children;
- depressions and depressions of various origin to which motor and ideatorny block accompanies;
- obsessivno-compulsive frustration;
- panic frustration;
- behavior disorders (superactivity or requirement of attention);
- chronic pain syndrome;
- narcolepsy in combination with a katalepsy;
- frequent headaches;
- nervous bulimia;
- syndrome of "cancellation" of cocaine;
- need of prevention of migraine;
- urine incontience.
It is impossible to use drug at a benign hyperplasia of a prostate, acute diseases of a liver and kidneys, infectious diseases, a diabetes mellitus and heart diseases in a decompensation stage, disturbances of a cordial rhythm and conductivity, the increased convulsive readiness, atony of a bladder, pregnancy (I trimester), breastfeeding, hypersensitivity to tricyclic antidepressants, diseases of bodies of a hemopoiesis, an active form of tuberculosis, a hyperthyroidism, the acute phase of a myocardial infarction expressed to cardiovascular insufficiency, closed-angle glaucoma, age till 6 flyings.
With care this medicine should be used in case of epilepsy.
Side reactions when using the drug Melipraminum can be the following:
- CCC: tachycardia, orthostatic hypotension, arrhythmia, conductivity disturbances;
- TsNS: agitation, a headache, paresthesias, spasms, disorders of coordination, a hallucination, inversion of a phase in case of bipolar psychosis, dizziness, sleeplessness, a tremor, a dysarthtia, confusion of consciousness, accommodation disturbance;
- system of a hemopoiesis: leukocytosis, eosinophilia;
- allergy: dieback;
- Gastrointestinal tract: locks;
- urinary and sexual systems: urination delay, decrease in a libido;
- endocrine system: gynecomastia, galactorrhoea;
- others: dryness in a mouth, a photosensitization, fever, a hair loss, the increased sweating.
In rare instances hepatitis, a leukopenia, an agranulocytosis develop.
Application instruction of Melipraminum (Way and dosage)
At administration of drug intramusculary it is necessary to begin with 25 mg 3 times a day. If it is necessary, in the next days the dosage can be raised gradually. But the day dose should not be more than 100 mg. After a week of use of medicine intramusculary the dose is gradually reduced by means of replacement of one prick by reception of a dragee or a tablet. From the 13th day of therapy completely pass to oral administration in a dosage 25 mg on 4 times every day. If symptoms of a disease return, it is possible over again to start doing intramuscular injections.
The application instruction of Melipraminum for elderly people recommends to begin therapy with small doses. Usually it is 10 mg/days. Then gradually the amount of drug is increased to 50 mg. The maximum dosage for elderly people – 100 mg.
Dragees and a pill are taken inside right after meals. Dosages are calculated in an individual order. Usually for adult patients the course begins with a dose in 25-50 mg every day on 3-4 times. The application instruction of Melipraminum reports that gradually daily dosage can be raised on 25 mg and to bring it to 250-300 mg. The highest doses of drug for adult patients the following:
- one-time – on 100 mg;
- day – on 300 mg at a hospital or on 200 mg it is out-patient.
Therapy duration in case of easy forms of a depression treatment on average 5 weeks.
For a maintenance therapy the single dose of medicine is recommended in the evening.
Children drug as antidepressant are given at the beginning of a course in a dosage 10 mg. Within 10 days of its treatment it is possible to increase gradually. For children the following maximum dosages are shown:
- the age of 6-8 years – is given on 20 mg;
- the age of 8-14 years – is given on 25 mg;
- the age is more senior than 14 years – give 100 mg (in 2 receptions).
In case of bed wetting at the beginning of therapy take medicine in the following dosages:
- children of 6-8 years – 25 mg;
- children of 9-12 years – 25-50 mg;
- children of 12 flyings – 50-75 mg.
It is necessary to do it once a day for an hour to a dream. If the incontience of urine is shown in early hours of a dream, the dosage can be divided in 2 receptions. In this case the first half is accepted in the middle of the day, and the second – just before a dream. If the due effect is not reached within a week, the dosage can be raised. The maximum day dose for children – 2,5 mg/kg.
In case of a heavy depression in the conditions of a hospital medicine can be applied at the same time intramusculary and orally. If drug is accepted as antidepressant, enter up to 100 mg a day in stages. The highest single dose for adult patients – 50 mg, day – 300 mg.
If to stop reception too early, it can lead to return of a depression. It is necessary to cancel medicine step by step.
At reception of means in the dosages exceeding norm dizziness, an ataxy, a stupor, a mydriasis, arrhythmia, repolarization disturbance, arterial hypotension, cyanosis, fever, excitement, spasms, a coma, AV blockade, sinus tachycardia, a collapse are possible with a high venous pressure, respiratory depression, vomiting.
As treatment appoint a gastric lavage using normal saline solution, and also reception of Absorbent carbon. It is necessary to control an ECG constantly. Perhaps slow intravenous administration of Physostigmine of salicylate: the adult on 1-3 mg, patients at children's age – in an initial dosage of 0,5 mg, it is raised if necessary with monitoring of function CCC and a nervous system to 2 mg. If it is necessary, Physostigmine is entered by each half an hour or hour, the dose at the same time is selected individually.
In the presence of the corresponding indications the symptomatic treatment is carried out by anticonvulsants: Diazepam or barbiturates of short action. The last are contraindicated if the patient received MAO inhibitors recently.
Antishock measures include intravenous injections of plasma substituting solutions, glucocorticoids, and also an oxygenotherapy.
In case of a hyperthermia cold rubdowns are applied.
Use of medicine together with MAO inhibitors is contraindicated. Such combination can cause superexcitation, fluctuations of pressure, a coma, spasms, a hyperthermia. Between reception of these means it is necessary to observe an interval at least of 2 weeks.
The combination to m-holinoblokatorami leads to summing of anticholinergic effects of medicines.
Interaction with hormonal drugs of a thyroid gland can cause strengthening of adrenergic action that provokes a tachyarrhythmia and attacks of stenocardia.
The combination to adrenomimetika increases probability of tachycardia, arterial hypertension and arrhythmia because of braking of an inactivation of catecholamines.
Drug reduces anti-hypertensive effect of alpha adrenoblockers and stimulators of the central alpha adrenoceptors, and also anticonvulsant effect of Phenytoinum.
Sedative action of Melipraminum increases under the influence of the ethanol and means oppressing a nervous system. Derivatives of benzodiazepine and a fenotiazina activate anticholinergic and sedative effects.
Biotransformation of active ingredient of Melipraminum is slowed down under the influence of inhibitors of enzymes of a microsomal oxidation. Besides, they increase its time of semi-removal because of what antidepressive effect and toxicity of drug increases.
Terms of sale
Medicine is on sale in drugstores only according to the recipe of the doctor.
This medicine needs to be stored in well protected from sunshine and the place, unavailable to small children. Optimum temperature – 15-25 °C.
Period of validity
The period of validity of tablets and dragee makes 3 years, solution for intramuscular introduction – 5 years.
Analogs of Melipraminum
Coincidence on the ATH code of the 4th level:
About Melipraminum at forums demonstrate that drug is successfully used for treatment of depressions of various origin, obsessivno-compulsive frustration, and also panic frustration. Patients report that its action develops gradually. Efficiency becomes noticeable several weeks later.
Responses at enuresis also generally positive. As a rule, drug is given in this case to children. There are messages on some side effects (generally nausea or drowsiness), but those who accepted this means, tell that all negative reactions have slight character and pass at reduction of a dosage.
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Section: For a nervous system
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