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Melipramin® [Imipramine]

Egis
1 Item
2019-09-19
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$29.94
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Clinical Pharmacology

Tricyclic antidepressant, a derivative of dibenzoazepine. Blocks reverse neuronal capture of monoamines in the brain; reduces motor inhibition, improves mood, helps normalize sleep, has an unexpressed psychostimulating effect. At the beginning of treatment, a predominance of sedative effect is possible, which is less pronounced than that of amitriptyline.

It has m-anticholinergic, myotropic antispasmodic, antihistamine effect. Does not inhibit MAO.

Antidepressant effect develops gradually; optimal therapeutic effect occurs 1-3 (to 4) weeks after the start of therapy.

Indications

Depression and depression of various etiologies, accompanied by motor and ideatory inhibition: astheno-depressive syndrome, depression (endogenous, involutional, menopausal, reactive, alcoholic), depression in psychopathy and neurosis, nocturnal enuresis in children, behavioral disorders (activity and attention), panic disorders, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pain in the face, postherpetic neuralgia, fasting traumatic neuropathy, diabetic or other peripheral neuropathy), narcolepsy accompanied by catalepsy, bulimia nervosa, cocaine withdrawal syndrome, urinary incontinence (with tension and urge to urinate), headache, migraine (prevention).

Composition

Excipients: ascorbic acid, sodium disulfite, sodium sulfite anhydrous, sodium chloride (for parenteral dosage forms), water d / and.

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Melipramin® [Imipramine]

Dosage and Administration

Inside, during or immediately after a meal (to reduce irritation of the gastric mucosa), individual dose selection is necessary, adults in the initial dose — 25–50 mg 3–4 times a day, then increase the dose daily by 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. After that, the dose is gradually reduced (by 25 mg every 2-3 days) and transferred to maintenance therapy at a dose of 25 mg 1-4 times a day for another 4-6 weeks. In older persons, the initial dose is 10 mg / day, with a gradual increase to 30-50 mg or more, until the optimum effect is obtained. To reduce the irritating effect on the gastric mucosa, a post-meal intake is recommended. For maintenance therapy, a single dose at night is often used, fractional administration is left in the elderly, adolescents, and in patients with cardiovascular disease. Higher doses for adults inside: single - 100 mg, daily - 200 mg (on an outpatient basis), 300 mg (in the conditions of a hospital) and 100 mg of elderly patients. Children, as an antidepressant, initial dose - 10 mg; within 10 days, the dose is gradually increased: for children aged 6-8 years - up to 20 mg, 8-14 years - up to 20-25 mg, over 14 years old - up to 50 mg and more (up to a maximum of 100 mg), at 2 divided doses. With bedwetting at the beginning of treatment, the daily dose: for children aged 6-8 years - 25 mg, 9-12 years - 25-50 mg, over 12 years - 50-75 mg, 1 time per day for 1 hour before sleep . With incontinence, manifested in the early night hours, the daily dose can be administered in 2 doses: one half of the dose is taken in the middle of the day, and the other - before bedtime. If there is no effect after 1 week of treatment, higher doses are prescribed. A daily dose above 75 mg does not usually improve the results. The highest daily dose for children is 2.5 mg / kg. In severe forms of depression in a hospital, you can apply a combination therapy - in / m and orally. As an antidepressant - up to 100 mg / day in divided doses. Higher doses for adults: single - 50 mg, daily - 300 mg. Children under 12 are not recommended. Too early discontinuation of treatment can lead to a resumption of depression. Imipramine should be abolished gradually.

Adverse reactions

On the part of the central nervous system and peripheral nervous system: headache, dizziness, excessive sedation, paresthesia, tremor, convulsions, dysarthria, coordination disorders, sleep disorders, hallucinations, agitation, accommodation disturbance.

On the part of the digestive system: dry mouth, stomatitis, nausea, vomiting, constipation, intestinal obstruction; rarely - hepatitis.

Since the cardiovascular system: tachycardia, arrhythmia, orthostatic hypotension.

On the part of the urinary system: urinary retention.

From the hemopoietic system: leukocytosis, eosinophilia; rarely - leukopenia, thrombocytopenia, agranulocytosis.

On the part of the endocrine system: gynecomastia, galactorrhea, decreased libido, changes in blood glucose levels.

Allergic reactions: urticaria, rash, angioedema.

Other: photosensitivity.

Hypersensitivity, use in conjunction with MAO inhibitors and 2 weeks before the start of treatment, myocardial infarction (acute and subacute periods); acute ethanol intoxication, sleeping pills, narcotic analgesics, and other drugs that depress the central nervous system; angle-closure glaucoma, severe violations of intracardiac conduction (blockade of the bundle of the bundle of His, AV blockade of Art. II), lactation period, childish age (up to 6 years).

Drug interactions

The simultaneous use of Melipramin and MAO inhibitors significantly increases the risk of developing excitement, seizures, blood pressure fluctuations, hyperthermia, coma. After discontinuation of MAO inhibitors, a break of 2-3 weeks is necessary before Melipramin is prescribed (and vice versa).

With simultaneous use of Melipramin and m-holinoblokatorov occurs the summation of the anticholinergic action of drugs.

With the simultaneous use of Melipramin and thyroid hormone preparations, adrenergic effects increase, which can cause tachyarrhythmias and the development of strokes.

The combined use of Melipramin with adrenomimetics (epinephrine, norepinephrine, mezaton) increases the risk of tachycardia, arrhythmias and arterial hypertension due to inhibition of inactivation of catecholamines Melipramin.

With simultaneous use of Melipramin with alpha-blockers and stimulants of central α-adrenoreceptors (clonidine, guanethidine, methyldopa), the antihypertensive effect of the latter decreases, which may be due to inhibition of their binding to presynaptic α-adrenoreceptors.

Imipramine reduces the anticonvulsant effect of phenytoin.

CNS depressants and ethanol increase the sedative effect of Melipramin, while benzodiazepine and phenothiazine derivatives increase the sedative and anticholinergic effects of Melipramin.

Inhibitors of microsomal oxidation enzymes (cimetidine, methylphenidate, oral contraceptives) slow down the metabolism of imipramine and increase its half-life, and therefore increase the antidepressant effect and toxicity of the drug.

Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation.

Special instructions

When prescribing Melipramin in patients with epilepsy, careful monitoring of the condition is necessary, since The drug can trigger an epileptic seizure in the first days of treatment.

When using the drug should note that the therapeutic effect occurs not earlier than 1-3 weeks from the start of treatment, the maintenance dose should be taken at least 3 months. In the initial period of Melipramin therapy, constant medical supervision of patients with suicidal tendencies is necessary.

When the drug is suddenly discontinued, withdrawal symptoms (nausea, headache, irritability, insomnia, arrhythmia, and extrapyramidal disorders) develop.

Do not use electroshock therapy while applying Melipramin.

In the case of bipolar depression, the drug may provoke the patient's transition to the manic phase.

In the first days of using tricyclic antidepressants to treat a panic condition, a paradoxically increased psychomotor anxiety may occur. If this condition does not pass in 2 weeks, then it is advisable to prescribe drugs - benzodiazepine derivatives.

Caution is prescribed Melipramin to patients with a tendency to constipation.

Melipramin should be carefully prescribed for pheochromocytoma or acute porphyria due to the threat of exacerbation of diseases with the development of the crisis.

Precautions should be prescribed the drug to elderly patients and children, because these groups of patients may have serious side effects.

During the period of treatment with Melipramin, systematic general blood tests, evaluation of liver function indicators, ECG monitoring and blood pressure levels are recommended.

Along with treatment with Melipramin, alcoholic beverages should not be consumed.

Influence on ability to drive motor transport and control mechanisms

During the period of use of Melipramin, it is prohibited to drive vehicles and perform other potentially hazardous work that requires increased concentration of attention and psychomotor speed.

Overdosage

Symptoms: psychomotor agitation, dry mouth, mydriasis, tachycardia, urinary retention, confusion, difficulty breathing, convulsions, coma.

Treatment: it is necessary to monitor the function of the cardiovascular and respiratory systems, symptomatic therapy is carried out. When seizures in / in enter diazepam, phenytoin, phenobarbital.

Imipramine does not undergo dialysis. Forced diuresis is also ineffective.

  • Brand name: Melipramin
  • Active ingredient: Imipramine
  • Dosage form: The solution for i / m administration is colorless or slightly colored (a greenish-yellow shade is possible), transparent, odorless.
  • Manufacturer: Egis
  • Country of Origin: Hungary

Studies and clinical trials of Imipramine (Click to expand)

  1. Imipramine and diet counseling with psychological support in the treatment of obese binge eaters: A randomized, placebo-controlled double-blind study
  2. Effects of single and multiple doses of dexnafenodone, imipramine and placebo on sleep of young healthy volunteers
  3. A Double-Blind Comparison of Sertraline and Imipramine in Outpatients with Major Depression: Acute (8 Weeks) and Continuation (16 Weeks) Treatment
  4. Severe Diarrhoea in an HIV-infected Patient with Chronic Hepatitis B Treated with Imipramine
  5. Panic disorder. A long-term treatment study: fluoxetine vs imipramine
  6. A double-blind comparison of the efficacy and safety of paroxetine and imipramine in the treatment of depression with dementia
  7. Dexamethasone suppression test identifies a subset of elderly depressed patients with reduced platelet serotonin transport and resistance to imipramine inhibition of transport
  8. Comparison of fluvoxamine, imipramine, and placebo in the treatment of outpatients with panic disorder
  9. CPT and VCRT performances as functions of imipramine and nialamide
  10. Concept identification and psychophysiological parameters in depressed schizophrenics as functions of Imipramine and Nialamide
  11. Imipramine in the treatment of bulimia: A double-blind controlled study
  12. A double-blind placebo-controlled comparison of phenelzine and imipramine in the treatment of bulimia in atypical depressives
  13. Effect of concurrent anxiety on response to sertraline and imipramine in patients with chronic depression
  14. External ophthalmoplegia, alpha and spindle coma in imipramine overdose: Case report and review of the literature
  15. Adrenergic Subsensitivity of a Cell-free Adenylate Cyclase from Rat Brain after Chronic Imipramine Treatment
  16. First Electrophilic Substitution of (−)-Agroclavine, Indoramine, Phenothiazine, Chlorpromazine, Iminodibenzyl, Imipramine, and Phenazone with Triethyl Orthoformate as an a1-Synthon
  17. Transdermal delivery of imipramine hydrochloride: Development and evaluation (in vitro and in vivo) of reservoir gel formulation
  18. Case study: The combined use of imipramine and behavior modification to reduce aggression in an adult male diagnosed as having autistic disorder
  19. Therapeutic monitoring of imipramine and desipramine by micellar liquid chromatography with direct injection and electrochemical detection
  20. Simultaneous measurement of imipramine and desipramine by selected ion recording with deuterated internal standards
  21. Determination of imipramine in plasma by high pressure liquid chromatography and field ionization mass spectrometry: Increased senditivity in comparison with gas chromatography mass spectrometry
  22. A sensitive method for the simultaneous determination in biological fluids of imipramine and desipramine or clomipramine and N-desmethylclomipramine by gas chromatography mass spectrometry
  23. A double-blind clinical trial of fluvoxamine and imipramine in patients with primary depression
  24. Effects of imipramine, bupropion, chlorpromazine, and clozapine on differential-reinforcement-of-low-rate (DRL) > 72-Sec and > 36-sec schedules in rat

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