Maprotiline

Chemical name

N-Метил-9,10-этанантраце н-9(10H)-пропанамин (as hydrochloride)

Gross

C20-H23-N

Characteristics

The white crystalline powder odourless.

Of drugs

Drugs, the antidepressant, anxiolytic, sedative. Selectively inhibits reverse takeover norarenalina and serotonin presinapticakimi neuronal membrane cortex brain; Blocking central alfa-adraino-, gistaminove and Holinoretseptora.pri ingestion slowly, but fully absorbed. Mean absolute bioavailability of 66-70%. Linking plasma protein-88-89%. The ratio between the distribution of the drug in the blood and plasma is 1.7. Concentration in spinal fluid is about 13% of it in the cell. To a large extent, is metabolized. The ethyl-dismetilproizvodnoe - pharmacologically active. T_1/2 43-hour general Cl - 510-570 ml / min. After intake of 50 mg C_max in the blood is about eight hours and ranges from 48 to 150 nmol / L (47 ng / ml). After 1 hour after a single on / in the 50 mg content in the blood, 54-182 nmol / L (17-57 ng / ml). In repeated ingestion or / in a 150 mg / day equilibrium concentration is achieved by 2 weeks of therapy, its value depends on the dose. Provided slow; 3 weeks after taking a single dose 57% derived from the urine, mostly in the form of metabolites (2-4% in unmodified form), and about 33% from faeces. The Association excreted in breast milk and the concentration in breast milk may be 1.3-1.5 times greater than any in the blood. In patients with the human kidney (Cl creatinine, 27-34 ml / min) T_1/2 and renal excretion vary slightly (subject to the normal functions of the liver), down metabolites in urine is reduced, but increased their withdrawal from jelchew.

Indications

Depression-endogenous, incl. inwaluie, psychogenic, incl. rocket and neurotic depression depletion, somatogenne (organic and symptomatic), a climax; depression mood with elements of anxiety, disforii or irritability, lethargy (particularly in old age), patients and somatic disorders caused by the depression, or fear.

Restrictions on the use of

Violations urination, persistent constipation, increased inner pressure, cardiovascular diseases (including over myocardial infarction, arrhythmia and / or disease). Appointment drug in pregnant women only if the expected benefit to the mother outweighs the potential risk to the fetus; A lifting treatment for at least seven weeks before the birth. During lactation is not recommended.

Contraindications

Hypersensitivity, epilepsy (or suspicion of epilepsy), the with improved sudorojna activity, the acute phase of myocardial infarction, violations conductivity infarction, arrhythmia, zakratougolnaya glaucoma, prostate adenoma cancer, acute alcohol intoxication, poisoning diet drugs, central analgetikami, psychotropic expressed by the human kidney and / or liver.

Side-Effects

Ortostatical gipotenzia, tachycardia, the conductivity, measuring, the AD, dizziness, headache, melcorazmashisty tremor, convulsions, ataxy, mioclonus, dizartria, parestesia, muscle weakness, diskinesia, coordination of movements and handwriting, fatigue, drowsiness or insomnia, nightmares, anxiety, arousal, increased appetite, aggression, impaired memory and concentration, increased depression, deliri, hallucinations, disorientation, irritability, uproar in the face, a change of taste, zalojennosti nose, worsening psychosis, depersonalization, dry mouth, constipation, increased sweating, a feeling of heat, the ambiguity of, a breach of ccomodation, violations mocheotdelenia, disease, dental caries, nausea, vomiting, increasing transaminaz in plasma, diarrhoea, hepatitis (jaundice with or without), allergic alveolitis, increased body mass index, violations and sexual potency, гинекомастия, галакторея, inadequate syndrome exists secreta, лейкопения, агранулоцитоз, эозинофилия, anaemia, skin rashes, urticaria, in some cases, with fever фоточувствительность, васкулит, itching, пурпура, oedema (local or Generalized), hair loss, алопеция, мультиформная erythema, the syndrome of "lifting" (nausea, vomiting, pain in the abdomen, diarrhoea, insomnia, headache, irritability, anxiety, increased depression, etc.).

Specific guidance

Patients receiving maprotilin, should refrain from activities potentially hazardous activities that require greater attention and rapid mental and motor reactions.

Patient interaction

Decreases антигипертензивный effect гуанетидина, бетанидина, резерпина, метилдофы, clonidine increased influence on the cardiovascular system симпатомиметических preparations (норадреналина, sports, изопреналина, ephedrine and фенилэфрина etc.), тироксина increases the activity of ethanol and этанолсодержащих preparations депримирующих funds (barbiturates anaesthetic, derivatives бензадиазепина), the proximity anticoagulants, сахароснижающих preparations (сульфанилмочевины derivatives, insulin), холинолитиков (atropine, biperiden) леводопы. Preparations mikrosomalnoe trigger oxidation in the liver (barbiturates, phenytoin, carbamazepine), oral contraceptives reduce antidepressant effect. Co-administration with tranquilizers increases concentration in the serum, reduces threshold sudorojna preparedness and as a source of convulsing. Methylfenidat, propranolol, fluoxetin, fluvoksamin, phenytoin, and possibly zimetidin increase concentration in plasma, increasing and the side effects.

Overdosing

There oppression or criminal Zns.simptoma : mood, anxiety, ataxy, convulsions, stalemate, coma, arousal, increased reflexes, muscle rigidity, horeoatetoz; Tachycardia, arrhythmia, arterial gipotenzia, violations conductivity, cardialny shock, heart failure, in rare cases, cardiac arrest; Respiratory depression, zianoz, vomiting, fever, midriaz, increased sweating, oliguria, anuria. Symptoms of overdose develop approximately 6700, reach a peak within 24 hours and can be preserved for a 4-6 суток.Лечение : symptomatic (specific antidote no). Introduction fizostigmina contraindicated because of the risk of a convulsing. Haemodialysis not effective.

Precautions

During treatment, patients should be under the supervision of a physician. A control mental and neurological status, regular study of the peripheral blood of the kidneys and liver. Patients with a high risk of side effects from the circulatory system shows control AD ECG. Apply after MAO inhibitors can be only two weeks. There should be the same interval and replacement maprotilina at MAO inhibitors.

Dosing and Administration

Inside. Dose is individually and depends on the degree of depression and sensitivity to the drug. The daily dose is 75 mg in 1-3 reception. The maximum daily intake for outpatient treatment, 150 mg, in inpatient-225 mg. Initial dose is 25 mg, in 2 weeks dose can be gradually increased. In reducing depressive symptoms single dose can be reduced gradually from 50 to 25 mg. Daily dose of the drug can be taken in one or more Priemov.v / in the drip in a daily dose of 100-mg. For one Infusion used 25-50 mg (1-2 contents vials), divorced in 250 ml izotoniceski solution of sodium chloride or 5% glucose solution; Infusion duration-half hours If necessary, the higher doses can be infuziu 75-150 mg (3-6 contents vials), divorced in 500 ml solvent; Infusion duration of 2-3 h. Once infuzionnaya therapy would have a significant antidepressant effect (in most cases, in 1-2 weeks) should go to the oral ingestion.

Directory → Neurotropic funds → 24.2.1 → Maprotiline