Buy at online pharmacy – Anafranil (clomipramine)
Anafranil 60 Caps x 75mg (generic) only $46.80
Buy online pharmacy, Anafranil (clomipramine)
Anafranil (clomipramine)
clomipramine: Anafranil, Gidifen, Klominal, clomipramine, Klofranil.
Anafranil – Clomipramine
Latin name:
Anafranil / Anafranil.
Active-active substance:
Clomipramine / Clomipramine taking a dog off clomipramine.
The composition and the form of:
Anafranil tablets, sugar-coated shell.
1 tablet Anafranil, covered sugar shell that contains 10 mg or 25 mg of clomipramine hydrochloride (active ingredient), as well as inactive ingredients: glycerin (85%, PH), lactose, magnesium stearate, maize starch, stearic acid, hydroxypropyl, copolymer of vinylpyrrolidone / vinyl acetate, microcrystalline cellulose, titanium dioxide, yellow iron oxide, macrogol 8000, polyvidone, sucrose, talc. Tablets 10 mg also contain gelatin. Tablets 25 mg also contain silica aerogels.
Anafranil retard tablets.
1 tablet Anafranil retard (divisible) contains 75 mg of clomipramine hydrochloride (active ingredient), as well as inactive ingredients: silica aerogels, calcium phosphate, calcium stearate, esters polyacryl copolymer / metakrila, hydroxypropylcellulose, polyethylene glycol, glyceryl oksistearat, red iron oxide, titanium dioxide, talc.
Anafranil injection clomipramine for dogs.
Anafranil 2 ml solution for injection (1 vial) contains 25 mg of clomipramine (active substance), as well as an inactive ingredient glycerol in water for injection.
Pharmacological properties:
Anafranil is a tricyclic antidepressant. It is believed that the curative effect Anafranila carried out due to its ability to inhibit neuronal capture of noradrenaline (NA) and serotonin (5-HT), released into the synaptic cleft, the most important is the inhibition of serotonin reuptake.
Anafranilu addition, inherent in a wide range of other pharmacological actions: alpha 1-adrenoliticheskoe, anticholinergic, antihistamine and antiserotoninergicheskoe (blockade of 5-HT-receptors).
Anafranil affects the depressive syndrome in general, including especially those of its typical symptoms like psychomotor retardation, depressed mood and anxiety. The clinical effect is usually observed after 2-3 weeks of treatment.
Anafranil is also a specific effect in obsessive-compulsive disorder, which differs from its antidepressant effect.
Step Anafranila in chronic pain syndromes caused by or caused by physical illness, associated with relief of nerve impulse transmission, mediated by serotonin and noradrenaline.
Pharmacokinetics:
Suction.
Dosage forms for oral administration. Clomipramine completely absorbed from the gastrointestinal tract. Systemic bioavailability of unchanged clomipramine is about 50%, which is associated with a pronounced during the first pass metabolism through the liver, leading to the formation dezmetilklomipramina. Eating does not significantly affect the bioavailability of clomipramine. Perhaps only a slight slowdown in the absorption and, consequently, increase the time to reach maximum concentration in the blood. Given the number of absorbed active substance coated tablets, and retard tablets are bioequivalent.
After receiving a constant dose of the drug inside the equilibrium concentration of clomipramine in plasma from individual patients varied greatly.
When the daily appointment of a drug at a dose of 75 mg / day (in the form of coated tablets, 25 mg 3 times daily, or as a retard tablets, 75 mg 1 time a day) the equilibrium concentration of drug in plasma is set in a range from 20 to 175 ng / ml. The values of the equilibrium concentration of the active metabolite desmetilklomipramina are in a similar range. Nevertheless, the appointment Anafranila to 75 mg per day, these values are 40-85% higher than the concentration of clomipramine.
Solution for injection.
After intramuscular injection of clomipramine absorbed completely. upon repeated intramuscular or intravenous Anafranila daily administration at a dose of 50-150 mg / day equilibrium concentration is reached at the 2nd week of treatment. The values of the equilibrium concentration of clomipramine ranges from less than 15 to 447 ng / ml, and the active metabolite desmetilklomipramina – from less than 15 to 669 ng / ml.
Distribution.
Binding clomipramine plasma proteins is 97.6%. The apparent volume of distribution is about 12-17 l / kg body weight. Concentrations of clomipramine in the cerebrospinal fluid is around 2% of its level in blood plasma. Clomipramine penetrates into the breast milk, which is determined at concentrations close to the concentrations in blood plasma.
Metabolism.
The main way of metabolism of clomipramine – demethylation with the formation of desmetilklomipramina. In addition, clomipramine and desmetilklomipramin subjected hydroxylation with the formation of 8-hydroxy-clomipramine and 8-gidroksidesmetilklomipramina, but there is little information on their pharmacological activity in vivo. The process of hydroxylation of clomipramine and desmetilklomipramina genetically determined (similarly metabolized debrizohina). In persons with poor metabolism debrizohina plasma concentration desmetilklomipramina can reach high values, whereas the effect on the concentration of clomipramine expressed to a lesser extent.
Excretion.
About 2 / 3 of a single dose of clomipramine is excreted as water-soluble conjugates in the urine and about 1 / 3 dose – with feces. Unchanged in the urine output of about 2% of the dose of clomipramine and about 0,5% desmetilklomipramina.
After receiving the drug inside the plasma half-life of clomipramine is on average 21 h (range of variation from 12 to 36 h), and dezmetilklomipramina – an average of 36 hours. After intramuscular and intravenous Anafranila final half-life of clomipramine is an average of 25 hours (range of variation from 20 to 40 h) and 18 h, respectively.
Pharmacokinetics in separate groups of patients
Elderly patients, regardless of the dosage used Anafranila, owing to decrease the intensity of metabolism of clomipramine concentration in plasma higher than in patients of younger age. Effect of human liver and kidney on the pharmacokinetics of clomipramine have not been studied.
Indications:
Treatment of depressive states of different etiology, occurring at different symptoms:
# Endogenous, reactive, neurotic, organic, masked, involutional forms of depression;
# Depression in patients with schizophrenia and psychopathy;
# Depressive syndromes occur in old age; buslovlennye chronic pain syndrome or chronic physical illness;
# Reactive depressive mood disorders, neurotic or psychopathic nature.
Obsessive-compulsive syndromes.
Chronic pain syndrome.
In addition to pills:
Phobias and panic disorder (attacks).
Cataplexy, concomitant narcolepsy.
Night enuresis (only in patients over the age of 5 years and subject to the exclusion of organic causes of disease).
In addition to the solution for injection:
Phobias.
Dosage and administration:
Dosage and route of administration is selected individually, taking into account the patient’s condition. Tactics of treatment is to achieve the optimum effect on the background of the lowest possible doses, and increasing them cautiously, especially in elderly patients and adolescents, who are generally more sensitive to Anafranilu than patients of intermediate age groups.
Dosage forms for oral administration:
Depression, obsessive-compulsive syndromes and phobias. Treatment is initiated with the purpose 1 film-coated tablet containing 25 mg of clomipramine, 2-3 times a day, or 1 retard tablets containing 75 mg of clomipramine, 1 time per day (preferably in the evening). Then, during the first week of treatment dose is gradually raised, for example, 25 mg every few days (depending on tolerability) until the daily dose is 4-6 tablets of 25 mg or 2 retard tablets, 75 mg. In severe cases, the daily dose can be increased to the maximum, is 250 mg. After the clearly expressed will be achieved better, pick up a supportive dose of 2-4 tablets of 25 mg or 1 tablet retard 75 mg.
Panic disorder, agoraphobia. Treatment is initiated with the use of 1 tablet containing 10 mg of clomipramine, in the day, possibly in combination with the drug from the group of benzodiazepines. Then, depending on the tolerability Anafranila, it increase the dose to achieve the desired effect, then gradually abolish the drug from the group of benzodiazepines. Required in these cases, the daily dose Anafranila greatly varies from patient to patient and is in the range from 25 to 100 mg. if necessary it can be increased to 150 mg. It is recommended not to stop treatment for at least 6 months, slowly decreasing during this time maintenance dose of the drug.
Cataplexy, concomitant narcolepsy. Daily dose Anafranila is 25-75 mg.
Chronic pain syndromes. Anafranila dose should be titrated individually (10-150 mg / day), with the concomitant analgesic admission means (taking into account the possibility of reducing their use).
Elderly patients. Treatment is initiated with the appointment of 1 tablet of 10 mg per day. Then, gradually, in approximately 10 days, the daily dose raised to the optimum level, which amounts to 30-50 mg, and maintain it at that level until the end of treatment.
Night enuresis. Anafranila initial dose in children aged 5-8 years is 2-3 tablets of 10 mg in children aged 9-12 years – 1-2 tablets of 25 mg in older children – 1-3 tablets of 25 mg. The use of higher doses showed those patients who have no clinical effect after 1 week of treatment. Typically, the entire daily dose is assigned to one reception after the dinner, but in cases where involuntary urination observed in the early hours of the night, part of the prescribed dose Anafranila earlier, in 16 hours. After achieving the desired effect, treatment should continue for 1-3 months, gradually reducing the dose Anafranila.
Experience of Anafranila in children aged under 5 years are not available.
Retard tablets should be swallowed whole, not chewed.
Ampoules:
Intramuscular injections. Started treatment with the introduction of 25-50 mg (contents of 1.2 ampoules), then increase the daily dose of 25 mg (1 vial) until the daily dose of 100-150 mg (4-6 ampoules). Once the improvements will be noted, the number of injections of gradually reduce and replace them with supportive therapy with oral forms of the drug.
Intravenous infusion. Treatment is initiated with an intravenous drip of 50-75 mg (contents of 2.3 vials) 1 times a day. for the preparation of infusion solution using 250-500 ml isotonic sodium chloride or glucose solution, the duration of infusion of 1.5-3 h. During infusion is necessary to carefully monitor patients for early detection of possible adverse reactions. Particular attention should be given to control blood pressure, as may develop orthostatic hypotension. If we managed to achieve a clear improvement, treatment with infusion should continue for a period of 3-5 days. Then, to maintain and secure the transition effect of the drug inside the reception, 2 tablets of 25 mg is usually equivalent to 1 Anafranila ampoule containing 25 mg. With a view to the gradual transition from infusion therapy to favor receiving oral medication can also transfer the patient to the first intramuscular injection.
Children parenteral injection of the drug is not recommended.
Overdose:
There were no reports of overdose injection solution Anafranila not available.
Symptoms and complaints, developing overdose Anafranila taken orally, are similar to those described in overdose other tricyclic antidepressants. The main complications are violations of the cardiac and neurological disorders. The children receive random drug inside should be regarded as very serious and threatening to fatal accident, regardless of the size of the dose.
Complaints and symptoms:
Symptoms usually appear within 4 hours of ingestion and reach maximum severity after 24 hours. Due to the delayed absorption (anticholinergic effect of the drug), a long half-life and recycling gepatoenteralnoy active substance, the time period during which the patient remains in the “risk”, is 4-6 days.
May experience the following complaints and symptoms:
The central nervous system, drowsiness, stupor, coma, ataxia, anxiety, agitation, increased reflexes, muscular rigidity, horeoatetoidnye movements, convulsions.
Since the cardiovascular system: hypotension, tachycardia, arrhythmias, disturbances in intracardiac conduction, shock, heart failure, in very rare cases – cardiac arrest.
In addition, possible respiratory depression, cyanosis, vomiting, fever, mydriasis, sweating, oliguria or anuria.
Treatment:
There is no specific antidote, treatment is mainly symptomatic and supportive. for suspected overdose Anafranila, especially in children, the patient should be hospitalized and closely monitored for at least 72 hours.
If the patient is conscious, should be as soon as possible to gastric lavage or induce vomiting. If the patient is unconscious, before gastric lavage to prevent aspiration should be to tracheal intubation using a tube with a cuff; vomiting in this case is. These measures are recommended in the case since the overdose was 12 hours and even more, since anticholinergic activity Anafranila may slow gastric emptying. to slow the absorption of the drug is useful to use activated carbon.
Treatment is based on the application of modern methods of intensive therapy with continuous monitoring of cardiac function, gas composition and blood electrolytes, as well as on the application if necessary, such urgent measures as the Anti-convulsive therapy, artificial ventilation and resuscitation techniques. Since then, as it was reported that physostigmine may cause bradycardia, asystole, and seizures, use this drug for the treatment of overdose Anafranila not recommended. Hemodialysis and peritoneal dialysis are not effective, as the concentration of clomipramine in plasma are small.
Contraindications:
Hypersensitivity to clomipramine or any other ingredients, cross-sensitivity to tricyclic antidepressants in the group dibenzazepina. Concurrent administration of MAO inhibitors, as well as the period of less than 14 days before and after their use. Is also contraindicated in concomitant use of selective inhibitors of MAO-A reversible action, such as moclobemide.
Recent myocardial infarction.
Use during pregnancy and lactation:
Experience with Anafranila during pregnancy is limited. As known to some reports of a possible link between taking a tricyclic antidepressant with violations of the fetal development should be avoided Anafranila during pregnancy, except in cases where the expected effect of treatment of the mother clearly outweighs the potential risk to the fetus.
In cases where tricyclic antidepressants were used during the pregnancy up until birth, the newborn during the first few hours or days of developing a withdrawal syndrome manifested wheezing, drowsiness, cramps, irritability, hypotension or hypertension, tremor or spastic phenomena. Avoid the development of this syndrome, Anafranil should be, if possible, gradually lifted, at least for 7 weeks before the expected birth.
Since the active ingredient passes into breast milk, you should either discontinue breast-feeding, either gradually abolish Anafranil.
Side effects:
The observed adverse events were generally mild and transient, are in the continuation of treatment or after dose reduction Anafranila. They are not always associated with the level of active ingredient in blood plasma or with the dose. Some undesirable effects, such as general weakness, sleep disturbances, agitation, anxiety, constipation, dry mouth, it is often difficult to distinguish from the manifestations of depression.
In the case of serious adverse reactions in the nervous system or mental status Anafranil should be repealed.
