Anafranil is a drug belonging to the group of tricyclic antidepressants, used for the treatment of depressive disorders, obsessive-compulsive disorder and some other mental conditions. The drug has a pronounced effect on the central nervous system, helping to normalize mood, reduce anxiety and eliminate intrusive thoughts or actions. In addition, it is used for relief of chronic pain and treatment of nocturnal enuresis in children, which makes it a universal remedy in psychiatric and neurological practice.
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Dosage | Package | Per Item | Per Pack | Order |
10 mg |
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25 mg |
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50 mg |
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The trade name of the drug is Anafranil. This is the registered name under which the drug is known on the pharmaceutical market.
The international nonproprietary name is clomipramine. It denotes the active active ingredient and is used in medical practice throughout the world.
Anafranil is available in several forms: coated tablets, 10 mg, 25 mg and 75 mg in blisters of 10 or 20 pieces; capsules with prolonged release (Anafranil SR) of 75 mg; solution for intramuscular and intravenous injections in ampoules of 25 mg/2 ml, packed in 10 pieces. The variety of forms allows to adapt the treatment to the individual needs of patients.
The main active ingredient is clomipramine hydrochloride. One tablet contains 10 mg, 25 mg or 75 mg of clomipramine hydrochloride, in a capsule SR - 75 mg, and in 1 ml of solution for injection - 12.5 mg.
Tablets contain lactose monohydrate, corn starch, microcrystalline cellulose, magnesium stearate and a coating of hypromellose, titanium dioxide, iron oxide yellow. The capsules include gelatin, titanium dioxide, modified starch. The solution for injection contains glycerin, water for injection, and sodium chloride for stabilization.
Clomipramine, the active ingredient in Anafranil, acts as a serotonin and norepinephrine reuptake inhibitor at synapses in the central nervous system. This mechanism increases the concentration of these neurotransmitters in the intercellular space, which contributes to improving mood, reducing depressive symptoms and eliminating obsessions. The drug has a more pronounced effect on the serotoninergic system, making it particularly effective in obsessive-compulsive disorder (OCD). In addition, clomipramine exhibits anticholinergic, antihistamine and alpha-adrenoblocking properties, which accounts for its sedative effect and influence on the autonomic nervous system.
Therapeutic effect develops gradually: the first improvements are noticeable after 1-2 weeks, and the full antidepressant result is achieved after 4-6 weeks of regular use. In OCD, the drug reduces the frequency and intensity of intrusive thoughts and rituals due to modulation of serotonin pathways in the brain. Anticholinergic action also helps with nocturnal enuresis by relaxing the smooth muscle of the bladder and increasing its capacity.
Clomipramine is well absorbed from the gastrointestinal tract after oral administration. Maximum plasma concentration is reached in 2-6 hours, bioavailability is about 50% due to the effect of first passage through the liver. When administered intravenously, absorption is immediate, which provides a faster onset of action.
The drug actively binds to plasma proteins (97-98%), mainly to albumin. The volume of distribution is 12-17 l/kg, indicating a wide penetration into tissues, including the brain. Clomipramine crosses the blood-brain barrier, providing central action.
Clomipramine is metabolized in the liver with the participation of cytochrome P450 enzymes, predominantly CYP2D6 and CYP1A2. The main active metabolite, desmethylclomipramine, has greater noradrenergic activity, complementing the serotoninergic effect of the parent substance. Metabolism occurs in two steps: first demethylation, then hydroxylation and conjugation with glucuronic acid.
The half-life of clomipramine is 19-37 hours, and of its metabolite - up to 50 hours. The drug is excreted through the kidneys (about 60%) and intestine (about 40%), mainly in the form of metabolites. Complete excretion takes 4-6 days.
Anafranil is prescribed for the following conditions:
The drug is effective for both acute treatment and maintenance therapy.
The use of Anafranil is prohibited in:
Cautious prescribing in epilepsy, hypothyroidism, severe hepatic or renal insufficiency.
Anafranil tablets and capsules are taken orally, drinking water (100-150 ml), preferably during or after meals to reduce gastric irritation. The solution for injection is administered intramuscularly or intravenously (slowly) only by medical personnel. The dose is increased gradually to minimize side effects.
For depression: initial dose is 25 mg 2-3 times daily, increasing to 100-150 mg/day for 1-2 weeks. For OCD: 25 mg daily with gradual increase to 100-250 mg/day. The maximum daily dose is 250 mg.
For nocturnal enuresis: 10-25 mg before bedtime; for OCD: 25 mg/day with increase up to 3 mg/kg body weight, but not more than 100 mg/day.
In renal or hepatic impairment, the initial dose is reduced to 10-25 mg/day with slow increases under physician supervision. In elderly patients, start at 10 mg/day.
Possible adverse reactions include:
Effects usually diminish with adaptation to the drug.
Doses above 500 mg may cause convulsions, coma, respiratory depression, arrhythmias, hypotension.
Stop taking, call an ambulance. Before the arrival of the doctor, the stomach is washed and activated charcoal is given. In case of injection overdose requires hospital treatment.
Anafranil enhances the effects of sedatives, anticholinergic drugs and alcohol. Co-administration with SSRIs may cause serotonin syndrome.
Alcohol enhances sedation and increases the risk of adverse reactions. Food decreases gastric irritation but does not affect absorption.
The drug is contraindicated in the first trimester of pregnancy; in the second and third trimesters only on strict indications. Clomipramine penetrates into milk, lactation is discontinued.
Driving and working with machinery are prohibited due to drowsiness and decreased concentration.
In the elderly, the dose is reduced due to the risk of side effects. In children use only when indicated from the lowest doses.