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Anafranil

Anafranil
Anafranil acts on depressive syndrome in general, incl. especially on such typical manifestations as psychomotor retardation, depressed mood and anxiety.

Brand: Clomipramine

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: September 2023
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Anafranil 75 mg
180 pills - 75 mg
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30 pills - 75 mg $80.99 $2.70 No Add to cart
Anafranil 50 mg
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Anafranil 25 mg
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Anafranil 10 mg
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Product description

Pharmacological action of Anafranil

Buy Anafranil in Canada

Antidepressant from the group of tricyclic compounds. The action of the drug is associated with the stimulation of adrenergic and serotonergic mechanisms in the central nervous system by inhibiting the reverse neuronal uptake of mediators. Mostly affects the seizure of serotonin; this, apparently, is due to its effectiveness in the treatment of obsessive-compulsive disorders. The antidepressant effect occurs relatively quickly (in the first week of treatment). It has adrenergic blocking (mainly alpha1), anticholinergic and antihistamine activity.

The psychostimulating effect of clomipramine is less pronounced than that of imipramine, and the sedative effect is weaker than that of amitriptyline.

Pharmacokinetics

Treatment of depression with anafranil

After oral administration or intramuscular administration, it is absorbed quickly and completely. Cmax in plasma is reached within 1.5-4 hours after oral administration. Plasma protein binding - 97.6%. Vd - 12 liters. It undergoes intensive metabolism with the formation of an active metabolite of desmethylclomipramine.

T1/2 in the final phase is 21 hours. It is excreted in the urine in the form of metabolites and unchanged substances, through the intestines - in the form of metabolites.

Indications for the active substances of Anafranil®

Depressive states of various etiologies (including endogenous, reactive, neurotic, organic, masked and involutional depressions); depressive syndrome in schizophrenia and personality disorders; presenile and senile depression; depressive conditions with prolonged pain syndrome and chronic somatic diseases; depressive disorders of a reactive, neurotic and psychopathic nature, including their somatic equivalents in children; obsessive-compulsive syndromes (phobia), panic attacks of fear, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pain in the face area, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathy), narcolepsy, narcolepsy, ; headache; prevention of migraine.

Dosage regimen

Packaging of Anafranil tablets

The method of administration and dosing regimen of a particular drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the used dosage form of a particular drug with indications for use and dosage regimen should be strictly observed.

Inside for adults - 25-50 mg 2-3 times / day; children, depending on age - 25-50 mg / day. Adults IM 25-100 mg / day, IV drip 50-75 mg 1 time / day.

Maximum doses: when taken orally by adults on an outpatient basis - 250 mg / day, in a hospital setting - 300 mg / day; children over 10 years old - 3 mg / kg / day, but not more than 200 mg / day.


Contraindications to use

Recent myocardial infarction, blockade of the myocardial conduction system, arrhythmias, mania, severe hepatic failure, angle-closure glaucoma, urinary retention, I trimester of pregnancy, lactation, hypersensitivity to clomipramine and other tricyclic antidepressants from the group of dibenzoazepine derivatives.

Application during pregnancy and lactation

Contraindicated for use in the first trimester of pregnancy. It should not be used in the II and III trimesters of pregnancy, except in cases of extreme necessity. There have been no adequate and well-controlled studies on the safety of clomipramine during pregnancy in humans.

Small amounts of clomipramine are excreted in breast milk, therefore, if necessary, use during lactation should decide whether to stop breastfeeding.

Application for violations of liver function

Contraindicated in severe hepatic failure.

Use with caution in severe liver disease.

Application for impaired renal function

Use withcaution in severe kidney disease.

Use in children

Not recommended for oral administration to children under 6 years of age, parenteral - to children under 12 years of age.

Special instructions

Use with caution in patients with a low seizure threshold; with severe liver or kidney disease; during treatment with steroid hormones; with pheochromocytoma and neuroblastoma due to the risk of developing a hypertensive crisis; with hyperthyroidism; diabetes mellitus (correction of the dosage regimen of hypoglycemic drugs is required).

Before starting treatment, it is necessary to control blood pressure, during treatment it is recommended to control the picture of peripheral blood, with prolonged therapy - to control the functions of the heart and liver.

Clomipramine can be used no earlier than 14 days after discontinuation of MAO inhibitors, starting therapy with a minimum dose. Should not be used simultaneously with sympathomimetic drugs, incl. with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine; with quinidine-like antiarrhythmic drugs. With the simultaneous use of clomipramine with alprazolam or disulfiram, a decrease in the dose of clomipramine is required.

Patients with a tendency to suicide in the initial period of treatment need constant medical supervision.

The use of electroshock while using clomipramine is possible only on strict indications and with close medical supervision.

With a sudden cessation of treatment, withdrawal syndrome may develop.

During the period of treatment, avoid alcohol consumption.

Not recommended for oral administration to children under 6 years of age, parenteral - to children under 12 years of age.

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, one should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug interactions

With simultaneous use with drugs that have a depressing effect on the central nervous system, a significant increase in the depressing effect on the central nervous system, hypotensive action, and respiratory depression is possible.

With simultaneous use with agents with anticholinergic activity, an increase in anticholinergic action is possible.

With the simultaneous use of clomipramine can reduce or completely eliminate the antihypertensive effect of antiadrenergic drugs that affect neuronal transmission of excitation (guanethidine, betanidine, reserpine, clonidine and alpha-methyldopa).

With simultaneous use with antipsychotics (neuroleptics), it is possible to increase the level of clomipramine in the blood plasma, reduce the threshold of convulsive readiness and develop seizures. The combination with thioridazine can lead to severe arrhythmias.

A decrease in the concentration of clomipramine in blood plasma due to the induction of microsomal liver enzymes under the action of barbiturates is possible.

With simultaneous use with MAO inhibitors, hypertensive crisis, hyperpyrexia, myoclonus, generalized convulsions, delirium and coma are possible.

With the simultaneous use of selective serotonin reuptake inhibitors (including fluoxetine and fluvoxamine), it is possible to enhance the effect on the serotonin system. Fluoxetine and fluvoxamine can increase the concentration of clomipramine in the blood plasma, which is accompanied by the development of corresponding side effects.

Clomipramine can enhance the effect on the cardiovascular system of adrenergic and sympathomimetic agents (epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine), including when these substances are combined with local anesthetics.

With simultaneous use with ademetionine, a case of the development of serotonin syndrome has been described; with sodium valproate - a case of increased plasma concentration of clomipramine and its metabolite desmethylclomipramine has been described.

There is a report of an increase in the concentration in blood plasma of clomipramine and its main metabolite (desmethylclomipramine) when used simultaneously with carbamazepine.

With simultaneous use with paroxetine, the plasma concentration of clomipramine of its metabolite S-desmethylclomipramine increases, apparently due to inhibition of the isoenzyme CYP2D6.

With simultaneous use with cimetidine, an increase in the concentration of clomipramine in the blood plasma is possible due to inhibition of microsomal liver enzymes under the influence of cimetidine.

A case of an increase in the concentration of clomipramine in the blood plasma is described, which is due to inhibition of CYP3A3 / 4 isoenzymes under the influence of erythromycin.

With simultaneous use with estrogens, a violation of the metabolism of clomipramine is possible.

The effect of ethanol may be enhanced, especially during the first few days of clomipramine therapy.


Side effect

From the side of the central nervous system: often - dizziness, fatigue, tremor, headache, myoclonus, visual impairment; rarely - disturbances in taste, fever, mydriasis, disorientation, hallucinations (most likely in elderly patients and with Parkinson's disease), anxiety, agitation, sleep disturbances, mania, hypomania, aggressiveness, memory impairments, depersonalization, yawning, nightmares , increased depression, impaired concentration, delirium, speech impairment, paresthesia, impaired muscle tone, tinnitus, convulsions, ataxia; in some cases - increased psychotic symptoms, glaucoma.

From the side of the cardiovascular system: rarely - postural hypotension, sinus tachycardia, ECG changes, palpitation, arrhythmias, increased blood pressure; in some cases - EEG changes, cardiac conduction disorders.

From the digestive system: often - nausea, dry mouth, constipation; rarely - vomiting, abdominal discomfort, diarrhea, anorexia, increased transaminase activity; in some cases - hepatitis, jaundice.

From the hematopoietic system: in some cases - leukopenia, agranulocytosis, thrombocytopenia, eosinophilia, thrombocytopenic purpura.

From the side of metabolism: often - increased appetite, weight gain.

From the endocrine system: often - violations of libido and potency, galactorrhea, enlargement of the mammary glands; in some cases - syndrome of inappropriate secretion of ADH, edema.

Dermatological reactions: rarely - photosensitization.

Allergic reactions: rarely - skin rash, itching.

Others: often - increased sweating; in some cases - an increase in body temperature.