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Active ingredients
Venlafaxine
Release form
Pills
Composition
1 tab. venlafaxine (in the form of hydrochloride) 75 mg. Excipients: anhydrous calcium hydrophosphate, anhydrous lactose, sodium carboxymethyl starch, magnesium stearate, anhydrous colloidal silicon dioxide, iron dye, red oxide (E172).
Pharmacological effect
Antidepressant. According to the chemical structure, venlafaxine does not belong to any class of antidepressants (tricyclic, tetracyclic or other), it is a racemate of two active enantomers. The mechanism of antidepressant action of the drug is associated with its ability to potentiate the transmission of nerve impulses to the central nervous system. Venlafaxine and its major metabolite O-desmethylvenlafaxine (EFA) are strong inhibitors of serotonin and noradrenaline reuptake and weak dopamine reuptake inhibitors. In addition, venlafaxine and EFA reduce beta-adrenergic reactivity, both after a single injection, and with continuous use. Venlafaxine and EFA equally effectively affect the reuptake of neurotransmitters. Venlafaxine has no affinity for the m-cholinergic receptors, histamine H1 receptors and the & # 945 .1-adrenergic receptors of the brain. Venlafaxine does not inhibit the activity of MAO. It has no affinity for opioid, benzodiazepine, phencyclidine or NMDA receptors.
Indications
- Depression of various etiologies (treatment and prevention).
Contraindications
- severe renal dysfunction (GFR less than 10 ml / min) - severe liver dysfunction - simultaneous administration of MAO inhibitors - age up to 18 years (safety and efficacy for this category of patients has not been proven) - established or suspected pregnancy - lactation period (breastfeeding ) - hypersensitivity to the drug. The drug should be prescribed with caution in recent myocardial infarction, unstable angina, arterial hypertension, tachycardia, a history of seizures, elevated intraocular pressure, angle-closure glaucoma, a history of manic, a predisposition to the bleeding of the arteries, and I amymptomatic, I amymptomatic, myocardial infarction; body, hyponatremia, hypovolemia, concomitant use of diuretics, suicidal tendencies,renal or hepatic failure.
Use during pregnancy and lactation
The safety of venlafaxine in pregnancy has not been proven, therefore the use of the drug in pregnancy (or presumptive pregnancy) is contraindicated. Women of childbearing age should be warned about this before starting treatment and should immediately consult a doctor if pregnancy occurs or pregnancy planning during the period of drug treatment. Women of childbearing age should use appropriate methods of contraception while taking venlafaxine. If the mother’s treatment was completed shortly before delivery, the newborn may experience withdrawal symptoms. Venlafaxine and its EFA metabolite are excreted in breast milk. The safety of these substances for newborns has not been proven, so taking venlafaxine during breastfeeding is not recommended. If necessary, taking the drug during lactation should decide on the termination of breastfeeding.
Side effects
Most side effects are dose dependent. With prolonged treatment, the severity and frequency of most of these effects is reduced, and there is no need to cancel therapy. Determination of the frequency of side effects: often (> 1%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%). From the side of the central nervous system: often - dizziness, asthenia, insomnia, nightmares, increased nervous irritability, paresthesia, hypertonic muscle, tremor, sedation. infrequently - apathy, hallucinations, myoclonus, syncope. rarely - convulsions, manic disorders, ZNS. Since the cardiovascular system: often - increased blood pressure, skin hyperemia. infrequently - decrease in blood pressure, postural hypotension, tachycardia. very rarely - a change in the QT interval, ventricular fibrillation, ventricular tachycardia (including ventricular fibrillation). On the part of the digestive system: often - loss of appetite, nausea, vomiting. infrequently - bruxism (involuntary grinding of teeth), increased activity of hepatic transaminases. rarely - hepatitis. On the part of the urinary system: often - a violation of urination. infrequently - urinary retention. On the part of the reproductive system: often - decreased libido, erectile dysfunction and / or ejaculation, anorgasmia, menorrhagia. infrequently - a violation of orgasm in women.On the part of the senses: often - disturbance of accommodation, mydriasis, blurred vision. infrequently - a violation of taste perception. On the part of the hematopoietic system: the frequency is unknown - agranulocytosis, aplastic anemia, neutropenia, pancytopenia. Allergic reactions: infrequently - rash, photosensitization. very rarely - erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylaxis. Laboratory indicators: infrequently - thrombocytopenia. rarely, increased bleeding time, hyponatremia. with prolonged administration and use in high doses - hypercholesterolemia. Other: often - loss of body weight, sweating (including night). infrequently - ecchymosis, weight gain. rarely - inadequate secretion syndrome ADH, serotonin syndrome (nausea, vomiting, abdominal pain, diarrhea, flatulence, psychomotor agitation, tachycardia, hyperthermia, muscle rigidity, convulsions, myoclonus, sweating, depression of consciousness of varying severity). If withdrawal occurs: dizziness, headache, asthenia, fatigue, sleep disturbances (changing the nature of dreams, drowsiness or insomnia, difficulty falling asleep), hypomania, anxiety, increased nervous irritability, confusion, paresthesia, increased sweating, dry mouth, loss of appetite, nausea, vomiting, diarrhea (most of these reactions are mild and do not require treatment).
special instructions
Most side effects are dose dependent. With prolonged treatment, the severity and frequency of most of these effects is reduced, and there is no need to cancel therapy. Determination of the frequency of side effects: often (> 1%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%). From the side of the central nervous system: often - dizziness, asthenia, insomnia, nightmares, increased nervous irritability, paresthesia, hypertonic muscle, tremor, sedation. infrequently - apathy, hallucinations, myoclonus, syncope. rarely - convulsions, manic disorders, ZNS. Since the cardiovascular system: often - increased blood pressure, skin hyperemia. infrequently - decrease in blood pressure, postural hypotension, tachycardia. very rarely - a change in the QT interval, ventricular fibrillation, ventricular tachycardia (including ventricular fibrillation).On the part of the digestive system: often - loss of appetite, nausea, vomiting. infrequently - bruxism (involuntary grinding of teeth), increased activity of hepatic transaminases. rarely - hepatitis. On the part of the urinary system: often - a violation of urination. infrequently - urinary retention. On the part of the reproductive system: often - decreased libido, erectile dysfunction and / or ejaculation, anorgasmia, menorrhagia. infrequently - a violation of orgasm in women. On the part of the senses: often - disturbance of accommodation, mydriasis, blurred vision. infrequently - a violation of taste perception. On the part of the hematopoietic system: the frequency is unknown - agranulocytosis, aplastic anemia, neutropenia, pancytopenia. Allergic reactions: infrequently - rash, photosensitization. very rarely - erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylaxis. Laboratory indicators: infrequently - thrombocytopenia. rarely, increased bleeding time, hyponatremia. with prolonged administration and use in high doses - hypercholesterolemia. Other: often - loss of body weight, sweating (including night). infrequently - ecchymosis, weight gain. rarely - inadequate secretion syndrome ADH, serotonin syndrome (nausea, vomiting, abdominal pain, diarrhea, flatulence, psychomotor agitation, tachycardia, hyperthermia, muscle rigidity, convulsions, myoclonus, sweating, depression of consciousness of varying severity). If withdrawal occurs: dizziness, headache, asthenia, fatigue, sleep disturbances (changing the nature of dreams, drowsiness or insomnia, difficulty falling asleep), hypomania, anxiety, increased nervous irritability, confusion, paresthesia, increased sweating, dry mouth, loss of appetite, nausea, vomiting, diarrhea (most of these reactions are mild and do not require treatment).