Venlafaxine

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Venlafaxine

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Velafax pills are recommended to be taken orally, during a meal, preferably at the same time, without chewing and squeezing fluid.

For treatment of depressions, the recommended initial dose is 37.5 mg 2 times / day, daily. If after several weeks of treatment there is no significant improvement, the dose can be increased to 150 mg / day - 75 mg 2 times / day.

If necessary, the use of the drug in a higher dose in severe depressive disorder or other conditions requiring inpatient treatment, you can immediately appoint 75 mg 2 times / day. After that, the daily dose can be increased by 75 mg every 2-3 days until the desired therapeutic effect is achieved. The maximum daily dose of the drug Velafax is 375 mg. After achieving the desired therapeutic effect, the daily dose can be gradually reduced to the minimum effective level. Supportive therapy and prevention of relapse continues for 6 months or more. The drug is prescribed in the minimum effective dose used in the treatment of a depressive episode.

Adverse reactions

Most of the side effects listed below 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.

Frequency of side effects: very often (≥10%), often (≥1%, but

On the part of the digestive system: often - loss of appetite, constipation, nausea, vomiting, dry mouth, dyspepsia, abdominal pain; infrequently - bruxism, increased activity of hepatic transaminases; rarely, hepatitis; in some cases, pancreatitis.

On the part of the metabolism: often - an increase in serum cholesterol level (especially after long-term intake or administration of the drug in high doses), a decrease or increase in body weight; infrequently - hyponatremia, syndrome of insufficient secretion of antidiuretic hormone (ADH); in some cases - an increase in the level of prolactin in blood plasma.

Since the cardiovascular system: often - increased blood pressure, redness of the skin; infrequently - decrease in blood pressure, postural hypotension, syncope, arrhythmia, tachycardia; very rarely - pirouette-type arrhythmia, prolongation of the QT interval, ventricular tachycardia, ventricular fibrillation.

On the part of the central nervous system and peripheral nervous system: often - dizziness, asthenia, nightmares, weakness, dizziness, insomnia, drowsiness, increased nervous irritability, paresthesias, stupor, muscle hypertonia, tremor, yawning, sedation; infrequently - apathy, hallucinations, myoclonus, syncope; seldom - convulsions, ataxia with impaired balance and coordination of movement, impaired speech, mania or hypomania, serotonin syndrome, symptoms resembling malignant neuroleptic syndrome, epileptic seizures; in some cases - delirium, extrapyramidal disorders, incl. dyskinesia and dystonia, tardive dyskinesia, psychomotor anxiety / akathisia.

From the side of mental status: frequency not established - depression, the appearance of suicidal thoughts and suicidal behavior during therapy and after discontinuation of the drug.

On the part of the hematopoietic system and the lymphatic system: infrequently - hemorrhages into the skin (ecchymosis) and mucous membranes, thrombocytopenia, prolonged bleeding time, hemorrhagic syndrome; in some cases - agranulocytosis, aplastic anemia, neutropenia and pancytopenia.

From the urinary system: often - urination disorders; infrequently - urinary retention.

On the part of the reproductive system: often - decreased libido, erectile dysfunction and / or ejaculation, anorgasmia in men, menorrhagia; infrequently - violation of the menstrual cycle, anorgasmia in women.

On the part of the senses: often - accommodation disturbances, mydriasis, visual disturbances, noise or tinnitus; infrequently - violations of taste sensations.

On the part of the skin and its appendages: often - excessive sweating (including night); infrequently - alopecia.

On the part of the respiratory system: infrequently - shortness of breath; in some cases - pulmonary eosinophilia.

On the part of the endocrine system: rarely - galactorrhea; in some cases - increased levels of prolactin.

Allergic reactions: infrequently - skin rash (including maculo-papular), pruritus, photosensitization, angioedema, urticaria; rarely erythema multiforme exudative, Stevens-Johnson syndrome; in some cases - anaphylactic reactions.

From the musculoskeletal system: often - arthralgia, myalgia; infrequently - muscle spasms; in some cases - rhabdomyolysis.

After abrupt cancellation of venlafaxine or dose reduction, increased fatigue, drowsiness, asthenia, headache, nausea, vomiting, anorexia, dry mouth, dizziness, diarrhea, insomnia, unusual dreams, difficulty falling asleep, anxiety, anxiety, irritability and emotional lability, anatomy, difficulty in falling asleep, anxiety, anxiety, irritability and emotional lability, anesthesia, difficulty falling asleep, anxiety, anxiety, irritability and emotional lability, math , confusion, disorientation, hypomania, tremor, paresthesias, excessive sweating, tachycardia, convulsions, ringing or tinnitus, refusal of food. To prevent the development of symptoms of withdrawal syndrome, it is very important to gradually reduce the dose of the drug, especially after taking it in high doses.

Contraindications

- pronounced impaired renal function (CC less than 10 ml / min) and / or liver;

- children's and teenage age up to 18 years;

- pregnancy;

- lactation period (breastfeeding);

- simultaneous administration of MAO inhibitors;

- individual intolerance to venlafaxine and other components of the drug.

Precautions to apply in case of recent myocardial infarction, unstable angina, hypertension, tachycardia, convulsive syndrome history, elevated intraocular pressure, angle-closure glaucoma, manic state history, hyponatremia, hypovolemia, dehydration, simultaneous administration of diuretics, suicidal tendencies, predisposition to bleeding (on the part of the skin and mucous membranes), with initially reduced body weight.

Drug interactions

The simultaneous use of MAO inhibitors and venlafaxine contraindicated. Reception venlafaksina can begin no earlier than 14 days after the end of therapy with MAO inhibitors. If a reversible MAO inhibitor (moccobemide) was used, this interval may be shorter (24 hours). Therapy with MAO inhibitors can be started no earlier than 7 days after the abolition of venlafaxine.

With simultaneous use of venlafaxine with lithium preparations may increase the level of lithium in the blood.

When applied simultaneously with imipramine, the pharmacokinetics of venlafaxine and its EFA metabolite do not change. Venlafaxine does not affect the metabolism of imipramine and its metabolite 2-hydroxyimipramine, however, it increases the value of AUC and Cmax in the plasma of desipramine (the main metabolite of imipramine), and also reduces the renal clearance of 2-hydroxydesipramine. The clinical significance of this phenomenon is unknown.

With simultaneous use with neuroleptics, the appearance of symptoms resembling a malignant neuroleptic syndrome may occur.

Venlafaxine reduces the renal clearance of haloperidol by 42%, while the AUC and Cmax values ​​increase by 70% and 88%, respectively. Haloperidol effects may be enhanced.

With simultaneous use with diazepam pharmacokinetics of drugs and their major metabolites are not significantly changed.

With simultaneous use with clozapine, an increase in its blood plasma level and the development of side effects (for example, epileptic seizures) can be observed.

With simultaneous use with risperidone, despite an increase in the AUC of the drug, the pharmacokinetics of the sum of the active components (risperidone and its active metabolite) did not change significantly.

The simultaneous use of ethanol and venlafaxine was not accompanied by a decrease in mental and physical activity. Despite this (as in the case of taking other drugs that affect the central nervous system), ethanol use is not recommended during venlafaxine therapy.

Cimetidine inhibits venlafaxine metabolism during the "first pass" through the liver and has no effect on the pharmacokinetics of EFA. In the majority of patients, only a slight increase in the total pharmacological activity of venlafaxine and EFA is expected (more pronounced in elderly patients and in impaired liver function). In elderly patients and in patients with impaired liver function, simultaneous use of cimetidine and venlafaxine should be carried out under medical supervision.

No clinically significant interaction of venlafaxine with antihypertensive drugs (including beta-blockers, ACE inhibitors and diuretics) and hypoglycemic drugs was detected.

Since the binding of plasma proteins venlafaxine and EFA is respectively 27% and 30%, drug interactions due to the competitive release of other drugs from plasma proteins are not expected.

Venlafaxine metabolism occurs with the participation of the cytochrome P450 system, CYP2D6 and CYP3A4 isoenzymes. Taking the drug with CYP2D6 isoenzyme inhibitors or patients with a genetically determined decrease in the activity of the CYP2D6 isoenzyme was not accompanied by significant changes in the concentration of the active substance and metabolite (venlafaxine and EFA), which allows not to reduce the dose of antidepressant. However, simultaneous administration with CYP3A4 isoenzyme inhibitors is accompanied by an increase in plasma venlafaxine concentration. Therefore, special care should be taken when prescribing venlafaxine with drugs that are inhibitors of the CYP3A4 isoenzyme (ketoconazole, erythromycin) or both isoenzymes (CYP2D6 and CYP3A4).

Venlafaxine is a relatively weak inhibitor of the isoenzyme CYP2D6 and does not inhibit the activity of the isoenzymes CYP1A2, CYP2C9 and CYP3A4. In vivo studies did not reveal the effect of venlafaxine on the metabolism of alprazolam (CYP3A4 isoenzyme), caffeine (CYP1A2 isoenzyme), carbamazepine (CYP3A4 isoenzyme) and diazepam (CYP3A4 and CYP2C19 isoenzymes).

With simultaneous use with warfarin, it is possible to enhance the anticoagulant effect of the latter, while the prothrombin time, expressed through MHO, is prolonged.

When taken simultaneously with indinavir, there is a decrease in the AUC value of indinavir by 28% and a decrease in its plasma Cmax by 36%, while the pharmacokinetic parameters of venlafaxine and EFA do not change. The clinical significance of this effect is unknown.

Venlafaxine can affect the pharmacodynamics of other drugs acting at the level of the serotonergic neurotransmitter system, so care should be taken when it is given simultaneously with triptans, other selective serotonin reuptake inhibitors and lithium drugs.

Pregnancy and Lactation

Special instructions

Overdosage