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What is Venlafaxine
Venlafaxine - an antidepressant with a new chemical structure that can not be attributed to tricyclic, tetracyclic or other known antidepressants. It is a racemic mixture of two active enantiomers. The mechanism of antidepressant effect of venlafaxine is associated with increased neurotransmitter activity of CNS. Venlafaxine and its major metabolite O-desmethyl venlafaxine (EFA) are potent inhibitors of the reverse of neuronal serotonin and norepinephrine, as well as inhibit the reuptake of dopamine. In addition, both single and prolonged administration of venlafaxine and EFA reduces ?-adrenergic response. They are equally effective influence on the reuptake of neurotransmitters.
Venlafaxine 37,5 mg
| Package | Price | Per Pill | Savings | Order |
| 37,5 mg × 30 pills | $ 42.99 | $ 1.42 | $ 0.00 |  |
| 37,5 mg × 60 pills | $ 71.99 | $ 1.20 | $ 13.20 | |
| 37,5 mg × 90 pills | $ 95.99 | $ 1.07 | $ 31.50 | |
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| 37,5 mg × 180 pills | $ 157.99 | $ 0.88 | $ 97.20 | |
| 37,5 mg × 240 pills | $ 201.99 | $ 0.84 | $ 139.20 | |
| 37,5 mg × 360 pills | $ 291.99 | $ 0.81 | $ 219.60 | |
Venlafaxine 75 mg
| Package | Price | Per Pill | Savings | Order |
| 75 mg × 10 pills | $ 23.99 | $ 2.40 | $ 0.00 | |
| 75 mg × 30 pills | $ 59.99 | $ 2.00 | $ 12.00 | |
| 75 mg × 60 pills | $ 104.99 | $ 1.75 | $ 39.00 | |
| 75 mg × 90 pills | $ 144.99 | $ 1.61 | $ 71.10 | |
| 75 mg × 120 pills | $ 180.99 | $ 1.51 | $ 106.80 | |
| 75 mg × 180 pills | $ 242.99 | $ 1.35 | $ 189.00 | |
| 75 mg × 240 pills | $ 306.99 | $ 1.28 | $ 268.80 | |
| 75 mg × 360 pills | $ 445.99 | $ 1.24 | $ 417.60 | |
Venlafaxine does not inhibit MAO activity. Venlafaxine has no affinity for opiate, benzodiazepine, fentsiklidinovym or N-methyl-d-aspartate (NMDA) receptors, and he also has no effect on noradrenaline release from brain tissue. Repeated use of the drug equilibrium concentrations of venlafaxine and its only active metabolite in plasma are attained within 3 days. Venlafaxine and EFA has linear pharmacokinetics at total daily doses ranging from 75 to 450 mg. Absorption of venlafaxine after receiving a single dose of the drug intake is nearly 92%, absolute bioavailability - about 45%. After application of capsules with prolonged action Velaksina maximum concentrations of venlafaxine and its active metabolite in plasma EFA levels are reached approximately for 6 and 8 h, respectively. The rate of absorption of venlafaxine released from sustained-release capsules, less than the rate of its elimination. Therefore, the average half-life of venlafaxine from the body after oral administration (15 ± 6 h) is actually a half-life of absorption phase, instead of half-life in distribution phase (5 ± 2 h), which is observed after the use of tablets. After application in equivalent doses of venlafaxine in the form of tablets or capsules in the form of sustained-release venlafaxine AUC exposure and EFA were similar when using both formulations, and their concentration in plasma was slightly lower after the use of venlafaxine in capsule form. Thus, the sustained-release capsules provide slower absorption, but the same degree of absorption (ie, AUC), and that venlafaxine tablets. Venlafaxine is extensively metabolized during the initial passage through the liver, mainly with the participation of CYP 2D6, with the formation of the main metabolite of EFA. He also is metabolized to N-desmethyl venlafaxine, and some other metabolites with the participation of CYP 3A3 / 4. Venlafaxine and its metabolites are distinguished primarily by the kidneys. About 78% of the dose of venlafaxine is determined in the urine over 48 hours as unchanged venlafaxine, unconjugated EFA EFA or conjugated other metabolites. In renal and liver failure half-lives of venlafaxine and its active metabolite EFA increased. Acceptance means the food has no effect on the absorption of venlafaxine and further education for EFA. Age and sex of the patient does not affect its pharmacokinetics. Venlafaxine does not accumulate in the body. Capsules contain venlafaxine sustained release microspheres, which are entering the gastrointestinal tract, slowly release the active ingredient. The insoluble part of these microspheres appears to kalom.bolee prolonged analgesic effect than antidepressants, which affect only one of the aminergic systems.
INDICATIONS:
- - depression (in the presence or absence of symptoms of anxiety), outpatient or inpatient treatment;
- - Prevention of recurrence after a first episode of depression or the prevention of new relapses;
- - Generalized anxiety disorder;
- - Social anxiety disorder (social phobia).
APPLICATION:
The capsules should be taken during the entire meal with liquid. Capsules can not divide, crush, chew or dissolve. The daily dose should be taken in one sitting (morning or evening) at the same time.
Depression
The recommended dose is 75 mg / day in one sitting.
When taking into account the course of the disease, a higher dose, such as major depression or inpatient treatment the patient may be recommended initial dose of 150 mg / day in one go. After that, the daily dose can be increased at intervals 37,5-75 mg ? 2 weeks, but not less than 4 days to reach the necessary therapeutic effect. The maximum recommended dose is 225 mg venlafaxine / day with moderate depression, and 350 mg - with major depression. After reaching the desired therapeutic effect, dosage should be gradually reduced to the minimum effective, taking into account individual response and tolerability for each patient. When used in high doses increases the risk of side effects of the drug.
Generalized anxiety disorder and social anxiety disorder (social phobia)
The recommended dose of venlafaxine, 75 mg / day in one sitting.
If after 2 weeks of treatment, not a noticeable improvement in the daily dose can be increased to 150 mg / day in one sitting. When used in a daily dose of 75 mg anxiolytic effect noted after 1 week.
Prevention of recurrences or new episodes
The efficiency of venlafaxine in long-term therapy (up to 12 months for depression and social phobia, and 6 months for generalized anxiety disorder). Treatment of acute episodes of depression should continue for at least 6 months.
Dose commonly used for prevention of recurrence or new episode, similar to doses that are used to treat patients with a primary episode. Should be regularly (at least 1 time in 3 months) to examine the patient for monitoring the effectiveness of long-term therapy venlafaxine.
The transfer of patients treated with venlafaxine in the form of tablets, to receive the drug in capsules
Depressed patients receiving venlafaxine tablets at a therapeutic dose can be transferred to the reception means in the form of sustained-release capsules to the appointment of the nearest equivalent dose. Sometimes an individual may need a dosage adjustment.
Renal failure
When the glomerular filtration rate 30 ml / min dose adjustment is required. When the glomerular filtration rate of 10-30 ml / min the dose should be reduced by 50%. Due to the increasing half-life of venlafaxine and its active metabolite in these patients, the daily dose should be taken in one sitting.
Not recommended for venlafaxine in the glomerular filtration rate ? 10 mL / min, since the data to conduct therapy in these patients is not enough.
Patients on hemodialysis, the daily dose should be reduced by 50% and the ability to apply after the completion of hemodialysis.
Hepatic failure
Mild hepatic insufficiency (prothrombin time ? 14 s), dose adjustment is required. With moderate hepatic insufficiency (prothrombin time - 14-18 s) the dose should be reduced by 50%. Venlafaxine is not recommended for use in severe hepatic insufficiency (prothrombin time 18 s), since the data on this therapy is not enough.
Elderly patients
Caution must be exercised in the appointment of elderly patients (because of the possibility of renal dysfunction), and the drug is prescribed in the lowest effective dose. With increasing dose the patient should be under regular medical supervision.
Cancel venlafaxine
The abrupt cessation of therapy, venlafaxine, especially after taking the drug at high doses, can cause the development of withdrawal symptoms, and therefore before the full withdrawal of the drug recommended a gradual reduction in dose. If the drug is used in high doses for 6 weeks is recommended during dose reduction of at least 2 weeks. The length of time required for dose reduction depends on the dose, duration of therapy, as well as on the individual sensitivity of the patient.
CONTRAINDICATIONS:
Hypersensitivity to venlafaxine. The simultaneous use of any antidepressant group of MAO inhibitors, as well as for 14 days after discontinuation of irreversible MAO inhibitors. After the complete withdrawal of venlafaxine therapy, MAO inhibitors can begin no earlier than 7 days. Diseases of the cardiovascular system (heart failure, coronary artery disease, ECG changes - the earlier increase in the Q-T interval on an electrocardiogram), hypertension, electrolyte imbalance. Age 18. During pregnancy and lactation.
SIDE EFFECTS:
Side effects are divided by body system and frequency of occurrence: very common (1 / 10), often (? 1 / 10, but 1 / 100), sometimes (? 1 / 100, but 1 / 1000), rarely (? 1 / 1000), very rare (? 1 / 10, 000). Common symptoms are: very common - fatigue, headache, and often - abdominal pain, chills, fever, rare - anaphylaxis. GI: very often - constipation, nausea, and often - loss of appetite, diarrhea, vomiting and sometimes - bruxism, reversible increases in liver enzymes, rare - gastrointestinal bleeding is very rare - pancreatitis. Cardiovascular System: Frequent - tachycardia, hypertension, vasodilation, and sometimes - hypotension / orthostatic hypotension, loss of consciousness, arrhythmias, tachycardia, very rarely - tachycardia type "pirouette", increasing the Q-T interval on the ECG, ventricular tachycardia, ventricular fibrillation. Respiratory System: Frequent - respiratory failure, yawn, very rarely - eosinophilic infiltrates in the lungs. Nervous system: Very common - dizziness, dry mouth, insomnia, anxiety, drowsiness, and often - abnormal dreams, agitation, anxiety, confusion, increased muscle tone, paresthesia, tremor, and sometimes - apathy, hallucinations, myoclonus, rare - with ataxia impaired balance and coordination, speech impairment, including dysarthria, mania or hypomania, as well as manifestations that resemble neuroleptic malignant syndrome (NMS), seizures, serotonergic syndrome are very rare - delirium, extrapyramidal disorders, including dyskinesias and dystonia, psychomotor agitation / akathisia. Urogenital: very often - anorgasmia, erectile dysfunction, impaired ejaculation and orgasm, and often - frequent urination, decreased libido, menstrual disorders, and sometimes - urinary retention, menorrhagia, rarely - galactorrhea. Special Senses: Frequent - blurred vision and accommodation, mydriasis, noise, and ringing in the ears, and sometimes - change in taste. Skin: very often - sweating, and often - a skin rash and itching, and sometimes - angioedema, maculopapular rash, urticaria, photosensitivity, alopecia, rarely - erythema multiforme, Stevens - Johnson. Blood system: sometimes - ecchymosis, bleeding from mucosa, rarely - increased bleeding time, bleeding, thrombocytopenia is very rare - agranulocytosis, aplastic anemia, neutropenia, pancytopenia. Metabolism: often - increasing the cholesterol level in blood serum, the increase or decrease in body weight, and sometimes - hyponatremia, elevated liver enzymes, rarely - hepatitis very rarely - increased prolactin levels. Musculoskeletal system: common - arthralgia, myalgia, and sometimes - muscle cramps, very rarely - rhabdomyolysis. Precautions: patients with depressive state before beginning any therapy must take into account the likelihood of suicide attempts. Therefore, to reduce the risk of an overdose of the initial dose should be as low, and the patient - to be under medical supervision. Reported aggressive behavior in a patient during use of venlafaxine (especially at the beginning of treatment and after discontinuation of the drug). The use of venlafaxine is associated with the development of psychomotor agitation, which is characterized by a subjectively unpleasant concern with the need to move. Most often this occurs during the first weeks of treatment. If you experience these symptoms should not increase the dose, so you must decide whether to continue receiving venlafaxine. Patients with affective disorders during treatment with antidepressants, including venlafaxine, may have hypomanic or manic state. Velaksin should be prescribed with caution in patients with a history of mania. These patients need medical supervision. Velaksin with caution in patients with indications of epileptic seizures in history. If you have seizures treatment should be stopped. Patients should be warned of the need to immediately contact a doctor if you experience skin rash, hives or other elements of the allergic reactions. Some patients in the use of venlafaxine may increase blood pressure dose-dependent, and therefore it is recommended to monitor blood pressure regularly, especially during the adjustment or increase the dose. May increase heart rate, especially when taken in high doses. In this case, medical supervision of the patient. Occasionally during treatment reported orthostatic hypotension. Patients, especially elderly, should be warned of the possibility of dizziness. Venlafaxine may increase the risk of bleeding into the skin and mucous membranes in patients predisposed to these conditions. Patients should be alert about this and recommend caution during treatment. During the application of venlafaxine, especially in dehydration or reduction of the bcc (including elderly patients and patients taking diuretics), it is possible hyponatremia and / or syndrome of insufficient secretion of antidiuretic hormone. During the application of funds may occur mydriasis, and therefore recommended for control of intraocular pressure in patients with a penchant for improving it, and takzhes narrow-angle glaucoma. When treating patients with impaired renal function or liver caution and careful medical monitoring of patients (possibly reducing the dose). Patients with recent myocardial infarction, with signs of decompensated heart failure, the drug should be used with caution under constant medical supervision. Safety and efficacy of combined use of venlafaxine and drugs used for weight reduction, including phentermine, have not been established, so that their simultaneous use is not recommended. In the long-term treatment facilities to carry out appropriate control cholesterol levels in blood serum. After discontinuation of venlafaxine, especially a sudden, often there is a withdrawal syndrome. The risk of developing withdrawal symptoms depends on the duration of treatment, the dose and rate of its decline. When withdrawal syndrome appear dizziness, paresthesia, sleep disturbances, agitation, anxiety, nausea, vomiting, tremors, sweating, headache, diarrhea, tachycardia, emotional disorders. These symptoms usually occur during the first days after drug withdrawal and are alone for 2 weeks. Therefore, reception facilities should be lifted gradually, reducing the dose of venlafaxine gradually over several weeks or months, depending on the patient's condition. Venlafaxine did not cause the development of phenomena of tolerance or dependence. Despite this, as in the treatment of other means of acting on the CNS, patients should be monitored for signs of abuse of venlafaxine (especially in patients with similar issues in history). During the application of venlafaxine women of childbearing age should use adequate contraception. Venlafaxine may affect the ability to drive vehicles and working with potentially dangerous machinery. Therefore, the doses at which may drive vehicles and operate machinery, is determined for each patient.
CONTRAINDICATIONS:
The simultaneous use of any antidepressant group of MAO inhibitors, as well as for 14 days after discontinuation of irreversible MAO inhibitors. After the complete withdrawal of venlafaxine therapy, MAO inhibitors can begin no earlier than 7 days. Diseases of the cardiovascular system (heart failure, coronary artery disease, ECG changes - the earlier increase in the Q-T interval on an electrocardiogram), hypertension, electrolyte imbalance. Age 18. During pregnancy and lactation.
INTERACTION:
Venlafaxine is contraindicated in application combined with MAO inhibitors: in this case may mark the tremor, myoclonus, sweating, nausea, vomiting, sensation of flushing, dizziness, fever, seizures, death. The use of venlafaxine may begin no earlier than 14 days after therapy MAO inhibitor. In the case of a reversible inhibitor of MAO, this interval may be shorter (24 h). After the abolition of venlafaxine should be a break of at least 7 days before treatment MAO inhibitors. Special caution is required when applying venlafaxine with drugs affecting the central nervous system. Should take into account the mutual influence of venlafaxine and such drugs: Lithium: There are reports of interaction between lithium and venlafaxine, resulting in the level of lithium in the blood. Imipramine: Venlafaxine pharmacokinetics and its metabolite, EFA does not change, thus reducing the dose of venlafaxine in the combined use of these drugs is not required. Haloperidol: its effect may be enhanced. Diazepam: pharmacokinetics of drugs and their major metabolites did not substantially change. Clozapine: marked increase in clozapine levels and the development of its side effects (eg seizures). Risperidone: the simultaneous use of these funds (despite the increase in AUC of risperidone), the pharmacokinetics of the amount of active ingredients (risperidone and its active metabolite) did not substantially change. Alcohol: inhibition of psychomotor activity under the influence of alcohol after taking venlafaxine does not increase, but the period of its application to consume alcoholic beverages is not recommended. Electroconvulsive therapy: during electroconvulsive therapy in patients receiving selective inhibitors of neuronal serotonin reuptake back marked increase in the duration of epileptic activity. Care should be taken to provide close medical supervision of the patient in the combined holding of this type of therapy and the use of venlafaxine. Medications metabolized by cytochrome P450 isoenzymes: CYP 2D6 enzyme cytochrome P450 converts the active metabolite of venlafaxine in EFA. Unlike many other antidepressants dose of venlafaxine can not cut a single application with drugs that inhibit the activity of CYP 2D6, or in patients with genetically determined decreased activity of CYP 2D6, since the total concentration of the active substance and metabolites (venlafaxine and EFA) remains unchanged. The main mode of excretion of venlafaxine include metabolism involving CYP 2D6 and CYP 3A4, and therefore should be particularly careful in the appointment of venlafaxine in combination with drugs, depressing both the enzyme. Venlafaxine - a relatively weak inhibitor of CYP 2D6 and does not inhibit the activity of the isoenzymes CYP 1A2, CYP 2C9 and CYP 3A4; should not be expected to interact with other drugs, the metabolism of which are involved, these liver enzymes. Cimetidine: inhibits metabolism of venlafaxine in its initial passage through the liver, but has no significant effect on its transformation into an EFA or EFA rate of elimination, concentration in the circulating blood is much higher. Therefore, there is no need to change the dose of venlafaxine and cimetidine in their combined use. This interaction may be more pronounced in patients who are elderly or with abnormal liver function, so in such cases, the combined use of cimetidine and venlafaxine requires medical supervision. Antihypertensive and antidiabetic agents: no clinically significant interactions with antihypertensive venlafaxine (including ?-blockers, blockers, ACE inhibitors and diuretics), and hypoglycemic agents. Drugs that bind to plasma proteins: binding to plasma proteins is 27% for venlafaxine and 30% - for EFA. Therefore we should not expect the interactions due to their binding with proteins. Warfarin: anticoagulant effect of the latter may be intensified, with increased prothrombin time. Indinavir: while the use of this tool changes the pharmacokinetics of indinavir (28% decrease in AUS and 36% reduction in the maximum concentration). Symptoms: ECG changes (increase in the interval Q-T, block bundle-branch block, the expansion of the complex QRS), sinus and ventricular tachycardia, bradycardia, hypotension, seizures, impaired consciousness. In some cases, the reported lethal outcome due to overdose when venlafaxine at high doses, taken with alcohol and / or other psychotropic drugs. Treatment: No specific antidote. Shown the use of gastric lavage and activated charcoal. Induce vomiting is not recommended. Necessary to ensure adequate airway, adequate ventilation and oxygenation. We recommend monitoring of ECG and vital body functions, as well as carrying out maintenance and supportive care. In case of overdose should consider the possibility of simultaneous reception of multiple psychotropic medications the patient. Venlafaxine and EFA are not displayed during dialysis.
The use of antidepressants in chronic pain
Major depressive disorder and generalized anxiety disorder is often accompanied by chronic pain syndromes. Examples of these syndromes may be back pain, headache, pain in the gastrointestinal tract and joint pain. In addition, the great difficulty of treatment and represent the number of pain syndromes are not associated with depressive and anxiety disorders (diabetic and post-herpetic neuralgia, cancer pain, fibromyalgia). The relationship between major depressive disorder and generalized anxiety disorder with painful and not painful somatic symptoms was noted by clinicians for a long time. In one international study has shown that during the initial examination, 69% of patients with major depressive disorder have had only somatic complaints, and they did not have any psychopathological symptoms. In another study showed that increasing the number of physical symptoms increases the likelihood of the patient's depression or anxiety. In addition to major depression and generalized anxiety disorder, pain is one of the major complaints in fibromyalgia, irritable bowel syndrome, chronic pelvic pain, migraines, vulvodynia, interstitial cystitis, the symptoms of TMJ. Some researchers suggest that such violations of the affective spectrum, as major depressive disorder, generalized anxiety disorder, social phobias, fibromyalgia, irritable bowel syndrome and migraine may have a common genetic predisposition. The exact causal relationship between chronic pain and depression remains unknown, but put forward the following hypotheses: depression precedes the development of chronic pain, depression is the result of chronic pain, episodes of depression occurring before the start of chronic pain, predispose to the development of depressive episodes after the onset of chronic pain, psychological factors such as maladaptive coping strategies that promote the formation of the interaction between depression and chronic pain, depression and pain have similar characteristics, but represent different disorders. Numerous studies have shown that antidepressants double action (selective serotonin reuptake inhibitors - SSRIs and noradrenaline), used to treat depression, may also be effective in treating chronic pain. Double-acting drugs such as tricyclic antidepressants (amitriptyline, clomipramine) and venlafaxine, or a combination of antidepressants with serotonergic and noradrenergic effects, have demonstrated efficacy bolshuyu treatment compared with antidepressant acting primarily on a single neurotransmitter system. For example, fluoxetine (at the expense of pre-emptive increase serotonin) and desipramine (due to the preferential increase in norepinephrine) cause more rapid and better therapeutic effect than monotherapy with desipramine. In another study showed that clomipramine (an antidepressant double action) causes remission of depression in 57-60% of cases compared with a group of patients who took antidepressants monoaminoergicheskie - citalopram or paroxetine (total remission in 22-28% of patients). Meta-analysis of 25 double-blind studies showed greater efficacy of antidepressants double action (clomipramine and amitriptyline), compared with tricyclic antidepressants monoaminergic action (imipramine, desipramine) and selective serotonin inhibitors (fluoxetine, fluvoxamine, paroxetine, citalopram). Analysis of 8 clinical studies on the effectiveness of venlafaxine compared with selective serotonin inhibitors (paroxetine, fluoxetine, fluvoxamine) found that the frequency response after 8 weeks of supplementation was significantly higher in patients receiving venlafaxine (45%) compared with those who received selective serotonin reuptake inhibitors (35%) or placebo (25%). Dual effect on serotonin and norepinephrine causes a more pronounced effect in the treatment of chronic pain. As serotonin, norepinephrine and are involved in pain control through the descending path of pain sensitivity. This explains why most investigators find an advantage with dual action antidepressants in the treatment of chronic pain. The exact mechanism of action by which antidepressants cause analgesic effect is unknown. Nevertheless, antidepressants with a dual mechanism of action have a more prolonged analgesic effect than antidepressants, which affect only one of the aminergic systems.
What does my medication look like?
venlafaxine available without a prescription under the brand name Effexor. Other brand or generic formulations may also be available. Ask your pharmacist to your questions about this medication, especially if it is new to you.
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