Effexor - Comprehensive Usage Guide: instructions, indications, composition, side effects
Composition
- Active Ingredient: Venlafaxine hydrochloride
- Excipients: May include microcrystalline cellulose, ethylcellulose, gelatin, hypromellose, iron oxide, magnesium stearate, cellulose, and other inactive ingredients depending on the formulation.
Official Forms
- Immediate-Release Tablets: Available in various strengths, including 25 mg, 37.5 mg, 50 mg, 75 mg, and 100 mg tablets.
Pharmacological Group
Effexor belongs to the pharmacological group of serotonin-norepinephrine reuptake inhibitors (SNRIs) (ATC code: N06AX16).
Pharmacological Properties
- Pharmacodynamics: Venlafaxine acts by inhibiting the reuptake of serotonin and norepinephrine in the synaptic cleft, increasing their neurotransmission in the central nervous system (CNS). It also has weak inhibitory effects on dopamine reuptake.
- Pharmacokinetics: Venlafaxine is well-absorbed after oral administration, with peak plasma concentrations achieved within 2 to 2.5 hours. It undergoes extensive hepatic metabolism via the cytochrome P450 enzyme system (primarily CYP2D6 and CYP3A4) and is excreted mainly in the urine.
Indications
Effexor is indicated for the treatment of:
- Major depressive disorder (MDD)
- Generalized anxiety disorder (GAD)
- Social anxiety disorder (SAD)
Contraindications
Effexor is contraindicated in individuals with:
- Hypersensitivity to venlafaxine or any component of the formulation
- Concomitant use of monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing MAOI therapy
- Uncontrolled narrow-angle glaucoma
- Concomitant use of thioridazine
Interactions
Venlafaxine may interact with other medications, including:
- MAOIs, SSRIs, SNRIs, tricyclic antidepressants, and other serotonergic drugs, increasing the risk of serotonin syndrome
- Drugs that inhibit CYP2D6 enzymes, potentially increasing venlafaxine levels and toxicity
- CNS depressants, alcohol, and drugs that impair cognitive or motor function, potentiating sedation and impairment
Specifics of Use
- Effexor tablets should be taken orally 2 to 3 times daily with food, as directed by a healthcare provider.
- The initial dosage for depression and anxiety disorders is typically 75 mg/day, gradually titrated to a therapeutic dose of 75-225 mg/day based on patient response and tolerability.
- Dosage adjustments should be made cautiously, with close monitoring for adverse effects, especially during initiation or dose changes.
Pregnancy and Breastfeeding
- Effexor should be used with caution during pregnancy, especially during the third trimester, and only if the potential benefits outweigh the potential risks to the fetus.
- Venlafaxine is excreted in breast milk, and breastfeeding is not recommended during Effexor treatment due to the potential risk to the infant.
Dosage and Administration
- Dosage adjustments may be necessary in patients with hepatic impairment or renal impairment to prevent drug accumulation and minimize the risk of adverse effects.
- Elderly patients may require lower initial doses and slower titration due to age-related changes in drug metabolism.
Overdose
In case of overdose, supportive measures should be initiated, and medical attention should be sought immediately. Symptoms of venlafaxine overdose may include nausea, vomiting, seizures, tachycardia, and coma.
Side Effects
Common side effects of Effexor may include:
- Nausea
- Headache
- Dizziness
- Somnolence
- Dry mouth
- Constipation