释义 |
EffexorenUK
Ef·fex·or (ĕf′ĕk-sôr′) A trademark for the hydrochloride form of the drug venlafaxine.EffexorenUK
venlafaxine hydrochloride Co Venlafaxine, Co Venlafaxine XR, Efexor (UK), Effexor, Effexor XR, Gen-Venlafaxine XR, Novo-Venlafaxine XR, PMS-Venlafaxine XR, Ratio-Venlafaxine XR, Riva-Venlafaxine XR, Sandoz Venlafaxine XR Pharmacologic class: Phenethylamine derivative Therapeutic class: Antidepressant, anxiolytic Pregnancy risk category C Action Inhibits neuronal serotonin and norepinephrine reuptake and slightly inhibits dopamine reuptake Availability Capsules (extended-release): 37.5 mg, 75 mg, 150 mg Tablets: 25 mg, 37.5 mg, 50 mg, 75 mg, 100 mg Tablets (extended-release): 37.5 mg, 75 mg, 150 mg, 225 mg Indications and dosages ➣ Depression Adults: In outpatients, 75 mg P.O. daily in two or three divided doses; may increase in increments of 75 mg/day q 4 or more days to a maximum of 225 mg/day; extended-release form can be given as a single daily dose. In hospitalized patients, 75 mg P.O. daily in two or three divided doses; may increase in increments of 75 mg/day q 4 days to a maximum of 375 mg/day given in three divided doses. ➣ Generalized anxiety disorder Adults: Single dose of 37.5 to 75 mg (extended-release) P.O. daily; may increase in increments of 75 mg/day q 4 days to a maximum of 225 mg/day ➣ Panic disorder Adults: 37.5 mg (extended-release) P.O. daily for 7 days; increase to 75 mg P.O. daily for 7 days; then increase by 75 mg daily at weekly intervals to a maximum of 225 mg P.O. daily ➣ Social anxiety disorder Adults: 75 mg (extended-release capsule) P.O. daily as a single dose Dosage adjustment • Hepatic or renal impairment Off-label uses • Premenstrual dysphoric disorder Contraindications • Hypersensitivity to drug • MAO inhibitor use within past 14 days Precautions Use cautiously in: • cardiovascular disease; hypertension; heart failure, recent myocardial infarction, and other conditions in which increased heart rate poses a danger; hepatic or renal impairment; glaucoma; hyperthyroidism; hyponatremia; syndrome of inappropriate antidiuretic hormone secretion (SIADH) • history of seizures, neurologic impairment, or drug abuse • pregnant or breastfeeding patients • children younger than age 18. Administration Don't give within 14 days of MAO inhibitors. Adverse reactions CNS: abnormal dreams, anxiety, dizziness, headache, insomnia, nervousness, abnormal thinking, agitation, confusion, depersonalization, drowsiness, emotional lability, worsening depression, twitching, tremor, asthenia, paresthesia, mania, hypomania, suicidal ideation or behavior (especially in child or adolescent) CV: chest pain, hypertension, palpitations, tachycardia, vasodilation EENT: visual disturbances, blurred vision, mydriasis, tinnitus, rhinitis GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, flatulence, dry mouth, anorexia GU: urinary frequency or retention, sexual dysfunction, abnormal ejaculation, anorgasmia, erectile dysfunction Metabolic: hyponatremia, SIADH Skin: bruising, pruritus, rash, diaphoresis, photosensitivity Other: altered taste, weight loss, chills, yawning Interactions Drug-drug. Cimetidine: increased venlafaxine effects MAO inhibitors: potentially fatal reactions Sumatriptan, trazodone: serotonin syndrome (including altered level of consciousness) Drug-diagnostic tests. Sodium: decreased level Drug-herbs. Chamomile, hops, kava, skullcap, valerian: increased CNS depression S-adenosylmethionine (SAM-e), St. John's wort: increased risk of sedative or hypnotic effects Patient monitoring Monitor neurologic status, particularly for seizures, worsening depression, and suicidal ideation. • Closely monitor vital signs and cardiovascular status. Stay alert for hypertension and tachycardia. • Monitor nutritional status, hydration, and weight. Patient teaching • Tell patient taking extended-release capsules to swallow them whole without chewing, breaking, dividing, or dissolving. Caution patient not to stop therapy abruptly. Advise patient to promptly report seizures, worsening depression, or suicidal thoughts (especially in child or adolescent). • Caution patient to avoid driving and other dangerous activities until drug effects are known. • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above. venlafaxine (ven-la-fax-een) venlafaxine, Effexor (trade name), Effexor XR (trade name) Classification Therapeutic: antidepressants Pharmacologic: selective serotonin norepinephrine reuptake inhibitors Pregnancy Category: C
IndicationsMajor depressive disorder.Generalized anxiety disorder (Effexor XR only).Social anxiety disorder (Effexor XR only).Panic disorder (Effexor XR only).Premenstrual dysphoric disorder.ActionInhibits serotonin and norepinephrine reuptake in the CNS.Therapeutic effectsDecrease in depressive symptomatology, with fewer relapses/recurrences.Decreased anxiety.Decrease in panic attacks.PharmacokineticsAbsorption: 92–100% absorbed after oral administration.Distribution: Extensive distribution into body tissues.Metabolism and Excretion: Extensively metabolized on first pass through the liver (primarily through CYP2D6 enzyme pathway). genetic implication A small percentage of the population are poor metabolizers and will have higher blood levels with ↑ effects. One metabolite, O-desmethylvenlafaxine (ODV), has antidepressant activity; 5% of venlafaxine is excreted unchanged in urine; 30% of the active metabolite is excreted in urine.Half-life: Venlafaxine—3–5 hr; ODV—9–11 hr (both are ↑ in hepatic/renal impairment).Time/action profile (antidepressant action)ROUTE | ONSET | PEAK | DURATION |
---|
PO | within 2 wk | 2–4 wk | unknown |
Contraindications/PrecautionsContraindicated in: Hypersensitivity;Concurrent use of MAO inhibitors or MAO-like drugs (linezolid or methylene blue);Use Cautiously in: Cardiovascular disease, including hypertension;Hepatic impairment (↓ dose recommended);Impaired renal function (↓ dose recommended);History of seizures or neurologic impairment;History of mania;History of ↑ intraocular pressure or angle-closure glaucoma;History of drug abuse; Obstetric: Use only if clearly required, weighing benefit to mother versus potential harm to fetus (potential for discontinuation syndrome or toxicity in the neonate when venlafaxine is taken during the 3rd trimester); Lactation: Potential for serious adverse reactions in infant; discontinue drug or discontinue breast feeding; Pediatric: ↑ risk of suicidal thinking and behavior (suicidality) in children and adolescents with major depressive disorder and other psychiatric disorders. Observe closely for suicidality and behavior changes.Adverse Reactions/Side EffectsCentral nervous system- neuroleptic malignant syndrome (life-threatening)
- seizures (life-threatening)
- suicidal thoughts (life-threatening)
- abnormal dreams (most frequent)
- anxiety (most frequent)
- dizziness (most frequent)
- headache (most frequent)
- insomnia (most frequent)
- nervousness (most frequent)
- weakness (most frequent)
- abnormal thinking
- agitation
- confusion
- depersonalization
- drowsiness
- emotional lability
- worsening depression
Ear, Eye, Nose, Throat- rhinitis (most frequent)
- visual disturbances (most frequent)
- epistaxis
- tinnitus
Cardiovascular- chest pain
- hypertension
- palpitations
- tachycardia
Gastrointestinal- abdominal pain (most frequent)
- altered taste (most frequent)
- anorexia (most frequent)
- constipation (most frequent)
- diarrhea (most frequent)
- dry mouth (most frequent)
- dyspepsia (most frequent)
- nausea (most frequent)
- vomiting (most frequent)
- weight loss (most frequent)
Genitourinary- sexual dysfunction (most frequent)
- urinary frequency
- urinary retention
Dermatologic- ecchymoses (most frequent)
- itching
- photosensitivity
- skin rash
Neurologic- paresthesia (most frequent)
- twitching
Miscellaneous- serotonin syndrome (life-threatening)
- chills (most frequent)
- bleeding
- yawning
InteractionsDrug-Drug interaction Concurrent use with MAO inhibitors may result in serious, potentially fatal reactions (wait at least 2 wk after stopping MAO inhibitor before initiating venlafaxine; wait at least 1 wk after stopping venlafaxine before starting MAO inhibitors).Concurrent use with MAO-inhibitor like drugs, such as linezolid or methylene blue may ↑ risk of serotonin syndrome; concurrent use contraindicated; do not start therapy in patients receiving linezolid or methylene blue ; if linezolid or methylene blue need to be started in a patient receiving venlafaxine, immediately discontinue venlafaxine and monitor for signs/symptoms of serotonin syndrome for 2 wk or until 24 hr after last dose of linezolid or methylene blue, whichever comes first (may resume venlafaxine therapy 24 hr after last dose of linezolid or methylene blue)Concurrent use with alcohol or other CNS depressants, including sedatives/hypnotics, antihistamines, and opioid analgesics in depressed patients is not recommended.Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SNRIs, fentanyl, buspirone, tramadol and triptans ↑ risk of serotonin syndromeLithium may have ↑ serotonergic effects with venlafaxine; use cautiously in patients receiving venlafaxine.↑ blood levels and may ↑ effects of desipramine and haloperidol.Cimetidine may ↑ the effects of venlafaxine (may be more pronounced in geriatric patients, those with hepatic or renal impairment, or those with pre-existing hypertension).Ketoconazole may ↑ the effects of venlafaxine.↑ risk of bleeding with NSAIDS, aspirin, clopidogrel, or warfarin.Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.↑ risk of serotinergic side effects including serotonin syndrome with St. John’s wort and SAMe.Route/DosageMajor Depressive DisorderOral (Adults) Tablets—75 mg/day in 2–3 divided doses; may ↑ by up to 75 mg/day every 4 days, up to 225 mg/day (not to exceed 375 mg/day in 3 divided doses); Extended-release (XR) capsules—75 mg once daily (some patients may be started at 37.5 mg once daily) for 4–7 days; may ↑ by up to 75 mg/day at intervals of not less than 4 days (not to exceed 225 mg/day).General Anxiety DisorderOral (Adults) Extended-release (XR) capsules—75 mg once daily (some patients may be started at 37.5 mg once daily) for 4–7 days; may ↑ by up to 75 mg/day at intervals of not less than 4 days (not to exceed 225 mg/day).Social Anxiety DisorderOral (Adults) Extended-release (XR) capsules—75 mg once daily.Panic DisorderOral (Adults) Extended-release (XR) capsules—37.5 mg once daily for 7 days; may then ↑ to 75 mg once daily; may then ↑ by 75 mg/day every 7 days (not to exceed 225 mg/day).Hepatic ImpairmentOral (Adults) ↓ daily dose by 50% in patients with mild-to-moderate hepatic impairment.Renal ImpairmentOral (Adults) CCr 10–70 mL/min—↓ daily dose by 25–50%; Hemodialysis—↓ daily dose by 50%.Availability (generic available)Tablets: 25 mg, 37.5 mg, 50 mg, 75 mg, 100 mg Cost: Generic — 25 mg $32.24 / 100, 37.5 mg $39.41 / 100, 75 mg $38.00 / 100Extended-release capsules: 37.5 mg, 75 mg, 150 mg Cost: Generic — 37.5 mg $32.14 / 90, 75 mg $271.37 / 100, 150 mg $29.94 / 100Nursing implicationsNursing assessment- Assess mental status and mood changes. Inform health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia.
- Assess suicidal tendencies, especially in early therapy. Restrict amount of drug available to patient. Risk may be increased in children, adolescents, and adults ≤24 yr.
- Monitor BP before and periodically during therapy. Sustained hypertension may be dose-related; decrease dose or discontinue therapy if this occurs.
- Monitor appetite and nutritional intake. Weigh weekly. Report continued weight loss. Adjust diet as tolerated to support nutritional status.
- Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyper-reflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs, triptans).
- Lab Test Considerations: Monitor CBC with differential and platelet count periodically during therapy. May cause anemia, leukocytosis, leukopenia, thrombocytopenia, basophilia, and eosinophilia.
- May cause an ↑ in serum alkaline phosphatase, bilirubin, AST, ALT, BUN, and creatinine.
- May also cause ↑ serum cholesterol.
- May cause electrolyte abnormalities (hyperglycemia or hypoglycemia, hyperkalemia or hypokalemia, hyperuricemia, hyperphosphatemia or hypophosphatemia, and hyponatremia).
- May cause false-positive immunoassay screening tests for phencyclidine (PCP) and amphetamine.
Potential Nursing DiagnosesIneffective coping (Indications) Risk for injury (Side Effects)
Implementation- Do not confuse Effexor with Effexor XR.
- Oral: Administer venlafaxine with food.
- Extended-release capsules should be swallowed whole; do not crush, break, or chew.
- Extended-release capsules may be opened and contents sprinkled on a spoonful of applesauce. Take immediately and follow with a glass of water. Do not store mixture for later use.
Patient/Family Teaching- Instruct patient to take venlafaxine as directed at the same time each day. Take missed doses as soon as possible unless almost time for next dose. Do not double doses or discontinue abruptly. Patients taking venlafaxine for >6 wk should have dose gradually decreased before discontinuation.
- Advise patient, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide; new or worse depression or anxiety; agitation or restlessness; panic attacks; insomnia; new or worse irritability; aggressiveness; acting on dangerous impulses, mania, or other changes in mood or behavior or if symptoms of serotonin syndrome occur.
- May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to the drug is known.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Caution patient to avoid taking alcohol or other CNS-depressant drugs during therapy.
- Instruct patient to notify health care professional if signs of allergy (rash, hives) occur.
- Instruct female patients to inform health care professional if pregnancy is planned or suspected or if breast feeding.
- Emphasize the importance of follow-up exams to monitor progress. Encourage patient participation in psychotherapy.
Evaluation/Desired Outcomes- Increased sense of well-being.
- Renewed interest in surroundings. Need for therapy should be periodically reassessed. Therapy is usually continued for several months.
- Decreased anxiety.
Effexor (ĕf′ĕk-sôr′) A trademark for the hydrochloride form of the drug venlafaxine.Effexor® Venlafaxine Psychiatry A mood-enhancing SSRI used for major depression, general anxiety disorder Contraindications Should not be combined with MAOIs. See Depression, Major depression, Monoamine oxidase inhibitor. Patient discussion about EffexorQ. Effexor Hi! I am new to the forum. I was diagnosed eight months ago with effexor - induced mania and now have been diagnosed as Bipolar II, rapid cycling, with mixed states. I have a 30 year old history of treatment-resistant depression. No mania prior to the effexor. I also self-treat the depression with one hour of vigorous exercise daily, sunlight, healthy diet, regular sleep, and no stimulants or depressants including coffee and alcohol. I take omega 3, magnesium malate, calcium, zinc, selenium, and super b-complex supplements as well.A. Well, I found out that goats get depressed too and it only happens when they are mineral deficient. I think the mineral deficiency that causes more health problems and especially related to the brain is Copper. Evidently it is critical to the absorption of many other minerals. If you've tried St. Johns Wort and found that it helps at all, I would suggest that it is because SJW contains lots of copper. Another really excellent source of copper is Kelp. Actually kelp is an excellent source of all the minerals, especially all the ones not yet discovered by man. **Natures Version** If you are anemic, you cannot absorb the iron without copper. Copper also helps the body to absorb calcium. I understand that there is a coating of calcium on the nerves. Unless you are eating a really old fashioned diet of mostly raw and unprocessed foods grown in remineralized soil, the food you are eating is most likely stripping more minerals from your body than adding to. More discussions about Effexor |