VENLAFAXINE (ven-la-fax′een)
Classifications: ANTIDEPRESSANT; SEROTONIN NOREPINEPHRINE REUPTAKE INHIBITOR (SNRI)
Therapeutic: ANTIDEPRESSANT; SNRI
Tablet; sustained release capsule; extended
release tablet. Desvenlafaxine: Extended release tablet
ACTION & THERAPEUTIC EFFECT
Potent inhibitor of neuronal serotonin and
norepinephrine reuptake. Antidepressant effect presumed to be due to
potentiation of neurotransmitter activity in the CNS.
Depression, generalized anxiety disorder; social
anxiety disorder.
Obsessivecompulsive disorder, hot flashes.
Hypersensitivity to venlafaxine, desvenlafaxine,
or other SNRI drugs; concurrent administration with MAO inhibitors or within 14
days of last dose; abrupt discontinuation; treatment for bipolar disorder;
serotonin syndrome symptoms; hyponatremia; suicidal ideation; lactation.
Renal and hepatic impairment, renal failure; anorexia nervosa,
history of mania or other psychiatric disorders, history of suicidal tendencies
or increase in suicidality especially in individuals younger than 24 y;
elevated intraocular pressure, acute closed-angle glaucoma; cardiac disorders,
recent MI, heart failure; hypertension; hyperthyroidism; CNS depression;
history of seizures or seizure disorders; older adults; pregnancy (category C).
Safety in children younger than 18 y is not established.
Adult: PO 25–125 mg t.i.d. Desvenlafaxine: 50 mg daily, may increase
dose (max: 400 mg/day)
Geriatric: PO (venlafaxine and desvenlafaxine) Start with lower doses in older adults
Adult: PO Start with 37.5 mg sustained release daily and increase to 75–225
mg sustained release/day
Renal Impairment Dosage Adjustment
CrCl 10–70 mL/min: Reduce total daily dose by 25–50%; less than 10 mL/min: Reduce total daily
dose by 50%
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Nursing Implications for Venlafaxine (ven-la-fax′een) |
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CrCl 3–50 mL/ min: Max dose: 50 mg/day; less than 30
mL/min: Max dose: 50 mg every other day
Pharmacogenetic Dosage Adjustment
Poor CYP2D6 metabolizer: Start with 70% of dose
- Give with food. Extended-release capsules must be swallowed
whole or carefully opened and sprinkled on a spoonful of applesauce. The
applesauce mixture should be swallowed without chewing and followed with a
glass of water. Extended-release tablets should be swallowed whole and not
divided, crushed, or chewed.
- Dosage increments of up to 75 mg/day are usually made at 4 days or
longer intervals.
- Allow 14 days interval after discontinuing an MAO inhibitor before
starting venlafaxine or desvenlafaxine.
- Do not abruptly withdraw drug after 1 wk or more of therapy.
- Store at room temperature, 15°–30° C (59°–86° F).
CV: Increased blood
pressure and heart rate, palpitations. CNS: Dizziness,
fatigue, headache, anxiety, insomnia, somnolence, suicidality. Endocrine:
Small but statistically significant increase in serum cholesterol, weight loss
(approximately 3 lb). GI: Nausea, vomiting, dry mouth, constipation.
Urogenital: Sexual dysfunction, erectile failure, delayed orgasm,
anorgasmia, impotence, abnormal ejaculation. Special Senses: Blurred
vision. Body as a Whole: Sweating, asthenia, Stevens Johnson
syndrome.
DIAGNOSTIC TEST INTERFERENCE
False positive urine drug screen may
occur for amphetamine or phencyclidine; use alternative tests to confirm
results.
Drug: Cimetidine, MAO INHIBITORS, desipramine, haloperidol may increase
levels and toxicity. Should not use in combination with MAO INHIBITORS: Do not
start until greater than 14 days after stopping MAO INHIBITOR; do not start MAO
INHIBITOR until 7 days after stopping venlafaxine/ desvenlafaxine. Trazodone
may lead to serotonin syndrome. Herbal: St. John’s wort, sour
date nut may cause serotonin syndrome.
Absorption: Well absorbed from
GI tract. Onset: 2 wk. Peak: Venlafaxine 1–2 h; metabolite 3–4 h.
Duration: Extensively tissue bound. Metabolism: Undergoes
substantial firstpass metabolism to its major active metabolite. Elimination:
~60% in urine as parent compound and metabolites. Half-Life: Venlafaxine
3–4 h, desvenlafaxine ~11 h.
Black Box WarningVenlafaxine has been associated with increased
risk of suicidal thinking and behavior.
Assessment & Drug Effects
- Monitor for worsening of depression or emergence of suicidal
ideation.
- Monitor cardiovascular status periodically with measurements of HR
and BP.
- Monitor neurologic status and report excessive anxiety,
nervousness, and insomnia.
- Monitor weight periodically and report excess weight loss.
- Assess safety, as dizziness and sedation are common.
- Montior lab tests: Periodic lipid profile.
Patient & Family Education
- Be aware of potential adverse effects and notify prescriber of those
that are bothersome.
- Report promptly worsening mental status, especially thoughts of suicide.
- Do not drive or engage in potentially hazardous activities until
response to drug is known.
- Avoid using alcohol while on venlafaxine.
- Do not use herbal medications without consulting prescriber.
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