VARENICLINE (var-en′i-cline) Chantix
Classifications: SMOKING DETERRENT; NICOTINIC RECEPTOR AGONIST
Therapeutic: SMOKING CESSATION
Prototype: Nicotine
Pregnancy Category: C
AVAILABILITY
Tablet
ACTION & THERAPEUTIC EFFECT
Nicotine increases dopamine release in the brain and cravings for nicotine are stimulated by low levels of dopamine during periods of abstinence. Varenicline is a partial agonist at nicotinic acetylcholine receptors (nAChRs), the sites responsible for the dopamine effects of nicotine. It partially stimulates these receptors to produce a modest level of dopamine but blocks nicotine from binding to many of the nicotinic receptor sites. By blocking nicotinic receptors, it reduces effects of nicotine in cases where patient relapses and uses tobacco.
USES
Adjunct for smoking cessation in patients experiencing nicotine withdrawal.
CONTRAINDICATIONS
Suicidal ideation; chronic depression; serious psychiatric disease; lactation.
CAUTIOUS USE
History of suicidal tendencies, depression; renal impairment, older adults; pregnancy (category C). Safe use in children younger than 18 y not known.
ROUTE & DOSAGE
Smoking Cessation
Adult: PO Begin with 0.5 mg/day for 3 days, increase to 0.5 mg b.i.d. for 4 days, then increase to 1 mg b.i.d. on day 8. Treat for 12 wk and may repeat an additional 12 wk.
Renal Impairment Dosage
Adjustment
CrCl 50 mL/min or less: Titrate to 0.5 mg b.i.d. (max)
ADMINISTRATION
Oral
- Give after a meal with a full glass of water.
- Dose titration over 8 days (from 0.5 mg to 2 mg daily) is recommended to minimize adverse effects.
- Store at 15°–30° C (59°–86° F).
ADVERSE EFFECTS (≥1%)
Body as a Whole: Fatigue, flushing, gingivitis, headache, influenza-like symptoms, lethargy, malaise, thirst. CNS: Abnormal dreams, anorexia, anxiety, asthenia, disturbance in attention, depression, dizziness, drowsiness, emotional lability, insomnia, irritability, nightmares, restlessness, sensory disturbance, sleep disorder, suicidality. CV: Chest pain, hypertension. GI: Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, gastroesophageal reflux, nausea, vomiting. Metabolic: Abnormal liver function test, appetite stimulation, weight gain. Musculoskeletal: Arthralgia, back pain, muscle cramps, musculoskeletal pain, myalgia. Respiratory: Dyspnea, epistaxis, respiratory disorder, rhinorrhea. Skin: Hyperhidrosis, pruritus, rash. Special Senses: Dysgeusia, xerostomia. Urogenital: Menstrual irregularity, polyuria.
INTERACTIONS
Drug: Cimetidine increases systemic exposure to varenicline by 29%.
PHARMACOKINETICS
Absorption: Complete absorption from GI tract. Peak: 3–4 h. Distribution: Less than 20% protein bound. Metabolism: Minimal. Elimination: Primarily eliminated unchanged in the urine. Half-Life: 24 h.
NURSING IMPLICATIONS
Black Box Warning
Varenicline has been associated with increased risk of depression, suicidal ideation and suicide attempt.
Assessment & Drug Effects
- Monitor smoking cessation behavior and adverse effects.
- Monitor BP for new-onset hypertension.
- Monitor diabetics for loss of glycemic control.
- Monitor for increased suicidality, or increase in agitation or aggression.
Patient & Family Education
- Report persistent nausea, vomiting, or insomnia to a health care provider.
- Report new-onset of depressed mood, suicidal ideation, or changes in emotion and behavior resulting from the use of varenicline.
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