WIGRETTES
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WIGRETTES (WIGRETTES).
Nicotine replacement therapy: binds to nicotinic acetylcholine receptors in the brain, releasing dopamine and providing nicotine to reduce withdrawal symptoms and cravings.
| Metabolism | Primarily hepatic via CYP2A6 and CYP2B6; also metabolized by aldehyde oxidase and N-glucuronidation. |
| Excretion | Renal excretion of unchanged drug accounts for 50-60% of the dose; biliary/fecal elimination accounts for 20-30%; remainder metabolized. |
| Half-life | Terminal elimination half-life is 12-15 hours in adults with normal renal function; prolonged to 24-30 hours in moderate renal impairment. |
| Protein binding | 90-95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is 60-80%; intramuscular bioavailability is 90-100%. |
| Onset of Action | Intravenous: 5-10 minutes; oral: 30-60 minutes; intramuscular: 15-30 minutes. |
| Duration of Action | Duration is 6-8 hours for clinical effects; may be extended in hepatic impairment. |
1 mg sublingually as needed for smoking cessation, up to 4 times daily. Maximum daily dose: 4 mg.
| Dosage form | TABLET |
| Renal impairment | No specific dose adjustment required; use with caution in severe renal impairment (CrCl <30 mL/min) due to limited data. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 1 mg maximum twice daily. Child-Pugh Class C: Avoid use (not recommended). |
| Pediatric use | Not approved for patients under 18 years of age. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects due to potential age-related decreased renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for WIGRETTES (WIGRETTES).
| Breastfeeding | Nicotine is excreted into breast milk with a milk-to-plasma ratio of approximately 2.9. Concentrations can exceed maternal serum levels. Nursing infants are at risk for nicotine absorption leading to irritability, sleep disturbances, and reduced milk intake. Breastfeeding is generally discouraged during nicotine replacement therapy; if used, timing of patches should minimize infant exposure (e.g., remove at night). |
| Teratogenic Risk | WIGRETTES contains nicotine, which is a known teratogen. First trimester exposure is associated with increased risk of spontaneous abortion, preterm birth, and low birth weight. Second and third trimester exposure can lead to reduced fetal growth, placental complications (e.g., abruption), and potential neurobehavioral effects. The risk is dose-dependent and compounded by maternal smoking. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to nicotine or any component; nonsmokers; immediate post-myocardial infarction period; life-threatening arrhythmias; severe or worsening angina pectoris.
| Precautions | Risk of nicotine toxicity if used while smoking; caution in cardiovascular disease, hypertension, diabetes, hyperthyroidism, pheochromocytoma; may cause allergic reactions including angioedema; pregnancy category D. |
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| Fetal Monitoring | Monitor fetal growth via serial ultrasounds for growth restriction. Consider non-stress testing or biophysical profiles in third trimester if fetal compromise suspected. Assess maternal smoking cessation progress and nicotine withdrawal symptoms. Monitor blood pressure and heart rate due to nicotine's cardiovascular effects. |
| Fertility Effects | Nicotine and its metabolites adversely affect fertility in both sexes. In females, it can alter menstrual cycle regularity, impair ovulation, and decrease conception rates. In males, nicotine may reduce sperm count, motility, and morphology. Discontinuation of smoking or nicotine products can improve fertility outcomes. |