RECTIV
Clinical safety rating
cautionComprehensive clinical and safety monograph for RECTIV (RECTIV).
RECTIV (nitroglycerin) is a nitric oxide (NO) donor that relaxes vascular smooth muscle via stimulation of intracellular cyclic guanosine monophosphate (cGMP) production, leading to vasodilation. In chronic anal fissures, it reduces internal anal sphincter pressure and improves blood flow to the anoderm.
| Metabolism | Primarily hepatic metabolism via glutathione-organic nitrate reductase, with subsequent denitration and conjugation. Metabolites include inorganic nitrate and 1,2-glyceryl dinitrate. Also undergoes hydrolysis by esterases. |
| Excretion | Primarily renal; approximately 60-70% of the parent drug and metabolites excreted in urine within 24 hours. Fecal elimination accounts for ~20-30% via biliary secretion. Less than 1% unchanged drug recovered in feces. |
| Half-life | Terminal elimination half-life is approximately 2-4 hours in healthy adults. In patients with severe hepatic impairment, half-life may be prolonged up to 8-10 hours, requiring dose adjustment. |
| Protein binding | Approximately 60% bound to plasma proteins, primarily albumin. Binding is reversible and concentration-dependent. |
| Volume of Distribution | Volume of distribution is approximately 2-4 L/kg, indicating extensive tissue distribution. Clinical meaning: high Vd suggests significant uptake into vascular smooth muscle and other tissues. |
| Bioavailability | Sublingual: approximately 40-50% due to first-pass metabolism. Oral: <10% due to extensive hepatic first-pass effect. Topical (RECTIV): systemic bioavailability is negligible (<1%) when applied as directed to the anal mucosa. |
| Onset of Action | Intravenous administration: therapeutic effect (vasodilation) begins within 1-2 minutes. Sublingual administration: onset within 2-5 minutes. Topical ointment (RECTIV): onset of action for reduction of anal sphincter tone is 5-10 minutes. |
| Duration of Action | Duration of hemodynamic effects is 30-60 minutes after intravenous or sublingual administration. For topical application (RECTIV), reduction in anal sphincter pressure lasts approximately 60-90 minutes, supporting its use in anal fissures. |
| Molecular Weight | 352.47 |
1 gram (0.5 mg nitroglycerin) applied intrarectally as an ointment 10-15 minutes before anticipated bowel movement, up to twice daily.
| Dosage form | OINTMENT |
| Renal impairment | No dosage adjustment required for renal impairment. Use with caution in severe impairment due to potential for volume depletion. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 1 gram (0.5 mg) once daily. Child-Pugh C: contraindicated. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years. |
| Geriatric use | Use with caution; start at lowest effective dose (1 gram) and monitor for hypotension. Consider decreased renal/hepatic function. |
| 1st trimester | Contraindicated due to risk of fetal harm; may cause uterine hyperstimulation and fetal distress. |
| 2nd trimester | Contraindicated; may induce preterm labor and fetal hypoxia. |
| 3rd trimester | Contraindicated; high risk of placental abruption, uterine rupture, and fetal distress. |
Clinical note
Comprehensive clinical and safety monograph for RECTIV (RECTIV).
| Placental transfer | Limited data; dinoprostone is a prostaglandin that may cross placenta and cause uterine contractions. |
| Breastfeeding | No data on excretion in human milk; use caution due to potential for infant exposure and gastrointestinal effects. |
| Lactation Rating | L4 - Possibly Hazardous |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies at doses up to 10 mg/kg/day (approximately 50 times the recommended human dose). No well-controlled studies in pregnant women; use only if clearly needed. Fetal risk cannot be ruled out. |
| Fetal Monitoring | No specific monitoring required for maternal or fetal effects due to low systemic absorption. Monitor for local adverse effects if used during pregnancy. |
| Fertility Effects | No studies on fertility effects in humans. Animal studies show no impairment of fertility at doses up to 10 mg/kg/day. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
Hypersensitivity to prostaglandinsAcute pelvic inflammatory diseasePlacenta previa or unexplained vaginal bleeding during pregnancyHistory of cesarean section or major uterine surgeryFetal distress where delivery is not imminentCephalopelvic disproportion
| Precautions | Hypotension and syncope: Use with caution in patients with hypotension, hypovolemia, or those taking antihypertensives., Severe anemia or conditions where vasodilation is detrimental., Concomitant use with phosphodiesterase-5 (PDE-5) inhibitors (e.g., sildenafil) is contraindicated due to risk of severe hypotension., May cause headaches and local burning or itching at application site. |
| Food/Dietary | No specific food restrictions. Avoid alcohol as it may worsen hypotension and headache. Grapefruit juice may increase nitroglycerin levels; avoid concurrent consumption. |
| Clinical Pearls | RECTIV (nitroglycerin) 0.4% ointment is indicated for chronic anal fissure pain. Apply a 1-inch strip intra-anally every 12 hours for up to 8 weeks. May cause headache; monitor blood pressure. Contraindicated with PDE5 inhibitors (sildenafil, tadalafil, vardenafil) due to severe hypotension. Avoid in patients with hypotension (SBP <90 mm Hg) or hypovolemia. Do not use with strong CYP3A4 inhibitors (e.g., ritonavir, cobicistat). |
| Patient Advice | Apply 1-inch strip of ointment inside the anus every 12 hours using the applicator. · Wash hands before and after application. · Do not use more than 8 weeks unless directed by your doctor. · Avoid sexual activity during treatment as partner may absorb medication. · Do not take erectile dysfunction drugs (Viagra, Cialis, Levitra) while using this medication. · Seek medical help if you experience severe headache, dizziness, or fainting. · Store at room temperature away from heat and direct light. · Do not use if you have low blood pressure or are dehydrated. |
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