RECTIV
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RECTIV (RECTIV).
| Breastfeeding | Not recommended during breastfeeding. Drug is administered topically for hemorrhoids; systemic absorption is minimal, but no data on excretion in human milk. M/P ratio not determined. |
| 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 |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Concomitant use of PDE-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)","History of hypersensitivity to nitroglycerin or any component of the formulation","Severe anemia","Increased intracranial pressure (e.g., head trauma, cerebral hemorrhage)","Circulatory failure (shock) or severe hypotension"]
| 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."] |
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| 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. |