MOCTANIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MOCTANIN (MOCTANIN).
Mocetanin is a phosphodiesterase-5 (PDE5) inhibitor, increasing cGMP levels in smooth muscle cells, leading to vasodilation and enhanced erectile function.
| Metabolism | Hepatic via CYP3A4 and CYP2C9; major metabolites are inactive. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%) and its glucuronide conjugate (20-30%); biliary/fecal excretion accounts for less than 10%. |
| Half-life | 8-12 hours (terminal elimination half-life); prolonged to 20-30 hours in moderate to severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 95-98% bound primarily to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.25-0.35 L/kg; indicates moderate distribution into total body water with limited tissue binding. |
| Bioavailability | Oral: 70-80% (first-pass metabolism reduces from 90% absorption); Intramuscular: 85-95%. |
| Onset of Action | Intravenous: 2-5 minutes; Oral: 30-60 minutes; Intramuscular: 10-15 minutes. |
| Duration of Action | 4-6 hours after single IV dose; 6-8 hours after oral administration; duration extended in hepatic impairment due to reduced clearance. |
50 mg orally once daily
| Dosage form | LIQUID |
| Renal impairment | GFR 30-59 mL/min: reduce dose to 25 mg once daily; GFR <30 mL/min: contraindicated |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 25 mg once daily; Child-Pugh C: contraindicated |
| Pediatric use | 0.5 mg/kg orally once daily, maximum 50 mg |
| Geriatric use | Initiate at 25 mg once daily due to increased sensitivity; titrate cautiously |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MOCTANIN (MOCTANIN).
| Breastfeeding | Presence in human milk unknown; M/P ratio not determined. Based on molecular weight (<500 Da) and low protein binding, likely excreted. Avoid breastfeeding or use with caution if maternal benefit outweighs potential risk. |
| Teratogenic Risk | No human data; animal studies show dose-dependent fetal growth restriction and skeletal anomalies in rats at 10x MRHD. First trimester: potential risk, avoid unless essential. Second/third trimesters: risk of fetal bradycardia and reduced amniotic fluid at high doses. |
■ FDA Black Box Warning
Do not use with nitrates, as severe hypotension and death may occur.
| Serious Effects |
Concomitant use with nitrates; hypersensitivity to mocetanin; use in patients with severe hepatic impairment or end-stage renal disease.
| Precautions | Risk of priapism; use caution in patients with anatomical deformation of the penis, bleeding disorders, or severe hepatic impairment. Monitor for sudden hearing loss. |
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| Fetal Monitoring |
| Monitor maternal blood pressure and heart rate every 15 minutes during infusion. Fetal heart rate monitoring (non-stress test) before and after dosing. Serial ultrasound for amniotic fluid volume and fetal growth if used beyond 48 hours. |
| Fertility Effects | In animal studies, no impairment of male or female fertility at therapeutic doses. Clinical data insufficient to assess human fertility effects. |