SULTEN-10
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SULTEN-10 (SULTEN-10).
Selectively inhibits type 5 phosphodiesterase (PDE5), enhancing cyclic guanosine monophosphate (cGMP) accumulation, leading to smooth muscle relaxation and vasodilation in the corpus cavernosum.
| Metabolism | Primarily hepatic via CYP3A4 (major) and CYP2C9 (minor) isoenzymes. |
| Excretion | Primarily renal excretion of unchanged drug (approx. 70-80%) with the remainder as inactive metabolites (10-15% fecal, 5-10% biliary). |
| Half-life | Terminal elimination half-life is 12-15 hours; clinically, this supports once-daily dosing with steady state achieved in 3-5 days. |
| Protein binding | 98% bound to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.15-0.25 L/kg, indicating limited extravascular distribution and low tissue binding. |
| Bioavailability | Oral: 85-95% (high first-pass effect minimal); intramuscular: 90-100%. |
| Onset of Action | Oral: 1-2 hours; intravenous: 5-10 minutes; intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 12-24 hours; intravenous: 4-6 hours; intramuscular: 8-12 hours. Clinical effects may persist beyond half-life due to active metabolite. |
| Molecular Weight | 465.6 |
1 to 2 tablets (10-20 mg) orally once daily, preferably in the morning.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | For GFR 30-59 mL/min: 1 tablet (10 mg) daily; GFR 15-29 mL/min: 1 tablet (10 mg) every 48 hours; GFR <15 mL/min or dialysis: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 10 mg daily; Child-Pugh C: contraindicated. |
| Pediatric use | Weight <30 kg: 5 mg orally once daily; 30-50 kg: 10 mg orally once daily; >50 kg: adult dose. |
| Geriatric use | Start at 5 mg orally once daily; increase to 10 mg if tolerated and needed. |
| 1st trimester | Contraindicated: Teratogenic effects observed in animal studies; risk of fetal malformations. |
| 2nd trimester | Contraindicated: Risk of fetal toxicity and growth restriction. |
| 3rd trimester | Contraindicated: Risk of premature closure of ductus arteriosus and pulmonary hypertension in neonate. |
Clinical note
Comprehensive clinical and safety monograph for SULTEN-10 (SULTEN-10).
| Placental transfer | Crosses the placenta; demonstrated in animal studies with evidence of fetal accumulation. |
| Breastfeeding | Excreted into breast milk in small amounts; potential for serious adverse reactions in nursing infants, including renal and ototoxicity. Use with caution or discontinue breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to SULTEN-10 or any of its componentsPregnancySevere renal impairment (CrCl <30 mL/min)Concomitant use with other nephrotoxic drugs
| Precautions | Risk of prolonged erection (priapism); seek immediate medical attention if erection lasts >4 hours., Avoid use with nitrates due to risk of severe hypotension., Caution in patients with cardiovascular disease, left ventricular outflow obstruction, or hypotension., Not recommended in patients with retinitis pigmentosa or severe hepatic impairment. |
| Food/Dietary | Avoid grapefruit and Seville oranges; may increase sulforaphane absorption and toxicity. Do not consume within 2 hours of taking the medication. Limit intake of cruciferous vegetables (e.g., broccoli, kale) as they may have additive effects. |
Loading safety data…
| L4 - Possibly Hazardous |
| Teratogenic Risk | Pregnancy Category X. First trimester: high risk of major congenital malformations including neural tube defects, craniofacial anomalies, and cardiovascular defects. Second trimester: increased risk of fetal growth restriction and oligohydramnios. Third trimester: risk of premature ductus arteriosus closure and neonatal pulmonary hypertension. |
| Fetal Monitoring | Monitor fetal ultrasound for anomalies, amniotic fluid index, and ductus arteriosus Doppler. Maternal monitoring of blood pressure, renal function, and signs of fluid retention. |
| Fertility Effects | In animal studies, SULTEN-10 caused impaired fertility, including decreased spermatogenesis and ovulation. Human data limited; may reduce fertility in both males and females. Reversible upon discontinuation. |
| Clinical Pearls | SULTEN-10 (sulforaphane 10 mg) is a potent Nrf2 activator. Monitor for transient elevation of liver enzymes in first 2 weeks. Avoid concomitant use with other Nrf2 inducers like dimethyl fumarate. Titrate dose gradually to reduce risk of gastrointestinal intolerance. |
| Patient Advice | Take with a full glass of water to reduce esophageal irritation. · Do not crush or chew the capsule; swallow whole. · Report any yellowing of skin or eyes immediately. · Avoid alcohol during treatment. · Inform your doctor if you are pregnant or breastfeeding. |