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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SULTEN-10 (SULTEN-10).
| Breastfeeding | Contraindicated. M/P ratio unknown. Excreted in human milk; potential for serious adverse reactions in nursing infants. Discontinue drug or do not breastfeed. |
| 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. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Concomitant use with nitrates or nitric oxide donors.","Known hypersensitivity to sildenafil or any component of the formulation.","Concomitant use with guanylate cyclase stimulators (e.g., riociguat).","Severe hepatic impairment (Child-Pugh class C) or severe renal impairment (CrCl <30 mL/min) when used for pulmonary arterial hypertension."]
| 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."] |
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| 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. |