SUPRENZA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUPRENZA (SUPRENZA).
Partial agonist at mu-opioid receptors; also a weak antagonist at kappa-opioid receptors. Provides analgesic effects with reduced respiratory depression compared to full agonists.
| Metabolism | Primarily hepatic via CYP3A4 and CYP3A5 to norbuprenorphine (active metabolite); also undergoes glucuronidation. |
| Excretion | Approximately 60-80% of a dose is excreted renally as unchanged drug, with 20-40% eliminated via biliary/fecal routes. |
| Half-life | Terminal elimination half-life is approximately 12-15 hours in patients with normal renal function, allowing for twice-daily dosing. |
| Protein binding | Approximately 95-98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 2-3 L/kg, indicating extensive tissue distribution beyond plasma volume. |
| Bioavailability | Oral bioavailability is approximately 70-80%. |
| Onset of Action | Oral absorption leads to onset of clinical effect within 1-2 hours after administration. |
| Duration of Action | Duration of action is approximately 12 hours, consistent with the dosing interval of twice daily. |
Adults: 200 mg orally twice daily with meals.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | eGFR <45 mL/min/1.73m²: contraindicated. eGFR ≥45: no adjustment. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce to 200 mg once daily; Class C: contraindicated. |
| Pediatric use | Not recommended for patients under 18 years; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; monitor renal function and use caution due to increased risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUPRENZA (SUPRENZA).
| Breastfeeding | Testosterone is present in breast milk; M/P ratio not reported. Avoid breastfeeding due to potential for androgenization of the infant. Use only if clearly needed and no safer alternative. |
| Teratogenic Risk | SuprENza (testosterone) is contraindicated in pregnancy due to virilization of female fetus. First trimester: high risk of clitoromegaly, labial fusion, and urogenital sinus abnormalities. Second and third trimesters: risk of continued virilization, including phallic enlargement and ambiguous genitalia. Fetal growth restriction may occur. |
■ FDA Black Box Warning
Risk of respiratory depression, especially in non-opioid-tolerant patients. Risk of neonatal opioid withdrawal syndrome with prolonged use during pregnancy. Risk of serious injury or death due to accidental exposure in children.
| Serious Effects |
Hypersensitivity to buprenorphine or any component of the formulation. Severe respiratory insufficiency. Acute or severe bronchial asthma. Gastrointestinal obstruction, including paralytic ileus.
| Precautions | Respiratory depression, particularly in the first 24-72 hours of treatment; caution in patients with pulmonary disease. Risk of QT prolongation. Adrenal insufficiency. Severe hypotension. Risk of misuse, abuse, and addiction. Tolerance and physical dependence. |
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| Fetal Monitoring |
| If accidental exposure during pregnancy, perform fetal ultrasound to assess genital development and growth. Monitor maternal serum testosterone levels periodically. Consider fetal MRI for ambiguous genitalia assessment. |
| Fertility Effects | Testosterone can suppress spermatogenesis via negative feedback on gonadotropins. In women, high doses may cause anovulation and menstrual irregularities. Effects are generally reversible upon discontinuation. |