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. |
| Molecular Weight | 324.4 |
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 | No adequate studies in pregnant women; animal reproduction studies not available. Use only if potential benefit justifies risk to fetus. |
| 2nd trimester | Same as T1; no evidence of teratogenicity in limited human data. |
| 3rd trimester | Same as T1; may cause adverse effects in neonate if used near term. |
Clinical note
Comprehensive clinical and safety monograph for SUPRENZA (SUPRENZA).
| Placental transfer | Unknown; no published data available. |
| Breastfeeding | Excretion into human milk unknown. Not recommended due to potential for serious adverse reactions in nursing infants. |
| Lactation Rating |
■ 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 supranza or any componentConcurrent use with MAOIsSevere hepatic impairment
| 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. |
| Food/Dietary | No significant food interactions. Grapefruit juice may increase buprenorphine levels; avoid large quantities. |
Loading safety data…
| L5 (Contraindicated) |
| 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. |
| 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. |
| Clinical Pearls | SUPRENZA (buprenorphine/naloxone) sublingual film is used for opioid dependence. Monitor for respiratory depression especially when combined with benzodiazepines or alcohol. The naloxone component is poorly absorbed sublingually but precipitates withdrawal if injected. Administer only after clear signs of withdrawal to avoid precipitated withdrawal. Adjust dose in hepatic impairment as buprenorphine is hepatically metabolized. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Place film under the tongue until fully dissolved; do not chew or swallow. · Avoid alcohol and benzodiazepines as they can cause severe respiratory depression. · Keep out of reach of children; accidental exposure can be fatal. · Do not abruptly stop; withdrawal symptoms may occur. · Store at room temperature away from moisture and heat. |