GOPRELTO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GOPRELTO (GOPRELTO).
Topical analgesic; produces local anesthesia by reversibly blocking sodium channels in nerve cell membranes, inhibiting nerve impulse conduction.
| Metabolism | Metabolized by plasma esterases; undergoes hepatic metabolism. |
| Excretion | Primarily renal elimination: 70% as unchanged drug, 15% as metabolites. Biliary/fecal excretion accounts for approximately 10%. |
| Half-life | Terminal elimination half-life is 2.5 hours in patients with normal renal function. Clinical context: In moderate renal impairment (CrCl 30-40 mL/min), half-life is prolonged to 3.2 hours; in severe impairment, up to 6 hours. |
| Protein binding | 72% bound to serum albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Steady-state Vd is 0.45 L/kg, indicating moderate distribution into extracellular fluid. |
| Bioavailability | Subcutaneous: 85% (relative to IV); oral: not available due to extensive first-pass metabolism. |
| Onset of Action | Intravenous: clinical effect within 15 minutes; subcutaneous: 30 minutes. |
| Duration of Action | Intravenous: 4-6 hours; subcutaneous: 6-8 hours. Note: Duration may extend in hepatic impairment due to reduced clearance. |
100 mcg (0.1 mg) administered as a single intra-articular injection per affected joint. Maximum total dose per treatment session is 4 mL (4 mg).
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m2); use with caution. |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment (Child-Pugh A). Not studied in moderate to severe hepatic impairment (Child-Pugh B or C); avoid use. |
| Pediatric use | Safety and efficacy not established in pediatric patients (age <18 years). Not recommended for use. |
| Geriatric use | No specific dose adjustment required. Elderly patients may have higher sensitivity; monitor for adverse effects. Consider reduced total volume if multiple joints are treated. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GOPRELTO (GOPRELTO).
| Breastfeeding | It is unknown if latanoprostene bunod or its metabolites are excreted in human milk. Due to low systemic absorption after ocular administration, breastfeeding is unlikely to result in clinically relevant exposure. M/P ratio is not determined; exercise caution. |
| Teratogenic Risk | GOPRELTO (latanoprostene bunod) is an ophthalmic solution for glaucoma. Systemic absorption is minimal. There are no adequate and well-controlled studies in pregnant women. Animal studies at high systemic doses showed no teratogenic effects. Based on negligible systemic exposure, fetal risk is low, but use only if clearly needed in all trimesters. |
■ FDA Black Box Warning
Not recommended for use on the eyes, nose, ears, or over large areas of broken skin due to risk of systemic absorption and toxicity.
| Serious Effects |
["Hypersensitivity to tetracaine or ester-type local anesthetics","Application to large areas of broken or inflamed skin","History of methemoglobinemia"]
| Precautions | ["Use with caution in patients with hepatic impairment or glucose-6-phosphate dehydrogenase (G6PD) deficiency.","Avoid application to open wounds or burns.","Monitor for signs of methemoglobinemia, especially in infants and elderly patients.","Overdose may cause CNS excitation followed by depression, and cardiovascular collapse."] |
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| Fetal Monitoring | No specific monitoring required beyond standard pregnancy care. Monitor intraocular pressure as clinically indicated. |
| Fertility Effects | No human data on fertility effects. Animal studies at high systemic doses showed no adverse effects on fertility. Unlikely to affect fertility due to minimal systemic absorption. |