CAVERJECT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CAVERJECT (CAVERJECT).
Causes relaxation of corpus cavernosum smooth muscle and vasodilation via increased intracellular cyclic guanosine monophosphate (cGMP) due to inhibition of phosphodiesterase type 5 (PDE5) by its active metabolite, alprostadil.
| Metabolism | Alprostadil is rapidly metabolized primarily in the lungs via oxidation, with 60-70% of the drug metabolized during one pass through the pulmonary circulation. Metabolites are excreted mainly in urine. |
| Excretion | Renal: 70-80% as metabolites, 20-30% unchanged; biliary/fecal: <5% |
| Half-life | Terminal elimination half-life is 1-2 hours; clinically, plasma levels decline rapidly after injection, with minimal systemic accumulation. |
| Protein binding | Approximately 80% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is approximately 0.3-0.4 L/kg (13 L for 70 kg adult), indicating distribution primarily in extracellular fluid. |
| Bioavailability | Intracavernosal injection: ~100% locally; oral bioavailability is negligible (<1%) due to extensive first-pass metabolism. |
| Onset of Action | Intracavernosal injection: 5-20 minutes; most patients achieve erection within 5-10 minutes. |
| Duration of Action | Erection lasts approximately 30-60 minutes (dose-dependent); clinical effect may persist up to 2 hours; risk of priapism if >4 hours. |
Initial dose 2.5 micrograms intracavernous injection, titrate to effect; maximum 60 micrograms per injection. Frequency no more than 3 times per week with at least 24 hours between doses.
| Dosage form | INJECTABLE |
| Renal impairment | No dosage adjustment required for renal impairment; GFR-based modifications not established. |
| Liver impairment | No dosage adjustment required for hepatic impairment; Child-Pugh based modifications not established. |
| Pediatric use | Not indicated in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment in elderly; initiate at low end of dosing range (2.5 micrograms) due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CAVERJECT (CAVERJECT).
| Breastfeeding | Not known if excreted in human milk. M/P ratio unknown. Due to lack of data and risk of adverse effects in infant, caution advised; use only if clearly needed. |
| Teratogenic Risk | Category C. No adequate studies in pregnant women. In animal studies, no teratogenic effects observed; however, fetal resorptions increased at maternally toxic doses. First trimester: unknown risk; second/third trimester: avoid use due to potential for maternal hypotension and decreased uteroplacental perfusion. |
| Fetal Monitoring |
■ FDA Black Box Warning
Prolonged erection (priapism) lasting more than 4 hours may occur. Patients should seek immediate medical attention to avoid permanent tissue damage.
| Serious Effects |
["Hypersensitivity to alprostadil","Conditions predisposing to priapism (sickle cell anemia, multiple myeloma, leukemia)","Penile implants","Anatomical penis deformities (angulation, cavernosal fibrosis, Peyronie's disease)","In men for whom sexual activity is inadvisable"]
| Precautions | ["Priapism risk: Instruct patient to report erections lasting >4 hours","Use with caution in patients with bleeding disorders or anticoagulant therapy","May cause hypotension or syncope","Do not use in patients with anatomical penis deformities","Do not use in patients with sickle cell anemia, multiple myeloma, or leukemia"] |
| Food/Dietary | No significant food interactions. Alcohol may reduce erectile response; limit consumption. |
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| Monitor maternal blood pressure, heart rate, and signs of priapism. Fetal assessment via ultrasound for growth and well-being if used in pregnancy. |
| Fertility Effects | No known adverse effects on fertility in animal studies. In men, used for erectile dysfunction; no impact on spermatogenesis. In women, effects unknown. |
| Clinical Pearls | Use a 27-30 gauge needle to minimize pain. Rotate injection sites between the left and right corpus cavernosum to prevent fibrosis. Do not exceed 2 injections per week with at least 24 hours between doses. The initial dose must be administered under medical supervision to detect priapism. Alprostadil can cause hypotension if injected intravascularly; aspirate before injecting. |
| Patient Advice | Injection should be given at the base of the penis into the side (corpus cavernosum), avoiding visible veins. · After injection, apply pressure to the injection site for 5 minutes to prevent bruising. · Do not use more than 2 times per week, with at least 24 hours between doses. · Seek emergency care if erection lasts longer than 4 hours (priapism). · The medication should be stored in the refrigerator (36-46°F) and protected from light. · Do not reuse needles; dispose of sharps properly. |