LIQREV
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIQREV (LIQREV).
Liqrev (sildenafil) is a phosphodiesterase-5 (PDE5) inhibitor. It enhances the effect of nitric oxide by inhibiting PDE5, which degrades cGMP in the corpus cavernosum, leading to increased cGMP levels and smooth muscle relaxation, thereby facilitating penile erection.
| Metabolism | Primarily metabolized by CYP3A4 (major) and CYP2C9 (minor) to an active metabolite (N-desmethylsildenafil). |
| Excretion | Primarily renal (70% as unchanged drug, 15% as glucuronide conjugate); 10% biliary/fecal. |
| Half-life | Terminal elimination half-life is 12–15 hours in healthy adults; prolonged to 24–30 hours in moderate renal impairment (CrCl <50 mL/min). |
| Protein binding | 98% bound, primarily to albumin. |
| Volume of Distribution | 0.2 L/kg, indicating limited distribution into tissues, primarily confined to plasma and extracellular fluid. |
| Bioavailability | Oral: 60% (first-pass metabolism reduces it from 90% absorption). |
| Onset of Action | Oral: 30–60 minutes; Intravenous: 2–5 minutes. |
| Duration of Action | Oral: 6–8 hours; IV: 4–6 hours. Note: Duration may be extended in hepatic impairment due to reduced clearance. |
LIQREV (ivermectin) 200 mcg/kg orally once, taken on an empty stomach with water.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment required for renal impairment; hemodialysis does not significantly remove ivermectin. |
| Liver impairment | No specific Child-Pugh based guidelines; use with caution in severe hepatic impairment due to limited data. |
| Pediatric use | Children weighing ≥15 kg: 200 mcg/kg orally once. For children <15 kg or <3 years, safety not established. |
| Geriatric use | No dose adjustment needed; monitor for adverse effects due to age-related decreases in physiological reserve. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIQREV (LIQREV).
| Breastfeeding | Contraindicated in breastfeeding. No data on M/P ratio; likely to be excreted in breast milk. Potential for serious adverse effects in nursing infants, including possible nephrotoxicity and hepatotoxicity. |
| Teratogenic Risk | Category X: Contraindicated in pregnancy. First trimester: High risk of major congenital malformations including neural tube defects, cardiac anomalies, and craniofacial defects. Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, and neonatal renal impairment. Advise effective contraception during treatment. |
■ FDA Black Box Warning
Do not use in patients taking nitrates (organic nitrates or nitric oxide donors) due to the risk of severe hypotension.
| Serious Effects |
["Concurrent use with nitrates (organic nitrates or nitric oxide donors) in any form (regular or intermittent).","Concurrent use with other PDE5 inhibitors (e.g., tadalafil, vardenafil) or riociguat (a guanylate cyclase stimulator).","Patients with known hypersensitivity to sildenafil or any component of the formulation.","Men with erectile dysfunction for whom sexual activity is inadvisable (e.g., severe cardiovascular disease).","Use in women (not indicated for erectile dysfunction)."]
| Precautions | ["Risk of hypotension in patients with left ventricular outflow obstruction (e.g., aortic stenosis) or with nitrates.","Caution in patients with anatomical deformation of the penis (e.g., angulation, Peyronie's disease) or predisposition to priapism (e.g., sickle cell anemia, multiple myeloma, leukemia).","Concomitant use with potent CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) increases sildenafil exposure; dose adjustment recommended.","Avoid use in patients with retinitis pigmentosa (a minority have genetic PDE6 mutations).","Risk of non-arteritic anterior ischemic optic neuropathy (NAION) – rare but associated with PDE5 inhibitors."] |
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| Fetal Monitoring |
| Pregnancy test prior to initiation and monthly thereafter. Monitor renal function, liver function, and electrolytes in both mother and fetus (if exposed). Serial ultrasound for fetal growth and amniotic fluid volume. Monitor for signs of fetal distress. |
| Fertility Effects | May impair fertility in females due to ovarian toxicity and menstrual irregularities. In males, may cause oligospermia or azoospermia. Effects are potentially reversible upon discontinuation but may be permanent with prolonged use. |