TADLIQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TADLIQ (TADLIQ).
Tadliq contains the active ingredient tadalafil, a phosphodiesterase-5 (PDE5) inhibitor. It enhances the effect of nitric oxide (NO) by inhibiting PDE5, which increases cGMP levels in corpus cavernosum smooth muscle, leading to relaxation and increased blood flow to the penis, facilitating erection. It also inhibits PDE5 in pulmonary vasculature, causing vasodilation.
| Metabolism | Primarily metabolized by CYP3A4 to an active metabolite (methylcatechol glucuronide). Also minor metabolism by CYP3A5 and CYP2C9. |
| Excretion | Primarily renal (approx. 80% as unchanged drug), with biliary/fecal elimination accounting for ~10-15%. |
| Half-life | 34-48 hours in healthy adults; may be prolonged in renal impairment (e.g., up to 100 hours in severe impairment), necessitating dose adjustment. |
| Protein binding | ~95% bound, primarily to albumin. |
| Volume of Distribution | Approximately 0.3-0.5 L/kg, indicating distribution mainly in extracellular fluid. |
| Bioavailability | Oral: 60-80%; subcutaneous: >90%. |
| Onset of Action | Oral: 1-2 hours; subcutaneous: 30-60 minutes. |
| Duration of Action | 24-48 hours (dose-dependent); therapeutic effect may persist 72 hours due to long half-life. |
| Molecular Weight | 523.6 |
TADLIQ (tadalafil) 2.5-5 mg orally once daily at approximately the same time of day; maximum 5 mg once daily.
| Dosage form | SUSPENSION |
| Renal impairment | CrCl 30-50 mL/min: 2.5 mg once daily; CrCl <30 mL/min: not recommended; hemodialysis: not studied. |
| Liver impairment | Child-Pugh A or B: 2.5 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy not established; no approved dosing. |
| Geriatric use | No dose adjustment required; consider age-related renal impairment and increased sensitivity. |
| 1st trimester | Avoid due to teratogenic risk; contraindicated in pregnancy. |
| 2nd trimester | Avoid; risk of fetal harm. |
| 3rd trimester | Avoid; may cause neonatal respiratory depression. |
Clinical note
Comprehensive clinical and safety monograph for TADLIQ (TADLIQ).
| Placental transfer | Crosses placenta; detected in fetal cord blood. |
| Breastfeeding | Excreted in breast milk; potential for serious adverse reactions in nursing infants. Discontinue drug or nursing. |
| Lactation Rating | L5 - Avoid |
■ FDA Black Box Warning
None.
| Serious Effects |
PregnancyHypersensitivity to drug or any component
| Precautions | Cardiovascular risk: Use not recommended in patients with unstable angina, recent MI, stroke, or uncontrolled hypertension., Priapism: Prolonged erection (>4 hours) requires immediate medical attention., Hearing loss: Sudden decrease or loss of hearing has been reported., Vision loss: Non-arteritic anterior ischemic optic neuropathy (NAION) has been reported., Avoid use with nitrates due to risk of severe hypotension., Caution in patients with severe renal or hepatic impairment., Not recommended for use with alpha-blockers (except for PAH indication) due to risk of hypotension. |
| Food/Dietary | High-fat meals may delay absorption and onset of action; avoid grapefruit products as they can increase tadalafil levels. Alcohol may increase risk of hypotension and dizziness. |
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| Teratogenic Risk |
| TADLIQ is not FDA-approved; no human pregnancy data. Animal studies suggest developmental toxicity only at maternally toxic doses. Theoretical risk of teratogenicity cannot be excluded; avoid in first trimester unless benefit outweighs risk. |
| Fetal Monitoring | Monitor liver function tests, renal function, and complete blood count periodically. Fetal ultrasound if used in pregnancy. |
| Fertility Effects | No human fertility studies. Animal studies show no impairment at clinically relevant doses. |
| Clinical Pearls | TADLIQ (tadalafil) is a PDE5 inhibitor used for erectile dysfunction (ED) and benign prostatic hyperplasia (BPH). Avoid co-administration with nitrates due to risk of severe hypotension. Use with caution in patients with left ventricular outflow obstruction or severe hepatic impairment. Monitor for sudden vision loss (non-arteritic ischemic optic neuropathy) or hearing loss. Onset of action is 30-60 minutes; effect lasts up to 36 hours. Dose adjustment needed in renal impairment (CrCl <30 mL/min). |
| Patient Advice | Do not take TADLIQ if you are taking nitrates for chest pain or heart problems; this can cause a dangerous drop in blood pressure. · Avoid consuming grapefruit or grapefruit juice while taking this medication as it may increase side effects. · Seek immediate medical attention if you experience sudden vision loss or hearing loss. · If you have an erection lasting more than 4 hours, seek emergency help to avoid permanent damage. · TADLIQ can be taken with or without food, but high-fat meals may delay onset of action. · Do not take more than one dose per day. |