爱悦达 盐酸伐地那非片, Vardenafil Hydrochloride Tablets, 10mg (8 tablets/box), for Erectile Dysfunction, ED

Drug Name
Vardenafil Hydrochloride Tablets

Ingredients
Active Ingredient: Vardenafil Hydrochloride
Chemical Name: 2-[2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one monohydrochloride trihydrate
Molecular Formula: C₂₃H₃₂N₆O₄S·HCl·3H₂O
Molecular Weight: 579.1

Physical Characteristics
This product is a light yellow to dark yellow film-coated tablet, white after removal of the film coat.

Indications
Treatment of male erectile dysfunction.

Storage
Store at room temperature.

Specifications
10 mg × 8 tablets

Expiration
24 months

Dosage and Administration
Administration: Oral
Recommended Dose: The recommended starting dose is 10 mg, taken approximately 25–60 minutes before sexual activity. In clinical trials, efficacy was observed when taken 4–5 hours prior to sexual activity. The maximum recommended dosing frequency is once daily. Vardenafil may be taken with or without food. Sexual stimulation is required for a response.
Dose Adjustment: The dose may be increased to 20 mg or decreased to 5 mg based on efficacy and tolerability. The maximum recommended daily dose is 20 mg.
Hepatic Impairment:

• Mild hepatic impairment (Child-Pugh A): No dose adjustment required.
• Moderate hepatic impairment (Child-Pugh B): Initiate therapy at 5 mg, with subsequent adjustment to 10 mg based on tolerability and efficacy.
• Severe hepatic impairment (Child-Pugh C): Pharmacokinetic studies have not been conducted.
  Renal Impairment: No dose adjustment is required for mild, moderate, or severe renal impairment. Pharmacokinetic studies in dialysis patients have not been conducted.
  Concomitant Medications:
• Co-administration with α-blockers may cause symptomatic hypotension. Initiate therapy at the lowest recommended starting dose (5 mg) in patients stabilized on α-blocker therapy. A dose interval should be observed when co-administered with other α-blockers.
• CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, indinavir, erythromycin) may require dose adjustment. The maximum dose of vardenafil should not exceed 5 mg when co-administered with erythromycin. Avoid co-administration with strong CYP3A4 inhibitors (e.g., indinavir, ritonavir).

Adverse Reactions
Frequency of Adverse Drug Reactions (ADRs): The table summarizes the frequency of ADRs reported with vardenafil, categorized by severity. Frequencies are defined as: Very Common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1000 to <1/100), Rare (≥1/10,000 to <1/1000), Very Rare (<1/10,000). ADRs detected only during post-marketing surveillance and with unestimable frequency are listed under "Unknown."

Contraindications

• Hypersensitivity to vardenafil or any excipients.
• Concomitant use with nitrates or nitric oxide donors (may enhance hypotensive effects).
• Concomitant use with HIV protease inhibitors (e.g., indinavir, ritonavir) due to strong CYP3A4 inhibition.

Precautions

• Cardiovascular Risk: Sexual activity carries inherent cardiac risk. Evaluate cardiac status before initiating therapy. Vardenafil may cause mild, transient hypotension. Use with caution in patients with left ventricular outflow obstruction (e.g., aortic stenosis, idiopathic hypertrophic subaortic stenosis). Avoid sexual activity in patients with unstable cardiovascular conditions.
• QT Prolongation: Vardenafil may prolong the QTc interval. Use with caution in patients with congenital QT prolongation or those receiving Class IA (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmics.
• Anatomical Penile Deformities: Use with caution in patients with anatomical deformities (e.g., Peyronie's disease) or conditions predisposing to priapism (e.g., sickle cell anemia, leukemia).
• Combination Therapy: Safety and efficacy of combination with other erectile dysfunction treatments have not been established.

Special Populations
Pediatric Use: Not indicated for use in children (birth to 16 years).
Pregnancy and Lactation: Not studied; no references available.

Drug Interactions

• Nitrates/NO Donors: Concomitant use with vardenafil may enhance hypotensive effects. Avoid co-administration.
• CYP Inhibitors:
• Cimetidine: No significant effect on vardenafil pharmacokinetics.
• Erythromycin: Increases vardenafil AUC and Cmax by 300% and 200%, respectively.
• Ketoconazole: Increases vardenafil AUC and Cmax by 900% and 300%, respectively.
• Indinavir: Increases vardenafil AUC by 1500% and Cmax by 600%.
• Ritonavir: Increases vardenafil Cmax by 13-fold and AUC by 49-fold.
• α-Blockers: Concomitant use may cause symptomatic hypotension. A dose interval is recommended.

Pharmacological Actions
Pharmacodynamics: Vardenafil inhibits PDE5, increasing cGMP levels and enhancing erectile function. Sexual stimulation is required for efficacy. Vardenafil is a selective PDE5 inhibitor with >15-fold selectivity for PDE5 over PDE6 and >1000-fold selectivity over other PDE isoforms.
Toxicology:

• Genotoxicity: Negative in Ames test, V79 cell mutation assay, chromosomal aberration test, and mouse micronucleus test.
• Reproductive Toxicity: No effects on fertility at doses up to 100 mg/kg/day in rats. No teratogenicity observed in rats or rabbits at doses up to 18 mg/kg/day.
• Carcinogenicity: No carcinogenicity observed in rats or mice after 24 months of dosing.