盐酸达泊西汀片, Dapoxetine Hydrochloride Tablets, Yansuan Daboxiting Pian, 30mg (6 tablets/box), for Premature Ejaculation (PE) in Adult Men

Drug Name
Dapoxetine Hydrochloride Tablets
盐酸达泊西汀片

Active Ingredient:
Dapoxetine Hydrochloride

Inactive Ingredients:
Microcrystalline cellulose-lactose, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate, and film coating premix.

Indications and Usage:
This product is indicated for the treatment of premature ejaculation (PE) in adult men aged 18 to 64 years who meet all the following criteria:

• Intravaginal ejaculatory latency time (IELT) of less than 2 minutes;
• Persistent or recurrent ejaculation with minimal sexual stimulation before, during, or shortly after vaginal penetration, and prior to or shortly after penetration and before desired sexual satisfaction;
• Significant personal distress or interpersonal difficulty due to PE;
• Poor ejaculatory control;
• History of PE in most sexual encounters over the past 6 months.

Storage:
Store at room temperature.

Strength:
30 mg (calculated as C21H23NO)

Packaging:
Aluminum-plastic packaging with PVC solid pharmaceutical hard sheets and pharmaceutical aluminum foil. Each blister contains 6 tablets, with 1 blister per box.

Expiration:
36 months

Dosage and Administration:
Oral administration. Swallow tablets whole with at least one full glass of water to minimize the risk of orthostatic hypotension-related adverse reactions (e.g., syncope, dizziness).

Adult Males (18–64 years):

• Recommended starting dose: 30 mg, taken 1–3 hours prior to anticipated sexual activity.
• Maximum dose: 60 mg (only for patients who do not achieve adequate efficacy with 30 mg and do not experience moderate or severe adverse reactions or prodromal symptoms suggestive of syncope).
• Frequency: Not for daily use. Maximum recommended frequency is one dose every 24 hours.
• Administration: May be taken with or without food (refer to [Pharmacokinetics]).

Clinical Evaluation:

• Evaluate risk-benefit balance after the initial 4 weeks of treatment or after 6 doses. For extended use beyond 24 weeks, reassess clinical need and risk-benefit profile every 6 months.

Geriatric Use (≥65 years):
Safety and efficacy not established due to limited data.

Pediatric Use (<18 years):
Not indicated for use in children or adolescents.

Renal Impairment:

• Mild/moderate impairment: No dose adjustment required; use with caution.
• Severe impairment: Not recommended.

Hepatic Impairment:

• Mild impairment: No dose adjustment required.
• Moderate/severe impairment (Child-Pugh Class C): Contraindicated.

CYP2D6 Poor Metabolizers/CYP3A4 Inhibitors:

• CYP2D6 poor metabolizers or patients on strong CYP2D6 inhibitors: Caution with dose escalation to 60 mg.
• Strong CYP3A4 inhibitors: Contraindicated. Moderate CYP3A4 inhibitors: Limit dose to 30 mg and use with caution.

Adverse Reactions:
Common dose-related adverse reactions in Phase 3 trials include nausea (11.0%/22.2% for 30 mg/60 mg), dizziness (5.8%/10.9%), headache (5.6%/8.8%), diarrhea (3.5%/6.9%), insomnia (2.1%/3.9%), and fatigue (2.0%/4.1%). Syncope and orthostatic hypotension have been reported, with prodromal symptoms (e.g., nausea, dizziness) occurring more frequently than with placebo.

Contraindications:

• Hypersensitivity to dapoxetine or any excipients.
• Cardiac conditions (e.g., heart failure, significant conduction abnormalities, severe ischemic heart disease).
• History of mania/hypomania or major depression.
• Concurrent use of MAOIs, thioridazine, SSRIs/SNRIs/TCAs, or serotonergic herbs (e.g., St. John’s Wort) within 14 days of discontinuation.
• Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir).
• Moderate/severe hepatic impairment.

Warnings and Precautions:

• Orthostatic Hypotension: Assess orthostatic vital signs before initiating therapy. Advise patients to avoid situations requiring alertness (e.g., driving) if prodromal symptoms occur.
• Syncope: Educate patients on recognizing prodromal symptoms and the importance of hydration. Advise lying down immediately if symptoms arise.
• Psychiatric Disorders: Monitor for suicidality, mania, or seizure exacerbation. Discontinue if symptoms emerge.
• Drug Interactions: Avoid concomitant use with recreational drugs (e.g., MDMA), alcohol, or vasodilators (e.g., α-blockers, nitrates).
• Discontinuation Syndrome: Gradual tapering may be required after prolonged use.

Special Populations:

• Pediatric/Geriatric/Pregnant/Lactating Women: Not indicated or studied in these populations.

Drug Interactions:

• MAOIs/Thioridazine: Contraindicated due to risk of serotonin syndrome or QTc prolongation.
• CYP Inhibitors: Dose adjustments required for strong CYP2D6/CYP3A4 inhibitors.

Pharmacology:
Dapoxetine, a selective serotonin reuptake inhibitor (SSRI), modulates ejaculatory reflexes by inhibiting serotonin reuptake, thereby enhancing neurotransmitter activity at pre- and post-synaptic receptors.