Extreme

Approved Indications:

• Premature Ejaculation (PE):
• Treatment of premature ejaculation in adult men aged 18–64 years.
• Indicated for men with a history of ejaculation occurring within approximately 1 to 2 minutes of vaginal penetration and inability to delay ejaculation.

Clinically Accepted Off-label Uses:

• Sometimes used off-label for other forms of ejaculatory dysfunction or sexual dysfunction, but evidence is limited.

Adults (18–64 years):

• Initial recommended dose: 30 mg orally, taken 1 to 3 hours before anticipated sexual activity.
• Depending on efficacy and tolerability, dose may be increased to 60 mg.
• Maximum dosing frequency: once every 24 to 72 hours; not intended for daily use.

Elderly (>64 years):

• Safety and efficacy not well established; use with caution.

Pediatrics (<18 years):

• Not recommended.

Special Populations:

• Use caution in patients with mild to moderate hepatic impairment; dose adjustment not established.
• Not recommended in severe hepatic or renal impairment.

Administration:

• Oral tablets; take with water. Food does not significantly affect absorption.

Dapoxetine is a short-acting selective serotonin reuptake inhibitor (SSRI) that increases serotonin activity in the synaptic cleft by inhibiting its reabsorption (reuptake) into the presynaptic neuron. Increased serotonin levels at specific receptors, especially 5-HT2c and 5-HT1a, enhance the inhibitory control over ejaculation reflex pathways in the central nervous system, thereby delaying ejaculation and increasing latency time during sexual activity. Its rapid absorption and elimination provide on-demand efficacy with reduced systemic side effects compared to longer-acting SSRIs.

Absorption:

• Rapidly absorbed with peak plasma concentration reached approximately 1 to 2 hours post-dose.

Distribution:

• Volume of distribution ~164 L; approximately 99% plasma protein bound.

Metabolism:

• Extensively metabolized primarily by CYP2D6 and CYP3A4 enzymes in the liver.

Elimination:

• Metabolites excreted mainly via urine and feces.
• Plasma half-life approximately 1.5 to 1.9 hours, supporting short duration of action.

• Pregnancy:
• Not indicated for use in females; no pregnancy category assigned.
• Lactation:
• Safety not established; use caution if exposed.

• Primary Class: Selective serotonin reuptake inhibitor (SSRI)
• Subclass: Short-acting SSRI used for sexual dysfunction

• Known hypersensitivity to dapoxetine or any formulation excipients.
• Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping MAOIs.
• Use with thioridazine or other medications contraindicated due to QT prolongation risk.
• Significant cardiac conditions including congenital long QT syndrome.
• Severe hepatic impairment.
• Use with potent CYP3A4 inhibitors is contraindicated.

• Cardiac Risk: Caution in patients with known QT prolongation, history of syncope, or family history of sudden cardiac death.
• Psychiatric Effects: Possible risk of suicidal ideation, anxiety, or agitation.
• Serotonin Syndrome: Risk increased when used with other serotonergic agents.
• CNS Effects: May cause dizziness, somnolence; caution driving or operating machinery.
• Use in Renal Impairment: Limited data; use cautiously in mild to moderate cases.
• Risk of Orthostatic Hypotension: Especially in combination with alcohol or antihypertensives.

Common:

• Nausea
• Dizziness
• Headache
• Diarrhea
• Insomnia
• Fatigue
• Dry mouth

Serious/Rare:

• Syncope or loss of consciousness
• Serotonin syndrome
• QT prolongation and arrhythmias (rare)
• Suicidal thoughts (rare)

• MAO Inhibitors: Risk of serotonin syndrome; contraindicated.
• Potent CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir): Increase dapoxetine levels; contraindicated.
• Other SSRIs or Serotonergic Drugs: Increased risk of serotonin syndrome.
• Drugs that prolong QT interval: Increased arrhythmia risk.
• Alcohol: May increase CNS depression and risk of orthostatic hypotension.

• Regulatory agencies emphasize contraindications with MAOIs and potent CYP3A4 inhibitors.
• Updated warnings about rare but serious cardiac effects have been included in labeling.
• Increasing clinical consensus supports dapoxetine as an effective on-demand treatment option for premature ejaculation with a favorable safety profile compared to chronic SSRIs.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep tablets in original packaging until use.
• Do not freeze.
• Keep out of reach of children.