Dapoxetine + Tadalafil

Usage

• Dapoxetine + Tadalafil is prescribed for the treatment of premature ejaculation and erectile dysfunction in men.
• Pharmacological classification: This combination drug falls under two classifications:
  • Dapoxetine: Selective Serotonin Reuptake Inhibitor (SSRI)
  • Tadalafil: Phosphodiesterase-5 (PDE5) inhibitor
• Mechanism of action: Tadalafil increases blood flow to the penis by inhibiting PDE5, facilitating erection. Dapoxetine increases serotonin levels, delaying ejaculation.

Alternate Names

• While “Dapoxetine + Tadalafil” represents the generic name, the combination is often marketed under brand names like Tadapox, Dapoxitime Long and others.

How It Works

• Pharmacodynamics: Tadalafil relaxes smooth muscles in the penis, allowing increased blood flow for erection upon sexual stimulation. Dapoxetine increases serotonin’s action at the synaptic cleft, delaying ejaculation.

• Pharmacokinetics:

  • Tadalafil is readily absorbed after oral administration, reaching peak plasma concentration in approximately 2 hours. It is metabolized primarily by CYP3A4 enzymes in the liver. Elimination is mainly through hepatic metabolism.

  • Dapoxetine is also rapidly absorbed with peak plasma concentration occurring around 1-2 hours after oral administration. It is extensively metabolized by the liver, primarily via CYP2D6 and CYP3A4.

• Mode of action: Tadalafil inhibits PDE5, preventing the breakdown of cyclic guanosine monophosphate (cGMP). Increased cGMP levels promote smooth muscle relaxation in the corpus cavernosum, leading to increased blood flow and erection. Dapoxetine inhibits the serotonin transporter, increasing serotonin levels in the synaptic cleft, delaying ejaculation.

• Elimination pathways: Both tadalafil and dapoxetine are primarily metabolized in the liver and excreted via urine and feces.

Dosage

Standard Dosage

Adults:

• The typical dose is one tablet containing 20mg tadalafil and 60mg dapoxetine, taken 1 to 3 hours before sexual activity. The maximum frequency is once per 24 hours.

Children:

• Dapoxetine + Tadalafil is contraindicated in children. Its safety and effectiveness have not been established in this population.

Special Cases:

• Elderly Patients: Dosage adjustments may be necessary based on individual tolerability and comorbidities. Close monitoring for side effects is important.
• Patients with Renal Impairment: Caution is advised, and dose adjustments may be necessary in patients with moderate to severe renal impairment.
• Patients with Hepatic Dysfunction: Dose adjustments may be required. The drug should be avoided in patients with severe hepatic dysfunction.
• Patients with Comorbid Conditions: Patients with cardiovascular disease, hypotension, or other relevant conditions need careful assessment before initiation.

Clinical Use Cases

Dapoxetine + Tadalafil is not indicated for use in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is specifically designed for the treatment of erectile dysfunction and premature ejaculation.

Dosage Adjustments

Dosage adjustments should be based on individual patient response, tolerability, and coexisting medical conditions, especially renal and hepatic impairment.

Side Effects

Common Side Effects

Headache, dizziness, nausea, diarrhea, flushing, insomnia, nasal congestion, and back pain.

Rare but Serious Side Effects

• Allergic reactions (e.g., rash, itching, swelling), vision changes (blurred vision, sudden loss of vision), priapism (prolonged erection lasting more than four hours), syncope, hypotension, mood changes (anxiety, depression), and seizures. These require immediate medical attention.

Long-Term Effects

Limited data exists on the long-term effects of the combined use of dapoxetine and tadalafil. Regular monitoring for potential adverse effects is advisable.

Adverse Drug Reactions (ADR)

Clinically significant ADRs that necessitate immediate intervention include severe allergic reactions, sudden vision or hearing loss, and priapism.

Contraindications

• Severe hepatic impairment, end-stage renal disease requiring dialysis, hypersensitivity to either component, recent myocardial infarction, unstable angina, uncontrolled hypertension, severe hypotension, history of non-arteritic anterior ischemic optic neuropathy (NAION), bleeding disorders, mania, or bipolar disorder.

Drug Interactions

• Nitrates (e.g., nitroglycerin), alpha-blockers, CYP3A4 inhibitors (e.g., ketoconazole, erythromycin), MAO inhibitors, SSRIs, SNRIs, and other serotonergic drugs can interact significantly with Dapoxetine + Tadalafil. Alcohol should be avoided or consumed with caution due to the potential for increased side effects like dizziness and hypotension.

Pregnancy and Breastfeeding

Dapoxetine + Tadalafil is contraindicated in women, including pregnant and breastfeeding individuals. Its safety and efficacy in these populations have not been established.

Drug Profile Summary

• Mechanism of Action: Tadalafil inhibits PDE5, promoting erection. Dapoxetine inhibits serotonin reuptake, delaying ejaculation.
• Side Effects: Common: Headache, dizziness, nausea. Serious: Priapism, vision changes, allergic reactions.
• Contraindications: Severe liver/kidney disease, heart conditions, hypotension, NAION history, hypersensitivity.
• Drug Interactions: Nitrates, alpha-blockers, CYP3A4 inhibitors, MAOIs, SSRIs, alcohol.
• Pregnancy & Breastfeeding: Contraindicated.
• Dosage: 20mg Tadalafil/60mg Dapoxetine, 1-3 hours before sexual activity, maximum once daily.
• Monitoring Parameters: Blood pressure, heart rate, vision changes, signs of allergic reaction, and prolonged erection.

Popular Combinations

Dapoxetine + Tadalafil itself represents a popular fixed-dose combination. Generally, it’s not recommended to combine it with other drugs for ED or PE due to potential drug interactions and increased risk of adverse effects.

Precautions

• Evaluate cardiovascular health, screen for contraindications, and advise patients on potential side effects, drug interactions, and precautions regarding alcohol consumption and driving.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Dapoxetine + Tadalafil?

A: One tablet containing 20mg Tadalafil and 60mg Dapoxetine, taken 1 to 3 hours before sexual activity, not exceeding once in 24 hours.

Q2: Can Dapoxetine + Tadalafil be taken daily?

A: No, it’s not recommended for daily use. It’s intended for on-demand use before anticipated sexual activity.

Q3: What are the most common side effects?

A: Headache, dizziness, nausea, flushing, and nasal congestion.

Q4: Who should not take Dapoxetine + Tadalafil?

A: Individuals with severe heart, liver, or kidney problems, uncontrolled high blood pressure, history of NAION, hypersensitivity to either component, and those taking nitrates or certain other medications.

Q5: How does Dapoxetine + Tadalafil work?

A: Tadalafil increases blood flow to the penis, aiding in achieving and maintaining an erection. Dapoxetine increases serotonin levels, leading to delayed ejaculation.

Q6: Can I drink alcohol while taking Dapoxetine + Tadalafil?

A: It’s advisable to avoid or limit alcohol consumption. Alcohol can increase the risk of side effects like dizziness and low blood pressure.

Q7: What should I do if I experience a prolonged erection (lasting more than four hours)?

A: Seek immediate medical attention. Priapism is a serious side effect and requires urgent intervention.

Q8: Can women take Dapoxetine + Tadalafil?

A: No, this medication is contraindicated for use in women.

Q9: Are there any drug interactions I should be aware of?

A: Yes, several. Inform your doctor about all medications you are taking, including nitrates, alpha-blockers, and certain antidepressants. Avoid grapefruit juice, as it can affect drug metabolism.