Susten 30mg Tablet

Description

Indications
Susten is indicated for the treatment of premature ejaculation (PE) in men aged 18 to 64 years who have one or more of the following:

• Persistent or recurrent ejaculation with minimal sexual stimulation before, on, or shortly after penetration, and before the patient wishes.
• Marked personal distress or interpersonal difficulty as a result of PE.
• Poor control over ejaculation.
  Use the medication as directed by a registered healthcare professional.

Pharmacology
The mechanism of action of Dapoxetine in treating premature ejaculation is linked to the inhibition of serotonin reuptake and the subsequent enhancement of serotonin’s action at pre- and post-synaptic receptors. Human ejaculation is primarily mediated by the sympathetic nervous system, with the ejaculatory pathway originating from a spinal reflex center and being influenced by several brain nuclei.

Dapoxetine is rapidly absorbed, reaching maximum plasma concentrations (Cmax) about 1-2 hours after ingestion. The absolute bioavailability is 42%, and more than 99% of Dapoxetine binds to human serum proteins. The active metabolite, Desmethyl Dapoxetine (DED), is 98.5% protein bound. The drug has a rapid distribution with a steady-state volume of distribution of 162 L. Dapoxetine is metabolized extensively into multiple metabolites, primarily via N-oxidation, N-demethylation, Naphthyl hydroxylation, glucuronidation, and sulfation. Evidence of presystemic first-pass metabolism after oral administration exists, with metabolites primarily eliminated through urine as conjugates. The terminal half-life of Dapoxetine is approximately 19 hours.

Dosage & Administration
For Premature Ejaculation:

• Adult men (18-64 years): The recommended starting dose is 30 mg, taken as needed, approximately 1 to 3 hours before sexual activity. The maximum recommended dosing frequency is once every 24 hours. If 30 mg is insufficient and side effects are acceptable, the dose may be increased to 60 mg. Dapoxetine may be taken with or without food.
• Children and adolescents: Dapoxetine should not be used in individuals under 18 years of age.
• Elderly (65 years and over): Safety and efficacy have not been established for this population, as limited data are available.
• Renal impairment: Caution is advised in patients with mild or moderate renal impairment. Dapoxetine is not recommended for patients with severe renal impairment.
• Hepatic impairment: Dapoxetine is contraindicated in patients with moderate or severe hepatic impairment.
  Always use the medication under the guidance of a registered healthcare professional.

Interaction

• CNS active medicinal products: The use of Susten with CNS active drugs has not been systematically studied in patients with premature ejaculation. Caution is advised when combining Susten with these drugs.
• PDE5 inhibitors: Tadalafil does not affect the pharmacokinetics of Susten. Sildenafil causes minor changes in pharmacokinetics that are not clinically significant. However, Susten should be prescribed cautiously to patients using PDE5 inhibitors due to possible reduced orthostatic tolerance.
• Tamsulosin: No changes were observed in the pharmacokinetics of Tamsulosin when administered with 30 mg or 60 mg doses of Susten. However, caution is recommended for patients using alpha-adrenergic receptor antagonists.
• Warfarin: There is no data on the effect of chronic Warfarin use with Susten; caution is advised for patients on Warfarin.
• Ethanol: Combining alcohol with Susten could increase adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. The combination may also heighten neurocardiogenic adverse events like syncope, increasing the risk of accidental injury. Patients should be advised to avoid alcohol while using Susten.

Contraindications
Susten is contraindicated in:

• Patients with hypersensitivity to Dapoxetine Hydrochloride.
• Patients with significant cardiac conditions such as heart failure (NYHA class II-IV), conduction abnormalities, ischemic heart disease, or significant valvular disease.
• Patients undergoing treatment with monoamine oxidase inhibitors (MAOIs) or thioridazine, or within 14 days after discontinuing treatment with MAOIs.
• Patients using serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), or other serotonergic drugs/herbal products, or within 14 days after stopping these products.

Side Effects
Common side effects of Susten include:

• Nausea, dizziness, dry mouth, headache, diarrhea, and insomnia.
  Discontinuation due to side effects is dose-related. Discontinuation rates were 0.3%, 1.7%, and 5.3% for placebo, Susten 30 mg, and Susten 60 mg, respectively. Unlike other SSRIs, Susten is associated with low rates of sexual dysfunction. It has very mild effects on libido (<1%) and erectile dysfunction (<4%).

Pregnancy & Lactation
Dapoxetine is not indicated for use by women, and it is not known whether Dapoxetine or its metabolites are excreted in human breast milk.

Precautions & Warnings

• Recreational drugs: Susten should not be used with recreational drugs, particularly those with serotonergic effects like ketamine, MDMA, and LSD, as they may cause serious reactions, including arrhythmias, hyperthermia, and serotonin syndrome.
• Ethanol: Avoid alcohol while taking Susten, as it may enhance neurocognitive and neurocardiogenic effects.
• Syncope: Some patients may experience syncope, often preceded by symptoms like nausea, dizziness, or confusion.
• Orthostatic hypotension: Perform an orthostatic test before starting therapy, especially in patients with a history of orthostatic reactions.
• Bleeding risk: Caution is advised in patients taking blood-thinning medications or those with a history of bleeding disorders.
• PDE5 inhibitors: Tadalafil and Sildenafil do not significantly affect the pharmacokinetics of Susten.
• Tamsulosin: Caution is needed when combining Susten with alpha-adrenergic receptor antagonists.

Overdose Effects
No overdose cases have been reported. In clinical trials, daily doses up to 240 mg (two 120 mg doses 3 hours apart) did not result in unexpected adverse effects. Symptoms of overdose may include serotonin-mediated reactions such as somnolence, gastrointestinal disturbances, tachycardia, tremor, agitation, and dizziness.

Therapeutic Class
Drugs for Erectile Dysfunction

Storage Conditions
Store below 30°C, protected from light and moisture. Keep out of reach of children.