Susten 30 mg

Description

Indications

Susten is prescribed for the management of premature ejaculation (PE) in adult men aged 18 to 64 years who experience one or more of the following conditions:

• Persistent or recurrent ejaculation occurring with minimal sexual stimulation, either before, during, or shortly after penetration, occurring sooner than the individual desires.
• Significant distress or difficulties in interpersonal relationships due to premature ejaculation.
• Limited control over the timing of ejaculation.

Note: Always take this medication as per the advice of a registered physician.

Pharmacology

Dapoxetine, the active ingredient in Susten, is believed to function by inhibiting the neuronal reuptake of serotonin, thereby enhancing its action at both pre- and post-synaptic receptors. Ejaculation in males is mainly regulated by the sympathetic nervous system, involving a reflex mechanism in the spinal cord that is influenced by brain structures such as the medial preoptic and paraventricular nuclei.

Dapoxetine is rapidly absorbed, reaching peak plasma concentration (Cmax) within 1-2 hours after oral intake. It has an absolute bioavailability of 42%, with over 99% of the drug binding to plasma proteins. The active metabolite, desmethyl dapoxetine (DED), is 98.5% protein-bound. The drug is widely distributed in the body, with a mean steady-state volume of distribution of 162 L.

Metabolism of Dapoxetine occurs primarily through N-oxidation, N-demethylation, naphthyl hydroxylation, glucuronidation, and sulfation pathways. It undergoes extensive first-pass metabolism, and its metabolites are primarily eliminated through the urine. The drug has a short elimination half-life of approximately 19 hours, making it suitable for on-demand use.

Dosage & Administration

For Premature Ejaculation:

• Adult Men (18-64 years): The initial recommended dose is 30 mg, taken 1 to 3 hours before sexual activity.
• If 30 mg is insufficient, and the patient tolerates the medication well, the dosage may be increased to a maximum of 60 mg.
• The medication should not be taken more than once in 24 hours.
• Susten may be taken with or without food.

Use in Specific Populations:

• Children & Adolescents: Not recommended for individuals under 18 years of age.
• Elderly (65+ years): Safety and efficacy have not been established due to limited clinical data.
• Renal Impairment: Caution is advised in patients with mild to moderate renal impairment. Not recommended for those with severe renal impairment.
• Hepatic Impairment: Contraindicated in moderate and severe hepatic impairment cases.

Note: Always take Susten under the guidance of a licensed medical professional.

Drug Interactions

• CNS-Active Medications: The interaction of Susten with other CNS-active drugs has not been thoroughly studied. Caution is advised when combining these drugs.
• PDE5 Inhibitors (Tadalafil, Sildenafil): While Tadalafil does not affect the pharmacokinetics of Susten, Sildenafil may cause minor changes. However, caution is required as combining these drugs may affect orthostatic tolerance.
• Tamsulosin (Alpha-Blockers): Susten does not alter the pharmacokinetics of Tamsulosin, but caution is advised due to the potential risk of orthostatic hypotension.
• Warfarin (Blood Thinners): The effects of long-term Warfarin use with Susten are unknown; thus, caution is advised.
• Alcohol: The combination of Susten with alcohol can lead to increased dizziness, drowsiness, slower reflexes, impaired judgment, and a higher risk of syncope (fainting). It is recommended to avoid alcohol while taking Susten.

Contraindications

Susten should not be used in patients who have:

• Known hypersensitivity to Dapoxetine Hydrochloride.
• Severe cardiovascular conditions such as:
  • Heart failure (NYHA Class II-IV)
  • Significant conduction abnormalities (e.g., second- or third-degree AV block, sick sinus syndrome without a pacemaker).
  • Severe ischemic heart disease or valvular disorders.
• Current or recent (within 14 days) use of:
  • Monoamine oxidase inhibitors (MAOIs)
  • Thioridazine
  • Selective serotonin reuptake inhibitors (SSRIs), Serotonin-norepinephrine reuptake inhibitors (SNRIs), Tricyclic antidepressants (TCAs), or any serotonergic herbal supplements.

Side Effects

Common side effects associated with Susten include:

• Nausea
• Dizziness
• Dry mouth
• Headache
• Diarrhea
• Insomnia (difficulty sleeping)

Discontinuation due to side effects is dose-dependent, with 0.3% of placebo users, 1.7% of those taking 30 mg, and 5.3% of those on 60 mg stopping treatment due to adverse reactions. Unlike other SSRIs used for depression, Susten has a low incidence of sexual dysfunction, with less than 1% experiencing libido loss and less than 4% experiencing erectile dysfunction (ED).

Pregnancy & Lactation

Susten is not intended for use in women. It is unknown whether Dapoxetine or its metabolites pass into breast milk.

Precautions & Warnings

• Recreational Drug Use: Avoid combining Susten with recreational drugs, particularly those affecting serotonin levels (ketamine, MDMA, LSD), as it may lead to serious reactions such as arrhythmia, hyperthermia, and serotonin syndrome.
• Ethanol Consumption: Alcohol should be avoided due to the increased risk of neurocognitive impairment and syncope.
• Risk of Syncope: Some patients may experience sudden fainting episodes (syncope), often preceded by symptoms like nausea, dizziness, lightheadedness, palpitations, or sweating.
• Orthostatic Hypotension: Patients with a history of low blood pressure upon standing should avoid taking Susten.
• Bleeding Risks: Use with caution in patients taking NSAIDs, antiplatelets, anticoagulants, or those with bleeding disorders, as SSRIs have been linked to bleeding abnormalities.

Overdose Effects

Although no overdose cases have been reported, excessive intake may lead to serotonin-related adverse effects, including:

• Severe drowsiness
• Gastrointestinal issues (nausea, vomiting, diarrhea)
• Increased heart rate (tachycardia)
• Tremors and agitation
• Dizziness and confusion

Withdrawal Effects

Clinical studies assessing 62-day use of Susten (either daily or as needed) showed no evidence of withdrawal syndrome upon discontinuation.

Therapeutic Class

Susten belongs to the Drugs for Erectile Dysfunction category.

Storage Conditions

• Store at temperatures below 30°C.
• Keep away from moisture and direct sunlight.
• Keep out of reach of children.