Ultimale

Uses

Indicated for the treatment of premature ejaculation (PE) in men 18 to 64 years of age, who have all 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 consequence of PE and poor control over ejaculation.

Ultimale is also used to associated treatment for these conditions: Premature Ejaculation

How Ultimale works

The drug's mechanism of action is thought to be related to inhibition of neuronal reuptake of serotonin and subsequent potentiation of serotonin activity. The central ejaculatory neural circuit comprises spinal and cerebral areas that form a highly interconnected network. The sympathetic, parasympathetic, and somatic spinal centers, under the influence of sensory genital and cerebral stimuli integrated and processed at the spinal cord level, act in synergy to command physiologic events occurring during ejaculation. Experimental evidence indicates that serotonin (5-HT), throughout brain descending pathways, exerts an inhibitory role on ejaculation. To date, three 5-HT receptor subtypes (5-HT(1A), 5-HT(1B), and 5-HT(2C)) have been postulated to mediate 5-HT's modulating activity on ejaculation.

Dosage

Ultimale dosage

Adult (18 to 64 years of age): The recommended starting dose for all patients is 30 mg, taken as needed approximately 1 to 3 hours prior to sexual activity. If the effect of 30 mg is insufficient and the side effects are acceptable, the dose may be increased to the maximum recommended dose of 60 mg. The maximum recommended dosing frequency is one dose every 24 hours.

Side Effects

Dizziness, Headache, Somnolence, Tremor, Blurred vision, Tinnitus, Sinus congestion, Nausea, Diarrhea, Abdominal pain, Dry mouth, Fatigue, Insomnia, Hypertension.

Precaution

Patient with bleeding disorders, epilepsy, susceptibility to angle-closure glaucoma or raised intraocular pressure. Not intended for use in women. Known CYP2D6 poor metabolisers.

Interaction

CNS active medicinal products: The use of Ultimale in combination with CNS active medicinal products has not been systematically evaluated in patients with premature ejaculation. Consequently, caution is advised if the concomitant administration of Ultimale and such medicinal products is required.

PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Ultimale. Sildenafil caused slight changes in Ultimale pharmacokinetics, which are not expected to be clinically significant. However, Ultimale should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.

Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Ultimale to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Ultimale should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.

Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Ultimale; therefore, caution is advised when Ultimale is used in patients taking Warfarin chronically.

Ethanol: Concomitant use of alcohol and Ultimale could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Ultimale may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Ultimale.

Elimination Route

Rapidly absorbed.

Half Life

Initial half-life of 1-2 hours.

Pregnancy & Breastfeeding use

Ultimale is not indicated for use by women. It is not known either dapoxetine or its metabolites are excreted through human breast milk.

Contraindication

• Patients with known hypersensitivity to Ultimale Hydrochloride.
• Patients with significant pathological cardiac conditions such as heart failure (NYHA class II-IV), conduction abnormalities (second or third degree AV block or sick sinus syndrome) not treated with a permanent pacemaker, significant ischemic heart disease of significant valvular disease.
• Concomitant treatment with monoamine oxidase inhibitors (MAOIs), thioridazine. Similarly, MAOIs or thioridazine should not be administered within 7 days after Ultimale has been discontinued.
• Concomitant treatment with serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs) or other medicinal/herbal products with serotonergic effects or within 14 days of discontinuing treatment with these medicinal/herbal products.

Acute Overdose

There were no unexpected adverse events in a clinical pharmacology study of Ultimale with daily doses up to 240 mg. In general, symptoms of overdose with SSRIs include serotonin-mediated adverse reactions such as somnolence, gastrointestinal disturbances such as nausea and vomiting, tachycardia, tremor, agitation and dizziness. In cases of overdose, standard supportive measures should be adopted as required.

Storage Condition

Store below 30°C. Protect from light and moisture. Keep out of reach of children

Innovators Monograph

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