Embagra-100 Jelly/Forte Composition, Use, Dose, Side Effect

Embagra is a drug for treating erectile dysfunction. It comes as embagra-100 oral jelly and embagra forte. The embagra forte is claimed to be more potent than others because of its ingredients. Embagra-100 oral jelly contains a PDE5 inhibitor (Sildenafil) and embagra forte contain that and an antidepressant. It is believed that the antidepressant acts synergistically to improve Sildenafil.

Embagra-100 oral jelly and Embagra forte is from Laborate pharmaceuticals India LTD through Embassy pharmaceutical and chemicals LTD, Nigeria, embagra forte is set to change treatment for erectile dysfunction.

Embagra

Dosage Form And Strength Of Embagra-100

Oral Solid Dosage Form- jelly

Each sachet contains:

Sildenafil citrate Equ. to Sildenafil 100mg

Dosage Form And Strength Of Embagra Forte

Oral Solid Dosage Form: tablet

Each film coated tablet contains:

Sildenafil Citrate Equ. to Sildenafil 50 mg

Dapoxetine Hydrochloride Equ. to Dapoxetine 30 mg

Excipients q. s.

Approved color used.

History Of Active Ingredients

Sildenafil Citrate is a drug used to treat erectile dysfunction and pulmonary arterial hypertension (PAH).

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Dapoxetine is indicated for the treatment of premature ejaculation (PE) in adult men aged 18 to 64 years.

Clinical Pharmacology

Pharmacodynamics

Embagra is an oral therapy for erectile dysfunction. In sexual stimulation, it restores impaired erectile function by increasing blood flow to the penis. The physiological mechanism responsible for erection of the penis involves the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. Nitric oxide then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood.

Sildenafil: It is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) in the corpus cavernosum, where PDE5 is responsible for degradation of cGMP. Sildenafil has a peripheral site of action on erections. Sildenafil has no direct relaxant effect on isolated human corpus cavernosum but potently enhances the relaxant effect of NO on this tissue. When the NO/cGMP pathway is activated, as occurs with sexual stimulation, inhibition of PDE5 by sildenafil results in increased corpus cavernosum levels of cGMP. Therefore, sexual stimulation is required in order for sildenafil to produce its intended beneficial pharmacological effects.

Dapoxetine: The mechanism of action of dapoxetine in premature ejaculation is presumed to be linked to the inhibition of neuronal reuptake of serotonin and the subsequent potentiation of the neurotransmitter's action at pre- and postsynaptic receptors.

Pharmacokinetics

Absorption

Sildenafil is rapidly absorbed. Maximum observed plasma concentrations are reached within 30 to 120 minutes (median 60 minutes) of oral dosing in the fasted state.

Dapoxetine is rapidly absorbed with maximum plasma concentrations (Cmax) occurring approximately 1-2 hours after tablet intake.

Distribution

The mean steady state volume of distribution (Vd) for sildenafil is 105 L, indicating distribution into the tissues. After a single oral dose of 100 mg, the mean maximum total plasma concentration of sildenafil is approximately 440 ng/ml (CV 4).

More than 99% of dapoxetine is bound in vitro to human serum proteins. The active metabolite desmethyl dapoxetine (DED) is 98.5% protein bound. Dapoxetine has a mean steady state volume of distribution of 162 L.

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Metabolism

Sildenafil is cleared predominantly by the CYP3A4 (major route) and CYP2C9 (minor route) hepatic microsomal isoenzymes. The major circulating metabolite results from N-demethylation of sildenafil.

In vitro studies suggest that dapoxetine is cleared by multiple enzyme systems in the liver and kidneys, primarily CYP2D6, CYP3A4, and flavin monooxygenase (FMO1). Following oral dosing of 14C-dapoxetine, dapoxetine was extensively metabolized to multiple metabolites primarily through the following biotransformational pathways: N-oxidation, N-demethylation, naphthyl hydroxylation, glucuronidation and sulfation. There was evidence of presystemic first-pass metabolism after oral administration.

Elimination

The total body clearance of sildenafil is 41 l/h with a resultant terminal phase half-life of 3-5 h. After oral administration, sildenafil is excreted as metabolites predominantly in the feces (approximately 80% of administered oral dose) and to a lesser extent in the urine (approximately 13% of administered oral dose).

The metabolites of dapoxetine were primarily eliminated in the urine as conjugates. Unchanged active substance was not detected in the urine.

Indication And Usage Of Embagra 

Treatment of men with erectile dysfunction, which is the inability to achieve or maintain a penile erection sufficient for satisfactory sexual performance.

Contra-indication

Hypersensitivity to the active substance or to any of the excipients.

Interactions

In patients receiving an SSRI in combination with a monoamine oxidase inhibitor (MAOI), there have been reports of serious, sometimes fatal, reactions including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma. Therefore, Embagra forte is not used in combination with MAOI. The use of Embagra Forte in combination with CNS active medicinal products (e.g., antiepileptics, antidepressants, antipsychotics, anxiolytics, sedative hypnotics) has not been systematically evaluated in patients with premature ejaculation.

Consequently, caution is advised if the concomitant administration of embagra Forte and such medicinal products are required.

Warnings

Embagra should not be prescribed to men who have not been diagnosed with Premature Ejaculation. Safety has not been established and there are no data on the ejaculation-delaying effects in men without Premature Ejaculation.

Pregnancy And Lactation

Pregnancy

Not Indicated for use by women.

Lactation

Not Indicated for use by women.

Precautions

Embagra is not recommended for use in patients with severe renal impairment and caution is advised in patients with mild or moderate renal impairment. The use of Embagra Forte has been associated with ocular effects such as mydriasis and eye pain. It should be used with caution in patients with raised intraocular pressure or those at risk of angle closure glaucoma.

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Adverse Reaction

Flushing, dyspepsia, visual disorders, nasal congestion, and visual color distortion.

Drug Abuse And Dependence

Not Applicable.

Symptoms Of Overdose And Antidote

No cases of overdose has been reported. In cases of overdose, standard supportive measures should be adopted as required. Due to high protein binding and large volume of distribution of dapoxetine hydrochloride, forced diuresis, dialysis, hemoperfusion and exchange transfusion are unlikely to be of benefit. No specific antidotes for Embagra Forte are known.

Dosage And Administration Of Embagra 

Embagra is taken orally.

Use in adults

Treatment with Embagra should be taken as needed approximately 1 to 3 hours prior to sexual activity. It is not intended for continuous daily use.

It should be taken only when sexual activity is anticipated. It must not be taken more than once every 24 hours.

Use In Elderly

Efficacy and safety have not been established in patients aged 65 years and over.

Use In Children And Adolescents

There is no relevant use of embagra forte in this population in the indication of premature ejaculation.

Or as directed by the physician