For the use only of a Registered medical practitioner, Hospital or Laboratory
Dapoxetine and Sildenafil Tablets
Each film coated tablet contains:
Dapoxetine Hydrochloride IP equivalent to Dapoxetine 60 mg
Sildenafil Citrate IP equivalent to Sildenafil 100 mg
Colours: Titanium Dioxide BP, Brilliant Blue
Sildenafil: 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1Hpyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate
Dapoxetine: (+)-(S)-N,N-dimethyl-(‹)-[2-(1-naphthalenyloxy)ethyl]-benzenemethanamine hydrochloride
Sildenafil: Selective phosphodiesterase type-5 (PDE5) inhibitor
Dapoxetine: Selective serotonin reuptake inhibitor (SSRI)
DESCRIPTION: SILJOY-MAX contains Sildenafil citrate 100 mg and Dapoxetine hydrochloride 60 mg.
Sildenafil: Part of the physiological process of erection involves the parasympathetic nervous system causing the release of nitric oxide (NO) in the corpus cavernosum of the penis. NO binds to the receptors of the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation (vasodilation) in the corpus cavernosum, resulting in increased inflow of blood and an erection. Sildenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and better erections.
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 post-synaptic receptors. Human ejaculation is primarily mediated by the sympathetic nervous system. The ejaculatory pathway originates from a spinal reflex centre, mediated by the brain stem, which is influenced initially by a number of nuclei in the brain (medial preoptic and paraventricular nuclei).
Sildenafil: Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25–63%). Pharmacokinetics is dose-proportional over the recommended dose range. It is eliminated predominantly by hepatic metabolism (mainly cytochrome P450 3A4) and is converted to an active metabolite with properties similar to the parent, sildenafil. The concomitant use of potent cytochrome P450 3A4 inhibitors (e.g., erythromycin, ketoconazole, itraconazole) as well as the nonspecific CYP inhibitor, cimetidine, is associated with increased plasma levels of sildenafil. Both sildenafil and the metabolite have terminal half-life of about 4 hours.
It is rapidly absorbed. Sildenafil and its major circulating N-desmethyl metabolite are both approximately 96% bound to plasma proteins. Protein binding is independent of total drug concentrations. 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 the administered oral dose).
Dapoxetine: Dapoxetine is rapidly absorbed with maximum plasma concentrations (Cmax) occurring approximately 1-2 hours after tablet intake. The absolute bioavailability is 42% (range 15- 76%). Ingestion of a high fat meal modestly reduced the Cmax (by 10%) and modestly increased the AUC (by 12%) of dapoxetine and slightly delayed the time for dapoxetine to reach peak concentrations; however, the extent of absorption was not affected by consumption of a high fat meal.
Greater than 99% of dapoxetine is bound in vitro to human proteins. The active metabolite desmethyldapoxetine is 98.5% protein bound.
Dapoxetine was extensively metabolized to multiple metabolites primarily through the following biotransformational pathways: N-oxidation, N-demethylation, naphthyl hydroxylation, glucuronidation and sulfation.
The terminal half-life is approximately 19 hours following oral administration.
SILJOY-MAX is used to achieve and maintain erections and delay premature ejaculation in men.
DOSAGE AND ADMINISTRATION
Take 1 tablet of SILJOY-MAX before 1-3 hours of sexual activity. The maximum recommended dosing frequency is once per day.
SILJOY-MAX is contraindicated in patients with known hypersensitivity, moderate and severe hepatic impairment, significant pathological cardiac conditions (such as heart failure (NYHA class II-IV), conduction abnormalities (second- or third-degree AV block or sick sinus syndrome), ischemic heart disease or valvular disease.
WARNINGS AND PRECAUTIONS
- SILJOY-MAX is prescribed for adult males only (18 years and older).
- SILJOY-MAX must not be used by anyone taking nitrate medication (even occasionally).
- Sildenafil citrate should not be taken if you are currently taking alpha blockers and should not be combined with other erectile dysfunction medications.
- Use of SILJOY-MAX is not recommended for people with a history of cardiac dysfunction.
- Avoid driving or operating machinery when taking this medication.
- Consult a medical professional immediately if you experience erections lasting longer than 4 hours or painful erections as prolonged erections can lead to permanent tissue damage.
SILJOY-MAX is contraindicated for concomitant treatment with azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, verapamil and doxazosin.
Common side effects are increased thirst and a light headedness following sudden movements.
The less frequently occurring side effects experienced by patients may include one or more of the following: nausea, dizziness and headaches, flushing, dyspepsia, nasal congestion, temporary visual abnormalities (including changes in color perception, increased sensitivity to light and blurred vision), urinary tract infections or temporary heat rashes.
PRESENTATION : Blister of 4 Tablets
STORAGE: Store in a cool and dry place below 30°C.
Protect from light and moisture.
Keep out of reach of children.
LAST UPDATE: October 2014.