CENFORCE-D is a very effective medicine for treatment of Erectile Dysfunction (ED) and Premature Ejaculation (PE).
Each coated tablet of Cenforce-D contains 100 mg of Sildenafil Citrate + 60 mg of Dapoxetine
Sildenafil citrate is the first clearly effective and FDA-approved oral therapy for the treatment of Erectile Dysfunction ED. Sildenafil is absorbed rapidly in the small intestine after oral administration, with times to peak plasma concentration from 30 to 120 minutes.4 Anything that delays gastric emptying will delay the time to peak plasma concentration. A high-fat meal will cause such a delay in gastric emptying and can delay the time to peak plasma concentration by 60 minutes and reduce the peak plasma concentration by 29%. Peak efficacy is seen after taking the medication on an empty stomach, where clinical efficacy has been observed within 19 minutes.
For more info on Sildenafil Citrate see our Bayagra page.
Dapoxetine is the first compound developed specially for the treatment of premature ejaculation (PE) in men 18–64 years old. Dapoxetine works by inhibiting the serotonin transporter, increasing serotonin’s action at the post synaptic cleft, and as a consequence promoting ejaculatory delay. As a member of selective serotonin reuptake inhibitor (SSRI) family, dapoxetine was initially created as an antidepressant. However, unlike other SSRIs, dapoxetine is absorbed and eliminated rapidly in the body. Its fast acting property makes it suitable for the treatment of Premature Ejaculationa (PE) but not as an antidepressant.
Randomized, double blind, placebo-controlled trials have confirmed the efficacy of dapoxetine for the treatment of PE. Dapoxetine, given 1–3 hours before sexual episode, prolongs IELT, increases the sense of control and sexual satisfaction in men of 18 to 64 years of age with PE. Since PE is associated with personal distress, interrelationship difficulty, dapoxetine provides help for men with PE to overcome this. Dapoxetine is a fast-acting SSRI. It is rapidly absorbed and eliminated from the body within a few hours. This favorable pharmacokinetics minimizes the risk of the drug’s accumulation in the body, and therefore reducing side effects.
Contraindications
Dapoxetine should not be used in men with moderate to severe hepatic impairment and in those receiving CYP3A4 inhibitors such as ketoconazole, ritonavir, and telithromycine. Dapoxetine can also not be used in patients with heart failure, permanent pacemaker, or other significant ischemic heart disease. Caution is advised in men receiving thioridazine, monoamine oxidase inhibitors, SSRIs, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressant. If a patient stops taking one of these drugs, he should wait for 14 days before taking dapoxetine. If a patient stops taking dapoxetine, he should wait for 7 days before receiving these drugs.
Adverse effects
The most common effects when taking dapoxetine are nausea, dizziness, dry mouth, headache, diarrhea, and insomnia. Unlike others SSRIs used to treat depression, which have been associated with high incidences of sexual dysfunction, dapoxetine is associated with low rates of sexual dysfunction. Taken as needed, dapoxetine has very mild adverse effects on loss of libido (<1%) and ED (<4%).
Ethanol doesn’t affect the pharmacokinetics of dapoxetine when taking concurrently with dapoxetine.
Mechanism of actions
The mechanism through which dapoxetine affects premature ejaculation is still unclear. However, it is presumed that dapoxetine works by inhibiting serotonin transporter and subsequently increasing serotonin’s action at pre and postsynaptic receptors[18] Human ejaculation is regulated by various areas in the central nervous system (CNS).[19] The ejaculatory pathway originates from spinal reflex at the thoracolumbar and lumbosacral level of spinal cord activated by stimuli from male genital. These signals are relayed to the brain stem, which then is influenced by a number of nuclei in the brain such as medial preoptic and paraventricular nulcei.[20] Clement's study performed on anaesthetized male rats showed that acute administration of dapoxetine inhibits ejaculatory expulsion reflex at supraspinal level by modulating activity of lateral paragigantocellular nucleus (LPGi) neurons. These effects cause an increase in pudendal motoneuron reflex discharge (PMRD) latency. However, it is unclear whether dapoxetine acts directly on LPGi or on the descending pathway in which LPGi located.
Metabolism
Dapoxetine is metabolized extensively in the liver and kidney by multiple enzymes such as CyP2D6, CyP3A4, and flavin monooxygenase 1 (FMO1).
The metabolites of dapoxetine are eliminated rapidly in the urine with a terminal half-life of 18.7 and 21.9 hours for a single dose of 30 mg and 60 mg respectively.
Safety and tolerability - Cardiovascular safety
The cardiovascular safety profile of dapoxetine has been studied extensively during the drug development. Phase I trials showed that dapoxetine had neither clinical significant electrocardiographic effects nor delayed repolarization effects, with dosing up to 4-fold greater than the maximum recommended dosage which is 60 mg. Phase III studies in men with PE showed a safety and well tolerate profile of dapoxetine with dosing of 30 and 60 mg. There is no cardiovascular adverse had been found. it is rapidly absorbed in the body. Dapoxetine's maximum plasma concentration (Cm) is reached 1–2 hours after oral administration. Dapoxetine can be taken with or without food.
Interactions of Dapoxetine With phosphodiesterase inhibitors (PDE5 inhibitors)
Many men that have PE also suffer from erectile dysfunction (ED). Treatment for these patients should consider the drug-drug interaction between dapoxetine and PDE5 inhibitors such as tadalafil (Cialis) or sildenafil (Viagra). In Dresser study (2006), plasma concentration of 24 subjects was obtained. Half of the sample pool were treated with dapoxetine 60 mg + tadalafil 20 mg; the other half were treated with dapoxetine 60 mg + sildenafil 100 mg. These plasma samples were then analyzed using liquid chromatography-tandem mass spectrometry. The results showed that dapoxetine does not alter the pharmacokinetic of tadalafil or sildenafil.
Storage
Keep out of reach of children. Store in a dark place at room temperature between 15 and 30 degrees C (59 and 86 degrees F)
Usage
For first time users it is recommended to start with half of the tablet dosage (the pills can be cut in half with a sharp knife).
This medicine should be taken 1–2 hours before sexual activity. Do NOT exceed a single dosage in 24 hour period.
PRECAUTIONS:
Kindly consult your physician before taking this or any medicine .
