(Sildenafil / Vardenafil / Tadalafil / Apomorphine)
15 mg / 15 mg / 15 mg / 2 mg
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Product Overview
Sildenafil / Vardenafil / Tadalafil / Apomorphine Description
This product is a sublingual formulation may be used to enhance genital blood flow and sexual desire in people that are experiencing sexual dysfunction.
Sildenafil1-3
Sildenafil, a phosphodiesterase type 5 (PDE5) inhibitor, has a half-life of 4 hours. Clinically, the drug is used to treat erectile dysfunction and pulmonary hypertension. It also has shown to be beneficial for female sexual arousal disorder. Orally, because of the half-life, the drug is used “on-demand” prior to sexual activity.
Tadalafil4-6
Tadalafil, a phosphodiesterase type 5 (PDE5) inhibitor, has a mean terminal half-life of over 17 hours. This half-life is much longer than other PDE-5 inhibitors. This half-life allows for once-daily or on-demand dosing. The drug is indicated for the treatment of pulmonary arterial hypertension (PAH), erectile dysfunction (ED), benign prostatic hypertrophy (BPH), or the concurrent treatment of ED and BPH.
Vardenafil7-9
Vardenafil, a phosphodiesterase type 5 (PDE5) inhibitor, has a mean terminal half-life of 4 to 6 hours. It is effective and generally well tolerated. Vardenafil is a potent and highly selective oral PDE5 inhibitor. The drug is indicated for erectile dysfunction and it is used for on-demand use for this indication.
Apomorphine10-13
Apomorphine is a dopamine receptor agonist that works in the brain (centrally) for erectile dysfunction. The drug improves the penis’s erectile response to stimuli. It has also been studied to enhance sexual motivation, desire and arousal especially for women. The onset of action is within 30 minutes. The drug is given sublingually to bypass absorption in the gastrointestinal tract and to prevent first pass metabolism in the liver. This will improve blood levels. The duration of activity of apomorphine is 60- 90 minutes with a half-life of approximately 100 minutes.
References
Sildenafil1-3
Phosphodiesterase (PDE) has many isoforms and is an enzyme that has many functions in the body including degrading the effect of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). PDE5 is an enzyme that is found in many parts of the body including in the smooth muscle of the corpus cavernosum, prostate, bladder, the vascular and visceral smooth muscle, skeletal muscle, urethra, platelets, kidney, lung, cerebellum, heart, liver, testis, seminal vesicle, and pancreas. Sildenafil is structurally similar to cGMP and prevents degradation of cGMP by competitively binding and inhibiting activity of PDE5. When PDE5 is inhibited, cGMP accumulates and leads to smooth muscle relaxation.
Tadalafil4-6
Phosphodiesterase (PDE) has many isoforms and is an enzyme that has many functions in the body including degrading the effect of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). PDE5 is an enzyme that is found in many parts of the body including in the smooth muscle of the corpus cavernosum, prostate, bladder, the vascular and visceral smooth muscle, skeletal muscle, urethra, platelets, kidney, lung, cerebellum, heart, liver, testis, seminal vesicle, and pancreas. Tadalafil is a selective inhibitor of PDE5, the enzyme responsible for the degradation of cGMP. The drug has selective activity on PDE5 than other phosphodiesterase isoforms. Tadalafil activity on PDE5 is more than 10,000-fold more than for PDE1, PDE2, PDE4, and PDE7 enzymes. Increased cGMP leads to smooth muscle relaxation in the corpus cavernosum which can help in maintaining an erection.
Vardenafil7-9
Phosphodiesterase (PDE) has many isoforms and is an enzyme that has many functions in the body including degrading the effect of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). PDE5 is an enzyme that is found in many parts of the body including in the smooth muscle of the corpus cavernosum, prostate, bladder, the vascular and visceral smooth muscle, skeletal muscle, urethra, platelets, kidney, lung, cerebellum, heart, liver, testis, seminal vesicle, and pancreas. Vardenafil is a selective inhibitor of PDE5, the enzyme responsible for the degradation of cGMP. Vardenafil’s activity on PDE5 has been shown to be approximately 10 fold to 25 fold more than sildenafil. Increased cGMP leads to smooth muscle relaxation in the corpus cavernosum which can help in maintaining an erection.
Apomorphine10-12
Apomorphine is a dopamine receptor agonist that has activity on dopamine-1 and dopamine-2 receptors in the hypothalamus. The hypothalamus (specifically the paraventricular nucleus (PVN)) has abundant dopamine receptors. The dopamine stimulation in the PVN may have several effects including increasing nitric oxide synthase to stimulate nitric oxide. Nitric oxide stimulates oxytocin which moves through the spinal cord to stimulate a genital blood flow. Increases in dopamine, one of the primary neurotransmitters involved in sexual function, may stimulate sexual desire, motivation and arousal.
Common1-8,13
Sildenafil
Tadalafil
Vardenafil
Apomorphine
Contraindications1-8,13
Precautions1-8,13
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