Available Dosage Strengths
2% / 3% / 1%
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This topical gel formulation contains sildenafil, arginine and menthol. The formulation may be used to enhance genital blood flow in people that are experiencing erectile dysfunction or female sexual arousal disorder. 1-7
Sildenafil1-5
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. Studies have shown it may also be beneficial for female sexual arousal disorder. Orally, because of the half-life, the drug is used “on-demand” prior to sexual activity.
Arginine6,7
L-Arginine, an essential amino acid, is converted to nitric oxide. It is naturally found in red meat, poultry, fish, and dairy. Nitric oxide is a powerful vasodilator and neurotransmitter. Arginine supports protein synthesis, immune function and wound healing.
Menthol8,9
Menthol has been used for medicinal purposes for thousands of years. It is a naturally occurring cyclic terpene alcohol of plant origin. In specific concentrations, topically, it has been used as an antipruritic, antiseptic, and analgesic.Studies indicate it may aid in penetration of drugs into the skin.
In addition, menthol, the active ingredient in topically applied analgesics, activates transient receptor potential melastatin 8 (TRPM8) receptors on sensory nerves and on the vasculature inducing a cooling sensation on the skin.
Sildenafil1-4
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. Studies have shown that sildenafil facilitates the relaxation of the clitoral corpus cavernosum through the nitric oxide-cGMP pathway. This may improve genital blood flow and vaginal engorgement.
Arginine6,7
L-Arginine is necessary for making proteins and is commonly used to promote circulation. The body converts arginine to nitric oxide (NO) through the action of nitric oxide synthase which relaxes blood vessels, allowing more blood to flow.
Menthol8,9
Antipruritic effects
Different opioid receptors have different effects on pruritus. Both mu-opioid receptor agonists and k-opioid receptor antagonists can induce itch, while mu-receptor antagonists and k-receptor agonists can reduce it. Menthol may affect pruritis by selectively activating k-opioid receptors.
Analagesic effects
Menthol may have analgesic properties through its activation of TRPM8 and/or inhibition of TRPA1.
Drug penetration into the skin
Menthol is also believed to increase penetration into the skin by the following mechanisms 1) disruption of the highly ordered lipid structure of the stratum corneum 2) by increasing drug partitioning into the stratum and 3) increasing electrical conductivity of tissues thereby opening polar pathways within the stratum.
Common (topically) 1-9
Oral (sildenafil)
Contraindications: 1-9
Precautions:
Store at 20–25°C (68–77°F). Protect from excessive heat, light, and moisture.
This information is for educational purposes only. This compounded product has not been reviewed, approved, or evaluated by the Food and Drug Administration for safety and effectiveness. This product is not intended to diagnose, treat, cure, or prevent any disease. No claims are made regarding treatment, cure, or prevention of any disease or condition.
This information may not cover all possible drug information about this product. Call your doctor for medical advice and/or about side effects. You may report side effects to the FDA at 1-800-FDA-1088. A Wells Pharmacy Network pharmacist will be happy to answer any questions. For consultation, please call 1-800-622-4510.
