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PDE5 inhibitor information


Chemical structure of sildenafil (Viagra), the prototypical PDE5 inhibitor

A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying various tissues. These drugs dilate the corpora cavernosa of the penis, facilitating erection with sexual stimulation, and are used in the treatment of erectile dysfunction (ED). Sildenafil was the first effective oral treatment available for ED. Because PDE5 is also present in the smooth muscle of the walls of the arterioles within the lungs, two PDE5 inhibitors, sildenafil and tadalafil, are FDA-approved for the treatment of pulmonary hypertension. As of 2019, the wider cardiovascular benefits of PDE5 inhibitors are being appreciated.[1]

  1. ^ Tzoumas N, Farrah TE, Dhaun N, Webb DJ (November 2019). "Established and emerging therapeutic uses of phosphodiesterase type 5 inhibitors in cardiovascular disease". British Journal of Pharmacology. 177 (24): 5467–5488. doi:10.1111/bph.14920. PMC 7707100. PMID 31721165.

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PDE5 inhibitor

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5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on...

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Tadalafil

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this may result in a serious drop in blood pressure. Tadalafil is a PDE5 inhibitor which increases blood flow to the penis. It also dilates blood vessels...

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Sildenafil

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relaxation. Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP...

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Discovery and development of phosphodiesterase 5 inhibitors

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inhibitor potency and differences between isotypes of PDE in the Q2 pocket can be exploited for selectivity between isotypes. Drugs that inhibit PDE5...

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Vardenafil

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dysfunction. It is a PDE5 inhibitor. It is taken by mouth. Vardenafil's indications and contraindications are the same as with other PDE5 inhibitors; it is closely...

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Dapoxetine

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serotonin reuptake inhibitor (SSRI) used for the treatment of premature ejaculation (PE) in men 18–64 years old. Dapoxetine works by inhibiting the serotonin...

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Erectile dysfunction

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many instances, medication-based therapies are used, specifically PDE5 inhibitors like sildenafil. These drugs function by dilating blood vessels, facilitating...

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Selective serotonin reuptake inhibitor

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Management strategies include: for erectile dysfunction the addition of a PDE5 inhibitor such as sildenafil; for decreased libido, possibly adding or switching...

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Anaphrodisiac

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to drastically increase sexual pleasure. MDMA in combination with a PDE5 inhibitor (trade names Viagra, Levitra, and Cialis) is termed "sextasy". This...

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Epimedium

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supplement is Epimedium grandiflorum. It contains icariin, which is a weak PDE5 inhibitor, in vitro. Its clinical effects are unknown. While there is little clinical...

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Avanafil

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Avanafil is a PDE5 inhibitor approved for erectile dysfunction by the FDA on April 27, 2012 and by EMA on June 21, 2013. Avanafil is sold under the brand...

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List of sulfonamides

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Udenafil (PDE5 inhibitor) Brinzolamide (carbonic anhydrase inhibitor for glaucoma) Dorzolamide (anti-glaucoma carbonic anhydrase inhibitor) Probenecid...

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Pomiferin

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efficacy as an antioxidant, cardioprotectant, antimicrobial, antidiabetic, PDE5 inhibitor and cytotoxicity for several cancer cell lines. Peterson and Fristad...

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Yohimbine

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clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs. Substances that have purported to be extracts from the...

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Udenafil

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It is within the PDE5 inhibitor class (which also includes avanafil, sildenafil, tadalafil, and vardenafil). Like other PDE5 inhibitors, it is used to treat...

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Anorgasmia

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is the use of vardenafil. Vardenafil is a type 5 phosphodiesterase (PDE5) inhibitor that facilitates muscle relaxation and improves penile erection in...

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Cyclic guanosine monophosphate

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(October 2003). "The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1...

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Phosphodiesterase

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pass in a variety of fields (e.g. sildenafil as a PDE5 inhibitor and Rolipram as a PDE4 inhibitor). The PDE nomenclature signifies the PDE family with...

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Pulmonary hypertension

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another PDE5 inhibitor, marketed under the name Adcirca. PDE5 inhibitors are believed to increase pulmonary artery vasodilation, and inhibit vascular...

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CYP3A4

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clearance. a Moderate inhibitor causes at least a 2-fold increase in the plasma AUC values, or 50–80% decrease in clearance. a Weak inhibitor causes at least...

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List of designer drugs

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Phenylpiracetam Piracetam Pramiracetam Tobacco Vitamin B1 Vitamin B6 Vitamin B9 PDE5 inhibitors are typically used to treat pulmonary hypertension and erectile dysfunction...

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Isosorbide mononitrate

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effects may include low blood pressure especially if also exposed to PDE5 inhibitors such as sildenafil. Use is not recommended in pregnancy. It is believed...

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Phosphodiesterase inhibitor

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cGMP-specific phosphodiesterase inhibitor which inhibits PDE9, a cGMP preferring phosphodiesterase. PDE9 is expressed as high as PDE5 in the corpus cavernosum...

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Icos

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pulmonary arterial hypertension (PAH). It is a phosphodiesterase type 5 (PDE5) inhibitor, similar in function to sildenafil. In addition to ED and PAH, tadalafil...

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Homosildenafil

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using a pde5 inhibitor", published 1 November 2001, assigned to Lilly ICOS LLC.  US 20090074796, Borrello IM, Serafini P, Noonan KA, Bronte V, "Pde5 inhibitor...

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