Medicinal Chemistry II (56) Drugs for Erectile Dysfunction = Introduction, Mechanism & SAR [R6WyPPTzH5h]

Medicinal Chemistry II (56) Drugs for Erectile Dysfunction = Introduction, Mechanism & SAR [R6WyPPTzH5h]

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Download the "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Tests and other GPAT Materials - Introduction to Drugs for Erectile Dysfunction: Erectile dysfunction (ED) is a condition characterized by the inability to achieve or maintain an erection sufficient for sexual intercourse. It can be caused by various factors, including physical, psychological, or a combination of both. Drugs for ED, also known as phosphodiesterase type 5 (PDE5) inhibitors, are a class of medications designed to improve blood flow to the penis, facilitating erections. Mechanism of Action: PDE5 inhibitors work by blocking the action of the enzyme phosphodiesterase type 5. This enzyme is responsible for breaking down cyclic guanosine monophosphate (cGMP), a chemical messenger that relaxes smooth muscle cells and increases blood flow to the penis during sexual stimulation. When PDE5 is inhibited, cGMP levels increase, leading to enhanced relaxation of smooth muscle cells in the erectile tissue and increased blood flow to the penis. This results in improved erectile function. Structure-Activity Relationship (SAR): The main drugs used for treating erectile dysfunction belong to the PDE5 inhibitor class. They include: Sildenafil (Viagra): Structure: Sildenafil's chemical structure consists of a pyrazolopyrimidinone core. SAR Highlights: The pyrazole ring is crucial for PDE5 inhibition. The substituents on the pyrazole ring affect the potency and selectivity of the drug. Modifications in the side chains can influence the drug's pharmacokinetics and duration of action. Tadalafil (Cialis): Structure: Tadalafil has a pyrazinopyridoindole core structure. SAR Highlights: The pyrazine and pyridine rings are essential for PDE5 inhibition. The substituents on the pyrazine ring can influence the drug's selectivity and potency. Tadalafil has a longer half-life compared to sildenafil, which allows for a longer duration of action. Vardenafil (Levitra): Structure: Vardenafil has a pyrazolopyrimidine core similar to sildenafil. SAR Highlights: The core structure is similar to sildenafil, but vardenafil has a different substituent pattern, affecting its pharmacological properties. Vardenafil exhibits enhanced selectivity for PDE5 compared to other PDE isoforms. Avanafil (Stendra): Structure: Avanafil has a unique pyrimidinone core. SAR Highlights: Avanafil's structure is distinct from the other PDE5 inhibitors, which contributes to its rapid onset of action and selectivity for PDE5. These drugs are generally well-tolerated, but they can interact with certain medications and have contraindications for individuals with specific medical conditions. It's crucial to consult a healthcare provider before starting any ED medication. Get in touch with the solution by just clicking the following links- Facebook Group- Mobile App - New Channel (Pharmacy Dictionary) E-Mail for official and other work - [email protected] #solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT