Drugs for Erectile Dysfunction in Medicinal Chemistry- PPT
Drugs for erectile dysfunction: Sildenafil, Tadalafil. Oral contraceptives: Mifepristone,
Norgestril, Levonorgestrol Corticosteroids: Cortisone, Hydrocortisone,
Prednisolone, Betamethasone, Dexamethasone
drugs for erectile dysfunction in medicinal chemistry PPT
Drugs for Erectile Dysfunction
Slide 2: Introduction to Erectile Dysfunction Drugs
- Definition: Erectile dysfunction (ED) is the inability to achieve or maintain an erection sufficient for sexual performance.
- Drugs: Phosphodiesterase type 5 (PDE5) inhibitors are the most commonly prescribed medications.
- Mechanism of Action: PDE5 inhibitors enhance the effects of nitric oxide (NO), which increases blood flow to the penis, facilitating an erection.
Slide 3: Sildenafil (Viagra)
- Chemical Structure: Sildenafil is a selective PDE5 inhibitor.
- Mechanism of Action:
- Inhibits PDE5, leading to increased cyclic GMP (cGMP) levels, which relaxes smooth muscles in the corpus cavernosum, allowing for increased blood flow.
- Onset and Duration:
- Onset: 30-60 minutes.
- Duration: 4-5 hours.
- Clinical Applications:
- Treatment of erectile dysfunction.
- Also used in pulmonary arterial hypertension.
- Side Effects: Headache, flushing, visual disturbances, hypotension.
Slide 4: Tadalafil (Cialis)
- Chemical Structure: Tadalafil is another selective PDE5 inhibitor.
- Mechanism of Action: Similar to sildenafil, but with a longer half-life.
- Onset and Duration:
- Onset: 30 minutes.
- Duration: Up to 36 hours (often called “the weekend pill”).
- Clinical Applications:
- Treatment of erectile dysfunction.
- Benign prostatic hyperplasia (BPH).
- Side Effects: Muscle aches, headache, dyspepsia, nasal congestion.
Part 2: Oral Contraceptives
Slide 5: Introduction to Oral Contraceptives
- Definition: Oral contraceptives are medications used to prevent pregnancy by altering hormone levels, affecting ovulation, and modifying the uterine lining.
- Mechanism of Action: They typically contain a combination of estrogen and progestin or progestin alone, which prevent the release of eggs from the ovaries (ovulation), thicken cervical mucus, and thin the endometrial lining.
Slide 6: Mifepristone (RU-486)
- Chemical Structure: Mifepristone is a synthetic steroid that acts as an antiprogestin.
- Mechanism of Action:
- Blocks progesterone receptors, which prevents progesterone from maintaining pregnancy, causing the breakdown of the endometrial lining.
- Often used in combination with misoprostol (a prostaglandin) to induce abortion.
- Clinical Applications:
- Medical termination of early pregnancy.
- Emergency contraception (off-label use).
- Side Effects: Cramping, nausea, bleeding, headache.
Slide 7: Norgestrel and Levonorgestrel
- Chemical Structure: Synthetic progestins.
- Mechanism of Action:
- Suppress ovulation by inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
- Thicken cervical mucus, making it difficult for sperm to reach the egg.
- Norgestrel:
- Commonly used in combination oral contraceptives.
- Levonorgestrel:
- Also used as an emergency contraceptive (“morning-after pill”).
- Available as an intrauterine device (IUD) for long-term contraception.
- Side Effects: Nausea, irregular bleeding, mood changes.
Part 3: Corticosteroids
Slide 8: Introduction to Corticosteroids
- Definition: Corticosteroids are synthetic drugs that mimic cortisol, a hormone produced by the adrenal glands. They are widely used to reduce inflammation and suppress the immune response.
- Classification:
- Glucocorticoids: Primarily influence metabolism and immune function.
- Mineralocorticoids: Regulate sodium and water balance.
Slide 9: Cortisone and Hydrocortisone
- Cortisone:
- Structure: A steroid hormone and a prodrug of hydrocortisone.
- Mechanism of Action: Converted to hydrocortisone (active form) in the liver, which binds to glucocorticoid receptors, reducing inflammation.
- Clinical Applications: Used to treat arthritis, allergies, and skin conditions.
- Hydrocortisone:
- Structure: The active form of cortisone.
- Clinical Applications: Used topically for skin inflammation and orally for adrenal insufficiency.
- Side Effects: Weight gain, hypertension, hyperglycemia, osteoporosis with long-term use.
Slide 10: Prednisolone
- Chemical Structure: Prednisolone is a synthetic glucocorticoid derived from cortisol.
- Mechanism of Action:
- Acts by binding to glucocorticoid receptors, reducing inflammation and immune response.
- Clinical Applications:
- Treats autoimmune diseases, allergic reactions, and inflammation (e.g., asthma, rheumatoid arthritis).
- Side Effects: Insomnia, fluid retention, increased appetite, risk of infection with prolonged use.
Slide 11: Betamethasone and Dexamethasone
- Betamethasone:
- Chemical Structure: Potent synthetic glucocorticoid.
- Mechanism of Action: Reduces inflammation and suppresses immune responses.
- Clinical Applications: Used for inflammatory skin conditions, fetal lung development in premature labor.
- Side Effects: Similar to other corticosteroids but more potent effects.
- Dexamethasone:
- Chemical Structure: Highly potent synthetic glucocorticoid.
- Mechanism of Action: Strong anti-inflammatory and immunosuppressant.
- Clinical Applications: Treats severe allergies, cerebral edema, cancer-related conditions, and COVID-19-induced inflammation.
- Side Effects: Adrenal suppression, mood changes, weight gain, osteoporosis.
Slide 12: Conclusion
- Key Takeaways:
- Erectile dysfunction drugs: Sildenafil and Tadalafil improve blood flow by inhibiting PDE5.
- Oral contraceptives: Mifepristone, Norgestrel, and Levonorgestrel are essential for pregnancy prevention and termination.
- Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone, and Dexamethasone effectively reduce inflammation but come with significant side effects with long-term use.
Slide 13: References
- List of scientific journals, textbooks, and other resources for further reading.
drugs for erectile dysfunction in medicinal chemistry PPT
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