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.