Medicinal Chemistry I is a core subject that explores the design, synthesis, and biological activity of drugs. It bridges organic chemistry and pharmacology to enhance understanding of therapeutic agents.
Phenylbutazone blocks COX enzymes, reducing prostaglandin synthesis to relieve pain and swelling. It is an NSAID used for arthritis, gout, and pain relief in inflammatory conditions. Chemical Formula: C₁₉H₂₀N₂O₂ Mechanism of Phenylbutazone: Potent non-selective COX inhibitor Strong anti-inflammatory effect Uses of Phenylbutazone: Ankylosing spondylitis (rare) Gout (historical) Side Effects: Aplastic anemia Agranulocytosis GI toxicity Notes: … Read more
Antipyrine is used as an analgesic and antipyretic, often in ear preparations for pain relief. It works by inhibiting prostaglandin synthesis, reducing pain, fever, and inflammation. Chemical Formula: C₁₁H₁₂N₂O Mechanism of Antipyrine: COX inhibition Also acts as antipyretic and analgesic Uses of Antipyrine: Historical use for fever, pain Component in ear drop formulations today Side … Read more
Piroxicam blocks COX enzymes, reducing prostaglandin synthesis to relieve pain and swelling. It is an NSAID for long-term management of arthritis, pain, and inflammation. Chemical Formula: C₁₅H₁₃N₃O₄S Mechanism of Piroxicam: Non-selective COX inhibitor Long half-life (~50 hrs) Uses of Piroxicam: Chronic inflammatory conditions (OA, RA) Once-daily dosing Side Effects: GI irritation/ulceration Photosensitivity Headache Notes: Long-acting … Read more
Phenacetin (Withdrawn) was withdrawn due to nephrotoxicity and carcinogenic risks linked to long use. It was once used as an analgesic and antipyretic for pain and fever relief. Chemical Formula: C₁₀H₁₃NO₂ Mechanism of Phenacetin (Withdrawn) : Central COX inhibition Mild analgesic and antipyretic Uses of Phenacetin (Withdrawn): Formerly used for fever and pain Side Effects: … Read more
Acetaminophen (Paracetamol) relieves pain and fever, widely used as an OTC analgesic-antipyretic. It inhibits central prostaglandin synthesis with minimal anti-inflammatory effect. Chemical Formula: C₈H₉NO₂ Mechanism of Acetaminophen (Paracetamol): Weak COX inhibition in CNS No peripheral anti-inflammatory effect Acts on serotonergic & endocannabinoid systems (minor) Uses of Acetaminophen (Paracetamol): Fever Mild to moderate pain Preferred in … Read more
Naproxen blocks COX enzymes, reducing prostaglandins to relieve pain, fever, and swelling. It is an NSAID used for arthritis, muscle pain, menstrual cramps, and inflammation. Chemical Formula: C₁₄H₁₄O₃ Mechanism of Naproxen: Reversible COX-1/COX-2 inhibitor Uses of Naproxen: Arthritis, ankylosing spondylitis Dysmenorrhea Fever, inflammation Side Effects: GI discomfort Cardiovascular risk (less than some NSAIDs) Fluid … Read more
Ibuprofen blocks COX enzymes, decreasing prostaglandin synthesis to ease pain and swelling. It is an NSAID used for pain, fever, arthritis, and inflammation relief. Chemical Formula: C₁₃H₁₈O₂ Mechanism of Action: Reversible COX-1 and COX-2 inhibitor Reduces prostaglandin synthesis → ↓ pain, fever, inflammation Uses: Mild to moderate pain Fever Dysmenorrhea Osteoarthritis, rheumatoid arthritis Side Effects … Read more
Ketorolac blocks COX enzymes, reducing prostaglandins to provide strong analgesic and anti-inflammatory effects. It is a potent NSAID for short-term management of moderate to severe pain. Chemical Formula: C₁₅H₁₃NO₃ Mechanism of Action: Potent non-selective COX inhibitor Primarily analgesic, weak anti-inflammatory Uses of Ketorolac: Moderate to severe acute pain (short-term, post-op) Alternative to opioids Side Effects … Read more
Diclofenac inhibits COX enzymes, reducing prostaglandin synthesis for strong anti-inflammatory action. It is widely used to treat pain, osteoarthritis, rheumatoid arthritis, and inflammation. Chemical Formula: C₁₄H₁₁Cl₂NO₂ Mechanism of Action: Potent COX-2 > COX-1 inhibitor Inhibits PG synthesis and may inhibit LOX and lipoxygenase enzymes (minor) Uses of Diclofenac: OA, RA, ankylosing spondylitis Post-op pain, dysmenorrhea … Read more
Tolmetin blocks COX enzymes, decreasing prostaglandins to relieve pain, fever, and inflammation. It is an NSAID used for osteoarthritis, rheumatoid arthritis, and juvenile arthritis. Chemical Formula: C₁₅H₁₅NO₃ Mechanism of Action: Inhibits COX enzymes Also inhibits leukocyte migration (minor) Uses of Tolmetin: OA, RA, juvenile arthritis Side Effects of Tolmetin: GI upset Headache Less frequent CNS … Read more
