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.
Zomepirac (Withdrawn) was discontinued due to severe anaphylactic and hypersensitivity reactions. It was an NSAID once used for pain relief in arthritis and acute conditions. Chemical Formula: C₁₁H₁₂N₂O₃ Mechanism of Zomepirac (Withdrawn): Non-selective COX inhibitor Uses of Zomepirac (Withdrawn): Formerly used for moderate to severe pain Side Effects: Fatal anaphylactic reactions GI toxicity Notes: Withdrawn … Read more
Sulindac inhibits COX enzymes, lowering prostaglandin synthesis to reduce pain and swelling. It is an NSAID effective in treating arthritis, pain, and inflammation. Chemical Formula: C₂₀H₁₇FO₃S Mechanism of Action: Prodrug → converted to active sulfide metabolite Inhibits COX-1 and COX-2 Uses of Sulindac: RA, OA, gout Familial adenomatous polyposis (FAP) (off-label) Side Effects of Sulindac: … Read more
Indomethacin is an NSAID used to relieve pain, inflammation, arthritis, and gout. It works by inhibiting COX enzymes, reducing prostaglandin synthesis and inflammation. Chemical Formula: C₁₉H₁₆ClNO₄ Mechanism of Action: Potent non-selective COX inhibitor Reduces inflammation, pain, fever Uses of Indomethacin: Gout (acute) RA, OA, ankylosing spondylitis Patent ductus arteriosus (PDA) closure in neonates Side Effects … Read more
Meclofenamate (Meclofenamic acid) is an NSAID effective in pain, inflammation, and arthritis relief. It inhibits COX enzymes, reducing prostaglandin synthesis and inflammation. Chemical Formula: C₁₄H₁₁Cl₂NO₂ Mechanism of Action: Reversible, non-selective COX-1/COX-2 inhibitor Inhibits prostaglandin synthesis Uses of Meclofenamate (Meclofenamic acid): Mild to moderate pain Dysmenorrhea Osteoarthritis, rheumatoid arthritis Side Effects of Meclofenamate (Meclofenamic acid): GI … Read more
Mefenamic Acid is an NSAID effective in treating pain, inflammation, and menstrual cramps. It inhibits COX enzymes, reducing prostaglandin synthesis for analgesic and anti-inflammatory action. Chemical Formula: C₁₅H₁₅NO₂ Mechanism: Reversible, non-selective COX inhibitor Reduces prostaglandin synthesis → pain relief, anti-inflammatory Uses: Dysmenorrhea Mild to moderate pain Musculoskeletal inflammation Side Effects: GI irritation Diarrhea CNS effects … Read more
Explore Aspirin (Acetylsalicylic acid) for pain relief, anti-inflammatory action, and cardiovascular protection. It works by inhibiting COX enzymes, reducing prostaglandin synthesis. Chemical Formula: C₉H₈O₄ Mechanism of Aspirin (Acetylsalicylic acid): Irreversible inhibitor of COX-1 & COX-2 Acetylates serine residue on COX enzymes Uses of Aspirin (Acetylsalicylic acid): Analgesic, antipyretic Anti-inflammatory (high dose) Anti-platelet (low dose) Side … Read more
Sodium Salicylate inhibits prostaglandin synthesis, reducing pain, fever, and inflammation. It is used as an analgesic, antipyretic, and anti-inflammatory agent. Chemical Formula: C₇H₅NaO₃ Mechanism of Action: Non-selective COX inhibitor Reduces PG synthesis → anti-inflammatory, antipyretic, analgesic Uses of Sodium Salicylate: Mild pain Fever Rheumatic fever, arthritis Side Effects of Sodium Salicylate: GI irritation Tinnitus (salicylism) … Read more
Naloxone Hydrochloride rapidly reverses opioid overdose by blocking opioid receptor activity. It is a pure opioid antagonist with fast onset and short duration of action. Chemical Formula: C₁₉H₂₁NO₄·HCl Mechanism of Action: Pure opioid antagonist Strong μ-receptor affinity (competitive) Also blocks κ and δ (lesser extent) Rapid onset; short half-life (~1–2 hrs) Therapeutic Uses: Emergency reversal … Read more
Levallorphan Tartrate blocks opioid receptors, counteracting morphine-like effects effectively. It is an opioid antagonist used to reverse opioid-induced respiratory depression. Chemical Formula: C₁₉H₂₅NO·C₄H₆O₆ Mechanism of Levallorphan Tartrate: μ-opioid receptor antagonist Partial κ-agonist Uses of Levallorphan Tartrate: Reversal of opioid-induced respiratory depression Anesthesia adjunct (historical use with pethidine) Side Effects: Dysphoria Confusion Tachycardia Hallucinations Notes: Similar … Read more
Nalorphine Hydrochloride treats opioid overdose by reversing respiratory depression. It acts as a mixed opioid agonist-antagonist at μ and κ receptors. Chemical Formula: C₁₉H₂₁NO₃·HCl Mechanism of Action: Mixed opioid agonist-antagonist μ-antagonist → blocks respiratory depression κ-agonist → mild analgesia and dysphoria Therapeutic Uses of Nalorphine Hydrochloride: Historically used to reverse opioid overdose Replaced by safer … Read more
