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.
Malathion is an organophosphate insecticide widely used to control pests in agriculture and public health. Malathion treats head lice, mosquito control, and protects crops, ensuring safety with proper dosage and handling. Chemical Formula: C₁₀H₁₉O₆PS₂ Mechanism of Action: Irreversible AChE inhibitor after conversion to malaoxon Uses of Malathion: Head lice treatment Scabies Agricultural pesticide Side Effects … Read more
Parathion is a highly toxic organophosphate pesticide used for pest control in crops. Parathion exposure can cause severe poisoning, affecting the nervous system. Chemical Formula: C₁₀H₁₄NO₅PS Mechanism of Action: Irreversible AChE inhibitor after bioactivation to paraoxon Uses: Agricultural insecticide (not for therapeutic use) Side Effects (Toxicity): SLUDGE syndrome: Salivation, Lacrimation, Urination, Diarrhea, GI upset, Emesis … Read more
Echothiophate Iodide Uses – Long-acting cholinesterase inhibitor for glaucoma, reducing intraocular pressure effectively. Echothiophate Iodide Action – Irreversibly inhibits cholinesterase, enhancing acetylcholine activity and improving ocular fluid outflow. Chemical Formula: C₉H₂₃I₂NO₄PS Mechanism of Action: Irreversible AChE inhibitor Long-acting due to covalent binding Uses: Chronic glaucoma Accommodative esotropia Side Effects: Miosis Brow ache Risk of cataracts … Read more
Isofluorphate (DFP – Diisopropyl fluorophosphate) Agents: Potent irreversible cholinesterase inhibitors used in glaucoma. Isofluorphate (DFP – Diisopropyl fluorophosphate) Agents: Organophosphate derivative with strong parasympathomimetic action. Chemical Formula: C₃H₈FO₄PS Mechanism of Action: Irreversible AChE inhibitor. Covalently binds AChE → long-lasting cholinergic effects. Uses: Previously used for glaucoma (rare today). Side Effects: Cholinergic crisis (if overdosed) Muscle … Read more
Ambenonium Chloride is a synthetic quaternary ammonium compound classified as a cholinesterase inhibitor. It functions by reversibly inhibiting the enzyme acetylcholinesterase, thereby increasing the concentration of acetylcholine at neuromuscular junctions. Chemical Formula: C₂₀H₂₈Cl₂N₄O₂ Mechanism of Action: Reversible AChE inhibitor Does not cross BBB Uses of Ambenonium Chloride: Myasthenia gravis (alternative to neostigmine/pyridostigmine) Side Effects of … Read more
Tacrine Hydrochloride is the hydrochloride salt form of Tacrine, a centrally acting cholinesterase inhibitor. It is primarily used in the management of mild to moderate Alzheimer’s disease to enhance cholinergic transmission in the brain by inhibiting the enzyme acetylcholinesterase. Chemical Formula: C₁₃H₁₄ClN Mechanism of Action: Reversible AChE inhibitor; crosses BBB. Also has NMDA antagonist Uses … Read more
Edrophonium Chloride is a short-acting, quaternary ammonium compound classified as a reversible acetylcholinesterase inhibitor. It temporarily increases acetylcholine levels at neuromuscular junctions by inhibiting the enzyme acetylcholinesterase. Chemical Formula: C₁₀H₁₆ClNO Mechanism of Action: Short-acting reversible AChE inhibitor. Binds via electrostatic + hydrogen bonding, not covalent. Uses of Edrophonium Chloride: Diagnosis of myasthenia gravis (Tensilon test) … Read more
Pyridostigmine is a quaternary ammonium compound, and a reversible acetylcholinesterase inhibitor used to enhance cholinergic transmission by preventing the breakdown of acetylcholine at neuromuscular junctions. It is primarily indicated for the symptomatic treatment of myasthenia gravis, reversal of non-depolarizing neuromuscular blockade, and as a prophylactic agent against nerve gas poisoning. Chemical Formula: C₉H₁₃N₂O₂ Mechanism of … Read more
Neostigmine is a synthetic quaternary ammonium compound that acts as a reversible cholinesterase inhibitor. It inhibits the enzyme acetylcholinesterase, thereby increasing the concentration of acetylcholine at neuromuscular junctions and cholinergic synapses. Chemical Formula: C₁₂H₁₉N₂O₂⁺ Mechanism of Action: Reversible AChE inhibitor. Also has some direct nicotinic agonist activity at NMJ. Uses of Neostigmine: Myasthenia gravis Reversal … Read more
Physostigmine is a naturally occurring reversible cholinesterase inhibitor derived from the seeds of Physostigma venenosum (Calabar bean). It inhibits acetylcholinesterase, leading to increased levels of acetylcholine at synaptic and neuromuscular junctions. Chemical Formula: C₁₅H₂₁N₃O₂ Mechanism of Action: Reversible AChE inhibitor. Crosses blood-brain barrier (BBB) → CNS effects. Uses of Physostigmine: Antidote for anticholinergic toxicity (e.g. … Read more
