Medicinal Chemistry I

Scopolamine Hydrobromide: Action – Blocks muscarinic receptors, reducing secretions, spasms, and vestibular stimulation. Scopolamine Hydrobromide: Uses – Anticholinergic drug for motion sickness, nausea, and pre-anesthetic medication. Formula: C₁₇H₂₁NO₄·HBr·3H₂O Mechanism of Scopolamine Hydrobromide: Muscarinic antagonist, stronger CNS penetration than atropine Uses of Scopolamine Hydrobromide: Motion sickness (transdermal) Postoperative nausea Sedation in palliative care Side Effects: Drowsiness … Read more

Hyoscyamine Sulfate: An anticholinergic drug used to treat GI disorders, spasms, and motion sickness effectively. Hyoscyamine Sulfate: Relieves cramps, reduces secretions, and improves smooth muscle control in therapeutic conditions. Formula: (C₁₇H₂₃NO₃)₂·H₂SO₄ Mechanism of Hyoscyamine Sulfate: Same as atropine but more potent due to stereoselectivity Uses of Hyoscyamine Sulfate: GI spasms Irritable bowel syndrome Urinary incontinence … Read more

Atropine Sulfate treats bradycardia, reduces secretions, and acts as an antidote in organophosphate poisoning. Atropine Sulfate blocks muscarinic receptors, producing anticholinergic effects for smooth muscle relaxation and eye dilation. Formula: (C₁₇H₂₃NO₃)₂·H₂SO₄ Mechanism of Atropine Sulfate: Competitive muscarinic receptor antagonist Affects M1–M5; especially heart (M2) and secretory tissues (M3) Uses: Bradycardia Pre-anesthetic (reduce secretions) Organophosphate poisoning … Read more

Definition of Cholinergic Blocking Agents (Cholinolytics / Anticholinergics) Cholinergic Blocking Agents (Cholinolytics / Anticholinergics) are compounds that inhibit the actions of acetylcholine (ACh) at muscarinic receptors (primarily), and in some cases, nicotinic receptors. They are also known as antimuscarinic agents or muscarinic antagonists. They block parasympathetic nerve impulses, leading to sympathomimetic effects, such as decreased … Read more

Pralidoxime Chloride (2-PAM): Antidote for organophosphate poisoning, reactivates acetylcholinesterase. Pralidoxime Chloride (2-PAM): Restores normal neuromuscular function, used in emergency toxicology. Chemical Formula: C₇H₉ClN₂O Mechanism of Action: Reactivates phosphorylated AChE by removing the phosphate group (only effective before “aging” of the bond). Must be given early in organophosphate poisoning. Uses of Pralidoxime Chloride (2-PAM): Antidote for … Read more

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