AChEinhibiittorit

AChEinhibiittorit are compounds that inhibit acetylcholinesterase (AChE), the enzyme that breaks down acetylcholine in cholinergic synapses and at the neuromuscular junction. By reducing hydrolysis of acetylcholine, these inhibitors increase its concentration and prolong signaling at cholinergic receptors.

AChEinhibiittorit can be classified as reversible or irreversible. Reversible inhibitors bind AChE temporarily and include drugs such as donepezil, rivastigmine, galantamine, physostigmine, neostigmine, and pyridostigmine. Irreversible inhibitors form a lasting bond with the enzyme; many are organophosphates (for example in certain pesticides and nerve agents) that phosphorylate the active site and may undergo aging, leading to prolonged inhibition.

Therapeutic uses vary by compound. Reversible peripheral AChE inhibitors are used to treat mild to moderate Alzheimer’s disease to modestly improve cognition and daily functioning, and to treat myasthenia gravis by increasing acetylcholine at the neuromuscular junction. Some inhibitors are used topically in glaucoma to reduce intraocular pressure. Neostigmine and pyridostigmine can reverse nondepolarizing neuromuscular blockade after anesthesia.

Toxicity from AChEinhibiittorit involves excessive cholinergic stimulation, producing muscarinic symptoms (salivation, lacrimation, urination, defecation, GI cramps, emesis; miosis; bradycardia) and nicotinic effects (muscle fasciculations, weakness). Management depends on the agent and exposure: atropine blocks muscarinic effects, while pralidoxime can reactivate AChE after organophosphate poisoning if given promptly.

In summary, AChEinhibiittorit modulate cholinergic signaling with diverse clinical applications and safety considerations, reflecting their central and peripheral pharmacology.