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A parasympathomimetic drug, sometimes called a cholinomimetic drug [1] or cholinergic receptor stimulating agent, [2] is a substance that stimulates the parasympathetic nervous system (PSNS). [ 3 ] [ 2 ] These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS.
A substance (or ligand) is cholinergic if it is capable of producing, altering, or releasing acetylcholine, or butyrylcholine ("indirect-acting"), or mimicking their behaviours at one or more of the body's acetylcholine receptor ("direct-acting") or butyrylcholine receptor types ("direct-acting").
Tacrine is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist (parasympathomimetic).It was the first centrally acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex.
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
Acetylcholine Acetylcholinesterase Acetylcholinesterase inhibition. Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, [1] inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate, [2] thereby increasing both the level and duration of action of acetylcholine in the central nervous system, autonomic ...
Physostigmine, an acetylcholinesterase inhibitor, can be used to treat glaucoma and delayed gastric emptying.Because it enhances the transmission of acetylcholine signals in the brain and can cross the blood–brain barrier, physostigmine salicylate is used to treat anticholinergic poisoning (that is, poisoning by substances that interfere with the transmission of acetylcholine signaling, such ...
Paraoxon and rivastigmine are both acetylcholinesterase inhibitors and butyrylcholinesterase inhibitors. [14] [11] [7]In 2015, the United States Food and Drug Administration's Adverse Event Reporting System database compared rivastigmine to the other ChEI drugs donepezil and galantamine found that rivastigmine was associated with a higher frequency of reports of death as an adverse event.
It is therefore classified as an indirect acetylcholine antagonist. [1] Acetylcholine is synthesized from choline and a donated acetyl group from acetyl-CoA, by the action of choline acetyltransferase (ChAT). Thus, decreasing the amount of choline available to a neuron will decrease the amount of acetylcholine produced.