Drugs (Midterm I) Flashcards
Nicotine, DMPP, TEA
Class: Nicotinic Ganglionic Stimulating Receptors
MOA: Activate and desensitize nAChR in ganglionic synapses
Muscarine, Pilocarpine
Class: Muscarinic Ganglionic Stimulating Drugs
MOA: Stimulate mAChR and stimulates sympathetic nervous system via late EPSP
Pentolinium, TEA, Hexamethanonium
Class: Ganglionic Blockers
MOA: competitive antagonists and block nAChR
Botulinum Toxin
MOA: Inhibits ACh by entering the nerve terminal and acts as a protease to prevent neurotransmitter release
Gallamine, Curarine, Pancurenium
Class: Neuromuscular Blockers (Competitive non-depolarizing blocker)
MOA: Classical competitive antagonists at the nAChRs
Decamethonium-C10, Succinyl Choline
Class: Neuromuscular Blockers (Depolarizing blocker)
MOA: Partial agonists that bind to the receptors and activate them but antagonize ACh action
Edrophonium (a), neostigmine (b), DFP (c), echothiophate (c)
Class: Acetylcholinesterase blockers
MOA: Prevents the breakdown of ACh, increasing ACh in the synapse
There are 3 types: a) Reversible, b) Carbamate esters, c) Organophosphates
Activate and desensitize nAChR in ganglionic synapses
Nicotinic Ganglionic Stimulating Receptors (Nicotine, DMPP, TEA)
Stimulate mAChR and stimulates sympathetic nervous system via late EPSP
Muscarinic Ganglionic Stimulating Drugs (Muscarine, Pilocarpine)
Competitive antagonists and block nAChR
Ganglionic Blockers (Pentolinium, TEA, Hexamethanonium)
Inhibits ACh by entering the nerve terminal and acts as a protease to prevent neurotransmitter release
Botulinum Toxin
Classical competitive antagonists at the nAChRs
Neuromuscular Blockers (Competitive non-depolarizing blocker: Gallamine, Curarine, Pancurenium)
Partial agonists that bind to the receptors and activate them but antagonize ACh action
Neuromuscular Blockers (Depolarizing blocker: Decamethonium-C10, Succinyl Choline)
Prevents the breakdown of ACh, increasing ACh in the synapse
Acetylcholinesterase blockers
There are 3 types: a) Reversible: Edrophonium, b) Carbamate esters: neostigmine, c) Organophosphates: echothiophate, DFP
Carbachol, Bethanechol, Bethanecholamine, ACh
Class: Choline esters
MOA: mAChR and nAChR agonists (except bethanechol, not an agonist at nAChR)
Muscarine, Arecoline, Pilocarpine, Oxotremorine, Aceclidine
Class: Cholinomimetic Alkaloids
MOA: Mimics choline esters, relatively selective for mAChRs except arecoline which also activates nAChRs.
Belladonna
Class: Antimuscarinic drugs
MOA: Reversible inhibition of mAChRs, block parasympathetic stimulation
N-methylatropine, Ipratropium, Scopolamine
Class: Quaternary Muscarinic Antagonists
MOA: Antagonists to the mAChR and the nAChR
Atropine, Diphenhydramine (Benadryl), tricyclics, Scopolamine (anti mAChRs)
Curare, Hexamethonium (anti nAChRs)
Class: Anticholinergics
MOA: Competitively inhibit binding of ACh, more commonly in mAChRs, less so in nAChRs
Physostigmine, Neostigmine
Class: Anticholinesterases
MOA: Cholinometric effects at both nicotinic and muscarinic synapses by inhibiting AChE
Albuterol, Ritodrine, Tertbutaline, Salmeterol
Class: b2AR agonists
MOA: Mostly selective for b2ARs, will stimulate cAMP and PKA. Relaxation of VSM, bronchodilators, can delay labor (ritodrine), some have cardio effects
Dobutamine
One isomer is an a1 agonist, the other an a1 antagonist. b1AR antagonist, increases heart rate
Fenoldopam
Class: D1 agonists
MOA: Activates D1 receptors and increases cAMP levels which can cause vasodilation, lowering BP. No AR activity
DOPA, carbidopa
Used in treatment of Parkinson’s Disease. Leads to production of dopamine from DOPA.
Cocaine
Blocks vasopressor response to tyramine and potentiates response to NE
Methamphetamine, Adderall, Cocaine, Pseudoephedrine
Class: Amphetamines
MOA: Blocks the uptake of NE and can stimulate both aARs and bARs causing increase in BP, decrease in HR, elevate cAMP in brain