Pharm - Drug Flashcards

Front 1

Edrophonium

Back 1

Clinical. Non-covalent, reversible prototype: short-acting AChEI, dx of MG.

Front 2

Physostigmine

Back 2

Clinical. Carbamate Ester: covalent, slowly reversible “suicide” AChEI inhibitor. Crosses BBB.

Front 3

Neostigmine

Back 3

Clinical. Carbamate Ester: covalent, slowly reversible “suicide” AChEI inhibitor. Reverses non-depolarizing NM blockade. Post-surgical use for bowel motility.

Front 4

Isoflurophate

Back 4

Organophosphate. Covalent, irreversible inhibitor of AChE. May undergo additional “aging” modifications.

Front 5

Echothiophate

Back 5

Organophosphate. Covalent, irreversible inhibitor of AChE. May undergo additional “aging” modifications.

Front 6

Pralidoxime

Back 6

Clinical. Organophosphate nucleophile “antidote.” Regenerates AChE (ineffective if “aged”/carbamylated.)

Front 7

Why are AChEI drugs used to treat Alzheimer’s patients?

Back 7

A loss of CNS cholinergic transmission is thought to play a major role in the cognitive deficits of Alzheimer’s patients.

Front 8

Donepezil

Back 8

Clinical. Central-acting non-competitive AChEI, used in Alzheimer’s tx. SE: nausea, diarrhea, vomiting.

Front 9

What are the “Congenital Myasthenic Syndromes”?

Back 9

Pre- or post-synaptic cholinergic mutations. Can be hyper- or hypoactive, depending on mutation/phenotype.

Front 10

What class of cholinergic receptors are lingand-gated?

Back 10

Nicotinic acetylcholine receptors are ligand-gated.

Front 11

What class of cholinergic receptors are metabotropic?

Back 11

Muscarinic acetylcholine receptors are ligand-gated.

Front 12

Milrinone (Primacor)

Back 12

Clinical. PDEI. Increases cardiac contractility, causes vasodilation. Short-term tx for CHF.

Front 13

What is is one mechanism for the down-regulation of GPCRs?

Back 13

Once active, GPCRs are subject to phosphorylation by GPCR Kinases, targeting them for internalization and possible degradation.

Front 14

How does BoTox function?

Back 14

BoTox is a protease, cleaving SNAPs required for ACh vesicle fusion and synaptic function.

Front 15

Mivacurium

Back 15

Non-depolarizing neuromuscular blocking agent. Antagonizes ACh receptors.

Front 16

Acetylcholine

Back 16

Choline Ester. Metabotropic ACh Receptor agonist. Few clinical uses.

Front 17

Hexamethonium

Back 17

Nicotinic ganglionic antagonist. Have little effect at the NMJ, only the ganglion.

Front 18

Trimethaphan

Back 18

Nicotinic ganglionic antagonist. Have little effect at the NMJ, only the ganglion.

Front 19

Mecamylamine

Back 19

Nicotinic ganglionic antagonist. Have little effect at the NMJ, only the ganglion.

Front 20

Carbachol

Back 20

Choline Ester. Non-specific acetylcholine receptor agonist. Not well absorbed, no CNS access. Main use is ophthalmic.

Front 21

Oxotremorine

Back 21

ACh Alkaloid Agonist. Non-specific MUSCARINIC cholinergic. Has CNS access, produces chorea/tremors (eponymic)

Front 22

Atropine

Back 22

Muscarinic competitive antagonist. Antidote to cholinergic OD. Mnemonic for excessive Atropine: "Hot as a hare, blind as a bat, dry as a bone, red as a beet, and mad as a hatter."

Front 23

acetylcholine

Back 23

Choline Ester. Prototype agonist for AChRs. Causes contraction of skeletal mm when released on the NMJ. Decreases contractility when released on cardiac myocytes. Used at all PANS and SANS pre-ganglionic synapses. Used at PANS post-ganglionic synapses.

Front 24

bethanechol

Back 24

Choline ester. Selective long-acting muscarinic agonist. Used to enhance bladder and bowel tone.

Front 25

carbachol

Back 25

Choline ester. Non-selective (M&N) medium-acting cholinergic agonist. Indicated for ophthalmic use for tx of glaucoma.

Front 26

methacholine

Back 26

Choline ester. Non-specific, long-acting muscarinic agonist. Clinically used to diagnose bronchial asthma (methacholine challenge). No CNS access.

Front 27

muscarine

Back 27

Muscarinic alkaloid. Metabotropic cholinergic agonist. No CNS access. Toxicity mnemonic: "SLUDGE"

Front 28

pilocarpine

Back 28

Muscarinic alkaloid. Metabotropic cholinergic agonist. Largely ophthalmic use, as well as xerostomia (induces secretion of saliva and sweat). Used to dx cystic fibrosis (chloride content of sweat.)

Front 29

dimethylphenyl piperazinium (DMPP)

Back 29

Nicotinic ganglionic agonist. Agent will activate both PANS and SANS response.

Front 30

hexamethonium (C6)

Back 30

Nicotinic ganglionic antagonist. No effect on NMJ or mAChRs. Originally used to treat HTN. SEs are both sympatholytic (orthostasis, sexual dysfunction) and parasympatholytic (constipation, urinary retention, glaucoma, decreased secretions.)

Front 31

mecamylamine

Back 31

Ganglionic nicotinic antagonist. GI and BBB crossing. Possible clinical use in smoking cessation and in severe depression. SEs as above.

Front 32

nicotine

Back 32

Alkaloid. Ganglionic and partial CNS nicotinic cholinergic agonist. Stimulant properties due to ganglionic stimulation of adrenal medullary innervation. Dopamine release in CNS responsible for habit-forming nature of drug.

Front 33

Phenoxybenzamine

Back 33

Non-selective alpha adrenergic antagonist. Drug covalently binds to all alpha receptors, cannot be competitively removed.

Front 34

Phentolamine

Back 34

Non-specific alpha adrenergic antagonist. Competitive inhibitor - drug may be competitively removed.

Front 35

Prazosin

Back 35

Alpha-1 specific adrenergic antagonist. Competitive inhibitor. Alpha-1 inhibitors widely used for HTN, BPH.

Front 36

Propranolol

Back 36

Non-selective beta adrenergic antagonist.

Front 37

Yohimbine

Back 37

Alpha-2 specific adrenergic antagonist. Competitive inhibitor. Off label use as a male sexual adjuvant and body-building drug.