First Aid 245-249 Pharm Flashcards
(41 cards)
Efficacy
maximum effect a drug can produce - inc efficacy = inc y value
Potency
amount of drug needed for given effect - Inc potency = to the left
Competitive antagonist shifts a curve in what direction? Does it affect potency? Efficacy?
Shift curve to the R - more potency, no change in efficacy
Can be overcome with increasing substrate level
Noncompetitive antagonist shifts curve in what direction? Does it affect potency? Efficacy?
Shifts curve down - dec efficacy (as expected)
Partial agonist - location of action. Does it affect potency? Efficacy?
Acts on the active site - same location as full agonist. Lower maximal effect, and therefore decreased efficacy. Potency is not related.
TD50
median toxic dose
ED50
median effective dose
Drugs with higher therapeutic index
digoxin, lithium, theophylline, warfarin
Parasympathetic Ach M-R are located where?
Cardiac, smooth muscle, gland cells, n. terminals
Sympathetic Ach M-R located where?
Sweat glands
Sympathetic (NE) stimulate alpha/beta -R where?
Cardiac and smooth musc, gland cells, n. terminals
Sympathetic Dopamine-R located where?
renal a/v, smooth musc
What stimulates the adrenal medulla to release Epi, NE?
Ach
Which toxin prevents the release of Ach?
Botulinum toxin
Nicotinic Ach receptors are connected to which type of channels?
Ligand gated Na/K channels
Muscarinic Ach receptors have what type of mechanisms, and what are the subtypes?
G protein coupled receptors acting through second messangers - 5 subtypes: M1-5
Which receptors are Gq coupled ?
alpha 1, Muscarinic 1 & 3, H1, V1
Which receptors are Gs coupled?
B1, B2, D1, H2, V2
Which receptors are Gi coupled?
a2, M2, D2
Pathway of Gq
PLC –> PIP2 splits into DAG + IP3. DAG –>PKC, IP3 –> inc Ca –> smooth musc contraction
Pathway of Gs/Gi
Gs and Gi stimulate and inhibit AC, respectively. AC –> inc cAMP –> stimulate PKA –> stimulate Ca in heart and myosin light chain kinase in smooth musc
Hemicholinium inhibits what?
the uptake of choline into a nerve terminal
Vesamicol inhibits what?
The uptake of Ach into a vesicle
What stimulates/inhibits the release of Ach into a synapse?
Ach release into a synapse is stimulated by Ca2+ and inhibited by Botulinum toxin