Flashcards in First Aid 245-249 Pharm Deck (41):
maximum effect a drug can produce - inc efficacy = inc y value
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.
median toxic dose
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?
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?
Which toxin prevents the release of Ach?
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
Metyrosine inhibits which reaction?
Tyrosine --> DOPA
Reserpine does what?
Inhibits the uptake of Dopamine into a vesicle via VMAT
What stimulates and inhibits NE release into the synapse?
Stimulate: ATII- R activation, Ca 2+, Amphetamine, Ephedrine
Inhibit - a2-R activation, Bretylium, Gaunethidine
Which drugs inhibit the reuptake of NE into the nerve terminal?
Cocaine, TCAs, Amphetamine
Major functions of a1 -R?
Inc vascular smooth m contraction, mydriasis, inc GI/Bladder sphinter musc contraction
Which G prot coupled receptor increases/dec insulin release?
Which receptor stimulates platelet aggregation?
Which receptor increases vascular permeability?
Which receptor increases H20 permeability and resorption in the kidney, and which part of the tubules?
V2R - (V 2in the 2-bules! ) in the collecting duct
Which G prot coupled receptor decreases heart rate and atrial contractility?
Reserpine is contraindicated with use of what other drug?
Guanethidine mech / contraindicated with which drug?
Guanethidine binds NE filled vesicles to stop NE realease, CI w/ TCAs (will inhibit uptake of Guanethidine)
Fun fact: Most G prot coupled rec'r have carboxylated tails with palmitoyl @ cysteine residues
It helps anchor them to plasma membrane
Which adr. rec'r dec uterine tone?
Which rec'r activation causes broncioloconstriction?
Which two rec'rs, when (+)'d, will cause vascular smooth muscle contraction?