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Pharmacology FINAL > Lecture 8 > Flashcards

Lecture 8 Flashcards

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1
Q

what kind of receptors are muscarinic receptors

A

G-protein coupled receptors

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2
Q

what kind of receptors are nicotinic receptors

A

cation-selective ion channels

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3
Q

muscarinic receptors contain ______ transmembrane domains.

the ____ cytoplasmic loop is coupled to _______ that function as _______

A

7 transmembrane domains

3rd cytoplasmic loop is coupled to G proteins that function as TRANSDUCERS

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4
Q

true or false

all muscarinic receptors are GPCR’s

A

true

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5
Q

location of M1

A

nerves

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6
Q

location of M2

A

heart
nerves
smooth muscle

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7
Q

location of M3

A

glands
smooth muscle
endothelium

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8
Q

location of M4

A

CNS

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9
Q

location of M5

A

CNS

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10
Q

what is another name for M2

A

cardiac M2

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11
Q

postreceptor mechanism of M1

A

IP3, DAG cascade
(Gq!)

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12
Q

postreceptor mechanism of M2

A

Gi

inhibits cAMP production, activates K+ channels
results in decreased heart rate - good for HTN pts

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13
Q

post receptor mechanism of M3

A

IP3, DAG cascade
(Gq!)

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14
Q

postreceptor mechanism of M4

A

inhibits cAMP production

Gi

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15
Q

postreceptor mechanism of M5

A

IP3, DAG cascade (Gq)

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16
Q

structural features of M1, M3, M5

A

seven transmembrane segments
Gq/11 protein-linked

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17
Q

structural features of M2, M4

A

seven transmembrane segments
Gi/o protein-linked

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18
Q

TRUE OR FALSE

NM and NN have the same postreceptor mechanism

A

TRUE

Na+, K+ depolarizing ion channel

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19
Q

location of Nm

A

skeletal muscle – neuromuscular junction

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20
Q

location of Nn

A

CNS -
postganglionic cell body, dendrites

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21
Q

structural features of Nn, Nm

A

pentamer

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22
Q

early studies on the effects of muscarine were termed……..
what does this mean?

A

parasympathomimetic

does not increase the amount of neurotransmitter, but mimics the neurotransmitter

muscarine has action on receptors on effector cells

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23
Q

alkaloid nicotine stimulates _________ but NOT _______

A

stimulates autonomic ganglia and NMJ at skeletal muscle, but NOT autonomic effector cells

relaxes our muscles and makes us feel good

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24
Q

name 2 types of drugs that can be considered cholinergic agonists, but 1 is direct and 1 is indirect

A

DIRECT = drugs that activate cholinoreceptors. true agonists

INDIRECT = cholinesterase inhibiting drugs. not a true agonist, but produces the same effect by preventing the degradation of ACh

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25
what can be considered ACh "amplifiers"
cholinesterase inhibiting drugs
26
true or false a drug cannot be selective to nicotinic or muscarinic receptors
FALSE - they can
27
explain how some drugs are selective for certain nicotinic receptors
some drugs stimulate the nicotonic receptors at NMJ and have less effect on the nicotinic receptors in the autonomic ganglia
28
how can organ selectivity of drugs for nicotonic/muscarinic receptors be achieved? give an example
by using different routes of administration muscarinic stimulants can be administered to the eye to modify ocular function while also minimizing systemic side effects
29
what is "pharmacokinetic selectivity"
achieving organ selectivity by using different routes of administration
30
which cholinoreceptor is found in the nerves
M1 (also M2 but mainly M1)
31
which Cholinoreceptor is found in the heart and smooth muscle?
M2 (M3 also smooth muscle)
32
which cholinoreceptor is found in the glands and endotheloium?
M3
33
name 2 types of drugs that are DIRECT ACTING cholinergic stimulants
choline and carbamic acid esters cholinomimetic alkaloids
34
name 2 types of drugs that are indirect acting cholinergic stimulants
carbamates organophosphates
35
true or false cholinomimetic alkaloids are indirect acting cholinergic stimulants
FALSE - direct acting
36
true or false carbamates are indirect acting cholinergic stimulants
true
37
name 4 cholinomimetic alkaloids are they direct acting or indirect acting?
DIRECT ACTING muscarine pilocarpine nicotine lobeline
38
name 4 carbamates that are cholinergic stimulants are they direct or indirect acting?
INDIRECT ACTING neostigmine carbaryl physostigmine edrophonium
39
name 4 organophosphates are they direct or indirecting cholinergic stimulants?
INDRECT parathion malathion sarin echothiophate pesticides - not used in humans
40
name 4 choline and carbamic acid esters are they direct or indirect acting cholinergic stimulants?
direct acting acetylcholine and methacholine = choline esters bethanachol carbachol both are carbamic acid esters
41
none of the clinically useful cholinergic stimulants are....
selective for receptor subtypes just selective for either nicotinic or muscarinic as a group
42
explain the structure of choline esters and name 2 choline esters are they direct or indirect acting?
direct acting acetylcholine methacholine have permanently charged quaternary ammonium group and are thus relatively insoluble in lipids
43
many naturally occuring and synthetic cholinomimetic drugs are........
alkaloids
44
the ________ receptor is strongly stereoselective explain
muscarinic (S)-bethanechol is almost 1000x more potent than R bethanechol
45
what is bethanechol
a carbamic acid ester. direct acting cholinergic stimulant
46
name a pharmacokinetic property of choline esters
they are poorly absorbed and poorly distributed into the CNS bc they are hydrophilic all are hydrolyzed in the GI tract and are thus less active by oral route
47
explain a pharmacokinetic consideration of acetylcholine
it is very rapidly hydrolyzed in the GI tract (it's a choline ester!), so to achieve desired effects large amounts have to be infused IV
48
differentiate between the resistance to hydrolysis between the choline and carbamic acid esters
negligible susceptibility to choline esterase: carbachol and bethanacol (the carbamic acid esters) little susceptibility: methacholine VERY SUSCEPTIBLE to cholinesterase: ACETYLCHOLINE
49
The carbamic acid esters have extremely little susceptibility to hydrolysis by cholinesterase methanachol has a little susceptibility, and acetycholine is EXTREMELY SUSCEPTIBLE what does this mean for duration of action?
the carbamic acid esters have much longer durations of action (bethanchol, carbachol)
50
the ______ group on bethanachol and methacholine reduces the potency of these drugs at _______ receptors
beta methyl group nicotinic
51
rank the carbamic acid esters and choline esters based on their muscarinic action
most: methacholine acetylcholine tied for last: carbachol and bethanchol
52
rank the carbamic acid and choline esters according to their nicotinic action
acetylcholine and carbachol tied for 1st methacholine and bethanachol have NO NICOTINIC ACTION (bc of beta methyl group!)
53
the beta methyl group of ___ and ___ reduces the potency of these drugs at nicotinic receptors
bethanachol and methacholine
54
explain the absorption of the natural tertiary cholinomimetic alkaloids (also name 3)
well absorbed from most sites of administration pilocarpine nicotine lobeline
55
can nicotine be absorbed across the skin?
yes it is sufficiently lipid soluble
56
is muscarine a tertiary amine? what does this mean about it's absorption?
not a tertiary amine - a quaternary amine it is less absorbed from the GI tract than the tertiary amines TOXIC when ingested from certain mushrooms - enters the brain
57
the tertiary amine natural cholinomimetic alkaloids - pilocarpine, nicotine, and lobeline are excreted mainly be the kidneys what accelerates their clearance?
acidification of the urine
58
when acetylcholine binds to M2, what happens?
decreased heart rate BY complex dissociates adenylyl cyclase activity is decreased and cAMP production is decreased PKA is also decreased - required to open calcium channel
59
where is the nicotinic receptor present in extremely high concentration
in the membranes of electric organs of electric fish
60
what happens when acetylcholine binds to nicotinic receptors?
in case of a NMJ - will cause depolariazation --- OPENING OF LIGAND-GATED SODIUM CHANNEL and EPSP generation and contraction of the muscle in case of neuron - will cause excitation
61
what does nicotinic and muscaranic action do?
causes parasympathetic nervous system events - rest and digest
62
PSNS: what happens to the eye?
the sphincter muscle of the iris contracts (miosis) the ciliary muscle contracts for near vision pupil gets smoler
63
what happens to the sinoatrial node when PSNS is activated
decreased rate (negative chronotrophy)
64
what happens to the atria and ventricles of the heart when PSNS is activated
atria - decrease in contractile strength (called negative inotropy) and decrease in refractory period ventricles - small decrease in contractile strength
65
what happens to the VA node when PSNS is activated
decrease in conduction velocity (negative dromotropy) increase in refractory period
66
what happens to the blood vessels (arteries and veins) when PSNS is activated
dilation via EDRF (endothelial derived relaxation factor) high dose direct effect - constriction
67
what happens to bronchial muscle and bronchial glands when PSNS is activated
bronchoconstriction bronchial glands are stimulated to release their secretions
68
what happens to: GI motility GI sphincters GI secretion when PSNS is stimulated
increased GI motility sphincters relax secretion is stimulated
69
true or false all glands release secretions when PSNS is activated
FALSE - all exc sweat glands sweat glands are under sympathetic control
70
what happens to urinary bladder: detrussor trigone sphincter when PSNS is stimulated
detrusor contracts trigone and sphincter relax
71

Pharmacology FINAL (11 decks)

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