Drugs & Receptors Flashcards
1
Q
Muscarinic effects on:heart
A
decrease HR, contractility, conduction at AV node
2
Q
M on blood vessels
A
vasodilation, not innervated
3
Q
m on blood pressure
A
hypotension
4
Q
m on lungs
A
bronchoconstrictionsecretions
5
Q
m on eye
A
miosis, accomodation, increase aqueous humour outflow (good for glaucoma), tears
6
Q
m on GI/GU
A
increase salivationopen sphincter and increase detrusorincrease motilitystimulates erection
7
Q
nicotinic on NMJ
A
muscle contraction
8
Q
m on CNS
A
memory, cognition, movement
9
Q
a1 on eye
A
pupil dilates
10
Q
b2 on trachea and bronchioles
A
dilates
11
Q
b1 on kidney
A
increases secretion of renin
12
Q
a1 on kidney
A
decreases secretion of renin
13
Q
a1/b2 on bladder
A
contraction of trigone and sphincter, relaxes detrusor
14
Q
a1 on male genetalia
A
stimulates ejaculation
15
Q
a1 on salivary glands
A
thick, viscous secretion
16
Q
b1 on heart
A
increased rate, increased contractility
17
Q
B2/A1 on GI
A
decrease in muscle motility and tone, contraction of sphincters
18
Q
b2 on female genetalia
A
relaxation of uterus
19
Q
B2 on blood vessels
A
skeletal vasodilation
20
Q
a1 on blood vessels
A
constriction
21
Q
a2 on blood pressure
A
decreases via central effect at vasomotor center
22
Q
a1 on eye
A
mydriasis for eye examsmydriasis = dilation of pupil
23
Q
b on eye
A
increase humour production (increases intraocular pressure)maintains glaucoma pathophysiology
24
Q
a1 on GU
A
close sphincter
25
b2 on female genetalia
uterine relaxation to prevent premature labour
26
b2 on NMJ
causes muscle tremors = bad
27
adrenergic on CNS
increases vigilance and focus for ADHD
28
b inhibition on cns
used to treat stage fright, essential tremor
29
What are the main direct cholinergic agonists?
bethanachol, pilocarpine
30
what do physostigmine and neostigmine do?
AchE inhibitors
31
What are main muscarinic receptor antagonists
atropine, scopolamine, tropicamide (all tertiary)ipratropium
32
what is donepezil?
tertiary ACHEi- crosses BBB, used in seizures
33
what is pralidoxime used for?
organophosphate poisiningDetaches organophosphates from AChE
34
How does botulinum toxin work?
Blocks ACh release.It lyses synapto- brevin, thereby preventing synaptic vesicle fusion and Ca2+-dependent release; used clinically to prevent spasms and reduce pain in ocular/facial muscles and to reduce severe underarm sweating (axillary hyperhidrosis); used cosmetically to lessen wrinkles; has a 2-4 mo duration/local injection.Leads to respiratory failure
35
How does black widow toxin work?
Promotes ACh releaseIt results in excessive clumping of vesicles and “explosive release”. Also leads to respiratory failure.
36
What is edrophonium?
Ultra short acting AChEi
37
What is the action of nicotine?
nAChr agonist
38
What is the action of curare?
Non-depolarizing blocker at muscle type nAChr'scompetitive antagonists at nAChRs at the NMJCauses flaccid paralysis of skeletal musclesrenal elimination
39
What is atracurium?
Non-depolarizing blocker at muscle-type nAChRs competitive antagonists at nAChRs at the NMJCauses flaccid paralysis of skeletal musclesCompared to curare: faster onset, shorter duration of action, fewer side effectsEliminated via spontaneous hydrolysis and hydrolysis by plasma ChEs$$$
40
WHat is Rocuronium?
Non-depolarizing blocker at muscle typenAChr's competitive antagonists atnAChRs at the NMJCauses flaccid paralysis of skeletal musclesCompared to atracurium: faster onset, similar duration of action(2) None of curare’s side effects(3) Eliminated via hepatic metabolism$$$
41
What is succinylcholine?
Depolarizing blocker at muscle type nAChr's (1) Like ACh, succinylcholine interacts with nAChRs to increase Na+ permeability; the resulting depolarization leads to a short burst of action potentials; this initial stimulation (1-5 min) is associated with muscle fasciculations and soreness.(2) Since succinylcholine is not as rapidly eliminated as ACh, depolarization at the NMJ is prolonged and depolarization block, as well as desensitization, produce flaccid skeletal muscle paralysis.Used to facilitate intubation and to allow controlled ventilation in ICU and as an adjuvant to surgical anesthesia
42
What is the tensilon test?
In myasthenia gravis, Ab to muscle type nAChr often result in skeletal muscle weakness and fatiguability. Endrophonium (tensilon) is an ultra-short acting AChEi that is used for diagnosis. The person would get a little stronger.
43
What is the depolarization blockade?
Prolonged stimulation of nAChRs, for example caused by AChE inhibitors increas- ing the lifetime of synaptic ACh, results in(1) depolarization blockade"
44
How do you usually treat myasthenia gravis?
reversible, long acting AChEi's like pyridostigmine (quaternary)SteroidsThymectomy
45
nicotine on nAChr in NMJ
blockade (depolarization block and nAChr desensitization)
46
n on periperal sesnsory receptors
stimulation(stretch receptors, chemo- receptors (carotid and aortic bodies), thermal receptors (skin and tongue), and pain receptors)
47
n on ANS ganglia
initial stimulation followed by blockade (depolarization block & nAChr desensitization)
48
n on CV system
increase HR and BP
49
n on CNS
stimulation followed by depression and addiction
50
What are the monoamines?
DA, NE, 5HT
51
What does MAO do?
Mitochondrial enzyme, converts catecholamines to aldehydes, isozymes with different substrate specificities exist (MAO A: norepinephrine, serotonin, tyramine; MAO B: dopamine).
52
What are MAOi's used for?What are some common MAOi's?
Depression:Phenylzine, tranylcypromine = irreversible inhibitors of MAO A, Bmoclobemide = reversible inhibitor MAO AParkinson's:Selegiline = irreversible MAO B
53
How would you stop premature labor?
B2 agonist
54
What receptors are on the eye?What do they do?
Muscarinic:Miosis, accomodation, increase aqueous humour outflowa1: mydriasisb: increases humor production
55
What receptors are involved in peeing?
Muscarinic: contracts detrusor, opens sphinctera1: closes sphincter, b2: relaxes detrusor
56
What receptors does propranolol work on?
B1, B2 antagonist
57
How do you treat Alzheimer's?
Overall goal is to increase ACh activityGive donepezil (AChEi)and memantine (NMDA-R antagonist)
58
Tell me about actions of B2 receptors.
Skeletal blood vessels: vasodilationBronchodilationSmooth muscle relaxation in GI tractUterine relaxationMuscle tremors @NMJDetrusor relaxationIncreases aqueous humour (B nonspecific)
59
What are 2 important muscarinic agonists?
bethanacol, pilocarpine, and ACh of course
60
What are the nicotinic receptor agonists?
ACh, nicotine
61
What are the muscarinic receptor antagonists?
Atropine, scopolamine, tropicamide
62
What are the AChE inhibitors?
Neostigmine, physostigmine, donepezil, edrophonium, organophosphates (irreversible)
63
What is an irreversible AChEi?What is the one drug you can use to reverse it?
OrganophosphatesPralidoxime
64
Adrenergic agonists at a1, b1, b2
EpinephrinePseudophedrine, Tyramine (indirect)
65
a1, b1 agonists
Ephedrine (indirect)NE
66
a1 selective agonist
phenylephrine
67
a2 selective agonist
clonidine
68
b1 selective agonist
dobutamine
69
a1 selective antagonist
prazosintamsulosin (flomax)
70
a1, a2 antagonist
phentolamine (reversible)phenoxybenzamine (irreversible)
71
b1 selective antonist
metoprolol, atenolol
72
b1,b2 antagonist
propranolol
73
b1, b2 agonist
isoproterenol
74
a1, b1, b2 antagonist
labetalolcarvedilol
75
b2 selective agonist
albuterol
76
Main COMT inhibitor
entacapone
