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Ch 6-9 Flashcards

(85 cards)

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1
Q

What effect does an agonist have on an M1 receptor?

A

modulation of neurotransmission. located on CNS and all pre-synapses

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2
Q

What effect does an agonist have on an M2 receptor?

A

slowing of heart rate and conduction. Located on cardiac SA/AV

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3
Q

What effect does an agonist have on an M3 receptor?

A

contraction of smooth muscles and stimulation of glandular secretion. located on ENS

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4
Q

what do nicotinic receptors do?

A

excite neurotransmission whereas activation causes contraction.

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5
Q

sympathomimetic

A

sympathetic agonist… drugs that mimic the effects of transmitter substances of the sympathetic nervous system

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6
Q

sympatholytic

A

sympathetic antagonist… a medication which inhibits the postganglionic functioning of the sympathetic nervous system

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7
Q

can acetylcholine release affect the sympathetic system?

A

yes, the presence of muscarinic receptors on sympathetic nerve terminals provides the interaction between the parasympathetic and sympathetic nervous systems: the release of acetylcholine from parasympathetic nerves inhibits the release of norepi form sympathetic nerves

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8
Q

what is the difference between direct and indirect acting in terms of acetylcholine agonists?

A

a direct agonist directly bidns to the receptor whereas an indirect agonist will increase the synaptic concentration of acetylcholine by inhibiting cholinesterase

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9
Q

what are some choline esters?

A

Ach, bethanecol and carbachol

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10
Q

what do choline esters do?

A

parasympathetic agonists.

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11
Q

Should we give choline esters to bad asthma pts?

A

not really since it causes brochoconstriction. even eye drops can cause it.

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12
Q

what is carbacol used for?

A

open angle glaucoma (if pilocarpine fails)

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13
Q

what is Ach used for?

A

opthalmic surgery requiring rapid/complete miosis and to diagnose vasospastic angina

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14
Q

what is bethanecol used for?

A

It’s selective for muscarinic receptors and is used to stimulate GI without cardiac effects (possibly m3)

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15
Q

what is pilocarpine used for?

A

choronic open angle glaucoma, acute angle closure glaucome and xerostomia

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16
Q

what is cevimeline (evoxac) used to treat?

A

used to radiation induced dry mouth

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17
Q

what is varenicline (chantix) used to treat?

A

smoking cessation but causes bronchoconstriction (nicotinic receptor agonist)

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18
Q

what are some of the risks of long term irreversible cholinesterase inhibitors (organophosphate)?

A

highly toxic. used for warfare agents, pesticides. highly lipid soluble - (absorbed from all sites including skin and stored in the 2nd compartment)

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19
Q

malathion

A

irreversible cholinesterase inhibitor used to treat lice. don’t leave on scalp for long or it can be absorbed systemically

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20
Q

what/where are the nicotinic receptors located?

A

post-synaptic receptors for acetlycholine and nicotine. located on skeletal muscles and in the brain

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21
Q

treatment of organophosphate exposure?

A

decontamination (gastric lavage and activated charcoal), atropine, pralidoximee (quickly!!)

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22
Q

what is ethylene glycole considered?

A

antifreeze is considered an organophosphate

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23
Q

what is atropine?

A

muscarinic receptor antagonist. mydriasis and inhibits lacrimal gland secretion.

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24
Q

what is pralidoxime?

A

an orphan drug which is effective in treating organophosphate drugs but must be given immediately! once the bond between the organophosphate inhibitor and cholinesterase becomes strong (ages) this drug is not effective!! pg60

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25
what is the brand name of sildenafil?
viagra
26
what does sildenafil do?
potentiate vasodilative effect of Ach from sacral parasympathetic neurons (M3), rapidly orally absorbed, metabolically by CYTP450 3a4 (grapefruit juice), contraindicated with nitrates (profound hypotension, relfex tachycardia), interacts with dixazosin (BPH)
27
what is doxazosin use for?
Benign prostatic hypertrophy
28
what do muscarinic receptor antagonists do?
relax smooth muscle, decrease gland secretions, and stimulate the heart
29
what do nicotinic receptor antagonist do?
neuromusclular blocking agents used to relax smooth muscle for surgery. if we then gave them an agonist, it would cause twitching
30
what would a pt on lots of belladonna look like?
it's an anticholinergic so dry as a bone, blind as a bat, red as a beet and mad as a hatter
31
what can you use atropine for?
examination of peripheral retina by paralyzing ciliary muscles, sinus bradycardia with hyotension or ischemia, limit respiratory secretions, relieve intestinal spasm, motion
32
what is ipratropium/tiotropium used to treat?
asthma/emphysema.
33
why should people wash their mouths after using ipratropium/tiotropium?
to limit side effects (tachycardia)
34
what is dicyclomine used for?
anticholinergic. to treat intestinal cramping, IBS. slows GI motility
35
What is glycopytolate used for?
used during surgery to inhibit salivary/respiratory tract secretions
36
what is scopalamine used for?
to treat motion sickness, nausea and is sedating
37
what is benztropine used for?
parkinson's disease and drug induced parkinson's disease. OD on haldol
38
how do you tell the difference between an anti-muscarinic poisoning vs psychotic episode?
true psychotic episode does not involve dry mouth, hyperthermia, dry skin, etc. aka dry as a bone, red as a beet, mad as a hatter
39
how do you treat antimuscarinic poisoning/ belladonna?
physostigmine
40
what are the major symptoms of overactive bladder?
urgency, frequency, nocturia and urge incontinence
41
how to you treat overactive bladder?
long term antimuscarinic to prevent peaks, don't cross the BBB and use muscarinic selective receptor
42
what does a non-depolarizing neuromuscular agent do/curariform drugs?
causes flaccid paralysis Don't cross the BBB aka the perceive pain. compete for Ach for binding nicotinic.
43
what are some of the curariform drugs?
atracurium,cisatracurium, pancuronium, rocuronium, vecuronium.
44
What is succinylcholine?
used for intibation, hydrolyzed by cholinesterase, no antidote!! can cause malignant hyperthermia. caution: children, burn victims: hyperkalemia increased effect.
45
What effect does an agonist have on an Alpha 1 receptor?
constricts vascular smooth muscle, vasoconstriction, iris dilator muscle and contraction of bladder
46
What effect does an agonist have on an Alpha 2 receptor?
mediate platelet aggregation, mediate inhibition of insulin (worry about diabetics)
47
What effect does an agonist have on Beta-1 receptor?
positive chronotrope, inotope, dromotrope and increases renin secretion
48
What effect does an agonist have on Beta-2 receptor?
relaxes bronchial, uterine, and vascular smooth muscle, mediates glycogenolysis
49
What effect does an agonist have on Beta-3 receptor?
selective agonist to treat obesity, no drugs to selectively get to this
50
what is positive chronotrope?
increase heart rate
51
what is inotrope?
an agent that alters the force or energy of muscular contractions
52
what is a dromotrope?
affects atrioventricular node (AV node) conduction
53
what does an agonist of dopamine 1 receptor do?
mediate vascular smooth muscle relaxation
54
what does an agonist of dopamine 2 receptor do?
modulate neurotransmitter release
55
what are some direct acting adrenoreceptor agonists?
catecholamines, dobutamine
56
what does norepinephrine do?
its a alpha 1 adrenoreceptor agonist, catecholamine. vasoconstriction, increased peripheral resistance, increased SBP/DBP watch out for reflex bradycardia --> can cause heart failure
57
what does epinephrine do?
increases HR and CO increases SBP/neutral or decreased DBP low dose = greater beta 2 stimulation and vasodilation higher dose = greater alpha 1 stimulation and increased DBP due to less selectivity
58
what does dobutamine do?
direct acting adrenoreceptor agonist decreases vascular resistance while stimulating the heart i.e. good for ischemics
59
what does dopamine dor?
catecholamine that increases BP and cardiac stimulation causes renal vasodilation (pts in shock)
60
what does isoproterenol do?
potent bronchodilator causes cardiac side effects so not good in asthma pts
61
what are some adverse side effects of direct acting adrenergic agonists?
vasoconstriction in areas of localized ischemia and necrosis extravasation can cause serious injury cardiac arrhythmias hyperglycemia
62
what uses does a direct acting adrenergic agonists have?
hypovolemic shock, cardiogenic shock, septic shock, anaphylactic shock
63
what are some noncatecholamine adrenergic agonists?
phenylephrine and midodrine
64
what does phenylephrine do and when is it used?
vasoconstrictor used in nasal decongestant, ocular decongestant hyotension due to decreased vascular resistant maintain BP during surgery
65
what does midodrine do and when is it used?
orthostatic hypotension used to treat dialysis pts primary ADR is hypertension
66
what are the benefits of albuterol, terbutaline via inhaler?
Inhaled will make for an easier side effect profile for asthma (and bypass first pass metabolism) Can cause restlessness, tremor , tachycardia and K imbalance
67
whwat are some indirect acting adrenoreceptor agonists?
amphetamine, cocaine
68
what are some mixed acting adrenoreceptor agonists?
ephedrine and pseudoephredrine
69
what is amphetamine and what does it do?
indirect acting adrenoreceptor agonist, causes vasoconstriction, cardiac stimulation, increased BP and CNS stimulation
70
what is cocaine and how does it work?
indirect acting adrenoreceptor agonist. causes local anesthetic and vasoconstrictive. prevents absorption into the blood stream. good for eye surgery
71
what is ephedrine and pseudoephedrine and what does it do?
mixed acting adrenoreceptor agonists. alpha 1 vasoconstriction and beta 2. can cause tachycardia, urinary retention and increased BP. used for colds
72
what is phentolamine used to treat for?
alpha antagonist used to treat pheochromocytoma and ischemia due to alpha adrenoreceptor agonist (epi shot in finger)
73
adverse effects of beta 1 blockade?
It can cause bradycardia, reduced CO, heart failure, AV heart block. AND if discontinued apruptly can cause rebound cardiac excitation
74
what are some adverse effects of beta 2 blockade?
bronchoconstiction, glycogenolysis, or if someone needs to use an epi-pen it could block the effect. needs 2 doses possibly
75
what does 1st generation betablocker do? ie proranolol
nonselective. blocks beta 1 and 2
76
what does 2nd generation betablocker do? ie metoprolol
cardioselective for beta 1
77
what does 3rd generation betablocker do? ie carvedilol
vasodilating and blocks norepi and epi. more selective than 1st and 2nd generation
78
what is propanolol and what does it do?
non-selective 1st generation beta blocker (both beta 1 and 2), causes bronchoconstriction, also blocks renal beta 1 (suppresses renin secretion)
79
what is propanolol and what does it do?
2nd gen beta blocker. cardioselective. will still mask tachycardia (bodies response to hypoglycemia)
80
what is labetalol and what does it do?
3rd generation beta blocker. blockers alpha receptors (warn of orthostatic hypotension) and beta receptors.
81
How do alpha blockers treat HTN?
by vasodilating blood vessels
82
how do alpha blockers reduce BPH symptoms?
by relaxing smooth muscles in the bladder neck
83
what are some adverse drug effects of alpha blockade?
orthostatic HTN, reflex tachycardia, nasal congestion, inhibition of ejaculation
84
what can cause first dose orthostatic hypotension?
alpha blockade so keep them in the office
85
what are some uses for beta blockers?
HTN, angina, heart failure, SVT, bradycardia

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