Pharmacology - Autonomic drugs Flashcards
(82 cards)
1
Q
Cholinomimetics (4)
A
- Bethane.chol
- Carba.chol
- Pilo.car.pine
- Metha.choline
2
Q
GPCR’s
- list them, and which G-protein
A
Adrenergics: QISS Muscarinics: QIQ Dopamine: SI Histamine: QS Vasopressin: QS
3
Q
actions of alpha-1
A
- vascular smooth muscle contraction
- pupillary dilator muscle contraction (mydriasis)
- intestinal and bladder sphincted muscle
Gq, so muscle contractions
4
Q
actions of alpha-2
A
- decrease sympathetic outflow
- decrease insulin release
- decrease lipolysis
- decrease blood flood 2/2 plt aggregation
Gi, so decreases stuff
5
Q
actions of beta-1
A
- increase HR and contractility
- increases renin
- increase lipolysis
Gs, so increase stuff
6
Q
actions of beta-2
A
- increase HR and contractility
- increase blood flow (vasodilation)
- increase breathing (bronchodilation)
- increase lipolysis
- increase insulin release
- increase aqueous humor production
- increase intraocular pressure (relaxing ciliary muscle)
- decrease uterine tone
Gs, so increases stuff … beta-2, so more than beta-1
7
Q
actions of M1
A
CNS and enteric NS
8
Q
actions of M2
A
- decrease HR
- decrease atrial contractility
anti-beta-2
Gi, so decrease stuff
9
Q
actions of M3
A
- exocrine gland muscle contraction –> secretions
- intestinal muscle contraction –> peristalsis
- bladder muscle contraction
- broncho muscle contraction (broncoconstriction)
- pupillary sphincter muscle contraction (miosis)
- ciliary muscle contration (accomodation and decreases IOP by allowing humor flow)
Gq, so contraction stuff
10
Q
actions of D1
A
relaxes renal vascular smooth muscle
11
Q
actions of D2
A
modulates NT release, esp brain
12
Q
actions of H1
A
- nasal and bronchial mucus production
- increase vascular permeability
- bronchoconstriction
- pruritis
- pain
Gq, so contraction stuff
13
Q
actions of H2
A
- increases gastric acid secretion by parietal cells
Gs, so increases stuff
14
Q
actions of V1
A
increase vascular smooth muscle contraction
Gq, so muscle contraction
15
Q
actions of V2
A
increase water permeability and reabsorption at collecting tubules
Gs, so increases stuff (v2, b/c 2 kidneys)
16
Q
choline transporter inhibitor
A
Hemicholinium
17
Q
Ach vescile loading inhibitor
A
Ves.ami.col
18
Q
Ach release inhibitor
A
botilinum
19
Q
Tyrosine hydroxylase inhibitor
A
Metyrosine
20
Q
Dopamine vesicle loading inhibitor
A
Reserpine
21
Q
vesicular NE release inhibitor
A
Bretylium
Guanethidine
22
Q
vesicular NE release stimulator
A
amphetamine
23
Q
Direct agonist Cholinomimetic agents (4)
A
- Bethane.chol
- Carb.a.chol
- Pilo.car.pine
- Metha.choline
24
Q
Cholinomimetic agents (4)
A
- Bethane.chol
- Carb.a.chol
- Pilo.car.pine
- Metha.choline
25
Carb.a.chol
- action
- clinical application
- Carbon copy of Ach
- Glaucoma, pupillary constriction, relief of IOP
via M3
26
Pilocarpine
- action
- clinical application
- contracts ciliary muscle (allows flow of humor), contracts pupillary sphincter (miosis), stimulates glands (sweat, tears, saliva)
- open and close angle glaucoma; used to dx CF
via M3
27
Metha.choline
- action
- clinical application
- stimulates muscarinic receptors in airway when inhaled
| - constricts bronchioles... used as the challenge test for asthma
28
Metha.choline
- action
- clinical application
- stimulates muscarinic receptors in airway when inhaled
| - constricts bronchioles... used as the challenge test for asthma
29
Indirect agonist Cholinomimetic drugs (via AchE inhibition) (5 of them)
1. Neo.stig.mine
2. Pryido.stig.mine
3. Physo.stig.mine
4. Donepezil, Riva.stig.mine, Galantamine
5. Edrophonium
30
Neo.stig.mine
- action
- clinical application
- increases endogenous Ach; NO cross BBB
| - post-op and neurogenic ileus, urinary retention, myasthenia gravis, reversal or NMJ blockade (post-op)
31
Pyrido.stig.mine
- action
- clinical application
- increase endogenous Ach; NO cross BBB
| - long acting Myasthenia Gravis relief of weakness
32
Physo.stig.mine
- action
- clinical application
- increases engodenous Ach; CAN cross BBB
| - fixes anticholinergic toxicity b/c can cross BBB (e.g. atropine overdose)
33
Donepezil
- action
- clinical application
- increases endogenous Ach
| - Alzheimers
34
Edrophonium
- action
- clinical application
- increases endogenous Ach
| - extremely short-acting relief of Myasthenia Gravis (historically used to dx it)
35
Cholinesterase Inhibitor poisoning leads to:
DUMBBELSS
- Diarrhea/Diaphoresis, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of CNS and skeletal muscle/Emesis, Lacrimation, Sweating, Salivation
CNS excitation is by nAchR
36
Cholinesterase Inhibitor poisoning leads to:
DUMBBELSS
| - Diarrhea/Diaphoresis, Urination, Miosis, Bronchospasm, Bradycardia, Emesis, Lacrimation, Sweating, Salivation
37
antidote for cholinesterase inhibitor poisoning?
Atropine (comp inhibitor) + Pralidoxine (releases AchE is given early)
38
antidote for cholinesterase inhibitor poisoning?
Atropine (comp inhibitor) + Pralidoxine (releases AchE is given early)
39
Muscarinic antagonists used on eye (3)
| - what action
1. Atropine
2. Homatropine
3. Tropicamide
- mydriasis and cyclopegia
40
Muscarinic antagonist used for CNS (2)
1. Benz.tropine for PD and EPS
| 2. Scopolamine for motion sickness
41
Muscarinic antagonist used for respiratory (2)
1. Ipra.tropium
2. Tio.tropium
for COPD and asthma
42
Muscarinic antagonist used for GU (3)
1. Oxy.buty.nin
2. Dari.fenacin
3. Soli.fenacin
- Reduce urgency in mild cystitis and reduce bladder spasms
43
Muscarinic antagonist used for GI and respiratory
Glyco.pyrro.late
IV: pre-op use to reduce airway secretions
PO: drooling, peptic ulcer
44
Atropine toxicity results in?
"Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter"
- Hot b/c can't sweat and tachycardic
- Dry mouth and skin
- Red skin
- Blind b/c cyclopegia and acute angle glaucoma (2/2 mydriasis)
- Mad b/c disorientation
45
Atropine toxicity results in?
"Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter"
- Hot b/c can't sweat and tachycardic
- Dry mouth and skin
- Red skin
- Blind b/c cyclopegia and acute angle glaucoma (2/2 mydriasis)
- Mad b/c disorientation
46
What garden plant leads to mydriasis
Jimson weed (Datura) 2/2 plant alklaloids
47
Direct Sympathomimetics (8)
1. Epi
2. NE
3. Iso.pro.terenol
4. Dopamine
5. Dobutamine
6. Phenylephrine
7. Albuterol, Salmetrol
8. Terbutaline
48
Epi
- what receptors (at high doses which one more)
- applications
- beta > alpha (but at high doses, alpha more)
| - anaphylaxis, open-angle glaucoma (not closed angle) w/alpha, asthma, hypotension
49
NE
- what receptors
- applications
- alpha-1 > alpha-2 > beta- 1
| - treats hypotension by contraction of vascular smooth muscle, but causes decrease in renal perfusion
50
Iso.pro.terenol
- what receptors
- applications
- beta-1 = beta-2
| - used in electrophysiological evaluation of tachyarrhythmias, but can worsen ischemia
51
Dopamine
- what receptors
- applications
- D1 = D2 > beta > alpha
| - unstable bradycardia, HF, shock; inotropic and chronotropic alpha effects predominante ate higher doses
52
Dobutamine
- what receptors
- applications
- beta-1 > beta-2
| - HF (inotropic > chronotropic); cardiac stress testing
53
Phenylephrine
- what receptors
- applications
- alpha-1 > alpha-2
| - hypotension (by vasoconstriction); ocular procedures (b/c mydriatic); rhinitis (decongestant)
54
terbutaline
- what receptors
- applications
- beta-2 > beta-1
| - reduce premature uterine contractions
55
terbutaline
- what receptors
- applications
- beta-2 > beta-1
| - reduce premature uterine contractions
56
Indirect Sympathomimetics (3)
1. Amphetamine
2. Ephedrine
3. Cocaine
57
Amphetamine
- effect
- applications
- indirect general agonist, reuptake inhibitor, release of stored catecholamines
- Narcolepsy, obesity, ADD
58
Ephedrine
- effect
- applications
- indirect general agonist releases stored catecholamines
| - Nasal decongestant, urinary incontinence, hypotension
59
what should you never give suspected cocaine intoxication? and why?
beta blockers
this would lead to unopposed alpha-1 activation and extreme hypertension b/c of loss of beta-2 which vasodilates and counteracts it
60
what should you never give suspected cocaine intoxication? and why?
beta blockers
this would lead to unopposed alpha-1 activation and extreme hypertension b/c of loss of beta-2 which vasodilates and counteracts it
61
NE vs. Isoproterenol
| - BP and HR effects
NE is more alpha and Isoproterenol is beta
NE: alpha-1 --> increases BP --> reflex bradycardia
Isoproterenol: beta -2 --> decrease BP --> reflex tacycardia + beta-1 tachycardia
62
Sympatholytics (alpha-2 agonists) (2)
1. clonidine
| 2. alpha-methyldopa
63
Clonidine
- what receptors
- applications
- toxicity
- alpha-2 agonist (decrease sympathetic outflow)
- HTN emergency (doesn't decrease renal flow); ADHD, severe pain, ethanol/opioid withdrawal
- toxic: CNS depression, bradycardia, hypotension, respiratory distress, miosis
64
alpha-methyldopa
- what receptors
- application
- toxicity
- alpha 2 agonist
- HTN in pregnancy b/c safe in pregnancy
- Direct Coombs + hemolytic anemia; SLE-like syndrome
65
Non-selective alpha blockers (2)
1. Phenoxybenzamine (irreversible)
| 2. Phentolamine (reversible)
66
Alpha-1 selective alpha blocker (4)
1. Praz.osin
2. Teraz.osin
3. Doxaz.osin
4. Tamsul.osin`
67
Alpha-2 selective alpha blockers (1)
Mirtazapine
68
Phen.oxy.benz.amine
- what receptors
- applications
- toxicity
- nonselective irreversible alpha blockade
- pheochromocytoma (used pre-op) to prevent catecholamine crisis
- orthostatic hypotension, reflex tachycardia
69
Phen.tol.amine
- what receptors
- applications
- toxicity
- nonselective reversible alpha blockade
| - give to pts on MAO-I's who eat tyramine containing foods
70
Mirtazapine (Remeron)
- what receptors
- applications
- toxicity
- selective alpha-2 antagonism
- depression
- sedation, increase serum cholesterol and increase appetite
71
Epinephrine vs. Phenylephrine on BP
- before and after alpha-blockade
Epi at high doses acts more on alphas, so acts as a pressor... however, if administered after alpha-blockade, will have beta response of vasodilation and decrease in BP
Phenylephrine is a pure alpha-agonist, so acts as a pressor... so after alpha-blockade, will have no effect on BP
72
Beta-1 selective Beta Blocker (5)
1. Ace.but.olol
2. A.ten.olol
3. Bet.ax.olol
4. Esm.olol
5. Metopr.olol
beta-1 .. first 1st half of alphabet
73
Non-selective Beta blocker (4)
1. Nad.olol
2. Pind.olol
3. Propran.olol
4. Tim.olol
both beta 1- and 2 ... second half of alphabet
74
non-selective alpha AND beta antagonism (2)
1. Carvedi.lol
2. Labeta.lol
these are not -olol's, but just -lol's
75
Special beta blocker that blocks beta-1 and activates beta-3
| what does it lead to?
Nebiv.olol
cardiac selective beta-1 blockade with beta-3 agonism
- beta-3 stimualtes activation of NO synthase in vasculature
76
How does BB work to treat: angina pectoris
decreases HR and contractility, resulting in decrease O2 consumption
77
How does BB work to treat: MI
| - which ones
metoprolol, carvedilol, bisoprolol
decreases mortality
78
How does BB work to treat: SVT
| - which ones
```
metoprolol and esmolol
- class II antiarrhythmics that decrease AV conduction velocity
```
79
How does BB work to treat: HTN
| - which ones
- decreases CO by decreasing HR and contractility
| - decreases renin secretion by blocking beta-1 on JGA cells
80
How does BB work to treat: CHF
- slows progression of chronic failure
81
How does BB work to treat: glaucoma
| - which one
Timolol
decreases secretion of aqueous humor (beta-2 blockade)
82
Toxicity of beta blockers (5)
1. impotence
2. CV ADRs (brady, AV block, CHF)
3. CNS ADRs (sz, sedation, sleep alteration)
4. Dyslipidemia (w/metoprolol)
5. Exacerbation of COPD and asthma
