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119 Cards in this Set

  • Front
  • Back
nAChR vs mAChR?
nAChR - ligand gated Na/K channels (Nn - autnomic ganglia; Nm - NMJ)

mAChR - Gprtn coupled receptors; 5 subtypes
which autonomic receptors are coupled to which G-prtns with what intracellular action? (mneumonic)
"QISS and QIQ till you're SIQ of SQS (sex)"

alpha1 - Gq
alpha 2 - Gi
beta 1 - Gs
beta 2 - Gs
M1 - Gq
M2 - Gi
M3 - Gq
D1 - Gs
D2 - Gi
H1 - Gq
H2 - Gs
V1 - Gq
V2 - Gs

order: Sympathetic, Parasympathetic (M1-M3), Dopamine, Histamine, Vasopressin
what intracellular mechanism for Gq?
Gq --> activates Phospholipase C --> PIP2 --> DAG which activates PKC & IP3 which increases Ca++ channel influx

(alpha 1, M1, M3, H1, V1)
what intracellular mechanism for Gi?
Gi --| inhibits adenylyl cyclase, decreases cAMP, decreased PKA activity
-PKA then does NOT activate myosin light chain kinase (smooth mm) nor increase Ca++ influx (heart)

(alpha2, M2, D2)
what intracellular mechanism for Gs?
Gs --> stimulates adenylyl cyclase --> increases cAMP --> activates PKA:
-heart --> increased Ca++ influx
-smooth mm --> increased myosin light chain kinase (increase mm activity)
what other receptors are coupled to Gs like the beta adrenergics?
TSH
PTH
Glucagon
what receptor mediates increased vascular smooth mm contraction?
alpha-1; Gq
V1; Gq
what receptor mediates increased pupillary dilatory mm contraction (mydriasis)?
alpha-1; Gq
what receptor mediates intestinal & bladder sphincter contraction?
alpha-1; Gq
what parasympathetic receptor mediates the CNS & enteric nervous system?
M1; Gq
what receptor mediates decreased HR & contractility of the atria?
M2; Gi
what receptor mediates increased exocrine gland secretion?
M3; Gq
(sweat, gastric acid)
what receptor mediates increased gut peristalsis?
M3; Gq
what receptor mediates increased bladder contraction?
M3; Gq
what receptor mediates bronchoconstriction?
M3; Gq
what receptor mediates increased pupillary sphincter mm contraction (miosis)?
M3; Gq
what receptor mediates ciliary mm contraction (accommodation)?
M3; Gq
what receptor mediates decreased sympathetic outflow?
alpha-2; Gi
what receptor mediates decreased insulin release?
alpha-2; Gi
what receptor mediates increased heart rate?
beta-1 (beta2 - according to FA...); Gs
what receptor mediates increased contractility?
beta-1 (& beta2 - according to FA...?); Gs
what receptor mediates increased renin release?
beta1; Gs
what receptor mediates increased lipolysis?
beta1, beta2; Gs
what receptor mediates vasodilation?
beta2; Gs
what receptor mediates bronchodilation?
beta2; Gs
what receptor mediates increased insulin release?
beta2; Gs
what receptor mediates decreased uterine tone?
beta2; Gs
what receptor mediates renal vascular smooth mm relaxation?
D1; Gs
what receptor mediates modulation of transmitter release, especially in the brain?
D2 (among others....); Gi
what receptor mediates increased nasal & bronchial mucus production?
H1; Gq
what receptor mediates contraction of bronchioles?
H1; Gq
what receptor mediates pruritis?
H1; Gq
what adrenergic receptor mediates pain?
H1; Gq
what receptor mediates increased gastric acid secretion?
H2; Gs
what receptor mediates increased H20 permeability & reabsorption in collecting tubules of kidney?
V2; Gs
(V2 is found in the 2 kidneys)
(V1 mediates vascular smooth mm contraction)
what inhibits the release of acetylcholine at the nerve termina?
botulinum
what inhibits the reuptake of choline into the nerve terminal?
hemicholinium
what inhibits ACh from being packaged into vesicles by ChAT?
vesamicol
what inhibits the conversion of tyrosine to DOPA?
metyrosine
what inhibits the packaging of dopamine & NE into vesicles?
reserpine
what inhibits the reuptake of NE at the nerve terminal?
cocain
TCA
amphetamine
what prevents release of NE filled vesicles at the nerve terminal?
Guanethidine
what increases release of NE by nerve?
amphetamine
on the cardiac NE nerve terminal what is the effect of
alpha2 receptor?
AII receptor?
M2 receptor?
alpha2 - inhibits NE release (negative feedback)
AII - promotes NE release (angiotensin II)
M2 - inhibits NE release
bethanechold?
direct cholinomimetic

-activates bowel & bladder smooth mm
-resistant to AChE
what direct cholinomimetic is resistant to AChE?
bethanecol (activates bowel & bladder)
pilocarpine (used for emergency glaucoma)
carbachol?
direct cholinomimetic agonist
(CARBon copy of AcetylCHOLine)
-used for eyes
used for postoperative & neurogenic ileus & urinary retention?
bethanechol
direct cholinomimetic agonist
used for glaucoma, pupillary contraction, & relief of intraocular pressure?
Carbachol
Pilocarpine?
direct cholinomimetic
-contracts mm of eye (open angle)
-contract pupillary sphincter (narrow angle)
-resistant to AChE
use for emergency glaucoma?
Pilocarpine
direct agonist cholinomimetic
"cry, drool, sweat on PILOw"

potent stim: sweat, tears, saliva
challenge test for diagnosis of asthma?
Methacholine
direct agonist cholinomimetic
-stimulate muscarinic receptors in airway when inhaled
Neostigmine?
anticholinesterase (indirect agonist)
NeO = no CNS penetration

used for postop neurogen ilues & urinary retention; myasthenia gravis, reversal of NMJ
Pyridostigmine?
anticholinesterase
used for myasthenia gravis (long acting)
does NOT penetrate CNS

pyRIDostigmine gets RID of myasthenia gravis
use for dx of myasthenia gravis?
Edrophonium
(anticholinesterase)
extremely short acting
Edrophonium?
anticholinesterase; extremely short acting
use for dx myasthenia gravis
Physostigmine?
anticholinesterase
use for glaucoma (crosses BBB)
use for atropine overdose
tx for atropine OD?
physostigmine
anticholinesterase useful in glauchoma?
Physostigmine (crosses BBB)
Echothiophate
echothiophate?
anticholinesterase
use for glaucoma
anticholinesterase for Alzheimer's?
Donepezil
Donepizil?
anticholinesterase
used for Alzheimer's
what are potential complications of cholinomimetic agents?
COPD exacerbation
asthma
peptic ulcers
cholinesterase inhibitor poisoning? antidote?
antidoe - atropine + pralidoxime (regenerates active AChE)

DUMBBELSS
diarrhea
urination
miosis
bronchospasm
bradycardia
Excitation - skeletal mm, CNS
Lacrimation
Sweating
Salivation
atropine?
muscarinic antagonist
used for eye
homatropine?
muscarinic antagonist
used for eye
tropicamide?
muscarinic antagonist
used for eye
benztropine?
muscarinic antagonist
used for Parkinson's
scopolamine?
muscarinic antagonist
used for motion sickness; side effects from tx of myasthenia gravis
ipratropium?
muscarinic antagonist
used for asthma, COPD
muscarinic antagonist for asthma / COPD?
Ipratropium
(I PRAy i can breathe soon)
oxybutinin?
muscarinic antagonist
used for Genitourinary
(reduce urgency in cystitis; reduce bladder spasms)
glycopyrrolate?
muscarinic antagonist
used for Genitourinary
(reduce urgency in cystitis; reduce bladder spasms)
methscopolamine?
muscarinic antagonist
used for peptic ulcer treatment
pirenzepine?
muscarinic antagonist
used for peptic ulcer tx
propantheline?
muscarinic antagonist
used for peptic ulcer tx
increase temp, less sweating, rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation?
atropine toxicity; in elderly can cause acute angle-closure glaucoma, urinary retention (if have prostatic hyperplasia) & hyperthermia in infants

"Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter"
indirect sympathomimetics?
amphetamine - releases stored catecholamines
ephedrine - releases stored catecholamines
cocaine - uptake inhibitor
epinephrine?
alpha1-----3+
alpha2-----3+
beta1-------4+
beta 2------4+
D1-----------0

used for anaphylaxis, open angle glaucoma, asthma, hypotension
norepinephrine?
alpha1-----4+
alpha2-----4+
beta1-------2+
beta 2------0
D1-----------0

used for Hypotension (but decreases renal perfusion)
isoproterenol?
alpha1-----0
alpha2-----0
beta1-------4+
beta 2------4+
D1-----------0

used for AV block (rare)
dopamine?
alpha1-----4+ (at high doses)
alpha2-----4+ (at high doses)
beta1-------4+ (at medium doses)
beta 2------2+ (at medium doses)
D1-----------+ (at low dose)

used for shock (renal perfusion), heart failure
inotropic & chronotropic

D1 > beta > alpha
dobutamine?
alpha1-----1+
alpha2-----1+
beta1-------4+
beta 2------1+
D1-----------0

heart failure, cardiac stress testing
inotropic and chronotropic
phenylephrine?
alpha1-----++++
alpha2-----++
beta1-------0
beta 2------0
D1-----------0

used for pupillary dilation, to induce vasoconstriction, for nasal decongestion
metaproterenol, albuterol, salmeterol, terbutaline?
albuterol, metaproterenol, terbutaline

alpha1-----0
alpha2-----0
beta1-------++
beta 2------++++
D1-----------0

MAST
acute asthma - Metaproterenol and Albuterol
long term tx - Salmeterol
reduce premature uterine contractions - Terbutaline
what to use to reduce premature uterine contractions?
terbutaline, ritodrine
what to use for acute asthma? long term tx?
acute - metaproterenol and albuterol
long term - salmeterol
indirect sympathomimetics?
amphetamine - releases stored catecholamines
ephedrine - releases stored catecholamines
cocaine - uptake inhibitor
epinephrine?
alpha1-----3+
alpha2-----3+
beta1-------4+
beta 2------4+
D1-----------0

used for anaphylaxis, open angle glaucoma, asthma, hypotension
norepinephrine?
alpha1-----4+
alpha2-----4+
beta1-------2+
beta 2------0
D1-----------0

used for Hypotension (but decreases renal perfusion)
isoproterenol?
alpha1-----0
alpha2-----0
beta1-------4+
beta 2------4+
D1-----------0

used for AV block (rare)
dopamine?
alpha1-----4+ (at high doses)
alpha2-----4+ (at high doses)
beta1-------4+ (at medium doses)
beta 2------2+ (at medium doses)
D1-----------+ (at low dose)

used for shock (renal perfusion), heart failure
inotropic & chronotropic

D1 > beta > alpha
dobutamine?
alpha1-----1+
alpha2-----1+
beta1-------4+
beta 2------1+
D1-----------0

heart failure, cardiac stress testing
inotropic and chronotropic
phenylephrine?
alpha1-----++++
alpha2-----++
beta1-------0
beta 2------0
D1-----------0

used for pupillary dilation, to induce vasoconstriction, for nasal decongestion
metaproterenol, albuterol, salmeterol, terbutaline?
albuterol, metaproterenol, terbutaline

alpha1-----0
alpha2-----0
beta1-------++
beta 2------++++
D1-----------0

MAST
acute asthma - Metaproterenol and Albuterol
long term tx - Salmeterol
reduce premature uterine contractions - Terbutaline
what to use to reduce premature uterine contractions?
terbutaline, ritodrine
what to use for acute asthma? long term tx?
acute - metaproterenol and albuterol
long term - salmeterol
ritodrine?
alpha1-----0
alpha2-----0
beta1-------0
beta 2------4+
D1-----------0

reduces premature uterine contractions
what happens to HR w/NE? Isoproterenol?
NE - reflex bradycardia (b/c casues increase in BP via vasoconstriction; alpha > beta)

Isoproterenol - reflex tachycardia; causes decreased BP from beta > alpha (vasodilation)
clonidine?
central acting alpha-2 agonist
decrease central adrenergic outflow

use to tx HTN, espeically w/renal dz - no decrease in blood flow to kidney
alpha-methyldopa?
central acting alpha-2 agonist
decrease adrenergic outflow

use for tx HTN especially w/renal dz (doesn't decrease blood flow to kidney)
good way to tx HTN in setting of renal dz?
central alpha-2 agonists (clonididne, alpha-methyldopa)
doesn't decrease flow to kidneys
phenoxybenzamine?
nonselective alpha adrenergic blocker
Irreversible
use for pheochromocytoma before removal b/c high levels of catecholimens won't overcome irreversible block
(also long t-half)
phentolamine?
nonselective alpha blocker
used for pts on MAO inhibitors who eat tyramine containing foods
toxicity of nonselective alpha blockers?
orthostatic hypotension
reflexive tachycardia
doxazosin, terazosin, prazosin?
alpha-1 selective alpha blockers
tx HTN, urinary retention in BPH
"1st dose orthostatic HTN, dizziness, headache"
mirtazapine?
alpha-2 selective alpha blocker
use for tx of depression
tox: sedation, increased cholesterol, increased appetite
Beta-blockers used for?
HTN
Angina pectoris
MI
SVT
CHF
Glaucoma
use of beta-blockers in HTN?
decrease CO
decrease renin secrection (receptors on JGA)
use of beta-blockers in Angina pectoris?
decrease HR & contractility
decreases O2 consumption
use of beta-blockers in MI?
decrease mortality
use of beta-blockers in SVT? which ones?
class II anti-arrythmics
decrease AV conduction velocity (region between P & QRS - PR interval)
-propranolol, esmolol
use of beta-blockers in CHF?
slow progression of chronic failure
use of beta-blockers in Glaucoma? which one?
decrease secretion of aqueous humor
Timolol
impotence, bradycardia, AV block, CHF, sedation, sleep alterations are toxicity of? use with caution in what populations?
beta blocker toxicity
-also asthma exacerbation, "CV & CNS adverse effects"

use w/caution in diabetics
Acebutol
Betaxolol
Esmolol
Atenolol
Metoprolol
A-BEAM of beta-1 selective blockers
-useful for comorbid pulmonary dz

special characteristics
-slow acting - esmolol
-partial agonist - acebutol
Pindolol
Nadolol
Timolol
Propranolol
Nonselective beta blockers

"Please Try Not being Picky"
Labetalol
Carvedilol
nonselective alpha & beta agonists - vasodilatory
Pindolol
Acebutol
partial beta agonists