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70 Cards in this Set

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Direct Cholinergic Agonists
metacholine

carbachol

bethanechol

pilocarpine (partial agonist)
Anticholinesterase categories
1) simple AchE competitive inhibitor

2) competitive AchE substrate - slowly hydrolyzed - carbamates

3) Irreversible substrate - organophosphates
Competitive AchE antagonist
edrophonium

donepezil

galantamine
Competitive AchE substrate

-slowly hydrolyzed

-carbamate
Physostigmine

neostigmine

democurium

pyridostigmine

rivastigmine
Organophosphate
echothiophate

parathion/malathion

sarin/soman
Muscarine poisoning
salivation/lacrim

nausea

headache

bronchospasm

bradycardia/ hypotension

shock

no muscle weakness

REVERSE W. ATROPINE
AchE intoxication
mix of muscarinic + nicotinic effects + CNS

can have coma, convulsion
Anti-Muscarinic
atropine

scopolamine

ipratropium

propantheline

oxybutynin

tolterodine

tropicamide
-chol
cholinergic agonist
-igmine
reversible AchE
Ganglionic blocker
depol: nicotine

non depol:
mecamylamine, hexamethonium, TEA
Anti-muscarinic effect
DRY as a bone - xerostomia
RED as a beet - cut. vasodil
HOT as a hare - no sweat
BLIND as a bat - mydrias
MAD as a hatter - CNS
Alternatives to anti-muscarinics
anti-histamine (diphenhydramine)
anti-depressants
phenothiazine antipsychotics
NMJ blockers

alpha agonist -- short mydriasis
NMJ blocker types
depolarizing AchR agonist

nondepolarizing AchR antagonist
Succinylcholine
Depolarizing competitive AchR agonist

NMJ blocker
Nondepolarizing competitive nAchR antagonist
Mivacurium
Rocuronium
Vecuronium
Cisatracurium
Atracurium
Pancuronium
Pipecuronium
Doxacurium
Metocurine
Tubocurarine
alpha antagonist
non selective (alpha 1 and 2)

REVERSIBLE
phentolamine
alpha antagonist
non selective (alpha 1 and 2)
irreversible

IRREVERSIBLE
phenoxybenzamine
alpha antagonist - nonselective

MOA
-block vasoconstriction
-decrease TPR and BP
-cause reflex tachy

-block alpha 2 so increase E and NE from chromaffin (tachy, increase CO)
PHENTOLAMINE
NS ALPHA ANTAG
REVERSIBLE

IV
2-3 hrs

USE:
PHECHROMOCYT (pre-op)
---avoid hypertensive crisis

-block reflex vasoconstriction in shock
(VASODILATOR)

other:
-histamine release (H2 agonistic) --> increase acid and pepsin

-cholinergic effect (GI motil)


AE:
tachycardia
angina
arrythmias
peptic ulcer disease
orthostatic hypotension

REVERSE WITH PHENYLEPHRINE (ALPHA AGONIST)
PHENOXYBENZAMINE
NS ALPHA ANTAG
IRREVERSIBLE

IV/PO DAYS

USE

Phechromocyt (pre-op and long term) avoid HTN crisis

Raynauds (periph vascular)

AE:
tachy
SEDATION
orthostatic hypotension
alpha antagonists selective
prazosin
terazosin
doxazosin
tamsulosin
selective alpha antago MOA
-blocks vasoconstriction
decrease TPR and BP

-doesnt block alpha 2 so no reflex tachy or change in CO
alpha 1 antagonists
PO
long duration: 1/day
---longest = doxazosin

metab in liver

anti-hypertension

BPH (tamsulosin, terazosin)

also:
decrease cholesterol, triglycerides, increase HDL

BAD:
first dose syncope
Adrenergic neuronal blockers
metyrosine
reserpine
guanethidine
guanadrel
metyrosine
FALSE NT

compete w. tyr hydroxylase

NOT USED
RESERPINE
DEPLETION

blocks packing of NE into vesicles by inhibiting Mg dependent Na/K ATPase

PO IM IV
-delayed onset (gradual depletion)
-long duration of action

ANTI-HTN
-decrease symp

:O(
DEPRESSION
GUANETHIDINE
GUANADREL
DISPLACEMENT

hydrolyze NE-ATP in vesicles

IV
-delayed onset

EMERGENCY HTN

:O(
severe diarrhea
tolerance

-dont enter CNS
block alpha 2
yohimbe (research)

tolazoline (NS)
block alpha and beta
labetalol
carvedilol
catecholamines
epi, ne, isop, da, dobutamine

high potency

rapid onset, short acting

poor CNS absorp

cant take oral (have 2 OH groups)
epi can be IM, SQ

metab:
COMT, MAO --> VMA
(measure in urine)
non-catecholamines
phenylephrine, ephedrine, amphetamine

metab:
liver p450
longer acting
better CNS
ok oral
epi use
asthma

anaphylactic shock

wide angle glaucoma (bc vasoconstricting and mydriasis)

epitaxis

cardiac arrest

w. LOCAL ANESTHETIC to prolong axn
NE use
shock

hypotensive emergency

decongestant
epi, ne, isop

AE
contraindic
EXCESS

seizures

high arterial pressures

cerebrovasc hemorr

ventricular arrythmias

Contraindications

HTN
hyperthyroid
ischemic heart disease
cerebrovasc insuff
brain damage
narrow angle glaucoma (bc increase iop)

excess heart stimulation and vasoconstriction can --> pulmonary edema and death
isop use
COPD - inhale

cardiac arrest
clonidine
alpha 2 agonist (cNS)

decrase symp

ANTI - HTN
phenylephrine
alpha agonist (1 and 2)

DECONGESTANT

-vasoconstricts

dont use if you have heart problems!
dobutamine
beta 1 agonist

cardiac arrest

shock
dopamine
low dose: DA effects
vasodil--> increased urine output

high dose: alpha1 and beta1 effects (heart and vasoconstriction)

MI DRUG

ER shock - increase CO, maintain perfusion to kidney by vasodilation of renal vasc
Beta 2 agonists
salmeterol (safest - least beta 1)
terbutaline
albuterol
retrodine (least safe, most beta 1)
safest beta 2 agonist
salmeterol
(least beta 1)
least safe beta 2 agonist
retrodine
(most beta 1)
beta 2 agonists
asthma

AE (if not selective for beta2))
tachycardia, palpitation
tyramine
indirect adrenergic agonist

NOT USED
EPHEDRINE
psuedophedrine
NE like - more effect on receptors - direct

DECONGESTANT

can take oral
AMPHETAMINES
benzadrine --> diet pills, affect CNS get addicted)

dextrodine
methamphetamine
amphetamines
Epi like - more on NE release

NARCOLEPSY
RITALIN

can take oral
methylphenidate
hyperactivity (but causes CV effects)
Beta blockers

selective
A-M
beta blockers

nonselective
N-S
beta blocker use
EVERY BETA BLOCKER USED FOR:

HTN

angina

hyperthyroidism (causes tachy)
acebutalol
active metabolite:

acetylated

ISA
-some

MSA
-some
atenelol
#1 FOR HYPERTENSION

lowest lipid solubility

NO CNS EFFECTS - NO INSOMNIA
ESMOLOL
IV

anti-arrythmic
(even tho no MSA)
METOPROLOL
MSA
-some
Naldolol
long half life - 24 hrs
Pindolol
HIGH ISA --> good for CHF
Some MSA
Propranalol
HIGHEST LIPID SOLUBILITY --> INSOMNIA

HIGHEST PLASMA BINDING

HIGH MSA

anti-arrythmic
MSA - mouth gets numb
migraine - vasoconstriction of dilated vessesl

METABOLITE: OH propranolol(by p450)

PO / IN

:O(
insomnia
Timolol
#1 for glaucoma CHRONIC Tx
(decreases aq humor production - beta 2))

(use pilocarpine for acute tx)
Sotalol
anti-arrythmic ONLY
(atrial fibrillation)
Labetalol/Carvedilol
mixed (affect beta1,beta2,alpha1)

-dont cause cold fingers (block alpha 1)

carvedilol = NS - antiarrythmic

labetelol -
# 1 for HTN in ER
Beta blockers adverse rxns
CNS - insomnia, sedation
(propranalol, metoprolol)

Cardiac - bradycardia, hypotension, arrest

(if NS) - causes cold extremities - block beta2

pulm (ns) - bronchoconstriction

biochem (NS) - hypoglycemia
betaxalol
longest activing selective

HTN
carvedilol
NS - alpha and beta

anti-arrythmic
beta blocker contraindications
CHF (except pindolol)

asthma
(cant use NS) bc causes bronchoconstriction since blocking beta 2

diabetes

(cant use NS because it blocks beta 2 and decreases glycogenolysis)
cocaine, tricyclic antidepressants
inhibit ne reuptake
hemicholinium
inhibit choline/Na cotransporter into cell
vesamicol
inhibits packaging Ach into vesicles
botulinum toxin
inhibits vesicle/membrane fusion and exocytosis of Ach