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70 Cards in this Set
- Front
- Back
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Direct Cholinergic Agonists
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metacholine
carbachol bethanechol pilocarpine (partial agonist) |
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Anticholinesterase categories
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1) simple AchE competitive inhibitor
2) competitive AchE substrate - slowly hydrolyzed - carbamates 3) Irreversible substrate - organophosphates |
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Competitive AchE antagonist
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edrophonium
donepezil galantamine |
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Competitive AchE substrate
-slowly hydrolyzed -carbamate |
Physostigmine
neostigmine democurium pyridostigmine rivastigmine |
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Organophosphate
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echothiophate
parathion/malathion sarin/soman |
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Muscarine poisoning
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salivation/lacrim
nausea headache bronchospasm bradycardia/ hypotension shock no muscle weakness REVERSE W. ATROPINE |
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AchE intoxication
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mix of muscarinic + nicotinic effects + CNS
can have coma, convulsion |
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Anti-Muscarinic
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atropine
scopolamine ipratropium propantheline oxybutynin tolterodine tropicamide |
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-chol
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cholinergic agonist
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-igmine
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reversible AchE
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Ganglionic blocker
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depol: nicotine
non depol: mecamylamine, hexamethonium, TEA |
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Anti-muscarinic effect
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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 |
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Alternatives to anti-muscarinics
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anti-histamine (diphenhydramine)
anti-depressants phenothiazine antipsychotics NMJ blockers alpha agonist -- short mydriasis |
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NMJ blocker types
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depolarizing AchR agonist
nondepolarizing AchR antagonist |
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Succinylcholine
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Depolarizing competitive AchR agonist
NMJ blocker |
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Nondepolarizing competitive nAchR antagonist
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Mivacurium
Rocuronium Vecuronium Cisatracurium Atracurium Pancuronium Pipecuronium Doxacurium Metocurine Tubocurarine |
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alpha antagonist
non selective (alpha 1 and 2) REVERSIBLE |
phentolamine
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alpha antagonist
non selective (alpha 1 and 2) irreversible IRREVERSIBLE |
phenoxybenzamine
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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) |
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PHENTOLAMINE
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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) |
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PHENOXYBENZAMINE
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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 |
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alpha antagonists selective
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prazosin
terazosin doxazosin tamsulosin |
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selective alpha antago MOA
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-blocks vasoconstriction
decrease TPR and BP -doesnt block alpha 2 so no reflex tachy or change in CO |
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alpha 1 antagonists
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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 |
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Adrenergic neuronal blockers
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metyrosine
reserpine guanethidine guanadrel |
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metyrosine
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FALSE NT
compete w. tyr hydroxylase NOT USED |
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RESERPINE
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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 |
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GUANETHIDINE
GUANADREL |
DISPLACEMENT
hydrolyze NE-ATP in vesicles IV -delayed onset EMERGENCY HTN :O( severe diarrhea tolerance -dont enter CNS |
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block alpha 2
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yohimbe (research)
tolazoline (NS) |
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block alpha and beta
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labetalol
carvedilol |
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catecholamines
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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) |
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non-catecholamines
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phenylephrine, ephedrine, amphetamine
metab: liver p450 longer acting better CNS ok oral |
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epi use
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asthma
anaphylactic shock wide angle glaucoma (bc vasoconstricting and mydriasis) epitaxis cardiac arrest w. LOCAL ANESTHETIC to prolong axn |
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NE use
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shock
hypotensive emergency decongestant |
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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 |
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isop use
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COPD - inhale
cardiac arrest |
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clonidine
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alpha 2 agonist (cNS)
decrase symp ANTI - HTN |
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phenylephrine
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alpha agonist (1 and 2)
DECONGESTANT -vasoconstricts dont use if you have heart problems! |
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dobutamine
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beta 1 agonist
cardiac arrest shock |
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dopamine
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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 |
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Beta 2 agonists
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salmeterol (safest - least beta 1)
terbutaline albuterol retrodine (least safe, most beta 1) |
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safest beta 2 agonist
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salmeterol
(least beta 1) |
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least safe beta 2 agonist
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retrodine
(most beta 1) |
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beta 2 agonists
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asthma
AE (if not selective for beta2)) tachycardia, palpitation |
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tyramine
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indirect adrenergic agonist
NOT USED |
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EPHEDRINE
psuedophedrine |
NE like - more effect on receptors - direct
DECONGESTANT can take oral |
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AMPHETAMINES
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benzadrine --> diet pills, affect CNS get addicted)
dextrodine methamphetamine |
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amphetamines
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Epi like - more on NE release
NARCOLEPSY RITALIN can take oral |
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methylphenidate
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hyperactivity (but causes CV effects)
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Beta blockers
selective |
A-M
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beta blockers
nonselective |
N-S
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beta blocker use
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EVERY BETA BLOCKER USED FOR:
HTN angina hyperthyroidism (causes tachy) |
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acebutalol
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active metabolite:
acetylated ISA -some MSA -some |
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atenelol
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#1 FOR HYPERTENSION
lowest lipid solubility NO CNS EFFECTS - NO INSOMNIA |
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ESMOLOL
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IV
anti-arrythmic (even tho no MSA) |
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METOPROLOL
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MSA
-some |
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Naldolol
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long half life - 24 hrs
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Pindolol
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HIGH ISA --> good for CHF
Some MSA |
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Propranalol
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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 |
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Timolol
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#1 for glaucoma CHRONIC Tx
(decreases aq humor production - beta 2)) (use pilocarpine for acute tx) |
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Sotalol
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anti-arrythmic ONLY
(atrial fibrillation) |
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Labetalol/Carvedilol
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mixed (affect beta1,beta2,alpha1)
-dont cause cold fingers (block alpha 1) carvedilol = NS - antiarrythmic labetelol - # 1 for HTN in ER |
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Beta blockers adverse rxns
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CNS - insomnia, sedation
(propranalol, metoprolol) Cardiac - bradycardia, hypotension, arrest (if NS) - causes cold extremities - block beta2 pulm (ns) - bronchoconstriction biochem (NS) - hypoglycemia |
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betaxalol
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longest activing selective
HTN |
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carvedilol
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NS - alpha and beta
anti-arrythmic |
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beta blocker contraindications
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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) |
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cocaine, tricyclic antidepressants
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inhibit ne reuptake
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hemicholinium
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inhibit choline/Na cotransporter into cell
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vesamicol
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inhibits packaging Ach into vesicles
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botulinum toxin
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inhibits vesicle/membrane fusion and exocytosis of Ach
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