Pharm Flashcards
Sympathomimetics
Norepinephrine - released from postG SNS endings into blood
epinephrine
isoproterenol - synthetic NE analogue
Sympatholytics
B-blockers
A-blockers
parasympathomimetics
pilocarpine - direct receptor agonist
cholinesterase - indirectly (inhibits AChE)
Parasympatholytics
atropine - muscarinic blocker
Class I - Na+ channel blockers
prolong the effective refractory period
increases threshold of excitability
decreases conduction velocity
IA - procainamide
IB - lidocaine
IC - flecainide
Class II - B-blockers
suppress positive ionotropic and chronotropic effects
reduce rate and contractility of the heart
Non-Selective - propranolol (do not give to asthmatics)
Cardiac Selective - -olols
Class III - K+ channel blockers
block K+ channels and prolong repolarization
amiodarone
Class IV - Ca2+ channel blockers
decrease slope of phase 4 AP
prolongs ERP
slows conduction (specifically AV node)
USED TO CONTROL SUPRAVENTRICULAR ARRYTHMIAS
verapamil, diltiazem
Class V
digoxin - increases intracellular Ca2+; and increases contractile force
atropine - mus blocker
epi - increase HR
adenosine - prevalent on atrial myocytes in SA and AV nodes; inhibits adenylyl cyclase; decreases conduction velocity; prolonged refractory period and decreased AV node automaticity
drug of choice for paroxysmal supraventricular tachycardia
phase I rxns
Generally makes less toxic and/or more water-soluble
reductions hydrolysis oxidation microsomal CYP450 FAD-containing monooxygenase (NADPH cofactor and FAD, to catalyse oxidation) non-microsomal MAO Alcohol Dehydrogenase
Phase II rxns
Generally conjugation rxns to make more water-soluble for excretion
Glucuronide Conjugation Glutathione Conjugation Acetylation Sulfate Conjugation Glycine Conjugation Methylation
First Order kinetics
Metabolism
Rate of metabolism of the drug; CONSTANT FRACTION per unit time; occurs at lower doses
Zero Order Kinetics
Rate of metabolism of the drug; CONSTANT AMOUNT per unit time; occurs at higher doses
CYP family
inducers - promote drug breakdown; increase dose
inhibit - inhibits drug breakdown; reduce dose