PHA453 Cardio II Exam 1 Drugs

sympatholytic:

displaces NT from storage vesicles inside the terminal --> less NT release

sympathomimetic:

displaces catecholamine NT vesicle from cytoplasmic pool --> more NT into cleft

can cause adrenergic crisis

sympathomimetic:

competes for NET
displaces NT vesicle from cytoplasmic pool
--> more monoamine NT into the cleft

sympathomimetic:

direct beta- and alpha-receptor stimulation

displaces NT vesicle from cytoplasmic pool --> more NT into cleft

Parasympathomimetic:

reversible competitive AChE-I

diagnostic for myasthenia crisis / cholinergic crisis

Parasympathomimetic:

reversible competitive AChE-I

tx for Alzheimer's

hepatotoxicity issues

parasympathomimetic:

competitive substrate AChE-I

tx for glaucoma

parasympathomimetic:

competitive substrate AChE-I

antidote to anticholinergic poisoning

parasympathomimetic:

competitive substrate AChE-I

tx for myasthenia gravis

parasympathomimetic:

competitive substrate AChE-I

tx for myasthenia gravis

parasympathomimetic:

competitive substrate AChE-I

tx for Alzheimer's

parasympathomimetic:

competitive substrate AChE-I

tx for Alzheimer's

parasympathomimetic:

competitive substrate AChE-I

tx for Alzheimer's

sympathomimetic:

non-selective MAOI (-A and -B)

sympathomimetic:

non-selective MAOI (-A and -B)

sympathomimetic:

selective MAOI (-B)

sympathomimetic:

selective MAOI (-B)

avoids dietary restriction
higher bioavailability than oral

parasympathomimetic:

cholinergic receptor agonist

injected into the eye --> rapid miosis

parasympathomimetic:

muscarinic receptor agonist

tx for post-op/-partum urinary retention; and gastroparesis

fewer CV effects than rest of class

parasympathomimetic:

muscarinic receptor agonist
--> salivary stimulation

tx for Sjogren's syndrome, dry mouth

parasympathomimetic:

muscarinic receptor agonist
--> salivary stimulation

tx for Sjogren's syndrome

parasympathomimetic:

muscarinic receptor agonist

miotic
tx for glaucoma, post eye surgery

short duration: dosed ~QID

parasympatholytic:

competitive cholinergic receptor antagonist

long-acting
dose-related predictable anticholinergic adverse effects

parasympatholytic:

cholinergic receptor antagonist

tx for nausea

crosses blood-brain barrier -->
blocks M3 in vestibular apparatus;
drowsiness

parasympatholytic:

cholinergic receptor antagonist
blocks M3 in bronchial smooth muscle --> dilation

tx for pulmonary disorders

parasympatholytic:

cholinergic receptor antagonist
blocks M3 in bronchial smooth muscle --> dilation

tx for pulmonary disorders

parasympatholytic:

cholinergic receptor antagonist
blocks M3 in striatal pathway --> reduced tremor/movement

tx for Parkinson's; EPS

parasympatholytic:

cholinergic receptor antagonist
blocks M3 in striatal pathway --> reduced tremor/movement

tx for Parkinson's; EPS

statin: HMG CoA reductase inhibitor
10mg ; 20mg ; 40mg
LDL: 34% (lowrange)
prodrug
crosses BBB
CYP3A4

statin: HMG CoA reductase inhibitor
20mg ; 40mg
LDL: 41% (midrange)
prodrug
crosses BBB
CYP3A4

statin: HMG CoA reductase inhibitor
10mg ; 20mg ; 30mg
LDL: 50% (upper-range)
lesser crossing of BBB
CYP3A4

statin: HMG CoA reductase inhibitor
20mg ; 40mg
LDL: 34% (lowrange)
does NOT cross BBB
NOT highly protein-bound
sulfonation

statin: HMG CoA reductase inhibitor
80mg
LDL: 17% (lowest)
lesser crossing of BBB
CYP2C9

statin: HMG CoA reductase inhibitor
5mg ; 10mg ; 20mg ; 40mg
LDL: 55% (highest)
does NOT cross BBB
CYP2C9

statin: HMG CoA reductase inhibitor
1mg ; 2mg ; 4mg
LDL: 55% (8mg)
crosses BBB
CYP2C9

bile acid sequestering resin

one quaternary ammonium group on divinylbeneze and polystyrene

bile acid sequestering resin

several secondary and tertiary amine groups (no quaternary amines): variously charged depending on pH

bile acid sequestering resin

most effective in class: two quaternary amines, plus several primary and secondary amines

cholesterol absorption inhibitor
10mg
LDL: 14-25%
VLDL: 7-9%
no effect on HDL

produg -- altered in liver, resecreted in bile

cholesterol absorption inhibitor / statin
10/10mg ; 10/20mg ; 10/40mg ; 10/80mg

possibly not more effective than simvastatin alone

nicotinic acid (vitamin B3)
500mg ; 750mg ; 1000mg

LDL: 20-30%
VLDL: 34-45%
HDL: 30-40% (most effective of all antihyperlipidemics)

main AEs: flushing, hepatotoxicity, GI upset, hyperglycemia, hyperuricemia

nicotinic acid / statin

nicotinic acid / statin

fibric acid derivative: activates peroxisome proliferator-activated receptor alpha
prodrug

metabolite interferes w/ statin metabolism

fibric acid derivative: activates peroxisome proliferator-activated receptor alpha

less interference w/ statin metabolism than gemfibrozil

fibric acid derivative: activates peroxisome proliferator-activated receptor alpha

less interference w/ statin metabolism than gemfibrozil

fibric acid derivative: activates peroxisome proliferator-activated receptor alpha

fibric acid: activates peroxisome proliferator-activated receptor alpha

less interference w/ statin metabolism than fenofibrate

non-dihydropyridine Ca++ channel blocker

DD intrxn w/ β-blocker: bradycardia, AV block

non-dihydropyridine Ca++ channel blocker

DD intrxn w/ β-blocker: bradycardia, AV block

dihydropyridine Ca++ channel blocker
1st gen

worst in class for reflex tachycardia

dihydropyridine Ca++ channel blocker
2nd gen

dihydropyridine Ca++ channel blocker
3rd gen

dihydropyridine Ca++ channel blocker
2nd gen

dihydropyridine Ca++ channel blocker
3rd gen

dihydropyridine Ca++ channel blocker
2nd gen

dihydropyridine Ca++ channel blocker
2nd gen

dihydropyridine Ca++ channel blocker
2nd gen

beta-blocker
non-selective

MSA (aka local anesthetic effect) - however dose required for MSA is higher than dose for treating arrhythmia

beta-blocker
non-selective

beta-blocker
non-selective

beta-blocker
non-selective

ISA

beta-blocker
non-selective

ISA

beta-blocker
β1 selective

beta-blocker
β1 selective

beta-blocker
β1 selective

beta-blocker
β1 selective

ISA
MSA (aka local anesthetic effect)

beta-blocker
β1 selective

beta-blocker
β1 selective

beta-blocker
β1 selective

rapid onset, short half-life
for use in hospital setting

beta-blocker
β1 preferential

"3rd generation"
increases NO in periphery --> vasodilation

beta-blocker
β1 β2 α1

ISA
3rd generation
periphery, coronary vasodilation
reverses peripheral vascular remodeling

beta-blocker
β1 β2 α1

3rd generation
periphery, coronary vasodilation
reverses peripheral vascular remodeling

β-blocker
non-selective

Ca++ N-channel blocker

from a snail
1000x more powerful than morphine

β-blocker
non-selective
ophthalmic
ISA

β-blocker
non-selective
ophthalmic

β-blocker
non-selective
ophthalmic

β-blocker
β1 selective

Funny-channel (HCN) blocker
reduces chronotropy w/o affecting QT interval

Late sodium-channel blocker
--> reduces sodium overload
--> reduces calcium overload
--> reduces abnormal contraction
Tx for classical angina

Thought to be a partial fatty acid metabolism inhibitor, but is not

May also inhibit K+ outward current --> prolong QT interval

irreversible COX inhibitor
low-dose selective for COX-1

blocks formation of TxA2 (but not PgI2 so much)
reduces platelet aggregation by 20-30%
low-doses remain in portal circulation

anti-platelets
inhibits adenosine deaminase (major)
inhibits PDE 5 (minor)
+
irreversible COX inhibitor
low-dose selective for COX-1

anti-platelet
inhibits adenosine deaminase (major)
inhibits PDE 5 (minor)

anti-platelet
inhibits PDE 3
Tx for intermittent claudication
inhibits platelet aggregation 10 to 30x greater than low dose aspirin

fibric acid derivative

prodrug

No longer marketed - gall bladder and cardiovascular problems

Ca2+channel blocker
2nd gen

nitrate
Tx for angina

nitrate

more stable than mononitrate

antiplatelet
ADP-receptor inhibitor

SE: headache, diarrhea, bleeding, increased cholesterol