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Flashcards in Rx Deck (117):
1

epinephrine

Class: Adrenergics
catecholamines
A1&A2&B1&B2&B3 agonist
sympathetic stimulation = inc heart rate, contractility, BP and CO
low doses: B preferred
uses: cardiac arrest, cardiogenic shock, severe hypotension, anaphylaxis, respiratory distress, urticaria, keep anesthetic "local"
side effect: hyperglycemic effect, tachycardia, arrhythmia, MI
~adrenaline

2

norepinephrine

Class: Adrenergics
catecholamines
A1&A2>B1 agonist
stimulates peripheral vasoconstriction and inc BP
use: shock, severe hyoptension
side effect: MI due to increased cardiac work

3

isoproterenol

Class: Adrenergics
catecholamines
B1 & B2 agonist
inc HR, contractility and cardiac output
use: bradycardia, asthma, bronchitis, and emphysema.
side effects: tachycardia, MI

4

dopamine

Class: Adrenergics
catecholamines
low dose: D1&D2&B1 agonist
high dose: A1&A2 agonist (act as vasopressor)
increase contractility and HR
use: cardiogenic shock, CHF
*causes renal vasodialtion
side effect: arrhythmias

5

dobutamine

Class: Adrenergics
catecholamines
B1 agonist
uses: cardiogenic shock, congestive heart failure
(increases contractility w/o increase HR) increases cardiac output
side effect: arrhythmias, hypotension

6

phenylephrine

adrenergic Agonists/ sympathomimetics
direct agents
A1>A2
vasopressor
uses: rhinitis, decongestion, SVT, hypotension, shock
*big vasoconstriction= increase systemic resistance= inc BP=vagal stimulation= slows heart rate
side effect: rebound mucous swelling

7

midodrine

Agonists/ sympathomimetics
direct agents
A1
uses: hypotension, retinal exams (dilates pupils)

8

brimonidine    

presynaptic anti-adrenergic
direct, Agonist A2
causes dec NE and suppresses sympathetic
uses: glaucoma (decreases aqueous humor formation)

9

clonidine

presynaptic anti-adrenergic
direct, Agonist A2
causes dec NE and suppresses sympathetic
uses: HTN, (inhibits sympathetic outflow)
side effect: sedation
(CNS active)

10

oxymetazoline (Afrin)

Agonists/ sympathomimetics
direct agents
A1 & A2
use: decongestion

11

albuterol/salmeterol/terbutaline (proventil/ventolin)

adrenergic Agonists/ sympathomimetics
direct agents
B2
causes bronchiodilation
use: asthma, COPD
side effects: tachycardia, tremor

12

fenoldopam 

adrenergic Agonists/ sympathomimetics
direct agents
D1
use: severe HTN
rapid renal and splanchnic vasodilating effects

13

amphetamine

adrenergic Agonists/ sympathomimetics
Indirect acting agents
mechanism: inhibits MAO, releases endogenous NE from storage vesicles= inc NE binding to adrenergic receptors
CNS excitation (can cross BBB)
stimulant: increases heart rate and blood pressure and decreases appetite

14

ephedrine

adrenergic Agonists/ sympathomimetics
Mixed agent
Indirect acting: inc NE release from neuron and binding to adrenergic receptor
DIRECTLY stimulates A1&B2
use: asthma, nasal decongestion, hypotension
side effect: HTN

15

phenoxybenzamine

adrenergic Antagonists/ adrenergic receptor blockers
A1 & A2,
noncompetitive, binds irreversibly
use: HTN
side effect: reflex tachycardia, increased insulin

16

phentolamine

Antagonists/ adrenergic receptor blockers
A1 & A2, competitive
causes: dilation of smooth muscle and dec BP
Uses: HTN
side effects: reflex tachycardia and arrhythmias

17

prazosin 

Antagonists/ adrenergic receptor blockers
A1 selective
competitive
causes blood vessel vasodilation and dec BP
use: HTN (does not cause tachycardia)
side effect: hypotension and dizziness
"minipress"

18

tamsulosin

Antagonists/ adrenergic receptor blockers
A1a selective (GU tract)
use: benign prostatic hypertrophy and bladder obstruction
side effect: floppy iris syndrome

19

terazosin

Antagonists/ adrenergic receptor blockers
A1a selective (GU tract)
use: benign prostatic hypertrophy, HTN

20

pindolol

Antagonists/ adrenergic receptor blockers
B1 & B2, weak
intrinsic sympathomimetic activity (less effect on resting HR)
use: HTN
side effect: bronchoconstriction

21

propranolol

Antagonists/ adrenergic receptor blockers,
Antiarrhythmic: class 2
B1 & B2, strong
effect: prolongs AV conduct and refract; decreases HR and contractility
use: angina pectoris, HTN, MI, SVT, ventricular arrhythmia, tachycardia, Afib, Aflutter
side effect: bronchoconstriction, heart failure

22

metoprolol

Antagonists/ adrenergic receptor blockers
Antiarrhythmic: class 2
B1 selective
(-) inotropy, (-) chronotropy
use: HTN, MI, SVT, CP, tachycardias, IHD, CHF
less likely to cause bronchoconstriction
side effect: bradycardia, enters brain (CNS sedation)

23

labetalol

Antagonists/ adrenergic receptor blockers
causes vasodilation
Mixed: A1 & B
use: HTN, angina pectoris, CHF
side effects: hypotension, fatigue, bradycardia

24

carvedilol

Antagonists/ adrenergic receptor blockers
Mixed: A1 & B
use: HTN, angina pectoris, tachycardia, CHF
(inc ejection fraction)

25

guanethidine

Antagonists/ block adrenergic neuronal function (peripheral pre-synaptic)
decreases NE in synaptic cleft
use: severe HTN, renal HTN
side effects: hypotension, fluid retention, impaired ejaculate, diarrhea, nerve toxicity
**not used anymore

26

hexamethonium (C6)

nonspecific Antagonist
adrenergic and nicotinic cholinergic receptors (nAChnR)
blocks all stimulation of pre-ganglionic neurons
stops release of NE and ACh
use: HTN
side effects: severe
not used clinically

27

atropine

anticholinergic
nonselective muscarinic Antagonist

use: bradycardia, vagal hyperactivity, bronchospasms, over-secretions
(treats DUMBBLSS)

side effect: "hot as a hare, dry as a bone, red as a beet, blind as a bat, and mad as a hatter"
flush, blurred vision, dec secretions, hyperthermia, delirium, hallucinations
big CNS effects

28

cocaine

adrenergic agonist; indirect sympathomimetic
block catecholamine reuptake by membrane transporter (NET)
increases NE in synapse
use: causes vasoconstriction, local anesthesia
side effect: MI

29

(+) inotropic drug

increase heart contractility

30

(+) chronotropic drug

increase heart rate

31

nicotine

nicotinic agonist
nicotinic acetylcholine receptors
stimulate both para- and sympathetic postganglionic neurons
causes skeletal muscle contraction
side effect: medullary depression, inc HR/BP/RR, spasms, toxic

32

succinylcholine (anectine)

nicotinic agonist
binds nicotinic acetylcholine receptors (Nm subtype)
causes prolonged neuromuscular depolarization
use: paralysis for surgery
side effect: malignant hyperthermia, hypotension, arrhythmias
depolarizing blockade- cannot be overcome by cholinesterase inhibitor

33

pancuronium, rocuronium

antinicotinic
competetive antagonist of nicotinic acetylcholine receptors (Nm)
use: paralysis for surgery
side effect: histamine release, hypotension, increase HR, edema
nondepolarizing blockade- can be overcome by cholinesterase inhibitor

34

ipratropium (atrovent)

antimuscarinic
nonselective antagonist acts on parasympathetic sites
inhaled to M3 acetylcholine receptors in bronchi
cause: dec bronchoconstrictions and secretions
use: COPD

35

Procainamide

Antiarrhythmic: class 1A: moderate Na channel blocker
binds Na in active state
slows conduction/prolong refractory period
reduces ectopic foci automaticity
use: reentry and ectopic; SVT, VT, VF, WPW
side effect: SLE, long QT

36

Quinidine

Antiarrhythmic: class 1A: moderate Na channel blocker
binds Na in active state
slows conduction/prolong refractory period
reduces ectopic foci automaticity
use: reentry and ectopic; SVT, VT, VF
side effect: long QT, thrombocytopenia, strong anti-cholinergic effect

37

Lidocaine

Antiarrhythmic: class 1B: WEAK Na channel blocker
binds Na in both active/inactive state
increase velocity at AV; decrease AP
reduces ectopic foci automaticity
may shorten QT
use: VT, VF, WPW, use after MI
side effects: CNS toxicity and cardiac depression
IV only

38

Flecainide

Antiarrhythmic: class 1C: STRONG Na channel blocker
reduces SA node and ectopic foci automaticity
reduces all conduction velocity
prolongs refractory period, long (QT, QRS, and PR)
use: Afib
side effects: heart block, arrhythmias

39

atenolol

Antiarrhythmic: class 2, B-blockers
B1 selective
use: HTN, CP/MI, does not cross BBB
decreases HR, output, renin release
little resp. effects (no B2)

40

labetalol

Antiarrhythmic: mixed alpha and beta blocker
A1, B1, B2 antagonist
lowers BP (A1), no reflex tachycardia (B1)
use: HTN, CHF, CP
side effect: orthostatic hypotension, heart failure

41

carvedilol

Antiarrhythmic: mixed alpha and beta blocker
A1, B1, B2 antagonist
lowers BP (A1), no reflex tachycardia (B1)
use: CHF, HTN, CP
side effect: orthostatic hypotension

42

amiodarone

Antiarrhythmic: class 3, prolong K repolarization
decrease K efflux
reduce conduction velocity
prolongs refractory and AP
use: VT, Vfib, Afib, Aflutter
side effects: long half life, long (QT, QRS, PR), eye dysfunctions
CYP3A4: affects renal/hepatic elimination (must change warfarin and digoxin levels)

43

sotalol

Antiarrhythmic: class 3, prolong K repolarization
AND nonselective B-blocker
prolong AP and refract period
use: VT
*less side effects than amiodarone

44

ibutilide

Antiarrhythmic: class 3, prolong K repolarization
prolong AP
slow inward Na current
use: Afib, Aflutter
side effect: long QT
IV only

45

bretylium

Antiarrhythmic: class 3, prolong K repolarization
blocks the release of norepi from nerve terminals
prolongs AP
use: HTN, only affects ventricle (VT, Vfib)

46

verapamil

Antiarrhythmic: class 4, slow inward Ca
Non-dihydropyridine calcium channel blocker
act on heart
reduce SA/AV conduction, prolong refractory (long PR)
use: SVT, atrial tachy, atrial flutter, Afib
side effects: bradycardia, hypotension, AV block, GI effects
do not use on WPW
CYP3A4: affects renal/hepatic elimination (must change warfarin and digoxin levels)

47

diltiazem

Antiarrhythmic: class 4, slow inward Ca
Non-dihydropyridine calcium channel blocker
act on heart
reduce SA/AV conduction, prolong refractory (long PR)
use: SVT, CP, Afib, HTN
side effects: bradycardia, hypotension, AV block

48

action of B-blockers as a class

decrease HR, contractility,
decrease SA/AV automaticity, conduction velocity
decreases renin
blocks vasoconstriction and decreases peripheral vascular resistance
bronchoconstriction
hyperglycemia sx

49

digoxin

antiarrhythmic: cardiac glycoside
slows conduction through AV node
block Na/K-ATPase pump
decrease conduction, prolong refract (long PR)
EKG: short QT, Twave inversion
enhance vagal activity at AV node, stimulates carotid baroreceptor
decrease HR
(+) ionotroph, increased intracellular Ca
use: ventricular response of Afib, Aflutter, cardiogenic shock, CHF
side effects: digitalis toxicity, bradycardia, fatigue, hypokalemia, arrhythmias, heart block, GI: n/v/d (vagal)
do not mix with quinidine

50

adenosine

antiarrhythmic
prolongs refract: increase K efflux=hyperpolarization
decreases AV conduction velocity, blocks Ca entry
EKG: long PR
induces transient heart block, break re-enty
use: re-entry SVT, vasodilation
works very quickly and lasts only a short period of time
side effects: flushing, CP, arrhythmia, dyspnea, hypotension

51

magnesium

use: torsades de pointes, dig toxicity

52

potassium

use: hypokalemia and electrolyte-associated cardiac arrhythmias
side effect: VT

53

bethanechol

direct cholinergic agonist
muscarinic: M1, M2, M3
AND nicotinic agonist
increase parasym and secretions
use: post-op GI and bladder motility
resistant to AChE
side effect: bradycardia, bronchoconstriction, parkinsonism

54

muscarine

cholinergic agonist
muscarinic: M1, M2, M3
not used clinically
mushroom product used to discover M receptor

55

pilocarpine

direct cholinergic agonist
muscarinic: M1, M2, M3

use: glaucoma (causes miosis), increase secretions (sweat/saliva)

56

carbachol

direct cholinergic agonist
muscarinic: M1, M2, M3
AND nicotinic agonist
increase parasym

use: glaucoma (causes miosis)

side effect: constriction

57

scopolamine

anticholinergic
muscarinic antagonist: alkaloid
receptors at eyes and glands
use: motion sickness, n/v/d
can enter BBB; less CNS than atropine

58

homatropine

anticholinergic
muscarinic antagonist: alkaloid
receptors at eye
causes mydiasis and cycloplegia
side effects: blurred vision, sensitivity, drowsiness
can enter BBB

59

oxybutynin/darifenacin/solifenacin

anticholinergic
muscarinic antagonist: tertiary
use: bladder spasms, leakage/incontinence
can enter BBB
side effects: dec secretions, mydiasis and cycloplegia

60

tolterodine

anticholinergic
muscarinic antagonist: tertiary
decreases bladder tone
use: overactive bladder
side effects: constipation, dry mouth, headache
can enter BBB

61

benztropine

anticholinergic
muscarinic antagonist: tertiary
central action
use: parkinsonism, tremors, rigidity, drooling, akinesia
side effects: tachycardia, hypotension, dry mouth
can enter BBB

62

ipratropium/tiotropium

anticholinergic
muscarinic antagonist: quaternary
local: respiratory
inhalation tx
use: bronchoconstriction, COPD, asthma

63

propantheline

anticholinergic
muscarinic antagonist: quaternary
local: GI, urinary
reduces motility and delays emptying stomach
use: peptic ulcers, spasms

64

glycopyrrolate

anticholinergic
muscarinic antagonist: quaternary
local: GI, urinary
use: peptic ulcers
also decreases secretions and cardiac relfexes in intubation

65

pirenzepine

muscarinic antagonist:
M1 selective
use: peptic ulcers (dec gastric acid)

66

trimethaphan

neural nicotinic (Nn) receptor antagonist
non-depolarizing ganglion blocker
use: HTN
causes vasodilation
triggers histamine release (inc HR, decrease contractility)
side effects: severe
not used clinically

67

varenicline

neural nicotinic (Nn) receptor partial agonist
selective A4B2 subtype in CNS
reduces nicotine stimulation
use: smoking cessation
side effects: psych, AMS

68

methyldopa

presynaptic anti-adrenergic
strong Agonist A2
causes dec NE and suppresses sympathetic
Use: HTN
side effect: sedation

69

esmolol

Antagonists/ adrenergic receptor blockers
B1 selective
Use: aortic dissection, tachycardia, SVT
rapid onset, short duration

70

propafenone

Antiarrhythmic: class 1C: STRONG Na channel blocker
slows AV conduction, prolongs refract
use: SVT, Afib
side effects: heart failure, bradycardia, arrhythmia
do not give post MI

71

dofetilide

Antiarrhythmic: class 3, prolong K repolarization
prolong AP
increase ERP
use: Afib, Aflutter
side effect: long QT, dizziness

72

Niacin

antihyperlipidemic agent: B vitamin.
effect: - decreases the synthesis VLDL by the liver
- decrease LDL.
- decreases the synthesis of cholesterol.
- increases the level of HDL (decrease the catabolism)
- decreases Lp(a)
- lowering serum triglycerides.
use: hypertriglyceridemia; combined with an HMG CoA reductase inhibitor to treat most forms of hypercholesterolemia
side effects: flushing, hepatotoxicity
con: need large dose

73

Fenofibrate


antihyperlipidemic agent: fibric acid derivatives
effect: -decrease triglycerides (VLDL) (by activating protein lipase activity)
- increases HDL
use: Familial hypertriglyceridemia, Dysbetalipoproteinemia
side effects: -myopathy and rhabdo
interacts with anti-coag tx
do not use in renal failure

74

Colestipol

antihyperlipidemic agent: Bile acid sequestants
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.

75

Cholestyramine

antihyperlipidemic agent: Bile acid sequestants
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.

76

Colesevelam

antihyperlipidemic agent: Bile acid sequestants
**best of the group
Action: binds and inhibits bile acids resorption, causes liver to reclaim cholesterol and serum LDL (increased clearance)
Effect:
- Increase (Apo B receptors) = decrease LDL, IDL, & VLDL
- Increase HLD
Use: high LDL; combine with statin therapy
Side effect: constipation, inc cholesterol production in liver
Interferes with many any drugs
are not absorbed by the body and therefore are passed in the stool.

77

Lovastatin

antihyperlipidemic agent: HMG-CoA reductase Inhibitors
*weak
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4

78

Simvastatin

antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4

79

Pravastatin

antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy

80

Atorvastatin

antihyperlipidemic agent: HMG-CoA reductase Inhibitors
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Drug interaction: CYP3A4

81

Rosuvastatin

antihyperlipidemic agent: HMG-CoA reductase Inhibitors
*newest
Effect: STOP cholesterol biosynthesis= liver inc ApoB receptors to reclaim LDL, IDL, and VLDL (inc clearance)
- Increase HDL
- Dec triglycerides
Use: hyperlipidemias, Familial Hypercholesterolemia, Combined Familial Hyperlipidemia, reduce MI risk
Side effect: rhabdo, hepatotoxicity, hyperglycemia
Teratogenic- NOT used in pregnancy
Asians show high levels

82

Ezetimibe

antihyperlipidemic agent: Cholesterol absorption inhibitor
Effects: inhibits dietary cholesterol GI absorption
- Lowers LDL
Use: lower serum cholesterol; can be combined with a statin
Side effects: minor GI

83

Laropiprant

Prostaglandin D2 antagonist
Use in Niacin therapy to reduce flushing

84

Neomycin

antihyperlipidemic agent: aminoglycoside antibiotic.
effect: inhibiting the reabsorption of cholesterol and bile salts.
effect: reduction of total body cholesterol.
- does not affect triglyceride levels.
Use: combination with niacin to lower Lp(a) levels

85

aliskiren

renin inhibitor
effect: blocks angiotensinogen conversion
use: HTN
side effects: hypotension, hyperkalemia, rash, GI, renal failure
CYP3A4
teratogenic

86

captopril, lisinopril, enalapril
"pril"

ACE inhibitor
prevents formation of angiotensin2
inc bradykinin and prostaglandins= vasodilation
use: high-renin HTN, arteriolar/venous vasodilation
post MI- enhance reperfusion
side effects: natriuresis, cough, airway irritation, angioedema, renal failure, hyperkalemia
teratogenic

87

losartan
"sartan"

angiotensin 2 antagonist- (ARB)
blocks receptor at vascular muscle
use: HTN, CHF
side effects: hypotension, dizziness, renal failure, hyperkalemia
teratogenic

88

spironolactone

aldosterone receptor antagonist
K sparing diuretic
use: edema, CHF, HTN
side effects: endocrine imbalances, hyperkalemia, gynecomastia

89

eplerenone

aldosterone receptor antagonist
K sparing diuretic
use: edema, CHF, HTN
side effects: hyperkalemia
**lower affinity for other steroid hormone receptors than spironolactone= less side effects

90

hydralazine

direct vasodilator
relaxes arterioles
dec BP and afterload
reflex inc HR and CO
directly inc renal blood flow
use: HTN, pregnancy
side effects: many side effects, SLE, fluid retention

91

minoxidil

direct vasodilator
prodrug
opens K channels=hyperpolarizes smooth muscle=relaxes arterioles
use: HTN, topical tx male pattern baldness
side effect: hirsuitism, reflex tachycardia, pulmonary damage, fluid retention

92

sodium nitroprusside

direct vasodilator
effect: dilates arteries and veins (dec preload and after load)
nitric oxide-->cGMP--> inactivate myosin= relax smooth muscle= vasodilation
use: IV HTN crisis
side effect: severe hypotension, cyanide toxicity, hepatotoxicity, renal toxicity

93

nitroglycerin

anti-anginal agent
nitric oxide-->cGMP--> inactivate myosin= relax smooth muscle= vasodilation
effect: dilates large coronary arteries= inc blood to heart
dec venous tone= dec cardiac preload
use: CP, MI
side effects: hypotension, reflex tachycardia, cerebral ischemia
do not use with: alcohol, vasodilatiors, PDE5 inhibitors ("afils")

94

nifedipine

anti-HTN/anti-anginal
calcium entry blocker
potent peripheral vasodilator
side effect= TOXIC, reflex tachy and inc CO, MI
not used

95

nicardipine, clevidipine

anti-HTN/anti-anginal
calcium entry blocker
potent peripheral vasodilator
use: CP, HTN emergency
side effect= reflex tachy and inc CO, palpitations

96

isosorbide dinitrate

anti-anginal nitrate
nitric oxide-->cGMP--> inactivate myosin= relax smooth muscle= vasodilation
use: CP, CHF
do not combine with vasodilation meds

97

isosorbide-5-mononitrate

anti-anginal nitrate
nitric oxide-->cGMP--> inactivate myosin= relax smooth muscle= vasodilation
use: CP, CHF
do not combine with vasodilation meds

98

nimodipine

anti-HTN/anti-anginal
calcium entry blocker
effects cerebral artery vasodilation
use: subarachnoid hemorrhage/CNS damage
side effect: carcinogenic and teratogenic

99

uses for mannitol, furosemide (lasix), and hydrochlorothiazide (HCTZ)

diuretic
use: edema, CHF, HTN
works on kidney to increase Na/water excretion

100

aspirin
acetylsalicylic acid

anti-platelet
irreversible cyclooxygenase inhibitor
dec thromboxane A2 and prostaglandins= dec platelet aggregation
use: MI, stroke, inflammation, fever, pain
side effects: GI ulcers, bleeding, hemorrhage, asthma
recommend: low dose, not for children
PO

101

clopidogrel (Plavix®), prasurgel (Effient®), Ticlopidine (Ticlid)

anti-platelet: thienopyridines
irreversibly blocks ADP receptor (P2Y1 and P2Y12)
use: acute coronary syndrome, atheroclerosis, peripheral arterial disease
side effects: GI ulcers, bleeding, thrombotic purpura
CYP450
PO, prodrug

102

ticagrelor (Brilinta®)

anti-platelet: thienopyridines
reversible ADP receptor blocker
use: reduce MI, stroke
combine tx with aspirin
side effect: bleeding
PO

103

dipyridamole

anti-platelet
PDE inhibitor= inc cAMP
vasodilator (inc levels of adenosine)
use: post heart valve replacement surgery, history stroke
combine tx with warfarin or aspirin
side effect: hypotension, syncope, headache, GI

104

cilostazol

anti-platelet
PDE 3 inhibitor= inc cAMP and PKA
effect: dilates lower ext blood vessels
use: intermittent claudication
side effects: headache, palpitations
CYP3A4, CYP2C19

105

abciximab

anti-platelet: glycoprotein 2b/3a inhibitor
monoclonal antibody
use: before coronary angioplasty (PCI), MI
side effect: bleeding
combine tx with heparin or aspirin

106

eptifibatide

anti-platelet: glycoprotein 2b/3a inhibitor
synthetic peptide, fibrinogen analog= blocks platelet crosslinking
use: acute coronary syndrome, before coronary angioplasty (PCI), MI
side effect: bleeding, renal failure

107

tirofiban

anti-platelet: glycoprotein 2b/3a inhibitor
reversible
use: unstable angina, before coronary angioplasty (PCI)
side effects: bleeding

108

heparin
Unfractionated heparin
(UFH)

anticoagulant
binds to antithrombin 3 (AT3)= more active= inactivates thrombin (factor 2) and active factor 10, 9, 11.= no fibrin
immediate action
use: DVT, PE, surgery, acute coronary syndrome
side effect: bleeding, hemorrhage, necrosis at injection site, thrombocytopenia
**highly variable anticoagulant response/effects/duration= LMWH used more
IV/injection
antidote: protamine sulfate
monitor aPTT
intrinsic pathway

109

Low-molecular-weight heparins, (LMWH)
enoxaparin "parin"'s

anticoagulant
smaller fragment of heparin
binds to antithrombin 3 (AT3)= more active= inactivates active factor 10
use: DVT, PE, surgery, acute coronary syndrome
side effect: bleeding, renal failure
****more controlled anticoagulant response/effects/duration= used more common
IV/injection
antidote: protamine sulfate
does not effect PT
intrinsic pathway

110

fondaparinux

anticoagulant
inhibits factor 10a
use: DVT, PE
side effect: bleeding, rash
does not effect PT

111

warfarin (coumadin)

anticoagulant
inhibits enzyme epoxide reductase (VKOR)= inactive vitamin K= loss of gamma-carboxylation rxn for dependent clotting factors (2,7,9,10)
uses:DVT, PE, Afib, dilated cardiomyopathy, prosthetic heart valves
side effects: bleeding, necrosis, GI
CYP2C9
many drug interactions
NOT in pregnancy
orally
monitor PT/INR/vit K
extrinsic pathway

112

lepirudin, bivalirudin

anticoagulant
direct thrombin inhibitor (from hirudin)
alternative to heparin (no HIT, does not use AT3)
side effect: bleeding, renal failure
IV

113

dabigatran (pradaxa),

anticoagulant
prodrug, direct thrombin (factor 2a) inhibitor
use: stroke, Afib, DVT, PE, post surgery
*no need to monitor PT
side effects: bleeding
NOT in pregnancy
orally

114

rivaroxaban, apixiban

anticoagulant
prodrug, direct factor 10a inhibitor
use: stroke, Afib, DVT, PE, post surgery
*no need to monitor PT
side effects: bleeding
CYP3A4
NOT in pregnancy
orally

115

argatroban

anticoagulant
direct thrombin inhibitor (from hirudin)
alternative to heparin (no HIT, does not use AT3)
side effect: bleeding
cleared through LIVER
CYP450
IV
*similar to lepirudin, bivalirudin, but better for bad renal pts

116

streptokinase, urokinase

thrombolytic agent
activates plasminogen= plasmin= degrades fibrin/fibrinogen
use: DVT, MI, stroke, dialysis pts with occlusion
side effect: bleeding, immune rxn
IV

117

tissue plasminogen activator (tPA)

thrombolytic agent
activates plasminogen= plasmin= degrades fibrin and ACTIVE clot
use: coronary occlusion
side effects: hematoma
IV