Catecholamines Flashcards Preview

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Flashcards in Catecholamines Deck (48):
1

Epi class

endogenous catecholamine that is nonselective adrenergic agonist

2

Epi MOA

binds to alpha1/2 and b1/2 receptors equally- activating g coupled protein receptors to increase cAMP causing an influx of intracellular Ca2+ causing agonist effects

3

Epi se

tachycardia, angina, arrhythmias, HTN, decrease RBF, vasoconstriction of- skin, Gi tract, muscle, liver and kidneys. gangrene in digits, hypoglycemia

4

Epi ci

caution in DM, hyperthyroid, pheochromocytoma, glaucoma, caution in pregnancy. Decrease LA absorption. avoid in peripheral LA blocks in fingers and toes

5

Epi PK

Onset 1-2 min
DOA 5-10 min
E1/2t 30 sec
Small vd= poor lipid solubility
reuptake or diffusion primary way drug gets out of system then metabolized by Catechol-o-methyltransferase (COMT) and monoamine oxidase enzymes biotransformations in blood, liver, kidneys

Metabolites Excreted in urine

6

epi dose

anaphylaxis- 0.1-1mg. 1mg q3-5min for CV arrest ACLS, 1-2mcg/min beta2 (asthma); 4-5mcg/min beta1 (poor co), 10-20mcg/min alpha and beta

7

NE/Levophed class

direct acting endogenous catecholamine and adrenergic agonist- sympathomimetic

8

NE MOA

binds to alpha 1 and 2 receptors and b1- lacks B2 and activates g coupled protein receptors to increase cAMP causing an influx of Ca2+ causing an agonist effect and increase contractility; potent vasoconstrictor; when it increase BP= causes baroreceptor activation and drops HR and increase SVR preserves coronary and cerebral BF in decrease BP; decrease venous return- CO and HR; low dose causes increase HR/CO; alpha at high doses

9

NE Pk

onset rapid; DOA 5-10min; E1/2 2.5min; reuptake or diffusion primary way metabolized then by MAO and COMT. excreted in urine

10

NE SE

increase SBP, DDBP, MAP; decreases HR bc baroreceptor activation, decrease RBF, HBF and splanchnic BF; organ ischemia and necrosis of extremities and digits

11

NE CI

pheochromocytoma, caution in liver and renal disease; MAOi's and TCAs, hypovolemai, thrombosis

12

NE dose

4-16mcg/min IV

13

Dopamine class

dopamine/adrenergic agonist; sympathomimetic endogenous precursor of NE
Preg class C

14

DA MOA

stimulates all adrenrgic receptors including DA receptors. extracted from L-dopa on catecholamine synthesis of tyrosine; small doses- DA effects- vasodilation by stimulation of adenyl cyclase-> increasing level of cAMP in vascular SM (renal, coronary and mesenteric beds); medium doses= beta causing increased myocardial contraction and increase HR; large doses= alpha and beta effects causing vasoconstriction of all vascular beds including renal increasing BP, CO, SVR; also increase endogenous NE release (doesn't work well with decreased catecholamine stores)

15

DA PK

Does not cross BBB, onset rapid, DOA 5-10min; E1/2 2 min; metabolized and elimated by MAO and COMP to 75% inactive and 25%NE. Must protect from light

16

DA SE

tachycardia, arrhythmias, angina, extravasation, N/V, increased IOP and UOP, widen qrs

17

DA CI

right HF, pheochromocytoma, thyroid storm, IOP, caution in CAD/post MI, sulfa allergy. Should not be used with methyldopa, non selective bb, tcas, and MAOIs

synergistic with Dobutamine to decrease SVR and increase CO (Da dilates cutaneous vascular beds while Dobutamine dilates other vascular beds)

18

DA dose

DA1- low dose 1-3mcg/kg/min ( increase GFR, RBF, UOP); beta 1 medium dose 3-10 mcg/kg/min; alpha large dose 10mcg/kg/min

19

Dobutamine class

sympathomimetic; synthetic catecholamine-synthetic analog of isoproterenol

20

Dobutamine MOA

beta 1 selective agonist and weak beta 2 and alpha 1; binds to receptor and activates G protein receptors in increase cAMP causing an influx of Ca2+= increase contractility and CO without increase HR or Bp too much (good for CHF)

21

Dobutamine PK

onset 1-2 min; DOA 5-10min, e1/2 2 min, metabolized and eliminated by MAO and COMT reuptake or diffusion away from active site

22

Dobutamine SE

minimal increase HR (weak activity at SA node), arrhythmias, angina, HTN, platelet inhibition, thrombocytompenia, coronary artery and pulmonary vasodilator, N, phlebitis

23

Dobutamine CI

avoid in hypertrophic cardiomyopathy, MAOis, TCAs, caution in CAD and MI (ok for CHF); not good if need an increased SVR

24

Dobutamine dose

Typical dose 2-10mcg/kg/min; (max is 40)
Beta15mcg/kg/min

25

Vasopressin class

exogenous antidiuretic peptide and vasopressor

26

Vasopressin MOA

vasoconstricts by stimulating the V1a receptors on vascular SM, glomerular efferent arteriole, mesangial cells and vasa recta. Works on V2 receptors in the collecting tubules by stimulating g coupled protein receptor adenylyl cyclase= ATP= cAMP= activates protein kinase that stimulates the vesicles containing aquaporin water channels to be come active and retain water.

27

Vasopressin PK

onset fast; e1/2 10-20 min; metabolized by tissue peptidase and urinary excretion

28

Vasopressin SE

angina, CA spasm, arrhythmias, increased peristalsis, N/V, abd pain, EKG changes, increase BP, bronchial constriction

29

Vasopressin Ci

HTN, CAD (caution), renal disease, NSAIDS increased effect

30

Vasopressin dose

40 units IVP for CV arrest ACLS; 20 units for varices; 0.04U/min gtt for sepsis

31

isoproterenol class

synthetic catecholamine

32

isoproterenol MOA

B1>B2; minimal alpha (cardiac pacemaker), acts on Gproteins to increase cAMP causing an influx of Ca2+ causing increase in contractility with NO change in SVR (can increase HR) , increases SBP, profound decrease DBP with no change in MAP; also is a pulmonary and systemic arterial vasodilator from B2 actions used to treat bronchospasm; used for HB especially 3rd degree, bradyarrhythmias, BB OD

33

isoproterenol PK

onset rapid; DOA 5-10min; e1/2 3-5mi; metabolized and eliminated rapidly by COMT in liver and pulmonary with 50% elimated unchanged in the urine

34

isoproterenol SE

bradycardia, angina, arrhythmias, decrease CA BF secondary to decrease DBP; B2 effects- peripheral vasodilation and hypotension; B1= increased contractility of the heart and increases o2 demand

35

isoproterenol CI

HTn, CAD (increases demand), pheochromocytoma, thyroid stomr, MI, hyper tropic cardiomyopathy, tachycardia, dig toxicity

36

isoproterenol dose

0.5-10mcg/min

37

ephedrine class

synthetic NON-catecholamine; direct and indirect (primarily) adrenergic agonist

38

ephedrine MOA

indirectly affects alpha and beta receptors by stimulating NE release; directly acting on b1 (increase myocardial contractility); increase SBp, DBP, CO and HR; increase CA and skeletal muscle BF; venous>arterial constriction; decrease HBF and splanchnic BF

39

ephedrinePK

onset rapid; DOA 1hr; E1/2 3hrs; slower/resistant to MAO metabolism since lacking catecholamines so slower metabolism and excreted 40% unchanged in the urine

40

ephedrine SE

arrhythmias, HTN, MI, CNS stimulation, decrease uterine activity; can cause tachyphylaxis

41

ephedrine CI

HTN, CAD, MAOis, TCAs, cocaine, caution in trauma, ephedra

42

ephedrine dose

5-25mg IV

43

phenylephrine class

direct acting synthetic NON-catecholamine selective alpha 1 agonist

44

phenylephrine MOA

direct stimulation of alpha 1 receptors with venous>arterial constriction, increase MAP, SBP, DBP, SVR and decrease in HR and CO (baroreceptors),

45

phenylephrine PK

90%PB, onset <1min, DOA 5-20min, e1/2 2.5hours; metabolized by MAO to phenolic and conjugates excreted in the urine 90%

46

phenylephrine SE

rebound nasal congestion, bradycardia, HTN, arrhythmias, decrease RBF and splanchnic BF= decrease UOP; metabolic acidosis

47

phenylephrine CI

HTN, arrhythmias, CHF, glaucoma, cocaine, ephedra
can prolong LA

48

phenylephrine dose

50-200mcg IVP; 20-50mcg/min gtt- double dilute