Exam V - CV Flashcards
What is the cell signaling for Alpha 1 receptors?
Gq protein coupled
activates
Phospholipase C
activates
PIP2 –> IP3 + DAG (increases Ca++ –> contraction)
What is the cell signaling for Alpha 2 receptors?
Gi protein coupled
inhibits
Adenlyl Cyclase
inhibits
ATP –> CAMP (Less CAMP)
*just think Gi –> i for inhibitory and the Alpha 2 is a presynaptic inhibitory receptor
What is the cell signalling for Beta 1 & 2 receptors?
Gs protein coupled (stimulatory)
activates
Adenlyl Cyclase
activates
ATP –> CAMP (More CAMP)
*think s for stimulatory and the beta receptors are stimulatory
If you are giving a ton of pressors, what route of med administration should you be worried about working?
SQ
(vasoconstriction is shunting blood away from skin/superficial tissues)
CAMP in the smooth muscle causes what (contraction or relaxation?)
Relaxation
so decreased CAMP will cause vasoconstriction in the vascular smooth muscle
CAMP in the cardiac muscle causes what (contraction or relaxation?)
Contraction
Increased CAMP causes contraction of the cardiac muscle (Inotropy/chronotropy)
Phenylephrine acts primarily on _______ tone with some _______
arterial
venous
Phenylephrine is metabolized by ______ not _________
MAO
Not COMPT
Phenylephrine DOA
<5mins
Would you want to give phenylephrine w/ pulmonary HTN pts?
NO
*it increases PVR duh
(t/f) Phenylephrine RARELY may induce vasospasm: IMA, radial, gastroepiploic artery
True
Dosing for phenylephrine
- IVP : 40-100 mcg
- Infusion: 40-180mcg/min
Does phenylephrine cause a big direct increase in preload?
No
Minimal direct effect on preload (less venous effects)
Ephedrine metabolism
Neither MAO or COMT
Excreted unchanged renally
DOA of ephedrine
5-10mins
*relatively long compared to phenylephrine
Ephedrine dosing
- 5-10mg IVP
- 25-50 mg IM
What drug has a risk of malignant HTN with MAOIs
Ephedrine
*makes sense b/c we are double increasing NE in synapse
Is HR drastically increased or slightly increased w/ ephedrine?
Slightly
Vasopressor after spinal anesthesia sympathectomy in c-section pts study: Decreased risk of fetal acidosis associated with ______________ use.
phenylephrine
*give NEO w/ NEOnates
____________ is converted to DOPA by ___________ hydroxylase
(rate-limiting step for
NE synthesis)!!!
Tyrosine (Tyr)
tyrosine hydroxylase
DOPA is converted to dopamine (DA) by DOPA _____________.
decarboxylase
Dopamine is transported into vesicles then converted to _____________ by dopamine β-hydroxylase (DBH)
norepinephrine (NE)
Dopamine transport into the vesicle can by blocked by the
drug ___________.
Reserpine
Both NE & Epi are metabolized by what
MAO & COMT
What is the final metabolite of NE & Epi metabolism?
Vanillylmandelic acid (VMA)
(t/f) NE hits B1 receptors less than Epi
False
(allegedly they are the same but they aren’t in real life)
(t/f) NE has less effects on B2 than Epi
True
NE dosing
2-4mcg/min starting gTT
*you could loose 2-4 limbs w/ norepinephrine
V1 receptors are located in the _________ and cause __________
Vasculature
Vasoconstriction
V2 receptors are located in the __________ and cause _________
Kidney
Fluid reabsorption
Vasopressin is released from the _______ ________
posterior pituitary
The V2 receptor can also release clotting factors _______ & ________
vWF
VIII
Cell signaling of vasopressin
Gq
activates
Phospholypase C
activates
IP3/DAG
Increased Ca++ release
activates
Myosin-light-chain kinase & phosphodiesterase
Vaso can do what to ur coags
Decrease platelet count
Vasoplegia is what
Super dilated vessels
Vasoplegic syndromes
w/ concominant ACEI and ARB administration unresponsive to phenylephrine
Vasopressin
Vasopressin dosing
Resuscitation dose 40 units
Infusion 4-6 units/hour
IVP 1-2 units
What is Methylphenidate
Amphetamine derivative; abuse potential
Normal byproduct of tyrosine metabolism; readily
metabolized by MAO in the liver
Issue with concomitant MAOIs
Tyramine
Levodopa and Fenoldopam are in what broad drug category?
Indirect acting sympathomimetics
(t/f) Inotropes activate phosphodiesterase
False
They inhibit it
Dopaminergic stimulation = _______and _________
vasodilation
renal
mesenteric
What is lusitropy
Loosey goosey ventricles that fill better
Inotrope slective for B1 activation
Dobutamine
Dobutamine metabolism
COMT
Dobutamine & isoproterenol plasma half life is what
2 min
IMPORTANT!!!
(t/f) dobutamine has less tachycardia than Isuprel or Dopamine
true
PDE degrades what
CAMP
B/c PDE degrades CAMP, you get __________ in the vessels when PDE is stimulated
vasoconstriction
Inotropes ________ PDE
inhibit
When dobutamine is given to β- blocked patients a(an) __________ in SVR may occur
Increase in SVR
*dobutamine may have alpha 1 effects so if the B1 receptor is block that it usually works on, A1 effects are the only action left
What med do you use with stress
echocardiography
Dobutamine
The decreased SVR from dobutamine is mediated from _____ receptor effects
B2
Dobutamine dosing
2-20 mcg/kg/min
Endogenous catecholamine, precursor to NE/Epi
Dopamine
what drug has a dose-responsive direct action on all adrenoreceptors
Dopamine
With dopamine at low doses, you stimulate on the ______ receptor which causes what?
DA1
Increased renal and mesenteric blood flow
Dopamine metabolism
MAO
and COMT
Dopamine inhibits aldosterone which equals __________
Naturesis
Eliminating Na+
Extremely potent β effects; very little/no α effects
ISOPROTERENOL
*ISOlates the B receptor
Isoproterenol metabolism
MAO & COMT
(t/f) Isoproterenol has no risk for CAD pts
False
Caution in CAD pts
Isoproterenol dosing
2-5 mcg/min
What drug (not epi) that is a inotrope can be nebulized for reactive airway mgmt
Isoproterenol
What drug is used for beta blocker overdose
Isoproterenol
*glucagon is better
Epi metabolism
MOA & COMT
1mg = _______ mcg
1000
PDE Type ___ is the isoenzyme targeted by current inotropic medications
type 3 (PDE3I)
Milronone is what class of drug
PDE3 inhibitor
Milronone metabolism
Unchanged in urine
This drug retains efficacy when NE stores are depleted (chronic CHF)
Milronone
Milronone dosing
Loading dose: 50 mcg/kg
TRO 10 minutes
Infusion: 0.5 mcg/kg/min
___________ is Necessary for cardiac
muscle contraction
Ca++
Treatment of beta-blockade overdose due to increase cAMP in the myocardium
Bypasses the inhibitory effect of beta-blockade
Glucagon
Peptide hormone
Increases intracellular cAMP
Glucagon
Glucagon dosing
1-5mg IV slowly
Indirect acting vasodilator: ____________
Nitroglycerin
Direct acting vasodilator: ____________
Nitroprusside
Nitroprusside can cause _______ toxicity
cyanide toxicity
Nitroprusside work more on ______ vessels
arterial
(t/f) Nitroglycerin has tachyphylaxis
True
NTG and NTP work by increasing _______ (NO)
Nitric oxide
What 2 ways does NO work?
- NO activates guanylyl cyclase to active cGMP. This decreases Ca++ which cause relaxation
- Activates K+ channels causing hyperpolarization causing relaxation
Increased in cGMP = ___________ in platelet aggregation
decrease
Nitrites react to form
_____________
methemoglobin
Cyanide toxicity treatment
Stop the NTP
100% O2
Sodium thiosulfate (150 mg/kg over 15 minutes)
Selective DA1 agonist w/ 6x greater potency than
Dopamine
Fenaldopam
What is fenaldopam used for?
Sever HTN tx