Heart Failure Flashcards
propranolol
beta 1 selective antagonists
increased potency
category C pregnancy
Pindolol
partial beta agonist
anything capable of H bonding at meta or para substituent = compound with ISA
Category B pregnancy
Metoprolol
B 1 selective antagonist
CYP 2D6 metabolism + genetic variability
Category C pregnancy
Nebivolol
most B1 selective of given compounds but is related to its metabolism
mix of 2 enantiomers
MOA also includes: direct vasodilator by formation of NO (EDRF)
Undergoes CYP2D6 hydroxylation at benzylic if fast metabolizer
Category C pregnancy
Labetolol
has weak ISA b/c hydroxyl group is para and not meta
has dec activity
undergoes 1st pass effect b/c of phase 2 transformation = glucuronidation
NOT CYP
R,R enantiomer = B blocker
S, R enantiomer = alpha blocker which is important in balancing peripheral vasoconstriction via beta blocking MOA
Category C pregnancy
Carvedilol
Beta and alpha blocker
beta is 100X greater than alpha blockade
S isomer = alpha and beta blockade
R isomer = alpha blockade
high PPB
NO ISA
non selective
greater effect to prevent remodeling
it undergoes hydroxylation via CYP 2D6, 2C9, and 3A4 metabolism which forms active metabolites which are then glucuronidated and eliminated
Does have negative inotropic effects - monitor severe pt
Digoxin
Cardiac glycoside
inhibits Na/K ATPase
at therapeutic doses: dec automaticity and inc diastolic resting membrane potential in atrial and AV node tissue due to an inc in vagal tone and a dec in sympathetic activity
effective refractory period is prolonged and ocnduction velocity is decreased in AV node tissue as well.
As dose inc, bradycardia or heart block results
In high concentrations, GC can lead to arrythmias
Has six OH groups
It is less lipophilic than digitoxin
onset of 15 - 30 min
oral adminstration
half life: 36 hours
Metabolized by eubacteria lentum in the gut –> less active compound
NO CYP
Digitoxin
Cardiac glycoside
has five OH groups
More lipophilic
25 - 120 min onset
oral admin
high PPB
4 - 6 day half life
metab: hepatic and renal
NO CYP
Dobutamine
stimulates B - 1 receptors —> inc Ca concentration in heart cells —> shortens PR interval and acts as pro-arrythmic
positive inotrope
short term therapy for ADHF
Does not raise BP
Heart rate will slightly increase
MAP slightly increase
SVR: dec
PCWP: dec
CO: inc
IV admin
hafl life 2 min
Metab: COMT, sulfate and glucuronide conjugation
Tolerance develops after 72 hours
DDI: MAOI, NE reuptake inhibitors
ADR: tachycardia, HTN, PVC
Milrinone
phosphodiesterase inhibitor
Admin IV
duration: 3 -5 hr
Metab: glucuronidated at carbonyl
excreted in urine
ADR: HA, hypotension, ventricular tachycardia, thrombocytopenia (< 1%)
used as short term therapy in heart failure
has positive inotropic effect and increase myocardial relaxation
Affect arteries and veins –> dec both periopheral and pulmonary resistance —> dec preload and pulmonary congestion
Reduces afterload —> inc CO
Amrinone
phosphodiesterase inhibitor
admin IV
duration 0.5 - 2 hr
metabolism: acetylation, glucuronidation
ADR: thrombocytopenia (2.4 %) - used less due to this ADR
has positive inotropic effect and increase myocardial relaxation
Affect arteries and veins –> dec both periopheral and pulmonary resistance —> dec preload and pulmonary congestion
Reduces afterload —> inc CO
