Beta Blockers and Vasodilators Flashcards
Two water soluble BB’s? What is unique about their pharmacokinetics?
- Atenolol, nadolol
- long half-lives
- metabolized by the kidney
How is esmolol metabolized?
plasma esterases (10 min half life)
Where are B2 receptors found?
vascular and bronchial smooth muscle
Which generation of BB’s is non-selective and vasodilatory?
3rd
Two ways 3rd gen BB’s assert vasodilation and associated drugs?
- direct via NO (carvedilol, nebivolol)
- indirect via alpha blockade (carvedilol, labetalol)
7 functions of carvedilol?
- non-selective BB
- alpha blocker
- calcium blocker
- NO
- anti-oxidant
- anti-proliferative
- blocks expression of genes involved in myocardial damage
Four classes of oral meds proven in RCT’s to reduce CV M&M?
- BB’s
- ACEI’s
- statins
- anti-platelets
3 typical functions of the B1 blockade?
- neg inotropism
- neg chronotropsim
- blocked renin secretion (regulated by B1R)
Two typical AE’s specific to non-selective BB’s?
- bronchoconstriction
- exacerbation of PVD
Three typical AE’s associated with all BB’s?
- sedation, fatigue, mental impairment
- hypotension and bradycardia
- inc tri’s and dec HDL
What 5 conditions can BB’s be used to treat?
- HF
- post-MI
- SVT
- ischemic HD
- HTN
Why should BB’s be used with cautious in diabetic patients?
- catecholamines utilize B2R to promote glycogenolysis and mobilize Glc
- block of this receptor may induce or exacerbate hypoglycemia (and mask tacky associated with hypoglycemia)
6 contraindications for BB Tx?
- severe brady
- high grade AVB
- cardiogenic shock (LVF)
- severe bronchospasm
- severe depression
- symptomatic PVD
In HF, what state should you make sure the patient is in before Rx’ing BB’s?
hemodynamically stable
What molecule does eNOS used to make NO?
L-arginine –> citrulline + NO
How are lipid soluble BB’s metabolized?
- hepatic – first-pass effect and variable bioavailability
- shorter 1/2 life but distributed in the fat
- cross BBB – CNS effects
Which BB has intrinsic sympathomimetic activity?
Pindolol (used in anxiety)