Beta Blockers Flashcards
Epi vs. NE R Specificity
Beta more vs. alpha more
Beta Subtype Distribution (& how CAT specificity is affected)
More Beta1 in heart causing increased HR and contraction
More Beta2 in periphery for dilatation and relaxation
So epi infusion gives you increased HR and peripheral dilatation, and NO gives you increased HR and constriction
BetaR Sensitization
Agonists desensitize by ligand dependent phospho and internalization w/ chronic stress, so myocardium in heart failure unresponsive to epi and Beta agonists. Antagonists allow re-sensitization and heart failure saving
Effect of Beta Blockers on HR
Put a “ceiling” on HR, don’t actively lower below pacemaker intrinsic rate
6 Indications for BBs
HTN Chronic CHF Afib Symptomatic premature beats (ectopy) Perioperative cardioprotection Prevention of post-MI remodeling
BBs in HTN
Pretty shitty because BP determined more by PVR. Might work for people who get super pissed off easily
2 Anti-B1 Selective Drugs
Atenolol
Metoprolol
Use of Anti-B1 Selective Drugs
Slow HR and contractility and don’t want to block B2s in asthmatics
Use of Anti-B2 Selective Drugs (2)
Vasoconstrictor effects and reduce intraocular pressure
Polarity Spectrum
More polar (atenolol) have decreased excretion and fewer CNS effects. Less polar (propanolol) are opposite
Inverse Agonist Effect
Lock R in inactive configuration, preventing intrinsic rate
Anti-Arrhythmic Effects of BBs (all and 1 specific)
All slow AV node conduction (prevent Afib irregular contractions)
Sotalol blocks K channels so used for Vfib
B Adrenergic Activation in CHF
Get R loss and tachycardia, and then Ca overload causes arrhythmias and can lead to sudden death (overtime!)
Chronic Beta R Stimulation Worsening Heart Failure
Get abnormal myocyte growth, leading to energy inefficiency, leading to myocyte death, leading to replacement myocardial fibrosis/adverse remodelling and scarring
BBs in CHF
Slow HR and permit longer filling times and prevent all that other shit I just talked about. In general BBs prevent mortality from heart failure by about one metric assload