All CV Drugs Flashcards
Inhibits the synthesis of ACh by inhibiting transport of choline into neurons
Hemicholinium
Inhibits the synthesis of ACh by inhibiting the packaging of ACh into storage vessicles
Vesamicol
Inhibits ACh function by inhibiting the release of ACh from neurons
Botox
How is ACh terminated? What enzyme?
ACh esterase
Inhibits formation of NE by inhibiting the enzyme tyrosine hydroxylase
Metyrosine
Inhibits formation of NE by preventing the transport of dopamine into storage vesicles
Reserpine
How is NE terminated?
Diffusion & Reuptake (unlike ACh which is metabolized by ACh esterase)
What drugs inhibit the reuptake of NE?
Cocaine & antidepressants
Once outside the synaptic cleft, however, NE is metabolized by?
MAO & COMT
24 hour levels of what give you a picture of the total body catecholamines?
VMA
This drug blocks NE synthesis by inhibiting tyrosine hydroxylase
Metyrosine
This drug blocks NE storage
Reserpine
This drug blocks NE release
Guanethidine
M1 muscarinic receptors are excitatory or inhibitory?
Excitatory!
M2 muscarinic receptors are excitatory or inhibitory?
Inhibitory :(
M1 muscarinic receptors are Gq coupled or Gi coupled?
Gq coupled… leads to increased IP3, increased phospholipase C, DAG cascade –> increase in intracellular Ca2+
M2 muscarinic receptors are Gq coupled or Gi coupled?
Gi… decrease cAMP and decrease HR
Alpha 1 receptor excitatory or inhibitory?
Excitatory; increases IP3 and DAG.. on post-synaptic neuron
Alpha 2 receptor excitatory or inhibitory?
Inhibitory; decreases cAMP… on pre-synaptic neuron as a negative feedback mechanism
What drugs treat pheochromocytoma?
NE blocking drugs: Metyrosine, Reserpine, Guanethidine
This beta blocker lowers BP in pts with increased renin
Propranolol
This beta blocker lowers BP in pts with normal renin
Pindolol
If someone is on a beta blocker, can you abruptly take them off of it?
Hell no! They could die a sudden death
Beta blockers have many “off target” effects. What is a beta blockers off target effect in the respiratory system?
Beta blockers cause bronchoconstriction; contraindicated in asthmatics
What is an off target CNS effect for beta blockers?
mental disorders, vivid dreams
beta blocker off target glucose effect?
hypoglycemia; Beta1 blockers mask the tachycardia that normally lets diabetics know that they are hypoglycemic
beta blocker off target lipid profile?
Beta blockers mediate lypolysis leading to increase TG and decreased HDL
HTN, post-MI, anxiety, migraines, esophogeal verices, CHF, hyperthyroidism, and glaucoma are clinical uses of?
Beta blockers
Beta receptors are divided into B1 and B2. B1 is found primarily in?
Cardiac muscle and JGA; increases HR and renin release when stimulated
B2 receptors are found primarily in?
Skeletal muscle; vasodilates skeletal muscle
Beta blocking drugs end in?
lol “I laugh out loud at beta blockers”
These beta blockers have a much higher specificity for B1 receptors
A-N
These beta blocker have equal affinity for B1 and B2 receptors
O-Z
Beta blocking drugs are grouped by different functions. Some have membrane stabilizing activity meaning they decrease the slope of phase O
Pro Ace Carver: Propranolol, Acebutolol, Carvedilol
Some beta blocking drugs have intrinsic sympathomimetic activity (ISA)
Ace Labeled 2 Pens in the Cart: Acebutolol, Labetalol, Pindolol, Penbutolol, Carteolol
Some beta blocking drugs are lipid soluble and can penetrane the BBB
Tim Met 3 People: Timolol, Metoprolol, Pindolol, Propranolol, Penbutolol
Which beta blockers induce NO (nitrous oxide) production?
NC: Now Cart this weight because you take NO: Nebivolol, Carteolol
This beta blocker is unique in that it actually activates beta 2 receptors while blocking beta1 receptors
Celip beta 2 in the Cart: Caliprolol, Carteolol
These two beta blockers are alpha1 receptor antagonists
LC: Labetolol, Carvedilol (Carvedilol is highly protein bound and has antioxidant activity)
this beta blocker blocks Ca2+ entry
Betaxolol & Carvedilol… it be taxin and Carvin those Ca2+ channels.
this is a particularly long acting beta blocker that decreases all mortality and treats glaucoma
Bisoprolol.. biso longo!
this beta blocker has a very short half life and is given IV
Esmolol… es muy pequino half life
this beta blocker treats open angle glaucoma
timolol; also long acting bisoprolol
In general side effects of beta blockers
cold extremities (Raynaud’s), bradycardia, bronchospasm, bad dreams, hypoglycemia, drug withdrawl syndrome
Do beta blockers cause salt and water retention?
No, so it is not necessary to co-prescribe a diuretic but it can still be helpful
Beta blockers are preferred in HTN pts who also have?
CHF, MI, hyperthyroidism, migraines
Drug of choice for metabolic syndrome
Nebivolol
Labetolol and Carvedilol (LC) are both beta blockers that also block alpha 1 receptors. Which of these is highly protein bound?
Carvedilol.. Carve sounds like carne (spanish for meat = protein).. it also has antioxidant properties
This beta blocker is a beta 1 blocker that has beta 2 agonist activity
Celip beta 2 in the Cart: Celiprolol, Cartedilol
Beta blockers are contraindicated with what two drugs?
Varapamil, Deltiazem
Difference between first/second generation beta blocker and third generation?
First/second are good for high renin HTN; 3rd generation best for CHF
