Part 23: Vasodilators Flashcards
in vascular smooth muscle, the interaction between ___ and ___ causes contraction, resulting in vasoconstriction
myosin and actin
during membrane depolarization of vascular smooth muscle cells, large amounts of ____ ions come in through ____ channels
Ca; voltage gated Ca channels
Ca can also enter BV smooth muscle cells through the ___- exchanger where ___ is removed from the cytoplasm and ca enters
Na/Ca (NCX); Na
compared to the voltage-gated Ca channels, the NCX is a ____ (major/minor) contributor of Ca influx
minor
when might there be reduced removal of Na from the cells and entry of Ca by the NCX?
if the patient is taking a diuretic that depletes the body’s Na
when diuretics indirectly affect the NCX does it cause a vasodilator or vasoconstrictive effect?
vasodilator
the guanylyl cyclase pathway promotes vasodilation by increasing _____ of myosin, which releases the contractile stste of the smooth muscle cell
dephosphorylation
organic nitrates like ____ act in this pathway to cause vasodilation in patients with angina
nitroglycerin
what drug class does prazosin belong to?
alpha 1 adrenergic receptor antagonist (antihypertensive)
what is the MOA of alpha-1 antagonists like prazosin?
competes for binding to the A1 receptor and prevents endogenous action of NE secreted by sympathetic neurons and results in less Ca for contraction
activation of the alpha 1 receptor causes a _____coupled signalling cascade
Gq
a rise in intracellular Ca results in activation of mysoin ____
light chain kinase
while some Ca may come in by the NCX, most of the Ca enters through _____ channels
L-type voltage gated Ca channels
if we can block Ca channels, there will be less calcium ____ activation and a reduction in myosin _____ activity
calmodulin; light chain kinase
what are the 2 types of Ca channel blockers?
- dihydropyridine (DHP)
2. non-dihydropyridine
what class of drug does nifedipine belong to?
dihydropyridine type Ca channel blockers (vasodilator; antihypertensive)
what class of drug does diltiazem belong to?
non-dihydropyridine type Ca channel blocker (vasodilator; antihypertensive)
what is the clinical distinction between DHP and non-DHP Ca channel blockers?
DHPs are only effective in blocking Ca channels in smooth muscle cells, but not those in cardiac muscle cells, but non-DHP act in both
blocking Ca channels in cardiac muscle cells generally causes a _______ (increase/decrease) in the activity of these cells
decrease
why are non-DHPs like diltiaem not typically used?
they can block ca channels in the heart wich reduces activity of heart cells
what are some of the common ADRs of vasodilators?
orthostatic hypotension, dizziness, headaches, bradycardia, cardiac suppression, urinary incontinence
what is the severity of hypotension, dizziness and headaches ADRs of vasodilators?
usually not serious, typically resolves over time, but if it doesnt resolve some ptaintes may need dose adjustments
bradycardia & cardiac suppression as ADRs are typically seen with what types of vasodilators?
non-DHPs like diltiazem
urinary incontinence as an ADR is typically not severe and is typically caused by what class of vasodilators?
A1 andronergic blockers also acting in other smooth muscle like prazosin
t/f prozosin can be used for the treatment of urinary retnetion
t
t/f vasodilators alone are typically not enough to manage hypertension
t