3.A-Hormone Pathways Flashcards

1
Q

What are the major hormones relating to blood pressure?

A

RAAS
sympathetic hormones (NE and epinephrine)
vasopressin (ADH)
peptide vasodilators (VIP, kinins, natriuretic peptides)
nitric oxide

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2
Q

Which tissues are influenced by epinephrine and norepinephrine?

A

heart (B1 receptors)
brains/CNS (a1 and a2 receptors)
lungs (B2 receptors)
kidney (B1 receptors)
blood vessels (a1 and B2 receptors)

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3
Q

Which drugs interfere with sympathetic nervous system actions?

A

beta-receptor antagonists
alpha-receptor antagonists
alpha-receptor agonists
(B2 agonists and a1 agonists augment SNS)

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4
Q

What happens when B1 receptors are activated in cardiac myocytes?

A

increased intracellular cAMP causing increased intracellular Ca which increases cardiac contractility and rate of contractions

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5
Q

What happens when B2 receptors are activated in smooth muscle cells of blood vessels?

A

increased intracellular cAMP causing decreased intracellular Ca which relaxes smooth muscle of the blood vessels (vasodilation)

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6
Q

Which receptors are blocked by beta-blockers?

A

B1
B2
a1

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7
Q

What do all beta-blockers end in?

A

-lol

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8
Q

What are the most common uses of B1 selective blockers?

A

high blood pressure (exact mechanism not clear)
high heart rate (tachycardia, tachyarrythmias)
cardiac workload/cardiac demand (angina)
cardiac damage (HF or heart attack)

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9
Q

Why are beta blockers used for cardiac damage?

A

if theres been damage to cardiac muscle, adrenaline can potentially worsen the damage so beta blockers act as a shield against the harmful effects of adrenaline

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10
Q

What are some B1 selective blockers?

A

bisoprolol
metoprolol
atenolol
acebutolol
esmolol

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11
Q

What are some non-selective beta-blockers?

A

nadolol
pindolol
propanolol
timolol

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12
Q

In addition to the effects that you would see through B1 antagonism, what are the effects of non-selective beta blockers?

A

smooth muscle:
-inhibition of B2 receptors in blood vessels, inhibiting
vasodilation
lung:
-inhibition of B2 receptors in airways

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13
Q

Are non-selective beta-blocker used for cardiac conditions? Why or why not?

A

rarely used for CV conditions anymore
theres very little benefit of non-selective beta-blockers over B1 selective blockers, also some tolerability issues

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14
Q

True or false: the selectivity between B1 and B2 is absolute

A

false
if you push the dose of a B1 receptor blocker, that agent will be become less selective

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15
Q

What are the non-selective beta and alpha blockers?

A

carvedilol
labetalol

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16
Q

What are the actions of non-selective beta and alpha blockers?

A

non-selective B1 and B2 inhibition
a1 receptor inhibition (vasodilatory effect)

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17
Q

True or false: there is a greater fall in blood pressure expected with non-selective beta and alpha blockers compared to other beta blockers

A

true

18
Q

What are cautions with the use of beta-blockers?

A

reduced blood pressure
reduced cardiac output
bradycardia (decreased HR)
heart block (AV block)
increased K
exacerbate circulation problems via B2 blockade (cold extremities)
theoretical interaction with respiratory medications
slight blood sugar increase possible

19
Q

What are the cautions in diabetics who are using beta-blockers?

A

reduced recognition of hypoglycemia
slight increase in blood sugar from vasoconstriction and reduced insulin release

20
Q

What is the mechanism of action of alpha-receptor antagonists?

A

inhibit vasoconstriction that is induced by the SNS

21
Q

After alpha-receptor antagonists have induced their action, what is often seen?

A

increases in HR, CO, and RAAS from the baroreceptor activation

22
Q

True or false: alpha-receptor antagonists are mainly used for BP control

A

false
mainly used for BPH

23
Q

What do all alpha-receptor antagonists end in?

A

-osin

24
Q

What are some alpha-receptor antagonists?

A

alfuzosin
doxazosin
prazosin
silodosin
tamsulosin
terazosin

25
Q

How do alpha-2 agonists work?

A

also called centrally-acting antihypertensives
lowering BP by affecting the brain
the a2 receptor is located on the pre-synaptic terminal and stimulation shuts down further release of messengers into the SNS nerve fiber

26
Q

What is the result of alpha-2 agonists?

A

decreased circulating NE and decreased SNS nerve transmission
lowers BP and HR

27
Q

What are side effects of alpha-2 agonists?

A

sedation
dry mouth (anti-cholinergic properties)

28
Q

What are two examples of alpha-2 agonists?

A

clonidine
methyldopa

29
Q

What are examples of endogenous peptide vasodilators?

A

vasoactive intestinal peptide (VIP)
kinins (bradykinin)
atrial natriuretic peptide (ANP)
brain natriuretic peptide (BNP)

30
Q

How do endogenous peptide vasodilators have relevance to drugs?

A

kinins, ANP, and BNP are all broken down by an enzyme called neprilysin

31
Q

What is an example of a neprilysin inhibitor? What is its partner drug?

A

sacubitril
valsartan

32
Q

What is sacubitril exclusively used for?

A

heart failure
no major effect on BP

33
Q

What is the action of nitric oxide?

A

a paracrine hormone synthesized by endothelial cells to signal smooth muscle cells to relax (vasodilation)

34
Q

Differentiate between paracrine, endocrine, and autocrine.

A

paracrine: affects cells in vicinity
autocrine: affects cell in which it is made
endocrine: secreted in blood for systemic effects

35
Q

How does relaxation result from nitric oxide?

A

activation of cGMP results in decreased cytoplasmic Ca which results in relaxation (vasodilation)

36
Q

What is the most common nitrate?

A

nitroglycerin

37
Q

Why is nitroglycerin not used for hypertension?

A

it causes vasodilation to veins thus little effect on BP

38
Q

True or false: nitrates are prodrugs that are converted to nitric oxide in the circulation

A

true

39
Q

If someone is using salbutamol and then they are prescribed either a non-selective beta-blocker (ex: propanolol) or a non-selective beta and alpha blocker (ex: carvedilol), what should warn this person about?

A

advise the patient to watch for a decreased response from their salbutamol
-non-selective beta blockers will inhibit B2 receptors in the
lung while the salbutamol is trying to activate the B2
receptors

40
Q

What is the effect of sacubitril on blood pressure?

A

no major effect on blood pressure

41
Q

What are the triggers of nitric oxide production in endothelial cells?

A

ACh
bradykinin
shear stress