Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Cardio Block > Antihypertensive Drugs > Flashcards

Antihypertensive Drugs Flashcards

0
Q

Alpha1 Adrenergic Receptor Blockers: Pharmacological Effects

A

Decrease TPR and reduce BP
Relieve symptoms of benign prostatic hyperplasia (BPH) by relaxing the muscles of the bladder and prostate
Increase HDL-C and lower LDL-C, and also have beneficial effect on insulin resistance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
1
Q

Alpha1 Adrenergic Receptor Blockers: MOA

A

Block alpha1 adrenergic receptors in arteries and veins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Alpha1 Adrenergic Receptor Blockers: Side Effects

A

First-dose hypotension with prazosin

Give drug at bedtime

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Alpha1 Adrenergic Receptor Blockers: Clinical Uses

A

Not recommended as monotherapy for HTN primarily as a consequence of ALLHAT study

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Beta Blockers: MOA

A

Block myocardial B1-adrenergic receptors
Decrease HR and Contractility –> Decrease CO
Block beta-1-AR in the JGA and therapy inhibit renin release
Very useful in patients with high renin HTN, but work well in hypertensive patients with normal-low renin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Beta Blockers: Clinical Use

A

Provide effective therapy for all grades of HTN
BB do not cause retention of salt and water and can be administered without a diuretic. However there anti-hypertensive effect is additive with a diuretic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are some additional uses of Beta Blockers?

A 
CHF 
MI
Sinus and AV arrhythmias
Open angle glaucoma
Additional off label uses include stage fright, altering memory
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are some compelling indications for the use of BB

A

Highly preferred in hypertensive patients with conditions such as MI, IHD or CHF.
Preferred in hypertensive patients who have hyperthyroidism and migraines (compelling indication)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Beta Blockers: Side Effects

A

Can affect 40-50% of patients
Cold extremities: worsens peripheral arterial insufficiency
Bradycardia: decrease AV nodal conduction
Bronchospasm: avoid with asthma; OK in COPD
CNS side effects: bad dreams, depression
Metabolic effects:
- block glycogenolysis and delay recovery from hypoglycemia in type I diabetics (not seen with B1-blockers)
- block HSL in adipocytes and increase LDL and reduce HDL and increase TGs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What happens with BB withdrawal?

A

DRUG WITHDRAWAL SYNDROME - prolonged drug use upregulated B-receptors in the heart. Abrupt withdrawal causes tachycardia, so WITHDRAW SLOWLY!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Name the 3rd Generation Drugs with Combined Alpha/Beta Blocking Activity

A

Labetalol
Carvedilol
Nebivolol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Labetalol

A

non-selective beta and alpha1-receptor antagonists

given IV for HYPERTENSIVE EMERGENCIES

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Carvedilol

A

Non-selective B and alpha1 receptor antagonist
Antioxidant - binds and scavenges ROS
Protects membranes from lipid peroxidation. Prevents LDL oxidation and decreases LDL uptake into coronary blood vessels.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is Carvedilol primarily used for?

A

Primarily used for CHF and HTN; decreases mortality and morbidity in patients with mild to moderate CHF.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Nebivolol

A

Highly B1 selective; with NO-mediated vasodilation
Promotes endothelial NO-mediated vasodilation
Has antioxidant activity/neutral to favorable effects on both carbohydrate and lipid metabolism.
Significantly increase SV, maintains CO and systemic blood flow

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is Nebivolol primarily used to treat?

A

HTN with metabolic syndrome!

Best drug to treat metabolic syndrome because it lowers the BP without affecting the LDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

ACE Inhibitors: MOA

A

Inhibit conversion of ATI to ATII and degradation of the potent vasodilator bradykinin
Secretion of aldosterone is decreased, but not seriously impaired
ACEI increases renal blood flow without an increase in GFR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

ACE Inhibitors: Pharmacological Effects

A

Inhibit all known effects of ATII
Dilate arteries and veins (basis for their use in CHF)
Reduced BP rarely followed by a minor increase in HR.
Baroreceptor mechanisms remain intact, no postural hypotension
Reduce ATII-mediated thickening of BV
Associated with positive impact on longevity in CHF

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is Captopril the preferred drug for?

A

Captopril increases synthesis of renal prostaglandins. Delays progression of renal disease in diabetics (renoprotective)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

ACE Inhibitors: Side Effects

A

Hypotension in hypovolemic and/or Na+ depleted patients
Hyperkalemia (especially with renal insufficiency, or in patients receiving K+ sparing diuretics or K+ supplements)
Dry cough (most common), angioneurotic edema or angiodema; both related to bradykinin actions.
Angioedema: infrequent but potentially fatal (reported with all ACEI)
Fetotoxicity: contraindicated in 2-3 trimesters

20
Q

What does bradykinin do and why does it matter with ACEI?

A

Bradykinin activates stretch receptors in the trachea, which might cause dry cough in 10-15% of patients receiving ACEI.

21
Q

ARBs: MOA

A

Selectively block ATII type I receptors, which are responsible for all of the effects of ATII
Cause vasodilation and increased Na+ and water excretion. Thus, they decrease TPR, plasma volume, CO, and BP
Have no effect on bradykinin, therefore they are THE substitute when ACEI causes cough

22
Q

Losartan

A

Pro-drug that is metabolized to active product
Competitive antagonist of TXA2 receptor; attenuates platelet aggregation.
**Unique in that it increases uric acid urinary excretion (Uricosuric so used in hypertensive patients with gout)

23
Q

Which of the ARBs does not affect uric acid or CYP enzymes, but what is their main side effect?

A

Irbesartan, valsartan and telmisartan DO NOT affect uric acid or CYP enzymes. Fetotoxicity is their main side effect!

24
Q

Name the 3 classes of calcium channel blockers (CCBs)

A

Phenylalkylamines: Verapamil
Benzothiazepines: Diltiazem
Dihydropyridines

25
Q

How do the 3 classes of CCBs differ?

A

Differ in basic chemistry and in relative selectivity for cardiac vs. vascular L-type Ca2+ channels

26
Q

Phenylalkylamines

A

Verapamil

Relatively selective for myocardium; less effective as systemic vasodilator.

27
Q

Benzothiazepines

A

Diltiazem

Intermediate between verapamil and dihydropyridines in its selectivity for vascular Ca2+ channels.

28
Q

Dihydropyridines

A

Selectively block L-type Ca2+ channels in blood vessels.

Used for HTN because they decrease SVR and arterial pressure

29
Q

Pharmacology of Dihydropyridines

A

CCB decreases BP by relaxing arteriolar smooth muscle cells and decreasing PVD.
Do not cause a large baroreceptor-mediated sympathetic discharge and changes in HR are usually mild to nonexistent

30
Q

Clinical uses of CCBs

A

More effective in decreasing BP than other drugs in patients with low renin HTN such as elderly subjects and in AA (typically have resistant HTN)
Preferred in older subjects with systolic HTN
No survival benefit demonstrated in large cohort studies

31
Q

Name the centrally acting alpha2A agonists

A

Clonidine
Guanfacine
Guanabenz

32
Q

What is the actions of centrally-acting alpha2A agonists

A

Agonists of postsynaptic alpha2A-adrenoceptors in the rostral ventrolateral medulla (RVLM)
Decrease sympathetic impulses from RVLM to heart and blood vessels
Decrease in peripheral vascular resistance and decrease in HR

33
Q

What is the use of the alpha2a agonists

A

Clonidine releases endogenous opiates; used as analgesic in neuropathic pain and is approved for treatment of ADHD
Tertiary use in HTN, i.e. used in triple combinations

34
Q

Side effects of alpha2A agonists

A

***SEDATION (less so with Guanfacine), drowsiness, fatigue

Clonidine withdrawal –> HTN; withdraw slowly

35
Q

Hydralazine MOA

A

Selective arteriolar smooth muscle relaxer; triggers reflex sympathetic stimulation –> increase catecholamine/renin secretion

36
Q

Hydralazine clinical uses

A

IV in hypertensive emergency from eclampsia

Reflexively activates SNS and causes Na+ retention -> used with BB and diuretics

37
Q

Hydralazine side effects

A

Palpitations; pronounced tachycardia (may trigger angina)

Autoimmune reactions: hemolytic anemia

38
Q

Minoxidil MOA

A

Relaxes arteriolar smooth muscle by opening K+ATP potassium channels in smooth muscles
Dilates arterioles but not veins, causes reflex tachycardia and is a powerful activator of renin secretion

39
Q

Minoxidil Side Effects

A

Increase renin

Causes hirsutism

40
Q

Nitroprusside MOA

A

Mainly works as a pro-drug
Forms NO, which stimulates smooth muscle guanylate cyclase
Increase levels of cGMP in vascular smooth muscle
Causes relaxation

41
Q

Nitroprusside Pharmacological Effects

A

Dilates both the arteries and veins
Reduces TPR and induces venous pooling
Decreases CO in normal subjects but increases CO in patients with LV failure because TPR (i.e. afterload) is reduced
Has very short half-life and is given IV for hypertensive emergencies in patients with ventricular failure

42
Q

Explain the rationale for using diuretics for HTN

A

Can be used as monotherapy or adjunctive with other antihypertensives; augment the actions of all antihypertensives
Diuretics, alone or with BBs decrease mortality in patients with HTN
Diuretics (low doses) and ACEIs are the best tolerated drugs for monotherapy of HTN
Patients with edematous conditions (HF and renal Insufficency) frequently require a diuretic for optimal control of BP

43
Q

Discuss the major therapeutic advantages of BBs

A

Secondary protection in CAD!
Particuarly useful in hypertensives with tachycardia, high CO, and/or high renin. Less effective in AA and the elderly.
Very useful in hypertensives with hyperthyroidism, migraine, glaucoma.

44
Q

Which is preferred - older generation BBs or 3rd generation BBs

A

3rd generation BBs are preferred d/t substantially fewer side effects

45
Q

What BB is considered as standard treatment option with ACEIs and diuretics?

A

Bisoprolol (b1 blocker)

46
Q

What are ACEI and ARBs useful in the management of?

A

Useful in the management of all degrees of HTN, but superior in hypertensives with high renin levels (young people and middle-aged Caucasians).
Increase the efficacy of diuretics.
Should be the initial antihypertensive drug in diabetic patients with HTN, following which, it is appropriate to consider adding a CCB if a second drug is needed.
May also preserve renal function in patients with nondiabetic nephropathies (Captopril)
Should be chosen as initial antihypertensive drug in patients prone to CHF

47
Q

When should you avoid the use of ACEI and ARBs

A

Avoid in any condition that may cause hyperkalemia

Contraindicated in pregnancy (exposure to ACEI/ARBs at conception appears to be safe)

Cardio Block (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions