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PHAMACOLOGY - Cardiology > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

What alpha blockers are used in the treatment of hypertension?

A
  • azosins
  • Prazosin
  • Doxazosin
  • Terazosin
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2
Q

What non-specific beta blockers are used in the treatment of hypertension?

A

-lol’s

  • Propanolol
  • Carvedilol
  • Pindolol
  • Timolol
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3
Q

What specific beta blockers are used in the treatment of hypertension?
• Which are 2st generation? 3rd generation?

A

-lol’s

  • Metoprolol (2nd gen)
  • Atenolol (2nd gen)
  • Bisoprolol (3rd gen)
  • Nebivolol (3rd gen)
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4
Q

What groups of drugs affect sympathetic activity in the nervous system?

A

Alpha and Beta Blockers

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5
Q

What 4 ace inhibitors do we need to know?

A

-pril’s

  • Captonopril
  • Lisinopril
  • Enalapril
  • Ramipril
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6
Q

What 5 AT-R blockers do we need to know?

A

–sARTan’s

  • Losartan
  • Valsartan
  • Irbesartan
  • Telmisartan
  • Candesartan
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7
Q

What drug acts as a renin inhibitor?

A

• Aliskerin

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8
Q

What are the 3 classes of Calcium Channel Blockers?

A
  • Phenylaklyamine
  • Benzothiazepine
  • Dihydropyridine
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9
Q

What drug falls under the category of a phenylalklamine?

A

• Verapamil

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10
Q

What drug falls under the category of a benzothiazepine?

A

• Dilatiazem

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11
Q

What are the 4 Dihydropyridines?

A

-dipine’s

  • Amoldipine
  • Nifedipine
  • Nicardipine
  • Nimodipine
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12
Q

What 2 drugs act as alpha-2 agonists?

A
  • Clonidine

* Methyldopa

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13
Q

What drugs act as Direct Vasodilators?

A
  • Minoxidil
  • Na-Nitroprusside
  • Hydralazine
  • Fenoldopam
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14
Q

Who should be put on blood pressure medicine according to JNC VIII?

A

Give Therapy
• Pts. older than 60 with 150/90
• Pts. under 60 with greater than 90 diastolic

Probably Don’t Give therapy
• Systolic of less than 140 is not

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15
Q

Alpha-1 Adrenergic Receptor Blockers
• Mechanism of Action
• Pharmacological Effects (specify by drug)

A

MOA:
• Block alpha-1 receptors on peripheral arteries and veins causing vasodilation

Phamacological Effects:
• PRAZOSIN - reduction in TPR and BP
• TERAZOSIN and DOXAZOSIN - Benign Prostatic Hyperplasia (BPH)

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16
Q

Alpha-1 Adrenergic Receptor Blocker
• Side effects
• Clinical Utility in HTN

A

Side Effects:
• First Dose Hypotension (orthostatic) so give at BEDTIME

Clinical Utility:
• NOT FRONT LINE IN TREATMENT OF HTN

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17
Q

Which of the Beta blockers are CARDIOSELECTIVE?

A

BisAM!!!

  • Bisoprolol
  • Atenolol
  • Metoprolol (also lipid soluble)
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18
Q

Which of the Beta blockers are most LIPOPHILIC?

A

Most:
• Propanolol
• Metoprolol

Pretty Lipophilic:
• Pindolol
• Timolol

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19
Q

Which of the Beta blockers show ISA (intrinsic sympathomimetic activity)?

A

Pindolol (and acebutolol)

Agonizing Ace-Pin

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20
Q

Which Beta Blockers would you definitely not want to use on someone with asthma?

A

Any of the 1st generations or non-specific 3rd generations

  • Propanolol
  • Timolol
  • Pindolol
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21
Q

What Beta blocker would you use in pheochromocytoma or in preeclampsia?
• Drug Selectivity?
• Administration?

A

Labetalol - given IV in emergencies

Selectivity: Non-selective ß; Alpha-1 selective

“Labor-talol”

Note: Non-specific alpha and beta blockers must be given in pheochromocytoma because of excessive catecholamine stimulation that would happen on unblocked receptors*

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22
Q

What is one of the best Beta blockers you could give someone with Congestive Heart Failure?
• Drug Selectivity?
• why?

A

Best Beta Blocker = Carvedilol

Selectivity: Non-selective ß; Alpha-1 selective

Why:
• Antioxidant (scavenges ROS) => Protects membrane from lipid Peroxidation
• REDUCES LDL uptake in to coronary vessels

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23
Q

Nebivolol
• Selectivity
• Extra Functions?

A
  • BETA-1 SELECTIVE

* stimulates NO production for Vasodilation

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24
Q

For Beta Blockers with NO sympathomimetic activity what is there general function on:
• Heart
• Kidney

***what patient population benefits the most from the use of these drugs?

A

Heart:
Function to Block Beta-1 activity causing:
• Decreased HR (less active Funny Channels b/c less cAMP)

  • Decreased Contractility (Calcium Channel and Calcium channel inhibitor not phosphorylated by cAMP dependent Kinsase)
  • Reduced Cardiac Output

Kidney:
• Decreased Renin secretion from Juxtaglomerular App.

Most useful in patient with HIGH RENIN HYPERTENSION

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25
Q

Clinically, when are Beta blockers used?

• do they need to be administered with diuretics?

A

JNC says you shouldn’t generally use Beta Blockers as First line therapy and IF you do, then used 3rd generation (less side effects)

• NO - beta blockers CAN be administered with diuretics but this is not necessary

if they are given with a diuretic, then the effect is additive

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26
Q

In what cases would use of a Beta blocker be preferred to the use of other antihypertensives?

A

Beta Blocker HIGHLY PREFERRED in cases of:
• Myocardial Infarction (MI)
• Ischemic Heart Disease
• Congestive Heart Failure

PREFERRED in cases of:
• Hyperthyroidism
• Migraines

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27
Q

Specifically what Beta blocker would you used in Congestive Heart Failure?

A
  • Carvedilol (reduction of LDL, and antioxidant effect)

* Metoprolol-XL (long acting)

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28
Q

What Beta blocker would you use in Open Angle Glaucoma?

A

Timolol

29
Q

Besides use to prevent HTN, what can Beta Blockers be used for?

A
  • Myocardial Infarction
  • Congestive Heart Failure
  • Open Angle Glaucoma
  • Stage Fright
  • Altering Memory
30
Q

Which Beta Blockers have the most adverse effects?

A

• First and Second Generation

31
Q

What are some side effects of using beta blockers?

4 major effects

A
  • COLD EXTREMITIES (more alpha-1 acted on by Catelcholamines => peripheral constriction, more blood in central compartment)
  • BRADYCARDIA (less AV nodal conduction)
  • CNS EFFECTS (Bad Dreams), depression
  • METABOLIC EFFECTS - Blocks glycogenolysis, Blocks HSL in adipocytes, increased LDL, Reduced HDL, Increased TGs
32
Q

T or F: its okay to pull someone off their Beta blocker if they experience a lot of adverse effects?

A

False, you should taper the drug back slowly

33
Q

What does ACE act on?

A

Angiotensin Converting Enzyme (ACE) works on… Angiotensin I

**Also acts on Bradykinin which is counterproductive to the overall effects of the drug because Bradykinin is important for vasodilation*

34
Q

T or F: angiotensin II is the most potent vasoconstrictor we have.

A

True

35
Q

How do the “prils” act to depress blood pressure?

A

prils = ACE inhibitors

  1. Prevent Angiotenin I conversion to Angiotensin II
  2. Depress Aldosterone (Temporary effect only)
  3. Increase RENAL blood flow but not GFR
  4. RENOPROTECTIVE - increased prostaglandin synthesis
36
Q

What are the pharmacological effects of the ACE inhibitors?

A
  • angiotensin effects inhibited, No BV thickening
  • ARTERIES AND VEINS DILATED
  • NO Postural HYPOTENSION
  • CHF = increased longevity
37
Q

Why is dilation of both arteries and vein important in CHF?

• why is postural hypotension not an issue?

A

CHF:
• ARTERIAL dilation = REDUCED afterload
• VENOUS dilation = INCREASED preload

Postural Hypotension:
• Baroreceptors are not effected so body can change vessel tone on standing

38
Q

How can angiotensin cause venous thickening?

A

• Activation of PKC which acts as a growth factor

39
Q

What are 5 effects of angiotensin II?

A
  • Cardiac and Vascular Hypertrophy
  • Release of ADH (antidiuretic hormone) from Hypothalmus
  • Release of Aldosterone from Adrenal Cortex
  • Systemic Vasconstriction
  • Increase Thirst
40
Q

Which of the Ace inhibitors are pro-drugs?

A

RamEn

Prils that require activation in LIVER
• Ramipril
• Enalapril

***Advantageous because of long half life

41
Q

What are some important side Effects of ACE inhibitors?

A
  • Hyperkalemia (monitor close in ppl. taking K+ or using K+ diuretics)
  • Dry Cough (related to inhibition of bradykinin)
  • Angioedema (also may be related to bradykinin)
  • Fetotoxicity
  • RENAL DYSFUNCTION (monitor SERUM CREATININE)
42
Q

What would you substitute for an ACE inhibitor in a patient who experienced dry cough?
• Why?

A
  • Angiotensin Receptor Blocker (ARB)
  • ARB’s do not change the activity of ACE on Bradyknin

Could give to patient that experience ACE induced angioedema, BUT chance of Recurrence is 1/10

43
Q

What is the MOA of the -sartans?

• Major Contraindication in all Sartans?

A
  • Blockage of Angiotensin II Receptors
  • Induce Vasodilation and increased Na+ and H2O secretion

Contraindication:
• FETOTOXICITY

44
Q

Losartan
• Drug Class
• Unique Features

A

Drug Class:
• Angiotensin Receptor Inhibitors

Unique Features:
• PROMOTES Urinary excretion of Uric Acid
• Competitive TXA2 antagonist (thus, prevents platelet aggregation)

45
Q

Which of the Calcium Channel Blockers would be most effective in the treatment of hypertension?
• Why?
• MOA of Calcium Channel Blockers?

• Name all 3 classes

A

Dihydropyridines = Most Effect because they act mostly on the VASCULATURE

MOA:
• Blockage of L-type Ca++ Channels prevents Smooth Muscle contraction

3 Classes:
• Dihydropyridines
• Benzothiazepines (Heart)
• Pheynlalkylamines (Heart)

46
Q

What patients respond best to Blood Pressure therapy by Ca++ Channel Blockers?

A

Patients with LOW RENIN HYPERTENSION

  • Elderly Patients - ESPECIALLY THOSE WITH SYSTOLIC HYPERTENSION
  • African Americans
47
Q

Dihydropyridine Effects on:
• Blood Pressure
• Heart

A

Blood Pressure - Reduced by smooth muscle relaxation (calcium channel blocked)

NO EFFECT ON HEART rate because no baroreceptor-mediated discharge

48
Q

How does the action of clonidine and methyldopa differ from that of many other drugs that work on alpha and beta receptors?

A
  • These drugs act mainly through the CNS

* Specifically they are alpha-2 agonists

49
Q

When would you use clonidine in antihypertensive therapy?

• what are some of the adverse effects?

A

Tertiary Use in HTN (would be the 3rd drug you added to a combo. to lower BP)

Side Effects:
• Sedation (drowsiness, fatigue, erectile dysfunction)
• HYPERTENSION ON WITHDRAW

50
Q

Clonidine

• MOA

A

• Agonists of Postsynaptic Adrenoreceptors in the Rostral Ventrolateral Medulla (RVLM)

  • DECREASE sympathetic impulses from RVL Medulla to Heart and BVs
  • DECREASE in peripheral Vascular Resistance and DECREASE in HR.
51
Q

Hydralazine
• Drug Class
• MOA
• Side Effects

A

Drug Class:
• Vasodilator

MOA:
• Arteriolar Smooth Muscle Relaxer
• REFLEX sympathetic stimulation
• Increases Catacholamine/Renin Release

Side Effects:
• Tachycardia (from reflex sympathetic stimulation)
• DRUG INDUCED LUPUS (autoimmune rxn)

52
Q

Fenoldopam
• Drug Class
• MOA
• Utility

A

Drug Class:
• Vasodilator

MOA:
• Partial Agonist of D1

Utility:
• Good in Hypertensive Emergencies

53
Q 
MINOXIDIL
• Drug Class
• MOA
• Utlility 
• Adverse Effects
A

Drug Class:
• Vasodilatory

MOA:
• Opens up ATP K+ channels to Relax Smooth muscle
• ONLY ACTS ON ATERIOLES (no veins) causes REFLEX sympathetic stimulation => Renin/Catecholamine Secreteion

Utility:
• ONLY USED IN SEVERE HTN (very rarely used)

Adverse Effects:
• HIRSUTISM

54
Q

Which of the vasodilators are sometimes used in preecampsia?

A

• Hydralazine

55
Q

Why vasodilators often have to be used in combination with other drugs?
• what other drugs are they administered with?

A
  • Reflex Sympathetic Stimulation = major problem for the vasodilators
  • BETA blockers and Diuretics are typically administered to prevent the sympathetic system from kicking in and to attenuate the effects of hypervolemia (diuretics)
56
Q

Nitroprusside
• MOA
•Difference between Nitroprusside and most vasodilators?

A
  • Nitric Oxide Pro-drug
  • Stimulates GUANYLATE CYCLASE in smooth muscles
  • more cGMP = smooth muscle Relaxation

Nitroprusside stimulates BOTH arterial and venous relaxation

57
Q

Nitroprusside
• Pharmacological Effects (CHF vs. Normal pts)
• Utility
• Side Effects

A

Pharm Effects:
• Reduction in TPR and Increased in Venous Pooling
• Normal people = Reduced CO
• Left Ventricular Failure = Increased CO

Utility:
• given IV in HYPERTENSIVE EMERGENCIES

Side Effects:
• Cyanide Accumulation in patients with RENAL FAILURE

58
Q

How useful are diuretics in the treatment of HTN?

• Most common diuretic?

A
  • Very Effective - they can either be used alone or in combination with other drugs
  • MORE effect that CCB (calcium channel blockers) or ACE inhibitors

Most Common:
• Thiazide-Type Diuretics

59
Q

What groups of Hypertensive patients would you want to give Diuretics to in addition to other therapies?

A

Pts. with Edematous Conditions
• Heart Failure
• Renal Insufficiency

Pts. with Low Renin HTN
• AFRICAN AMERICANS
• OLD PEOPLE

60
Q

Why might a patient respond as expected to thiazide diruretics?

A
  • May eat too much Sodium

* May not have renal capacity to excrete sodium (old ppl)

61
Q

Over how many days should you taper the dose of a Beta Blocker?

A

• 10-14 days

62
Q

What is the MAJOR advantage to using a beta blocker to treat HTN?

A

• Protection is conferred against Coronary Artery Disease as well

**Usefule in hyperthyroidism, migraine, and glaucoma

63
Q

What is the 1st line therapy against essential hypertension?
• Ideal patient to use these drugs on

A

Ideal Patient:
• Young and Middle Aged Caucasians

  • ACE Inhibitors
  • ARBs
64
Q

In what patients is it particularly necessary to administer a Thiazide along with their ACE inhibitor?

A

• African Americans

*Typically you will want to use a Calcium Channel Blocker in this population

65
Q

T or F: Beta blockers are 1st line antihypertensive therapy for people with CHF.

A

False, ACE inhibitors and ARB’s should be 1st line antihypertensive therapy in these patients

ALSO 1st LINE THERAPY IN PATIENTS WITH NON-DIABETIC NEPHROPATHIES or CHRONIC KIDNEY DISEASE*

66
Q

In what cases would you defer from using ACE inhibitors, Renin inhibitors, and ARB’s as 1st line therapy?

A
  • People that Hyperkalemic

* Pregnant women/ANY woman of CHILDBEARING age

67
Q

What are the 4 Dihydropyridine calcium channel blockers?
• Which SHOULD NOT be used in treatment of HTN?
• why not?

A

Amoldipine
Nicardipine
Nimodipine
Nifedipine***

*Don’t use Nifedipine - its too SHORT ACTING

68
Q

T or F: if someone is hypertensive you’ll want to start them on the full effective dose immediately.

A

False, must buildup slowly or these people will get problems with Sexual Dysfunction and Headaches etc.

PHAMACOLOGY - Cardiology (11 decks)

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