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Systemic Pharmaco > Anti-Hypertensives > Flashcards

Anti-Hypertensives Flashcards

1
Q

What is defined as hypertension?

A

> 140/90mmHg

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2
Q

What are some consequences (sequelae) of hypertension?

A
  1. Congestive heart failure
  2. Myocardial infarction
  3. Renal damage
  4. Cerebrovascular accidents (eg. stroke)
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3
Q

What are the major factors affecting blood pressure?

A

BP = CO x TPR

  • Preload (ventricular filling - HR, contractility, filling pressure)
  • Afterload (vascular tone - peripheral resistance)
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4
Q

What are the 5 main groups of drugs used in hypertension?

A
  1. Diuretics
  2. Sympathoplegics (ß blockers)
  3. Vasodilators (nitrates)
  4. Angiotensin antagonists (ACE inhibitor, AT1-R blocker)
  5. Calcium channel blocker`
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5
Q

How is blood pressure controlled? (mechanisms)

A
  1. Sympathetic activity (ß1AR of heart, a1AR in SM) - rapid moment-to-moment
  2. RAAS (renin, aldosterone) - long-term
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6
Q

What are the determinants of vascular tone (contraction & relaxation)?

A

Myosin-LC

  1. Ca2+, calmodulin
  2. Adenylyl cyclase, cAMP, PKA
  3. Nitric oxide, guanylyl cyclase, cGMP
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7
Q

What are the ACE inhibitors?

A

Captopril
Enalapril
Ramipril
Lisinopril

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8
Q

What is the MOA of ACE inhibitors?

A
  1. Decrease ANGII

2. Decrease inactivation of bradykinin, bradykinin accumulates, increase in NO, PG

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9
Q

What are the clinical uses of ACE inhibitors?

A
  1. Hypertension
  2. Cardiac failure
  3. Following MI
  4. Renal insufficiency
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10
Q

What are the adverse effects of ACE inhibitors?

A
  1. Severe hypotension
  2. Acute renal failure
  3. Hyperkalemia
  4. Angioedema, dry cough
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11
Q

What are the contraindications for ACE inhibitors?

A

Pregnant women, interferes with renal function of fetus

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12
Q

What are the AT1 blockers?

A 
Losartan
Valsartan
Candesartan
Eprosartan
Irbesartan
Telmisartan
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13
Q

What is the MOA of AT1 blockers?

A

Block ANGII from binding to AT1 receptor

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14
Q

Why are ACE inhibitors and ANGII blockers not used tgt?

A
  1. No additive effect from 2 drugs working in the same pathway
  2. May lead to additive side effects
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15
Q

What are the adverse effects of AT1 blockers?

A

Similar to ACE inhibitors but less/no dry cough

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16
Q

What are the contraindications in AT1 blockers?

A

Similar to ACE inhibitors -

pregnant women, interferes with renal function of fetus

17
Q

What is the MOA of ß-blockers?

A
  • Binds ß1 receptors in heart (G protein)
  • Inhibit adenylyl cyclase, decrease cAMP
  • Decrease PKA
  • Decrease activation of L-type voltage sensitive Ca channel
  • Decrease calcium induced calcium release
  • Decrease contractility
18
Q

Apart from the effects on the heart, ß blockers also have effect on what other organ?

A

Lungs - bronchoconstriction

  • Decrease cAMP
  • Decrease phosphorylation of MLCK into inactivated form (less)
  • Less bronchodilation
  • More prone to bronchoconstriction
19
Q

What are the non-selective ß blockers?

A

Propranolol
Pindolol
Carvedilol

20
Q

What are the cardioselective (ß1) ß blockers?

A

Atenolol
Bisoprolol
Metoprolol

21
Q

Which ß blockers are also specifically approved to treat heart failure?

A

Bisoprolol
Metoprolol
Carvedilol

22
Q

What are the clinical uses of ß blockers?

A
  1. Hypertension
  2. Cardiac failure
  3. Following MI
  4. Abnormal heart rhythm
  5. Anxiety disorders (but not 1st line)
23
Q

What are the adverse effects of ß blockers?

A
  1. Hypotension
  2. Bradycardia
  3. AV nodal block
  4. Reduced exercise capacity
  5. Bronchoconstriction (esp. asthmatics)
  6. CNS: vivid dreams, clinical depression (“ß blocker blues”)
24
Q

What are the dihydropyridines (DHPs) calcium channel blockers?

A

Nifedipine

Amlodipine

25
Q

What are the clinical uses of DHP calcium channel blockers?

A
  1. Anti-hypertensive
  2. Anti-angina (decrease contractility, CO, O2 requirement) for stable angina - Amlodipine
  3. MI and stroke prevention - Amlodipine
26
Q

What is the MOA of DHP calcium channel blockers?

A
  • Block L-type voltage sensitive Ca channel
  • Decrease Ca2+-calmodulin complex
  • Decrease activated form of MLCK
  • Decrease phosphorylation of Myosin-LC (active)
  • Decreased contraction
27
Q

What are the adverse effects of DHP calcium channel blockers?

A
  1. Hypotension
  2. Heart failure
  3. MI (esp. of 1st time)
28
Q

What 2 anti-hypertensive drugs are never used in combination?

A

ACE inhibitors and AT1 blockers

29
Q

In drug combination therapy for hypertension, 1 drug decreases the BP by how much?

A

10/5mmHg

30
Q

What are the contraindications for ß-blockers?

A
  1. Asthmatics

2. Diabetics (mask hypoglycemia)

31
Q

What are the contraindications for DHP calcium channel blockers?

A

Congestive heart failure (worsen LV output)

Systemic Pharmaco (6 decks)

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