antihypertensives Flashcards

1
Q

what are the first line antihypertensives?

A
  1. ACE inhibitors
    - lisinopril, captorpil, enalapril
  2. Angiotensin II Type 1 Blockers
    - valsartan, losartan, smth ‘sartan’
  3. Beta adrenoreceptor Antagonists
    - [non-selective] propanolol, pindolol, carvedilol
    - [beta-1 selective] atenolol, bisoprolol, metoprolol
    - [mixed - 3rd gen] nebivolol
  4. Calcium channel blockers
    - dihydropyridines (nifedipine, amlodipine)
    - non-DHP (verapamil, diltiazem)
  5. Diuretics
    - thiazide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the second line antihypertensives?

A
  1. Alpha adrenoreceptor Antagonists
    - prazosin, smth “zosin”
  2. Hydralazine
  3. Mineralocorticoid Receptor Blockers
    - spironolactone, smth ‘one’
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the MOA of ACE inhibitors?

A
  • inhibits ACE
  • prevents Angiotensin I from converting to Angiotensin II
  • decrease in angiotensin II
  • decrease vasoconstriction -> decrease peripheral resistance
  • decrease aldosterone -> decrease Na+/H2O retention
    => lowers BP
  • reduce bradykinin inactivation
  • bradykinin increases and starts to accumulate
  • increases NO, PG
  • increases vasodilation
    => lowers BP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Contradictions using ACE Inhibitors (“pril”)?

A

Pregnancy

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

What is the MOA of Angiotensin II Type 1 blockers (“sartan”)?

A
  • blocks AT1 receptor -> blocks angiotensin II
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Contraindications using Angiotensin II Type 1 blockers (“sartan”)

A

Prenancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What beta adrenoreceptor blockers are also heart failure meds?

A

Carvedilol, Bisoprolol, Metoprolol, Nebivolol

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

MOA of beta adrenoreceptor antagonists (“olol”)

A
  • blocks B1 adrenoreceptor on cardiac myocytes
  • decrease adenylate cyclase
  • decrease ATP conversion to cAMP
  • decrease PKA activation
  • decrease opening of Ca2+ channels
  • decrease influx of Ca2+ into cardiac myocytes
  • decrease cytosolic Ca2+
  • decrease calcium induced calcium release
  • decrease activation of sarcoplasmic reticulum calcium
  • decrease calmodulin activation
  • decrease activation of actin-myosin complex
  • decrease contractility of cardiac myocytes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

MOA of calcium channel blocker

A
  • blocks calcium channels
  • decrease influx of Ca2+
  • decrease cytosolic Ca2+
  • decrease calcium induced calcium release
  • decrease activation of sarcoplasmic reticulum calcium
  • decrease calmodulin activation
  • decrease activation of actin-myosin complex
  • decrease contractility of cardiac myocytes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Effects of calcium channel blocker

A
  • decrease SA and AV nodes -> decrease supra ventricular reentry tachycardia (non-DHP)
  • decrease contractility of cardiac myocytes -> decrease O2 demand & CO (DHP)
  • decrease vascular smooth muscle tone -> decrease BP (DHP)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What calcium channel blockers are preferred for lowering BP?

A

verapamil = diltiazem = nifedipine

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

What calcium channel blockers are preferred as vasodilator?

A

nifedipine > diltiazem > verapamil

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

What calcium channel blockers are preferred as cardiac depressant?

A

verapamil > diltiazem > nifedipine

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

What are NON-DHP

A

verapamil, diltiazem
- anti-arrhythmic

higher affinity to Ca channels on smooth muscles /electrical conduct of the heart
- blocks SA and AV nodal conduction

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

MOA of diuretics (thiazides)

A
  • Ca2+ is reabsorbed at the distal convoluted tubule epithelial cell via apical Ca2+ channels and basolateral Na+/Ca2+ exchanger
  • Thiazides will block Na+/Cl- transporter, inhibiting Na+ reabsorption
  • concentration of Na+ in the tubular cells will decrease, increasing the activity of Na+/Ca2+ exchanger, driving the reabsorption of Ca2+ through the Ca2+ epithelial channels
  • increased Ca2+ reabsorption -> decrease hypercalciuria
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Prostaglandins will help the action of thiazides. What counters thiazides?

A

ADH will counter the action of thiazides
PGs will counter ADH. If prostaglandins are inhibited by NSAIDs, it allows ADH to work strongly against thiazides

16
Q

What are the adverse effects of thiazides?

A
  1. hypokalaemic metabolic alkalosis
  2. hyponatremia
  3. hyperuricaemia
  4. hyperglycaemia
  5. hyperlipidaemia
  6. hypercalcemia
17
Q

Why is hypokalaemic metabolic alkalosis an adverse effect of using thiazide?

A

due to an increase of aldosterone-mediated K+ and H+ excretion from the intercalated cells of the collecting duct

18
Q

Why is hyponatremia an adverse effect of using thiazide?

A

due to decrease in Na+ reabsorption

19
Q

Why is hyperuricaemia an adverse effect of using thiazide?

A

thiazides increase the reabsorption of urate from proximal convoluted tubules -> increases the risk of developing gout

20
Q

Why is hyperglycaemia an adverse effect of using thiazide?

A

due to hypokalaemia, there’s a decrease of K+ in the interstitium, K+ channels will open for an extended period of time -> hyperpolarization of the cell -> blocks the opening of voltage gated calcium channels -> decreases the exocytosis of insulin granules which is activated by calcium influx -> insulin response to hyperglycaemia is impaired

21
Q

MOA of alpha adrenoreceptor antagonists (“zosin”)

A

decrease vasoconstriction
decrease peripheral resistance
=> decrease BP

22
Q

Can alpha adrenoreceptor antagonists be used for renally impaired patients?

A

Yes as they do not affect GFR or renal blood flow

23
Q

What is alpha adrenoreceptor antagonists (“zosin”) used for?

A

treat symptoms of benign prostate hyperplasia