Antihypertensive drugs Flashcards
1
Q
Angiotensin II
A
- Peptide hormone that acts as a AT1
- Activated by a Gq coupled receptor
- Vasoconstriction activation
- Stimulates the thirst
2
Q
ACE inhibitor
A
- Zinc containing dipeptidyl carboxypeptidase
- Produced in the lung
3
Q
Arterial and venous vasodilation
A
- Decrease arterial and venous pressure
- Decrease in ventricular preload
- Decrease blood vol
- Downregulation of sympathetic activity
- Suppression of hypertrophy
3
Q
What is the ending of ACE inhibitor
A
- Ending of -pril lowering blood pressure reduce vasoconstriction decrease peripheral resistance
4
Q
Pharmacokinetics of ACE inhibitor
A
- 40-60% bioavailable depending on drug
- Bind to tissue
- Metabolism in the liver
- Eliminated through the kidney
5
Q
Captopril
A
- Absorbed and eliminated quickly
6
Q
Enalapril
A
- Later ACE inhibitor inactive pro-drug that requires hydrolysis
during or active absorption
7
Q
Lisinopril
A
- Itself active
- Lisinopril is not metabolized and is
excreted as an unchanged drug - Completely eliminated in the urine
8
Q
Mechanism of ACE
A
- Bradykinin is a potent vasodilator and this is stimulated by specific endothelial B2 receptor
- Dilates arterioles releasing prostacyclin and nitric oxide
- ACE converts bradykinin to inactive peptide
9
Q
Common Adverse effect of ACE inhibitor
A
- Dry irritated cough due to bradykinin accumulation
10
Q
Function Of ACE inhibitor
A
- Block breakdown of bradykinin therefore there is an increase in levels
- Effects sensory nerves adapting stretch receptors and C-fiber receptors that release neurokinin
- Cause contraction of smooth muscle causes bronchoconstriction and dry cough
11
Q
Rare adverse effects
A
- Hyperkalemia - increase potassium cause depolarization can be lethal - aldosterone mediated
- Taste disturbance - contain zinc bitterness in the mouth
- Hypotension - rapid decease bp become low
- Renal impairment (stenosis in kidney)
- Increase in bradykinin cause angioedema rash and large lip
12
Q
Clinical considerations
A
- Cough is not dose dependent it is a class effect
- Hypotension - combine with low dose diuretics
Dehydration - vom and diarrhea temp suspend
13
Q
Renal risk assessment
A
- Beneficial for patients with chronic renal failure and hypertension
- Assess renal function
- Monitor serum creatinine
14
Q
When to avoid ACE inhibitor
A
- Patient 55 and above years
- Caribbean black or African origin
- Pregnant and breastfeeding women
- Diabetic patients
15
Q
Angiotensin receptor blocker
A
- Receptor antagonist that block type 1 angiotensin II
- AT1 receptors are coupled with Gq-proteins and IP3 signal transduction for muscle contraction
- Ending with sartan