ACEIs/ARBs/CCBs/renin inhibitors Flashcards
ACEIs inhibitors examples
Enalapril
Lisinopril
Ramipril
-pril
clinical uses of ACEIs
°Hypertension
°Heart failure
°Post MI
°High risk of ischemic heart disease
°Diabetic nephropathy
°Chronic renal insufficiency to prevent progression
AE of ACEIs
1) Hypotension
2) Dry cough (due to bradykinin accumulation)
3) Hyperkalaemia (because of reduced aldosterone secretion)
4) Angioedema
5) Renal failure in renal artery stenosis
contraindications of ACEIs
1)Renal stenosis/ Kidney injury
2)NSAIDS (ACEIs interact Interactions with
NSAIDs at renal A. –> dilation of efferent A. = lower GFR)
3) Pregnancy
MoA of ACEIs
blocks the conversion of Angiotensine I to AT II so:
1) ↓Bp
2) ↓ Cardiac load = ↑ CO (to the heart)
So, Renin accumulates, ATI accumulate and ATII is low
*note: ACEIs DO NOT affect Cardiac contractility
ARBs examples
Losartan
Valsartan
-sartan
MoA of ARBs
Similar to ACEIs but do not cause cough (they do not affect Bradykinin)
Blocks Angiotensine II receptors (on blood vessles) so:
1) ↓Bp
2) ↓ Cardiac load = ↑ CO (to the heart)
when they block the ATII this causes accumulation of renin, ATI and ATII
AE of ARBs
Teratogenic
Contraindications of ARBs
1) NSAIDS (Interactions with NSAIDs at renal A. –> dilation of efferent A. = lower GFR)
2) PREGNANCY
Clinical uses of ARBs
Hypertension in:
1) young patients (as they have higher renin than older people)
2) diabetics
3) Hypertension complicated by LV Hypertrophy
4) HF
5) Diabetic Nephropathy
Used mainly in Asthmatic patietns or when dry cough from ACEIs
Renin Inhibitors Examples
Aliskiren
MoA of Aliskiren
renin inhibitor–> lowers Bp
(but clinicaly somewhat unsuccessful)
AE of Aliskiren
1) Diarrhoea,
2) acute renal failure,
3) angioedema and
4) severe allergies (rare)
Contraindications of Renin Inhibitors?
1) PREGNANCY
2) Africans and old patients have lower renin levels thus a renin inhibitor is contraindicated.
The 3 classes of CCBs + Examples
1) Phenylalkylamine: Verapamil
2) Benzothiazepines : Dilitiazem
3) Dihydropyridines
a) (Chronic)
- Nifedipine
- Amlodipine
b) (Acute)
- Clevidipine
- Nicardipine
MoA of Verapamil
1) Acts mainly on Cardiac Myocytes :
- ↓ HR and
- ↓ force of contraction
2) Strong Intropic effects by blocking phase 2 plateau
*phase 2 platue : when Ca+2 enters the ventricles (Contraction)
Clinical uses of Verapamil
1) Angina
2) Arrhythmias
3) Hypertension
Contraindications of Verapamil
1) HF (blocks phase 2 plateau)
2) w/ beta-blockers
AE of Verapamil
1) Constipation (block CA+2 channels in the GI tract)
2) Effects on cardiac rhythm (heart block) and
contraction force (worsen heart failure)
3) Hyperprolactinemia((because it inhibits dopamine release)
MoA of Diltiazem
Acts on both cardiac and vascular myocytes.
No change in HR
Clinical uses of Dilitiazem
°Angina
°Hypertension
Contraindications of Dilitiazem
Don’t give in case of
HF (since they depress Ca+
channels in the heart) also in combo w/ beta blockers
MoA of CCBs Dihydropyridines
*Nifedipine, Amlodipine, Clevidipine, Nicardipine
Bind at the A1 subunit in LTCC (LType Ca+ Channels)
-Generalized arterial/arteriolar vasodilation = ↓ BP
-Little effect on veins
- ↓ TPR = ↓ heart afterload but can cause reflex
tachycardia
Clinical uses of Nifedipine, Amlodipine, Clevidipine, Nicardipine
1) Nifedipine, Amlodipine,
- Varient Angina (vasodialtion of CA)
- Hypertension
- Raynaud Phenomenon
2) Clevidipine, Nicardipine
- Hypertensive Crises Emergency (IV)
Raynaud Phenomenon: decreased blood flow to the fingers
AE of CCBs Dihydropyridines
- Flushing and headache (because they vasodilate)
- Peripheral oedema (ankle swelling)
- Gingival hyperplasia
Contraindications of Dihydropyridines
1) Unstable Angina
2) safe in pregnancy
