ACE Inhibitors And ARBs Flashcards
T or F
ACE inhibitors only inhibit formation of angiotensin II
False
Also block the breakdown of bradykinin (a vasodilator) and block the breakdown of substance P
General action mechanism of ACE inhibitors
1-
2-
3-
4-
1-vasodilation(inhibition of formation of angiotensin II and metabolism of bradykinin)
2-blocking the effect of angitensin II on sympathetic release of norepi
3-promote Na and water excretion by blocking aldosterone release
4- inhibit cardiac and vascular remodeling
Therapeutic uses
1-
2-
3-
Heart failure
Hypertension
Post myocardial infarct
T or false
The difference between ACE inhibitor drugs is that they have different duration of action and half life
True
Effects on heart failure
1-
2-
3-
4-
5-
1- reduced afterload which enhances ventricular volume and improves ejection fraction
2- reduced preload which decrease pulmonary and systemic congestion and edema
3- reduced sympathetic activation
4- decreased myocardium oxygen demand by decreasing afterload and preload
5-prevents heart remodeling ( hypertrophy) caused by angiotensin II
ACE inhibitors may be classified to —- groups according to their —— of their active moiety
Captopril have ——- group
Fosinopril is the only drug that have —— group
Majority contain —— group
3
Chemical structure
Sulfhydryl
Phosphinyl
Carboxyl
T or F
Captopril and enalapril are prodrugs
False
Captopril isn’t
T or F
Majority of ACE inhibitors are prodrugs
T
T or F
ACE inhibitors are cleared prodominately by liver
False
Kidney
Majority of ACE inhibitors have ——– oral bioavailability
High because they are administered as prodrugs
T or F
Dose reduction is not essential in case of renal dysfunction because ACEI are mostly excreted in bile
False
Dose reduction is important laanu bytla3u bl pipi :(
T or F
Enalapril was the first agent developed
Falseeee
Captoooo
Enalapril and most ACEIs are ——
Esterified by plasma esterases to become active (enalaprilat)
Side effects of ACE inhibitors
1-
2-
3-
4-
5-
6-
1-dry cough (10-20%) because of elevated bradykinin
2-hypotension
3-angioedema (life threatening airway swelling and obstruction)
4-hyperkalemia (aldosterone reduction)
5-dizziness headache drowsiness diarrhea
6-dysguesia
Sulhydryl related effects (captopril)
1-
2-
3-
Neutropenia
Rash
Nephrotic range proteinuria
AngII cause vasocontriction of —– and —- arterioles which maintain GF
ACE inhibitor cause vasodilation of —– arteriole which lead to —– GF
Afferent and efferent
Efferent
Decreased
Contraindications
1-
2-
Pregnancyyy byaamel birth defects
Stenosis of both arteries supplying kindey
Drug interaction
1-
2-
1-potassium supplements, potassium sparing diuretics or other drugs that increase pirassium levels will cause severe and toxic hyperkalemia when administered with ace imhibitors
2-NSAIDs may reduce the effect of ACEIs
ARBs mode of action
Block angII receptors typeI (ATI) on blood vessels and other tissues such as heart
T or F
ATI are coupled to Gs protein
False
Gq IP3 transduction pathway
T or F
ARBs and ACEIs have similar effects and are used for the same indications
True
List the names of drugs included and half lives of each
Candesartan (atacand)
Irbesartan (aprovel) 11-15 hr
Telmisartan (micardis) 24 hr
Valsartan (diovan) 6 hr
Losartan (cozaar) 6-9 hr
T or F
All ARBs are well absorbed after oral administration
True
Actions of ARBs
Similar to ACEIs
ARBs adverse effects:
1-
2-
3-
4-
1- hyperkalemia
2-impairment of renal function if bilaretal renal artery stenosis
3-rare dizziness
4- headache diarrhea abnormal taste rash
ARBs contraindications:
1-
2-
1- pregos
2- bilateral renal artery stenosis with ARBs may lead to renal failure
T or F
ARBs increase bradykinin levels so they cause dry cough and angioedema like ACEIs
Falseeeee
Ma bezedu l bradykinin
So ma byaamlu dry cough and angioedema
