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CH 44

Drugs acting on RAAS

1. ACE inhibitors "PRIL" - Important drugs for treating hypertension, heart failure, diabetic neuropathy, and MI - used to PREVENT adverse cardiovascular events - Block production of Aldosterone - inhibit Kinase II which increases bradykinin in lungs (cough)
ACE inhibiors Adverse effecs - **cough** (most common reason for discontinuing therapy) -**angiodema (life threatening allergic reaction)** - first-dose hypertension=widespread vasodilation - hyperkalemia - FETAL INJURY-discontinue immediately - Neutropenia
How do beneficial effects for ACE inhibitors occur? - suppressing formation of angiotension II - dilate blood vessels
How are ACE inhibitors administered? - all orally except for enalaprilat (given IV) - All given with food except for captopril & moexipril - ALL are prodrugs except for lisinopril - ALL excreted by the kidneys
ACE suffix? "PRIL"
Do ACEs interfere w/ cardiovascular reflexes? NO
Most importantly.. - ACEs reduce the risk of cardiovascular mortality causes by hypertension
ACE drug interactions DO NOT TAKE WITH: - Diuretics (intensify first dose Hypotension) - Antihypertensive agents (causes additive hypotensive effects) - Drugs that raise K+ levels (ex: K+ sparing diuretics) - Lithium -NSAIDs(reduce antihypertensive effects of ACE)
2. Angiotension II Receptor Blockers (ARBs) "ARTAN - treat hypertension -heart failure - diabetic nephropathy & Retinopathy -MI - stroke -death in people at high risk for cardiovacular events
What do ARBs do? - decrease the influence of angiotension II (block the action) - By decreasing aldosterone. renal excretion of NA and H2O is increased
DO they produce cough like ACE? NO!! Pose much lower risks for cough - great for patients who can't tolerate ACE cough
ARB suffix? "ARTAN"
ARB adverse effects - DO NOT CAUSE hyperkalemia like ACEs :) - DO CAUSE: Angiodema - FETAL HARM - RENAL Failure
ARB drug interactions - Hypotensive effects are additive with other hypertensive drugs
Administration of ARBs - ALL given PO and be taken with or with out food
3. Aliskiren - A Direct Renin Inhibior (DRI) (AKA Tekturna) - Act on renin to inhibit the conversion of angiotension into angiotension 1 - By inhibiting angio 1, entire RAAS can be suppressed
Aliskiren (DRI) Therapeutic use - Hypertension ONLY - Older hypertensives should be used over DRIs
Aliskiren (DRI) administration - given orally
Aliskiren (DRI) adverse effects: - DIARRHEA -Avoided during pregnancy (fetal harm) - Angiodema & cough (low risk) - hyperkalemia (if combined w/ other drugs)
Aldosterone Antagonists: Eplerenone (Inspra) ("ONE") - produces selective blockade of aldosterone receptors - causes retention of K+ and increased loss of sodium and water leading to reduced blood volume and blood pressure
- Aldosterone Antagonists: Eplerenone (Inspra) THERAPEUTIC USE: -Hypertension - Heart failure
Aldosterone Antagonists: Eplerenone (Inspra) administration - given orally and is not effected by food
Aldosterone Antagonists: Eplerenone (Inspra) ADVERSE EFFECTS -**Hyperkalemia**: occur secondary to potassium retention - diarrhea, abdominal pain, cough, fatigue, gynecomastia, & flu-like syndrome OCCUR SLIGHTLY
Aldosterone Antagonists: Eplerenone (Inspra):DRUG INTERACTION - Inhibitors of CYP3A4 can increase levels of Eplernone - Drugs that raise K+ levels increase risk of Hyperkalemia
Aldosterone Antagonists: SPIRONOLACTONE ("ONE") - blocks receptors for aldosterone
Aldosterone Antagonists: SPIRONOLACTONE beneficial effects - hypertension & heart failure
Aldosterone Antagonists: SPIRONOLACTONE adverse effects - **hyperkalemia** - gynecomastia - menstrual irregularities - impotence - hirsutism - deepening of voice
What does the RAAS regulate? - BP, blood volume, and F & E balance
How does the RAAS act? - through production of Angiotension II
What does Angiotension II cause? - Vasoconstriction & release of aldosterone
What does Aldosterone do? - acts on kidneys to promote retention of sodium and water
What converts angiotensinogen to angiotension 1? - renin
What convert angio 1 to angio 2? - ACE
What does angio 2 promote? - secretion of aldosterone
Created by: KristinL