Question | Answer |
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 |