Calcium channel, ACEI, ARB Flashcards
What are the Calcium Channel Blockers?
- **Amlodipine (Norvasc)
- **Nicardipine (Cardene)
- Diltiazem (oral)
- Nifedipine
- Verapamil
Prescription for Amlodipine (Norvasc)?
Amlodipine 10 mg One tablet daily • Maintenance AND the max dose Most start at 5 mg Range = 2.5-10 mg
Prescription for Nicardipine (Cardene)?
Nicardipine infusion
Start at 5 mg/hour and titrate to effect every 15 minutes up to a maximum of 15 mg/hour
Once up to 15 mg/hour and BP controlled, drop dose to 3 mg/hour as maintenance
How do calcium channel blockers work?
o Normally calcium flows in to muscle cells resulting in smooth muscle contraction and cardiac myocyte contraction
Calcium channel blockers do exactly that, block calcium from entering muscle cells
• Reduce smooth muscle contraction and reduce myocyte contraction
• Reduced blood pressure
What are the differences of calcium channel blockers?
- Pharmacokinetics: Amlodopine and Felodipine are only ones that can be once a day. All other ones are extended release.
- Effect on cardiac conduction: Verapamil has biggest effect
- Adverse Drug Reactions
What are the Adverse Drug Reactions of the calcium channel blockers?
- Dihydropyridines: Vascular side effects
- Non-dihydropyridines: Cardiac conduction effects
o That AV node effect Bradycardia or… AV block o That vasculature effect Excessive hypotension Dizziness Peripheral edema
Indications for Amlodipine?
Treatment of hypertension
Treatment of symptomatic chronic stable angina, vasospastic angina
Prevention of hospitalization due to angina with documented CAD
Indications for Nicardipine (oral and intravenous)?
Management of hypertension (immediate and sustained release products)
Parenteral only for short-term use when oral treatment is not feasible
Chronic stable angina (immediate-release product only)
Indications for Diltiazem?
- Primary hypertension
- Chronic stable angina or angina from coronary artery spasm
Indications for Nifedipine?
- Treatment of hypertension (sustained release products only)
- Management of chronic stable or vasospastic angina
Indications for Verapamil?
- Treatment of hypertension
- Angina pectoris (vasospastic, chronic stable, unstable)
- Supraventricular tachyarrhythmia (PSVT, atrial fibrillation/flutter )
Are the Calcium Channel Blockers a 1st line drug?
NO!!!
Diuretics are first line in the newly diagnosed hypertensive patient with no other cardiovascular diseases
Then a choice of:
ACE inhibitor
Calcium channel blocker
Beta blocker
What are the advantages for the Calcium Channel Blockers?
No metabolic effects, no increase in lipid levels and safe in mild to moderate renal failure
What do all the Calcium Channel Blockers interact with?
β-blockers –> additive or synergistic effects
o All interact with CYP3A4 –> ↑ level of CCB
o All interact with General Anesthetics –> Potentiation of cardiac effects and vascular dilation of anesthetic agent
What are the ACE inhibitors?
- Lisinopril (Zestril)
- Captopril (Capoten)
- Ramipril (Altace)
Prescription for Lisinopril?
20 mg
One tablet daily
• Antihypertensive dose, need at least this for optimized dose
Starting dose = 10 mg
40 mg is also a good dose, 80 mg is too high
Watch K+ levels and renal function
Prescription for Captopril?
50 mg One tablet three times a day Good for Diabetic nephropathy If go up to 100 mg, can get bad side effects, but 50 mg is a good dose
How do the ACE inhibitors work?
o Block the conversion of angiotensin I to angiotensin II
Lower arteriolar resistance
Increase venous capacity
Increased cardiac output and cardiac index, stroke work and volume
Lower renovascular resistance
o Reduce the progress of diabetic nephropathy
o
Besides blocking the conversion of angiotensin I to angiotensin II, what else do they do?
- Cut down on breakdown of bradykinin, so get more bradykinin which leads to more vasodilation and lower BP.
- Also get increased prostaglandin synthesis, so NSAIDS can block this effect
What is the main difference between ACE inhibitors?
- Half life –> Captopril is short acting, and Lisinopril is long acting
Indication for Lisinopril?
Treatment of hypertension, either alone or in combination with other antihypertensive agents
Adjunctive therapy in treatment of heart failure
Treatment of acute myocardial infarction within 24 hours in hemodynamically-stable patients to improve survival
Treatment of left ventricular dysfunction after myocardial infarction
Indication for Captopril ?
Management of hypertension
Treatment of heart failure
Left ventricular dysfunction after myocardial infarction
Diabetic nephropathy
Indication for Enalapril?
- Treatment of hypertension
- Treatment of symptomatic heart failure
- Treatment of asymptomatic left ventricular dysfunction
- Only injectable
Indication for Ramipril?
- Treatment of hypertension, alone or in combination with thiazide diuretic
- Treatment of left ventricular dysfunction after MI
- To reduce risk of MI, stroke, and death in patients at increased risk for these events
What do ACEI inhibitors reduce?
reduce mortality in post-myocardial infarction patients and help prevent the development of heart failure
When are ACEI inhibitors contraindicated?
- pregnancy –> fetal death
- o Renal artery stenosis (Bilateral)
o Previous angioedema associated with ACE inhibitor therapy
What are the side effects for the ACEI inhibitors ?
o Hypotension o Cough o Hyperkalemia o Headache, dizziness, fatigue o Renal impairment o
What are the Angiotensin Receptor Blockers (ARBs)?
- Losartan (Cozaar)
* Valsartan (Diovan)
Prescription for Losartan?
Losartan 50 mg One tablet daily Range = 25-100 mg Can be dosed 25 mg, two times a day
Prescription for Valsartan?
Valsartan
160 mg
One tablet daily
Max dose is 320 mg
How do the ARBs work?
o Block the receptor site where angiotensin II activates all of the “bad” effects
Blockade that results in Drop in blood pressure
o Get rid of vasoconstriction and aldosterone
What is the indication for Losartan?
Treatment of hypertension
Treatment of diabetic nephropathy in patients with type 2 diabetes mellitus and a history of hypertension
Stroke risk reduction in patients with HTN and left ventricular hypertrophy
What is the indication for Valsartan?
Alone or in combination with other antihypertensive agents in the treatment of primary hypertension
Reduction of cardiovascular mortality in patients with left ventricular dysfunction postmyocardial infarction
Treatment of heart failure (NYHA Class II-IV)
What is the indication for Azilsartan?
Treatment of hypertension; may be used alone or in combination with other antihypertensives
What 2 ARBs are approved for heart failure?
- Valsartan (Diovan™)
- Candesartan (Atacand™)
What are the Adverse drug reactions of ARBS?
o Same as ACEI
o ↑ risk of cancer
- But lower incidence of dry cough
What is the renin antagonist?
Tekturna (Aliskiren)
What is the prescription for Tekturna?
Tekturna
300 mg
One tablet daily
There is a 150 mg
How does the renin antagonist (Tekturna) work?
Blockade of conversion of angiotensinogen to angiotensin I
What are the side effects of the renin antagonist?
Side effects same as ACEI and ARBs
Why don’t people used the renin antagonist?
VERY VERY Expensive and have same clinical outcome as ACEI and ARBs, so not used
What are the generic combinations of the antihypertensive drugs?
- ACEIs and thiazides
- ARBs and thiazides
- ARBs and calcium channel blockers
- Calcium channel blockers and “statins”
Should you use combinations of the antihypertensive drugs?
NO, resist!
- Start off with a single agent 1st, so you can adjust.
- only use with the elderly if they’re always on it and have good effects; this way easier to remember and possibly may be cheaper