Pharmacology HTN
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- List some causes of secondary hypertension
- - chronic renal disease - renovascular disease - exogenous substances (steroids, NSAIDs, estrogens, alcohol)
- Name some risk factors for hypertension
- - age (males > 55, females > 65) - diabetes (#1 risk factor) - increased LDL, decreased HDL - GFR less than 60 - family history - obesity - tobacco - physical inactivity
- Give examples of target organ damage due to hypertension
- 1. in the heart, such as revascularization, left ventricular hypertrophy (LVH), angina/MI, CHF 2. in the kidney, such as chronic kidney disease, nephropathy, retinopathy 3. in the brain, such as stroke, TIA, dementia
- Give examples of lifestyle modifications to reduce hypertension
- - weight loss (10 lb weight loss decreases BP 6-8 mm Hg) - limit alcohol intake - increase aerobic physical activity - reduce sodium intake - stop smoking - reduce intake of saturated fats and cholesterol
- Generally, what do diuretics do?
- decrease cardiac output and decrease fluid
- What is the mechanism of action (MOA) of thiazide diuretics?
- - inhibt Na/Cl symporter at the early distal convoluted tubule and cortical portion of the thick ascending limb of the loop of Henle - increased Na, Cl, and H20 excretion
- Why are thiazide diuretics good for patients with osteoporosis?
- thiazide diuretics reduce Ca++ excretion
- What are some uses of thiazide diuretics?
- - CHF - HTN - hepatic cirrhosis - renal disease - edma associated with corticosteroid and estrogen use - osteoporosis
- What are side effects of thiazide diuretics?
- - hyponatremia - hypokalemia - hypovolemia - hypomagnesemia - hyperuricemia
- Name 4 thiazide diuretics and their dosages
- 1. HCTZ 12.5 - 25 mg daily 2. Chlorthalidone 12.5 - 50 mg daily 3. Indapamide 1.25 - 5 mg daily 4. Metolazone 2.5 - 10 mg daily (weakest of thiazide diuretics)
- What is the mechanism of action of loop diuretics?
- - acts primarily on the ascending loop of Henle by inhibiting the Na-K-Cl symporter - increases Na, Cl, K, and H20 excretion in large amounts
- What are uses of loop diuretics?
- - CHF - HTN - hepatic cirrhosis - renal disease - hypercalcemia
- What are side effects of loop diuretics?
- - hyponatremia - hypokalemia - hypovolemia (greatest with loop diuretics) - hypomagnesemia - hyperuricemia
- Name 4 loop diuretics and their dosages
- 1. furosemide (Lasix) 40 - 240 mg bid - tid 2. Bumetanide (Bumex) 0.5 - 4 mg bid - tid 3. Torsemide (Demadex) 5 - 100 mg bid - tid 4. Ethacrynic Acid (Edecrin) 25 - 100 mg bid - tid
- ___ mg of Bumetadine = ___ mg of Furosemide
- 1 mg of Bumetadine = 20 mg of Furosemide
- Which loop diuretic can be used to treat hypercalcemia?
- Torsemide (Demadex)
- Which loop diuretic is used for truely sulfa-allergic patients?
- Ethacrynic Acid (Edecrin)
- What are the 2 groups of potassium-sparing diuretics?
- 1. inhibitors of the renal epithelial Na channels; acts at the late distal tubule (Triametrene, Amiloride) 2. Aldosterone antagonist (spironalactone, elperelone)
- When do you use potassium-sparing diuretics?
- - used in adjunct treatment with thiazides and loop diuretics - to treat edema secondary to hyperaldosteronism
- What are side-effects of potassium-sparing diuretics?
- - gynecomastia (spironalactone) - hyperkalemia - hyponatremia
- Name 4 potassium-sparing diuretics and their dosage
- 1. Amiloride 5-10 mg daily 2. Spironalactone 25 - 100 mg daily 3. Triameterene 25 - 100 mg daily 4. Elperelone 25 - 100 mg daily
- What are general characteristics of Beta-Blockers?
- 1. reduce cardiac output through negative chronotropic and inotropic effectson the heart 2. blockade of beta receptors at the juxtaglomerular cells decrease release of renin 3. central action (crosses the blood brain barrier)
- Which is the most potent beta-blocker that can cross the blood brain barrier?
- propanolol
- What are the 4 classifications of beta-blockers?
- 1. nonselective 2. selective 3. with ISA (intrinsic sympathetic activity) 4. without ISA
- Which beta-blockers are nonselective?
- - carvedilol - labetalol - nadolol - pindolol - propanolol
- Which beta-blockers are selective?
- - atenolol - metoprolol - acetobutolol - bisoprolol
- Which beta-blockers are approved to use for CHF?
- - carvedilol - metoprolol succinate (Toprol XL) - bisoprolol (approved in Europe)
- What are the effects of beta-blockers with ISA? Give 2 examples.
- - beta-blockers with ISA lower blood pressure without reducing resting heart rate - examples are Pindolol (nonselective) and Acetobutolol (selective)
- Beta-blockers are used for what conditions?
- - hypertension - angina pectoris - arrhythmias - myocardial infarction - stable CHF (not acute CHF)
- What are side effects of beta-blockers?
- - bradycardia - bronchodilation - cold extremities - hypotension - increase serum lipids - mask symptoms of hypoglycemia
- What are contraindications for using beta-blockers?
- - second and third degree heart block - bradycardia (HR less than 50) - COPD with nonselective beta-blocker - beta blockers without ISA in PVD
- What can occur if beta blockers are withdrawled abruptly?
- - can get rebound angina and tachycardia - should reduce beta-blocker by 50% everyday to avoid withdrawl symptoms
- Name 6 beta blockers and their dosage ranges
- 1. Acebutolol 200 - 800 mg daily 2. Atenolol 25 - 100 mg daily (or BID) 3. Carvedilol 6.25 - 50 mg BID 4. Metoprolol 50 - 300 BID 5. Pindolol 10 - 60 mg BID 6. Propanolol 40 - 480 BID
- What is MOA of calcium channel blockers?
- inhibit calcium entry through voltage dependant channels
- Describe how calcium channel blockers affect smooth muscle, cardiac muscle, and the cardiac conduction system
- 1. smooth muscle - decreases muscle contraction (decreases total peripheral resistance through arteriolar relaxation) 2. cardiac muscle - decreases depolarization and reduces myocardial contractility (inhibits action potential) 3. cardiac conduction system - inhibition of pacemaker potential and slows AV conduction
- What are the 2 classifications of calcium channel blockers?
- - nondihydropyridines (used for rate control as antiarrhythmics) - dihydropyridines (used for HTN)
- Name some examples of nondihydropyridines
- - diltiazem - verapamil - nifedipine
- Name examples of dihydropyridines
- - amlodipine (Norvasc) - felodipine - nicardipine - nisoldipine
- What are indications for use of Nicardipine?
- - used in patients with a bleed - used for post-operative HTN
- What are indications for using Nisoldipine?
- - used with acute hemmorhagic stroke - must be given with 8 hrs of stroke
- What are the dosages for Diltiazem?
- - comes in immediate-release (IR) or sustained-release (SR) Diltiazem IR (Cardizem): 30, 60, 90 mg Q 8hrs Diltiazem SR (aka Cardizem CD, Tiazac): 120, 240, 320, 360, 480 mg Q 24
- What is the dosage for Verapamil?
- IR: 40, 80 mg Q 8-12 hr SR: 80, 160, 240, 320 mg Q 24 hr
- What is the dosage of Nifedipine?
- IR: 10 mg PRN SR (Procardia): 30, 60, 90 mg Q 12-24 hrs
- What are the dosages for the dihydropyridines?
- Amlodipine: 5-10 mg Q 24 Felodipine: 5-10 mg Q 24 Nicardipine: 30, 60, 90 mg Q 24 (90 mg is IV formulation) Nisoldipine: 10 mg Q 6 hrs
- What are clinical indications for using calcium channel blockers?
- - HTN - effort induced angina - arrhythmias - esophageal spasm
- What are side effects of calcium channel blockers?
- - constipation - flushing - headaches - palpitations - peripheral edema (seen in non-DHPs)
- What is the MOA for ACE inhibitors?
- - blocks the conversion of angiotensin I to angiotensin II - leads to a decrease in total peripheral resistance (TPR) and causes vasodilation - inhibts the breakdown of bradykinin (causes vasodilation)
- List 7 examples of ACE inhibitors
- - Benazepril (Lotensin) - Captopril - Enalapril (Vasotec) - Lisinopril (Zestril) - Quinapril (Accupril) - Ramipril (Altace) - Trandolapril
- Which is the only ACE inhibitor to come IV?
- Enalapril 1.25 mg IV
- What are the dosages of Ramipril (Altace)?
- 2.5, 5, 10 mg Q 24 hr
- What is the dosage for Enalapril?
- 2.5, 5, 10, 20 mg Q 12-24 hrs
- What are the dosages for Lisinopril (Zestril)?
- 2.5, 5, 10, 20 mg Q 12-24 hrs
- What are the dosages for Benazepril (Lotensin)?
- 5, 10, 20, 40 mg Q 12-24 hrs
- What is the dosage for Quinapril (Accupril)?
- 2.5, 5, 10 mg Q 24hrs
- What is the dosage for Captopril?
- 6.25, 12.5, 25, 50 mg Q 8hrs - drug is a TID drug which is not good for patient compliance
- What are indications for using ACE inhibitors?
- - HTN - proteinuria - CHF - myocardial infarction - diabetic nephropathy
- What are side effects of ACE inhibitors?
- - angioedema (due to increase of bradykinin, which causes vasodilation) - cough (due to increase of bradykinin, which causes vasodilation) - hyperkalemia - hypotension - increased serum creatinine (stop if SCR doubles or triples in 2 days) - taste disturbances
- What are contraindications of ACE inhibitors?
- - acute renal failure - bilateral renal stenosis - pregnancy
- What is the MOA of angiotensin receptor blockers?
- - blocks angiotensin II from binding to receptor - leads to a decrease in afterload and preload
- Why is there a lower incidence in cough with ARBs?
- ARBs do not affect bradykinin
- Name 4 ARBs
- - Losartan (Cozaar) - Valsartan (Diovan) - Candesartan (Atacand) - Irbesartan (Avapro)
- What is the dosing for Losartan (Cozaar)?
- 25-100 mg Q24 hr
- What is the dosing for Valsartan (Diovan)?
- 40, 80, 120 mg Q24
- What is the dosing for Candesartan (Atacand?
- 6, 8, 12, 24, 32 mg Q24
- What is the dosing for Irbesartan (Avapro)?
- 75, 150, 30 mg Q24
- What are clinical indications are ARBs?
- - CHF - diabetic nephropathy - HTN - myocardial infarction - proteinuria
- What are side effects of ARBs?
- - angioedema - hyperkalemia - hypotension - increase Scr
- What are contraindications for ARBs?
- - same as ACE inhibitors - patients with bilateral renal stenosis - acute renal failure - pregnancy
- What is the MOA of alpha 1 receptor blockers?
- dilate both resistance and capacitance vessels, reducing total peripheral resistance and venous return
- Why do you administer alpha 1 receptor blockers at night?
- to prevent orthostatic hypotension
- Name 3 alpha 1 receptor antagonists and their dosing
- Prazosin 2-30 mg BID Doxazosin (Cardura) 1-16 mg Q24 Terazosin 1-20 mg Q24
- What are clinical indications for using alpha 1 receptor antagonists?
- - HTN - benign prostatic hyperplasia (BPH)
- What are side effects of alpha 1 receptor antagonists?
- - hypotension - orthostatic hypotension
- What are contraindications for alpha 1 receptor antagonist?
- decreased heart rate
- What is the MOA for alpha 2 agonist?
- - firing of the sympathetic nerve decreases - decreases the amount of norepinephrine found at the nerve terminals - works on catecholamines
- Name 2 alpha 2 agonists and their dosing
- Clonidine 0.2-1.2 mg po BID Methyldopa 125-500 mg po BID
- What are side effects of alpha 2 agonist?
- - drowsiness - dry mouth - hypotension - sedation
- What is the indication for using methlydopa?
- methlydopa is the drug of choice for pregnant women with HTN
- What is the first line drug for a patient with diabetes type 1 and HTN?
- ACE inhibitor or ARB
- What drug should you use with a diabetic type 1 patient with HTN and a contraindication to ACE inhibitors?
- - calcium channel blockers - hydralazine with a nitrate
- What are first line drugs for treatment of heart failure?
- - ACE inhibitor or ARBs - diuretics used with an ACE inhibitor or ARBs
- What are first line drugs for acute myocardial infarction?
- - Beta - blockers (non-ISA) such as pindolol or acebutolol - ACE inhibitor or ARB in conjunction with a beta-blocker (ACE-I prevents myocardial remodeling)
- What drugs are contraindicated with COPD?
- beta-blockers unless there are compelling indications like MI
- Which drugs should be avoided in patients with gout?
- thiazide and loop diuretics
- Which drugs are contraindicated with 2nd and 3rd degree heart block?
- avoid beta-blockers and calcium channel blockers