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26 Cards in this Set

  • Front
  • Back
Black patients respond well to ___1___ and ___2___, but mono therapy with ___3___ or ___4___ is often less effective.

1. Diuretics


2. Calcium-channel blockers


3. Beta-Blockers


4. ACE inhibitors

Describe the actions of Thiazide Diuretics.

Lower blood pressure initially by increasing sodium & water excretion. This causes a decrease in extracellular volume, resulting in a decrease in cardiac output and renal blood flow. With long-term treatment, plasma volume approaches a normal value, but peripheral resistance decreases.




Potassium-sparing diuretics are often used in combination with thiazides to reduce the amount of potassium loss induced by the thiazide diuretics.

What are the therapeutic uses of Thiazide Diuretics?

1. Decrease blood pressure in both supine & standing position. Postural hypotension is rarely observed except in elderly patient, volume depleted patients.




2. These agents counteract the sodium and water retention observed with other agents used in the treatment of hypertension (for example, hydralazine). They are useful in combination therapy with a variety of other antihypertensive agents, including Beta-blockers, ACE inhibitors, angiotensin-receptor blockers, and potassium-sparing sparing diuretics.




3. Are particularly useful in the treatment of black and elderly patients.




4. With the exception of metolazone, thiazide diuretics are not effective in patients with inadequate kidney function (creatinine clearance, less than 50mL/min). Loop diuretics may be required in these patients.

Describe the pharmokinetics of Thiazide Diuretics.

Thiazide diuretics are orally active. Absorption and elimination rates vary considerably, although no clear advantage is present for one agent over another. All thiazides are ligands for the organic acid secretary system of the nephron, and, as such, they may compete with uric acid for elimination.

What are the adverse effects of Thiazide Diuretics?

Induce hypokalemia and hyperuricemia in 70% of patients and hyperglycemia in 10% of patients. Acute gout attacks may be triggered. Hypomagnesemia may also occur. Serum potassium levels should be monitored closely in patients who are predisposed to cardiac arrhythmias (particularly individuals with left ventricular hypertrophy, ischemic heart disease, or chronic heart failure) and those who are concurrently being treated with both thiazide diuretics and digoxin. The incidence of side effects is reduced when employing low dose of diuretics (6.25 to 25 mg/day of hydrochlorothiazide).

Name some Loop Diuretics?

Furosemide, bumetanide, and torsemide.

______ ______ act promptly, even in patients with poor renal function or who have not responded to thiazides or other diuretics.

Loop diuretics!

How do loop diuretics work?

Loop diuretics cause decreased renal vascular resistance and increased renal blood flow. [Note: Loop diuretics increase the Ca2+ content of urine, whereas thiazide diuretics increase it.]

Name some Potassium-sparing Diuretics?

1. Amirloride & Triamterene (inhibitors of epithelial sodium transport at the late distal and collecting ducts)


2. Spironolactone & Eplereone (aldosterone-receptor antagonists) reduce potassium loss in the urine. Spironolactone has the additional benefit of diminishing the cardiac remodeling that occurs in heart failure.

______ are currently recommended as first-line drug therapy for hypertension when concomitant disease is present.

Beta-blockers! Concomitant disease, for example, include MI patients or in patients with a previous MI. These drugs are efficacious but have some contraindications.

What is the mode of action of Beta-blockers?

Beta-blockers reduce blood pressure primarily by decreasing cardiac output. They may also decrease sympathetic outflow from the CNS and inhibit the release of renin from the kidneys, thus decreasing the formation of angiotensin II and the secretion of aldosterone.

What is a Beta-blocker that acts at both Beta1 & Beta2 receptors (nonselective)?

Propranolol & Nadolol

Nebivolol

Selective blocker of Beta1 receptor, which also increases the production of nitric oxide leading to vasodilation.

Selective blockers of Beta1 receptors which are among the most commonly prescribed Beta-blockers?

Atenolol & Metoprolol

The selective Beta-blockers may be administered cautiously to hypertension patients who also have ______.

Asthma. The nonselective Beta-blockers, such as propranolol and nodal, are contraindicated due to their blockade of Beta2-mediated bronchodilation.

The Beta-blockers should be used cautiously in the treatment of patients with ______ ______ ______ or ______ ______ ______ .

acute heart failure & peripheral vascular disease

What are the therapeutic uses of Beta-blockers?

1. Subsets of the hypertensive population: More effective for treating hypertension in white than in black patients and in young compared to elderly patients. Conditions that discourage the use of Beta-blockers (for example, severe chronic obstructive lung disease, chronic congestive heart failure, and severe symptomatic occlusive peripheral vascular disease) are more commonly found in elderly and in diabetic patients.




2. Hypertensive patients with concomitant diseases: Useful in treating conditions that may coexist with hypertension, such as supra ventricular tachyarrhythmia, pervious myocardial infarction, angina pectoris, and chronic heart failure. Beta-blockers are also used to prevent migraine and cluster headaches.

Describe the pharmokinetics of Beta-blockers?

The beta-blockers are orally active. Propranolol undergoes extensive and highly variable first-[ass metabolism. The beta-blockers may take several weeks to develop their full effects.

What are the adverse effects of Beta-blockers?

- Hypotension, bradycardia, fatigue, insomnia, and sexual dysfunction (more likely to reduce compliance).




- Beta-blockers may disturb lipid metabolism, decreasing high-density lipoprotein cholesterol and increasing plaza triglycerides.




- Abrupts withdrawal may induce angina, I, and even sudden death in patients with ischemic heart disease. Therefore, the dose of these drugs must be tapered over 2 to 3 weeks in patients with hypertension and ischemic heart disease.

The ACE inhibitors, such as ___1___ and ___2___, are recommended when the preferred front-line agents (diuretics or Beta-blockers) are contraindicated or ineffective, or if there are compelling reasons to use them such as in diabetes mellitus.

1. Enalapril


2. Lisinopril

Describe the action of ACE inhibitors.

They lower the blood pressure by reducing the peripheral vascular resistance without reflexively increasing the CO, rate, or contractility. These drugs block the ACE that cleaves angiotensin I to form the potent vasoconstrictor angiotensin II. The converting enzyme is also responsible for the breakdown of bradykinin, which increases the production of NO and of prostacyclin by the blood vessels. Both NO and prostacyclin are potent vasodilators.

What are the therapeutic uses of ACE inhibitors?

Like Beta-blockers, ACE inhibitors are most effective in hypertensive patients who are white and young. However, when used in combination with a diuretic, the effectiveness of ACE inhibitors is similar in white and black patients with hypertension.




Along with the ARBs, ACE inhibitors slow the progression of diabetic nephropathy and decrease albuminuria and are, thus, a compelling indication for patients with diabetic nephropathy.

______ are standard

Answer

What are the adverse effects of ACE inhibitors?

1. Dry cough due to increased levels of bradykinin in the pulmonary tree. It occurs more frequently in women and nonsmokers and with longer-acting ACE inhibitors. It resolves a few days after therapy discontinuation.


2. Hyperkalemia


3. Skin rash


4. Hypotension


5. Fever.

The ______ ______ ______ are alternatives to ACE inhibitors.

Angiotensin II Receptor Blockers (ARB)

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