NurseReview.Org - Antihypertensives Updates (pharmacology review notes)

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Published on September 10, 2008

Author: jben501

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Antihypertensive Agents

Hypertension High blood pressure Normal: Systolic < 130 mm Hg Diastolic < 85 mm Hg

High blood pressure

Normal: Systolic < 130 mm Hg Diastolic < 85 mm Hg

Classification of Blood Pressure Category Systemic BP (mm Hg) Diastolic BP (mm Hg) Normal <130 <85 High normal 130-139 85-89 Hypertension Stage 1 140-159 90-99 Stage 2 160-169 100-109 Stage 3 180-209 110-119 Stage 4  210  120

Category Systemic BP (mm Hg) Diastolic BP (mm Hg)

Normal <130 <85

High normal 130-139 85-89

Hypertension Stage 1 140-159 90-99 Stage 2 160-169 100-109 Stage 3 180-209 110-119 Stage 4  210  120

Classification of Blood Pressure Primary Hypertension Specific cause unknown 90% of the cases Also known as essential or idiopathic hypertension Secondary Hypertension Cause is known (such as eclampsia of pregnancy, renal artery disease, pheochromocytoma) 10% of the cases

Primary Hypertension

Specific cause unknown

90% of the cases

Also known as essential or idiopathic hypertension

Secondary Hypertension

Cause is known (such as eclampsia of pregnancy, renal artery disease, pheochromocytoma)

10% of the cases

Blood Pressure = CO x SVR CO = Cardiac output SVR = Systemic vascular resistance

CO = Cardiac output

SVR = Systemic vascular resistance

Instructors may want to insert EIC Image #69: Blood Pressure: Normal Regulation

Antihypertensive Agents Medications used to treat hypertension

Medications used to treat hypertension

Antihypertensive Agents: Categories Adrenergic agents Angiotensin-converting enzyme inhibitors Angiotensin II receptor blockers Calcium channel blockers Diuretics Vasodilators

Adrenergic agents

Angiotensin-converting enzyme inhibitors

Angiotensin II receptor blockers

Calcium channel blockers

Diuretics

Vasodilators

Antihypertensive Agents: Categories Adrenergic Agents Alpha1 blockers Beta blockers (cardioselective and nonselective) Centrally acting alpha blockers Combined alpha-beta blockers Peripheral-acting adrenergic agents

Adrenergic Agents

Alpha1 blockers

Beta blockers (cardioselective and nonselective)

Centrally acting alpha blockers

Combined alpha-beta blockers

Peripheral-acting adrenergic agents

Antihypertensive Agents: Mechanism of Action Adrenergic Agents Alpha1 Blockers (peripherally acting) Block the alpha1-adrenergic receptors The SNS is not stimulated Result: DECREASED blood pressure Stimulation of alpha1-adrenergic receptors causes HYPERtension Blocking alpha1-adrenergic receptors causes decreased blood pressure

Adrenergic Agents

Alpha1 Blockers (peripherally acting)

Block the alpha1-adrenergic receptors

The SNS is not stimulated

Result: DECREASED blood pressure

Stimulation of alpha1-adrenergic receptors causes HYPERtension

Blocking alpha1-adrenergic receptors causes decreased blood pressure

Antihypertensive Agents: Adrenergic Agents Alpha1 Blockers doxazosin (Cardura) prazosin (Minipress) terazosin (Hytrin)

Adrenergic Agents

Alpha1 Blockers

doxazosin (Cardura)

prazosin (Minipress)

terazosin (Hytrin)

Antihypertensive Agents: Mechanism of Action Adrenergic Agents Central-Acting Adrenergics Stimulate alpha2-adrenergic receptors Sympathetic outflow from the CNS is decreased Result: decreased blood pressure

Adrenergic Agents

Central-Acting Adrenergics

Stimulate alpha2-adrenergic receptors

Sympathetic outflow from the CNS is decreased

Result: decreased blood pressure

Antihypertensive Agents: Adrenergic Agents Central-Acting Adrenergics clonidine (Catapres) methyldopa (Aldomet) (drug of choice for hypertension in pregnancy)

Adrenergic Agents

Central-Acting Adrenergics

clonidine (Catapres)

methyldopa (Aldomet) (drug of choice for hypertension in pregnancy)

Antihypertensive Agents: Mechanism of Action Adrenergic Agents Adrenergic Neuronal Blockers (peripherally acting) Inhibit release of norepinephrine Also deplete norepinephrine stores SNS (peripheral adrenergic nerves) is not stimulated Result: decreased blood pressure

Adrenergic Agents

Adrenergic Neuronal Blockers (peripherally acting)

Inhibit release of norepinephrine

Also deplete norepinephrine stores

SNS (peripheral adrenergic nerves) is not stimulated

Result: decreased blood pressure

Antihypertensive Agents: Adrenergic Agents Adrenergic Neuronal Blockers (peripherally acting) reserpine guanadrel (Hylorel) guanethidine (Ismelin)

Adrenergic Agents

Adrenergic Neuronal Blockers (peripherally acting)

reserpine

guanadrel (Hylorel)

guanethidine (Ismelin)

Antihypertensive Agents: Adrenergic Agents Therapeutic Uses Alpha1 blockers (peripherally acting) Treatment of hypertension Relief of symptoms of BPH Management of of severe CHF when used with cardiac glycosides and diuretics

Therapeutic Uses

Alpha1 blockers (peripherally acting)

Treatment of hypertension

Relief of symptoms of BPH

Management of of severe CHF when used with cardiac glycosides and diuretics

Antihypertensive Agents: Adrenergic Agents Therapeutic Uses Central-Acting Adrenergics Treatment of hypertension, either alone or with other agents Usually used after other agents have failed due to side effects Also may be used for treatment of severe dysmenorrhea, menopausal flushing, glaucoma Clonidine is useful in the management of withdrawal symptoms in opioid- or nicotine-dependent persons

Therapeutic Uses

Central-Acting Adrenergics

Treatment of hypertension, either alone or with other agents

Usually used after other agents have failed due to side effects

Also may be used for treatment of severe dysmenorrhea, menopausal flushing, glaucoma

Clonidine is useful in the management of withdrawal symptoms in opioid- or nicotine-dependent persons

Antihypertensive Agents: Adrenergic Agents Therapeutic Uses Adrenergic neuronal blockers (peripherally acting) Treatment of hypertension, either alone or with other agents Seldom used because of frequent side effects

Therapeutic Uses

Adrenergic neuronal blockers (peripherally acting)

Treatment of hypertension, either alone or with other agents

Seldom used because of frequent side effects

Antihypertensive Agents: Adrenergic Agents Side Effects Most common: dry mouth drowsiness sedation constipation Other: headaches sleep disturbances nausea rash cardiac disturbances (palpitations) HIGH INCIDENCE OF ORTHOSTATIC HYPOTENSION

Side Effects

Most common: dry mouth drowsiness sedation constipation

Other: headaches sleep disturbances nausea rash cardiac disturbances (palpitations)

HIGH INCIDENCE OF ORTHOSTATIC HYPOTENSION

Antihypertensive Agents: Categories Angiotensin-Converting Enzyme Inhibitors (ACE Inhibitors) Large group of safe and effective drugs Often used as first-line agents for CHF and hypertension May be combined with a thiazide diuretic or calcium channel blocker

Angiotensin-Converting Enzyme Inhibitors

(ACE Inhibitors)

Large group of safe and effective drugs

Often used as first-line agents for CHF and hypertension

May be combined with a thiazide diuretic or calcium channel blocker

Antihypertensive Agents: Mechanism of Action ACE Inhibitors RAAS: Renin Angiotensin-Aldosterone System When the enzyme angiotensin I is converted to angiotensin II, the result is potent vasoconstriction and stimulation of aldosterone Result of vasoconstriction: increased systemic vascular resistance and increased afterload Therefore, increased BP

ACE Inhibitors

RAAS: Renin Angiotensin-Aldosterone System

When the enzyme angiotensin I is converted to angiotensin II, the result is potent vasoconstriction and stimulation of aldosterone

Result of vasoconstriction: increased systemic vascular resistance and increased afterload

Therefore, increased BP

Antihypertensive Agents: Mechanism of Action ACE Inhibitors Aldosterone stimulates water and sodium resorption. Result: increased blood volume, increased preload, and increased B

ACE Inhibitors

Aldosterone stimulates water and sodium resorption.

Result: increased blood volume, increased preload, and increased B

Antihypertensive Agents: Mechanism of Action ACE Inhibitors ACE Inhibitors block the angiotensin-converting enzyme, thus preventing the formation of angiotensin II. Also prevent the breakdown of the vasodilating substance, bradykinin Result: decreased systemic vascular resistance (afterload), vasodilation, and therefore, decreased blood pressure

ACE Inhibitors

ACE Inhibitors block the angiotensin-converting enzyme, thus preventing the formation of angiotensin II.

Also prevent the breakdown of the vasodilating substance, bradykinin

Result: decreased systemic vascular resistance (afterload), vasodilation, and therefore, decreased blood pressure

Antihypertensive Agents ACE Inhibitors captopril (Capoten) Short half-life, must be dosed more frequently than others enalapril (Vasotec) The only ACE inhibitor available in oral and parenteral forms lisinopril (Prinivil and Zestril) and quinapril (Accupril) Newer agents, long half-lives, once-a-day dosing Several other agents available

ACE Inhibitors

captopril (Capoten)

Short half-life, must be dosed more frequently than others

enalapril (Vasotec)

The only ACE inhibitor available in oral and parenteral forms

lisinopril (Prinivil and Zestril) and quinapril (Accupril)

Newer agents, long half-lives, once-a-day dosing

Several other agents available

Antihypertensive Agents: Therapeutic Uses ACE Inhibitors Hypertension CHF (either alone or in combination with diuretics or other agents) Slows progression of left ventricular hypertrophy after an MI Renal protective effects in patients with diabetes Drugs of choice in hypertensive patients with CHF

ACE Inhibitors

Hypertension

CHF (either alone or in combination with diuretics or other agents)

Slows progression of left ventricular hypertrophy after an MI

Renal protective effects in patients with diabetes

Drugs of choice in hypertensive patients with CHF

Antihypertensive Agents: Side Effects ACE Inhibitors Fatigue Dizziness Headache Mood changes Impaired taste Dry, nonproductive cough, reverses when therapy is stopped NOTE: first-dose hypotensive effect may occur!!

ACE Inhibitors

Fatigue Dizziness

Headache Mood changes

Impaired taste

Dry, nonproductive cough, reverses when therapy is stopped

NOTE: first-dose hypotensive effect may occur!!

Antihypertensive Agents: Categories Angiotensin II Receptor Blockers (A II Blockers or ARBs) Newer class Well-tolerated Do not cause coughing

Angiotensin II Receptor Blockers (A II Blockers or ARBs)

Newer class

Well-tolerated

Do not cause coughing

Antihypertensive Agents: Mechanism of Action Angiotensin II Receptor Blockers Allow angiotensin I to be converted to angiotensin II, but block the receptors that receive angiotensin II Block vasoconstriction and release of aldosterone

Angiotensin II Receptor Blockers

Allow angiotensin I to be converted to angiotensin II, but block the receptors that receive angiotensin II

Block vasoconstriction and release of aldosterone

Antihypertensive Agents: Angiotensin II Receptor Blockers losartan (Cozaar) eposartan (Teveten) valsartan (Diovan) irbesartan (Avapro) candesartan (Atacand) telmisartan (Micardis)

Angiotensin II Receptor Blockers

losartan (Cozaar)

eposartan (Teveten)

valsartan (Diovan)

irbesartan (Avapro)

candesartan (Atacand)

telmisartan (Micardis)

Antihypertensive Agents: Therapeutic Uses Angiotensin II Receptor Blockers Hypertension Adjunctive agents for the treatment of CHF May be used alone or with other agents such as diuretics

Angiotensin II Receptor Blockers

Hypertension

Adjunctive agents for the treatment of CHF

May be used alone or with other agents such as diuretics

Antihypertensive Agents: Side Effects Angiotensin II Receptor Blockers Upper respiratory infections Headache May cause occasional dizziness, inability to sleep, diarrhea, dyspnea, heartburn, nasal congestion, back pain, fatigue

Angiotensin II Receptor Blockers

Upper respiratory infections

Headache

May cause occasional dizziness, inability to sleep, diarrhea, dyspnea, heartburn, nasal congestion, back pain, fatigue

Antihypertensive Agents: Categories Calcium Channel Blockers Benzothiazepines Dihydropyridines Phenylalkylamines

Calcium Channel Blockers

Benzothiazepines

Dihydropyridines

Phenylalkylamines

Antihypertensive Agents: Mechanism of Action Calcium Channel Blockers Cause smooth muscle relaxation by blocking the binding of calcium to its receptors, preventing muscle contraction This causes decreased peripheral smooth muscle tone, decreased systemic vascular resistance Result: decreased blood pressure

Calcium Channel Blockers

Cause smooth muscle relaxation by blocking the binding of calcium to its receptors, preventing muscle contraction

This causes decreased peripheral smooth muscle tone, decreased systemic vascular resistance

Result: decreased blood pressure

Antihypertensive Agents Calcium Channel Blockers Benzothiazepines: diltiazem (Cardizem, Dilacor) Phenylalkamines: verapamil (Calan, Isoptin) Dihydropyridines: amlodipine (Norvasc), bepridil (Vascor), nicardipine (Cardene) nifedipine (Procardia), nimodipine (Nimotop)

Calcium Channel Blockers

Benzothiazepines:

diltiazem (Cardizem, Dilacor)

Phenylalkamines:

verapamil (Calan, Isoptin)

Dihydropyridines:

amlodipine (Norvasc), bepridil (Vascor), nicardipine (Cardene)

nifedipine (Procardia), nimodipine (Nimotop)

Antihypertensive Agents: Therapeutic Uses Calcium Channel Blockers Angina Hypertension Dysrhythmias Migraine headaches

Calcium Channel Blockers

Angina

Hypertension

Dysrhythmias

Migraine headaches

Antihypertensive Agents: Side Effects Calcium Channel Blockers Cardiovascular hypotension, palpitations, tachycardia Gastrointestinal constipation, nausea Other rash, flushing, peripheral edema, dermatitis

Calcium Channel Blockers

Cardiovascular

hypotension, palpitations, tachycardia

Gastrointestinal

constipation, nausea

Other

rash, flushing, peripheral edema, dermatitis

Antihypertensive Agents: Diuretics Decrease the plasma and extracellular fluid volumes Results: decreased preload decreased cardiac output decreased total peripheral resistance Overall effect: decreased workload of the heart, and decreased blood pressure

Decrease the plasma and extracellular fluid volumes

Results: decreased preload decreased cardiac output decreased total peripheral resistance

Overall effect: decreased workload of the heart, and decreased blood pressure

Antihypertensive Agents: Mechanism of Action Vasodilators Directly relaxes arteriolar smooth muscle Result: decreased systemic vascular response, decreased afterload, and PERIPHERAL VASODILATION

Vasodilators

Directly relaxes arteriolar smooth muscle

Result: decreased systemic vascular response, decreased afterload, and PERIPHERAL VASODILATION

Antihypertensive Agents Vasodilators diazoxide (Hyperstat) hydralazine HCl (Apresoline) minoxidil (Loniten, Rogaine) sodium nitroprusside (Nipride, Nitropress)

Vasodilators

diazoxide (Hyperstat)

hydralazine HCl (Apresoline)

minoxidil (Loniten, Rogaine)

sodium nitroprusside (Nipride, Nitropress)

Antihypertensive Agents: Therapeutic Uses Vasodilators Treatment of hypertension May be used in combination with other agents Sodium nitroprusside and diazoxide IV are reserved for the management of hypertensive emergencies

Vasodilators

Treatment of hypertension

May be used in combination with other agents

Sodium nitroprusside and diazoxide IV are reserved for the management of hypertensive emergencies

Antihypertensive Agents: Side Effects Vasodilators Hydralazine: dizziness, headache, anxiety, tachycardia, nausea and vomiting, diarrhea, anemia, dyspnea, edema, nasal congestion Sodium nitroprusside: bradycardia, hypotension, possible cyanide toxicity

Vasodilators

Hydralazine:

dizziness, headache, anxiety, tachycardia, nausea and vomiting, diarrhea, anemia, dyspnea, edema, nasal congestion

Sodium nitroprusside:

bradycardia, hypotension, possible cyanide toxicity

Antihypertensive Agents: Nursing Implications Before beginning therapy, obtain a thorough health history and head-to-toe physical examination. Assess for contraindications to specific antihypertensive agents. Assess for conditions that require cautious use of these agents.

Before beginning therapy, obtain a thorough health history and head-to-toe physical examination.

Assess for contraindications to specific antihypertensive agents.

Assess for conditions that require cautious use of these agents.

Antihypertensive Agents: Nursing Implications Educate patients about the importance of not missing a dose and taking the medications exactly as prescribed. Patients should never double up on doses if a dose is missed; check with physician for instructions on what to do if a dose is missed. Monitor BP during therapy. Instruct patients to keep a journal of regular BP checks.

Educate patients about the importance of not missing a dose and taking the medications exactly as prescribed.

Patients should never double up on doses if a dose is missed; check with physician for instructions on what to do if a dose is missed.

Monitor BP during therapy. Instruct patients to keep a journal of regular BP checks.

Antihypertensive Agents: Nursing Implications Instruct patients that these drugs should not be stopped abruptly, as this may cause a rebound hypertensive crisis, and perhaps lead to CVA. Oral forms should be given with meals so that absorption is more gradual and effective. Administer IV forms with extreme caution and use an IV pump.

Instruct patients that these drugs should not be stopped abruptly, as this may cause a rebound hypertensive crisis, and perhaps lead to CVA.

Oral forms should be given with meals so that absorption is more gradual and effective.

Administer IV forms with extreme caution and use an IV pump.

Antihypertensive Agents: Nursing Implications Remind patients that medications is only part of therapy. Encourage patients to watch their diet, stress level, weight, and alcohol intake. Patients should avoid smoking and eating foods high in sodium. Encourage supervised exercise.

Remind patients that medications is only part of therapy. Encourage patients to watch their diet, stress level, weight, and alcohol intake.

Patients should avoid smoking and eating foods high in sodium.

Encourage supervised exercise.

Antihypertensive Agents: Nursing Implications Instruct patients to change positions slowly to avoid syncope from postural hypotension. Patients should report unusual shortness of breath; difficulty breathing; swelling of the feet, ankles, face, or around the eyes; weight gain or loss; chest pain; palpitations; or excessive fatigue.

Instruct patients to change positions slowly to avoid syncope from postural hypotension.

Patients should report unusual shortness of breath; difficulty breathing; swelling of the feet, ankles, face, or around the eyes; weight gain or loss; chest pain; palpitations; or excessive fatigue.

Antihypertensive Agents: Nursing Implications Men taking these agents may not be aware that impotence is an expected effect. This may influence compliance with drug therapy. If patients are experiencing serious side effects, or believe that the dose or medication needs to be changed, they should contact their physician immediately.

Men taking these agents may not be aware that impotence is an expected effect. This may influence compliance with drug therapy.

If patients are experiencing serious side effects, or believe that the dose or medication needs to be changed, they should contact their physician immediately.

Antihypertensive Agents: Nursing Implications Hot tubs, showers, or baths; hot weather; prolonged sitting or standing; physical exercise; and alcohol ingestion may aggravate low blood pressure, leading to fainting and injury. Patients should sit or lie down until symptoms subside. Patients should not take any other medications, including OTC drugs, without first getting the approval of their physician.

Hot tubs, showers, or baths; hot weather; prolonged sitting or standing; physical exercise; and alcohol ingestion may aggravate low blood pressure, leading to fainting and injury. Patients should sit or lie down until symptoms subside.

Patients should not take any other medications, including OTC drugs, without first getting the approval of their physician.

Antihypertensive Agents: Nursing Implications Monitor for side/adverse effects (dizziness, orthostatic hypotension, fatigue) and for toxic effects. Monitor for therapeutic effects Blood pressure should be maintained at less than 140/90 mm Hg

Monitor for side/adverse effects (dizziness, orthostatic hypotension, fatigue) and for toxic effects.

Monitor for therapeutic effects

Blood pressure should be maintained at less than 140/90 mm Hg

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