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59 Cards in this Set

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Behavioral changes to treat HTN should be used for ____ months before adding pharm agent
3-6
Antihypertensive drugs: Nonpharmacological therapy
Sodium restriction
Weight reduction
Exercise
Stress reduction
Elimination of risk factors
Cholesterol
Tobacco
Alcohol
Loop diuretics
Furosemide (Lasix)
Ethacrynic acid (Edecrin)
Diuretics: Potassium-sparing
Amiloride (Midamor)
Spironolactone (Aldactone)
Triamterene (Dyrenium)
Diuretics: MOA
Produce a moderate but persistent decrease in extracellular fluid and plasma volume
Initial reduction in BP is due to reduced CO
Later long-term BP reduction due to autoregulation which reduces TPR
Diuretics: Advantages
Effective in large number of patients as mono- or combination therapy
Inexpensive
Few side effects
Good experience and knowledge base in medical community
Diuretics: Disadvantages
Electrolyte imbalances can occur
Can elevate serum lipids
Can produce metabolic alkalosis
Carbohydrate metabolism can be impaired
Hyperuricemia can occur or increase
Diuretics are effective first-line therapy in what pts?
Effective first-line therapy in obese, elderly or black patients
when is diuretic dose given?
Dose patient once a day, early in the morning to decrease the incidence of nocturia
Uses of diuretics other than BP
Decrease intracranial pressure
Reduce intraocular pressure
Reduce edema/pulmonary edema
Treat congestive heart failure
Most common problems with diuretics
Loss of electrolytes is usually the most common problem
Dizziness
Cramps
Nausea
Postural hypotension
Effects usually diminish after few days
What is spironolactone?
Aldosterone antagonist
Weak progesterone
Bad effects of spironolactone?
Hyperkalemia can occur due to reduced K excretion
Gynecomastia (may or may not be reversible)
Cautions with diuretics and renal, gout, and DM pts
Thiazides reduce GFR - do not use in patients with decreased renal function
May precipitate gout by decreasing secretion of uric acid
Use cautiously in diabetics - can produce hyperglycemia
Include triameterine and amiloride
Do not antagonize aldosterone
Effective regardless of aldosterone status
More reliable than spironolactone
May produce hyperkalemia
Potassium-sparing diuretics: Direct-acting agents
Work at the loop of Henle
Urine volume is greater than with other agents
May cause hyperuricemia
Misuse can be life-threatening
Loop diuretics
CNS antihypertensive drugs
Methyldopa (Aldomet)
Clonidine (Catapres)
Guanabenz (Wytensin)
Guanfacine (Tenex)
Mechanism of methyldopa
Must be taken up into the neuron
Methyldopa is converted to methylNE and acts as false transmitter
Stimulates central alpha-2 receptors to decrease SNS outflow
Methyldopa: Side effects
Sexual dysfunction
Orthostatic hypotension
Adverse effects on lipid profiles
Somnolence is common especially during initial weeks of therapy
Depression may be unmasked or exacerbated
Methyldopa: Drug interactions
Haloperidol - dementia and sedation
Lithium - Lithium toxicity
Levodopa - hypotension
Propranolol - paradoxical hypertension
Sympathomimetics - hypertension
Tolbutamide - hypoglycemia
Clonidine mechanism
Direct alpha-2 receptor agonist


(Can stimulate alpha-1 receptors in the periphery and elevate BP)
Clonidine: Side effects
Dry mouth
Dizziness
Sedation
Constipation
Orthostatic hypotension
Sexual dysfunction
Incidence of side effects lower with cutaneous patch
Skin reactions with patch more frequent in women and patients with fair complexions
Insomnia
Depression
Nervousness
Agitation
Restlessness
Anxiety
Clonidine: Unlabeled uses
Alcohol withdrawal
Methadone/opiate detoxification
Smoking cessation
Menopausal flushing
Clonidine: Drug interactions
Beta blockers - increased severity of withdrawal syndrome
Tricyclic antidepressants - block hypotensive effects of clonidine
Actions similar to clondine
Duration of action may be longer
Side effect incidence appears to be less than with clonidine
Unlabeled uses include treatment of heroin withdrawal and migraine
Guanfacine
What is withdrawal syndrome related to stopping CNS acting BP drugs?
Occurs after abrupt discontinuation of CNS acting antihypertensives
BP is elevated and may exceed pretreatment levels
Anxiety, tremors, tachycardia and excessive SNS activity also observed
Typically occurs 18-36 hrs following drug discontinuation
May involve a central opioidergic component
Nonselective Beta blocking drugs
Propranolol (Inderal)
Nadolol (Corgard)
Timolol (Blocadren, Timoptic)
Penbutolol (Levatol)
Beta-1 selective Beta blocking drugs
Atenolol (Tenormin)
Acebutolol (Sectral)
Metoprolol (Lopressor)
Bisoprolol (Zebeta)
Betaxolol (Kerlone)
ISA
intrinsic sympathomimetic activity
Non-selective + ISA Beta blocking drugs
Pindolol (Viskin)
Carteolol (Cartrol)
Vasodilatory beta blocking drugs
Celiprolol (Selecor)
Beta blocking drugs: MOA
Beta blockade - decreases CO
Adrenergic blocking action
Taken up by presynaptic neuron
Displaces NE
Acts as ‘false transmitter’
Acts in CNS to reduce SNS outflow
Inhibits renin release

(MOST OF US THINK THIS INFO IS INCORRECT)
problems with propranolol
Highly protein bound (= side effects)
Subject to first pass metabolism


(compare to Nadolol
Long half-life
Not extensively protein bound)
Timolol can be used to treat what eye problem
glaucoma
Side effects of Excessive beta blockade
Bradycardia
Hypotension
Heart failure
Pulmonary dysfunction
CNS effects of beta blocking drugs
Depression
Nightmares
Insomnia
Beta blockers and DM problem
May mask signs of hypoglycemia in diabetics
Mixed blocking agents
Combines alpha-1 and beta-1 blockade
Labetolol (Normodyne, Transdate) and Carvedilol (Coreg)
Nonselective beta blockade more of a problem with carvedilol than ________
labetolol
Alpha antagonists
Prazosin (Minipress)
Terazosin (Hytrin)
Doxazosin (Cardura)
Alpha blockers are good to treat what male precancerous condition?
Useful in the treatment of benign prostatic hyperplasia (BPH)
Sympatholytics
Rauwolfia (Raudixin)
Reserpine (Serpasil, Serapase, Sandril)
Guanethidine (Ismelin)
Guanadrel (Hylorel)
Depletes NE from neuron by preventing storage of NE in granules
Inhibits amine transport system of granules
Reserpine
Adrenergic neuronal blockade due to:
Inhibition of action potential induced release of NE
Inhibition of NE reuptake
Displacement of NE
Guanethidine
Vasodilators (2)
Hydralazine (Apresoline)
Minoxidil (Loniten)
Hydralazine:
Side effects related to extensions of pharmacological effect or immune system
Tachycardia
Fluid retention
Headaches
Flushing
Hypotension
AND WHAT ELSE?
Lupus (at dosages >400 mg/day)
Minoxidil side effects
Fluid and water retention
Activation of reflexes
Hypertrichosis
Angiotensin converting enzyme (ACE) inhibitors
Captopril (Capoten)
Enalapril (Vasotec)
Enalaprilat
Lisinopril (Prinivil, Zestril)
Quinapril (Accupril)
Benazepril (Lotensin)
Ramipril (Altace)
Fosinopril (Monopril)
Moexipril (Univasc)
ACE inhibitors: Side effects
Hypotension (exacerbated by diuretics, low salt intake, high renin levels)
Cough
Angioedema (rare, but can lead to death)
Taste disturbances
Avoid in patients taking potassium sparing diuretics - can produce hyperkalemia
AII antagonists
Losartan (Cozaar)
Side effects of AII antagonists
diarrhea, dyspepsia, myalgia
Calcium antagonists
Verapamil (Calan, Isoptin)
Nifedipine (Procardia, Adalat)
Diltiazem (Cardizem)
Nimodipine (Nimotop)
Nicardipine (Cardene)
Isradipine (DynaCirc, Lomir, Prescal)
Amlodipine (Norvasc)
Felodipine (Plendil)
Nisoldipine
Nitrendipine
Bepridil (Vascor)
CCB with greatest effect on cardiac conduction (dromotropic effect)
Verapamil
CCB with minimal side effects
Diltiazem
uses of CCB
Angina
Hypertension
Arrhythmias (verapamil)
Raynaud’s disease
Hypertrophic cardiomyopathy
Side effects of CCBs
Cardiodepression
Hypotension
Peripheral edema (unresponsive to diuretics)
Constipation, dyspepsia, nausea
Headache
Facial flush, tingling, burning
Good effects of CCBs
Do not alter blood lipids
Maintain or increase GFR
Do not interfere with exercise
May induce slight natriuresis
_____and _______shown to increase digoxin levels
Verapamil and nifedipine
What CCB should not be used with beta blocking drugs due to synergistic cardiodepression
Verapamil