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81 Cards in this Set

  • Front
  • Back
What are 85-90% of Hypertension cases due to?
Unknown = Essential HTN
How is Hypertension usually manifested initially?
usually a SILENT DISEASE that is asymptomatic as most hypertensives usually feel well & progressive cardiovascular damage develops very gradually

Generally remains asymptomatic for 15-20 years until vital organs (Heart, brain, kidneys) become damaged
What is the 1st step in the treatment of Hypertension?
Life-stype modifications
1. exercise
2. weight reduction
3. moderatation of dietary salt, fats, & alcohol
4. avoid or reduce smoking
5. before, or together with, drug therapy
What is the most common cause of treatment failure in treating HTN?
List the 3 main goals of Anti-HTN drug treatment
1. lower BP & keep it normal
2. reduce CV risks
3. produce minimal side-effects without decreasing quality of life
Aside from mechanism of action, how do most Anti-HTN drugs differ?
Adverse or side effects
At what diastolic pressure is there inadequate Coronary perfusion & increased CV morbidity & mortality?
lower than 90 mm Hg
How do drugs lower BP?
1. Reduce blood volume = ?
2. Interrupt Sympathetic tone = ?
3. Vasodilation = ?
1. Diuretics

2. Sympatholytics

3. Direct Vasodilators; CCA's; ACE inhibitors & AT-II Antagonists
What are the 2 mechanisms in which Diuretics lower BP?
1. initially deplete body Na+ stores -> reduce blood volume

2. Later activate K+ channels -> reduce vascular resistance
Diuretic that is recommended for Mild to Moderate HTN & when used:
-alone will lower BP in 40-60% of patients, and
-in drug combinations will enhance efficacy of other Anti-HTN drugs
Which doses of Diuretics are higher, those used for Anti-HTN purposes or those used for Diuresis?
Diuresis = 100-200 mg

Anti-HTN = 6-12 mg
Which diuretic is primarily used for HTN?
Which diuretic is primarily used for CHF?
-Ethacrynic acid
What 2 general types of Sympatholytic Drugs are used to lower BP?
1. Central agonists = stimulate medullary receptors

2. Peripheral Antagonists = block receptors at nerve endings
Why are Sympatholytics generally not recommended for monotherapy?
produce Side-effects of:
1. Postural Hypotension
2. Sodium retention
List the 4 Centrally Acting Sympatholytics
1. Clonidine
2. Methyldopa
3. Guanabenz
4. Guanfacine
This is a prodrug Centrally Acting Sympatholytic
Methyldopa = converted to alpha-methylnorepinephrine
What is the mechanism of action of the Centrally Acting Sympatholytics?
Act as AGONISTS that stimulate Medullary Alpha-2 adrenergic receptors to reduce peripheral Sympathetic tone & lower BP by:
1. decreasing Vasoconstrictor tone = Vasodilation
2. Decrease Renal Renin Secretion
How are the Centrally Acting Sympatholytics usually administered?

Which one can be used as a Transdermal or Skin Patch?

What are the side effects of the Centrally Acting Sympatholytics?
CNS effects = Sedation, Nausea, dizziness, nightmaires, depression, Postural Hypotension

Dry mouth
Sudden withdrawal of this Centrally Acting Sympatholytic may cause of Hypertensive Crisis
Centrally acting Sympatholytic that may produce Hemolytic Anemia with a Positive Coombs test
What are the possible side effects of Methyldopa use?
1. Hemolytic anemia with + Coombs test
2. Hepatotoxicity
3. Gynecomastia
4. Lactation
What 3 drugs act by binding to Secretory Vesicles that normally store & release NE in peripheral endings?
1. Guanadrel

2. Guanethidine

3. Reserpine

*reduce sympathetic activity by preventing NE release to reduce sympathetic activity, cause vasodilation, & lower BP
Sudden release of endogenous NE when _______ is given IV may elevate BP
What are the common ADR's of Guanethidine?
1. Postural Hypotension
2. Fluid retention
3. Diarrhea
4. Retrograde ejactulation
What are the common ADR's of Reserpine?
1. Sedation
2. Psychic depression
3. Nasal stuffiness
4. Dry mouth
5. GI disturbances
List the Non-selective Beta Antagonists
1. Propranolol
2. Cartelol
3. Nadolol
4. Sotalol
5. Timolol
List the Cardioselective Beta-1 blockers
1. Betaxolol & Bisoprolol
2. Esmolol
3. Acebutolol
4. Atenolol
5. Metoprolol
List the 3 Intrinsic Sympathomimetic Activity Beta blockers that manufacturers claim produce less Cardiac Depression & are preferred for Hypertensive pts with CHF
1. Penbutolol
2. Acebutolol
3. Pindolol
List the 3 ways in which Beta blockers lower BP
by blocking Beta receptors in:
1. Heart to reduce CO = Beta-1
2. Kidneys to reduce Renin secretion = Beta-1
3. CNS to reduce sympathetic vasomotor tone
In what group of people are the Beta blockers most efficacious in?
Caucasians & younger people
In what patients are Beta blockers recommended for monotherapy?
Young White Males
What are Beta blockers combined with other Anti-HTN drugs to counteract? (2)
1. Reflex Tachycardia caused by Vasodilators

2. Increased Renin secretion caused by Thiazide & Loops Diuretics
What may Beta blockade worsen the symptoms of?
1. Pts with reduced Myocardial reserve = Beta-1 blockade
2. Asthma = Beta-2 blockade
3. Peripheral Vascular Insufficiency
4. Diabetes = Beta-2 blockade of Insulin release
When may Beta blockers increase exercise tolerance?

When may they decrease exercise tolerance?
In patients being treated for Angina

In patients with CHF -> reduces CO -> earlier onset of fatigue
How may Beta blockers predispose to Atherogenesis?
1. increasing plasma Triglycerides

2. decreasing HDL-cholesterol
What does Beta blockade delay the recovery of>
Normoglycemia b/c it inhibits hyperglycemic responses mediated by Epinephrine on pancreatic Beta-2 receptors to release Insulin
What are minor side effects of Beta blockers?
GI = NVD, constipation

CNS = insomnia, lassitude, nightmares, depression

Skeletal muscle tremors
List the common ending for the Alpha-1 antagonists

1. Prazosin
2. Terazosin
3. Doxazosin
How do the "-ZOSIN's" reduce blood pressure?
Alpha-1 blockade reduces NE-induced vasoconstriction to dilate both arteries & veins
What are the common ADR's of the -AZOSIN's?
1. Postural Hypotension (usually with 1st dose)
2. Dizziness, headache, drowsiness, palpitations, heachache, easy fatigability
What 2 drugs have combined Alpha & Beta blockade?
1. Labetalol

2. Carvedilol

*lower BP by non-selective blockade of both Alpha- & Beta receptors
What is the Beta:Alpha block ration after ORAL LABETALOL is given?
Beta:Alpha = 3:1
What are the ADR's of Labetalol & Carvedilol?
1. Orthostatic Hypotension
2. Bronchospasm
3. Hepatotoxicity
What are Labetalol & Carvedilol used mainly for the treatment of?
1. Hypertensive emergencies

2. Pheochromocytoma = tumor of the Adrenal Medulla that secretes Epi & NE
Vasodilators given orally for Chronic Anti-HTN treatment
Hydralazine or Minoxidil
Vasodilators given IV for Hypertensive emergencies (5)
1. Sodium Nitroprusside
2. Diazoxide
3. Fenoldopam
4. Enalaprilat
5. Nicardipine

These 3 vasodilators dilate ARTERIES selectively without affecting venous smooth muscles
1. Hydralazine

2. Minoxidil

3. Diazoxide
Dilates arteries by acting as a Dopamine D1-agonist
Non-selective or balanced vasodilator that dilates both arteries & veins
Sodium Nitroprusside
Are Vasodilators used for Monotherapy? Why?

Anti-hypertensive effects tend to diminish with time b/c of Reflex Tachycardia & increased Renin secretion
When are Vasodilator drugs most effective?
When combined with other drugs to prevent undesirable side-effects
What are Hydralazine & Minoxidil combined with?
1. Diuretics = to avoid fluid retention

2. Beta blockers = to diminish Renin secretion & Reflex Tachycardia
-Renin secretion blockage = Beta-1 blockage
-Reflex Tachycardia blockage = Beta-1 blockage
Hypotension produced by any Vasodilator drug will be accompanied by these things
1. Reflex Tachycardia, increased Myocardial contractions

2. Increased Renin secretion

3. Fluid retention, headaches, flushing, palpitations, or dizziness
What 2 drugs may induce Anginal attacks & Myocardial Ischemia through reflex increases in Cardiac Output in Elderly patients with coronary artery disease?

Vasodilator that may cause a Lupus-like syndrome consisting of fever, skin rashes, arthralgia, & myalgia
Vasodilator that causes Hyperthrichosis (excess hair growth); topical ointment "Rogaine"
List the drugs contained within the Calcium Channel Blockers class
1. Verapamil
2. Diltiazem
3. Dihydropyridines = "-DIPINES"
What is the mechanism of action of the CCA's in lowering BP?
1. reduce IC Ca++
2. relax Arteriolar smooth muscles
3. vasodilation & lower BP
Drugs that are equally effective for monotherapy in mild to moderate HTN especially in the Elderly & African-Americans
Calcium Channel Blockers

CCA that is the strongest Vasodilator and most likely to produce Reflex Tachycardia

*also has smallest inhibition of AV conduction
Why do Verapamil & Diltiazem not cause Reflex Tachycardia?
b/c they depress SA & AV node conduction directly
When are Verapamil & Diltiazem contraindicated?
in patients with SA or AV node abnormalities


*may cause Bradycardia in the presence of SA node dysfunction
MC side effect of Verapamil
CCA's that are most likely to cause headache, flushing, dizziness, & peripheral edema
Dihydropyridines = '-DIPINE's' = Nifedipine

Greatest effect is Vasodilation
What is the common ending for ACE inhibitors?
Only active ACE inhibitor, all others are prodrugs that have to be converted to the corresponding di-acid
How do ACE inhibitors lower BP?
Inhibit ACE = inhibit conversion of Antiogentin I -> Angiotensin II

-Inhibit AT-II vasoconstriction
-also inhibit ACE destruction of Bradykinin
What are the side effects of the ACE inhibitors?
CAPTOPRIL + Hyperkalemia
1. Cough (due to Bradykinin)
2. Angioedema & Anaphylaxis(due to Bradykinin)
3. Proteinuria
4. Taste changes
5. hypOtension
6. Pregnancy proglems (fetal renal damage)
7. Rash
8. Increased renin
9. Lower angiotensin-II
List the advantages of ACE Inhibitors
1. lower BP without compromising blood supply to the heart, brain, or kidneys

2. side-effects are mild, fewer, & without lipid changes

3. do not cause reflex tachycardia b/c of concurrent baroreceptor resetting or vagal activation

4. are effective orally for monotherapy & will lower BP in 50% of pts with mild to moderate HTN
What groups of people are ACE inhibitors most effective in?
Young & Middle-aged Caucasians

*less effective in Elderly AA's
What 3 things are ACE inhibitors the 1st choice of treatment for HTN in pts?
1. Diabetes

2. Chronic Renal disease

3. Left Ventricle Hypertrophy
What is the common ending for Angiotensin Receptor Antagonists?
Which receptor do the -SARTAN's bind to? Where is this receptor located?
AT1 receptor in vascular smooth muscle
What are the 2 important differences between Angiotensin receptor antagonists & ACE inhibitors?
1. -SARTAN's are more specific than ACE inhibitors b/c AT-II antagonists do not affect Bradykinin metabolism = no coughing or Angioedema

2. -SARTAN's have more complete inhibition of Angiotensin action b/c enzymes other than ACE can generate Angiotensin-II
What are some adverse effects of the -SARTAN's?

Fetal Renal toxicity
What Anti-hypertensive drugs can be used as monotherapy?
1. Diuretics
2. Beta blockers
3. ACE inhibitors
4. CCA's
With what anti-HTN drugs do Elderly males often complain of Impotence?
Thiazides or Sympatholytics