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Human Disease And Therapeutics > Week 6 (test 2) > Flashcards

Week 6 (test 2) Flashcards

1
Q

What are the four classes of antihypertensive drugs?

A

Diuretics

Sympathaoplegics

Direct vasodilators

Anti-angiotensin agents

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2
Q

How do direct vasodilators work?

A

Relax vascular smooth muscle, thus dilating resistance vessels and sometimes increasing capacitance

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3
Q

How do anti-angiotensin agents work?

A

Inhibit action/production of angiotensin and thus reduce peripheral vascular resistance (and sometimes blood volume)

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4
Q

How do diuretics work?

A

Deplete sodium, reduce blood volume, and perhaps by other mechanisms.

Long-term diuretic - decreased TPR

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5
Q

How do sympathoplegics work?

A

Reduce peripheral vascular resistance. (Also inhibit cardiac function, and increase venous pooling, thus reducing cardiac output)

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6
Q

Where do osmotic agents (mannitol) work on the nephron? Describe how it works.

A

Mannitol is a diuretic that works on the thin descending limb.

Mannitol is not reabsorbed and thus water is retained

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7
Q

What is mannitol used to treat?

A

Not HTN. It is used for increased intracranial pressure after head trauma

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8
Q

Where does acetazolamide work on the nephron? What does it do?

A

On the proximal convoluted tubule.

It is a carbonic anhydrase inhibitor. It shuts down resorption of bicarbonate into interstitial space. Thus less sodium resabsorption. Thus more NA in the lumen remains.

Causes alkaline urine (more bicarbonate in urine)

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9
Q

What are carbonic anhydrase inhibitors used to treat?

A

Not HTN. Used as a diuretic for glaucoma and other disorders.

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10
Q

Name two loop diuretics. How well do these work?

A

***Furosemide (lasix)

Bumetanide (bumex)

These are very efficacious

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11
Q

Describe how loop diuretics work.

A

Inhibit the luminal Na/K/2Cl transporter in the thick ascending limb of the loop of henle. Thus reducing NaCl absorption, thus increasing urine output.

More potent and more side effects

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12
Q

Loop diuretics are inhibited by ___ under certain conditions.

A

NSAIDs

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13
Q

What is a major side effect of loop diuretics? Why is this an issue?

A

Hypokalemia - increase luminal sodium and thus stimulates the aldosterone-sensitive sodium pump to increase sodium reabsorption in exchange for potassium which is lost in the urine.

This can cause heart arrhythmias

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14
Q

Where do thiazide diuretics work?

A

On the distal convoluted tubule of the nephron

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15
Q

Name two thiazides

A

***Hydrochlorthiazide

Chlorthalindone

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16
Q

How do thiazides work? What is a side effect? What is it inhibited by?

A

Inhibit NaCl reabsorption by blocking the Na/Cl transporter.

Can cause hypokalemia

Inhibited by NSAIDs under certain conditions

Note that it is often first order elimination

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17
Q

In addition to heart arrhythmias, hypokalemia can also lead to…

A

Decreased insulin secretion and thus hyperglycemia

*dont give drugs that cause hypokalemia to pts with poor glucose control

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18
Q

Name 3 potassium-sparing diuretics

A

Spironolactone

Amiloride

Trimterene

Usually combined with other diuretics, especially the thiazides

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19
Q

Describe how potassium-sparing diuretics work

A

Prevent K secretion by antagonizing effects of aldosterone in collecting tubules (via blockade of mineralocorticoid receptors) (spironolactone)

Or Na+ influx through ion channels in the luminal membrane (amiloride)

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20
Q

Potassium sparing diuretics are often used in combination with ____ to offset hypokalemia. They are not used with ___ because it worsens hypokalemia

A

Loop diuretics

ACE-1

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21
Q

Describe how ACE-inhibitors work

A

ACE inhibitors prevent the conversion of angiotensin 1 to angiotensin 2.

Angiotensin 2 normally leads to constriction, so less angiotensin = less constriction and lower BP

ACE normally will breakdown Bradykinin. If ACE is inhibited, bradykinin accumulates which will ultimately lead to vasodilation

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22
Q

What kind of a drug is captopril? How does it work?

A

ACE inhibitor

Inhibits the converting enzyme (peptidyl dipeptidase) that hydrolyzes angiotensin 1 to angiotensin 2

Increases bradykinin levels (potent vasodilator)

Therefore inhibit renin-angiotensin system and a stimulate the kallikrein-kinin system

Hyperkalemia because little aldosterone (aldosterone promotes Na retention and thus lower plasma K levels)

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23
Q

What is a side effect of increased bradykinin?

A

Dry cough

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24
Q

What kind of a drug is losartan? How does it work?

A

Antiotensin 2 inhibitor

Decreases peripheral vascular resistance

No effect on bradykinin metabolism and therefore more selective blocker of angiotensin effects than ACE inhibitors

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25
Q

What kind of drug is hydralazine, verapamil, diltiazem, nifedipine, and minoxidil?

A

These are all direct vasodilators

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26
Q

What is the mechanism of action of hydralazine, nitroglycerin and nitroprusside direct vasodilators?

A

Release of nitric oxide form drug or endothelium

Note that hydralazine also hyperpolarizes smooth muscle?

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27
Q

What is the mechanism of verapamil and diltiazem, (direct vasodilators)?

A

Reduction of calcium influx (causing muscle relaxation)

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28
Q

What is the mechanism of minoxidil and diazoxide (direct vasodilators)?

A

Hyperpolarization of smooth muscle membrane through opening of potassium channels

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29
Q

What is the mechanism of fenoldopam (direct vasodilator)

A

Activation of D1 receptors

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30
Q

True or false… sodium nitroprusside also relax veins

A

True

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31
Q

Why dont direct vasodilators cause orthostatic hypotension?

A

Decreased arterial resistance and decreased mean arterial BP elicit compensatory responses, mediated by baroreceptors and the sympathetic nervous system. Because sympathetic reflexes are intact, vasodilator therapy generally does not cause orthostatic hypotension.

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32
Q

Where are some locations where sympathoplegics act?

A

Sympathetic nerve terminals

B-receptors of heart

A-receptors of vessels

Sympathetic ganglia

Vasomotor center (central)

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33
Q

True or false… clonidine has its antiHTN affects based on central mechanisms

A

True

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34
Q

What is the mechanism of clonidine? What are some side effects?

A

It is an alpha 2 agonist (recpetors in medulla)

Reduces sympathetic tone, resulting in decreased blood pressure

Dry mouth and sedation are common. Both effects are centrally mediated and dose dependent

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35
Q

What is mecamylamine?

A

In is a Nn antagonist. It binds nicotinic cholinoceptors and post ganglionic neurons in both sympathetic and parasympathetic ganglia.

Causes both sympathoplegia (excessive orthostatic hypotension) and parasympatheplegia (constipation, urinary retention, glaucoma, blurred vision, dry mouth etc.)

Rarely used

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36
Q

What is guanethidine? How does it work? What is a side effect of it?

A

Adrenergic blocking agent

Inhibits the release of NE from sympathetic nerve endings by depleting NE stores.

Causes orthostatic hypotension (because of lack of sympathetic compensation), diarrhea

37
Q

What kinds of drugs are atenolol and metoprolol?

A

B1 antagonists (cardioselective)

38
Q

What kind of drug is propranolol and nadolol?

A

B1 and B2 antagonists. (Non-cardioselective)

39
Q

Propranolol ___ the stimulation of renin production by ____ and thus it is likely that propranolol’ effect is due in part to depression of the renin-angiotensin-aldosterone system

A

Inhibits

Catecholamines

40
Q

What kind of drug is labetalol and carvedilol?

A

Beta + alpha 1 antagonist

41
Q

Beta blockers can be used to treat what three things?

A

HTN

Angina

Open-angle glaucoma

42
Q 
What are beta blockers' effects on the following tissues? 
Cardiac
Vascular
Renal
Respiratory
Metabolic
Aqueous humor
Arrhythmias
A

Cardiac: decreased HR and contractility (impairs excerise tolerance)

Vascular: increased TPR (blockade of B2 in skeletal muscle)

Renal: decreased renin release

Respiratory: bronchial constriction

Metabolic**: decreased glycogenolysis in response to hypoglycemia

Decreased aqueous humor production

May block tachycardia associated with hypoglycemia

43
Q

What kind of drug is prazosin, terazosin, and doxazosin?

A

Alpha 1 antagonists. (Cardioselective) prevents catecholamines from causing vasoconstriction

44
Q

What kind of drug is phentolamine and phenoxybenzamine?

A

Alpha 1 and alpha 2 antagonists. (Non-cardioselective)

45
Q

What are the effects and uses for alpha 1 antagonists?

A

Vasodilation (because it prevents vasoconstriction) and thus decreased TPR and decreased BP

Uses: treat HTN. Benign prostatic hypertrophy (use tamsulosin)

46
Q

What are the side effects of alpha 1 antagonists?

A

Orthostatic hypotension (if someone is one prazosin, be careful getting them out of the dental chair)

Nasal congestion

47
Q

What kind of a drug is hydrochlorthizide?

A

Thiazides

48
Q

What kind of a drug is furosemide?

A

Loop diuretic

49
Q

What is the most common cause of angina pectoris?

A

Ischemic heart disease

50
Q

What are the two treatment strategies to treat angina?

A

Vasodilation (using direct vasodilators) - immediate but short acting relief

Decrease O2 consumption - prevent the pain onset by decreasing the demand of oxygen of the heart (use b-blockers, and calcium channel blockers)

51
Q

What are the two types of nitrates/nitrites that are used to treat angina? Describe them.

A

Nitroglycerin (administer sublingually). Volatile -store in closed glass container. Also long-lasting patches (~8hours) tolerance occurs, exposes pt to side effects. If pain goes away with nitroglycerin, it probably isn’t a heart attack

Amyl nitrate - ample crusehd and fumes inhaled. Short acting. Not used much anymore.

52
Q

What are the side effects of nitroglycerin/amylnitrate?

A

Toxicity and tolerance (tolerance develops rapidly. Need ~8 hours between use to diminish tolerance)

Orthostatic hypotension

Tachycardia

Throbbing headache

53
Q

What is the mechanism of calcium channel blockers in the use of treating angina?

A

Prevent calcium influx through L-type channels and block contraction of smooth and cardiac muscle-reduce O2 demand

54
Q

Name three calcium channel blocker drugs that are used as prophylaxis for angina (lasts 4-8 hours)

A

Verapamil

Nifedipine

Diltiazem

(These are also used as antihypertensives)

55
Q

Describe the toxicity associated with calcium channel blockers

A

Cardiac depression and bradycardia - heart failure

Flushing and dizziness

56
Q

True or false.. B-blockers are vasodilators

A

False. They reduce output by decreasing HR and contractility, decreasing BP and decreasing O2 requirements

Used as a prophylactic

57
Q

What are the principal B-blockers used for prophylaxis of angina

A

Propranolol (non selective B antagonist)

Atenolol (B1 selective antagonist. Less risk for bronchospasms)

Toxicity: asthma and acute heart failure

58
Q

True or false… cigarette smoking raises HDL values

A

False, it lowers it. Low HDL is a risk factor for atherosclerosis

59
Q

Hypertriglyceridemia is associated with increased __ and ___

A

VDL and LDL

60
Q

What are the non-drug treatments for lower cholesterol?

A

Dietary (doesn’t help more than 10%) Reduce fat, avoid alcohol if VLDL elevated, avoid red meats, include complex carbohydrates and fiber

Exercise

61
Q

True or false. Cholesterol-lowering drugs should be avoided in pregancy. Why or why not?

A

True. The fetus needs cholesterols to develop the brain

62
Q

What is the mechanism of statins?

A

Competitive inhibitors of HMG-COA reductase (enzyme that synthesizes cholesterol)

63
Q

Name three statins

A

Lovastatin

Atorvastin

Simvastatin

64
Q

Statins reduce synthesis of ___ and have most effect on ___.

A

Cholesterol

LDL (some decrease in triglycerides)

Doesn’t really have an impact on HDLs. These drugs will reduce coronary events

65
Q

What are the toxic effects of statins?

A

Liver damage

Weakness and pain in skeletal muscles

66
Q

What is the mechanism of fibrates?

A

Increases lipolysis in liver and muscles

Reduces VLDL most. Modest effect on LDL. Some reduction in triglycerides. Moderate increases in HDL.

67
Q

What kind of a drug is fenobrate?

A

Fibrate (used to decrease cholesterol)

68
Q

What are the toxic effects of fibrates?

A

Primarily GI symptoms (gas and cramps)

69
Q

What is the mechanism of niacin (nicotinic acid)? What are its side effects?

A

Decreases triglyceride and LDL

Side effects: flushing. Tolerance develops

70
Q

What kind of a drug is cholesteramine? Describe its mechanism and its toxicity.

A

Bile acid-binding agent

Reduces reabsorption of biles acids and metabolites

Toxicity: constipation and bloating

71
Q

What kind of a drug is ezetimibe? How does it work?

A

Inhibitor of intestinal sterol absorption

Inhibits intestinal absorption of cholesterol and reduces LDL

72
Q

What is the main goal with drugs that treat heart failur?

A

Control symptoms and slow progression

Symptoms such as...
Tachycardia
Reduced exercise tolerance
Myocardial hypertrophy
Shortness of breath
Peripheral and pulmonary edema
73
Q

Name two positive ionotropic drugs. What is their mechanism and side effects?

A

Digitalis and milrinone

Increases intracellular calcium and cardiac contractility - in turns increases blood ejection

Side effects: premature depolarization- arrhythmias. Ectopic beats. Affects all excitable tissues

74
Q

True or false.. positive ionotropic drugs are orally effective

A

True

75
Q

What kind of a drug is dobutamine? What is a side effect?

A

B-1 adenoceptor agonist

Used to treat heart failure

Side effect: can cause arrhythmias

76
Q

Diuretics, especially ___ are useful in treating heart failure. It has no positive ionotropic effect but how does it work?

A

Furosemide

Reduces salt and H2O retention

Reduces venous pressure and ventricular preload

77
Q

How are ACE inhibitors such as ___ useful in treating heart pain?

A

Captopril

Reduces peripheral resistance by reducing salt and water retention

78
Q

Vasodilators such as ___ are used to treat heart failure because it…

A

Hydralazine

Reduces pre- and post- load/smooth muscle relaxant

79
Q

B-adenoceptor blockers such as ___ are used to treat heart failure because it…

A

Metoprolol

Reduces heart rate and blocks sympathetic NS

80
Q

What is a non drug treatment for treating heart failure?

A

Eat less salt!

81
Q

80% of pateints with arrhythmias have a history of ___

A

Myocardial infarction

Note that treatment of arrhythmias can precipitate serious arrhythmias itself

82
Q

Name 7 treatments for heart failure

A

Positive ionotropic drugs

B1 adenoceptor agonists

Diuretics

ACE inhibitors

Vasodilators

B-adrenoceptor blocker

Eat less salt

83
Q

How do sodium channel blockers treat arrhythmias?

A

Slows action potential conduction

Effective for most atrial and ventricular arrhythmias

Can precipitate new arrhythmias

Usually not first choice drug

84
Q

Name 3 sodium channel blockers used to treat arrhythmias

A

Procainamide (never first choice)

Quinidine

Lidocaine (low toxicity, first choice for ventricular arrhythmias)

85
Q

What is the first choicedrug for treating ventricular arrhythmias?

A

Lidocaine

86
Q

Name one beta blocking drug used for treating arrhythmias

A

Propranolol (class 2)

87
Q

Describe the 4 different classes of drugs that are used to treat arrhythmias

A

Class 1 - sodium channel blockers

Class 2 - block sympathetic autonomic effects on heart

Class 3 - prolong refractory period

Class 4 - calcium channel blockers

88
Q

Name one drug that prolongs the refractory period used for treating arrhythmias. What is a side effect?

A

Amiodarone (treats ventricular arrhythmias and atrial fibrillation)

Causes pulmonary fibrosis

89
Q

Name two calcium channel blockers (class 4) used to treat arrhythmias

A

Verapamil
Diltiazem

Prolongs refractory time and causes vasodilation (antihypertensive effect)

Human Disease And Therapeutics (13 decks)

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