Pharm - S2B2 - 09 Ans 4

Front 1

List a REVERSIBLE (competitive) non-selective Alpha-adrenoceptor Antagonist?

Back 1

Phentol-amine

Front 2

List an IRREVERSIBLE non-selective Alpha-adrenoceptor Antagonist

Back 2

Phenoxy-benzamine

**long duration of action

Front 3

What is the pharmacologic effect of Alpha receptor Antagonists?

Back 3

Lower the PERIPHERAL VASCULAR RESISTANCE = reduce Blood Pressure

Front 4

What can be used to "reverse" Epinephrine?

Back 4

Alpha Antagonists
-block the Alpha-1 pressor effects
-do not block the Beta-2 venodilation effects = Postural Hypotension & reflex tachycardia

Front 5

What happens when you administer Epinephrine in the presence of an Alpha Antagonist? Explain

Back 5

Tachycardia & Decreased blood pressure
-decreased Diastolic blood pressor due to Epi on Beta-2
-tachycardia is due to reflex

Front 6

What happens when you give Phentolamine?

Back 6

Nonselective competitive Alpha antagonist
-reduces TPR & MAP
-produces reflex tachycardia = SNS reflex

Front 7

What drug is similar to Phentolamine?

Back 7

Tol-azol-ine

Front 8

What are Phentolamine and Phenoxybenzamine used for to treat?

Back 8

Pheochromocytoma = catecholamine secreting tumor

Front 9

What limits the use of both Phentolamine & Phenoxybenzamine?

Back 9

Postural hypotension & reflex tachycardia

Front 10

2 Alpha-1 Antagonists

Back 10

Pr-azosin & Ter-azosin

**1000-fold less potent at Alpha-2

Front 11

Alpha-1 Antagonist with a long half-life

What is it used to treat? (2)

Back 11

Dox-azosin

HTN & Urinary retention in BPH

Front 12

2 newer Competitive Alpha-1 Antagonists that have good efficacy in treating urinary retention in BPH

Back 12

Tamsul-osin

Alfuz-osin

Front 13

Alpha-2 selective antagonist that has no established clinical role but has been used in Erectile Dysfunction (with poor specificity)

Back 13

Yohim-bine

Front 14

What are Pheochromocytoma's?

What are the symptoms?

What is used to treat it? What is rarely used to treat it?

Back 14

Tumor of the Adrenal Medulla that releases a mixture of Epinephrine & Norepinephrine

HTN, Headaches, Palpitations, Sweating

Main: Phenoxybenzamine
Rarely: Metyrosine = competitive inhibitor of Tyrosine hydroxylase (Tyrosine ➡ L-dopa)

Front 15

What drugs are used in Hypertensive Emergencies?

Back 15

Direct Vasodilators = Nitrates

Front 16

Alpha Antagonists are effective in treating Chronic HTN, but may not prevent what?

What is their side effect?

Back 16

Heart Failure

Postural Hypotension

Front 17

What is the common ending for all Beta Antagonists?

Back 17

-olol

Front 18

T or F: There are NO Beta-antagonists that are absolutely specific for Beta-1 receptors

Back 18

TRUE

Front 19

Most Beta-antagonists are well absorbed after oral administration
1. when do peak concentrations occur?
2. What is the exception drug?

Back 19

1. 1-3 hours after ingestion

2. Esmolol = rapid hydrolysis produces half-life of 10 min

Front 20

Beta-antagonist that undergoes extensive hepatic (first-pass) metabolism

Back 20

Propanolol
-bioavailability is relative low
-must be accomodated for in: parenteral administration & individual differences in metabolism

Front 21

What effects do Beta-blockers have on the Cardiovascular system?

Back 21

1. lower Blood Pressure in patients with HTN (but doesn't cause hypotension in subjects with normal BP)

2. Negative Inotropic & Chronotropic effects

3. Slowed AV conduction; increased PR interval

Front 22

What effect do Beta-blockers have on the Respiratory tract?

Back 22

Inhibits Bronchodilation = increases airway resistance

Front 23

What are 2 Beta-1 antagonists that can exacerbate Asthmatic attacks?

Back 23

Metoprolol

Atenolol

**Beta-2's are usually the ones that cause Vasodilation but so can Beta-1's

Front 24

What effect do Beta-blocking agents have on the Eye?

Back 24

reduce Intraocular pressure = decreased Aqueous Humor production = Glaucoma treatment

Front 25

What metabolic effects do Beta-blockers possess?

In what patients should they be used with caution?

What is chronic use associated with? (2)

Back 25

Inhibit SNS stimulation of Lipolysis & Glycogenolysis (which is caused by Beta-2)

Insulin-dependent diabetics

1. increased plasma VLDL
2. decreased HDL cholesterol

Front 26

What does “Intrinsic sympathomimetic activity” mean when referring to Beta-blockers?

Back 26

While they provide blockade of the receptor, they can retain some partial agonist activity

Front 27

What is an example of a Beta-blocker with “Intrinsic sympathomimetic activity”?

Back 27

Dichlor-iso-proter-enol

Front 28

What 3 things may Beta-blockers with Partial agonist activity prevent?

Back 28

1. precipitation of asthma
2. Bradycardia
3. Alteration of plasma lipid profile

**may not be as effective as the pure antagonists in prevention of second MI

Front 29

Prototypical nonselective Beta-blocking drug

Back 29

Pro-pran-olol

Front 30

List 6 selective Beta-1 Antagonists

Back 30

Meto-prolol
Esm-olol
Aten-olol
Acebut-olol
Bextax-olol
Biso-prolol

Front 31

List 3 Beta-blockers with partial agonist activity (“Intrinsic sympathomimetic activity”)

Back 31

Pind-olol

Acebut-olol

Carte-olol

PAC partial agonist

Front 32

2 nonselective Beta-antagonists with very long duration of action

Back 32

Nad-olol

Tim-olol

Front 33

Reversible Alpha-1 antagonist with Nonselective Beta-blocker activity

Back 33

Labet-alol

Front 34

What happens when given Labetalol?

Back 34

Hypotension with less Tachycardia than alpha-blockers

**is an Alpha-1 blocker & nonselective Beta-blocker

Front 35

Ultra-short-acting Beta-1 blocker with it's structure containing ester linkage

Back 35

Es-m-olol

**esterases in RBC's rapidly hydrolyze to a low affinity metabolite

Front 36

Selective Beta-2 blocker

Back 36

Butox-amine


**has no clinical application

Front 37

List 5 general uses of Beta-blockers

Back 37

1. HTN

2. Ischemic Heart Disease

3. Cardiac Arrhythmias

4. Glaucoma

5. Hyperthyroidism

Front 38

What are Beta-blockers often used in combo with for treating HTN?

Back 38

Diuretic or Vasodilator drugs

Front 39

Discuss Beta-blockers and Ishcemic Heart Disease

Back 39

1. reduce the frequency of Anginal episodes
2. improve exercise tolerance
3. decrease cardiac work
4. reduce myocardial oxygen demand
5. good evidence that long-term use prolongs survival after MI

Front 40

What types of Arrhythmias are Beta-blockers effective in treating?

Back 40

Supraventricular

Ventricular

Front 41

What effects do Beta-blockers have that help in treatment of Arrhythmias?

Back 41

1. increase AV node refractory period

2. slows ventricular response rates in Atrial Fibrillation

3. Reduce ventricular ectopic beats

Front 42

What type of Glaucoma are Beta-blockers used to treat?

What 2 drugs are they better tolerated than in treating this type of glaucoma?

Back 42

Open-angle Glaucoma = decreased aqueous outflow into the Canal of Schlemm

Epinephrine or Pilocarpine

Front 43

What is the mechanism of action in which Beta-blockers treat glaucoma?

Back 43

reduce production of Aqueous Humor by the Ciliary Epithelium

Front 44

Why are Beta-blockers used to treat Hyperthyroidism?

Back 44

Many of the symptoms mimic sympathetic discharge

Beta-blockers limit excessive catecholamine activity

Front 45

List 4 minor toxic effects of Beta-blockers

Back 45

1. Rash
2. Fever
3. Sedation
4. Depression

Front 46

List the major adverse effects of Beta-blocker toxicity

Back 46

1. worsening of preexisting asthma

2. depression of myocardial contractility & excitability

3. Supersensitivity with abrupt discontinuation after chronic use

4. can exacerbate Hypoglycemic episodes in Diabetics

Front 47

What could happen if you abruptly discontinue Beta-blocker use after chronic use?

Back 47

Supersensitivity could cause Hypertensive Crisis

**to prevent, gradually taper dosage

Front 48

What are 2 Adrenergic neuron blocking drugs (get into neuron and prevent catecholamine packaging)

Back 48

Reserpine = inhibits transport of NE into vesicles

Guanadrel