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48 Cards in this Set

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List a REVERSIBLE (competitive) non-selective Alpha-adrenoceptor Antagonist?
Phentol-amine
List an IRREVERSIBLE non-selective Alpha-adrenoceptor Antagonist
Phenoxy-benzamine

**long duration of action
What is the pharmacologic effect of Alpha receptor Antagonists?
Lower the PERIPHERAL VASCULAR RESISTANCE = reduce Blood Pressure
What can be used to "reverse" Epinephrine?
Alpha Antagonists
-block the Alpha-1 pressor effects
-do not block the Beta-2 venodilation effects = Postural Hypotension & reflex tachycardia
What happens when you administer Epinephrine in the presence of an Alpha Antagonist? Explain
Tachycardia & Decreased blood pressure
-decreased Diastolic blood pressor due to Epi on Beta-2
-tachycardia is due to reflex
What happens when you give Phentolamine?
Nonselective competitive Alpha antagonist
-reduces TPR & MAP
-produces reflex tachycardia = SNS reflex
What drug is similar to Phentolamine?
Tol-azol-ine
What are Phentolamine and Phenoxybenzamine used for to treat?
Pheochromocytoma = catecholamine secreting tumor
What limits the use of both Phentolamine & Phenoxybenzamine?
Postural hypotension & reflex tachycardia
2 Alpha-1 Antagonists
Pr-azosin & Ter-azosin

**1000-fold less potent at Alpha-2
Alpha-1 Antagonist with a long half-life

What is it used to treat? (2)
Dox-azosin

HTN & Urinary retention in BPH
2 newer Competitive Alpha-1 Antagonists that have good efficacy in treating urinary retention in BPH
Tamsul-osin

Alfuz-osin
Alpha-2 selective antagonist that has no established clinical role but has been used in Erectile Dysfunction (with poor specificity)
Yohim-bine
What are Pheochromocytoma's?

What are the symptoms?

What is used to treat it? What is rarely used to treat it?
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)
What drugs are used in Hypertensive Emergencies?
Direct Vasodilators = Nitrates
Alpha Antagonists are effective in treating Chronic HTN, but may not prevent what?

What is their side effect?
Heart Failure

Postural Hypotension
What is the common ending for all Beta Antagonists?
-olol
T or F: There are NO Beta-antagonists that are absolutely specific for Beta-1 receptors
TRUE
Most Beta-antagonists are well absorbed after oral administration
1. when do peak concentrations occur?
2. What is the exception drug?
1. 1-3 hours after ingestion

2. Esmolol = rapid hydrolysis produces half-life of 10 min
Beta-antagonist that undergoes extensive hepatic (first-pass) metabolism
Propanolol
-bioavailability is relative low
-must be accomodated for in: parenteral administration & individual differences in metabolism
What effects do Beta-blockers have on the Cardiovascular system?
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
What effect do Beta-blockers have on the Respiratory tract?
Inhibits Bronchodilation = increases airway resistance
What are 2 Beta-1 antagonists that can exacerbate Asthmatic attacks?
Metoprolol

Atenolol

**Beta-2's are usually the ones that cause Vasodilation but so can Beta-1's
What effect do Beta-blocking agents have on the Eye?
reduce Intraocular pressure = decreased Aqueous Humor production = Glaucoma treatment
What metabolic effects do Beta-blockers possess?

In what patients should they be used with caution?

What is chronic use associated with? (2)
Inhibit SNS stimulation of Lipolysis & Glycogenolysis (which is caused by Beta-2)

Insulin-dependent diabetics

1. increased plasma VLDL
2. decreased HDL cholesterol
What does “Intrinsic sympathomimetic activity” mean when referring to Beta-blockers?
While they provide blockade of the receptor, they can retain some partial agonist activity
What is an example of a Beta-blocker with “Intrinsic sympathomimetic activity”?
Dichlor-iso-proter-enol
What 3 things may Beta-blockers with Partial agonist activity prevent?
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
Prototypical nonselective Beta-blocking drug
Pro-pran-olol
List 6 selective Beta-1 Antagonists
Meto-prolol
Esm-olol
Aten-olol
Acebut-olol
Bextax-olol
Biso-prolol
List 3 Beta-blockers with partial agonist activity (“Intrinsic sympathomimetic activity”)
Pind-olol

Acebut-olol

Carte-olol

PAC partial agonist
2 nonselective Beta-antagonists with very long duration of action
Nad-olol

Tim-olol
Reversible Alpha-1 antagonist with Nonselective Beta-blocker activity
Labet-alol
What happens when given Labetalol?
Hypotension with less Tachycardia than alpha-blockers

**is an Alpha-1 blocker & nonselective Beta-blocker
Ultra-short-acting Beta-1 blocker with it's structure containing ester linkage
Es-m-olol

**esterases in RBC's rapidly hydrolyze to a low affinity metabolite
Selective Beta-2 blocker
Butox-amine


**has no clinical application
List 5 general uses of Beta-blockers
1. HTN

2. Ischemic Heart Disease

3. Cardiac Arrhythmias

4. Glaucoma

5. Hyperthyroidism
What are Beta-blockers often used in combo with for treating HTN?
Diuretic or Vasodilator drugs
Discuss Beta-blockers and Ishcemic Heart Disease
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
What types of Arrhythmias are Beta-blockers effective in treating?
Supraventricular

Ventricular
What effects do Beta-blockers have that help in treatment of Arrhythmias?
1. increase AV node refractory period

2. slows ventricular response rates in Atrial Fibrillation

3. Reduce ventricular ectopic beats
What type of Glaucoma are Beta-blockers used to treat?

What 2 drugs are they better tolerated than in treating this type of glaucoma?
Open-angle Glaucoma = decreased aqueous outflow into the Canal of Schlemm

Epinephrine or Pilocarpine
What is the mechanism of action in which Beta-blockers treat glaucoma?
reduce production of Aqueous Humor by the Ciliary Epithelium
Why are Beta-blockers used to treat Hyperthyroidism?
Many of the symptoms mimic sympathetic discharge

Beta-blockers limit excessive catecholamine activity
List 4 minor toxic effects of Beta-blockers
1. Rash
2. Fever
3. Sedation
4. Depression
List the major adverse effects of Beta-blocker toxicity
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
What could happen if you abruptly discontinue Beta-blocker use after chronic use?
Supersensitivity could cause Hypertensive Crisis

**to prevent, gradually taper dosage
What are 2 Adrenergic neuron blocking drugs (get into neuron and prevent catecholamine packaging)
Reserpine = inhibits transport of NE into vesicles

Guanadrel