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Flashcards in Adrenergic Pharm I Deck (36):
1

Alpha receptors are predominantly known for what action? Due to this, how does it effect the cardiovascular system?

Vasoconstrictor of smooth muscle

Increases vascular resistance and blood pressure

2

Predominant effects of beta receptors?

Affect glucose and lipid mobilization

Stimulate chronotropic and inotropic state of the heart

Increase CO

Relax bronchial smooth muscle

3

Apha 1 receptor effect:

1. vascular smooth muscle?

2. pupillary dilator muscle?

3. Genitourinary smooth muscle/prostate?

4. Intestinal smooth muscle?

5. Heart?

6. Liver?

1. contraction

2. contraction

3. contraction

4. relaxation

5. Increase inotropy and exciteablility

6. glucogenolysis/gluconeogenesis

4

Alpha 2 receptor effect:

1. Pancreatic Beta-cells?

2. Platelets?

3. Nerve?

4. Vascular smooth muscle?

5. Endothelium?

6. CNS?

7. Fat cells?

1. DECREASE insulin

2. Aggregates

3. DECREASE NE release

4. Contracton

5. Release of NO

6. DECREASE BP

7. Inhibits lipolysis

5

Beta 1 receptor effects:

1. Heart?

2. Renal juxtaglomerular cells?

1. INCREASE chronotropy, inotropy, and AV-node conduction

2. INCREASE renin secretion

6

Beta 2 receptor effects:

1. Smooth muscle?

2. Liver?

3. Skeletal muscle?

1. RELAXATION

2. Glycogenolysis/gluconeogenesis

3. Glycogenolysis and K+ uptake

7

Epinepherine is an agonist at what receptors? What receptors does it stimulate at low concentrations?

Both alpha and beta; predominantly beta

8

Epinepherine effect on beta 1 receptors?

POSITIVE inotrope/chronotrops, INCREASED CO, INCREASED systolic bp, and INCREASED cardiac oxygen consumption

9

Epinepherine effect on beta 2?

Vasodilation (DECREASED TPR), INCREASED skeletal muscle blood flow, and a DECREASE in diastolic bp while causing glucose mobilization and bronchodilation

10

1. Norepinepherine is an agonist of what receptors?

2. What is the predominant net effect?

3. Norepinepherine has a direct positive ____ effect but this is counteracted by ___ responses to its ____ effect. 

4. Norepinepherine and role in CO?

1. Alpha 1 and Beta 1

2. INCREASE peripheral vascular resistance, INCREASE systolic and diastolic BP

3. chronotropic; reflex; hypertensive

4. No alteration of CO

11

Dopamine at a low dose activates D1 receptors and causes?

Dopamine and a supraphysiological dose activates what receptor? Net effect?

 

1. dilation of renal circulation (INCREASE RBF), as well as mesenteric and coronary circulation (stimulation of adenylyl cyclase and formation of cAMP)

2. Beta 1; stimulates the heart

12

Epinepherine, Norepinepherine, or Both

1. Increased CO?

2. Increased systolic bp?

3. Increased diastolic bp?

4. Increase TPR?

5. Increase muscle blood flow?

6. Increase oxygen consumption?

7. Increase blood glucose and lactic acid?

1. Epinepherine

2. Both

3. NE

4. NE

5. Epinepherine

6. Epinepherine

7. Epinepherine

13

Clinical uses of Epinepherine?

Dental use? How does it work?

Bronchodilator inhalant for acute asthma attack and respiratory effects of severe allergic reactions

Causes focal vasoconstriction around sites of local anesthetic injections for dental work. Decreased BF and extends local anesthetic action.

14

Clinical uses of NE?

Its vasoconstrictive and acute pressor effect is used in emergency treatment of shock

15

Clinical uses of Dopamine?

Treat shock associated with LOW CO and DEPRESSED RENAL FUNCTION

16

5 alpha 1 selective (not specific) adrenergic receptor agonists?

Phenylephrine, pseudoephedrine, mephentermine, metaraminol, and midodrine

17

Phenylephrine and Pseudoephedrine

1. Receptor agonist?

2. Main action?

3. Therapeutic use?

4. Adverse events/contraindications?

1. Alpha 1

2. ARTERIAL vasoconstriction

3. Topically as a nasal decongestant (constrict the BV in the nose to decrease swelling), mydriatic, and orthostatic hypotenstion

4. No notable adverse events but as soon as the drug concentration falls there is rebound nasal vasodilation and congestion

18

Mephentermine and Metaraminol

1. Receptor agonist?

2. Main action? Why could they also be more appropriately described as sympathomimetic agents?

3. Therapeutic uses?

4. Adverse events and contraindications?

1. Alpha 1

2. Enhance cardiac contraction, INCREASE CO/BP; bc it also releases NE from sympathetic nerve terminals

3. Hypotension associated with anesthesia/surgery

4. CNS stimulation, excessive elevation of BP and cardiac arrhythmias

19

Midodrine

1. Receptor type?

2. Prodrug converted in body to cause?

3. Theraputic effect? More often used in patients with?

4. Adverse events and contraindications?

1. Alpha 1

2. INCREASED BP as a result of BOTH arterial AND venous smooth muscle contraction

3. Treat autonomic insufficiency with concurrent postural hypotension (venous effect); life threatening hypotension

4. CNS stimulation, excessive elevation of BP and cardiac arrhythmias

20

1. Primary action of Alpha 2 adrenergic agonists?

2. Treats hypertension with what agents?

3. What is another function? What agents are used?

4. Tizanidine is used for?

1. Stimulate receptors in CV control centers in the CNS to reduce sympathetic nerve outflow and BP

2. Clonidine, guanficine, and guanabenz

3. DECREASE IOP (via decreasing production of aqueous humor - glaucoma); Apraclonidine and Brimonidine

4. Muscle spasms

21

Beta adrenergic receptor agonists are used primarily in the treatment of what two things?

Minor acute uses?

1. Asthma and COPD (short term)

2. torsades de pointes, bradycardia, complete heart block in shock, surgically induced cardiac decompensation, heart failure, or MI

22

Main nonselective beta agonist?

Isoproterenol

23

Isoproterenol

1. IV infusion causes what cardiovascular responses? Smooth muscle?

2. Therapeutic uses?

3. Adverse effects and contraindications?

1. DECREASES peripheral vascular resistance/MAP, INCREASES CO bc of positive ionotrope and chronotrope effects (even though there is decreased peripheral vascular resistance); relaxation

2. Emergency use for patients with bradycardia/heart block or patients with torsades de pointes (ventricular arrhythmia), also bronchodilator inhalant

3. Hypotension, arrhythmias

24

Main Beta 1 selective agonist?

Dobutamine

25

Dobutamine

1. Receptor?

2. Functions? What does it not effect?

3. Therapeutic use?

4. Half life? Speed of onset?

5. Adverse reactions and contraindications?

1. Beta 1

2. Positive chronotrope and ionotrope --> INCREASE CO; no effect in TPR

3. Short term treatment of cardiac decompensation, acute CHF, or acute MI to increase CO.

4. Very short (2 min); rapid

5. Possivle increase in BP/HR, INCREASED ventricular rate in atrial fibrillation (due to facilitation of AV conduction), and Increased myocardial O2 demand and enlargement of an area in an MI

26

Name 7 Beta 2 selective agonists?

Metaproterenol, Terbutaline, Albuterol, Pirbuterol acetate, Salmeterol, Formoterol

27

Metaproterenol

1. Receptor affected?

2. Main function? Resistant to degradation by?

3. Therapeutic use?

4. Adverse events and contraindications?

1. Beta 2

2. smooth muscle relaxation; COMT (degrades catecholamines)

3. Long-term treatment of COPD, asthma, or acute bronchospasm

4. some possible CV actions

28

Terbutaline

1. Receptor agonist?

2. Main action? Resistant to degradation by?

3. Route of administration?

4. Therapeutic use?

5. Adverse effects and contraindications?

1. Beta 2

1. Bronchodilator; COMT

3. Oral, subcutaneous, inhalation

4. Long term COPD, acute bronchospasam, and parenteral use for emergency treatment of status asthmaticus (asthma exacerbation resistan to other bronchodilators/corticosteroids)

5. Inhaled: none, CV at high doses

29

Albuterol and Pirbuterol acetate

1. Receptor agonist?

2. Main effects? Route of administration?

3. Therapeutic use?

4. Adverse events and contraindications?

1. Beta 2

2. bronchodilator; oral or inhaled

3. Symptomatic relief of bronchospasm

4. None, CV effects much weaker than isoproterenol

30

Salmeterol

1. Receptor agonist?

2. Duration of activation? Speed of onset?

3. Selectivity in comparison to Albuterol?

4. Therapeutic use?

5. Adverse effects and contraindications?

1. Beta 2

2. Long (>12hrs); slow

3. 50x

4. COPD

5. NOT for acute breakthrough bronchospasms, potential to INCREASE HR/plasma glucose, to produce tremors, and to DECREASE K+ in plasma

31

Formoterol

1. Receptor agonist?

2. Duration of action?

3. Therapeutic uses?

4. What can it be used in conjunction with?

5. Adverse events and contraindications?

1. Beta 2

2. Long

3. Nocturnal asthma, asthma, bronchospasm, prophylaxis of exercise induced bronchospasm, and COPD

4. short acting Beta 2 agonists, glucocorticoids, or theophylline

5. None if inhaled

32

Common adverse effects with excessive Beta 2 selective agonists on:

1. Skeletal muscle?

2. Heart in general?

3. Patients with coronary artery disease?

4. Patients on MAOIs?

 

1. Tremors

2. Tachycardia (although HR may decrease with agonist in severe asthma attack)

3. Arrhythmias and myocardial ischemia

4. Arrhythmias and myocardial ischemia

33

Common adverse effects with excessive Beta 2 selective agonists on:

1. Decreased ____ during treatment of acute exacerbations of asthma

2. ___ from asthma with prolonged use ( ____ and downregulation of beta receptor)

3. With parenteral administration?

1. PAO2

2. Death; tolerance

3. INCREASED plasma glucose/lactate/FFA and DECREASED plasma potassium

34

Review: Agonist for hypotension when incication of hypoperfusion of the ___, ___, or ____ is present?

Alpha agonist; heart; brain; kidneys

35

Review: What two things are used for cardiac arrthythmias?

Epinepherine in cardiac arrest along with alpha agonists

36

Review: what is used for nasal decongestion?

Review: what is used for asthma?

Review: What is used for allergic reactions?

Alpha agonists

Beta 2 agonists

Epinepherine