Adrenergic Drugs (Agonists)

Question 1

Conversion of tyrosine to DOPA is _________

Answer 1

Rate limiting step

Question 2

How are catecholamines made up?

Answer 2

Benzene ring with 2 hydroxyls and one amine

Question 3

Alpha 1 adrenergic receptors

Answer 3

Gq (IP3, DAG, Ca)
Vasoconstriction*
Causes mydriasis, contraction of urinary sphincter and urinary retention, glycogenolysis

Question 4

Alpha 2 adrenergic receptors

Answer 4

Gi (decreased cAMP)
Pre-synaptic inhibits NE release
Centrally- sedation, pain modification
Pancreas- decreased insulin secretion

Question 5

What glycoprotein do beta adrenergic receptors use?

Answer 5

Gs that increases cAMP

Question 6

Beta 1 adrenergic receptors

Answer 6

Heart: Increases HR, contractility, AV conduction
Kidney: Increase renin secretion and BP

Question 7

Beta 2 adrenergic receptors

Answer 7

Lungs- bronchodilation
Uterine relaxation
Vasodilation
Gi reduced motility

Question 8

Beta 3 adrenergic receptors

Answer 8

Adipose tissue- lipolysis

Question 9

Catecholamines are classified as ____________

Answer 9

Adrenergic agonists (sympathometic drugs)

Question 10

Types of catecholamines

Answer 10

1. Epinephrine, Norepinephrine and dopamine: endogenous substances and drugs
2. Isoprotereonol and dobutamine (synthetic)
3. Adrenaline, noradrenaline, isoprenaline

Question 11

Catecholamines uses (adrenaline, etc.)

Answer 11

Localized vasoconstriction (a1)
Controlling bleeding from capillaries and small arterioles
Hypotension and shock
Heart block
Anaphylactic and allergic reactions

Question 12

Beta 2 adrenergic agonists

Answer 12

Metaproterenol
Albuterol
Terbutaline
Salmeterol
Formoterol
Clenbuterol

Question 13

Clenbuterol (Ventipulmin)

Answer 13

Horses: recurrent airway obstruction (COPD)
Banned for food-producing animals
Humans: used by inhalation

Question 14

Phenylpropanoline

Answer 14

Indirectly acting by inducing NE release (a1)
Treats urinary incontinence in dogs- orally
Initially approved in humans as appetite suppressant and decongestant

Question 15

Why was phenylpropanoline stopped given to humans?

Answer 15

Because of incidence of hemorrhagic stroke in women

Question 16

Dopamine

Answer 16

Natural NT in the basal ganglia
Short half-life
Unstable in alkaline solution

Question 17

How does dopamine affect the heart

Answer 17

Cardiogenic shock from myocardial infarction (MI)
Congestion heart failure or septic shock

Question 18

Dopamine in large doses

Answer 18

Affects A receptors

Question 19

Dopamine in medium doses

Answer 19

Effects B receptors

Question 20

Dopamine in small doses

Answer 20

Effects D2 receptors

Question 21

What does dopamine treat?

Answer 21

Given as IV infusion for treatment of cardiogenic and septic shock

Question 22

When are adrenergic drugs used?

Answer 22

For vasoconstriction and increase BP
Congestion (a2): oxymetazoline

Question 23

How are adrenergic drugs used in surgery?

Answer 23

Prolongs the action of local anesthetics- epinephrine
Hypotension during spinal anesthesia- NE
^^ both a1

Question 24

Cardiac effects of adrenergic drugs

Answer 24

Raise BP and treat cardiac arrest
Paroxysmal atrial tachycardia (a1)
Complete heart block, cardiac arrest (b1): epi or iso

Question 25

Dobutamine effects

Answer 25

Acute heart failure (b1) Decreases pulmonary vascular resistance (PVR) through partial B2 effect

Question 26

Adrenergic drug for respiratory application

Answer 26

Emphysema, bronchitis Selective B2 agonists- acute asthamatic bronchoconstriction

Question 27

Terbutaline

Answer 27

Orally effective B2 agonist- bronchodilator Used in animals with heart disease, hyperthyroidism or hypertension

Question 28

What drug is used for anaphylaxis shock?

Answer 28

Epinephrine (a1, b1, b2)

Question 29

Adrenergic drugs ophthalmic application

Answer 29

Phenylephrine (a1 agonist)- mydriasis to prevent conjunctival itching, congestion and glaucoma Epi and dipivefrin- glaucoma

Question 30

Which drugs work on the genitourinary tract

Answer 30

Ritodrine, terbutaline (b2)- premature labor Ephedrine- long acting and improves urinary continence

Question 31

What drug is used for CNS for which disorders?

Answer 31

Amphetamine Narcolepsy, attention deficit hyperkinetic syndrome, weight reduction, metabolism (b2&3) and anorexant

Question 32

How are central a2 agonists used?

Answer 32

Sedation and tranquilization, hypertension Menopausal hot flashes

Question 33

Adverse reactions from peripherally acting drugs

Answer 33

a1: hypertension, bradycardia b1: palpation, sinus tachycardia, arrhythmias b2: skeletal muscle tremor

Question 34

Catecholamines adverse reactions

Answer 34

Vasoconstriction, edema, hemorrhage, cardiac arrhythmias, MI, tissue necrosis, negligible CNS toxicity

Question 35

Phenylisoprpylines adverse reactions

Answer 35

Nervousness, insomnia, anorexia with only small doses, CNS toxicity (mild to severe)

Question 36

Reuptake inhibitors

Answer 36

Direct acting sympathomimetics Cocaine v. NE

Question 37

Tyramine

Answer 37

MAO inhibitors Hypertensive crisis may occur due to massive levels of NE

Question 38

________ increases the action of epinephrine on the heart, so you should ______ the dose of adrenergic drugs

Answer 38

Hyperthyroidism Reduce

Question 39

Why can’t Catecholamines be given orally?

Answer 39

Highly polar Metabolized COMT and MAO rapidly MAO and COMT are located at liver and git wall