SYMPATHOMIMETICS

Question 1

 Constitute a group of drugs used for

• Cardiovascular
• Respiratory
• Other conditions

Answer 1

Adrenomimetics

Question 2

Adrenomimetics
Subdivided into:
 Mode of action

Answer 2

Direct-acting

 Indirect-acting

Question 3

Adrenomimetics
Subdivided into:
 Spectrum of action

Answer 3

 Alpha
 Beta
 Dopamine receptor affinity

Question 4

A. MODE OF ACTION

 Bind to and activate the adrenoceptors
 Result to sympathetic stimulation

Answer 4

DIRECT-ACTING SYMPATHOMIMETICS

Question 5

A. MODE OF ACTION

 Displacement of stored cathecolamines in
the synapse
 Tyramine, amphetamine

Answer 5

INDIRECT-ACTING SYMPATHOMIMETICS

Question 6

A. MODE OF ACTION

 Inhibit the reuptake of cathecolamines by
nerve terminals
 Cocaine, tricyclic antidepressants

Answer 6

INDIRECT-ACTING SYMPATHOMIMETICS

Question 7

 Present in the mitochondria in the adrenergic nerve endings
 Inactivates portion of dopamine and norepinephrine in the cytoplasm

Answer 7

MONOAMINE OXIDASE (MAO)

Question 8

 May increase the stores of these transmitters and other amines in
the nerve endings

Answer 8

MONOAMINE OXIDASE INHIBITORS

Question 9

subgroups of alpha

Answer 9

alpha 1

alpha 2

Question 10

subgroups of beta

Answer 10

beta 1
beta 2
beta 3

Question 11

 Single prototype with effects at all receptors
 Alpha1 and alpha2
 Beta1,beta2 and beta3

Answer 11

EPINEPHRINE

Question 12

 Separate prototype

 Alpha

Answer 12

PHENYLEPHRINE

Question 13

 Separate prototype
 Beta
 Synthetic cathecolamine
 Similar to the endogenous transmitters
 Not readily taken up into the nerve ending

Answer 13

ISOPROTERENOL

Question 14

B. SPECTRUM OF ACTION

 Constitute a third class of adrenoceptors
 Drugs mentioned have little effect on
dopamine
 May act as a potent dopamine receptor
agonist itself

Answer 14

DOPAMINE

Question 15

 Epinephrine, norepinephrine, and dopamine
 Endogenous adrenoceptor agonists
Rapidly metabolized by COMT and MAO
 Inactive when given by the oral route
 Short duration of action
 When given IV, they do not enter the CNS
in significant amounts

Answer 15

CATHECOLAMINES

Question 16

 Not a cathecolamine
 Resistant to MAO
 Resistant to COMT
 Orally active
 Enter the CNS
 Longer effects

Answer 16

AMPHETAMINES

Question 17

 Presence of OH groups at carbons 3 and 4
 Degraded by cathecol-o-methyl transferase
(COMT)

Answer 17

PHENYLETHYLAMINE

Question 18

PHENYLETHYLAMINE

 Removal of OH will:

Answer 18

 Make it resistant to COMT
 Prolong the duration of action
 Increase bioavailability
 Increase the ability to penetrate the CNS

Question 19

 Alter the alpha carbon, add CH3
Phenylisopropylamine
Ephedrine, amphetamine

Answer 19

PHENYLETHYLAMINE

Question 20

 Alter the beta carbon, add OH
Direct-acting
Important in the storage of cathecolamines

Answer 20

PHENYLETHYLAMINE

Question 21

 G-protein coupled
 Need a 2nd messenger to induce
sympathetic effect

Answer 21

ADRENOCEPTORS

Question 22

 Epinephrine > NE > isoproterenol
 Alpha1
 Increase in phosphatidyl inositol (IP3)
 Release of calcium
 Alpha2

Answer 22

ALPHA RECEPTOR ACTIVATION

Question 23

 Receptors found in renal vasculature, brain

Answer 23

DOPAMINE RECEPTOR ACTIVATION

Question 24

beta1 = beta2

Answer 24

DOBUTAMINE

ISOPROTERENOL

Question 25

beta2 > beta1

Answer 25

TERBUTALINE

Question 26

ADRENOCEPTORS ALPHA SELECTIVE alpha1 > alpha2 alpha1 activation

Answer 26

 PHENYLEPHRINE

Question 27

ADRENOCEPTORS ALPHA SELECTIVE alpha2 > alpha1 alpha2 activation

Answer 27

 CLONIDINE

Question 28

``` ADRENOCEPTORS MIXED (activates both alpha and beta) alpha1 = alpha2 beta1 > beta2  EPINEPHRINE alpha1 = alpha2 beta1 = beta2 ```

Answer 28

 NE

Question 29

ADRENOCEPTORS MIXED (activates both alpha and beta) ``` alpha1 = alpha2 beta1 = beta2 ```

Answer 29

 EPINEPHRINE

Question 30

CLINICAL USES A. ANAPHYLAXIS ```  Drug of choice for the immediate treatment of anaphylactic shock  Rapid acting  Pressor agent  Used for cardiac arrest ```

Answer 30

EPINEPHRINE

Question 31

B. CNS  Narcolepsy  Attention deficit disorder  With appropriate control, weight reduction

Answer 31

PHENYLISOPROPYLAMINES | AMPHETAMINES

Question 32

CLINICAL USES C. EYE  Used topically to produce mydriasis  Used to reduce conjunctival itching and congestion caused by irritation and allergy

Answer 32

PHENYLEPHRINE

Question 33

D. BRONCHI  Drugs of choice in the treatment of acute asthmatic attacks

Answer 33

TERBUTALINE, ALBUTEROL, METAPROTERENOL

Question 34

CLINICAL USES D. BRONCHI  Long-acting  Recommended for prophylaxis

Answer 34

SALMETEROL

Question 35

CLINICAL USES F. GUT ```  Long-acting oral sympathomimetic used to improve urinary incontinence in children and the elderly with enuresis  Mediated by the alpha receptors in the trigone of the bladder ```

Answer 35

EPHEDRINE

Question 36

CATHECOLAMINES  Pressor agent  Cardiac arrest  Anaphylactic shock

Answer 36

EPINEPHRINE

Question 37

CATHECOLAMINES  Pressor agent ISOPROTERENOL  Cardiogenic shock

Answer 37

NOREPINEPHRINE

Question 38

CATHECOLAMINES  Cardiogenic shock

Answer 38

ISOPROTERENOL

Question 39

CATHECOLAMINES  Congestive heart failure  Inotropic effect

Answer 39

DOBUTAMINE

Question 40

CATHECOLAMINES  Inotropic effect  Lower doses cause renal vasodilation  Higher doses cause vasoconstriction

Answer 40

DOPAMINE

Question 41

NON-CATHECOLAMINES  Pressor agent  Mydriatic  Decongestant

Answer 41

PHENYLEPHRINE

Question 42

NON-CATHECOLAMINES  Pressor agent  IV form only

Answer 42

METHOXAMINE

Question 43

NON-CATHECOLAMINES  Pressor agent  Orthostatic hypotension

Answer 43

MIDODRINE

Question 44

NON-CATHECOLAMINES  OXYMETAZOLINE, XYLOMETAZOLINE  Topical decongestants

Answer 44

DRIXINE

Question 45

NON-CATHECOLAMINES  Bronchial asthma

Answer 45

TERBUTALINE

Question 46

NON-CATHECOLAMINES  Inhibits premature labor

Answer 46

RITODRINE

Question 47

NON-CATHECOLAMINES  Local vasoconstrictive  Anesthetic effect

Answer 47

COCAINE

Question 48

NON-CATHECOLAMINES  Derivative of tyrosine  Increase BP  Found in cheese and wine

Answer 48

TYRAMINE