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SYMPATHOMIMETICS Flashcards

1
Q

 Constitute a group of drugs used for

  • Cardiovascular
  • Respiratory
  • Other conditions
A

Adrenomimetics

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2
Q

Adrenomimetics
Subdivided into:
 Mode of action

A

Direct-acting

 Indirect-acting

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3
Q

Adrenomimetics
Subdivided into:
 Spectrum of action

A

 Alpha
 Beta
 Dopamine receptor affinity

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4
Q

A. MODE OF ACTION

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

A

DIRECT-ACTING SYMPATHOMIMETICS

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5
Q

A. MODE OF ACTION

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

A

INDIRECT-ACTING SYMPATHOMIMETICS

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6
Q

A. MODE OF ACTION

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

A

INDIRECT-ACTING SYMPATHOMIMETICS

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7
Q

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

A

MONOAMINE OXIDASE (MAO)

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8
Q

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

A

MONOAMINE OXIDASE INHIBITORS

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9
Q

subgroups of alpha

A

alpha 1

alpha 2

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10
Q

subgroups of beta

A

beta 1
beta 2
beta 3

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11
Q

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

A

EPINEPHRINE

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12
Q

 Separate prototype

 Alpha

A

PHENYLEPHRINE

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13
Q 
 Separate prototype
 Beta
 Synthetic cathecolamine
 Similar to the endogenous transmitters
 Not readily taken up into the nerve ending
A

ISOPROTERENOL

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14
Q

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
A

DOPAMINE

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15
Q

 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

A

CATHECOLAMINES

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16
Q 
 Not a cathecolamine
 Resistant to MAO
 Resistant to COMT
 Orally active
 Enter the CNS
 Longer effects
A

AMPHETAMINES

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17
Q

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

A

PHENYLETHYLAMINE

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18
Q

PHENYLETHYLAMINE

 Removal of OH will:

A

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

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19
Q

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

A

PHENYLETHYLAMINE

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20
Q

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

A

PHENYLETHYLAMINE

21
Q

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

A

ADRENOCEPTORS

22
Q 
 Epinephrine > NE > isoproterenol
 Alpha1
 Increase in phosphatidyl inositol (IP3)
 Release of calcium
 Alpha2
A

ALPHA RECEPTOR ACTIVATION

23
Q

 Receptors found in renal vasculature, brain

A

DOPAMINE RECEPTOR ACTIVATION

24
Q

beta1 = beta2

A

DOBUTAMINE

ISOPROTERENOL

25
Q

beta2 > beta1

A

TERBUTALINE

26
Q

ADRENOCEPTORS
ALPHA SELECTIVE
alpha1 > alpha2
alpha1 activation

A

 PHENYLEPHRINE

27
Q

ADRENOCEPTORS
ALPHA SELECTIVE
alpha2 > alpha1
alpha2 activation

A

 CLONIDINE

28
Q 
ADRENOCEPTORS
MIXED (activates both alpha and beta)
 alpha1 = alpha2
beta1 > beta2
 EPINEPHRINE alpha1 = alpha2
beta1 = beta2
29
Q

ADRENOCEPTORS
MIXED (activates both alpha and beta)

alpha1 = alpha2
beta1 = beta2
A

 EPINEPHRINE

30
Q

CLINICAL USES
A. ANAPHYLAXIS

 Drug of choice for the immediate
treatment of anaphylactic shock
 Rapid acting
 Pressor agent
 Used for cardiac arrest
A

EPINEPHRINE

31
Q

B. CNS

 Narcolepsy
 Attention deficit disorder
 With appropriate control, weight
reduction

A

PHENYLISOPROPYLAMINES

AMPHETAMINES

32
Q

CLINICAL USES
C. EYE

 Used topically to produce mydriasis
 Used to reduce conjunctival itching
and congestion caused by irritation
and allergy

A

PHENYLEPHRINE

33
Q

D. BRONCHI

 Drugs of choice in the treatment of
acute asthmatic attacks

A

TERBUTALINE, ALBUTEROL, METAPROTERENOL

34
Q

CLINICAL USES
D. BRONCHI

 Long-acting
 Recommended for prophylaxis

A

SALMETEROL

35
Q

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
36
Q

CATHECOLAMINES

 Pressor agent
 Cardiac arrest
 Anaphylactic shock

A

EPINEPHRINE

37
Q

CATHECOLAMINES

 Pressor agent
ISOPROTERENOL
 Cardiogenic shock

A

NOREPINEPHRINE

38
Q

CATHECOLAMINES

 Cardiogenic shock

A

ISOPROTERENOL

39
Q

CATHECOLAMINES

 Congestive heart failure
 Inotropic effect

A

DOBUTAMINE

40
Q

CATHECOLAMINES

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

41
Q

NON-CATHECOLAMINES
 Pressor agent
 Mydriatic
 Decongestant

A

PHENYLEPHRINE

42
Q

NON-CATHECOLAMINES

 Pressor agent
 IV form only

A

METHOXAMINE

43
Q

NON-CATHECOLAMINES

 Pressor agent
 Orthostatic hypotension

44
Q

NON-CATHECOLAMINES

 OXYMETAZOLINE, XYLOMETAZOLINE
 Topical decongestants

45
Q

NON-CATHECOLAMINES

 Bronchial asthma

A

TERBUTALINE

46
Q

NON-CATHECOLAMINES

 Inhibits premature labor

47
Q

NON-CATHECOLAMINES

 Local vasoconstrictive
 Anesthetic effect

48
Q

NON-CATHECOLAMINES

 Derivative of tyrosine
 Increase BP
 Found in cheese and wine

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