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Botany > Sympathomimetics > Flashcards

Sympathomimetics Flashcards

1
Q

 Constitute a group of drugs used for
Cardiovascular
Respiratory
Other conditions

A

adrenomimetics

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2
Q

Type of adrenomimetics based on mode of action
 Bind to and activate the adrenoceptors
 Result to sympathetic stimulation

A

DIRECT-ACTING SYMPATHOMIMETICS

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3
Q

INDIRECT-ACTING SYMPATHOMIMETICS

 Displacement of stored cathecolamines in the synapse

A

releasers

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4
Q

example of releasers

A

tyramine, amphetamine

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5
Q

INDIRECT-ACTING SYMPATHOMIMETICS

Inhibit the reuptake of cathecolamines by nerve terminals

A

Reuptake inhibitors

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6
Q

example of Reuptake inhibitors

A

Cocaine, tricyclic antidepressants

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7
Q 
	Constitute a third class of adrenoceptors
	Drugs mentioned have little effect on dopamine receptors
	May act as a potent dopamine receptor agonist itself
	Intermediate doses activate beta receptors
	Large doses activate alpha receptors
A

DOPAMINE

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8
Q

dopamine

Intermediate doses activate – receptors

A

beta

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9
Q

dopamine

Large doses activate –receptors

A

dopamine

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10
Q

 Drug preferentially binds to one subgroup of receptors at concentrations too low to interact with another receptor

A

RECEPTOR SELECTIVITY

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11
Q

 Parent compound of sympathetic drug

A

phenylethylamine

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12
Q

effect of Increasing the size of alkyl substituents

A

Enhanced activity for beta 2 receptors

Lowers alpha receptor activity

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13
Q

 Methyl substitution on NE yields —-
Effect:
Enhanced activity for beta 2 receptors

A

epinephrine

Effect: Enhanced activity for beta 2 receptors

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14
Q

 Isopropyl substitution on NE yields

A

isoproterenol

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15
Q

 -OH groups at the C? and C? positions yield cathecolamines

A

c3 and c4

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16
Q

effect of  Absence of one or both –OH group

A

Increases bioavailability after oral administration
 COMT resistant
 Increase distribution to the CNS
 Amphetamine and ephedrine

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17
Q

effect of C. Substitution on the alpha carbon

 Add methyl group

A

MAO resistant

Amphetamine and ephedrine

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18
Q

effect of D. Substitution on the beta carbon

 Add OH group

A

Facilitates activation of adrenoceptors
For storage of cathecolamines
Direct-acting sympathomimetics
Dopamine does not contain beta-OH group

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19
Q

does dopamine contain a beta-OH group

A

Dopamine does not contain beta-OH group

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20
Q

comparative competency for alpha receptors

A

E > NE> isoproterenol

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21
Q

receptor responsible for
Increase in phosphatidyl inositol (IP3)
Release of calcium

A

alpha 1

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22
Q

receptor responsible for decrease cAMP

A

D1 and alpha 2

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23
Q

comparative competency BETA RECEPTOR ACTIVATION

A

Isoproterenol > epinephrine > NE

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24
Q

receptors responsible for increase cAMP

A

B1, B2, B3

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25
Q

Penetrates the CNS producing stimulant effects

A

Amphetamine

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26
Q

ORGAN SYSTEM EFFECTS
B. EYE

A

Pupillary dilator responds with mydriasis
 Accommodation is not significantly affected
 Alpha agonists reduce intraocular pressure by increasing outflow of aqueous humor

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27
Q

—- agonists reduce intraocular pressure by increasing outflow of aqueous humor

A

Alpha

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28
Q

ALPHA agonists reduce intraocular pressure by

A

increasing outflow of aqueous humor

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29
Q

EFFECT OF BETA ANTAGONISTS IN AQUEOUS HUMOR

A

 Beta antagonists decrease production of aqueous humor

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30
Q

ORGAN SYSTEM EFFECTS

BRONCHI

A

C. BRONCHI
 Marked relaxation of the smooth muscles of the bronchi
 Most efficacious and reliable for reversing bronchospasm

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31
Q

 Well endowed with both alpha and beta receptors
 Located on the smooth muscles and neurons of the enteric nervous system

A

GIT

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32
Q

WHAT ORGAN

Activation of either receptors leads to the relaxation of the smooth muscles

A

GIT

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33
Q

—- agonist causes uterine relaxation in pregnancy

A

Beta2

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34
Q

Responsible for Vasoconstriction

A

Alpha1 agonists

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35
Q

agonists that can reduce PVR and BP

A

beta2

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36
Q

causes vasodilatation in the splanchnic and renal vascular beds

A

Dopamine

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37
Q

 Well supplied with beta1 and beta2 receptors

A

G. HEART

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38
Q

 increases renin release

A

Beta1

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39
Q

increases insulin secretion (gluconeogenesis)

A

Beta2

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40
Q

Stimulate lipolysis

A

beta3

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41
Q

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

A

EPINEPHRINE

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42
Q

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

A

PHENYLISOPROPYLAMINES (AMPHETAMINES)

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43
Q

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

A

PHENYLEPHRINE

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44
Q

 Drugs of choice in the treatment of acute asthmatic attacks (3)

A

TERBUTALINE, ALBUTEROL, METAPROTERENOL

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45
Q

 Long-acting

 Recommended for prophylaxis of asthma

A

SALMETEROL

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46
Q

? agonists maybe useful in situations like Acute cardiac failure, Some types of shock

A

Beta1

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47
Q

? agonists are useful in situations in which vasoconstriction is needed

A

Alpha1

48
Q

 Used to suppress premature labor

 Cardiac stimulant effect may be hazardous to both mother and fetus

A

RITODRINE, TERBUTALINE

49
Q

 Long-acting oral sympathomimetic usedto improve urinary incontinence in children and the elderly with enuresis
 Mediated by the alpha receptors in the trigone of the bladder

A

EPHEDRINE

50
Q

 Pressor agent
 Cardiac arrest
 Anaphylactic shock

A

EPINEPHRINE

51
Q

 Potent vasodilator

A

ISOPROTERENOL

52
Q

 Congestive heart failure

 Inotropic effect

A

DOBUTAMINE

53
Q

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

A

DOPAMINE

54
Q

catecholamines

A

dopamine, dobutamine, isoproterenol, epinephrine, norepinephrine

55
Q

 Pressor agent
 Mydriatic
 Decongestant

A

PHENYLEPHRINE

56
Q

 Pressor agent, limited clinical application

 IV form only

A

METHOXAMINE

57
Q

 Pressor agent

 Orthostatic hypotension

A

MIDODRINE

58
Q

 DRIXINE (brand name)

 Topical decongestants

A

OXYMETAZOLINE, XYLOMETAZOLINE

59
Q

 Bronchial asthma

A

TERBUTALINE

60
Q

 Inhibits premature labor

A

RITODRINE

61
Q

 Local vasoconstrictive

 Anesthetic effect

A

COCAINE

62
Q

 Byproduct of tyrosine
 Increase BP
 Found in fermented food
Cheese and wine

A

TYRAMINE

63
Q

Not advised for patients taking MAO inhibitors

A

TYRAMINE

64
Q

Toxicity of sympathomimetic drugs speciifically endogenous catecholamines

A

 Limited penetration to the brain
 Little CNS toxicity when given systemically
 In the periphery

65
Q

Toxicity in the peripheral vasculature

A

Excessive vasoconstriction
Cardiac arrhythmias
Myocardial infarction
Pulmonary edema or hemorrhage

66
Q

? agonists cause hypertension

A

Alpha

67
Q

? agonists cause sinus tachycardia

and serious arrhythmia

A

Beta1

68
Q

? agonists cause skeletal muscle tremor

A

Beta 2

69
Q

? agonists cause skeletal muscle tremor

A

Beta 2

70
Q

α1 Most vascular smooth muscle

A

Contracts (↑ vascular resistance)

71
Q

Pupillary dilator muscle

α1

A

Contracts (mydriasis)

72
Q

Pilomotor smooth muscle

α1

A

Contracts (erects hair)

73
Q

Liver (in some species, eg, rat)

α1

A

Stimulates glycogenolysis

74
Q

Adrenergic and cholinergic nerve terminals

A

Inhibits transmitter release

75
Q

Platelets α2

A

Stimulates aggregation

76
Q

Some vascular smooth muscle α2

A

Contracts

77
Q

Fat cells α2

A

Inhibits lipolysis

78
Q

α2

Pancreatic β (B) cells

A

Inhibits insulin release

79
Q

β1 Heart

A

Stimulates rate and force

80
Q

β1Juxtaglomerular cells of kidney

A

Stimulates renin release

81
Q

Beta 2 Airways, uterine, and vascular smooth muscle

A

Relaxes

82
Q

Liver (human) Beta 2

A

Stimulates glycogenolysis

83
Q

Pancreatic β (B) cells Beta 2

A

Stimulates insulin release

84
Q

Somatic motor neuron terminals (voluntary muscle) Beta 2

A

Causes tremor

85
Q

Heart Beta 2

A

Stimulates rate and force

86
Q

β3 Fat cells

A

Stimulates lipolysis

87
Q

Dopamine1 (D1) Renal and other splanchnic blood vessels

A

Dilates (↓ resistance)

88
Q

Dopamine2 (D2) Nerve terminals

A

Inhibits adenylyl cyclase

89
Q

mechanism of action of E

A

α1, α2, β1, β2, β3 agonist

90
Q

mechanism of action of NE

A

α1, α2, β1, agonist

91
Q

mechanism of action of Dopamine

A

D1, α1, α2, β1, β2, β3 agonist

92
Q

mechanism of action of Isoproterenol:

A

β1, β2, β3 agonist;

93
Q

mechanism of action of Dobutamine:

A

β1 agonist

94
Q

mechanism of action of PHENYLEPHRINE

A

α1, α2 agonist

95
Q

mechanism of action of Albuterol, metaproterenol, terbutaline

A

β2 agonist

96
Q

Displaces stored
catecholamines from nerve
endings

A

Amphetamine,

methamphetamine

97
Q

Very high addiction
liability. Hypertension,
arrhythmias, seizures

A

COCAINE

98
Q

Displaces stored catecholamines

No clinical use but found in fermented foods

A

TYRAMINE

99
Q

An α-agonist drug that reduces conjunctival, nasal, or oropharyngeal mucosal
vasodilation by constricting blood vessels in the submucosal tissue

A

decongestant

100
Q 
A  derivative (eg, norepinephrine, epinephrine), a relatively
polar molecule that is readily metabolized by catechol-O-methyltransferase
A

Catecholamine

101
Q

catecholamine is derived from

A

dihydroxyphenylethylamine

102
Q

A derivative of phenylisopropylamine (eg, amphetamine, ephedrine). Unlike
catecholamines, they usually have oral activity, a long half-life,
CNS activity, and cause release of stored catecholamines

A

Phenylisopropylamine

103
Q

A drug that mimics stimulation of the sympathetic autonomic nervous system

A

Sympathomimetic

104
Q

An indirect-acting drug that increases the activity of transmitters in the synapse by
inhibiting their reuptake into the presynaptic nerve ending. May act selectively on
noradrenergic, serotonergic, or both types of nerve endings

A

Reuptake inhibitor

105
Q

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

A

MONOAMINE OXIDASE (MAO)

106
Q

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

A

MONOAMINE OXIDASE INHIBITORS

107
Q

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

A

EPINEPHRINE

108
Q 
 Not a cathecolamine
 Resistant to MAO
 Resistant to COMT
 Orally active
 Enter the CNS
 Longer effects
A

AMPHETAMINES

109
Q

Signaling mechanism of adrenoceptors

A

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

110
Q

ALPHA SELECTIVE

alpha1 > alpha2

A

 PHENYLEPHRINE

111
Q

ALPHA SELECTIVE

alpha2 > alpha1

A

CLONIDINE

112
Q

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

A

 NE

113
Q

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

A

EPINEPHRINE

114
Q

beta1 > beta2

A

DOBUTAMINE

115
Q

beta2 > beta1

A

TERBUTALINE

116
Q

beta1 = beta2

A

ISOPROTERENOL

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