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Sympathomimetics Flashcards

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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
Penetrates the CNS producing stimulant effects
Amphetamine
26
ORGAN SYSTEM EFFECTS B. EYE 
Pupillary dilator responds with mydriasis  Accommodation is not significantly affected  Alpha agonists reduce intraocular pressure by increasing outflow of aqueous humor
27
---- agonists reduce intraocular pressure by increasing outflow of aqueous humor
Alpha
28
ALPHA agonists reduce intraocular pressure by
increasing outflow of aqueous humor
29
EFFECT OF BETA ANTAGONISTS IN AQUEOUS HUMOR
 Beta antagonists decrease production of aqueous humor
30
ORGAN SYSTEM EFFECTS | BRONCHI
C. BRONCHI  Marked relaxation of the smooth muscles of the bronchi  Most efficacious and reliable for reversing bronchospasm
31
 Well endowed with both alpha and beta receptors  Located on the smooth muscles and neurons of the enteric nervous system 
GIT
32
WHAT ORGAN | Activation of either receptors leads to the relaxation of the smooth muscles
GIT
33
---- agonist causes uterine relaxation in pregnancy
Beta2
34
Responsible for Vasoconstriction
Alpha1 agonists
35
agonists that can reduce PVR and BP
beta2
36
causes vasodilatation in the splanchnic and renal vascular beds
Dopamine
37
 Well supplied with beta1 and beta2 receptors
G. HEART
38
 increases renin release | 
Beta1
39
increases insulin secretion (gluconeogenesis)
Beta2
40
Stimulate lipolysis
beta3
41
 Drug of choice for the immediate treatment of anaphylactic shock  Rapid acting  Pressor agent  Used for cardiac arrest
EPINEPHRINE
42
 Narcolepsy  Attention deficit disorder  With appropriate control, weight reduction
PHENYLISOPROPYLAMINES (AMPHETAMINES)
43
 Used topically to produce mydriasis  Used to reduce conjunctival itching and congestion caused by irritation and allergy
PHENYLEPHRINE
44
 Drugs of choice in the treatment of acute asthmatic attacks (3)
TERBUTALINE, ALBUTEROL, METAPROTERENOL
45
 Long-acting |  Recommended for prophylaxis of asthma
SALMETEROL
46
? agonists maybe useful in situations like Acute cardiac failure, Some types of shock
Beta1
47
? agonists are useful in situations in which vasoconstriction is needed
Alpha1
48
 Used to suppress premature labor |  Cardiac stimulant effect may be hazardous to both mother and fetus
RITODRINE, TERBUTALINE
49
 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
EPHEDRINE
50
 Pressor agent  Cardiac arrest  Anaphylactic shock
EPINEPHRINE
51
 Potent vasodilator
ISOPROTERENOL
52
 Congestive heart failure |  Inotropic effect
DOBUTAMINE
53
 Inotropic effect  Lower doses cause renal vasodilation  Higher doses cause vasoconstriction
DOPAMINE
54
catecholamines
dopamine, dobutamine, isoproterenol, epinephrine, norepinephrine
55
 Pressor agent  Mydriatic  Decongestant
PHENYLEPHRINE
56
 Pressor agent, limited clinical application |  IV form only
METHOXAMINE
57
 Pressor agent |  Orthostatic hypotension
MIDODRINE
58
 DRIXINE (brand name) |  Topical decongestants
OXYMETAZOLINE, XYLOMETAZOLINE
59
 Bronchial asthma
TERBUTALINE
60
 Inhibits premature labor
RITODRINE
61
 Local vasoconstrictive |  Anesthetic effect
COCAINE
62
 Byproduct of tyrosine  Increase BP  Found in fermented food Cheese and wine
TYRAMINE
63
Not advised for patients taking MAO inhibitors
TYRAMINE
64
Toxicity of sympathomimetic drugs speciifically endogenous catecholamines
 Limited penetration to the brain  Little CNS toxicity when given systemically  In the periphery
65
Toxicity in the peripheral vasculature
Excessive vasoconstriction Cardiac arrhythmias Myocardial infarction Pulmonary edema or hemorrhage
66
? agonists cause hypertension
Alpha
67
? agonists cause sinus tachycardia | and serious arrhythmia
Beta1
68
? agonists cause skeletal muscle tremor
Beta 2
69
? agonists cause skeletal muscle tremor
Beta 2
70
α1 Most vascular smooth muscle
Contracts (↑ vascular resistance)
71
Pupillary dilator muscle | α1
Contracts (mydriasis)
72
Pilomotor smooth muscle | α1
Contracts (erects hair)
73
Liver (in some species, eg, rat) | α1
Stimulates glycogenolysis
74
Adrenergic and cholinergic nerve terminals
Inhibits transmitter release
75
Platelets α2
Stimulates aggregation
76
Some vascular smooth muscle α2
Contracts
77
Fat cells α2
Inhibits lipolysis
78
α2 | Pancreatic β (B) cells
Inhibits insulin release
79
β1 Heart
Stimulates rate and force
80
β1Juxtaglomerular cells of kidney
Stimulates renin release
81
Beta 2 Airways, uterine, and vascular smooth muscle
Relaxes
82
Liver (human) Beta 2
Stimulates glycogenolysis
83
Pancreatic β (B) cells Beta 2
Stimulates insulin release
84
Somatic motor neuron terminals (voluntary muscle) Beta 2
Causes tremor
85
Heart Beta 2
Stimulates rate and force
86
β3 Fat cells
Stimulates lipolysis
87
Dopamine1 (D1) Renal and other splanchnic blood vessels
Dilates (↓ resistance)
88
Dopamine2 (D2) Nerve terminals
Inhibits adenylyl cyclase
89
mechanism of action of E
α1, α2, β1, β2, β3 agonist
90
mechanism of action of NE
α1, α2, β1, agonist
91
mechanism of action of Dopamine
D1, α1, α2, β1, β2, β3 agonist
92
mechanism of action of Isoproterenol:
β1, β2, β3 agonist;
93
mechanism of action of Dobutamine:
β1 agonist
94
mechanism of action of PHENYLEPHRINE
α1, α2 agonist
95
mechanism of action of Albuterol, metaproterenol, terbutaline
β2 agonist
96
Displaces stored catecholamines from nerve endings
Amphetamine, | methamphetamine
97
Very high addiction liability. Hypertension, arrhythmias, seizures
COCAINE
98
Displaces stored catecholamines | No clinical use but found in fermented foods
TYRAMINE
99
An α-agonist drug that reduces conjunctival, nasal, or oropharyngeal mucosal vasodilation by constricting blood vessels in the submucosal tissue
decongestant
100
``` A derivative (eg, norepinephrine, epinephrine), a relatively polar molecule that is readily metabolized by catechol-O-methyltransferase ```
Catecholamine
101
catecholamine is derived from
dihydroxyphenylethylamine
102
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
Phenylisopropylamine
103
A drug that mimics stimulation of the sympathetic autonomic nervous system
Sympathomimetic
104
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
Reuptake inhibitor
105
 Present in the mitochondria in the adrenergic nerve endings  Inactivates portion of dopamine and norepinephrine in the cytoplasm
MONOAMINE OXIDASE (MAO)
106
 May increase the stores of these transmitters and other amines in the nerve endings
MONOAMINE OXIDASE INHIBITORS
107
 Single prototype with effects at all receptors  Alpha1 and alpha2  Beta1,beta2 and beta3
EPINEPHRINE
108
```  Not a cathecolamine  Resistant to MAO  Resistant to COMT  Orally active  Enter the CNS  Longer effects ```
AMPHETAMINES
109
Signaling mechanism of adrenoceptors
 G-protein coupled  Need a 2nd messenger to induce sympathetic effect
110
ALPHA SELECTIVE | alpha1 > alpha2
 PHENYLEPHRINE
111
ALPHA SELECTIVE | alpha2 > alpha1
CLONIDINE
112
MIXED (activates both alpha and beta) alpha1 = alpha2 beta1> beta2
 NE
113
MIXED (activates both alpha and beta) alpha1 = alpha2 beta1 = beta2
EPINEPHRINE
114
beta1 > beta2
DOBUTAMINE
115
beta2 > beta1
TERBUTALINE
116
beta1 = beta2
ISOPROTERENOL

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