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PHA 037 - PHARMACOLOGY > SAS 10: ADRENORECEPTOR AGNOST AND SYMPATHOMIMETIC DRUGS > Flashcards

SAS 10: ADRENORECEPTOR AGNOST AND SYMPATHOMIMETIC DRUGS Flashcards

1
Q

what is the precursor of the effect in symptomatic again?

A

release of the NE and binding to receptors

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2
Q

acts as neurotransmitter in adrenergic transmission

A

Norepinephrine

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3
Q

a cholinomimetic that acts more like a hormone

A

Epinephrine

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4
Q

what is the MOA of direct agonist?

A

directly interact and activate adrenoreceptor

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5
Q

what is the MOA of indirect agonist?

A

enhances the affinity of the endogenous catecholamines

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6
Q

what are the endogenous cathecholamines?

A

Dopamine
Norepinephrine
Epinephrine (adrenaline)

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7
Q

what are the different mechanism of indirect agonist?

A

> displaces stored catecholamines in the adrenergic nerve ending
inhibits re-uptake of the released catecholamines
prevents the metabolic enzyme in the synaptic cleft

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8
Q

> displaces stored catecholamines in the adrenergic nerve ending

: what are the mixed sympathomimetics (indirect-acting) that are capable of releasing stored transmitters from noradrenergic nerve endings by a CALCIUM INDEPENDENT PROCESS

A

tyramine, amphetamine, ephedrine

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9
Q

> inhibits re-uptake of the released catecholamines

: what are the drugs that can inhibit the NET?

A

Imipramine(anti-depressant)
cocaine
duloxetine(norepinephrine-serotonin re-uptake inhibitors)

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10
Q

> prevents the metabolic enzyme in the synaptic cleft

: what are 2 major enzymes responsible for the metabolism in the synaptic cleft

A

Monoamine oxidase
Catechol-o-methyltransferase

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11
Q

what type of receptor is Adrenoreceptor

A

G-coupled receptor

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12
Q

what are the post-receptor in the adrenergic transmission again?

A

dopamine, alpha, beta receptors

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13
Q

what type of G-protein is the a1 receptor?

A

Gq

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14
Q

what are the effects of a1 receptor?

A

increase in IP3 and DAG

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15
Q

what type of G-protein is the a2 receptor?

A

Gi

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16
Q

what is the effect of a2 receptor?

A

decrease in cAMP

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17
Q

what type of G-protein is the beta receptor?

A

Gs

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18
Q

what type of G-protein is the D1 and D5 receptor?

A

Gs

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19
Q

what type of G-protein is the D2-D4 receptor?

A

Gi

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20
Q

if a2 is decrease in cAMP then beta receptor is?

A

increase in cAMP

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21
Q

Phenylephrine is what agonist receptor?

A

a1 receptor

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22
Q

Clonidine is what agonist receptor?

A

a2 receptor

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23
Q

Isoproterenol is what agonist receptor?

A

Beta receptor

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24
Q

Does dopamine have an antagonist?

A

None

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25
Q

what is IP3 stands for?

A

1,4,5-triphosphate

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26
Q

This enzyme hydrolyzes
polyphosphoinositides, leading to the
formation of inositol 1,4,5-triphosphate (IP3)
and diacylglycerol (DAG).

A

Alpha 1 receptor

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27
Q

This receptors inhibit adenylyl cyclase
activity and cause intracellular cyclic
adenosine monophosphate (cAMP) levels
to decrease.

A

Alpha 2 receptor

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28
Q

is the major second messenger of the b-receptor activation

A

Cyclic AMP

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29
Q

what is the CAUSE of the increase in the influx of calcium across the
cell membrane and its sequestration inside the
cell.

A

increase in cAMP

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30
Q

is typically associated with the stimulation of adenylyl cyclase

A

D1 receptor

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31
Q

have been found to inhibit
adenylyl cyclase activity, open potassium
channels and decrease calcium influx

A

D2 receptor

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32
Q

a drug may preferentially bind to
one subgroup of receptors at low concentration but
when at high interact with related class receptors.

A

selectivity

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33
Q

considers the parent compound of sympathomimetic

A

Phenylethylamine

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34
Q

what forms a sympathomimetic drugs (known as catecholamines)

A

-OH substitution in the 3 and 4 positions of the benzene ring

35
Q

a synthetic catecholamines
- very potent b-receptor agonist; little effect on a receptor.

A

Isoproterenol

36
Q

The absence of one or the other of these groups,
particularly the hydroxyl at C3 without other substitutions on
the ring may dramatically, what?

A

reduce the potency of the drug

37
Q

why catecholamines is inactive orally?

A

COMT (metabolic enzyme) is only found in the gut and liver

38
Q

This increases the bioavailability orally and prolongs action;
and, this also increases distribution in the CNS.

A

absence of one or both -OH in the benzene ring

39
Q

an increase in the alkyl substituents may, what?

A

increase B-receptor activity

40
Q

an increase in the alkyl substituents may, what?

A

increase B-receptor activity

41
Q

a substituent to the alpha carbon may, what?

A

blocks MAO hence, increase activity

42
Q

alpha carbon-substituent is called

A

phenylisopropylamines

43
Q

a substitution in this creates a direct-acting sympathomimetic drugs expect dopamine drug affinity

A

beta carbon substitution

44
Q

-leads to arterial and venous vasoconstriction
*phenylephrine increases peripheral arterial resistance and
decreases venous capacitance. (The ENHANCED ARTERIAL RESISTANCE USUALLY LEADS TO DOSE-DEPENDENT rise in blood pressure.)

A

activation of alpha 1 receptor

45
Q
  • leads to vasoconstriction when given locally in high dose (or thru IV)
  • leads to vasodilation when given systematically

is activation of what receptor?

A

a2 receptor

46
Q

is a nonselective β agonist;
it activates both β1 and β2 receptors

A

Isoproterenol

47
Q

activation of this receptor results in increased calcium influx in cardiac cell

A

B-receptor

48
Q

Pacemaker activity involves?

A

increase chronotropy and dromotropy

49
Q

Activation of ____________ IN THE RENAL VASCULATURE may also induce natriuresis.

A

activiation of D1 receptor

50
Q
  • Dopamine activates β1 receptors in the heart.
  • At low doses, peripheral resistance may decrease.
    At higher rates of infusion, dopamine activates
    vascular α receptors, leading to vasoconstriction.
A

Dopamine effect

51
Q

Activation in _______________ in fat cells leads to
_____________ with enhanced release of free
fatty acids and glycerol into the blood

A

B adrenoreceptors leads to increased (lipolysis)

52
Q

inhibit lipolysis by (decreasing) intracellular cAMP

A

a2 receptor in fat cells

53
Q

Renin secretion is stimulated by ______ and inhibited by ______________

A

stimulated by b1; inhibited by a2 receptors

54
Q

Renin secretion is inhibited by?

A

a2

55
Q

Renin secretion is stimulated by?

A

B1

56
Q

_______ with INdirect action (eg. amphetamines) readily enters the CNS from circulation which produces varying CNS effects.

EFFECTS: mild altering, with improve attention to boring tasks; through
elevation of mood, insomnia, euphoria, and
anorexia; to either full-blown psychotic behavior

A

noncatecholamines

57
Q

an agonist at both α and β receptors

A

Epinephrine

58
Q
  • examples are Levarterenol,
    noradrenaline
  • agonist at both α1 and α2 receptors
A

Norepinephrine

59
Q

*the immediate precursor of norepinephrine

A

Dopamine

60
Q

DIRECT-ACTING SYMPHATHOMIMETICS: has a longer duration of action than the catecholamines. It is an effective mydriatic
and decongestant and can be used o raise the
blood pressure.

A

Phenylephrine

*Methoxamine

61
Q
  • prodrug that is enzymatically hydrolyzed to
    desglymidodrine, a selective α1-receptor
    agonist
  • the drug may treat hypotension but causes hypertension when laying
A

Midodrine

62
Q

acts pharmacologically like
*phenylephrine (predominantly a1 agonist)

A

Methoxamine

63
Q

Clonidine, methyldopa, guanfacine, and guanabenz are examples of

A

A2 selective agonist

64
Q

DEXmedetomidine

A

sedation of //initially// intubated/ and
/mechanically/ ventilated patients during
treatment in an intensive care setting.

65
Q

sedation of //initially// intubated/ and
/mechanically/ ventilated patients during
treatment in an intensive care setting.

A

DEXmedetomidine

66
Q

used as a central muscle relaxant

A

TIZAnidine

67
Q

TIZAnidine

A

central muscle relaxant

68
Q

Topical decongestants

A

Xylo-line, Oxy-line

XYLOmetazoLINE and OXYmetazoLINE

69
Q

Dobutamine

A

resembles dopamine but binds to a and b receptors

70
Q

first orally active sympathomimetic
drug found in Ma huang, a popular
herbal medication.

A

Ephedrine

71
Q

Ma huang, herbal

A

Ephedrine

72
Q

component of many decongestant
mixtures.

*pseudo

A

pseudoephedrine

73
Q

Phenylpropanolamine

A

common component in OTC
appetite suppressants

74
Q

Common, OTC *P

A

Phenylpropanolamine

75
Q

similar to amphetamine but with higher ratio of central to peripheral
actions *meth

A

methamphetamine

76
Q

a variant of phenylisopropylamine with
amphetamine-like effects. It has been promoted as
an anorexiant and is also a popular drug of abuse.

A

Phenmetrazine

77
Q

an amphetamine variant whose major
pharmacologic effects and abuse potential are
similar to those of amphetamine.
-effective in children with ADHD

A

Methylphenidate

78
Q

is psychostimulant that differs from
amphetamine

A

Modafinil

79
Q

byproduct of Tyrosine metabolism

A

Tyramine

80
Q

Amphetamine, Methamphetamine, Phenmetrazine, Methylphenidate, Modafinil, Tyramine are example of what

A

Indirect-acting symphathomimetics

81
Q

Atomoxetine, Reboxetine, Sibutramine, Duloxetine, Cocaine are example of what?

A

Catecholamine reuptake inhibitor

82
Q

Fenoldopam and Levodopa are examples of what?

A

Dopamine agonist

83
Q

why catecholamines cannot be given orally?

A

because they are greatly degraded in the liver and gastrointestinal mucosa.
In contrary to non-catecholamines.

PHA 037 - PHARMACOLOGY (19 decks)

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