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Pharmacology 1 > ANS 2 (Sympathetic) Adrenergic Agonists drugs > Flashcards

ANS 2 (Sympathetic) Adrenergic Agonists drugs Flashcards

1
Q

Sympathetic/ adrenergic response of pupils

A

Mydriasis

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2
Q

Sympathetic/ adrenergic response of heart

A

Tachycardia

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3
Q

Sympathetic/ adrenergic response of lungs

A

Bronchodilation

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4
Q

Sympathetic/ adrenergic response of liver

A

Inc conversion of glycogen to glucose

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5
Q

Sympathetic/ adrenergic response of adrenal glands in kidney

A

Secretion of noradrenaline and adrenaline

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6
Q

Enumerate the preview pathway of adrenergic transmission

A

1) hydroxylation of precursor aa tyrosine to DOPA or dihydroxyphenylalanine by the tyrosine hydroxylasr
2) decarboxylation to dopamine by the dopa decarboxylase
3) hyroxylation to noradrenaline /ne by the dopamine beta-hydroxylase
4) methylation to adrenaline or epi by the phenylethanolamine n-methyltransferase

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7
Q

What ion is needed for the tyrosine to enter the cell?

A

Sodium

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8
Q

As tyrosine enters the cell it will convert to ____ and this will convert to _____ .
Identify also the enzymes

A

Dopa or dihydroxyphenylalanine

Dopamine

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9
Q

First step of adrenergic transmission

Indicate its inhibitors

A

Synthesis of dopamine ( rls)

Inh: metyrosine , carbidopa

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10
Q

Second step of adrenergic transmission

Inhibitors?

A

Uptake of dopamine into vesicles ( converting it within the vesicle to norepi)

Inh: reserpine

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11
Q

Third step of adrenergic transmission

Inh?

A

Calcium causes release of ne

Inh: guanethidine, bretylium

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12
Q

What drugs causes NE release in adrenergic transmission process?

A

Amphetamine, methamphetamine, ephedrine, tyramine

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13
Q

Fourth step of adrenergic transmission

A

Binding of ne to receptors in the postsynaptic cleft

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14
Q

Fifth step of adrenergic transmission which decreases ne, epi and dopamine levels in blood
Inh?

A

Removal of ne, epi amd dopamine

Inh: cocaine tricyclic antidepressants (tca)

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15
Q

Urine metabolite of dopamine

A

Vma ( vanillylmabdelic acid)

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16
Q

Urine metabolite of epinephrine

A

Metanephrine

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17
Q

Urine metabolite of norepi

A

Normetanephrine

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18
Q

Receptors in heart and its adrenergic responses

A

Beta 1

Increased heart rate (chonotropy) and constriction ( inotropy) leading to increasef bp

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19
Q

Receptors in blood vessels and its adrenergic effect

A

Alpha 1: vasoconstriction

Beta 2: vasodilation

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20
Q

Receptors in beta islet cells of pancreas and its adrenergic effect

A

Alpha 2: decrease insulin and increases glucose, hyperglycemia
Beta 2 : stimulates insulin release

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21
Q

Receptors in bronchus and its adrenergic effect

A

B2 : bronchodilation

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22
Q

Receptor/s that promotes gluconeogenesis and glycogenolysis and what location?

A

B2 : metabolism

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23
Q

Receptor/s in presynaptic terminal / autoreceptor and its adrenergic effect

A

Alpha 2
Dec catecholamine or norepi release and bp
Dec vasomotor tone

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24
Q

Receptor/s in cns and its adrenergic effects

A

Dopamine 2

Stimulation of cns

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25
Q

D1-like receptors

A

D1,5

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26
Q

D2-like receptors

A

D2,3,4

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27
Q

T/f : all alpha receptors produces sympathetic responses

A

Not all; different response is based on the location and type of receptors

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28
Q

Divisions of adrenergic agonists

A

Direct acting
Indirect
Mixed

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29
Q

Divisions of direct acting adrenergic agonists Based on chemical structure

A

Catecholamines

Non-catecholamines

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30
Q

Drugs under catecholamines

A 
Epi
Norepi
Dopamine
Isoproterenol
Dobutamine
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31
Q

Drugs under non catecholamines adrenergic agonsist

A

Phenylephrine
Metaprotereno
Methoxamine

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32
Q

Absence of one or both OH groups on the phenyl ring without other substitutions on the ring (effect?)

A

Reduce potency if the drugs

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33
Q

Effect of absence of one or both OH groups on the phenyl ring after oral admin

A

Increases its BA and prolongs duration of action

Increase the cns effects

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34
Q

Effects of substitutions in alpha carbon

A

Block oxidation by moa or monoamine oxidases and prolong action particularly noncatecholamines

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35
Q

Substitution of hydroxyl on beta carbon

A

Decreases actions within the cns,

Enhances agonist activity of alpha and beta adrenergic receptors

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36
Q

Contain 3,4-dihydroxybenzene ring
Highest potency in activating alpha or beta receptors
Metabolized by COMT , MAO
brief period action
Polar and do not readily penetrate into the CNS

A

Catecholamines

37
Q

Longer half lives because not metabolized by comt and mao
Increased lipid solubility and greater access to the cns
Lack the 3,4-dihydroxybenzene ring

A

Non-catecholamines

38
Q

Moa of direct acting sympathomimetic

A

Directly bind to adrenergic receptors

39
Q

Classification of direc acting sypathomimetics/ adrenergic agonists

A

Alpha agonists
Beta agonists
Alpha and beta agonists

40
Q

3 divisions under alpha agonists

A

Alpha 1 agonists
Alpha 2 agonists
Alpha 1 and 2 agonists

41
Q

Drugs under alpha -1 agonists

A

Phenyelphrine
Phenylpropanolamine
Pseudoephedrine
Methoxamine

42
Q

Drugs under alpha-2 agonists

A

Clonidine
Methyldopa
Guanfacine
Guanabenz

43
Q

Drugs under alpha 1 and 2 agonists

A

Oxymetazoline

Xylometazoline

44
Q

Causes intense vasoconstriction
I: hypotensive management, paroxysmal atrial tachycardia, nasal congestion
Ae: hypertensive headache, cardiac irregularities

A

Phenylephrine

45
Q

Otc nasal congestant ( <25 mg)

Ae: hypertension

A

Phenylpropanolamine

46
Q

Nasal decongestant taken orally other than phenypropanolamine
Ae: htn

A

Pseudoephedrine

47
Q

Same with phenylephrine
Causes intense vasoconstriction
I: paroxysmal atrial tachycardia
Ae: hypertensive headache and vomiting

A

Methoxamine

48
Q

Term for a2 agonists because it acts as antagonists but binds at a2 receptors

A

Sympathoplegic or sympatholytics

49
Q

Tx of htn
Dec preganglionic sympathetic outflow from brain , dec norepi resulting in dec bp
Ae: orthostatic htn, withrawal induced rebound htn

A

Clonidine

50
Q

Doc for gestational htn
Converted to _____ , a potent a2 receptor agonist
Dec preganglionic sympathetic outflow from brain resulting in dec bp

A

Methyldopa

Alpha-methylnorepinephrine

51
Q

Ae: mild orthoatatic htn, rebound htn, Coombs positive rbc which causes reversible hemolysis

A

Methyldopa

52
Q

Other drug which
I: clinical htn
Potent a2 agonist
Ae: orthostatic htn

A

Guanabenz, guanfacine

53
Q

Effects depends on its affinity to each alpha receptor

A

Alpha 1 and 2 agonists

54
Q

Higher affinity in alpha 1: nasa decongestant

A

Oxymetazoline

Xylometazoline

55
Q

Drugs under b2 agonist

A 
PASing oF FB in MRT
Pirbuterol
Albuterol/ salbutamol
Salmeterol
Formoterol
Fenoterol
Bitolterol
Metaproterenol
Ritodrine
Terbutaline
56
Q

Drugs under b1and 2 agonists

A

Isoproterenol

57
Q

Bronchodilation to manage asthma

Relax uterus in near-term pregnant woman

A

B2 agonists

58
Q

Causes intense vasodilation and doesn’t bind to alpha1
Reduces mean arterial preasure
I: heart failure because it stimulates heart more than epi
Ae: same w/ epi

A

Isoproterenol ( b1&2 agonist)

59
Q

Rapid onset but brief duration
Aka adrenaline
I: bronchodpasm(b2) , anaphylactic rxn(a1) , cardiac arrest (b1), open angle glaucoma (a1)
Combined with local anesthetics which delays distribution of anesthetic away from the injection site due to vasoconstriction (a1)

A

Epinephrine

60
Q

Receptor which has higher affinity with epi

A

Alpha 1

61
Q

More intense vasoconstriction than epi because drug fails to bind to b2 receptors or beta
I: hypotension

A

Norepinephrine

62
Q

Receptors affected by low dose of dopamine

A

Dopamine receptors

63
Q

Receptors affected by moderate doses of dopamine

A

Dopamine and beta receptors

64
Q

Receptors affected by high doses of dopamine

A

Dopamine, beta and alpha receptors ( constricts all vessels)

65
Q

B1 > b2 > alpha and doesnt bind to dopamine
I: chf
And increases cardiac output (b1)

A

Dobutamine

66
Q

Moa of indirect acting adrenergic agonists

A

Drugs Causing norepi release from presynaptic terminals but do not bind to receptors

67
Q

Drug causing htn in depressed patients takine maoi

A

Tyramine

68
Q

I: narcolepsy, adhd, appetite suppression m, Parkinson’s disease
Improve brain development, and nerve growth due to increase nt activity

A

Amphetamine, metamphetamine

69
Q

Moa of Mixed adrenergic agonist

A

Indirect plus direct

70
Q

Mixed adrenergic agonist
I: Asthma, nasal congestion, narcolepsy, myasthenia gravis
Longer duration (poor substrate for comt and mao) but leas potent than epi
Ae: less cns toxic than amphetamines

A

Ephedrine

71
Q

I: shock, acute hypotension and when norepi or dopamine is not possible
Little cns toxicity

A

Metaraminol

72
Q

2 divisions of adrenergic antagonists

A

Direct and indirect

73
Q

Divisions under direct adrenergic antagonists

A

Alpha blockers

Beta blockers

74
Q

Divisions under alpha blockers

A

Alpha 1 blockers
Alpha 2 blockers
Alpha 1 and 2 blockers

75
Q

Drugs under a1 blockers

A 
Trimazosin
Prazosin
Doxazosin
Alfuzosin
Terazosin
76
Q

Drug/s for hypertension, benign prostatic hyperplasia (BPH) hard to urinate
Ae: first-dose syncope (fainting)

A 
Trimazosin 
Prazosin 
Doxazosin 
Alfuzosin 
Terazosin
77
Q

Drug/s under a2 blockers

A

Yohimbine

78
Q

Indole alkaloid
Found in the bark of the tree Pausinystalia yohimbe and in Rauwolfia root
Treat erectile dysfunction

A

Yohimbine

79
Q

2 drugs if a1 and a2 blockers

A

Phenoxybenzamine

Phentolamine

80
Q

I: hypertension due to pheochromocytoma or too much adrenaline released from adrenal gland causing a tumor
Or may be due ti intake of MAO
Raynaud’s syndrom

A

Phenoxybenzamine

Phentolamine

81
Q

A1 &2 blocker
Irreversible antagonist
Long lasting but short onset

A

Phenoxybenzamine

82
Q

A1&2 blocker reversible antagonist

Short half life, rapid onset

A

Phentolamine

83
Q

3 phases of raynaud’s syndrome

A

1) ischemia
2) cyanosis
3) rubor

84
Q

Prototype ninselective vasoconstrictor
I: hypertension, glaucoma, chronic migraine, severe hyperthroidism, chronic managemnt of stable angina, myocardial infarction, arrythmias

A

Propranolol

85
Q

Ae: fasting hypoglycemia due to decrease glycogenolysis

A

Propranolol

86
Q

More potent than propranolol

I: htn, angina pectoris

A

Nadolol

87
Q

Chronic open angle glaucoma by reducing intraocular pressure

A

Timolol

88
Q

Has action potential prolonging class/phase 3 (repolarization) relaxed heart
-life thratening ventricular arrythmias

A

Sotalol

89
Q

B1 and b2 blockers that are non selective both a and b

A

Labetalol

Carvedilol

Pharmacology 1 (3 decks)

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