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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
D1-like receptors
D1,5
26
D2-like receptors
D2,3,4
27
T/f : all alpha receptors produces sympathetic responses
Not all; different response is based on the location and type of receptors
28
Divisions of adrenergic agonists
Direct acting Indirect Mixed
29
Divisions of direct acting adrenergic agonists Based on chemical structure
Catecholamines | Non-catecholamines
30
Drugs under catecholamines
``` Epi Norepi Dopamine Isoproterenol Dobutamine ```
31
Drugs under non catecholamines adrenergic agonsist
Phenylephrine Metaprotereno Methoxamine
32
Absence of one or both OH groups on the phenyl ring without other substitutions on the ring (effect?)
Reduce potency if the drugs
33
Effect of absence of one or both OH groups on the phenyl ring after oral admin
Increases its BA and prolongs duration of action | Increase the cns effects
34
Effects of substitutions in alpha carbon
Block oxidation by moa or monoamine oxidases and prolong action particularly noncatecholamines
35
Substitution of hydroxyl on beta carbon
Decreases actions within the cns, | Enhances agonist activity of alpha and beta adrenergic receptors
36
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
Catecholamines
37
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
Non-catecholamines
38
Moa of direct acting sympathomimetic
Directly bind to adrenergic receptors
39
Classification of direc acting sypathomimetics/ adrenergic agonists
Alpha agonists Beta agonists Alpha and beta agonists
40
3 divisions under alpha agonists
Alpha 1 agonists Alpha 2 agonists Alpha 1 and 2 agonists
41
Drugs under alpha -1 agonists
Phenyelphrine Phenylpropanolamine Pseudoephedrine Methoxamine
42
Drugs under alpha-2 agonists
Clonidine Methyldopa Guanfacine Guanabenz
43
Drugs under alpha 1 and 2 agonists
Oxymetazoline | Xylometazoline
44
Causes intense vasoconstriction I: hypotensive management, paroxysmal atrial tachycardia, nasal congestion Ae: hypertensive headache, cardiac irregularities
Phenylephrine
45
Otc nasal congestant ( <25 mg) | Ae: hypertension
Phenylpropanolamine
46
Nasal decongestant taken orally other than phenypropanolamine Ae: htn
Pseudoephedrine
47
Same with phenylephrine Causes intense vasoconstriction I: paroxysmal atrial tachycardia Ae: hypertensive headache and vomiting
Methoxamine
48
Term for a2 agonists because it acts as antagonists but binds at a2 receptors
Sympathoplegic or sympatholytics
49
Tx of htn Dec preganglionic sympathetic outflow from brain , dec norepi resulting in dec bp Ae: orthostatic htn, withrawal induced rebound htn
Clonidine
50
Doc for gestational htn Converted to _____ , a potent a2 receptor agonist Dec preganglionic sympathetic outflow from brain resulting in dec bp
Methyldopa | Alpha-methylnorepinephrine
51
Ae: mild orthoatatic htn, rebound htn, Coombs positive rbc which causes reversible hemolysis
Methyldopa
52
Other drug which I: clinical htn Potent a2 agonist Ae: orthostatic htn
Guanabenz, guanfacine
53
Effects depends on its affinity to each alpha receptor
Alpha 1 and 2 agonists
54
Higher affinity in alpha 1: nasa decongestant
Oxymetazoline | Xylometazoline
55
Drugs under b2 agonist
``` PASing oF FB in MRT Pirbuterol Albuterol/ salbutamol Salmeterol Formoterol Fenoterol Bitolterol Metaproterenol Ritodrine Terbutaline ```
56
Drugs under b1and 2 agonists
Isoproterenol
57
Bronchodilation to manage asthma | Relax uterus in near-term pregnant woman
B2 agonists
58
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
Isoproterenol ( b1&2 agonist)
59
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)
Epinephrine
60
Receptor which has higher affinity with epi
Alpha 1
61
More intense vasoconstriction than epi because drug fails to bind to b2 receptors or beta I: hypotension
Norepinephrine
62
Receptors affected by low dose of dopamine
Dopamine receptors
63
Receptors affected by moderate doses of dopamine
Dopamine and beta receptors
64
Receptors affected by high doses of dopamine
Dopamine, beta and alpha receptors ( constricts all vessels)
65
B1 > b2 > alpha and doesnt bind to dopamine I: chf And increases cardiac output (b1)
Dobutamine
66
Moa of indirect acting adrenergic agonists
Drugs Causing norepi release from presynaptic terminals but do not bind to receptors
67
Drug causing htn in depressed patients takine maoi
Tyramine
68
I: narcolepsy, adhd, appetite suppression m, Parkinson's disease Improve brain development, and nerve growth due to increase nt activity
Amphetamine, metamphetamine
69
Moa of Mixed adrenergic agonist
Indirect plus direct
70
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
Ephedrine
71
I: shock, acute hypotension and when norepi or dopamine is not possible Little cns toxicity
Metaraminol
72
2 divisions of adrenergic antagonists
Direct and indirect
73
Divisions under direct adrenergic antagonists
Alpha blockers | Beta blockers
74
Divisions under alpha blockers
Alpha 1 blockers Alpha 2 blockers Alpha 1 and 2 blockers
75
Drugs under a1 blockers
``` Trimazosin Prazosin Doxazosin Alfuzosin Terazosin ```
76
Drug/s for hypertension, benign prostatic hyperplasia (BPH) hard to urinate Ae: first-dose syncope (fainting)
``` Trimazosin Prazosin Doxazosin Alfuzosin Terazosin ```
77
Drug/s under a2 blockers
Yohimbine
78
Indole alkaloid Found in the bark of the tree Pausinystalia yohimbe and in Rauwolfia root Treat erectile dysfunction
Yohimbine
79
2 drugs if a1 and a2 blockers
Phenoxybenzamine | Phentolamine
80
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
Phenoxybenzamine | Phentolamine
81
A1 &2 blocker Irreversible antagonist Long lasting but short onset
Phenoxybenzamine
82
A1&2 blocker reversible antagonist | Short half life, rapid onset
Phentolamine
83
3 phases of raynaud's syndrome
1) ischemia 2) cyanosis 3) rubor
84
Prototype ninselective vasoconstrictor I: hypertension, glaucoma, chronic migraine, severe hyperthroidism, chronic managemnt of stable angina, myocardial infarction, arrythmias
Propranolol
85
Ae: fasting hypoglycemia due to decrease glycogenolysis
Propranolol
86
More potent than propranolol | I: htn, angina pectoris
Nadolol
87
Chronic open angle glaucoma by reducing intraocular pressure
Timolol
88
Has action potential prolonging class/phase 3 (repolarization) relaxed heart -life thratening ventricular arrythmias
Sotalol
89
B1 and b2 blockers that are non selective both a and b
Labetalol | Carvedilol

Pharmacology 1 (3 decks)

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