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2nd Year - Pharmacology > 2.06 Adrenergic Drugs > Flashcards

2.06 Adrenergic Drugs Flashcards

1
Q

Enumerate the four catecholamines

A

Norepinephrine
Epinephrine
Dopamine
Isoproterenol

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2
Q

Used for narcolepsy treatment

A

Modafinil

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3
Q

Mechanism of action of cocaine and TCA in increasing NE activity

A

Cocaine and TCAs inhibit uptake 1 or neuronal uptake

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4
Q

MOA of pargyline in increasing NE activity

A

MAO inhibitor

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5
Q

Epinephrine receptor selectivity

A

a1, a2, B1, B2, B3

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6
Q

Core drug for anaphylactic shock

A

Epinephrine

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7
Q

Primary neurotransmitter released in nerve endings

A

Norepinephrine

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8
Q

Norepinephrine receptor selectivity

A

a1, a2, B1, B3

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9
Q

Isoproterenol receptor selectivity

A

a1, a2, B1, B3

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10
Q

Selective a1 receptor agonists

A

Phenylephrine
Methoxamine
Midodrinel
Imidazole derivatives

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11
Q

Midodrine

A

Prodrug used for treatment of patients with autonomic insufficiency and postural hypotension

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12
Q

Selective a2 receptor agonists: properties, MOA

A

Sympathomimetic agonist, but the effect is sympathetic depression

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13
Q

Selective a2 receptor agonists

A 
Clinidine
Methyldopa
Guanfacine
Guanabenz
Tizanidine
Apraclonidine, Brimonidine
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14
Q

Tizanidine

A

Muscle relaxant in the treatment of muscle spasticity

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15
Q

Apraclonidine, Brimonidine

A

Used for the treatment of wide-angle glaucoma

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16
Q

Selective B1 receptor agonists

A

Dobutamine

Prenalterol

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17
Q

Selective B2 receptor agonists

A 
Terbutaline
Salbutamol
Fenotero
Bililetro
Clenbuterol
Prcatero
Salmeterol
Formoterol
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18
Q

Short active selective b2 receptor agonists that is short acting medication for acute asthma attach

A

Terbutaline

Salbutamol

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19
Q

Long acting B2 selective receptor agonists for asthma

A

Indicaterol
Salmeterol
Formoterol

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20
Q

Ritodrine

A

Tocolytic; uterine smooth muscle relaxant, prevents premature labor

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21
Q

Isoxuprine

A

Also a tocolytic agent

Used in treatment of peripheral vasospastic disease

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22
Q

Catecholamines are inactivated by

A

COMT

MAO

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23
Q

Norepinephrine is primarily eliminated by

A

Uptake 1

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24
Q

Epinephrine is primarily eliminated by

A

Uptake 2

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25
Isoproterenol is primarily eliminated by
Uptake 2
26
Monoamine oxidase is present in ___
surface membrane of mitochondria in liver and intestinal epithelium
27
COMT is present in
Adrenal medulla, and other tissues, but not in nerve endings
28
a1 sympathomimetic effect on smooth muscles
a1 receptors: vasoconstriction--> pallor contraction of radial smooth muscles of the iris--> mydriasis pilomotor contraction--> goosebumps
29
B2 sympathomimetic effect on smooth muscles
relaxation of walls of urinary bladder, contracted sphincter--> urinary retention Relaxation of walls of GIT--> consitpation Relaxation of bronchial smooth muscles Relaxation of uterus
30
Receptor involved and sympathomimetic effect on the Heart
B1 receptor agonist (+) chronotropy (+) inotropy (+) dromotropy
31
Receptor involved and sympathomimetic effect on metabolism
Glycogenolysis in liver and muscle | Hyperglycemia, hyperlipidemia, hyperlactacidemia
32
Receptor involved and sympathomimetic effect on pancreatic islets
B receptors: increased glucagon from a cells, increased insulin from beta cells
33
Catecholamine most potent on beta receptors
Isoproterenol | Epinephrine
34
Catecholamine most potent on alpha receptors
Norepinephrine
35
Considered asthe parent compound form which sympathomimetic drugs are derived
Phenyethylamine
36
Phenylethylamine consists of
a benzene ring | ethylamine side chain
37
Structure of dopamine as compared to phenyethylamine
OH group at c3 and c4
38
Structure of NOREPINEPHRINEas compared to phenyethylamine
OH group at c3 and c4 | OH group at B carbon
39
Structure of EPINEPHRINE as compared to phenyethylamine
OH group at c3 and c4 OH group at B carbon Methyl group at amino terminal--> increased B activity (with B2)
40
Structure of ISOPROTERENOL as compared to phenyethylamine
OH group at c3 and c4 OH group at B carbon Bigger alkyl substitution--> activity on B1, B2, B3 but not on alpha receptors
41
Effect of increasing size of alkyl substituents
Increases B receptor activity and lowers alpha receptor activity Example: Epinephrine - methyl substitution of NE Isoproterenol - isopropyl substitution at amino group of E
42
Effect of substitution on alpha carbon
Blocks oxidation by MAO--> prolonged duration of action
43
Epinephrine: Give polarity, CNS penetration, metabolization, receptor selectivity
``` Polar drug Poorly penetrates the CNS No oral preparation Rapidly metabolized in the intestinal mucosa and liver Activates all adrenoceptors ```
44
Location of a1 receptors
Vascular smooth muscles
45
Location of a2 receptors
``` Presynaptic adrenergic nerve terminals: decreased sympathetic outflow Platelets Lipocytes GI smooth muscles JG cells ```
46
Location of B1 receptors
HEART lipocytes brain JG cells
47
Location of B2 receptors
Bronchial smooth muscles Blood vessels Heart muscle Uterus
48
Location of B3 receptors
Lipocytes
49
In small doses, epinephrine will first affect __ with regards to effect on BP
B2 receptors--> decreased TPR
50
In large doses, epinephrine will affect __ with regards to effect on BP
ALL receptors will be activated a1 and B2--> biphasic response B1--> increased contraction
51
Epinephrine effect on metabolism
B2: enhanced glycogenolysis in the liver-> increased glucose and lactic acid release a2: inhibition of pancreatic B cells--> decreased insulin B2: stimulation of pancreatic a cells--> increased glucagon B3 on adipocytes--> increased FFA
52
What is tachyphylaxis
Rapid increase in responsiveness of drugs given in successive intervals in small doses
53
Relative receptor affinities: Phenyephrine, methoxamine
a1>a2>>>>>>>B
54
Relative receptor affinities: Clonidine, methylnorepinephrine
a2>a1>>>>>>>B
55
Relative receptor affinities: Norepinephrine
a1=a2; B1>B3>>>>>>>B2
56
Relative receptor affinities: Epinephrine
a1=a2; B1=B2
57
Relative receptor affinities: Dobutamine
B1>B2>>>>>>a
58
Relative receptor affinities: Isoproterenol
B1=B2>>>>>>a
59
Relative receptor affinities: Albuterol, Terbutaline, Metaproterenol, Ritodrine
B2>B1>>>>>>a
60
Relative receptor affinities: Dopamine
D1=D2>>B>>a
61
Relative receptor affinities: Fenoldopam
D1>>D2
62
Cardiovascular effect of Norepinephrine
B1: increased CO, SV a1: vasoconstriction--> increased DP Greater increase in BP that epinephrine
63
Adrenergic effect of dopamine in the CVS
Low dose: D1 receptor--> vasodilation, tissue perfusion, decreased peripheral resistance Higher dose: B1 receptor--> (+) inotropic effect, tachycardia, release of NE from nerve terminals Higher dose: A1 receptor--> vasoconstriction
64
Adrenergic effect of dopamine in the kidney
Low dose: D1 receptor: increased renal blood flow, increased GFR--> natriuresis and diuresis
65
Fenoldpeam
D1 receptor agonist Moderate affinity to a2 adrenoceptors: decrease release of transmitter substance Severe hypertension
66
Isoproterenol: affinity, inactivation
activates all b1, b2, b3 receptors relatively poor substrate for MAO potent bronchodilator
67
Used in Reynaud's phenomenon, and Buerger's disease
Isoproterenol
68
Dobutamine: affinity
B1>B2>>>>a
69
Therapeutic use for dobutamine
Shot term treatment of cardiac decompensation post cardiac surgery; CHF; AMI
70
General therapeutic use of B2 selective adrenoreceptor agonists
Treatment of asthma and COPD as bronchodilator
71
Most common ADR of long term use of B2 selective adrenoreceptor agonists
Physiological skeletal muscle tremor Severe pulmonary edema worsened hyperglycemia in diabetic patients
72
Terbutaline therapeutic use
Treatment of asthma, COPD, bronchitis | Management of premature labor
73
Agent of choice together with formoterol for nocturnal asthma
Salmeterol
74
Salmeterol
partial agonist prolonged action highly selective for B2 receptors
75
Formoterol
Full agonist | Long acting, lipophillic, high affinity for B2 receptors
76
Therapeutic use of ritodrine
Uterine relaxant to arrest premature labor and prolong pregnancy
77
Indicaterol
Ultra long acting, selective B2 agonist | Treatment ONLY FOR COPD
78
General actions of alpha 1 selective adrenoceptor agonists
``` Vasoconstriction reflex bradycardia Pupillary dilation Goosebumps Contraction of prostate Inotropy ```
79
Phenylephrine
Selective a1 agonists | activates b1 only at HIGHER CONCENTRATIONS
80
Midodrine
Selective a1 receptor agonist | ORTHOSTATIC HYPERTENSION
81
First orally active sympathomimetic drug
Ephedrine
82
Ephedrine
All adrenergic receptors, but less efficacious than epinephrine
83
Used to treat cardiogenic shock
Dobutamine | Dopamine
84
Selective a1 agonist which causes reflex bradycardia
Phenylephrine

2nd Year - Pharmacology (18 decks)

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