Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

2nd Year - Pharmacology > 2.06 Adrenergic Drugs > Flashcards

2.06 Adrenergic Drugs Flashcards

1
Q

Enumerate the four catecholamines

A

Norepinephrine
Epinephrine
Dopamine
Isoproterenol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Used for narcolepsy treatment

A

Modafinil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Mechanism of action of cocaine and TCA in increasing NE activity

A

Cocaine and TCAs inhibit uptake 1 or neuronal uptake

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

MOA of pargyline in increasing NE activity

A

MAO inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Epinephrine receptor selectivity

A

a1, a2, B1, B2, B3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Core drug for anaphylactic shock

A

Epinephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Primary neurotransmitter released in nerve endings

A

Norepinephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Norepinephrine receptor selectivity

A

a1, a2, B1, B3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Isoproterenol receptor selectivity

A

a1, a2, B1, B3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Selective a1 receptor agonists

A

Phenylephrine
Methoxamine
Midodrinel
Imidazole derivatives

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Midodrine

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Selective a2 receptor agonists: properties, MOA

A

Sympathomimetic agonist, but the effect is sympathetic depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Selective a2 receptor agonists

A 
Clinidine
Methyldopa
Guanfacine
Guanabenz
Tizanidine
Apraclonidine, Brimonidine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Tizanidine

A

Muscle relaxant in the treatment of muscle spasticity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Apraclonidine, Brimonidine

A

Used for the treatment of wide-angle glaucoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Selective B1 receptor agonists

A

Dobutamine

Prenalterol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Selective B2 receptor agonists

A 
Terbutaline
Salbutamol
Fenotero
Bililetro
Clenbuterol
Prcatero
Salmeterol
Formoterol
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

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

A

Terbutaline

Salbutamol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Long acting B2 selective receptor agonists for asthma

A

Indicaterol
Salmeterol
Formoterol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Ritodrine

A

Tocolytic; uterine smooth muscle relaxant, prevents premature labor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Isoxuprine

A

Also a tocolytic agent

Used in treatment of peripheral vasospastic disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Catecholamines are inactivated by

A

COMT

MAO

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Norepinephrine is primarily eliminated by

A

Uptake 1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Epinephrine is primarily eliminated by

A

Uptake 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Isoproterenol is primarily eliminated by

A

Uptake 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Monoamine oxidase is present in ___

A

surface membrane of mitochondria in liver and intestinal epithelium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

COMT is present in

A

Adrenal medulla, and other tissues, but not in nerve endings

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

a1 sympathomimetic effect on smooth muscles

A

a1 receptors:
vasoconstriction–> pallor
contraction of radial smooth muscles of the iris–> mydriasis
pilomotor contraction–> goosebumps

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

B2 sympathomimetic effect on smooth muscles

A

relaxation of walls of urinary bladder, contracted sphincter–> urinary retention

Relaxation of walls of GIT–> consitpation
Relaxation of bronchial smooth muscles
Relaxation of uterus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Receptor involved and sympathomimetic effect on the Heart

A

B1 receptor agonist
(+) chronotropy
(+) inotropy
(+) dromotropy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Receptor involved and sympathomimetic effect on metabolism

A

Glycogenolysis in liver and muscle

Hyperglycemia, hyperlipidemia, hyperlactacidemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Receptor involved and sympathomimetic effect on pancreatic islets

A

B receptors: increased glucagon from a cells, increased insulin from beta cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Catecholamine most potent on beta receptors

A

Isoproterenol

Epinephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Catecholamine most potent on alpha receptors

A

Norepinephrine

35
Q

Considered asthe parent compound form which sympathomimetic drugs are derived

A

Phenyethylamine

36
Q

Phenylethylamine consists of

A

a benzene ring

ethylamine side chain

37
Q

Structure of dopamine as compared to phenyethylamine

A

OH group at c3 and c4

38
Q

Structure of NOREPINEPHRINEas compared to phenyethylamine

A

OH group at c3 and c4

OH group at B carbon

39
Q

Structure of EPINEPHRINE as compared to phenyethylamine

A

OH group at c3 and c4
OH group at B carbon
Methyl group at amino terminal–> increased B activity (with B2)

40
Q

Structure of ISOPROTERENOL as compared to phenyethylamine

A

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
Q

Effect of increasing size of alkyl substituents

A

Increases B receptor activity and lowers alpha receptor activity
Example: Epinephrine - methyl substitution of NE
Isoproterenol - isopropyl substitution at amino group of E

42
Q

Effect of substitution on alpha carbon

A

Blocks oxidation by MAO–> prolonged duration of action

43
Q

Epinephrine: Give polarity, CNS penetration, metabolization, receptor selectivity

A 
Polar drug
Poorly penetrates the CNS
No oral preparation
Rapidly metabolized in the intestinal mucosa and liver
Activates all adrenoceptors
44
Q

Location of a1 receptors

A

Vascular smooth muscles

45
Q

Location of a2 receptors

A 
Presynaptic adrenergic nerve terminals: decreased sympathetic outflow
Platelets
Lipocytes
GI smooth muscles
JG cells
46
Q

Location of B1 receptors

A

HEART
lipocytes
brain
JG cells

47
Q

Location of B2 receptors

A

Bronchial smooth muscles
Blood vessels
Heart muscle
Uterus

48
Q

Location of B3 receptors

A

Lipocytes

49
Q

In small doses, epinephrine will first affect __ with regards to effect on BP

A

B2 receptors–> decreased TPR

50
Q

In large doses, epinephrine will affect __ with regards to effect on BP

A

ALL receptors will be activated
a1 and B2–> biphasic response
B1–> increased contraction

51
Q

Epinephrine effect on metabolism

A

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
Q

What is tachyphylaxis

A

Rapid increase in responsiveness of drugs given in successive intervals in small doses

53
Q

Relative receptor affinities: Phenyephrine, methoxamine

A

a1>a2»»»>B

54
Q

Relative receptor affinities: Clonidine, methylnorepinephrine

A

a2>a1»»»>B

55
Q

Relative receptor affinities: Norepinephrine

A

a1=a2; B1>B3»»»>B2

56
Q

Relative receptor affinities: Epinephrine

A

a1=a2; B1=B2

57
Q

Relative receptor affinities: Dobutamine

A

B1>B2»»»a

58
Q

Relative receptor affinities: Isoproterenol

A

B1=B2»»»a

59
Q

Relative receptor affinities: Albuterol, Terbutaline, Metaproterenol, Ritodrine

A

B2>B1»»»a

60
Q

Relative receptor affinities: Dopamine

A

D1=D2»B»a

61
Q

Relative receptor affinities: Fenoldopam

A

D1»D2

62
Q

Cardiovascular effect of Norepinephrine

A

B1: increased CO, SV
a1: vasoconstriction–> increased DP
Greater increase in BP that epinephrine

63
Q

Adrenergic effect of dopamine in the CVS

A

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
Q

Adrenergic effect of dopamine in the kidney

A

Low dose: D1 receptor: increased renal blood flow, increased GFR–> natriuresis and diuresis

65
Q

Fenoldpeam

A

D1 receptor agonist
Moderate affinity to a2 adrenoceptors: decrease release of transmitter substance
Severe hypertension

66
Q

Isoproterenol: affinity, inactivation

A

activates all b1, b2, b3 receptors
relatively poor substrate for MAO
potent bronchodilator

67
Q

Used in Reynaud’s phenomenon, and Buerger’s disease

A

Isoproterenol

68
Q

Dobutamine: affinity

A

B1>B2»»a

69
Q

Therapeutic use for dobutamine

A

Shot term treatment of cardiac decompensation post cardiac surgery; CHF; AMI

70
Q

General therapeutic use of B2 selective adrenoreceptor agonists

A

Treatment of asthma and COPD as bronchodilator

71
Q

Most common ADR of long term use of B2 selective adrenoreceptor agonists

A

Physiological skeletal muscle tremor
Severe pulmonary edema
worsened hyperglycemia in diabetic patients

72
Q

Terbutaline therapeutic use

A

Treatment of asthma, COPD, bronchitis

Management of premature labor

73
Q

Agent of choice together with formoterol for nocturnal asthma

A

Salmeterol

74
Q

Salmeterol

A

partial agonist
prolonged action
highly selective for B2 receptors

75
Q

Formoterol

A

Full agonist

Long acting, lipophillic, high affinity for B2 receptors

76
Q

Therapeutic use of ritodrine

A

Uterine relaxant to arrest premature labor and prolong pregnancy

77
Q

Indicaterol

A

Ultra long acting, selective B2 agonist

Treatment ONLY FOR COPD

78
Q

General actions of alpha 1 selective adrenoceptor agonists

A 
Vasoconstriction
reflex bradycardia
Pupillary dilation
Goosebumps
Contraction of prostate
Inotropy
79
Q

Phenylephrine

A

Selective a1 agonists

activates b1 only at HIGHER CONCENTRATIONS

80
Q

Midodrine

A

Selective a1 receptor agonist

ORTHOSTATIC HYPERTENSION

81
Q

First orally active sympathomimetic drug

A

Ephedrine

82
Q

Ephedrine

A

All adrenergic receptors, but less efficacious than epinephrine

83
Q

Used to treat cardiogenic shock

A

Dobutamine

Dopamine

84
Q

Selective a1 agonist which causes reflex bradycardia

A

Phenylephrine

2nd Year - Pharmacology (18 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions