Brainscape's Knowledge GenomeTM

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


See full index

House Pharmacology > Adrenergic Receptor Agonist And Antagonist > Flashcards

Adrenergic Receptor Agonist And Antagonist Flashcards

1
Q

ADRENOCEPTORS

 NA & Adr. play important roles in ___ control, _____ contractile rate & force, _____ reactivity and variety of metabolic & CNS functions.

A

BP

myocardial

airway

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

ADRENOCEPTORS CONT’D
 Agonists & antagonists have proved useful in treatment of variety of diseases including ______, _____ , CHF, _____, ______ , _____ & ______.

A

hypertension

angina pectoris; asthma

depression; BPH

Glaucoma

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

ADRENOCEPTORS CONT’D

Also useful in therapeutic situations e.g. ____ ,_____ labour, _______ & as adjuncts to general _______.

A

shock

premature; opioid withdrawal

anaesthesia

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

Outliers

_____ may represent a particular conformational state of the α1A-ADR.

___ is a species orthologue of the human α2A subtype hence it is not considered to be a separate subtype.

A

α1L

α2D

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

Location of beta1 receptors

A

Heart

Juxtaglomerular cells

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

Location of beta 3 receptors

A

Fat cells

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

Beta 2 isn’t in 3 places

List them

A

Eye
Skin
Genital tract

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

Alpha 1 isn’t in some places
Mention them

A

Lungs, bronchioles, pancreas, kidney

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

Location of alpha 1 receptors

A

Most vascular smooth muscle
Pupillary dilator muscle
Pilomotor smooth muscle

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

Location of beta 2 receptors

A

Respiratory, uterine and vascular smooth muscle
Liver
Pancreatic B cells

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

Location of alpha 2 receptors

A

Platelets
Some vascular smooth muscle
Adrenergic and cholinergic nerve terminals

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

Action of alpha 1 receptor in the pilomotor smooth muscle

A

Contracts to erect hair

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

Action of alpha 2 receptor in the Adrenergic and cholinergic nerve terminals

A

Inhibit neurotransmitter release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Action of alpha 2 receptor in platelets

A

Stimulates aggregation

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

Action of beta 1 receptor in the juxtaglomerular cells

A

Stimulates renin release

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

Action of beta 2 receptor in the respiratory, uterine, and vascular smooth muscle

A

Relaxes

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

Action of beta 2 receptor in the liver

A

Stimulates glycogenolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Action of beta 2 receptor in the pancreatic B cells

A

Stimulates insulin release

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

Action of beta 2 receptor in the somatic motor nerve terminals

A

Causes tremor

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

Action of beta 3 receptor in the fat cells

A

Lipolysis

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

AGONISTS

 Non-selective agonists: ____. (α1, α2, β1 , β2 , β3); ____ (α1, α2, β1&raquo_space; β2 ); ______ (β1 + β2).

A

Adr
NA

Isoprenalol

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

Isoprenalol uses _____ adrenergic receptors

A

Beta1 and beta2

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

α1 agonists:

List 6

A

Methoxamine,
Mephentermine
Phenylephrine
Midodrine
Oxymetazoline
Tetrahydrozoline
Xylometazoline
Metaraminol

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

Alpha 1 agonists

________ and ______also act indirectly to release NA.

A

Mephentermine & Metaraminol

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

Alpha 1 agonists

________ is a pro-drug.

A

Midodrine

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

AGONISTS (α1 agonists)

Prominent Pharmacological Action (PPA): vaso_______

Principal Therapeutic Uses (PTUs):

Pressor agents (Rx of _____ & shock – _______ and _______ )

_____ decongestants (_____,_____,_____,______ & some preparations of phenylephrine).

A

Vasoconstriction

hypotension; methoxamine & phenylephrine

nasal; oxymetazoline, tetrahydrozoline, xylometazoline, naphazoline

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

________________________ (PPA)

A

Prominent Pharmacological Action

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

PTU= ________

A

Principal therapeutic uses

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

AGONISTS (α1 agonists)

Adverse Effects (AEs): ____tension, headache, ______ cardia, excitability, restlessness, ____ mouth, sedation & rebound ______ ff. abrupt withdrawal.

A

Hyper

reflex brady

dry

Sedation

hypertension

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

α2 agonists:

List 8

A

Clonidine
Apraclonidine
Brimonidine
dexmedetomidine
Guanfacine
Guanabenz
α-methyldopa
Clenbuterol.

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

α2 agonists

_______ and ______ are used topically for glaucoma and ocular hypertension.

_______ is converted in CNS to α-methylNA (α2 agonist).

A

Apraclonidine & Brimonidine

Methyldopa

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

Alpha 2 agonist drugs Used very often as centrally-acting sympatholytic
vasodilators for the Rx of hypertension.

A

F

occasionally as centrally-acting sympatholytic
vasodilators for the Rx of hypertension.

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

AGONISTS (α2 agonists)
 PPAs: (decreased or increased?) sympathetic outflow resulting in (decreased or increased?) peripheral vascular resistance and (decreased or increased?) production of aqueous humour.

A

Decreased

Decreased

Decreased

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

Alpha 2 agonists

PTUs:
Adjunct therapy in _____; ____tension; to (decrease or increase?) sympathetic response to withdrawal from narcotics, alcohol & tobacco; ______.

A

shock

hyper; decrease

glaucoma

35
Q

AE=________

A

Adverse effects

36
Q

Alpha 2 agonists

AEs:_______, ____ mouth & nasal mucosa, cardia, orthostatic ____tension, _____, constipation, nausea & gastric upset, ____arrythmia, (reduced or increased?) CO, ___tension etc.

A

Sedation

dry; brady

hypo; impotence

brady

Reduced; hypo

37
Q

β1 agonists:

Mention 3

A

Dobutamine, Denopamine and Xamoterol.

38
Q

β1 agonists:

 Use with caution in patients with _______ or ________

Administer only through ___.

A

IV

39
Q

β1 agonists:

PPAs:

(decrease or increase?) in cardiac contractility
some (decrease or increase?) in HR
(decrease or increase?) AV conduction.

A

Increase
Increase
Increase

40
Q

β1 agonists:

Dobutamine has strong _____ effect with little __ effect = ________________________

A

inotropic; chronotropic

increase in CO without significant increase in HR.

41
Q

β1 agonists:

PTUs: (Short or long?) -term treatment of impaired cardiac function after cardiac surgery, CHF and myocardial infarction.

A

Short

42
Q

β1 agonists:

AEs: (increased or decreased?) BP and HR.

A

Increased

43
Q

β2 agonists:

List 11

A

Albuterol
Bitolterol
Fenoterol
Procaterol
Formoterol
Salmeterol
Isoetharine
Ritodrine
Terbutaline
Metaproterenol
Salbutamol.

44
Q

Salmeterol is a (short or long?) acting beta ___ agonist

A

2

45
Q

Beta 2 agonist

Use with caution in patients with __________

Danger is reduced by ______ administration; as _____)

minimal side effects →_____ acting.

A

CV disease

inhalational; aerosols

intermediate

46
Q

Agonists (β2 agonists)

PPAs:

(Contraction or Relaxation?) of bronchial smooth muscle

(Contraction or Relaxation?) of uterine SM

activation of other β2Rs after ____

A

Relaxation
Relaxation

systemic administration.

47
Q

Agonists (β2 agonists)

PTUs:

______ and _______ disease

acute _____ (use ______ acting drugs);

______________

prophylaxis in respect of _______ (use ____ acting agents).

A

Asthma & chronic obstructive pulmonary

bronchospasm

short & intermediate

premature labour

premature labour; long

48
Q

For premature labour use ______

A

Ritodrine

49
Q

Agonists (β2 agonists)

AEs: Headache, anxiety, nausea, muscle ______, ________,_______etc

A

tremors

nervousness

palpitations

50
Q

β3 agonists:

List 4 etc.

A

Amibegron, Mirabegron, Ro40-2148, Solabegron, Vibegron

51
Q

α1 Adrenergic Receptors

Are positively coupled to ____ via ______ α protein of the heterotrimetric G protein family to increase ____

A

PLC

Gq/11

IP3/DAG.

52
Q

α1 Adrenergic Receptors

Sequence of events e.g. for vascular smooth muscle contraction
I.________
II. Activation of ____ by ____ subunit
III. Liberation of ____
IV. Activation of ____ receptors ( ____release channel in ___ )
V. Release of _____ into intracellular space leading to increased __ concentrations
VI.Stimulation of smooth muscle (contraction or relaxation?)

A

Binding of agonist

PLC; Gαq

IP3 and DAG

IP3; Ca; SR

stored Ca

Ca

Contraction

53
Q

α2 Adrenergic Receptors

_____vely couple to __ via ____ subunit which (stimulates or inhibits ?) ____ formation.

A

Negati

Adenyl Cyclase

Gαi

Inhibits; cAMP

54
Q

α2 Adrenergic Receptors

Sequence of events e.g. for inhibition of NT release

I. Binding of agonist
II. Inhibition of _______
III. Reduced ____
IV. Reduced activation of ____
V. Reduced ______ of __-type ___ channels on nerve terminals
VI. Reduced _____ during membrane depolarization
VII. Reduced vesicular release of NT

A

adenylyl cyclase

cAMP

PKA

phosphorylation; N; Ca

Ca influx

55
Q

β1 Adrenergic Receptors

___vely couple to ________ via ___ protein leading to ____eased ——- formation.

A

Posti

adenylyl cyclase

Gαs

increased cAMP

56
Q

β1 Adrenergic Receptors

Sequence of events e.g. for positive chronotropy
I. Binding of agonist
II. Activation of _____
III. Increased ____
IV. Activation of ___
V. Promotion of ______ of ____ channels in the membrane of _____ cells
VI. Increased __ward ___ current
VII. (Slower or Faster?) nodal cell _______ to the _______
VIII.Positive chronotropy

A

adenylyl cyclase

cAMP; PKA

phosphorylation; Ca; SA node

in; Ca

Faster; depolarization; firing threshold

57
Q

β1 Adrenergic Receptors

Sequence of events e.g. for positive ionotropy

I. Binding of agonist
II. Activation of _____
III. Increased ____
IV. Increased _____-dependent ____ of __-type calcium channels in _____ membrane
V. Enhanced ___ influx
VI. Larger trigger signal for release of Ca from the ___ into the intracellular space
VII. Entry of trigger Ca into the ___ leading to ______ such that next trigger _____________ through _______ receptors

A

adenylyl cyclase

cAMP; PKA

phosphorylation; L; myocyte

Ca; SR

SR; increased Ca storage

initiates larger efflux of calcium

ryanodine

58
Q

β2 Adrenergic Receptors

Sequence of events e.g. for vascular smooth muscle relaxation:

I. Binding of agonist
II. _______ of adenylyl cyclase
III.______ cAMP
IV._____ of PKA
V._______ and ______ of ________ kinase
VI. Reduced ___________________
VII. Reduced ______ thus ability to _________ is inhibited.
VIII.Reduced smooth muscle contraction

A

Activation

Increased; Activation

Phosphorylation and inactivation; myosin light chain

affinity of MLCK for Ca-calmodulin

activity of MLCK; phosphorylate myosin light chain

59
Q

α2 Adrenergic Receptors
 Sequence of events e.g. for peripheral vasoconstriction
I. Binding of agonist
II.______ of adenylyl cyclase
III._______ camp
IV._______ of pKa
V. _______ of MLCK
VI. Vascular smooth muscle constriction

A

Inhibition

Reduced

Inhibition

Activation

60
Q

Alpha 1 ANTAGONISTS

PPAs:

(increased or decreased?) peripheral vascular resistance (promote vaso_____)

(Tense or relax?) smooth muscles in neck of bladder & in prostate.

A

Decreased ; dilation

Relax

61
Q

Alpha 1 ANTAGONISTS

PTUs: Primary ___tension; ____ retention; (increased or decreased?) urine flow in BPH.

A

hyper

urinary

Increased

62
Q

Alpha 1 ANTAGONISTS

AEs: _______ tension when therapy is instituted; reflex _____cardia

A

Postural hypo

tachy

63
Q

α2 antagonists

PPAs:

(Increased or decreased?) sympathetic outflow & potentiate release of NA from nerve endings

Results in _______ of α1 & β1 Rs in the heart & peripheral vasculature → ↑ BP.

A

Increased

activation

64
Q

Alpha 2 ANTAGONISTS

PTUs: Ingredient in many _____ products; extensive use in treatment of _________

AEs: ____eased HR ,BP and can cause _____

A

weight loss

male sexual dysfunction.

Incr; severe tremors

65
Q

β-BLOCKERS

PPAs:
(Increased or decreased?) HR
(Increased or decreased?) contractility
(Increased or decreased?) CO
(Fast or slow?) conduction in atria & AV node
(Increased or decreased?) refractory period, AV node
Broncho (constriction or dilatation?)
prolonged ____glycaemia
(Increased or decreased?) plasma free fatty acids
(Increased or decreased?) HDLc
(Increased or decreased?) LDLc & triglycerides
——kalemia.

A

Decreased
Decreased
Decreased
Slow
Increased
Constriction
Hypo
Decreased
Decreased
Increased
Hypo

66
Q

β-BLOCKERS

PTUs:
______
____tension
cardiac _____
__________ failure
______________
________
hypertropic obstructive cardiomyopathy
_____thyroidism
____ prophylaxis
_________ symptoms
substance _______
_______ bleeding in portal hypertension.

A

Angina pectoris hyper
arrhythmias
Congestive heart
pheochromocytoma
glaucoma
Hyper
migraine
acute panic
withdrawal
variceal

67
Q

β-BLOCKERS

AEs:

___cardia
__ve ionotropic effect
(Increased or decreased ?)CO
___________
(Increased or decreased ?) AV conduction
Broncho (constriction or dilatation?)
fatigue
____ disturbances
prolongation of ___glycemia
__________ in men
drug interactions.

A

Brady
Negati
Decreased
bradyarrythmias
Decreased
constriction
Sleep
hypo
sexual dysfunction

68
Q

Beta blockers

Pharmacological effects depend largely on _________________

A

degree of sympathoadrenal tone.

69
Q

Beta blockers

Bronchoconstriction is of concern in _______ and _____

A

asthmatics & COPD.

70
Q

β-BLOCKERS CONT’D

Hypoglycemia is of concern in ______ and ______

A

hypoglycemics and diabetics.

71
Q

β-BLOCKERS CONT’D
 3rd generation non-selective agents have as their PPAs – _________ effect; ISA; _________.

A

membrane stabilizing

vasodilation

72
Q

ISA =_________________

A

Intrinsic sympathomimetic activity

73
Q

The non-selective alpha adrenergic blocker; *_______________ * is the major drug used to treat PHEOCHROMOCYTOMA

A

PHENOXYBENZAMINE

74
Q

Alpha 1 agonists end with ????

Mention the exception

A

Ines (mine, line, rine)

Metaraminol

75
Q

Alpha 2 agonists end with ????

Mention the exception

A

Dine

Clenbuterol
Alpha methyl dopa
Guanfacine
Guanabenz

76
Q

List the beta 1 agonists

A

Dobutamine
Denopamine
Xamoterol

77
Q

Beta 2 agonists all end with???

List the exceptions

A

Terol

Metaproterenol
Isoetharine
Ritodrine
Salbutamol
Terbutaline

78
Q

Beta 3 agonists all end with ??

A

Begron

79
Q

List the alpha non selective antagonists

A

Phenoxybenzamine
Phentolamine
Tolazoline

80
Q

Alpha 1 selective antagonists end with ??

A

Osin

81
Q

List the alpha 2 selective Antagonists

A

Yohimbine
Imiloxan
Idazoxan

82
Q

Beta 2 selective antagonists?

A

Butoxamine

83
Q

Beta non selective antagonists end with ?

A

Lol

84
Q

Beta 1 selective antagonists are?

A

A
A
B iso
B eta
M
E
N ebivolol

House Pharmacology (50 decks)

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