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Pharmacology > Adrenergic Receptors Agonist And Antagonists > Flashcards

Adrenergic Receptors Agonist And Antagonists Flashcards

1
Q

What are the adrenoceptors❓

A 
a1:
a1A
a1B
a1D
a1L

a1A=a1L

a2:
a2A
a2B
a2C
a2D

a2D=a2A

b:
b1
b2
b3

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2
Q

What are the actions of a1 receptors on:

  1. Vascular smooth muscle
  2. Pupillary dilator muscle
  3. Pilomotor smooth muscle
A
  1. Vasoconstriction
  2. Constriction of pupillary dilator muscle (mydriasis)
  3. Contraction

*Refer to photos

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3
Q

What are the actions of a2
receptors on:

  1. Adrenergic and cholinergic nerve endings
  2. Platelets
  3. Some vascular smooth muscle
A
  1. Inhibits transmitter release
  2. Aggregation
  3. Vasoconstriction of some smooth muscle

*Refer to photos

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4
Q

What are the actions of b1 receptors on:

  1. Heart
  2. Glomerular cells
A
  1. ⬆️rate and force of contraction
  2. Stimulates renin release

*Refer to photos

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5
Q

What are the actions of b2 receptors on:

  1. Respiratory, uterine and vascular smooth muscle
  2. Liver
  3. Pancreatic B cells
A
  1. Relaxation of respiratory, uterine and vascular smooth muscle
  2. Hepatic glycogenolysis
  3. Stimulates insulin release
    * Refer to photos
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6
Q

What are the actions of b3 receptors on fat cells❓

A

Stimulates lipolysis

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7
Q

List some a1 agonists?

A 
Methoxamine
Phenylephrine
Mephentermine 
Metaraminol 
Midodrine 
Oxymetazoline
Tetrahydrozoline
Xylometazoline
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8
Q

What is the principal pharmacological action of a1 agonists?

A

Vasoconstriction

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9
Q

What is the principal therapeutic uses of a1 agonists?

A
  1. Treatment of shock and hypotension

2. Treatment of nasal congestion

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10
Q

What are the adverse effects of a1 agonists?

A 
Hypertension 
Headaches 
Reflex bradycardia 
Excitability 
Restlessness 
Dry mouth 
Sedation
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11
Q

List some a2 agonists?

A 
Clonidine
Apraclonidine 
Brimonidine 
Guanfacine 
Guanabenz
a-methyldopa
dexmedetomidine 
clenbuterol
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12
Q

What is the principal pharmacological action of a2 agonists?

A

⬇️sympathetic outflow
⬇️peripheral vascular resistance
⬇️production of aqueous humour

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13
Q

What is the principal therapeutic uses of a2 agonists?

A
  1. Adjunct therapy in shock
  2. Hypertension
  3. ⬇️sympathetic response from withdrawal from narcotics eg alcohol and tobacco
  4. Glaucoma
    - brimonidine
    - apraclonidine
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14
Q

What are the adverse effects of a2 agonists?

A 
Sedation
Dry mouth and nasal mucosa
Hypotension
Bradycardia
Impotence 
Constipation 
Nausea and gastric upset
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15
Q

List some b1 agonists?

A

Dobutamine
Denopamine
Xamoterol

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16
Q

What is the principal pharmacological action of b1 agonists?

A

⬆️rate and force of contraction

⬆️AV nodal conduction

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17
Q

What is the principal therapeutic uses of b1 agonists?

A

Chronic heart failure

Myocardial infarction

Impaired cardiac function after surgery

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18
Q

What are the adverse effects of b1 agonists?

A

⬆️BP

Tachycardia

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19
Q

List some b2 agonists?

A 
Intermediate acting:
Albuterol
Bitolterol 
Fenoterol 
Isoetharine
Metaproterenol 
Procaterol 
Terbutaline 
Ridotrine

Long acting:
Formoterol
Salmeterol

Salbutamol

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20
Q

List some a1 agonist drugs you’d request for if you needed to treat shock or hypotension

A

Methoxamine

Phenylephrine

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21
Q

List some a1 agonist drugs you’d request for if you needed to treat nasal congestion

A

Oxymethazoline

Tetrahydrozoline

Xylometazoline

Naphazoline

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22
Q

Some a2 agonists can be used in treating glaucoma.

List them

A

Brimonidine

Apraclonidine

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23
Q

Midodrine is a prodrug

True or false

A

True

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24
Q

Dobutamine is a b1 agonist that _____CO and ______HR

A

Dobutamine ⬆️CO and has no effect on HR

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25
Q

What are the precautions you would take if you wanted to administer b1 agonist to a pt❓

How is it administered❓

A

Make sure pt

  • Is not hypertensive
  • does not have arrhythmias

IV only!

26
Q

What are the principal pharmacological actions of b2 agonists❓

A

Relaxation of bronchial smooth muscle

Relaxation of uterine smooth muscle

Activation of other b2 receptors

27
Q

What symptoms would you be looking forward to alleviate if you administer a b2 agonist❓ (PTU)❓

A

Asthma

COPD

Acute bronchospasm

Premature labour

Prophylaxis

28
Q

Premature labour can be well taken care of with which b2 agonist❓

A

Ritodrine

29
Q

b2 agonist should be used with caution in which pts❓

A

Pts with Cardiovascular disease

30
Q

What are some of the side effects of b2 agonist❓

A 
Headache 
Anxiety 
Nausea 
Muscle tremors 
Nervousness
Palpitations
31
Q

List some b3 agonists you know❓

A

Amibegron
Mirabegron
Solabegron
Vibegron

32
Q

What are some a-non selective antagonists you know❓

A

Phenoxybenzamide
Phenotolamine
Tolazoline
Ergot alkaloids

33
Q

What are some a1 selective antagonists you know❓

A

Prazosin (1st agent)

Teraxosine long half-life)

Doxazosine (long half-life)

Alfuzosin

Tamsulosin

Indoramine

Urapidil

Bunazosin

Trimazosin

Niguldipine

34
Q

What do a1 antagonists do❓ (PPA)❓

A

⬇️peripheral vascular resistance

⬆️vasodilation

Relaxation of smooth muscles of bladder neck and prostate

35
Q

What might prompt you to select a1 antagonist for treatment❓

What are the side effects of a1 antagonist❓

A

1
Primary hypertension
Urinary retention
BPH

  1. Postural hypotension
    Reflex tachycardia
36
Q

What are some a2 selective antagonists you know❓

A

Yohimbine

Imilozan

Idazoxan

37
Q

What are conditions that could make you decide to administer a2 antagonists❓

A

Treatment of male sexual dysfunction

Obesity

38
Q

What are the PPA of a1 antagonists❓

What are the adverse effects❓

A
  1. ⬆️sympathetic output

⬆️HR and BP

Activation of a1 and b1 receptors in the heart and peripheral vasculature

  1. ⬆️HR, BP
    Severe tremors
39
Q

What are some b-non selective antagonists you know❓

A

Nadolol

Penbutolol

Pindolol

Propranolol

Timolol

Carteolol

Carvedilol

Bucindolol

Labetalol

40
Q

Yohimbine, a2 antagonist, is the major active compound in what plant❓

A

Pausinystalia yohimbine

41
Q

List some b-non selective antagonists that can block a1 receptors

A

Carvedilol

Labetalol

42
Q

What are some b1 selective antagonists you know❓

A

Acebutolol

Atenolol

Bisoprolol

Esmolol (quick onset/short duration)

Metoprolol

Betaxolol

Celiprolol

Nebivolol

43
Q

What are some b2 selective antagonists you know❓

A

Butoxamine

44
Q

What are the principal pharmacological actions of b2 antagonists❓

A 
⬇️HR
⬇️Heart contraction
⬇️CO
Slow conduction in AV node 
⬆️Refractory period, AV node

Bronchoconstriction

Prolonged hypoglycemia
⬇️Plasma free fatty acids
⬇️HDLs
⬆️LDLs, triglycerides

Hypokalemia

45
Q

What might prompt you to select b2 antagonist for treatment❓

A 
Angina pectoris 
Hypertension 
Cardiac arrhythmias 
CHF
Hypertrophic obstructive cardiomyopathy

Pheochromocytoma

Glaucoma

Hyperthyroidism

Migraine prophylaxis

Substance withdrawal

Variceal bleeding in portal hypertension

46
Q

What are the side effects of b2 antagonist❓

A 
Bradycardia 
Bradyarrythmias
-ve ionotropic effect 
⬇️CO
⬇️AV conduction

Bronchoconstriction*

Fatigue

Sleep disturbances

Prolonged hypoglycemia

Sexual dysfunction in men

Drug interactions

47
Q

The bronchoconstriction effect of b2 receptors should be of concern in what type of people❓

A

Asthmatics

COPD

48
Q

The prolonged hypoglycemic effect of b2 receptors should be of concern in what type of people❓

A

Hypoglycemics

Diabetics

49
Q

Membrane stabilization effect is associated with which beta antagonists❓

A

Propanolol

Acebutolol

Carvedilol

Betaxolol

50
Q

Intrinsic sympathomimetic activity is strong for which beta antagonist❓

A

Pindolol

51
Q

Intrinsic sympathomimetic activity is weak for which beta antagonist❓

A

Penbutolol

Carteolol

Labetalol

Betaxolol

52
Q

What are the 3rd generation non-selective beta agents❓

What is their PPA❓

What is their intrinsic sympathomimetic activity❓

What is their multiple mechanism of action❓

A 
1.
Carteolol 
Carvedilol 
Bucindolol
Labetalol

2.
Membrane stabilizating effect

  1. Vasodilation
4. 
a1 antagonism
b2 agonism
Release of NO
🚫Ca2+ channel 
Opening K+ channels
53
Q

Alpha1 adrenergic receptors are:

  1. Coupled to PLC via Gq/11 a-protein
  2. Increase IP3/DAG

True or false❓

A

True

54
Q

Describe the sequence of events for vascular smooth muscle contraction (a1 agonist)

A 
Binding of agonist 
⬇️
Activation of PLC by Gq/11 a-subunit
⬇️
Liberation of IP3 and DAG 
⬇️
Activation of IP3 receptors by IP3
⬇️
Release of stored Ca2+ into IC space 
⬇️
Increase Ca2+ concentrations
⬇️
Stimulation of smooth muscle contraction
55
Q

Alpha2 adrenergic receptors are:

  1. -vely coupled to adenyly cylase via Gai subunit
  2. Inhibits cAMP formation

True or false❓

A

True

56
Q

Describe the sequence of events for inhibition of NT release (a2 agonist)

A 
Binding of agonist 
⬇️
Inhibition of adenyly cyclase
⬇️
Reduced cAMP
⬇️
Reduced activation of PKA
⬇️
Reduced phosphorylation of N-type Ca channels on nerve terminals 
⬇️
Reduced Ca2+ influx 
⬇️
Reduced vesicular uptake of NT
57
Q

Beta1 adrenergic receptors are:

  1. Actively coupled to adenyly cylase via G-alpha-s protein
  2. ⬆️cAMP formation

True or false❓

A

True

58
Q

Describe the sequence of events for +ve chronotropy (b1 agonist)

A 
Binding of agonist
⬇️
Activation of adenyly cyclase 
⬇️
Increased cAMP
⬇️
Activation of PKA 
⬇️
Phosphorylation of Ca2+ channel in SA nodal cells
⬇️
Faster nodal cell depolarization 
⬇️
Positive chronotropy
59
Q

Describe the sequence of events for +ve ionotropy (b1 agonist)

A 
Binding of agonist
⬇️
Activation of adenyly cyclase 
⬇️
Increased cAMP
⬇️
PKA-dependent phosphorylation of L-type Ca2+ channels 
⬇️
Enhanced Ca2+ influx
⬇️
Increased release and storage of Ca2+ in SR ready for release through ryanodine receptors
60
Q

Beta2 adrenergic receptors are:

  1. Actively coupled to adenyly cylase via G-alpha-s protein
  2. ⬆️cAMP formation

True or false❓

A

True

61
Q

Describe the sequence of events for vascular smooth muscle relaxation (b2 agonist)

A 
Binding of agonist 
⬇️
Activation of adenyly cyclase 
⬇️
Increased cAMP
⬇️
Activation of PKA
⬇️
Phosphorylation and inactivation of myosin light chain kinase MLCK
⬇️
Reduced affinity of MLCK for Ca-calmodulin 
⬇️
Reduced activity of MLCK 
⬇️
MLCK 🚫phosphorylate myosin light chain 
⬇️
Reduced smooth muscle contraction.
62
Q

Describe the sequence of events for vascular smooth muscle contraction (a2 agonist)

A 
Binding of agonist 
⬇️
Inhibition of adenyly cyclase
⬇️
Reduced cAMP
⬇️
Inhibition of PKA
⬇️
Activation of MLCK
⬇️
Vascular smooth muscle constriction

Pharmacology (10 decks)

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