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Pharmacology > Adrenergic Receptors Agonist And Antagonists > Flashcards

Adrenergic Receptors Agonist And Antagonists Flashcards

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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
What are the precautions you would take if you wanted to administer b1 agonist to a pt❓ How is it administered❓
Make sure pt * Is not hypertensive * does not have arrhythmias IV only!
26
What are the principal pharmacological actions of b2 agonists❓
Relaxation of bronchial smooth muscle Relaxation of uterine smooth muscle Activation of other b2 receptors
27
What symptoms would you be looking forward to alleviate if you administer a b2 agonist❓ (PTU)❓
Asthma COPD Acute bronchospasm Premature labour Prophylaxis
28
Premature labour can be well taken care of with which b2 agonist❓
Ritodrine
29
b2 agonist should be used with caution in which pts❓
Pts with Cardiovascular disease
30
What are some of the side effects of b2 agonist❓
``` Headache Anxiety Nausea Muscle tremors Nervousness Palpitations ```
31
List some b3 agonists you know❓
Amibegron Mirabegron Solabegron Vibegron
32
What are some a-non selective antagonists you know❓
Phenoxybenzamide Phenotolamine Tolazoline Ergot alkaloids
33
What are some a1 selective antagonists you know❓
Prazosin (1st agent) Teraxosine long half-life) Doxazosine (long half-life) Alfuzosin Tamsulosin Indoramine Urapidil Bunazosin Trimazosin Niguldipine
34
What do a1 antagonists do❓ (PPA)❓
⬇️peripheral vascular resistance ⬆️vasodilation Relaxation of smooth muscles of bladder neck and prostate
35
What might prompt you to select a1 antagonist for treatment❓ What are the side effects of a1 antagonist❓
1 Primary hypertension Urinary retention BPH 2. Postural hypotension Reflex tachycardia
36
What are some a2 selective antagonists you know❓
Yohimbine Imilozan Idazoxan
37
What are conditions that could make you decide to administer a2 antagonists❓
Treatment of male sexual dysfunction Obesity
38
What are the PPA of a1 antagonists❓ What are the adverse effects❓
1. ⬆️sympathetic output ⬆️HR and BP Activation of a1 and b1 receptors in the heart and peripheral vasculature 2. ⬆️HR, BP Severe tremors
39
What are some b-non selective antagonists you know❓
Nadolol Penbutolol Pindolol Propranolol Timolol Carteolol Carvedilol Bucindolol Labetalol
40
Yohimbine, a2 antagonist, is the major active compound in what plant❓
Pausinystalia yohimbine
41
List some b-non selective antagonists that can block a1 receptors
Carvedilol Labetalol
42
What are some b1 selective antagonists you know❓
Acebutolol Atenolol Bisoprolol Esmolol (quick onset/short duration) Metoprolol Betaxolol Celiprolol Nebivolol
43
What are some b2 selective antagonists you know❓
Butoxamine
44
What are the principal pharmacological actions of b2 antagonists❓
``` ⬇️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
What might prompt you to select b2 antagonist for treatment❓
``` Angina pectoris Hypertension Cardiac arrhythmias CHF Hypertrophic obstructive cardiomyopathy ``` Pheochromocytoma Glaucoma Hyperthyroidism Migraine prophylaxis Substance withdrawal Variceal bleeding in portal hypertension
46
What are the side effects of b2 antagonist❓
``` Bradycardia Bradyarrythmias -ve ionotropic effect ⬇️CO ⬇️AV conduction ``` Bronchoconstriction* Fatigue Sleep disturbances Prolonged hypoglycemia Sexual dysfunction in men Drug interactions
47
The bronchoconstriction effect of b2 receptors should be of concern in what type of people❓
Asthmatics | COPD
48
The prolonged hypoglycemic effect of b2 receptors should be of concern in what type of people❓
Hypoglycemics Diabetics
49
Membrane stabilization effect is associated with which beta antagonists❓
Propanolol Acebutolol Carvedilol Betaxolol
50
Intrinsic sympathomimetic activity is strong for which beta antagonist❓
Pindolol
51
Intrinsic sympathomimetic activity is weak for which beta antagonist❓
Penbutolol Carteolol Labetalol Betaxolol
52
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❓
``` 1. Carteolol Carvedilol Bucindolol Labetalol ``` 2. Membrane stabilizating effect 3. Vasodilation ``` 4. a1 antagonism b2 agonism Release of NO 🚫Ca2+ channel Opening K+ channels ```
53
Alpha1 adrenergic receptors are: 1. Coupled to PLC via Gq/11 a-protein 2. Increase IP3/DAG True or false❓
True
54
Describe the sequence of events for vascular smooth muscle contraction (a1 agonist)
``` 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
Alpha2 adrenergic receptors are: 1. -vely coupled to adenyly cylase via Gai subunit 2. Inhibits cAMP formation True or false❓
True
56
Describe the sequence of events for inhibition of NT release (a2 agonist)
``` 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
Beta1 adrenergic receptors are: 1. Actively coupled to adenyly cylase via G-alpha-s protein 2. ⬆️cAMP formation True or false❓
True
58
Describe the sequence of events for +ve chronotropy (b1 agonist)
``` 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
Describe the sequence of events for +ve ionotropy (b1 agonist)
``` 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
Beta2 adrenergic receptors are: 1. Actively coupled to adenyly cylase via G-alpha-s protein 2. ⬆️cAMP formation True or false❓
True
61
Describe the sequence of events for vascular smooth muscle relaxation (b2 agonist)
``` 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
Describe the sequence of events for vascular smooth muscle contraction (a2 agonist)
``` 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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