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PHA314 > Adrenoceptors > Flashcards

Adrenoceptors Flashcards

1
Q

General functions of Adr and NA

A

BP control
Myocardial contractility
Airway reactivity
Metabolic and CNS functions

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2
Q

Order of potency for B-ADRs

A

Isoprenaline
Adrenaline
Noradrenaline

Greater than or equal to for last two

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3
Q

Order of potency for a-ADRs

A

Adrenaline
Noradrenaline
Isoprenaline

(Greater than or equal to for all three)

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4
Q

Selective a-ADRs antagonist

A

Phenoxybenzamine

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5
Q

Selective antagonist for b-ADRs

A

Propanolol

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6
Q

Why did adrenaline cause a fall in arterial pressure after animal pre-treatment with ergot derivative?

A

The derivative is an a-ADR antagonist and the receptor’s blockade caused transition to b-ADR agonist effects.

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7
Q

Explain Ahlquist’s receptor name designations

A

a-ADRs on smooth muscles where catechol amines produce excitatory responses and b-ADEs where inhibitory responses are produced. GIT is an exception because it is relaxed by both agonist action

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8
Q

Adrenoceptor subtypes

A

Alpha-1A, 1B, 1D, (1L)
Alpha-2A, 2B, 2C, (2D)
Beta-1
Beta-2
Beta-3
Beta-4

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9
Q

Alpha-1 location and actions

A

Vascular smooth muscle - Increased vascular resistance
Eye - Mydriasis
Pilomotor - Hair erection
Liver - Glycolgenolysis
Vas Deferens - Ejaculation

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10
Q

Alpha-2 location and actions

A

Adrenergic and cholinergic nerve terminals - Inhibits transmitter release
Platelets - Stimulates aggregation
Some vascular smooth muscle - Contraction
Pancreas- Decreased insulin release

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11
Q

Beta-1 location and actions

A

Heart - Stimulates rate and force
Juxtaglomerular cells - Stimulates renin release

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12
Q

Beta-2 location and actions

A

Bronchioles - Dilation
Uterus - Relaxation
Vascular smooth muscle - Vasodilation
Liver - Glycogenolysis
Pancreatic B cells - Insulin release
Skeletal muscles - Tremors

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13
Q

Beta-3 location and actions

A

Fat cells (with B-1 and 2) - Lipolysis

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14
Q

Alpha 1 agonists

A

4MPTOX

Mephentermine
Methoxamine
Metaraminol
Midodrine
Phenylephrine
Tetrahydrozoline
Xylometazoline

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15
Q

Non-selective adrenergic agonists

A

Adrenaline (all)
NA (all except B3 and B4, less at B2)
Isoprenalol (B1 and B2)

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16
Q

Peculiarities of Alpha-1 agonists

A

Mephentermine and Metaraminol also act indirectly to release NA

Midodrine is a pro-drug

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17
Q

PPA of Alpha 1 agonists

A

Vasoconstriction

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18
Q

PTU of Alpha 1 agonists

A
  • Pressor agents in treatment of of
    hypotension & shock –)
  • Nasal decongestants
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19
Q

Which Alpha 1 agonists are used as pressor agents in the treatment of hypotension & shock?

A

Methoxamine & Phenylephrine

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20
Q

Which Alpha 1 agonists are used as treat nasal congestion?

A

Oxymetazoline
Tetrahydrozoline,
Xylometazoline
Naphazoline
Some preparations of phenylephrine

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21
Q

Adverse Effects (AEs) of Alpha 1 agonists

A

Hypertension
Headache
Reflex bradycardia
Excitability
Restlessness
Dry mouth
Sedation
Rebound hypertension ff. abrupt withdrawal

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22
Q

Alpha 2 agonists

A

A2C2GBAD

Apraclonidine
Clonidine
Clenbuterol
Guanfacine
Guanabenz,
Brimonidine
α-methyldopa
Dexmedetomidine

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23
Q

Peculiarities of Alpha 2 agonists

A
  • Apraclonidine & Brimonidine are used topically for glaucoma
    and ocular hypertension.
  • Methyldopa is converted in CNS to α-methylNA (α2 agonist).
  • Used very occasionally as centrally-acting sympatholytic vasodilators for the Rx of hypertension.
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24
Q

Which Alpha 2 agonists are used topically for glaucoma and ocular hypertension?

A

Apraclonidine & Brimonidine

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25
Q

PPA of Alpha 2 agonists

A

Reduced sympathetic outflow resulting in reduced peripheral
vascular resistance and reduced production of aqueous humour.

26
Q

PTU of Alpha 2

A
  • Adjunct therapy in shock
  • Hypertension
  • To reduce sympathetic response to withdrawal from narcotics,
    alcohol & tobacco
  • Glaucoma treatment
27
Q

AE of Alpha 2 agonists

A

Sedation
Dry mouth & nasal mucosa
Bradycardia
Orthostatic hypotension
Impotence
Constipation
Nausea & gastric upset
Bradyarrythmia
Reduced cardiac output
Hypotension

28
Q

Beta 1 agonists

A

DDX

Dobutamine
Denopamine
Xamoterol.

29
Q

Caution for Beta 1 agonists

A

Use with caution in patients with hypertension or cardiac
arrhythmias; used only IV.

30
Q

PPAs of Beta 1 agonists

A

Increases cardiac contractility
Increased heart rate
Increased atrioventricular conduction.

31
Q

Peculiarities of Beta 1 agonists

A

Dobutamine has strong inotropic effect with little chronotropic
effect = increase in CO without significant increase in HR.

32
Q

PTU of Beta 1 agonists

A

Short-term treatment of impaired cardiac function after
cardiac surgery, congestive heart failure, and myocardial infarction.

33
Q

AEs of Beta 1 agonists

A

Increased BP and HR

34
Q

Beta 2 agonists

A

MIFFAB2SPTR (Miffab2EsPita)

Metaproterenol
Isoetharine
Fenoterol
Formoterol
Albuterol
Bitolterol
Salmeterol
Salbutam
Procaterol
Terbutaline
Ritodrine

35
Q

Which Beta 2 agonists are long-acting?

A

Salmeterol and Salbutamol

36
Q

Which Beta 2 agonists are intermediate-acting?

A

All expect 2S

37
Q

Peculiarities of B2 agonists

A

Use with caution in patients with CV disease (reduced by
inhalational administration; as aerosols); minimal side
effects → intermediate acting.

38
Q

PPAs of Beta 2 agonists

A
  • Relaxation of bronchial smooth muscle
  • Relaxation of
    uterine SM
  • Activation of other β2Rs after systemic
    administration.
39
Q

PTUs of Beta 2 agonists

A
  • Asthma & chronic obstructive pulmonary disease
  • Acute bronchospasm (short & intermediate acting drugs)
  • Premature labour (Ritodrine)
  • Prophylaxis (long acting agents).
40
Q

AEs of Beta 2 agonists

A

Headache
Anxiety
Nausea
Muscle tremors
Nervousness
Palpitations

41
Q

β3 agonists

A

Amibegron
Mirabegron
Ro40-2148,
Solabegron
Vibegron

42
Q

α-non selective antagonists

A

Phenoxybenzamine
Phentolamine
Tolazoline
Ergot alkaloids

43
Q

α1-selective antagonists

A

BPITTDAUNT

  • Prazosin (1st agent)
  • Terazosin (longer half-life)
  • Doxazosin (longer half-life)
  • Alfuzosin
  • Tamsulosin
  • Indoramin
  • Urapidil
  • Bunazosin
  • Trimazosin
  • Niguldipine.
44
Q

PPAs of Alpha 1 selective antagonists

A
  • Decreased peripheral vascular resistance (promote vasodilation);
  • Relax smooth muscles in neck of bladder & in prostate.
45
Q

PTUs of Alpha 1 antagonists

A
  • Primary hypertension
  • Urinary retention
  • Increased urine flow in Benign Prostate Hyperplasia
46
Q

AEs of alpha 1 antagonists

A
  • Postural hypotension when therapy is instituted
  • Reflex tachycardia
47
Q

α2-selective antagonists

A

Yohimbine
Imiloxan
Idazoxan

48
Q

PPAs of alpha-1 antagonists

A
  • Blockade of decreased sympathetic outflow (aka increased sympathetic outflow) & potentiates release of NA
    from nerve endings; i.e. effects opposite of clonidine
  • Enters CNS =>
    increased sympathetic output => increased HR and BP.
  • Results in activation of α1 & β1 Rs in the heart & peripheral vasculature
49
Q

PTUs of alpha-1 antagonists

A
  • Ingredient in many weight loss products
  • Extensive use in
    treatment of male sexual dysfunction
50
Q

AEs of alpha-1 antagonists

A

Increased HR, BP and can cause severe tremors

51
Q

Non-selective β antagonists

A

Nadolol
Penbutolol
Pindolol
Propranolol
Timolol
Carteolol
Carvedilol
Bucindolol
Labetalol

52
Q

Carvedilol & Labetalol also block…

A

…α1Rs

53
Q

β1-selective antagonists

A

Acebutolol
Atenolol
Bisoprolol,
Esmolol (quick onset/short duration => used in urgent settings),
MetoprololBetaxolol
Celiprolol
Nebivolol

54
Q

β-2 selective antagonists

A

Butoxamine

55
Q

PPAs of B-blockers

A

↓ HR
↓ contractility
↓ CO; slow conduction in atria & AV node
↑ refractory period, AV node
Bronchoconstriction;
Prolonged hypoglycaemia
↓ plasma free fatty acids
↓ HDLc
↑ LDLc & triglycerides
Hypokalemia

56
Q

PTUs of B-blockers

A

Angina pectoris
Hypertension
Cardiac arrhythmias
CHF
Pheochromocytoma
Glaucoma
Hypertropic obstructive cardiomyopathy
Hyperthyroidism
Migraine prophylaxis
Acute panic symptoms
Substance withdrawal
Variceal bleeding in portal hypertension

57
Q

AEs of B-blockers

A

Bradycardia
-ve ionotropic effect
↓ CO
Bradyarrythmia
↓ AV conduction
Bronchoconstriction
Fatigue
Sleep disturbances (insomnia, nightmares
Prolongation of hypoglycemia
Sexual dysfunction in men
Drug interactions.

58
Q

3rd generation non-selective agents

A

Carteolol
Carvedilol
Bucindolo
Labetalol

59
Q

PPAs of 3rd generation B-blockers

A

membrane
stabilizing effect; ISA (intrinsic sympathomimetic activity);
vasodilation.

60
Q

Mechanism of action of B-blockers

A

α1 antagonism
β2 agonism
Release of NO
Ca2+ channel blockade
Opening of K+ channels

PHA314 (4 decks)

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