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Pharmacology > SNS > Flashcards

SNS Flashcards

1
Q

Steps of catecholamine synthesis

A

Tyrosine—>dopa—>dopamine—>norepinephrine—>epinephrine

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2
Q

What’s the rate limiting step for catecholamine synthesis

A

Tyrosine —> dopa

Catalysed by tyrosine hydroxylase

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3
Q

Potency of catecholamines on adrenergic receptors

A

a —> epinephrine > norepinephrine&raquo_space; isoproterenol
B —> isoproterenol > epinephrine ~ = norepinephrine
On B1 epinephrine ~ norepinephrine
On B2 epinephrine&raquo_space; norepinephrine

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4
Q

What are the effects of activating the adrenergic receptors on blood pressure

A

a1 - Vaso constriction - increases TPR - increasing BP
B1 - increases heart rate - increases cardiac output - increasing blood pressure
B2 - vasodilation- decreasing TPR - decreasing blood pressure

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5
Q

Phenylephrine which receptors

A

Selective a1 agonist

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6
Q

Phenylphrine indications

A

To cause mydriasis, nasal decongestant and for hypotension

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7
Q

Phenylphrine side effects

A

Hypertensive headache and arrhythmia

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8
Q

How can phenylphrine be used for its indications and for its side effects

A
  • patient with rhinitis and nasal congestion (vasoconstriction increase TPR and BP)
  • patient with hypotenuse during spinal anaesthesia (increases BP)
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9
Q

Naphzoline, oxymetazoline, xylometazoline way of administration

A

Topical

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10
Q

Naphzoline, oxymetazoline, xylometazoline receptors activity

A

selective a1 agonist

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11
Q

Naphzoline, oxymetazoline, xylometazoline indications

A

Nasal congestion and conjunctivitis

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12
Q

Naphzoline, oxymetazoline, xylometazoline adverse effects

A

Hypetenisve headache and arrhythmias

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13
Q

Drugs in the treatment of hypertension

A

Etilefrine and midodrine

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14
Q

Etilefrine receptors activity

A

acts on a1, B1, B2 (B1>B2)

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15
Q

Etilefrine indication

A

Causes an increase in heart rate, CO, TPR hence raising the blood pressure so it is used for hypotension

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16
Q

Etilefrine adverse effects

A

Tachycardia

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17
Q

Midodrine receptors activity

A

a1 only so no cardiac effect

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18
Q

Midodrine indication

A

Causes vasoconstriction increasing TPR and increasing BP hence used for hypotension

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19
Q

Midodrine adverse effects

A

Reflex bradycardia

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20
Q

Clonidine receptors

A

Selective a2 agonist (mainly presynaptic)

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21
Q

Clonidine actions

A

Vasodilation through central inhibition of norepinephrine release

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22
Q

Clonidine indications

A

Hypertension and withdrawal of opiates and benzodiazepines

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23
Q

Dobutamine receptors

A

B1 selective

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24
Q

Dobutamine actions

A

Causes an increase in cardiac output

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25
Q

Dobutamine indication

A

Acute heart failure

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26
Q

Dobutamine contraindications

A

Atrial fibrillation

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27
Q

What are the B2 adrenergic agonists

A

SABA- short acting B agonists

LABA- long acting B agonists

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28
Q

SABA examples and uses

A

Albuterol and fenoterol

- quick relief of symptoms of asthmatic attacks

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29
Q

LABA examples and uses

A

Prevention of bonchospasm and asthma attacks
Formoterol—> both
Salmeterol

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30
Q

Epinephrine receptor activation and action at low does

A

B1, a1 increase CO and decrease TPR

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31
Q

Epinephrine receptor activation and action at high doses

A

B1, a1>B2 causing an increase in heart rate and stroke volume —> increase in CO and TPR
(Can cause reflex bradycardia)

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32
Q

How is epinephrine administered

A

Subcutaneous, intramuscular or intravenous

33
Q

What metabolises epinephrine

A

COMT AND MAO

34
Q

epinephrine indications

A
  • Hypersensitivity reactions (anaphylaxis) given i.m and S.C
  • Cardiac arrest I.V
  • prolongs duration of action of Anaesthesia(vasoconstriction -> ŁA absorption -> increase local effect)
35
Q

Epinephrine adverse effects

A

Cardiac arrhythmias, haemorrhage and CNS disturbances (anxiety tremors)

36
Q

Norepinephrine receptors

37
Q

Norepinephrine therapeutic uses

A

Shock(increases vascular resistance) and adjacent to local anaesthesia

38
Q

Norepinephrine and epinephrine similarities

A

Used in cardiac arrest and adjacent to Local anaesthesia

39
Q

Only epinephrine and not norepinephrine

A

Anaphylaxis and bronchospasm (due to B2 properties)

40
Q

Dopamine receptors activation

A

At low doses D1, D2, At moderate doses B1 and at high doses a1

41
Q

Dopamine at different doses with receptors activation and actions

A

a1 (higher than 10mg/kg/min)- vasoconstriction- increases blood pressure
B1(5-10mg/kg/min) - increase in heart rate and cardiac output
D1 and D1 (5mg/kg/min)- vasodilation in renal bed

42
Q

Dopamine therapeutic uses

A

Cardiogenic and septic shock also hypotension and bradycardia

43
Q

What is pseudoephedrine used for

A

Nasal decongestant

44
Q

What is tachyphylaxis

A

Decreased in response to drug after repeated exposure

45
Q

What are amphetamine and ephedrine used for and why are they not used

A

Used for asthma but they cause hypertension

46
Q

Phenoxybenzamine receptor activity

A

Irreversible binding to a1 and a2

Causes vasodilation-> reflex tachycardia

47
Q

Phenoxybenzamine indications

A

Pheochromactoma

48
Q

Phenoxybenzamine adverse effects

A

Postural hypotension, nasal stiffness and baroreceptor reflex tachycardia

49
Q

Phentolamine receptors

A

Competitive a1 and a2

50
Q

Phentolamine indications

A

Pheochromacytoma and reverses the actions of a - adrenomimetics

51
Q

Phentolamine adverse effects

A

Postural hypotension nasal stiffness and baroreceptor reflex tachycardia

52
Q

Prazosin, terazosin, oxazosin, alfuzosin and tamsulosin - receptor activation

A

Competitive a1 blockers

53
Q

Prazosin, terazosin, oxazosin, alfuzosin and tamsulosin - adverse effects

A

Orthostatic hypotension and nasal congestion

54
Q

Prazosin, terazosin, oxazosin, alfuzosin and tamsulosin actions and indications

A

Causes vasodilation and relaxation of smooth muscles in urinary tract
Indications for - hypertension and BPH

55
Q

Which a1 blockers are only used for BPH

A

Alfuzosin and tamsulosin

56
Q

Which a1 blockers are used for both BPH and hypertension

A

Doxazosin and terazosin

57
Q

How many generations of B blockers are there

A

4 generations

58
Q

Why shouldn’t B blockers be stopped abruptly

A

Could lead to angina and rebound hypertension

59
Q

What is the 1st generation B blockers

A

Non selective B blocker - prevents the effects of epinephrine in anaphylaxis
It includes
Propanolol
Timolol —> used for glaucoma

60
Q

What is the 2nd generation B blockers

A 
B1 selective B blockers 
It includes :- 
Atenolol
Bisoprolol
Esmolol 
Acebutolol
Metoprolol
61
Q

What is the 3rd generation B blockers

A

Non selective B blockers + additional effects
It includes :-
Carvedilol
Labetolol

62
Q

What is the 4th generation B blockers

A

B1 selective B blocker + additional effects
It includes :-
Nebivolol
Betaxolol

63
Q

What is nebivolol additional effects

A

Increase NO production

64
Q

What is celiprolol additional effects

A

B2 agonism

65
Q

What is carvedilol and labetolol additional effects

A

a1 antagonism (used in amphetamine overdose)

66
Q

What is carvedilol and betaxolol additional effects

A

Ca2+ enter blockade

67
Q

Does propanolol penetrate the CNS

A

Yes it does

68
Q

Propanolol actions

A

Non selective B blocker so causes decrease in CO and BP

  • cause peripheral vasoconstriction and bronchoconstriction
  • can cause a decrease in glycogenolysis and glucagon secretions —> hypoglycaemia
69
Q

Propanolol indications

A

Migraine prophylaxis, hypertension, angina, MI and arrhythmias

70
Q

Propanolol therapeutic uses

A

Migraine
Hyperthyroidism
Tremor
Stage fright

71
Q

Propanolol adeverse effects

A

Hypotension, bradycardia and decrease in cardiac contractility am an cause asthma attack and insomnia

72
Q

Cardioselective B blockers uses

A

Can be used for asthma and diabetes (little effect on carbs metabolism)

73
Q

B blocker with intrinsic sympthomimitic activity

A

Acebutolol and pindolol

74
Q

B blockers with a1 blocking properties

A

Labetolol and carvedilol

75
Q

a1 agonist ending

76
Q

a1 antagonist ending

77
Q

B2 agonist ending

78
Q

B1 antagonist ending

Pharmacology (33 decks)

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