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MP324 > MP324 - PHARMACOLOGY > Flashcards

MP324 - PHARMACOLOGY Flashcards

1
Q

short-acting B2 adrenoceptor agonists

A

salbutamol
piralbuterol
levalbuterol

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2
Q

mechanism of action of B2 adrenoceptor agonists

A
  • function via a cyclin AMP-dependent relaxation of smooth muscle
  • Ins(1,4,5)P3 receptor in the sarcoplasmic reticulum
  • may be inactivated by protein kinase A (less calcium is released, inhibits contraction)
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3
Q

function of stimulating adenylyl cyclase

A

this enzyme catalyses the formation of cyclic AMP

cAMP then activates protein kinase A

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4
Q

actions of protein kinase A

A

inhibit MCLK
promote calcium efflux
inhibit the MPK pathway by phosphorylating and inhibiting Raf-1 kinase

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5
Q

mechanism of action of long-acting B2 adrenoceptor agonists

A

have lipophilic groups attached which interact with exo-sites on the receptor

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6
Q

problem with B2 adrenoceptor agonists

A

desensitisation

however less with salmeterol because partial agonist

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7
Q

3 mechanisms of desensitisation

A
  • phosphorylation of the occupied receptor by B-adrenoceptor kinase (B-ARK)
  • internalisation of the receptor
  • phosphorylation of the occupied receptor by protein kinase B (negative feedback)
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8
Q

corticosteroids

A

beclamethasone
budesonide
fluticasone
mometasone
ciclesonide

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9
Q

mechanism of action of corticosteroids

A
  • dampen inflammation
  • used as prophylactic therapy
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10
Q

standard oral steroid

A

prednisolone

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11
Q

intravenous steroids

A

hydrocortisone
methylprednisolone

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12
Q

glucocorticoid effect on mediators

A

blocked/inhibited mediators:
- PAF
- LTB4
- PGD2
- Histamine

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13
Q

steroid side effects

A
  • weight gain/water retention
  • mood changes
  • increased appetite
  • sweating/rashes
  • shortness of breath
  • sleep problems/moon face
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14
Q

leukotriene inhibitors

A

zafirlukast
montelukast

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15
Q

leukotriene B4

A

neutrophil chemoattractant

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16
Q

leukotriene C4 and D4

A

cause bronchoconstriction
increased bronchial reactivity, mucosal oedema and mucous hypersecretion

17
Q

montelukast unique side-effects

A

eosinophilia
Churg Strauss syndrome (eosinophil granulomatosis in small vessels)

18
Q

xanthines

A

theophylline
emprofylline

19
Q

mechanism of adenosine receptor antagonists

A

block the inhibitory action of adenosine upon adenylyl cyclase (via its receptors), and allow intracellular cAMP to accumulate and promote relaxation

20
Q

mechanism of phosphodiesterase inhibitor

A

blocks reduction in intracellular cAMP and relax smooth muscle; increase catecholamines release

21
Q

effects of theophylline in asthma

A
  • smooth muscle relaxation
  • inhibit anaphylactic release of mediators
  • suppress oedema
  • central stimulation of ventilation
22
Q

problems with xanthines

A
  • doses should be low to avoid gastro-abdominal problems
  • CNS stimulation is a problem when maintenance administration is increased too quickly
  • toxicity is a risk of seizures and arrhythmias
23
Q

oral theophylline most serious side-effects

A

anorexia
vomiting
mild CNS stimulation

24
Q

problems with xanthines through IV routes

A

increase arrhythmia, palpitations, and tachycardia at doses above 30mg/L

25
Q

long-acting B2 adrenoceptor agonists

A

salmeterol
formoterol

26
Q

clinical efficacy of SABA (salbutamol)

A
  • onset of action is within 3 minutes
  • peak activity after 2.5 hours
  • duration of action is between 4-6 hours
27
Q

clinical efficacy of LABA (salmeterol vs formoterol)

A
  • option for patients that are symptomatic despite regular SABA use
  • both are lipophilic, but the water solubility of formoterol lets it diffuse rapidly to the B2AR and cause bronchodilation in between 1-3 min
  • salmeterol has longer onset of action
28
Q

side effects of SABAs

A

tachycardia/palpitations
tremor
hypokalemia
headache

29
Q

short-acting muscarinic antagonists (SAMAs)

A

ipratropium bromide

30
Q

mechanism of action of SAMAs

A
  • blocks all muscarinic receptors without sub-type selectivity
  • onset of action within minutes
  • peak activity between 1-2 hours
  • duration of action approximately 4 hours
31
Q

long-acting muscarinic antagonists (LAMAs)

A

tiotropium

32
Q

mechanism of action of LAMAs

A
  • binds to M1-M3 receptors and is 10x more potent than SAMAs
  • dissociates slowly from M1 and M3 receptors
  • dissociates relatively rapidly from M2 receptor (kinetic selectivity)
    -onset occurs within 30 min
  • peak activity at 3 hours
  • duration of action over 24hours
33
Q

why are muscarinic receptors a good target

A

parasympathetic activity mediates both bronchial smooth muscle contraction and the release of mucus into the airway lumen through stimulation of muscarinic receptors

34
Q

location of M1 receptors

A

expressed in peribronchial ganglia

35
Q

location of M3 receptors

A

bronchial smooth muscle cells

36
Q

location of M2 receptors

A

post ganglionic parasympathetic nerve and act as auto receptors

37
Q

adverse effects of muscarinic antagonists

A

associated with its anti-cholinergic activity
- dry mouth
- exacerbation of narrow-angle glaucoma and myasthenia gravis (autoimmune disease)

38
Q

oxygen therapy reduces…

A
  • haematocrit
  • pulmonary artery pressures
  • rapid eye movement related hypoxemia

MP324 (10 decks)

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