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Pharmacology > 12 Respiratory system > Flashcards

12 Respiratory system Flashcards

1
Q

12.01 β2-RECEPTOR AGONISTS

Long-acting: salmeterol, formoterol, etc. - actions

A

selective β2 agonists
bronchodilatation - a physiological antagonist of spasmogenic mediators
minimal action on heart: ↑rate and force

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2
Q

12.01 β2-RECEPTOR AGONISTS

Long-acting: salmeterol, formoterol, etc. - MOA

A

↓calcium-mediated contraction in bronchioles
↑cAMP which activates protein kinase A (PKA)
PKA inhibits myosin light chain kinase - the mediator of contraction

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3
Q

12.01 β2-RECEPTOR AGONISTS

Long-acting: salmeterol, formoterol, etc. - abs/distrib/elim

A

by regular inhalation for chronic asthma
salmeterol: slower onset and long-acting (8-12h) when compared to salbutamol (3-5h)

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4
Q

12.01 β2-RECEPTOR AGONISTS

Long-acting: salmeterol, formoterol, etc. - clinical use

A

asthma and obstructive airways disease (main use)
long-acting compounds are typically used together with inhaled corticosteroids for nocturnal asthma, exercise-induced asthma and long-term control

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5
Q

12.01 β2-RECEPTOR AGONISTS

Long-acting: salmeterol, formoterol, etc. - adverse effects

A

tremors
tachycardia, sometimes dysrhythmias
nervousness
some peripheral dilatation

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6
Q

12.02 XANTHINES

Theophylline (similar: roflumilast, aminophylline = theophylline ethylenediamine) - actions

A

bronchodilatation
also stimulates CNS and CVS

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7
Q

12.02 XANTHINES

Theophylline (similar: roflumilast, aminophylline = theophylline ethylenediamine) - MOA

A

inhibits phosphodiesterase (PDE4) thus ↑cAMP (and ?cGMP), thus relaxing smooth muscle
inhibition of PDE4 in inflammatory cells can ↓mediator release

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8
Q

12.02 XANTHINES

Theophylline (similar: roflumilast, aminophylline = theophylline ethylenediamine) - abs/distrib/elim

A

theophylline and roflumilast are given orally
aminophylline can be given IV
metabolised mainly by cytochrome P450
plasma concentrations: ↑by liver disease, cardiac failure and viral infection; ↓by heavy drinking and smoking
plasma concentrations are affected by drug interaction: ↓by rifampicin, phenytoin and carbamazepine; ↑by erythromycin, diltiazem, fluconazole and caffeine

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9
Q

12.02 XANTHINES

Theophylline (similar: roflumilast, aminophylline = theophylline ethylenediamine) - clinical use

A

theophylline is a fourth-line drug for chronic asthma not adequately controlled by other agents
aminophylline IV is used for severe acute asthma
roflumilast is used as an add-on to bronchodilators for severe COPD

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10
Q

12.02 XANTHINES

Theophylline (similar: roflumilast, aminophylline = theophylline ethylenediamine) - adverse effects

A

GIT disturbances, tachycardia, anxiety, insomnia
high plasma concentrations of theophylline can cause serious dysrhythmias or seizures, and should be monitored

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11
Q

12.03 LEUKOTRIENE ANTAGONISTS

Montelukast (similar: zafirlukast) - actions

A

reverse bronchoconstriction
relax airway smooth muscle in mild asthma

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12
Q

12.03 LEUKOTRIENE ANTAGONISTS

Montelukast (similar: zafirlukast) - MOA

A

the drug is an antagonist at the cysteinyl leukotriene receptor (CysLT1) on which the bronchospasmic mediators LTC4, LTD4 and LTE4 act
it can ↓both the early- and late-phase responses to the inhaled allergen

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13
Q

12.03 LEUKOTRIENE ANTAGONISTS

Montelukast (similar: zafirlukast) - abs/distrib/elim

A

given orally
metabolised in the liver through cytochrome P450 2C8 and excreted mainly in bile
half-life 3-5h

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14
Q

12.03 LEUKOTRIENE ANTAGONISTS

Montelukast (similar: zafirlukast) - clinical use

A

a third-line drug for asthma
used as an adjunct to inhaled corticosteroids and long-acting β2 agonists
effective in aspirin-induced asthma and exercise-induced asthma

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15
Q

12.03 LEUKOTRIENE ANTAGONISTS

Montelukast (similar: zafirlukast) - adverse effects

A

headache
abdominal pain

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16
Q

12.04 INHALED MUSCARINIC ANTAGONISTS

Short-acting: ipratropium; long-acting: tiotropium, aclidinium, umeclidinium, glycopyrronium - actions

A

bronchodilatation by inhibiting acetylcholine-mediated bronchoconstriction and mucus secretion
no effect on the late phase

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17
Q

12.04 INHALED MUSCARINIC ANTAGONISTS

Short-acting: ipratropium; long-acting: tiotropium, aclidinium, umeclidinium, glycopyrronium - MOA

A

competitively antagonises acetylcholine action on muscarinic receptors

18
Q

12.04 INHALED MUSCARINIC ANTAGONISTS

Short-acting: ipratropium; long-acting: tiotropium, aclidinium, umeclidinium, glycopyrronium - abs/distrib/elim

A

given by inhalation
ipratropium lasts 3-5h
long-acting agents last 12-24h

19
Q

12.04 INHALED MUSCARINIC ANTAGONISTS

Short-acting: ipratropium; long-acting: tiotropium, aclidinium, umeclidinium, glycopyrronium - clinical use

A

for chronic asthma as an adjunct to long-acting β2 agonists and corticosteroids
for COPD
nebulised ipratropium is used in the emergency management of asthma

20
Q

12.04 INHALED MUSCARINIC ANTAGONISTS

Short-acting: ipratropium; long-acting: tiotropium, aclidinium, umeclidinium, glycopyrronium - adverse effects

A

urinary retention
dry mouth
constipation
pharyngitis

21
Q

12.05 INHALED GLUCOCORTICOIDS

Beclometasone, budesonide, fluticasone, etc. - actions

A

reduce hyper-reactivity and decrease the inflammatory delayed phase
no effect on the immediate phase

22
Q

12.05 INHALED GLUCOCORTICOIDS

Beclometasone, budesonide, fluticasone, etc. - MOA

A

reduce the activation of inflammatory cells and the release of mediators, especially cytokines

23
Q

12.05 INHALED GLUCOCORTICOIDS

Beclometasone, budesonide, fluticasone, etc. - abs/distrib/elim

A

given by inhalation with metered dose inhaler
the full action takes days to occur
often formulated together with long-acting β2 agonists in combined inhalers

24
Q

12.05 INHALED GLUCOCORTICOIDS

Beclometasone, budesonide, fluticasone, etc. - clinical use

A

added to bronchodilator therapy if this is inadequate alone
an IV glucocorticoid (e.g. hydrocortisone) is life-saving in acute severe asthma (status asthmaticus)

25
Q

12.05 INHALED GLUCOCORTICOIDS

Beclometasone, budesonide, fluticasone, etc. - adverse effects

A

hoarse voice
oral candidiasis (thrush)
regular high doses of inhaled corticosteroids can be absorbed and cause adrenal suppression and other adverse effects

26
Q

12.06 INHIBITOR OF MAST CELLS

Omalizumab - actions

A

reduces plasma immunoglobulin E (IgE) levels and decreases the magnitude of both early and late phases

27
Q

12.06 INHIBITOR OF MAST CELLS

Omalizumab - MOA

A

monoclonal antibody that inhibits the binding of IgE to mast cells (and eosinophils), thus reducing mediator release

28
Q

12.06 INHIBITOR OF MAST CELLS

Omalizumab - abs/distrib/elim

A

given SC at 2- to 4-week intervals

29
Q

12.06 INHIBITOR OF MAST CELLS

Omalizumab - clinical use

A

for persistent allergic asthma not completely controlled with an inhaled corticosteroid plus long-acting β2 agonist

30
Q

12.06 INHIBITOR OF MAST CELLS

Omalizumab - adverse effects

A

hypersensitivity reactions

31
Q

12.07 INHIBITION OF INTERLEUKIN-5

Monoclonal antibodies: mepolizumab, reslizumab - actions

A

inhibits IL-5, which is the main cytokine responsible for growth and activation of eosinophils

32
Q

12.07 INHIBITION OF INTERLEUKIN-5

Monoclonal antibodies: mepolizumab, reslizumab - MOA

A

monoclonal antibody that blocks the binding of IL-5 to the receptor complex on the surface of eosinophil cells, thus leading to reduced production and survival of eosinophils

33
Q

12.07 INHIBITION OF INTERLEUKIN-5

Monoclonal antibodies: mepolizumab, reslizumab - abs/distrib/elim

A

given by IV injection every 4 weeks
broken down by proteolytic enzymes throughout the body

34
Q

12.07 INHIBITION OF INTERLEUKIN-5

Monoclonal antibodies: mepolizumab, reslizumab - clinical use

A

severe refractory eosinophilic asthma

35
Q

12.07 INHIBITION OF INTERLEUKIN-5

Monoclonal antibodies: mepolizumab, reslizumab - adverse effects

A

headache, injection site reactions, back pain, myalgia

36
Q

12.08 ANTI-FIBROTIC AGENTS

Drugs for idiopathic pulmonary fibrosis: pirfenidone, nintedanib - actions

A

reduction of inflammation and fibrosis in lung tissue

37
Q

12.08 ANTI-FIBROTIC AGENTS

Drugs for idiopathic pulmonary fibrosis: pirfenidone, nintedanib - MOA

A

pirfenidone has immunosuppressant effects in reducing fibroblast proliferation and mediators of fibrosis
nintedanib is a tyrosine kinase inhibitor that interrupts the signalling cascades involved in fibroblast growth and differentiation

38
Q

12.08 ANTI-FIBROTIC AGENTS

Drugs for idiopathic pulmonary fibrosis: pirfenidone, nintedanib - abs/distrib/elim

A

given orally 2-3× daily
mainly metabolised in the liver (dose may need to be adjusted in liver impairment)

39
Q

12.08 ANTI-FIBROTIC AGENTS

Drugs for idiopathic pulmonary fibrosis: pirfenidone, nintedanib - clinical use

A

pulmonary fibrosis, to slow the decline in lung function

40
Q

12.08 ANTI-FIBROTIC AGENTS

Drugs for idiopathic pulmonary fibrosis: pirfenidone, nintedanib - adverse effects

A

nausea, diarrhoea, loss of appetite

Pharmacology (34 decks)

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