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Pharmacology > Asthma > Flashcards

Asthma Flashcards

1
Q

Characteristics of category 1 asthma (4)

A

Intermittent
Daytime symptoms <2 /week
Nocturnal <2 per month
PEFR >80%

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2
Q

Characteristics of category 2 asthma (4)

A

Mild persistent
Daytime symptoms 3-4 / week
Nocturnal 2-4 / month
PEFR >80%

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3
Q

Characteristics of category 3 asthma (4)

A

Moderate persistent
Daytime symptoms >4 / week
Nocturnal > 4 / month
PEFR 60-80%

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4
Q

Characteristics category 4 asthma (4)

A

Persistent severe
Daytime symptoms continuous
Nocturnal frequent
PEFR <60%

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5
Q

Name 3 examples of short acting B2 agonists.

A

Salbutamol!
Fenoterol
Terbutaline

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6
Q

Half life of salbutamol

A

4-6 hours

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7
Q

MOA B2 adrenoreceptor agonists (7-2 direct,4 indirect )

A

Increase cAMP by stimulating adenylyl cyclase via stimulatory G proteins. cAMP phosphorylates a cascade of enzymes which results in:
• Relaxation smooth muscle
• bronchodilation (direct effect-functional antagonists to reverse bronchoconstriction)
• inhibit release of inflammatory mediators (mast cells,TNF-alpha from monocytes ) (indirect)
• increased mucociliary clearance
• prevent microvascular leakage, therefore limit mucosal oedema
• reduce presynaptic acetylcholine release, preventing reflex cholinergic bronchoconstriction

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8
Q

Route of admin of ß2 agonists

A

Inhale mostly.
Oral: only children and people unable to use inhalers
Salbutamol can be given as nebuliser, also iv if life threatening.

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9
Q

3 main classes of bronchodilators

A
  • B2 adrenergic agonists (sympathomimetics)
  • Anticholinergics (muscarinic receptor antagonists)
  • Methylxanthines and PDE4 inhibitors
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10
Q

Indications inhaled ß2 adrenoreceptor agonists

A

Drug of choice in management acute bronchoconstriction or spasm. Principle management of asthma and COPD.

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11
Q

Contraindications to B2 agonists (3)

A

Hyperthyroidism
Cardiovascular disease
Arrhythmia
(Caution)

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12
Q

Adverse effects B2 agonists (3)

A
  • Fine tremor
  • Tachycardia and palpitations
  • Hypokalaemia
  • Nervousness, headache (vasodilation), dizzy. ‘
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13
Q

Drug interactions B2 agonists (2)

A

Corticosteroids - increase R hypok and hyperglycemia

Digoxin and diuretics- increase risk cardiac arrhythmia

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14
Q

Name 2 examples of long acting B2 agonists

A

Salmeterol!

Formoterol

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15
Q

Half life of salmetorol

A

12 hours

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16
Q

Name 2 examples of methylxanthines

A

-Phylline.
Aminophylline!
Theophylline
Bronchodilators

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17
Q

MOA xanthines

A

Inhibit enzyme phosphodiesterase, which catalyse hydralysis of CAMP to AMP
Therefore increased CAMP - relax smooth muscle → bronchodilation
Also antagonise adenosine at A2 receptors (a potent broncoconstrictor) and has anti-inflammatory activity on t cells by decrease release platelet activating factor (PAF)

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18
Q

Route administration Xanthines

A

Oral (theophylline)

Aminophylline IV for severe attacks.

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19
Q

Indications methylxanthines

A
  • Second line treatment for acute, severe and chronic persistent asthma !
  • Also in children unable to use inhalers
  • IV in status asthmaticus (aminophylline)
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20
Q

Contraindications xanthines (3)

A

Cardiac disease
HT
Hepatic impairment (metabolised by liver)

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21
Q

Adverse effects methylxanthine. 2 GIT, 5 CV, 3 CNS

A

GIT: nausea, vomit,
Cardiovascular: tachycardia, dysrythmias. Headache, flushing, hypotension (dilate smooth muscle)
CNS: insomnia, tremor, anxiety

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22
Q

What is the therapeutic index of Xanthines?

A

Very narrow! 10-20 mcg/ml

This causes adverse effects more easily and small increases above therapeutic dose can be toxic and even fatal.

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23
Q

When do methylxanthines become most effective?

A

6 days after starting

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24
Q

Drug interaction Xanthines

A

Macrolides. Macrolidies occupy the enzymes involved in theophylline breakdown, increasing the plasma conc. Small increases above therapeutic dose toxic/fatal.

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25
Q

MOA glucocorticoids in treatment asthma (4 nb, 8 total)

A

INHIBIT INFLAMMATORY CASCADE
• Induce formation lipocortin -1!, which inhibits phospholipase A2. This reduces free arachidonic acid and therefore decreased LEUKOTRIENE
• reduced mucosal oedema and mucous production
• inhibit generation PROSTAGLANDIN E2 and PGI2 by inhibit COX2
• decrease formation CYTOKINES (esp th2), eosinophils, macrophages, T cells, mast cell infiltration
• B2 - adreno receptor upregulation
• decrease permeability capillaries
• decrease hyper responsiveness to sensitive stimuli eg cold, allergens

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26
Q

Indications glucocorticosteroids in asthma (3)

A
  • Most effective controller therapy!
  • For asthma (prevent progression), usually in combination with B2 agonists, or severe frequent exacerbations COPD
  • rescue course in rapidly deteriorating conditions
  • iv for acute exacerbations
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27
Q

Contraindications glucocorticoids (2)

A

Caution in growing children, systemic and local resp/ear, nose, throat infections

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28
Q

Adverse effects glucocorticosteroids (4)

A

Oral candidiasis (rinse mouth)
Irritation, hoarseness voice, dysphonia
Suppression hypothalamic-pituitary-adrenal axis: Cushings, HT, diabetes
Headache, skin reactions and bruises, psych, paradoxical bronchoconstriction, hypersensitivity

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29
Q

Name 2 examples of Leukotriene R antagonists

A

Montelukast!

Zafirlukast

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30
Q

Leukotriene R antagonists MOA

A

Selective reversible inhibitors of cysteinyl leukotriene -1 R, thus blocking the effects of leukotrienes LTC4, LTD 4, LTE 4
Causing bronchodilation

31
Q

Indications leukotriene r antag

A

Prophylaxis and PREVENTOR asthma to decrease response to allergens.
Children
Allergic rhinitis

Not effective in COPD

32
Q

Contraindications leukotriene R antagonists (4)

A

Not useful in COPD or severe asthma
Elderly
Pregnancy
Churg - Strauss syndrome

33
Q

Adverse effects Leukotriene R antagonists (4)

A

GIT disturbance
Headache
Eosinophilia, Vasculitis ( churg Strauss Syndrome)
Rash, dry mouth, anaphylaxis, liver dysfunction (very rare)

34
Q

Drug interactions Leukotriene R antagonists. (4)

A

Warfarin (enhance anticoag effect)
Erythromycin, terfenadine (zafirlukast levels reduced)
Theophylline (zafirlukast levels reduced)
(Zafirlukast extensively metabolised by liver. Inhibit cyp 3a4 and Cyp 2c9)
NSAIDs: may narrow the airway when interact with LRA

35
Q

Anticholinergics examples (2)

A 
Ipratropium bromide (short acting)
Tiotropium (long acting)
36
Q

Muscarinic receptor antags MOA

A
  • Competitive agonists of ach on m3 receptors. This blocks effect of ach, block direct constrictor effect on bronchial smooth muscle mediated by PLC-IP3-Ca path, block ach mediated tracheobronchial constriction
  • bronchodilation by inhibit parasymp vagal fibres
37
Q

Indications antimuscarinics in obstructive airway diseases (4)

A
  • Adjuncts to B 2 agonists to treat obstructive airway diseases (synergistic)
  • More useful in COPD - long term maintenance elderly
  • Pts that can’t tolerate adverse effects B 2 agonists, especially elderly
  • Cystic Fibrosis
38
Q

Contraindications muscarinic anticholinergics (3)

A

Glaucoma!
Prostatic hypertrophy (urinary retention)
Pregnancy

39
Q

Adverse effects muscarinic receptor antagonists (2)

A
  • May precipitate glaucoma in elderly (direct contact)!
  • Dry mouth
  • Paradoxical bronchoconstriction , rebound airway hyperresponsiveness when abruptly stopped (rare), constipation rare
40
Q

Name 3 pathophysiological causes of asthma symptoms

A
  • broncoConstriction muscle
  • oedema mucosal lining of small bronchi
  • plugging bronchial lumen with viscous mucus and inflammatory cells
41
Q

Name 2 classes asthma preventers with examples

A

Anti-inflammatory to prevent attacks
• inhaled corticosteroids: beclomethasone, budesonide, ciclesonide, fluticasone
• oral corticosteroids:prednisone

(Cromylons, sodium cromoglycate)

42
Q

Name 3 classes asthma controllers with examples

A

Sustained bronchodilator action but weak/unproven anti inflammatory effect
• Long acting beta 2 agonists eg salmeterol
• methylxanthines eg theophylline
• leukotriene receptor antagonists eg montelukast, zafirlukast

43
Q

Name 3 classes asthma relievers with examples

A
  • Short acting beta 2 agonists eg salbutamol
  • anticholinergics eg ipratropium, tiotropium
  • short acting theophylline (xanthine)
44
Q

Name 2 iv corticosteroids for asthma

A
  • Methylprednisolone

* hydrocortisone

45
Q

Name 2 mast cell stabilisers

A
  • sodium chromoglycate
  • ketotifen ( second gen h1 r antag )
  • Nedocromil (chromones)
46
Q

What is the treatment of choice for acute bronchoconstriction?

A

Beta 2 agonists

47
Q

Moa anticholinergics for asthma?

A
  • Parasympathetic vagal fibres provide broncoconstrictor tone to smooth muscle of airway. They are activated by reflex on stimulation of sensory (irritant) receptors in airway walls.
  • antimuscarinics block muscarinic r, especially m3
48
Q

Name 3 inhaled corticosteroids for asthma controller

A

• Beclomethasone
. Budesonide
• fluticasone

49
Q

Name 4 systemic corticosteroids for asthma controller

A
  • Prednisone
  • methylprednisolone
  • betamethasone
  • dexamethasone, hydrocortisone
50
Q

Name 3 classes mediator antagonists in treatment asthma and examples. (Adjunctive therapy)

A
  • Antihistamines eg chlorphenIramine (allergex) (H1),
  • anti-leukotrienes eg montelukast, zafirlukast
  • mast cell stabilisers eg sodium cromoglycate
51
Q

Name 4 first generation traditional (sedative) h1 antihistamines

A
  • Chlorphenamine (allergex)
  • promethazine
  • cyclizine (valoid)
  • hydroxizine (aterax)
52
Q

Difference in pharmacokinetics for first and second generation h1 receptor antagonists? (4)

A
  • Nonselective vs selective for h1
  • cross BBB vs minimal penetration
  • t1/2 shorter (4-8h) vs longer (10 h) (thus daily dosing)
  • metabolised by liver vs minimally metabolised, excreted by kidney unchanged
53
Q

Name 5 indications for first generation h1 receptor antagonists?

A
  • allergic conditions eg chronic urticaria
  • acute urticaria, acute anaphylaxis
  • angioedema
  • motion sickness, nausea, vomiting
  • common cold and rhinorrhea!
54
Q

Name indications for second generation h1 receptor antagonists?

A

• Allergic conditions symptomatic treatment: allergic rhinitis, chronic urticaria, atopic dermatitis
Not effective against common colds like first gen because not anticholinergic!

55
Q

Name 5 second generation h1 antihistamines (non-sedative)

A
  • Cetirizine
  • loratadine
  • ebastine
  • fexofenadine
  • ketotifen (mast cell stabiliser)
56
Q

Indications ketotifen?

A

Adjunct to bronchodilator therapy in highly allergic children <3 who have atopic eczema or hay fever in addition to asthma

57
Q

Moa Chromones mast cell stabilisers?

A

Stabilise antigen-sensitised mast cells by reduce calcium influx and subsequent release of inflammatory mediators.

58
Q

Name 3 indications mast cell stabilisers (chromones)

A
  • Prophylactic anti-inflammatory to reduce bronchial hyperactivity ( not acute attacks)
  • allergic rhinitis spray
  • allergic conjunctivitis drops
59
Q

Name a phosphodiesterase 4 inhibitor for copd/asthma

A

Roflumilast

60
Q

Indication roflumilast?

A

Antiinflammatory adjunct only in severe COPD and asthma with frequent exacerbations (severe git side effects)

61
Q

When are immunosuppressants used in asthma?

A

Last resort

62
Q

Name 3 immunosuppressants that may be used as last resort in asthma or COPD

A
  • Methotrexate
  • cyclosporine
  • iv immunoglobulins
63
Q

Which monoclonal antibody may be considered for use in asthma?

A

Omalizumab.

Block IgE

64
Q

Name 3 indirect acting adrenergics causing release of ne from storage vesicles

A

• Amphetamine
• cocaine
• ephedrine
Used in cold and flu preparations.

65
Q

Name 3 direct acting adrenergics that are agonists on alpha 1 receptors

A 
.Pseudoephedrine (oral)
•Phenylpropanolamine (oral).
• phenylephrine (oral and topical )
• oxymetazoline (topical)
• naphazoline (topical)
• xylometazoline (topical)
66
Q

Name indications direct agonists postsynaptic alpha 1 receptors respiratory

A

• Systemic and topical nasal decongestants

67
Q

Name 3 antitussives

A 
Opium alkaloids (opioids)
• codeine
• pholcodeine
• dextromethorphan
• methadone
68
Q

Moa opium alkaloids as antitussives?

A
  • Opiate receptor agonists on mu receptors

* lower doses needed for pain relief, only suppress medullary cough centre brainstem.

69
Q

Name 3 adverse effects opioids as antitussives

A

• Constipation, git disturbances, dizzy
• inhibit mucociliary clearance, decrease bronchial secretions (thicken sputum)
• respiratory depression
. Confusion, sedation

70
Q

Name 3 mucolytics

A

• Carbocisteine
• acetylcysteine (acc)
. Bromhexine
Clear excess bronchial secretions.

71
Q

Moa mucolytics?

A

Cleave disulphide bonds cross-linking mucus glycoprotein molecules, loosening sputum and reducing viscosity and facilitate expectoration by coughing.

72
Q

Name 3 expectorants and what do they do?

A 
Increase volume mucus to decrease viscosity and enhance coughing, enhance ciliary movement. Can also be used as emetic because irritate gi mucous membrane
• guaifenesin
• ammonium chloride
• chloroform
• Menthol
73
Q

Name 5 drugs that may trigger asthma attack

A
  • Sympatholytics: beta blockers
  • parasympathomimetics: cholinergic agonists (ach, bethanechol)., anticoline esterase’s (neostigmine)
  • NSAIDs
  • hypersensitivity reactions: penicillins, tubocurarine, pancuronium morphine
  • irritants: tartrazine, carbamazepine, Iron dextran complex, preservatives

Pharmacology (34 decks)

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