Pharmacology > Asthma > Flashcards

Asthma Flashcards

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1
Q 
Pathogenesis of asthma
Inflammatory cells
Structural cells
Mediators
Effects
A 
Inflammatory cells
- mast cells
- eosinophils
- Th2 cells
- basophils
- neutrophils
- platelets
Structural cells
- epithelial cells
- smooth mm cells
- endothelial cells
- fibroblasts
- nerves

Mediators

  • histamines
  • leukotrienes
  • prostanoids
  • PAF
  • kinins
  • adenosine
  • endothelins
  • nitric oxide
  • cytokines
  • chemokines
  • growth factors

Effects

  • bronchospasm
  • plasma exudation
  • mucus secretion
  • AHR
  • structural changes
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2
Q

Guideline goals for successful asthma management

A 
Current control 
- control of symptoms
- maintain normal activity levels
- maintain pulmonary function
Future risk
- avoid adverse treatment effects
- prevent asthma exacerbation
- prevent asthma mortality
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3
Q

M3 receptor under stimulation by the agonist Ach mimics what effect?

A

Bronchoconstriction
Increased bronchial gland secretions
Increased mediator release

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4
Q

Beta 2 receptor under stimulation by the agonist NA mimics what effect?

A

Bronchodilatation
Mast cell stabilization
Increased mucocilliary clearance
Decreased microvascular permeability

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5
Q

Alpha 1, Alpha 2 receptor under stimulation by the agonist NA mimics what effect?

A

Bronchoconstriction

Decreased gland secretions

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6
Q

H1 receptor under stimulation by the agonist histamine mimics what effect?

A

Bronchoconstriction

Inflammatory reaction

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7
Q

5-HT3 receptor under stimulation by the agonist serotonin mimics what effect?

A

Bronchoconstriction

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8
Q

Beta 2 receptor under stimulation by the agonist bradykinin mimics what effect?

A

Bronchoconstriction

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9
Q

Pharmaceutical options for asthma treatment

A 
Corticosteroids
Leukotriene antagonists
Mast cell stabilizers
Anticholinergic drugs
Theophylline
Selective beta 2 adrenergic agonists
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10
Q

Which drug class of asthma pharmacotherapy results in reduced bronchial hyper-reactivity?

A

Mast cell stabilizers

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11
Q 
Which drug class of asthma pharmacotherapy results in 
decreased response to allergens?
A

Leukotriene antagonists

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12
Q

Which drug class of asthma pharmacotherapy results aids in prevention of progression of chronic asthma, rescue course in rapidly deteriorating conditions and IV for acute exacerbations?

A

Corticosteroids

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13
Q

Which drug class of asthma pharmacotherapy results in relief of acute exacerbation and control/prevention of chronic asthma?

A

Anticholinergic drugs
Theophylline
Selective beta 2 adrenergic agonists

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14
Q

Definition of severe asthma

A

Asthma that requires treatment w/ high dose inhaled corticosteroids + a second controller and/or systemic corticosteroids to prevent it from becoming uncontrolled or that remains uncontrolled despite this therapy

To qualify:
Asthma diagnosis should be confirmed
Comorbidities should be address

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15
Q

Definition of uncontrolled asthma

A

At least 1 of the following

  • poor symptom control (ACQ consistently >1.5, ACT<20)
  • frequent severe exacerbations (>2 burts of systemic corticosteroids in the prev year)
  • serious exacerbations (> hospitalization or ICU stay in prev year)
  • airflow limitation (FEV1 <80% predicted after withholding bronchodilators
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16
Q

What should you check for in uncontrolled asthma before changing the treatment?

A 
Incorrect diagnosis
Significant comorbidities
Poor compliance
Poor inhaler technique
Environmental factors (allergen exposure, occupation, smoking)
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17
Q

Management of refractory asthma

A

Life-threatening
Most commonly precipitated by URTIs

Hydrocortisone 100 – 200 mg 4 – 8hourly infusion
Nebulised salbutamol 2.5 – 5mg with ipratropium bromide 0.5 mg driven by O2
High flow humidified O2
Intubation & mechanical ventilation prn
Antibiotic treatment of respiratory tract infection
Correct dehydrationand acidosis
Saline + sodium bicarbonate infusion

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18
Q

Inhaled + local corticosteroid options

A

Beclometasone (Beclate)
Budesonide (Pulmicort)
Ciclesonide (Alvesco)
Fluticasone (Flixotide)

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19
Q

Systemic (oral/IV) corticosteroid options

A 
Prednisone (Meticorten)
Methylprednisolone (Medrol)
Betamethasone (Celestone)
Dexamethasone (Decasone)
Hydrocortisone (Solucortef)
Triamcinolone (Kenalog)
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20
Q

Indication for corticosteroid use in asthma treatment?

A

Most effective controller therapy available for asthma

ICS not systemic (severe S/E)

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21
Q

Mechanism of action of corticosteroids in asthma treatment

A
  1. Decrease formation of cytokines (esp Th2), eosinophils, macrophages and T lymphocytes - Th2 recruit and activate eosinophils and are responsible for promoting the production of IgE and the expression of IgE receptors)
  2. Reversing mucosal oedema
  3. Inhibit the generation of PGE2 and PGI2 by inhibiting induction of COX-2
  4. Decreases down-regulation of B-receptors
  5. Decrease permeability of capillaries
  6. Decrease release of leukotrienes and histamine which cause bronchoconstriction
  7. Decrease hyperresponsiveness of airway smooth muscle to
    sensitive stimuli such as cold, irritants, allergens etc
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22
Q

What is the pathophysiology of cysteinyl leukotrienes in asthma?

A 
Constriction of bronchiolar smooth muscle
Airway hyperresponsiveness
Plasma exudation
Eosinophilic inflammation
Increased endothelial permeability
Promotion of mucous secretion
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23
Q

Mechanism of action of anti-leukotrienes in asthma treatment?

A

Selective reversible inhibitors of cysteinyl
leukotrine-1 receptor, thus blocking the effects of cysteinyl leukotrines (LTC4, LTD4, LTE4) (Montelukast, Zafirlukast)
Inhibitor of 5-lipoxygenase pathway (Zileuton)

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24
Q

Anti-leukotriene options for asthma treatment?

A

Montelukast (Singulair)
Zafirlukast (Accolate)
Zileuton (not available in SA)

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25
Pharmacokinetics of anti-leukotrienes in asthma treatment?
Good oral absorption 90% plasma protein bound Undergo biliary excretion Pharmacological response within 24hrs
26
What are adverse effects of anti-leukotrienes?
``` Abdominal pain Headache Rash Anaphylaxis Eosinophilia, vasculitis (Churg Strauss Syndrome) Liver dysfunction (rare) ```
27
Drug interactions of anti-leukotriene options?
Zafirlukast extensively metabolized by liver (inhibitor of CYP3A4 and CYP2C9) Enhances anticoagulant effect of warfarin Erythromycin + terfenadine combination reduces zafirlukast levels Theophylline reduces zafirlukast levels
28
Name options in the short acting beta 2 agonist drug class
``` Salbutamol (Ventolin) Fenoterol (Berotec) Terbutaline (Bricanyl) Hexoprenaline (Ipradol) Orsiprenaline /Metaproterenol ```
29
Name options in the long acting beta 2 agonist drug class
Salmeterol (Serevent) Formoterol (Foradil) Indacaterol (Onbrez)
30
Adverse effects of beta 2 agonists?
``` Muscle tremors Palpitations Restlessness Nervousness Throat irritation Ankle oedema ```
31
Name anti-cholinergic options for asthma treatment and their half life
M3 receptor antagonists - Ipratropium bromide (t1/2 = 4 - 6 hours) - Tiotropium bromide (t1/2 = 24 hours) Slower response than beta 2 agonists
32
Adverse effects of anticholinergics
``` Mostly elderly affected Sedation Confusion Hallucination Mydriasis + blurred vision Sinus tachycardia Urinary retention Constipation Dry mouth Parotitis ```
33
Name methylxanthine options for asthma treatment
Theophylline Aminophylline Caffeine Oxtryphyline
34
Mechanism of action of methylxanthines?
Multiple mechanisms responsible, but most important respiratory effects due to inhibition of PDE (phosphodiesterase) which is responsible for intracellular metabolism of cAMP
35
Pharmacokinetics of methylxanthines
Variable t½ (3-12hrs) Good oral absorption Metabolized by liver (substrate for CYP1A2 and CYP3A4) NB – Very narrow therapeutic index (10 20mcg/ml) Therapeutic drug monitoring recommended
36
Adverse effects of methylxanthines
Adverse effects are related to plasma concentration (if >15mg/L) + may be reduced by gradually increasing the dose until therapeutic concentrations are achieved Most common side effects: headache, nausea, vomiting and increased acid secretion (due to inhibition of PDE4) CNS irritability tremor, nervousness, convulsions Tachycardia, arrhythmias (fatal) (due to inhibition of cardiac PDE3 Transient urinary frequency (due to inhibition of adenosine A1 receptors)
37
Name options of mast cell stabilizers?
Cromolyn (Vividrin) | Nedocromil
38
Mast cell stabilizers have no effect when?
If already bronchoconstricted
39
Mechanism of action of mast cell stabilizers
Block calcium channels essential for mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators -> without intracellular calcium, the histamine vesicles cannot fuse to the cell membrane and degranulate
40
Indications for mast cell stabilizers
Effective prophylactic anti-inflammatory agents - not for use in acute asthmatic attacks Useful in allergic rhinitis (nasal sprays) Allergic conjunctivitis (eye drops)
41
Pharmacokinetics of mast cell stabilizers
Efficacy only determined after 4-6 weeks | Short duration of action – tds, qid dosing
42
Another name for the drug class of mast cell stabilizers?
Cromones
43
Adverse effects of mast cell stabilizers?
``` Minimal adverse effects Mainly transient e.g - pharyngeal irritation - chest tightness - coughing + nasal congestion - mouth dryness ```
44
Immunomodulatory therapy in asthma treatment
Immunosupressive therapy could be considered when ALL other treatments are unsuccessful Anti-IgE receptor therapy (monoclonal antibodies) - consider omalizumab - blocks IgE binding to receptors
45
Immunomodulatory treatment is routine in the treatment of asthma True or false
False Less effective and more side effects than oral corticosteroids therefore NOT recommended for routine therapy
46
Give examples of medications that fall under the antitussive drug group
Cough suppressants (opium alkaloids) ``` Dextromethorphan Noscapine Pholcodine Codeine Dihydrocodeine Methadone ```
47
Mechanism of action of opium alkaloid cough suppressants
Suppress medullary cough centre in brain by acting on μ opioid receptors in lower doses than needed for pain relief
48
Side effects of of opium alkaloid cough suppressants
``` Decreases bronchial secretions (thickens sputum) Inhibits ciliary activity Constipation GI disturbances Dizziness Respiratory depression Confusion and sedation ```
49
Drug interactions with opium alkaloid cough suppressants
``` CNS depressants Potentially fatal - amiodarone - fluoxetine - MAOI ```
50
Give examples of medications that fall under the mucolytic drug group
Acetylcysteine (ACC) Carbocisteine (Mucospect) Bromhexine (Bisolvon) Sodium-2-mercapto-ethane sulphonate (Mesna/Mistabron)
51
Give examples of medications that fall under the expectorant drug group
``` Guaifenesin (Benylin) Tinct ipecacuanha Ammonium chloride Chloroform Sodium citrate Menthol ```
52
Definition of allergic rhinitis
A symptomatic disorder of the nose, induced after allergen exposure, by an IgE- mediated inflammation of the nasal membranes "Hay fever"
53
Clinical presentation of allergic rhinitis
``` Rhinorrhoea, Nasal congestion/blockage Nasal itching Sneezing Postnasal drip ```
54
Least effective drugs for alleviating nasal itching in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Intranasal decongestants Anticholinergics LTRA
55
Most effective drugs for alleviating nasal itching in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Antihistamines
56
Least effective drugs for alleviating sneezing in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Intranasal decongestants Anticholinergics LTRA
57
Most effective drugs for alleviating sneezing in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Antihistamines
58
Least effective drugs for alleviating rhinorrhoea in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Intranasal decongestants
59
Most effective drugs for alleviating rhinorrhoea in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Intranasal corticosteroids Antihistamines (but anticholinergics only work for rhinorrhoea symptoms)
60
Least effective drugs for alleviating nasal obstruction in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Intranasal decongestants
61
Most effective drugs for alleviating nasal obstruction in allergic rhinitis? ``` Intranasal corticosteroids Antihistamines Intranasal cromones Intranasal decongestants Anticholinergics LTRA ```
Anticholinergics
62
Nasal irrigation in the treatment of allergic rhinitis
Nasal irrigation is a simple and inexpensive non- pharmacological form of therapy for AR that has been shown to improve symptoms and QOL scores and reduce medication requirements
63
Give examples of direct acting agonists in the treatment of allergic rhinitis
``` Oral (tablets, syrups) - pseudoephedrine - phenylephrine - phenylpropanolamine Topical (nasal spray, drops) - oxymetazoline - naphazoline - xylometazoline - phenylephrine ```
64
Mechanism of action of direct acting agonists in the treatment of allergic rhinitis
Direct agonists on postsynaptic alpha 1 receptors -> constricts dilated arterioles in nasal mucosa and reduce airway resistance
65
Indications for the use of direct acting agonists in the treatment of allergic rhinitis
``` Systemic and topical nasal decongestants Only direct acting agents used - indirect agents are illicit in cold/flu preparations Usually in combination with antihistamines ```
66
Contraindications to use of direct acting agonists in the treatment of allergic rhinitis
Severe hypertension | MAOI
67
Precautions in the use of direct acting agonists in the treatment of allergic rhinitis
``` Rhinitis medicamentosa (>7 days use) Cardiovascular disease Hyperthyroidism Diabetes Prostatic hypertrophy Renal impairment Hepatic impairment ```
68
Adverse effects of the use of direct acting agonists in the treatment of allergic rhinitis
``` CNS stimulation (anxiety, restlessness, tremors, headache) Reduced appetitie N+V Hypertension Cerebral haemorrhage Pulmonary oedema ```
69
Give examples of 1st generation antihistamines used in the treatment of allergic rhinitis
``` Promethazine (Phenergan) Chlorpheniramine (Allergex) Cyclizine (Valoid) Cyproheptadine (Periactin) Hydroxizine (Aterax) Diphenhydramine (DPH) ```
70
Indications for use of of 1st generation antihistamines used in the treatment of allergic rhinitis
``` Allergic conditions Urticaria Angioedema Acute anaphylaxis Motion sickness Nausea Vomiting Common cold Rhinorrhoea ```
71
Pharmacokinetics of 1st generation antihistamines used in the treatment of allergic rhinitis
Non selective Crosses BBB Good absorption + metabolised by liver t1/2 between 2-8hrs
72
Adverse effects of 1st generation antihistamines used in the treatment of allergic rhinitis
Sedation Hallucinations Seizure precipitation (epileptics) Anticholinergic effects (useful in drying up secretions during cold/flu)
73
Drug interactions with 1st generation antihistamines used in the treatment of allergic rhinitis
Potentiates effects of CNS depressants Potentiates effects of anticholinergic agents Antidepressants
74
Give examples of 2nd generation antihistamines used in the treatment of allergic rhinitis
``` Cetirizine (Zyrtec) Desloratadine (Deselex) Levocetirizine (Xyzal) Loratadine (Clarityne) Ebastine (Kestine) Fexofenadine (Telfast) Mizolastine (Mizollen) Ketotifen (Zaditen) ```
75
Indications for use of of 2nd generation antihistamines used in the treatment of allergic rhinitis
Non sedative Symptomatic treatment for allergic conditions Not very effective in common colds due to lack of anticholinergic effects
76
Pharmacokinetics of 2nd generation antihistamines used in the treatment of allergic rhinitis
Selective for H1 receptors t½ 10h (thus daily dosing ) Minimal BBB penetration Minimal metabolism - excreted unchanged by kidney
77
Adverse effects of 2nd generation antihistamines used in the treatment of allergic rhinitis
``` Sedation (uncommon) Headache Dizziness GI disturbances Hypersensitivity reactions Potential for cardiac arrhythmias (QT prolongation) ```
78
Drug interactions with 2nd generation antihistamines used in the treatment of allergic rhinitis
``` CNS depressants Drugs with arrhythmogenic potential - ketoconazole - erythromycin - protease inhibitors - quinine ```
79
Mechanism of action of ketotifen as a mast cell stabilizer in the treatment of allergic rhinitis
2nd generation antihistamine with mast cell stabilizing effects - Histamine antagonist - Functional leukotriene antagonist - Phosphodiesterase inhibitor
80
Indications for us of ketotifen as a mast cell stabilizer in the treatment of allergic rhinitis
Useful adjunct to bronchodilator therapy in highly allergic children <3 years who have atopic eczema or hay-fever in addition to asthma
81
Drug interactions with of ketotifen as a mast cell stabilizer in the treatment of allergic rhinitis
``` Oral antidiabetic preparations enhances the risk of reversible thrombocytopenia. Potentiates the effect of - sedatives - hypnotics - antihistamines - alcohol ```
82
Adverse reactions with use of ketotifen as a mast cell stabilizer in the treatment of allergic rhinitis
``` Somnolence (reversible) Zerostomia (reversible) Mild dizziness (reversible) Fatigue (reversible) Weight gain Increased appetite Hypersensitivity in immunocompromized patients ```
83
Management of anaphylaxis
Severe systemic IgE mediated hypersensitivity reaction Drug of choice = adrenaline Other options - glucocorticoids - antihistamines - supportive therapy (positioning, inotropes, vasopressors)
Pharmacology
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