Pharmacology

Question 1

What does stimulation of postganglionic cholinergic fibres cause? (2) (parasymp)

Answer 1

Bronchial smooth muscle contraction

Increased mucous secretion

Question 2

What does stimulation of postganglionic noncholinergic fibres cause? (parasymp)

Answer 2

Bronchial smooth muscle relaxation

Question 3

In the sympathetic division, what brings about bronchial smooth muscle relaxation via β2-adrenoceptors on ASM cells?

Answer 3

Activation by adrenaline from adrenal gland

Question 4

In the sympathetic division, what is the result of stimulated B2-adrenoreceptors? (3)

Answer 4

Bronchial smooth muscle relaxation
Decreased mucous secretion
Increased mucociliary clearance

Question 5

In the sympathetic division, what is the result of stimulated a1-adrenoreceptors?

Answer 5

Vascular smooth muscle contraction

Question 6

Effect of PKA on activity of MLC

Answer 6

Phosphorylates and inhibits MLCK
Phosphorylates and stimulates myosin phosphatase
–>Dephosphorylates MLC
–>Causes relaxation of bronchial smooth muscle

Question 7

Asthma

Answer 7

A recurrent and reversible obstruction to the airways in response to stimuli that are not necessarily noxious

Question 8

Causes of asthma attacks (4)

Answer 8

Allergens (in atopic individuals)
Exercise (cold, dry air)
Respiratory Infections (e.g.viral)
Smoke, dust, environmental pollutants

Question 9

Intermittent attacks of bronchoconstriction can cause (4)

Answer 9

Tight chest
Wheezing
Cough
Difficult breathing

Question 10

Chronic Asthma

Answer 10

Involves pathological changes to the bronchioles that result from long-standing inflammation

Question 11

Pathological changes from chronic asthma (5)

Answer 11

Increased mass of smooth muscle (hypertrophy, hyperplasia)
Accumulation of interstitial fluid (oedema)
Increased secretion of mucus
Epithelial damage (exposing sensory nerve endings)
Sub-epithelial fibrosis

Question 12

FEV1

Answer 12

Forced expiratory volume in 1 second

Question 13

PEFR

Answer 13

Peak expiratory flow rate

Question 14

What is bronchial hyper-responsiveness in asthma?

Answer 14

Exposed sensory nerve endings leads to increased sensitivity of the airways to bronchoconstrictor influences (hyper-reactivity and hypersensitivity)

Question 15

Type I Hypersensitivity reaction

Answer 15

Immediate/ early phase
Bronchospasm and acute inflammation
Fall in FEV1

Question 16

Type IV Hypersensitivity reaction

Answer 16

Late phase
Bronchospasm and delayed inflammation
More prolonged and more severe fall in FEV1 than with type 1

Question 17

Low level TH1 response to allergen in non atopic individual

Answer 17

Phagocytosis by antigen presenting (dendritic) cell

Cell-mediated immune response involving IgG and macrophages

Question 18

Strong TH2 response to allergen in atopic individual

Answer 18

Phagocytosis by antigen presenting (dendritic) cell

Antibody-mediated immune response involving IgE

Question 19

Cysteinyl leukotriene (CysLTs) receptors

Answer 19

Derived from mast cells and infiltrating inflammatory cells

Cause smooth muscle contraction, mucus secretion and oedema

Question 20

Short acting B2-adrenoceptor agonists

SABAs

Answer 20

e.g. salbutamol
Are first line treatment for mild, intermittent, asthma
Are relievers taken as needed
Act rapidly to relax bronchial smooth muscle, increase mucous clearance and decrease mediator release from mast cells and monocytes

Question 21

Long-acting B2-adrenoceptor agonists

LABAs

Answer 21

e.g.salmeterol, formoterol
Used for treatment of nocturnal asthma
LABAs must always be co-administered with a glucocorticoid.

Question 22

Relievers in treatment of asthma

Answer 22

Act as bronchodilators
Relief of acute bronchal spasms
SABAs and LABAs
CysLT1 receptor antagonists

Question 23

Preventors/ Controllers in treatment of asthma

Answer 23

Act as anti-inflammatory agents that reduce airway inflammation
Reduce frequency and severity of asthma attack
Glucocorticoids
Cromoglicate
Humanises monoclonal IgE antibodies

Question 24

CysLT1 receptor antagonists

Answer 24

e.g. montelukast, zafirlukast
Relax bronchial smooth muscle in response to cysLTs,
Effective as add on therapy against early and late bronchospasm in mild persistent asthma
Effective in combination with other medications, including inhaled corticosteriods in more severe conditions

Question 25

Methylxanthines

Answer 25

e.g. theophylline and aminophylline Inhibit mediator release from mast cells, increase mucus clearance Increase diaphragmatic contractility and reduce fatigue Are second line drugs used in combination with B2-adrenoceptor agonists and glucocorticoids Have a very narrow therapeutic window

Question 26

Glucocorticoids

Answer 26

``` E.g.hydrocortisone/cortisol Decreases Inflammatory responses Decreases Immunological responses Increase translation of anti-inflammatory genes Used in prevention of asthma attacks ```

Question 27

Chromones

Answer 27

Second line drugs used preventatively in treatment of allergic asthma Decrease sensitivity of irritant receptors and stabilise mast cells

Question 28

Short acting muscarinic antagonists used for treatment of COPD

Answer 28

Ipatropium

Question 29

Long acting muscarinic antagonists used for treatment of COPD

Answer 29

Tiotropium Glycopyrronium Aclidinium Umeclidinium

Question 30

Which part of muscarinic receptor antagonists' chemical structure reduces absorption and systemic exposure?

Answer 30

Quaternary ammonium group

Question 31

M1 muscarinic receptors

Answer 31

Increase frequency of action potential resulting from nicotinic receptor stimulation

Question 32

M2 muscarinic receptors

Answer 32

Reduce release of ACh

Question 33

M3 muscarinic receptors

Answer 33

Mediate contraction to ACh

Question 34

What muscarinic antagonist is the most useful in treatment of COPD

Answer 34

M3 muscarinic receptor antagonist

Question 35

What is the drawback of using ipatropium? (SAMA)

Answer 35

Non-selective blocker of M1, M2 and M3 receptors

Question 36

How is functional selectivity of M3 receptors achieved?

Answer 36

Differences in rates of association and dissociation- Drugs act on M3 receptors longer than M1 and M2 receptors

Question 37

Short acting B2 adrenoreceptor agonists used in treatment of COPD

Answer 37

Salbutamol

Question 38

Long-acting B2 adrenoreceptor agonists used in treatment of COPD

Answer 38

Formoterol | Salmeterol

Question 39

Ultra-LABA's used in maintenance treatment for COPD

Answer 39

Indacaterol | Olodaterol

Question 40

Rofumilast

Answer 40

Selective PDE4 inhibitor | Suppresses inflammation and emphysema in COPD

Question 41

Drawbacks of rofumilast

Answer 41

Adverse gastrointestinal effects

Question 42

Benefits/ limitations of administering glucocorticoids in combination with LABAs in COPD

Answer 42

Of benefit in patients who develop frequent and severe exacerbations when given with a LABA Do not in themselves suppress inflammation

Question 43

Reason for glucocorticoid unresponsiveness in COPD patients

Answer 43

Oxidative/nitrative stress | Reduced HDAC2

Question 44

Drugs used in triple inhalers as one daily treatment for COPD

Answer 44

Fluticasone Umeclidinum Vilanterol

Question 45

Rhinitis

Answer 45

Inflammation of the nasal mucosa

Question 46

Symptoms of rhinitis

Answer 46

Rhinorrhoea Sneezing Itching Nasal congestion and obstruction

Question 47

Types of rhinitis

Answer 47

Allergic Non-allergic Mixed

Question 48

Anti-inflammatory treatment of rhinitis

Answer 48

Glucocorticoids

Question 49

Mediator receptor blockade in treatment of rhinitis

Answer 49

CysLT1 receptor antagonist | H1 receptor antagonists

Question 50

Treatment to target nasal blood flow in rhinitis

Answer 50

Vasoconstrictors

Question 51

Anti-allergic treatment for rhinitis

Answer 51

Sodium cromoglicate

Question 52

Mechanism of glucocorticoids

Answer 52

Suppress recruitment of cytokines and mediators, eosinophils, basophils into nasal mucosa Reduce vascular permeability

Question 53

Examples of glucocorticoids

Answer 53

beclometasone fluticasone prednisolone

Question 54

Mechanism of anti-histamines

Answer 54

Antagonists that block effects of histamine

Question 55

Examples of second generation anti-histamines

Answer 55

Loratidine Fexofenadine Cetirizine

Question 56

Mechanism of anti-cholinergic drugs

Answer 56

Antagonists which block muscarinic receptors on nasal glands that stimulate watery secretions when activated by ACh

Question 57

Possible side effects of anti-cholinergic drugs

Answer 57

Dryness of nasal membrane

Question 58

Example of anti-cholinergic drug

Answer 58

Ipatropium

Question 59

Mechanism of sodium cromoglicate

Answer 59

Mast cell stabilization

Question 60

Mechanism of cysteinyl leukotriene receptor antagonists

Answer 60

Reduce effects of CysLTs upon nasal mucosa

Question 61

Example of CysTL receptor antagonist

Answer 61

Montelukast

Question 62

Mechanism of vasoconstrictor

Answer 62

Mimic effects of noradrenaline | Act on a1-adrenoreceptors to decrease swelling in vascular mucosa

Question 63

Example of vasconstrictor

Answer 63

Oxymetazoline

Question 64

Classifications of allergic rhinitis

Answer 64

Seasonal allergic rhinitis (SAR) Perennial allergic rhinitis (PAR) Episodic allergic rhinitis (EAR)

Question 65

Classifications of non-allergic rhinitis

Answer 65

``` Infectious rhinitis Hormonal rhinitis Vasomotor rhinitis Nonallergic rhinitis with eosinophila syndrome (NARES) Drug induced rhinitis ```

Question 66

Types of rhinitis in which glucocorticoids are used

Answer 66

SAR PAR NARES Vasomotor rhinitis

Question 67

Types of rhinitis in which anti-histamines are used

Answer 67

SAR PAR EAR

Question 68

Types of rhinitis in which anti-cholinergic drugs are used

Answer 68

Reduce rhinorrhoea in SAR and PAR

Question 69

Types of rhinitis in which CysTL receptor antagonists are used

Answer 69

SAR | PAR