Respiratory Pharmacology 2

Question 1

State examples of inhaled corticosteroids?

Answer 1

Beclometasone 
Budesonide 
Ciclesonide 
Fluticasone propionate 
Fluticasone furoate 
Mometasone furoate

Question 2

Adverse effects of corticosteroids?

Answer 2

SO MANY.
Sleep disturbance, psychosis, acne, oedema, intracranial hypertension, Diabetes mellitus, osteoporosis, cataracts, growth retardation

Question 3

Difference between Cushing’s disease and Cushing’s syndrome?

Answer 3

Cushings disease: caused by a tumour on pituitary gland, PG produces too much ACTH. ACTH responsible for cortisol production.

Cushing’s syndrome: due to causes outside body increasing levels of cortisol
- e.g. taking corticosteroids

Question 4

How do long acting beta 2 agonists work for longer?

Answer 4

• Long tail and lipid soluble benzene ring.
• Tail end in lipid membrane
• anchored in membrane
• hence hangs around receptor for longer.

Question 5

Describe the BTS guidelines towards giving LABA?

Answer 5

LABA 1st choice add-on therapy to inhaled corticosteroids.

Considered before increasing dose of inhaled corticosteroids.

Question 6

Why should LABAs be given only as an add-on?

Answer 6

• Chronic exposure to LABAs can be associated with tolerance
• and reduced sensitivity to bronchodilator effects of salbutamol.
• More people die on LABA monotherapy than as add on therapy.

Question 7

Describe the relatively new medication Vilanterol and its perks?

Answer 7

Main difference is that other LABAs have to be taken twice a day. However vilanterol can be taken once a day, may improve patient adherence to medication

Question 8

Fostair inhaler

Answer 8

Combination of beclomethasone diproprionate and formoterol fumarate

Question 9

Duoresp

Symbicort

Answer 9

Budesonide and formoterol fumarate

Question 10

Relvar

Answer 10

Fluticasone furoate and vilanterol

Question 11

AirFluSal

Seretide

Answer 11

Fluticasone propionate
Salmeterol

• Most people are on Seretide

Question 12

Examples of leukotriene receptor antagonists

Answer 12

Montelukaust
- v.tasty tablet
Zafirlukast

Pranlukast (not licensed in UK)

Question 13

Arachidonic acid

Answer 13

Major constituent of cell membrane phospholipids.

Question 14

Leukotrienes

Answer 14

Potent bronchial smooth muscle constrictors.

- Leukotrienes C4 & D4 approx. 1000x more potent than histamine.

Question 15

Formation of leukotrienes through which pathway depends on the lipoxygenation of arachidonic acid?

Answer 15

5-lipoxygenase pathway

Question 16

Describe some side effects of taking Montelukast neuropsychiatric ADRs

Answer 16

Sleep disturbances, depression and agitation.

Disturbances of attention or memory.

Hallucinations

Suicidal behaviour

Question 17

What is the difference between aminophylline and theophylline?

Answer 17

Aminophylline: drug combo of theophylline and ethylenediamine in a 2:1 ratio.

Question 18

Aminophylline may be administrated via

Answer 18

ONLY GIVEN AS IV.

Question 19

Theophylline may be administered

Answer 19

Orally.

Used in oral version,

Question 20

Describe jist of the action of theophylline

Answer 20

Relaxes smooth muscle of bronchial airways, pulmonary BV and reduces airway responsiveness to histamine, methacholine, adenosine and allergen.

Question 21

Describe mechanism of action of theophylline?

Answer 21

Competitively inhibits type III and type IV phosphodiesterase.
- enzyme responsible for breaking down cAMP in smooth muscle cells

Also binds to the adenosine A2B receptor and blocks adenosine mediated bronchochonstriction.

Question 22

Describe action of theophylline in inflammatory states?

Answer 22

• Activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription.

Question 23

Describe the toxicity of theophylline?

Answer 23

Very toxic.

Requires therapeutic drug monitoring to ensure high levels are avoided.

Question 24

Theophylline overdose can cause…

Answer 24

Vomiting, agitation, restlessness, dilated pupils, sinus tachycardia, and hyperglycaemia

More serious:

• haematemesis
• convulsions
• supraventricular and ventricular arrhythmia’s

Question 25

What are some biologic therapies?

Answer 25

Omalizumab

• anti-IgE monoclonal antibody
• subcutaneous inj every two or four weeks, depending on IgE level and weight,

Mepolizumab, Reslizumab and benralizumab
- Anti-IL-5 monoclonal antibody

Question 26

Describe when omalizumab may be given?

Answer 26

Via subcutaneous injection

• for patients with convincing IgE mediated asthma.
• may take 12-16 weeks to show effectiveness

Question 27

What are complementary determining regions CDRs?

Answer 27

Part of variable chains in immunoglobulins and T cell receptors.

Question 28

How does Omalizumab work?

Answer 28

1. Humanized mAb against IgE
2. Binds circulating IgE regardless of specificity
3. Forms small, biologically inert Omalizumab: IgE complexes
4. Does not activate complement

Question 29

Omalizumab works by

Answer 29

1. Binding to free IgE
2. Decreases cell bound IgE
3. Decreases expression of high affinity receptors
4. Decreases mediator release
5. Decreases allergic inflammation
6. Prevents exacerbation of asthma and reduces symptoms.

Question 30

How does mepolizumab work?

Answer 30

Meopolizumab binds with high affinity to IL-5, thus preventing its interaction with the IL-5 receptor expressed by eosinophils and to a lesser extent basophils.