Asthma I

Question 1

Ashtmatics have activated?

Answer 1

T-cells

Question 2

what is used in Asthma tx?

Answer 2

1) Bronchodilators
2) Anti-inflammatory drugs

Question 3

Main Bronchodilators used in the tx of Asthma

Answer 3

β2-ADRENOCEPTOR AGONISTS
1) SABA –> salbutamol (albuterol), metaproterenol, terbutaline
2) LABA –> salmeterol and formoterol

Question 4

MoA of β2 -ADRENOCEPTOR AGONISTS
β2- adrenoceptor stimulation –> smooth muscle relax –> ——– -> inhibit mediator release from mast cells –> ———– from monocytes –> Increase —- by action on cilia

Answer 4

β2- adrenoceptor stimulation –> smooth muscle relax –> bronchodilation –> Bronchodilation Inhibit mediator release from mast cells. Inhibit TNF-α release from monocytes
–> Increase mucus clearance by action on cilia

Question 5

Administration of Salbutamol (Albuterol), Salmeterol and Formoterol

Answer 5

• Given by inhalation (Aerosol, Powder, Nebulizer)
• Also orally and IV

Question 6

3 Short-acting adrenergic β2 agonists (SABA) drugs used for symptomatic releif of Asthma

Answer 6

salbutamol (albuterol), metaproterenol, terbutaline
(Duration of action is 3–5 h)

Question 7

duration of action of LABA

Answer 7

8-12 hrs

Question 8

duration of action of SABA

Answer 8

3-5 hrs

Question 9

2 Longer-acting adrenergic
β2 agonists (LABA) drugs used in the tx of Asthma

Answer 9

salmeterol and formoterol
(Duration of action is 8–12 h)

Question 10

Clinical uses of Albuterol

Answer 10

Short-acting used for Acute symptoms of Asthma
(Wheezing, chest pain, coughing, dizinessn fainting)

Question 11

Clinical uses of Salmeterol and Formoterol

Answer 11

Long-acting, used to contorl Acute symptoms of Asthma

Question 12

AE of Salbutemol, Salmeterol and Formoterol

Answer 12

1) Tremor (most common)
2) Arrythmias
3) Anxiety
4) headache
5) Tachycardia
6) high doses - lactic acidosis and Hypokalaemia

Question 13

Contraindications of β2 -ADRENOCEPTOR AGONISTS

Answer 13

CV disease
- drugs cause Arrythmias and Tachycardia

Question 14

Asthma drugs that block leukotriene receptors (CysLT1)

Answer 14

Montelukast and zafirlukast

* not as effective as β2-ADRENOCEPTOR AGONISTS

Question 15

MoA of Montelukast and zafirlukast

Answer 15

Antileukotrines –> block leukotriene receptors (CysLT1)

Question 16

CU of Montelukast and zafirlukast

Answer 16

1) Exercise-induced asthma
2) Adjunct to tx
3) Alternative to tx w/ ICS (inhaled corticosteroids) for Chronic asthma

Question 17

MoA of Cysteneil (CysTL 1/2) Leukotrienes and their receptors

Answer 17

1) Potent spasmogens of bronchial muscle
2) Increase mucus secretion
3) May contribute to bronchial hyperactivity

Question 18

Do Montelukast ,zafirlukast and Zileuton provide symptomatic relief in Asthma patients?

Answer 18

NO

Question 19

AntiLeukotriene drugs

Answer 19

1) Montelukast, zafirlukast
2) Zileuton

(Oral drugs)

Question 20

MoA of Zileuton

Answer 20

5-LOX inhibitor –> decreases the conversion of Arachidonic acid to leukotrienes

Question 21

AE of Antileukorienes

* Montelukast , zafirlukast, Zileuton

Answer 21

1) Hepatotoxicity (esp Zileuton)
2) headache
3) GI disturbances
4) increased risk of respiatory tract infection

 **SOS: Neuropsychotic events**

Question 22

Clinical uses of Zileuton

Answer 22

Adjunctive to steroids in the tx of Asthma

Question 23

Mthyelxanthines used in the tx of Asthma

Answer 23

Theophylline-oral (also used as aminophylline- IV)

Question 24

MoA of Theophylline

Answer 24

Methylxanthine –> bronchodilation by inhibiting PDE IV
* It also has anti-inflammatory actions

Question 25

Clinical uses of Theophylline

Answer 25

1) w/ steroids, in patients whose asthma does not respond adequantly to β2-receptor agonists. 2) in addition to steroids in COPD 3) IV theophylline+ ehtylenendiamine (to increase H2O solubility) in acute severe asthma

Question 26

AE of Theophylline

Answer 26

1) Nausea, diarrhea 2) Insomnia, nervousness 3) **Serious dysrhythmias** (cardiotoxicity), which can be fatal 4) **Seizures** (neurotoxicity), which can be fatal

Question 27

what hepatic enzyme meatbolizes Theophylline

Answer 27

**CYP450**, Therfore limited use due to narrowe theraputic index (causes neuro-/cardio-toxicity)

Question 28

Glucocorticoids used in the tx of Acute severe Asthma

Answer 28

Beclometasone, **budesonide**, **fluticasone**, mometasone, ciclesonide, flunisolide

Question 29

What drugs are used to **prevent the progression of Chronic Asthma**, and is **effective in acute sever asthma**?

Answer 29

**budesonide, fluticasone** (Glucocorticoids)

Question 30

Administration of **budesonide, fluticasone**

Answer 30

inhalation with a metered-dose or dry powder inhaler

Question 31

1st line therapy for chronic asthma?

Answer 31

**budesonide, fluticasone** **Main anti-inflammatory drugs in asthma for all ages**

Question 32

MoA of Glucocorticoids

Answer 32

**Anti-inflammatories** --> inhibit the synthesis of virtually all Cytokines and inflammatory agents

Question 33

AE of Glucorticoids such as budesonide and fluticasone, used for chronic asthma therapy

Answer 33

1) **Oral thrush** --> Oropharyngeal candidiasis 2) Sore throat and croaky voice

Question 34

How can oral thrush be prevented when using inhaled Glucocorticoids

Answer 34

1) "Spacing" devices 2) Rinse mouth after use

Question 35

Treatment approach for sever acute asthma

Answer 35

**O2, Nebulised salbutamol, IV hydrocortisone followed by a course of oral prednisolone** * Additional measures: Nebulised ipratropium, IV salbutamol, IV aminophylline, Abx (if bacterial infection is present) | * medical emergency

Question 36

Biological therapy in Asthma

Answer 36

**Omalizumab** - Tezelelumab - Benralizumab - Dupilumab | - umab

Question 37

# ** MoA of Omalizumab?

Answer 37

Anti-inflammatory biological therapy **Anti-IgE**