Drugs acting on Respiratory system. Explain the various Respiratory disorders such as Asthma and COPD.

1. SUBMITTED BY
ARATHY.V.A
1st Yr M PHARM
PHARMACOLOGY
1
BRONCHODIALATORS
Presented By
Mr. Jithin Mathew, M.Pharm.,
Assistant Professor
Department of Pharmacology

2. CHRONIC OBSTRUCTIVE PULMONARY
DISEASE
2

3.  Is a chronic condition of the airways characterized by
airflow obstruction that is progressive and not fully
reversible.
3

4. 4

5. The most important processes
causing lung damage are
 Oxidative stress produced by the high concentrations
of free radicals in tobacco smoke
 Cytokine release due to inflammation as the body
responds to irritant particles such as tobacco smoke in
the airway
 Tobacco smoke and free radicals impair the activity of
antiprotease enzymes such as alpha 1-antitrypsin,
allowing protease enzymes to damage the lung
5

6.  Two major forms
• Chronic bronchitis
• Emphysema
6

7. CHRONIC BRONCHITIS
 Lung damage &Inflammation in the airway results in
chronic bronchitis.
 Chronic bronchitis is a common condition defined
clinically as “persistent cough with expectoration on most
days at least three month of the year for two or more
consecutive years”.
 Cough is caused by over secretion of mucous.
7

8.  The excess mucus blocks the airway causing a build up
of carbon dioxide in the blood and a decrease in
oxygen which leads to respiratory acidosis
 Patients with advanced COPD that have primarily
chronic bronchitis rather than emphysema were
commonly referred to as ‘BLUE BOATERS’.
8

9.  The hypoxia and fluid retention leads to them being
called ‘blue boaters
9

10. EMPHYSEMA
 A combination of permanent dilation of air spaces distal to
the terminal bronchioles and destruction of the walls of the
dilated air spaces.
10

11.  The destruction of the air space walls reduce the
surface area available for the exchange of oxygen and
co2 during breathing
 The patients suffering emphysema “pink puffers”
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12. 12

13. SPIROMETRY
 The diagnosis of COPD is confirmed by spirometry
 Spirometry can help to determine the severity of
COPD.
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14. Severity of COPD (GOLD scale) FEV1 % predicted
Mild (GOLD 1) ≥80
Moderate (GOLD 2) 50–79
Severe (GOLD 3) 30–49
Very severe (GOLD 4) <30 or chronic respiratory failure
symptoms
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15.  A chest X-ray demonstrating severe COPD..
 Electrocardiogram
 Sputum analysis
 Blood tests
 Blood oxygen level
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16. 16

17. Bronchodilators
 Bronchodilators are medicines that relax smooth
muscle around the airways, increasing the caliber of
the airways and improving air flow.
 They can reduce the symptoms of shortness of breath,
wheeze and exercise limitation, resulting in an
improved quality of life for people with COPD
17

18.  Bronchodilators are usually administered with
an inhaler or via a nebulizer
2 types
Short acting bronchodilators
Long acting bronchodilatrors
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19. Short acting bronchodilators
 β2 agonists
 β2 agonists stimulate β2 receptors on airway smooth
muscles, causing them to relax.
 β2 agonists - Salbutamol and terbutaline
 Anticholinergic
 Ipratropium bromide-inhibit the vagal mediated
response by reversing the action of acetyl choline,
producing smooth muscle relaxation
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20.  Long acting bronchodilators
 Long acting β2 agonists such
as salmeterol and formoterol are used as
maintenance therapy and lead to improved
airflow, exercise capacity, and quality of life.
20

21. Anticholinergics
 Anticholinergic drugs cause airway smooth muscles to
relax by blocking stimulation from cholinergic nerves
 Eg-tiotropium
21

22. Corticosteroids
 Corticosteroids (steroids)
 are the primary medication given to reduce the
inflammation
 These are used in tablet or inhaled form to treat and
prevent acute exacerbations of COPD.
 prednisone
22

23.  Expectorants
 Acetyl cysteine , which is administered by nebulizer
five minutes after the patient receives a
bronchodilator.
 Ammonium chloride ,Sodium citrate–in various cough
mixtures
 Guaifenesin , Guaiacol-orally(100-200mg BD/TDS)
23

24. • Methylxanthines, which generally are used for severe
cases of COPD.
• They may have serious side effects, so they are not usually
recommended.
 Other medication
 Antibiotics specifically macrolides such
as azithromycin
24

25. Surgery
 Surgery is an option for some people with some
forms of severe emphysema who aren't helped
sufficiently by medications alone:
 Lung volume reduction surgery. In this
surgery,removes small wedges of damaged lung
tissue.
 This creates extra space in chest cavity so that the
remaining lung tissue and the diaphragm work
more efficiently.
25

26.  Lung transplantation
 Transplantation can improve ability to breath and
to be active
 But it's a major operation that has significant
risks, such as organ rejection, and it obligates to
take lifelong immune-suppressing medications.
26

27. Oxygen Therapy
Long-term oxygen therapy (>15 h per day) is introduced
in very severe hypoxemic COPD and improves survival,
exercise, sleep and cognitive performance.
Oxygen therapy is also temporarily used for hospital
treatment of hypoxemic COPD exacerbations.
In addition to improving oxygenation, oxygen
therapy is thought to be effective because it reduces
pulmonary hypertension by opposing hypoxic
pulmonary vasoconstriction.
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28. BRONCHIAL ASTHMA
28

29.  Asthma is a common chronic inflammatory disease of
the airways characterized by variable and recurring
symptoms, reversible airflow obstruction,
and bronchospasm.
 Common symptoms include wheezing, coughing,
chest tightness, and shortness of breath
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30.  Acute severe asthma, previously known as status
asthmaticus, is an acute exacerbation of asthma that
does not respond to standard treatments of
bronchodilators and corticosteroids.
 Half of cases are due to infections with others caused
by allergen, air pollution, or insufficient or
inappropriate medication use.
30

31.  Brittle asthma is a kind of asthma distinguishable by
recurrent, severe attacks.
 Type 1 brittle asthma is a disease with wide peak flow
variability, despite intense medication.
 Type 2 brittle asthma is background well-controlled
asthma with sudden severe exacerbations.
31

32. 32

33. 33

34. CLASSIFICATION
 BRONCHODILATORS
 Selective β2 agonists
Salbutamol,terbutaline,
salmetrol,formeterol,
bambuterol
 Nonselective
sympathomimetics
epinephrine,ephedrine,
isoprenaline
 Anticholinergics
iprtropium
bromide,tiotropium
bromide,oxitropium
 Methyl xanthines
theophylline,aminophyllie,
diprophylline
34

35.  CORTICOSTEROIDS
 Oral
Prednisone,prednisolone,
methyl prednisolone
 Parenteral
Methyl prednisolone,
 Inhalational
Beclomethasone,
fluticasone,Budesonide,
35

36.  LEUKOTRIENE
MODULATORS
 5-lipoxygenase
inhibitor
zileuton
 Cysteinyl leukotriene –
receptor antagonists
Montelukast ,zafirlukast,
pranlukast
36

37.  MAST CELL STABILISERS
sodium cromoglycate,nedocromil
 MONOCLONAL ANTI-IGE ANTIBODY
omalizumab
 MISCELLANEOUS
Nitric oxide donors
37

38. SYMPATHOMIMETICS
 Sympathomimetics
act by stimulating
β2 receptors in the cAMP
bronchial smooth
muscles & mast cells bronchodilation
inhibit the release of
histamine from mast cells
promote mucociliary clearance
38

39. Salbutamol
 Highly selective 2 agonist
 Inhaled salbutamol produces bronchodilation within
5 min & actions lasts for 2-4 hrs
 Side effect-muscle tremors,ankle edema,palpitation
 Oral salbutamol-acts for 4-6h
 Route & dose:inhalation-100-200mcg every 6hrs/when
required through MDI to terminate an acute attack

39

40.  It is the first long-acting selective β2 agonist with a
slow onset of action
 Used by inhalation on a twice daily schedule for
maintenance therapy and for nocturnal asthma
 But not for acute symptoms
 Concurrent use of inhaled salmeterol with inhaled
glucocorticoid produces effects equivalent to double
dose of the corticoid alone

Salmeterol
40

41. NONSELECTIVE SYMPATHOMIMETIC
 Produces powerful bronchodilation by acting through
β2 adrenergic receptors
 Useful in an acute attack
 Given subcutaneously 0.2-0.5ml of solution
 Side effects: tachycardia,hypertension,worsening of
angina
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42. METHYL XANTHINES
cAMP bronchodilation
bronchodilation
inhibit release of histamines
improve mucociliary clearance
42
Theophylline
Inhibit
phosphodiesterase
Blokage of
adenosine receptors

43.  Theophylline are generally used as combination
therapy with β2 agonists
 Methyl xanthines are the 3rd /4th line drugs in the
treatment of asthma
43

44. PHARMACOLOGICAL ACTIONS
CNS STIMULATION
HEART STIMULATION
BLOOD RELAXATION
BRONCHI DILATION
KIDNEY DIURESIS
SK MUSCLE INCRASED
CONTRACTILITY
GASTRIC IRRITATION
PHOSPHOSE DIESTERASE INHIBITION
ADENOSINE ANTAGONISM
44

45.  ANTICHOLINERGICS
 Atropine drugs cause bronchodilation by binding to
M3 receptors on airway smooth muscle & preventing
the action of acetylcholine released from
parasympathetic nerves
 Nebulized ipratropium mixed with salbutamol
produce greater and more prolonged bronchodilation
 Used in acute severe asthma
45

46. Leukotriene antagonists
X cysteinyl -LTreceptors
leukotrines
bronchodilation
bronchial inflammation
hyper reactivity
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Montelukast
zafirlukast

47.  Mast cell stabilizers
stabilize
allergic mediators
are not released
47
Sodium
cromoglycate
ketotifen
Mast cell

48. CORTICOSTEROIDS
corticosteroids
48
receptor
responses
Inhibit
release of
prostagla
ndins &
LT
Produce
eosinope
nia
Inhibit
cytokini
ns

49.  Oral corticosteroids
 For a period of 7-10 days to suppress the symptoms &
to prevent relapse
 Systemic steroid therapy
 Severe chronic asthma-not controlled by
bronchodilators and inhaled steroids ,or when there
are frequent recurrences of increasing severity
 Status asthmatics
 COPD
 Eg-Hydrocortisone ,prednisolone
49

50.  Inhaled steroids
 Budesonide
 Beclomethasone dipropionate
 fluticasone
50

51. MONOCLONAL ANTI-IGE ANTIBODY
 Omalizumab prevent the binding of IgE to mast cell &
prevent mast cell degranulation
 Administered parenterally
 Use :moderate-severe asthma,food allergy,nasal allergy
 Side effects:redness,stinging,itching
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52. MISCELLANEOUS DRUGS
 Nitric oxide donors
 Non-noradrenergic noncholinergic
neurotansmitter(NANC)
 Dilate the pulmonary blood vessels & relax the airway
smooth muscles
 Eg: sildenafil
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53. REFERENCE
 H.P.Rang.,M.M.Dale.,2011.,Pharmacology.,7th edn.,356-
360
 K.D.Tripathi,essentials of medical pharmacology.,6th
edition.,page no:213-220
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54. THANK
YOU
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