Cough is a protective reflex that expels secretions or particles from the airways. Antitussives suppress the cough center in the central nervous system and reduce cough reflex. Opioids like codeine and non-opioids like dextromethorphan are common antitussives. Expectorants increase bronchial secretions to facilitate removal of mucus while coughing. Asthma is characterized by airway inflammation and constriction. Bronchodilators such as salbutamol and corticosteroids are used to treat asthma. Salbutamol is a short-acting beta-2 agonist that causes bronchodilation. Corticosteroids reduce inflammation and prevent exacerbations.

1. DRUGS FOR COUGH
• Cough is a protective reflex with expulsion of
respiratory secretions or foreign particles from air
passages.
• It occurs due to stimulation of mechano- or
chemoreceptors in throat, respiratory passages or
stretch receptors in the lungs.

3. Antitussives (Cough centre suppressants)
1. Opioids: Codeine, Ethylmorphine, Pholcodeine
2. Nonopioids: Noscapine, Dextromethorphan
3. Antihistamines: Chlorpheniramine,
Diphenhydramine, Promethazine
MOA: Antitussives supress the
cough centre in the CNS. It raises
the threshold of cough centre
or act peripherally in respiratory
tract to reduce tussal impulses,
or both these actions.

4. Opioids
Codeine is an opium alkaloid, that decreases the
sensitivity of cough centres in the central nervous
system to peripheral stimuli and decreases mucosal
secretion. It is qualitatively similar to and less
potent than morphine, but is more selective for
cough centre. Codeine is regarded as the standard
antitussive; suppresses cough for about 6 hours.
Side effects: constipation, respiratory depression
and drowsiness, driving may be impaired.
Contraindicated in asthmatics, patients with
diminished respiratory reserve; should be avoided in
children.

5. Dose: 10–30 mg; children 2–6 years 2.5–5 mg,
6–12 years 5–10 mg, frequently used as syrup
codeine phosphate 4–8 ml.
Uses:
Dry and irritating
cough

6. Non-Opoids
Dextromethorphan is a central NMDA (N-methyl D-
aspartate) receptor antagonist that suppresses the
response of the central cough center.
Dextromethorphan does not depress mucociliary
function of the airway mucosa and is practically
devoid of constipating action.
Side effect: Dizziness, nausea, drowsiness; at high
doses hallucinations and ataxia may occur.
Dose: 10–20 mg, children 2–6 years 2.5–5 mg, 6–12
years 5–10 mg. It is a common ingredient of many
proprietary cough formulations.

7. Uses:
Dry and irritating
cough

8. Histamine
Histamine is synthesized & stored in two type of
cells; mast cells & basophils. Levels are high in Skin,
lungs & GIT. Release of histamine from mast cells is
produced by allergic reactions.
Actions:
In blood vessels it causes dilation & increases
capillary permeability.
In bronchi it produces constriction.
In stomach it stimulates secretion of acid.
In CNS it acts a as neurotransmitter.

9. Antihistamines
MOA: H1 antihistamines bind selectively to H1
receptors & prevent the action of histamines at
these sites.
Many H1 antihistamines provide relief in cough due
to their sedative and anticholinergic actions. They
have been specially promoted for cough in
respiratory allergic states.
• Chlorpheniramine (2–5 mg)
• Diphenhydramine (15–25 mg)
• Promethazine (15–25 mg)
• Cetirizine/Levocetrizine (5–10 mg)
• Fexofenadine (120–180 mg)

11. Indications:
• Allergic rhinitis & common cold, Allergic dermatitis,
itching, urticaria
• Wasp stings/ bite: pain and itching decreases
• Mild blood transfusion reactions, Allergic conjunctivitis
• Motion sickness: dimenhydrinate, promethazine
• Morning sickness: promethazine
• Vertigo: cinnarizine
• Appetite stimulant: cyprohepatidine
• Drug induced Parkinsonism: Diphenhydramine,
Adverse effects:
• Sedation, Dizziness, Fatigue, dry Mouth, blurred
Vision, constipation, urinary Retention
Contraindicated with CNS depressants
(potentiates action)

12. Expectorants (Mucokinetics)
1. Bronchial secretion enhancers: Na+ or K+ citrate,
K+ iodide, Guaiphenesin, balsum of Tolu, Vasaka,
Ammonium chloride
2. Mucolytics: Bromhexine, Ambroxol,
Acetyl cysteine, Carbocisteine, Dornase α
MOA: Expectorants increase bronchial
secretion or reduce its viscosity,
facilitating its removal by coughing.

13. • Na+ & K+ citrate increase bronchial secretion by
salt action.
• K+ iodide irritates the airway mucosa & increases
volume of secretion.
• Guaiphenesin, vasaka, tolu balsum are plant
products which enhance bronchial secretion and
mucociliary function.
• Ammonium salts also increase respiratory
secretions.

14. Mucolytics
Bromhexine is a derivative of the alkaloid vasicine obtained
from Adhatoda vasica (Vasaka), is a potent mucolytic and
mucokinetic, capable of inducing thin copious bronchial
secretion.
It depolymerises mucopolysaccharides directly as well as by
liberating lysosomal enzymes. It is particularly useful if mucus
plugs are present.
Side effects are rhinorrhoea and lacrimation, nausea, gastric
irritation, hypersensitivity.
Dose: adults 8 mg TDS, children 1–5 years 4 mg BD, 5–10 years
4 mg TDS.
Ambroxol A metabolite of bromhexine having similar mucolytic
action, uses and side effects.
Dose: 15–30 mg TDS
Carbocisteine have free sulphydryl groups that open disulphide
bonds in mucus and reduce its viscosity.

16. Bronchial asthma is a chronic inflammatory disorder of
bronchial airways resulting in narrowing of air tubes,
increased secretion, mucosal edema and mucus plugging.
Asthma is characterized by hyperreactivity of
tracheobronchial smooth muscles to a variety of stimuli.
Airway obstruction begins with binding of allergens such
as dust, pollen grains, cold air, and tobacco smoke with
antibodies on mast cells.
Antigen-antibody reaction causes mast cells to release
histamines, leukotrienes, prostaglandins & interleukins
that mediates inflammation.

18. Symptoms include:
• Dyspnea
• Bronchoconstriction
• Wheezing
• Cough
• Chest tightness
• Rapid respiration
Drugs for Asthma
A. Bronchodilators B. Anti-inflammatory

19. Drugs for Asthma
A. Bronchodilators
1. β2 Sympathomimetics: Salbutamol, Terbutaline,
Bambuterol, Salmeterol, Formoterol, Ephedrine
2. Methylxanthines: Theophylline, Aminophylline,
Doxophylline
3. Anticholinergics: Ipratropium bromide,
Tiotropium bromide

20. β2 agonist causes β2 receptor stimulation
increased cAMP formation in bronchial muscle
cell
bronchial relaxation (bronchodilatation)
MECHANISM OF ACTION OF β2 AGONIST
BRONCHODILATORS

21. Salbutamol (Albuterol) is a short acting selective β2
agonist mostly inhaled from pressurized metered dose
inhaler (pMDI) produces bronchodilation within 5 min
and the action lasts for 2–4 hours.
MOA: Salbutamol is β2 agonist that stimulates β2
receptors in the respiratory tract, increases cAMP
production, stabilize mast cell, inhibits release of
histamine and causes bronchodilation.
Indications:
• Abort and terminate attacks of asthma
• Airways obstruction in asthma and in some patients
with COPD
• Decreases uterine contractility in premature labour
• Dose: 2–4 mg oral, 100–200 μg by inhalation.

23. Adverse effects:
-Muscle tremor -Palpitation
-Restlessness -Nervousness
-Throat irritation -Ankle edema
-Hypokalemia
Contraindications:
• Hypertension
• Ischemic Heart Disease
• Arrhythmias
• Diabetes
• Hyperthyroidism

24. Salmeterol is long acting selective β2 agonist with a
slow onset of action; used by inhalation on a twice daily
schedule. It is more β2 selective than salbutamol, as
well as more lipophilic which accounts for its longer
duration of action.
Indications:
• Abort and terminate attacks of asthma
• Reduce breathlessness in COPD
Dose: 25 μg per metered dose inhaler; 2 puffs BD;
severe cases 4 puffs BD
Ephedrine is oral sympathomimetic that has α + β1 + β2
actions; causes mild slowly developing
bronchodilatation lasting for 3–5 hours. It is used for
mild to moderate chronic asthma.

25. Methylxanthines
Theophylline, caffeine, and theobromine are three
closely related plant alkaloids. Theophylline is used in
asthma and COPD due to its bronchodilatory action.
Actions:
• CNS: CNS stimulants, improves alertness
• CVS: stimulate the heart and increase force of
myocardial contractions
• Smooth muscles: smooth muscles are relaxed, most
prominent effect is exerted on bronchi, especially in
asthmatics. Slow and sustained dose-related
bronchodilatation is produced
• Kidney: mild diuretic action

26. MOA: Theophylline inhibits phosphodiesterase
(PDE) enzyme leading to an accumulation of cAMP
levels and also blocks adenosine receptors that
results in bronchodilation.

27. Indication & Dose:
• Bronchial Asthma & COPD
• Apnoea & premature infant
• Theophylline is poorly water soluble, cannot be
injected. 100–300 mg TDS orally.
• Because solubility of theophylline is low, a number of
soluble complexes and salts have been prepared:
• Aminophylline (Theophylline-ethylenediamine; 85%
theophylline) 250-500 mg oral, 250 mg/10 ml inj
• Etophylline (80% theophylline)
• Oxtryphylline (64% theophylline)
• Doxyphylline Dose: 400 mg OD or BD

28. Adverse effects: Nausea, Vomiting, Headache, Insomnia, GI
hemorrhage, Arrhythmias, Hypokalemia, Allergic reactions
Contraindications: Hypersensitivity to xanthine derivatives,
Porphyria, Peptic ulcer, Pregnancy

29. Anticholinergic/Atropinic drugs
MOA: Induce bronchodilatation by blocking M3
receptor mediated cholinergic constriction in the
larger airways.
Ipratropium bromide is a short acting (4–6 hours)
inhaled anticholinergic bronchodilator.
Tiotropium bromide is long acting (24 hours)
They are the bronchodilators of choice in COPD.
Combined treatment of ipratropium with β2
adrenergic agonists results in slightly greater and
more prolonged bronchodilation.

30. Ipratopium Inhaler

31. B. Anti-inflammatory
1. Leukotriene antagonists: Montelukast,
Zafirlukast, Zileuton
2. Mast cell stabilizers: Sodium cromoglycate,
Nedocromil sodium, Ketotifen
3. Corticosteroids
3.a. Systemic: Hydrocortisone, Prednisolone
3.b. Inhalational: Beclomethasone dipropionate,
Budesonide, Fluticasone propionate, Flunisolide
4. Anti-IgE antibody: Omalizumab

32. LEUKOTRIENE ANTAGONISTS
MOA: Montelukast and Zafirlukast competitively
antagonize cysteinyl leukotrienes (cysLT1) receptor mediated
bronchoconstriction, airway mucus secretion, increased
vascular permeability and recruitment of eosinophils.
Bronchodilatation, reduced sputum eosinophil count,
suppression of bronchial inflammation, mucus and
hyperreactivity.
Parameters of lung function show variable improvement.
Indications:
• mild-to-moderate asthma
• additive effect with inhaled steroids
• Montelukast: 10 mg OD; children 4-5 mg OD in evening
• Zafirlukast: 20 mg BD; children 5–11 yr 10 mg BD

34. Zileuton is a selective and specific inhibitor of 5-
lipoxygenase enzyme, preventing the formation of
both LTB4 and the cysteinyl leukotrienes. It is
orally active and used for the maintenance
treatment of Asthma.
Adverse effects:
-Headache -Rashes
-Eosinophilia -Neuropathy
Contraindications:
Hypersensitivity, Depression, Eosinophilia

35. Mast cell stabilizers
MOA: Sodium cromoglycate (Cromolyn sod.) inhibits
degranulation of mast cells and blocks release of
inflammatory mediators of asthma like histamine, LTs,
PAF, interleukins, etc. It decreases the cellular
inflammatory response & bronchial hyperreactivity.
Indications:
• Bronchial asthma
• Allergic rhinitis
• Allergic conjunctivitis
Sod. cromoglycate is not absorbed orally. Thus, it is
administered as an aerosol through metered dose
inhaler delivering 1 mg per dose: 2 puffs 4 times a day.

36. Mechanism of Mast cell stabilizers

37. Ketotifen is an H1 antihistaminic with sodium
cromoglycate like action; inhibits immunogenic and
inflammatory cells (mast cells, macrophages,
eosinophils, lymphocytes, neutrophils) and
inflammatory mediators are stopped.
Dose: 1–2 mg BD; children 0.5 mg BD.
Adverse effects: Sedation, dry mouth, dizziness,
nausea, weight gain
Contraindications: Hypersensitivity, Pregnancy

38. CORTICOSTEROIDS (Glucocorticoids & Mineralocorticoids)
Glucocorticoids
MOA: Glucocorticoids binds to the glucocorticoid
receptor and regulates the expression of anti-
inflammatory proteins. It supresses the expression
of pro-inflammatory proteins.
It has two major functions:
• Immune: Anti-inflammatory
• Metabolic: Gluconeogenesis
Glucocorticoids reduce bronchial hyperreactivity,
mucosal edema and suppress inflammatory
response to AG:AB reaction or other trigger stimuli.

40. Summary:

41. Hydrocortisone
Prednisolone
Nonfluorinated
prednisolones
Fluorinated prednisolones
Methylprednisolone
Betamethasone, Dexamethasone
Fluticasone, Triamcinolone
The most used glucocorticoids

42. Systemic Corticosteroids: Used in severe chronic asthma
& status asthmaticus/acute asthma exacerbation.
Hydrocortisone acts rapidly but has short duration of action. In
addition to primary glucocorticoid, it has significant
mineralocorticoid activity as well.
Dose: Shock, asthma, acute adrenal insufficiency: 100 mg i.v.
bolus + 100 mg 8 hourly i.v. infusion.
Prednisolone is 4 times more potent than hydrocortisone, also
more selective glucocorticoid, having intermediate duration of
action. It causes less pituitary-adrenal suppression when a
single morning dose or alternate day treatment is given.
Dose: 5–60 mg/day oral, 10–40 mg i.m.
Methylprednisolone is slightly more potent and more selective
than prednisolone.
Indication & Dose: 4–32 mg/day oral

43. Inhaled Corticosteroids: These are glucocorticoids
with high topical and low systemic activity (due to
poor absorption and marked first pass metabolism).
• Step one for all asthma patients for airway
inflammation and bronchial remodelling from
beginning.
• Suppress bronchial inflammation, increase peak
expiratory flow rate, reduce need for rescue β2-
agonist inhalations and prevent episodes of acute
asthma.
• Safe during pregnancy !
• No role during acute asthma

44. Beclomethasone dipropionate is anti-inflammatory
synthetic corticosteroid used for the treatment of asthma &
allergic rhinitis. Available as inhaler 50 μg, 100 μg, 200 μg
per metered dose.
Budesonide has high topical: systemic activity ratio. Small
fraction is absorbed & rapidly metabolized so less systemic
effects. Dose: 200–400 μg BD–QID by inhalation in asthma;
200–400 μg/day by intranasal spray for allergic rhinitis.
A/E: Nasal irritation, sneezing, crusting, itching of throat and
dryness may occur, especially in the beginning.
Contraindication: Presence of infection or nasal ulcers.
Fluticasone propionate has high potency (about double
of beclomethasone); longer duration and negligible oral
bioavailability. The inhalational dose is 100–250 μg BD (max
1000 μg/day). Preferred in patients requiring higher doses.

45. Indications:
• Asthma
• COPD
• Allergic rhinitis
• Allergic conjunctivitis
• Inflammation
• Autoimmune disorders
Adverse Effects: Hoarseness of voice, dysphonia,
sore throat, oropharyngeal candidiasis, osteoporosis,
growth retardation, hyperglycaemia and pituitary
adrenal suppression.
Contraindications: Hypersensitivity reactions

47. Type of Inhalation Device
THERE ARE THREE TYPES OF DEVICE IN
COMMON USE.
• METERED DOSE INHALER
• DRY POWDER INHALER
• NEBULIZER

48. Metered dose inhaler

49. how much medicine is left?

50. Spacer

51. Zerostat spacer

52. Rotahaler

53. Nebulizer

55. ANTI-IgE ANTIBODY
• Omalizumab is a humanized monoclonal
antibody against IgE.
• MOA: Administered s.c., it neutralizes free IgE in
circulation without activating mast cells and other
inflammatory cells.
• In severe extrinsic asthma, omalizumab has been
found to reduce exacerbations and steroid
requirement.
• It is very expensive and reserved for resistant
asthma patients with positive skin tests or raised
IgE levels who require frequent hospitalization.

57. Nasal Decongestants
are α adrenergic
agonist that induces
vasoconstriction of
blood vessels in nose,
throat and paranasal
sinuses.
Nasal Decongestants
reduces inflammation
and mucus formation
in nose, throat and
paranasal sinuses.

58. Nasal Decongestants
Topical: Oxymetazoline, Xylometazoline, Naphazoline,
Ephedrine HCl
• alpha2 agonist, long duration of action
• Use cautiously in hypertensive patients
Oral: Phenylephrine, Pseudoephedrine,
Phenylpropanolamine (PPA)
• Produce vasoconstriction in mucosa & skin
• Used orally as decongestant of upper respiratory
tract, nose & eustachian tubes
• Avoided in hypertensive patients
• PPA banned in Nepal (risk of haemorrhagic stroke)

59. Nasal
Decongestants
MOA Indications Adverse Effects
Ephedrine
Hydrochloride
0.5%-1%
Nasal drops
Sympathomimetic
αadrenergic agonist
and act as a
vasoconstrictor
common cold
sinusitis
hay fever
Allergies
burning and
stingling
sensation, dryness
of mouth and
throat, headache
Precaution:
Hypertension
Oxymetazoline
0.025-0.05%
Nasal drops
(NASIVION)
(SINAREST)
Sympathomimetic
or
αadrenergic agonist
vasoconstrictor
Nasal
congestion by
Common cold
Allergy
hay fever
burning and
stingling
sensation, dryness
of nose, headache
Nasal Decongestants
Ephedrine HCl, Xylometazoline, Oxymetazoline,
Pseudoephedrine, Phenylephrine