DRUGS ACTING ON
RESPIRATORY SYSTEM
BY BEKAN. A.
Introduction
The respiratory system includes:
– the upper airway passages,
the nasal cavities,
pharynx and
– trachea as well as the bronchi and
bronchioles
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ASTHMA
Asthma is characterized by fluctuating airways
obstruction, with diurnal variation and nocturnal
exacerbations.
o Clinically by recurrent coughing, chest
tightness, breathlessness and wheezing.
Physiologically These symptoms are due to
a combination of constriction of bronchial
smooth muscle, oedema of the mucosa lining
the small bronchi, and plugging of the
bronchial lumen withBy:viscous
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Bronchial asthma
Impairment of airflow in bronchial asthma is
caused by three bronchial abnormalities.
– Contraction of airway smooth muscles.
– Thickening of bronchial mucosa from
edema and cellular infiltration.
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Asthma triggering factors
Respiratory infection: rhinovirus, influenza,
pneumonia
Allergens: airborne pollens, house-dust mites,
animal danders
Environment: tobacco smoke, wood smoke
Emotions: anxiety, stress
Exercise: particularly in cold, dry climate
Drugs/preservatives: NSAIDs, β-blockers(non
selective)
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PHARMACOTHERAPY OF BRONCHIAL
ASTHMA
Drugs used in the treatment of bronchial asthma can be
grouped into three main categories:
1. Bronchodilators
a. β- Adrenergic agonists which include:
Non selective β-agonists
Selective β-agonists
b. Methylxanthines; theophylline derivatives
c. Muscranic receptor antagonists
2. Mast cell stabilizers
cromolyn sodium,
nedocromil,
3. Anti-inflammatory agents:
corticosteroids
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Sites of action bronchodilators
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1. Bronchodilators
A. β- ADRENERGIC AGONISTS
Non- selective- β-agonists
– Epinephrine,
– Ephedrine,
– Isoprotenerol
Selective β2-agonists
– Salbutamol,
– Terbutaline,
– Salmeterol,
– Formaterol
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MOA
– Relax smooth muscles
– Inhibit release of inflammatory mediator or
broncho constricting substances from mast
cells.
– Increase mucociliary transport.
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Non-selective β- agonists
– Cause more cardiac stimulation (mediated by a
β1 receptor), they should be reserved for special
situation.
– Epinephrine (Adrenaline) : very effective,
rapidly acting bronchodilator especially
preferable for the relief of acute attack of
bronchial asthma.
Administered by inhalation or Sc
S/Es
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worsening
BA of angina 11
Ephedrine: compared to epinephrine,
– longer duration of action but more
pronounced central effect and lower
potency.
– It can be given orally
– currently infrequently used
development of more efficacious and
beta2-selective agents
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Beta2 adrenoreceptor agonists…
Short-Acting 2-AR Agonists
Drugs: albuterol, levalbuterol, metaproterenol,
terbutaline, and pirbuterol, salbutamol.
Used for acute inhalational treatment of broncho spasm.
Inhalation drugs has rapid onset of broncho dialation (1-
5 min) which lasts for about 2 to 6 hours.
Are the preferred treatment for rapid symptomatic
relief of dyspnea associated with asthmatic broncho
constriction.
Are used as-needed basis..PRN
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Beta2 adrenoreceptor agonists…
Long-Acting 2-AR Agonists
Drugs: include Salmeterol and formoterol
They have a long duration of action: at least
12 hours
They shouldn’t be used for quick relief of an
acute asthma attack.
Agent of choice for nocturnal asthma
The higher lipophilicity of the drugs may be
responsible for the extended
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effect. 14
Side effects
– Tremors, anxiety, insomnia, tachycardia,
headache, hypertension and etc.
Contraindications:
– hypersensitivity to the drugs
Precautions:
– hypertension,
– cardiac dysfunction,
– hyperthyroidism, glaucoma,
– diabetes, pregnancy
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B. METHYLXANTHINES
The three important methylxanthines are
– theophylline, theobromine, and
– caffeine
Aminophylline is theophylline preparations most
commonly used for therapeutic purposes.
– It is combination of (theophylline and
diethylamine).
MOA: Inhibit the release of histamines and
leukotriens from the mast cells.
– Competitively inhibit By:PDE
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enzyme leading to 16
– Well absorbed from GIT and metabolized by
liver
Doses should be decreased in cases of
liver disease and heart failure
Adverse Effects:
– Anorexia, NV, abdominal discomfort,
headache, anxiety, insomnia, seizures,
arrhythmias.
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C. MUSCRANIC RECEPTOR ANTAGONISTS
MOA: inhibit effect of Ach at muscarinic receptors
–hence
– block the contraction of air way smooth muscle
and
– decrease in secretion of mucus
Ipratropium bromide is poorly absorbed and does not
readily enter the CNS
hence, It can safely be used for bronchial asthma.
Systemic ADR as a result of rapid
absorption(Atropine
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Antimuscranic antagonist drugs
– less effective than β- agonists agents in
reversing asthmatic bronchospasm.
– Ipratropium enhances the bronchodilator
produced by nebulizer albuterol in acute
sever asthma.
– They are useful as alternative therapies
for patients intolerant of β – agonists.
– COPD
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2. ANTI-INFLAMMATORY AGENTS
A. Corticosteroids
The most effective drugs available for long
term control
Lower the production and release of
inflammatory substances such as histamine,
prostaglandins, and leukotriene's, and reduce
mucus and edema secondary to decreasing
vascular permeability.
May be inhaled or taken orally, as well as IV.
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Corticosteroids....
MoA: Act primarily by suppressing:-
Synthesis & release of inflammatory
mediators.
Infiltration & activation of inflammatory cells.
Stabilize mast cell and basophil membranes:
decrease histamine release.
Reduce expression of cyclooxygenase-2
Reduces bronchial hyper reactivity.
↑Number of B2 adrenoceptors ↑
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responsiveness to agonist.
The corticosteroids commonly used are
hydrocortisone, prednisolone,
beclomethasone, triamcinolone and etc.
– taken by inhalation as aerosol,
oral(tapering), or an IV administration.
– reserved for patient who need urgent
treatment and those who have not
improved with bronchodilator.
Because of severe adverse effects
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Clinical uses in bronchial asthma
– Urgent treatment of severe asthma not improved
with bronchodilator
IV, inhalation or oral.
– Nocturnal asthma prevention
oral or inhalation
– Chronic asthma
Regular aerosol corticosteroids
Side effects:
– Suppression of the hypothalamic-pituitary-adrenal
axis
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B. MAST CELL STABILIZERS
Cromolyn Sodium, nedocromil
Very safe & effective for prophylaxis of asthma
MOA:
-Inhibit release of histamine and other mediators from
mast cells
Clinical uses
– Exercise and antigen induced asthma
– Occupational asthma
Side effects
– Poorly absorbed so minimal side effect
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C. LEUKOTRIENE INHIBITORS
LTs are mediators released from mast cells upon contact with
allergens.
Leukotriene (LT) B4 and the cysteinyl leukotrienes LTC4, LTD4, and
LTE4, are products of the 5-lipoxygenase pathway of arachidonic
acid metabolism and part of the inflammatory cascade.
o LTB4 is a potent chemo-attractant for neutrophils and
eosinophils.
o Cysteinyl leukotrienes constrict bronchiolar smooth muscle,
increase endothelial permeability, and promote mucous
secretion.
Both contribute powerfully to both inflammation and
bronchoconstriction
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Leukotriene inhibitors…
1. Inhibitor of leukotriene synthesis: Zileuton
5-Lipoxygenase enzyme inhibitor.
Inhibit both LTB4 and cysteinyl leukotriene
synthesis.
2. Leukotriene receptor antagonist
(Zafirkulast, Monteleukast)
Selective, reversible inhibition of the cysteinyl
leukotriene-1 receptor.
Blocking the effects of cysteinyl leukotrienes
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Leukotriene inhibitors…
MOA:
Decrease effect of leukotrienes on bronchial smooth
muscles;
Decrease inflammation
Decrease bronchoconstriction
Decrease edema and mucus formation
Decrease recruitment of eosinophils (zileuton)
Therapeutic uses:
For the prophylaxis of asthma.
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Severe acute asthma (status
Asthmaticus)
• Medical emergency requiring hospitalization
• Treatment includes
o oxygen
o Inhalation salbutamol
o Intravenous hydrocortisone followed by a
course of oral prednisolone
• Additional measures
- IV fluid to avoid dehydration
- Antibiotics if there is infection
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Allergic rhinitis
Allergic rhinitis is an inflammation of nasal mucous
membrane characterized by :
o Nasal congestion, itching, redness, sneezing, and
rhinorrhea
An attack may be precipitated by inhalation of an
allergen.
Allergens interact with mast cells coated with IgE.
Mast cells release mediators, such as histamine,
leukotrienes, and chemotactic factors that promote
bronchiolar spasm and mucosal
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thickening. 29
Allergic rhinitis
Antihistamines and/or intranasal
corticosteroids are preferred therapies for
allergic rhinitis.
o Oral antihistamines (loratadine,
fexofenadine, Cetrizine,
Dexchlorpheniramine maleate,
Chlorpheniramine)
o Nasal decongestants (Xylometazoline,
phenylephrine).
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ANTI-TUSSIVES
Cough is a protective reflex, which serves
the purpose of expelling sputum and other
irritant materials from the respiratory
airway. Cough
Productive Dry or Non
productive
Effectively expels Due to smoking and loca
secretions and irritants
exudates
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Anti-tussives
– used to suppress the intensity and frequency of
coughing.
1. Central anti- tussives
– Suppress the medullary cough center
– Opoid e.g. codeine, hydro codeine, etc
– Non opoid e.g. dextromethorphan
2. Peripheral antitussives
– Decrease the input of stimuli from the
cough receptor in the respiratory passage
e.g: Demulcents e.g. liquorices lozenges,
honey
– Demulcents
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Coat the irritated pharyngeal
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mucosa and exert
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Expectorant
– Drug that aid in removing thick tenacious
mucus from respiratory passages,
e.g. Ipecac alkaloid,
sodium citrate,
saline expectorant,
Mucolytics
– Agents that liquefy mucus and facilitate
expectoration,
e.g.N-acetylcysteine
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DECONGESTANTS
– drugs that reduce congestion of nasal passages,
open clogged nasal passages and enhances
drainages of the sinuses.
– Includes:-
Phenylephrine
Oxymetazoline etc.
MOA
– α1 agonists-- produce localized vasoconstriction on
the small blood vessels of the nasal membrane.
– Reduce congestion in By:
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nasal
BA
passages. 34
Classification:
– Short acting
topically
– phenylephrine, phenylpropanolamine
– Long acting
orally
– ephedrine, pseudoephedrine, naphazoline
topical
– Xylometazoline
– Oxymetazoline
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Clinical uses
– congestion associated with
rhinitis, hay fever, allergic rhinitis and to a lesser extent
common cold.
– administered
nasally or orally
Side effects:
– Ischemic changes in mucus membranes
– Nasal burning, stinging, dryness
– Tachycardia, arrhythmia, nervousness, restlessness,
insomnia, blurred vision
Contraindications
– Hypertension, severe coronary artery disease
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Z END
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