Lecture 24drugs For Respiratoy Disease

DRUGS FOR RESPIRATORY
DISORDERS
STRATEGIES OF ASTHMA THERAPY
Acute bronchospasm(reliver Long term preventive
drugs) treatment(controller drugs)
• Beta2 agonists • Corticosteroids
• muscarinic antagonists • Long-acting β2 agonists can
improve the response to
• theophylline
corticosteroids
• Anti-IgE antibodies also appear
promising for chronic therapy
• leukotriene antagnnists are
used only for prophylaxis.
Beta adrenoreceptor agonist
Mechanism of action
• Beta-adrenoceptor agonists stimulate adenylyl cyclase (via the
β2-adrenoceptor–Gs-coupling protein-adenylyl cyclase
pathway)
• increase cyclic adenosine monophosphate (cAMP) in smooth
muscle
• The increase in cAMP results in a powerful bronchodilator
response
Patients with COPD often Loss of responsiveness
have concurrent cardiac (tolerance, tachyphylaxis)
disease and may have is an unwanted effect of
arrhythmias even at excessive use of the short-
normal dosage acting sympathomimetics
METHYLXANTHINES
Theophylline is the only member of

this group that is important in the
treatment of asthma
USES
• The major clinical use of methylxanthines is
asthma and COPD
• Slow-release theophylline (for control of

nocturnal asthma) is the most commonly used
methylxanthine
Toxicity
• The common adverse effects of methylxanthines include
• gastrointestinal distress
• Tremor
• Insomnia
• Severe nausea
• Diuretic
• vomiting
• hypotension,
• cardiac arrhythmias
• seizures may result from overdosage.
• Very large overdoses (eg, in suicide attempts) are potentially lethal because of arrhythmias
and seizures.
• Beta blockers are useful in reversing severe cardiovascular toxicity from theophylline
Theophyllinie interection
• Clearance varies with age (highest in young
adolescents)
• smoking status (higher in smokers
• concurrent use of other drugs that inhibit or
induce hepatic enzymes
• Don’t Give it with enzyme inhibitors
MUSCARINIC ANTAGONISTS
Mechanism of action
• When given by aerosol, ipratropium and
tiotropium competitively block muscarinic
receptors in the airways and effectively
prevent bronchoconstriction mediated by
vagal discharge
Clinical use
• in COPD, which is often associated with acute
episodes of bronchospasm, the antimuscarinic
agents may be more effective and less toxic than β
agonists.
• Ipratropium is a beneficial in the management of
chronic obstructive pulmonary disease
• In treating asthma in patients who are unable to

take adrenergic agonists.
• Because of its positive charge(as it’s a quaternary
amine), it does not enter the systemic circulation
or the CNS, isolating its effects to the pulmonary
system
Corticosterioids
Cromolyn, nedocromi
Mechanism of action
• It decreases the release of mediators (such as
leukotrienes and histamine).
• The drugs have no bronchodilator action but can
prevent bronchoconstriction caused by a
challenge with antigen to which the patient is
allergic. C
• romolyn and nedocromil are capable of
preventing both early and late responses to
challenge
Use
• Rarely used prophylaxis of asthma;
• cromolyn also used for ophthalmic,
nasopharyngeal, and gastrointestinal allergy
Leukotriene antagonists
• Montelukast
• zafirlukast
MechANISM OF ACTION
• Pharmacologic antagonists at LTD4 receptors
• Use:prophylaxis of asthma
Zileuton
• Inhibitor of lipoxygenase
• reduces synthesis of leukotrienes
• Prophylaxis of asthma
• Oral
Omalizumab
• Binds IgE antibodies on mast cells; reduces
reaction to inhaled antigen
• Prophylaxis of severe, refractory asthma not

responsive to all other drugs
MgSO4 IV
• It should be used only in severe acute attck or
status asthmaticus
• DONOT use MgSOE4 in routine attacks of

asthma
Status asthmaticus
• Status asthmaticus is an older, less precise
term for what's now more commonly known
as acute severe asthma or a severe asthma
exacerbation. It refers to an asthma attack
that doesn't improve with traditional
treatments, such as inhaled bronchodilators.
These attacks can last for several minutes or
even hours.
Management of status asthmaticus
Non pharmacological Pharmacological
• Oxygen inhalation • Albuterol or salbutamol
• IV steroid(hydrocortisone or
• Propped up position methylprednislone)
• Maintain airway • IV aminophylline infusion
• IV MgSO4
• Save IV line
• Start mechanical ventilation in

coma,respiratory
arrest,confusion,drowsiness or
Note:Beta-agonists, corticosteroids, deterioration of ABGs
and theophylline are mainstays in
the treatment of status asthmaticus
Prophylaxis of asthma
• Montelukast or zafirlukast
• Cromolyn Na
• Anti IgE antibodies
• Steroids
Acute attacks
• Salbutamol(albuterol) SABA
• Inhaled steroid(beclomethasone)
• Oxygen inhalation
• Propped up position
Chronic asthma
• Salmeterol(LABA)
• Inhaled steroids
• Albuterol inhaler(Taken as required or used as
needed)
Past Seqs
• 1. A 19-year-old moves from a small town to
your city, and is now your patient. He has a
history of asthma and his previous primary
care physician was managing it with albuterol
and theophylline. What is the main
mechanism that accounts for the beneficial
effect of these drugs? (3) [Annual 2018]
• Mechanism of action of albuterol
• Albuterol acts on beta-2 adrenergic receptors to relax
the bronchial smooth muscle.Beta 2 selective
adrenoreceptor agonist drugs stimulate adenylyl
cyclase via Gs coupling pathway and increase cAMP in
smooth muscle cells.It results in bronchodilator
respone
• It also inhibits the release of immediate
hypersensitivity mediators from cells, especially mast
cells
• Mechanism of action of theophylline
• 1st mechanism
• The methylxanthines inhibit phosphodiesterase (PDE), the enzyme that
degrades cAMP to AMP), and thus increase cAMP. This anti-PDE effect,
however, requires high concentrations of the drug.
• 2nd Mechanism
• Methylxanthines also block adenosine receptors in the central nervous
system (CNS) and elsewhere, but a relation between this action and the
bronchodilating effect has not been clearly established.
• It is possible that bronchodilation is caused by a third as yet unrecognized
action. In asthma, bronchodilation is the most important therapeutic
action of theophylline.
• What is the route of administration of
ipratropium in COPD and why is it considered
better than atropine in this condition? (3)
[Supple 2017 held in 2018]
• 5. A 12-year-old is brought to emergency room with
shortness of breath and wheezing. His pulse rate and
respiration are increased and he is restless. His father
gave previous history of asthma. What emergency
measure will you take to treat and what is long term
control? [Annual 2016]
• 6. Classify drugs for the prevention and treatment of
bronchial asthma with two examples for each group.
[Supple 2016]

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DRUGS FOR RESPIRATORY

Theophylline is the only member of

• Slow-release theophylline (for control of

• In treating asthma in patients who are unable to

• Prophylaxis of severe, refractory asthma not

• DONOT use MgSOE4 in routine attacks of

• Start mechanical ventilation in

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