*Asthma
*COPD
*Cough
chronic inflammatory disorder of
the airways usually accompanied with
attacks of bronchoconstriction.
Specific abnormality is hyperactivity
. of the lung to one or more stimuli
Obstruction is often reversible
either spontaneously or with
treatment and not progressive like
.COPD
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Shortness of breath, dyspnea (narrowing of bronchi),if silent
chest means complete obstruction of airways.
Cough(worse in the morning, copious sputum)
wheezing(voice of hard breath due to difficulty in pushing air
out against the narrowed bronchi, mainly during expiration)
rapid respiration
Deaths due to asthma are
relatively infrequent, but
significant morbidity results in :
high outpatient costs
numerous hospitalizations
decreased quality of life.
Unfortunately we don’t
have a drug that is
bronchodilator and anti-
inflammatory at the same
time
Drugs goes directly to site of action ,thus
rapid action.(large surface area of alveoli)
Avoid systemic adverse reactions that
could happens if drug given parentreally or
orally.
Short acting SABA
Long acting LABA
Short acting(SABA): rapid onset(5-10 min)
salbutamol
terbutaline
Long acting(LABA) {12-24h}: slow onset(15-30min)
Salmeterol
formeterol
SE: tremor, tachycardia.
*β2-agonist stimulate adenylyl cyclase thus increase
cAMP smooth muscle relaxation and
bronchodilatation.
β2-adrenoceptor stimulation lead to:
Bronchodilatation.
An Increase in mucocilliary
clearance.
Inhibition of histamine release
from mast cell.
Tremor in skeletal muscle.
Effects within 5-10 mint and persists for 3-
4h.
Taken on as- needed basis
If nocturnal asthma more than twice a
month . Or this rescue therapy required
more than twice a week thus additional
therapy is needed.
Short acting B2-
agonists(SABA) are first
line quick relievers in
asthma and COPD .
* They achieve long duration(12h) due to high lipid solubility.
*Given regularly twice daily as adjunctive therapy in patient
whose asthma not well controlled by ICS.
*not useful in acute attack .
* LABA Reduce the doses of Corticosteroids and Relief the
symptoms for longer duration → so { LABA + Inhaled
Corticosteroids } is a very good combination for persistent
Mild to Moderate Asthma
Long acting B2-
agonists(lABA) should not
be used alone.
Ipratropium bromide :
*Has rare side effect (polar),slow onset
compared to SABA.
*Used in COPD.as an adjunct to β2 agonist and
steroids in asthma. For bronchospasm caused by β-
blockers.
*Available only as inhaler.
*It is methylxanthine.
*It is well absorbed cheap oral bronchodilator .
*Inhibit PDE4 thus increase cAMP(smooth
muscle relaxation, stimulate heart)
*Improves the strength of contraction of
diaphragm.
*Dose is 3-4 mg/Kg every 6h.
*Has narrow TI. thus need TDM(10-20mg\l).
*Overdose may cause fatal arrhythmia, seizures.
due to hypokalemia.
(plasma conc>40 mg/l).
*Clarithromycin inhibit its metabolism.
*Aminophylline(theophylline ethlenediamine): very
*Can be given :
orally (SR tab) as add-on therapy to ICS
and LABA.
Aminophylline: oral ,rectal parenteral
IV Aminophylline: slow infusion for status
asthmaticus.
*Narrow therapeutic index.
*Risk of drug-drug interactions
ICS are first -line in patients with moderate to severe
persistent asthma.
Effective in long –term control of asthma and COPD in
children and adult.
They inhibit phospholipase A2.
They potentiate the effect of B receptors, and they
decrease the number of mast cells.
They reverse mucosal edema and after months they
reduce hyperresponsiveness.
Phospholipid
)from cell membrane(
Corticosteroids -
Phospholipase A2
Lipoxygena
se- NSADS
inhibitors Arachidonic acid
Cyclooxygenase
Lipoxyenase-5
Prostacyclin (PGI2)
Leukotrienes PGE2
PGH2
PGF2
Inhalation:Beclomethason
* It is the most important route for chronic
use.
Oral:prednislon
*Used only in severe uncontrolled cases, when
the patient is not responding to inhaled
corticosteroid & LABA .
*short course of oral corticosteroid
*Not stopped suddenly
Injection:methylprednisolone,hydrcortison.
* Used in severe uncontrolled cases in the ER.
* High incidence of side effects.
*A spacer is a large-volume
chamber attached to a metered-
dose inhaler. Spacers decrease the
deposition of drug in the mouth
caused by improper inhaler
technique
*Spacer reduce velocity of injected
aerosol thus large particles deposit
in chamber and small particles
reach target tissue .
*Advised to all patients (children,
elderly)
* Patients should be counseled
about
*regular washing of spacers to
reduce the risk of bacterial
infection.
Inhaled have few systemic effect.
*Oropharyngeal candidiasis due to T-cell
inhibition. (gargle water and spit out).
*Hoarseness of voice due to local effect
on vocal cord.
Zileuton is 5-lipoxy-genase inhibitor, Montelukast
and Zafirlukast are LTD4 antagonists.
Montelukast available as chew tab for 6year and
older.
Used as additional drugs along with others. Mainly
used in Aspirin-induced asthma. In prophylaxis of
antigen-,exercise –induced asthma.
SE: Zileuton can elevates hepatic enzyme.
*It is recommended in prophylaxis of
asthma & COPD, especially during
allergic seasons like in the spring.
* Reduce the dose of corticosteroids
(we use it instead of increasing the
dose of corticosteroids because of its
high toxicity).
*They cannot be used alone without
corticosteroids.
Pharmacologic
antagonists are
less effective
because not
individual
mediators
responsible for
bronchoconstrictio
.n
*They are mast cell stabilizers.
*Effectively inhibit allergen and exercise-induced
asthma.
*Ineffective in reversing bronchospasm.(they don,t
affect already released mediators thus mainly used
for prophylaxis)
*Available as inhaler.(poorly absorbed by GIT)
*Short duration(4times daily) thus affect compliance.
*Effective in allergic rhinoconjunctivitis.(ND,ED)
*SE(rare): throat irritation, cough.
Anti-inflammatory drugs alone
are not useful in acute attack
Short acting B2-agonists are
always the first line.
*It is protective reflex that remove foreign
material and secretions from bronchi.
* it is common complain that is not only
related to respiratory system, It is
common SE of ACE inhibitors.
Productive cough: producing sputum. should not
suppressed unless it is exhausting the patient and
preventing sleep or rest ,we use expectorant that
facilitate expelling by cilia.
Nonproductive(dry cough): irritable and has to
be suppressed by antitussive drugs.
Cough is a reflex, a symptom, and not always
bad
We always try to treat dry cough, and let the
productive cough.
Management of cough → Treat the underlining
cause .
The most common cause:
Respiratory infection (Viral or bacterial).
Allergic Reaction.
we need to suppress cough when it's dry and
long-term because it's bothering the patient and
interfere with his normal life
1- Antitussives
2- Expectorants
3- Mucolytic
Codeine:
* weak opioid.
* mild cough suppressant in dose below dose to produce
analgesia(15mg).
* Has addictive effect and causes constipation.
Dextromethrophan:
synthetic derivative of Morphine.
it has no analgesic effect .
available in OTC preparations.
Less Constipation and addiction than codeine.
the first line in cough suppression.
*They loosen sputum and decreasing its viscosity,
and increasing the amount of respiratory fluid.
*Present in OTC cough mixture:
Ammonium chloride
guaifenesin.
* they reduce viscosity of mucus.
Carbocisteine
Acetyl cysteine.
*<Q> An acute attack of bronchial
asthma is best managed by:
<C>Formeterol.
<C>Beclomethason.
<C+>Salbutamol.
<C>Zileuton.
<C>Aminophylline.
<Q> Hoarseness of the voice is
recognized adverse effect of:
<C> Terbutaline.
<C>Zileuton.
<C+> Beclomethasone
<C>Formeterol
<C>Theophylline.
<Q> Which of the following drugs has
an antitussive effect?
C+>Codeine.
<C> Guaifensin.
<C> Salbutamol.
<C> Carbocisteine.
<C>None of listed drugs.
