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RASIONALITATION IN ANTI-ASTHMA DRUGS

Nurfatimah I.R. (030100088)


Pipi Malindo H. (030100092)
Deyvia Daulay (030100094)

Department of Pharmacology and Therapeutic


Faculty of Medicine
Universitas Sumatera Utara
2006
Asthma-Pathology -2

Percent Change in Age-Adjusted


ASTHMA!!!
Death Rates, U.S., 1965-1998

Proportion of 1965 Rate


3,0
3.0
Coronary Stroke Other CVD COPD All Other
2,5
2.5 Heart Causes
Disease
2,0
2.0

1,5
1.5

1,0
1.0

0,5
0.5

0,0 0
–59% –64% –35% +163% –7%
1965 - 1998 1965 - 1998 1965 - 1998 1965 - 1998 1965 - 1998
Shashi
DEFINITION
“ Asthma is a disease which characterized by
bronchial and tracheal hyperresponsiveness
with stimulants, resulting widely airway
constriction and the degrees of this disease
can change anytime, spontaneously or
because of therapeutic reactions “
(The American Thoracic Society )
Ethiology of Asthma
 Two factors provoke asthma:

Triggers; result in tightening of the


airways (bronchoconstriction).
Inducers; result in inflammation of
the airways.

 Genetic???
Asthma-Pathology -5

Pathogenesis: INDUCERS
Allergens,Chemical sensitisers,
Airway Air pollutants, Virus infections
Hyperresponsiveness
Genetic*

INFLAMMATION/
BRONCHOCONSTRICTION
Airflow Limitation

TRIGGERS
Allergens, Exercise, SYMPTOMS
Cold Air, SO2 Particulates Cough Wheeze
Dyspnoea

Shashi
Signs & Symptoms
 Signs of asthma:
Faster and deeper breathing
Anxiety
Sitting uncomfortablely
Airway muscle working hard to
get enough airflow
 Symptoms of Asthma:

Coughing
Wheezing
Chest pain
Dyspnoe
Increase of respiratory rate
Pulmonary Obstruction Diseases

• The classification of pulmonary/airways


obstruction diseases:
Asthma or reversible pulmonary
obstruction disease
COPD (Chronic Obstruction
Pulmonary Disease), such as
chronic bronchitis and emphysema
• The symptoms of asthma, chronic
bronchitis, and emphysema are same,
especially in the tightening of airways.
• The tightening of these airways may
cause:
Hyperventilation
Abnormal distribution between
air ventilation and pulmonary
blood circulation
Disturbance of air difusion in
alveoli
Comparison of airways tightening
pathophysiology between asthma,
chronic bronchitis, and emphysema
Asthma Chronic Emphysema
Bronchitis
- constriction of Hipertrophy of Loss of
airways smooth airways smooth pulmonary
muscle muscle and elastic recoil
- Mucosal oedema mucous gland
- Bronchial
hypersecretion
Asthma Pathogenesis
Mediator inflammation in asthma:

–Histamin
–Leukotrien
–Eosinophile Chemotactic Factor
of Anaphylaxis (ECF-A)
–Platelet Activating Factor (PAF)
Asthma-Pathology -13

Wheezing Pathophysiology

Shashi
Asthma treatment goals:
 Relief airways tightening/ bronchoconstriction
immediately.
 Education of asthma management.

How to choose the right asthma treatment?


Make sure that the airways tightening caused by
asthma.
Make sure that wheezing sound caused by asthma.
Make sure that there is airways inflammation
caused by alergy reaction.
Choice of Anti-asthma

 Long Term Control Medicines

 Quick Relief Medication

 Imunology Therapy

 Anti Ig E monoclonal antibody


Classification of asthma drugs
based on their effects:

Anti-inflammation.
Bronchodilator.
Combination of anti-inflammation
and bronchodilator.
RASIONALITATION OF ANTI-ASTHMA DRUGS
Inhaled Corticosteroid
beclomethasone, triamcinolone, flunisolide, fluticasone,
budesonide, and mometasone
Used for asthma control therapy(long term medication)
Most effective → Aerosol.
Advantages:
- Effective in reducing asthma symptoms and increasing
pulmonary function of the mild asthma patients.
- Reducing or replacing the used of oral corticosteroid
in more serious asthma patients.
- Reducing bronchial reactivity.
Contraindication:
hypersensitivity, nasal infection and haemorrhage,
candidiasis orofaring, and patient with recurrent
epistaxis.
Oral and I.V corticosteroid

Prednisone, methylprednisolone, and


prednisolone
Therapeutic effect as same as inhaled
corticosteroid.
More side effects!!!
Used as quick relief medication
Contraindication:
- During pregnancy and breast-feeding
- Patients with osteoporosis
Mast Cell Stabilizer
Cromolyn sodium
Used for preventing asthma attack
Advantages:
- As the prophylaxis of asthma attack
caused by allergen, exercise, aspirin,
and working.
- Used for long term medication
Disadvantages:
- Using dosage four times a day
- Expensive
- Less effectivity than inhaled corticosteroid
- side effects: throat iritation, cough, dry mouth, and
bad taste of tongue.
Leucotrien Receptor Antagonist

Zafirlukast, Montelukast, and Zileuton


Drug of choice for asthma caused by aspirin.
Advantages:
→ effective to reduce asthma excacerbation
Disadvantages:
- Less effective than inhaled corticosteroid
- Using dosage four times a day (Zileuton)
- Side effect: Hepatotoksisitas
Contraindication:
Hypersensitivity of cromolyn, patients with
coronary heart disease, and cardiac arythmias.
IgE Antibody

Omalizumab
Used as intravenous or intramuscular
anti-asthma.Advantages:
- Decreasing the degrees of asthma
- Reducing the used of corticosteroid
- Repaired nasal symptoms for patients
with allergic rhinitis.
Disadvantage:
→ very expensive
2 Agonist

Salmeterol, formoterol, budesonide, and


fluticasone
Drug of choice for asthma therapy and
management.
Base on their time of action:
- Short Acting 2 Agonist
→ Quick Relief Medications.
- Long Acting 2 Agonist
Can be used as combination with inhaled
corticosteroid (Symbicort and Seretide).
Anti-cholinergic
Ipratropium bromida
Needs a high therapeutic dose to get the
therapeutic effect.
Used for the patients who intolerant with 2
Agonist.
Contraindication:
hypersensitivity with belladona alcaloid,
alergy with soya lechitine & bean protein,
glaucoma-closure angle.
Effectivity ↑ → combination with 2 Agonist
(Combivent)
Methylxanthine

Bronchodilator (theophylline)→ used if


therapy with 2 Agonist failed.
Efficacy ???
Advantage:
→ the cheapest among anti-asthma
drugs.
Drugs interactions
• Corticosteroid with:
- Acetaminophen
- Alcohol and sedative drugs
- Antacide

• Zafirlukast with:
- Aspirin
- Erythromycin
- Theophylline
• 2 Agonist with:
- Corticosteroid and methylxanthine
- TCA

• Anti-cholinergic with:
- Tacrine

• Methylxanthine with:
- Alcohol, allopurinol, cimetidine
- Carbamazepine and phenobarbital
conclusion

 Asthma is a chronic inflammatory disorders


of the respiratory airways and marked by
recurrent of wheezing, coughing, and
dyspnoe.
 2 kinds of anti-asthma:
- Short term management
- Long term management
 Goals of asthma treatment:
→ the medications can control asthma
symptoms

“Don’t let asthma manage you,


but you manage your asthma”
“The greatest lesson in life is to know
that
even fools are right sometimes”
Sir Winston Churchill
Triggers
• Cold air
• Dust
• Strong fumes
• Air pollution
• Emotional and stress
• Drugs
• Nutrients
• Gastro-esofageal reflux
• Cigarette smoke
Inducers
• Allergens
• Virus

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