MAST CELL STABILIZERS
BY
Mr. Kanishk Deep
Sharma
LEUKOTRIENE ANTAGONISTS
CORTICOSTEROIDS
SODIUM CROMOGLYCATE, KETOTIFEN
THEY ARE CHROMONE
DERIVATIVES THAT BLOCK
CHLORIDE CHANNELS ESSENTIAL
FOR MAST CELL DEGRANULATION
WHICH INTURN
STABILIZE THE MAST CELL
-PREVENTING HISTAMINE RELEASE
& RELATED MEDIATORS
Sodium cromoglycate
Ketotifen
Sodium cromoglycate
USE?
BRONCHI
AL
ASTHMA
ALLERGI
C
RHINITIS
ALLERGI
C
CONJUN
C--
TIVITIS
ADVERSE EFFECT
HEADACHE DIZZINES
S
ARTHRALGIA
RASHES
DYSURIA
KETOTIFEN
ANTIHISTAMINIC
WITH
CROMOGLYCOL
ATE LIKE
ACTION
NOT A
BRONCHO DILATOR
PRODUCES
SEDATION
SYMPTOMATIC RELIEF IN
1.ATOPIC DERMATITIS
2.PERENNIAL RHINITIS
3.CONJUNCTIVITIS
4.URTICARIA
5.FOOD ALLERGY
ABSORBED ORALLYBIOAVAILIBILITY: 50%
T1/2 : 22HOURS
ADVERSE EFFECT
HEADACHE
DIZZINESS
WEIGHT GAIN
RASHES
DYSURIA
SEDATION
DRY MOUTH
MONTELUKAST, ZAFIRLUKAST, ZILEUTON
LEUKOTRIENES
FATTY COMPOUNDS
PRODUCED BY IMMUNE
SYSTEM THAT CAUSE
INFLAMMATION IN ASTHMA &
BRONCHITIS , & CONSTRICTS
AIRWAYS
THEY ANTAGONISE
RECEPTOR CYSLT1
•MONTELUKAS
T
•ZAFIRLUKAST
• BROCHODILATATION
• REDUCED SPUTUM EOSINOPHIL COUNT
• SUPPRESION OF BRONCHIAL INFLAMMATION
• MILD TO MODERATE ASTHAMA:
ALTERNATIVE TO INHALED
GLUCOCORTICOIDS
• SEVERE ASTHMA: PERMIT STEROID
DOSE
REDUCTION &
RESCUE B2
AGONIST INHALATION
• WELL ABSORBED ORALLY
• HIGHLY PLASMA PROTEIN BOUND
• PLASMA T1/2 : 3-6HOURS(MONTELUKAST)
• PLASMA T1/2 : 8-12 HOURS(ZAFIRLUKAST)
ADVERSE EFFECT
HEADACHE
NEUROPATHY
RASHES
CHURG-STRAUSS SYNDROME
EOSINOPHILIA
ZILEUTON
5-LOX INHIBITOR
BLOCKS LTC4/D4/B4 SYNTHESIS
CLINICAL EFFICACY SIMILAR TO MONTELUKAST
SHORT ACTION
HEPATOTOXIC POTENTIAL
RESTRICTED USE
asthma medical treatment
• GLUCOCORTICOIDS ARE STEROID
HORMONES
• ANTI-INFLAMMATORY
• PREVENT PHOSPHOLIPID RELEASE
• DECREASE EOSINOPHIL ACTION
TYPE OF
THERAPY
SYSTEMIC
STEROID
THERAPY
INHALED
STEROIDS
PREDNISOLONE BUDESONIDE
BECLOMETHASONE DIPRPIONATE
SYSTEMIC STEROIDS
O USED IN 2 SITUATIONS
1. SEVERE CHRONIC ASTHMA
2. STATUS ASTHAMATICUS
1. SEVERE CHRONIC
ASTHMA
WHEN NOT CONTROLLED BY
BROCHODILATORS/INHALED STEROIDS
START PREDNISOLONE 20-60Mg/DAY
2. STATUS ASTHMATICUS
HIGH DOSE I.V. GLUCOCORTICOID, ACT IN
6-24 HRS
INHALED STEROIDS
O HIGH TOPICAL LOW SYSTEMIC
ACTIVITY
O SHOULD BE ‘STEP 1’ FOR ALL ASTHMA
PATIENTS
O INDICATED WHEN B2 AGONIST
REQUIRED DAILY
O START 100-200 mg BD
EFFECT
O SUPRESS BRONCHIAL INFLAMMATION
O INCREASE PEAK EXPIRATORY FLOW
RATE
O NO ROLE IN ACUTE ATTACK
O PEAK EFFECT IN 4-7 DAYS
O DOESN’T PRECIPITATE ASTHMA,
MUUSCULAR PAIN, LASSITUDE,
DEPRESSION, HYPOTENSION
IN COPD
O HIGH DOSE INHALED STEROIDS
BENEFICIAL ONLY IN ADVANCED
CASES
O NO PROOF THAT THEY SLOW
DISEASE PROGRESSION
ADVERSE EFFECT
HOARSENESS OF VOICE
SYMPTOMATIC OROPHARYNGEAL CANDIDIASIS
SYSTEMC EFFECT AT >600 mg
DOSE/DAY
• MOOD CHANGES
• OSTEOPOROSIS
• BRUISING
• PETECHIAE
• PITUITARY-ADRENAL SUPPRESION
DYSPHONIA
EXAMPLES
OBUDESONIDE
OBECLOMETHASONE
DIPRPIONATE
OFLUTICASONE PROPIONATE
OFLUNISOLIDE
OCICLESONIDE
THANK YOU

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