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 cromoglycateKetotifen

Sodium cromoglycate

USE?

BRONCHIAL

ASTHMA

ALLERGIC

RHINITIS

ALLERGIC

CONJUNC--

TIVITIS

ADVERSE EFFECT

HEADACHE DIZZINES

S

ARTHRALGIARASHES

DYSURIA

KETOTIFEN

ANTIHISTAMINIC

WITH

CROMOGLYCOL

ATE LIKE

ACTION

NOT A

BRONCHO DILATOR

PRODUCESSEDATION

SYMPTOMATIC RELIEF IN

1.ATOPIC DERMATITIS

2.PERENNIAL RHINITIS

3.CONJUNCTIVITIS

4.URTICARIA

5.FOOD ALLERGY

ABSORBED ORALLYBIOAVAILIBILITY: 50%

T1/2 : 22HOURS

ADVERSE EFFECT

HEADACHEDIZZINESS

WEIGHT GAINRASHES

DYSURIA

SEDATION

DRY MOUTH

MONTELUKAST, ZAFIRLUKAST, ZILEUTON

LEUKOTRIENESFATTY 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

NEUROPATHYRASHES

CHURG-STRAUSS SYNDROME

EOSINOPHILIA

ZILEUTON

5-LOX INHIBITOR

BLOCKS LTC4/D4/B4 SYNTHESIS

CLINICAL EFFICACY SIMILAR TO MONTELUKAST

SHORT ACTION

HEPATOTOXIC POTENTIAL

RESTRICTED USE

• 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

ASTHMAWHEN NOT CONTROLLED BY

BROCHODILATORS/INHALED STEROIDS

START PREDNISOLONE 20-60Mg/DAY

2. STATUS ASTHMATICUSHIGH 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