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Asthma

Drugs

Action

Albuterol,
Metaproterenol,
Terbutaline

Shortacting2
agonist(SABA)

Salmeterol,
Formoterol

Longacting2
agonist(LABA)

Theophylline
Aminophylline

Methylxanthines
PDE4inhibition,
adenosineblock

Atropine

Tertiaryamine
Mblock

Ipratropiumbromide
[Spiriva]

Quaternaryamine
Mblock

Tiotropium

M1&M3block

Prednisone
Beclomethasome,
Budesonide,
Fluticasone,
Flunisolide

Glucocorticoidanti
inflammatory

Ciclesonide
Monteleukast,
Zafirleukast
Zileuton

5LOXinhibitor

Cromolyn,
Nedocromil

BlockCa2+influx
whenstimulatedby
IgEAbAb
interactionwith
mastcells

LTD4Rblock

Stabilizemastcell
degranulation

Omalizumab[Xolair]

AntiIgEAb
Early&Late
phasereactions
Eosinsputum

Pharmacokinetics
Inhalational,rapid
onset,highpotency
Bronchodilation,
pulmonaryVD,
mucociliary
clearance
Givenp.o.
(100%bioavailability)
Hepaticmetabolism
(CYP450interactions!)
Parenteral
Hepaticmetabolism
Rapidonset
Inhalation(metered
dose)
Delayedonset
Longduration(68h)
Inhalation(powder)
Delayedonset
Longduration(24h)
Oral,parenteral
Delayedonset(48h,
peaks:1020h)
Inhalation
Veryslowdelayed
onset
Highpotency;poor
absorption
Inhalation
LessA/E(prodrug)
Givenp.o.
Rapidonset
Lowpotency

Indications
Mildasthma,
rescuetherapy,
exercise
prophylaxis
Combination
therapy:synergistic
withsteroids

COPD,rarely
asthma

COPD,
combination
therapywith
agonists

A/E,Toxicity,Other
Tolerance
(B16:GlyArg),
tachycardia,HTN,
tremor,hypokalemia,
worseningV/Q
Mastcells&
inflammation
Toxicity:arrhythmias,
seizures
Sametoxicityas
theophylline
Tachycardia,mydriasis
(dilatedpupil),urinary
retention,CNSaccess
NOCNSaccess;
mydriasis(withdirect
eyecontact)

COPD,
maintenance
therapy

MI,stroke(if
predisposed)

Maintenance
therapy;longterm,
ifsevere

Inhaled:OPcandidiasis,
hoarseness,osteoporosis,
growthretardation
Oral:+asepticnecrosis
ofthehip,adrenal
suppression,glucose
intolerance,HTN,
weightgain,cataracts,
hypokalemia

Mildasthma
maintenance;ASA
sensitivity

Minimal

Inhalation
Delayedonset(notas
longascorticosteroids)
Poorabsorption,
insolublesalts

Childhoodasthma
(atopic
extrinsic,allergic)

Pretreatmentblocks
immediate&delayed
reactions
Bronchial
hyperreactivity
Requiresseveralweeks
beforemaximumeffect
A/E:rarely,hoarseness,
pharyngitis

Parenteral,powder

Moderate
persistentasthma;
combinationTx,
lesssteroidsneeded

Notanaphylactogenic
FreeIgE;totalIgE
unchanged

Mepolizumab

IL5inhibition

Parenteral

Steroidresistant
eosinophilicasthma

Reducesexacerbations