Respiratory Drugs Part I-II

Drugs Class Mechanism

Guaifenesin (OTC) Expectorant

Opiod derivative
Dextromethrophan (OTC) Antitussive whichlacks analgesic or
addictive properties

Mucous membrane
Phenyephrine (OTC) Alpha-antagonist
Decongestant
Central acting,
OpioidsLaudanum
analgesicdepresses both
Codine ( only one really used) Antitussive
the respiratory center
Hydrocodone
and the cough reflex
-Exerts antitussive action on
stretch or cough receptors
Benzonatate Antitussive
in the lung
-Peripheral acting

Active sulfhydral
groupopens disulfide
Acetylcysteine
Mucolytic linkagesin mucus therby
( oral or inhaled)
lowering its viscosity thus
facilitating its expulsion

Epinephrine
Alpha-adrenergic receptor
Sympathomimetic
activators
Ephedrine
Beta-adrenergic agonist;
activateadenyl cyclase
Isoproterenol Sympathomimetic
coupling w/ Gs increase
cAMP

Beta 2 adrenergic
Albuterol Sympathomimetic receptor agonist( same
mech as isoproterenol)

Theophylline Methyxanthine relax bronchial Sm Musc

 Zileuton 5-lipoxygenase inhibitor
Leukotriene Pathway
Zafirulkast LTD4 receptor
Inhibitors
Montelukast antagonists

Anti-inflammatory, inhibit
cytokine production,
Prednisone prevent infiltration of
Corticosteroids
Certolizumab lymphocytes, eosinophils
and mast cells into
asthmatic airways

Activated by esterase in
Ciclesonide Corticosteroids
bronchial epithelial cells
Atropine inhibit of Ach causes
Muscarinic Antagonists
Ipratropium Br smooth muscles to relax

Alter chloride channels

Mast cells inhibition =>

Cromolyn decreased histamine
Mast cell Stabilizers
Nedocromil release

Eosinophil inhibition =>

decreased allergic response

Anti-IgE mAb => decrease

Omalizumab Monoclonal Ab
IgE in plasma
Respiratory Drugs Part I-II

Side Effects

Hallucinagenic @ high doses

-Histamine release
-Resistance to cough suppresison
-Mucus accumulation

Caustic to esophagus if pill broken

Tachycardia, arrhythmia, angina

pectoris

high doses can cause cardiac

arrhythmias

tremor, nervousness, headache,

muscle cramps,dry mouthand
palpitations

High doses in pts on diuretics,

xanthine derivatives, or renal failure
=>hypokalaemia

clearance increasedby induction of

hepatic enzymes (smoking; dietary
effects)
Systemic Effx:Adrenal
suppresion,oropharnygeal
candidiasis( tx by rinsing mouth with
water after medication), osteoporosis,
cataracts, glucose intoleranceLocal
Effx:Vocal cords, hoarseness

minor, localized to deposition sites

Throat irritation, cough and mouth

dryness
 Notes
Often used w/ anti-histamines (H2),
decongestants and antitussives in many
combination products

Drug-Drug interactions:MAO
inhibitors:isocarboxazid, phenelzine, selegiline,
tranylcypromineSerotonin reuptake
inhibitors:fluoxetine and paroxetine

Adults only

Contraindicated:Asthmatics, MAO
inhibitorsHydrocodone: semi-synthetic opiod; used
to treat acetaminophen, alcohol related toxicity
Contraindicated:patients who cannot swallow
whole pill

Needs to beswallowed whole

Indications:adjuvant for pts with chronic

bronchopulmonary disease, acute
bronchopulmonary disease, pulmonary
complications of cystic fibrosis, acetaminphen
overdoseContraindications:patient
hypersensitivity

Sc or inhalation administration, rapid acting

less potent, more centrally acting, not used as much
for treating asthma

potent bronchodilator, administered by inhalation

administered by inhalation, see effect after 5-20

minutes

Most effective Xanthine bronchodilator ( others:

Theobromine and caffeine),oraladministration,
narrow therapeutic window
oral administration

oral and pharnygeal

Aerosol tx most effective = avoid systemic effects

pro drug
lower dose so no increased HR
High dose = does not enter CNS

Clinical indications:pretreatment with either agent

blocked bronchoconstriction caused by allergen
inhalation, exercise,sulfur dioxide, occupation
asthmaRestrictions:not as effective as inhaled
corticosteroids, decreased use in childhood

reduces degree of both early and late

bronchiospastic response to Ag challenge

Reduction of the severity of asthma exacerbation =

reduction in corticosteroid requirements

Lots of $$, cancer chemo