Respiratory Drugs Part I-II

Drugs

Class

Guaifenesin (OTC)

Expectorant

Dextromethrophan (OTC)

Antitussive

Phenyephrine (OTC)

Mucous membrane
Decongestant

OpioidsLaudanum
Codine ( only one really used)
Hydrocodone

Antitussive

Benzonatate

Antitussive

Mechanism

Opiod derivative
whichlacks analgesic or
addictive properties

Alpha-antagonist
Central acting,
analgesicdepresses both
the respiratory center
and the cough reflex
-Exerts antitussive action on
stretch or cough receptors
in the lung
-Peripheral acting

Mucolytic

Active sulfhydral
groupopens disulfide
linkagesin mucus therby
lowering its viscosity thus
facilitating its expulsion

Sympathomimetic

Alpha-adrenergic receptor
activators

Isoproterenol

Sympathomimetic

Beta-adrenergic agonist;
activateadenyl cyclase
coupling w/ Gs increase
cAMP

Albuterol

Sympathomimetic

Beta 2 adrenergic
receptor agonist( same
mech as isoproterenol)

Theophylline

Methyxanthine

relax bronchial Sm Musc

Acetylcysteine
( oral or inhaled)

Epinephrine
Ephedrine

Zileuton
Zafirulkast
Montelukast

Prednisone
Certolizumab

Ciclesonide
Atropine
Ipratropium Br

Leukotriene Pathway
Inhibitors

Corticosteroids

5-lipoxygenase inhibitor
LTD4 receptor
antagonists
Anti-inflammatory, inhibit
cytokine production,
prevent infiltration of
lymphocytes, eosinophils
and mast cells into
asthmatic airways

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

Alter chloride channels

Cromolyn
Nedocromil

Mast cell Stabilizers

Mast cells inhibition =>

decreased histamine
release
Eosinophil inhibition =>
decreased allergic response

Omalizumab

Monoclonal Ab

Anti-IgE mAb => decrease

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