Pharmacology Review Sheets: Drugs Affecting the Respiratory System Rx of asthma, p.

1
Bronchodilators
Drug
Albuterol
(Proventil)
Terbutaline
(Brethine)

Drug Class
Sel. -agonist

Salmeterol
(Serevent)

Sel. -agonist

Epinephrine

, 1, -agonist

Theophylline

Methylxanthines

Atropine sulfate
Anticholinergic
(Isopto atropine)
Ipratropium
Anticholinergic
bromide
(Atrovent)

Pharmacokinetics/Action
Action: Stimulates adenyl cyclase,
thus cAMP
Admin: Inhalation
Duration of action: 6 hrs for albuterol,
4-5 hrs for terbutaline
Action: Stimulates adenyl cyclase,
thus cAMP
Admin: Inhalation
Duration of action: 12+ hrs
Action: Stimulates adenyl cyclase,
thus cAMP
Admin: Parental (im, iv)
Duration of action: 20 mins
Action: Inhibition of adenosine
receptors, inhibition of PDE
(which breaks down cAMP)
Admin: Inhalation
Metabolism: Liver
Action: Blocks musc. ACh receptors
Action: Blocks musc. ACh receptors
Duration of action: Peaks at 1-2 hrs

Effects and Uses

Short-acting relief of asthma

Adverse Effects
Skeletal muscle fasciculations (20%)

Long-acting relief of asthma

Tachycardia
Skeletal muscle fasciculations (20%)
Note: These side effects are minimized when inhaled

Severe, life-threatening asthmatic situations

Drug of choice for anaphylaxis
Very potent bronchodilator

Cardiac arrhythmias, palpitations

Contraindicated w/pre-existing cardiac conditions
Drug interaction with cocaine (cocaine potentiates it)
Contraindicated in hyperthyroidism
Narrow therapeutic window (5-15 g/mL)
CNS: nervousness, tremor
GI: Secretion of gastric acid, digestive enzymes
Cardiovascular: Cardiac dysrhythmias

Asthma former drug of choice (see side effects)

(effectiveness of adrenoreceptor agonists are better)

Limited use due to systemic side-effects not really

used anymore
Anticholinergic used for asthma

Systemic side effects (see section on atropine)

Effects and Uses

Rx of asthma, by mechanism of action listed

Adverse Effects
Oral candidiasis (prevent by gargling water after
inhalation)
Hypertension
Diabetes
Iatrogenic Cushings Disease
Osteoporosis
Peptic ulcers
Note: Flunisolide has < side effects than beclomethasone
Xerostomia (mouth dryness)
Throat irritation
Dry cough

Less side effects (esp. with spacer) i.e. xerostomia, etc.

Anti-inflammatory agents
Drug
Beclomethasone
Flunisolide
(Flovent)

Drug class
Corticosteroids

Cromolyn
Nedrocromil

Zilutin
(Ziflo)

LT synt. inhibitor

Zafirlukast
(Accolate)

LT synt. inhibitor

Pharmacokinetics/Action
Action: eosinophils, mucosal
edema, synthesis/sensitivity of
b-adrenergic receptors, gene
regulation for cytokines,
lipooxygenase
Admin: Inhalers, spacers
Metabolism: Extensive, by liver

Action: Stabilizes membranes, thus

* Rx for asthma
release by mast cells
Note: these dont work for everyone!
Admin: Inhaler
Absorption: Poor systemically (these
are insoluble salts)
Excretion: kidney
Action: Inhibits lipooxygenase
Rx for asthma (newer drug)
Admin: Oral
Metabolism: mostly liver
Action: Blocks binding of LTD4,
Rx for asthma (newer drug)
LTE4

GI: Indigestion, constipation, etc.

GI: Abdominal pain, nausea, etc.

Inhibits CYP3A4 and CYP2A9

Admin: Oral
Metabolism: mostly liver