Dosing & Uses
Dosage Forms & Strengths
powder for inhalation
aerosol for inhalation
Inhaled powder: 1 actuation PO q12hr (initial dose determined by asthma severity); not to exceed 1 actuation of 50 mcg/500 mcg q12hr
Inhaled aerosol: 2 actuations PO q12hr (initial dose determined by asthma severity); not to exceed 2 actuations of 21 mcg/230 mcg q12hr
Chronic Obstructive Pulmonary Disease
Inhaled powder: 1 actuation of 50 mcg/250 mcg PO q12hr
Treatment of symptomatic exophthalmos associated with thyroid-related eye disease
- Lithera, Inc, 9191 Towne Center Drive, San Diego, CA 92122
Inhaled powder: If dyspnea occurs between doses, chronic obstructive pulmonary disease (COPD) patients may take inhaled short-acting beta agonist (SABA) for immediate relief
Dosage Forms & Strengths
powder for inhalation
aerosol for inhalation
- <4 years: Safety and efficacy not established
- 4-12 years: 1 actuation of 50 mcg/100 mcg PO q12hr
- ≥12 years: 1 actuation PO q12hr (initial dose determined by asthma severity); not to exceed 1 actuation of 50 mcg/500 mcg q12hr
- <12 years: Safety and efficacy not established
- ≥12 years: 2 actuations PO q12hr (initial dose determined by asthma severity); not to exceed 2 actuations of 21 mcg/230 mcg q12hr
Serious - Use Alternative
Significant - Monitor Closely
Upper respiratory tract infection (21-27%)
Candidiasis, nonspecific site (0-10%)
Throat irritation (7-9%)
Musculoskeletal pain (2-9%)
Upper respiratory inflammation (4-7%)
Viral respiratory infections (4-6%)
Nausea or vomiting (4-6%)
Hoarseness or dysphonia (2-5%)
Gastrointestinal (GI) discomfort or pain (1-4%)
Oral candidiasis (1-4%)
Muscle cramps or spasms (3%)
Malaise or fatigue (2-3%)
Viral GI infections (0-3%)
Cardiac: Arrhythmias, ventricular tachycardia
Endocrine: Cushing syndrome, cushingoid features, growth velocity reduction in children and adolescents, hyperadrenocorticism
GI: Abdominal pain, dyspepsia, xerostomia
Immunologic: Immediate and delayed hypersensitivity reaction, anaphylactic reaction in patients with severe milk protein allergy (very rare)
Metabolic: Hyperglycemia, weight gain
Musculoskeletal: Arthralgia, cramps, myositis, osteoporosis
Neurologic: Paresthesia, restlessness
Psychiatric: Agitation, aggression, depression, behavioral changes (eg, hyperactivity, irritability; rare and occurring primarily in children)
Respiratory: Congestion, tightness, dyspnea, facial and oropharyngeal edema, immediate bronchospasm, paradoxical bronchospasm, tracheitis, wheezing, upper respiratory symptoms (eg, laryngeal spasm, irritation, or swelling, such as stridor or choking)
Dermatologic: Ecchymoses, photodermatitis
Black Box Warnings
Long-acting beta agonists (LABAs), such as salmeterol, may increase risk of asthma-related death; therefore, they should be used only as additional therapy for patients whose asthma is not adequately controlled on other asthma-control medications (eg, low- to medium-dose inhaled corticosteroids) or whose disease severity clearly warrants initiation of treatment with 2 maintenance therapies, including LABAs
Because of risk, use of LABAs without concomitant long-term asthma-control medication (eg, inhaled corticosteroid) is contraindicated
Once asthma control is achieved or maintained, assess at regular intervals; step down therapy (eg, discontinue LABA) if doing so is possible without loss of asthma control, and maintain patient on long-term asthma-control medication (eg, inhaled corticosteroid)
Do not use LABAs if asthma is adequately controlled on low- or medium-dose inhaled corticosteroids
Controlled clinical trials suggest that LABAs increase risk of asthma-related hospitalization in pediatric and adolescent patients; if such patients require addition of LABA to inhaled corticosteroid, use fixed-dose combination product containing both inhaled corticosteroid and LABA to ensure adherence
Hypersensitivity to drug, components of frmulation, or milk proteins, which may result in anaphylaxis, angioedema, rash, and urticaria
Not to be used as rescue therapy for status asthmaticus, acute bronchospasm
Patients with acute asthma, pulmonary tuberculosis, arrhythmias, or acute COPD
Aerosol not indicated in pediatric patients
Dosing frequency should not exceed q12hr
Risk of potentially fatal acute asthma
Aerosol not recommended when patient is being switched from PO to inhaled corticosteroids
Risk of localized Candida albicans infections in mouth and pharynx in some patients; mouth must be rinsed after inhalation to reduce risk
Monitor COPD patients for signs and symptoms of pneumonia and lung infection
Risk of more serious or fatal course of chickenpox or measles in susceptible patients (eg, unvaccinated or immunologically unexposed individuals); care must be taken to avoid exposure
Excessive use may suppress hypothalamic-pituitary-adrenal function; monitor closely, especially postoperatively or during periods of stress
Particular care is needed in switching patients from systemic to inhaled corticosteroids; potentially fatal adrenal insufficiency may occur before or afterward; taper withdrawal gradually by reducing daily prednisone dose by 2.5 mg on weekly basis
During stress or severe asthma attack, patients who have been withdrawn from systemic corticosteroids should resume PO corticosteroids immediately
Risk of paradoxical bronchospasm, which may be life-threatening; discontinue, and treat immediately with inhaled SABA
Cardiovascular and central nervous system (CNS) effects may occur as consequences of excess beta-adrenergic stimulation; may result in asthma-related death; caution is advised in patients with cardiovascular or convulsive disorders or thyrotoxicosis
Bone mineral density may decrease after long-term administration of corticosteroids; monitor patients at risk
May decrease growth velocity in children
Risk of cataracts, glaucoma, and increased intraocular pressure
Rare cases of vasculitis (Churg-Strauss syndrome) or other systemic eosinophilic conditions may occur
Use caution in patients with diabetes mellitus; beta2 agonists may increase glucose levels
Use caution in patients with hepatic impairment; may lead to accumulation of fluticasone in plasma; monitor closely; glaucoma: consider eye exams in chronic users
Use caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation
Changes in thyroid status may require dosage adjustments; hyperthyroidism may increase corticosteroids clearance while it may decrease in hypothyroidism
Prolonged corticosteroid use may increase incidence of secondary infection, mask acute infection, prolong or exacerbate viral infections, or limit response to vaccines
Corticosteroids may cause psychiatric manifestations, including depression, euphoria, insomnia, mood swings, and personality changes; may also exacerbate preexisting psychiatric conditions
Laryngeal spasm, irritation and swelling (choking) may occur
Risk of transient hypokalemia; supplementation may not be required
Pregnancy & Lactation
Pregnancy category: C
Lactation: Unknown whether agent is excreted in breast milk; salmeterol plasma levels are very low after inhalation
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Salmeterol: Selective LABA; stimulates intracellular adenyl cyclase resulting in increased cAMP levels causing bronchial smooth muscle relaxation; also inhibits release of mediators of immediate hypersensitivity from cells, especially from mast cells
Fluticasone: Trifluorinated corticosteroid with potent anti-inflammatory activity; inhibits multiple cell types (eg, mast cells, eosinophils, basophils, lymphocytes, macrophages, neutrophils) and mediator production or secretion (eg, histamine, eicosanoids, leukotrienes, cytokines) involved in the asthmatic response
Bioavailability: Fluticasone, 5%
Onset (salmeterol): Asthma, 30-48 min; COPD, 2 hr
Onset (fluticasone): >1-2 weeks
Peak plasma time: Fluticasone, 1-2 hr; salmeterol, 20 min
Peak plasma concentration: Fluticasone, 110 pg/mL; salmeterol, 196-223 pg/mL
Time to peak effect (salmeterol): Asthma, 3 hr; COPD, 2-5 hr
Protein bound: Fluticasone, 99%; salmeterol, 96%
Vd: Fluticasone, 4.2 L/kg
Minimally metabolized, because of minimal absorption
Fluticasone metabolized in liver by CYP3A4 to metabolite with negligible activity; salmeterol extensively metabolized by hydroxylation
Half-life: Fluticasone, 11-12 hr; salmeterol, 5.5 hr
Excretion (fluticasone): Feces (95%), urine (5%)
Excretion (salmeterol): Feces (60%), urine (25%)
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