albuterol (Proventil HFA, Ventolin HFA, Proair HFA, ProAir RespiClick, Proventil, AccuNeb, Ventolin Injection, Ventolin Nebules PF, Ventolin Oral Liquid, Ventolin Respirator Solution, Vospire ER)

Dosing and uses of Proventil HFA, Ventolin HFA (albuterol)

• Adult
• Pediatric

 

Adult dosage forms and strengths

aerosol metered-dose inhaler

• 90mcg (base)/actuation (equivalent to 108mcg albuterol sulfate)

powder metered-dose inhaler

• 90mcg (base)/actuation (equivalent to 108mcg abluterol sulfate); ProAir RespiClick

tablet

• 2mg
• 4mg

tablet, extended release

• 4mg
• 8mg

nebulizer solution

• 0.083%
• 0.5%
• 1.25mg/3mL
• 0.63mg/3mL

syrup

• 2mg/5mL

 

Bronchospasm

Nebulizer solution: 2.5 mg BID/TID PRN; 1.25 - 5 mg q4-8hr PRN for quick relief

Aerosol metered-dose inhaler: 180 mcg (2 puffs) inhaled PO q4-6hr; not to exceed 12 inhalations/24 hr

Powder metered-dose inhaler: 180 mcg (2 puffs) inhaled PO q4-6hr; not to exceed 12 inhalations/24 hr; in some patients 1 inhalation (90 mcg) q4hr may be sufficient

Tablet and syrup: 2-4 mg PO q6-8hr; not to exceed 32 mg/day

Extended release: 8 mg PO q12hr; in some patients 4 mg PO q12hr sufficient; not to exceed 32 mg/day

 

Acute or Severe Bronchospasm

Nebulizer solution: 2.5-5 mg q20min for 3 doses; follow with 2.5-10 mg q1-4hr PRN or 10-15 min by continuous nebulization

Metered-dose inhaler: 4-8 puffs inhaled q20min for up to 4 hr and then q1-4hr PRn

 

Exercise-Induced Bronchospasm

Aerosol or powder metered-dose inhaler: 180 mcg (2 puffs) inhaled 15-30 min before exercise

 

Spinal Cord Injury (Orphan)

Prevention of paralysis caused by spinal cord injury

Orphan indication sponsor

• MotoGen, Inc, 3 Pine View Road, Mount Kisco, NY 10549

 

Pediatric dosage forms and strengths

aerosol metered-dose inhaler

• 90mcg (base)/actuation (equivalent to 108mcg albuterol sulfate)

powder metered-dose inhaler

• 90mcg (base)/actuation (equivalent to 108mcg abluterol sulfate); ProAir RespiClick

tablet

• 2mg
• 4mg

tablet, extended release

• 4mg
• 8mg

nebulizer solution

• 0.083%
• 0.5%
• 1.25mg/3mL
• 0.63mg/3mL

syrup

• 2mg/5mL

 

Bronchospasm

Treatment and prevention of bronchospasm associated with obstructive airway disease

Aerosol metered-dose inhaler

• <4 years: Safety and efficacy not established
• ≥4 years: 90-180 mcg (1-2 puffs) inhaled PO q4-6 hr

Powder metered-dose inhaler (ProAir RespiClick)

• <4 years: Safety and efficacy not established
• ≥4 years: 180 mcg (2 puffs) inhaled PO q4-6hr; not to exceed 12 inhalations/24 hr
• In some patients 1 inhalation (90 mcg) q4hr may be sufficient

Nebulizer solution

• <2 years (off-label): 0.2-0.6 mg/kg/day divided q4-6hr
• 2-12 years and <15 kg: 2.5 mg/0.5mL (0.5 % solution) q6-8hr; not to exceed 10 mg (4 vials)/24hr
• 2-12 years and >15 kg: 1 vial (2.5 mg/3mL) q6-8hr; not to exceed 10 mg (4 vials)/24hr
• >12 years: 2.5 mg (1 vial) q6-8hr PRN; not to exceed 10 mg/24hr
• Flow rate of delivery adjusted over period of 5-15 minutes

AccuNeB

• <2 years: Safety and efficacy not established
• 2-12 years 1 vial (1.25 or 0.63 mg/vial) q6-8hr inhaled PO via nebulizer over 5-15 min; 4 vials (5 mg)/24 hr
• >12 years: Not studied

Tablet

• <6 years: 0.3-0.6 mg/kg/day PO divided q8hr; not to exceed 12 mg/day
• 6-12 years: 2 mg PO q6-8hr; may be gradually increased to ≤24 mg/day in divided doses
• >12 years: 2-4 mg PO q6-8hr; not to exceed 32 mg/day

Extended Release Tablet

• <6 years: Safety and efficacy not established
• 6-12 years: 4 mg PO q12hr; not to exceed 24 mg/day
• >12 years: 8 mg PO q12hr; in some patients 4 mg q12hr sufficient

Syrup

• 2-6 years: 0.1 mg (0.25 mL)/kg PO q8hr initially, not to exceed 2 mg (5 mL) q8hr; if necessary, may be increased to 0.2 mg/kg PO q8hr, not to exceed 4 mg (10 mL) q8hr
• 6-14 years: 2 mg (5 mL) PO q6-8hr; may be gradually increased to ≤24 mg/day in divided doses
• >14 years: 2-4 mg PO q6-8hr; not to exceed 32 mg/day

 

Exercise Induced Bronchospasm Prevention

Aerosol metered-dose inhaler

• <4 years: Safety and efficacy not established
• ≥4 years: 180 mcg (2 puffs) inhaled 15-30 min before exercise

Powder metered-dose inhaler (ProAir RespiClick)

• <4 years: Safety and efficacy not established
• ≥4 years: 180 mcg (2 puffs) inhaled 15-30 min before exercise

 

Dosing Considerations

Potential toxic dose for children <6 years: 1 mg/kg

 

Proventil HFA, Ventolin HFA (albuterol) adverse (side) effects

>10%

Tremor (20%)

Nervousness in children aged 2-6 years (20%)

Insomnia in children aged 6-12 years receiving 4-12 mg q12hr (11%)

 

1-10%

Nausea (10%)

Fever (1.6-9%)

Bronchospasm (8%)

Vomiting (7%)

Headache (4-7%)

Dizziness (1-7%)

Cough (5%)

Allergic reactions (4%)

Otitis media (3.3%)

Epistaxis in children (3%)

Increased appetite (3%)

Urinary tract infection (3%)

Dry mouth (<3%)

Eructation or flatulence (<3%)

Increased sweating (<3%)

Pain (2.7%)

Dyspepsia (1-2%)

Hyperactivity (1-2%)

Chills (<2%)

Lymphadenopathy (<2%)

Ocular pruritus (<2%)

Sweating (<2%)

Conjunctivitis in children aged 2-6 years (1%)

Dysphonia (>1%)

Flu syndrome

Nervousness

 

<1%

Epigastric pain

Epistaxis in adults

Hyperactivity in children

 

Frequency not defined

Adverse reactions such as hypertension, angina, vertigo, central nervous system stimulation, insomnia, headache, metabolic acidosis, and drying or irritation of oropharynx

Hypersensitivity

Hypokalemia

Increased blood glucose levels

Prolonged QT interval and ST-segment depression

Sleeplessness

Tachycardia (incidence varies with formulation)

Urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema (rare)

 

Warnings

Contraindications

Hypersensitivity to albuteroL

Severe hypersensitivity to milk proteins

 

Cautions

Some inhalers use hydrofluoroalkane (HFA) as propellant instead of chlorofluorocarbons (CFCs); otherwise, devices are equivalent

Hypokalemia and changes in blood glucose may occur

Paradoxical bronchospasm may occur

Need for more doses than usual may be a sign of deterioration of asthma and requires reevaluation of treatment

Use with caution in patients with cardiovascular disease, asthma, glaucoma, diabetes, hypokalemia, hyperthyroidism, or seizures

Use face mask in children <4 years

Excessive use may be fatal; do not exceed recommended dose; serious adverse effects occur when administered dose exceeds recommended dose

May exacerbate heart failure in patients with reduced ejection fraction (dose related increased risk for hospital admission)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Unknown whether drug is excreted in milk; not recommended

 

Pregnancy categories

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.

 

Pharmacology of Proventil HFA, Ventolin HFA (albuterol)

Mechanism of action

Beta2 receptor agonist with some beta1 activity; relaxes bronchial smooth muscle with little effect on heart rate

 

Absorption

Onset: 25 min (Ventolin HFA); 0.5-2 hr (nebulization); 2-3 hr (PO)

Duration: 4-6 hr (PO);

Peak plasma time: Inhalation, 2-5 hr; PO, 2-2.5 hr

 

Distribution

Protein bound: 10%

 

Metabolism

Metabolized in liver

 

Elimination

Half-life: 3-8 hr (inhalation); 3.7-5 hr (PO)

Excretion: Urine

 

Administration

Solution for Nebulization

Remove one vial from the foil pouch

Twist the cap completely off the vial and squeeze the contents into the nebulizer reservoir

Connect the nebulizer to the mouthpiece or face mask

Connect the nebulizer to the compressor

Sit in a comfortable, upright position; place the mouthpiece in your mouth or put on the face mask, and turn on the compressor

Breathe as calmly, deeply and evenly as possible through your mouth until no more mist is formed in the nebulizer chamber (about 5-15 minutes); at this point, the treatment is finished

Clean the nebulizer according to manufacturer instructions

 

Aerosol Metered-Dose Inhaler

For oral inhalation only

Prime the inhaler before using for the first time and in cases where the inhaler has not been used for >2 weeks by releasing 4 “test sprays” into the air, away from the face

Patient instructions for administration

• Shake well before each use
• Breathe out fully through the mouth, expelling as much air from your lungs as possible; place the mouthpiece fully into the mouth, holding the inhaler in its upright position and close the lips around it
• While breathing in deeply and slowly through the mouth, fully depress the top of the metal canister with your index finger
• Hold your breath as long as possible, up to 10 seconds; before breathing out, remove the inhaler from your mouth and release your finger from the canister
• If your physician has prescribed additional puffs, wait 1 minute, shake the inhaler again, and repeat steps listed above; replace the cap after use

Cleaning

• To maintain proper use of this product, it is important that the mouthpiece be washed and dried thoroughly at least once a week
• Keeping the plastic mouthpiece clean is very important to prevent medication buildup and blockage
• The inhaler may cease to deliver medication if not properly cleaned and air dried thoroughly
• If the mouthpiece becomes blocked, washing the mouthpiece will remove the blockage

 

Powder Metered-Dose Inhaler

For oral inhalation only

Does NOT require priming

Do not use with a spacer or volume holding chamber

Cleaning

• Keep clean and dry at all times
• Never wash or put any part of inhaler in water
• Routine maintenance not required
• If the mouthpiece needs cleaning, gently wipe with a dry cloth or tissue as needed

 

Extended-release oral tablets

Do not chew, crush, or mix with food

 

Storage

Solution for nebulization

• Store between 2-25° C (36-77° F)
• Vials should be protected from light before use, therefore, keep unused vials in the foil pouch

Aerosol metered-dose inhaler

• Store at room temperature (15-25°C [59-77°F])

Powder metered-dose inhaler

• Store at room temperature (15-25°C [59-77°F])
• Avoid exposure to extreme heat, cold, or humidity
• Discard 13 months after opening the foil pouch, when the dose counter displays zero, or after the expiration date on the product, whichever comes first