budesonide/formoterol/glycopyrrolate

Contraindicated in:

Hypersensitivity;
Asthma;
Acutely deteriorating COPD or acute respiratory symptoms.

Use Cautiously in:

Systemic corticosteroid therapy (should not be abruptly discontinued when inhaled therapy is started; additional corticosteroids needed during stress or trauma);
Prolonged immobilization, family history of osteoporosis, postmenopausal status, cigarette smoking, advanced age, or poor nutrition (↑ risk of osteoporosis);
Narrow-angle glaucoma;
Seizure disorders;
Thyrotoxicosis;
Urinary retention, prostatic hyperplasia, bladder-neck obstruction;
Diabetes;
Severe hepatic impairment;
Severe renal impairment or end-stage renal disease requiring dialysis (use only if expected benefit exceeds potential risk);
OB: Safety not established in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Exercise Extreme Caution in:

Concurrent use of MAO inhibitors, tricyclic antidepressants, or drugs that prolong the QTc interval.

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias, hypertension, tachycardia

EENT: cataracts, glaucoma, sinusitis

Endo: adrenal suppression (high dose, long-term therapy only), hyperglycemia

F and E: hypokalemia

GI: diarrhea, oropharyngeal candidiasis

MS: ↓bone density, muscle spasms

Resp: bronchospasm, cough, pneumonia

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA, URTICARIA, OR RASH)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including atazanavir, clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, and ritonavir, may ↑ levels and risk of toxicity.
Anticonvulsants, oral corticosteroids, and proton pump inhibitors may ↑ risk of osteoporosis.
Concurrent use with other adrenergics may ↑ adrenergic adverse reactions of formoterol (↑ heart rate, ↑ BP, jitteriness).
Xanthine derivatives, corticosteroids, and diuretics may ↑ risk of hypokalemia or ECG changes with formoterol.
↑risk of serious adverse cardiovascular effects with MAO inhibitors, tricyclic antidepressants, and QT interval prolonging drugs; use with extreme caution.
Effectiveness of formoterol may be ↓ by beta blockers; use cautiously and only when necessary.
↑risk of anticholinergic adverse reactions with glycopyrrolate when used concurrently with other anticholinergics; avoid concurrent use.

Availability ⬆ ⬇

Inhalation aerosol: budesonide 160 mcg/glycopyrrolate 9 mcg/formoterol 4.8 mcg per inhalation in 10.7-g canister (120 inhalations)

Route/Dosage ⬆ ⬇

Inhaln (Adults ): 2 inhalations twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Budesonide: Potent, locally acting anti-inflammatory; formoterol: a beta₂-adrenergic agonist that stimulates adenyl cyclase, resulting in accumulation of cyclic adenosine monophosphate at beta₂-adrenergic receptors resulting in bronchodilation; glycopyrrolate: acts as an anticholinergic by inhibiting M3 muscarinic receptors in bronchial smooth muscle resulting in bronchodilation.

Therapeutic effects:

Bronchodilation with decreased airflow obstruction.

Classifications ⬆ ⬇

Therapeutic Classification: corticosteroids, bronchodilators

Pharmacologic Classification: corticosteroids, long-acting beta2-adrenergic agonists (LABAs), anticholinergics

Pharmacokinetics ⬆ ⬇

Budesonide

Absorption: Unknown.

Distribution: Extensively distributed to extravascular tissues.

Metabolism/Excretion: Primarily metabolized by the liver by the CYP3A4 isoenzyme into inactive metabolites; primarily excreted in urine and feces as metabolites.

Half-Life: 5 hr.

Formoterol

Absorption: Unknown.

Distribution: Extensively distributed to extravascular tissues.

Metabolism/Excretion: Primarily metabolized by the liver by glucuronidation and O-demethylation to inactive metabolites; 62% of drug excreted in urine; 24% excreted in feces.

Half-Life: 10 hr.

Glycopyrrolate

Absorption: Unknown.

Distribution: Extensively distributed to extravascular tissues.

Metabolism/Excretion: Primarily metabolized by the liver, with the CYP2D6 isoenzyme playing a minor role in elimination; 85% excreted in urine.

Half-Life: 15 hr.

Time/Action Profile ⬆ ⬇

( improvement in FEV₁)

ROUTE	ONSET	PEAK	DURATION
Inhalation	within 5 min	4 wk	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct to use as directed. Do not discontinue therapy without discussing with health care professional, even if feeling better. If a dose is missed, skip dose and take next dose at regularly scheduled time. Do not double doses. Use a rapid-acting bronchodilator if symptoms occur before next dose is due. Caution patient not to use >2 times a day; may cause adverse effects, paradoxical bronchospasm, or loss of effectiveness of medication.
Advise patient to consult health care professional before taking any Rx, OTC, or herbal products or alcohol concurrently with this therapy. Caution patient also to avoid smoking and other respiratory irritants.
Advise patient that inhaler should be discarded when display window indicates zero or 3 mo (120-inhalation canister) or 3 wk (28-inhalation canister) after removal of canister from pouch, whichever comes first. Never immerse the canister into water to determine the amount remaining in the canister ("float test").
Caution patient not to use medication to treat acute symptoms. A rapid-acting inhaled beta-adrenergic bronchodilator should be used for relief of acute asthma attacks. Notify health care professional immediately if symptoms get worse or more inhalations than usual are needed from rescue inhaler.
Advise patient to rinse the mouth with water without swallowing after inhalation to help ↓ the risk of getting a fungus infection (thrush) in the mouth and throat.
Instruct patient to contact health care professional immediately if shortness of breath is not relieved by medication or if nausea; vomiting; shakiness; headache; fast or irregular heartbeat; sleeplessness; or signs and symptoms of narrow-angle glaucoma (eye pain or discomfort, blurred vision, visual halos or colored images, red eyes), urinary retention (difficulty passing urine, painful urination), or pneumonia (increase in mucus [sputum] production, change in mucus color, fever, chills, ↑ cough, ↑ breathing problems) occur.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Classifications ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆