glycopyrrolate/formoterol

Glycopyrrolate: acts as an anticholinergic by inhibiting M3 muscarinic receptors in bronchial smooth muscle resulting in bronchodilation; Formoterol: a beta₂-adrenergic agonist that stimulates adenyl cyclase, resulting in accumulation of cyclic adenosine monophosphate at beta₂—adrenergic receptors resulting in bronchodilation.

Therapeutic effects:

Bronchodilation with decreased airflow obstruction.

Pharmacokinetics ⬆ ⬇

Glycopyrrolate

Absorption: Some systemic absorption from lungs and GI tract (40%).

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP2D6 isoenzyme; eliminated primarily unchanged in the urine and bile.

Half-Life: 33–53 hr.

Formoterol

Absorption: Majority of inhaled drug is swallowed and absorbed.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP2D6 and CYP2C9, and CYP2C19 isoenzymes; 10–18% excreted unchanged in urine.

Half-Life: 10 hr.

Time/Action Profile ⬆ ⬇

(bronchodilation)

ROUTE	ONSET	PEAK	DURATION
formoterol—Inhaln	within 3 min	15 min	unknown
glycopyrrolate—Inhaln	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

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

Use Cautiously in:

History of cardiovascular disorders (coronary insufficiency, arrhythmias, hypertension);
History of seizures;
Thyrotoxicosis;
Narrow-angle glaucoma;
Urinary retention, prostatic hyperplasia, bladder-neck obstruction;
Hepatic impairment;
OB: Formoterol may interfere with uterine contractility during labor; use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

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

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, hypertension, tachycardia

F and E: hypokalemia

GI: dry mouth, vomiting

GU: urinary tract infection

MS: arthralgia, muscle spasms

Neuro: anxiety, dizziness, headache

Resp: cough, paradoxical bronchospasm

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

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with other adrenergics may ↑ adrenergic adverse reactions (↑ heart rate, BP, jitteriness).
↑risk of hypokalemia or ECG changes with xanthine derivatives, corticosteroids, loop diuretics or thiazide diuretics.
↑risk of serious adverse cardiovascular effects with MAO inhibitors, tricyclic antidepressants, QT-interval prolonging drugs; use with extreme caution.
Effectiveness may be ↓ by beta-blockers; use cautiously and only when necessary.
↑risk of anticholinergic adverse reactions when used concurrently with other anticholinergics; avoid concurrent use.

Route/Dosage ⬆ ⬇

Inhaln
(Adults ): 2 inhalations twice daily.

Availability ⬆ ⬇

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

Assessment ⬆ ⬇

Assess lung sounds, pulse, and BP before administration and during peak of medication. Note amount, color, and character of sputum produced.
Monitor pulmonary function tests before initiating and periodically during therapy to determine effectiveness.
Observe for paradoxical bronchospasm (wheezing, dyspnea, tightness in chest) and hypersensitivity reaction (rash; urticaria; swelling of the face, lips, or eyelids). If condition occurs, withhold medication and notify health care professional immediately.
Monitor ECG periodically during therapy. May cause prolonged QTc interval.
Monitor patient for signs of hypersensitivity reactions (difficulties in breathing or swallowing, swelling of tongue, lips and face, urticaria, or skin rash) throughout therapy. Discontinue therapy and consider alternative if reaction occurs.

Lab Test Considerations:

May cause ↑ serum glucose and decreased serum potassium.

Implementation ⬆ ⬇

Inhaln: Administer as 2 inhalations twice daily, morning and evening. Shake well prior to use. Prime by releasing 4 sprays into air away from face before 1st use and by releasing 2 sprays if unused for more than 7 days. See Medication Administration Techniques for use of metered-dose inhalers.

Patient/Family Teaching ⬆ ⬇

Instruct patient to use medication 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 more than 2 times a day; may cause adverse effects, paradoxical bronchospasm, or loss of effectiveness of medication. Instruct patient to review Medication Guide before starting therapy and with each Rx refill in case of changes.
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 clean inhaler each wk so medicine will not build up and block spray through mouthpiece. Take canister out of the actuator, run warm water through actuator, and allowing actuator to air-dry overnight. Shake and reprime with 2 sprays before use.
Instruct patient to contact health care professional immediately if shortness of breath is not relieved by medication or 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) or urinary retention (difficulty passing urine, painful urination) occur.
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.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. May interfere with uterine contractility if used during labor or delivery; use during labor only if the potential benefit justifies the potential risk.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇