Version May 2024
Asthma, maintenance/controller (adjunctive agent): Note: Use in combination with an inhaled corticosteroid and not as monotherapy (Ref).
Foradil [Canadian product]: Dry powder inhaler (12 mcg/capsule): Oral inhalation: Contents of 1 capsule inhaled via Aerolizer device every 12 hours (maximum dose: 2 capsules/day) (Ref).
Oxeze Turbuhaler [Canadian product]: Dry powder inhaler (6 or 12 mcg/actuation): Oral inhalation: Initial: 6 or 12 mcg every 12 hours (maximum total daily dose: 24 mcg/day) (Ref).
Chronic obstructive pulmonary disease, maintenance: Note: Depending on symptoms and exacerbation risk, use monotherapy long-acting bronchodilator (long-acting beta agonist or long-acting muscarinic antagonist). In patients with more symptoms (eg, Group B), use in combination with long-acting muscarinic antagonist. In addition, a short-acting bronchodilator is used for intermittent symptom relief (Ref).
US labeling: Perforomist: Nebulization solution: Oral inhalation: 20 mcg twice daily.
Canadian labeling: Foradil: Dry powder inhaler (12 mcg/capsule): Oral inhalation: Contents of 1 or 2 capsules inhaled every 12 hours using Aerolizer device (maximum dose: 4 capsules/day).
Exercise-induced bronchospasm: Note: May consider a combination ICS-formoterol for either an as-needed basis or for maintenance of symptoms (Ref).
Canadian labeling: Oxeze Turbuhaler: Dry powder inhaler (6 or 12 mcg/actuation): Oral inhalation: 6 mcg or 12 mcg at least 15 minutes before exercise on an occasional "as needed" basis (maximum dose: 48 mcg/24-hour period).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing.
(For additional information see "Formoterol: Pediatric drug information")
Note: Dosing provided is for products available in Canada. The product available in the United States is not labeled for use in pediatric patients.
Asthma, maintenance therapy: Note: For asthma control, long-acting beta2-agonists (LABAs) should only be used in combination with inhaled corticosteroids; monotherapy is contraindicated.
Canadian labeling:
Foradil [Canadian product]: Dry powder inhaler: 12 mcg/inhalation:
Children ≥6 years and Adolescents ≤16 years: Oral inhalation: 12 mcg every 12 hours; maximum daily dose: 24 mcg/day.
Adolescents ≥17 years: Oral inhalation: 12 mcg every 12 hours; in severe cases, 24 mcg every 12 hours may be necessary; maximum daily dose: 48 mcg/day.
Oxeze Turbuhaler [Canadian product]: Dry powder inhaler: 6 mcg/inhalation and 12 mcg/inhalation:
Children ≥6 years and Adolescents ≤16 years: Oral inhalation: 6 mcg or 12 mcg every 12 hours; maximum daily dose: 24 mcg/day.
Adolescents ≥17 years: Oral inhalation: 6 mcg or 12 mcg every 12 hours; in severe cases, 24 mcg every 12 hours may be necessary; maximum daily dose: 48 mcg/day.
Exercise-induced bronchospasm, prevention:
Note: If already using formoterol in combination with inhaled corticosteroids for asthma maintenance, then patients should not use additional doses for exercise-induced bronchospasm. Because long-acting beta2-agonists (LABAs) may disguise poorly-controlled persistent asthma, frequent or chronic use of LABAs for exercise-induced bronchospasm is discouraged by asthma guidelines (Ref). Tolerance to the protective effects of LABAs against exercise-induced bronchospasm may develop with regular use (ie, daily) (Ref).
Canadian labeling: Oxeze Turbuhaler [Canadian product]: Dry powder inhaler: 6 mcg/inhalation and 12 mcg/inhalation:
Children ≥6 years and Adolescents: Oral Inhalation: 6 mcg or 12 mcg before exercise on an occasional "as needed" basis; maximum daily dose: 24 mcg/day.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Cardiovascular: Chest pain (2% to 3%)
Central nervous system: Anxiety (2%), dizziness (2%), insomnia (2%), voice disorder (1%), headache
Dermatologic: Pruritus (2%), skin rash (1%)
Gastrointestinal: Diarrhea (5%), nausea (5%), xerostomia (1% to 3%), vomiting (2%), abdominal pain, dyspepsia, gastroenteritis
Neuromuscular & skeletal: Muscle cramps (2%), tremor
Respiratory: Respiratory tract infection (3% to 7%), exacerbation of asthma (ages 5 to 12 years: 5% to 6%; age >12 years: <4%; acute deterioration: <1%), bronchitis (5%), pharyngitis (3% to 4%), sinusitis (3%), dyspnea (2%), tonsillitis (1%)
Miscellaneous: Fever (2%)
<1%, postmarketing, and/or case reports: Agitation, anaphylaxis (including severe hypotension/angioedema), angina pectoris, atrial fibrillation, behavioral changes, cardiac arrhythmia, cough, decreased glucose tolerance, dermatitis, disturbed sleep, dysgeusia, fatigue, hyperglycemia, hypertension, hypokalemia, malaise, metabolic acidosis, muscle spasm, nervousness, palpitations, paradoxical bronchospasm, prolonged QT interval on ECG, restlessness, tachycardia, urticaria, variable blood pressure, ventricular premature contractions
Monotherapy (without use of a concomitant inhaled corticosteroid) in the maintenance treatment of asthma.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to formoterol or any component of the formulation; presence of tachyarrhythmias.
Concerns related to adverse effects:
• Asthma-related deaths: Use of long-acting beta-2 agonists (LABAs) as monotherapy (without inhaled corticosteroids) is associated with an increased risk of asthma-related death, asthma-related hospitalizations in pediatric and adolescent patients, and an increased risk of severe exacerbations (SMART 2006; Walters 2007). Data from large randomized, double-blind controlled trials do not show a significant increase in risk of serious asthma-related events (including hospitalizations, intubations, and death) in adults, adolescents, and pediatric patients when fixed-dose LABAs are used with inhaled corticosteroids combined in a single inhaler compared with inhaled corticosteroid monotherapy (FDA 2017). Current asthma guidelines recommend the use of an as-needed low dose inhaled corticosteroid with formoterol as the preferred reliever agent (GINA 2023).
• Bronchospasm: Paradoxical bronchospasm (which can be life-threatening) may occur with use of inhaled agents; this reaction should be distinguished from inadequate response. Discontinue immediately if paradoxical bronchospasm occurs and institute alternative therapy.
• Hypersensitivity reactions: Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) have been reported.
• Serious effects/fatalities: Do not exceed recommended dose or frequency or use with other medications containing LABAs; serious adverse events, including fatalities, have been associated with excessive use of inhaled sympathomimetics.
Disease-related concerns:
• Asthma: Appropriate use:
- Foradil [Canadian product]: Not indicated for the initial (rescue) treatment of acute episodes of bronchospasm. Do not initiate in patients with significantly worsening or acutely deteriorating asthma; reports of severe (sometimes fatal) respiratory events have been reported when formoterol has been initiated in this situation.
- Perforomist: Not FDA approved for the treatment of asthma; safety and efficacy in asthma patients have not been established with this product.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (arrhythmia, coronary insufficiency, or hypertension); beta-agonists may cause elevation in blood pressure and heart rate and result in CNS stimulation/excitation. Beta-2 agonists have been reported to produce ECG changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression.
• Chronic obstructive pulmonary disease: Appropriate use: Do not use for acute episodes of COPD. Do not initiate in patients with significantly worsening or acutely deteriorating COPD. Available data do not suggest an increased risk of death with use of LABAs in patients with COPD.
• Diabetes: Use with caution in patients with diabetes mellitus; beta-2 agonists may increase serum glucose and aggravate preexisting diabetes mellitus and ketoacidosis.
• Exercise-induced bronchospasm: Because LABAs may disguise poorly controlled persistent asthma, frequent or chronic use of LABAs for exercise-induced bronchospasm is discouraged (ATS [Parsons 2013]).
• Hyperthyroidism: Use with caution in hyperthyroidism; may stimulate thyroid activity.
• Hypokalemia: Use with caution in patients with hypokalemia; beta-2 agonists may transiently decrease serum potassium.
• Seizures: Use with caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation.
Special populations:
• Pediatric: Foradil [Canadian product]: LABAs, when used as monotherapy, may increase the risk of asthma-related hospitalization in pediatric and adolescent patients. When LABAs are used in a fixed-dose combination with inhaled corticosteroids, data from large clinical trials in adolescents do not show a significant increase in the risk of serious asthma-related events (hospitalizations, intubations, death) compared to inhaled corticosteroids alone.
Dosage form specific issues:
• Foradil [Canadian product]: The contents of the capsules are for inhalation only via the Aerolizer device. There have been reports of incorrect administration (swallowing of the capsules).
• Lactose: Powder for oral inhalation may contain lactose; very rare anaphylactic reactions have been reported in patients with severe milk protein allergy.
Other warnings/precautions:
• Patient information: Patients using inhaled, short-acting beta-2 agonists should be instructed to discontinue routine use of these medications prior to beginning treatment; short-acting agents should still be provided to patients; however, use should be reserved for symptomatic relief of acute symptoms. Patients must be instructed to seek medical attention in cases where acute symptoms are not relieved or a previous level of response is diminished. The need to increase frequency of use of short-acting beta-2 agonists may indicate deterioration of asthma or COPD, and medical evaluation must not be delayed.
• Tolerance/Tachyphylaxis: Tolerance to the bronchodilator effect, measured by FEV1, has been observed in studies.
Foradil Aerolizer is no longer available in the US.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Nebulization Solution, Inhalation, as fumarate dihydrate:
Perforomist: 20 mcg/2 mL (2 mL)
Generic: 20 mcg/2 mL (2 mL)
Yes
Nebulization (Formoterol Fumarate Inhalation)
20 mcg/2 mL (per mL): $4.07 - $10.60
Nebulization (Perforomist Inhalation)
20 mcg/2 mL (per mL): $11.15
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Aerosol Powder Breath Activated, Inhalation:
Oxeze Turbuhaler: 6 mcg/actuation (51.4 g); 12 mcg/actuation (51.4 g) [contains lactose]
Capsule, Inhalation, as fumarate:
Foradil: 12 mcg [DSC] [contains milk protein]
Foradil [Canadian product]: Dry powder inhaler (capsule): For oral inhalation only (do not swallow capsules); administer at the same time each day. Remove capsule from blister pack immediately before use. Place capsule directly into capsule chamber of the Aerolizer inhaler; close inhaler and pierce capsule by pressing both blue side buttons simultaneously once only and then release. Exhale fully (do not exhale into inhaler) then close lips tightly around mouthpiece; inhale a deep breath through the mouthpiece; hold breath for as long as possible. If any powder remains in capsule, exhale and inhale again. Repeat until capsule is empty. Small pieces of gelatin may reach the mouth or throat after inhalation (minimized by not piercing capsule more than once); if this occurs, capsule is made of edible gelatin and is not harmful if ingested. Throw away empty capsule; do not leave in inhaler. If mouthpiece needs cleaning, wipe with a dry cloth or small soft brush.
Oxeze Turbuhaler [Canadian product]: Dry powder inhaler: Hold inhaler upright. Turn colored grip as far as it will go in one direction and then turn back to original position; a clicking sound should be heard which means the inhaler is ready for use. Exhale fully. Do not exhale into mouthpiece of inhaler. Place mouthpiece to lips and inhale forcefully and deeply. Do not chew or bite on mouthpiece. Clean outside of mouthpiece once weekly with a dry tissue. Avoid getting inhaler wet. If the inhaler is accidently dropped or shaken, or if the patient exhales into the inhaler, the dose will be lost and a new dose should be loaded.
Perforomist: Nebulization solution: Remove unit-dose vial from foil pouch immediately before use. Solution does not require dilution prior to administration; compatibility with other medications (eg, budesonide, revefenacin) in nebulizer has been reported (Ref); also refer to institution-specific policies. Place contents of unit-dose vial into the reservoir of a standard jet nebulizer connected to an air compressor; assemble nebulizer based on the manufacturer's instructions and turn nebulizer on; breathe deeply and evenly until all of the medication has been inhaled. The average inhalation time is 9 minutes. Discard any unused medication immediately; do not ingest contents of vial. Clean nebulizer after use.
Foradil [Canadian product]: Dry powder inhaler: Remove capsule from blister pack immediately before use. The contents of a capsule are aerosolized via a device called an Aerolizer. Place the capsule into the capsule compartment in the base of the Aerolizer inhaler. Capsules must not be swallowed; must only use the Aerolizer Inhaler. Press both blue buttons only once and then release. Keep inhaler in a level, horizontal position with the blue buttons to the left and right (not up and down) to avoid displacing powder. Exhale fully (with face pointed away from inhaler). Do not exhale into inhaler as this may dislodge powder. Tilt head slightly back and inhale (rapidly, steadily, and deeply). Hold breath as long as possible. If any powder remains in capsule, exhale and inhale again. Repeat until capsule is empty. Throw away empty capsule; do not leave in inhaler. Do not use a spacer with the Aerolizer Inhaler. Always keep capsules and inhaler dry.
Oxeze Turbuhaler [Canadian product]: Dry powder inhaler: To prepare inhaler prior to use, load dose by holding inhaler in upright position and turn greenish-blue grip as far as it will go in one direction and then turn it as far as it will go in the other direction. Prior to first use, this procedure should be done twice; with subsequent dosing, perform this procedure once. Clicking sound means inhaler is loaded with dose and ready for use. Exhale fully. Do not exhale into mouthpiece of inhaler. Place mouthpiece between teeth and close lips over mouthpiece. Inhale deeply and forcefully. Do not chew or bite on mouthpiece. Do not exhale through inhaler. If the Turbuhaler is dropped, shaken, or breathed into after it is loaded, the dose will be lost and a new dose will need to be loaded. Clean outside of mouthpiece once weekly with a dry tissue. Avoid getting inhaler wet. Discard device after a 0 displays in the dose window.
US labeling:
Chronic obstructive pulmonary disease, maintenance: Maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD).
Canadian labeling:
Asthma: Treatment of asthma (only in combination with an inhaled corticosteroid) in ≥6 years of age and adult patients with reversible obstructive airway disease, including patients with symptoms of nocturnal asthma (Foradil, Oxeze Turbuhaler).
Chronic obstructive pulmonary disease, maintenance: Maintenance treatment of COPD (Foradil).
Exercise-induced bronchospasm: Prevention of exercise-induced bronchospasm when administered on an as-needed basis (monotherapy may be indicated in patients without persistent asthma) in ≥6 years of age and adult patients (Oxeze Turbuhaler).
Foradil [CAN] may be confused with Toradol
Foradil capsules for inhalation are for administration via Aerolizer inhaler and are not for oral use.
Foradil [Canada and multiple international markets] may be confused with Fortical brand name for calcium carbonate [LB] and Theradol brand name for tramadol [Netherlands]
Substrate of CYP2C9 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Atomoxetine: May enhance the tachycardic effect of Beta2-Agonists. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Atosiban: Beta2-Agonists may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Risk C: Monitor therapy
Beta2-Agonists (Long-Acting): May enhance the adverse/toxic effect of other Beta2-Agonists (Long-Acting). Risk X: Avoid combination
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Beta2-Agonists. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Risk C: Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Risk X: Avoid combination
Caffeine and Caffeine Containing Products: May enhance the adverse/toxic effect of Formoterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Formoterol. Risk C: Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination
Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider therapy modification
Loop Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Loop Diuretics. Risk C: Monitor therapy
Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Risk X: Avoid combination
Methacholine: Beta2-Agonists (Long-Acting) may diminish the therapeutic effect of Methacholine. Management: Hold long-acting beta2 agonists for 36 hours before methacholine use. Risk D: Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Theophylline Derivatives: Beta2-Agonists may enhance the adverse/toxic effect of Theophylline Derivatives. Specifically, sympathomimetic effects may be increased. Theophylline Derivatives may enhance the hypokalemic effect of Beta2-Agonists. Risk C: Monitor therapy
Thiazide and Thiazide-Like Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Maternal use of beta-2 agonists are not associated with an increased risk of fetal malformations (GINA 2023). Uncontrolled asthma is associated with adverse events in pregnancy (increased risk of perinatal mortality, preeclampsia, preterm birth, low birth weight infants, cesarean delivery, and the development of gestational diabetes). Poorly controlled asthma or asthma exacerbations may have a greater fetal/maternal risk than what is associated with appropriately used asthma medications. Maternal treatment improves pregnancy outcomes by reducing the risk of some adverse events (eg, preterm birth, gestational diabetes) (ERS/TSANZ [Middleton 2020]; GINA 2023).
Formoterol may be used when a long-acting beta-2 agonist (LABA) is needed for the management of asthma in pregnancy. Patients adequately controlled on formoterol for asthma may continue therapy; if initiating treatment during pregnancy, use of a LABA with more data in pregnant patients may be preferred (ERS/TSANZ [Middleton 2020]). Stepping down controller treatment is not recommended during pregnancy (GINA 2023). Maternal asthma symptoms should be monitored monthly (ERS/TSANZ [Middleton 2020], GINA 2023).
Beta agonists may interfere with uterine contractility if administered during labor.
Data collection to monitor pregnancy and infant outcomes associated with asthma and the medications used to treat asthma in pregnancy is ongoing. Health care providers are encouraged to enroll exposed pregnant patients in the MotherToBaby Pregnancy Studies conducted by the Organization of Teratology Information Specialists (877-311-8972 or https://mothertobaby.org). Patients may also enroll themselves.
It is not known if formoterol is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Formoterol oral inhalation is considered probably acceptable for use while breastfeeding (ERS/TSANZ [Middleton 2020]).
FEV1, peak flow, and/or other pulmonary function tests; shortness of breath; blood pressure, heart rate; CNS stimulation; serum glucose, serum potassium
Relaxes bronchial smooth muscle by selective action on beta2 receptors with little effect on heart rate. Formoterol has a long-acting effect.
Onset of action: Dry powder inhaler: Within 3 minutes.
Peak effect: Dry powder inhaler: 80% of peak effect within 15 minutes; Nebulization solution: 2 hours.
Duration: Improvement in FEV1 observed for 12 hours in most patients.
Absorption: Rapidly into plasma.
Protein binding: 61% to 64% in vitro at higher concentrations than achieved with usual dosing.
Metabolism: Hepatic via direct glucuronidation and O-demethylation; CYP2D6, CYP2C8/9, CYP2C19, CYP2A6 involved in O-demethylation.
Half-life elimination: Dry powder inhaler: ~10 to 14 hours; Nebulization solution: ~7 hours.
Time to peak: Maximum improvement in FEV1 in 1 to 3 hours.
Excretion:
Children 5 to 12 years: Urine (7% to 9% as direct glucuronide metabolites, 6% as unchanged drug).
Adults: Urine (15% to 18% as direct glucuronide metabolites, 2% to 10% as unchanged drug).
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