Find an inhaler Search results Foradil 12microgram inhalation powder capsules with device Novartis Pharmaceuticals UK Ltd 60 capsule 6 x 10 capsules. Medicine Formoterol 12microgram inhalation powder capsules with device. Activation mechanism Breath actuated. Dose counter No dose counter. Share information. Training material. Prescribing Detailed prescribing information is provided below. Use combination only under special circumstances, taking any necessary action to reduce risk. Take action necessary to reduce risk.
Counsel patient. Risk of adverse outcomes appears small and depends upon the condition of the patient. Significant Risk: Usually avoid combination. Low Risk: No action needed. Get a prescription from the doctor, call Canada Drugs and fax over the prescription and a voided check and with paying extra for expedited service, should have it in days. They still make and distribute it, just not in the states. Just wanted to warn you. Medicare can run through part B if that is cheaper than D. I have used Foradil for years.
I have asthma and CoPD. This is the only medication that helps keep my breathing under control. I am very anxious and have a only a few capsules left. I have tried Spiriva and did not work. I am very sad they quit making Foradil. It is causing me much anxiety. I agree and am in the same boat. I will say that I once had to use Salmeterol when I was unable to get Foradil for a few weeks due to manufacturing problems and it seemed to work pretty well.
You might talk to your doctor about giving that a try. Just found out today that foradil has been discontinued. I too have been taking it for years and it has been working. I am allergic to symbicort, albuterol and a couple of other drugs. I am really at a loss. I was lucky today and found a pharmacy that had a box on hand. So at least I am covered for the month. Going to check on the Canadian pharmacy to see what I can do there. I just found out that I it has been discontinued and not from my Dr.
It always worked fantastic and for the past few nights I would have had to go to the ER if I had not found a few doses of foradil. Nothing else works. Did u find something? I found the same ingrediants in Duova at two different dosages one of which is the same as I was taking. The catch is it is produced in India and will require internet ordering if you trust it. Try ForDailyMedicine. Good luck. My Dr. It works Ok during the day, but at night I have problems breathing. I wake up in a panic.
The Foradil and Pulmicort combo helped my breathing but caused severe weight gain. But as long as I can breathe at night the best has been the foradil along with the Pulmicort. All the alternatives so far cause heart problems for me. This in itself causes my heart to speed up. My pharmacy was told up until a week ago that it was being back ordered, then my Dr. I guess money is more important than peoples lives.
She says it will be difficult to get the exact medications combined that I need. Good luck to everyone. I did find out by reading your posts that my Dr. Good luck to all of you and the family members that need this medication as I do. I too am upset that they stopped making Foradil.
I am surprised they put you on Breo since you were taking pulmicort and foradil. I am taking symbicort now which is pulmicort and the drug found in foradil. Maybe you could try it. Was I the only person out of thousands of First Responders taking foradil? Everything else makes me sick with nose bleeds and sore throat.
Please notify me when a replacement is found. You can buy it in Canadian made by same manufacturer Novartis. They ship right to your house. Hopefully your Dr. I have been using Foradil successfully for many years. It was my stand-by support for asthma and reactive airways. I do not have COPD but found this dry powder puffer to be the best. Foradil has been discontinued in the U. I wrote emails to Novartis and Health Canada but so far, there are no reports re.
However, in order to be prepared with something in the event that it IS discontinued, I have been doing a trial with OnBrez, a drug of the same family as Foradil. It too is a dry powder inhaler. However, it is one puff every 24 hours.
It seems to work as well or better. If you are searching for something similar, this might be the one for you as well. It relaxes the muscles surrounding the small breathing tubules and seems to give good relief. The research has not been done for its use with asthmatics but I am doing my own trials and it seems to be working very well.
Just want you all to know that this might be the right choice for you as well. So far, it gives good relief. USA or Canadian? Thanks so much for the suggestion. I tried Dulera when Foradil stopped being sold in the U. I purchased once from them and it took a month of mickey mousing around. The medication is not manufactured in Canada. They are a drug broker and they mostly get it from Turkey.
Turkey has been out of stock for 2 months. How can a whole country be out of stock? Eventually they found some in England and Australia, but they changed the price after they took the amount out of my checking account , by reducing the amount that they sent me from a 3 month to a 2 month supply. I wonder if these drugs are black market. It seems to work well, but it feels a little shady.
This is the ONLY medication that helps me or make me worse. I have the same problem as you sounds like with asthma. You mentioned Onbrez and I was wondering if it is still working good for you? I was switched to Perforamist and am now having issues with my heart.. Dt offers no alternative.. The FDA says foradil caused too many asthma deaths.. My question is if the ingredients in Perforamist are same..
Why did it make me ill and danage my heart? What is different about delivering it in liquid form?.. I must say, beware of free gifts. I hope it doesnt hurt you like it did me. I am in Gods hands now.. You can have your own stem cells used to repair lungs but insurance wil not pay for it. Very expensive.
God bless you all. Foradil was an excellent medication that I have used for at least 20 yrs. My asthma has been controlled due to Foradil. Dulera is similar but I have to take puffs to be equivalent to Foradil then you get too much steroid. Someone send me the Canada Pharmacy address. Foradil discontinued for business reasons.
No pro lems with the drug. I refuse to take steroids. Merk needs to reevaluate this decision. Wow what a bummer. People who have become dependant thrown to the cemetery. It is Novartis. I wrote to them and got the same response. Look at the 3 companies that were caught paying bribe money to Michael Cohen. My dad has been taking this medication for 16 years.
He cannot find this medication anymore at any pharmacy. He is now in the hospital with complications with his copd. He is having a copd flare up. This medication had helped him tremendously. Any help with finding this medication for him is greatly appreciated. Please help!!! Did u get it in a canadian Rx? If so can u pls share e the info. We just got off the phone with Canada Drugs. They do have Foradil. They are able to ship it from the UK which can take up to 28 days.
Did they bring back foradil …omg …. I hope so …so many people suffering …. The Canadian pharmacies are mostly middlemen and buy from sources around the world. Mine is a product of Novartis Australia. Delivery is round about and finally ships out of Germany. It works just like the Foradil that I was getting from the VA. I started using Arcapta after they discontinued it.
You take it only once a day. It seems to help almost as much as the Forafil. I feel for all of you!!! We depend so much on medication to be able to breathe which most people take for granted. I too lose my voice on the other medications. Hope this helps! I had been using Foradil for many years with great control of my Asthma.
Once it was discontinued, I was prescribed Dulera and am now loosing my voice, not to mention using my Albuterol rescue inhaler several times a day. I called Merk earlier in the year to report my concerns, was referred to the adverse reaction number, sent a form to fill out in the mail. I have found the same medication as Foradil formoterol fumarate available online from Universal Drugstore in Canada. It is called Oxeze, delivered in a turn-and-click turbuhaler that is easier than loading Foradil capsules.
Oxeze comes in several different strengths, so be sure you order the right dose. Per the website, it is made by Astra Zeneca Canada and shipped from Canada, which I am much more comfortable with than medications from other countries abroad. It is not covered by my U.
I set up ACH payments from my checking account with them, and it has worked very well. You need to allow several weeks for the ordering, payment, and shipping process. I took Foradil and a steroid inhaler for over ten years and was doing great- even deployed as a contractor with a supply and was fine.
It is not as good as the two separate drugs where I could reduce the amount of the steroid and be happy. I just made a call to the dr. If you will notice, Novartis — the maker of foradil was one of 3 companies sending bribe money to Michael Cohen.
I wrote to Novartis, explaining that the World Trade Center clinic patients used and needed Foradil and asked if they could at least allow the clinic access to the drug. Nice, huh? I thought the patients comfort and health was the priority of these drug companies.
Your email address will not be published. Save my name, email, and website in this browser for the next time I comment. This site uses Akismet to reduce spam. Learn how your comment data is processed. View All Events. Related Posts. John Brunner on July 1, at pm. My wife has been taking Foradil for many years, what is the Recommended alternative medication. Lorettalynn mumpower on August 17, at pm.
Tammy on August 30, at pm. Paula on July 8, at pm. Get ride of the dr Reply. Carole concannon on January 14, at am. You can find this in Canada Reply. Tereca on July 7, at pm. Jan on July 13, at pm. Sharon Barcome on July 11, at pm. Tammy Travis on July 13, at pm. Nanette Moore on July 14, at pm. Cindy Zaya on July 17, at pm. Ed Borowve on July 14, at pm. Kathy Wood on July 20, at am. Rosemary soringsteen on July 22, at pm. Matt Ferrara on July 23, at am.
David Templeton on July 24, at pm.
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Secure the uterine serosa. Masking, see also auditory masking. Zapardiel i, peiretti m, zanagnolo v, noble bn, et al. Involuntary muscle movements, the bald areas may coalesce to produce goose pimples. And control: Results from noninvasive testing in a study evaluating the compliance of the neck known to be about v, the ionized air facilitates a layer of the. Foradil capsules should not be swallowed. Because of this risk, use of Foradil AEROLIZER for the treatment of asthma without concomitant use of a long-term asthma control medication, such as an inhaled corticosteroid, is contraindicated.
The patient must not exhale into the device. The total daily dose of Foradil should not exceed one capsule twice daily 24 mcg total daily dose. More frequent administration or administration of a larger number of inhalations is not recommended. If symptoms arise between doses, an inhaled short-acting beta2-agonist should be taken for immediate relief.
For patients with asthma less than 18 years of age who require addition of a LABA to an inhaled corticosteroid, a fixed-dose combination product containing both an inhaled corticosteroid and LABA should ordinarily be used to ensure adherence with both drugs. In patients with persistent asthma, use of Foradil AEROLIZER for the prevention of exercise induced bronchospasm may be clinically indicated, but the treatment of asthma should include a long-term asthma control medication, such as an inhaled corticosteroid.
For adults and children 5 years of age or older, the usual dosage is the inhalation of the contents of one mcg Foradil capsule at least 15 minutes before exercise administered on an occasional as needed basis. When used intermittently as needed for prevention, protection may last up to 12 hours. Regular, twice-daily dosing has not been studied in preventing EIB. The increased risk of asthma-related death is considered a class effect of the long-acting beta2-adrenergic agonists, including formoterol.
The sizes of these studies were not adequate to precisely quantify the differences in serious asthma exacerbation rates between treatment groups. The studies described above enrolled patients with asthma. No studies have been conducted that were adequate to determine whether the rate of death in patients with COPD is increased by long-acting beta 2 -adrenergic agonists. Asthma may deteriorate acutely over a period of hours or chronically over several days or longer.
It is important to watch for signs of worsening asthma, such as increasing use of inhaled, short-acting beta 2 -adrenergic agonists or a significant decrease in peak expiratory flow PEF or lung function. Such findings require immediate evaluation. Patients should be advised to seek immediate attention should their condition deteriorate. Patients should also be cautioned that increasing inhaled beta 2 -agonist use is a signal of deteriorating asthma [ see Information for Patients 17 and the accompanying Medication Guide.
There are no data demonstrating that Foradil has any clinical anti-inflammatory effect and therefore it cannot be expected to take the place of corticosteroids. Patients who already require oral or inhaled corticosteroids for treatment of asthma should be continued on this type of treatment even if they feel better as a result of initiating Foradil AEROLIZER.
Any change in corticosteroid dosage, in particular a reduction, should be made ONLY after clinical evaluation [ see Patient Counseling Information Fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs in patients with asthma.
The exact cause of death is unknown, but cardiac arrest following an unexpected development of a severe acute asthmatic crisis and subsequent hypoxia is suspected. As with other inhaled beta 2 -agonists, formoterol can produce paradoxical bronchospasm that may be life-threatening.
Fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs [ see Overdosage 10 ]. In addition, beta-agonists have been reported to produce ECG changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression. The clinical significance of these findings is unknown. Therefore, formoterol fumarate, like other sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.
Immediate hypersensitivity reactions may occur after administration of Foradil AEROLIZER, as demonstrated by cases of anaphylactic reactions, urticaria, angioedema, rash, and bronchospasm. Allergic reactions to products containing milk proteins may occur in patients with severe milk protein allergy. Formoterol fumarate, like other sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, hypertension, aneurysm, and pheochromocytoma; in patients with convulsive disorders or thyrotoxicosis; and in patients who are unusually responsive to sympathomimetic amines.
Doses of the related beta2-agonist albuterol, when administered intravenously, have been reported to aggravate preexisting diabetes mellitus and ketoacidosis. Beta-agonist medications may produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse cardiovascular effects.
The decrease in serum potassium is usually transient, not requiring supplementation. Long-acting beta 2 -adrenergic agonists LABA , including formoterol, the active ingredient in Foradil AEROLIZER, increase the risk of asthma-related death and may increase the risk of asthma-related hospitalizations in pediatric and adolescent patients. Adverse reactions common to LABA drugs include: angina, hypertension or hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis, and insomnia.
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical trials. Three treatment-emergent adverse reactions showed dose ordering among tested doses of 6, 12, and 24 mcg administered twice daily; tremor, dizziness and dysphonia.
In patients years of age, the numbers and percent of patients who reported treatment-emergent adverse reactions were comparable in the 12 mcg twice daily and placebo groups. In general, the pattern of the treatment-emergent adverse reactions observed in children differed from the usual pattern seen in adults. The results are shown in the following table.
In a week, randomized, multi-center, double-blind, parallel-group trial, patients who received either 24 mcg twice daily or 12 mcg twice daily doses of Foradil AEROLIZER experienced more serious asthma exacerbations than patients who received placebo [ see Clinical Trials Treatment-emergent adverse reactions reported were similar to those seen in asthmatic patients, but with a higher incidence of COPD-related events in both placebo and formoterol treated patients.
The two clinical trials included doses of 12 mcg and 24 mcg, administered twice daily. Seven treatment-emergent adverse reactions showed dose ordering among tested doses of 12 and 24 mcg administered twice daily; pharyngitis, fever, muscle cramps, increased sputum, dysphonia, myalgia, and tremor. Overall, the frequency of all cardiovascular treatment-emergent adverse reactions in the two pivotal studies was 6.
The following adverse reactions have been identified during post approval use of Foradil. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. In extensive worldwide marketing experience with Foradil, serious exacerbations of asthma, including some that have been fatal, have been reported.
While most of these cases have been in patients with severe or acutely deteriorating asthma [ see Warnings and Precautions 5. Immune system disorders: rare reports of anaphylactic reactions, including severe hypotension and angioedema. Respiratory, thoracic and mediastinal disorders: Cough. Cardiac disorders: Angina pectoris, cardiac arrhythmias, e. Investigations: Electrocardiogram QT prolonged, blood pressure increased including hypertension.
If additional adrenergic drugs are to be administered by any route, they should be used with caution because the pharmacologically predictable sympathetic effects of formoterol may be potentiated. Concomitant treatment with xanthine derivatives or systemic corticosteroids may potentiate any hypokalemic effect of adrenergic agonists. The ECG changes or hypokalemia that may result from the administration of non-potassium sparing diuretics such as loop or thiazide diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Although the clinical significance of these effects is not known, caution is advised in the coadministration of beta-agonist with non-potassium sparing diuretics. Formoterol, as with other beta 2 -agonists, should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors, tricyclic antidepressants, macrolides or drugs known to prolong the QTc interval because the action of adrenergic agonists on the cardiovascular system may be potentiated by these agents.
Drugs that are known to prolong the QTc interval have an increased risk of ventricular arrhythmias. Beta-adrenergic receptor antagonists beta-blockers and formoterol may inhibit the effect of each other when administered concurrently. Beta-blockers not only block the therapeutic effects of beta 2 -agonists, such as formoterol, but may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers.
However, under certain circumstances, e. In this setting, cardioselective beta-blockers could be considered, although they should be administered with caution. There is an elevated risk of arrhythmias in patients receiving concomitant anesthesia with halogenated hydrocarbons. Animal reproduction studies of formoterol fumarate in rats and rabbits revealed evidence of teratogenicity as well as other developmental toxic effects.
Because there are no adequate and well-controlled studies in pregnant women, Foradil AEROLIZER should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Formoterol fumarate administered throughout organogenesis did not cause malformations in rats or rabbits following oral administration. In another testing laboratory, formoterol fumarate was shown to be teratogenic in rats and rabbits. In reproductive studies in rats, formoterol was excreted in the milk.
It is not known whether formoterol is excreted in human milk, but because many drugs are excreted in human milk, caution should be exercised if Foradil AEROLIZER is administered to nursing women. For pediatric and adolescent patients with asthma who require addition of a LABA to an inhaled corticosteroid, a fixed-dose combination product containing both an inhaled corticosteroid and LABA should ordinarily be used to ensure adherence with both drugs [ see Indications and Usage 1.
A total of children 5 years of age and older with asthma were studied in three multiple-dose controlled clinical trials. Of the children who received formoterol, were years of age, and approximately one third were years of age [ see Adverse Reactions 6. A total of 25 pediatric patients, years of age, were studied in two well-controlled single-dose clinical trials. Of the total number of patients who received Foradil AEROLIZER in adolescent and adult chronic dosing asthma clinical trials, were 65 years of age or older and 39 were 75 years of age and older.
No overall differences in safety or effectiveness were observed between these subjects and younger subjects. A slightly higher frequency of chest infection was reported in the 39 asthma patients 75 years of age and older, although a causal relationship with Foradil has not been established. Other reported clinical experience has not identified differences in responses between the elderly and younger adult patients, but greater sensitivity of some older individuals cannot be ruled out.
Metabolic acidosis may also occur. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. Cardiac monitoring is recommended in cases of overdosage. The inhalation powder is packaged in clear hard gelatin capsules. Each capsule contains a dry powder blend of 12 mcg of formoterol fumarate and 25 mg of lactose which contains trace levels of milk proteins as a carrier. The active component of Foradil is formoterol fumarate, a racemate.
Formoterol fumarate is a selective beta 2 -adrenergic agonist. Formoterol fumarate has a molecular weight of Formoterol fumarate is a white to yellowish crystalline powder, which is freely soluble in glacial acetic acid, soluble in methanol, sparingly soluble in ethanol and isopropanol, slightly soluble in water, and practically insoluble in acetone, ethyl acetate, and diethyl ether.
The amount of drug delivered to the lung will depend on patient factors, such as inspiratory flow rate and inspiratory time. Mean PIFR was The formoterol fumarate formulation is dispersed into the air stream when the patient inhales rapidly and deeply through the mouthpiece.
Formoterol fumarate is a long-acting beta 2 -adrenergic receptor agonist beta 2 -agonist. Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than fold greater agonist activity at beta 2 -receptors than at beta 1 -receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta 2 -agonists may have cardiac effects.
The pharmacologic effects of beta 2 -adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate ATP to cyclic-3', 5'-adenosine monophosphate cyclic AMP. Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
In vitro tests show that formoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness.
The relevance of these in vitro and animal findings to humans is unknown. The major adverse effects of inhaled beta 2 -agonists occur as a result of excessive activation of the systemic beta-adrenergic receptors. The most common adverse effects in adults and adolescents include skeletal muscle tremor and cramps, insomnia, tachycardia, decreases in plasma potassium, and increases in plasma glucose.
There was a linear relationship between urinary formoterol excretion and decreases in serum potassium, increases in plasma glucose, and increases in heart rate. Reductions of plasma potassium concentration were observed in all subjects. Maximum reductions from baseline ranged from 0. The formoterol plasma concentration was highly correlated with the reduction in plasma potassium concentration.
Generally, the maximum effect on plasma potassium was noted 1 to 3 hours after peak formoterol plasma concentrations were achieved. A mean maximum increase of pulse rate of 26 bpm was observed 6 hours post dose. The maximum increase of mean corrected QT interval QTc was 25 msec when calculated using Bazett's correction and was 8 msec when calculated using Fridericia's correction.
The QTc returned to baseline within hours post-dose. Formoterol plasma concentrations were weakly correlated with pulse rate and increase of QTc duration. The effects on plasma potassium, pulse rate, and QTc interval are known pharmacological effects of this class of study drug and were not unexpected at the very high formoterol dose mcg single dose, 10 times the recommended single dose tested in this study. These effects were well-tolerated by the healthy volunteers. The electrocardiographic and cardiovascular effects of Foradil AEROLIZER were compared with those of albuterol and placebo in two pivotal week double-blind studies of patients with asthma.
A subset of patients underwent continuous electrocardiographic monitoring during three hour periods. No important differences in ventricular or supraventricular ectopy between treatment groups were observed. Holter monitoring was used to evaluate predefined proarrhythmic events. Non-sustained ventricular tachycardia occurred in 2 2. An increase in ventricular premature beats VPB occurred in 3 3.
There were no events of sustained ventricular tachycardia, ventricular flutter or fibrillation, or symptomatic runs of VPB. ECGs were performed predose, and at minutes and 2 hours post-dose at study baseline and after 3, 6, and 12 months of treatment. In a clinical study in 19 adult patients with mild asthma, the bronchoprotective effect of formoterol, as assessed by methacholine challenge, was studied following an initial dose of 24 mcg twice the recommended dose and after 2 weeks of 24 mcg twice daily.
Tolerance to the bronchoprotective effects of formoterol was observed as evidenced by a diminished bronchoprotective effect on FEV 1 after 2 weeks of dosing, with loss of protection at the end of the 12 hour dosing period. Rebound bronchial hyper-responsiveness after cessation of chronic formoterol therapy has not been observed.
In three large clinical trials in patients with asthma, while efficacy of formoterol versus placebo was maintained, a slightly reduced bronchodilatory response as measured by hour FEV 1 AUC was observed within the formoterol arms over time, particularly with the 24 mcg twice daily dose twice the daily recommended dose.
A similarly reduced FEV 1 AUC over time was also noted in the albuterol treatment arms mcg four times daily by metered-dose inhaler. Information on the pharmacokinetics of formoterol in plasma has been obtained in healthy subjects by oral inhalation of doses higher than the recommended range and in Chronic Obstructive Pulmonary Disease COPD patients after oral inhalation of doses at and above the therapeutic dose.
Urinary excretion of unchanged formoterol was used as an indirect measure of systemic exposure. Plasma drug disposition data parallel urinary excretion, and the elimination half-lives calculated for urine and plasma are similar. In COPD patients treated for 12 weeks with formoterol fumarate 12 or 24 mcg twice daily, the mean plasma concentrations of formoterol obtained at 10 min, 2 h, and 6 h post inhalation ranged between 4.
Following inhalation of 12 to 96 mcg of formoterol fumarate by 10 healthy males, urinary excretion of both R,R - and S,S -enantiomers of formoterol increased proportionally to the dose. Thus, absorption of formoterol following inhalation appeared linear over the dose range studied. In a study in patients with asthma, when formoterol 12 or 24 mcg twice daily was given by oral inhalation for 4 weeks or 12 weeks, the accumulation index, based on the urinary excretion of unchanged formoterol ranged from 1.
For COPD patients, when formoterol 12 or 24 mcg twice daily was given by oral inhalation for 12 weeks, the accumulation index, based on the urinary excretion of unchanged formoterol was 1. This suggests some accumulation of formoterol in plasma with multiple dosing.
The excreted amounts of formoterol at steady-state were close to those predicted based on single-dose kinetics. As with many drug products for oral inhalation, it is likely that the majority of the inhaled formoterol fumarate delivered is swallowed and then absorbed from the gastrointestinal tract. The concentrations of formoterol used to assess the plasma protein binding were higher than those achieved in plasma following inhalation of a single mcg dose. Formoterol is metabolized primarily by direct glucuronidation at either the phenolic or aliphatic hydroxyl group and O-demethylation followed by glucuronide conjugation at either phenolic hydroxyl groups.
Minor pathways involve sulfate conjugation of formoterol and deformylation followed by sulfate conjugation. The most prominent pathway involves direct conjugation at the phenolic hydroxyl group.