Formoterol: Uses, Dosage, Side Effects, and Safety Guidelines

Overview:

The alternative name for Formoterol is a bronchodilator. This drug will dilate your bronchioles. If you have asthma and chronic obstructive pulmonary disease (COPD), you can take this drug with water. These drugs relax your airway channels. A bronchodilator means that this drug will widen your airway channels so that you can breathe easily. It will also relieve you from other asthma symptoms. But if your child is below the age of five, you are advised not to give this drug to your child. The United States FDA (Food and Drug Administration) approved Formoterol fumarate use on September 25, 2001. It is also marketed in combination formulations like Budesonide and Formoterol or Mometasone and Formoterol.

For Patients:

How Is Formoterol Used for Asthma?

During an asthma attack, your airway channels get blocked, and you will find it difficult to breathe. There will also be swelling, and mucus will be excessively produced. The causes can be any dust, chemical fumes, gases, or even any physical activity. Without taking drugs, you will not get any relief. If you have asthma, you can take the Formoterol drug to kill your symptoms. This drug will remove tightness from your airway channels.

How Does Formoterol Work?

Formoterol is a long-acting beta-agonist (LABA). This drug can provide you with symptom-free time for up to 12 hours. However, the short-acting beta agonist, like Salbutamol, will provide you with symptom-free time for only up to five to six hours. It relaxes the airway muscles. However, long-acting beta-agonists will not help you if you are suffering from an acute type of asthma. Even asthma exacerbation can be cured with this type of drug.

Formoterol selectively binds to the beta-2 adrenergic receptors in the bronchial smooth muscles. This activates intracellular adenylyl cyclase and changes it from adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP), resulting in bronchodilation.

What Should I Know About Formoterol Before Using It?

Some measures that you should know about Formoterol before using it:

• You must read the instructions present on the package before using it.

• You should know about the benefits and risks associated with this drug, such as asthma-related hospitalizations and deaths.

• You must be instructed to continue using their long-term asthma control medication, and adding Formoterol to the therapy is not a substitute.

• This drug is not effective against acute asthma. For this, you can take a short-acting beta-agonist.

• You should take only the dose that is prescribed by your doctor.

• If you are symptom-free after taking corticosteroids and Formoterol, you should not change the dose of these two drugs.

• For exercise-induced asthma, you should take this drug 15 minutes before exercise, and for the next 12 hours, you should not take this drug.

• You must not use a Formoterol with a spacer and should never exhale into the device.

• The inhaler must never be washed and should be kept dry. Also, a new inhaler that comes with a refill must be used.

• If you are a pregnant and breastfeeding mother, you should tell your doctor before taking this drug.

• The capsules must be used immediately after removing them from the blister and must be pierced only once.

• The patients must be aware of how to use the inhaler.

Dosage and Administration:

You should use an inhaler to take this drug. You should not directly swallow or ingest this drug. The contents of one 12 mcg capsule must be inhaled every 12 hours using an aerosolized inhaler. You should only inhale, not exhale, into the inhaler. The total daily dose must not exceed 24 mcg. Your doctor can give you short-acting beta-agonists for sudden relief. If you have severe asthma after doing an exercise, Formoterol can be taken. The dosage is one capsule of 12 mcg administered through an inhaler at least 15 minutes before exercise. It may protect for up to 12 hours. In COPD patients, the recommended dosage is one 12 mcg capsule every 12 hours using the aerolizer inhaler. A total daily dose must not exceed 24 mcg.

Missed Dose:

If you did not take the regular dose, you should take it at that time. If you remember the missed dose at the time of the next dose, then you should take the regular dose, not the missed dose.

Overdose:

In the case of overdose, you should not take the Formoterol. There is a need for supportive therapy. Also, there is a need for heart monitoring.

Do Not Exceed the Recommended Dosage:

If you take an excess dose of Formoterol, it may harm you and cause asthma attacks. You may also die due to cardiac arrest. The cause of cardiac arrest can be hypoxia and severe asthma attacks.

Side Effects:

The side effects include:

• Angina.

• Hypotension or hypertension.

• Tachycardia.

• Arrhythmia.

• Nervousness.

• Headache.

• Tremor.

• Muscle cramps.

• Seizures.

• Dry mouth.

• Dizziness.

• Palpitation.

• Nausea.

• Fatigue.

• Hypokalemia.

• Hyperglycemia.

• Insomnia.

• Metabolic acidosis.

• Cardiac arrest and death.

For Doctors:

What Are the Indications and Uses of Formoterol?

Formoterol is indicated for use in the following conditions:

• In the treatment of asthma.

• In the treatment of COPD.

• Used in preventing exercise-induced breathing problems.

Clinical Pharmacology:

Mechanism of Action:

Formoterol is a long-acting selective beta2 agonist. The inhaled drug acts locally in the lungs as a bronchodilator. The pharmacological effects of Formoterol are due to the stimulation of intracellular adenylyl cyclase and the change in cyclic AMP (cyclic 3’, 5’-adenosine monophosphate).

Pharmacokinetics:

Absorption:

After inhalation of a single 120 mcg dose, within five minutes, the drug was absorbed. The maximum drug concentration was 92 pg/mL (picograms per milliliter). COPD patients who received 12 or 24 mcg of Formoterol for 12 weeks had mean plasma concentrations ranging from 4 to 8.8 pg/mL and 8 to 17.3 pg/mL, respectively, at ten minutes, two, and six hours post-inhalation. As with many drugs, it was observed that most inhaled Formoterol was swallowed and absorbed into the gastrointestinal tract.

Distribution:

The percentage of Formoterol that bound to human plasma proteins was 61 to 64 percent in vitro at concentrations between 0.1 and 100 ng/mL. Binding to human serum albumin was 31 to 38 percent at concentrations of 5 to 500 ng/ml. Formoterol concentrations are used to assess plasma protein binding.

Metabolism:

The metabolization is at the aliphatic or phenolic hydroxyl group, and O-demethylation is followed by glucuronide conjugation at phenolic hydroxyl groups. Minor pathways involve the sulfate conjugation of Formoterol, followed by deformylation. The most important pathway involves direct conjugation at the phenolic hydroxyl group. The second important pathway involves o-demethylation followed by conjugation at the phenolic 2’-hydroxyl group.

Excretion:

Formoterol leaves the body through your urine and feces. Based on plasma concentration studies, following inhalation of a single 120 mcg dose, it was noted that the mean terminal half-life was ten hours.

Drug Abuse and Dependence:

There is no clinical data regarding the drug abuse of Formoterol and dependence.

How Is Formoterol Supplied?

Formoterol is supplied in aluminum blister-packaged 12 mcg clear gelatin capsules. The capsules have “CG” printed on one end and “FXF” printed on the other. They are also supplied with an aerosolizer and a medication guide.

It is available in two unit doses:

• Unit dose-blister pack (Box of 12, with strips of 6).

• Unit dose-blister pack (Box of 60, with strips of 6).

• Formoterol capsules must be used with an aerolizer inhaler. The inhaler must not be used for other capsules.

• Before dispensing, the medicine must be stored in a refrigerator at 2 to 8 degrees Celsius.

• After dispensing to the patient, it must be stored at 20 to 25 degrees Celsius.

• The medicine must be protected from heat and moisture.

• Capsules must always be stored in the blister and removed before use.

• Formoterol and the aerosizer must be discarded at the “ by use” date, and a new one must be used as per the prescription.

• The medicine must be kept out of reach of children.

What Are the Warnings and Precautions of Formoterol?

Asthma-Related Death:

If you do not take Formoterol with an inhaled corticosteroid, it can increase the risk of asthma-related death. If, after taking inhaled corticosteroids, there is no change in your symptoms, there is a need for additional therapy. When your asthma symptoms get under control, the dose should be reduced and then stopped.

Pediatric and Adolescent Patients:

If your child or an adult is taking LABA, asthma-related hospitalization will increase. Therefore, when the therapy has to be considered, a fixed-dose combination therapy containing both an inhaled corticosteroid and LABA must be considered.

Formoterol must not be used in the following cases:

• Patients with worsening or acutely deteriorating asthma.

• In conjunction with another long-acting beta2 agonist (LABA).

• The corticosteroid dosage must not be reduced and must not be stopped if Formoterol usage is initiated.

• Patients taking short-acting beta2 agonists four times a day regularly must be instructed to stop them and use them only for symptomatic relief from acute asthma attacks when Formoterol is started.

Paradoxical Bronchospasm:

The drug can cause paradoxical bronchospasm. If it occurs after taking this drug, then immediately stop taking it.

Use of Anti-Inflammatory Agents:

No data suggests the anti-inflammatory effects of Formoterol. But if you are taking oral or inhaled corticosteroids and Formoterol, you must not stop even if you feel better. You can change only the dose of corticosteroids.

Cardiovascular Effects:

The drug can cause heart effects, such as an increase in pulse rate and blood pressure. If you experience any of the above effects, you should not take that drug. If such effects occur, the drug must be discontinued. Also, ECG (electrocardiogram) changes like flattening of the T wave, depression of the ST segment, and prolongation of the QTc interval can occur. If you have any heart disorder, you should take this drug carefully; otherwise, you may have hypertension, cardiac arrhythmia, and coronary insufficiency.

Immediate Hypersensitivity Reactions:

A few patients can experience immediate hypersensitivity reactions, such as anaphylactic reactions, rash, urticaria, angioedema, and bronchospasm.

Precautions:

General:

• If you have acute asthma, you should not use this drug.

• Even if you're taking Formoterol twice a day, your doctor can give you a short-acting beta-agonist to treat acute asthma.

• If you take an excess dose of a short-acting beta-agonist, your health can deteriorate.

• Care should be taken while giving to patients with cardiovascular disorders, convulsive disorders, and thyrotoxicosis, and who are unusually responsive to sympathomimetic amines.

• Pre-existing conditions, like diabetes mellitus and ketoacidosis, can worsen if you take short-acting beta-agonists.

• Beta-agonist medications can produce transient hypokalemia, resulting in cardiovascular effects due to intracellular shunting.

• If you are allergic to milk, then you might be allergic to Formoterol because of the presence of traces of lactose.

Drug Interactions:

• In case of the use of additional adrenergic drugs through any route, they must be used cautiously as the predictable sympathetic effects of Formoterol may be potentiated.

• Hypokalemic effects of adrenergic agonists may be potentiated if they are used concomitantly with steroids, diuretics, or xanthine derivatives.

• Caution is advised during the co-administration of beta-agonists with non-potassium-sparing diuretics like loop or Thiazide diuretics.

• Formoterol must be used with caution in patients on monoamine oxidase inhibitors, tricyclic antidepressants, and those who prolong the QTc interval. These drugs can potentiate the action of adrenergic agonists on the cardiovascular system. Drugs that prolong the QTc interval can also cause ventricular arrhythmia.

• When administered concomitantly, beta-blockers and Formoterol can inhibit each other's actions. Apart from blocking Formoterol's therapeutic effects, beta blockers can produce severe bronchospasms in asthmatic patients. In cases like prophylaxis after myocardial infarction, where beta-blockers must be used, they must be used with extreme caution.

Contraindications:

The contraindications are as follows:

• Due to the risk of asthma-related hospitalization and death, using Formoterol without the concomitant use of an inhaled corticosteroid (long-term asthma control medication) is contraindicated.

• It is also contraindicated in patients with hypersensitivity to Formoterol or its components.

Specific Considerations:

Asthma:

Use Formoterol to treat asthma and prevent bronchospasms. It can only be used as a concomitant therapy along with a long-term asthma control medication, like inhaled corticosteroids. If your child is over five years old and has reversible obstructive airway disease or nocturnal asthma symptoms, you can give Formoterol.

LABAs, like Formoterol, can increase the risk of asthma-related deaths. Therefore, monotherapy without concomitant use of long-term asthma control medications, like inhaled corticosteroids, is not advisable. Also, in patients who have good asthma control with low—or medium-dose inhaled corticosteroids, Formoterol must not be used.

Pediatric and Adolescent Patients:

Children and adults are at risk of asthma attacks. Therefore, in patients where separate long-term asthma control medications, like inhaled corticosteroids and LABA, are required, steps must be taken to ensure adherence to both components. Otherwise, a dose combination product containing both drugs can be used.

Exercise-Induced Bronchospasm (EIB):

Formoterol is used for acute cases of EIB, so it must be used only when needed. The drug can be used as a single therapy in patients without asthma, but it can only be used as an adjunct to an inhaled corticosteroid in asthmatic patients.

Chronic Obstructive Pulmonary Disease:

You can take Formoterol for a long time if you are suffering from chronic obstructive pulmonary disease.

Hepatic and Renal Impairment: However, limited data are available on pediatric patients.

In a clinical study conducted in pediatric patients between five and 12 years of age who were administered 12 mcg to 24 mcg twice daily for 12 weeks, about 6 percent to 6.5 percent and 9 percent of the dose was recovered in the urine unchanged as conjugated Formoterol, respectively.

Geriatric and Pediatric Patients: Formoterol pharmacokinetics have not been studied in patients with hepatic and renal impairment.

Key Takeaway From iCliniq

Formoterol is a fast-acting bronchodilator drug that is used to manage asthma symptoms. It can even manage chronic obstructive pulmonary disease. If you are pregnant or breastfeeding, you can contact our doctors; they will suggest it to you. Our specialist doctor will tell you how and when to take Formoterol.