Products
Formoterol is commercially available in the form of capsules for inhalation (Foradil) and as a powder inhaler (Oxis). Furthermore, combination products with budesonide (Symbicort Turbuhaler, Vannair Dosieraerosol) and fluticasone propionate are available (Formoterol Dosieraerosol). Formoterol is also combined with beclometasone fixed, see under beclometasone and formoterol (Foster). Furthermore, in 2020, a fixed combination with beclometasone, formoterol, and glycopyrronium bromide was approved (Trimbow). Formoterol has been approved in many countries since 1995. In some countries, arformoterol, the pure ,-enantiomer, is also marketed (Brovana). Sales of Foradil HFA metered-dose inhaler were discontinued at the end of 2015.
Structure and properties
Formoterol (C19H24N2O4, Mr = 344.4 g/mol) is present in drugs as formoterol fumarate dihydrate, a white to pale yellow powder that is sparingly soluble in water. Formoterol is a racemic mixture of the ,- and ,-enantiomers. Arformoterol, the ,-enantiomer, is pharmacologically more active.
Effects
Formoterol (ATC R03AC13) has bronchodilator and anti-inflammatory properties. The effects are due to selective agonism at beta2 receptors. They occur rapidly, within 1-3 minutes, and last for a long time, up to 12 hours.
Indications
Formoterol is used to prevent and treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD).
Dosage
According to the SmPC. Formoterol is administered for long-term treatment in the morning and evening or only once daily. Relief of acute symptoms is allowed with some drugs (eg, Symbicort).
Contraindications
- Hypersensitivity
- Certain cardiovascular diseases
- Thyrotoxicosis
- Patients with known or suspected QT interval prolongation.
For complete precautions, see the drug label.
Interactions
Agents that prolong the QT interval should be combined with formoterol only with caution. Other drug interactions are possible with sympathomimetics, MAO inhibitors, xanthine derivatives (theophylline), steroids, diuretics, levodopa, levothyroxine, oxytoxin, and beta-blockers.
Adverse effects
The most common possible adverse effects include headache, tremor, and a palpable heartbeat (palpitations). Occasionally, bronchospasm, sore throat, muscle cramps and pain, dizziness, taste disturbances, rapid pulse, and edema may occur. Other possible side effects include hypokalemia, elevated blood pressure, hyperglycemia, and prolongation of the QT interval.
