Indications for use
- bronchospasm prevention and treatment in patients with bronchial asthma as an addition to inhaled corticosteroids treatment in adult patients;
- prevention of acute bronchospasm attacks caused by allergens, cold air or physical activity in adult patients and children over 6 years;
- treatment of bronchospasm in adult patients with chronic obstructive pulmonary disease (COPD) such as emphysema and chronic bronchitis;
- bronchospasm prevention and treatment in children over 6 years with asthma.
International Nonproprietary Name: Formoterol
Drug form: inhalation powder in capsules 12 mcg.
Composition
1 capsule contains:
Active substance: formoterol fumarate (in a form of formoterol fumarate dihydrate) – 12 mcg;
Excipients: lactose monohydrate.
Capsule shell composition: hydroxypropyl methylcellulose (E464).
Pharmacotherapeutic group
Drugs for the treatment of obstructive pulmonary diseases. Adrenergic drugs for inhalation use. Selective β2-adrenergic agonist.
ATC code: RO3AC13
Pharmacological properties
Formoterol is a selective β2 receptor agonist. It possesses a bronchodilatory effect in patients with reversible pulmonary obstruction. The drug’s effect is quick (develops within 1-3 minutes) and persists for 12 hours after inhalation. When used in therapeutic doses the effect on the cardiovascular system is minimal and noted only in rare cases.
Formoterol inhibits the release of histamine and leukotrienes from a passively sensitized human lung.
Formoterol effectively prevents bronchospasm caused by inhaled allergens, physical exercises, cold air, histamine or methacholine.
Pharmacokinetics
Absotbtion
Similarly to other inhaled drugs approximately 90% of formoterol used for inhalation is taken orally and subsequently absorbed from the gastrointestinal tract (GIT). Consequently the pharmacokinetic characteristics of the oral drugs with formoterol are significantly applicable to powdered drugs.
Multiple doses in a range from 40 μg to 160 μg per day do not lead to significant drug cumulation in the body. After inhalation in a therapeutic dose formoterol was not detected in plasma determined by modern analytical methods. However, urinary excretion rates indicate rapid absorption after inhalation. Maximum excretion rate after intake of 12 - 96 mcg is achieved in 1-2 hours (maximum).
Excretion
Formoterol and its metabolites are completely eliminated from the body; approximately two thirds of the oral dose is determined in urine and one third in the feces. On average, after inhalation about 6 - 9% of the dose excretes unchanged into the urine.
The renal clearance of formoterol is 150 ml/min.
Indications for use
- bronchospasm prevention and treatment in patients with bronchial asthma as an additional drug to inhaled corticosteroids in adult patients;
- prevention of acute bronchospasm attacks caused by allergens, cold air or physical activity in adult patients and children over 6 years;
- bronchospasm treatment in adult patients with chronic obstructive pulmonary disease (COPD), such as emphysema and chronic bronchitis;
- bronchospasm prevention and treatment in children over 6 years with asthma.
Dosage and administration
The drug’s Ormota is designed to be used for inhalation.
The drug is placed into a capsule contained powder for inhalation which should be inhaled only with the use of special device included into the package.
Indications for the treatment of bronchial asthma
Supportive bronchodilator therapy with long-acting β2-adrenoreceptor agonists is indicated for patients with bronchial asthma only in combination with anti-inflammatory therapy (for example, inhaled corticosteroids). Therefore, it is possible to prescribe Ormota only when the patient receives the therapy mentioned above.
Long-term treatment (in addition to corticosteroids)
Adult patients, including elderly patients: the drug is taken 2 times a day, 1 capsule (12 mcg) – by inhalation. Ormota is only prescribed in addition to inhaled corticosteroids. The most effective therapy timing is in the morning and in the evening. In case of necessity to reduce the existing symptoms an additional intake of 1 - 2 capsules per day is permitted provided that the recommended maximum daily dose should not exceed 48 mcg. However, when additional doses are required for more than 2 days a week this may indicate deterioration in the main disease condition and the treatment should be reviewed.
In severe cases the dose can be increased to 2 capsules 2 twice a day (24 mcg) by inhalation, taking the second capsule approximately 2 minutes after the first capsule. The highest recommended dose is 48 mcg per day.
Children over 6 years: the drug is taken 2 times a day, 1 capsule (12 mcg) inhaled (in the morning and evening). Ormota is prescribed only in addition to inhaled corticosteroids (ICS).
The highest recommended supportive therapy is 24 mcg per day.
Ormota should not be used to relieve acute symptoms of bronchial asthma attack. In case of an acute attack the fast-acting β2-agonist should be taken.
Bronchospasm prevention in bronchial asthma of physical origin
Adult patients, including elderly: at least 15 minutes before the expected physical exercise or contact with the allergen 1 capsule (12 mcg) should be taken. Patients with a history of severe bronchospasm for prophylaxis may need 2 capsules (24 mcg) taken in 2 minutes break.
In patients with persistent bronchial asthma Ormota can be clinically indicated to prevent bronchospasm caused by physical exercises or advisable for prevention of known allergen attack, when the contact is inevitable, however, the treatment of bronchial asthma should include the ICS drug.
Children over 6 years: at least 15 minutes before the expected contact with allergen the contents of one capsule (12 mcg) should be inhaled.
In patients with persistent bronchial asthma Ormota can be clinically indicated to prevent bronchospasm caused by physical exertion or it is advisable to prevent the action of known allergen when the contact is inevitable, however, the treatment of bronchial asthma should include ICS drug.
Ormota should be prescribed only as an additional drug to inhaled corticosteroid.
In children aged 6 to 12 years the treatment with combination drug contained an inhaled corticosteroid and long-acting β2-agonist (LABA) is recommended unless separate administration of an inhaled corticosteroid and long-acting β2-agonist is required.
Chronic Obstructive Pulmonary Disease (COPD)
Supportive therapy: 1-2 capsules (12-24 mcg) 2 times a day.
Elderly patients: dose correction is not required
Inhalation procedure
In order to ensure correct procedure of the drug intake the doctor or other medical staff should show the patient how to use an inhaler; to explain that capsules with powder for inhalation should only be used with an inhaler; warn that capsules are for inhalation purpose only and not for oral administration.
Due to the capsule destruction small pieces of the shell as a result of inhalation can get into the mouth or throat. In order to minimize this effect puncture the capsule just once. Remove the capsule from the blister pack immediately before use.
In children and adolescents inhalation of Ormota should be carried out under the adults supervision. You must make sure that the child performs the inhalation technique correctly. Rinsing the mouth with water after formoterol inhalation can prevent irritation of the oral mucosa and pharynx and reduce the risk of systemic adverse events.
Instruction for inhalation device application
1. Remove the cap from the inhalation device.
2. Hold the inhalation device firmly by the base and turn the mouthpiece into the arrow direction.
3. Place the capsule into the cell located at the base of the inhalation device (designed in a capsule form). It should be kept in mind that the capsule is necessary to remove from the blister pack immediately before inhalation.
4. Turn the mouthpiece to close the inhalation device.
5. Hold the device in a strictly vertical position and once press firmly red buttons on the sides. Then release them.
At this stage the pierced capsule may break down and as a result small particles of the shell may come into the mouth or throat. To prevent the capsule’s complete break down the following requirements should be met: do not pierce the capsule more than once; comply with storage conditions; remove the capsule from the blister just before inhalation.
6. Take a deep breath in and out.
7. Take a mouthpiece into the mouth and slightly bend the head back. Grasp the mouthpiece tightly with the lips and take a quick, steady, maximum deep breath. At this moment the patient should hear characteristic rattling sound caused by capsule rotation and powder-spraying. If there was no characteristic sound device for inhalation should be opened and inspected the problem with the capsule. Perhaps it was stuck in a cell. In this case the capsule should be removed carefully. It is absolutely prohibited to release the capsule by repeated pressing on the buttons.
8. In case of a characteristic sound during inhalation hold your breath for as long as possible. At the same moment remove the mouthpiece from the mouth. Then exhale. Open the device and check if the powder remains in the capsule. If the powder remains in the capsule, repeat the steps described in paragraphs 6-8.
9. Following an inhalation procedure completion open the device, remove the empty capsule, close the mouthpiece and close the device with a cap.
To remove powder residues wipe the mouthpiece and the cell with a dry cloth or use a soft brush.
Side effect
Determination of the adverse reactions frequency: very often (≥1/10), often (≥ /100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10,000, <1/1000), very rarely (<1/10 000), and the unknown frequency (the frequency cannot be estimated according to the available data).
Immune system disorders: very rarely – hypersensitivity reactions, such as hypotension, angioedema; rarely - hypersensitivity reactions, such as itching, urticaria, exanthema, bronchospasm.
Metabolism and nutrition disorders: rarely - hypokalemia; very rarely - hyperglycemia.
Mental disorders: infrequently - agitation, anxiety, increased irritability, restlessness, insomnia.
Musculoskeletal system and connective tissue disorders: infrequently - muscle cramps, myalgia.
Cardiovascular system disorders: often - heart palpitations; infrequently - tachycardia; rarely - heart arrhythmia (atrial fibrillation, supraventricular tachycardia, extrasystoles); very rarely - peripheral edema, angina pectoris, QT interval elongation, blood pressure deviation.
Nervous system disorders: often - headache, tremor; infrequently - dizziness; very rarely - ageustia.
Respiratory system, chest and mediastinal organs disorders: infrequently - bronchospasm, oropharyngeal irritation, including paradoxical bronchospasm, asthma attack; frequency unknown - cough.
Skin and subcutaneous tissues disorders: rash – frequency is unknown.
Gastrointestinal tract disorders: rarely - nausea; dry mouth – frequency is unknown.
Contraindications
- hypersensitivity to the drug components or other β2-adrenergic stimulants;
- children up to 6 years;
- tachyarrhythmia, third degree atrioventricular block, idiopathic subvalvular aortic stenosis, hypertrophic obstructive cardiomyopathy, thyrotoxicosis.
Overdose
Symptoms: nausea, vomiting, headache, tremor, drowsiness, palpitations, tachycardia, ventricular extrasystole, hypertension, metabolic acidosis, hypokalemia, hyperglycemia.
Treatment: supportive and symptomatic therapy. In severe cases hospitalization is indicated. The use of cardioselective β2-blockers can be considered, but only under close medical supervision, subject to extreme caution due to the risk of bronchospasm.
Pregnancy and lactation
Formoterol safety in pregnancy and lactation has not been established. Ormota should not be used in pregnancy and lactation unless the intended benefit to the mother outweighs the potential risk to the fetus. Similar to β2-adrenergic stimulants labor pain can be inhibited due to the relaxing effect on the uterus smooth muscles.
It is not known whether formoterol passes into the breast milk. The drug is not recommended during breast-feeding.
Pediatric Use
The drug is not recommended to use in children under 6 years due to limited experience of administration in this age group.
Drug-to-drug interactions
Ormota like other β2-adrenostimulants should be used with caution in patients taking the following drugs: quinidine, disopyramide, procainamide, phenothiazine, antihistamines, macrolide antibiotics, tricyclic antidepressants, monoamine oxidase inhibitors as well as other drugs responsible for QT interval elongation since in these cases the adrenostimulants effect on the cardiovascular system can be enhanced. When using drugs that can cause QT interval elongation the risk of ventricular arrhythmias increases. Simultaneous use of Ormota with other sympathomimetic drugs can lead to side effects aggravation.
Concomitant administration of xanthine derivatives, steroids or diuretics can enhance the potential hypokalemic effect of β2-adrenergic agonists. Hypokalemia may increase predisposition to cardiac arrhythmias development in patients receiving digitalis-based medicines.
β-adrenergic blockers can weaken the effect of Ormota. In this regard Ormota should not be used together with β-blockers (including eye drops) unless there is no other alternative.
L-dihydroxyphenylalanine, L-thyroxine and oxytocin can enhance the side effect of β2-agonists, including Ormota on the cardiovascular system.
There is an increased risk of arrhythmias in case of simultaneous use of anesthesia with a halogenated hydrocarbon.
Storage conditions and shelf-life
Keep in a place protected from moisture at temperature not more than 25°С.
Keep out of reach of children!
Shelf-life is 3 years. Do not use after the expiration date indicated on the pack.
Prescription status
By prescription
Package
10 капсул с порошком для ингаляций в контурной ячейковой упаковке из комбинированной полиамидно-алюминиево-поливинилхлоридной пленки и гибкой упаковки на основе алюминиевой фольги.
6 контурных ячейковых упаковок вместе с прибором для ингаляции и листком-вкладышем помещают в пачку картонную.
10 capsules with inhalation powder in a blister made of a combined polyamide-aluminum-polyvinyl chloride film and flexible base with aluminum foil.
6 blister packs together with an inhalation device and a leaflet are placed into a cardboard box.
Manufacturer Information
Foreign production and trade unitary enterprise “Reb-Pharma”, 223216, Republic of Belarus, Minsk region, Chervensky district, Smilovichi, Sadovaya st., 1, tel./fax: (+375) 17 240 26 35,
e-mail: rebpharma@rebpharma.by, http://www.rebpharma.by
Comment type is not specified in the component properties.