Partusisten (Tablets, Concentrate) Instructions for Use

ATC Code

R03AC04 (Fenoterol)

Active Substance

Fenoterol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Bronchodilator drug – beta₂-adrenergic agonist

Pharmacotherapeutic Group

Tocolytic agent – selective beta2-adrenomimetic

Pharmacological Action

Beta-adrenomimetic. It acts primarily on β₂-adrenergic receptors. The mechanism of action is associated with the activation of adenylate cyclase coupled to the receptor, which leads to an increase in the formation of cAMP, which stimulates the work of the calcium pump, resulting in a decrease in the concentration of calcium in the myofibrils.

When used as a bronchodilator, it dilates the bronchi, increases the frequency and volume of breathing, and improves the function of the bronchial ciliated epithelium. It has a vasodilating effect, reduces the contractile activity and tone of the myometrium.

As a tocolytic agent, it is used orally and intravenously. Along with lowering the tone and contractile activity of the myometrium, it improves uteroplacental blood flow, which leads to an increase in the concentration of oxygen in the fetal blood.

Pharmacokinetics

After inhalation, 10-30% of fenoterol reaches the lower respiratory tract. The remainder is deposited in the upper respiratory tract and in the mouth and is then swallowed. The absolute bioavailability of fenoterol after inhalation is 18.7%. After oral administration, approximately 60% of the fenoterol dose is absorbed. Plasma protein binding is from 40 to 55%. Fenoterol undergoes intensive metabolism in the liver by conjugation to glucuronides and sulfates. The swallowed portion of the fenoterol dose is metabolized primarily by sulfation. This metabolic inactivation of the parent substance begins already in the intestinal wall. Fenoterol is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. After inhalation, 2% of the dose is excreted through the kidneys unchanged within 24 hours. Fenoterol can cross the placental barrier and enter breast milk.

Indications

Attacks of bronchial asthma or other conditions with reversible airway obstruction, chronic bronchitis, COPD; prevention of bronchial asthma attacks due to physical exertion. As a bronchodilator before inhalation of other drugs (antibiotics, mucolytic agents, glucocorticosteroids). Conducting bronchodilator tests in the study of external respiratory function.

ICD codes

Dosage Regimen

Determine the dosage individually based on the clinical situation, indication, and patient age.

For bronchial asthma and reversible airway obstruction, administer one 2.5 mg tablet three to four times daily.

For severe or acute attacks, a single dose may be increased to 5 mg under medical supervision.

The maximum daily dose for adults is 20 mg of fenoterol.

For prophylaxis of exercise-induced asthma, administer 2.5 mg to 5 mg approximately 30 minutes prior to physical exertion.

As a tocolytic agent for premature labor, initiate with 2.5 mg to 5 mg, repeated at 4 to 6 hour intervals as required to suppress uterine contractions.

For intravenous tocolytic therapy, use the concentrate for solution under strict hospital supervision.

Adjust the dose for elderly patients and those with hepatic impairment; initiate therapy at the lower end of the dosing range.

Do not exceed the recommended maximum daily dose due to the risk of tachycardia and other cardiovascular adverse effects.

Monitor serum potassium levels during treatment, especially with concomitant use of diuretics or corticosteroids.

Discontinue treatment if paradoxical bronchospasm occurs.

Adverse Reactions

Immune system disorders: frequency unknown – hypersensitivity reactions.

Metabolism and nutrition disorders uncommon – hypokalemia, including severe hypokalemia.

Psychiatric disorders: uncommon – agitation; frequency unknown – nervousness.

Nervous system disorders: common – tremor; frequency unknown – headache, dizziness.

Cardiac disorders: uncommon – arrhythmia; frequency unknown – increased systolic blood pressure, decreased diastolic blood pressure, myocardial ischemia, tachycardia, palpitations.

Respiratory, thoracic and mediastinal disorders common – cough; uncommon – paradoxical bronchospasm; frequency unknown – irritation of the larynx and pharynx.

Gastrointestinal disorders uncommon – nausea, vomiting.

Skin and subcutaneous tissue disorders: uncommon – itching; frequency unknown – hyperhidrosis, skin rash, urticaria.

Musculoskeletal and connective tissue disorders frequency unknown – muscle weakness, muscle spasm, myalgia.

Contraindications

Hypersensitivity to fenoterol; hypertrophic obstructive cardiomyopathy; tachyarrhythmia; pediatric age – depending on the dosage form.

With caution

Arterial hypotension, arterial hypertension, hyperthyroidism, hypokalemia, inadequately controlled diabetes mellitus, recent myocardial infarction (within the last 3 months), severe organic diseases of the heart and blood vessels, such as chronic heart failure, coronary artery disease, coronary artery diseases, heart defects (including aortic stenosis), severe lesions of cerebral and peripheral arteries, pheochromocytoma.

Use in Pregnancy and Lactation

During pregnancy, especially in the first trimester, and during breastfeeding, it should be used with caution, only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Pediatric Use

It is possible to use in children according to indications, in age-appropriate recommended doses and dosage forms. It is necessary to strictly follow the instructions in the fenoterol drug labels regarding contraindications for the use of specific fenoterol dosage forms in children of different ages.

In children under 6 years of age, it should be used with caution, only under medical supervision.

Geriatric Use

It should be prescribed with caution to elderly patients to avoid worsening of concomitant diseases.

Special Precautions

When used in obstetrics in patients with water metabolism disorders, impaired functions of the cardiovascular and respiratory systems, the possibility of developing pulmonary edema should be considered.

During the use of fenoterol, it is recommended to monitor the level of potassium in the blood; with oral or intravenous administration, control of blood pressure, maternal heart rate and fetal heart rate is necessary.

When using fenoterol in pregnant women, the inhibitory effect of fenoterol on the contractile activity of the uterus should be taken into account.

Fenoterol should be used with caution simultaneously with corticosteroids.

It is not recommended to use Fenoterol simultaneously with calcium preparations, vitamin D preparations, mineralocorticoids.

Effect on ability to drive vehicles and mechanisms

During the use of fenoterol, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Beta-adrenergic, anticholinergic agents, xanthine derivatives, corticosteroids and diuretics may enhance the action and side effects of fenoterol (especially in hypokalemia).

A significant decrease in the effectiveness of fenoterol is possible with the simultaneous use of beta-blockers.

With simultaneous use with MAO inhibitors and tricyclic antidepressants, an enhancement of the effect of fenoterol is noted.

Inhalation of halogenated hydrocarbon anesthetics (halothane, trichloroethylene, enflurane) may enhance the effect of fenoterol on the cardiovascular system.

Simultaneous administration of bronchodilators with a similar mechanism of action leads to an additive effect and overdose phenomena.

Fluorothane sensitizes the myocardium to the action of fenoterol, contributing to the development of arrhythmia.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.