Pectolvane® c

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PECTOLVAN® C (PECTOLVAN C)

Composition:

Active substances: ambroxol hydrochloride, carbocisteine;

5 ml of the preparation contains ambroxol hydrochloride calculated as 100 % substance – 15 mg, carbocisteine calculated as 100 % substance – 100 mg;

Excipients: glucose monohydrate; sorbitol (E 420); propylene glycol; glycerol; meglumine; disodium edetate; citric acid monohydrate; sodium benzoate (E 211); aspartame (E 951); strawberry flavoring; purified water.

Pharmaceutical form. Syrup.

Main physicochemical properties: clear, colorless, viscous liquid with a strawberry taste.

Pharmacotherapeutic group. Mucolytics. Combinations. ATC code R05CB10.

Pharmacological properties.

Pharmacodynamics.

Pectolvan® C is a combined mucolytic and expectorant agent containing a balanced combination of two components – ambroxol and carbocisteine.

Ambroxol is an active metabolite of bromhexine, but more effective. It increases secretion of the respiratory tract glands, promotes liquefaction of viscous bronchial secretions, and facilitates their expectoration by enhancing mucociliary clearance and altering the ratio between serous and mucous components of sputum. Ambroxol stimulates Clara cells and activates hydrolytic enzymes, which also contributes to reduced sputum viscosity. Ambroxol has secretomotor properties – it stimulates ciliated bronchial epithelium, restores drainage function of small bronchi and bronchioles. The drug promotes formation of endogenous surfactant, does not cause excessive secretion, and reduces spastic hyperreactivity of bronchi. Cough and sputum volume are significantly reduced. Ambroxol hydrochloride has demonstrated anti-inflammatory effects in vitro. In vitro studies have shown that ambroxol hydrochloride significantly reduces cytokine release from blood and tissue binding of mononuclear and polymorphonuclear cells.

Carbocisteine exerts mucolytic and expectorant effects; by breaking disulfide bonds of glycoproteins, it causes liquefaction of excessively viscous bronchial secretions, thereby facilitating sputum elimination. The mucoregulatory effect of carbocisteine is associated with activation of sialyltransferase – an enzyme of goblet cells in the bronchial mucosa. It normalizes the quantitative ratio of acidic and neutral sialomucins, thus reducing viscosity of bronchial secretions. It facilitates sputum expectoration by increasing mucociliary clearance and possesses antioxidant and pneumoprotective properties due to the ability of sulfhydryl groups to bind free radicals. It also promotes regeneration of the mucous membrane, normalizes its structure, reduces goblet cell hyperplasia, and consequently decreases mucus production. Carbocisteine activates ciliated epithelium, restores IgA secretion (specific protection), and increases the number of sulfhydryl groups in mucus components (non-specific protection). It exhibits anti-inflammatory effects through kinin-inhibiting activity of sialomucins, leading to reduced edema and bronchoobstruction.

Pharmacokinetics.

After oral administration, ambroxol is almost completely absorbed in the gastrointestinal tract and penetrates well into lung tissues. Absolute bioavailability after oral administration is 70–80%. Maximum plasma concentration is reached approximately 2 hours after oral intake. Elimination half-life is 7–12 hours. It is excreted mainly in urine (up to 90%). Ambroxol crosses the blood-brain barrier and is excreted in breast milk, but does not accumulate.

After oral administration, carbocisteine is rapidly absorbed. Peak plasma concentration of the active substance is achieved within 2 hours. Bioavailability is low – less than 10% of the administered dose (due to intensive metabolism in the gastrointestinal tract and first-pass liver effect). Carbocisteine is excreted almost entirely as inactive metabolites (inorganic sulfates, diacetylcysteine) in urine. Only a small amount is excreted unchanged in feces. It may cross the placental barrier and accumulate in amniotic fluid.

Clinical characteristics.

Indications.

Acute and chronic respiratory tract diseases associated with the production of difficult-to-expectorate secretions:

• chronic obstructive pulmonary disease;
• pneumonia;
• bronchial asthma with severe sputum expectoration;
• bronchiectasis;
• respiratory distress syndrome;
• management of complications following lung surgery;
• care of tracheostomy before and after bronchoscopy.

Inflammatory diseases of the middle ear and paranasal sinuses.

Contraindications.

Hypersensitivity to any component of the medicinal product. In rare hereditary conditions incompatible with excipients of the medicinal product (see section "Special precautions for use"), the use of the medicinal product is contraindicated.

Peptic ulcer of the stomach and duodenum during the exacerbation period. First trimester of pregnancy due to insufficient data on teratogenic and embryotoxic effects.

Interaction with other medicinal products and other types of interactions.

Enhances the efficacy of glucocorticoid and antibacterial therapy in the treatment of inflammatory diseases of the upper and lower respiratory tract. However, concomitant use with tetracycline antibiotics (except doxycycline) is not recommended; the interval between administrations should be at least 2 hours.

Simultaneous use of ambroxol and antitussive agents may lead to excessive mucus accumulation due to suppression of the cough reflex. Therefore, such combination should only be considered after careful evaluation by a physician of the expected benefit versus potential risk.

During treatment with carbocysteine, antitussive agents and drugs that suppress bronchial secretion should not be used.

Special precautions for use

Productive cough is a fundamental protective mechanism of the bronchopulmonary system and therefore should not be suppressed. It is irrational to combine medicinal products that modify bronchial secretion with cough-suppressant agents and/or agents that reduce secretion (anticholinergic group, e.g. atropine-like drugs).

The use of mucolytic agents may lead to impaired bronchial clearance in children under 2 years of age. In infants during the first year of life, the ability to clear bronchial secretions is limited due to age-related anatomical and physiological characteristics. Therefore, mucolytic agents should not be used in children under 2 years of age.

Treatment should be re-evaluated if there is no therapeutic effect or if symptoms worsen.

There have been reports of severe skin reactions associated with ambroxol use, including: erythema multiforme, Stevens–Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), and acute generalized exanthematous pustulosis. These are mostly attributable to the severity of the underlying disease and/or concomitant use of other medications. Therefore, if new skin lesions or mucosal involvement occur, immediate medical attention should be sought and treatment with ambroxol hydrochloride should be discontinued.

In the early stages of Stevens–Johnson syndrome or Lyell’s syndrome, patients may present with non-specific, flu-like symptoms such as fever, malaise, rhinitis, cough, and sore throat. These non-specific, flu-like symptoms may lead to inappropriate symptomatic treatment with cough and cold remedies.

The drug should be used with caution in patients with impaired bronchial motility and increased mucus secretion (e.g. in rare conditions such as primary ciliary dyskinesia), as ambroxol may increase mucus secretion.

Patients with renal impairment or severe hepatic insufficiency should take the drug only after consultation with a physician. When ambroxol, like any active substance metabolized in the liver and subsequently excreted by the kidneys, is administered, metabolites formed in the liver may accumulate in patients with severe renal insufficiency.

Close medical supervision is required in cases of purulent sputum and high fever.

The drug should be used with caution in patients with a history of gastric or duodenal ulcer.

The drug contains sorbitol; therefore, it should not be taken by patients with rare hereditary fructose intolerance.

The drug contains aspartame, a phenylalanine derivative, which may be harmful to patients with phenylketonuria. Therefore, the drug should not be used in this patient group.

The drug contains glucose; therefore, patients with hereditary glucose intolerance or glucose-galactose malabsorption should avoid taking this medication.

Use during pregnancy or breastfeeding

Contraindicated during the first trimester of pregnancy. During the second and third trimesters of pregnancy, the drug may be used only after careful assessment of the benefit-risk ratio for mother and fetus/child, as determined by the physician. Use during breastfeeding is not recommended.

Preclinical studies have not indicated a direct or indirect harmful effect on fertility.

Effect on ability to drive or operate machinery

Studies on the effect of the drug on the ability to drive vehicles or operate machinery have not been conducted. If dizziness occurs, patients should refrain from driving or operating machinery.

Method of administration and dosage.

For oral use.

Children aged 6 to 12 years – 5 ml (1 measuring spoon) 2–3 times daily; children aged 2 to 6 years – 2.5 ml (1/2 measuring spoon) 2–3 times daily.

The duration of treatment should generally not exceed 7–10 days.

The duration of use in children should be as short as possible, no more than 5 days.

Children.

The drug may be used in children aged 2 years and older. Treatment of children should be carried out under medical supervision.

Overdose.

Symptoms: stomach pain, nausea, vomiting, diarrhea.

Treatment: symptomatic and supportive.

Adverse Reactions.

Immune system disorders: hypersensitivity reactions, including angioedema, anaphylactic reactions, anaphylactic shock.

Skin and subcutaneous tissue disorders: skin rashes (including macular, maculopapular, papular, confluent plaques), urticaria, pruritus, dermatitis, severe skin reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), acute generalized exanthematous pustulosis.

Nervous system disorders: dysgeusia (taste disturbance), dizziness, headache, restlessness.

Gastrointestinal disorders: nausea, oral numbness, vomiting, diarrhea, dyspepsia, heartburn, stomach pain, abdominal pain, digestive disorders, dry mouth, constipation, hypersalivation, gastrointestinal bleeding.

Respiratory, thoracic and mediastinal disorders: pharyngeal numbness, rhinorrhea, dyspnea (as a symptom of hypersensitivity reaction), dry throat.

Renal and urinary disorders: dysuria.

Cardiac disorders: palpitations.

General disorders: general weakness, fever, mucosal reactions.

Shelf life. 1 year 6 months.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not refrigerate.

Shelf life after opening the bottle: 60 days at a temperature not exceeding 25 °C. Do not refrigerate.

Keep out of reach of children.

Packaging.

100 ml in a brown glass bottle with a screw neck, closed with a screw cap with a tamper-evident ring or a tamper-evident screw cap with first-opening control.

One bottle with a dosing spoon/measure in a carton.

Availability classification. Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's address and location of business activity.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.