Instructions for Abrol SR capsules 75 mg No. 10
Composition
active ingredient: ambroxol hydrochloride;
Each prolonged-release capsule contains: ambroxol hydrochloride 75 mg;
excipients: microcrystalline cellulose, xanthan gum, hypromellose, hydroxypropylcellulose, magnesium stearate, hard gelatin capsule*;
*hard gelatin capsule: gelatin, purified water, titanium dioxide (E 171).
Dosage form
Extended-release capsules.
Main physicochemical properties: opaque capsules with a creamy-white body and a creamy-white cap, containing white powder.
Pharmacotherapeutic group
Medicines used for coughs and colds. Mucolytics.
ATX code R05C B06.
Pharmacological properties
Pharmacodynamics
The active ingredient of Abrol®SR extended-release capsules – ambroxol hydrochloride – increases the proportion of the serous component of bronchial secretions. Ambroxol enhances the secretion of pulmonary surfactant by directly affecting type II pneumocytes in the alveoli and Clara cells in the bronchioles, and also stimulates the activity of the cilia of the ciliated epithelium, as a result of which the viscosity of sputum decreases and its excretion improves (mucociliary clearance). The improvement of mucociliary clearance has been proven during clinical and pharmacological studies.
Increased production and decreased viscosity of secretions and improved mucociliary clearance promote expectoration and facilitate coughing up of sputum.
Long-term use (6 months) of ambroxol hydrochloride (in oral slow-release form 75 mg) in patients with COPD resulted in a significant reduction in exacerbations after a two-month treatment period. In patients receiving ambroxol hydrochloride, the duration of the disease and antibiotic therapy was significantly shorter. Compared with placebo, treatment with ambroxol hydrochloride, in oral slow-release form, showed a statistically significant improvement in symptoms related to expectoration problems, cough, dyspnea and auscultatory signs.
The local anesthetic effect of ambroxol hydrochloride, which may be explained by its sodium channel blocking properties, was observed in a rabbit eye model.
In vitro studies have shown that ambroxol hydrochloride blocks neuronal sodium channels; binding was reversible and concentration-dependent.
Ambroxol hydrochloride has demonstrated anti-inflammatory effects in vitro. In vitro studies have shown that ambroxol hydrochloride significantly reduces the release of cytokines from mononuclear and polymorphonuclear blood cells and tissues.
Clinical trials involving patients with pharyngitis have demonstrated a significant reduction in pain and redness in the throat when using ambroxol hydrochloride.
Due to the pharmacological properties of ambroxol, pain was quickly relieved during the treatment of upper respiratory tract diseases, which was observed during studies of the clinical efficacy of inhaled forms of ambroxol.
After the use of ambroxol hydrochloride, the concentrations of antibiotics (amoxicillin, cefuroxime, erythromycin and doxycycline) in bronchopulmonary secretions and sputum increase. No clinical significance of this fact has been identified to date.
Pharmacokinetics
Absorption. Absorption of ambroxol hydrochloride from oral immediate-release formulations is rapid and fairly complete, with a linear dose dependence in the therapeutic range. Maximum plasma levels are reached after 1-2.5 hours with oral immediate-release formulations and on average after 6.5 hours with slow-release formulations.
Distribution. When administered orally, the distribution of ambroxol hydrochloride from the blood to the tissues is rapid and pronounced, with the highest concentration of the active substance in the lungs. The volume of distribution when administered orally is 552 l. In blood plasma in the therapeutic range, approximately 90% of the drug is bound to blood proteins.
Metabolism and elimination. Approximately 30% of the dose after oral administration is excreted as a result of presystemic metabolism. Ambroxol hydrochloride is metabolized mainly in the liver by glucuronidation and cleavage to dibromanthranilic acid (approximately 10% of the dose). Studies in human liver microsomes have shown that CYP3A4 is responsible for the metabolism of ambroxol hydrochloride to dibromanthranilic acid.
After 3 days of oral administration, about 6% of the dose is excreted in the urine in unchanged form, approximately 26% of the dose in conjugated form.
The plasma half-life is about 10 hours. Total clearance is in the range of 660 ml/min. Renal clearance is about 8% of the total. After 5 days, about 83% of the total dose is excreted in the urine.
Pharmacokinetics in special patient groups. In patients with impaired liver function, the excretion of ambroxol hydrochloride is reduced, which results in a 1.3-2 times higher level in the blood plasma. Since the therapeutic range of ambroxol hydrochloride is quite wide, it is not necessary to change the dosage.
Food intake does not affect the bioavailability of ambroxol hydrochloride.
Indication
Secretolytic therapy for acute and chronic bronchopulmonary diseases associated with disorders of bronchial secretion and impaired mucus movement.
Contraindication
Abrol®SR should not be used in patients with known hypersensitivity to ambroxol hydrochloride or to any of the other ingredients of the drug.
Abrol®SR is not intended for use in children under 12 years of age due to the amount of active ingredient contained in the capsule.
Interaction with other medicinal products and other types of interactions
The simultaneous use of Abrol®SR and cough suppressants may lead to excessive mucus accumulation due to suppression of the cough reflex. Therefore, such a combination is possible only after a careful assessment by the doctor of the ratio of the expected benefit and the possible risk of use.
Application features
Severe skin reactions: erythema multiforme, Stevens-Johnson syndrome (SJS)/toxic epidermal necrolysis (TEN) and acute generalised exanthematous pustulosis (AGEP) have been reported in association with the use of ambroxol hydrochloride. If signs of progression of the skin rash (sometimes associated with blistering or mucosal involvement) are present, ambroxol hydrochloride treatment should be discontinued immediately and medical advice should be sought.
In cases of impaired bronchial motility and increased mucus secretion (for example, in a rare disease such as primary ciliary dyskinesia), Abrol®SR should be used with caution due to the risk of promoting secretion accumulation.
Patients with impaired renal function or severe hepatic insufficiency should take Abrol®SR, prolonged-release tablets, only after consulting a doctor. In patients with severe renal insufficiency, when using ambroxol, as with any active substance that is metabolized in the liver and then excreted by the kidneys, accumulation of metabolites formed in the liver is possible.
Use during pregnancy or breastfeeding
Pregnancy.
Ambroxol hydrochloride crosses the placental barrier. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development.
Clinical studies of the use of ambroxol hydrochloride after the 28th week of pregnancy have not revealed any harmful effects on the fetus.
However, the usual precautions regarding taking medications during pregnancy should be observed. In particular, Abrol®SR prolonged-release capsules are not recommended in the first trimester of pregnancy.
Breast-feeding.
According to preclinical studies, ambroxol hydrochloride passes into breast milk. Abrol®SR is not recommended for use during breastfeeding.
Fertility.
Preclinical studies do not indicate direct or indirect harmful effects with respect to fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
There are no data on the effect of ambroxol on the reaction speed when driving vehicles or working with other mechanisms. Studies on the effect on the reaction speed when driving vehicles or working with other mechanisms have not been conducted.
Method of administration and doses
Unless otherwise stated, the following dosage of Abrol®SR is recommended:
Adults and children over 12 years of age: 1 capsule once daily (equivalent to 75 mg/day of ambroxol hydrochloride) in the morning or evening after a meal. The capsules should be swallowed whole with sufficient water.
In general, there are no restrictions on the duration of use, but long-term therapy should be carried out under medical supervision.
Abrol®SR should not be used for longer than 4-5 days without consulting a doctor.
Children.
The drug should not be used in children under 12 years of age due to the amount of active substance contained in the capsule. For children under 12 years of age, it is recommended to use ambroxol in the form of syrup 15 mg/5 ml or 30 mg/5 ml.
Overdose
There are no reports of specific symptoms of overdose yet. The symptoms known from isolated reports of overdose and/or cases of medication errors correspond to the known adverse reactions when using ambroxol hydrochloride at recommended doses and require symptomatic treatment.
Adverse reactions
Adverse reactions are listed below by organ system and frequency:
very common (≥1/10), common (≥1/100,
Immune system disorders: Rare: hypersensitivity reactions; Not known: anaphylactic reactions, including anaphylactic shock, angioedema and pruritus.
Skin and subcutaneous tissue disorders: rare - rash, urticaria; unknown - serious skin adverse reactions (including erythema multiforme, Stevens-Johnson syndrome/toxic epidermal necrolysis and acute generalized exanthematous pustulosis).
Gastrointestinal: often - nausea; infrequently - vomiting, diarrhea, dyspepsia, abdominal pain; very rarely - drooling; unknown - decreased sensitivity in the oral cavity, dry mouth, dry throat.
Respiratory, thoracic and mediastinal disorders: not known – dyspnoea (as a hypersensitivity reaction), decreased sensitivity in the pharynx.
General disorders: infrequently - fever, mucous membrane reactions.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after the registration of a medicinal product is an important procedure. This allows for continued monitoring of the benefit/risk balance of this medicinal product. Healthcare professionals are asked to report all suspected adverse reactions via the national reporting system and to the applicant via the feedback form on the website: https://kusum.ua/pharmacovigilance/.
Expiration date
2 years.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 capsules in a blister. 1 or 2 blisters in a cardboard box.
Vacation category
Without a prescription.
Producer
"KUSUM FARM" LLC.
Address
40020, Ukraine, Sumy region, Sumy city, Skryabina st., 54.
