Carbocisteine 250mg/5ml sugar-free oral solution

Summary of Product Characteristics Updated 25-Nov-2021 | Aspire Pharma Ltd

1. Name of the medicinal product

Carbocisteine 250 mg / 5 ml sugar-free oral solution

2. Qualitative and quantitative composition

Active substance: Carbocisteine

Each 5ml of the sugar-free oral solution contains 250 mg Carbocisteine.

Excipient(s) with known effect:

Each 5ml of carbocisteine contains 7.5 mg of sodium methyl parahydroxybenzoate (E219)

Each 5ml of carbocisteine contains 63.5 mg (2.76mmol) of sodium,

Each 5ml of carbocisteine contains 250 mg of glycerol (E422).

For a full list of excipients, section 6.1.

3. Pharmaceutical form

Sugar-Free Oral Solution

4. Clinical particulars
4.1 Therapeutic indications

Carbocisteine is a mucolytic agent for the adjunctive therapy of respiratory tract disorders characterised by excessive, viscous mucus, including chronic obstructive airways disease.

4.2 Posology and method of administration

Posology

Adults including the elderly and adolescents over 12 years: Dosage is based upon an initial daily dosage of 2250 mg Carbocisteine in divided doses, reducing to 1500 mg daily in divided doses when a satisfactory response is obtained e.g. for oral solution 15 ml three times a day reducing to 10 ml three times a day.

Children 2-5 years: The usual dose is 1.25 - 2.5 ml four times a day.

Children 5-12 years: The usual dose is 5ml three times a day.

Method of administration

This medicine is for oral use.

This medicine, due to its composition (does not contain sugar), is suitable for administration to diabetics.

An oral dosing syringe is provided for use for dosing.

How to use the oral dosing syringe

The syringe end should be placed into the neck of the bottle below the liquid fill line.

To fill the syringe whilst holding the syringe in place, gently pull the plunger down drawing the medicine to the correct mark on the syringe. Remove the syringe from the bottle neck carefully. Place the end of the syringe into the mouth against the cheek and gently press the plunger down slowly to gently release the medicine. After use replace the bottle cap. Wash the syringe in warm water and allow to dry. Store out of the reach of children.

4.3 Contraindications

Hypersensitivity to the active substance (Carbocisteine) or to any of the excipients referred to in section 6.1.

Active peptic ulcer.

Children less than 2 years of age.

4.4 Special warnings and precautions for use

- Asthmatic patients with a history of bronchospasm;

- Severe respiratory failure;

- Debilitated patients. By decreasing the cough reflex there is a risk of obstruction of the airways as a consequence of the secretions amount increase.

The use of Carbocisteine will result in less viscous mucus, requiring clearance via epithelial ciliary action and an intact cough reflex. The concomitant use of antitussives is therefore not recommended (see section 4.5).

Caution is recommended in the elderly and in patients with a history of gastroduodenal ulcers, or those who are receiving concomitant medications that are known to cause gastrointestinal bleeding. If gastrointestinal bleeding occurs, patients should discontinue medication immediately.

This medicine contains sodium methyl parahydroxybenzoate (E219), which can cause allergic reactions (possibly delayed).

This medicine contains 12.7 mg sodium per ml. It should be taken into account by patients in controlled sodium diet.

4.5 Interaction with other medicinal products and other forms of interaction

No drug interactions have been identified

4.6 Fertility, pregnancy and lactation

Pregnancy

There are no available data on carbocisteine use in pregnant women. No conclusions can be drawn regarding whether or not carbocisteine is safe for use during pregnancy. The use of carbocisteine in pregnant women is not recommended, especially during the first trimester.

Breast-feeding

There are no available data on the presence of carbocisteine in human milk, milk production, or the effects on the breastfed infant. No conclusions can be drawn regarding whether or not carbocisteine is safe for use during breastfeeding. The use of carbocisteine in breastfeeding women is not recommended.

Fertility

There is no consistent evidence on the effects of carbocisteine on fertility.

4.7 Effects on ability to drive and use machines

Carbocisteine has no or negligible influence on the ability to drive or use machines.

4.8 Undesirable effects

Adverse reactions are listed by System Organ Class. Frequencies are defined using the following convention: very common (≥1/10); common ( ≥1/100 to <1/10); uncommon (≥1/1,000 to ≤1/100); rare (≥1 / 10,000 to ≤1 / 1,000); very rare (≤1 / 10,000); not known (cannot be estimated from the available data).

System Organ Class

Frequency

Adverse Reaction

Gastrointestinal Disorders

Uncommon

Nausea, vomiting, and diarrhoea

Very Rare

Gastrointestinal bleeding

Not known

Gastric discomfort

Immune System Disorders

Rare

Urticaria and bronchospasm **

Very Rare

Rash

Cardiac Disorders

Rare

Palpitations

Musculoskeletal and connective tissue disorders

Rare

Muscle Pain

Nervous System Disorders

Rare

Headache, dizziness, urinary incontinence, palpitations

Respiratory, thoracic and mediastinal disorders

Rare

Shortness of Breath

Not known

Bronchorrhoea

Skin and subcutaneous tissue disorders

Not known

Stevens-Johnsons syndrome, erythema multiforme

Endocrine Disorders

Not known

Hypothyroidism *

* Special attention in patients with compromised thyroid function due to the risk of transient hypothyroidism occurrence.

** Special attention in asthmatic to the risk of bronchoconstriction occurrence (contraction of a muscle of the bronchial wall that leads to a reduction in airflow). In these cases, treatment discontinuation is recommended.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme, website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.

4.9 Overdose

Gastric lavage may be beneficial, followed by observation. Gastrointestinal disorders is the most likely symptom of overdosage. In such cases, it is advised to reduce the dosage.

5. Pharmacological properties
5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Mucolytic, ATC code: R05CB03

Carbocisteine (S-carboxymethyl L-cysteine) has been shown in normal and bronchitic animal models to affect the nature and amount of mucus glycoprotein which is secreted by the respiratory tract. An increase in the acid:neutral glycoprotein ratio of the mucus and a transformation of serous cells to mucus cells is known to be the initial response to irritation and will normally be followed by hypersecretion. The administration of carbocisteine to animals exposed to irritants indicates that the glycoprotein that is secreted remains normal; administration after exposure indicates that return to the normal state is accelerated. Several studies have demonstrated that carbocisteine reduces goblet cell hyperplasia. Carbocisteine can therefore be demonstrated to have a role in the management of disorders characterised by abnormal mucus.

5.2 Pharmacokinetic properties

Carbocisteine is rapidly absorbed from the gastrointestinal tract. In a study, at steady state (7 days). Carbocisteine capsules 375mg given as 2 capsules three times daily to healthy volunteers gave the following pharmacokinetic parameters:

Plasma Determinations

Mean

Range

T Max (Hr)

2.0

1.0-3.0

T½ (Hr)

1.87

1.4-2.5

KEL (Hr-1)

0.387

0.28-0.50

AUC0-7.5 (mcg.Hr.ml-1)

39.26

26.0-62.4

Derived Pharmacokinetic Parameters

*CLS (L.Hr-1)

20.2

-

CLS (ml.min-1)

331

-

VD (L)

105.2

-

VD (L.Kg-1)

1/75

-

5.3 Preclinical safety data

There are no preclinical data of relevance to the prescriber, which are additional to those already included in other sections of the SmPC.

6. Pharmaceutical particulars
6.1 List of excipients

Glycerol

Sodium Methyl Parahydroxybenzoate

Saccharin Sodium,

Sodium Hydroxide

Hydrochloric acid

Hydroxyethyl cellulose

Purified Water

Strawberry Flavour

Caramel Colorant

6.2 Incompatibilities

Not applicable

6.3 Shelf life

30 months

After opening, use within 6 months

6.4 Special precautions for storage

Do not store above 25°C.

6.5 Nature and contents of container

300ml type III amber glass bottles, with a polypropylene Safety Screw Cap with a measuring device in the form of a 2.5-15 mL measuring dosing plastic cup graduated to 2.5 ml and an oral dosing syringe which is marked per 0.25ml.

6.6 Special precautions for disposal and other handling

Any unused medicinal product or waste material should be disposed of in accordance with local requirements

7. Marketing authorisation holder

Aspire Pharma Limited

Unit 4 Rotherbrook Court

Bedford Road

Petersfield, Hampshire

GU32 3QG

United Kingdom

8. Marketing authorisation number(s)

PL 35533/0182

9. Date of first authorisation/renewal of the authorisation

23/12/2020

10. Date of revision of the text

12/07/2021

Company Contact Details
Aspire Pharma Ltd
Address

4 Rotherbrook Court, Bedford Road, Petersfield, Hampshire, GU32 3QG, UK

Telephone

+44 (0)1730 231148

Customer Care direct line

+44 (0)1730 231148

WWW

http://www.aspirepharma.co.uk

Medical Information Direct Line

+44 (0)1730 231148