CARBOCISTEINE 375 MG CAPSULES - summary of medicine characteristics

1 NAME OF THE MEDICINAL PRODUCT

Carbocisteine 375mg Capsules

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Each capsule contains carbocisteine 375mg.

For the full list of excipients, see section 6.1.

3 PHARMACEUTICAL FORM

Capsule, hard.

Size 0 capsule with opaque blue cap and opaque yellow body, containing white to off-white odourless powder.

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

Dosage is based upon an initial daily dosage of 2250 mg carbocisteine (6 capsules) in divided doses, reducing to 1500 mg (4 capsules) daily in divided doses when a satisfactory response is obtained. For example, two capsules three times a day reducing to one capsule four times a day.

Paediatric population

This formulation is not recommended for use in children.

Method of administration

For oral use.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

Use in patients with active peptic ulceration.

4.4 Special warnings and precautions for use

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

4.5 Interaction with other medicinal products and other forms of interaction There are no known interactions with other medicinal products or other forms of interaction.

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 breast-feeding. The use of carbocisteine in breast-feeding women is not recommended.

4.7 Effects on ability to drive and use machines

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

4.8 Undesirable effects

The following CIOMS frequency rating is used, when applicable: 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).

Immune system disorders

There have been reports of anaphylactic reactions, allergic skin eruption and fixed drug eruption.

Gastrointestinal disorders

There have been reports of diarrhoea, nausea, epigastric discomfort and gastrointestinal bleeding occurring during treatment with carbocisteine.

Frequency not known: vomiting, gastrointestinal bleeding

Skin and subcutaneous tissue disorders

There have been reports of skin rashes and allergic skin eruptions. Isolated cases of dermatitis bullous such as Stevens-Johnson syndrome and erythema multiforme have also been reported.

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 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 disturbance is the most likely symptom of carbocisteine overdosage.

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Mucolytic, ATC code: R05C B03

Mechanism of action

Carbocisteine (5-carboxymethyl L-cysteine) has been shown in normal and bronchitic animal models to affect the nature and amount of mucus glycoprotein that 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 secreted remains normal; administration after exposure indicates that return to the normal state is accelerated.

Studies in humans have demonstrated that carbocisteine reduces goblet cell hyperplasia. Carbocisteine can therefore play a role in the management of disorders characterised by abnormal mucus.

5.2 Pharmacokinetic properties

Absorption

Carbocisteine is rapidly absorbed from the GI tract.

Distribution

Equilibrium pharmacokinetics were established in healthy volunteers following administration of carbocisteine 375mg capsules, 2 capsules t.d.s. for seven days. The mean Tmax was 2.0 hours (range 1.0 –3.0); T^ 1.87 hours (range 1.4 – 2.5); KEL 0.387 hour-1 (range 0.28 – 0.50) and AUC0–7.5 was 39.26 mcg.hr/ml (range 26.0 – 62.4).

Values for derived pharmacokinetic values were CLS 331ml.min-1; VD 105.2 L and VD 1.4 L/Kg.

5.3 Preclinical safety data

No additional data of relevance to the prescriber.

6.1

Capsule contents:

Microcrystalline Cellulose

Macrogol

Magnesium Stearate

Capsule:

Gelatin

Titanium dioxide (E171)

Iron Yellow Oxide (body, E172)

Brilliant Blue FCF (cap, E133)

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

5 years.

6.4 Special precautions for storage

Store below 25°C.

6.5 Nature and contents of container

The capsules are packed in PVC/Aluminium blisters containing 20, 30, 60, 100 and 120 capsules. Not all pack sizes may be marketed.

6.6 Special precautions for disposal

No special requirements.

7 MARKETING AUTHORISATION HOLDER

Accord Healthcare Limited

Sage House

319 Pinner Road

North Harrow

Middlesex

HA1 4HF

United Kingdom

8 MARKETING AUTHORISATION NUMBER(S)

PL 20075/0670