SUMMARY OF PRODUCT CHARACTERISTICS

1 NAME OF THE MEDICINAL PRODUCT

Carbocisteine 375mg Capsules

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Each capsule contains carbocisteine 375mg.

For a 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

For oral use.

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.

Children:

This formulation is not recommended for use in children.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients. Active peptic ulceration.

4.4 Special warnings and precautions for use

There are no known special warnings or precautions for use.

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

Although tests in mammalian species have revealed no teratogenic effects, carbocisteine is not recommended during the first trimester of pregnancy.

Lactation

It is unknown whether carbocisteine and / or its metabolites are excreted in human milk. A risk to the newborn or infant cannot be excluded.

A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from carbocisteine therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman.

4.7 Effects on ability to drive and use machines

None known

4.8 Undesirable effects

Rare (>1/10,000 to <1/1,000)

Immune System Disorders

Anaphylactic reactions and fixed drug eruption

Gastrointestinal disorders

Gastrointestinal bleeding

Skin and subcutaneous tissue disorders Skin rashes and allergic skin eruptions

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

4.9 Overdose

Gastric lavage may be beneficial, followed by observation. Gastrointestinal disturbance is the most likely symptom of carbocisteine overdosage.

5    PHARMACOLOGICAL PROPERTIES

5.1    Pharmacodynamic properties

Pharmacotherapeutic group: Mucolytic, ATC code: R05C B03

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

Carbocisteine is rapidly absorbed from the GI tract. Equilibrium pharmacokinetics were established in healthy volunteers following administration of carbocisteine 375mg capsules, 2 capsules t.d.s. for seven days. The mean T_max was 2.0 hours (range 1.0 -3.0); T/ 1.87 hours (range 1.4 - 2.5); K_EL 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 CL_S 331ml.min^-1; V_D 105.2 L and V_D 1.4 L/Kg.

5.3 Preclinical safety data

No additional data of relevance to the prescriber.

6    PHARMACEUTICAL PARTICULARS

6.1    List of excipients

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.