Opilon tablets

1. Name Of The Medicinal Product

Opilon 40mg tablets

2. Qualitative And Quantitative Composition

Each tablet contains moxisylyte hydrochloride 45.22mg (equivalent to moxisylyte base 40mg).

3. Pharmaceutical Form

A pale yellow film-coated tablet

4. Clinical Particulars

4.1 Therapeutic Indications

Moxisylyte is an alpha-adrenergic blocking agent. Opilon tablets are indicated in the short term control of the symptoms of primary Raynaud's phenomenon.

4.2 Posology And Method Of Administration

Oral administration.

Adults:

Initially one tablet to be taken four times a day. This may be increased to two tablets four times a day if initial response is poor. For patients exposed to the cold during the daytime, one tablet should be administered every three hours during the period when symptoms are most likely to occur. In the event that a response is not evident within 2 weeks, the drug should be discontinued.

Elderly (over 65 years):

As for adults.

No clinical or pharmacokinetic data specific to this age group are available. Whilst at normal dosage no problems have been reported, caution nevertheless is advised when Opilon tablets are prescribed in the elderly.

Children:

Opilon tablets are not indicated for use in children.

4.3 Contraindications

Opilon tablets are contraindicated in those with a hypersensitivity to any of the ingredients or who have active liver disease.

4.4 Special Warnings And Precautions For Use

The alpha-adrenergic blocking action of Opilon tablets will produce a vasodilating effect which may theoretically potentiate the effect of a number of drugs used in the management of hypertension. In practice, with the recommended dosage of Opilon tablets, this has not been reported.

Opilon tablets should be used with caution in diabetes as, theoretically, insulin requirements may be reduced. Tricyclic antidepressants may increase any hypotensive effect produced by alpha blockade.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

See section 4.4 (Special Warnings and Precautions for Use).

4.6 Pregnancy And Lactation

The safety of Opilon tablets for use during pregnancy and lactation has not been established. Opilon tablets should not, therefore, be used by women who are pregnant or breast-feeding.

4.7 Effects On Ability To Drive And Use Machines

None known.

4.8 Undesirable Effects

Occasionally, mild nausea, diarrhoea, vertigo, headache, facial flushing and rash may be encountered. These are, however, rare and transient.

There have also been rare reports of hepatotoxicity, including cases of hepatitis and cholestatic jaundice, which are reversible on stopping treatment. Opilon tablets should be withdrawn promptly if hepatic dysfunction develops.

4.9 Overdose

In excessive overdosage a fall in blood pressure is the main symptom. The patient should be nursed in the supine position until the blood pressure has been restored to normal.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Moxisylyte is an alpha-adrenergic blocking agent which is used for the treatment of the symptoms of Raynaud's phenomenon.

5.2 Pharmacokinetic Properties

Moxisylyte is rapidly absorbed after oral administration. In plasma, the drug is rapidly converted to desacetylmoxisylyte (metabolite I) and desmethyldesacetylmoxisylyte (metabolite II) which are pharmacologically active. Other circulatory species are the sulphate and glucuronide conjugates of metabolites I and II. Excretion is almost exclusively via the kidneys. The half life of total radioactivity, after radiolabelled moxisylyte was administered to man, was 1 to 2 hours.

5.3 Preclinical Safety Data

There are no pre-clinical safety data of relevance to the prescriber which are additional to those already included in other sections of the Summary of Product Characteristics.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Lactose

Colloidal silicon dioxide

Microcrystalline cellulose

Magnesium stearate

Maize starch

The film coating contains:

Methylhydroxypropylcellulose

Propylene glycol

Opaspray M-1-22900 (E464, E171, E104, E124 and E132)

Water

6.2 Incompatibilities

None known.

6.3 Shelf Life

36 months.

6.4 Special Precautions For Storage

Store at a temperature not exceeding 30ºC.

6.5 Nature And Contents Of Container

Blister pack comprising white PVC and aluminium foil backing containing 112 tablets.

6.6 Special Precautions For Disposal And Other Handling

Not applicable.

7. Marketing Authorisation Holder

Archimedes Pharma UK Limited

250 South Oak Way

Green Park

Reading

Berkshire

RG2 6UG

UK

8. Marketing Authorisation Number(S)

PL 12406/0017

9. Date Of First Authorisation/Renewal Of The Authorisation

1 May 1999

10. Date Of Revision Of The Text

October 2008

11. Legal Category

POM

® Opilon is a registered trade mark

SPC0408