Praxilene

1. Name Of The Medicinal Product

Praxilene 100mg Capsules

2. Qualitative And Quantitative Composition

100mg naftidrofuryl oxalate equivalent to 81.0 mg naftidrofuryl and 19.0 mg oxalate.

3. Pharmaceutical Form

Capsule

4. Clinical Particulars

4.1 Therapeutic Indications

Peripheral vascular disorders - intermittent claudication, night cramps, rest pain, incipient gangrene, trophic ulcers, Raynaud's Syndrome, diabetic arteriopathy and acrocyanosis.

Cerebral vascular disorders - cerebral insufficiency and cerebral atherosclerosis, particularly where these manifest themselves as mental deterioration and confusion in the elderly.

4.2 Posology And Method Of Administration

Peripheral vascular disorders - one or two capsules three times daily for a minimum of three months, or at the discretion of the physician.

Cerebral vascular disorders - one 100mg capsule three times daily for a minimum of three months, or at the discretion of the physician.

There is no recommended use for children.

Administration:

For oral administration. The capsules should be swallowed whole during meals with a sufficient amount of water (minimum) of one glass.

4.3 Contraindications

Hypersensitivity to the drug. Patients with a history of hyperoxaluria or recurrent calcium-containing stones.

4.4 Special Warnings And Precautions For Use

A sufficient amount of liquid should be taken during treatment to maintain an adequate level of diuresis.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

None known.

4.6 Pregnancy And Lactation

Pregnancy: There is no, or inadequate, evidence of the safety of naftidrofuryl oxalate in human pregnancy, but it has been in wide use for many years without apparent ill consequence, animal studies having shown no hazard. If drug therapy is needed in pregnancy, this drug can be used if there is no safer alternative.

Lactation: No information is available.

4.7 Effects On Ability To Drive And Use Machines

None known.

4.8 Undesirable Effects

Naftidrofuryl oxalate is normally well tolerated in the dosage recommended. Occasionally nausea, epigastric pain and rashes have been noted.

Rarely, hepatitis has been reported. Very rarely, calcium oxalate kidney stones have been reported.

4.9 Overdose

Signs and symptoms: Depression of cardiac conduction and convulsions may occur.

Treatment: The stomach should be emptied by gastric lavage and emesis. Activated charcoal may be employed if necessary. Cardiovascular function and respiration should be monitored and, in severe cases, electrical pacemaking or the use of isoprenaline should be considered. Convulsions may be managed by diazepam.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Naftidrofuryl oxalate has been shown to exert a direct effect on intracellular metabolism. Thus it has been shown in man and animals that it produces an increase of ATP levels and a decrease of lactic acid levels in ischaemic conditions, evidence for an enhancement of cellular oxidative capacity. Furthermore, naftidrofuryl oxalate is a powerful spasmolytic agent.

5.2 Pharmacokinetic Properties

Naftidrofuryl oxalate is well absorbed when given orally. Peak plasma levels occur about 30 minutes after dosing and the half life is about an hour, although inter subject variation is relatively high. Accumulation does not occur at a dose level of 200mg three times daily.

The drug becomes extensively bound to plasma proteins and is excreted principally via the urine, all in the form of metabolites.

5.3 Preclinical Safety Data

No toxic effects were seen in animal studies which provide additional information to that obtained in man. In repeated dose studies the no effect level was 25mg/kg/day or greater. There was no evidence of effects on reproduction below doses which caused maternal toxicity.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Talc

Magnesium Stearate

Purified Water*

Denatured Ethanol*

Capsule Shells:

Erythrosine (E127)

Titanium Dioxide (E171)

Gelatine

Printing ink:

Black iron oxide (E172)

*Not present in final product

6.2 Incompatibilities

None known.

6.3 Shelf Life

36 months.

6.4 Special Precautions For Storage

Store below 20°C in a dry place away from light.

6.5 Nature And Contents Of Container

Pack size 10 (medical sample), 21 and 84 capsules:-

Cardboard carton containing blister strips comprising heat-sealable PVC (250μm) and aluminium foil (30μm).

Pack size 100 and 500:

Polyethylene securitainers with tamper evident closures.

6.6 Special Precautions For Disposal And Other Handling

None.

7. Marketing Authorisation Holder

Merck Serono Ltd

Bedfont Cross

Stanwell Road

Feltham

Middlesex

TW14 8NX, UK

8. Marketing Authorisation Number(S)

PL 11648/0064

9. Date Of First Authorisation/Renewal Of The Authorisation

24 March 2009

10. Date Of Revision Of The Text

24 March 2009