Begsan®

Topical relief of mild to moderate pain in painful and inflammatory states of soft tissues.

4.2     Posology and method of administration

Adults and over 15-year old adolescents: The gel is applied to the treated body area 1‑2 times a day and gently massaged into the skin. The skin of the treated area should be intact. The amount of gel used depends on the size of the treated area. Daily amount should not exceed 15 g (7.5 g corresponds to about 14 cm of gel). The duration of the treatment course is individual (1 to 10 days). The gel is meant for external use.

4.3     Contraindications

-        History of any photosensitivity reaction.

-        Known hypersensitivity reactions, such as symptoms of asthma, allergic rhinitis to ketoprofen, fenofibrate, tiaprofenic acid, acetylsalicylic acid or to other non-steroidal anti‑inflammatory drugs (NSAID) and the excipients of the drug.

-        History of skin allergy to ketoprofen, fenofibrate, tiaprofenic acid or UV blocker or parfumes.

-        Sun exposure, even in case of hazy sun, including UV light from solarium, during the treatment and 2 weeks after its discontinuation.

-        Injured or inflammatory skin (e.g. eczema, acne, open wounds); the drug should be not applied into the eyes or near them or to mucosal membranes.

-        Children and adolescents, as sufficient data in this age group are absent.

-        Last trimester of pregnancy.

4.4    Special warnings and precautions for use

Contact with mucous membranes, eyes or injured skin should be avoided, if rash occurs the use of the drug should be discontinued. Hands should be washed thoroughly after each application of the product.

It is recommended to protect treated areas by wearing clothing during all the application of the product and 2 weeks following its discontinuation to avoid the risk of photosensitisation.

Treatment should be discontinued immediately upon development of any skin reaction including cutaneous reactions after co-application of octocrylene containing products.

If huge amounts of gel are used, systemic adverse effects, including hypersensitivity and asthma, may occur.

The gel should be used with caution in patients with renal impairment.

The gel should be not used with occlusion dressing.

The drug should not be used in children and adolescents under 15 years of age.

Begsan 25 mg/g gel contains methyl parahydroxybenzoate (E 218) and propyl parahydroxybenzoate (E 216) as excipients, which may cause allergic reactions (incl. late-type).

4.5     Interaction with other medicinal products and other forms of interaction

The bioavailability of externally applied ketoprofen is low; therefore the possibility of interactions is unlikely.

4.6     Pregnancy and lactation

Pregnancy

There is no data about externally applied ketoprofen during pregnancy. Animal testing does not reveal any direct or indirect harmful effects on pregnancy, development of foetus, delivery or postnatal development.

During the first and second trimester of pregnancy the drug should be used only after careful consideration of the risk-benefit ratio.

During the third trimester of pregnancy all prostaglandin synthesis inhibitors, including ketoprofen, may cause cardiopulmonary and renal toxicity to the foetus. Also the prostaglandin synthesis inhibitors may prolong the bleeding time in mother and child. Therefore Begsan 25 mg/g gel should not be used during the last trimester of pregnancy.

Lactation

Although the bioavailability of externally applied ketoprofen is low and harmful effects on the child during external administration unlikely, the use of Begsan 25 mg/g gel is not recommended during breast-feeding.

4.7     Effects on ability to drive and use machines

Not relevant.

4.8     Undesirable effects

Skin and subcutaneous tissue disorders

Local skin reactions may develop, which may expand further than the treated area and may be serious and generalised in individual cases.

Uncommon adverse effects (<1/100, >1/1 000): erythema, pruritis, eczema and burning sensation.

Rare adverse effects (<1/1 000, >1/10 000): photosensitivity, urticaria, bullous or phyctenular eczema which may spread or become generalized.

Immune system disorders

Hypersensitivity reactions.

Very rare adverse effects (<1/10 000): angioedema.

A few cases of anaphylactic reactions have occurred.

If the gel is used for long time and/or in huge amounts, systemic adverse reactions characteristic to non-steroidal anti-inflammatory drugs may develop in individual cases.

As Begsan 25 mg/g gel contains alcohol, frequent use may cause skin dryness and irritation.

4.9     Overdose

The bioavailability of externally applied ketoprofen is low; therefore, the possibility of overdosage is unlikely.

Systemic adverse reactions may develop due to incorrect use (unintentional ingestion) or accidental overdosage: drowsiness, dizziness, nausea, vomiting, epigastric pain.

Treatment: There is no specific antidote. The treatment of overdose is symptomatic and generally supportive as in case of overdose of oral non-steroidal anti-inflammatory drugs. Gastric lavage and activated charcoal may be of benefit within 1 hour of ingestion of a potentially toxic amount. Forced diuresis, haemodialysis, or haemoperfusion are unlikely to be of benefit for NSAID overdosage. Renal and liver function should be closely monitored. Patients should be observed for at least four hours after ingestion of potentially toxic amounts.

Pharmacotherapeutic group: topical products for joint and muscular pain. ATC code: M02AA10

Ketoprofen is a non-steroidal anti-inflammatory and analgesic agent (derivative of phenyl propionic acid) which inhibits the synthesis of prostaglandins, thromboxanes and leukotrienes by inhibiting the activity of enzymes cyclooxygenase and lipooxygenase. The pain and oedema induced by the inflammation are reduced.

5.2     Pharmacokinetic properties

After repeated external administration of ketoprofen (e.g. 375 mg of ketoprofen) the ketoprofen plasma concentration is approximately 100 times lower than after single oral dose of 150 mg of ketoprofen.

Ketoprofen is metabolized to acyl glucoronides and excreted mainly with urine. The mean half-life of ketoprofen after repeated application is 17 hours and bioavailability about 5 %.

5.3     Preclinical safety data

Preclinical and clinical studies have shown no serious adverse effects although there have been controversial reports about the occurrence of systemic adverse effects.

Ethanol (96 per cent), carbomer, diethanolamine, lavender oil, methyl parahydroxybenzoate, neroli oil, propyl parahydroxybenzoate, water purified.

6.2     Incompatibilities

Not applicable.

6.3     Shelf life

2 years.

6.4              Special precautions for storage

Do not store above 25 ºC. Do not freeze.

6.5     Nature and contents of container

30 g or 50 g of gel in aluminium tube.

6.6     Special precautions for disposal and other handling

No special requirements.