COMPOSITION

Each gram of gel contains:

Diclofenac Diethylamine BP 1.16% w/w

(Equivalent to Diclofenac sodium 1.0% w/w)

Menthol USP 5.0% w/w

Methyl Salicylate BP 10.0% w/w

Linseed oil BP 3.0% w/w

ADDITIONAL INGREDIENTS

Excipients: Propylene glycol, Carbomer 940, Disodium EDTA, Polysorbate 80, Sodium hydroxide, Benzyl alcohol, Purified water

INDICATIONS

Local treatment of inflammatory and dege

nerative forms of diseases of musculoskeletal system, which are accompanied by pain and swelling such as rheumatoid arthritis, ankylosing spondylitis (Bechterew’s disease), acute podagric (related to gout), inflammation, psoriatic and post-traumatic arthritis, rheumatic damage of soft tissues (tendonitis bursitis, myositis), degeneration diseases of joints (arthrosis of large and small joints), osteochondritis of spinal column, myalgia, neuralgia, lumbosacral radiculitis, trauma pain , ligamentous laxity, sprain of ligaments, muscles, tendons, pain in muscles and joints, induced by hard physical activity.

RECOMMENDED DOSE AND MODE OF ADMINSTRATION

Depending on area of painfulness 2-4 g of gel (strip is 4 to8 cm) is applied on skin is rubbed lightly 2-3 times per day. Average daily dose compound 10 g of gel, equivalent to 100 mg of Diclofenac.

The drug should not be applied on damaged skin. One should be careful to avoid accidental contact with the eyes and on mucous tunic. It shouldn’t apply the gel on open wound.

UNDESIRABLE EFFECTS

Generally, the preparation is tolerated well. The small part of drug (about 5 %) is absorbed into the bloodstream when used locally. It more or less eliminates possibility of side effects associated with NSAIDs.

Sometimes skin irritation such as, skin rash, oedema, appearance of wheals, papules, scutes, reddening, burning, prickling, skin itch occur at the site of application. If Diclofenac is used on large area for long duration following systemic side effects may appear occur, in cases of concurrent usage of Diclofenac tablets, suppository and/or ampoules

Side effects related to GIT, appearance of generalize rash, development of reaction of increased sensibility, such as oedema of face (angioedema), apnoea, photosensitivity is rare.

In a case of any unusual reactions it is necessary to consult the doctor immediately and stop the further usage of the medicine.

ADVERSE DRUG REACTIONS

*”Inform doctors about unexpected reactions after using drugs.”

INTERACTIONS WITH OTHER MEDICINAL PRODUCTS

Fanigan Fast Gel can be used along with other medicines, because the components of this drug do not interact systemically with other medicines, including use of Diclofenac sodium by oral route.

But in cases of long usage of Fanigan Fast Gel in large dosage it is necessary to know that Diclofenac can increase effect of anticoagulants, GCS, Lithium and it can decrease action of furosemide, thiazide diuretics. It can increase concentration of digoxin in plasma and decrease tolerance of other NSAID, increasing their ulcerogenic action on mucous coat of GIT.

The concurrent s local usage some medicines, containing NAAA, can irritate the skin locally in the form of urtricaria, reddening, desquamation.

PREGNANCY AND LACTATION

It is not allowed to apply gel on big areas of body or to use for a long time in last three months of pregnancy and during lactation period, because data about safety of the drug on foetus and neonates is not available.

WARNINGS AND PRECAUTIONS

Consult the doctor before using the medicine

The drug is prescribed carefully for patients with hypersensitivity to local usage of acetylsalicylic acid, different salicylates and other NSAID (bronchial asthma attacks, skin reactions and acute rhinitis). It is necessary to weigh all factors of usefulness and risk.

Fanigan is used carefully in patients with ulcer of the stomach or intestines, disorders of the liver and kidney, haematological disorders, relapse of nasal polyposis

It is necessary to wash hands after usage of medicine to avoid the accidental entry of drug in eyes and mucous tunics.

OVERDOSES AND TREATMENT

The overdose is not possible as a result of local application of Fanigan Fast Gel.

CONTRAINDICATIONS

• Hypersensitivity to Diclofenac and other components of this drug;

• Aspirin induced bronchial asthma;

• Break in the skin or open wound in area should be avoided

• Children below 12 years of age (because there is no data about external usage this medicine in this age group).

PHARMACEUTICAL FORM

Topical Gel

PHARMACOTHERAPEUTIC GROUP: Topical Anti inflammatory Agent

PHARMACOLOGICAL PROPERTIES:

PHARMACODYNAMIC PROPERTIES:

Action of each component of Fanigan Fast gel is explained as follows.

Diclofenac inhibits the cyclooxygenase, suppresses synthesis of prostaglandins – endogenous substances, which play a significant role in the genesis of the inflammation, pain, and fever. Diclofenac reduces pain, eliminates inflammation.

Menthol acts on the temperature receptors. It is gives sensation of coolness, constricts capillaries, and decrease of their permeability. It provides local counter-irritation and gentle analgesic actions.

Methyl salicylate is a derivative of salicylic acid, which has local irritation action. Methyl salicylate decreases the pain because of irritation of skin receptors. Methyl salicylate inhibits synthesis of prostaglandins, decreases swelling and infiltration of inflamed tissues.

Linseed oil is alfalinoleic acid, which has anti-inflammatory, antioxidant actions, improves blood circulation at place of application.

The action of medicine begins within few minutes after application on skin. During 20-30 min it achieves maximum activity level. It provides relief from the symptoms from day one of beginning of treatment.

PHARMACOKINETIC PROPERTIES

Absorption

When Diclofenac gel is applied topically, Diclofenac is absorbed into the epidermis. In a study in patients with com-promised skin (mainly atopic dermatitis and other dermatitis conditions) of the hands, arms or face, approximately 10% of the applied dose (2 grams of 3% gel over 100 cm2) of Diclofenac was absorbed systemically in both normal and compromised epidermis after seven days, with four times daily applications.

After topical application of 2 g Diclofenac gel three times daily for six days to the calf of the leg in healthy subjects, Diclofenac could be detected in plasma. Mean bioavailability parameters were AUC0-t 9±19 ng•hr/mL (mean±SD) with a Cmax of 4±5 ng/mL and a Tmax of 4.5±8 hours. In comparison, a single oral 75 mg dose of diclofenac produced an AUC of 1600 ng.hr/mL. Therefore, the systemic bioavailability after topical application of Diclofenac gel is lower than after oral dosing.

Blood drawn at the end of treatment from 60 patients with AK lesions treated with Diclofenac gel in three adequate and well-controlled clinical trials was assayed for Diclofenac levels. Each patient was administered 0.5 g of Diclofenac Gel twice a day for up to 105 days. There were up to three 5 cm X 5 cm treatment sites per patient on the face, forehead, hands, forearm, and scalp. Serum concentrations of Diclofenac were, on average, at or below 20 ng/mL. These data indicate that systemic absorption of Diclofenac in patients treated topically with Diclofenac gel is much lower than that occurring after oral daily dosing of Diclofenac sodium.

No information is available on the absorption of Diclofenac when Diclofenac gel is used under occlusion.

Distribution

Diclofenac binds tightly to serum albumin. The volume of distribution of diclofenac following oral administration is approximately 550 mL/kg.

Metabolism

Biotransformation of Diclofenac following oral administration involves conjugation at the carboxyl group of the side chain or single or multiple hydroxylation’s resulting in several

phenolic metabolites, most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically active, however to a much smaller extent than Diclofenac. Metabolism of Diclofenac following topical administration is thought to be similar to that after oral administration. The small amounts of Diclofenac and its metabolites appearing in the plasma following topical administration makes the quantification of specific metabolites imprecise.

Elimination

Diclofenac and its metabolites are excreted mainly in the urine after oral dosing. Systemic clearance of Diclofenac from plasma is 263±56 mL/min (mean±SD). The terminal plasma half-life is 1-2 hours. Four of the metabolites also have short terminal half-lives of 1-3 hours

Systemic exposure (area under the concentration-time curve) and maximum plasma concentrations of diclofenac are significantly lower with diclofenac Gel than with comparable oral treatment of Diclofenac sodium. Systemic exposure with recommended use of diclofenac Gel (4 x 4 g per day applied to 1 knee) is on average 17 times lower than with oral treatment.

(Basis: treatment with Diclofenac Gel of 1 knee, 4 times a day versus 50 mg, 3 times a day of oral diclofenac tablets). The amount of diclofenac sodium that is systemically absorbed from diclofenac Gel is on average 6% of the systemic exposure from an oral form of Diclofenac sodium. The average peak plasma concentration with recommended use of Diclofenac Gel (4 x 4 g per day applied to 1 knee) is 158 times lower than with the oral treatment. The pharmacokinetics of diclofenac Gel has been tested under conditions of moderate heat (application of a heat patch for 15 minutes prior to gel application) and of moderate exercise (first gel application followed by a 20-minute treadmill exercise). No clinically relevant differences of systemic absorption and of tolerability were found between applications of diclofenac Gel (4 x 4 g per day on 1 knee) with and under the conditions tested. However, the pharmacokinetics of diclofenac Gel was not tested under the condition of heat application following gel application. Therefore, concurrent use of Diclofenac Gel and heat is not recommended.

STORAGE CONDITION

Store below 30°C.

DOSAGE FORMS AND PACKAGING AVAILABLE

Fanigan Fast Gel is packed in 30 g or 100 g laminated tubes. A Tube and instruction pack insert is packed in carton package.

SHELF LIFE

2 years

NAME AND ADDRESS OF MANUFACTURER/MARKETING AUTHORIZATION HOLDER

Kusum Healthcare Private Limited

SP 289 (A), RIICO Industrial Area

Chopanki, Bhiwadi, India

DATE OF REVISION OF PACKAGE INSERT

Not Applicable