Flector Rapid (Solution) Instructions for Use

Marketing Authorization Holder

IBSA Institut Biochimique, S.A. (Switzerland)

Manufactured By

IBSA Farmaceutici Italia S.r.l. (Italy)

ATC Code

M01AB05 (Diclofenac)

Active Substance

Diclofenac (Rec.INN registered by WHO)

Dosage Forms

	Flector Rapid	Solution for intramuscular and subcutaneous administration 25 mg/ml: 1 ml amp. or syringes 1, 3 or 5 pcs.
		Solution for intramuscular and subcutaneous administration 50 mg/ml: 1 ml amp. or syringes 1, 3 or 5 pcs.
		Solution for intramuscular and subcutaneous administration 75 mg/ml: 1 ml amp. or syringes 1, 3 or 5 pcs.

Dosage Form, Packaging, and Composition

Solution for intramuscular and subcutaneous administration from colorless to yellowish-brownish, transparent.

Excipients : hydroxypropylbetadex – 110 mg, polysorbate 20 – 0.06 mg, water for injection – up to 1 ml.

1 ml – ampoules – cardboard packs.
1 ml – ampoules (3) – cardboard packs.
1 ml – ampoules (5) – cardboard packs.
1 ml – syringes complete with needles for subcutaneous administration 1 pc. and for intramuscular administration 1 pc. – cardboard packs.
1 ml – syringes (3) complete with needles for subcutaneous administration 3 pcs. and for intramuscular administration 3 pcs. – cardboard packs.
1 ml – syringes (5) complete with needles for subcutaneous administration 5 pcs. and for intramuscular administration 5 pcs. – cardboard packs.

Solution for intramuscular and subcutaneous administration from colorless to yellowish-brownish, transparent.

Excipients : hydroxypropylbetadex – 220 mg, polysorbate 20 – 0.12 mg, water for injection – up to 1 ml.

1 ml – ampoules – cardboard packs.
1 ml – ampoules (3) – cardboard packs.
1 ml – ampoules (5) – cardboard packs.
1 ml – syringes complete with needles for subcutaneous administration 1 pc. and for intramuscular administration 1 pc. – cardboard packs.
1 ml – syringes (3) complete with needles for subcutaneous administration 3 pcs. and for intramuscular administration 3 pcs. – cardboard packs.
1 ml – syringes (5) complete with needles for subcutaneous administration 5 pcs. and for intramuscular administration 5 pcs. – cardboard packs.

Solution for intramuscular and subcutaneous administration from colorless to yellowish-brownish, transparent.

Excipients : hydroxypropylbetadex – 330 mg, polysorbate 20 – 0.18 mg, water for injection – up to 1 ml.

1 ml – ampoules – cardboard packs.
1 ml – ampoules (3) – cardboard packs.
1 ml – ampoules (5) – cardboard packs.
1 ml – syringes complete with needles for subcutaneous administration 1 pc. and for intramuscular administration 1 pc. – cardboard packs.
1 ml – syringes (3) complete with needles for subcutaneous administration 3 pcs. and for intramuscular administration 3 pcs. – cardboard packs.
1 ml – syringes (5) complete with needles for subcutaneous administration 5 pcs. and for intramuscular administration 5 pcs. – cardboard packs.

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect.

The mechanism of action is associated with inhibition of COX activity, the main enzyme of arachidonic acid metabolism, which is a precursor of prostaglandins that play a major role in the pathogenesis of inflammation, pain and fever.

The analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).

It inhibits proteoglycan synthesis in cartilage.

In rheumatic diseases, it reduces joint pain at rest and during movement, as well as morning stiffness and joint swelling, and helps to increase the range of motion.

It reduces post-traumatic and postoperative pain, as well as inflammatory edema.

It suppresses platelet aggregation. With long-term use, it has a desensitizing effect.

When applied topically in ophthalmology, it reduces swelling and pain in inflammatory processes of non-infectious etiology.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, while the degree of absorption does not change. About 50% of the active substance is metabolized during the “first pass” through the liver.

With rectal administration, absorption occurs more slowly.

The time to reach C_max in plasma after oral administration is 2-4 hours depending on the dosage form used, after rectal administration – 1 hour, after intramuscular administration – 20 minutes.

The concentration of the active substance in plasma is linearly dependent on the applied dose.

It does not accumulate. Binding to plasma proteins is 99.7% (mainly with albumin). It penetrates into the synovial fluid, C_max is reached 2-4 hours later than in plasma.

It is largely metabolized to form several metabolites, two of which are pharmacologically active, but to a lesser extent than Diclofenac.

The systemic clearance of the active substance is approximately 263 ml/min. T_1/2 from plasma is 1-2 hours, from synovial fluid – 3-6 hours.

Approximately 60% of the dose is excreted as metabolites by the kidneys, less than 1% is excreted unchanged in the urine, the rest is excreted as metabolites with bile.

Indications

Joint syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathies), post-traumatic inflammation of soft tissues and the musculoskeletal system (sprains, contusions).

Back pain, neuralgia, myalgia, arthralgia, pain syndrome and inflammation after operations and injuries, pain syndrome in gout, migraine, algodysmenorrhea, pain syndrome in adnexitis, proctitis, colic (biliary and renal), pain syndrome in infectious and inflammatory diseases of the ENT organs.

For topical application: inhibition of miosis during cataract surgery, prevention of cystoid macular edema associated with lens removal and implantation, inflammatory processes of the eye of non-infectious nature, post-traumatic inflammatory process in penetrating and non-penetrating wounds of the eyeball.

ICD codes

Dosage Regimen

For oral administration for adults, a single dose is 25-50 mg 2-3 times/day.

The frequency of administration depends on the dosage form used, the severity of the disease and is 1-3 times/day, rectally – 1 time/day.

For the treatment of acute conditions or relief of exacerbation of a chronic process, it is administered intramuscularly at a dose of 75 mg.

For children over 6 years of age and adolescents, the daily dose is 2 mg/kg.

For topical use, apply 2-4 g (depending on the area of the painful area) to the affected area 3-4 times/day.

When used in ophthalmology, the frequency and duration of administration are determined individually.

Maximum daily dose for adults when taken orally is 150 mg/day.

Adverse Reactions

From the digestive system nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases – erosive and ulcerative lesions, bleeding and perforations of the gastrointestinal tract; rarely – impaired liver function.

With rectal administration, in isolated cases, inflammation of the colon with bleeding, exacerbation of ulcerative colitis were noted.

From the central nervous system and peripheral nervous system dizziness, headache, agitation, insomnia, irritability, feeling of fatigue; rarely – paresthesia, visual disturbances (blurred vision, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremor, mental disorders, depression.

From the hematopoietic system rarely – anemia, leukopenia, thrombocytopenia, agranulocytosis.

From the urinary system rarely – impaired renal function; in predisposed patients, edema is possible.

Dermatological reactions rarely – hair loss.

Allergic reactions skin rash, itching; when used in the form of eye drops – itching, redness, photosensitization.

Local reactions at the site of intramuscular injection, burning is possible, in some cases – formation of infiltrate, abscess, necrosis of adipose tissue; with rectal administration, local irritation, appearance of mucous discharge with an admixture of blood, painful defecation are possible; with topical application in rare cases – itching, redness, rash, burning; with topical application in ophthalmology, transient burning sensation and/or temporary blurred vision immediately after instillation are possible.

With long-term topical application and/or application to large body surfaces, systemic side effects due to the resorptive action of diclofenac are possible.

Contraindications

Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin triad”, hematopoiesis disorders of unclear etiology, hypersensitivity to diclofenac or other NSAIDs.

Use in Pregnancy and Lactation

Use during pregnancy and lactation is possible in cases where the intended benefit to the mother outweighs the potential risk to the fetus or newborn.

Use in Hepatic Impairment

Use with particular caution in patients with a history of liver disease.

Use in Renal Impairment

Use with particular caution in patients with a history of kidney disease.

Pediatric Use

Not recommended for use in children under 6 years of age.

Geriatric Use

Use with particular caution in elderly patients.

Special Precautions

Use with particular caution in patients with a history of liver, kidney, gastrointestinal diseases, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after major surgical interventions, as well as in elderly patients.

In case of a history of allergic reactions to NSAIDs and sulfites, Diclofenac should be used only in emergency cases.

During treatment, systematic monitoring of liver and kidney function, peripheral blood picture is necessary.

Rectal administration is not recommended in patients with anorectal diseases or a history of anorectal bleeding.

Topical application should be used only on intact skin areas.

Avoid contact of diclofenac with the eyes (except for eye drops) or mucous membranes.

Patients using contact lenses should apply eye drops no earlier than 5 minutes after removing the lenses.

Not recommended for use in children under 6 years of age.

During treatment with systemic dosage forms, alcohol consumption is not recommended.

Effect on ability to drive vehicles and mechanisms

During treatment, a decrease in the speed of psychomotor reactions is possible.

If clarity of vision deteriorates after using eye drops, you should not drive a car or engage in other potentially hazardous activities.

Drug Interactions

With simultaneous use of antihypertensive drugs with diclofenac, their effect may be weakened.

There are isolated reports of seizures in patients taking NSAIDs and quinolone antibacterial drugs simultaneously.

With simultaneous use with corticosteroids, the risk of side effects from the digestive system increases.

With simultaneous use of diuretics, a decrease in the diuretic effect is possible.

With simultaneous use with potassium-sparing diuretics, an increase in the concentration of potassium in the blood is possible.

With simultaneous use with other NSAIDs, the risk of side effects may increase.

There are reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus who used Diclofenac simultaneously with hypoglycemic drugs.

With simultaneous use with acetylsalicylic acid, a decrease in the concentration of diclofenac in the blood plasma is possible.

Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, isolated cases of bleeding have been described with simultaneous use of diclofenac and warfarin.

With simultaneous use, an increase in the concentration of digoxin, lithium and phenytoin in the blood plasma is possible.

Absorption of diclofenac from the gastrointestinal tract decreases with simultaneous use with cholestyramine, to a lesser extent – with colestipol.

With simultaneous use, an increase in the concentration of methotrexate in the blood plasma and an increase in its toxicity are possible.

With simultaneous use, Diclofenac may not affect the bioavailability of morphine, however, the concentration of the active metabolite of morphine may remain elevated in the presence of diclofenac, which increases the risk of side effects of the morphine metabolite, including respiratory depression.

With simultaneous use with pentazocine, a case of a major seizure has been described; with rifampicin – a decrease in the concentration of diclofenac in the blood plasma is possible; with ceftriaxone – the excretion of ceftriaxone with bile increases; with cyclosporine – an increase in the nephrotoxicity of cyclosporine is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.