Nise^® Activgel (Gel) Instructions for Use

Marketing Authorization Holder

Dr. Reddy’s Laboratories, LLC (Russia)

Manufactured By

Dr. Reddy’s Laboratories Ltd. (India)

ATC Code

M01AX17 (Nimesulide)

Active Substance

Nimesulide (Rec.INN registered by WHO)

Dosage Form

Nise® Activgel

Gel for external use 1%: tubes 20 g, 50 g, or 100 g

Dosage Form, Packaging, and Composition

Gel for external use from colorless to pale yellow, transparent, homogeneous, with a characteristic odor.

Excipients: dimethyl sulfoxide, diethylene glycol monoethyl ether, propylene glycol, citric acid monohydrate, Sepineo P600 (copolymer of acrylamide/sodium acryloyldimethyltaurate, isohexadecane, polysorbate 80), flavor “Calm Valley”, purified water.

20 g – laminated aluminum tubes^x (1) – cardboard packs.
50 g – laminated aluminum tubes^x (1) – cardboard packs.
100 g – laminated aluminum tubes^x (1) – cardboard packs.

^x with first opening control

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID from the sulfonanilide class, a selective, competitive, reversible inhibitor of COX-2. When applied externally, it exerts a local analgesic and anti-inflammatory effect.

It reduces the concentration of short-lived prostaglandin H₂, a substrate for kinin-stimulated synthesis of prostaglandin E₂, at the site of inflammation and in the ascending pathways of pain impulse conduction in the spinal cord. The decrease in the concentration of prostaglandin E₂ (a mediator of inflammation and pain) reduces the activation of EP-type prostanoid receptors, which is manifested by analgesic and anti-inflammatory effects.

When applied externally, it causes a reduction or disappearance of pain at the site of application of the medicinal product, including joint pain at rest and during movement, reduces morning stiffness and joint swelling. Contributes to an increase in the range of motion.

Pharmacokinetics

When applied externally, the concentration of the active substance in the systemic circulation is extremely low. C_max after a single application is noted by the end of the first day, its value is more than 300 times lower than that for oral dosage forms of nimesulide. Traces of the main metabolite of nimesulide – 4-hydroxynimesulide are not detected in the blood.

Indications

Local symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system: joint syndrome during exacerbation of gout; rheumatoid arthritis; psoriatic arthritis; ankylosing spondylitis; osteoarthritis; osteochondrosis with radicular syndrome; radiculitis; inflammatory lesions of ligaments, tendons, bursitis; sciatica, lumbago; muscle pain of rheumatic and non-rheumatic origin; post-traumatic inflammation of soft tissues and the musculoskeletal system (injuries and ruptures of ligaments, contusions).

ICD codes

Dosage Regimen

Apply a sufficient amount of gel to cover the affected area three to four times daily.

Use a 3 cm (approx. 1.2 inch) strip of gel for an area the size of a palm.

Gently rub the gel into the skin until fully absorbed.

Do not apply to skin with open wounds, abrasions, or signs of infection.

Avoid contact with eyes and mucous membranes.

Wash hands thoroughly after application unless the hands are the treated area.

Do not use with occlusive or airtight dressings.

The maximum duration of self-treatment without medical consultation is 10 days.

Discontinue use and consult a physician if symptoms persist or worsen.

For pediatric patients (7 to 12 years), apply no more than twice daily under adult supervision.

In elderly patients, adhere to the standard regimen with increased monitoring for adverse effects.

Adverse Reactions

Local reactions itching, urticaria, peeling, transient skin discoloration (not requiring treatment discontinuation).

Systemic reactions when applied to large skin areas or with prolonged use, heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, increased activity of liver transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); thrombocytopenia, leukopenia, anemia, agranulocytosis, prolonged bleeding time.

Contraindications

Hypersensitivity to nimesulide, erosive-ulcerative lesions of the gastrointestinal tract in the acute phase, gastrointestinal bleeding, dermatoses, damage to the epidermis and skin infections in the area of application, severe renal failure (creatinine clearance <30 ml/min), severe hepatic failure, history of bronchospasm in connection with the use of acetylsalicylic acid or other NSAID, pregnancy, lactation period (breastfeeding), children under 7 years of age.

With caution

Hepatic insufficiency; renal insufficiency; severe heart failure; arterial hypertension; type 2 diabetes mellitus; elderly age, children.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency.

With caution hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal failure (creatinine clearance < 30 ml/min).

With caution renal insufficiency.

Pediatric Use

Contraindicated in children under 7 years of age.

With caution the drug should be prescribed to children over 7 years of age.

Geriatric Use

With caution the drug should be prescribed to elderly patients.

Special Precautions

It is recommended to apply only to intact skin areas, avoiding contact with open wounds.

Should not be used under airtight dressings.

Drug Interactions

Pharmacokinetic interaction with drugs competing for plasma protein binding cannot be excluded.

Nimesulide should be used with caution simultaneously with digoxin, phenytoin, lithium preparations, diuretics, cyclosporine, methotrexate, other NSAIDs, antihypertensive and hypoglycemic agents.

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

Over-the-Counter

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.