Planil 2X Gel

White to practically white, cream-like gel.
PLANIL 2X GEL, each gram contains: Diclofenac diethylamine 23.2 mg.

Pharmacology: Pharmacodynamics: Diclofenac has pharmacological actions similar to those of other prototypical non-steroidal anti-inflammatory drugs (NSAIDs). It exhibits anti-inflammatory, analgesic, and antipyretic activity.
Diclofenac inhibits the synthesis of prostaglandins in body tissues by inhibiting cyclooxygenase (COX); at least 2 isoenzymes, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), have been identified that catalyze the formation of prostaglandins in the arachidonic acid pathway.
Diclofenac, like other prototypical NSAIDs, inhibits both COX-1 and COX-2. Although the exact mechanisms have not been clearly established, NSAIDs appear to exert anti-inflammatory, analgesic, and antipyretic activity principally through inhibition of the COX-2 isoenzymes; COX-1 inhibitory presumably is responsible for the drugs' unwanted effects on GI mucosa and platelet aggregation.
Pharmacokinetics: Absorption: Diclofenac is also absorbed into systemic circulation following topical application, but plasma concentrations generally are very low compared with oral administration.
Following topical application of diclofenac sodium (1%) gel (4 g) 4 times daily, to one knee, the mean peak plasma diclofenac concentrations of 15 ng/mL occur in about 14 hours. Likewise, when gel is applied to both knees and both hands 4 times daily (48g), the mean peak plasma diclofenac concentrations of 53.8 ng/mL occur in about 10 hours.
Application of a heat patch for 15 minutes before the application of the gel did not affect systemic absorption. Moderate exercise did not affect systemic absorption of the drug.
The absorption for diclofenac, 1% and 3%, gel may take around 10 to 14 hours and approximately 5 hours, respectively.
Distribution: Diclofenac is absorbed percutaneously when applied. At therapeutic concentrations, it is more than 99% bound to plasma proteins, mainly to albumin. Diclofenac penetrates synovial fluid where concentrations may persist even when plasma concentration fall. Only small amounts are distributed into breast milk. The terminal half-life is around 1 to 2 hours.
As diclofenac accumulates in the applied area, skin, acts as reservoir, which creates a sustained release of drug into the underlying tissues. It then preferentially distributes and persists in deep inflamed sites, rather than in blood stream.
Metabolism: The exact metabolic rate of diclofenac has not been fully elucidated, but the drug is rapidly and extensively metabolized in the liver. Diclofenac is metabolized to 4'-hydroxydiclofenac, 5-hydroxydiclofenac, 3'-hydroxydiclofenac, and 4', 5-dihydroxydiclofenac via hydroxylation, glucuronidation and sulfidation.
Excretion: Its glucuronide and sulfate conjugates are excreted mainly in the urine (about 60%) but also in the bile (about 35%); less than 1% is excreted as unchanged diclofenac.

For the relief of pain, inflammation, and swelling in: Soft-tissue injuries: trauma of the tendons, ligaments, muscles, and joints, e.g. due to sprains, strains, bruises, and backaches (sports injuries); Localized forms of soft tissue rheumatism: tendonitis (e.g. tennis elbow), bursitis, shoulder-hand syndrome, and periarthropathy.
For the relief of pain of non-serious arthritis of the knee or fingers localized forms of degenerative rheumatism e.g. osteoarthritis of the peripheral joints and of the vertebral column.

Adult and adolescents aged 12 years and over: PLANIL 2X GEL is administered by applying 2 times daily, morning and evening. It should be rubbed gently into skin at the affected area.
The amount needed depends on the size of the painful area: 2 g to 4 g (a quantity ranging in size from a cherry to a walnut) of gel is sufficient to treat an area of about 400-800 cm².
Wash the hands after each application, unless they are the site being treated.
The duration of treatment depends on the indication and clinical response. This should not be used for more than 14 days for soft-tissue injuries and soft tissue rheumatism, 21 days for arthritis pain, unless recommended by the doctor.
When used without prescription, patients should consult their doctor if the condition does not improve within 7 days, or if it gets worse.
Pediatric patients (under 12 years of age): PLANIL 2X GEL is not recommended for use in children below 12 years of age.
Elderly patients (over 65 years of age): The usual adult dosage may be used.

The low systemic absorption of topical diclofenac renders overdoses very unlikely. However, undesirable effects, similar to those observed following an overdose of orally administrated diclofenac, can be expected if PLANIL 2X GEL is ingested.
In the event of accidental ingestion resulting in significant systemic adverse effects, general therapeutic measures normally adopted to treat poisoning with NSAIDs should be used. Further management may require supportive treatment.

Hypersensitivity to diclofenac or any component of the formulation.
Patients with the history of hypersensitivity reactions, such as asthma, bronchospasm, urticaria, acute rhinitis or angioedema in response to acetylsalicylic acid (ASA) or non-steroidal anti-inflammatory drugs (NSAIDs).
The use in children and adolescents under 12 years of age.
During the last trimester of pregnancy.
The use on nonintact or damaged skin, including the exudative dermatitis, eczema, infected lesions, burns or wounds; avoid to come in contact with the eyes. In case, if any of the mentioned sites are in contact with PLANIL 2X GEL, rinse the sites with water or saline. Patients should consult with the doctor if the irritation persists.

The possibility of systemic adverse events cannot be excluded if the preparation is used on large areas of skin over a prolonged period. Therefore, it should be used with caution by patient with reduced renal function, heart function and liver function, including the ones with active peptic ulcer in both the stomach and duodenum. It is not recommended for patients with advanced renal disease.
PLANIL 2X GEL should be applied only to intact, non-diseased skin and not to skin wounds or open injuries and also not come into contact with the eyes or mucous membranes.
Avoid occlusive dressings and/or heat application to the treated area. The non-occlusive bandages can be used to support the treatment but must avoid an airtight occlusive dressing. Discontinue the treatment immediately, if a skin rash develops after applying the product.
Moreover, when the concomitant use of diclofenac sodium 1% gel with the oral NSAIDs, it may result in increased adverse effects.

The systemic concentration of diclofenac is lower after topical administration, compared to oral formulations. With reference to experience from treatment with NSAIDs with systemic uptake, the following is recommended: Pregnancy: Since NSAIDs, such diclofenac, inhibit the synthesis of prostaglandin which could affect with laboring, pregnancy prolongation, and fetal renal function, the treatment should avoid during the last trimester of pregnancy.
PLANIL 2X GEL should be used during the first two trimesters of pregnancy, only if the expected benefit justifies the potential risk to the fetus.
Breast-feeding: The excretion of the topical diclofenac in breast milk is unknown; however, regards to the distribution of diclofenac, small amount can be distributed into breast milk. Therefore, PLANIL 2X GEL should only be used during lactation if the expected benefit justifies the potential risk to the new born. If there are compelling reasons for using it, it should not be applied to the breasts or to large areas of skin, nor should it be used for a prolonged period.

Most common side effects for topical diclofenac, mostly appear at the application site, such as pain, rash, pruritus, erythema, paresthesia, dryness, vesicles, irritation, or papules.
When the gel is applied on large areas of skin and over a prolonged period, the possibility of systemic undesirable effects (e.g. renal, hepatic or gastrointestinal undesirable effects, systemic hypersensitivity reactions) as they occur possibly after systemic administration of diclofenac-containing medicinal products cannot be excluded.

Since systemic absorption of diclofenac from topical application is very low, such interactions are very unlikely.

Store at temperature not exceeding 30°C. Avoid freezing.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M02AA15 - diclofenac ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.

NDD