Diclofenac, Levomenthol

Pharmacological properties

Diclofen gel, when applied topically, has a pronounced anti-inflammatory, analgesic, decongestant, and antiplatelet effect, which is associated with inhibition of the biosynthesis of prostaglandins, kinins, and other inflammatory mediators. the drug reduces the permeability of the vascular wall of the capillaries, stabilizes the membrane of lysosomes, reduces the temperature in the focus of inflammation.

Menthol, which is part of the drug, has a quick analgesic effect due to the cooling effect, enhancing the analgesic effect of diclofenac.

Diclofen gel helps to reduce swelling of the joints and periarticular tissues, reduces the severity of pain at rest and during movement, reduces morning stiffness, increases the range of motion in the joints, their functional and motor ability. Reducing the aggregation ability of platelets, the drug improves local microcirculation.

The amount of diclofenac penetrating the skin is proportional to the time of contact of the diclofen gel and the area of ​​the skin on which it is applied, and also depends on the dose of the drug and the degree of skin hydration. After applying Diclofen-gel to the skin surface, the absorption of diclofenac is about 6%. An occlusive dressing can increase diclofenac resorption several times. After topical application, diclofenac is determined in the blood plasma, synovial membrane and synovial fluid of the joints. Diclofenac binds to plasma proteins by 99%. Diclofenac metabolism occurs mainly by hydroxylation with the formation of several derivatives, two of which are pharmacologically active, but to a much lesser extent than diclofenac. Diclofenac and its metabolites are excreted mainly in the urine in the form of glucuronides.

In patients with kidney diseases, cumulation of diclofenac and its metabolites was not observed.

In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics and metabolism of diclofenac do not change.

Indications

Topical use in the treatment of inflammatory processes, pain with:

• localized forms of inflammatory and degenerative diseases of the joints and spine, including osteoarthritis, osteoarthritis of the peripheral joints and spine;
• soft tissue rheumatic diseases (including tenosynovitis, shoulder-hand syndrome, bursitis, periarthritis, periarthropathy);
• post-traumatic inflammation of the soft tissues, tendons, ligaments, muscles and joints (sprain, dislocation, overstrain, bruises, swelling).

Application

The drug is used externally. 1 g of diclofen gel (a strip of gel 2.5–3 cm long) is applied with an even thin layer to the skin and rubbed lightly for 1-2 minutes. After applying the drug, wash your hands (except in cases where the application is carried out on the area of ​​the hands). the procedure is repeated 2–4 times a day. the average daily dose for adults is 4–5 g of gel, which corresponds to 120–150 mg of diclofenac sodium.

The duration of treatment with Diclofen-gel for post-traumatic inflammation of the soft tissues or for rheumatic diseases of the soft tissues is 10-14 days, in the treatment of osteoarthritis - up to 4 weeks.

If necessary, the simultaneous use of diclofen gel with diclofenac tablets, the daily dose of the latter should not exceed 50 mg.

Contraindications

• Hypersensitivity to diclofenac, menthol or other components of the drug; a history of asthma attacks, urticaria, acute rhinitis or other allergic reactions caused by the use of acetylsalicylic acid or other NSAIDs; During pregnancy and breastfeeding; children under 15 years old.

Side effects

In this dosage form, diclofen gel is well tolerated.in some patients, if the application rules are not followed or in case of an overdose, local skin irritation phenomena may be noted: rarely - allergic or contact dermatitis with the formation of papules, bulla or skin desquamation; individual cases of photosensitization, the formation of infiltrate, abscess, adipose tissue necrosis are possible.

The occurrence of systemic side effects after topical application of Diclofen-gel is unlikely. Given the possibility of prolonged use, the application of the drug to large areas of the skin, the likelihood of using doses exceeding the recommended doses, the simultaneous use of drugs also containing diclofenac or other NSAIDs may indicate such adverse reactions (more typical for injectable and tablet forms of diclofenac):

from the gastrointestinal tract: heartburn, loss of appetite, nausea, vomiting, constipation or diarrhea, pain in the epigastric region, intestinal cramps, flatulence; rarely - ulcerogenic effect with or without bleeding or perforation; in some cases, the development of nonspecific hemorrhagic colitis, aphthous stomatitis, glossitis, damage to the esophagus, pancreatitis, exacerbation of hemorrhoids;

on the part of the kidneys: edema, in some cases - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, necrotizing papillitis;

on the part of the liver: toxic hepatitis may develop;

from the side of the central nervous system: dizziness, headache, very rarely - increased fatigue, in some cases - paresthesia, memory impairment, disorientation, insomnia, irritability, anxiety, depression, nightmares, tremors, psychotic reactions, convulsions, aseptic meningitis, visual impairment ( diplopia), hearing impairment (tinnitus), taste disturbance;

on the part of the cardiovascular system: tachycardia, chest pain, increased blood pressure, heart failure;

allergic reactions: in some cases, generalized skin rash, bullous rashes, eczema, polymorphic erythema, purpura, urticaria, erythroderma, Stevens-Johnson syndrome, Lyell syndrome (toxic epidermal necrolysis), bronchospasm;

changes in laboratory parameters: anemia, leukopenia, thrombocytopenia, agranulocytosis, a decrease or increase in the level of glucose and potassium in the blood, an increase in the activity of serum aminotransferases is possible.

The appearance of the above symptoms requires the abolition of the drug Diclofen-gel and the appointment of symptomatic treatment.

special instructions

Diclofen gel is used only externally.

The drug must be applied to intact skin. Do not allow the drug to get into the eyes and other mucous membranes, and in case of contact, rinse them with a sufficient amount of running water. Do not apply the gel under dressings that do not allow air (occlusal), it is necessary to avoid thermal procedures, insolation (including artificial) on the skin areas with the gel.

Do not use simultaneously with sunscreens, cosmetic creams, repellents or other local remedies in the areas of Diclofen-gel application.

You can dress no earlier than 10 minutes after applying the drug, take a shower / bath no earlier than 1 hour after application of the gel.

Be sure to wash your hands after the application procedure (except in cases where the application is carried out on the site of the hands).

Given the possible long-term use of the drug and / or application over a large area, it is prescribed with caution (taking into account the increased risk of adverse effects) to elderly people, weakened, with low body weight, with a history of gastrointestinal and ulcerative diseases, with BA, hematopoiesis, AH, heart failure, severe diseases of the liver, kidneys.

It should not be used simultaneously with other drugs containing diclofenac.

With prolonged use, periodic monitoring of the blood formula and the functions of the liver, kidneys, blood pressure monitoring, analysis of feces for occult blood is necessary.

Drinking alcohol, smoking increases the risk of gastrointestinal bleeding.

Use during pregnancy and lactation. The use of the drug during pregnancy is contraindicated. If it is necessary to use the drug during breastfeeding during the course of treatment, it is recommended to stop breastfeeding.

Children. There is no experience with children under the age of 15 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. There is no data on the ability of the drug Diclofen-gel to affect the reaction rate when driving vehicles or working with other mechanisms.

Interactions

When using diclofen gel, the possibility of interaction with other drugs is minimal. however, given the possibility of prolonged use, the use of doses exceeding the recommended doses of the drug on large areas of the skin, in the case of the simultaneous use of other drugs of diclofenac or other NSAIDs, the possibility of such interactions cannot be ruled out:

• with anticoagulants, antithrombotic agents, the risk of bleeding increases;
• Diclofen gel may decrease the effectiveness of antihypertensive therapy with angiotensin converting factor inhibitors;
• with acetylsalicylic acid or other NSAIDs, the risk of side effects increases;
• with glucocorticoids, alcohol, the ulcerogenic effect is enhanced;
• the use of Diclofen gel with digoxin, phenytoin, lithium preparations, quinolones can lead to an increase in the concentration of these drugs in blood plasma;
• Diclofen-gel can reduce the effectiveness of diuretics, when prescribed with potassium-sparing diuretics, the development of hyperkalemia is possible;
• the use of diclofen gel within 24 hours before or after taking methotrexate can lead to an increase in the concentration of methotrexate in blood plasma and, accordingly, to the manifestation of its toxic effects;
• when combined with oral hypoglycemic drugs, both hypo- and hyperglycemia may develop;
• Diclofen gel may enhance cyclosporin nephrotoxicity.

Overdose

No cases of overdose have been reported. given the method of application, when performing the dosing regimen and due to the low systemic absorption of diclofenac, an overdose of diclofen gel is unlikely. but with prolonged use of the drug in doses exceeding the recommended, and / or when applied to a large area of ​​the skin, the above systemic side effects may occur due to resorptive action.

Treatment. Remove or wash off the remaining gel from the skin. There is no specific antidote. Therapy is symptomatic. Forced diuresis is ineffective due to the high degree of binding of diclofenac with plasma proteins.

Storage conditions

At a temperature not exceeding 25 ° c.