Diclofenac tablets: instructions for use

Diclofenac in different forms of release: indications for use

Medicine in tablets, injections, ointments, gels, suppositories can be used for short-term suppression of painful sensations that arise as a consequence of:

osteochondrosis, rheumatic tissue lesions, osteoarthrosis, arthritis;
sciatica, peripheral nerve damage, lumbago;
gout, migraines;
inflammation in the pelvic area, injuries and surgical interventions.

Suppositories are prescribed as an addition to the main therapy for complex inflammatory processes such as otitis, laryngitis, and pharyngitis.

Injection administration of Diclofenac according to the instructions is recommended to obtain a quick analgesic effect. The drug is administered for renal and hepatic colic, acute pain syndrome in damaged muscles, after surgery. Prevention and treatment of postoperative discomfort is carried out by intravenous infusion of Diclofenac.

Eye drops are prescribed to patients:

to prevent inflammation and swelling during surgical interventions;
with penetrating and non-penetrating injuries of the eyeballs;
to suppress discomfort during laser vision correction.

What does Disclofenac tablets help with: the indications are similar to the injectable forms of the medication. It is sometimes used to relieve toothache. Gel and ointment are used to treat disorders of the locomotor system, rectal suppositories are used when it is impossible to take the medication orally.

Suppositories are safer and are not capable of causing complications from parenteral administration of Diclofenac: necrosis, infiltrates, suppuration at the needle entry site. Suppositories are used in combined regimens: tablets or injections are prescribed during the day, and rectal medications are prescribed at night. In gynecological practice, suppositories are prescribed for acute pain syndrome that occurs against the background of an inflammatory process in the ovaries or painful menstruation.

Diclofenac, 20 pcs., 50 mg, enteric-coated tablets

In order to reduce the risk of adverse events, the drug should be used at the lowest effective dose for the shortest period necessary to relieve symptoms.

Therapy with NSAIDs, including diclofenac, particularly long-term and high-dose therapy, may be associated with a small increased risk of serious cardiovascular thrombotic events (including myocardial infarction and stroke).

In patients with significant risk factors for cardiovascular events (eg hypertension, hyperlipoproteinemia, diabetes mellitus and smoking), treatment with diclofenac-containing products should only be initiated after careful evaluation and analysis.

Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing the drug to patients with cardiac or renal failure, hypertension, elderly patients, patients taking diuretics or other drugs that affect renal function, and patients with For some reason, there is a decrease in circulating blood volume (for example, after extensive surgery). If diclofenac is prescribed in such cases, monitoring of renal function is recommended as a precaution. After cessation of drug therapy, normalization of renal function indicators to initial values is usually observed.

When using diclofenac, phenomena such as bleeding or ulceration/perforation of the gastrointestinal tract, in some cases fatal, were observed. These phenomena may occur at any time when using the drug in patients with or without previous symptoms and a history of serious gastrointestinal diseases. In elderly patients, such complications can have serious consequences. If patients receiving diclofenac develop bleeding or ulceration of the gastrointestinal tract, the drug should be discontinued. To reduce the risk of toxic effects on the gastrointestinal tract, the drug should be used in the minimum effective dose for the shortest possible time, especially for patients with gastrointestinal ulcers. especially complicated by bleeding or perforation in history, as well as elderly patients.

Patients with an increased risk of developing gastrointestinal complications, as well as those receiving therapy with low doses of acetylsalicylic acid or other drugs that can increase the risk of damage to the gastrointestinal tract, should take gastroprotectors.

Patients with a history of gastrointestinal disorders, especially the elderly, should report all symptoms of the digestive system to their doctor.

When carrying out long-term therapy, it is necessary to monitor liver function, peripheral blood patterns, and stool analysis for occult blood.

With long-term use of diclofenac, there may be an increase in the activity of one or more liver enzymes. If liver dysfunction persists or progresses or signs of liver disease or other symptoms occur (for example, eosinophilia, rash, etc.), the drug should be discontinued. It should be borne in mind that hepatitis during the use of diclofenac can develop without prodromal phenomena.

Caution must be exercised when using diclofenac in patients with hepatic porphyria, since the drug can provoke attacks of porphyria.

Diclofenac can reversibly inhibit platelet aggregation, therefore, in patients with hemostasis disorders with long-term use, careful monitoring of relevant laboratory parameters is necessary.

In patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including nasal polyps), chronic obstructive pulmonary disease, chronic respiratory tract infections (especially those associated with allergic rhinitis-like symptoms), as well as in patients with allergies to other medications (rash, itching, urticaria) when prescribing diclofenac, special care should be taken (preparedness for resuscitation measures).

Severe, in some cases fatal, skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, have been very rarely reported with the use of diclofenac. The highest risk and incidence of severe dermatological reactions were observed in the first month of treatment with diclofenac. If patients receiving the drug develop the first signs of skin rash, damage to the mucous membranes or other symptoms of hypersensitivity, diclofenac should be discontinued.

The anti-inflammatory effect of NSAIDs, including diclofenac, may complicate the diagnosis of infectious processes.

Due to the negative effect on fertility, the drug is not recommended for women planning pregnancy. In patients with infertility (including those undergoing examination), it is recommended to discontinue the drug.

Contraindications and non-standard reactions from Diclofenac

The instructions indicate that the medication is not prescribed:

in case of individual intolerance to the component composition;
bleeding from the gastrointestinal tract, ulcers, perforation and inflammation of the digestive canal;
bronchial asthma arising under the influence of NSAIDs;
liver, kidney, heart failure.

Diclofenac is contraindicated for proctitis (in suppositories), after coronary artery bypass surgery, during pregnancy and for children under 6 years of age. Ointments and gels are not used for skin damage. Suppositories and tablets are prescribed to patients over 14 years of age. Increased caution is needed when treating patients with herpetic keratitis, children, the elderly, and nursing women.

The following side effects may occur when taking tablets:

dyspeptic disorders;
erosions and ulcers of the gastrointestinal tract;
bleeding in the digestive tract;
drowsiness, unreasonable irritability;
attacks of dizziness, allergies.

Diclofenac drops can provoke:

burning, cloudiness of the cornea;
decreased visual acuity (temporary);
allergies, iritis.

Intramuscular administration of the drug is sometimes accompanied by unpleasant sensations, and in difficult cases leads to tissue necrosis and abscess.

Pharmacological properties of the drug Diclofenac

NSAID, a derivative of phenylacetic acid with pronounced anti-inflammatory, analgesic and antipyretic activity. The pharmacological properties of diclofenac are due to its ability to inhibit the biosynthesis of certain prostaglandins as a result of inhibition of the enzyme prostaglandin synthetase. By blocking the synthesis of prostaglandins, diclofenac eliminates or significantly reduces the severity of symptoms of inflammation. Diclofenac reduces the increased sensitivity of nerve endings to mechanical stimuli and biologically active substances produced at the site of inflammation, induced by prostaglandins; leads to a decrease in body temperature, preventing the effect of prostaglandins on the hypothalamic link of the thermoregulation process; reduces the concentration of prostaglandins in menstrual blood and the intensity of pain during primary dysmenorrhea. The use of diclofenac helps to increase the range of motion in the affected joints, reduce pain at rest and during movement. In vitro , diclofenac at a concentration equivalent to that achieved in human tissue during treatment does not inhibit the biosynthesis of cartilage tissue proteoglycans. Inhibits platelet aggregation. Diclofenac is quickly and completely absorbed from the digestive tract. The maximum concentration in the blood after taking diclofenac orally in tablet form is achieved within 20–60 minutes. Eating at the same time slightly slows down the rate, but not the volume, of absorption. Considering that about 50% of diclofenac is metabolized during the first passage through the liver, the AUC when diclofenac is taken orally or used in the form of rectal suppositories is almost 2 times less than in the case of parenteral administration of an equivalent dose. After repeated administration of diclofenac, the pharmacokinetic parameters do not change. Almost 99.7% of diclofenac binds to serum proteins (mainly albumin). The apparent volume of distribution is 0.12–0.17 l/kg body weight. Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2–4 hours later than in the blood plasma. The apparent half-life from synovial fluid is 3–6 hours. 2 hours after reaching the maximum concentration in the blood plasma, the concentration of diclofenac in the synovial fluid remains higher; this pattern persists for approximately 12 hours. Biotransformation of diclofenac occurs partly by glucuronidation of the unchanged molecule, but mainly through single and multiple methoxylation, which leads to the formation of several phenolic metabolites (3′-hydroxy-, 4′-hydroxy-, 5′- hydroxy-, 4′,5-dihydroxy- and 3′-hydroxy-4′-methoxydiclofenac), most of which are conjugated with glucuronic acid. Two of them are pharmacologically active, but to a much lesser extent than diclofenac. The total systemic clearance of diclofenac from blood plasma is 263 ± 56 ml/min, the final half-life from blood plasma is 1–2 hours. The half-life of 4 metabolites, including two pharmacologically active ones, is also short and amounts to 1–3 hours. One of the metabolites is 3-hydroxy-4-methoxydiclofenac - has a longer half-life, but this metabolite is pharmacologically inactive. About 60% of administered diclofenac is excreted in the urine in the form of glucuronic conjugates of the intact molecule of the active substance and in the form of metabolites, most of which are also converted into glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The rest of the administered dose is excreted as metabolites in bile and feces. There are no significant changes in the pharmacokinetics of diclofenac in elderly people, patients with kidney disease, chronic hepatitis or compensated cirrhosis.

Special instructions for the use of Diclofenac

Prescribed with caution to persons with dyspeptic symptoms, diseases of the digestive tract, hypertension (arterial hypertension) or circulatory failure, renal failure, as well as patients who have recently undergone surgery. Throughout the course of treatment, it is recommended to monitor renal and liver function. When taking diclofenac for a long time, you should refrain from driving vehicles and performing potentially dangerous activities that require increased attention and speed of reactions. Taking diclofenac during pregnancy is contraindicated. During breastfeeding, it can be prescribed only according to strict indications and under close medical supervision.