Diclofenac, 100 mg 20 pcs

A nonsteroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid.

Diclofenac has anti-inflammatory, analgesic, antiaggregant and antipyretic effects.

Indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), disrupts arachidonic acid metabolism, reduces the number of prostaglandins in the focus of inflammation. It is most effective for pain of inflammatory nature.

In rheumatic diseases the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness and joint swelling and improves the functional state of the joint.

In case of injury and in the postoperative period diclofenac reduces pain and inflammatory swelling.

Absorption is fast and complete, food slows the rate of absorption by 1-4 hours and reduces the maximum concentration (Cmax) by 40%.

After oral administration of 100 mg tablets, Cmax – 0.5 mcg/ml is reached after -4-5 hours. Plasma concentrations are linearly related to the amount of the administered dose.

There is no change in pharmacokinetics of diclofenac on repeated administration. It does not cumulate if the recommended interval between doses is observed.

The bioavailability is 50%. Binding with plasma proteins is more than 99% (most of it is bound with albumin). It penetrates into synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma.

The half-life (T½) of synovial fluid is 3-6 h (the concentration of the active substance in synovial fluid is higher in synovial fluid 4-6 h after administration than in plasma and stays higher for 12 h).

The relationship between the concentration of the drug in synovial fluid and the clinical efficacy of the drug has not been elucidated.

Metabolism: 50% of the active substance is metabolized during the “first passage” through the liver.

Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid.

The CYP2C9 isoenzyme is involved in metabolism of the drug. The pharmacological activity of the metabolites is lower than that of diclofenac.

The systemic clearance is about 260±50 ml/min, the volume of distribution is 550 ml/kg.

T½ from plasma averages about 2.5 hours. 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile.

In patients with severe renal insufficiency (creatinine clearance (CK) less than 10 ml/min) excretion of metabolites in bile is increased, while there is no increase in their blood concentrations.

In patients with chronic hepatitis or compensated liver cirrhosis pharmacokinetic parameters of diclofenac are not changed.

Diclofenac penetrates into breast milk.

Indications

Symptomatic treatment of musculoskeletal system disorders (rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Behterev’s disease);

Particular arthritis, rheumatic soft tissue lesions, osteoarthritis of peripheral joints and spine including radicular syndrome, tendovaginitis, bursitis).

The drug relieves or reduces pain and inflammation during treatment, while not affecting the progression of the disease.

Pain syndrome of mild to moderate severity: neuralgia, myalgia, lumboinsychialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodysmenorrhea, adnexitis, proctitis, toothache.

In the complex treatment of infectious and inflammatory diseases of the ear, throat, nose, with a pronounced pain syndrome (pharyngitis, tonsillitis, otitis).

Active ingredient

Composition

One film-coated sustained release tablet contains:

The active ingredient:

Diclofenac sodium 100.0000 mg;

Associates:

Saccharose – 94.7880 mg,

Cetyl alcohol – 54.8200 mg,

Silicon dioxide colloid – 0.7900 mg,

Talc – 3.9500 mg,

Povidone K-25 – 1.0530 mg,

Magnesium stearate – 7.8990 mg;

Shell:

Hypromelose – 3.4355 mg,

Titanium dioxide E 171 CI 77891 – 0.8649 mg,

Talc – 2.4178 mg,

Polysorbate 80 – 0.3826 mg,

Macrogol 6000 – 0.6894 mg,

Punsenic dye [Ponceau 4R] [E124] – 0.0441 mg, brown dye [sunset yellow dye [E110] + azorubin dye [E122] + diamond black dye [E151]] – 0.0147 mg, aluminum varnish based on sunset yellow dye [E110] – 0.0500 mg.

How to take, the dosage

In all patients receiving diclofenac, it should be used in the lowest effective dose for the shortest time required to reduce the severity of symptoms.

Overly, without chewing, with or after meals, with plenty of water.

1 tablet once a day. If additional dosing is necessary, 50 mg tablets are used. The maximum daily dose is 150 mg.

Interaction

Directions for use

Special Instructions

In order to reduce the risk of adverse events, the drug should be used in 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 slightly increased risk of serious cardiovascular thrombotic complications (including myocardial infarction and stroke).

In patients with significant cardiovascular risk factors (e.g., arterial hypertension, hyperlipoproteinemia, diabetes mellitus, and smoking), treatment with diclofenac preparations should be initiated only after careful evaluation and assessment.

Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing the drug in patients with cardiac or renal insufficiency, hypertension,

Elderly patients, patients taking diuretics or other drugs that affect renal function, or patients who have a decreased circulating blood volume for any reason (e.g., after extensive surgery)

If diclofenac is prescribed in these cases, it is recommended that renal function be monitored as a precaution.

After discontinuation of therapy with the drug, normalization of renal function to baseline values is usually noted.

When using diclofenac there have been events such as bleeding or gastrointestinal ulcers/perforations, in some cases with fatal outcome.

These events can occur at any time when using the drug in patients with or without pre-existing symptoms and a history of serious gastrointestinal disease.

In elderly patients, such complications may have serious consequences.

If patients receiving diclofenac develop gastrointestinal bleeding or ulceration, the drug should be discontinued.

In order to reduce the risk of gastrointestinal toxicity, the drug should be used in the lowest effective dose for the shortest time possible, particularly in patients with gastrointestinal ulcers, especially those with a history of bleeding or perforation, and in older patients.

Patients at increased risk of gastrointestinal complications, as well as those receiving therapy with low-dose acetylsalicylic acid or other medications that can increase the risk of gastrointestinal damage, should take gastroprotective agents.

Patients with a history of gastrointestinal damage, especially the elderly, should inform their physician of any digestive symptoms.

Long-term therapy should include monitoring of liver function, peripheral blood count, and fecal occult blood tests.

In prolonged use of diclofenac an increase in activity of one or more “liver” enzymes may be noted.

If liver function abnormalities persist and progress or signs of liver disease or other symptoms (e.g., eosinophilia, rash, etc.) the drug must be stopped.

It should be noted that hepatitis with diclofenac may occur without prodromal signs.

Precautions must be taken when using diclofenac in patients with hepatic porphyria because the drug may provoke attacks of porphyria.

Diclofenac may reversibly inhibit platelet aggregation; therefore, in patients with hemostasis disorders during long-term use it is necessary to monitor closely the corresponding laboratory parameters.

In patients with bronchial asthma, seasonal allergic rhinitis, nasal mucosal edema (including with nasal polyps), chronic obstructive pulmonary disease, chronic respiratory tract infections

(especially associated with allergic rhinitis-like symptoms), and in patients with allergies to other medications (rash, itching, urticaria) special caution must be exercised when diclofenac is prescribed (readiness for resuscitation).

In the use of diclofenac, severe, in some cases fatal, skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis have very rarely been reported.

The highest risk and incidence of severe dermatologic reactions were noted in the first month of treatment with diclofenac.

If patients receiving the drug develop the first signs of skin rash, mucosal lesions or other symptoms of hypersensitivity, diclofenac should be discontinued.

The anti-inflammatory effects of NSAIDs, including diclofenac, can make it difficult to diagnose infections.

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

When taking 100 mg tablets for patients with diabetes, take into consideration the sucrose content of the drug (1 tablet contains 94.7880 mg of sucrose).

Impact on driving and operating machinery

Patients who have visual disturbances, dizziness, somnolence or other central nervous system disorders while using diclofenac should not drive motor vehicles or operate machinery.

Synopsis

Features

Contraindications

Side effects

Criteria for evaluating the frequency of adverse reactions: very common (>1/10), common (≥1/100, < 1/10), infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000) and very rare (< 1/10000); frequency is unknown – the frequency cannot be determined from available data.

Gastrointestinal disorders:

often – epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia;

Rarely – gastritis, proctitis, gastrointestinal (GI) bleeding (vomiting with blood, melena, diarrhea with blood mixed in), GI ulcers (with or without bleeding or perforation);

very rarely – stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn’s disease, occurrence of diaphragm-like strictures in the intestine, constipation, pancreatitis.

Liver and biliary tract disorders:

often – increased aminotransferase activity;

rarely – hepatitis, jaundice, impaired liver function;

very rarely – fulminant hepatitis, liver necrosis, liver failure.

Nervous system disorders:

often – headache, dizziness; rarely – somnolence; very rarely – sensory disorders, including paresthesias, memory disorders, tremors, seizures, anxiety, cerebrovascular disorders, aseptic meningitis.

Mental disorders: very rarely – disorientation, depression, insomnia, nightmares, irritability, mental disorders.

Sense organs disorders:

often – vertigo;

very rarely – visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disorders.

Renal and urinary tract disorders:

very rarely – acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

Disorders of the blood and lymphatic system:

very rarely – thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis, eosinophilia.

Disorders of the immune system:

anaphylactic/anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock;

very rare – angioedema (including facial).

Disorders of the cardiovascular system:

very rarely – palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

Respiratory system disorders:

Thoracic and mediastinal organs: rarely – exacerbation of bronchial asthma, cough, laryngeal edema; very rarely – pneumonitis.

Skin and subcutaneous tissue disorders:

often – skin rash; rarely – urticaria;

very rarely – bullous rashes, eczema, including.including multiforme and Stevens-Johnson syndrome, Lyell syndrome, exfoliative dermatitis, itching, hair loss, photosensitization, purpura, including allergic.

General disorders and disorders at the site of administration:

rarely – edema.

Overdose

Symptoms:

Vomiting, gastrointestinal bleeding, epigastric pain, diarrhea, dizziness, tinnitus, lethargy, seizures, rare – increased BP, acute renal failure, hepatotoxic effects, respiratory depression, coma.

Treatment:

Gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating BP increase, renal dysfunction, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis are ineffective (due to significant binding to proteins and intense metabolism).

Pregnancy use

There are insufficient data on the safety of diclofenac use in pregnant women.

Therefore, diclofenac should be administered in the first and second trimesters of pregnancy only when the expected benefit to the mother exceeds the potential risk to the fetus.

Diclofenac, like other prostaglandin synthesis inhibitors, is contraindicated in the last 3 months of pregnancy (inhibition of uterine contractility and premature closure of the fetal arterial duct may occur).

Diclofenac passes in small amounts into breast milk. To prevent undesirable effects on the baby, the drug should not be prescribed to breastfeeding women.

Breast-feeding should be stopped if the drug has to be used.

Similarities