Tabuk-DI (Tablets) Instructions for Use

Marketing Authorization Holder

TABUK PHARMACEUTICALS, MFG. Co. (Saudi Arabia)

ATC Code

M01AB05 (Diclofenac)

Active Substance

Diclofenac (Rec.INN registered by WHO)

Dosage Forms

	Tabuk-DI	Film-coated tablets, 25 mg: 10, 20, 30, 40, 60 or 80 pcs.
		Film-coated tablets, 50 mg: 10, 20, 30, 40, 60 or 80 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light pink in color, round, biconvex; on cross-section – white or almost white.

10 pcs. – blisters (1) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (2) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (3) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (4) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (1) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (2) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (3) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (4) made of PVC/PVDC film and aluminum foil – cardboard packs.

Film-coated tablets light pink in color, round, biconvex; on cross-section – white or almost white.

10 pcs. – blisters (1) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (2) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (3) made of PVC/PVDC film and aluminum foil – cardboard packs.
10 pcs. – blisters (4) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (1) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (2) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (3) made of PVC/PVDC film and aluminum foil – cardboard packs.
20 pcs. – blisters (4) made of PVC/PVDC film and aluminum foil – cardboard packs.

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic, and antipyretic effect.

The mechanism of action is based on the inhibition of prostaglandin synthesis (which play a major role in the pathogenesis of inflammation, pain, and fever) by suppressing the cyclooxygenase (COX) enzyme.

In traumatic and postoperative conditions, the drug quickly reduces the severity of pain (including pain during movement), as well as tissue swelling in inflammation and injuries.

In primary dysmenorrhea, the drug relieves pain and reduces bleeding intensity. The drug may temporarily inhibit platelet aggregation.

Pharmacokinetics

After oral administration, Diclofenac potassium is rapidly absorbed from the gastrointestinal tract.

C_max in blood plasma is reached within 40 minutes.

V_d is 550 ml/kg. Diclofenac potassium penetrates into the synovial fluid and is excreted in breast milk. It is metabolized to form inactive metabolites (glucuronic and sulfate conjugates).

More than 50% of the dose is excreted in the urine within the first 4 hours. 30-35% of the dose is excreted in bile as metabolites.

Indications

For the rapid relief of pain and short-term therapy of the following acute conditions

• Pain and inflammation after injuries and surgical interventions;
• Primary and secondary algodysmenorrhea;
• Adnexitis;
• Back pain;
• Arthralgia;
• As part of combination therapy for infectious and inflammatory diseases of the ENT organs with severe pain;
• Headache.

ICD codes

Dosage Regimen

Orally. The dose is set individually, depending on the severity of the pain syndrome.

To quickly achieve the desired therapeutic effect, the drug is taken 30 minutes before meals.

In other cases, it is taken before, during, or after meals, without chewing, with a sufficient amount of water.

Adults are prescribed a daily dose of 75-150 mg, divided into 2-3 doses. For adolescents over 14 years old, the daily dose is 75-100 mg in 2-3 doses.

For primary dysmenorrhea, the initial daily dose is 50-100 mg, the average daily dose is 50-150 mg, and the maximum daily dose is 200 mg.

For elderly patients, especially debilitated and weakened ones, the use of the drug in the minimum effective dose is recommended.

Tabuk-Di should be taken for no more than 5 days to relieve pain without consulting a doctor. If the pain persists within this period, you should urgently consult a doctor.

Adverse Reactions

Very common – >10%; common – >1% and <10%; uncommon – >0.1% and <1%; rare – >0.01 % and <0.1%; very rare – <0.01%.

From the digestive system common – epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rare – gastritis, proctitis, gastrointestinal bleeding (vomiting blood, melena, diarrhea with blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rare – stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn’s disease, constipation, pancreatitis, fulminant hepatitis.

From the nervous system common – headache, dizziness; rare – drowsiness; very rare – sensory disturbances, including paresthesia, memory disorders, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the sensory organs common – vertigo; very rare – visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disturbance.

From the urinary system very rare – acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the hematopoietic organs very rare – thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

Allergic reactions rare – anaphylactic/anaphylactoid reactions, including a pronounced decrease in blood pressure and shock; very rare – angioedema (including facial).

From the cardiovascular system very rare – palpitations, chest pain, increased blood pressure, vasculitis, myocardial infarction.

From the respiratory system rare – bronchial asthma (including shortness of breath); very rare – pneumonia.

From the skin common – skin rash; rare – urticaria; very rare – bullous eruptions, eczema, including multiforme and Stevens-Johnson syndrome, Lyell’s syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, including allergic.

Contraindications

• Complete or incomplete combination of bronchial asthma;
• Recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in history);
• Erosive and ulcerative lesions of the stomach and duodenum;
• Active gastrointestinal bleeding;
• Inflammatory bowel diseases (Crohn’s disease, ulcerative colitis);
• Severe hepatic and heart failure;
• The period after coronary artery bypass grafting;
• Severe renal failure (creatinine clearance less than 30 ml/min);
• Progressive kidney diseases;
• Active liver disease;
• Confirmed hyperkalemia;
• Pregnancy (III trimester);
• Lactation period;
• Children under 15 years of age;
• Hereditary lactose intolerance;
• Glucose-galactose malabsorption;
• Lactase deficiency;
• Hypersensitivity (including to other NSAIDs).

With caution

Peptic ulcer of the stomach and duodenum, ulcerative colitis, Crohn’s disease in history, history of liver diseases, hepatic porphyria, chronic hepatic insufficiency, chronic heart failure, arterial hypertension, significant decrease in circulating blood volume (including after extensive surgical intervention), elderly patients (including those receiving diuretics, debilitated patients and those with low body weight), bronchial asthma, simultaneous use of corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, chronic renal failure (creatinine clearance 30-60 ml/min), presence of Helicobacter pylori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases.

Use in Pregnancy and Lactation

No clinical studies have been conducted to study the effect of diclofenac during pregnancy.

Therefore, in the I and II trimesters of pregnancy, the drug is prescribed only if the potential benefit to the mother’s health outweighs the risk to the fetus.

The use of diclofenac is contraindicated in the III trimester of pregnancy due to possible uterine atony and/or premature closure of the arterial duct (ductus arteriosus).

Diclofenac penetrates into breast milk in small amounts, therefore it is not recommended for use during breastfeeding to prevent undesirable side effects in the child.

Use in Hepatic Impairment

Contraindicated in active liver disease and severe hepatic failure.

In patients with hepatic insufficiency (chronic hepatitis, compensated liver cirrhosis), the kinetics and metabolism do not differ from those in patients with normal liver function.

Use in Renal Impairment

Contraindicated

• Severe renal failure (creatinine clearance less than 30 ml/min);
• Progressive kidney diseases.

Due to the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing to patients with cardiac or renal failure, as well as during therapy for elderly patients taking diuretics, and patients in whom, for any reason, there is a decrease in circulating blood volume (including after extensive surgical intervention).

If Diclofenac is prescribed in such cases, it is recommended to monitor renal function as a precaution.

Pediatric Use

Contraindicated in children under 15 years of age.

Geriatric Use

For elderly patients, especially debilitated and weakened ones, the use of the drug in the minimum effective dose is recommended.

Special Precautions

Due to the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing to patients with cardiac or renal failure, as well as during therapy for elderly patients taking diuretics, and patients in whom, for any reason, there is a decrease in circulating blood volume (including after extensive surgical intervention).

If Diclofenac is prescribed in such cases, it is recommended to monitor renal function as a precaution.

In patients with hepatic insufficiency (chronic hepatitis, compensated liver cirrhosis), the kinetics and metabolism do not differ from those in patients with normal liver function.

During long-term therapy, it is necessary to monitor liver function, peripheral blood picture, and stool analysis for occult blood.

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

To reduce the risk of adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible course.

Effect on the ability to drive vehicles and mechanisms

During treatment, a decrease in the speed of mental and motor reactions is possible, therefore it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, convulsions, with significant overdose – acute renal failure, hepatotoxic effect.

Treatment gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating increased blood pressure, impaired renal function, convulsions, gastrointestinal irritation, respiratory depression.

Forced diuresis, hemodialysis are not very effective (due to significant protein binding and intensive metabolism).

Drug Interactions

Increases the plasma concentration of digoxin, methotrexate, lithium preparations and cyclosporine.

Reduces the effect of diuretics; against the background of potassium-sparing diuretics, the risk of hyperkalemia increases; against the background of anticoagulants, antiplatelet and thrombolytic drugs (alteplase, streptokinase, urokinase), the risk of bleeding increases.

Reduces the effect of antihypertensive and hypnotic drugs.

Increases the likelihood of side effects of other NSAIDs and corticosteroids (gastrointestinal bleeding), the toxicity of methotrexate and the nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Simultaneous use with paracetamol increases the risk of nephrotoxic effects of diclofenac.

Reduces the effect of hypoglycemic drugs.

Cefamandole, cefoperazone, cefotetan, valproic acid and plicamycin increase the incidence of hypoprothrombinemia.

Cyclosporine and gold preparations enhance the effect of diclofenac on prostaglandin synthesis in the kidneys, which is manifested by increased nephrotoxicity.

Selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding.

Simultaneous administration with ethanol, colchicine, corticotropin and St. John’s wort preparations increases the risk of gastrointestinal bleeding.

Drugs that cause photosensitization increase the sensitizing effect of diclofenac to UV radiation.

Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its efficacy and toxicity.

Antibacterial drugs from the quinolone group – risk of seizures.

Storage Conditions

Store the drug in a dry place protected from light, at a temperature from 15°C (59°F) to 30°C (86°F). Keep out of reach of children.

Shelf Life

Shelf life – 3 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

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.