Diclofenac, rectal suppositories 100mg, 10pcs

Composition

Active ingredient:

diclofenac 100 mg;

Auxiliary substances:

1,2-propylene glycol,

aerosil,

vitepsol

Pharmacological action

Pharmaceutical Group:

NSAIDs.

Pharmaceutical action:  

NSAIDs, a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effects. By indiscriminately inhibiting COX 1 and COX 2, it disrupts arachidonic acid metabolism and reduces the amount of Pg in the inflammatory focus. It is most effective for inflammatory pain. Like all NSAIDs, the drug has antiplatelet activity.

Pharmacokinetics:

Absorption-fast and complete, food slows down the rate of absorption. After oral use of 50 mg, Cmax – 1.5 mcg / ml, TCmax-2-3 hours.

Long-acting Diclofenac: as a result of the delayed release of the drug, Cmax in plasma is lower than that created by the introduction of short-acting drugs; however, it remains high for a long time after use. Cmax-0.5-1 mcg / ml, TCmax-5 hours after taking 100 mg of long-acting tablets.

After intravenous drip use of 75 mg, Cmax is 1.9 mcg / ml (5.9 mmol / l). After intravenous use, Cmax is 2.5 mcg / ml (8 mmol / L), TCmax is 20 min.

With rectal use, TCmax is 30 minutes.

The plasma concentration is linearly dependent on the amount of the administered dose.

There were no changes in the pharmacokinetics of diclofenac during repeated use. It does not accumulate if the recommended interval between meals is observed.

Bioavailability – 50%. Binding to plasma proteins is more than 99% (most of them are bound to albumins). Penetrates into breast milk, synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. T1 / 2 from synovial fluid – 3-6 hours (concentrations of the drug in synovial fluid 4-6 hours after its use are higher than in plasma, and remain higher for another 12 hours).

50% of the drug is metabolized during the” first pass ” through the liver; AUC is 2 times less after oral use of the drug than after parenteral use of the same dose. Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid. The CYP2C9 isoenzyme is also involved in drug metabolism. The pharmacological activity of the metabolites is less than that of diclofenac.

Systemic clearance is 260 ml / min. T1 / 2 from plasma – 1-2 h. 60% of the administered dose is excreted as metabolites through 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 less than 10 ml / min), the excretion of metabolites in the bile increases, while no increase in their concentration in the blood is observed.

In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters do not change.

Indications

Inflammatory and inflammatory-activated degenerative forms of rheumatism:  

• chronic polyarthritis;
• ankylosing spondylitis (Ankylosing spondylitis);
• arthrosis;
• spondyloarthritis;
• neuritis and neuralgia, such as cervical syndrome, lumbago (lumbago), sciatica;
• acute attacks of gout.

Rheumatic soft tissue lesions.

Painful swelling or inflammation after injuries or surgery.

Non-rheumatic inflammatory pain conditions.

Contraindications

Hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis and intolerance to ASA or other NSAIDs (including in the anamnesis), erosive and ulcerative lesions of the gastrointestinal tract and duodenum, active gastrointestinal bleeding, inflammatory bowel diseases, severe liver and heart failure; the period after coronary artery bypass grafting; severe renal insufficiency (creatinine clearance less than 30 ml/min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (third trimester), lactation, children (up to 14 years-for enteric-coated tablets 50 mg and rectal suppositories 50 mg, up to 18 years-for long – acting tablets and suppositories 100 mg).

For rectal use (optional): proctitis.

For medicinal products containing lactose (optional): hereditary lactose intolerance, glucose-galactose malabsorption, lactase deficiency.

With caution. Gastric ulcer and 12 duodenal ulcer, ulcerative colitis, Crohn’s disease, liver disease, a history of hepatic porphyria, chronic renal failure, CHF, hypertension, a significant decrease in BCC (including after extensive surgery),

elderly patients (including receiving diuretics, debilitated patients and those with a low body weight), bronchial asthma, concomitant use of corticosteroids (e. g. prednisone), anticoagulants (including warfarin), antiplatelet agents (including ASA, clopidogrel), selective inhibitors of serotonin reuptake (including citalopram, fluoxetine, paroxetine, and sertraline), ischemic heart disease, cerebrovascular disease, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral artery disease, Smoking, chronic renal failure (KK 30-60 ml/min), the presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe somatic diseases.

Side effects

From the digestive system:  nausea, vomiting, epigastric pain, anorexia, flatulence, constipation, gastritis up to erosive with bleeding, increased transaminase activity, drug-induced hepatitis, pancreatitis.

From the urinary system:  interstitial nephritis.

From the central nervous system:  headache, dizziness, disorientation, agitation, insomnia, irritability, fatigue, aseptic meningitis.

Respiratory system disorders:  bronchospasm.

From the hematopoietic system:  anemia, thrombocytopenia, leukopenia, agranulocytosis.

Dermatological reactions:  exanthema, erythema, eczema, hyperemia, erythroderma, photosensitization.

Allergic reactions:  erythema multiforme, Lyell’s syndrome, Stevens-Johnson syndrome, anaphylactic reactions, including shock.

Local reactions:  at the injection site, burning, infiltrate formation, and adipose tissue necrosis are possible.

Other services:  fluid retention in the body, edema, increased blood pressure.

Interaction

Concomitant use of Diclofenac with digoxin, phenytoin or lithium preparations may increase the plasma concentrations of these drugs; with diuretics and antihypertensive agents, the effect of these drugs may decrease; with potassium-sparing diuretics, hyperkalemia may develop; with acetysalicylic acid, a decrease in the concentration of diclofenac in blood plasma and an increased risk of side effects.

Diclofenac may increase the toxic effect of cyclosporine on the kidneys.

Diclofenac can cause hypo – or hyperglycemia, so when used concomitantly with hypoglycemic agents, monitoring of blood glucose concentration is required.

When using methotrexate for 24 hours before or after taking Diclofenac, it is possible to increase the concentration of methotrexate and increase its toxic effect.

When used concomitantly with anticoagulants, regular monitoring of blood clotting parameters is necessary.

How to take, course of use and dosage

Rectally. For adults:  100 mg 1 time a day,50 mg 2 times a day or 25 mg 3-4 times a day.

The maximum daily dose is 150 mg.

Children over 12 years of age: 50 mg 1-2 times a day or 25 mg 2-3 times a day.

Form of production

rectal suppositories

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 C. Keep out of reach of children.

Active ingredient

Diclofenac

Conditions of release from pharmacies

By prescription

Dosage form

rectal suppositories

Description

Pregnant women in the first and second trimester as prescribed by a doctor, For adults, Pregnant women as prescribed by a doctor

Indications

Bursitis, Sciatica, Periarthritis, Adnexitis, Osteoarthritis, Lumbago, Swelling after injuries and operations, Tendon inflammation, Osteoarthritis, Arthritis