Relipain Drug Information [ Gerolymatos ]

Table of content

Relipain category:

• Human
• Cyclooxygenase-2 COX-2 Inhibitors
• Other Nonsteroidal Antiimflammatory Agents

Active ingredients:

• Diclofenac Sodium

Relipain companies and manufacturers:

• Gerolymatos

General Information

Relipain forms, composition and dosages:

• N / A

Indications, usages and classification codes:

• M01AB05 - Diclofenac

There is an additional general information about this medication active ingredient diclofenac:

Pharmacological action

NSAIDs, a derivative of phenylacetic acid, diclofenac has a pronounced anti-inflammatory, analgesic and mild antipyretic effect. The mechanism of action is associated with inhibition of COX activity - the main enzyme metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).
Inhibits synthesis of proteoglycan in cartilage.
In rheumatic diseases, diclofenac reduces joint pain at rest and in motion, as well as morning stiffness and swelling of the joints, helps to increase range of motion; reduces post-traumatic and postoperative pain, and inflammatory edema.
Inhibits platelet aggregation. With prolonged use has a desensitizing effect.
When used topically in ophthalmology reduces swelling and pain in inflammatory processes non-infectious etiology.

Pharmacokinetics

After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach C_max in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.
Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, C_max is achieved in 2-4 hours later than in plasma.
To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than diclofenac.
Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.

Why is Relipain by Gerolymatos prescribed?

Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of musculoskeletal system (osteochondrosis, osteoarthritis, periartropatii), post-traumatic inflammation of soft tissue and musculoskeletal system (sprains, bruises). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after surgery or injury, pain in gout, migraine, algomenorrhea, pain with Bursitis, proctitis, colic (biliary and renal), pain in infectious and inflammatory diseases of ENT organs.
For local use: the inhibition of miosis during surgery for cataract prevention of cystoid macular edema associated with removal and lens implantation, inflammatory eye non-infectious nature, post-traumatic inflammation in penetrating and nonpenetrating wound of the eyeball.

Dosage and administration

For oral use for adult single dose is 25-50 mg 2-3 times / 24 h. Frequency of admission depends on the dosage form employed, the severity of the disease and is 1-3 times / 24 h, rectally - 1 times / 24 h, for the treatment of acute conditions or the exacerbation of chronic edema use intramuscular in dose of 75 mg.
For children older than 6 years and adolescents daily dose is 2 mg / kg.
Topical applied at a dose of 2-4 g (depending on the size of painful area) on the affected area 3-4 times / 24 h.
When used in ophthalmology frequency and duration of administration are determined individually.
The maximum oral daily dose for adults is 150 mg.

Relipain by Gerolymatos side effects

Digestive system: nausea, vomiting, anorexia, abdominal pain and discomfort in the epigastrium, flatulence, constipation, diarrhea, and in some cases - erosive-ulcerative lesions, gastrointestinal bleeding and perforation; rarely - abnormal liver function. When rectal administration - in isolated cases were observed inflammation of the colon bleeding, exacerbation of ulcerative colitis.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue, rarely - paresthesia, visual disturbances (blurred, double vision), tinnitus, insomnia, cramps, irritability, tremors, mental disorders, depression.
Hemopoietic system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis.
Urinary system: rarely - renal failure; in predisposed patients may be swelling.
Dermatological reactions: rarely - hair loss.
Allergic reactions: skin rash, itching, when used in the form of eye drops - itching, redness, photosensitivity.
Local reactions: in the place of I.M. introducing possible burning, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue in the rectal administration may be local irritation, the appearance of mucous discharge mixed with blood, painful defecation, when used externally, in rare cases - itching, redness, rash, burning sensation, when applied topically in ophthalmology may be a transient burning sensation and / or temporary blurred vision immediately after instillation.
With long-term topical use and / or drawing on a vast surface of body are possible systemic side effects due to resorptive action of diclofenac.

Contraindications

known hypersensitivity to diclofenac sodium or to any accessory ingredient that is part of the drug diclofenac;
anamnestic information about the attacks of bronchial asthma, urticaria, acute rhinitis associated with the use of aspirin or other NSAIDs;
hemodyscrasia unknown origin;
children under 6 years
pregnancy (III trimester);
lactation
increased sensitivity to sulfite (for injection solution).
children under age 15 - tablets of 50 mg to 18 years - injection.

Using during pregnancy and breastfeeding

Use during pregnancy and lactation is possible in cases where the potential benefits for the mother exceeds than the potential risk to the fetus or newborn.

Special instructions

With extreme caution is used in diseases of liver, kidney, gastrointestinal history, dyspepsia, asthma, hypertension, heart failure, after major surgery, as well as elderly patients.
When referring to a history of allergic reactions to NSAIDs diclofenac and sulfites are used only in urgent cases. In the course of treatment requires systematic monitoring of liver function and kidney picture of peripheral blood.
Do not recommended the use for rectal patients with diseases of anorectal region or anorectal bleeding in history. Topical should be applied only to intact skin areas.
Avoid contact with diclofenac in the eye (except for eye drops), or on mucous membranes. Patients who use contact lenses, eye drops should be applied no earlier than 5 minutes after removing the lenses.
Not recommended for children under 6 years.
During the period of treatment drugs for systemic use is not recommended alcohol consumption.
During the period of treatment may decrease the speed of psychomotor reactions. With worsening blurred vision after application of eye drops should not be driving and doing other potentially danger activities.

Relipain by Gerolymatos drug interactions

At simultaneous application with diclofenac antihypertensive drugs may be weakening their actions.
There are few reports on the occurrence of seizures in patients taking both NSAIDs and antibacterial drugs quinolic series.
At simultaneous application with GCS and increased risk of side effects from the digestive system.
With simultaneous use of diuretics may decrease diuretic effect. With the simultaneous use of potassium-sparing diuretics may increase the concentration of potassium in the blood.
With simultaneous use with other NSAIDs may increase the risk of side effects.
There are reports of hypoglycemia or hyperglycemia in patients with diabetes who engaged in diclofenac together with hypoglycemic drugs.
When applied simultaneously with acetylsalicylic acid may decrease the concentration of diclofenac in plasma.
Although clinical studies have not found the influence of diclofenac on the action of anticoagulants, describes the individual cases of bleeding when used with diclofenac and warfarin.
With simultaneous use may increase digoxin, lithium, and phenytoin in blood plasma.
The absorption of diclofenac from the gastrointestinal tract is reduced by simultaneous application with kolestiraminom, to a lesser extent - with colestipol.
With simultaneous use may increase the concentration of methotrexate in plasma and increased its toxicity.
With simultaneous application of diclofenac could not affect the bioavailability of morphine, but the concentration of the active metabolite of morphine may be enhanced in the presence of diclofenac, which increases the risk of side effects metabolites of morphine, including respiratory depression.
When applied simultaneously with pentazocine described a case of great convulsions, and rifampicin - may decrease the concentration of diclofenac in plasma, with ceftriaxone - increases excretion of ceftriaxone in bile; with cyclosporine - may increase cyclosporine nephrotoxicity.

Relipain by Gerolymatos in case of emergency / overdose

Symptoms: may cause hypotension, renal failure, convulsions, gastrointestinal irritation or respiratory depression. Treatment: There is no specific antidote. In acute poisoning as soon as possible to stop drug absorption from the gastrointestinal tract. There is indicated gastric lavage, activated charcoal appointment and conduct of other symptomatic and supportive therapy. The use of forced diuresis, dialysis or blood transfusion is not justified because NSAIDs largely associated with serum proteins and possess extensive metabolism.

Storage conditions

In a dry, protected from light place, at temperature not above 25°C. Common expiration date for diclofenac: 3 years.

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