Diclofenac injections a course of treatment how many injections. Diclofenac: instructions for the use of tablets and ointments

1 ml of solution contains

active substance - diclofenac sodium 25 mg,

excipients: mannitol, benzyl alcohol, sodium metabisulfite, propylene glycol, sodium hydroxide, water for injection.

Description

Transparent solution from colorless to pale yellow.

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drugs. Acetic acid derivatives. Diclofenac

ATX code М01АВ05

Pharmacological properties

Pharmacokinetics

It is rapidly absorbed after intramuscular administration. The time to reach the maximum concentration when used at a dose of 75 mg is
15-30 minutes, the value of the maximum concentration is 1.9-4.8 (on average
2.7) μg / ml. 3 hours after administration, plasma concentrations average 10% of the maximum.

It is metabolized in the liver, mainly by oxidation and conjugation. About 99% binds to plasma proteins, mainly albumin. Approximately 2/3 of the administered dose is excreted in the urine, and the remainder in the bile. In 72 hours after administration, almost 90% of the administered dose is excreted from the body. It creates high concentrations in the synovial fluid. It passes into breast milk in small quantities. 50% of the drug is metabolized during the "first pass" through the liver. The area under the concentration-time curve (AUC) is two times less after oral administration of the drug than after parenteral administration of the same dose. In patients with chronic hepatitis or compensated cirrhosis of the liver, pharmacokinetic parameters do not change.

In patients with renal failure with creatinine clearance less than 10 ml / min, the excretion of metabolites in the bile increases, therefore, an increase in their concentration in plasma is not observed.

Pharmacodynamics

Diclofenac has anti-inflammatory and analgesic effects. By indiscriminately inhibiting cyclooxygenase (COX) 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammation focus. With injuries, in the postoperative period, Diclofenac reduces pain and inflammatory edema.

Indications for use

Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, gouty arthritis)

Degenerative diseases of the musculoskeletal system (osteoarthritis, osteochondrosis)

Neuralgia, myalgia

Tenosynovitis, bursitis

Post-traumatic pain syndrome with inflammation, postoperative pain syndrome

Renal colic

Method of administration and dosage

The drug is used in adult patients. The drug is administered intramuscularly by deep injection into the gluteal region. Single dose for adults - 75 mg (one ampoule). If necessary, re-introduction is possible, but not earlier than 12 hours later.

The duration of the drug is not more than 2 days, if it is necessary to increase the course of treatment, they switch to the oral form of the drug.

Side effects

Sometimes

Epigastric pain, nausea, vomiting, diarrhea, abdominal cramps,

dyspepsia, bloating, anorexia

Headache, dizziness

Skin rash

Increased serum aminotransferase levels

Reactions at the site of intramuscular injection in the form of local pain and

seals

Seldom

Gastrointestinal bleeding (bloody vomiting, melena, diarrhea with

mixed with blood)

Ulcers of the stomach and intestines, with or without

bleeding or perforation

Drowsiness

Hives

Hepatitis, sometimes accompanied by jaundice

Bronchial asthma

Systemic anaphylactic / anaphylactoid reactions

Hypotension

In some cases

Aphthous stomatitis

Glossitis

Lesions of the esophagus

The appearance of diaphragm-like strictures in the intestine

Nonspecific hemorrhagic colitis, exacerbation of nonspecific

ulcerative colitis or Crohn's disease, constipation

Pancreatitis

Sensory disturbances, paresthesias, memory disorders,

disorientation, insomnia, irritability, convulsions, depression,

feelings of anxiety, nightmares, tremors, psychotic reactions

Aseptic meningitis

Visual impairment (blurred vision, diplopia)

Hearing impairment, tinnitus

Taste disorders

Blistering skin eruptions, eczema, erythema multiforme,

Stevens-Johnson, Lyell's syndrome (acute toxic epidermolysis),

erythroderma (exfoliative dermatitis), hair loss,

photosensitivity, purpura, incl. allergic

Acute renal failure, changes in urine sediment (hematuria and

proteinuria), interstitial nephritis, nephrotic syndrome

Papillary necrosis

- fulminant hepatitis

Thrombocytopenia, leukopenia, hemolytic anemia, aplastic

agranulocytosis

Vasculitis

Pneumonitis

Heart palpitations

Chest pain

Hypertension

Congestive heart failure

Local abscesses and necrosis at the site of intramuscular injection

Contraindications

Hypersensitivity to diclofenac and any other ingredients of the drug, anesthetics

Complete or incomplete combination of bronchial asthma, recurrent pollinosis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs

Peptic ulcer and / or intestinal ulcer, peptic ulcers or bleeding (at least two episodes), including a history

Gastrointestinal bleeding or perforation due to the use of nonsteroidal anti-inflammatory drugs

Violation of hematopoiesis of unknown etiology

Cerebrovascular or other active bleeding

Severe heart failure, severe cardiac conduction disturbances, bradycardia, cardiogenic or hypovolemic shock

Severe liver and kidney dysfunction

Pregnancy and lactation

Children and adolescents up to 18 years old

Drug interactions

Diclofenac increases the plasma concentration of digoxin and lithium preparations.

It has been established that Diclofenac reduces the effect of diuretics. While taking potassium-sparing diuretics, the risk of developing hyperkalemia increases, and therefore, regular monitoring of the potassium content in the blood serum is necessary.

Against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase), the risk of bleeding increases (usually of the gastrointestinal tract).

Diclofenac reduces the effect of antihypertensive and hypnotics.

Concomitant use with other non-steroidal anti-inflammatory drugs and glucocorticosteroid drugs increases the likelihood of side effects (bleeding of the gastrointestinal tract).

Diclofenac increases the concentration of methotrexate and cyclosporine in the blood, which can lead to increased toxicity of methotrexate and increased nephrotoxicity of cyclosporin. Use Diclofenac with caution within 24 hours before and after taking methotrexate.

Acetylsalicylic acid reduces the concentration of Diclofenac in the blood.

There is evidence of an increase in the concentration of antibacterial drugs of the quinolone group in the blood when taken simultaneously with Diclofenac.

When used together with cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin, the incidence of hypoprothrombinemia increases.

Cyclosporine and gold preparations increase the effect of Diclofenac on the synthesis of prostaglandins in the kidneys, which is manifested by an increase in nephrotoxicity.

Concomitant use with paracetamol increases the risk of developing nephrotoxic effects of Diclofenac.

The simultaneous appointment with ethanol, colchicine, corticotropin and St. John's wort increases the risk of bleeding in the gastrointestinal tract.

There are reports of the development of hypoglycemic or hyperglycemic reactions when Diclofenac is used together with hypoglycemic agents.

Drugs that cause photosensitization increase the sensitizing effect of Diclofenac to ultraviolet radiation.

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

special instructions

Caution should be exercised when prescribing the drug to patients with bronchial asthma, congestive heart failure, arterial hypertension, edematous syndrome, alcoholism, diverticulitis, diabetes mellitus induced by acute hepatic porphyria, in the postoperative period, and the elderly.

During the period of drug treatment, systematic monitoring of liver function should be carried out. If clinical symptoms of liver disease appear, as well as if liver function abnormalities persist or increase, the use of Diclofenac should be discontinued.

When using the drug, gastrointestinal bleeding or ulcers of the gastrointestinal tract may develop, sometimes complicated by perforation. These complications are not necessarily preceded by precursor symptoms or a history of peptic ulcer disease. In those rare cases when these complications develop in patients taking Diclofenac, the drug should be discontinued.

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Among the many drugs that have anesthetic, antipyretic and anti-inflammatory effect on the human body, Diclofenac is especially popular with doctors and patients.

This drug, which is available in the form of tablets, rectal suppositories, oral syrup, solution for intramuscular injection, patch and topical ointment, is widely used to treat diseases of the musculoskeletal system.

Also, Diclofenac is used in the complex treatment of diseases that are accompanied by fever and discomfort in the joints and muscles.

pharmachologic effect

In the overwhelming majority of cases, pharmaceutical companies produce diclofenac sodium, although recently diclofenac potassium can also be seen on the shelves of pharmacies - the effectiveness of the drug does not depend at all on the form of which salt this drug is produced.

Diclofenac refers to anti-inflammatory drugs of a non-steroidal structure - this drug has a pronounced anti-inflammatory and analgesic and moderate antipyretic effect. Accordingly, the main indications for the use of this drug are diseases of the organs of movement, which are accompanied by pain in the joints and soft tissues surrounding the joints.

Under the action of diclofenac, pain that exists at rest and increases with movement decreases, the severity of morning stiffness inherent in inflammatory and degenerative-dystrophic diseases of the joints decreases - these measures help to restore the normal range of motion of the organs of the musculoskeletal system. The lasting effect of the therapy in this case is achieved after 8-10 days of systematic intake of this drug.

In this case, it is necessary to start treatment with the introduction of the drug in the form of intramuscular injections, and then, depending on the type of pathology and the patient's condition, other forms of this drug (tablets, ointments, rectal suppositories, plasters) may be prescribed. If necessary, the doctor can prescribe the patient to administer diclofenac in several dosage forms - in this case, it is important not to exceed the maximum daily dose of the drug.

In the case when diclofenac is prescribed as a remedy for the symptomatic treatment of fever and hyperthermia, its dose should be recommended by a doctor who will assess the patient's condition and decide whether there is a need to take an antipyretic drug. Usually they are limited to 1-2 doses of diclofenac in the form of tablets, suppositories and injections.

Indications for the use of Diclofenac

The appointment of diclofenac is justified in the following cases:

• rheumatism, including conditions that are accompanied by simultaneous damage to the organs of the musculoskeletal system;
• degenerative-dystrophic diseases of the organs of movement - arthrosis, osteoarthritis, osteochondrosis of the spine;
• ankylosing spondylitis (ankylosing spondylitis)
• musculoskeletal system injuries;
• autoimmune diseases of the connective tissue;
• inflammatory processes of joints and muscles, accompanied by pain syndrome;
• postoperative pain;
• neuralgia, which are accompanied by severe pain syndrome.

Who is contraindicated for Diclofenac - solution for injection?

The use of the drug is contraindicated:

• in early childhood - Diclofenac is not prescribed for children under 6 years of age;
• women in the last trimester of pregnancy and during breastfeeding;
• patients who suffer from gastric ulcer and duodenal ulcer, gastritis, duodenitis, esophagitis;
• patients who have had bleeding from the gastrointestinal tract during their life;
• patients suffering from "aspirin" bronchial asthma and allergic reactions to non-steroidal anti-inflammatory drugs;
• people suffering from severe chronic liver and kidney diseases with a stage of decompensation.

It is undesirable to prescribe the drug simultaneously with other nonsteroidal anti-inflammatory drugs.

Features of injections - how to give Diclofenac injections, dosage

In the case when the patient starts treatment with Diclofenac, in the first days of therapy, this drug is often prescribed intramuscularly. When performing an injection, it is important to choose the right place for injecting the drug - injections can only be made into large masses of muscle tissue.

Most often, the injection is performed in the outer upper quadrant of the buttock - a syringe with a volume of 5 ml or more with a long needle is suitable for an injection. When injecting, you need to insert the needle into the muscle and pull the syringe plunger towards you - this will help make sure that the needle has not entered the blood vessel.

The introduction of diclofenac into the blood vessels (veins), as well as subcutaneously, is strictly contraindicated - this can cause necrosis of the blood vessel or subcutaneous fatty tissue.

It is advisable to change the side of administration of the drug daily - to make an injection alternately in the right and left buttock.

In most cases, a single intramuscular injection of the drug is sufficient, but if necessary, you can combine injections of the drug and taking diclofenac tablets inside, topical application of diclofenac ointment or gel to the area of \u200b\u200bthe affected joint. In the event that it is necessary to prescribe this remedy for children, then you can use rectal suppositories, ingestion or topical application of ointment - the injections are quite painful.

For an adult, it is recommended, regardless of the method of administration of the drug, not to exceed the daily dose of Diclofenac of 150 mg. If you calculate how many maximum injections per day you can do, then you need to rely on this figure.

The dose of the drug for children depends on the age and body weight of the patient (depending on the condition of the child, the drug is prescribed in a dose of 2 mg / kg of weight), and the daily dose is divided into several equal doses.

The duration of drug treatment in each case is determined on an individual basis.

Generalized patient reviews about Diclofenac injections

Most of the patients to whom doctors prescribe diclofenac in injections, in their reviews, note a fairly rapid onset of the drug's action (a decrease in pain can be seen after 20-30 minutes), while after ingestion, the effect becomes noticeable only after 1.5-2 hours. Regardless of the method of administration, the effect of the drug lasts for 6-8 hours - that is why the drug must be taken orally again (several times a day).

When injected intramuscularly, the drug is absorbed from the muscle gradually, so it can be limited to a single injection. A detailed course of treatment will be selected by your doctor.

Patients note that the most frequent side effects of Diclofenac are dyspeptic symptoms (from the gastrointestinal tract), dizziness, drowsiness and irritability, as well as allergic reactions. With intramuscular injection, a strong burning sensation is possible at the injection site, the development of a limited abscess or diffuse necrosis of the subcutaneous tissue.

Analogs of the drug Diclofenac for intramuscular injections and injections

On the shelves of pharmacies, this drug can be found under the names Voltaren, Ortofen, Diklak, Dikloberl, Olfen, Diclofenac, Diklobene - they contain the same active ingredient.

Other non-steroidal anti-inflammatory drugs have a similar effect, which can be prescribed by a doctor for intolerance to Diclofenac, so the question of how to replace Diclofenac in the modern world is not worth it.

Diclofenac is one of the oldest drugs belonging to the group of non-steroidal anti-inflammatory drugs (NSAIDs). In addition to, in fact, anti-inflammatory, it has anesthetic, antipyretic (antipyretic), antirheumatic and antiaggregatory (anti-thrombotic) action. Its mechanism of action is based on inhibition of the activity of the enzyme cyclooxygenase, as a result of which the synthesis of inflammatory mediators of prostaglandins is suppressed. In terms of the severity of the anti-inflammatory effect among NSAIDs, diclofenac is second only to indomethacin, surpassing such well-known drugs as ibuprofen, analgin and aspirin. In terms of the severity of the analgesic effect, diclofenac is also among the leaders, occupying an honorable second place after ketorolac. As for the antipyretic effect, here diclofenac has no equal at all, leaving behind piroxicam, analgin, indomethacin, aspirin, ibuprofen and other drugs. At the same time, the high efficiency of diclofenac is harmoniously combined with its good tolerance, which makes this drug one of the most frequently prescribed drugs in the NSAID group. Diclofenac perfectly realizes its anti-inflammatory effect in diseases such as rheumatoid arthritis, osteoarthritis, myositis, ankylosing spondylitis, pericarditis, glomerulonephritis. As a pain reliever, it is ideal for postoperative pain, dysmenorrhea, hepatic and renal colic. Side effects when taking diclofenac develop in about 20% of cases (which looks quite decent compared to other NSAIDs), while only in 2% of patients the severity of adverse events forces the drug to be canceled.

Most often, the side effects of diclofenac are localized within the gastrointestinal tract (NSAID gastropathy) and the liver. Allergic reactions, dizziness and headache are not excluded.

Diclofenac is available in four dosage forms: tablets, solution for injection, gel and rectal suppositories. Tablets are taken with food or immediately after it, 50 mg 2-3 times a day or 100 mg 1 time per day (adults and adolescents over 15 years old). The maximum daily dose of diclofenac is 150 mg. As the desired therapeutic effect is achieved, the dose of the drug is gradually reduced down to 50 mg per day. Diclofenac solution is intended for short-term - no more than 2 days - use, after which they switch to tablets or suppositories. A single dose of the injected solution is 75 mg, which is equivalent to 1 ampoule. Re-introduction is allowed no earlier than 12 hours from the moment of the first injection. The gel can be used at an age younger than tablets - from 12 years. It is applied in a thin layer to the area affected by inflammation, after which it is lightly rubbed. This manipulation is performed 3-4 times a day. The amount of the drug is determined by the area of \u200b\u200bthe lesion, while a single dose should not exceed 2-4 g (you can focus on the size of a large cherry). If two weeks of using diclofenac did not bring the expected result, you should consult your doctor to continue taking it. As for suppositories, the daily dose for this dosage form is 100-150 mg 2-3 times. The maximum daily dose in this case should not exceed 200 mg.

Pharmacology

NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme of the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The 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 the synthesis of proteoglycan in cartilage.

In rheumatic diseases, it reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase the range of motion. Reduces post-traumatic and postoperative pain, as well as inflammatory edema.

Suppresses platelet aggregation. With prolonged use, it has a desensitizing effect.

When applied topically in ophthalmology, it reduces swelling and pain in inflammatory processes of non-infectious etiology.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, while the degree of absorption does not change. About 50% of the active substance is metabolized during the "first pass" through the liver. With rectal administration, absorption is slower. The time to reach C max in plasma after oral administration is 2-4 hours, depending on the dosage form used, after rectal administration - 1 hour, intramuscular administration - 20 minutes. The concentration of the active substance in plasma is linearly dependent on the size of the applied dose.

Does not cumulate. Plasma protein binding is 99.7% (mainly albumin). Penetrates into synovial fluid, C max is reached 2-4 hours later than in plasma.

It is metabolized to a large extent with the formation of several metabolites, among which two are pharmacologically active, but to a lesser extent than diclofenac.

The systemic clearance of the active substance is approximately 263 ml / min. T 1/2 from plasma is 1-2 hours, from synovial fluid - 3-6 hours. Approximately 60% of the dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted in the urine unchanged, the rest is excreted as metabolites in the bile.

Release form

10 pieces. - contour cell packaging (1) - cardboard packs.
10 pieces. - blisters (1) - cardboard packs.
10 pieces. - contour cell packages (2) - cardboard packs.
10 pieces. - blisters (2) - cardboard packs.

Dosage

For oral administration for adults, a single dose is 25-50 mg 2-3 times / day. The frequency of administration depends on the dosage form used, the severity of the disease and is 1-3 times / day, rectally - 1 time / day. For the treatment of acute conditions or relief of an exacerbation of a chronic process, an intramuscular dose of 75 mg is used.

For children over 6 years of age and adolescents, the daily dose is 2 mg / kg.

Topically applied in a dose of 2-4 g (depending on the area of \u200b\u200bthe painful area) to the affected area 3-4 times / day.

When used in ophthalmology, the frequency and duration of administration are determined individually.

The maximum daily oral dose for adults is 150 mg / day.

Interaction

With the simultaneous use of antihypertensive drugs with diclofenac, their effect may be weakened.

There are isolated reports of seizures in patients taking both NSAIDs and quinolone antibacterial drugs.

With simultaneous use with GCS, the risk of side effects from the digestive system increases.

With the simultaneous use of diuretics, it is possible to reduce the diuretic effect. With simultaneous use with potassium-sparing diuretics, an increase in the concentration of potassium in the blood is possible.

With simultaneous use with other NSAIDs, the risk of side effects may increase.

There are reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus who used diclofenac simultaneously with hypoglycemic drugs.

With simultaneous use with acetylsalicylic acid, it is possible to reduce the concentration of diclofenac in blood plasma.

Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, isolated cases of bleeding have been described with the simultaneous use of diclofenac and warfarin.

With simultaneous use, it is possible to increase the concentration of digoxin, lithium and phenytoin in the blood plasma.

The absorption of diclofenac from the gastrointestinal tract decreases with simultaneous use with colestyramine, to a lesser extent with colestipol.

With simultaneous use, it is possible to increase the concentration of methotrexate in the blood plasma and increase its toxicity.

With the simultaneous use of diclofenac may not affect the bioavailability of morphine, however, the concentration of the active metabolite of morphine may remain elevated in the presence of diclofenac, which increases the risk of side effects of the morphine metabolite, incl. respiratory depression.

With simultaneous use with pentazocine, a case of the development of a large seizure has been described; with rifampicin - a decrease in the concentration of diclofenac in the blood plasma is possible; with ceftriaxone - increased excretion of ceftriaxone with bile; with cyclosporine - an increase in the nephrotoxicity of cyclosporine is possible.

Side effects

From the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases - erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rarely - liver dysfunction. With rectal administration, in isolated cases, there was inflammation of the colon with 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 impairment (blurredness, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremors, mental disorders, depression.

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

From the urinary system: rarely - impaired renal function; edema is possible in predisposed patients.

Dermatological reactions: rarely - hair loss.

Allergic reactions: skin rash, itching; when applied in the form of eye drops - itching, redness, photosensitivity.

Local reactions: at the place of intramuscular injection, burning is possible, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue; with rectal administration, local irritation, the appearance of mucous discharge mixed with blood, painful bowel movements are possible; when applied externally in rare cases - itching, redness, rash, burning; when applied topically in ophthalmology, a transient burning sensation and / or temporary blurred vision may occur immediately after instillation.

With prolonged external use and / or application to extensive body surfaces, systemic side effects are possible due to the resorptive action of diclofenac.

Indications

Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathy), post-traumatic inflammation of the soft tissues and musculoskeletal system (sprains, bruises). Spinal pain, neuralgia, myalgia, arthralgia, pain syndrome and inflammation after operations and injuries, pain syndrome with gout, migraine, algomenorrhea, pain syndrome with adnexitis, proctitis, colic (biliary and renal), pain syndrome with infectious and inflammatory diseases of the ENT - organs.

For topical use: inhibition of miosis during cataract surgery, prevention of cystoid macular edema associated with removal and implantation of the lens, inflammatory processes of the eye of a non-infectious nature, post-traumatic inflammatory process with penetrating and non-penetrating wounds of the eyeball.

Contraindications

Erosive and ulcerative lesions of the gastrointestinal tract in the exacerbation phase, "aspirin triad", hematopoietic disorders of unknown etiology, hypersensitivity to diclofenac and the components of the dosage form used, or other NSAIDs.

Application features

Application during pregnancy and lactation

Application during pregnancy and lactation is possible in cases where the potential benefit to the mother outweighs the potential risk to the fetus or newborn.

Application for violations of liver function

Use with extreme caution in case of liver disease in history.

Application for impaired renal function

Use with extreme caution in case of a history of kidney disease.

Application in children

Not recommended for use in children under 6 years of age.

special instructions

Use with extreme caution in case of liver, kidney, gastrointestinal tract diseases in history, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after serious surgical interventions, as well as in elderly patients.

If there is a history of allergic reactions to NSAIDs and sulfites, diclofenac is used only in urgent cases. In the course of treatment, systematic monitoring of liver and kidney function, and peripheral blood patterns is necessary.

Avoid getting diclofenac in the eyes (with the exception of eye drops) or mucous membranes. Patients using contact lenses should apply eye drops no earlier than 5 minutes after removing the lenses.

During the period of treatment with dosage forms for systemic use, alcohol is not recommended.

Influence on the ability to drive vehicles and use mechanisms

During the treatment period, a decrease in the speed of psychomotor reactions is possible. If the clarity of vision deteriorates after using the eye drops, do not drive and engage in other potentially hazardous activities.

Composition and release form of the drug

Solution for i / m administration transparent, colorless or slightly yellowish, with a slight specific odor.

Excipients: - 6 mg, propylene glycol - 200 mg, benzyl alcohol - 40 mg, sodium disulfite - 0.6 mg, sodium hydroxide solution 1M - up to pH 7.8-8.8, water d / i - up to 1 ml.

3 ml - polyethylene ampoules (5) - cardboard packs.
3 ml - polyethylene ampoules (10) - cardboard packs.

pharmachologic effect

NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme of the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever. The 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).

In vitro, at concentrations equivalent to those achieved in the treatment of patients, does not inhibit the biosynthesis of proteoglycans in cartilage tissue.

In rheumatic diseases, it reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase the range of motion. Reduces post-traumatic and postoperative pain, as well as inflammatory edema.

In case of post-traumatic and postoperative inflammatory events, it quickly relieves pain (arising both at rest and during movement), reduces inflammatory edema and edema of a postoperative wound.

Suppresses platelet aggregation. With prolonged use, it has a desensitizing effect.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, while the degree of absorption does not change. About 50% of the active substance is metabolized during the "first pass" through the liver. With rectal administration, absorption is slower. The time to reach C max after oral administration is 2-4 hours, depending on the dosage form used, after rectal administration - 1 hour, intramuscular administration - 20 minutes. The concentration of the active substance in the plasma is linearly dependent on the size of the applied dose.

Does not cumulate. Plasma protein binding is 99.7% (mainly with). Penetrates into synovial fluid, C max is reached 2-4 hours later than in plasma.

It is metabolized to a large extent with the formation of several metabolites, among which two are pharmacologically active, but to a lesser extent than diclofenac.

The systemic clearance of the active substance is approximately 263 ml / min. T 1/2 from plasma is 1-2 hours, from synovial fluid - 3-6 hours. Approximately 60% of the dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted in the urine unchanged, the rest is excreted as metabolites in the bile.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system, incl. rheumatoid, juvenile, chronic arthritis; ankylosing spondylitis and other spondyloarthropathies; osteoarthritis; gouty arthritis; bursitis, tendovaginitis; spinal pain syndrome (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, sciatica); post-traumatic postoperative pain syndrome accompanied by inflammation (for example, in dentistry and orthopedics); algodismenorrhea; inflammatory processes in the small pelvis (including adnexitis); infectious and inflammatory diseases of the ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.

Isolated fever is not an indication for the drug.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Contraindications

Hypersensitivity to diclofenac and excipients of the drug used; "aspirin triad" (attacks of bronchial asthma, urticaria and acute rhinitis when taking or other NSAIDs); erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; proctitis (only for suppositories); pregnancy (for i / m administration); III trimester of pregnancy (for oral and rectal administration); children and adolescents up to 18 years old (for i / m administration and for dosage forms of prolonged action).

Carefully:suspicion of a gastrointestinal disease; a history of gastrointestinal bleeding and ulcer perforation (especially in elderly patients), Helicobacter pylori infections, ulcerative colitis, Crohn's disease, dysfunction; mild to moderate liver dysfunction, hepatic porphyria (diclofenac can provoke porphyria attacks); in patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including with polyps in the nasal cavity), COPD, chronic respiratory tract infections (especially associated with allergic rhinitis-like symptoms); cardiovascular diseases (including ischemic heart disease, cerebrovascular disease, compensated insufficiency, peripheral vascular disease); impaired renal function, including chronic renal failure (CC 30-60 ml / min); dyslipidemia / hyperlipilemia; diabetes; arterial hypertension; a significant decrease in the BCC of any etiology (for example, in the periods before and after massive surgical interventions); violation of the hemostatic system; the risk of thrombosis (including myocardial infarction and stroke); elderly patients, especially those who are weak or have low body weight (diclofenac should be used in the minimum effective dose); in patients receiving drugs that increase the risk of gastrointestinal bleeding, including systemic corticosteroids (including), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel, acetylsalicylic acid), selective reverse inhibitors seizure of serotonin (including citalopram, fluoxetine, paroxetine, sertraline); simultaneous treatment with diuretics or other drugs that can impair renal function; in the treatment of smoking patients or patients with alcohol abuse; when administered intramuscularly to patients with bronchial asthma due to the risk of exacerbation of the disease (since sodium bisulfite, which is contained in some dosage forms for injections, can cause severe hypersensitivity reactions).

Dosage

For oral and rectal administration

Adults

When taken orally in the form of tablets of the usual duration of action or rectally in the form of suppositories, the recommended initial dose is 100-150 mg / day. In relatively mild cases of the disease, as well as for long-term therapy, 75-100 mg / day is sufficient. The daily dose should be divided into several doses.

When taken in the form of prolonged-release tablets, the recommended initial dose is 100 mg 1 time / day. The same daily dose is used for moderate symptoms, as well as for long-term therapy. In cases where the symptoms of the disease are most pronounced at night or in the morning, it is advisable to take extended-release tablets at night.

For relief of night pain or morning stiffness in addition to taking the drug during the day, diclofenac is prescribed in the form of rectal suppositories before bedtime; the total daily dose should not exceed 150 mg.

When primary dysmenorrhea the daily dose is selected individually; usually it is 50-150 mg. The initial dose should be 50-100 mg; if necessary, during several menstrual cycles, it can be increased to 150 mg / day. The drug should be taken when the first symptoms appear. Depending on the dynamics of clinical symptoms, treatment can be continued for several days.

No initial dose adjustment is required.

Have debilitated patients, patients with low body weight it is recommended to adhere to the minimum dose.

Children aged 1 year and older

The drug is prescribed in a dose of 0.5-2 mg / kg of body weight / day (in 2-3 doses, depending on the severity of the disease). For treating rheumatoid arthritis the daily dose can be maximally increased to 3 mg / kg (in divided doses). The maximum daily dose is 150 mg.

The drug in the form of sustained-release tablets should not be used in children and adolescents under the age of 18.

For parenteral administration

Adults

Injected deep into the / m. Single dose - 75 mg. If necessary, re-introduction is possible, but not earlier than after 12 hours.

The duration of use is not more than 2 days, if necessary, then they switch to oral or rectal use of diclofenac.

In severe cases (for example, with colic), as an exception, 2 injections of 75 mg can be given, with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, intramuscular administration 1 time / day (75 mg) can be combined with diclofenac in other dosage forms (tablets, rectal suppositories), while the total daily dose should not exceed 150 mg.

When migraine attacks diclofenac is recommended to be administered as early as possible after the onset of an attack, intramuscularly at a dose of 75 mg, followed by the use of suppositories at a dose of up to 100 mg on the same day, if required. The total daily dose should not exceed 175 mg on the first day.

Have elderly patients (65 years and older) no initial dose adjustment is required. In debilitated patients, patients with low body weight, it is recommended to adhere to the minimum dose.

The drug should be used with extreme caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing cardiovascular diseases. If long-term therapy is necessary (more than 4 weeks) in such patients, the drug should be used in a daily dose not exceeding 100 mg.

Children and adolescents under 18

Diclofenac should not be used intramuscularly in children and adolescents under 18 years of age due to the difficulty of dosing the drug.

Side effects

Determination of the frequency of adverse reactions: very often (≥1 / 10), often (≥1 / 100,<1/10) нечасто (≥1/1000, <1/100), редко (≥1/10 000, <1/1000), очень редко (<1/10 000).

From the digestive system:often - abdominal pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, loss of appetite, anorexia, increased serum aminotransferase activity; rarely - gastritis, gastrointestinal bleeding, vomiting of blood, melena, diarrhea mixed with blood, stomach and intestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; very rarely - stomatitis, glossitis, damage to the esophagus, the occurrence of diaphragmatic strictures in the intestine, colitis (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis, liver necrosis, liver failure.

From the nervous system:often - headache, dizziness; rarely - drowsiness; very rarely - sensory disturbances, including paresthesias, memory disorders, tremors, convulsions, anxiety, acute cerebrovascular accidents, aseptic meningitis; very rarely - disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the senses:often - vertigo; very rarely - visual impairment (blurred vision), diplopia, hearing impairment, tinnitus, dysgeusia.

Dermatological reactions:often - skin rash; rarely - urticaria; very rarely - bullous rashes, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), exfoliative dermatitis, pruritus, hair loss, photosensitivity reactions; purple, Shenlein-Henoch purple.

From the genitourinary system:very rarely - acute renal failure, hematuria, proteinuria, tubulointerstitial nephritis, nephrotic syndrome, papillary necrosis.

With sides of the hematopoietic system:very rarely - thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.

Allergic reactions:rarely - hypersensitivity, anaphylactic / anaphylactoid reactions, including decreased blood pressure and shock; very rarely - angioedema (including facial edema).

On the part of the cardiovascular system:very rarely - a feeling of palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction. There is evidence of a slight increase in the risk of developing cardiovascular thrombotic complications (for example, myocardial infarction), especially with long-term use of diclofenac in high doses (daily dose more than 150 mg).

From the respiratory system:rarely asthma (including shortness of breath); very rarely - pneumonitis.

General reactions:rarely - edema.

Drug interactions

Potent inhibitors of CYP2C9 -with the joint appointment of diclofenac and powerful inhibitors of CYP2C9 (such as voriconazole), it is possible to increase the concentration of diclofenac in the blood serum and increase the systemic effect caused by inhibition of the metabolism of diclofenac.

Lithium, digoxin -possibly an increase in the concentration of lithium and digoxin in the plasma curve. Monitoring of the concentration of lithium, digoxin in the blood serum is recommended.

Diuretics and antihypertensive drugs -when used simultaneously with diuretics and antihypertensive drugs (for example, beta-blockers, ACE inhibitors), diclofenac can reduce their hypotensive effect.

Cyclosporine -the effect of diclofenac on the activity of prostate glandins in the kidneys may increase the nephrotoxicity of cyclosporine.

Drugs that can cause hyperkalemia -the combined use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim can lead to an increase in the level of potassium in the blood plasma (in the case of such a combination, this indicator should be monitored frequently).

Quinolone derivatives antibacterial agents -there are separate reports of the development of seizures in patients who received both quinolone derivatives and diclofecac.

NSAIDs and GCS - with the simultaneous systemic use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of adverse events (in particular, from the gastrointestinal tract).

Anticoagulants and antiplatelet agents - an increase in the risk of bleeding cannot be ruled out with the simultaneous use of diclofenac and with drugs of these groups.

Selective serotonin reuptake inhibitors- the risk of gastrointestinal bleeding may increase.

Hypoglycemic drugs -it is impossible to exclude cases of both hypoglycemia and hyperglycemia, which necessitated a change in the dose of hypoglycemic drugs against the background of the use of diclofenac.

Methotrexate - when using diclofenac within 24 hours before or within 24 hours after taking methotrexate, it is possible to increase the concentration of methotrexate in the blood and increase its toxic effect.

Phenytoin -it is possible to enhance the effect of phenytoin.

special instructions

Use with extreme caution in case of liver, kidney, gastrointestinal tract diseases in history, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after serious surgical interventions, as well as in elderly patients.

If there is a history of allergic reactions to NSAIDs and sulfites, diclofenac is used only in urgent cases. In the course of treatment, systematic monitoring of liver and kidney function, and peripheral blood patterns is necessary.

Avoid getting diclofenac in the eyes (with the exception of eye drops) or mucous membranes. Patients using contact lenses should apply eye drops no earlier than 5 minutes after removing the lenses.

During the period of treatment with dosage forms for systemic use, alcohol is not recommended.

Influence on the ability to drive vehicles and mechanisms

During the treatment period, a decrease in the speed of psychomotor reactions is possible. If the clarity of vision deteriorates after using the eye drops, do not drive and engage in other potentially hazardous activities.

Pregnancy and lactation

There is insufficient data on the safety of diclofenac use in pregnant women. Therefore, the appointment in the I and II trimesters of pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Diclofenac (like other inhibitors of prostaglandin synthesis) is contraindicated in the third trimester of pregnancy (suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus is possible).

Despite the fact that diclofenac is excreted in breast milk in small quantities, use during lactation (breastfeeding) is not recommended. If necessary, use during lactation, breastfeeding should be discontinued.

Since diclofenac (like other NSAIDs) can have a negative effect on fertility, it is not recommended for women planning a pregnancy.

For patients undergoing examination and treatment for infertility, the drug should be canceled.

Childhood use

With impaired renal function

Use with extreme caution in case of a history of kidney disease.

For violations of liver function

Use with extreme caution in case of liver disease in history.

Use in the elderly

Use with extreme caution in elderly patients.

Painful sensations in muscles and joint pain are unpleasant symptoms, moreover, they can lead to serious consequences. Diclofenac is one of the universal drugs for combating such painful inflammations. This remedy combines several useful properties and is used by doctors and inflammatory processes for dysfunction of the musculoskeletal system.

The substance belongs to the group of non-steroidal anti-inflammatory drugs and has an analgesic effect. Intramuscular administration of the agent is especially effective. So consider, what helps the drug Diclofenac:

• for back pain:
• relieves inflammation, swelling and improves joint mobility;
• indicated for a hernia of the spine;
• has a high analgesic activity;
• due to intramuscular injection, the effect of pain relief comes quickly enough;
• excretion and half-life are transient;
• the effectiveness of the drug is higher than the possible side effects.

Using Diclofenac injections, it is worthwhile to understand that improperly selected self-medication with medications often exposes the patient to the risk of developing serious consequences. Therefore, the dosage and course of treatment with Diclofenac injections should be prescribed only by a qualified specialist.

Each package with ampoules of Diclofenac for injection has detailed instructions for the drug. The medicine is packed in ampoules with a dosage of 3 ml of solution, it is prescribed for injection.

Indications for the use of Diclofenac injections:

• rheumatic diseases of heterogeneous etiology;
• pain spasms in the spine;
• diseases of the rheumatic nature of the periarticular tissues;
• acute attack of gout;
• the period of postoperative intervention, accompanied by tissue edema and inflammatory processes;
• severe types of migraine;
• acute renal and bilious pain.

The drug is indicated for blocking painful spasms in chronic exacerbations, as well as for suppressing acute inflammatory conditions. The indicated dosage for adults and how many days you can inject Diclofenac injections:

• 75 mg (contents of one ampoule) is injected intramuscularly 1-2 times a day, not exceeding a two-day course;
• then the injections are replaced with other forms, rectal suppositories.

It is best to inject Diclofenac solution for injection into the gluteus muscle using a syringe with a volume of up to 5 ml with a needle length. Blocking of pain syndrome occurs within 30 minutes after the injection. It is important that the injection is done by a specialist with a medical education, because if incorrectly administered, unpleasant consequences such as necrosis of the subcutaneous tissue or a limited abscess are possible.

For the treatment of a more susceptible child's body, it will organically use candles and ointment with Diclofenac components, not exceeding 2 mg of the daily intake of the drug.

You should not set the duration of treatment yourself, since the complex of therapeutic measures is selected by the doctor on an individual basis.

You can find out more detailed information about Diclofenac injections, dosage, course of treatment, and how often you can inject them in the instructions for use and from your doctor. And the doctor will tell you how to inject Diclofenac if the injections are supposed to be done at home. In the hospital, a nurse makes them.

You should know that the effectiveness of the action of the components of the drug depends on the individual characteristics of the organism and cannot be safe for all patients. The reaction can be mixed due to the presence of chronic diseases. So, we list the contraindications to the use of Diclofenac injections:

• severe types of gastritis, gastrointestinal bleeding;
• ulcerative colitis, intestinal inflammation;
• hypersensitivity to the composition and components of Diclofenac injections;
• allergic manifestations in the form of asthmatic attacks, sudden rhinitis, urticaria;
• children and adolescents up to 18 years of age;
• diclofenac injections are not prescribed during pregnancy and lactation period;
• cardiovascular disorders;
• severe forms of liver disease (cirrhosis, ascites);
• dehydration of the body;
• blood diseases, hematopoiesis disorders, postoperative bleeding;
• postoperative period of cardiac surgery.

As for side reactions to the components of the substance, in the case of Diclofenac, they are possible with a low frequency. So, the presence of side effects can be identified by the following signs:

• dysfunction of the gastrointestinal system: colic, diarrhea, vomiting, nausea, anorexia; less often - bleeding, ulcers, colitis, pancreatitis;
• endemic of the central nervous system: migraine, dizziness, insomnia, memory impairment, depression and anxiety, tremors, nightmares;
• dysfunction of the sense organs: tinnitus, visual impairment, hearing impairment, impaired taste;
• dermatological disorders: skin rashes, urticaria, eczema, erythema, dermatitis;
• kidney dysfunction: swelling; rarely - acute renal failure, interstitial nephritis, nephrotic syndrome;
• liver dysfunction: possibly jaundice; in some cases - fulminant hepatitis;
• violation of hematopoiesis: various forms of anemia, leukopenia;
• cardiovascular disorders: chest pain, increased heart rate, heart failure;
• hypersensitivity reactions: asthmatic attacks, anaphylactic reactions.

Despite such a serious list of adverse reactions, cases of the development of these symptoms are quite rare in medical practice.

Diclofenac ampoules price in a pharmacy

You can buy a drug in any specialized store, the cost of ampoules for Diclofenac injections depends on the form of release, manufacturer and pharmacy network, but should not exceed three hundred rubles.

The solution for intramuscular injection includes 5 ampoules of 25 mg / 3 ml, the price of such Diclofenac injections in a pharmacy is from 50 to 60 rubles per package. To clarify the prices for Diclofenac for injection in the necessary pharmacy networks, you can use Internet resources, for example, Apteka.ru.

In conclusion, the basic principles of using Diclofenac injections should be noted once again:

1. The course of treatment and dosage is prescribed only by a qualified specialist.
2. Before using the medication, you must read the instructions for use, since Diclofenac has a number of restrictions on the health group.
3. It is necessary to resort to the help of doctors for the correct setting of the injection, self-medication can turn the fight against the disease into the development of serious complications.

Diclofenac is a kind of drug, the reception of which provides for many nuances. Therefore, it requires special care. And when reading reviews about Diclofenac injections on the Internet, you should not self-medicate, even if many write that the drug helped them.

What other injections can be given for joint pain besides Diclofenac, information on the video: