Voltaren instructions for use injections. Injections using Voltaren injections

Composition and release form of the drug

Solution for intramuscular administration from colorless to light yellow.

Excipients: - 18 mg, propylene glycol - 600 mg, benzyl alcohol - 120 mg, sodium disulfite - 2 mg, sodium hydroxide - up to pH 7.8-8.0, water for injection - up to 3 ml.

3 ml - colorless glass ampoules with a break point or break ring (5) - cardboard packs with an insert with cells for ampoules.

pharmachologic effect

NSAID, phenylacetic acid derivative. 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 in 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 when treating patients, it does not inhibit the biosynthesis of cartilage tissue proteoglycans.

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

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

Suppresses platelet aggregation. With long-term use it has a desensitizing effect.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, but the degree of absorption does not change. About 50% of the active substance is metabolized during the “first pass” through the liver. When administered rectally, absorption occurs more slowly. The time to reach Cmax 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 dose applied.

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

It is extensively metabolized to form several metabolites, of which two are pharmacologically active, but to a lesser extent than diclofenac.

Systemic clearance of the active substance is approximately 263 ml/min. T1/2 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 unchanged in the urine, the rest is excreted in the form of metabolites in bile.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system, incl. rheumatoid, juvenile, chronic arthritis; ankylosing spondylitis and other spondyloarthropathy; osteoarthritis; gouty arthritis; bursitis, tendovaginitis; pain syndrome from the spine (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis); post-traumatic postoperative pain syndrome accompanied by inflammation (for example, in dentistry and orthopedics); algodismenorrhea; inflammatory processes in the 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 use of the drug.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and 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 intramuscular administration); III trimester of pregnancy (for oral and rectal administration); children and adolescents up to 18 years of age (for intramuscular administration and for long-acting dosage forms).

Carefully: suspicion of gastrointestinal disease; indications in the anamnesis of bleeding from the gastrointestinal tract and perforation of the ulcer (especially in elderly patients), Helicobacter pylori infections, ulcerative colitis, Crohn's disease, dysfunction; mild to moderate liver dysfunction, hepatic porphyria (diclofenac can provoke attacks of porphyria); in patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including polyps in the nasal cavity), COPD, chronic infectious diseases of the respiratory tract (especially those associated with allergic rhinitis-like symptoms); cardiovascular diseases (including coronary artery disease, cerebrovascular diseases, compensated insufficiency, peripheral vascular diseases); impaired renal function, including chronic renal failure (creatinine clearance 30-60 ml/min); dyslipidemia/hyperlipilemia; diabetes; arterial hypertension; a significant decrease in blood volume of any etiology (for example, in the periods before and after major surgical interventions); violation of the hemostasis system; risk of developing thrombosis (including myocardial infarction and stroke); elderly patients, especially those who are weakened 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 inhibitors of reverse serotonin uptake (including citalopram, fluoxetine, paroxetine, sertraline); simultaneous treatment with diuretics or other drugs that can impair renal function; when treating smoking patients or patients who abuse alcohol; 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 injection, can cause severe hypersensitivity reactions).

Dosage

For oral and rectal use

Adults

When taken orally in the form of tablets of regular duration 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 extended-release tablets, the recommended initial dose is 100 mg 1 time / day. The same daily dose is used for moderately severe 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.

To relieve 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; in this case, the total daily dose should not exceed 150 mg.

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

No adjustment of the initial dose is required.

U weakened 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 body weight/day (in 2-3 doses, depending on the severity of the disease). For treatment of rheumatoid arthritis the daily dose can be maximally increased to 3 mg/kg (in several doses). The maximum daily dose is 150 mg.

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

For parenteral use

Adults

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

Duration of use is no more than 2 days, if necessary, then switch to oral or rectal use of diclofenac.

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

At migraine attacks Diclofenac is recommended to be administered as early as possible after the onset of an attack, IM 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.

U elderly patients (65 years and older) no adjustment of the initial dose is required. In weakened patients and 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 hypertension) or a high risk of developing cardiovascular diseases. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg.

Children and teenagers under 18 years of age

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, decreased appetite, anorexia, increased aminotransferase activity in the blood serum; rarely - gastritis, gastrointestinal bleeding, vomiting 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 diaphragm-like 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 paresthesia, 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, itching, hair loss, photosensitivity reactions; purpura, Henoch-Schönlein purpura.

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

Co 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 swelling).

From the cardiovascular system: very rarely - 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 - swelling.

Drug interactions

Potent CYP2C9 inhibitors - When diclofenac is co-administered with strong CYP2C9 inhibitors (such as voriconazole), it is possible to increase the concentration of diclofenac in the blood serum and enhance the systemic effect caused by inhibition of the metabolism of diclofenac.

Lithium, digoxin - it is possible to increase the concentration of lithium and digoxin in plasma. It is recommended to monitor the concentration of lithium and digoxin in the blood serum.

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

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

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

Antibacterial agents quinolone derivatives - There are isolated reports of the development of seizures in patients receiving quinolone derivatives and diclofecac simultaneously.

NSAIDs and GCS - with 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 excluded when diclofenac is used simultaneously with drugs from these groups.

Selective serotonin reuptake inhibitors- there may be an increased risk of gastrointestinal bleeding.

Hypoglycemic drugs - Cases of both hypoglycemia and hyperglycemia cannot be excluded, which necessitated the need to change the dose of hypoglycemic drugs during the use of diclofenac.

Methotrexate - When using diclofenac within 24 hours before or within 24 hours after taking methotrexate, the concentration of methotrexate in the blood may increase and its toxic effect may increase.

Phenytoin - the effect of phenytoin may be enhanced.

special instructions

Use with extreme caution in patients with a history of liver, kidney, gastrointestinal diseases, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after major 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 emergency cases. During treatment, systematic monitoring of liver and kidney function and peripheral blood patterns is necessary.

Avoid contact of diclofenac with the eyes (except for eye drops) or mucous membranes. Patients using contact lenses should use eye drops no earlier than 5 minutes after removing the lenses.

During treatment with dosage forms for systemic use, alcohol consumption is not recommended.

Impact on the ability to drive vehicles and machinery

During the treatment period, the speed of psychomotor reactions may decrease. If your vision becomes blurred after using eye drops, you should not drive a car or engage in other potentially hazardous activities.

Pregnancy and lactation

There is insufficient data on the safety of diclofenac in pregnant women. Therefore, administration in the first and second 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 (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus).

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

Since diclofenac (like other NSAIDs) may have a negative effect on fertility, use in women planning pregnancy is not recommended.

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

Use in childhood

For impaired renal function

Use with extreme caution if you have a history of kidney disease.

For liver dysfunction

Use with extreme caution if you have a history of liver disease.

Use in old age

Use with extreme caution in elderly patients.

In this article you can read the instructions for use of the drug Voltaren. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Voltaren in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Voltaren in the presence of existing structural analogues. Use for the treatment of inflammatory and degenerative diseases of the musculoskeletal system in adults, children, as well as during pregnancy and lactation.

Voltaren- non-steroidal anti-inflammatory drug. Voltaren contains diclofenac sodium (the active ingredient of the drug), a non-steroidal substance that has a pronounced anti-inflammatory, analgesic and antipyretic effect.

The main mechanism of action of diclofenac, established under experimental conditions, is considered to be inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the genesis of inflammation, pain and fever.

In rheumatic diseases, the anti-inflammatory and analgesic properties of Voltaren provide a clinical effect, characterized by a significant reduction in the severity of such manifestations of diseases as pain at rest and during movement, morning stiffness and swelling of the joints, as well as an improvement in the functional state.

In case of post-traumatic and postoperative inflammatory phenomena, Voltaren quickly relieves pain (arising both at rest and during movement), reduces inflammatory swelling and swelling of the postoperative wound.

When using Voltaren in tablets and suppositories, a pronounced analgesic effect of the drug was noted for moderate and severe pain of non-rheumatic origin. When using the drug in the form of a solution for intramuscular administration, the effect of the drug occurs within 1-15 minutes. It was also found that Voltaren is able to reduce pain and reduce blood loss during primary dysmenorrhea.

In addition, Voltaren relieves migraine attacks (when used in suppositories).

Pharmacokinetics

After ingestion of enteric-coated tablets, diclofenac is completely absorbed from the intestine. Although absorption is rapid, its onset may be delayed due to the enteric coating of the tablet. The degree of absorption is directly dependent on the dose. If you take a Voltaren tablet during or after a meal, its passage through the stomach slows down (compared to taking it on an empty stomach), but the amount of diclofenac absorbed does not change. After repeated doses of the drug, the pharmacokinetics do not change. If the recommended dosage regimen is followed, no accumulation is observed.

Absorption of Voltaren from rectal suppositories begins quickly, although the rate of absorption is less compared to the same indicator when ingesting enteric-coated tablets. With repeated administration of the drug in the form of suppositories, the pharmacokinetic parameters do not change. Provided the recommended dosage regimen is followed, no accumulation is observed.

After intramuscular administration of Voltaren at a dose of 75 mg, its absorption begins immediately. The degree of absorption is directly dependent on the dose. With subsequent administrations of the drug, the pharmacokinetic parameters do not change. Provided that the recommended intervals between administrations of the drug are observed, no accumulation is observed.

About 60% of the drug dose is excreted in the urine in the form of glucuronic conjugates of the unchanged active substance, as well as in the form of metabolites, most of which are also glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The remainder of the drug dose is excreted in the form of metabolites in bile.

After taking the drug orally, there are no differences in absorption, metabolism or excretion of the drug associated with the age of patients. In children, diclofenac plasma concentrations when taking equivalent doses of the drug (mg/kg body weight) are similar to the corresponding indicators in adults.

Indications

• inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, ankylosing spondylitis, spondyloarthritis, osteoarthritis, juvenile rheumatoid arthritis (for enteric-coated tablets, 25 mg and 50 mg or rectal suppositories 25 mg);
• inflammatory and degenerative forms of rheumatic diseases: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondyloarthritis (for solution for intramuscular administration);
• diseases of the spine accompanied by pain;
• rheumatic diseases of extra-articular soft tissues;
• acute attack of gout (for enteric-coated tablets and solution for intramuscular administration);
• renal colic (for solution for intramuscular administration);
• biliary colic (for solution for intramuscular administration);
• post-traumatic and postoperative pain syndromes accompanied by inflammation and swelling;
• gynecological diseases accompanied by pain and inflammation (for example, primary algodismenorrhea, adnexitis);
• as an additional remedy for severe infectious and inflammatory diseases of the ear, nose and throat, occurring with severe pain, for example, pharyngitis, tonsillitis, otitis (with the exception of prolonged-release tablets). The main treatment of the disease is carried out in accordance with generally accepted principles, incl. with the use of etiotropic therapy. Isolated fever is not an indication for the use of the drug;
• migraine attacks (for suppositories);
• severe migraine attacks (for solution for intramuscular administration).

Intramuscular administration of the drug is especially preferable at the beginning of exacerbations of inflammatory and degenerative diseases with high inflammatory activity and in pain conditions caused by inflammation of non-rheumatic origin.

Release forms

Tablets, coated, soluble in the intestine 25 mg and 50 mg (rapid).

Film-coated tablets, prolonged action 100 mg (retard).

Suppositories for rectal use 25 mg, 50 mg and 100 mg.

Solution for intramuscular administration (injections in injection ampoules) 25 mg/ml.

Gel for external use 1% Voltaren Emulgel.

Eye drops 0.1% Voltaren Ofta.

Voltaren Akti (Diclofenac potassium tablets).

There is no release form in the form of an ointment; perhaps it is a counterfeit or another drug based on Diclofenac.

Instructions for use and dosage

Enteric-coated tablets

The tablets should be swallowed whole with liquid, preferably before meals.

For adults, the recommended starting dose is 100-150 mg per day. In relatively mild cases of the disease, as well as for long-term therapy, 75-100 mg per day is sufficient. The daily dose should be divided into several doses. If it is necessary to treat night pain or morning stiffness, in addition to taking the drug during the day, Voltaren is prescribed in the form of suppositories before bedtime; in this case, the total daily dose should not exceed 150 mg.

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

Children weighing more than 25 kg are prescribed the drug at a dose of 0.5-2 mg/kg body weight per day (in 2-3 doses, depending on the severity of the disease). For the treatment of rheumatoid arthritis, the daily dose can be increased to a maximum of 3 mg/kg (in several doses).

The use of enteric-coated tablets 50 mg in children is not recommended.

Extended-release film-coated tablets

The tablets should be swallowed whole, preferably with meals.

For adults, the recommended starting dose is 100 mg (1 extended-release tablet) per day. The same dose is used in relatively mild cases of the disease, 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.

Long-acting tablets should not be given to children.

Rectal suppositories

For adults, the recommended starting dose is 100-150 mg per day. In relatively mild cases of the disease, as well as for long-term therapy, 75-100 mg per day is sufficient. Frequency of application - 2-3 times. To relieve night pain or morning stiffness, Voltaren is prescribed in suppositories before bedtime, in addition to taking the drug in tablet form during the day; in this case, the total daily dose should not exceed 150 mg.

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

For a migraine attack, the initial dose is 100 mg. The drug is prescribed at the first symptoms of an approaching attack. If necessary, on the same day you can additionally apply Voltaren in suppositories at a dose of up to 100 mg. If it is necessary to continue treatment in subsequent days, the daily dose of the drug should not exceed 150 mg (in several administrations).

For children weighing more than 25 kg, the drug is prescribed at a dose of 0.5-2 mg/kg body weight per day (the daily dose, depending on the severity of the disease, should be divided into 2-3 single doses). For the treatment of juvenile rheumatoid arthritis, the daily dose can be increased to a maximum of 3 mg/kg (in several administrations).

The use of 50 mg and 100 mg suppositories in children is not recommended.

Solution for intramuscular administration

Voltaren is administered by deep injection into the gluteal muscle. Voltaren injections should not be used for more than 2 days in a row. If necessary, treatment can be continued with Voltaren in the form of tablets or rectal suppositories.

When performing an IM injection, in order to avoid damage to the nerve or other tissues, it is recommended to inject the drug deep IM into the upper outer quadrant of the gluteal region.

The dose is usually 75 mg (contents of 1 ampoule) once a day.

In severe cases (for example, with colic), as an exception, 2 injections of 75 mg each can be given, with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, one injection of the drug per day (75 mg) can be combined with other dosage forms of Voltaren (tablets, rectal suppositories), and the total daily dose should not exceed 150 mg.

During migraine attacks, the best result is achieved if Voltaren is administered as early as possible after the onset of the attack, IM 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.

Gel

The drug is used externally.

For adults and children over 12 years of age, the drug is applied to the skin 3-4 times a day and lightly rubbed. The required amount of the drug depends on the size of the painful area. A single dose of the drug is 2-4 g (which is comparable in volume to the size of a cherry or walnut, respectively). After applying the drug, hands must be washed.

The duration of treatment depends on the indications and effectiveness of therapy (to enhance the effect, the gel can be used together with other dosage forms of Voltaren). After 2 weeks from the start of therapy, it is recommended to evaluate the advisability of further use of the drug.

Side effect

• pain in the epigastric region;
• nausea, vomiting;
• diarrhea;
• abdominal cramps;
• dyspepsia;
• flatulence;
• anorexia;
• gastrointestinal bleeding (vomiting blood, melena, diarrhea mixed with blood);
• ulcers of the stomach and intestines, accompanied or not accompanied by bleeding or perforation;
• aphthous stomatitis;
• glossitis;
• damage to the esophagus;
• nonspecific hemorrhagic colitis;
• exacerbation of ulcerative colitis or Crohn's disease;
• constipation;
• headache;
• dizziness;
• drowsiness;
• sensory disturbances, including paresthesia;
• memory disorders;
• insomnia;
• irritability;
• convulsions;
• depression;
• feeling of anxiety;
• visual impairment (blurred vision, diplopia);
• hearing impairment;
• noise in ears;
• taste disturbances;
• chest pain;
• increased blood pressure;
• skin rash;
• hives;
• eczema;
• erythema multiforme;
• hair loss;
• swelling;
• hematuria (blood in the urine);
• thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis;
• bronchospasm;
• systemic anaphylactic/anaphylactoid reactions, including arterial hypotension;
• abscesses, necrosis (with intramuscular injection).

Contraindications

• stomach or intestinal ulcer;
• history of attacks of bronchial asthma, urticaria, acute rhinitis associated with the use of acetylsalicylic acid or other NSAIDs, as well as any drugs that suppress the production of prostaglandins;
• proctitis (only for suppositories);
• children and adolescents up to 18 years of age (for solution for intravenous administration);
• hypersensitivity to diclofenac and any other ingredients of the drug.

The solution for intramuscular administration is not prescribed during pregnancy.

Use during pregnancy and breastfeeding

The use of Voltaren during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. The drug is prescribed in the minimum effective dose. As with the use of other prostaglandin synthetase inhibitors, these recommendations are especially important in the 3rd trimester of pregnancy (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus).

The use of Voltaren in the form of a solution for intramuscular administration during pregnancy is not recommended.

When Voltaren is taken orally at a dose of 50 mg every 8 hours, diclofenac passes into breast milk, but in such small quantities that there is no reason to expect any adverse effects in a breastfed baby.

If it is necessary to prescribe Voltaren in the form of a solution for intramuscular administration during lactation, the issue of stopping breastfeeding should be decided.

special instructions

During the use of Voltaren, careful medical supervision is necessary for those patients who have complaints indicating gastrointestinal diseases; having a history of ulcerative lesions of the stomach or intestines; those suffering from ulcerative colitis or Crohn's disease, as well as those with impaired liver function.

During the use of Voltaren, as well as other NSAIDs, the level of one or more liver enzymes may increase. Therefore, during long-term therapy with Voltaren, monitoring of liver function is indicated as a precautionary measure. If abnormal liver function tests persist or worsen, or if clinical manifestations of liver disease or other symptoms (including eosinophilia, rash) occur, Voltaren should be discontinued. It should be borne in mind that hepatitis during the use of Voltaren can occur without prodromal phenomena.

Caution is necessary when prescribing Voltaren to patients with hepatic porphyria, because the drug can provoke attacks of porphyria.

Since prostaglandins play an important role in maintaining renal blood flow, special caution is required when treating patients with impaired cardiac or renal function, patients receiving diuretics, as well as patients who have a significant decrease in circulating blood plasma volume of any etiology, for example, in the period before and after major surgical interventions. In these cases, monitoring of renal function is recommended as a precautionary measure during the use of Voltaren. Discontinuation of the drug usually results in renal function returning to baseline levels.

Caution should be exercised when using Voltaren in elderly patients. This is especially true in frail or low-weight elderly people; they are recommended to prescribe the drug at the minimum effective dose.

Particular caution should be observed when administering Voltaren intramuscularly to patients with bronchial asthma, due to the risk of increasing the severity of symptoms of the disease.

During the use of Voltaren, gastrointestinal bleeding may occur (for the first time or repeatedly) or ulceration/perforation of the gastrointestinal tract may develop, accompanied or not accompanied by precursor symptoms. More serious consequences of these complications may occur in older patients. In those rare cases where these complications develop in patients receiving Voltaren, the drug should be discontinued.

When using Voltaren for the first time, as well as other NSAIDs, in rare cases allergic reactions may develop, including anaphylactic and anaphylactoid reactions.

Voltaren, due to its pharmacodynamic properties, can mask the manifestations of infectious diseases.

Voltaren, like other NSAIDs, may temporarily inhibit platelet aggregation. Therefore, in patients with hemostasis disorders, careful monitoring of relevant laboratory parameters is necessary.

With long-term use of Voltaren, like other NSAIDs, systematic monitoring of peripheral blood patterns is indicated.

Impact on the ability to drive vehicles and operate machinery

Patients who experience dizziness or other central nervous system disorders, including visual impairment, while taking Voltaren, should not drive or operate machinery while using the drug.

Drug interactions

Voltaren may increase plasma concentrations of lithium and digoxin when used concomitantly with these drugs.

Voltaren, like other NSAIDs, may reduce the effect of diuretics. The simultaneous use of Voltaren with potassium-sparing diuretics can lead to an increase in the level of potassium in the blood (in the case of such a combination of drugs, this indicator should be monitored frequently).

Concomitant use of Voltaren with other NSAIDs may increase the risk of side effects.

Although clinical studies have not established the effect of Voltaren on the action of anticoagulants, there are isolated reports of an increased risk of bleeding in cases of their combined use. Close monitoring of patients receiving these drugs concomitantly is recommended.

Voltaren can be prescribed together with oral hypoglycemic drugs and the effectiveness of the latter does not change. However, there are isolated reports of the development in such cases of both hypoglycemia and hyperglycemia, which necessitated the need to change the dose of hypoglycemic drugs during the use of Voltaren.

Caution should be exercised when using NSAIDs less than 24 hours before starting or after stopping methotrexate therapy, because its blood concentration (and therefore toxicity) may increase.

The effect of NSAIDs on the activity of prostaglandins in the kidneys may enhance the nephrotoxicity of cyclosporine.

There are isolated reports of the occurrence of seizures in patients taking NSAIDs and quinolone antibacterial drugs simultaneously.

Pharmaceutical interactions

The Voltaren solution contained in ampoules should not be mixed with solutions of other drugs for injection.

Analogues of the drug Voltaren

Structural analogues of the active substance:

• Arthrex;
• Veral;
• Voltaren Acti;
• Voltaren Ofta;
• Voltaren Rapid;
• Voltaren Emulgel;
• Diclak Lipogel;
• Diklak;
• Diclobene;
• Dicloberl;
• Diclovit;
• Diclogen;
• Diclomax;
• Diclomelan;
• Diclonac;
• Diclonate;
• Dicloran;
• Diclorium;
• Diclofen;
• Diclofenac;
• Diclofenac Bufus;
• Diclofenac potassium;
• Diclofenac sodium;
• Diclofenac retard;
• Diclofenac Sandoz;
• Diclofenac Stada;
• Diclofenac-AKOS;
• Diclofenac-Acri;
• Diclofenac-Altpharm;
• Diclofenac-ratiopharm;
• Diclofenac-UBF;
• Diclofenac-FPO;
• Diclofenac-Eskom;
• Diclofenaclong;
• Diclofenacol;
• Diphen;
• Dorosan;
• Naklof;
• Naklofen;
• Diclofenac sodium;
• Ortofen;
• Orthofer;
• Orthoflex;
• Revmavec;
• Remetan;
• Sanfinak;
• SwissJet;
• Feloran;
• Flotak.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

From time to time in the life of every person there are situations when it is impossible to do without painkillers. These can be various injuries, inflammatory lesions, neurological problems. Regardless of the reason, there is a need to relieve pain. NSAIDs cope well with this task. Voltaren injections are often used. Reviews from patients indicate the drug as a highly effective remedy.

Description of the medicine

The active ingredient of the drug "Voltaren" is a non-steroidal compound with pronounced properties:

• anti-inflammatory,
• antirheumatic,
• antipyretic,
• painkillers.

The medicine inhibits the biosynthesis of prostaglandins. Namely, they play a major role in the occurrence of pain, inflammation, and fever in humans. This property is the main mechanism of action of the drug Voltaren.

For rheumatic pathologies, the effect of the drug can reduce the symptoms of the disease. There is less swelling, less pain, and improved joint function.

The analgesic effect after administration of the drug appears, as a rule, after 15-30 minutes. The medicine can eliminate migraine attacks. In addition, Voltaren injections have been used in patients in postoperative and post-traumatic conditions. They can significantly relieve pain and reduce swelling caused by wounds and inflammation.

Application of medicine

Voltaren injections are widely used in medical practice. Indications for use of this product are as follows:

• inflammatory processes in the genitourinary system;
• rheumatism, arthritis;
• childbirth (used as an analgesic medicine);
• algodismenorrhea;
• attacks of gout;
• inflammation of the middle ear;
• hepatic and renal colic;
• neuralgia;
• radiculitis;
• migraine attacks;
• myalgia;
• (acts as an analgesic);
• oncological pathologies (is a powerful pain reliever).

The drug "Voltaren" in this dosage form is prescribed exclusively by specialists. Injections are used only during inpatient treatment. The drug has a large number of specific nuances. Therefore, this remedy is not used for self-medication.

Two types of medication administration may be prescribed:

• intramuscular;
• intravenous.

The dosage completely depends on the course of the pathology and the patient’s individual tolerance to the drug “Voltaren” (injections). The course of treatment is two days. Longer use of injections is prohibited. If necessary, further therapy is continued with suppositories or tablets.

1. After opening, the solution must be applied immediately. If the contents remain unused, then such medicine should be discarded.
2. Each ampoule is used for one-time administration.
3. The recommended dose is usually 75 mg - one ampoule per day.
4. In case of severe pathologies (for example, colic), the norm may increase. In this case, two 75 mg injections are allowed throughout the day. A time interval of several hours must be maintained between injections. It is recommended that the second injection be given in the other buttock.
5. Sometimes, to enhance the analgesic effect (for example, during severe migraine attacks), Voltaren injections are combined with suppositories or tablets. In this case, the maximum daily dose cannot be more than 175 mg.

Side effects

Despite the high effectiveness of the drug, the patient may experience unwanted reactions. This is evidenced by the instructions for the drug “Voltaren” (injections). Reviews from patients largely confirm the occurrence of side effects.

Unpleasant reactions that may occur during the use of injections are usually the following:

1. Dysfunction of the gastrointestinal tract. Patients may experience abdominal pain, vomiting, and lack of appetite. Some patients complain of changes in the shape of the stool. Sometimes ulcers appear.
2. Malfunctions of the cardiovascular system. Patients may experience increased blood pressure and chest pain. Some patients experience tachycardia.
3. Changes in the functioning of the nervous system. When treated with this drug, headache and dizziness may occur. Sometimes patients experience a loss of ability to navigate in space. Possible: Some patients experience sleep disturbances and a depressive state.
4. Disturbances in the sensory organs. Deafness may occur and taste sensations may change. Some patients report worsening vision.

The side effects described above that may accompany the use of this drug are quite serious. That is why this remedy is used exclusively as prescribed by a doctor and only in hospital settings.

Contraindications for use

There are many known conditions and pathologies for which Voltaren injections are not prescribed. Contraindications for use must be taken into account by the attending physician.

It would be nice if the patient himself knows about them. Especially if, contrary to all recommendations, he self-medicates.

So, injections of the drug "Voltaren" are contraindicated for:

1. Hypersensitivity to the components of the drug.
2. The occurrence of asthma attacks, acute rhinitis, urticaria after taking the drug "Acetylsalicylic acid". In this case, any NSAIDs are contraindicated for the patient.
3. Active bowel, bleeding or perforation.
4. Severe renal and liver failure.
5. Inflammatory bowel pathologies - nonspecific ulcerative colitis, Crohn's disease.
6. Heart failure, in severe form.
7. High risk of postoperative bleeding.
8. Pregnancy (in the third trimester).
9. Postoperative pain syndrome after

Possible overdose

It is extremely dangerous to use the medicine “Voltaren” (injections) indefinitely. There are no typical clinical signs of overdose. Sometimes the patient may experience vomiting, diarrhea, and dizziness. In some cases, gastrointestinal bleeding, convulsions, or ringing in the ears are observed.

In severe poisoning, the patient experiences liver damage and kidney failure.

Treatment in cases of overdose requires symptomatic treatment. First of all, all measures should be aimed at eliminating the following consequences:

• renal failure;
• hypotension;
• convulsions;
• respiratory depression;
• gastrointestinal disorders.

Analogues of the drug

If the need arises, the doctor will recommend certain medications that can replace Voltaren injections. It is absolutely not advisable to select analogues that have a similar effect and composition on your own. It is better to enlist the help of a doctor.

Effective analogues are:

• "Diclofenac".
• "Arthrex".
• "Diklak."
• "Diclonate."
• "Veral."
• "Ortofen".

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Voltaren injections are a drug that has anti-inflammatory, antipyretic and analgesic functions.

Severe pain, as a rule, causes exacerbation of chronic diseases and acute inflammatory reactions. Voltaren injections are included in many drugs in various forms of production. The complexity of these injections requires instructions for the safe and effective use of the drug, which is produced in Switzerland.

Compound

The composition of one ampoule of the product contains 75 mg of the main substance - diclofenac.

Diclofenac also has an auxiliary composition:

• pyrogen-free mannitol (18 mg);
• distilled propylene glycol (600 mg);
• benzyl alcohol (120 mg);
• sodium bisulfite (120 mg).

The composition of the solution is adjusted to the required acidity using sodium hydroxide. Dilute the product to a volume of 3 ml of water for injection.

Voltaren ampoules and other medications are produced by the Swiss company Novartis in the form of a solution and sold in cardboard boxes of 5 ampoules of 3 ml each.

For comparison: the composition of 1 tablet of Voltaren contains only 25 or 50 mg of diclofenac sodium.

Pharmacology

Voltaren is a non-steroidal anti-inflammatory drug. Voltaren stops the production of prostaglandins. Prostaglandins play a critical role in causing pain, inflammation and fever.

Voltaren performed flawlessly in the fight against frequent headaches. Injections of the drug can relieve spontaneous pain after operations and in cases of injury.

Voltaren has the following effects:

• reduces pain intensity;
• reduces swelling and swelling of tissues;
• increases joint mobility;
• improves the overall condition.

Voltaren is absorbed within the same seconds after the injection enters the blood. The substance concentrates in the blood after 20 minutes.

The absorption of the substance by injection is twice as high as when using tablets or rectal suppositories of the same dosage.

Diclofenac is concentrated in the blood plasma of children in the same volume as in adults, if the dose is proportional to body weight.

Metabolism and absorption do not differ between ages, however, 15 minutes of intravenous administration of the drug to an elderly patient will produce plasma concentration readings 50% higher in patients than in a younger patient. Voltaren binds to blood proteins up to 99.7%.

Diclofenac is completely concentrated in the fluid inside the joint (synovial fluid) only a few hours after the maximum level of diclofenac in the blood plasma.

Voltaren injections: benefits

In the form of a solution for injections, the drug can be administered either intramuscularly or intravenously.

The use of intravenous injections in the vast majority of situations is required for the purpose of therapy and pain prevention after surgery.

Rectal suppositories and tablets are inferior to Voltaren injections in the following parameters:

The effect of Voltaren injections is twice as strong as the same dose of the drug in tablet form. This result is achieved by the absence of an important “barrier”, at which 50% of the substance is “utilized” - the liver.

Pain relief by injection is carried out immediately (a little more than 20 minutes) in comparison with the use of Voltaren orally (several hours), because the injection allows you to quickly reach the maximum concentration of the substance in the blood plasma and joint fluid.

Indications for use

What diseases could these be?

• migraine;
• spondylosis;
• gout;
• dorsalgia;
• rheumatism, unspecified;
• ankylosing spondylitis;
• unspecified pain;
• inflammatory syndrome;
• eye diseases (surgery on the eyeball);
• unspecified renal colic;
• rheumatoid arthritis;
• osteoarthritis;
• vertebral pain;
• polymyalgia rheumatica;
• dyskinesia of the biliary tract and gallbladder;
• local damage;
• complications after operations;
• bile duct stones.

Recently, Voltaren has found its use in the treatment of vertebral hernias. For osteochondrosis, Voltaren injections are allowed only if there are indications of acute exacerbation.

It is worth noting that the same chemical composition does not make Voltaren injections as safe as those in the form of tablets and suppositories.

Application

How many days can you inject the medicine? Voltaren is not recommended for use for more than 2 days. If there is an urgent need, it is better to switch to the form of tablets or suppositories. The medication can be taken together with other drugs. However, it is prohibited to mix other solutions of medications for injections with Voltaren.

Some patients allow themselves to use the drug for 5-10 days. Moreover, this technique is approved by the doctor. In this case, side effects may be avoided, but nevertheless, in all instructions for use, the period of use is no more than 2 days, so it is better not to take risks.

One ampoule of the drug implies only one-time use. The injection can only be given once a day. The injection should be made using a deep injection method according to the instructions in the upper part of the outer quadrant of the sciatic major muscle. In difficult cases, according to the instructions, you can give the injection twice a day with the condition that there are several hours between the two procedures and the injections are made in different buttocks (that is, the injection is given first in one buttock and then in the other).

Repeated use of the drug requires compliance with the intervals specified in the instructions (2 days). In general, instructions for use are not enough. Side effects, contraindications, how to inject - all this and more should be told to you by your attending physician.

If the patient experiences gastrointestinal bleeding while taking Voltaren, then the medication should be discontinued.

Side effects

Side effects when using Voltaren in injections are usually the same as when taking it orally, but their severity can be observed in a stronger volume.

The most common negative phenomena:

• migraine, dizziness;
• vertigo;
• rash;
• pain, reaction in the localization of the injection, hardening;
• vomiting, nausea;
• elevated levels of transaminases;
• joint swelling, fluid retention;
• diarrhea, dyspepsia, abdominal pain, anorexia;
• flatulence.

Voltaren injections can be actively used for arthrosis. For arthrosis of the shoulder joint and knee joint, injections help eliminate the resulting inflammation. In addition to inflammation, Voltaren injections for arthrosis of the shoulder joint will relieve severe pain.

The drug is also indicated for arthrosis of the shoulder joint of a deforming nature. Sharp pain in the shoulder joint, knee and other localizations is best eliminated with the help of injections, since this method will bring a positive result much faster.

Injections for inflammation of the sciatic nerve

The inflammatory process of the sciatic nerve is well eliminated by Voltaren injections. Diclofenac relieves pain and helps cure inflammation of the sciatic nerve. As a rule, it is believed that injection treatment is a last resort, however, many people know that it is very effective in cases of sudden exacerbation of the disease.

Injections for inflammation of the sciatic nerve are best done as close as possible to the location of the lesion. In this case, the lumbar puncture technique is used. Lumbar puncture will locally affect the inflammation of the sciatic nerve, as a result of which the effectiveness of treatment will sharply increase.

Voltaren injections for inflammation of the sciatic nerve are prescribed by a doctor. This treatment of the sciatic nerve will reduce the side effects of medications and will be highly effective. Doses and number of injections for inflammation of the sciatic nerve are determined by the doctor after diagnostic procedures have been carried out and the symptoms of the disease have been studied.

Injections for back pain

Voltaren injections help eliminate tearing back pain. As a rule, patients complain to doctors of back pain after a cold snap. Tolerable pain can be drowned out with pills, but if the pain is very disturbing, then in this case it will not be possible to do without an injection.

Voltaren: instructions for use and reviews

Latin name: Voltaren

ATX code: М01АВ05, М02АА15

Active substance: diclofenac

Manufacturer: Novartis Pharma, Novartis Consumer Health (Switzerland), GlaxoSmithKline Healthcare (UK)

Updating the description and photo: 16.08.2019

Voltaren is a non-steroidal drug with pronounced analgesic, antipyretic and anti-inflammatory effects.

Release form and composition

Dosage forms of Voltaren:

• Tablets: round, biconvex, enteric-coated, chamfered and engraved “CG” on one side; on the other side there is an engraving “BZ” - yellow shell, “GT” - light brown (10 pieces in blisters, 2 or 3 blisters in a cardboard box);
• Extended-release tablets: round, biconvex, pink film-coated, chamfered, marked in black ink “CG” on one side, “CGC” on the other (10 pcs. in blisters, 1 or 3 blisters in a cardboard box) ;
• Solution for intramuscular (IM) administration: light yellow or colorless liquid (3 ml in glass ampoules with a break point or break ring, 5 pieces in a cardboard box);
• Rectal suppositories: torpedo-shaped, from white to white with a yellow tint, with a smooth or slightly uneven surface and a slight odor (5 pcs. in blisters, in a cardboard pack - 1 or 2 blisters);
• Spray for external use: transparent yellow liquid with the smell of mint and isopropanol (15 or 30 ml each in dark glass bottles with a dosing device, 1 bottle in a cardboard box);
• Transdermal patch: beige rectangle made of polyester, an adhesive layer of light yellow color is applied to one of the surfaces, with a slight odor, covered with a transparent film (2, 5, 7 or 10 pieces in aluminum foil bags, 1 bag in cardboard packs) .

The active component of Voltaren is diclofenac sodium, its content depending on the dosage form:

• 1 yellow tablet with “BZ” engraving – 25 mg;
• 1 light brown tablet with “GT” engraving – 50 mg;
• 1 pink extended-release tablet with “CGC” engraving – 100 mg;
• 1 suppository – 25, 50 or 100 mg;
• 1 ampoule – 75 mg;
• 1 dose of spray – 8 mg;
• Transdermal patch 7 by 10 cm – 15 mg;
• Transdermal patch 10 by 14 cm – 30 mg.

Excipients:

• Enteric-coated tablets: microcrystalline cellulose, magnesium stearate, colloidal anhydrous silicon dioxide, lactose monohydrate, sodium carboxymethyl starch, corn starch, povidone K30;
• Extended-release tablets: magnesium stearate, anhydrous colloidal silicon dioxide, sucrose, cetyl alcohol, povidone K30;
• Solution for intramuscular administration: benzyl alcohol, mannitol (pyrogen-free), sodium bisulfite, distilled propylene glycol, sodium hydroxide and water for injection;
• Suppositories: solid fat;
• Spray for external use: ethanol, propylene glycol, sodium hydrogen phosphate dodecahydrate, isopropanol, disodium edetate, soy lecithin, sodium dihydrogen phosphate dihydrate, ascorbyl palmitate, peppermint leaf oil, water;
• Transdermal patch: polyisobutylene, levomenthol, isoprenestyrene copolymer, methylpyrrolidone, mercaptobenzimidazole, propylene glycol esters of fatty acids, citric acid, butylated hydroxytoluene, esterified gum, liquid paraffin, polyester base and protective film.

Additionally, Voltaren tablets contain:

• Colored enteric coating: macrogol 8000, methacrylic acid-ethyl acrylate copolymer (1:1), silicone antifoam emulsion SE2, hypromellose, titanium dioxide, macrogol glyceryl hydroxystearate, talc, iron oxide yellow and red;
• Film shell: hypromellose, polysorbate 80, red iron oxide dye (E172), talc, titanium dioxide;
• Polishing: crystalline sucrose, macrogol 8000, black ink (shellac solution in ethanol), black iron oxide dye (E172), ammonium hydroxide 28% (E527), propylene glycol (E1520).

Pharmacological properties

Pharmacodynamics

Diclofenac sodium is a non-steroidal substance, the main mechanism of action of which is considered to be inhibition of prostaglandin biosynthesis through non-selective inhibition of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), as well as disruption of arachidonic acid metabolism.

Prostaglandins play a significant role in the pathogenesis of pain, inflammation and fever. In vitro, diclofenac sodium does not inhibit the biosynthesis of cartilage tissue proteoglycans. Since the active component of Voltaren has an anti-inflammatory and analgesic effect, in rheumatic diseases a clinical effect is provided, manifested in the form of a significant reduction in the severity of symptoms of the disease such as morning swelling and stiffness of the joints, pain both at rest and during movement. An improvement in the patient's functional state is also observed. For moderate and severe pain of non-rheumatic origin, the use of Voltaren is accompanied by a pronounced analgesic effect. The pain subsides 15–30 minutes after Voltaren enters the body.

In postoperative and post-traumatic inflammatory processes, diclofenac sodium quickly relieves pain and reduces swelling of the postoperative wound, as well as swelling of inflammatory origin. When the drug is used in combination with opioids in patients with postoperative pain, the need for opioid analgesics is reduced, which has been experimentally proven. Voltaren also alleviates migraine attacks when used in the form of rectal suppositories, and also reduces discomfort and reduces blood loss during primary dysmenorrhea.

Pharmacokinetics

After intramuscular injection of 75 mg of diclofenac sodium, it begins to be absorbed immediately. The average value of its maximum concentration in blood plasma is about 2.5 mcg/ml (8 μmol/l) and is achieved approximately 20 minutes after diclofenac sodium enters the body. There is a linear dependence of the amount of absorbed active component on the dose of Voltaren.

After oral administration of enteric-coated tablets, diclofenac is almost 100% absorbed in the intestine. The rate of absorption is quite high, but its onset may be delayed due to the presence of an enteric coating in the tablet. After a single dose of 50 mg of Voltaren in this dosage form, its maximum concentration is 1.5 μg/ml (5 μmol/l) and is achieved approximately 2 hours after administration. If the tablet is taken during or after a meal, its passage through the stomach is somewhat slower than when taken on an empty stomach, but the concentration of the absorbed active component in the blood does not decrease.

Diclofenac is rapidly absorbed from rectal suppositories, but the rate of absorption is lower compared to oral administration of enteric-coated tablets. After administration of a suppository containing 50 mg of the active substance, its maximum concentration in the blood plasma is achieved within approximately 1 hour, but the value of this parameter, calculated per unit dose taken, is about 2/3 of the maximum concentration, determined after ingestion of enteric tablets.

Based on the amount of unchanged diclofenac excreted in the urine and its hydroxylated metabolites, the extended-release tablet results in the same amount of active ingredient Voltaren being released and absorbed as with conventional enteric-coated tablets. However, in the first case, the bioavailability of diclofenac does not exceed 82% of the value of this indicator when taking enteric-coated tablets in a similar dose. This can be explained by the excellent severity of the first-pass effect through the liver for a dosage form characterized by a delayed release of the active substance. As a result, the maximum content of diclofenac in the blood plasma is less than when taking an enteric-coated tablet. After taking a prolonged-release tablet at a dose of 100 mg, the maximum concentration of the active component in the blood plasma averages 0.5 mcg/ml (1.6 μmol/l) and is achieved after approximately 4 hours. There is no clinically significant effect of food on the absorption of diclofenac extended-release tablet and its systemic bioavailability. After taking a prolonged-release tablet at a dose of 100 mg, the maximum concentration of diclofenac in the blood plasma for 1 day is approximately 13 ng/ml (40 nmol/l). The basal concentration of the active substance, which is determined in the morning before taking the next dose of Voltaren in the form of extended-release tablets, is approximately 22 ng/ml (70 nmol/l) when taken during a course of treatment at a dose of 100 mg 1 time per day.

After applying 1.5 g of Voltaren to the skin in the form of a spray for external use, rapid absorption of diclofenac is observed, with systemic absorption not exceeding 6%. In the first 30 minutes after application, the content of diclofenac in the blood plasma is approximately 0.001 μg/ml, and then over the next 24 hours the maximum concentration of this substance in plasma is reached, amounting to 0.003 μg/ml. The reported concentration of diclofenac is approximately 50 times lower than the concentration after oral administration of an equivalent dose of Voltaren in any of the oral forms.

The area under the concentration-time curve (AUC) after intramuscular injection of Voltaren is approximately 2 times greater than after oral or rectal administration. This is explained by the fact that in the latter cases, about 50% of the amount of diclofenac is metabolized during the first passage through the liver. With subsequent administrations of Voltaren, the pharmacokinetic parameters do not change. If the recommended intervals are observed between administrations of diclofenac, there is no accumulation of the substance in the body.

Diclofenac is approximately 99.7% bound to serum proteins (mainly to albumin, the degree of binding to which is 99.4%). The apparent volume of distribution is 0.12–0.17 l/kg. Diclofenac is determined in the synovial fluid, where its maximum level is recorded 2–4 hours later than in the blood plasma. The apparent half-life from synovial fluid is 3–6 hours. 2 hours after reaching the maximum concentration of the active substance in the plasma, its concentration in the synovial fluid still remains higher than in the plasma for at least 12 hours.

Diclofenac was detected in low concentrations (about 100 ng/ml) in the breast milk of one of the nursing patients participating in the experiment. The estimated amount of the drug that passes through breast milk into the child’s body was equivalent to 0.03 mg/kg/day.

Diclofenac is metabolized partly through glucuronidation of the untransformed molecule, but mainly through single and multiple hydroxylation and methoxylation, resulting in the formation of several phenolic metabolites (3′-hydroxy-4′-methoxy-, 4′,5-dihydroxy-, 5 ′-hydroxy-, 4′-hydroxy- and 3′-hydroxydiclofenac), most of which are converted into glucuronide conjugates. Two phenolic metabolites have pharmacological activity, but to a much lesser extent than diclofenac itself.

The total systemic plasma clearance of the active substance Voltaren is 263 ± 56 ml/min. The terminal half-life reaches 1–2 hours. The half-life of the four metabolites, including two biologically active ones, is also short, ranging from 1 to 3 hours. One of the metabolites, 3′-hydroxy-4′-methoxydiclofenac, has a prolonged half-life, but has no pharmacological activity.

Approximately 60% of the Voltaren dose is excreted through the kidneys in the form of glucuronic conjugates of diclofenac, as well as in the form of metabolites, most of which are also glucuronic conjugates. In unchanged form, diclofenac is excreted less than 1%. The remaining amount of the drug is excreted in the form of metabolites with bile. There is a linear dependence of the content of diclofenac in the blood plasma on the dose taken.

Absorption, metabolism and excretion of diclofenac are not determined by the age of the patient. However, in some elderly patients, intravenous infusion of the drug over 15 minutes provoked an increase in plasma concentrations of diclofenac by 50% compared with the expected value in adult patients.

In patients with renal dysfunction, there is no accumulation of unchanged diclofenac if the prescribed dosage regimen is observed. With a QC of less than 10 ml/min, the theoretical equilibrium concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers, and the excretion of metabolites occurs exclusively in bile. In patients with compensated liver cirrhosis or chronic hepatitis, the pharmacokinetic parameters of diclofenac are identical to those in patients with unimpaired liver function.

Indications for use

According to the instructions, Voltaren is indicated for the symptomatic treatment of pain and inflammatory processes:

• Joints: inflammatory diseases (chronic gouty arthritis, rheumatoid arthritis, ankylosing spondylitis, rheumatism), degenerative diseases (osteochondrosis, deforming osteoarthritis);
• Spine: lumbago, radiculitis, sciatica, myalgia, ossalgia, neuralgia, arthralgia;
• Extra-articular tissues: bursitis, tendovaginitis, rheumatic soft tissue damage;
• Acute attack of gout;
• Hepatic and renal colic;
• Postoperative and post-traumatic pain syndrome accompanied by inflammation;
• Inflammatory processes in the pelvis, adnexitis, primary disalgomenorrhea;
• Migraine attack;
• Infectious inflammation of the ENT organs with severe pain: pharyngitis, tonsillitis, otitis media;
• Residual effects of pneumonia.

The use of Voltaren does not affect the progression of the disease.

Contraindications

• Urticaria, acute rhinitis, attacks of bronchial asthma that occur while taking acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs) (history);
• III trimester of pregnancy;
• Breastfeeding period;
• Hypersensitivity to the components of Voltaren.

Contraindications to the use of Voltaren tablets, solution and suppositories:

• Peptic ulcer of the stomach and duodenum in the acute phase (internal bleeding, perforation);
• Crohn's disease, ulcerative colitis and other destructive inflammatory bowel diseases in the acute phase;
• Severe form of renal, liver, heart failure;
• Active liver disease;
• Coronary artery bypass grafting (perioperative period);
• Hyperkalemia (diagnosed);
• Conditions accompanied by a risk of bleeding.

The solution for intramuscular injection should not be prescribed during pregnancy.

The use of suppositories for proctitis is contraindicated.

Under close medical supervision, Voltaren should be used in the form of tablets, solution and suppositories in patients with bronchial asthma, cardiovascular diseases or a high risk of their development, seasonal allergic rhinitis, chronic infectious pathologies of the respiratory system, swelling of the nasal mucosa (including polyps ), diabetes mellitus, arterial hypertension, dyslipidemia or hyperlipidemia, disorders of the hemostasis system, alcohol and/or tobacco addiction.

Diclofenac is used with extreme caution when treating elderly patients.

Do not apply the spray or patch to areas with damaged skin integrity.

Use with caution:

• Spray and patch: for severe dysfunction of the liver and kidneys, erosive and ulcerative lesions of the stomach and/or intestines;
• Patch: for chronic heart failure, hepatic porphyria (in the acute stage), bronchial asthma, in old age;
• Spray: for hemorrhagic diathesis, peptic ulcers, in the first and second trimester of pregnancy.

The use of Voltaren is contraindicated in people aged:

• Up to 18 years in the form of extended-release tablets and solution;
• Up to 15 years in the form of transdermal patch and spray;
• Up to 14 years in the form of enteric-coated tablets of 50 mg;
• Up to 6 years in the form of enteric-coated tablets of 25 mg.

Instructions for use of Voltaren: method and dosage

• Enteric-coated tablets are taken orally before meals, without chewing, with water. The recommended initial dose is 50 mg 2-3 times a day; for mild disease or the need for long-term treatment, 75-100 mg per day is sufficient. Treatment of primary dysmenorrhea is recommended to begin from the moment pain appears at a daily dose of 50-100 mg. If necessary, after several menstrual cycles, the dose can be increased to 150 mg per day;
• Extended-release tablets are swallowed whole with meals. The recommended initial dose is 100 mg per day, it is followed during long-term therapy or moderately severe symptoms;
• The solution is used by deep, slow intramuscular injection for the initial relief of severe pain. The recommended dose is 75 mg once a day. In severe cases, including severe colic, you can give 2 injections of Voltaren 75 mg per day with a break of several hours;
• Suppositories are used rectally, preferably after bowel movement. Dosage for adult patients is 100-150 mg per day, with a frequency of administration of 2-3 times. With long-term use and pathologies in mild forms, 75-100 mg per day is prescribed. For the treatment of a migraine attack, the recommended initial dose is 100 mg; Voltaren should be used at the first signs of the disease. If long-term therapy (more than 4 weeks) is necessary for patients with diseases of the cardiovascular system or with a high risk of developing this pathology, the drug should be used in a daily dose of no more than 100 mg. For children under 1 year of age, the dose is determined at the rate of 0.5-2 mg per 1 kg of child weight per day, with a frequency of administration of 2-3 times. When treating juvenile rheumatoid arthritis, it is allowed to increase the dose to 3 mg per 1 kg of weight per day;
• The spray is sprayed onto the skin in the affected area, then it must be rubbed in and allowed to dry. Depending on the size of the painful area, 4-5 presses are made on the bottle dispenser. It is recommended to carry out the procedure 3 times a day with regular breaks. The maximum daily dose is 120 mg or 15 spray presses;
• The transdermal patch is used externally in the form of applications to the skin over the painful area of ​​the body. It is allowed to apply 1 application per day; the size of the patch is selected individually, depending on the size of the painful area. It is recommended to use no more than 14 days for the treatment of soft tissues and no more than 21 days for diseases of the joints and muscles. If you feel worse or if there is no therapeutic effect after 7 days of treatment, you should consult a doctor. For elderly patients, the dosage does not change.

The doctor prescribes dosage forms, dose and period of treatment individually, taking into account the patient’s condition and clinical indications.

In the case of combined use of various dosage forms of Voltaren, the maximum total dose of diclofenac should not exceed 150 mg per day.

Side effects

Voltaren in the form of tablets, solution and suppositories can cause the following side effects:

• From the gastrointestinal tract: often - loss of appetite, abdominal pain, diarrhea, nausea, vomiting, dyspepsia, flatulence. Rarely - gastritis, gastrointestinal bleeding, vomiting blood, diarrhea mixed with blood, melena, stomach and intestinal ulcers (bleeding or perforation are possible). Very rarely - pancreatitis, stomatitis, colitis (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), glossitis, damage to the esophagus, the occurrence of diaphragm-like strictures in the intestine, constipation, dysgeusia;
• From the liver and biliary tract: often - increased activity of aminotransferases in the blood plasma. Rarely - liver dysfunction, hepatitis, jaundice. Very rarely - liver failure, fulminant hepatitis, liver necrosis;
• From the nervous system: often – dizziness, headache; rarely - drowsiness. Very rarely - sensory disturbances, paresthesia, acute cerebrovascular accidents, memory disorders, tremor, anxiety, convulsions, aseptic meningitis. Sometimes mental disorders in the form of disorientation, depression, insomnia, nightmares, irritability;
• From the skin and subcutaneous tissues: often – skin rash; rarely – urticaria. Very rarely - bullous rashes, erythema multiforme exudative, eczema, Stevens-Johnson syndrome, itching, toxic epidermal necrolysis, exfoliative dermatitis, hair loss, purpura, photosensitivity reactions;
• From the senses: often – vertigo; very rarely - blurred vision, diplopia, dysgeusia, hearing impairment, tinnitus;
• From the cardiovascular system: very rarely - chest pain, palpitations, increased blood pressure (BP), vasculitis, heart failure, myocardial infarction;
• From the genitourinary system: very rarely - tubulointerstitial nephritis, acute renal failure, proteinuria, hematuria, nephrotic syndrome, papillary necrosis;
• From the respiratory system: rarely – asthma; very rarely - pneumonitis;
• Allergic reactions: rarely - hypersensitivity, anaphylactic or anaphylactoid reactions, decreased blood pressure and shock. Very rarely - angioedema (including facial swelling);
• From the hematopoietic system: very rarely - thrombocytopenia, hemolytic anemia, leukopenia, agranulocytosis, aplastic anemia;
• Local reactions: often - pain, compaction at the injection site or irritation at the site of insertion of the suppository; rarely – swelling, necrosis at the injection site (for solution).

Side effects of using Voltaren spray: skin itching and the development of systemic reactions with prolonged use and/or application to a large area of ​​skin; most often: abdominal pain, renal dysfunction, bronchial asthma, hypersensitivity reactions, digestive system disorders.

Applications of the Voltaren patch are characterized by temporary and moderately severe skin manifestations at the site of application:

• Local reactions: often - erythema, dermatitis, eczema; rarely – bullous dermatitis. Very rarely - pustular rashes;
• Systemic reactions: very rarely - generalized skin rash, allergic reactions.

If signs of side effects appear, you should immediately consult a doctor.

Overdose

You can suspect an overdose of Voltaren by the following symptoms: tinnitus, dizziness, seizures, gastrointestinal bleeding, vomiting. When used in very high doses, severe liver damage and the development of acute renal failure are possible.

If the patient is diagnosed with serious complications associated with overdose (gastrointestinal disorders, decreased blood pressure, convulsions, respiratory depression, renal failure), supportive and symptomatic therapy is recommended. Hemoperfusion, hemodialysis or forced diuresis are ineffective for removing diclofenac from the body, since this substance is largely bound to plasma proteins and is intensively involved in metabolic processes.

In case of an overdose that threatens death (most often when taking Voltaren orally in high doses), it is necessary to perform gastric lavage as quickly as possible, followed by the intake of activated charcoal in order to quickly prevent absorption of the drug.

When using the Voltaren transdermal patch externally, overdose is considered almost impossible due to the very low systemic absorption of diclofenac.

special instructions

Treatment with Voltaren must strictly comply with all doctor’s recommendations.

In the first and second trimesters of pregnancy, the drug is prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.

Severely weakened and low body weight patients are recommended to be prescribed a minimum dose of diclofenac.

Voltaren injections should be given immediately after opening the ampoule; mixing it with other drugs in the same syringe is not allowed.

It is advisable to use combination therapy: tablets are prescribed during the day, and suppositories are prescribed before bedtime.

Elderly patients do not require adjustment of the initial dose of suppositories.

1 dose of Voltaren spray corresponds to a single press on the dosing device of the bottle.

Patients who experience drowsiness, visual disturbances, dizziness, vertigo and other changes in the central nervous system during Voltaren therapy are advised to refrain from driving.

Use during pregnancy and lactation

Today, there is practically no reliable information about the safety of using Voltaren in pregnant women. Taking diclofenac in the first and second trimesters of pregnancy is justified only in cases where the potential benefits of treatment for the mother significantly outweigh the possible risks for the fetus. The drug, like other prostaglandin synthesis inhibitors, is not prescribed in the last 3 months of pregnancy due to the possible suppression of uterine contractility, potential renal dysfunction in the fetus, accompanied by subsequent oligohydramnios, and/or the risk of premature closure of the ductus arteriosus in the fetus.

Although diclofenac passes into breast milk in small quantities, the drug is not recommended for nursing women to avoid undesirable effects on the baby. If treatment with Voltaren is necessary during lactation, breastfeeding must be stopped.

Since diclofenac, like other NSAIDs, can negatively affect fertility, patients planning pregnancy should avoid taking the drug. Women who are undergoing examination and treatment for infertility should not take Voltaren.

In some cases, during lactation, the use of Voltaren spray in therapeutic doses is allowed. However, due to the lack of controlled studies in which lactating women took part, the drug in this form is used strictly as prescribed by the doctor. However, the spray should not be applied to the mammary glands of nursing patients, as well as to large surfaces of the skin or for a long period of time.

For impaired renal function

Since the role of prostaglandins in maintaining renal blood flow is high, special care must be taken when treating patients with renal dysfunction, as well as patients receiving diuretics. In these cases, it is advisable to regularly monitor renal function during the course of therapy. Discontinuation of Voltaren usually results in restoration of renal function to initial levels.

For liver dysfunction

During treatment with Voltaren, strict medical monitoring is necessary for patients diagnosed with liver dysfunction.

The use of diclofenac, like other NSAIDs, may lead to an increase in the concentration of one or more liver enzymes. Therefore, when undergoing a course of therapy with Voltaren, monitoring of liver function is recommended as a precautionary measure. If abnormalities in liver function parameters persist or worsen, or clinical manifestations of liver disease or other signs are observed (for example, rashes, eosinophilia, etc.), the drug should be discontinued. It must be taken into account that hepatitis during treatment with Voltaren can develop without prodromal phenomena.

Voltaren is prescribed with caution to patients with hepatic porphyria, since diclofenac can provoke attacks of porphyria.

Use in old age

When prescribing Voltaren to elderly patients, caution should be exercised, especially in the case of weakened or low body weight elderly people. In this case, it is recommended to use diclofenac in the minimum effective dose.

Drug interactions

Concomitant use of the drug with CYP2C9 inhibitors increases the concentration of diclofenac in the blood.

Voltaren may increase the levels of digoxin and lithium in the blood plasma.

The drug reduces the effect of antihypertensive and diuretic drugs.

The combination of diclofenac with anticoagulants, antiplatelet agents, and serotonin reuptake inhibitors increases the risk of bleeding in patients.

Concomitant use with other non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of side effects.

Concomitant use with hypoglycemic agents is allowed with regular monitoring of blood glucose concentrations.

Concomitant use with potassium-sparing diuretics may cause an increase in potassium levels in the blood.

Voltaren enhances the nephrotoxicity of cyclosporine and the systemic effect of phenytoin.

Analogues

Analogs of Voltaren are: Diclofenac, Diclofenac-Akos, Diclofenac-Eskom, Diclofenac-Altfarm, Diclofenac-Ratiopharm, Diclofenac Retard, Diclak, Diclovit, Naklofen SR, Ortofen, Swissjet.

Terms and conditions of storage

Store in a dark, dry place, out of reach of children, at a temperature:

• Tablets, solution, suppositories – no higher than 30 °C;
• Spray, patch – no higher than 25 °C.

Best before date:

• Long-acting tablets – 5 years;
• Enteric-coated tablets, suppositories, spray – 3 years;
• Solution, patch – 2 years.

After opening the bottle, the spray is usable for 6 months.

Conditions for dispensing from pharmacies

Tablets, injection solution and suppositories are available with a prescription. The spray and patch are available without a prescription.