Diclofenac injections instructions for use side effects. Diclofenac sodium, solution: instructions for use. During pregnancy and lactation

IN Diclofenac gel 5 percent active substance - diclofenac sodium (Diclofenac sodium) - included in a concentration of 50 mg/g, in 1 percent— at a concentration of 10 mg/g. Excipients: isopropyl alcohol, benzyl alcohol, carbomer 940, sodium metabisulfite, polysorbate 80, triethanolamine, purified water.

Compound Diclofenac ointment: Diclofenac sodium (10 or 20 mg/g), propylene glycol, dimethyl sulfoxide, macrogol 400 and 1500.

Compound Diclofenac injections: Diclofenac sodium (25 mg/ml), sodium metabisulfite, mannitol (E421), benzyl alcohol, sodium hydroxide, propylene glycol, water for injection.

IN rectal suppositories Diclofenac includes 50 or 100 mg Diclofenac sodium and solid fat.

Compound enteric-coated tablets: 25 or 50 mg Diclofenac sodium, disubstituted calcium phosphate, starch, magnesium stearate, polyvinylpyrrolidone K30, purified talc, cellulose acetate, indoresin, diethyl phthalate, carmoisin varnish, titanium dioxide, Ponceau 4R varnish, iron oxide red and yellow.

Compound tablets po.: 25 mg Diclofenac sodium, milk sugar, sucrose, povidone, stearic acid, potato starch. Shell: Castor oil, cellacephate, titanium dioxide, tropeo-lin O dyes and azorubin.

Compound retard tablets: 100 mg Diclofenac sodium, hypromellose, hyaetellose, Kollidon SR, sodium alginate, MCC, magnesium stearate. Shell: collicut MAE 100 R, povidone, talc, propylene glycol, titanium dioxide, iron oxide yellow and red.

Compound eye drops : Diclofenac sodium (1 mg/ml), sodium chloride and dihydrogen phosphate dihydrate, propylene glycol, sodium hydroxide, hydrogen phosphate dodecahydrate and disodium edetate, water d/i.

Release form

For external use: gel 1 and 5%; ointment 1 and 2%.

Parenteral administration: solution 25 mg/ml, rectal suppositories 50 and 100 mg, drops for eye treatment 0.1% (ATC code - S01BC03).

Tablet forms: tablets in a s/r coating 25 mg, in a p/o coating 25 and 50 mg, retard 100 mg.

pharmachologic effect

Anti-inflammatory, analgesic, antipyretic.

Pharmacodynamics and pharmacokinetics

The NSAID Diclofenac is a derivative phenyl acetic acid . Its mechanism of action is based on the ability to suppress the biosynthesis of Pg (prostaglandins) - biologically active lipids that are mediators of fever, pain and inflammation.

Like other NSAIDs, it prevents aggregation .

The drug is quickly and completely absorbed; food slows down absorption for 1-4 hours (reducing Cmax by 40%). Cmax when taken orally is observed after 2-3 hours. Changes in this indicator are dose-dependent.

The pharmacokinetic profile does not change with repeated administration. If the recommendations for use are followed, it does not accumulate in the body.

Bioavailability – 50%. More than 99% bound to plasma proteins (mainly bound to albumins ). Penetrates the synovium and breast milk.

Half dose taken metabolized during the “first passage” through the liver. The process is based on single or multiple hydroxylation and conjugation with glucuronic acid. Plasma T1/2 - 1-2 hours.

60% of the dose is excreted by the kidneys in the form of metabolic products, less than 1% - in pure form, the remaining amount of the administered drug is excreted in bile.

Indications for the use of Diclofenac in injections and suppositories. What does Diclofenac tablets help with?

Diclofenac tablets, ointment, gel, suppositories and injections are used for short-term treatment moderately intense pain, including pain that develops against the background of:

  • degenerative and inflammatory diseases musculoskeletal system (the drug is prescribed for , ,spondyloarthritis , rheumatic diseases soft tissues, etc.);
  • lesions peripheral nerves, sciatica, lumbago ;
  • seizures And ;
  • inflammatory processes in the pelvic organs, algodismenorrhea ;
  • injuries and operations.

Suppositories are also prescribed in addition to the main treatment for severe inflammatory ENT diseases (For example, otitis , or ).

When is it advisable to use Diclofenac in injections?

As a rule, indications for the use of injections are situations in which it is necessary to achieve an analgesic effect as quickly as possible. The injection solution is administered for liver or acute pain in the back or muscles if they are damaged, after surgery.

For the treatment and prevention of postoperative pain syndrome IV administration of Diclofenac is indicated.

What is Diclofenac tablets for?

Indications for the use of tablet forms of the drug are the same as for the injection solution. Sometimes Diclofenac tablets are also used to relieve toothache.

A special form of the drug is Diclofenac retard- tablets with delayed release of the active substance. If the use of injections allows you to quickly relieve pain, then the use of retard tablets allows you to maintain the effect for a longer time (and reduce the frequency of use of the drug).

Retard tablets are preferred when long-term treatment is required. They are mainly used in rheumatological practice for chronic pain syndromes .

What does Diclofenac ointment and gel form help with?

Gel and ointment with Diclofenac are easy to dose and convenient to use. After applying them to the skin, the active substance accumulates in soft tissues, practically not entering the bloodstream (no more than 6% of the substance enters the blood). Specified dosage forms used for various kinds violations locomotor system .

Application of gel with five percent content diclofenac allows you to significantly reduce the dose taken orally and sometimes completely replace tablets.

For what diseases are rectal suppositories prescribed?

The drug is prescribed when it is impossible to take the medicine by mouth: in the presence of esophageal strictures, in weakened patients, etc.

When taken orally, the medicine damages the cells of the gastric mucosa; when using suppositories, the risk of damage is significantly lower. In addition, suppositories do not cause the complications that can develop with parenteral administration: muscle necrosis , formation of infiltrates and suppurations at the injection site.

Very often candles are used in combination therapy: During the day the patient receives tablets or injections, and at night - Diclofenac in the form of suppositories. This treatment regimen allows you to achieve better results due to a more uniform and prolonged maintenance of a certain plasma concentration of the drug.

Suppositories with Diclofenac are considered one of the the best candles from . At rectal use the drug does not pass through the liver and almost completely enters the prostate .

In gynecology, suppositories with Diclofenac are used for sudden acute pain (for example, with inflammation of the ovaries or algomenorrhea ).

The choice in favor of suppositories is explained by the fact that their use allows you to achieve the desired effect as quickly as possible. short time: in the vagina, the medicine quickly dissolves under the influence of temperature and is just as quickly (and in the maximum volume) delivered to the diseased organ.

Indications for use of the drug in the form of eye drops

Eye drops, according to the annotation, are prescribed for:

  • inhibition of miosis during surgical treatment ;
  • relief of inflammation in the postoperative period, as well as inflammation after injury eyeball(both penetrating and non-penetrating);
  • prevention of non-infectious inflammation affecting the anterior parts of the eye;
  • prevention of edema before and after surgery for lens removal and implantation;
  • pain relief during vision correction surgery using an excimer laser.

Additionally

In some cases, to improve efficiency conservative therapy neuralgic syndrome it is recommended to prescribe a combination of drugs “ And Diclofenac ”.

What's happened Milgamma ? This combination drug, which is based on Vgroup B itamins . The latter potentiate the effects analgesics , allowing at the same time to reduce the dose of NSAIDs, and reliably have a pronounced anti-inflammatory And antinociceptive effects .

Contraindications for use

The description of the drug Diclofenac indicates that the drug is contraindicated in:

  • hypersensitivity to its components;
  • active ulcer, wall perforation alimentary canal, stomach and intestinal bleeding;
  • inflammatory diseases of the digestive tract;
  • aspirin asthma ”;
  • pronounced functional impairment heart, kidneys, liver.

General contraindications for Diclofenac are also recently previous surgery coronary artery bypass surgery , pregnancy (contraindication for suppositories - the last 3 months of pregnancy), lactation and age up to 6 years.

Rectal use of the drug is also contraindicated in proctitis .

Ointment and gel should not be used on areas of the body with damaged skin integrity.

In pediatric practice, 50 mg suppositories and O-coated tablets are prescribed from the age of 14. Retard tablets and 100 mg suppositories are intended exclusively for the treatment of patients over 18 years of age.

An absolute contraindication to the use of eye drops is hypersensitivity to their components.

Drops should be prescribed with caution when “ aspirin asthma ”, superficial herpetic keratitis , diseases that are accompanied by disorders of plasma hemostasis; children, elderly people, pregnant and lactating women.

Side effects of Diclofenac

When taken orally, the following side effects are possible: dyspeptic symptoms, erosive and ulcerative lesions digestive canal, perforation of its walls, gastric and intestinal bleeding, increased drowsiness, dizziness, hypersensitivity reactions, irritability.

After using the drops the following are noted:

  • burning sensation;
  • corneal clouding;
  • impaired clarity of perception (immediately after instillation);
  • iritis;
  • hypersensitivity reactions.

Side effects of injections

Intramuscular injections of Diclofenac may be accompanied by a burning sensation at the injection site, abscess, and necrosis of adipose tissue.

Instructions for use of Diclofenac

Diclofenac injections: instructions for use

To relieve acute conditions or stop an aggravated chronic disease Diclofenac in ampoules is administered 1 time intramuscularly (deeply). IN further patient transferred to taking the tablet form of the drug.

The dosage of injections is 25-50 mg 2 or 3 times a day.

Diclofenac is administered intravenously by drip. The highest dose is 150 mg/day. Before administration, the contents of the ampoule should be diluted in 0.1-0.5 l NaCl solution 0.9% or dextrose solution 5%. Sodium bicarbonate solution is first added to the infusion solutions (0.5 ml if the solution concentration is 8.4%, and 1 ml if the concentration is 4.2%).

The duration of the infusion, depending on the intensity of the pain, is from half an hour to an hour and a half.

To prevent postoperative pain, the infusion is recommended to be carried out with a “shock” dose - 25-50 mg of Diclofenac over 15-60 minutes. Subsequently, the drug is administered at a rate of 5 mg/hour (until the highest daily dose is reached - 150 mg).

How many days can you inject Diclofenac?

IM injections of Diclofenac are allowed for no more than 2 days in a row. IN in some cases The course of treatment with injections can last up to 5 days.

How often can you inject the drug?

NSAIDs cause quite serious side effects, so it is optimal to use Diclofenac no more than once every three months, 3-5 injections per course.

Diclofenac gel: instructions for use

A single dose of the gel depends on the size of the painful area. As a rule, from 2 to 4 grams of the product are used. The cream should be applied to the skin at the site of pain projection and rubbed gently. During the day, the procedure is repeated 3-4 times.

To enhance the effect, the gel can be used with tablets, suppositories or injections of medication.

Diclofenac ointment: instructions for use

The ointment is taken in the same quantity as the gel and rubbed into the skin over the inflammation in the same way. Maximum dose- 8 g/day. Frequency of use: 2-3 times/day.

Diclofenac tablets: instructions for use

Diclofenac tablets (Acri, UBF, Stada, Sandoz, etc.) are taken orally with food or after meals (without chewing or crushing). Adults should take 50 to 150 mg/day. in 2-3 doses.

Diclofenac: how to take retard tablets?

Diclofenac retard is taken 100 mg once a day.

If after taking 100 mg of Diclofenac the desired effect is not achieved, you can additionally take 1 tablet of 50 mg (usual duration of action).

Diclofenac suppositories: instructions for use

The starting dose for an adult is 50-150 mg/day, depending on the indications. In this case, the patient should receive no more than 150 mg of diclofenac sodium in total during the day. The daily dose should be divided into 2-3 doses.

For children 6-15 years old, the dose is selected at the rate of 0.5-2 mg/kg/day. At rheumatoid arthritis the highest daily dose may be 3 mg/kg.

Instructions for eye drops

Before surgery, the patient is administered 1 drop of solution 5 times every 30-35 minutes. After surgery - 3 times, 1 drop. IN further treatment continue, instilling 3-5 rubles/day. 1 drop each. The duration of treatment depends on the characteristics of the clinical situation.

Additionally

Scheme of drug use different manufacturers the same: that is, there is no difference in how to apply Diclofenac-Acree and, for example, Diclofenac Stada .

Overdose

An overdose can cause central nervous system disorders and digestive disorders. The first ones most often manifest themselves:

  • dizziness and headaches;
  • increased excitability;
  • clouding of consciousness;
  • phenomena of hyperventilation with increased convulsive readiness.

Disorders from the outside digestive system manifested by: nausea, abdominal pain, vomiting, gastrointestinal bleeding.

At severe poisoning possible liver damage, acute renal failure, respiratory depression, hypotension.

The drug does not have an antidote. Special measures, such as hemoperfusion , dialysis or forced diuresis , do not guarantee the removal of the drug due to its almost complete binding to plasma proteins and intensive metabolism.

Due to the low systemic absorption of the gel/ointment, overdose is considered unlikely. Accidental ingestion of the gel or ointment may cause systemic adverse reactions.

The patient is prescribed gastric lavage, induced vomiting, and given a drink. enterosorbent . Therapy is symptomatic.

Interaction

Simultaneous use with:

  • lithium preparations , or — helps to increase the plasma concentration of these drugs;
  • antihypertensive drugs and diuretics - reduces the effectiveness of these funds;
  • potassium-sparing diuretics - leads to hyperkalemia ;
  • GCS or other NSAIDs - causes adverse reactions from the gastrointestinal tract;
  • acetylsalicylic acid - helps to reduce the serum concentration of diclofenac;
  • - increases the nephrotoxic effect of the latter;
  • antidiabetic drugs - may provoke hyper- or hypoglycemia ;
  • - can lead to increased concentration and increased toxicity of the latter;
  • anticoagulants - requires regular monitoring hemocoagulation .

If indicated eye drops can be combined with others ophthalmic agents, which include corticosteroids (between instillations it is necessary to maintain at least a 5-minute break).

Terms of sale

Means for external therapy belong to the category of over-the-counter products. All other dosage forms are available by prescription.

Storage conditions

List B. Optimal temperature regime— 10-25°C.

Best before date

Diclofenac (eye drops) has the following analogues: synonyms - Voltaren Ofta , Diklo-F , Diclofenaclong , Uniclofen ; drugs similar in their mechanism of action - , Acular LS, ,Ketadrop , Broxinac .

What is better - ointment or gel? Why is the gel prescribed and what is the ointment for?

The basic basis of the ointment is fat, the gel is water, so the ointment is a more viscous substance compared to the gel. It absorbs more slowly and in some cases can cause clogged pores.

The gel quickly spreads and dries on the skin, forming a thin protective film and leaving no stains on clothes. It simultaneously supplies moisture and dries.

Due to the presence of fat in its composition, the ointment has a predominantly softening and moisturizing effect. Because of this, ointments are used mainly to treat irritated and flaky skin. The gel is more effective for the deeper layers of the skin and joints.

Voltaren or Diclofenac - which is better?

is an imported (and, accordingly, more expensive) generic version of the drug. That is, there is no significant difference in the action of these funds.

Voltaren is distinguished only by the fact that when applied externally, it is more quickly absorbed into tissues and penetrates into the site of inflammation, and when taken orally, it retains the concentration necessary to relieve pain and inflammation longer.

Which is better: Movalis or Diclofenac?

Active substance meloxicam (a derivative of ethanol acid), like diclofenac sodium, belongs to NSAID group. Diclofenac non-selectively inhibits the activity of the COX-1 and COX-2 enzymes, while meloxicam exhibits selectivity for COX-2.

Suppression of COX-2 ensures the therapeutic effectiveness of NSAIDs, suppression of COX-1 can provoke adverse reactions from the kidneys and gastrointestinal tract.

Thus, if we talk about the effectiveness of the drugs, they have proven themselves to be approximately the same. Comparing which is better - diclofenac or meloxicam , - according to the frequency of development side effects, we can conclude that Movalis (meloxicam ) is better tolerated by patients.

In addition, unlike the analogue, meloxicam has a stimulating effect on the metabolism of cartilage tissue.

Which is better: Diclofenac or Ibuprofen?

Preparations based on ibuprofen indiscriminately inhibit COX. That is, having the same indications for use and contraindications, they also provoke the same side effects.

However, unlike its counterpart, It is somewhat better tolerated by children and pregnant women, which makes it possible to use it (albeit with caution) in pediatrics and obstetrics and gynecology practice.

Ketonal or Diclofenac - which is better?

Ketonal belongs to the group of drugs ketoprofen - a substance with a strong analgesic and anti-inflammatory effect. Ketonal tens of times more effective than drugs ibuprofen , which makes it advisable to use it for the treatment of spinal injuries and osteochondrosis .

Non-selectively suppressing COX, it quickly causes adverse reactions from the gastrointestinal tract, even when used externally.

What is better - Diclofenac or Ketorol?

is a non-selective COX inhibitor. According to doctors, the effectiveness of the tablets Ketorola higher than the effectiveness of Diclofenac tablets, and the effectiveness of the injection solution is comparable. Moreover, with comparable analgesic efficacy, the duration of action Ketorola twice that of its counterpart.

Diclofenac (more often in injections than tablets) more often than Ketorol , caused adverse reactions - mainly from the gastrointestinal tract. They were regarded by the physician as minor and doubtfully related to therapy, and did not require discontinuation of treatment.

Which is better: Diclofenac or Ortofen?

Drugs Diclofenac and have no fundamental differences, since they are based on the same active substance.

Which is better: Diclofenac or Diclofenac Retard?

Pills Retard used for treatment chronic rheumatic pain . Regular tablets are used to relieve acute pain. Thus, the choice of dosage form is completely determined by the indications for use.

Aceclofenac and Diclofenac - the difference

Aceclofenac is a derivative of phenylacetylic acid.

It is distinguished by its high bioavailability and high speed achieving peak concentration in the blood (1-3 hours), the ability to be completely metabolized into pharmacologically active products (one of which, by the way, is diclofenac).

In addition to the main action, Aceclofenac suppresses the synthesis of interleukin-1 and tumor necrosis factor, which are the most important pro-inflammatory cytokines.

Today this drug is considered one of the best. Its advantages:

  • availability;
  • high quality;
  • a balanced combination of anti-inflammatory and analgesic effectiveness with
  • well tolerated.

Diclofenac with alcohol - compatible or not?

Diclofenac and alcohol are incompatible.

Consequences of alcohol with NSAIDs

Drinking alcohol during NSAID treatment may cause:

  • deterioration of liver function;
  • reducing the effectiveness of the drug;
  • development of unpredictable complications and adverse reactions;
  • and, as a consequence, strengthening stagnation V circulatory system and intoxication of the body.

Injections and alcohol are not compatible, because injection form The drug stimulates the activity of the central nervous system, while alcohol, on the contrary, inhibits it. As a result, quite serious violations neurological nature.

Diclofenac during pregnancy and breastfeeding

All dosage forms during pregnancy are used in exceptional cases taking into account the benefit/risk ratio.

Like other NSAIDs, in the 3rd trimester the drug can cause a lack of uterine contraction in a woman in labor and/or premature closure of the ductus arteriosus in a newborn.

The medicine can penetrate not only into milk, but also through the placental barrier, even when using dosage forms for external therapy. Thus, even the use of gel and ointment during pregnancy can disrupt the development of the fetus.

The drug affects fertility, so it is not recommended for women who are planning a pregnancy, as well as for women who have problems with fertilization.

This product is intended to eliminate swelling, get rid of inflammation and relieve painful sensations resulting from injuries and damage to tissues and muscles. Diclofenac also found indications for use in angina to reduce body temperature. The drug is most actively used for the treatment of arthrosis and arthritis in order to prevent joint destruction and improve their mobility.

Diclofenac - methods of use

The tool can be used in the following ways:

  1. Ointments and gels are the only form of diclofenac that can be used without medical instructions.
  2. Diclofenac suppositories help cope with stomach ulcers and are effective in reducing fever.
  3. Diclofenac has found use for pain in the spine, neuralgia, and tissue inflammation; tablets are prescribed.
  4. The advantage of diclofenac in ampoules is its immediate effect.

Diclofenac tablets - indications for use

This dosage form of Diclofenac is prescribed to eliminate symptoms and reduce pain, but it is not able to overcome the disease. Tablets help cope with pain caused by:

  • neuralgia;
  • migraine;
  • operation
  • sciatica;
  • radiculitis;
  • adnexitis.

Diclofenac is used for pain during infectious diseases such as otitis media, pharyngitis and tonsillitis.

Diclofenac sodium, according to the instructions for use, is drunk before meals (half an hour before). An adult (from 15 years of age) should take 25-50 mg of medication three times a day. If improvement is detected, the dose is reduced to fifty mg per day. Maximum permissible norm is 15 mg per day.

Diclofenac solution - instructions for use

The solution is intended for intramuscular administration. Before giving the injection, it is advisable to warm the ampoule with the drug in your hands. This activates the activity of the components and relieves pain. The injection is given only deep into the gluteal muscle. Avoid intravenous or subcutaneous administration.

The maximum daily dose is 150 mg. Patients are prescribed one ampoule (75 mg). IN serious cases may increase the daily dose to two ampoules. Typically, when treating with diclofenac, the duration of use does not exceed five days. To improve the results, the patient can be transferred to other forms of this drug (tablets, suppositories). The tablets are taken whole before meals and washed down a small amount water.

Diclofenac - contraindications for use

The drug may be contraindicated in the following cases:

  • if you are sensitive to the components of the product;
  • persons under the age of 18;
  • in case of hematopoietic function disorders;
  • stomach diseases and intestinal system ulcerative form.

It is necessary to take the medicine under the supervision of a doctor if:

  • kidney problems;
  • liver dysfunction;
  • if you suspect a stomach ulcer;
  • persons with autoimmune diseases;
  • immediately after the operation.

Among the side effects caused by the use of the drug Diclofenac are:

It is a non-steroidal anti-inflammatory drug made from phenylacetic acid. Creates a pronounced anti-inflammatory, analgesic and moderate antipyretic effect.

Instructions for use:

The drug is effective due to blocking the action of the enzyme cyclooxygenase (the main enzyme in the metabolism of arachidonic acid), which is a precursor of prostaglandins, which play a major role in the formation of the inflammatory process, pain and feverish syndrome.

Important: The description of the drug Diclofenac is not intended for prescribing treatment without the participation of a doctor.

Release form and composition

Diclofenac is available in the following dosage forms:

injection solution: transparent, from slightly yellow to colorless, with a characteristic faint odor of benzyl alcohol (in ampoules of 3 ml, 5 ampoules in strip packs, 2 packs in a cardboard box);
ointment for external use: almost white or white, with a weak specific odor (in aluminum tubes of 30 g, 1 tube in a cardboard box);
candles rectal: torpedo-shaped, white with a creamy tint or white (in blister packs of 5 suppositories, 2 packs in a cardboard box);
gel for external use 1% or 5%: homogeneous, white with cream or yellowish tint or white, with a specific odor (in aluminum tubes of 30 or 50 g, 1 tube in a cardboard box);
pills, covered with an enteric coating: orange or orange-yellow, round, biconvex (in blister packs of 10 pcs., 1, 2, 3, 5, 10 packs in a cardboard box; in blister packs of 20 pcs., each 1-3 packages in a cardboard box; in dark glass jars of 30 pcs., 1 jar in a cardboard box);
eye drops 0.1%: transparent or almost transparent solution from light yellow to colorless (in polymer dropper bottles of 5 ml, 1 bottle in a cardboard box).

Pharmacological properties

Pharmacodynamics

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 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 proteoglycan synthesis in cartilage.

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 edema. Suppresses platelet aggregation.

At long-term use has a desensitizing effect. At local application in ophthalmology it reduces swelling and pain during inflammatory processes of non-infectious etiology.

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% active substance metabolized during the “first pass” through the liver. At rectal administration absorption occurs more slowly.

The time to reach Cmax 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 dose applied.

Does not accumulate. Plasma protein binding is 99.7% (mainly albumin). 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 for use of Diclofenac

  • pain in the spine;
  • neuralgia;
  • myalgia;
  • arthralgia;
  • pain and inflammation after operations and injuries;
  • pain syndrome due to gout;
  • migraine;
  • algodismenorrhea;
  • pain syndrome with adnexitis, proctitis;
  • colic (bilious and renal);
  • pain syndrome in infectious and inflammatory diseases of the ENT organs.

For topical use:

Directions for use and doses

For oral administration for adults, a single dose is 25-50 mg 2-3 times a 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 exacerbations chronic process used intramuscularly at a dose of 75 mg.
For children over 6 years of age and adolescents, the daily dose is 2 mg/kg.
Apply externally in a dose of 2-4 g (depending on the area of ​​the painful area) to the affected area 3-4 times a day.
When used in ophthalmology, the frequency and duration of administration are determined individually.
The maximum daily dose for adults when taken orally is 150 mg/day.

Solution for injections

Intramuscular deep injection. A single dose for patients is 75 mg, which corresponds to 1 ampoule of solution. Repeated administration is permissible no earlier than after 12 hours. Duration of use - 2 days. Then, if it is necessary to continue treatment, they switch to rectal or oral administration drug.

Eye drops

Before surgery, instill into the conjunctival sac, 1 drop five times over 3 hours. After surgery in early period– 1 drop three times, then – 1 drop three to five times a day. For other diseases: 1 drop 4-5 times a day. Treatment course, no more than 28 days.

Ointment for external use

Apply externally, 2-4 grams, in a thin layer. Frequency: three to four times a day.

Candles

Intended for rectal administration, as deeply as possible, after defecation: 50 mg twice a day or 100 mg once a day. Maximum dose for daily use– 150 mg. The duration of treatment is determined individually. The suppositories are administered whole, without cutting into parts, because this can lead to impaired absorption.

Gel

The gel is applied externally, with clean hands, carefully spreading over the painful area. Gel 1% - 2-4 g per single use, gel 5% - up to 2 g. Adults and children over 12 years of age apply the drug three to four times a day. For children 6-12 years old, 1% gel is applied to the skin in a dose of up to 2 g no more than 2 times a day, 5% gel - up to 1 g for a single application maximum 2 times a day. The duration of treatment is determined individually.

Pills

Take half an hour before meals if a quick therapeutic effect is needed. In other cases, the tablets are taken after or during meals without chewing and with water.

Adult patients and adolescents: 25-50 mg twice or thrice daily (maximum 150 mg daily). When a therapeutic effect occurs, the dosage is reduced to 50 mg per day.

IN childhood The following doses should be adhered to:

  • 6-7 years: 25 mg 1 time per day;
  • 8-11 years: 25 mg 2-3 times a day;
  • 12-14 years: 25-50 mg 3-4 times a day.

Features of application

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

If the history indicates allergic reactions for 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 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.

Side effects

  • nausea;
  • vomit;
  • 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. When administered rectally, in isolated cases, inflammation of the colon with bleeding and exacerbation of ulcerative colitis were observed.

From the central nervous system and peripheral nervous system:

  • dizziness;
  • headache;
  • excitation;
  • insomnia;
  • irritability;
  • feeling tired.
  • paresthesia;
  • visual impairment (blurredness, diplopia);
  • noise in ears;
  • sleep disorders;
  • convulsions;
  • irritability;
  • tremor;
  • mental disorders;
  • depression.

From the hematopoietic system:

  • anemia;
  • leukopenia;
  • thrombocytopenia;
  • agranulocytosis.

From the urinary system:

  • renal dysfunction;
  • swelling may occur in predisposed patients.

Dermatological reactions:

Rarely - hair loss.

Allergic reactions:

  • skin rash;

When used in the form of eye drops:

  • redness;
  • photosensitivity.

Local reactions:

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

Interaction with other drugs

When used simultaneously:

With antibacterial drugs quinolone series there are isolated reports of seizures;
With hypoglycemic drugs laugh at reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus;
absorption of diclofenac from the gastrointestinal tract decreases with cholestyramine, to a lesser extent - with colestipol;
increased concentration methotrexate in blood plasma and increasing its toxicity;
With warfarin isolated cases of bleeding have been described;
Diclofenac may not affect bioavailability morphine, however, the concentration of the active morphine metabolite may remain elevated in the presence of diclofenac, which increases the risk of developing side effects of the morphine metabolite, incl. respiratory depression;
With antihypertensive medicines their effect may be weakened;
With GKS the risk of side effects from the digestive system increases;
With diuretics possible decrease in diuretic effect;
With potassium-sparing diuretics possible increase in potassium concentration in the blood;
With other NSAIDs there may be an increased risk of side effects;
With acetylsalicylic acid it is possible to reduce the concentration of diclofenac in the blood plasma;
With pentazocine a case of the development of a grand mal seizure is described;
With rifampicin- a decrease in the concentration of diclofenac in the blood plasma is possible;
With ceftriaxone- excretion of ceftriaxone with bile increases;
With cyclosporine- possible increase in nephrotoxicity of cyclosporine.

Contraindications

  • erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
  • "aspirin triad" - intolerance to aspirin;
  • hematopoietic disorders of unknown etiology;
  • hypersensitivity to diclofenac or other NSAIDs.

Overdose

From the digestive system:

  • nausea;
  • vomit;
  • diarrhea;
  • bleeding from the gastrointestinal tract.

From the nervous system:

  • dizziness;
  • headache;
  • increased convulsive readiness;
  • hyperventilation of the lungs.

Treatment

To treat an overdose, symptomatic therapy is carried out.

Diclofenac price

Analogues of Diclofenac

The following drugs are analogues of Diclofenac:

  • Adolor;
  • Bioran;
  • Diklo-F;
  • Diklak;
  • Dicloran;
  • Diclovit;
  • Diclogen;
  • Diclobene;
  • Dorosan;
  • Voltaren;
  • Ortofen;
  • SwissJet;
  • Naklofen SR;
  • Uniclofen.

Many people, especially older people, are well aware of Diclofenac. After all, this remedy is intended to treat inflammation and relieve pain in joints and muscles, which especially often make themselves felt in old age. Even those people who do not know what this drug is, most likely still used diclofenac, but under a different trade name.

In Russia, Diclofenac is included in the list of vital important drugs. The reason for this is the powerful anti-inflammatory effect of the drug. This factor, together with the low price of Diclofenac, has made it extremely common. The drug is available in pharmacies without a prescription.

Description and principle of operation

The drug was first introduced in 1973 by the Swiss pharmaceutical company Novartis and has since gained popularity as one of the most effective non-steroidal anti-inflammatory drugs.

In my own way chemical structure the active substance of the drug belongs to acetic acid derivatives. Its exact name is 2-(2,6-dichloraniline) phenylacetic acid. IN medicines located sodium salt This acid is diclofenac sodium.

Diclofenac has three types of action:

  • Anti-inflammatory
  • Antipyretic
  • Painkiller

The anti-inflammatory properties of Diclofenac are especially strong. Its antipyretic effect is also quite strong. Often the drug helps when other means do not work. Diclofenac can also relieve pain, although its analgesic effect is not so powerful, so the drug is more suitable for relieving mild to moderate pain.

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The mechanism of action of Diclofenac is based on the fact that it suppresses the synthesis of prostaglandins and cyclooxygenase - substances that play an important role in inflammation. As a result, such unpleasant symptoms inflammation, such as pain and swelling. The drug also has the ability to regulate immunity. With long-term use, the anti-allergenic properties of Diclofenac appear. After taking the tablets, the active substance is quickly absorbed into the blood plasma, and from there enters the synovial fluid located in the joints.

Dosage forms

The main dosage forms of diclofenac are tablets and ointment. Rectal suppositories, gel, eye drops, solutions for injections and infusions are also produced.

There are two types of tablets - regular, enteric-coated and extended-release (retard) film-coated tablets. Extended-release tablets release the active substance more slowly, thereby ensuring its necessary therapeutic concentration in the blood. The maximum concentration of the substance in the blood plasma when taking regular tablets is achieved after 2 hours, and after taking retard tablets - after 4 hours. Both types of tablets are accompanied by an annotation that contains their characteristics and instructions for use.

Enteric tablets have two dosage options for the main substance - 25 and 50 mg. Also, in addition to the active substance, the tablets contain many auxiliary substances:

  • lactose
  • sucrose
  • povidone
  • potato starch
  • stearic acid

Retard tablets have a dosage of 100 mg. Excipients included in their composition:

  • hypromellose
  • hyaetellosis
  • Kollidon SR
  • sodium alginate
  • Magnesium stearate
  • Collicut MAE 100 R
  • povidone
  • talc
  • propylene glycol
  • titanium dioxide
  • iron oxide

The ointment can have two dosage options - 10 mg and 20 mg of active substance per 1 g. Other substances included in the ointment:

  • polyethylene oxide-400
  • polyethylene oxide-1500
  • dimexide
  • 1,2-propylene glycol

The injection solution is supplied in 3 ml ampoules and contains 25 mg of active substance per 1 ml. The solution also contains water, sodium hydroxide, benzyl alcohol, propylene glycol, and mannitol.

Indications

Diclofenac tablets are intended primarily to relieve the symptoms of inflammatory processes in diseases of the musculoskeletal system. These include:

  • arthritis of various natures
  • rheumatoid soft tissue lesions
  • osteoarthritis
  • bursitis
  • herniated discs

The drug is successfully used to relieve moderate or mild pain in conditions such as:

  • neuralgia
  • myalgia
  • proctitis
  • migraine
  • headache
  • toothache
  • postoperative pain
  • injuries

The drug is also used for:

  • pelvic inflammatory processes
  • algodismenorrhea
  • complex therapy infectious diseases respiratory organs

Diclofenac injections are indicated for:

  • exacerbations of osteochondrosis
  • radiculitis
  • arthritis
  • rheumatic organ damage of cardio-vascular system and eye
  • acute otitis and sinusitis
  • postoperative and post-traumatic pain
  • conjunctivitis
  • acute form of gout

Photo: Alexander Raths/Shutterstock.com

The ointment is intended for external use and penetrates faster than other dosage forms into tissues located close to the surface of the skin. The ointment can relieve swelling of the joints, increase their mobility and relieve pain. In addition, when using the ointment, there is a risk of negative phenomena associated with drug overdose is minimized.

  • soft tissue injuries
  • muscle pain
  • Pain due to sprains, ligament injuries, dislocations, bruises
  • arthritis
  • rheumatic lesions of the skin and soft tissues

It is worth keeping in mind that the drug, like other anti-inflammatory and painkillers, does not treat the causes of diseases, but only relieves their most unpleasant symptoms. Therefore, Diclofenac is recommended to be used only as one of the drugs in complex therapy.

Contraindications

Diclofenac should not be taken while breastfeeding. The drug should not be taken on later pregnancy (in the third trimester). This prohibition also applies to external forms - ointment and gel. There are several reasons for this circumstance. Firstly, the drug weakens the contractility of the uterus, which can prolong the labor process. Secondly, it can increase bleeding during childbirth.

The ban on the use of the drug during lactation is due to its ability to pass into breast milk. The use of ointment and gel during lactation is possible, but treatment with Diclofenac in this case should be carried out under the supervision of a doctor.

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The drug negatively affects fertility, so women who are trying to get pregnant or suffering from infertility should not resort to Diclofenac.

You should also not take Diclofenac if:

  • severe pathologies of the liver and kidneys
  • stomach and intestinal ulcers
  • gastrointestinal bleeding
  • bronchial asthma
  • individual intolerance to components
  • disorders of hematopoiesis and hemostasis
  • heart failure
  • peripheral arterial diseases
  • coronary heart disease
  • under 6 years of age

The drug is taken with caution and under the supervision of a doctor when:

  • diabetes mellitus
  • over 65 years of age
  • high blood cholesterol levels
  • kidney and liver dysfunction
  • anemia
  • connective tissue pathologies
  • hypertension
  • early stages of pregnancy (1st and 2nd trimester)
  • hyperthermia in children

When treating with ointment or gel, they should not be applied to damaged skin. It is necessary to ensure that these dosage forms do not come into contact with open wounds, as well as in the eyes.

Instructions for use

For post-traumatic and postoperative edema the patient can take the drug without consulting a doctor. In other cases, taking the drug is possible only after a doctor's prescription. You should not self-medicate with Diclofenac, since it has many side effects and contraindications, which are especially pronounced during long-term therapy.

Pills

Food slows down the absorption of the drug, but does not interfere with it. Therefore, if you need the maximum fast action drug, then the tablets must be taken half an hour before meals. IN otherwise The tablets should be taken during or after meals. The tablet must be swallowed without chewing and washed down with water.

For retard tablets, the optimal daily dose is 100 mg. It is taken at a time, in the form of one tablet. The course of treatment with tablets should not exceed two weeks.

For children weighing more than 25 kg, the drug is prescribed taking into account body weight. The dosage is calculated individually, depending on the disease and age. The recommended dosage is 0.5-2 mg/kg. When treating rheumatoid arthritis, the dosage can be increased to 3 mg/kg. It is not recommended to give 50 mg tablets to children.

Ointments

It is necessary to easily rub a thin layer of ointment into the affected area 3-4 times a day. A single dose is 2-4 g, the maximum daily dose is 8 g. For children under 12 years of age, a single dose should not exceed 2 g, and the number of procedures per day should be no more than two.

Injections

No matter how effective diclofenac tablets and ointment are, often intramuscular injections are the best or even the only possibility dock acute condition patient and deliver the drug to the site of inflammation. In this case, it is necessary to undergo a course of treatment with diclofenac injections. In addition, when injected, the drug enters the bloodstream faster, which increases the speed of its action. Usually when intramuscular injection the effect begins to be felt after 20-30 minutes. In this case, the total duration of action does not decrease.

Injections are given in the buttock area. The dosage for one injection is 25-75 mg, injections should be given 2-3 times a day. The maximum daily dose should not exceed 150 mg. If other dosage forms are taken simultaneously with injections, then they must be taken into account so that the total dose does not exceed this number.

The course of injections must be carried out within 2 days. In some cases, this period can be extended to 7 days. If after this it is necessary to carry out additional treatment, then it can be continued with tablets.

Side effects

From the gastrointestinal tract, the following phenomena are possible:

  • nausea
  • dyspepsia
  • diarrhea
  • vomit
  • flatulence

Rarely, hepatitis and gastric bleeding may occur.

From the central nervous system the following may be observed:

  • headache
  • insomnia
  • drowsiness
  • dizziness
  • tremor
  • depression
  • visual impairment

Dermatological reactions are sometimes possible:

  • eczema
  • hives

Renal failure, anemia, hypotension or hypertension, disorders menstrual cycle. According to latest research, long-term treatment Diclofenac drugs increase the risk of heart attack by 40%. Therefore, long-term treatment with the drug can be carried out only if there are no alternatives.

Drug interactions

It is not recommended to use diclofenac with other non-steroidal anti-inflammatory drugs and anticoagulants, as this may increase the risk of side effects, in particular bleeding. Acetylsalicylic acid reduces the concentration of Diclofenac in the blood. Paracetamol increases the nephrotoxic effect of Diclofenac.

The drug weakens the effect of antihypertensive, hypnotic and hypoglycemic drugs. At simultaneous administration Convulsions may occur with quinolone antibiotics. When taken simultaneously with diuretics, it may weaken their effect or cause the accumulation of potassium in the blood.

Analogs

You can find many drugs on the market where active substance is Diclofenac. Among the tablets are Ortofen, Voltaren, Naklofen. Among other ointments with Diclofenac, Voltaren ointment can be noted. However, Voltaren, as a foreign-made drug, does not have the same affordable price.

Indirect analogues of Diclofenac include other non-steroidal anti-inflammatory drugs - Meloxicam, Nise, Ketonal, Naproxen, Butadione, Indomethacin. However, their action is somewhat different from the action of the drug; they also have a different list of contraindications. Therefore, they will not always be able to replace it.