Diclofenac in ampoules - course of treatment, instructions for use and reviews. Side effects of diclofenac. What is better - ointment or gel? Why is the gel prescribed and why is the ointment

The drug "Diclofenac" belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). Used as an anesthetic for disorders of the functioning of the joints and skeletal muscles. Produced in a variety of forms, including in the form of a composition for intramuscular injection. In addition to liquid for injection, it is made in the form of tablets, ointments, gels, suppositories. The last three forms are medicines local action, while diclofenac in injections and tablets is systemic.

Diclofenac is a substance formed from phenylacetic acid.

The injection solution is sold in 3 ml ampoules and packaged in packs of 5 pieces.

Diclofenac: instructions for use

Dosage form

Solution for injection in ampoules 3 ml.

Compound

• Diclofenac sodium - active ingredient (25 milligrams)
• Sodium hydroxide
• sodium metabisulphate
• benzyl alcohol
• Mannitol
• propylene glycol
• Water is sterile

Action

Provides anti-inflammatory, analgesic and antipyretic effect. It blocks the release of arachidonic acid from damaged areas of cells, which provokes inflammation. Thus, it prevents the onset of a chemical reaction leading to vasodilation and edema, as well as damage and destruction of cells. Inhibits the action of cyclooxygenase. Inhibits the synthesis of prostaglandins. It is an antiplatelet agent. Reduces the concentration of chemicals that initiate inflammatory reactions in the area of ​​the damaged area. The recurrence of pain is prevented. Helps to improve blood supply, decrease the inflammatory process, protects cells from damage. Restores the functionality of the joints. Reduces joint stiffness. The severity of vascular hyperemia in the area of ​​inflammation, the intensity of pain are reduced.

The inflammatory process is caused by squeezing the damaged area and exposure to chemicals in the body that serve as inflammatory mediators. The process also prevents nutrients from reaching the tissues. Often, with swelling of the affected area, adjacent joints and nerve roots are compressed, which leads to more worst consequences. Initially healthy cells are damaged and die. Diclofenac reduces the risk of such complications, neutralizes the mediators of the inflammatory reaction, blocks their release, so that the pain goes away and the likelihood of relapse decreases.

Decreased concentration of prostaglandins in digestive tract, due to which unpleasant side effects can occur in this part of the body.

Absorption begins immediately after the drug enters the muscle tissue. After twenty to thirty minutes after the injection, the concentration of the substance in the blood reaches its maximum value. Accumulation does not occur if the correct time interval between injections is observed.

Almost the entire volume active substance after administration, it binds to blood proteins, in particular, albumin. Penetrates into the joint fluid, where high values ​​persist up to 12 hours after administration. 2 hours after the establishment of the peak content in the blood, the substance in the joint fluid becomes greater than in the serum.

The half-life is 2 hours, derivatives are excreted longer. The main metabolism is carried out in the liver cells. Most of decay products are excreted in the urine, and some more - in the feces.

The initial molecules of the agent are partially glucuronized, predominantly hydroxylated and methoxylated. Metabolic intermediates are then converted into glucuronic molecules.

Indications for use

Painful conditions in which pain is caused by an inflammatory process: gout, rheumatism, rheumatoid arthritis. Degenerative-dystrophic diseases of the joints and spine: arthrosis, osteochondrosis. Bechterew's disease. Uncomfortable sensations caused by physical activity. Diseases of extra-articular areas: bursitis, tendovaginitis. Lumbago, neuralgia and muscle pain. Complications after operations, injuries.

With deforming osteoarthritis, the drug relieves pain, eliminates synovitis, and prevents the destruction of nearby cartilage and bones.

In addition to diseases of the musculoskeletal system, diclofenac injections are prescribed for pneumonia, renal and hepatic colic, migraine attacks, in gynecology - from adnexitis, salpingitis, painful menstruation, in otolaryngology - from acute inflammatory diseases respiratory tract- otitis, sinusitis, eustachitis.

Contraindications

Diclofenac injections are contraindicated in the following cases: children's age (up to 15 years), hypersensitivity to any of the components of the drug, allergic reactions to painkillers from the group of non-steroidal anti-inflammatory drugs, ulcerative lesions of the stomach or duodenum (during an exacerbation or perforation), bleeding in the digestive system, impaired blood clotting or hematopoiesis, intestinal inflammation, renal and liver failure, myocardial infarction and bypass surgery, heart failure, hemorrhagic stroke or the risk of its development, atherosclerosis, large blood loss, dehydration, pregnancy (last trimester) and lactation, infertility.

Relative contraindications: ulcerative lesion of the large intestine (Crohn's disease) in the past, impaired functioning of the liver, kidneys, systemic lupus erythematosus, porphyria, a significant increase in blood pressure, old age.

Before starting the reception, make sure that there are no contraindications.

Important! It should not be given in combination with other NSAIDs.

If there is any of the contraindications, the doctor should choose drugs that are similar in action (and not in composition).

Dosage and administration: how to inject diclofenac

In the first days of treatment with this drug, injections are used. Strictly intramuscular administration is indicated, in no case should it be administered intravenously. How to inject diclofenac: after disinfecting the surface, a 5 ml syringe (deep injection of the drug is required, for which the needle of this syringe is best suited) is injected deep into the gluteal muscle or the front surface of the thigh. The recommended dose is 1 ampoule (75 mg active substance) per day. If necessary, you can enter the drug again at least 30 minutes after the first injection. The duration of treatment is 2-3 days. Then the doctor can extend it to 5 days, if there is an indication for this. It is permissible to combine intramuscular injections with forms of the same drug intended for local action - ointments, gels.

For some time after the injection, a burning sensation may remain at the injection site.

A frequent complication is the appearance of an infiltrate at the injection site, while it is recommended to apply ice for 1-2 minutes to avoid the appearance of an abscess.

In total, the dose of diclofenac per day should not exceed 150 mg.

Attention! Do not use without doctor's prescription! There is a risk of developing NSAID-associated gastropathy, stomach ulcers, consequences from the nervous and cardiovascular systems.

Injections can only be given to large muscle masses, for example, to the outer upper quadrant of the buttocks. When selecting a syringe smaller than 5 ml, due to its short needle, there is a risk of the drug entering the subcutaneous tissue.

It is better to change the place of injection of the drug - for example, alternate injections in the left and right buttocks.

How to check that the needle has not entered a blood vessel: after insertion, pull the plunger of the syringe.

It is strictly contraindicated to administer the drug intravenously and subcutaneously in order to avoid necrosis of blood vessels and subcutaneous tissue.

Side effects

The list of side effects of diclofenac is quite wide. Most of them are associated with the inhibition of prostaglandins, which perform a number of functions in the body. important functions. If any of the following symptoms appear, you must stop taking the medicine:

Adverse events related to digestive system: lack of appetite, nausea, vomiting, diarrhea, bloating, abdominal and epigastric pain, development of erosion of the stomach, duodenum, gastrointestinal bleeding (the first sign is the appearance of blood in the stool, staining it black). Inflammation in oral cavity(stomatitis). Pancreatitis. Increased activity of transaminases, indicating damage to liver cells. Perhaps the development of a stomach ulcer. Due to the blocking of cyclooxygenase, which protects the stomach from the aggressive effects of acids, the digestive system suffers the most.

From the nervous system: dizziness, headache, irritability, irritability, sleep disturbance, accompanied by nightmares. Feelings of anxiety and fear. Hand tremor, elevation convulsive readiness striated muscles. Paresthesia (impaired skin sensitivity). Tinnitus, hearing loss, visual impairment. The central nervous system is affected mainly if the recommended dosage is exceeded.

Blood, Bone marrow: decrease in hemoglobin level, development of anemia (aplastic and hemolytic anemia), decrease in the number of platelets and leukocytes, reduced clotting blood. Depression of bone marrow function.

From the side excretory system: violation of the functionality of the kidneys, their inflammation, the appearance of erythrocytes in the urine.

Cardiovascular system: increased blood pressure, tissue edema caused by a delay in the outflow of fluid from the body due to the presence of sodium ions in the preparation.

Respiratory organs: very rarely - pneumonitis, asthmatic phenomena.

Skin and hairline: redness of the skin, increased photosensitivity (up to daylight intolerance), hair loss (alopecia), itching, rash, Lyell's syndrome, Stevens-Johnson syndrome.

Complications in the work of the immune system: increased sensitivity, angioedema, anaphylactic shock. Allergic reactions with rejection of the epidermis.

AT rare cases post-injection abscess may occur. There are cases of compaction and soreness at the injection site, less often - swelling, necrosis.

There is a risk of developing aseptic meningitis.

Important! Side effects and their intensity largely depend on the dose of the drug. It is advisable to use the minimum effective dose. With prolonged use and excess dosage, the risk of complications increases, in particular, this applies to the heart and blood vessels.

In the event of any negative reactions organism on the drug, inform your doctor immediately. A common side effect is bad feeling associated with the GI tract, it may just be a minor side effect, but may also signal an ulcer/bleeding.

Interaction with other chemicals and drugs

Lithium preparations, digoxin, phenytoin: diclofenac increases the concentration of drugs in the blood.

The effect of antihypertensive and diuretic drugs is weakened. Potassium-sparing diuretics, when taken with diclofenac, give the effect of hyperkalemia.

Reception with other NSAIDs is undesirable, as the risk of side effects from the digestive system increases.

The use of quinolone derivatives increases the risk of seizures.

Cyclosporine increases nephrotoxicity.

With the simultaneous use of methotrexate, its concentration increases and toxic properties increase.

Combination with anti-diabetic drugs can cause sharp spikes in insulin levels: both a significant decrease and an increase.

Diclofenac injections are categorically contraindicated if the patient abuses alcohol. The drug is not compatible with ethyl alcohol: simultaneous reception is fraught with stomach bleeding and liver damage.

Use the drug with caution while prescribing anticoagulants, antiplatelet agents, antidepressants from the SSRI group, and glucocorticosteroids.

Captopril, enalapril - diclofenac reduces their concentration, as a result of which the dose must be increased.

special instructions

Since the active substance of the drug prevents platelet aggregation, it is necessary to take laboratory control blood clotting.

During pregnancy, diclofenac injections are prescribed only if the benefit to the mother is greater than potential danger for the fetus. Treatment is possible only in the first and second semester, in the third semester the drug is contraindicated due to the risk of intrauterine hypoxia. In general, it is best not to use this remedy at any stage of pregnancy. Diclofenac can adversely affect the fetus, increasing the likelihood of intrauterine malformations (it is a teratogenic substance). Also, the remedy affects labor activity, when it is taken, it can become weak. There is a risk of developing postpartum hemorrhage. If it becomes necessary to inject the drug during lactation, it is worth stopping breastfeeding for the duration of treatment.

Reduce the dose when using other NSAIDs. Tell your doctor if you are taking any medications at the same time as diclofenac. Check out their interactions.

Work that requires a high speed of psychomotor reactions and increased concentration of attention during the treatment period is undesirable.

Strict medical supervision is necessary when diclofenac is used in patients with the following conditions: inflammatory and ulcerative lesions history of digestive system systemic diseases connective tissue, dysfunction of the liver and organs of the excretory system, diabetes mellitus, hypertension, heart failure, induced porphyria, chronic infectious diseases respiratory tract, accompanied by their inflammation, chronic obstructive pulmonary disease, the period after surgery, lipid metabolism disorders, old age.

Avoid contact with mucous membranes and eyes, otherwise an allergic reaction may develop.

Overdose

If the recommended doses are exceeded, the phenomena of dysfunction of the digestive and nervous systems develop: nausea, diarrhea, vomiting, sharp pain in the abdomen, gastric and intestinal bleeding, headache, dizziness, hyperventilation of the lungs, clouding of consciousness, increased convulsive readiness of the muscles. These conditions are treated with symptomatic therapy aimed at correcting kidney function, reducing negative side effects on the digestive system, stopping seizures, and normalizing breathing. There is no specific antidote. Methods such as forced diuresis, hemodialysis do not help.

Terms of dispensing from pharmacies

Without recipe.

Analogues

Diclofenac sodium or potassium is the active substance in the following drugs: Diclofen, Diclomax, Diclorium, Diclonac, Voltaren, Diclomelan, Naklofen, Ortofen, Revmavek, Diclonat P.

Prices

Diclofenac is an inexpensive drug, in Moscow pharmacies its cost is 67 - 93 rubles. The cost depends on the manufacturer. For example, a Serbian-made product costs from 10 rubles per 1 ampoule. Analogues (Voltaren, Naklofen, Diklonat P) are more expensive.

Frequently Asked Questions about Diclofenac

• Which dosage form is better - tablets or injections?

Depending on the characteristics of the case of the disease and the phase of treatment. At first, injections are prescribed as a faster form. Then they move on to pills and local medicines(ointments, gels). If it is necessary to treat children with this drug, suppositories are often prescribed because of the pain of injections.

• Which injectable drug is better - Diclofenac or Voltaren?

Voltaren is an analogue of Diclofenac, since active ingredient they are one and the same.

• Is it possible to take Diclofenac and Milgamma at the same time?

Can. This is a complex of vitamins, and it is quite acceptable to prescribe them at the same time.

• If there are contraindications, which analogue is better to choose?

If you have states that are absolute or even relative contraindications to receive diclofenac, it would be advisable to use instead drugs similar in action, but differing in composition with it: selective inhibitors of cyclooxygenase of the second type, for example, Movalis, are suitable. However, only your doctor can answer which medicine is better for you to replace it with.

Features of the composition of the drug

There are solvents - water for injection and benzyl alcohol, almost no excipients.

If we compare diclofenac with other drugs of the NSAID group, we will notice that it has a weaker effect on the gastric mucosa, and also has less cardiotoxicity.

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Any diseases of the musculoskeletal system are accompanied by pain. It becomes especially strong after sleep, when soft tissues accumulate fluid, which manifests itself in the form of puffiness and swelling. by the most the best option eliminate this kind of pain, by removing the inflammatory process and rapid pain relief, is taking Diclofenac. The non-steroidal anti-inflammatory drug has a fairly wide choice of forms of release (gels and creams, injections, tablets, suppositories), which increases its effectiveness by treating not only the focus of inflammation, but also acting on it from the inside. How to use this drug correctly, and what contraindications it has, we will consider further.

pharmachologic effect

Diclofenac belongs to the group of NSAIDs. The active substance is diclofenac sodium affects the synthesis of prostaglandins in the focus of inflammation, reducing their concentration. Also, the drug inhibits the metabolic processes of arachidonic acid and cyclooxygenase. All this together allows you to achieve such favorable results as:

• removal of inflammation;
• relief of pain in the focus of inflammation;
• elimination of hyperemia of the skin (fever).

A drug able to penetrate the synovial fluid and linger there, being in maximum concentration. After taking Diclofenac, it is well absorbed into the blood. Maximum concentration in plasma is achieved, depending on the form of administration:

• tablets - 2-3 hours;
• injections - 15-20 minutes;
• ointment and gel - 2-4 hours.

Almost completely associated with blood albumin, where in the process of metabolism in the liver they break down into simpler compounds that are excreted through the kidneys after 6-12 hours. Diclofenac does not accumulate, so it can be used for long-term treatment, not addictive without compromising their effectiveness.

Composition and form of release

Depending on the form of release, the content of the main component of diclofenac sodium is excellent:

Ask your question to a neurologist for free

Irina Martynova. Graduated from the Voronezh State medical University them. N.N. Burdenko. Clinical intern and neurologist of BUZ VO "Moscow polyclinic".

1. Tablets coated, white or yellowish color. There can be two dosages: 25 and 50 mg of the active substance. Auxiliary components are also present:

• corn starch;
• dye;
• titanium dioxide.

Tablets are packed in 10, 20, 30 pieces in blisters or dark glass jars.

1. Injection- contains diclofenac sodium:

• 1 ampoule - 25 mg;
• 1 ampoule - 75 mg.

Excipients:

• purified water;
• benzyl alcohol;
• propylene glycol;
• sodium metabisulphite;
• sodium hydroxide.

Ampoules are packed in cardboard or plastic boxes, 3-5 ampoules in each.

1. Candles contain 25 mg of diclofenac sodium, as well as auxiliary components, including solid fat, glycerin and dye. Packed rectal suppositories 5-10 pieces in a sealed package.
2. Ointment 2% packed in an iron tube, with a volume of 30 g. The content of diclofenac sodium in 1 g of ointment is 20 mg. Used for external use.
3. Gel 5%- Diclofenac Forte, which has increased concentration active ingredient, contains in 1 g:

• diclofenac sodium - 50 mg;
• dimexide;
• propylene glycol;
• purified water;
• macrogol.

It has a homogeneous gel consistency, transparent color, sometimes with air bubbles. One tube has a volume of 40 g.

1. Gel and ointment 1%- contain in their composition diclofenac sodium 10 mg per 1 g of ointment or gel. Such a dosage is convenient if complex treatment is performed, requiring not only oral administration, but also a local effect on the focus of inflammation.
2. Eye drops 0.1%- Packed in a bottle of 5 or 10 ml with a dispenser. In 1 ml of drops 1 mg of the active substance. Drops of a transparent color, sometimes with a yellowish tint. Auxiliary components:

• sodium chloride;
• distilled water;
• sodium hydroxide.

Application

Diclofenac is prescribed in the treatment of diseases such as:

1. Inflammatory processes of the musculoskeletal system and joints:

• osteoarthritis;
• spondylitis;
• osteochondrosis of the spinal column;
• lumbago;
• sprains and ruptures of ligaments;
• soft tissue injuries and bruises.

1. As part of complex therapy in the treatment of ENT diseases:

• pharyngitis;
• otitis;
• tonsillitis.

1. Preparing for eye surgery, as well as eliminating negative reactions after it:

• cataract;
• edema yellow spot retina of the eye;
• photophobia.

1. Removal of pain syndrome at:

• renal and hepatic colic;
• proctitis;
• adnexitis;
• algomenorrhea;
• migraine.

Depending on the form of release, the drug is used as follows:

1. Tablets- apply between meals(the process of absorption and digestibility fall sharply when consumed with meals), without chewing in the oral cavity, drinking water. Permissible daily dose - 150 mg. It is recommended to use 25-50 mg (1-2 tablets) 2-3 times a day. After achieving the effect, the dosage should be reduced to the minimum. AT childhood(from 6 years old) the dosage is calculated from the proportion of 2 mg tablets per 1 kg of weight.
2. Solution for injection - injected deep intramuscularly, not more than 75 mg (1 ampoule). If necessary, the injection is repeated, but not earlier than after 12 hours. After 2-3 days of drug administration, it is recommended to switch to oral administration of the drug, maintaining the dosage.

Diclofenac in injections is never administered intravenously, as this can provoke not only chemical burn soft tissues, but also to develop severe intoxication

1. Rectal suppositories- enter 1-2 candles per anus , must first be set cleansing enema for maximum absorption active ingredients in the rectum. Suppositories are effective in inflammatory processes of the pelvic region, as well as gynecological diseases.
2. Eye drops- bury in the conjunctival sac 1 drop every 3-4 hours. After surgery, the frequency of instillations is regulated by the attending physician.
3. Gels and ointments inflict on clean skin with smooth massaging movements rubbing well into the skin until completely absorbed. The number of daily applications should not exceed 2-3 times.

Since some types of gels with diclofenac sodium have an increased concentration (5%), you need to make sure that an overdose does not occur if tablets, injections or suppositories are used in addition to ointments and creams.

Contraindications

• children's age up to 6 years;
• period of pregnancy and lactation;
• gastric and duodenal ulcer in the acute stage;
• violation of hematopoiesis;
• poor blood clotting, as well as a tendency to bleed.

With extreme caution used in the presence of such diseases:

• renal and liver failure;
• cardiovascular diseases;
• diabetes;
• anemia;
• arrhythmia;
• bronchial asthma;
• advanced age.

The presence of contraindications, and adverse reactions says that treatment with Diclofenac should be done only on the recommendation of a doctor, strictly following all his recommendations regarding forms and dosages.

In no case should you combine medication with alcoholic beverages, as this can lead to severe intoxication and collapse, which is extremely life-threatening.

Overdose

With a slight excess specified daily allowable dose , the patient may have the following symptoms:

• nausea, vomiting, dizziness up to loss of consciousness;
• convulsions;
• cardiopalmus;
• bleeding;
• pain in the epigastric region.

If there is an overdose carry out symptomatic treatment meaning:

1. Washing the gastrointestinal tract, which reduces the concentration of toxins;
2. The introduction of a large dose of any sorbent that binds and neutralizes toxins.
3. Plentiful drink boiled water room temperature

If the symptoms are life-threatening, you need to urgently call an ambulance.

Side effects

The most common adverse reactions found in patients who used Diclofenac are:

• stomach ache;
• swelling of the limbs;
• noise in ears;
• anemia;
• sleep disturbance;
• chest cough.

most dangerous side effect considered an allergic reaction, which can take the form:

• skin rash - small vesicular tubercles filled with a clear liquid;
• swelling of the mucous membranes;
• skin itching;
• anaphylactic shock and angioedema.

If taking Diclofenac caused at least one of the adverse reactions, treatment is stopped until the allergy is completely eliminated and studied.

With the rapid development of an allergic reaction, the patient is injected deeply intramuscularly with any antihistamine in a double dose. If resuscitation is necessary, the products of the metabolism of diclofenac sodium are removed by dialysis (the introduction of a large amount of liquid by drip).

drug interaction

Diclofenac May reduce the effectiveness of diuretics, increasing and retaining sodium and lithium salts in large quantities. Reduces the activity of antihypertensive drugs, as well as neutralizes the effects of sleeping pills drugs.

• corticotropin;
• ethanol in pure form;
• colchicine;
• cefoperazone;
• plicacimin.

Their simultaneous use leads to the development of internal erosions and bleeding in the gastrointestinal tract.

It makes no sense to use acetylsalicylic acid, since it significantly reduces the effectiveness of Diclofenac, by dissolving it during metabolism into inactive particles (pacifiers).

Advantages

The most important advantage Diclofenac, regardless of the form of release, is its affordable price. This is one of the most affordable NSAIDs, which absolutely any patient can afford. Also drug not addictive. Its constant introduction does not affect the effectiveness. The course of treatment can be selected individually, gradually reducing the dosage to a minimum.

Price

The average price for medicines containing diclofenac sodium is as follows:

• tablets - 15-20 rubles for 10 pieces;
• ointments and gels - 25-60 rubles (depending on the dosage and volume of the tube);
• rectal suppositories - 35-70 rubles for 5 pieces;
• solutions for intramuscular injection - 30-35 rubles per pack;
• eye drops- 20-45 rubles (5 and 10 ml).

Terms of dispensing from pharmacies

Tablets, eye drops and injection solution are dispensed strictly by prescription. Other forms are allowed for free OTC sale.

Storage conditions

Tablets, suppositories and ampoules for injections are stored in a cool dry place (preferably in the refrigerator). Ointments and gels can be stored in the first aid kit, tightly closing the cap of the tube after each use.

Best before date

Eye drops and rectal suppositories are stored for no more than 1 year from the date of manufacture. Other forms are stored up to 2 years from the date of production.

Analogues

Among the drugs that have a similar effect on the body, the following analogues can be distinguished:

• Naklofen - 100 rubles;
• - 40 rubles;
• - 320 rubles;
• Diklovit candles - 150 rubles;
• - 120 rubles;
• - 15 rubles.

In this way, Diclofenac has a huge choice of forms of use, however, you need to understand that you do not need to use them all together at the same time. This can provoke an overdose, which will lead to intoxication and a lot of negative effects on the body. Treatment should be carried out exclusively under the supervision of doctors who will select a reasonable dosage and the most suitable form. Instructions for use may not reflect the danger that the medicine contains.

AT Diclofenac gel 5% 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 ointment Diclofenac: 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 injections.

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

Compound enteric coated tablets: 25 or 50 mg Diclofenac sodium, dibasic 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 in p / o: 25 mg Diclofenac sodium, milk sugar, sucrose, povidone, stearic acid, potato starch. Shell: Castor oil, cellacephate, titanium dioxide, tropeo-lin O and azorubine dyes.

Compound retard tablets: 100 mg Diclofenac sodium, hypromellose, gietellose, kollidone SR, sodium alginate, MCC, magnesium stearate. Sheath: collicute 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 for injections.

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, eye drops 0.1% (ATC code - S01BC03).

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

pharmachologic effect

Anti-inflammatory, analgesic, antipyretic.

Pharmacodynamics and pharmacokinetics

NSAID Diclofenac is a derivative phenylacetic acid . The mechanism of its action is based on the ability to inhibit 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 by 1-4 hours (while reducing Cmax by 40%). Cmax when taken orally is noted after 2-3 hours. Changes in this indicator are dose-dependent.

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

Bioavailability - 50%. It binds to plasma proteins by more than 99% (the connection is mainly with albumin ). Penetrates into synovia and breast milk.

Half taken dose 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 rest of the administered drug is excreted in the bile.

Indications for the use of Diclofenac in injections and suppositories. What helps Diclofenac in tablets?

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

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

Candles are also prescribed in addition to the main treatment for severe inflammatory ENT diseases (for example, otitis media , 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 solution for injection is administered with either the liver, acute pain in the back or muscles when they are damaged, after surgery.

For the treatment and prevention of postoperative pain syndrome, the introduction of Diclofenac intravenously is indicated.

Why diclofenac tablets?

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

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

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

What do the ointment and gel form of Diclofenac help from?

Gel and ointment with Diclofenac are easy to dose and easy to use. After applying them to the skin, the active substance accumulates in soft tissues, practically without getting into the bloodstream (no more than 6% of the substance enters the bloodstream). These dosage forms are used for various kinds of disorders. locomotor system .

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

What diseases are prescribed rectal suppositories?

The drug is prescribed when it is impossible to take the medicine through the mouth: in the presence of strictures of the esophagus, in debilitated patients, etc.

When taken orally, the drug 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 , the formation of infiltrates and suppuration 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 best results due to a more uniform and longer maintenance of a certain plasma concentration drug.

Suppositories with Diclofenac are considered one of the best suppositories from . When administered rectally, the drug does not pass through the liver and almost completely enters the prostate .

In gynecology, candles 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 in the maximum short time: in the vagina, the medicine quickly dissolves under the influence of temperature and is also 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 inflammation of a non-infectious nature affecting the anterior sections of the eye;
• prevention of edema before and after surgery to remove and implant the lens;
• relief of pain 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 Milgamma ? it combination drug, which is based on initamines of group B . The latter potentiate the effects analgesics , while allowing to reduce the dose of NSAIDs, and significantly 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, perforation of the walls of the digestive canal, gastric and intestinal bleeding;
• inflammatory diseases of the digestive tract;
• “aspirin asthma ”;
• severe functional insufficiency of the heart, kidneys, liver.

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

Rectal administration 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, suppositories 50 mg and tablets in a c / r shell are prescribed from the age of 14. Retard tablets and suppositories 100 mg 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.

With caution, drops are prescribed for " aspirin asthma ”, superficial herpetic keratitis , diseases that are accompanied by impaired plasma hemostasis; children, the elderly, pregnant and lactating women.

Side effects of Diclofenac

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

After applying the drops are noted:

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

Side effects of injections

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

Application instruction of Diclofenac

Diclofenac injections: instructions for use

For the relief of acute conditions or relief of exacerbated chronic disease Diclofenac in ampoules is administered 1 time intramuscularly (deeply). In the future, the patient is transferred to the tablet form of the drug.

Dosage of injections - 25-50 mg 2 or 3 rubles / 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 of NaCl solution 0.9% or dextrose solution 5%. Infusion solutions are preliminarily added with a solution of sodium bicarbonate (0.5 ml, if the concentration of the solution is 8.4%, and 1 ml, if the concentration is 4.2%).

Duration of infusion - depending on the intensity of pain - from half an hour to one and a half hours.

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

How many days can I inject Diclofenac?

V / m injections of Diclofenac are allowed to do no more than 2 days in a row. In some cases, the course of treatment with injections can be 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.

Gel Diclofenac: instructions for use

A single dose of the gel depends on the size of the painful area. As a rule, 2 to 4 grams of the product is 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 drug injections.

Ointment Diclofenac: instructions for use

The ointment is taken in the same amount as the gel, and similarly rubbed into the skin over the focus of inflammation. Maximum dose- 8 g / day. Multiplicity of application - 2-3 rubles / day.

Tablets Diclofenac: instructions for use

Diclofenac tablets (Acri, UBF, Stada, Sandoz, etc.) are taken per os with food or after eating (without chewing or crushing). Adults should take 50 to 150 mg/day. for 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 desired effect not achieved, you can additionally take 1 tablet of 50 mg (usual duration of action).

Candles Diclofenac: 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 the operation, the patient is administered 5 times every 30-35 minutes, 1 drop of the solution. After the operation - 3 times 1 drop. AT further treatment continue, burying 3-5 rubles / day. 1 drop. The duration of treatment depends on the characteristics of the clinical situation.

Additionally

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

Overdose

Overdose can cause CNS disorders and digestive disorders. The first most often appear:

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

Gastrointestinal disorders are manifested by: nausea, abdominal pain, vomiting, gastrointestinal bleeding.

In severe poisoning, liver damage, acute kidney failure, respiratory depression, hypotension.

The drug has no antidote. special measures, such as hemoperfusion , dialysis or forced diuresis , do not guarantee the withdrawal 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, an overdose of them is considered unlikely. Accidental swallowing gel or ointment can provoke systemic adverse reactions.

The patient is prescribed a gastric lavage, stimulate vomiting, give a drink enterosorbent . Therapy is symptomatic.

Interaction

Simultaneous use with:

• lithium preparations , or — promotes increase in plasma concentration of the specified means;
• 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 - can provoke hyper- or hypoglycemia ;
• - can lead to an increase in the concentration and increased toxicity of the latter;
• anticoagulants - requires regular monitoring hemocoagulation .

If indicated, eye drops can be combined with other ophthalmic agents, which include corticosteroids (at least a 5-minute break must be maintained between instillations).

Terms of sale

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

Storage conditions

List B. The optimal temperature regime is 10-25 ° C.

Best before date

Diclofenac (eye drops) has the following analogues: synonyms - Voltaren Ofta , Diklo-F , Diclofenaklong , Uniclofen ; drugs with similar 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, thus the ointment is a more viscous substance in comparison with the gel. It is absorbed more slowly and in some cases can cause clogging of 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 mainly used to treat irritated and flaky skin. The gel is more effective for deep layers of skin and joints.

Voltaren or Diclofenac - which is better?

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

Voltaren differs only in that, when applied externally, it is more quickly absorbed into the tissues and penetrates into the focus 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 (derivative of ethanolic acid), like diclofenac sodium, belongs to the group of NSAIDs. Diclofenac non-selectively inhibits the activity of COX-1 and COX-2 enzymes, while meloxicam shows selectivity for COX-2.

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

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

Moreover, unlike analogous meloxicam has a stimulating effect on the metabolism of cartilaginous tissue.

Which is better: Diclofenac or Ibuprofen?

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

However, unlike its counterpart, somewhat better tolerated by children and pregnant women, which makes it possible to use it (albeit with caution) in pediatrics and obstetric and gynecological 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 ten times more effective than drugs ibuprofen , which makes it appropriate to use it for the treatment of spinal injuries and osteochondrosis .

By non-selectively suppressing COX, it quickly causes adverse reactions from the gastrointestinal tract, even when applied externally.

Which is better - Diclofenac or Ketorol?

- this is non-selective inhibitor SOH. According to doctors, the effectiveness of pills Ketorola higher than the effectiveness of Diclofenac tablets, and the effectiveness of the solution for injection is comparable. At the same time, with comparable analgesic efficacy, the duration of action Ketorola twice as large as 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?

Diclofenac drugs and Dont Have fundamental differences, since they are based on the same active substance.

Which is better: Diclofenac or Diclofenac Retard?

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

Aceclofenac and Diclofenac - difference

Aceclofenac is a derivative of phenylacetic acid.

It is distinguished by high bioavailability and a high speed of reaching peak blood concentration (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 inhibits the synthesis of interleukin-1 and tumor necrosis factor, which are the most important pro-inflammatory cytokines.

To date, this drug is considered one of the best. Its advantages:

• availability;
• high quality;
• balanced combination of anti-inflammatory and analgesic efficacy with
• good tolerance.

Diclofenac with alcohol - compatible or not?

Diclofenac and alcohol are incompatible.

Consequences of alcohol with NSAIDs

Drinking alcohol during treatment with NSAIDs can cause:

• deterioration of the liver;
• reducing the effectiveness of the drug;
• development of unpredictable complications and adverse reactions;
• and, as a consequence, increased congestion in the circulatory system and intoxication of the body.

Injections and alcohol do not have compatibility, since the injectable form of the drug stimulates the activity of the central nervous system, and 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 provoke a lack of uterine contraction in a parturient woman and / or premature closure of the ductus arteriosus in a newborn.

The drug 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 a 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.

Back pain in osteochondrosis occurs due to an inflammatory reaction in the intervertebral joints, muscles and roots of the spinal nerves.

Insufficient supply nutrients to tissues leads to the destruction of their cells with the release into the surrounding space of biologically active substances - pro-inflammatory mediators. They trigger an inflammatory response that is manifested by swelling, pain, and dysfunction of the spine.

Eliminate most effectively pain syndrome in such cases, non-steroidal anti-inflammatory drugs (NSAIDs). One of the representatives of the group is Diclofenac, which we will dwell on in detail.

Pharmacological action of Diclofenac injections

Diclofenac refers to anti-inflammatory drugs of non-hormonal origin. It combines a pronounced analgesic and anti-inflammatory action.

Diclofenac prevents the release of the main precursor of inflammatory substances - arachidonic acid from the membranes of damaged cells. Thus, the drug stops the cascade chemical reactions, leading to the expansion of blood vessels, the release of fluid from them and tissue edema.

Pain during inflammation is caused by compression of sensitive nerve receptors and exposure to pro-inflammatory mediators. Diclofenac blocks their synthesis, thanks to which it quickly eliminates the pain syndrome and prevents its recurrence.

Often the inflammatory response loses its protective function and contributes to additional damage to the intervertebral joints and nerve roots. Prolonged stagnation of blood in the vessels leads to a deterioration in the nutrition of tissues, the accumulation of metabolic products in them and acidification of the environment in the focus of inflammation. Cells that are not initially affected by the degenerative process cannot function under such conditions and die.

Accordingly, a new release of arachidonic acid enhances the inflammatory process and the pathological circle closes. Diclofenac breaks it: it improves blood circulation and protects living cells from destruction. The inflammatory reaction quickly subsides, the pain syndrome stops.

Compound

Diclofenac is produced as a solution for intramuscular injection, packaged in 3 ml glass ampoules. 1 ml of solution is:

• diclofenac 25 mg;
• mannitol;
• benzyl alcohol;
• sodium hydroxide;
• sodium metabisulfite;
• propylene glycol;
• sterile water up to 1 ml.

Excipients in the solution serve as preservatives and stabilizers of the active ingredient.

Indications for use

It is indicated in most situations, the pain in which is due to the inflammatory process:

• , plexitis, neuritis;
• lumbago ( , );
• rheumatic diseases (spondylitis, sacroiliitis, rheumatoid arthritis, gout, osteoarthritis);
• rheumatic damage to the eyes, heart, blood vessels;
• renal and hepatic colic;
• pain after injury or surgery;
• painful menstruation, acute inflammatory diseases female reproductive system(adnexitis, salpingitis);
• severe headache (including migraine);
• acute otitis media, sinusitis, eustachitis.

Contraindications

Diclofenac should not be used in the following cases:

• hypersensitivity to the drug or to other members of its group;
• erosive and ulcerative lesions of the stomach and duodenum during an exacerbation or with a history of perforation;
• reduced blood clotting;
• bleeding at any level of the digestive tract;
• violation of hematopoiesis;
• allergic reactions to NSAIDs, including aspirin asthma;
• severe liver and kidney failure;
• decompensated heart failure;
• hemorrhagic stroke in history or the risk of its development;
• previous myocardial infarction, coronary artery bypass surgery;
• peripheral arterial disease (pronounced atherosclerosis);
• dehydration or acute blood loss;
• inflammatory bowel disease;
• infertility (when trying to conceive a child);
• last trimester of pregnancy, feeding;
• childhood.

The course of treatment with injections: instructions for use

A solution of Diclofenac is injected intramuscularly deep into the buttock or front of the thigh. The injection is performed with a 5 ml syringe: its needle is long enough for intramuscular injection.

A burning sensation may be felt at the injection site, which disappears within a short time.

Diclofenac is absorbed from the muscle into the blood and creates a high concentration in the tissues within half an hour.

Side effects of the drug are directly related to its dose, so it is recommended to use the minimum effective amount of the substance.

Usually start with 75 mg per day, if necessary, increasing to 150 mg of Diclofenac per day.

Injections are performed once a day, but if necessary, you can re-introduce the drug in at least half an hour. The maximum dosage of Diclofenac is 150 mg (6 ml) per day. The course of treatment with injections is 2 days, the attending physician can extend it up to 5 days according to indications.

Side effects

Along with high efficiency, Diclofenac has an extensive list of adverse reactions. They are associated with the cessation of the synthesis of prostaglandins, which, in addition to participating in the inflammatory response, play important role in many organs and systems: protect the gastric mucosa from aggression of hydrochloric acid, for example.

The use of Diclofenac can cause:

• decreased blood clotting;
• inhibition of red bone marrow function;
• allergic reactions (including dangerous skin reactions with rejection of the epidermis);
• irritability, depression, insomnia, headache;
• drowsiness, hallucinations, impaired sensitivity, memory, vision;
• aseptic inflammation of the meninges;
• ringing in the ears and hearing impairment;
• lowering blood pressure;
• asthma, pneumonia;
• nausea, vomiting, abdominal pain, ulcer perforation, bleeding (vomiting and bloody stools), stomatitis, pancreatitis;
• liver damage (hepatitis, hepatonecrosis);
• hair loss;
• photosensitivity;
• kidney damage (nephritis, necrosis of the renal papillae);
• formation of infiltrate and abscess at the injection site;
• respiratory dysfunction.

During pregnancy

The use of Diclofenac is possible in the 1st and 2nd trimesters of pregnancy strictly according to indications and after a doctor's prescription! The drug affects the development of the embryo and increases the risk of congenital malformations. Diclofenac is prescribed in a minimal amount and for a short time.

In the 3rd trimester of pregnancy, the use of the drug can lead to severe fetal hypoxia and death. In addition, Diclofenac reduces the contractility of the uterus, which is fraught with weakness. labor activity and postpartum hemorrhage.

Interaction with alcohol

The combined use of Diclofenac with ethanol increases the risk of gastrointestinal bleeding and liver damage.

Medicine price

Diclofenac is an affordable drug, the average cost is:

• ampoules (made in Serbia) 3 ml 10 rubles per 1 pc.;
• ampoules 3 ml 51 rubles for 5 pcs.;
• ampoules (made in Belarus) 3 ml 45 rubles for 10 pcs.

Analogues

Diclofenac as an active substance contains solutions:

• Voltaren;
• Diclomax;
• Diclonac;
• Diclorium;
• Diclofen;
• Nakloof;
• Diclomelan;
• Naklofen;
• Ortofen;
• Orthofer;
• Diklonat P;
• Revmavek.