Artrum

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Artrum: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Artrum

ATX code: M01AE03

Active ingredient: ketoprofen (Ketoprofen)

Manufacturer: Biosynthesis, PJSC (Russia)

Description and photo updated: 2019-27-08

Prices in pharmacies: from 113 rubles.

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Solution for intravenous and intramuscular administration Artrum

Artrum is a non-steroidal anti-inflammatory drug for internal, external and local use.

Release form and composition

Artrum is available in the following forms:

prolonged-release tablets: biconvex, round, white (20 pieces in dark glass bottles, one bottle in a cardboard box);
solution for intravenous and intramuscular administration: transparent, with a slight yellowish tinge or colorless (2 ml in dark glass ampoules, 5 ampoules in a blister, two packs in a cardboard box; 2 ml in dark glass ampoules, in a cardboard box 10 ampoules);
rectal suppositories: torpedo-shaped, white with a yellowish or creamy tinge (5 pieces in a blister strip, in a cardboard box 1 or 2 packages);
gel for external use: colorless, not greasy, with a specific odor (30 g or 50 g each in aluminum tubes, one tube in a cardboard box).

Each pack also contains instructions for using Artrum.

Composition of 1 tablet:

active substance: ketoprofen - 150 mg;
auxiliary components: povidone, hypromellose, colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate.

Composition of 1 ml solution:

active substance: ketoprofen - 50 mg;
auxiliary components: benzyl alcohol, 96% ethanol, sodium hydroxide to maintain the pH level of 6.0-7.5, propylene glycol, water for injection.

Composition of 1 suppository:

active substance: ketoprofen - 100 mg;
auxiliary components: polysorbate-80, witepsol W-35, distilled monoglycerides, solid fat or witepsol N-15.

Composition of 1 g of gel:

active substance: ketoprofen - 25 mg or 50 mg (in terms of 100% substance);
auxiliary components: trolamine, ethanol, lightly crosslinked polyacrylate, propylene glycol, purified water.

Pharmacological properties

Pharmacodynamics

The active substance in Artrum is ketoprofen, which is a non-steroidal anti-inflammatory drug. It has anti-inflammatory, analgesic and antipyretic effects.

Blocks the action of the enzyme COX-1 and -2 (cyclooxygenase 1 and 2) and, in part, lipoxygenase, as a result, the synthesis of prostaglandins is suppressed (including in the central nervous system, most likely in the hypothalamus). Stabilizes liposomal membranes, inhibits the synthesis of leukotrienes and bradykinin at high concentrations.

Ketoprofen does not have a negative effect on the condition of the articular cartilage.

Pharmacokinetics

Extended-release tablets

The substance is well absorbed from the gastrointestinal tract, the bioavailability level is 90%. Communication with blood plasma proteins - 99%. C _max (maximum concentration of the substance) in plasma after oral administration of 150 mg is 10.4 ug / ml, the time to achieve - 4-6 hours.

Ketoprofen is associated with blood plasma proteins by 99%, mainly with the albumin fraction; V _d (volume of distribution) - 0.1 l / kg.

The substance penetrates into the synovial fluid, where it reaches a concentration equal to 30% of the plasma concentration. Plasma clearance of ketoprofen is about 0.08 l / kg / h. The effective concentration of a substance in the blood is determined 24 hours after its administration.

Under the action of microsomal liver enzymes, ketoprofen undergoes intensive metabolism, T _1/2 (half-life) is less than 2 hours. It binds to glucuronic acid and is excreted as glucuronide. There are no active metabolites. Up to 80% of ketoprofen is excreted by the kidneys in 24 hours, mainly in the form of ketoprofen glucuronide.

In the case of using Artrum at a dose of 100 mg or more, excretion by the kidneys may be difficult. In patients with severe renal impairment, most of the substance is excreted through the intestines.

When high doses are taken, hepatic clearance also increases. Up to 40% of ketoprofen is excreted through the intestines.

Plasma concentration of a substance in liver failure is doubled; with such a concomitant disease, Artrum should be prescribed in the minimum therapeutic dose. The clearance of ketoprofen in renal failure is reduced, however, dose adjustment should be performed only in severe renal failure.

Metabolism and excretion of ketoprofen in elderly patients slows down. This is of clinical importance only in the case of severe renal failure.

Solution for intravenous and intramuscular administration

The biological availability of ketoprofen is more than 90%. Binds to plasma proteins at a level of 99%. With parenteral administration, C _max in plasma is reached within 15–30 minutes. Penetrates into synovial fluid.

Ketoprofen has a first pass effect through the liver. The substance undergoes intensive metabolism with the participation of microsomal liver enzymes. It binds to glucuronic acid and is excreted from the body in the form of glucuronide.

Up to 80% of ketoprofen is excreted by the kidneys, mainly (more than 90%) in the form of ketoprofen glucuronide, about 10% through the intestines. Biological T _1/2 is less than 2 hours, which is associated with a fast metabolism.

With renal failure, ketoprofen is excreted more slowly, its T _1/2 increases by 60 minutes. In liver failure, T _1/2 also increases, so there may be an accumulation of the substance in the tissues.

Metabolism and excretion of ketoprofen in elderly patients proceed more slowly, this is of clinical importance only against the background of severe renal failure.

Rectal suppositories

The absorption of ketoprofen is fast, bioavailability is 90%. Up to 99% of absorbed ketoprofen binds to plasma proteins (mainly albumin). The substance penetrates well into connective tissues and synovial fluid. C _max in synovial fluid is about 30% of serum, and 4–6 hours after drug administration, it exceeds its value.

Ketoprofen crosses the blood-brain barrier.

Excretion: the main part of the dose - by the kidneys, 1–8% - through the intestines. T _1/2 is in the range from 1.6 to 1.9 hours. In elderly patients, this indicator increases to 3-5 hours, in patients with renal failure (with creatinine clearance from 20 to 60 ml / min) - about 3.5 hours. Does not cumulate.

Gel for external use

With cutaneous application, ketoprofen is absorbed slowly. It practically does not accumulate in the body. Bioavailability of Artrum in gel form is approximately 5%.

Indications for use

symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system (tendinitis, bursitis, periarthritis, tendosynovitis, arthrosynovitis, lumbago);
articular syndrome (osteoarthritis, gout, rheumatoid arthritis, ankylosing spondylitis, reactive arthritis, psoriatic arthritis, osteoarthritis, pseudogout);
pain syndrome (headache, algomenorrhea, neuralgia, myalgia, radiculitis, pain in cancer, post-traumatic and postoperative pain);
inflammatory diseases of the lymphatic vessels, veins and lymph nodes (lymphangitis, phlebitis, superficial lymphadenitis, periphlebitis);
uncomplicated injuries (including dislocations, bruises, sports injuries, sprains or ruptures of tendons and ligaments, post-traumatic pain).

Contraindications

Extended-release tablets, solution for intravenous and intramuscular administration

Absolute:

Crohn's disease, ulcerative colitis;
exacerbation of gastric or duodenal ulcer;
complete (incomplete) combination of bronchial asthma with recurrent polyposis of the nose / paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a burdened history);
hemophilia and other blood clotting disorders;
period after coronary artery bypass grafting;
severe renal failure: severe renal failure (in patients with creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;
severe liver failure;
decompensated heart failure;
chronic dyspepsia;
cerebrovascular, gastrointestinal and other bleeding (or suspicion of them);
age up to 15 years;
III trimester of pregnancy and breastfeeding period;
individual intolerance to the components of Artrum, as well as salicylates or other non-steroidal anti-inflammatory drugs.

Relative (Artrum is prescribed under medical supervision):

burdened history of bronchial asthma;
arterial hypertension, chronic heart failure, blood diseases;
clinically expressed cerebrovascular, cardiovascular and peripheral arterial diseases;
chronic renal failure (in patients with creatinine clearance from 30 to 60 ml / min);
liver failure, dyslipidemia, alcoholic liver cirrhosis, hyperbilirubinemia;
dehydration;
diabetes;
combined use with selective serotonin reuptake inhibitors (including fluoxetine, citalopram, paroxetine, sertraline), anticoagulants (including warfarin), oral glucocorticosteroids (including prednisolone), antiplatelet agents (including clopidogrel);
long-term use of non-steroidal anti-inflammatory drugs;
burdened history of peptic ulcer of the gastrointestinal tract, the presence of Helicobacter pylori infection;
smoking;
elderly age;
I and II trimester of pregnancy.

Rectal suppositories

Absolute:

hemorrhoids, rectal bleeding, inflammation or trauma of the rectum;
gastrointestinal, cerebrovascular and other bleeding (or suspicion of them);
burdened history of bronchial asthma, the development of which is associated with ketoprofen, other non-steroidal anti-inflammatory drugs, or acetylsalicylic acid;
peptic ulcer;
Crohn's disease, ulcerative colitis, diverticulitis;
insufficiency of the circulatory system;
recurrent peptic ulcer of the stomach and duodenum;
hemophilia and other blood clotting disorders;
severe hepatic / renal failure;
childhood;
pregnancy and lactation;
individual intolerance to the components of Artrum.

Relative contraindications for which Artrum is prescribed under medical supervision: bronchial asthma, blood diseases (including leukopenia), anemia, arterial hypertension, chronic heart failure, coronary heart disease, tobacco smoking, alcoholism, alcoholic liver cirrhosis, hepatic / renal failure, hyperbilirubinemia, stomatitis, dehydration, diabetes mellitus, sepsis, old age.

Gel for external use

Absolute:

violation of the integrity of the skin, weeping dermatoses, eczema;
bronchial asthma in combination with polyposis of the nasal mucosa;
age up to 6 years;
III trimester of pregnancy and breastfeeding period;
individual intolerance to the components of Artrum, as well as salicylates or other non-steroidal anti-inflammatory drugs.

Relative contraindications in which Artrum gel is prescribed under medical supervision: bronchial asthma, erosive and ulcerative lesions of the gastrointestinal tract, exacerbation of hepatic porphyria, chronic heart failure, severe liver and kidney dysfunction, age up to 12 years, old age, I and II trimester of pregnancy.

Artrum, instructions for use: method and dosage

Extended-release tablets

Artrum tablets are taken orally, with meals. The recommended dose is 1 tablet 2 times a day. The maximum daily dose is 300 mg.

Solution for intravenous and intramuscular administration

The recommended dose for intramuscular injection is 100 mg 1-2 times a day. Intravenous Artrum is administered only in a hospital setting. With a short intravenous infusion, ketoprofen is administered within 30-60 minutes, repeated administration is possible after 8 hours. With prolonged intravenous infusion, Artrum is administered within 8 hours, repeated administration is possible after 8 hours. The maximum daily dose is 200 mg.

To prepare a solution for short-term infusion, 1-2 ampoules (100-200 mg) of ketoprofen are diluted in 100 ml of isotonic sodium chloride solution. To prepare a solution for continuous infusion, 1-2 ampoules (100-200 mg) of ketoprofen are diluted in 500 ml of one of the infusion solutions (5% dextrose solution, isotonic sodium chloride solution or lactate-containing Ringer's solution).

Parenteral administration of Artrum can be combined with pills or rectal suppositories. The drug in the form of a solution is used for no more than 3 days. If further use of ketoprofen is necessary, the patient is transferred to other dosage forms of Artrum (tablets, suppositories, gel).

Rectal suppositories

Suppositories Artrum is injected deep into the rectum. The recommended dose is 1 suppository 2 times a day (morning and evening).

Gel for external use

Gel Artrum is used externally. A single dose is 3-5 g (corresponds to one large cherry in volume). The gel is applied to the damaged area 2-3 times a day and rubbed gently until completely absorbed. Without consulting a doctor, the duration of treatment should not exceed 10 days.

Side effects

digestive system: dyspeptic disorders (nausea, vomiting, heartburn, increased or decreased appetite, flatulence, constipation or diarrhea), NSAID gastropathy, dry mouth, taste changes, stomatitis, liver dysfunction, abdominal pain; with long-term treatment in high doses - ulceration of the mucous membrane of the gastrointestinal tract, exacerbation of Crohn's disease, perforation of the walls of the gastrointestinal tract, melena, various bleeding (gingival, hemorrhoidal, gastrointestinal);
cardiovascular system: peripheral edema, tachycardia, increased blood pressure;
hematopoietic system: leukopenia, anemia and hemolytic anemia;
central nervous system: fatigue, insomnia or drowsiness, dizziness, asthenia, nightmares, headache, depression, agitation, forgetfulness, nervousness, migraine, confusion or loss of consciousness, hallucinations, peripheral polyneuropathy, speech disorder, disorientation;
sense organs: change in taste, dryness of the mucous membrane of the eyes, conjunctival hyperemia, blurred vision, tinnitus, eye pain, vertigo, hearing loss;
urinary system: interstitial nephritis, urethritis, renal dysfunction, nephrotic syndrome, cystitis, hematuria;
laboratory parameters: decreased platelet aggregation, anemia, purpura, transient increase in the activity of liver enzymes, agranulocytosis, thrombocytopenia;
allergic reactions: itching, rash, shortness of breath, exfoliative dermatitis, anaphylactoid reactions, rhinitis, bronchospasm, angioedema;
other reactions: menometrorrhagia, myalgia, hemoptysis, thirst, nosebleeds, muscle twitching, photosensitivity, increased sweating; with long-term treatment in high doses - vaginal bleeding;
local reactions: when applying the gel - a rash on the skin and itching at the site of application; when using suppositories - painful bowel movements, irritation of the rectal mucosa.

Overdose

With the systemic use of Artrum (tablets of prolonged action, solution for intravenous and intramuscular administration), the main symptoms of an overdose are headache, melena, nausea, pain in the abdomen, vomiting (including with blood), respiratory depression, impaired consciousness, convulsions, renal failure, impaired renal function.

Therapy: gastric lavage and intake of activated carbon; symptomatic and supportive treatment. It is possible to weaken the effect of ketoprofen on the gastrointestinal tract with the help of agents that reduce the secretion of gastric glands (in particular, proton pump inhibitors) and prostaglandins. It is necessary to control the activity of the respiratory and cardiovascular systems. Hemodialysis is ineffective, the specific antidote is unknown.

The main symptoms of ketoprofen overdose with intrarectal administration of Artrum (suppositories) are drowsiness, nausea, vomiting, abdominal pain, bleeding, renal and liver dysfunction. To relieve the condition, symptomatic treatment is recommended.

Overdose cases of Artrum in the form of a gel for external use have not been registered.

special instructions

During treatment with the drug, it is necessary to systematically monitor the functions of the kidneys and liver.

With prolonged use of Artrum and other non-steroidal anti-inflammatory drugs, it is necessary to monitor blood counts, especially in elderly patients.

Patients with hypertension and cardiovascular disease leading to fluid retention require regular blood pressure monitoring.

Artrum can mask the symptoms of infectious diseases.

Influence on the ability to drive vehicles and complex mechanisms

Patients taking ketoprofen should be careful when driving and performing work that requires a quick reaction and increased concentration.

Application during pregnancy and lactation

Extended-release tablets, solution for intravenous and intramuscular administration, gel for external use:

III trimester of pregnancy and the period of breastfeeding: therapy is contraindicated;
I and II trimester of pregnancy: Artrum should be used under medical supervision only in cases where the expected benefit is higher than the possible risk to the fetus.

With inhibition of prostaglandin synthesis, an undesirable effect on the course of pregnancy and / or embryonic development is possible. There is information about an increase in the likelihood of spontaneous abortion and the formation of heart defects (~ 1-1.5%).

In the third trimester, the contraindication to the use of Artrum is associated with the possibility of developing the following conditions:

increased bleeding time;
weakness of labor activity of the uterus and / or premature closure of the ductus arteriosus;
renal failure and oligohydramnios.

There is no information on the release of ketoprofen into breast milk.

Rectal suppositories Artrum during pregnancy / lactation are not prescribed.

Pediatric use

prolonged-release tablets, solution for intravenous and intramuscular administration: contraindicated in patients under 15 years of age;
rectal suppositories: not used in pediatrics;
gel for external use: therapy is contraindicated for children under 6 years old, from 6 to 12 years old, Artrum should be used under medical supervision.

With impaired renal function

Extended-release tablets, solution for intravenous and intramuscular administration:

severe renal failure (in patients with creatinine clearance less than 30 ml / min): therapy is contraindicated;
chronic renal failure (in patients with creatinine clearance of 30-60 ml / min): apply Artrum under medical supervision.

Rectal suppositories:

severe renal failure: therapy is contraindicated;
renal failure: Artrum should be used under medical supervision.

Artrum gel for external use with severe renal dysfunction should be used with caution.

For violations of liver function

Extended-release tablets, solution for intravenous and intramuscular administration:

severe hepatic failure: therapy is contraindicated;
moderate and mild liver failure, alcoholic cirrhosis of the liver, hyperbilirubinemia: Artrum should be used under medical supervision.

Rectal suppositories:

severe hepatic failure: therapy is contraindicated;
liver failure, alcoholic cirrhosis of the liver, hyperbilirubinemia: Artrum should be used under medical supervision.

Artrum gel for external use in severe renal dysfunction, exacerbation of hepatic porphyria should be used with caution.

Use in the elderly

Artrum in all dosage forms in elderly patients should be used with caution.

Drug interactions

With the simultaneous use of Artrum with diuretics and antihypertensive drugs, their effect may be weakened, with oral hypoglycemic and some anticonvulsants, their effects may be enhanced.

When taken together with salicylates, ethanol, glucocorticosteroids and other non-steroidal anti-inflammatory drugs, the risk of developing complications from the gastrointestinal tract increases.

When taken simultaneously with thrombolytics, anticoagulants and antiplatelet agents, the likelihood of bleeding increases; with ACE inhibitors or diuretics - the risk of renal dysfunction increases; with mifepristone - a decrease in the effectiveness of mifepristone is possible (ketoprofen should be taken no earlier than 8-12 days after its cancellation); with cardiac glycosides, cyclosporine, methotrexate, lithium preparations and blockers of slow calcium channels - the plasma concentrations of these drugs increase.

Artrum is combined with central analgesics; the solution can be mixed in one vial with morphine, it is forbidden to mix with tramadol (precipitate falls).

Analogs

Arketal Rompharm, Artrozilen, OKI, Profenid, Ketoprofen, Oruvel, Flexen, Bystrumkaps, Flamax, Ketonal, etc. are analogues of Artrum.

Terms and conditions of storage

Store in a dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life: extended-release tablets, rectal suppositories and gel for external use - 2 years; solution for parenteral administration - 3 years.

Terms of dispensing from pharmacies

prolonged-release tablets, solution for parenteral administration, rectal suppositories - by prescription;
gel for external use - without a prescription.

Reviews about Artrum

Reviews about Artrum are mostly positive. In some cases, several dosage forms of the drug are used simultaneously for therapy. Most of the responses about the use of Artrum in the form of an external gel. Indicate that the action of the drug develops rapidly. Its analgesic properties are also noted. The cost is estimated in different ways - from acceptable to somewhat overestimated.

Price for Artrum in pharmacies

The approximate price for Artrum is: a solution of 50 mg / ml (10 ampoules of 2 ml) - 89 rubles, suppositories (10 pcs. 100 mg each) - 130 rubles, gel (1 tube of 30 g) - 83 rubles.

Artrum: prices in online pharmacies

Drug name

Price

Pharmacy

Artrum 2.5% gel for external use 50 g 1 pc.

113 RUB

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Artrum 100 mg rectal suppositories 10 pcs.

119 RUB

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Artrum rectal suppositories 100mg 10 pcs.

127 RUB

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Artrum 150 mg extended release tablets 20 pcs.

199 RUB

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Artrum 5% gel for external use 50 g 1 pc.

232 RUB

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!