Ketonal: instruction on the use of tablets, injections, capsules

Ketonal nyxes: instructions for use

Ketonal has a pronounced anti-inflammatory, analgesic and antipyretic effect.

It refers to NSAIDs, is a non-hormonal non-narcotic drug and is able to cure pain of both medium and high intensity.

The medication helps to relieve the condition with radiculitis, neuralgia, arthritis, with trauma and many other pathological conditions.

Composition and form of Ketonal

The active substance of the drug is ketoprofen and depending on the form of release of the drug, it is present in it at a certain dosage.

There are also capsules Ketonal Duo and Uno, the active substance content of which is 150 and 200 mg respectively.

Most forms of the drug are intended to be taken or administered orally, since this option provides the most effective therapeutic effect.

Pharmacological action of the agent

Three therapeutic effects, which give injections Ketonal, is anesthesia, reduction of inflammation and removal of fever. The last action is not as pronounced as the first two.

At the molecular level, the analgesic effect of the agent is explained in this way - ketoprofen blocks activity of enzymes involved in the synthesis of the main provocators of pain and inflammation - prostaglandins.

A special feature of Ketonal is its wide spectrum of action. In connection with this, it is used to relieve the pain syndrome of different origin and localization.

With arthritis, the drug stops pain and helps to reduce swelling and stiffness that occur in the affected areas in the morning.

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Indications for use Ketonal

All dosage forms of the agent in question, with the exception of the external agents (cream and gel), contain practically identical lists of diseases in which instructions are indicated for their use. However, this or that form is prescribed for reasons of convenience of use and the nature of the symptomatology.

Musculoskeletal system

In the first place, injections and other forms of Ketonal for ingestion or ingestion are indicated when degenerative and inflammatory diseases of joints and other elements musculoskeletal system:

Pain of another etiology

Secondly, Ketonal injections are prescribed for relief of pains of different localization and etiology.

These can be headaches, bursitis and tendonitis, renal colic and painful periods, myalgia and neuralgia, lumbago, trauma and condition after surgery, phlebitis and many others pathology.

How to apply injections?

A solution for intravenous or intramuscular administration is indicated if it is necessary to quickly and effectively relieve pain, and also if, for some reason, ingestion is not possible.

Injectable form can be combined with oral (tablets, capsules) and rectal (suppository) forms of the drug. The duration of application of injections and all other forms of Ketonal is determined by the rate at which the pain syndrome is eliminated.

And the maximum allowed daily dose of the drug is established, regardless of the form of release - it is 200 mg.

Each ampoule contains 2 ml of an injection solution containing 100 mg of ketoprofen. Intravenous administration is prescribed 1-2 times a day for 1 ampoule (100 mg each).

The injections are placed where the muscles are located close to the skin (the upper arm or thigh).

In the buttock, injections are not recommended, since a layer of subcutaneous fat can interfere with the full penetration of the drug into the muscles and reduce efficiency.

You will be interested to read: Side effects: aspirin

Ketonal injections intramuscularly with the possession of technology can be done at home. Intravenous fluids of the solution are produced exclusively in a hospital by a medical professional.

The attending physician may prescribe short or long droppers. In the first case, 1-2 ampoules of the preparation (100-200 mg of ketoprofen) are taken per 100 ml of physiological solution and injected for 30-90 minutes.

In the second case, a similar volume of Ketonal is dissolved in 500 ml of physiological saline and placed on a dropper for 8 hours.

Between the procedures for intravenous administration of the drug, regardless of the duration, it must take at least eight hours.

Features and Precautions

Pregnant and lactating women

In the first and second trimester Ketonal is prescribed exclusively in cases where the benefit to the mother exceeds the risk for the child.

The third trimester suggests a complete ban of this drug, since ketoprofen can cause late and complicated births.

If Ketonal is needed during breastfeeding, the baby is transferred to artificial mixtures.

Mechanism management

Directly, ketoprofen does not affect the ability to control complex mechanisms or devices that require attention and reaction speed. But to apply it in such cases is still not recommended, because the list of side effects of the drug there are violations from the nervous system.

Interaction with other drugs

Injections and other forms of Ketonal reduce the effectiveness of Mifepristone, diuretics and drugs to reduce blood pressure, but enhances the effect of hypoglycemic medications (to reduce the level of sugar in blood).

In combination with other NSAIDs (Diclofenac, Aspirin, Ketorol, etc.), alcohol and glucocorticosteroids can provoke gastrointestinal bleeding.

Impaired renal function is possible with simultaneous administration of Ketonal with diuretics and ACE inhibitors (Enalapril, Captopril, etc.).

When a ketonal is combined with cardiac glycosides, methotrexate, lithium preparations or calcium channel blockers, the concentration of the listed agents in the blood increases.

Important instructions

Contraindications

Ketonal injections, like other forms, are contraindicated in the case of an allergy to aspirin and other NSAIDs. It could be like an allergic rhinitis and urticaria, and asthma. It is also unacceptable to apply the drug under such conditions as:

• a stomach ulcer or 12 duodenal ulcer in an acute stage;
• hemophilia and other problems with blood coagulability;
• acute phase of inflammatory bowel disease;
• renal pathology, hepatic and renal insufficiency;
• coronary artery bypass grafting done less than 2 months ago;
• the presence of a different kind of bleeding and a tendency to them;
• digestive problems;
• heart failure;
• 28-40 weeks of pregnancy;
• the period of breastfeeding;
• children under 15;
• individual intolerance of components.

Analogues of Ketonal

In addition to the Ketonal drug, there are other medicines containing ketoprofen as an active ingredient. Here are some examples of such drugs:

• Arketal Rompharm;
• Fleksen;
• Artrum;
• Arthrosylen;
• Bystrumcaps;
• Flamax;
• Ketoprofen;
• Flamax forte

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Ketonal nyxes: instructions for use

Non-steroidal anti-inflammatory drugs for injection.

Form of preparation, its composition and packaging

Ketonal is available in the form of a solution for injection in ampoules. The solution is characterized by transparency, a slight yellowish tinge.

Used for intramuscular and intravenous injections. At visual inspection the solution should not have a sediment or mechanical inclusions.

Otherwise, it can not be used for administration to the body.

1 ampoule solution Ketonal contains 50 or 100 mg of ketoprofen, as well as additional substances: ethyl alcohol, propylene glycol, benzyl alcohol, water for injection. Ampoules of 2 ml in an amount of 5 pieces are enclosed in blisters. Blisters for 1 or 2 pieces are enclosed in cardboard packs with the corresponding marking.

Mechanism of action

Ketoprofen is an anti-inflammatory agent of a non-steroidal nature. It has analgesic, anti-inflammatory effects, reduces body temperature.

The action is due to inhibition of cyclooxygenase type 1 and type 2.

Because of this, the production of prostaglandins is inhibited, which disrupts the development of the inflammatory reaction.

With the use of high concentrations of the drug, the production of leukotriene and bradykinin is also inhibited.

Ketonal has no deleterious effect on the state of the cartilaginous tissue.

Pharmacokinetics

Ketonal injections have a high bioavailability - about 90%. The maximum concentration is fixed in the blood 15-30 minutes after parenteral administration.

Ketoprofen has a high affinity with plasma proteins and binds to them by 99%. Well enters the synovial fluid (about 50% of the total blood).

The drug undergoes intensive metabolic processes in the liver under the influence of a system of microsomal enzymes. In the process of metabolism, inactive metabolites are formed. The half-life is 120 minutes. Excretion occurs through the kidneys in the form of glucuronide.

With liver dysfunction, the concentration of the drug increases because of the slowing of metabolism. Therefore, this category of patients should use the most minimal dosage of the drug.

With renal failure, the elimination of ketoprofen decreases, but dose adjustment is necessary only in the severe form of renal dysfunction.

For elderly patients, the slowing of metabolism and elimination of the drug is characteristic, but only those with concomitant renal insufficiency in the anamnesis have clinical significance.

To whom and when is recommended to apply nyxes Ketonal

Ketonal in pricks is prescribed for the following diagnoses:

• inflammatory processes of various origin
• diseases of bones and joints of an inflammatory and degenerative nature
• arthritis of various nature and nature
• gout
• osteoarthritis
• pain in muscles and joints of weak and moderate character
• pain in the head, including migraine
• inflammation of the muscles and nerves
• pain after trauma or surgery
• pain in cancer
• inflammation and pain associated with dysfunction of the pelvic organs in women.

Who and when is not recommended to apply nyxes Ketonal

Do not apply Ketonal nyxes if the patient has:

• reaction to other drugs from the NSAID group in the form of bronchial asthma, urticaria, or rhinitis
• stomach ulcer or gastritis
• ulcerative colitis, Crohn's disease
• reduced blood clotting ability, hemophilia
• hepatic dysfunction
• chronic severe kidney disease, organ failure
• heart failure of non-compensatory type
• period after aortic bypass surgery
• bleeding from the gastrointestinal tract or others
• chronic dyspeptic phenomena
• age less than 15 years
• lactation period
• pregnancy in the third trimester
• individual intolerance of the ingredients of the drug.

Care should be taken with concomitant asthma and stomach ulcer, heart and vascular disease, liver and / or kidney dysfunction, problems with functioning of the gastrointestinal tract, violations of blood coagulability, abuse of alcoholic beverages and smoking, with intolerance to aspirin, with sugar diabetes.

How to apply

Ketonal is used for intramuscular and intravenous administration.

Intramuscularly administered for 100 mg with a frequency of 1-2 times a day.

Intravenous infusion of the drug only in hospital settings. 1-2 ampoules of the drug are diluted with a physiological solution of 100 ml. The resulting solution is introduced for 30-60 minutes. After 8 hours, the intravenous injection can be repeated.

Also there is a variant of a longer administration of the drug. just 1-2 Ketonal ampules are diluted in 500 ml of a solution of sodium chloride or Ringer and injected intravenously for 8 hours. Repetition of the injection is possible 8 hours after the end of the previous administration.

In addition to injectable administration, the use of Ketonal Tablets or Capsules can be used in combination, and the rectal form of the drug can also be used. Maximum of a day can be consumed up to 200 mg of ketoprofen.

Symptoms of an overdose of Ketonal

With the introduction of excessive doses of the drug, the following symptoms are observed: dyspepsia, vomiting with a blood admixture, gastralgia, respiratory center depression, convulsive attacks, liver and / or kidney dysfunction.

Therapy: gastric lavage and the intake of sorbent drugs. If necessary, treat according to the symptoms observed.

If the negative impact on the gastrointestinal tract is expressed, drugs from the proton pump inhibitor group should be taken.

With severe disruption of the kidneys, hemodialysis should be performed.

Interaction of Ketonal with other drugs

Ketonal reduces the effectiveness of diuretics and antihypertensive drugs.

Ketonal induces effects of hypoglycemic agents for oral administration and some agents from the group of anticonvulsants.

Parallel reception of ketoprofen together with other anti-inflammatory drugs, glucocorticosteroids, ethyl alcohol leads to an increase in the risk of lesions of the gastrointestinal tract.

Drugs affecting blood clotting - anticoagulants, antiaggregants, thrombolytics when taken together with Ketonalom lead to the development of bleeding.

It is possible to increase the potassium content in the blood with parallel intake of ketoprofen with ACE inhibitors, other NSAIDs, heparin, trimethoprim.

Ketonal increases the content of CH, antagonists of calcium channels, methotrexate.

When combined with methotrexate and cicosporin, the toxicity of these medicines is significantly increased.

Ketonal injection during pregnancy and lactation

The conducted studies showed that the use of the NSAID group during the gestation period increases the risk spontaneous abortion, there is a detrimental effect on the embryonic development of the child with the possible formation of vices heart.

Use of the drug in the first and second trimester of pregnancy is allowed only when assessing the benefit to the mother / risk to the fetus.

The use of Ketonal nyxes during the third trimester is contraindicated due to a decrease in labor activity, the development of renal dysfunction.

There is no data on the possible penetration of ketoprofen into breast milk. Therefore, when prescribing this drug during lactation, the issue of stopping breastfeeding of the baby should be resolved.

Side effects

From the hematopoiesis: a decrease in the level of leukocytes, platelets, anemia of the hemorrhagic type, a violation of the functioning of the bone marrow.

From the side of immunity: anaphylaxis.

From the side of the central nervous system: pain in the head, sleep disturbance, decreased sensitivity, convulsions, violation of taste buds.

From the viewpoint: reduced visual acuity.

From the side of hearing: noises.

From the heart and blood vessels: heart failure, increased blood pressure, widening of peripheral vessels.

From the sides of the stomach and intestines: indigestion, pain, frustration or constipation, flatulence, inflammation of the mucosa stomach, deterioration of the pi state of Crohn's disease, bleeding from the intestine, perforation of the intestinal wall or stomach.

From the hepato-biliary system: inflammation of the liver, increase in the content of enzymes.

From the skin: rashes, itching, swelling, baldness, redness, necrolysis.

From the kidneys: organ dysfunction, inflammatory process.

Others: fatigue, puffiness, weight gain.

How to store

Ketonal should be stored at a temperature of no higher than 250 C, no more than 3 years from the date of production. Keep away from children.

Conditions of leave from pharmacies

Ketonal refers to the list of prescription drugs, for its purchase in the pharmacy you need to provide a prescription for a doctor.

special instructions

With prolonged use of the drug for treatment, it is necessary to periodically monitor liver and kidney function parameters, analyze the blood picture, and perform a fecal occult blood test.

In the presence of cardiovascular diseases, patients taking ketoprofen should more often measure blood pressure and be cautious.

If against the background of taking the medication a deterioration in vision should be immediately abolished the use of Ketonal.

Ketonal may mask the signs of the inflammatory process in the body associated with infection. Therefore, if there are symptoms of infection and worsening of the patient's condition, it is necessary to urgently consult a doctor.

Patients taking high doses of the drug should be carefully monitored for a long time if they have problems with the gastrointestinal tract.

The drug can reduce the ability of women to conceive, therefore, should not be used to treat women with infertility.

The ability to drive vehicles after taking Ketonal depends on the individual tolerability of the drug.

Visual disturbances, it is necessary to refrain from driving and performing other works associated with increased attention and reaction.

The drug can be used for elderly patients, keeping the kidneys and liver functioning under control.

Children should not use ketonal injections. The minimum age for the use of the drug is 15 years.

Analogues of injections Ketonal

To preparations with a similar composition, which can replace injections Ketonal include: Flamax, Oki, Arthrosilen, Artrum.

Ketonal in ampoules price

The average cost of Ketonal drug in ampoules in pharmacies in Moscow is

A source: http://bezboleznej.ru/ketonal-ukoly

Ketonal - instruction, application, purpose

Ketonal is a non-steroidal anti-inflammatory drug used in symptomatic therapy diseases of the musculoskeletal system, as well as to eliminate the pain syndrome of various origin.

Pharmacological action of Ketonal

Ketonal has anti-inflammatory, analgesic and antipyretic properties.

The action of ketoprofen, the active substance Ketonal, is due to the ability of the drug to raise the pain threshold by suppressing the synthesis of bradykinin, stabilize the lysosomal membranes and delay the release of enzymes from them, which in chronic inflammation contribute to the destruction tissues.

The maximum concentration of ketoprofen in the blood can be observed after, -2 hours after application Ketonal tablets, 65-80 minutes after the application of rectal suppositories and after 5 minutes with intravenous administered.

About 90% of Ketonal is excreted by the liver, the half-life is about 2 hours. The delayed excretion of Ketonal in renal failure requires dose adjustment for patients with such a disease.

Indications for use

Appointment Ketonal recommends the instruction for such degenerative and inflammatory diseases of the musculoskeletal system as:

• psoriatic arthritis (inflammation of the joints during psoriasis);
• rheumatoid arthritis (inflammatory-destructive lesion of large and small joints of limbs);
• Bechterew's disease (persistent limitation of spinal mobility with possible involvement of internal organs in the inflammatory process);
• osteoarthritis (joint disease, provoked by the defeat of their cartilaginous tissue);
• gouty arthritis (joint disease caused by the deposition of uric acid salts in various tissues).

The use of Ketonal is also advisable when:

• pain in the muscles;
• Neuralgia (defeat of peripheral nerves, accompanied by attacks of pain);
• ossaly (pain as a result of damage to bone tissue);
• pain in the joints;
• tendonitis (inflammation around or inside the tendon);
• radiculitis (lesion of bundles of nerve fibers leaving the spinal cord);
• bursitis (inflammation of the articular bags);
• adnexitis (inflammation of the uterine appendages);
• dental and headaches.

Ketonal is used as an analgesic for posttraumatic and postoperative pain syndrome, accompanied by inflammation, cancer, algodismorrhoea (painful menstruation), childbirth.

Instructions for use Ketonal

Ketonal is available in forms intended for oral administration: capsules, tablets, granules for the preparation of a suspension.

For intramuscular injections Ketonal is used as a solution or lyophilizate for solution preparation. Only the solution is administered by the intravenous route. For external use Ketonal is available in the form of gel, cream, spray and solution. Candles Ketonal are intended for rectal use.

Take Ketonal Capsules Instruction recommends three times a day for 1 pc. (50 mg), not exceeding the daily dose of 300 mg. With osteoarthritis and rheumatoid arthritis, 50 mg of the drug is taken four times a day.

To drink Ketonal follows a sufficient amount of milk or water, take the drug is recommended during meals. Capsules Ketonal Duo, containing 150 mg of ketoprofen, usually take 1 pc.

Tablets Ketonal appoint usually 1-2 times a day for 1 pc. (150 mg), not exceeding the daily dose of 300 mg.

Duration of treatment - two weeks, if necessary, the duration of the drug can be increased by a doctor.

Tablets Ketonal should be taken during or immediately after meals, with plenty of water.

Candles Ketonal, the use of which can be combined with the use of tablets or capsules, is usually prescribed for 1 pc. (100 mg) in the morning and evening.

Intramuscular ketonal injections are routinely prescribed 1-3 times a day for 1 ampoule (100 mg). Intravenously, ketonal injections should be done only in a hospital setting.

With intermittent administration of 1-2 ampoules of the drug dilute 100 ml of "saline solution" and injected for half an hour-hour.

With continuous administration, the same amount of Ketonal is diluted in 500 ml of "saline" or glucose and injected for 8 hours. Repeated intravenous ketonal injections are administered after 8 hours.

Gel and Ketonal cream are for external topical application.

Ketonal cream should be applied to the affected areas 2 times a day, and the gel - 1 or 2 times. An occlusive dressing is not recommended. The maximum daily dose is 200 mg (10 cm Ketonal cream). The duration of treatment is 7-10 days.

Side effects

According to the instructions, Ketonal may be the cause of the following undesirable phenomena:

• abdominal pain, stool disorders, vomiting, nausea, dry mouth, stomatitis, impaired liver function, gastrointestinal bleeding;
• nervousness, fatigue, headache, migraine, sleep disturbance, dizziness, speech disorder;
• change in taste, tinnitus, conjunctivitis, blurred vision, pain in the eyes;
• Arterial hypertension, tachycardia, peripheral edema;
• anemia, agranulocytosis, thrombocytopenia;
• nephrotic syndrome, impaired renal function, the presence of blood in the urine in excess of the norm;
• allergic reactions to the skin, dyspnea, bronchospasm, rhinitis, angioedema.

Ketonal cream and gel can provoke vascular edema, hives, skin rashes, skin necrosis, dermatitis.

Contraindications to the use of Ketonal

The use of Ketonal is prohibited with hypersensitivity, "aspirin" asthma, peptic ulcer, ulcerative colitis, peptic ulcer, diverticulitis (protrusion intestinal wall), Crohn's disease (inflammation of the digestive tract, which can affect all of its departments), blood clotting disorders, chronic illness kidney.

According to the instructions, Ketonal is contraindicated in children under 14 years of age, pregnant and breast feeding women.

With care Ketonal is prescribed for patients suffering from bronchial asthma, anemia, alcoholism, alcoholic cirrhosis liver, liver failure, sepsis, diabetes, arterial hypertension, edema, stomatitis, diseases blood. The use of Ketonal by elderly patients should occur according to the intended use and under the supervision of the physician.

Additional Information

Ketonal should be stored in a dark, dry place where the air temperature does not exceed 250C.

A source: http://www.neboleem.net/ketonal.php

Instructions for injections Ketonal

Ketonal is a potent and effective drug that is widely used in medical practice. Ketonal is produced in the form of capsules, tablets, suppositories, cream and liquid for injections.

Pharmacological action of Ketonal

The active substance Ketonal is ketoprofen, which has anti-inflammatory, antipyretic and analgesic effect. The maximum concentration of the drug in the blood is reached after 65-80 minutes with rectal administration, and for 5 minutes with intravenous administration.

The half-life of Ketonal is approximately 2 hours. 90% of the drug is excreted by the liver. With renal failure, the elimination process slows down by 1 hour, which requires appropriate dose adjustment of Ketonal.

Indications for use Ketonal

Ketonal preparation in the form of injections is recommended for such inflammatory and degenerative diseases of the musculoskeletal system as:

• Rheumatoid arthritis (involvement of large and small joints of inflammatory-destructive extremities);
• osteoarthrosis (joint disease due to damage to the cartilaginous tissue);
• psoriatic arthritis (inflammation of the joints caused by psoriasis);
• gouty arthritis (joint disease, which is caused by the deposition of uric acid salts in various tissues);
• Bechterew's disease (limitation of spine mobility, caused by inflammation of the intervertebral joints and their adhesion).

Ketonal is also prescribed for such diseases as:

• neuralgia (defeat of the peripheral nervous system, which is accompanied by bouts of pain);
• muscle pain;
• tendonitis (inflammation inside or around the tendons);
• joint pain;
• ossalgia (pain caused by damage to bone tissue);
• bursitis (inflammation of the articular bags);
• radiculitis (inflammation of the nerve roots that enter the intervertebral foramen);
• andexitis (inflammation of the uterine appendages);
• severe toothache.

As an analgesic Ketonal is used in postoperative pain syndrome with the presence of the inflammatory process, oncological diseases, painful menstruation and childbirth.

Method of application Ketonal

Ketonal in injections is prescribed for 1 ampoule (, g) 3 times a day by pricking into the muscle. Intravenously the drug is used only in a hospital. In this case, the drug is administered in two ways:

• Intermittent. The contents of 1-2 ampoules of Ketonal (100-200 mg) are diluted in 100 ml of physiological solution and injected for 30-60 minutes. After 8 hours the procedure is repeated;
• Continuous. The contents of 1-2 ampoules of the drug (100-200 mg) are diluted in 500 ml of glucose solution or physiological solution and injected for 8 hours. The procedure is repeated after 8 hours.

If necessary (severe pain), Ketanol is combined with narcotic analgesics. With morphine Ketanol can be mixed in one container, and with tramadol, the drug must be administered separately in order to avoid the formation of sediment.

Side effects and contraindications to the use of Ketonal

Side effects of the drug are rare, and in the case of occurring are rapid. Most often there is nausea, stool, headache and dizziness. Less common side effects in the form of suppression of hemopoiesis, which leads to anemia.

Perhaps the development of depression, insomnia, confusion, asthenia, bronchospasm and bronchial asthma, drug nephritis, visual impairment, tinnitus, liver dysfunction, sometimes uterine bleeding. In elderly patients, there may be complications in the form of peptic ulcers.

Contraindications to the use of Ketonal are:

• intolerance to any components of the drug;
• peptic ulcer of the stomach and duodenum;
• renal and hepatic impairment;
• asthma attacks.

The drug Ketonal in most cases does not affect the ability to manage complex mechanisms or vehicles. In those cases when there is drowsiness and dizziness, it is better to give up actions that require a high rate of psychic reactions.

Overdose of the drug can cause disruption of the gastrointestinal tract and kidney function.

Use of Ketonal in injections should be done under the supervision of a doctor. This manual is an introductory and not a material for the practical use of the drug.

A source: http://MoreHealthy.ru/material/instruktsiya-ukolov-ketonal-392.html

Ketonal for injection - official instructions for use, analogues

Symptomatic treatment of osteoarthritis, rheumatoid arthritis, Bechterew's disease and other inflammatory and degenerative diseases accompanied by pain syndrome. Anomalies, articles

Instructions
on the use of medicinal product for medical use

• Keep this manual for future reference.
• If you have any questions, contact your doctor.

Registration number:

П N013942 / 01

Trade name of the preparation:

Ketonal®.

International Nonproprietary Name:

solution for intravenous and intramuscular administration.

1 ampoule contains:
active substance: ketoprofen - 100 mg;
auxiliary substances: propylene glycol 800 mg; ethanol 200 mg; benzyl alcohol - 40 mg; water for injection - up to 2 ml.

Description:

Transparent, colorless or slightly yellowish solution.

Pharmacotherapeutic group:

Non-steroidal anti-inflammatory drug (NSAID).

ATX Code: МО1АЕ03 - ketoprofen.

Pharmacological properties

Pharmacodynamics Ketoprofen is a non-steroidal anti-inflammatory drug. Ketoprofen has an anti-inflammatory, analgesic and antipyretic effect.

Ketoprofen blocks the action of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2) and, in part, lipoxygenase, which leads to the suppression of the synthesis of prostaglandins (including in the central nervous system, most likely in hypothalamus).

Stabilizes in vitro and in vivo liposomal membranes, at high concentrations in vitro ketoprofen inhibits the synthesis of bradykinin and leukotrienes.

Ketoprofen does not adversely affect the condition of the articular cartilage.

Pharmacokinetics

Suction

With intravenous administration of ketoprofen, the mean plasma concentration after 5 minutes from the start of infusion and up to 4 minutes after its termination is 2, ±, μg / ml. Bioavailability is 90%.

With a single intramuscular injection of 100 mg of ketoprofen, the drug is detected in the blood plasma 15 minutes after the start of the infusion, and the peak concentration (, μg / ml) is reached after 2 hours. Bioavailability of the drug increases linearly with increasing dose.

Distribution Ketoprofen by 99% is associated with blood plasma proteins, mainly with albumin fraction. The volume of distribution in the tissues is, l / kg.

Ketoprofen penetrates into the synovial fluid, and with intravenous administration of 100 mg after 3 hours its concentration reaches, μg / ml, which is 50% of the concentration in the blood plasma (about 3 μg / ml).

After 9 hours, the concentration in the synovial fluid is, μg / ml, and in the blood plasma μg / ml, which means that ketoprofen slowly penetrates into the synovial fluid and is slowly withdrawn from it.

Stationary plasma concentrations of ketoprofen are determined even after 24 hours after its administration.

After a single intramuscular injection of 100 mg of ketoprofen, the drug is detected in the cerebrospinal fluid, like blood serum, after 15 minutes.
Metabolism Ketoprofen undergoes intensive metabolism involving microsomal liver enzymes. It binds to glucuronic acid and is excreted from the body in the form of glucuronide. There are no active metabolites of ketoprofen.

Excretion

The half-life (T1 / 2) of ketoprofen is 2 hours.

In patients with renal insufficiency, ketoprofen is excreted more slowly, its T1 / 2 increases by 1 h.

In patients with hepatic insufficiency, T1 / 2 increases, so it is possible to accumulate ketoprofen in tissues.
In elderly patients, the metabolism and excretion of ketoprofen is slower, which is of clinical importance only for patients with severe renal insufficiency.

Indications for use

Symptomatic therapy of pain syndrome, incl.

inflammatory processes of various origin:

1. rheumatoid arthritis;
2. seronegative arthritis:
3. ankylosing spondylitis (Bechterew's disease), psoriatic arthritis, reactive arthritis (Reiter's syndrome);
4. gout, pseudogout;
5. degenerative diseases of the musculoskeletal system, incl. osteoarthritis;
6. mild, moderate and severe pain syndrome with headache, migraine, tendinitis, bursitis, myalgia, neuralgia, radiculitis;
7. Post-traumatic and post-operative pain syndrome, including Accompanied by inflammation and fever;
8. pain syndrome in cancer;
9. algodismenorea.

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

• • hypersensitivity to ketoprofen or other components of the drug, as well as salicylates or other non-steroidal anti-inflammatory drugs (NSAIDs);
• • complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to acetylsalicylic acid or other NSAIDs (incl. in the anamnesis);
• • Stomach ulcer or duodenal ulcer in the stage of exacerbation;
• • Ulcerative colitis, Crohn's disease;
• • hemophilia and other bleeding disorders;
• • Children's age (up to 15 years);
• • severe hepatic impairment;
• • severe renal failure: severe renal failure (creatinine clearance less than 30 mL / min), confirmed hyperkalemia, progressive kidney disease;
• • Decompensated heart failure;
• • Postoperative period after coronary artery bypass grafting;
• • gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
• • chronic dyspepsia;
• • III trimester of pregnancy;
• • the period of breastfeeding.

Carefully

• history of peptic ulcer disease, presence of Helicobacter pylori infection; • history of bronchial asthma;

• • clinically expressed cardiovascular, cerebrovascular diseases and diseases of peripheral arteries;
• • dyslipidemia, liver failure, hyperbilirubinemia, alcoholic liver cirrhosis;
• • chronic renal failure (CK 30-60 ml / min);
• • chronic heart failure, arterial hypertension, blood diseases;
• • Dehydration, diabetes mellitus;
• • Smoking;
• • elderly age;
• • long-term use of NSAIDs, simultaneous administration of anticoagulants (including warfarin), antiaggregants (including clopidogrel), oral glucocorticosteroids (incl. prednisolone), selective serotonin reuptake inhibitors (including fluoxetine, paroxetine, citalopram, sertraline) (see the section "Interaction with other medicinal means ").

Application in pregnancy and during breastfeeding

Inhibition of prostaglandin synthesis may have an adverse effect on the course of pregnancy and / or on embryonic development.

Data from epidemiological studies using early-stage inhibitors of prostaglandin synthesis pregnancy, confirm the increased risk of spontaneous abortion and the formation of heart defects (up to,%) and birth defects in the anterior of the abdominal wall.

The risk increases with increasing dose and duration of treatment. Prescribe the drug to pregnant women in the I and II trimesters of pregnancy is possible only if the benefits for the mother justify the possible risk to the fetus. In this case, the minimum effective dose should be applied as short as possible.

Contraindicated in the use of ketoprofen in pregnant women during the third trimester of pregnancy because of the possible development of weakness of the uterine labor, increased bleeding time, antiaggregant effect (even when taken in small doses), as well as effects on the fetus (cardiopulmonary toxicity, incl. premature closure of the arterial duct and pulmonary hypertension, renal dysfunction that can progress to renal failure with development lack of water).

To date, there is no data on the isolation of ketoprofen in breast milk, so when the need to prescribe ketoprofen to the nursing mother, the question of stopping the breast feeding.

Intravenous, intramuscular. To reduce the incidence of adverse reactions, it is recommended to use the minimum effective dose of the drug.

The maximum daily dose is 200 mg.

It is necessary to carefully evaluate the ratio of expected benefit and risk to the initiation of ketoprofen administration at a dose of 200 mg / day.

Intramuscular injection: 100 mg (1 ampoule) 1-2 times a day.

Intravenous infusion of ketoprofen should only be performed in a hospital setting. The duration of the infusion should be from, to 1 h.

Intravenous route of administration should be applied no more than 48 hours.

A short intravenous infusion: from 100 (to 200) mg (1-2 ampoules) of ketoprofen diluted in 100 ml,% solution of sodium chloride, is introduced for 1 hour.

Continuous intravenous infusion: from 100 (to 200) mg (1-2 ampoules) of ketoprofen diluted in 500 ml of infusion solution (,% solution sodium chloride, lactate-containing Ringer's solution, 5% dextrose solution), administered within 8 hours; can be re-introduced after 8 hours. The maximum daily dose is 200 mg.

Ketoprofen can be combined with analgesics of central action; it can be mixed with opioids (eg, morphine) in a single vial, is pharmaceutically incompatible with tramadol solution due to prolapse draft.

Parenteral administration of Ketonal® can be combined with the use of oral forms (tablets, capsules) or rectal suppositories.

A source: https://medi.ru/instrukciya/ketonal-dlya-inektsij_5418/