Ketonal film-coated tablets 100 mg 20 pcs. in Moscow

Ketonal film-coated tablets 100 mg 20 pcs. in Moscow

Ketoprofen should not be combined with other NSAIDs and/or COX2 inhibitors.

With long-term use of NSAIDs, it is necessary to periodically evaluate a clinical blood test, monitor kidney and liver function, especially in elderly patients (over 65 years), and conduct a stool test for occult blood.

It is necessary to be careful and monitor blood pressure more often when using ketoprofen to treat patients suffering from arterial hypertension and cardiovascular diseases that lead to fluid retention in the body.

If visual disturbances occur, treatment should be stopped immediately.

Like other NSAIDs, ketoprofen can mask the symptoms of infectious and inflammatory diseases. If you notice signs of infection or deterioration in health while using the drug, you should immediately consult a doctor.

If there is a history of contraindications from the gastrointestinal tract (bleeding, perforation, peptic ulcer), long-term therapy and the use of high doses of ketoprofen, the patient should be under close medical supervision.

Because of the important role of prostaglandins in maintaining renal blood flow, particular caution should be exercised when using ketoprofen in patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics and patients who, for any reason, have a decrease in circulating volume. blood.

The drug should be discontinued before major surgery.

The use of ketoprofen can affect female fertility, therefore, patients with infertility (including those undergoing examination) are not recommended to use the drug.

Impact on the ability to drive vehicles and machinery

There is no data on the negative effect of the drug Ketonal® in recommended doses on the ability to drive a car or operate machinery. At the same time, patients who experience drowsiness, dizziness or other unpleasant sensations from the nervous system, including visual impairment, while using the drug, should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Ketonal 150mg n20 tablets extended release

Latin name

Ketonal

Release form

Long-acting tablets.

Package

20 tablets of 150 mg.

pharmachologic effect

Ketonal is an NSAID, a derivative of propionic acid.

It has analgesic, anti-inflammatory and antipyretic effects.

The mechanism of action is associated with inhibition of prostaglandin synthesis at the level of cyclooxygenase.

In addition, ketoprofen inhibits lipoxygenase, has antibradykinin activity, stabilizes lysosomal membranes, and causes significant inhibition of neutrophil activity in patients with rheumatoid arthritis.

The pronounced analgesic effect of ketoprofen is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).

Indications

Symptomatic treatment of painful inflammatory processes of various origins (including postoperative and post-traumatic pain, sciatica, myalgia, radiculitis, bruises and muscle strains, rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, acute attack of gout, tenosynovitis, bursitis).

Contraindications

— gastrointestinal diseases in the acute phase;

- severe liver dysfunction;

- severe renal dysfunction;

- blood disorders (leukopenia, thrombocytopenia, blood coagulation system disorders); I

- children under 15 years of age;

- hemorrhoids and proctitis (for suppositories);

- hypersensitivity to ketoprofen, acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria and rhinitis caused by taking acetylsalicylic acid).

Use during pregnancy and breastfeeding

The use of Ketonal in the third trimester of pregnancy is contraindicated.

The use of Ketonal in the first and second trimesters of pregnancy is possible only when the potential benefit to the mother outweighs the risk to the fetus.

If it is necessary to use Ketonal during lactation, the issue of stopping breastfeeding should be decided.

special instructions

With long-term use of Ketonal, like other NSAIDs, regular monitoring of hematological parameters, liver and kidney function parameters is required, especially in elderly patients.

Ketoprofen should be prescribed with caution to patients with arterial hypertension and heart disease accompanied by fluid retention in the body; blood pressure monitoring is recommended.

Ketonal can mask the symptoms of infectious diseases.

Due to the photosensitivity of the drug, bottles with infusion solution should be wrapped in dark paper or foil.

There is no data on the negative effect of Ketonal in recommended doses on the ability to drive a car or operate machinery. However, when using the drug, caution should be exercised by persons whose activities require rapid psychomotor reactions (driving a car, working with machinery).

Compound

1 tablet contains:

Active substance: ketoprofen - 150 mg.

Excipients: magnesium stearate, colloidal silicon dioxide, povidone, microcrystalline cellulose, hypromellose.

Directions for use and doses

Adults: the drug is prescribed 1-2 caps. 2-3 times/day, or 1 tablet. 2 times/day, or 1 tablet. prolonged action 1 time/day.

Capsules and tablets should be taken during or immediately after meals, without chewing, with a sufficient amount of water or milk (liquid volume - at least 100 ml).

Oral forms can be combined with the use of rectal suppositories or dosage forms of Ketonal for external use (cream, gel).

The maximum daily dose (including when using various dosage forms) is 200 mg.

Side effects

Allergic reactions:

common - skin reactions (itching, urticaria); uncommon - rhinitis, shortness of breath, bronchospasm, angioedema, anaphylactoid reactions.

Digestive system:

common - dyspepsia (nausea, diarrhea or constipation, flatulence, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth, uncommon (with long-term use in large doses) - ulceration of the gastrointestinal mucosa, impaired liver function; rare - perforation of the gastrointestinal tract, exacerbation of Crohn's disease, melena, gastrointestinal bleeding.

CNS:

common - headache, dizziness, sleep disturbance, fatigue, nervousness, nightmares; rare - migraine, peripheral polyneuropathy; very rare - hallucinations, disorientation and speech disorder.

Sense organs:

rare - tinnitus, change in taste, blurred vision, conjunctivitis.

SSS:

uncommon - tachycardia, arterial hypertension, peripheral edema.

Urinary system:

rare - renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria (more often develops in people taking NSAIDs and diuretics for a long time).

Other:

rare - hemoptysis, menometrorrhagia.

Laboratory indicators:

ketoprofen reduces platelet aggregation; transient increase in liver enzyme levels; rare - anemia, thrombocytopenia, agranulocytosis, purpura.

Drug interactions

Since ketotifen is significantly bound to plasma proteins, the doses of anticoagulants, diphenylhydantoin or sulfur-containing drugs used simultaneously with Ketonal should be reduced.

Overdose

Symptoms: nausea, vomiting, abdominal pain, vomiting blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function, renal failure.

Treatment: gastric lavage, administration of activated carbon, symptomatic therapy.

The use of histamine H2 receptor blockers, proton pump inhibitors, and prostaglandin inhibitors is indicated. There is no specific antidote.

Storage conditions

Store out of the reach of children at a temperature not exceeding 25°C.

Best before date

5 years.

Conditions for dispensing from pharmacies

On prescription

Ketonal solution d/iv and IM injection 50 mg/ml 2 ml No. 10

Compound

Active substance:

Excipients: propylene glycol - 800 mg, ethanol - 200 mg, benzyl alcohol - 40 mg, water for injection - up to 2 ml.

Pharmacokinetics

Absorption
Ketoprofen is easily absorbed from the gastrointestinal tract when taken orally. After oral administration of ketoprofen extended-release capsules 200 mg, maximum plasma concentrations of Cmax from 3.1 to 3.4 ± 1.2 mg/l are achieved within 5 hours.

The bioavailability of the drug is 90%. Food intake does not affect the overall bioavailability of ketoprofen, but reduces the rate of absorption.

Distribution

Ketoprofen is 99% bound to plasma proteins, mainly to the albumin fraction. The volume of distribution is 0.1 l/kg. Ketoprofen penetrates into the synovial fluid and reaches a concentration there equal to 50% of the concentration in the blood plasma. Plasma clearance of ketoprofen is approximately 0.08 l/kg/h. Effective concentrations of ketoprofen are determined in the blood even 24 hours after its administration.

Metabolism and excretion

Ketoprofen undergoes intensive metabolism under the action of microsomal liver enzymes, the half-life is less than 2 hours. Ketoprofen binds to glucuronic acid and is excreted from the body in the form of glucuronide. There are no active metabolites of ketoprofen. Up to 80% of ketoprofen is excreted by the kidneys within 24 hours, mainly in the form of ketoprofen glucuronide. In patients with severe renal impairment, most of the drug is excreted through the intestines. When taking high doses, hepatic clearance also increases. Up to 40% of the drug is excreted through the intestines. In patients with liver failure, the plasma concentration of ketoprofen is doubled (probably due to hypoalbuminemia and the resulting high level of unbound active ketoprofen); such patients should be prescribed the drug at the minimum therapeutic dose.

In patients with renal failure, the clearance of ketoprofen is reduced, but dose adjustment is required only in cases of severe renal failure.

In elderly patients, the metabolism and elimination of ketoprofen is slower, which is of clinical significance only for patients with severe renal impairment.

Indications for use

Symptomatic treatment of painful and inflammatory processes of various origins, including:

• inflammatory and degenerative diseases of the musculoskeletal system;
• rheumatoid arthritis, seronegative arthritis: ankylosing spondylitis - ankylosing spondylitis, psoriatic arthritis, reactive arthritis (Reiter's syndrome);
• gout, pseudogout;
• osteoarthritis;
• pain syndrome: mild, moderate and severe with headaches, migraines, tendonitis, bursitis, myalgia, neuralgia, radiculitis, post-traumatic and postoperative pain syndrome, including those accompanied by inflammation and fever, pain syndrome in oncological diseases, algodismenorrhea, inflammatory processes of organs pelvis, including adnexitis.

Contraindications

• Hypersensitivity to ketoprofen or other components of the drug, as well as salicylates or other non-steroidal anti-inflammatory drugs;
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);
• peptic ulcer of the stomach or duodenum in the acute stage;
• nonspecific ulcerative colitis, Crohn's disease;
• hemophilia and other bleeding disorders;
• children's age (up to 15 years);
• severe liver failure;
• severe renal failure: severe renal failure (creatinine clearance (CC) less than 30 ml/min), confirmed hyperkalemia, progressive kidney disease;
• uncompensated heart failure;
• postoperative period after coronary artery bypass surgery;
• gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
• chronic dyspepsia;
• III trimester of pregnancy;
• lactation period.

Carefully:

• History of peptic ulcer, presence of Helicobacter pylori infection;
• history of bronchial asthma;
• clinically significant cardiovascular, cerebrovascular and peripheral arterial diseases;
• dyslipidemia, liver failure, hyperbilirubinemia, alcoholic cirrhosis of the liver;
• chronic renal failure (creatinine clearance 30-60 ml/min);
• chronic heart failure, arterial hypertension, blood diseases;
• dehydration, diabetes mellitus;
• smoking;
• elderly age;
• long-term use of NSAIDs, simultaneous use of anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), oral glucocorticosteroids (including prednisolone), selective serotonin reuptake inhibitors (including fluoxetine, paroxetine, citalopram, sertraline).

Directions for use and doses

Intravenously, intramuscularly.
To reduce the frequency 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 benefits and risks before starting to take ketoprofen at a dose of 200 mg/day.

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

Intravenous infusion of ketoprofen should be carried out only in a hospital setting. The duration of infusion should be from 0.5 to 1 hour. The intravenous route of administration should be used for no more than 48 hours.

Short intravenous infusion: from 100 (to 200) mg (1 - 2 ampoules) of ketoprofen, diluted in 100 ml of 0.9% sodium chloride solution, administered over 0.5-1 hour.

Continuous intravenous infusion: from 100 (to 200) mg (1-2 ampoules) of ketoprofen, diluted in 500 ml of infusion solution (0.9% sodium chloride solution, lactate containing Ringer's solution, 5% dextrose solution), administered over 8 hours ; re-administration is possible after 8 hours. The maximum daily dose is 200 mg.

Ketoprofen can be combined with centrally acting analgesics; it can be mixed with opioids (eg morphine) in the same vial and is pharmaceutically incompatible with tramadol solution due to precipitation.

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

Storage conditions

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

Best before date

3 years. Do not use the drug after the expiration date.

special instructions

With long-term use of NSAIDs, it is necessary to periodically evaluate a clinical blood test, as well as monitor renal and liver function, especially in elderly patients (over 65 years), and conduct a stool test for occult blood.
It is necessary to be careful and monitor blood pressure more often when using ketoprofen to treat patients suffering from arterial hypertension and cardiovascular diseases that lead to fluid retention in the body. If visual disturbances occur, treatment should be stopped immediately.

Like other NSAIDs, ketoprofen can mask the symptoms of infectious and inflammatory diseases. If you notice signs of infection or deterioration in health while using the drug, you should immediately consult a doctor.

If there is a history of contraindications from the gastrointestinal tract (bleeding, perforation, peptic ulcer), long-term therapy and the use of high dosages of ketoprofen, the patient should be under close medical supervision.

Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing ketoprofen to patients with cardiac or renal insufficiency, as well as when treating elderly patients taking diuretics and patients who, for any reason, have a decrease in circulating volume. blood (for example, after surgery).

The use of ketoprofen can affect female fertility, therefore, patients with infertility (including those undergoing examination) are not recommended to use the drug.

Description

Non-steroidal anti-inflammatory drug (NSAID).

Use in children

Contraindicated in children (under 15 years of age).

Pharmacodynamics

Ketoprofen is a non-steroidal anti-inflammatory drug.
Ketoprofen has anti-inflammatory, analgesic and antipyretic effects. Ketoprofen blocks the action of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2) and, partially, lipoxygenase, which leads to suppression of prostaglandin synthesis (including in the central nervous system, most likely in the hypothalamus).

Stabilizes liposomal membranes in vitro and in vivo; at high concentrations in vitro, ketoprofen inhibits the synthesis of bradykinin and leukotrienes. Ketoprofen does not have a negative effect on the condition of articular cartilage.

Side effects

According to the World Health Organization (WHO), adverse effects are classified according to their frequency as follows: very common (≥ 1/10), common (≥1/100, <1/10), uncommon (≥1/1000, < 1/100), rare (≥1/10000, <1/1000) and very rare (<1/10000); frequency unknown (the frequency of events cannot be determined from the available data).

From the hematopoietic and lymphatic systems: rarely - hemorrhagic anemia, hemolytic anemia, leukopenia; frequency unknown - agranulocytosis, thrombocytopenia, bone marrow dysfunction.

From the immune system: frequency unknown - anaphylactic reactions (including anaphylactic shock).

From the nervous system: often - insomnia, depression, asthenia; uncommon - headache, dizziness, drowsiness; rarely - paresthesia, confusion or loss of consciousness, peripheral polyneuropathy; frequency unknown - convulsions, taste disturbances, emotional lability.

From the senses: rarely - blurred vision, tinnitus, conjunctivitis, dry mucous membrane of the eye, pain in the eyes, hearing loss; frequency unknown - optic neuritis.

From the cardiovascular system: infrequently - tachycardia; frequency unknown - heart failure, increased blood pressure, vasodilation.

From the respiratory system: rarely: exacerbation of bronchial asthma, nosebleeds, laryngeal edema; frequency unknown: bronchospasm (especially in patients with hypersensitivity to NSAIDs), rhinitis.

From the gastrointestinal tract: often - nausea, vomiting, dyspepsia, abdominal pain, NSAID gastropathy; uncommon - constipation, diarrhea, bloating, gastritis; rarely: peptic ulcer, stomatitis; very rarely: exacerbation of ulcerative colitis, Crohn's disease, gingival, gastrointestinal, hemorrhoidal bleeding, melena, perforation of the gastrointestinal tract; frequency unknown - gastrointestinal discomfort, stomach pain.

From the liver and biliary tract: rarely - hepatitis, increased activity of liver enzymes and bilirubin.

From the skin: infrequently - skin rash, itching; frequency unknown - photosensitivity, alopecia, urticaria, exacerbation of chronic urticaria, angioedema, erythema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis, purpura.

From the urinary system: rarely - cystitis, urethritis, hematuria; very rarely - acute renal failure, interstitial nephritis, nephrotic syndrome, abnormal values ​​of renal function indicators; frequency unknown - fluid retention in the body and, as a result, weight gain, hyperkalemia.

Other: infrequently - peripheral edema, fatigue; rarely - hemoptysis, menometrorrhagia, shortness of breath, thirst, muscle twitching.

Use during pregnancy and breastfeeding

Inhibition of prostaglandin synthesis may have undesirable effects on pregnancy and/or embryonic development. Data obtained from epidemiological studies with the use of prostaglandin synthesis inhibitors in early pregnancy confirm an increased risk of spontaneous abortion and the formation of heart defects (~1-1.5%).

Prescribing the drug to pregnant women in the first and second trimesters of pregnancy is possible only when the benefits for the mother justify the possible risk to the fetus.

The use of ketoprofen in pregnant women during the third trimester of pregnancy is contraindicated due to the possibility of developing weakness of labor in the uterus and/or premature closure of the ductus arteriosus, a possible increase in bleeding time, oligohydramnios and renal failure.

To date, there is no data on the release of ketoprofen into breast milk, therefore, if it is necessary to prescribe ketoprofen to a nursing mother, the issue of stopping breastfeeding should be addressed.

Interaction

Undesirable combinations of drugs
The combined use of ketoprofen with other NSAIDs (including selective cyclooxygenase-2 inhibitors), salicylates in high doses is not recommended, due to an increased risk of gastrointestinal bleeding and ulceration of the gastrointestinal mucosa.

Simultaneous use with anticoagulants (heparin, warfarin), antiplatelet agents (ticlopidine, clopidogrel) increases the risk of bleeding. If the use of such a combination is unavoidable, the patient's condition should be carefully monitored.

When used simultaneously with lithium preparations, it is possible to increase the concentration of lithium in the blood plasma up to toxic values. The concentration of lithium in the blood plasma should be carefully monitored and the dose of lithium preparations should be promptly adjusted during and after treatment with NSAIDs.

Increases the hematological toxicity of methotrexate, especially when used in high doses (more than 15 mg per week). The time interval between stopping or starting therapy with ketoprofen and taking methotrexate should be at least 12 hours.

Combinations to use with caution

During therapy with ketoprofen, patients taking diuretics, especially if dehydration develops, have a higher risk of developing renal failure due to a decrease in renal blood flow caused by inhibition of prostaglandin synthesis. Before starting to use ketoprofen in such patients, rehydration measures should be carried out. After starting treatment, it is necessary to monitor kidney function.

Combined use of the drug with ACE inhibitors and angiotensin II receptor blockers in patients with impaired renal function (with dehydration, elderly patients) can lead to worsening deterioration of renal function, including the development of acute renal failure.

During the first weeks of simultaneous use of ketoprofen and methotrexate at a dose not exceeding 15 mg/week, blood tests should be monitored weekly. In elderly patients or if there are any signs of renal impairment, the study should be performed more frequently. Combinations to take into account

Ketoprofen may weaken the effect of antihypertensive drugs (beta blockers, angiotensin-converting enzyme inhibitors, diuretics).

Concomitant use with selective serotonin reuptake inhibitors (SSRIs) increases the risk of gastrointestinal bleeding.

Concomitant use with thrombolytics increases the risk of bleeding.

Concomitant use with potassium salts, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor blockers, NSAIDs, low molecular weight heparins, cyclosporine, tacrolimus and trimethoprim increases the risk of developing hyperkalemia.

When used simultaneously with cyclosporine and tacrolimus, there may be a risk of additive nephrotoxicity, especially in elderly patients.

The use of several antiplatelet drugs (tirofiban, eptifibarid, abciximab, iloprost) increases the risk of bleeding.

Increases the plasma concentration of cardiac glycosides, slow calcium channel blockers, cyclosporine, methotrexate and digoxin.

Ketoprofen may enhance the effect of oral hypoglycemic and some anticonvulsants (phenytoin).

Concomitant use with probenecid significantly reduces the plasma clearance of ketoprofen.

Nonsteroidal anti-inflammatory drugs may reduce the effectiveness of mifepristone. Taking NSAIDs should be started no earlier than 8-12 days after stopping mifepristone.

Pharmaceutically incompatible with tramadol solution due to precipitation.

Overdose

In case of an overdose of ketoprofen, headache, nausea, vomiting, abdominal pain, vomiting of blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal failure may occur.

In case of overdose, gastric lavage and the use of activated carbon are indicated.

Treatment - symptomatic and supportive therapy; the effect of ketoprofen on the gastrointestinal tract can be weakened with the help of agents that reduce the secretion of gastric glands (for example, proton pump inhibitors) and prostaglandins; monitoring of respiratory and cardiovascular activity; no specific antidote has been found; hemodialysis is ineffective.

Impact on the ability to drive vehicles and operate machinery

During the period of use of the drug, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, since the drug can cause dizziness and other side effects that can affect these abilities.