Ketorol Express - Instructions For The Use Of Tablets, Price, Reviews

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

Ketorol Express

Ketorol Express: instructions for use and reviews

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

Latin name: Ketorol Express

ATX code: M01AB15

Active ingredient: ketorolac (Ketorolac)

Manufacturer: Dr. Reddy's Laboratories, Ltd. (Dr. Reddy's Laboratories, Ltd.) (India)

Description and photo update: 2020-01-08

Prices in pharmacies: from 36 rubles.

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Ketorol Express is a non-steroidal anti-inflammatory drug (NSAID) with a moderate antipyretic and pronounced analgesic effect.

Release form and composition

The drug is produced in the form of tablets dispersed in the oral cavity: pale yellow, flat, round, with a chamfer, on one side with an engraving "|" (10 pcs. in a blister, in a cardboard box 1 or 2 blisters and instructions for the use of Ketorol Express).

1 tablet contains:

• active ingredient: ketorolac - 10 mg;
• excipients: butylhydroxyanisole, microcrystalline cellulose, sucralose, silicon dioxide, crospovidone (type A), mannitol, magnesium stearate, quinoline yellow dye (E104), mint flavor.

Pharmacological properties

Pharmacodynamics

Ketorolac, the active ingredient of Ketorol Express, has an analgesic, anti-inflammatory and mild antipyretic effect. The mechanism of action of the agent is due to the non-selective suppression of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes the conversion of arachidonic acid to prostaglandins (PG), which play an important role in the pathogenesis of pain, inflammation and fever.

Ketorolac is a racemic mixture of [-] S- and [+] R-enantiomers, while its analgesic effect is associated with the [-] S-form.

Ketorol Express does not inhibit respiration, does not affect opioid receptors, does not lead to drug dependence, does not demonstrate sedative and anxiolytic effects. After oral administration of the drug, the analgesic effect begins to appear after 1 hour, the maximum therapeutic effect is noted after 1–2 hours.

Pharmacokinetics

With oral administration of Ketorol Express, ketorolac is intensively absorbed in the gastrointestinal tract (GIT). In the blood plasma, the maximum concentration (C _max) of 0.7–1.1 μg / ml is observed 40 minutes after taking it on an empty stomach at a dose of 10 mg. Foods rich in fats reduce the C _{max of the} substance in the blood and increase the time to reach it by 1 hour. Ketorolac binds to plasma proteins by 99%, the proportion of free substance in the blood increases against the background of hypoalbuminemia, bioavailability varies from 80 to 100%, the volume of distribution (V _d) is 0.15–0.33 l / kg.

In the case of oral administration of ketorolac 4 times a day, 10 mg (the daily dose exceeds the subtherapeutic dose), the equilibrium concentration is reached after 24 hours.

The agent penetrates into breast milk. After taking ketorolac at a dose of 10 mg by a nursing woman, its C _max in breast milk is determined after 2 hours and is 7.3 ng / ml after the first dose, and 7.9 ng / ml after the second.

The substance is metabolized in the liver in an amount exceeding ½ of the dose taken. As a result of its biotransformation, pharmacologically inactive derivatives are formed. The main metabolites include renally eliminated glucuronides and p-hydroxyketorolac. 6% is excreted through the intestines, 91% by the kidneys.

In persons with normal renal function, the half-life (T _1/2) after taking the drug at a dose of 10 mg is 2.4-9 hours; total clearance - 0.025 l / h / kg. T _1/2 increases in elderly patients and decreases in young patients. During hemodialysis, the drug is not excreted from the body.

Indications for use

Ketorol Express is recommended for the relief of moderate to severe pain syndrome, including for the following diseases / conditions:

• trauma;
• rheumatic affections;
• pain in the postoperative period;
• oncological diseases;
• neuralgia, myalgia, arthralgia, sciatica;
• sprains, dislocations;
• toothache.

Ketorol Express is used for symptomatic treatment, weakening the inflammatory process and reducing the intensity of pain at the time of use. The drug does not affect the progression of the underlying disease.

Contraindications

Absolute:

• recurrent polyposis rhinosinusitis, bronchial asthma and intolerance to NSAIDs, including acetylsalicylic acid (full or partial combination, including a history);
• ulcerative colitis, Crohn's disease and other inflammatory bowel diseases;
• active bleeding from the gastrointestinal tract, erosive and ulcerative lesions of the gastrointestinal tract;
• severe impairment of renal function [with creatinine clearance (CC) below 30 ml / min]; confirmed hyperkalemia;
• active liver disease or severe liver failure;
• myelosuppression, damage to the bone marrow and blood (thrombocytopenia; leukopenia, including data in anamnesis; hypocoagulation, including hemophilia), bleeding or a high probability of their occurrence;
• the period after the operation of coronary artery bypass grafting;
• active cerebrovascular disease (including confirmed or suspected intracranial hemorrhage);
• anesthesia during extensive surgical interventions, as well as before their implementation (due to the significant threat of bleeding);
• combination therapy with the following drugs: probenecid, pentoxifylline, lithium salts, anticoagulants (heparin, warfarin), acetylsalicylic acid and other NSAIDs, including selective COX-2 inhibitors;
• age under 16;
• pregnancy, labor and lactation;
• hypersensitivity to any component of the drug and to other NSAIDs.

Relative (take Ketorol Express tablets with caution):

• chronic heart failure (CHF), ischemic heart disease (IHD); arterial hypertension;
• edematous syndrome;
• moderate renal impairment (CC 30–60 ml / min);
• active hepatitis, cholestatic syndrome;
• the presence of factors that aggravate gastrointestinal toxicity: cholecystitis, alcoholism, tobacco smoking;
• bronchial asthma;
• systemic lupus erythematosus;
• sepsis;
• cerebrovascular diseases;
• the presence of Helicobacter pylori infection, a history of ulcerative gastrointestinal defects;
• peripheral arterial lesions;
• diabetes;
• dyslipidemia / hyperlipidemia;
• pathology of the thyroid gland;
• severe somatic diseases;
• tuberculosis;
• postoperative period;
• age after 65 years;
• long-term use of NSAIDs;
• concomitant use of the following drugs: selective serotonin reuptake inhibitors (SSRIs) (including sertraline, paroxetine, citalopram, fluoxetine), antiplatelet agents (including clopidogrel), oral glucocorticosteroids (GCS) (including prednisolone).

Ketorol Express, instructions for use: method and dosage

Ketorol Express tablets are taken orally. They should be placed on the tongue and kept in the mouth for a few seconds until completely dissolved.

Oral dispersible tablets do not need to be taken with water. Since the drug also does not lead to an increase in saliva production, it can be taken by patients with deviations in the act of swallowing, concomitant neurological and behavioral disorders.

A single dose of Ketorol Express is 10 mg (1 tablet). Depending on the severity of the pain syndrome, the drug can be taken from 1 to 4 times a day. The maximum permissible daily dose is 40 mg, the maximum course of therapy is 5 days.

In order to reduce the risk of side effects, Ketorol Express should be used in the lowest effective dose for the shortest possible course.

In the case of a switch from parenteral administration of ketorolac to its oral administration, on the day of transfer, the total daily dose of both forms of the drug for patients under 65 years of age should not exceed 90 mg, for patients over 65 years of age or with impaired renal function - no more than 60 mg. In this case, the dose of ketorolac in tablet form (for oral administration) should not exceed 30 mg.

Side effects

• respiratory system: rarely - rhinitis, dyspnea or bronchospasm, laryngeal edema (shortness of breath and difficulty breathing);
• digestive system: often (mainly in patients over 65 years of age, with a history of erosive and ulcerative gastrointestinal defects) - diarrhea, gastralgia; infrequently - a feeling of fullness in the stomach, constipation, vomiting, flatulence, stomatitis; rarely - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including perforation and / or bleeding - heartburn, abdominal pain, burning / spasm in the epigastric region, vomiting like coffee grounds, melena), acute pancreatitis, cholestatic jaundice, hepatomegaly, hepatitis;
• hemostatic system: rarely - nosebleeds, bleeding from a postoperative wound, rectal bleeding;
• hematopoietic organs: rarely - eosinophilia, anemia, leukopenia;
• cardiovascular system: infrequently - increased blood pressure (BP); rarely - fainting, pulmonary edema;
• sense organs: rarely - hearing impairment, ringing in the ears, visual impairment, including blurred vision; with an unknown frequency - taste disturbance;
• nervous system: often - drowsiness, dizziness, headache; rarely - aseptic meningitis (stiff neck / back muscles, severe headache, fever, convulsions), hyperactivity, including anxiety, mood changes; depression, psychosis, hallucinations;
• skin: infrequently - purpura, skin rash (including maculopapular); rarely - urticaria, exfoliative dermatitis (thickening / peeling of the skin, flushing, fever with or without chills, tenderness and / or swelling of the palatine tonsils), toxic epidermal necrolysis, Stevens-Johnson syndrome;
• urinary system: rarely - back pain, frequent urination, polyuria, oliguria, hematuria, azotemia, renal edema, acute renal failure, hemolytic uremic syndrome (thrombocytopenia, purpura, renal failure, hemolytic anemia), interstitial nephritis; with an unknown frequency - urinary retention;
• allergic reactions: rarely - anaphylactoid reactions (itching, discoloration of the face, urticaria, skin rash, wheezing, dyspnea / tachypnea, shortness of breath, shortness of breath, eyelid edema, periorbital edema, tongue edema, heaviness in the chest), anaphylaxis;
• other reactions: often - an increase in body weight, swelling, including of the legs, ankles, face, fingers, feet; infrequently - excessive sweating; rarely, fever; with an unknown frequency - hyperkalemia, hyponatremia.

Overdose

The main symptoms of ketorolac overdose include nausea, vomiting, abdominal pain, erosive and ulcerative gastrointestinal defects, metabolic acidosis, and renal dysfunction.

Therapy: gastric lavage, use of activated carbon; symptomatic treatment aimed at maintaining blood circulation, respiration and other vital functions. With dialysis, Ketorol Express is poorly eliminated.

special instructions

Before starting therapy with Ketorol Express, it is necessary to establish whether there is a history of previous allergy to ketorolac or other NSAIDs.

Due to the threat of allergic reactions, the first dose should be taken under medical supervision.

Ketorol Express inhibits platelet aggregation and leads to an increase in blood clotting time. After 24-48 hours after taking the drug, no effect on platelet aggregation is detected.

With existing blood clotting disorders, especially in the postoperative period, when a thorough assessment of the state of hemostasis is required, Ketorol Express should be used only with constant monitoring of the platelet count.

Patients with hypovolemia have an increased risk of adverse events from the urinary system.

The threat of side effects is exacerbated by an increase in the duration of therapy and taking Ketorol Express in doses above 40 mg / day.

It is not recommended to use the drug for sedation and maintenance anesthesia.

In the course of clinical studies, it was found that taking some NSAIDs in doses exceeding therapeutic ones can increase the risk of arterial thrombotic complications, including myocardial infarction and stroke. Against the background of ketorolac therapy, such side effects were not observed, however, the possibility of their development cannot be completely ruled out due to the lack of available data.

To reduce the threat of NSAID-induced gastropathy recommended during treatment applied antacids, misoprostol and means for lowering gastric secretion, including proton pump inhibitors and blockers of H ₂ receptors of histamine.

Influence on the ability to drive vehicles and complex mechanisms

During therapy, patients who drive vehicles or other complex mechanisms should be careful.

Application during pregnancy and lactation

The use of Ketorol Express during pregnancy is contraindicated due to the possible premature closure of the aortic duct in the fetus.

Since ketorolac, by suppressing the production of PG, can adversely affect the blood circulation of the fetus, as well as weaken the contractions of the uterus, exacerbating the threat of uterine bleeding, its use during delivery and in the early postpartum period is contraindicated.

Ketorolac is excreted in breast milk, therefore, Ketorol Express is not prescribed for lactating women.

Pediatric use

For children and adolescents under 16 years of age, drug therapy is contraindicated, since the effectiveness and safety of using Ketorol Express in pediatrics has not been established.

With impaired renal function

In patients with renal insufficiency, the V _{d of} ketorolac can increase by 2 times, and the V _{d of} its R-enantiomer - by 20%. During therapy of patients with impaired renal function (at a plasma creatinine level of 19-50 mg / l or 168-442 μmol / l) T _{1/2 of} ketorolac is 10.3-10.8 hours, in the case of more severe renal failure - over 13.6 hrs

In the presence of confirmed hyperkalemia, severe renal dysfunction (CC below 30 ml / min), the drug is contraindicated. Patients with moderate renal insufficiency (CC 30-60 ml / min) are advised to use Ketorol Express with caution.

For violations of liver function

The presence of liver dysfunction does not affect T _{1/2 of the} drug.

Contraindications to taking Ketorol Express are active liver disease or severe liver failure. Patients with cholestasis or active hepatitis should use the drug with caution.

Use in the elderly

Taking Ketorol Express in patients over 65 requires caution, since its T _1/2 increases in old age.

Drug interactions

• thrombolytics, antiplatelet agents, indirect anticoagulants, cefoperazone, pentoxifylline, cefotetan: the threat of bleeding is aggravated;
• paracetamol: increases the nephrotoxicity of ketorolac, if a combination therapy is necessary, the course should be no more than 2 days;
• GCS, ethanol, acetylsalicylic acid and other NSAIDs, calcium preparations, corticotropin: the likelihood of side effects, including gastrointestinal ulcers and gastrointestinal bleeding, increases significantly;
• probenecid: Vd and plasma clearance of ketorolac decreases, its content in blood plasma and T1 / 2 increases;
• COX-2 inhibitors and other NSAIDs: the risk of fluid retention, increased blood pressure, cardiac decompensation increases;
• valproate: possible violation of platelet aggregation;
• cyclosporine, tacrolimus, other nephrotoxic agents (including gold preparations): the threat of nephrotoxicity is increasing;
• insulin, oral antidiabetic drugs: ketorolac enhances their hypoglycemic effect, which may require a change in the dose of these drugs;
• lithium preparations: the clearance of lithium decreases, its content in plasma increases and the toxic effect increases; this combination is contraindicated;
• nifedipine, verapamil: the concentration of these substances in the blood plasma increases;
• methotrexate: the hepato- and nephrotoxicity of this substance is aggravated; simultaneous administration with ketorolac is possible only in the case of using methotrexate in low doses, it is required to monitor the plasma level of the latter;
• quinolone antibiotics: the risk of seizures increases;
• myelotoxic drugs, zidovudine: aggravate the hematotoxicity of Ketorol Express;
• mifepristone: the effectiveness of this substance decreases; do not use NSAIDs for 8-12 days after mifepristone therapy;
• means that block tubular secretion: lower the clearance of ketorolac, as a result of which its plasma level in the blood increases;
• digoxin: there is no violation of its binding to plasma proteins; therapeutic concentrations of this substance do not affect the connection of ketorolac with blood proteins;
• narcotic analgesics: the therapeutic effect of these drugs increases, a significant reduction in their doses may be required;
• diuretics, antihypertensive drugs: their effectiveness decreases due to the effect of Ketorol Express on the synthesis of PG in the kidneys;
• antacids: do not alter the absorption of ketorolac.

Analogs

The analogues of Ketorol Express are Ketorolac, Ketokam, Ketanov, Ketorolac-Eskom, Dolak, Ketalgin, Ketorol, Ketofril, Ketorolac-OBL, etc.

Terms and conditions of storage

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

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ketorol Express

Reviews of Ketorol Express are mostly positive. Patients note that the remedy effectively and quickly copes with pain syndrome of varying intensity arising from injuries, rheumatic diseases, neuralgia, radiculitis, myalgia, arthralgia, and also relieves toothache and postoperative pain well. The cost of the drug is called low, and the release form is convenient.

The disadvantages of Ketorol Express most often include a large number of contraindications and adverse adverse reactions, especially from the gastrointestinal tract. Sometimes they complain about the unpleasant taste of the tablets, which is why they had to be washed down with water. In isolated cases, the lack of a therapeutic effect is noted.

Price for Ketorol Express in pharmacies

The price of Ketorol Express in the form of tablets, dispersible in the oral cavity, averages 60 rubles. per pack of 20 10 mg each.

Ketorol Express: prices in online pharmacies

Drug name Price Pharmacy

Ketorol Express 10 mg orodispersible tablets 20 pcs. RUB 36 Buy

Ketorol express tab. dispersion in the oral cavity 10 mg 20 pcs. RUB 48 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!