Ketorolac-Solopharm, 30 mg/ml 1 ml 10 pcs
€4.49 €3.74
A nonsteroidal anti-inflammatory drug.
The ATX code: M01AB15
Pharmacological properties
Pharmacodynamics
Ketorolac refers to non-steroidal anti-inflammatory drugs (NSAIDs), has a pronounced analgesic effect, also has anti-inflammatory and moderate antipyretic effects.
The mechanism of action is associated with non-selective inhibition of cyclooxygenase 1 (COX 1) and cyclooxygenase 2 (COX 2) activity, catalyzing formation of prostaglandins (Pg) from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form. It is comparable with morphine in analgesic effect and is significantly superior to other NSAIDs. The onset of analgesic action is noted after 0.5 h, the maximum effect is reached after 1-2 h and lasts about 4-6 h.
Pharmacokinetics
Absorption
Bioavailability is complete and fast. After intramuscular administration of 30 mg, maximum concentration (Cmax) is 1.74-3.1 mcg/ml, 60 mg – 3.23-5.77 mcg/ml, time to reach maximum concentration (TCmax) is 15-73 min and 30-60 min, respectively. After intravenous administration in a dose of 15 mg, Cmax is 1.96-2.98 mcg/ml; in a dose of 30 mg, Cmax is 3.69-5.61 mcg/ml.
Distribution
The binding to plasma proteins is 99%. Time to reach equilibrium concentration (Csr) – 24 h, Csr is 0.65-1.13 mcg/ml with intramuscular administration of 15 mg 4 times daily, 30 mg – 1.29-2.47 mcg/ml.
The volume of distribution is 0.15-0.33 l/kg. In patients with renal insufficiency, the volume of distribution of ketorolac may increase by 2-fold and the volume of distribution of its R-enantiomer by 20%.
Transfers to breast milk: after giving 10 mg of ketorolac the Cmax in milk is reached after 2 hours and is 7.3 ng/ml; after 2 hours after the second dose of ketorolac (when using the drug 4 times daily) it is 7.9 ng/l.
Metabolism
More than 50% of the administered dose is metabolized in the liver to form pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. 91% is excreted by the kidneys, and 6% – through the intestine.
The elimination half-life (T1/2) in patients with normal renal function averages 5.3 h (3.5-9.2 h after intramuscular administration of 30 mg). The T1/2 is increased in elderly patients and decreased in younger patients. Liver function has no effect on the T1/2. In patients with impaired renal function and creatinine concentration in plasma is 19-50 mg/l (168-442 μmol/l), T1/2 is 10.3-10.8 hours; in more severe renal failure it is more than 13.6 hours. Total clearance when administered intramuscularly 30 mg is 0.023 l/h/kg, when administered intravenously 30 mg – 0.03 l/kg/h.
Ketorolac is not excreted by hemodialysis.
Indications
Active ingredient
Composition
How to take, the dosage
Interaction
Special Instructions
Before prescribing the drug, it is necessary to find out about previous allergy to ketorolac or other NSAIDs. Due to the risk of allergic reactions, the first dose should be administered under close medical supervision. Hypovolemia increases the risk of nephrotoxic adverse reactions. If necessary, it may be used with opioid analgesics.
It is not recommended to use as an agent for premedication, maintenance of anesthesia. When co-administered with other NSAIDs, fluid retention, decompensation of cardiac activity, increased blood pressure may be observed. The risk of drug complications increases with prolongation of treatment (in patients with chronic pain) and increasing of the drug dose. Antacids, misoprostol, omeprazole are used to reduce the risk of NSAID gastropathy.
Impact on driving and operating machinery
When using the drug, caution must be exercised while driving motor vehicles and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.
Contraindications
– anamnestic evidence of an attack of bronchoobstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete combination of bronchial asthma, polyposis of the nose and sinuses and intolerance to acetylsalicylic acid and other NSAIDs);
– hypovolemia (regardless of the cause);
– gastrointestinal erosive-ulcerative lesions with acute conditions, peptic ulcers, bleeding or high risk of bleeding, hypocoagulation (including hemophilia), inflammatory bowel disease (Crohn’s disease, ulcerative colitis);
– Severe hepatic impairment or active liver disease;
– Severe renal impairment (serum creatinine > 700 μmol/L), advanced renal disease;
– confirmed hypokalemia;
– decompensated heart failure, post aortocoronary bypass;
– The drug is not to be used for pain relief before and during surgical interventions due to the high risk of bleeding;
– intracranial hemorrhage or suspected bleeding;
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– confirmed hyperkalemia;
– pregnancy, childbirth, breastfeeding period;
– children under 16 years of age (effectiveness and safety not established).
With caution
Hypersensitivity to other NSAIDs, bronchial asthma, presence of factors that increase gastrointestinal toxicity (alcoholism, smoking, cholecystitis); postoperative period; chronic heart failure (CHF), coronary heart disease (CHD), edema syndrome, arterial hypertension; moderate renal failure (serum creatinine 300-700 μmol/L); cholestasis; sepsis; systemic lupus erythematosus; concurrent use with other NSAIDs, long-term use of NSAIDs; cerebrovascular disease; dyslipidemia, hyperlipidemia, diabetes, peripheral artery disease; history of peptic ulcers, presence of H. pylori; severe somatic diseases; systemic connective tissue diseases; inflammatory bowel disease without exacerbation; concomitant use of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), older age (over 65 years).
Side effects
Overdose
Symptoms: abdominal pain, nausea, vomiting, gastrointestinal erosive and ulcerative lesions, impaired renal function, metabolic acidosis.
Treatment: there is no specific antidote, gastric lavage, administration of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital body functions) are recommended. Ketorolac is not eliminated sufficiently by dialysis.
Pregnancy use
Do not take the drug during pregnancy (adverse effect on the cardiovascular system of the fetus – premature closure of the arterial duct), during childbirth, in the early postpartum period (inhibits the synthesis of prostaglandins, the drug may adversely affect the fetal circulation and weaken uterine contractility, which increases the risk of uterine bleeding) and during breast-feeding (the drug enters the breast milk).
If it is necessary to use the drug during lactation, breastfeeding should be stopped.
Similarities
Weight | 0.100 kg |
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Shelf life | 3 years. Do not use after the expiration date! |
Conditions of storage | Store at a temperature not exceeding 25 ºC. Store out of the reach of children. |
Manufacturer | Grotex Ltd, Russia |
Medication form | solution |
Brand | Grotex Ltd |
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