Ketofril, 10 mg 20 pcs.

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID)

ATX code: [M01AB15]

Pharmacological action

PharmacodynamicsKetorolac has a pronounced analgesic effect, also has anti-inflammatory and moderate antipyretic effects.

The mechanism of action is related to non-selective inhibition of cyclooxygenase 1 and 2 enzyme activity, mainly in peripheral tissues, with the consequence of inhibition of prostaglandin biosynthesis – modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of |-]S and [+]R enantiomers, with analgesic effect due to the [-]S form.

The drug does not influence opioid receptors, does not suppress respiration, does not cause drug addiction and has no sedative and anxiolytic action.

In terms of the analgesic effect, it is comparable with morphine and is considerably superior to other NSAIDs. After oral administration the onset of analgesic effect is noted respectively in 1 hour, the maximum effect is reached after 1-2 hours.

Pharmacokinetics

On oral administration Ketorolac is well absorbed in the gastrointestinal tract – maximum concentration (Cmax) in blood plasma (0.7-1.1 mcg/ml) is reached 40 min after an empty stomach dose of 10 mg. Fat-rich food reduces the maximum blood concentration of the drug and delays its achievement by 1 hour.

99% of the drug is bound to plasma proteins and in case of hypoalbuminemia the amount of free substance in blood increases.

The bioavailability is 80-100%. Time of reaching equilibrium concentration (Css) by oral administration – 24 hours when administered 4 times a day (higher than subtherapeutic) and is 0.39-0.79 mcg/ml after 10 mg oral administration. The volume of distribution is 0.15-0.33 l/kg. In patients with renal insufficiency the distribution volume of the drug may increase 2-fold, and the distribution volume of its R-enantiomer – by 20%.

Transfers to breast milk: when the mother takes 10 mg of ketorolac, the Cmax in milk is reached 2 hours after the first dose and is 7.3 ng/ml, 2 h after the second dose of ketorolac (when the drug is used 4 times a day) it is 7.9 ng/ml.

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. It is excreted 91% by the kidneys, 6% – through the intestine.

The half-life (T½ in patients with normal renal function is on average 5.3 h. T½ is longer in older patients and shorter in younger patients. Liver function has no effect on T½ In patients with impaired renal function with plasma creatinine concentration of 19-50 mg/l (168-442 μmol/l) T½ is 10.3-10.8 hours, in more severe renal insufficiency – more than 13.6 hours. It is not excreted during hemodialysis.

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Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Hypersensitivity to the active substance or excipients; anamnestic, evidence of an attack of bronchoobstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome – rhinosinusitis, urticaria, nasal polyps, bronchial asthma); angioedema, hypovolemia (regardless of its cause), dehydration.

Erotic ulcerative changes of the mucosa of the stomach or 12 duodenum, active gastrointestinal bleeding; inflammatory bowel disease; hypocoagulation (including hemophilia).

Developed hepatic insufficiency or active liver disease; marked renal insufficiency (plasma creatinine above 50 mg/l), advanced renal disease; confirmed hyperkalemia.

Hemorrhagic stroke (confirmed or suspected), hemorrhagic diathesis, concomitant use with other NSAIDs, high risk of development or recurrence of bleeding (including after surgery), hematopoiesis disorders.

Pregnancy, childbirth and lactation.

Children under 16 years of age (effectiveness and safety not established).

The period after aortocoronary bypass surgery;

The drug is not used for pain relief before and during surgical procedures because of the high risk of bleeding, and for the treatment of chronic pain.

With caution – bronchial asthma; cholecystitis; chronic heart failure; coronary heart disease, cerebrovascular disease, arterial hypertension; dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, renal impairment (plasma creatinine below 50 mg/L); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; elderly (over 65 years); nasal and nasopharyngeal polyps.

Anamnestic evidence of gastrointestinal ulcers, Helicobacter pylori infection, long-term use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs:

Side effects

Overdose

Similarities