Index
- Introduction: what is it?
- Dosage: how is it used and how does it work?
- Warnings and Precautions
- Overdose
- Interactions and side effects
- Pregnancy and breastfeeding
- Notes (validity, storage conditions)
Questions and answers
Introduction: what is it?
The OKI drug is used for the symptomatic and short-term treatment of inflammatory states associated with pain such as those affecting the osteoarticular system, post-operative pain and ear infections. The higher dosages are reserved for the symptomatic treatment of more serious inflammatory states such as: rheumatoid arthritis, ankylosing spondylitis, painful arthrosis, extraarticular rheumatism, post-traumatic inflammation. The injectable form is also used for the treatment of neoplastic pain.
The active ingredient contained in OKI is Ketoprofen lysine salt, a drug with anti-inflammatory , analgesic and antipyretic activity. Ketoprofen lysine salt is more soluble than acid ketoprofen.
OKI is available as:
- 80 mg granulesfor oral solution. One bipartite sachet contains ketoprofen 80 mg lysine salt corresponding to 50 mg of ketoprofen.
- Suppositorieswith different dosages from 30 mg, 60 mg, 160 mg.
- Oral drops, solution 80 mg / ml. 100 ml of solution contain 8 g ketoprofen lysine salt (1 drop contains 4 mg) corresponding to 5 g of ketoprofen.
- Solution for injectionin ampoules for intramuscular use of 160 mg / 2 ml. Each vial contains 160 mg of ketoprofen lysine salt (corresponding to 100 mg of ketoprofen).
All these formulations of OKI require a repeatable medical prescription , while only the ampoules and sachets are loanable (for some pathologies).
There are formulations on the market that can be purchased without a prescription (buccal sachets, tablets, sprays or mouthwash).
OkiTask is presented as an orosoluble granulate to be dissolved directly on the tongue, with the advantage of faster absorption, or as a coated tablet; the amount of active ingredient present is 40 mg, half of a traditional sachet. OKiTask is indicated for the treatment of pain of various origins and nature, and in particular headache, toothache, neuralgia, menstrual pain, muscle and bone pain. OKI inflammation and pain
is also available1.6% which is presented as a mouthwash (100 ml of mouthwash contain as active ingredient: Ketoprofen lysine salt 1.6 grams) or as a spray (100 ml of oral mucosal spray contain as active ingredient: Ketoprofen lysine salt 0 , 16 grams corresponding to 0.10 grams of Ketoprofen). OKI mouthwash or spray is indicated for the symptomatic treatment of irritative-inflammatory states also associated with oropharyngeal pain (eg gingivitis, stomatitis, pharyngitis (sore throat)), as a result of conservative or extractive dental therapy.
See the directions for taking this drug in patients infected with COVID-19 coronavirus:
Taking NSAIDs and COVID-19 coronaviruses
Dosage: how is it used and how does it work?
The ketoprofen lysine salt , like ketoprofen, belongs to the class of anti-inflammatory non-steroidal drugs (NSAIDs).
It has an anti-inflammatory action mainly due to the inhibition of the synthesis of prostaglandins from their precursor (arachidonic acid), to the stabilization of the lysosomal membrane with inhibition of the release of enzymes, to the antibradykinin activity and to the antiplatelet activity, all involved in the pathogenesis of inflammatory phenomena.
The mechanism of action of NSAIDs is related to the reduction of prostaglandin synthesis by inhibiting the cyclooxygenase enzyme .
Specifically, there is an inhibition of the transformation of arachidonic acid into cyclic endoperoxides, PGG2 and PGH2, precursors of prostaglandins PGE1, PGE2, PGF2 and PGD2 and also of prostacyclin PGI2 and thromboxanes (TxA2 and TxB2).
Furthermore, the inhibition of prostaglandin synthesis can interfere with other mediators such as kinins, causing an indirect action that adds to the direct action.
Ketoprofen lysine salt possesses a marked analgesic effect, correlated both with its anti-inflammatory effect and with an effect on the central nervous system. Furthermore, it performs an antipyretic activity without interfering with the normal thermoregulation processes. The painful inflammatory manifestations are eliminated or attenuated by promoting joint mobility.
The form for oral use allows the assumption of the active principle already in aqueous solution and therefore leads to a rapid increase in plasma levels and an early reaching of the peak value. This leads to a more rapid appearance and a greater intensity of the analgesic and anti-inflammatory effect. The kinetic profile in the child does not differ from that in the adult.
Dosage: for taking it is recommended to follow the medical prescription.
The maximum daily dose is 200 mg of ketoprofen , corresponding to 320 mg of ketoprofen lysine salt. The risk / benefit ratio must be carefully considered before starting treatment with the daily dose of 200 mg of ketoprofen, and higher doses are not recommended.
Undesirable effects can be minimized by using the shortest possible duration of treatment that is needed to control symptoms.
In the treatment of elderly patients, the posology must be carefully established by the physician who will have to evaluate a possible reduction in dosages.
Since the recommended posology in children should be between 1 and 2 mg / kg per administration, the following dosage regimen is recommended:
Children aged 6 years or older
- body weight less than 30 kg: 1 suppository OKi 30 mg 2-3 times a day
- body weight over 30 kg: 1 suppository OKi 60 mg 2-3 times a day.
It is recommended not to use injection therapy beyond three days, after which it is advisable to switch to oral or rectal therapy.
Warnings and Precautions
OKI is contraindicated in children under 6 years of age.
OKI is contraindicated in patients with hypersensitivity to ketoprofen or to any of the excipients and in patients with severe hepatic and renal dysfunction.
In patients with mild or moderate renal insufficiency it is recommended to monitor the volume of urine produced and renal function. If necessary, reduce the starting dose and practice maintenance therapy with the lowest effective dose. Individualized adjustments can be considered only after establishing good tolerability of the drug.
Patients with mild or moderate hepatic impairment should be followed closely and treated with the lowest effective daily dose.
Undesirable effects can be minimized by using the lowest effective dose for the shortest possible duration of treatment needed to control symptoms.
The concomitant use of OKi with other NSAIDs including selective cyclooxygenase-2 inhibitors should be avoided. Cases of gastrointestinal ulceration, perforation or bleeding, which can be fatal, with or without warning symptoms or a previous history of serious gastrointestinal events, have been reported during treatment with all NSAIDs.
The risk of gastrointestinal ulcer, perforation or haemorrhage is higher in patients with a history of ulcer, especially if aggravated by haemorrhage or perforation and in the elderly. These patients should start treatment at the lowest possible dose. Combination therapy with gastro-protective drugs (e.g. misoprostol or proton pump inhibitors) should be considered for these patients and for those who have to take concomitantly low doses of acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal events.
NSAIDs should be administered with caution to patients with a history of gastrointestinal disease(ulcerative colitis, Crohn’s disease) as these conditions can be exacerbated. Patients with a history of gastrointestinal toxicity, particularly when elderly, should report any unusual abdominal symptoms (especially gastrointestinal bleeding) particularly in the initial stages of treatment.
Caution should be exercised in patients taking concomitant medications that may increase the risk of ulceration or bleeding, including oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid.
If gastrointestinal bleeding or ulceration occurs, discontinue treatment with ketoprofen immediately.
Senior citizens: Elderly patients have an increased frequency of adverse reactions to NSAIDs, particularly gastrointestinal bleeding and perforation, which can be fatal.
In some pediatric patients treated with ketoprofen lysine salt, gastrointestinal bleeding, occasionally severe, and peptic ulcer have been reported; therefore the product must be administered under strict supervision of the physician who will have to evaluate the necessary dosage schedule each time.
SKIN REACTIONS
In very rare cases, severe skin reactions, some of them fatal, such as exfoliative dermatitis , Stevens-Johnson syndrome and toxic epidermal necrolysis , have been observed following combination with other NSAIDs . Patients appear to have an increased risk of developing these reactions early in treatment, with the onset of reactions in most cases within the first month of treatment.
Stop taking ketoprofen at the first appearance of skin rashes, mucosal lesions or any other signs of hypersensitivity.
PRECAUTIONS
Cardiovascular, renal and hepatic dysfunction.
In patients with impaired renal function , administration of ketoprofen should be performed with particular caution in view of the essentially renal elimination of the drug.
At the start of treatment, renal function should be carefully monitored in patients with heart failure, cirrhosis and nephrosis, in patients on diuretic therapy or with chronic renal failure, especially if elderly. In these patients, administration of ketoprofen can induce a reduction in renal blood flow caused by the inhibition of prostaglandins and lead to renal decompensation.
As with all NSAIDs, thedrug can increase plasma uric nitrogen and creatinine .
Caution is required in patients receiving diuretic or hypovolaemic therapy as the risk of nephrotoxicity is increased.
As with other prostaglandin synthesis inhibitors, the drug may be associated with adverse events in the renal system which can lead to glomerular nephritis, renal papillary necrosis, nephrotic syndrome and acute renal failure.
In patients with liver function test abnormalities or with a history of liver disease, transaminase levels should be checked periodically, especially with long-term therapy.
As with other NSAIDs, the drugit can cause transient small increases in some liver parameters and also significant increases in SGOT and SGPT liver enzymes. In the event of a significant increase in these parameters, therapy must be stopped.
With the use of ketoprofen, rare cases of jaundice and hepatitis have been reported. Liver and kidney function tests and blood counts should be checked during long-term therapy.
Elderly patients are more prone to decreased renal, cardiovascular or hepatic function.
Cardiovascular and cerebrovascular effects.
As with all NSAIDs, patients with uncontrolled hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial disease and / or cerebrovascular disease should only be treated with ketoprofen lysine salt after careful consideration. Similar considerations should be made before initiating long-term treatment in patients with risk factors for cardiovascular disease (e.g. hypertension, hyperlipidaemia, diabetes mellitus, smoking).
Adequate monitoring and instruction are required in patients with a history of mild to moderate hypertension and / or congestive heart failure as fluid retention and edema have been reported in association with NSAID treatment.
Clinical studies and epidemiological data suggest that the use of some NSAIDs (especially at high doses and in long-term treatments) may be associated with an increased risk of arterial thrombo-embolic events (e.g. myocardial infarction or stroke). There are insufficient data to exclude that ketoprofen is also associated with these risks.
An increased risk of atrial fibrillation associated with the use of NSAIDs has been reported.
Hyperkalaemia may occur, especially in patients with underlying diabetes, renal insufficiency, and / or concomitant treatment with agents promoting hyperkalaemia.
In these circumstances, potassium levels need to be monitored.
Infections.
Like other NSAIDs, in the presence of an infectious disease, the anti-inflammatory, analgesic and antipyretic properties of ketoprofen can mask common symptoms of the progression of the infection, such as fever.
Administer with caution in patients with allergic manifestations or previous allergy.
Respiratory pathologies.
The use of ketoprofen in patients with bronchial asthma or allergic diathesis can cause an asthmatic crisis.
Patients with asthma associated with chronic rhinitis, chronic sinusitis and / or nasal polyposis have a higher risk of allergy to acetylsalicylic acid and / or NSAIDs than the rest of the population. The administration of this drug can cause asthma attacks or bronchospasm, shock and other allergic phenomena especially in subjects allergic to acetylsalicylic acid or NSAIDs.
Due to its effect on the metabolism of arachidonic acid, the administration of OKi to asthmatics and predisposed subjects can cause a crisis of bronchospasm and possibly shock and other allergic phenomena.
Visual disturbances.
In case of visual disturbances, such as blurred vision, treatment should be stopped.
OKi should be administered with caution in patients with haematopoietic disorders, systemic lupus erythematosus or mixed connective tissue disease.
Overdose
Cases of overdose have been reported with doses up to 2.5 g of ketoprofen. In most cases, benign symptoms have been observed and limited to lethargy, somnolence, nausea, vomiting, epigastric pain and abdominal pain, headache, dizziness and diarrhea.
Hypotension, respiratory depression and gastrointestinal bleeding have been observed in severe overdose .
The patient must be immediately transferred to a specialist center to begin symptomatic treatment. There is no specific antidote to ketoprofen overdose. In case of suspected massive overdose, gastric lavage is recommended and symptomatic and supportive treatment instituted to compensate for dehydration, monitor urinary excretion and, if necessary, correct acidosis.
In cases of kidney failure, hemodialysis can be helpful in removing the drug from the body.
Interactions and side effects
Like all medicines, OKi can cause side effects , although not everybody gets them. The most commonly observed adverse events are gastrointestinal in nature .
Several combinations with other drugs are not recommended:
- Other NSAIDs(including selective cyclooxygenase-2 inhibitors) and high-dose salicylates: increased risk of bleeding and gastrointestinal ulceration.
- Anticoagulants(heparin and warfarin): NSAIDs can amplify the effects of anticoagulants such as warfarin; increased risk of bleeding. If concomitant administration cannot be avoided, patients should be carefully monitored.
- Platelet aggregation inhibitors(ticlopidine and clopidogrel): increased risk of bleeding due to inhibition of platelet function and damage to the gastrointestinal mucosa. If co-administration is unavoidable, patients should be closely monitored.
- Lithium: Risk of increased plasma lithium levels, sometimes to toxic levels, due to decreased renal excretion of lithium. If necessary, plasma lithium levels should be closely monitored and the lithium dosage adjusted during and after NSAID therapy.
- Methotrexate: Increased risk of haematological toxicity to methotrexate, especially when administered at high doses (> 15mg / week), possibly related to plasma protein displacement of methotrexate and decreased renal clearance. Allow at least 12 hours between stopping or starting treatment with ketoprofen and administering methotrexate.
- Hydantoins and sulfonamides: the toxic effects of these substances can be increased.
Combination with other drugs requires caution :
- Diuretics: NSAIDs may reduce the effect of diuretics. Patients who are taking diuretics, and among them those who are particularly dehydrated, are at greater risk of developing renal failure secondary to the reduction in renal blood flow caused by the reduction of prostaglandin levels. Such patients should be rehydrated prior to initiation of concomitant therapy and closely monitoring renal function after initiation of treatment.
- Drugs or therapeutic categories that may promote hyperkalaemia(e.g. potassium salts, potassium-sparing diuretics, enzyme converter inhibitors (ACE inhibitors), angiotensin II receptor blockers, NSAIDs, heparins (low molecular weight or not) fractionated), cyclosporine, tacrolimus and trimethoprim). The occurrence of hyperkalaemia may depend on the presence of cofactors. The risk is enhanced when the above-mentioned drugs are administered concomitantly.
- Tenofovir :Concomitant administration of tenofovir disoproxil fumarate and NSAIDs may increase the risk of renal failure.
- ACE inhibitors and angiotensin II antagonists: In patients with impaired renal function (e.g. dehydrated patients and elderly patients), co-administration of an ACE inhibitor or angiotensin II antagonist and agents capable of inhibiting cyclooxygenase may result in further deterioration of this renal function. Therefore the combination should be administered with caution, especially in elderly patients. Patients should be adequately hydrated and monitoring of renal function should be considered after initiation of concomitant therapy.
- Methotrexateat doses below 15 mg / week: increased blood toxicity of methotrexate due to a decrease in its renal clearance due to anti-inflammatory agents in general. During the first weeks of the association, perform a weekly monitoring of the complete blood count. Increase the frequency of monitoring in the presence of even a slight worsening of renal function as well as in the elderly.
- Corticosteroids: increased risk of gastrointestinal ulceration or bleeding.
- Pentoxifylline: increased risk of bleeding. Carry out more frequent clinical checks and monitor bleeding time.
- Sulfonylureas: NSAIDs can increase the hypoglycemic effect of sulfonylureas by displacing them from binding sites to plasma proteins.
- Zidovudine: risk of increased red blood cell toxicity, with severe anemia occurring one week after starting treatment with the NSAID. Check the complete blood count and reticulocyte count one to two weeks after starting treatment with the drug.
- Cardiac glycosides: NSAIDs can exacerbate heart failure, reduce the rate of glomerural filtration and increase cardiac glycoside levels.
With other drugs, the combination should be evaluated :
- Antihypertensivedrugs (beta-blockers, ACE inhibitors, diuretics): NSAIDs can reduce the effect of antihypertensive drugs (NSAIDs inhibit vasodilating prostaglandins).
- Thrombolyticdrugs : increased risk of bleeding.
- Antiplateletagents (ticlopidine and clopidogrel) and selective serotonin reuptake inhibitors (SSRIs): increased risk of gastrointestinal bleeding.
- Probenecid: co-administration of probenecid may markedly reduce the plasma elimination of ketoprofen and consequently the plasma concentrations of ketoprofen may be increased.
- Diphenylhydantoin and sulfonamides: As the plasma protein binding of ketoprofen is high, it may be necessary to reduce the dose of diphenylhydantoin or sulfonamides that should be administered concurrently.
- Ciclosporin, tacrolimus: concomitant treatment with NSAIDs may entail a greater risk of nephrotoxicity, especially in elderly subjects.
- Mifepristone: The effectiveness of the contraceptive method can theoretically be reduced due to the antiprostaglandin properties of NSAIDs, including aspirin.
- Quinolone antibiotics: NSAIDs may increase the risk of seizures associated with the use of quinolone antibiotics.
- Gemeprost: reduced efficacy of gemeprost.
- Intrauterine contraceptive devices(IUDs): the effectiveness of the device may be reduced resulting in pregnancy.
Avoid the simultaneous intake of alcohol.
Ketoprofen is contraindicated in patients with a history of hypersensitivity reactions such as bronchospasm, asthma attacks, rhinitis, urticaria, nasal polyps, angioneurotic edema or other allergic reactions to ketoprofen, acetyl salicylic acid (ASA, aspirin) or other NSAIDs. Severe, rarely fatal, anaphylactic reactions have been observed in these patients.
Pregnancy and breastfeeding
PREGNANCY
The use of ketoprofen during the first and second trimester of pregnancy should be avoided. Ketoprofen is contraindicated during the third trimester of pregnancy.
Inhibition of prostaglandin synthesis can adversely affect pregnancy and / or embryo / fetal development. Results of epidemiological studies suggest an increased risk of miscarriage and cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The risk is believed to increase with dose and duration of therapy.
During the first and second trimester of pregnancy, ketoprofen should not be administered except in strictly necessary cases.
If ketoprofen is used by awoman wishing to become pregnant , or during the first and second trimester of pregnancy, the dose and duration of treatment should be kept as low as possible.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors can:
- expose the fetus to cardiopulmonary toxicity (with premature closure of the arterial duct and pulmonary hypertension);
- renal dysfunction, which can progress to renal failure;
- the mother and the newborn, at the end of pregnancy, to a possible prolongation of the bleeding time, and an antiplatelet effect which can occur even at very low doses;
- inhibition of uterine contractions resulting in delayed or prolonged labor.
The use of the drug near birth can cause haemodynamics alterations of the small circulation of the unborn child with serious consequences for breathing.
FEEDING TIME
There is no information available on the excretion of ketoprofen in human milk . Ketoprofen is not recommended during breastfeeding.
Fertility
The use of NSAIDs may impair female fertility and is not recommended in women planning to become pregnant. The use of OKI, as well as any drug that inhibits prostaglandin synthesis and cyclooxygenase, is not recommended in women who intend to become pregnant.
In women who have fertility problems or who are undergoing fertility investigations, discontinuation of treatment should be considered.
Patients should be advised of the possibility of somnolence, dizziness or convulsions and to avoid driving, operating machinery or carrying out activities requiring vigilance if these symptoms appear.
Notes (validity, storage conditions)
OKi granules for oral solution are valid for 3 years.
OKi suppositories are valid for 3 years; store at a temperature not exceeding 25 ° C.
OKi drops, mouthwash, spray have a validity of 2 years.
OKi solution for injection is valid for 2 years; Protect from heat and store in the original container to keep away from light.
The expiry date indicated on the label refers to the product in intact packaging, correctly stored.
Read the article on Tachipirina
Read the article on Xanax
Questions and answers
IS OKI A MEDICINE USED FOR?
OKi is a non-steroidal anti-inflammatory drug and is used for the symptomatic and short-term treatment of inflammatory conditions including muscle and joint pain, pain in the teeth, pain in the urinary tract and inflammation of the respiratory system, post-operative pain and ear infections.
OKI AND KETOPROFEN, WHAT’S THE DIFFERENCE?
OKi contains Ketoprofen lysine salt, a drug with anti-inflammatory, analgesic and antipyretic activity. Ketoprofen lysine salt is more soluble than acid ketoprofen.
WHAT ARE THE EFFECTS OF OKI?
The Ketoprofen contained in OKi has an anti-inflammatory and analgesic action, mainly due to the inhibition of the activity of cyclooxygenase and therefore of the synthesis of prostaglandins from their precursor, arachidonic acid. This explains its use for the short-term treatment of inflammatory states associated with pain such as headache, toothache, neuralgia, menstrual pain, muscle and bone pain.
IS IT POSSIBLE TO TAKE KETOPROFEN AND IBUPROFEN TOGETHER?
Ketoprofen and ibuprofen are both cyclooxygenase inhibitors and their concomitant intake should be avoided.
WHAT IS THE DIFFERENCE BETWEEN OKI AND TACHIPIRINA?
Tachipirina contains paracetamol and is the drug of choice in pediatric age for the treatment of pain and febrile states since it does not cause gastric injurious side effects, but on the other hand it has no anti-inflammatory action. OKi, which contains ketoprofen, should only be reserved for cases where fever and / or pain are caused by acute inflammatory processes or in cases of chronic inflammation.
