Dexketoprofen Trometamol

TRADE / BRAND  NAMES OF DEXKETOPROFEN  IN KENYA

Infen®, Emcure Pharmaceuticals Ltd

Ketesse®, Menarini International Operations Luxembourg S.A

 

Dexketoprofen Chemical Structure: Dexketoprofen in Kenya
Dexketoprofen Chemical Structure

MODE OF ACTION

The mechanism of action of non-steroidal antiinflammatory drugs is related to the reduction of prostaglandin synthesis by the inhibition of cyclooxygenase pathway. Specifically, there is an inhibition of the transformation of arachidonic acid into cyclic endoperoxides, PGG2 and PGH2, which produce prostaglandins PGE1, PGE2, PGF2α and PGD2 and also prostacyclin PGI2 and thromboxanes (TxA2 and TxB2). Furthermore, the inhibition of the synthesis of prostaglandins could affect other inflammation mediators such as kinins, causing an indirect action which would be additional to the direct action.

INDICATIONS

Symptomatic treatment of pain of mild to moderate intensity, such as musculo-skeletal pain, dysmenorrhoea, dental pain.

DOSAGE AND ADMINISTRATION

Adults

According to the nature and severity of pain, the recommended dosage is generally 12.5 mg every 4-6 hours or 25 mg every 8 hours. The total daily dose should not exceed 75 mg.

Undesirable effects may be minimised by using the lowest effective dose for the shortest duration necessary to control symptoms .

Dexketoprofen is not intended for long term use and the treatment must be limited to the symptomatic period.

Elderly

In elderly patients it is recommended to start the therapy at the lower end of the dosage range (50 mg total daily dose). The dosage may be increased to that recommended for the general population only after good general tolerance has been ascertained.

Hepatic impairment

Patients with mild to moderate hepatic dysfunction should start therapy at reduced doses (50 mg total daily dose) and be closely monitored.Dexketoprofen should not be used in patients with severe hepatic dysfunction.

Renal impairment

The initial dosage should be reduced to 50 mg total daily dose in patients with mildly impaired renal function (creatinine clearance 60 – 89 ml / min) (see section 4.4). Keral tablets should not be used in patients with moderate to severe renal dysfunction (creatinine clearance ≤ 59 ml / min).

Paediatric Population

Dexketoprofen has not been studied in children and adolescent. Therefore the safety and efficacy in children and adolescents have not been established and the product should not be used in children and adolescent.

CONTRAINDICATIONS

Dexketoprofen must not be administered in the following cases:

  • patients hypersensitive to the active substance, to any other NSAID, or to any of the excipients
  • patients in whom substances with a similar action (e.g. acetylsalicylic acid, or other NSAIDs) precipitate attacks of asthma, bronchospasm, acute rhinitis, or cause nasal polyps, urticaria or angioneurotic oedema.
  • known photoallergic or phototoxic reactions during treatment with ketoprofen or fibrates
  • patients with history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • patients with active peptic ulcer/gastrointestinal haemorrhage or any history of gastrointestinal bleeding, ulceration or perforation
  • patients with chronic dyspepsia.
  • patients who have other active bleedings or bleeding disorders.
  • patients with Crohn’s disease or ulcerative colitis.
  • patients with severe heart failure.
  • patients with moderate to severe renal dysfunction (creatinine clearance ≤59 ml/min).
  • patients with severely impaired hepatic function (Child-Pugh score 10 – 15).
  • patients with haemorrhagic diathesis and other coagulation disorders.
  • patients with severe dehydration (caused by vomiting, diarrhoea or insufficient fluid intake)
  • during the third trimester of pregnancy and lactation period

DRUG INTERACTIONS

The following interactions apply to non-steroidal antiinflammatory drugs (NSAIDs) in general:

Inadvisable combinations:

  • Other NSAIDs (including cyclooxygenase-2 selective inhibitors) and high doses of salicylates (≥ 3 g/day): administration of several NSAIDs together may increase the risk of gastrointestinal ulcers and bleeding, via a synergistic effect.
  • Anticoagulants: NSAIDs may enhance the effects of anti-coagulants, such as warfarin , due to the high plasma protein binding of dexketoprofen and the inhibition of platelet function and damage to the gastroduodenal mucosa. If the combination cannot be avoided, close clinical observation and monitoring of laboratory values should be carried out.
  • Heparins: increased risk of haemorrhage (due to the inhibition of platelet function and damage to the gastroduodenal mucosa). If the combination cannot be avoided, close clinical observation and monitoring of laboratory values should be carried out.
  • Corticosteroids: there is an increased risk of gastrointestinal ulceration or bleeding .
  • Lithium (described with several NSAIDs): NSAIDs increase blood lithium levels, which may reach toxic values (decreased renal excretion of lithium). This parameter therefore requires monitoring during the initiation, adjustment and withdrawal of treatment with dexketoprofen.
  • Methotrexate, used at high doses of 15 mg/week or more: increased haematological toxicity of methotrexate via a decrease in its renal clearance by antiinflammatory agents in general.
  • Hydantoines and sulphonamides: the toxic effects of these substances may be increased.

Combinations requiring precautions:

  • Diuretics, ACE inhibitors, antibacterial aminoglycosides and angiotensin II receptor antagonists: Dexketoprofen may reduce the effect of diuretics and antihypertensive drugs. In some patients with compromised renal function (e. g. dehydrated patients or elderly patients with compromised renal function), the coadministration of agents that inhibit cyclo-oxygenase and ACE inhibitors, angiotensin II receptor antagonists or antibacterial aminoglycosides may result in further deterioration of renal function, which is usually reversible. In case of combined prescription of dexketoprofen and a diuretic, it is essential to ensure that the patient is adequately hydrated and to monitor renal function at the start of the treatment.
  • Methotrexate, used at low doses, less than 15 mg/week: increased haematological toxicity of methotrexate via a decrease in its renal clearance by antiinflammatory agents in general. Weekly monitoring of blood count during the first weeks of the combination. Increased surveillance in the presence of even mildly impaired renal function, as well as in the elderly.
  • Pentoxyfilline: increased risk of bleeding. Increase clinical monitoring and check bleeding time more often.
  • Zidovudine: risk of increased red cell line toxicity via action on reticulocytes, with severe anaemia occurring one week after the NSAID is started. Check complete blood count and reticulocyte count one to two weeks after starting treatment with the NSAID.
  • Sulfonylureas: NSAIDs can increase the hypoglycaemic effect of sulfonylureas by displacement from plasma protein binding sites.

Combinations needing to be taken into account:

  • Beta-blockers: treatment with a NSAID may decrease their antihypertensive effect via inhibition of prostaglandin synthesis.
  • Cyclosporin and tacrolimus: nephrotoxicity may be enhanced by NSAIDs via renal prostaglandin mediated effects. During combination therapy, renal function has to be measured.
  • Thrombolytics: increased risk of bleeding.
  • Anti-platelet agents and selective serotonin reuptake inhibitors (SSRIs): increased risk of gastrointestinal bleeding .
  • Probenecid: plasma concentrations of dexketoprofen may be increased; this interaction can be due to an inhibitory mechanism at the site of renal tubular secretion and of glucuronoconjugation and requires adjustment of the dose of dexketoprofen.
  • Cardiac glycosides: NSAIDs may increase plasma glycoside concentration.
  • Mifepristone: There is a theoretical risk that prostaglandin synthetase inhibitors may alter the efficacy of mifepristone. Limited evidence suggests that co-administration of NSAIDs on the day of prostaglandin administration does not adversely influence the effects of mifepristone or the prostaglandin on cervical ripening or uterine contractility and does not reduce the clinical efficacy of medical termination of pregnancy.
  • Quinolone Antibiotics: Animal data indicate that high doses of quinolones in combination with NSAIDs can increase the risk of developing convulsions.
  • Tenofovir: concomitant use with NSAID can increase plasma urea nitrogen and creatinine, renal function should be monitored in order to control a potential synergic influence on renal function.
  • Deferasirox: concomitant use with NSAIDs can increase the risk of gastrointestinal toxicity. Close clinical monitoring is required when deferasirox is combined with these substances.
  • Pemetrexed: concomitant use with NSAIDs may decrease pemetrexed elimination, therefore caution should be made when administering higher doses of NSAIDs. In patients with mild to moderate renal insufficiency (creatinine clearance from 45 to 79 ml/min), the concomitant administration of pemetrexed with NSAIDs doses should be avoided for 2 days before and 2 days following pemetrexed administration.

ADVERSE EFFECTS

SYSTEM ORGAN CLASS

Common

(≥1/100 to <1/10)

Uncommon

(≥1/1,000 to <1/100)

Rare

(≥1/10,000 to <1/1,000)

Very rare

(<1/10,000)

Blood and lymphatic system disordersNeutropenia, thrombocytopenia
Immune system disordersLaryngeal oedemaAnaphylactic reaction, including anaphylactic shock
Metabolism and nutrition disordersAnorexia
Psychiatric disordersInsomnia, anxiety
Nervous system disordersHeadache, dizziness, somnolenceParaesthesia, syncope
Eye disordersBlurred vision
Ear and labyrinth disordersVertigoTinnitus
Cardiac disordersPalpitationsTachycardia
Vascular disordersFlushingHypertensionHypotension
Respiratory, thoracic and mediastinal disordersBradypnoeaBronchospasm, dyspnoea
Gastrointestinal disordersNausea and/or vomiting, abdominal pain, diarrhoea, dyspepsia.Gastritis, constipation, dry mouth, flatulencePeptic ulcer, peptic ulcer haemorrhage or peptic ulcer perforation (see section 4.4)Pancreatitis
Hepatobiliary disordersHepatocellular injury
Skin and subcutaneous tissue disordersRashUrticaria, acne, sweating increasedStevens Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), angioedema, facial oedema, photosensitivity reaction, pruritus
Musculoskeletal and connective tissue disordersBack pain
Renal and urinary disordersAcute renal failure, PolyuriaNephritis or nephrotic syndrome
Reproductive system and breast disordersMenstrual disorder, prostatic disorder
General disorders and administration site conditionsFatigue, pain, asthenia, rigors, malaisePeripheral oedema
InvestigationsLiver function test abnormal
Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:

Dexketoprofen in Kenya
Dexketoprofen in Kenya
Dexketoprofen in Kenya
Dexketoprofen in Kenya
Dexketoprofen in Kenya
Dexketoprofen in Kenya
Dexketoprofen in Kenya

Clinical | Pharmacokinetic data

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