Dexketoprofen

Intramuscular, Intravenous
Moderate to severe acute pain

Oral
Mild to moderate pain

Oral:

CrCl (mL/min)	Dosage
≤59	Contraindicated.
60-89	Initiate at the lower end of the dosing range. Max initial dose: 50 mg daily.

Intravenous/Intramuscular:

CrCl (mL/min)	Dosage
≤59	Contraindicated.
60-89	50 mg total daily dose.

Oral:
Mild to moderate: Initiate at the lower end of the dosing range. Max initial dose: 50 mg daily. Severe: Contraindicated.

Intravenous/Intramuscular:
Mild to moderate: 50 mg total daily dose. Severe: Contraindicated.

Should be taken on an empty stomach. Take 30 min before meals, especially for quick relief of acute pain.

Solution for IV infusion: Dilute the contents of the 2 mL amp (labelled as containing 50 mg) with 30-100 mL of NaCl 0.9%, dextrose 5% in water, or Lactated Ringer's solution.

Syringe: May be precipitated with solutions of dopamine, promethazine, pentazocine, pethidine or hydroxyzine. Diluted solution for infusion: Incompatible with promethazine or pentazocine.

Hypersensitivity to dexketoprofen, or any other NSAIDs. History of asthma attacks, bronchospasm, angioneurotic oedema, acute rhinitis, nasal polyps, urticaria, or other allergic-type reaction after taking aspirin or other NSAIDs; known photoallergic or phototoxic reactions during therapy with ketoprofen or fibrates; active or suspected peptic ulcer or haemorrhage, history of gastrointestinal bleeding, ulceration, or perforation, including cases related to previous NSAID therapy; other active bleedings or bleeding disorders, haemorrhagic diathesis and other coagulation disorders, chronic dyspepsia, Crohn's disease or ulcerative colitis, varicella infection, severe heart failure; severe dehydration due to vomiting, diarrhoea or insufficient fluid intake. Moderate to severe renal (CrCl ≤59 mL/min) and severe hepatic (Child-Pugh score 10-15) impairment. Pregnancy (3rd trimester) and lactation.

Patient with history of gastrointestinal disease (e.g. ulcerative colitis, Crohn's disease) or toxicity; history of hypertension, uncontrolled hypertension; mild to moderate heart failure; ischaemic heart disease, peripheral arterial disease, cerebrovascular disease, risk factors for CV disease (e.g. hyperlipidaemia, diabetes mellitus, smoking), haematopoietic disorders, SLE, mixed connective tissue disease, congenital disorder of porphyrin metabolism (e.g. acute intermittent porphyria); asthma combined with chronic rhinitis, chronic sinusitis and/or nasal polyposis. Patient who underwent major surgery. Dehydrated and debilitated patients. May mask signs and symptoms of infections. Not recommended for treatment of perioperative pain in the setting of CABG. Not intended for long-term use. Mild renal (CrCl 60-89 mL/min) and mild to moderate hepatic impairment. Elderly. Pregnancy (1st-2nd trimester).

Significant: Glomerular nephritis, interstitial nephritis, renal papillary necrosis, nephrotic syndrome, acute renal failure; increased ALT or AST; risk for arterial thrombotic events (e.g. MI or stroke); risk for asthma attacks or bronchospasm; fluid retention, oedema, decreased platelet adhesion and aggregation, prolonged bleeding time, new-onset or worsening of hypertension. Rarely, severe acute hypersensitivity reactions (e.g. anaphylactic shock).
Cardiac disorders: Palpitations.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea, vomiting, dyspepsia, gastritis, constipation, flatulence, dry mouth.
General disorders and administration site conditions: Fatigue, asthenia, rigors, malaise; inj site reaction (e.g. pain, inflammation, haemorrhage, bruising).
Nervous system disorders: Headache, dizziness, somnolence.
Psychiatric disorders: Insomnia, anxiety.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Flushing.
Potentially Fatal: Gastrointestinal bleeding, ulceration or perforation. Very rarely, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

IM/IV/Parenteral/PO: Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)

This drug may cause dizziness, visual disturbances or drowsiness, if affected, do not drive or operate machinery.

Monitor CBC, occult blood loss, hepatic (periodically) and renal function; blood pressure.

Symptoms: Anorexia, abdominal pain, vomiting, headache, somnolence, vertigo, disorientation. Management: Symptomatic treatment. Administer activated charcoal if more than 5 mg/kg has been ingested within an hour. May perform dialysis.

Increases plasma concentrations of lithium, methotrexate and cardiac glycosides. May increase the toxic effects of hydantoins and sulfonamides. May decrease the effect of diuretics and antihypertensive drugs (e.g. β-blockers). Increased risk of bleeding with pentoxifylline and thrombolytics. Risk of increased red cell line toxicity with zidovudine. May increase the hypoglycaemic effect of sulfonylureas. May enhance the nephrotoxic effect with ACE inhibitors, ciclosporin and tacrolimus. Probenecid may increase the plasma concentrations of dexketoprofen. May alter the efficacy of mifepristone. May increase the risk of developing convulsions with quinolone antibiotics. Concomitant use with tenofovir may result in increased plasma urea nitrogen and creatinine. May increase the risk of gastrointestinal toxicity with deferasirox. Dexketoprofen may decrease pemetrexed elimination. Increased risk of hyperkalaemia with K-sparing diuretics.
Potentially Fatal: Increased risk of gastrointestinal ulcers and bleeding with other NSAIDs (including COX-2 selective inhibitors), corticosteroids, SSRIs, anticoagulants (e.g. warfarin, heparin), and antiplatelet agents (e.g. aspirin).

Delayed absorption with food. May enhance the adverse effects with alcohol.

May result in false-positive aldosterone/renin ratio (ARR).

Description:
Mechanism of Action: Dexketoprofen, the S-(+) enantiomer of ketoprofen, is an analgesic, anti-inflammatory and antipyretic agent. It reduces the synthesis of prostaglandin by inhibiting cyclooxygenase pathway which also affects other inflammation mediators (e.g. kinins), causing further increase in anti-inflammatory activity.
Duration: Oral: 4-6 hours. IM or IV: Approx 8 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Delayed absorption with food. Time to peak plasma concentration: 15-60 minutes (tab); 15-20 minutes (granules for oral solution); 10-45 minutes (IM).
Distribution: Volume of distribution: <0.25 L/kg. Plasma protein binding: 99%.
Metabolism: Metabolised in the liver via glucuronidation.
Excretion: Via urine (primarily as metabolites). Elimination half-life: 1-2.7 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 667550, Dexketoprofen. https://pubchem.ncbi.nlm.nih.gov/compound/Dexketoprofen. Accessed Apr. 27, 2023.

Store below 30°C. Protect from light.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AE17 - dexketoprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.

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