Dexketoprofen


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular, Intravenous
Moderate to severe acute pain
Adult: For short-term treatment (≤2 days): 50 mg 8-12 hourly via slow IV inj over at least 15 seconds or IV infusion over 10-30 minutes, or via deep IM inj. Doses may be repeated with a minimum interval of 6 hours if needed. Max: 150 mg daily. Switch to oral treatment when possible.

Oral
Mild to moderate pain
Adult: 12.5 mg 4-6 hourly or 25 mg 8 hourly. Max: 75 mg daily.
Elderly: Initiate at the lower end of the dosing range with total dose not exceeding 50 mg daily. May increase dose within usual adult dose range if tolerated.
Suy thận
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.
Suy gan
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.
Cách dùng
Should be taken on an empty stomach. Take 30 min before meals, especially for quick relief of acute pain.
Hướng dẫn pha thuốc
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.
Tương kỵ
Syringe: May be precipitated with solutions of dopamine, promethazine, pentazocine, pethidine or hydroxyzine. Diluted solution for infusion: Incompatible with promethazine or pentazocine.
Chống chỉ định
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.
Thận trọng
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).
Tác dụng không mong muốn
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.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, visual disturbances or drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor CBC, occult blood loss, hepatic (periodically) and renal function; blood pressure.
Quá liều
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.
Tương tác
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).
Tương tác với thức ăn
Delayed absorption with food. May enhance the adverse effects with alcohol.
Ảnh hưởng đến kết quả xét nghiệm
May result in false-positive aldosterone/renin ratio (ARR).
Tác dụng
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.
Đặc tính

Chemical Structure Image
Dexketoprofen_01

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.

Bảo quản
Store below 30°C. Protect from light.
Phân loại MIMS
Thuốc kháng viêm không steroid
Phân loại ATC
M01AE17 - dexketoprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.
Tài liệu tham khảo
Anon. Dexketoprofen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/03/2023.

Buckingham R (ed). Ketoprofen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/03/2023.

Joint Formulary Committee. Dexketoprofen. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/03/2023.

Keral 25 mg Film-coated Tablets (Menarini International O.L.S.A.). MHRA. https://products.mhra.gov.uk. Accessed 13/03/2023.

Keral 25 mg Oral Solution in Sachet (Menarini International O.L.S.A.). MHRA. https://products.mhra.gov.uk. Accessed 13/03/2023.

Ketesse 25 mg Film Coated Tablet (A. Menarini Singapore Pte. Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/03/2023.

Ketesse 25 mg Granules for Oral Solution (A. Menarini Singapore Pte. Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/03/2023.

Ketesse 50 mg/2 mL Solution for Injection or Concentrate for Solution for Infusion (A. Menarini Singapore Pte. Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/03/2023.

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