Ketorolac


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular, Intravenous
Postoperative pain
Adult: Short-term management of moderate to severe acute cases: Initially, 10 mg, followed by 10-30 mg 4-6 hourly as needed; may also be given as often as 2 hourly in the initial postoperative period if necessary. Max: 90 mg daily. In patients weighing <50 kg: Dose reduction is required (Max: 60 mg daily). All doses are given via bolus IV inj over at least 15 seconds or slow IM inj. Use the lowest effective dose for the shortest possible duration. Max treatment duration: 2 days. Convert to oral treatment once possible. Dosage recommendations may vary among countries and individual products (refer to detailed product guideline).
Elderly: Short-term management of moderate to severe acute cases: ≥65 years Use the lowest effective dose for the shortest possible duration. Max: 60 mg daily.

Nasal
Acute pain
Adult: Short-term management of moderate to moderately severe cases: 1 spray (15.75 mg) in each nostril 6-8 hourly. Max: 126 mg daily. In patients weighing <50 kg: 1 spray (15.75 mg) in only 1 nostril 6-8 hourly (Max: 63 mg daily). Use the lowest effective dose for the shortest possible duration. Max treatment duration: 5 days (alone or sequential use with oral or IM/IV form).
Elderly: Short-term management of moderate to moderately severe cases: ≥65 years 1 spray (15.75 mg) in only 1 nostril 6-8 hourly. Max: 63 mg daily.

Ophthalmic
Postoperative ocular inflammation
Adult: For cases following cataract surgery: As 0.5% eye drops solution: As prophylaxis and for reduction of inflammation: Instil 1 drop tid starting 24 hours before ocular surgery and continue for up to 3 weeks of postoperative period. Alternatively, as treatment: Instil 1 drop into the affected eye(s) 4 times daily starting 24 hours after ocular surgery and continue for 2 weeks of postoperative period. As 0.45% eye drops solution: Instil 1 drop into the affected eye(s) bid starting 24 hours prior to ocular surgery and until the day of surgery, then continue for 2 weeks of postoperative period. Dosage recommendations may vary among countries and individual products (refer to detailed product guideline).

Ophthalmic
Seasonal allergic conjunctivitis
Adult: For short-term relief of ocular itching: As 0.5% eye drops solution: Instil 1 drop into the affected eye(s) 4 times daily.

Ophthalmic
Postoperative ocular pain
Adult: For cases following cataract surgery: As 0.45% eye drops solution: Instil 1 drop into the affected eye(s) bid starting 24 hours prior to ocular surgery and until the day of surgery, then continue for 2 weeks of postoperative period. For cases following corneal refractive surgery: As 0.4% eye drops solution: Instil 1 drop into the affected eye(s) 4 times daily as necessary for up to 4 days after surgery.

Oral
Postoperative pain
Adult: Short-term management of moderate to severe acute cases: As continuation treatment after parenteral (IM/IV) dosing: Initially, 20 mg as single dose, followed by 10 mg 4-6 hourly as needed. In patients weighing <50 kg: 10 mg 4-6 hourly as needed. Use the lowest effective dose for the shortest possible duration. Max: 40 mg daily. Max duration: 5 days (combined oral and IM/IV use).
Elderly: Short-term management of moderate to severe acute cases: As continuation treatment after parenteral (IM/IV) dosing: ≥65 years 10 mg 4-6 hourly as needed. Max: 40 mg daily. Max duration: 5 days (combined oral and IM/IV use).
Suy thận
Oral:
Mild: As continuation treatment after parenteral (IM/IV) dosing: 10 mg 4-6 hourly as needed. Max: 40 mg daily. Moderate to severe: Contraindicated. Treatment recommendations may vary among countries and individual products (refer to detailed product guideline).

Intramuscular; Intravenous:
Mild: Dose reduction is required. Max: 60 mg daily. Moderate to severe: Contraindicated. Treatment recommendations may vary among countries and individual products (refer to detailed product guideline).

Nasal:
1 spray (15.75 mg) in only 1 nostril 6-8 hourly. Max: 63 mg daily. Advanced renal impairment: Contraindicated.
Suy gan
Intramuscular; Intravenous:
Severe: Contraindicated.
Tương kỵ
May form precipitation with morphine, pethidine, promethazine, or hydroxyzine when mixed in small volume (e.g. in a syringe).
Chống chỉ định
Hypersensitivity to ketorolac, aspirin, or other NSAIDs. History of bronchospasm, asthma, rhinitis, urticaria or other allergic-type reactions associated with aspirin or NSAID therapy; active or history of peptic ulcer disease or gastrointestinal haemorrhage (≥2 distinct episodes of proven ulceration or bleeding), recent gastrointestinal bleeding or perforation; confirmed or suspected cerebrovascular bleeding, haemorrhagic diathesis, incomplete haemostasis, high risk of bleeding, severe heart failure. Patient at risk of renal failure due to volume depletion or dehydration. Use in the setting of CABG surgery, during labour and delivery, or as a prophylactic analgesic prior to any major surgery. Patient currently receiving aspirin, anticoagulants, or other NSAIDs. Moderate to severe or advanced renal impairment; severe hepatic impairment (IV/IM). Pregnancy (3rd trimester). Concomitant use with probenecid, lithium, or pentoxifylline.
Thận trọng
Patient with history of inflammatory bowel disease (e.g. ulcerative colitis, Crohn's disease), risk factors for gastrointestinal bleeding (e.g. smoking, alcohol use), hypertension, oedema, diabetes mellitus, SLE, mixed connective tissue disorders, other forms of asthma, recent MI, history of kidney disease, low body weight (<50 kg). Debilitated patients. Mild renal and hepatic impairment. Elderly. Pregnancy (1st and 2nd trimester) and lactation. Concomitant use of oral corticosteroids, SSRIs, other antiplatelets, diuretics, or ACE inhibitors. Ophthalmic: Patient with complicated ocular surgery or repeat ocular surgery (within a short timeframe), corneal epithelial defects, corneal denervation, ocular surface disease (e.g. dry eye syndrome), rheumatoid arthritis, predisposition to bleeding.
Tác dụng không mong muốn
Significant: Hypersensitivity reactions (e.g. bronchospasm); renal papillary necrosis (prolonged use), acute renal failure, interstitial nephritis, nephrotic syndrome, new onset or exacerbation of hypertension, Na and fluid retention, hyperkalaemia, prolonged bleeding time, elevated liver enzymes, anaemia. Ophthalmic: Keratitis, corneal thinning, erosion, ulceration, or perforation; delayed healing time, exacerbation of asthma.
Blood and lymphatic system disorders: Purpura, thrombocytopenia. Rarely, agranulocytosis.
Ear and labyrinth disorders: Tinnitus, hearing loss, vertigo.
Eye disorders: Ophthalmic: Blurred vision, increased intraocular pressure, conjunctival hyperaemia, lacrimation, corneal infiltrates, iritis, retinal haemorrhage, cystoid macular oedema, eye or eyelid oedema; eye inflammation or infection; transient stinging and burning (on instillation).
Gastrointestinal disorders: Abdominal pain or discomfort, taste abnormality, dyspepsia, nausea, flatulence, constipation, diarrhoea, heartburn, vomiting, stomatitis, gastrointestinal fullness.
General disorders and administration site conditions: Inj site reactions (IV/IM).
Nervous system disorders: Headache, drowsiness, dizziness, paraesthesia.
Renal and urinary disorders: Increased urinary frequency, oliguria, urinary retention.
Respiratory, thoracic and mediastinal disorders: Nasal: Nasal discomfort, rhinalgia, throat irritation, rhinitis.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Potentially Fatal: Gastrointestinal bleeding, ulceration, or perforation; CV thrombotic events (e.g. MI, stroke), anaphylactoid reactions, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms. Rarely, severe hepatic reactions (e.g. jaundice, fulminant hepatitis, hepatic necrosis or failure).
IM/IV/Ophth/Parenteral/PO: C; Nasal: C (prior to 30 weeks gestation), D (starting at 30 weeks gestation); 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 drowsiness, dizziness, and blurred vision, if affected, do not drive or operate machinery. Ophthalmic: Remove contact lenses prior to use and reinsert them after at least 15 minutes.
Chỉ số theo dõi
Monitor response (range of motion, grip strength, pain, mobility, inflammation), renal function (serum creatinine, BUN, urine output), LFTs, CBC and platelets, chemistry profile; blood pressure (prior to initiation and periodically during use). Observe for signs and symptoms of bleeding, gastrointestinal effects (e.g. bleeding, abdominal pain), allergic reactions, hepatotoxicity, weight gain.
Quá liều
Symptoms: Lethargy, drowsiness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, headache, disorientation, excitation, drowsiness, fainting, tinnitus, and anaphylactoid reactions. Rarely, diarrhoea, occasional convulsions, hypertension, acute renal failure, respiratory depression, and coma. Management: Symptomatic and supportive treatment. May consider emesis and/or administration of activated charcoal (60-100 g in adults; 1-2 g/kg in children) and/or osmotic cathartic within 4 hours of ingestion in patients with symptoms or after a large oral overdose (5-10 times the normal dose). Administer IV diazepam in case of frequent or prolonged convulsions. Ensure good urine output of the patient. Closely monitor renal and hepatic function.
Tương tác
May increase the risk of bleeding with oral corticosteroids, SSRIs, and other antiplatelet agents. May increase the risk of renal impairment with ACE inhibitors, angiotensin II receptor blockers (ARBs), ciclosporin, and diuretics. May diminish the effects of ACE inhibitors, ARBs, diuretics, or β-blockers (e.g. propranolol). Increased risk of seizure with antiepileptic drugs (e.g. phenytoin, carbamazepine). Hallucinations may occur when used with psychoactive drugs (e.g. fluoxetine, tiotixene, alprazolam). Ketorolac IV/IM may enhance the adverse effect (particularly episodes of apnoea) of nondepolarising muscle relaxants. May increase the serum concentration of methotrexate and digoxin.
Potentially Fatal: Increased risk of serious NSAID-related adverse events with aspirin or other NSAIDs. Increased plasma levels and reduced clearance with probenecid. May increase the risk of bleeding with pentoxifylline and anticoagulants (e.g. heparin, warfarin). Reduces clearance and elevates the plasma levels of lithium, which may increase lithium toxicity.
Tương tác với thức ăn
May decrease peak concentrations and delay time to peak plasma concentrations (by approx 1 hour) with high-fat food.
Tác dụng
Description: Ketorolac is a prototypical NSAID with antipyretic and analgesic properties, it is a racemic mixture of (-)S- and (+)R-enantiomers, with the S-form as the biologically active form. It reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, resulting in decreased formation of prostaglandin precursors. Administration via the ophthalmic route decreases the levels of prostaglandin E2 in the aqueous humour.
Onset: Analgesia: Approx 30 minutes; within 20 minutes (nasal). Peak effect: Approx 2-3 hours (oral); 1-2 hours (IV/IM).
Duration: Analgesia: 4-6 hours.
Pharmacokinetics:
Absorption: Well absorbed (oral); rapidly and completely absorbed (IM). Bioavailability: 100% (oral, IM); approx 60% (nasal; relative to IM route). Decreased peak and delayed time to peak plasma concentrations with high-fat meal (oral). Time to peak plasma concentrations: Approx 45 minutes (oral); 1-3 minutes (IV); approx 30-45 minutes (IM); 0.75 hours (nasal).
Distribution: Poor penetration into the CSF. Distributed mainly in the nasal cavity and pharynx following nasal administration, with <2% in the oesophagus and stomach and negligible distribution in the lungs (<5%). Crosses the placenta; enters breast milk (small amounts). Volume of distribution: Approx 13 L (nasal). Plasma protein binding: 99%.
Metabolism: Extensively metabolised in the liver via glucuronic acid conjugation and hydroxylation.
Excretion: Via urine (approx 92%; approx 40% as metabolites, approx 60% as unchanged drug); faeces (approx 6%). Elimination half-life: Approx 5 hours; range: 2-9 hours ([-]S-enantiomer: approx 2.5 hours, [+]R-enantiomer: approx 5 hours).
Đặc tính

Chemical Structure Image
Ketorolac

Source: National Center for Biotechnology Information. PubChem Database. Ketorolac, CID=3826, https://pubchem.ncbi.nlm.nih.gov/compound/Ketorolac (accessed on Jan. 21, 2020)

Bảo quản
Tab: Store between 20-25°C. Protect from excessive humidity and light. IV or IM inj/ophthalmic drops: Store between 15-30°C. Protect from light. Nasal spray: Store unopened bottle between 2-8°C. Do not freeze. Protect from light. Once opened, store between 15-30°C. Protect from direct sunlight.
Phân loại MIMS
Thuốc kháng viêm không steroid / Thuốc giảm sung huyết, gây tê, kháng viêm trong Nhãn khoa
Phân loại ATC
S01BC05 - ketorolac ; Belongs to the class of non-steroidal antiinflammatory agents. Used in the treatment of inflammation of the eye.
M01AB15 - ketorolac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.
Tài liệu tham khảo
Acular Ophthalmic Solution 0.5% (Allergan Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 24/09/2021.

Acuvail Ophthalmic Solution 0.45% (Allergan Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 24/09/2021.

Allergan New Zealand Ltd. Acular 5 mg/mL Eye Drops data sheet May 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 06/09/2021.

Anon. Ketorolac (EENT). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/09/2021.

Anon. Ketorolac (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2021.

Anon. Ketorolac (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2021.

Anon. Ketorolac (Systemic). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/09/2021.

Anon. Ketorolac (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2021.

Buckingham R (ed). Ketorolac Trometamol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2021.

Fresenius Kabi New Zealand Limited. Ketorolac Kabi 30 mg/1 mL Solution for Intramuscular Injection data sheet 20 April 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 06/09/2021.

Joint Formulary Committee. Ketorolac Trometamol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2021.

Keto Film Coated Tablet (Y.S.P. Industries [M] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 12/10/2021.

Ketorolac Trometamol 0.5% w/v Eye Drops, Solution (Brown & Burk UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 06/09/2021.

Ketorolac Trometamol 10 mg/mL Solution for Injection (Baxter Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 06/09/2021.

Ketorolac Tromethamine Injection (Hospira Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/09/2021.

Ketorolac Tromethamine Ophthalmic Solution 0.4% (Aurobindo Pharma USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/09/2021.

Ketorolac Tromethamine Solution/Drops 0.45% (Akorn, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/10/2021.

Ketorolac Tromethamine Solution/Drops 0.5% (Sun Pharmaceutical Industries, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/10/2021.

Ketorolac Tromethamine Tablet, Film Coated (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/09/2021.

Sprix Spray, Metered (Zyla Life Sciences U.S. Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/10/2021.

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