Midazolam


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular, Intravenous
Premedication in surgery
Adult: 0.07-0.1 mg/kg (approx 5 mg) via IM inj, given 20-60 minutes before surgery. Alternatively, 1-2 mg via IV inj, repeated if necessary, given 5-30 minutes before surgery.
Elderly: 0.025-0.05 mg/kg given approx 20-60 minutes before surgery via IM inj. Alternatively, 0.5 mg given IV 5-30 minutes before procedure, repeated slowly if required.
Child: 1-15 years 0.08-0.2 mg/kg via IM inj given 15-30 minutes before surgery.

Intravenous
Sedation
Adult: Conscious sedation for procedures; for dental and minor surgical procedures: Initially, 2-2.5 mg given at a rate of 2 mg/minute 5-10 minutes before procedure, with increments of 0.5-1 mg at intervals of at least 2 minutes if required until the desired endpoint is achieved.
Elderly: Initially, 0.5-1 mg at a max rate of 2 mg/minute, 5-10 minutes before procedure, with increments of 0.5-1 mg if required. Max total dose: 3.5 mg or until the desired endpoint is achieved.
Child: 6 months to 5 years Initially, 0.05-0.1 mg/kg, up to 0.6 mg/kg if necessary. Max: 6 mg; 6-12 years Initially, 0.025-0.05 mg/kg, up to 0.4 mg/kg if necessary. Max: 10 mg; >12 years Same as adult dose. Initial doses are given over 2-3 minutes, 5-10 minutes before procedure, with an additional interval of 2-5 minutes before giving further doses.

Intravenous
Sedation in critical care
Adult: Loading dose: 0.03-0.3 mg/kg, may be given in increments of 1-2.5 mg, injected slowly over 20-30 seconds, allowing 2 minutes between each dose. Maintenance: 0.03-0.2 mg/kg/hour. Patient with hypovolaemia, vasoconstriction or hypothermia: Reduce or omit loading dose and reduce maintenance dose.
Elderly: Dose reduction may be necessary.
Child: ≤6 months 0.06 mg/kg/hour via continuous IV infusion; >6 months Loading dose: 0.05-0.2 mg/kg via slow IV inj over 2-3 minutes. Maintenance: 0.06-0.12 mg/kg/hour via continuous IV infusion. Doses are titrated slowly and adjusted based on clinical response.

Intravenous
Induction of anaesthesia
Adult: Premedicated patient: 0.15-0.2 mg/kg via slow IV inj. Non-premedicated patient: 0.3-0.35 mg/kg via slow IV inj. For resistant cases, a total dose up to 0.6 mg/kg may be given. For sedation in combined anaesthesia: 0.03-0.1 mg/kg by inj repeated as required or by infusion in a dose of 0.03-0.1 mg/kg/hour.
Elderly: >60 years Premedicated patient: 0.05-0.15 mg/kg. Non-premedicated patient: 0.15-0.3 mg/kg.

Oral
Seizures
Child: 3-6 months Hospital setting: 2.5 mg; >6 months to <1 year 2.5 mg; 1->5 years 5 mg; 5->10 years 7.5 mg; 10->18 years 10 mg. Doses are given as single dose.

Oral
Preoperative sedation
Child: 6 months to 16 years 0.25-1 mg/kg as single dose 15-30 minutes prior to procedure, depending on patient status and desired effect. Max: 20 mg.

Oral
Short-term management of insomnia
Adult: 7.5-15 mg at night. Max: 15 mg.
Elderly: 7.5 mg at night.
Suy thận
Oral:
Short-term management of insomnia:
Dose reduction may be necessary.
Suy gan
Oral:
Preoperative sedation; Short-term management of insomnia; Seizures:
Severe: Contraindicated.

Intravenous:
Sedation; Induction of anaesthesia; Sedation in critical care:
Dose reduction may be necessary.

Intravenous/Intramuscular:
Premedication in surgery:
Dose reduction may be necessary.
Cách dùng
May be taken with or without food.
Tương kỵ
IV: Visual incompatibility by immediate formation of white precipitate with dimenhydrinate, pentobarbital Na, perphenazine, prochlorperazine edisilate, ranitidine hydrochloride, furosemide, thiopental and parenteral nutrition solutions.
Chống chỉ định
Acute narrow-angle glaucoma, severe respiratory insufficiency, severe respiratory failure, acute respiratory depression, myasthenia gravis, sleep apnoea syndrome; severe hepatic impairment (oral). Concomitant use with CYP3A4 inhibitors.
Thận trọng
Patient with uncompensated acute illnesses (e.g. severe fluid or electrolyte disturbances), CV disease (e.g. heart failure), respiratory disease (e.g. COPD), history of alcohol or drug abuse; at risk of falls; obese, debilitated. Avoid abrupt withdrawal. Renal and hepatic impairment. Neonates, children, and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Anterograde amnesia, CNS depression, hypotension, paradoxical reactions (e.g. hyperactive or aggressive behaviour), suicidal ideation, withdrawal symptoms.
Cardiac disorders: Bradycardia, tachycardia.
Gastrointestinal disorders: Nausea, vomiting, constipation, dry mouth, hiccups.
General disorders and administration site conditions: Fatigue, inj site reactions (e.g. erythema, pain, phlebitis, thrombosis).
Injury, poisoning and procedural complications: Falls, fractures.
Musculoskeletal and connective tissue disorders: Muscle weakness.
Nervous system disorders: Sedation (prolonged and post-operative), decreased alertness, somnolence, headache, dizziness, drowsiness, ataxia.
Psychiatric disorders: Confusion, euphoric mood, depression, hallucinations, physical drug dependence, withdrawal syndrome.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, laryngospasm, bronchospasm, cough.
Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus.
Potentially Fatal: Cardiorespiratory effects (e.g. respiratory depression, respiratory arrest, apnoea, cardiac arrest).
Buccal/IM/IV/Nasal/Parenteral/PO: D
Thông tin tư vấn bệnh nhân
This drug may cause sedation, amnesia, impaired concentration and muscular function, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor the level of sedation, respiratory rate, heart rate, blood pressure, oxygen saturation (e.g. pulse oximetry), vital signs.
Quá liều
Symptoms: Sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma and deleterious effects on vital signs. Management: Symptomatic and supportive treatment. Monitor respiration, pulse rate, blood pressure and hepatic function. Maintain adequate airway and support of ventilation, including administration of oxygen. IV fluid therapy, repositioning, judicious use of appropriate vasopressors may be done in case of hypotension. Gastrointestinal decontamination (e.g. lavage, activated charcoal) may be considered within 1-2 hours after ingestion or once the patient’s airway is secured. Flumazenil may be given as an antidote.
Tương tác
Decreased plasma concentration with CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin). Potentiate the action of antipsychotics, barbiturates, propofol, ketamine, sedative antidepressants, antihistamines and centrally acting antihypertensive drugs.
Potentially Fatal: Increased plasma concentrations with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, boceprevir, nefazodone). Increased risk of profound sedation, respiratory depression, coma and death with opioids (e.g. morphine, meperidine, fentanyl).
Tương tác với thức ăn
Enhanced CNS depressant effects of alcohol. Decreased plasma concentration with St. John’s wort. Increased plasma concentration with grapefruit juice.
Tác dụng
Description:
Mechanism of Action: Midazolam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at various sites within the CNS, including limbic system and reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to Cl ions, which results in hyperpolarisation and stabilisation.
Onset: Approx 15 minutes; 3-5 minutes (IV); 10-20 minutes (oral).
Duration: Up to 6 hours (IM); <2 hours (IV: single dose).
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: 40-50% (oral); >90% (IM). Time to peak plasma concentration: 0.5-1 hour (IM); 0.17-2.65 hours (oral).
Distribution: Widely distributed in the body, including CSF. Crosses the placenta and enters the breastmilk. Volume of distribution: 1-3.1 L/kg, increased in females, elderly and obesity. Plasma protein binding: Approx 97%, mainly albumin.
Metabolism: Extensively metabolised in the liver by CYP3A isoenzyme; 60-70% of biotransformed midazolam is 1-hyrdoxy-midazolam or α-hydroxymidazolam (active metabolite).
Excretion: Oral: Via urine (approx 90% within 24 hours; mainly as glucuronide conjugates [60-70%]; <3% as unchanged drug); faeces (approx 2-10% over 5 days). Elimination half-life: 3 hours; 4.2±1.87 hours (IM); <1 hour (active metabolite).
Đặc tính

Chemical Structure Image
Midazolam

Source: National Center for Biotechnology Information. PubChem Database. Midazolam, CID=4192, https://pubchem.ncbi.nlm.nih.gov/compound/Midazolam (accessed on Jan. 22, 2020)

Bảo quản
Store between 15-30°C.
Phân loại MIMS
Thuốc ngủ & thuốc an thần
Phân loại ATC
N05CD08 - midazolam ; Belongs to the class of benzodiazepine derivatives. Used as hypnotics and sedatives.
Tài liệu tham khảo
Anon. Midazolam (Pediatric and Neonatal Lexi-Drugs). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/06/2023.

Anon. Midazolam Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 31/07/2023.

Anon. Midazolam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/06/2020.

Buckingham R (ed). Midazolam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/06/2023.

Dormicum Ampoules (Roche). MIMS Singapore. http://www.mims.com/singapore. Accessed 02/06/2020.

Dormicum Tablets (Roche). MIMS Singapore. http://www.mims.com/singapore. Accessed 02/06/2020.

Dormizol 5 mg/mL Solution for Injection (Harson Laboratories). MIMS Philippines. http://www.mims.com/philippines. Accessed 02/06/2020.

Epistatus 10 mg Oromucosal Solution (Veriton Pharma Ltd). MHRA. https://products.mhra.gov.uk. Accessed 17/06/2020.

Joint Formulary Committee. Midazolam. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/06/2020.

Midazolam 1 mg/mL Injection (Aurum Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 11/04/2023.

Midazolam 2 mg/mL Solution for Injection/Infusion (Mercury Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/06/2020.

Midazolam Hydrochloride (Gland Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 31/07/2023.

Midazolam Hydrochloride Injection, Solution (Alvogen Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/06/2020.

Midazolam Hydrochloride Syrup (Paddock Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/06/2020.

Midazolam Injection 5 mg/mL Hameln (Hameln Pharmaceuticals GmbH). MIMS Singapore. http://www.mims.com/singapore. Accessed 02/06/2020.

Midazolam Orpha 15 mg Film-coated Tablets (Orpha-Devel Handels und Vertriebs GmbH). MHRA. https://products.mhra.gov.uk. Accessed 02/06/2020.

Midazolam. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 31/07/2023.

Paediatric Formulary Committee. Midazolam. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 27/06/2023.

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