This salt form of the compound has also recently been approved for procedural sedation in China. A second development program of remimazolam was later initiated in China, using a slightly different salt form, remimazolam tosylate. It has, however, recently been approved for anesthesia in Japan and South Korea, procedural sedation in the United States, China, and Europe, and for compassionate use in intensive care unit sedation in Belgium. The development of remimazolam besylate has been slow by industry standards, primarily because of the resource limitations of these small companies. Via the GSK ventures initiative, the program was acquired by the small biotechnology company, TheraSci, and, through successive acquisitions, developed as the besylate salt at CeNeS and PAION. The project at Glaxo was shelved for strategic reasons at the late lead optimization stage. Remimazolam was identified as one of the lead compounds. The program focussed on the identification of ester-based benzodiazepine derivatives that are rapidly broken down by esterases.
Midazolam Hydrochloride Injection, Solution (Alvogen Inc.). Midazolam 2mg/mL Solution for Injection/Infusion (Mercury Pharmaceuticals Limited). Epistatus 10 mg Oromucosal Solution (Veriton Pharma Ltd).
Dormizol 5 mg/mL Solution for Injection (Harson Laboratories). Wolters Kluwer Clinical Drug Information, Inc. Elimination half-life: 3 hours 4.2☑.87 hours (IM) <1 hour (active metabolite).Īnon. Metabolism: Extensively metabolised in the liver by CYP3A isoenzyme 60-70% of biotransformed midazolam is 1-hyrdoxy-midazolam or α-hydroxymidazolam (active metabolite).Įxcretion: Oral: Via urine (approx 90% within 24 hours mainly as glucuronide conjugates <3% as unchanged drug) faeces (approx 2-10% over 5 days). Plasma protein binding: Approx 97%, mainly albumin. Volume of distribution: 1-3.1 L/kg, increased in females, elderly and obesity. Crosses the placenta and enters the breastmilk. Time to peak plasma concentration: 0.5-1 hour (IM) 0.17-2.65 hours (oral).ĭistribution: Widely distributed in the body, including CSF. Onset: Approx 15 minutes 3-5 minutes (IV) 10-20 minutes (oral).ĭuration: Up to 6 hours (IM) 90% (IM). 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. respiratory depression, respiratory arrest, apnoea, cardiac arrest).ĭescription: Midazolam binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at various sites within the CNS, including limbic system and reticular formation. Potentially Fatal: Cardiorespiratory effects (e.g.
MIDAZOLAM ANTIDOTE SKIN
Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, laryngospasm, bronchospasm, cough. Psychiatric disorders: Confusion, euphoric mood, depression, hallucinations, physical drug dependence, withdrawal syndrome. Nervous system disorders: Sedation (prolonged and post-operative), decreased alertness, somnolence, headache, dizziness, drowsiness, ataxia. Musculoskeletal and connective tissue disorders: Muscle weakness. Injury, poisoning and procedural complications: Falls, fractures. General disorders and administration site conditions: Fatigue, inj site reactions (e.g.
Gastrointestinal disorders: Nausea, vomiting, constipation, dry mouth, hiccups. hyperactive or aggressive behaviour), suicidal ideation, withdrawal symptoms.Ĭardiac disorders: Bradycardia, tachycardia. Significant: Anterograde amnesia, CNS depression, hypotension, paradoxical reactions (e.g.
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