DIAZEMULS Emulsion Ref.[2739] Active ingredients: Diazepam

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2020  Publisher: Accord Healthcare Limited, Sage House, 319 Pinner Road, North Harrow, Middlesex, HA1 4HF, United Kingdom

Pharmacodynamic properties

Mechanism of action

Diazepam is a potent anxiolytic, anticonvulsant and central muscle relaxant mediating its effects mainly via the limbic system as well as the postsynaptic spinal reflexes. Diazemuls contains diazepam dissolved in the oil phase of an oil-in-water emulsion. Release of the diazepam from the lipid particles of the emulsion has been demonstrated by clinical studies showing comparable efficacy with injectable diazepam preparations.

Pharmacokinetic properties

Biotransformation

Diazepam is metabolised in the liver. Diazepam is metabolised to two active metabolites, one of which, desmethyldiazepam, has an extended half-life. Diazepam is therefore a long acting benzodiazepine and repeated doses may lead to accumulation. Impaired hepatic function may prolong the duration of action of diazepam.

Elimination

Diazepam is excreted via the kidney. Impaired renal function may prolong the duration of action of diazepam.

Special populations

It is recommended that elderly and debilitated patients receive initially one half the normal recommended dose.

During prolonged administration, for example in the treatment of tetanus, the dosage should generally be reduced after 6-7 days, to reduce the likelihood of accumulation and prolonged CNS depression.

Preclinical safety data

Not applicable.

© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.