Search results
Results from the WOW.Com Content Network
The tables below contain a sample list of benzodiazepines and benzodiazepine analogs that are commonly prescribed, with their basic pharmacological characteristics, such as half-life and equivalent doses to other benzodiazepines, also listed, along with their trade names and primary uses.
An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug. [5] For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the ...
Etizolam (marketed under numerous brand names) is a thienodiazepine derivative [5] which is a benzodiazepine analog. [6] The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine. [7] [8]
A benzodiazepine can be placed into one of three groups by its elimination half-life, or time it takes for the body to eliminate half of the dose. [189] Some benzodiazepines have long-acting active metabolites , such as diazepam and chlordiazepoxide, which are metabolised into desmethyldiazepam .
The half-life of chlordiazepoxide is from 5 to 30 hours but has an active benzodiazepine metabolite, nordiazepam, which has a half-life of 36 to 200 hours. [31] The half-life of chlordiazepoxide increases significantly in the elderly, which may result in prolonged action as well as accumulation of the drug during repeated administration.
Clorazepate is a long-acting benzodiazepine drug. [10] Clorazepate produces the active metabolite desmethyl-diazepam, which is a partial agonist of the GABA A receptor and has a half life of 20–179 hours; a small amount of desmethyldiazepam is further metabolised into oxazepam.
Its elimination half-life is 51–103 hours. [8] Its mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound. [9] Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite.
Similar to other benzodiazepines clotiazepam has anxiolytic, sedative, hypnotic, amnesic, anticonvulsant and muscle relaxant pharmacological properties. [7] Clotiazepam binds to the benzodiazepine site of the GABA A receptor where it acts as a full agonist; this action results in an enhanced GABA inhibitory effect at the GABA A receptor which results in the pharmacological effects of clotiazepam.