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The formation of phenyl-hydroxy bromazolam was catalysed by CYP2B6, CYP2C19, and CYP3A4. 4-hydroxy bromazolam, as well as α-hydroxy bromazolam, were formed by CYP2B6, CYP2C19, CYP3A4, and CYP3A5. Additionally, CYP2C9 was found to catalyse the formation of α-hydroxy bromazolam as well. α-4-dihydroxy bromazolam was only found in incubations ...
Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.) These are non subtype selective IC 50 values averaged across all GABA A receptor subtypes , so subtype selective compounds with strong binding at one subtype but weak at others will appear unusually weak due to averaging ...
[6] [21] The long-term effects of benzodiazepines may differ from the adverse effects seen after acute administration of benzodiazepines. [22] An analysis of cancer patients found that those who took tranquillisers or sleeping tablets had a substantially poorer quality of life on all measurements conducted, as well as a worse clinical picture ...
Brotizolam [3] (marketed under brand name Lendormin) is a sedative-hypnotic [4] thienotriazolodiazepine [5] drug which is a benzodiazepine analog. [6] It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to other short-acting hypnotic benzodiazepines such as triazolam or midazolam. [7]
Bromazepam, sold under many brand names, is a benzodiazepine.It is mainly an anti-anxiety agent with similar side effects to diazepam.In addition to being used to treat anxiety or panic states, bromazepam may be used as a premedicant prior to minor surgery.
Initially, common side effects in the short term may include drowsiness, sedation, and mild cognitive impairment. [ 10 ] [ 11 ] Overdose may include muscle weakness , ataxia , dysarthria and particularly in children paradoxical excitement, as well as diminished reflexes, confusion and coma may ensue in more severe cases.
Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R1 and R4. The benzyl ring of phenazepam is substituted at R7 with a bromine group. Like most benzodiazepines, phenazepam has a phenyl ring in R5 which is substituted by chlorine in the R2' group.
Lower doses of relugolix (<40 mg/day) are under investigation for achieving partial sex hormone suppression in the treatment of endometriosis and uterine fibroids. [14] This is intended to reduce the incidence and severity of menopausal symptoms such as hot flushes and decreased bone mineral density that are secondary to estrogen deficiency .