Oxazepam
7-chloro-3-hydroxy-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one
Overview
Oxazepam belongs to Depressants / Benzodiazepines.
Effects
- Reduced anxiety, calm and relaxation, drowsiness and easier sleep, with muscle relaxation.
- Impaired coordination, concentration and short-term memory, and dizziness: coming on relatively gradually because of the slow absorption.
- With regular use: tolerance, dependence, and rebound anxiety/insomnia and other withdrawal symptoms on stopping.
Dosing & duration
Oral (tablets/capsules), prescribed and dose-adjusted by a clinician. Figures are therapeutic (prescribing) context, not a recreational guide.. Oxazepam is a prescription medicine for short-term use. The lowest effective dose and shortest course are used, with lower doses in the elderly. Its slow onset means effects build over 30–120 minutes, so redosing before it takes hold risks overshooting. It should not be combined with alcohol, opioids or other sedatives, and users should not drive while affected.
Dose ranges
10–30 mg, 3–4 times daily
15–30 mg
Lower doses (e.g. 10 mg up to 3×/day), titrated
Duration
≈30–120 min (slow)
Several hours (short–intermediate)
Possible next-morning drowsiness. Rebound anxiety/insomnia on stopping
Chemical & Physical Properties
| Formula | C15H11ClN2O2 |
| Molar mass | 286.71 g/mol |
| State | Solid |
| Melting point | 205–206 °C |
| Boiling point | Not reported |
| Density | Not reported |
| Vapor pressure | 4.2×10⁻¹² mmHg at 25 °C (estimated) |
| pKa | pKa1 1.55 (-C=N-), pKa2 10.9 (-OH) (estimated) |
| LogP | 2.24 |
| Solubility | less than 1 mg/mL at 19 °C (NTP, 1992), Soluble in alcohol, chloroform, dioxane, 1 g soluble in >10,000 mL water, 220 mL alcohol, 270 mL chloroform, 2200 mL ether |
| Refractive index | Not reported |
Identifiers & Synonyms
| CAS | 604-75-1 |
| CAS (enantiomer) | |
| PubChem CID | 4616 |
| InChIKey | ADIMAYPTOBDMTL-UHFFFAOYSA-N |
| InChI | InChI=1S/C15H11ClN2O2/c16-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)18-15(20)14(19)17-12/h1-8,15,20H,(H,17,19) |
| SMILES | C1=CC=C(C=C1)C2=NC(C(=O)NC3=C2C=C(C=C3)Cl)O |
Synonyms
- Serax
- Adumbran
Pharmacodynamics & Biochemistry
Oxazepam (Serax, Adumbran) is a short-to-intermediate-acting benzodiazepine. Like the rest of the class it is a positive allosteric modulator at the benzodiazepine site of the GABA-A receptor (the α/γ2 subunit interface): in the presence of GABA it increases the frequency of chloride-channel opening, enhancing inhibitory neurotransmission to produce anxiolysis, sedation, muscle relaxation and anticonvulsant effects. It is also a natural downstream metabolite of several other benzodiazepines, including diazepam, temazepam and prazepam. Its distinctive feature is its metabolism: oxazepam is cleared by direct glucuronidation (mainly UGT2B15) to an inactive glucuronide, WITHOUT the oxidative (CYP) metabolism that most benzodiazepines undergo and WITHOUT any active metabolites. Because this conjugation is well preserved in old age and liver disease, oxazepam does not accumulate the way long-acting, oxidatively-metabolised agents do, and it is one of the benzodiazepines preferred in the elderly and in hepatic impairment (alongside lorazepam and temazepam). Its half-life is roughly 6–9 hours and its onset is comparatively slow (30–120 min), which gives it less of an abrupt 'rush' and somewhat lower abuse appeal than fast-onset benzodiazepines. Oxazepam has a single chiral centre (C3) and is used as the racemate. Its two enantiomers interconvert (racemise) readily, and no therapeutic advantage of a single enantiomer over the racemate has been found. Its high-affinity benzodiazepine-site binding is not separately curated in the major binding database, so it is described here qualitatively rather than with a receptor-binding table.
Biological targets
- GABA-A
Binding & functional measurements
Pharmacokinetics
| Bioavailability | Not reported |
| Tmax | Slow onset ≈30–120 min |
| Half-life | ≈6–9 h (short–intermediate) |
| Vd | Not reported |
| Protein binding | Not reported |
| Metabolism | Direct hepatic glucuronidation (mainly UGT2B15) to an inactive glucuronide. No oxidative (CYP) metabolism and no active metabolites |
| Excretion | Renal (as the glucuronide) |
Toxicology & Safety
Not reported
Oxazepam is a comparatively mild, short-to-intermediate benzodiazepine, but it carries the class's core risks. It causes dose-dependent sedation, drowsiness, dizziness, impaired coordination, memory and reaction time, so it impairs driving and increases fall risk (though it accumulates less than long-acting agents). Like all benzodiazepines it produces tolerance, physical dependence and, on stopping after regular use, a withdrawal syndrome (rebound anxiety and insomnia, tremor, sweating and, after high-dose or abrupt cessation, seizures), so courses are kept short and doses tapered. It can cause respiratory depression, which becomes dangerous when combined with opioids, alcohol or other CNS depressants: the usual mechanism of benzodiazepine-related death. Its slow onset makes it somewhat less appealing recreationally, but it is still misused. Because it is directly conjugated rather than oxidised, it has fewer pharmacokinetic drug interactions than most benzodiazepines and is comparatively safe in liver disease and old age. Use cautiously in sleep apnoea, severe respiratory insufficiency, myasthenia gravis, and in pregnancy.[2]
Legal Status
US: Schedule IV. UK: Class C (Schedule 4). DE: BtMG Anlage III
Interactions & Contraindications
Drug interactions
Contraindications
No interactions or contraindications listed.
Usage & Context
- A prescription anxiolytic and hypnotic for the short-term treatment of anxiety (including anxiety with depression) and insomnia, and for managing the symptoms of alcohol-withdrawal syndrome.
- Particularly favoured in older people and in patients with impaired liver function, because its direct-conjugation metabolism avoids the accumulation and active metabolites of long-acting benzodiazepines.
- Also encountered as the pharmacologically active endpoint of diazepam, temazepam and prazepam metabolism, and misused recreationally.
Sources & Evidence
- PubChem: Oxazepam (CID 4616) — identifiers & experimental properties
- Wikipedia: Oxazepam (Serax) — GABA-A benzodiazepine-site PAM, direct-glucuronidation metabolism (no active metabolites), racemate, uses, adverse effects & legal status CC BY-SA 4.0
- DEA Diversion Control Division: Controlled Substance Schedules (oxazepam is Schedule IV)
- GOV.UK: Controlled drugs list — oxazepam is Class C / Schedule 4 (Misuse of Drugs legislation) OGL v3.0