Bromazepam

7-Bromo-5-(2-pyridyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one

Lexotanil, Lectopam, Lexotan, Lexomil, Lexilium

Psychoactive Class

Chemical Class

Bromazepam is a benzodiazepine patented in 1961 by Roche and approved for medical use in 1974.¹ It is primarily prescribed as an anxiolytic for treating anxiety and panic disorders,¹² and is occasionally used as a premedicant prior to minor surgery.³⁴⁵ Compared to other classical benzodiazepines, bromazepam is noted for being less sedating at typical doses²⁵ while producing greater muscle relaxation.⁶ Some experts suggest it carries elevated abuse potential due to its rapid onset of action.

Dosage & Duration

Dosage

Threshold1.5 mg

Light1.5-3 mg

Moderate3-6 mg

Strong6-12 mg

Heavy12+ mg

Bioavailability

84%

The acute toxic dose for an adult without tolerance or drug combinations has been estimated at 180 mg orally.

Duration

Onset14-15 minutes

Come Up15-120 minutes

Peak2-12 hours

Offset0.5-1 hours

After Effects12-22 hours

Total6-15 hours

Half-life

10-20 hours

Subjective Effects

The experience is dominated by anxiety relief, sedation, and muscle relaxation, with little in the way of sensory alteration. Owing to its fast absorption, the onset of effects is comparatively rapid for a long-acting benzodiazepine, and the overall character of the experience is broadly similar to that of diazepam. At moderate to high doses, memory formation becomes unreliable and coordination is noticeably impaired.

Physical

Drowsiness, heavy sedation, and pronounced muscle relaxation are the primary physical effects, accompanied by dizziness and unsteady, uncoordinated movement. Unsteadiness is reported to be less pronounced than with some other benzodiazepines such as lorazepam.

Coordination

Dizziness

Sedation

Muscle relaxation

Cognitive

The headspace is calm and anxiety-free but cognitively dulled, with reduced working memory, slowed processing of environmental information, and impaired attention. Anterograde amnesia can occur, leaving partial or absent recall of the period after ingestion.

Suppressions

Cognitive effects are dominated by suppression of anxiety alongside a general dampening of memory, attention, and mental processing.

Decreased libido

Reagent Testing

Loading reagent data

Expected colorimetric results are being prepared.

Pharmacology

Pharmacodynamics

Bromazepam acts as a positive allosteric modulator at the benzodiazepine binding site of the GABA-A receptor.⁷ It binds to this site and produces a conformational change that potentiates the inhibitory effects of GABA, enhancing the receptor's response when GABA is present.⁷ Other neurotransmitter systems are not directly influenced.

Pharmacokinetics

Bromazepam is well absorbed orally with a bioavailability of approximately 84%. It is metabolized hepatically via oxidative pathways involving a cytochrome P450 enzyme,⁸⁹ producing hydroxybromazepam as its major metabolite, which is pharmacologically active and has a half-life similar to the parent compound.¹⁰⁸ The elimination half-life of bromazepam is 10 to 20 hours.⁹

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholGHB/GBLOpioidsTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

DiphenhydraminePCP

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

DXMKetamineMXE

TripSit

Tolerance

Full Tolerance

Tolerance to the behavioral effects of benzodiazepines develops within different timeframes depending on the specific effects considered, but generally appears within several days of continuous use.

Cross Tolerance

Benzodiazepines, GABAergic depressants

Harm Potential

Addiction & Dependence

Psychological

High

Bromazepam presents significant abuse potential,⁸ reportedly greater than other benzodiazepines due to its fast absorption and rapid onset of action. Compulsive redosing is documented, and rebound anxiety following use can perpetuate cycles of dependence.⁸

Physical

High

Physical dependence can develop within one to six months of continuous use,⁸¹¹ with up to 30% of long-term users developing dependence.¹² Abrupt withdrawal after chronic use, even at therapeutic doses, can lead to severe withdrawal syndrome including status epilepticus and symptoms resembling delirium tremens.⁸¹³ Withdrawal symptoms include anxiety, insomnia, tremor, sweating, nausea, seizures, hallucinations, and hyperthermia.⁸

Toxicity

Hepatic

Liver damage of the cholestatic type, with or without jaundice, has been reported; the manufacturer recommends regular laboratory examinations for patients on long-term therapy.⁸

Hematological

Leukopenia has been observed in some patients during treatment.⁸

Central Nervous System

Chronic use commonly causes impairments to memory functions including reduced working memory and reduced ability to process environmental information; long-term use may also cause mood swings, depression, depersonalization, and perceptual disturbances.¹³

Psychosis Risk

Paradoxical reactions including violent behavior, loss of impulse control, and suicidal behavior occur rarely, with an incidence rate below 1% in the general population.⁸ These reactions occur more frequently in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimens.⁸ Withdrawal may produce hallucinations and delirium in severe cases.⁸¹³

Seizure Risk

Paradoxical increased seizures in epileptics are rare during use.⁸ However, abrupt withdrawal after chronic use poses significant seizure risk, including potential for status epilepticus.¹³¹² Gradual dose reduction eliminates withdrawal-related seizure risk.⁸

History & Culture

Bromazepam was developed by the Swiss pharmaceutical company Roche, receiving its patent in 1961. The compound was subsequently approved for medical use in 1974, entering the pharmaceutical market as an intermediate-acting anxiolytic medication.…

Legality

International

UN Convention on Psychotropic Substances 1971 (Schedule IV)

By Country

United StatesSchedule IV

Controlled under the Controlled Substances Act as a Schedule IV depressant.²⁴ Sales require a license, and possession is allowed only with a valid license or prescription.

Czech RepublicPrescription only

Regulated as a prescription medication.¹⁸ Available only through licensed pharmacies with valid medical authorization.

NetherlandsList II (Opiumwet)

Scheduled on List II of the Opium Law.²¹ Preparation, possession, delivery, providing, and transport without authorization are prohibited.²² However, possession of small quantities for personal use is typically not prosecuted, and recreational use itself is not prohibited under Dutch law.²³

CanadaSchedule IV CDSA

Controlled under the Controlled Drugs and Substances Act. All benzodiazepines, including bromazepam, are regulated as Schedule IV substances requiring a prescription.¹⁷

GermanyPrescription only

Available by prescription only.¹⁹ Marketed under brand names including Bromazanil (Hexal).¹⁹ Not classified under Anlage listings of the Betäubungsmittelgesetz but regulated as a prescription-only medication.²⁰

References

Source Pages

Citations

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Bromazepam

7-Bromo-5-(2-pyridyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one

Lexotanil, Lectopam, Lexotan, Lexomil, Lexilium

Psychoactive Class

Depressant Anxiolytic Sedative

Chemical Class

Benzodiazepine