Bromazepam

2.05

2.05

3.99e-02 g/L

Solid

2591；2626；2601；2613；2626；2633；2613

2626；2637.7

159.8 Ų [M+H]+ [CCS Type: TW; Method: Major Mix IMS/Tof Calibration Kit (Waters)]

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]；H315 (87.8%): Causes skin irritation [Warning Skin corrosion/irritation]；H319 (87.8%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]；H335 (87.8%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure; Respiratory tract irritation]

P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 49 reports by companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.；Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website.

DEA schedule IV controlled substance

2H-1,4-Benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-: Does not have an individual approval but may be used under an appropriate group standard

IMAP assessments - 2H-1,4-Benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-: Environment tier I assessment；IMAP assessments - 2H-1,4-Benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-: Human health tier I assessment

Acute Tox. 4 (100%)；Skin Irrit. 2 (87.8%)；Eye Irrit. 2 (87.8%)；STOT SE 3 (87.8%)

General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended.

They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.

Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.

Bromazepam binds to the GABA receptor GABA_A, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced.

No indication of carcinogenicity to humans (not listed by IARC).

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

Bromazepam

DILI Positive

DOI:10.1016/j.drudis.2019.09.022

◉ Summary of Use during Lactation；Bromazepam is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Three partially breastfed infants were apparently not adversely affected by bromazepam in milk. However, the death of a newborn infant breastfed by a mother who was apparently using bromazepam was reported. If a mother of an older infant requires bromazepam, it is not a reason to discontinue breastfeeding; however, because of its relatively long half-life, an alternate drug is preferred, especially while nursing a newborn, preterm or sick infant.；◉ Effects in Breastfed Infants；A 4-week-old infant with a 5-day history of near-miss sudden infant death syndrome was brought to the emergency room with asystole and unresponsive pupils. Despite resuscitation, the infant died. The infant’s serum contained a plasma concentration of 0.38 mcg/mL of “diazepam equivalents” and the infant’s urine was positive for bromazepam. The mother appeared to have been taking sedatives over the last few days, while partially breastfeeding, because of nervousness and sleeplessness. Bromazepam probably contributed to the infant’s death.；Three infants whose mothers were taking bromazepam during pregnancy and postpartum in dosages of 1 or 2 mg three times daily were partially breastfed. No abnormalities were found at the 1-month and the 3-month checkups of any of the infants.；◉ Effects on Lactation and Breastmilk；Relevant published information was not found as of the revision date.

DEA schedule IV controlled substance

2H-1,4-Benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-: Does not have an individual approval but may be used under an appropriate group standard

N05BA08

N - Nervous system；N05 - Psycholeptics；N05B - Anxiolytics；N05BA - Benzodiazepine derivatives；N05BA08 - Bromazepam

QN - Nervous system；QN05 - Psycholeptics；QN05B - Anxiolytics；QN05BA - Benzodiazepine derivatives；QN05BA08 - Bromazepam

70%

Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. It does not possess any antidepressant qualities. Bromazepam, like other benzodiazepines, presents a risk of abuse, misuse, and dependence. According to many psychiatric experts, Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action.

Bromazepam binds to the GABA-A receptor producing a conformational change and potentiating its inhibitory effects. Other neurotransmitters are not influenced.

10-20 hours

Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes). One of the main metabolites is 3-hydroxybromazepam. It is pharmacologically active and the half life is similar to that of the parent compound.

Bromazepam has known human metabolites that include 3-Hydroxybromazepam.

Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes). One of the main metabolites is 3-hydroxybromazepam. It is pharmacologically active and the half life is similar to that of the parent compound. Route of Elimination: Urine (69%), as metabolites Half Life: 10-20 hours

Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here.

Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.

Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.

Urine (69%), as metabolites

1.56 L/kg

0.82 mL/min/kg.

Membrane

Use (kg; approx.) in Germany (2009): >250；Use (kg) in France (2004): 2604；Consumption (g per capita; approx.) in Germany (2009): 0.00305；Consumption (g per capita) in France (2004): 0.0431；Calculated removal (%): 9.5

For the short-term treatment of insomnia, short-term treatment of anxiety or panic attacks, if a benzodiazepine is required, and the alleviation of the symptoms of alcohol- and opiate-withdrawal.

Pharmaceuticals