Drug information of Bromazepam

Bromazepam

Drug group:

One of the benzodiazepines that is used in the treatment of anxiety disorders. It is a Schedule IV drug in the U.S. and Canada and under the Convention on Psychotropic Substances. It is a intermediate-acting benzodiazepine

Bromazepam

Mechanism of effect

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

Pharmacodynamic

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.

Pharmacokinetics

Absorption
Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.
Volume of distribution
1.56 L/kg
Protein binding
70%
Metabolism
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
Clearance
0.82 mL/min/kg.

Drug indications

  • Alcohol withdrawal.
  • Anxiety.
  • Anxiety attack.
  • Delirium tremens.
  • Preventive treatment for delirium tremens

Dosage

Normal Dosage
    Oral route
        Anxiety neurosis
            a) Initial dosage: 6 to 18 mg orally daily in equally divided doses, reassess need for continued therapy and adjust dosage as needed after 1 week
            b) Optimal dosage: 6 to 30 mg orally daily in divided doses; short courses of therapy recommended
            c) Limited experience with higher doses up to 60 mg orally daily
Dosage in Renal Failure
    A) Initiate therapy at a very low dose
Dosage in Hepatic Insufficiency
    A) Mild to moderate impairment: Initiate therapy at a very low dose
    B) Severe impairment: Contraindicated
Dosage in Geriatric Patients
    A) Initial dosage should not exceed 3 mg orally daily. After 1 week may adjust dosage based on response and tolerability

Drug contraindications

A) Hypersensitivity to bromazepam, other benzodiazepines, or any other ingredient, or components of the container
B) Myasthenia gravis
C) Severe hepatic insufficiency
D) Severe respiratory insufficiency
E) Sleep apnea syndrome
F) Narrow angle glaucoma

Side effects

Cardiovascular Effects
Cardiac arrest
Heart failure
    Cardiac arrest
        1) Postmarketing
        a) Has been reported
    Heart failure
        1) Postmarketing
        a) Has been reported
Immunologic Effects
Anaphylaxis
Hypersensitivity reaction
    Anaphylaxis
        1) Adult Clinical Trials
        a) Has been reported in very few cases with benzodiazepine use; incidence not given
    Hypersensitivity reaction
        1) Adult Clinical Trials
        a) Has been reported with benzodiazepine use; incidence not given
Musculoskeletal Effects
    Fracture of bone
        1) General Information
        a) Increased risk of falls and fractures with concomitant use of sedatives and alcohol
        b) Increased risk with elderly patients
        2) Adult Clinical Trials
        a) Falls and fractures have been reported; incidence not given
Neurologic Effects
Anterograde amnesia
Ataxia
Dizziness
Somnolence
    Anterograde amnesia
        1) General Information
        a) May occur with therapeutic doses of benzodiazepines, but the risk is increased with higher doses
        b) Associated with inappropriate behavior
        2) Adult Clinical Trials
        a) Has been reported; incidence not given
    Ataxia
        1) General Information
        a) Occurs mostly at the start of therapy and dissipates with repeated administration
        2) Adult Clinical Trials
        a) Has been reported frequently; incidence not given]
    Dizziness
        1) General Information
        a) Occurs mostly at the start of therapy and dissipates with repeated administration
        2) Adult Clinical Trials
        a) Has been reported frequently; incidence not given
    Somnolence
        1) General Information
        a) Occurs mostly at the start of therapy and dissipates with repeated administration
        2) Adult Clinical Trials
        a) Has been reported frequently; incidence not given
Psychiatric Effects
    Hostile behavior
        1) General Information
        a) Release of hostility and other reactions, including excitability, agitation, delusion, anger, hallucinations, psychosis, and other adverse behavioral effects have been reported with use of benzodiazepines
        b) More likely to occur in children and the elderly
        2) Prevention and Management
        a) Discontinue use if occurs
        3) Adult Clinical Trials
        a) Has been reported with benzodiazepine use; incidence not given
Respiratory Effects
    Respiratory depression
        1) Prevention and Management
        a) Avoid concomitant use with alcohol or CNS depressants
        2) Postmarketing
        a) Has been reported
Other
   
        1) General Information
        a) Increased risk with concomitant use of sedatives and alcohol
        b) Increased risk with elderly patients
        2) Adult Clinical Trials
        a) Has been reported with benzodiazepine use; incidence not given

Interactions

Ethchlorvynol , Aripiprazole , Olopatadine , Isoniazid , Baclofen , Buspirone , Theophyline , primaquine , Scopolamine , Chloral hydrate , Efavirenz , vemurafenib , eszopiclone , Carbamazepine , Rifabutin , Grapefruit , Tapentadol , Ethinyl Estradiol , Mirtazapine , Cimetidine , Phenytoin , Gabapentin , Lamotrigine , Levetiracetam , Medroxyprogesterone , Tramadol , Tranylcypromine , Topiramate , Gemfibrozil , Deferasirox , Rifampin
  • alcohol
  • antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • aprepitant
  • aripiprazole
  • "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • baclofen
  • barbiturates (e.g., butalbital, phenobarbital)
  • benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
  • buspirone
  • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
  • carbamazepine
  • chloral hydrate
  • cimetidine
  • deferasirox
  • efavirenz
  • ethinyl estradiol (birth control pills)
  • gabapentin
  • gemfibrozil
  • grapefruit juice
  • isoniazid
  • lamotrigine
  • levetiracetam
  • macrolide antibiotics (e.g., clarithromycin, erythromycin)
  • medroxyprogesterone
  • mexiletine
  • mirtazapine
  • muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
  • narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
  • olopatadine
  • phenytoin
  • primaquine
  • proton pump inhibitors (e.g., lansoprazole, omeprazole)
  • rifampin
  • rifabutin
  • quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
  • scopolamine
  • St. Johns wort
  • tapentadol
  • theophylline
  • topiramate
  • tramadol
  • tranylcypromine
  • tricyclic antidepressasnts (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
  • vemurafenib
  • zopiclone

Alerts

A) Addiction potential: Physical and psychic dependence with subsequent withdrawal symptoms may occur with long-term or short-term therapy, especially at high doses; avoid abrupt discontinuation
B) Alcohol or drug abuse history: Increased risk of physical and psychic dependence with subsequent withdrawal symptoms
C) Concomitant use: Alcohol or CNS depressants should be avoided
D) Elderly and debilitated patients: Increased risk for CNS depression; initiate treatment with lower doses and titrate slowly
E) Falls and Fractures: May occur, especially with concomitant sedative use and in elderly patients
F) Lactose intolerance: Avoid use in galactose intolerance, including Lapp lactase deficiency or glucose-galactose malabsorption
G) Neurologic: Anterograde amnesia may occur; increased risk with higher doses
H) Neurologic: Sedation, amnesia, and impaired muscular function may occur; do not drive or engage in other hazardous activities during the first few days of therapy
I) Pregnancy and Lactation: Avoid use
J) Psychiatric: Not recommended in patients with depressive disorders, psychosis, psychotic tendencies, obsessive compulsive disorder, or personality disorders
K) Respiratory: Use with caution in patients with chronic respiratory diseases
L) Respiratory: Respiratory depression may occur; increased risk with preexisting airway obstruction, brain damage, or concomitant use of medications that cause respiratory depression
M) Tolerance: Loss of response may occur after prolonged use

Pregnancy level

Available evidence is inconclusive or is inadequate for determining fetal risk when used in pregnant women or women of childbearing potential. Weigh the potential benefits of drug treatment against potential risks before prescribing this drug during pregnancy.

Breast feeding warning

Available evidence and/or expert consensus is inconclusive or is inadequate for determining infant risk when used during breastfeeding. Weigh the potential benefits of drug treatment against potential risks before prescribing this drug during breastfeeding.

Drug forms

Lexotan, Lexotanil

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