Drug information of Clorazepate


Clorazepate


Brand drugs:Tranxene T-Tab, Tranxene SD

Clorazepate is a benzodiazepine (ben-zoe-dye-AZE-eh-peen). Clorazepate affects chemicals in the brain that may be unbalanced and cause anxiety or seizures.
Clorazepate is used to treat anxiety disorders, partial seizures, or alcohol withdrawal symptoms.

Mechanism of effect

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system and reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors. Benzodiazepines do not bind to GABA-B receptors.

Pharmacodynamic

Metabolism
Rapidly decarboxylated to nordiazepam (active) in acidic stomach prior to absorption; nordiazepam is hepatically hydroxylated by CYP 2C19 and CYP3A4 to oxazepam (active) and undergoes glucuronidation to form a glucuronide conjugate .
Time to Peak
Serum: ~0.5 to 2 hour
Excretion
Urine (62% to 67%; primarily metabolites of conjugated oxazepam); feces (15% to 19%)
Half life
Nordiazepam: 20 to 160 hours; Oxazepam: 6 to 24 hours

Drug indications

Alcohol withdrawal: Symptomatic relief of acute alcohol withdrawal

Anxiety disorders: Management of anxiety disorders and short-term relief of the symptoms of anxiety

Partial seizures: Adjunct therapy in the management of partial seizures

Dosage

Usual Adult Dose for Anxiety
Initial dose: 15 mg orally at bedtime or in divided doses
Maintenance dose: 15 to 60 mg orally in divided doses
Usual Adult Dose for Alcohol Withdrawal
Day 1: 30 mg orally, followed by 30 to 60 mg in divided doses
Day 2: 45 to 90 mg orally in divided doses
Day 3: 22.5 to 45 mg orally in divided doses
Day 4: 15 to 30 mg orally in divided doses
After Day 4: The daily dose should be reduced to 7.5 to 15 mg
Maximum dose: 90 mg/day
Usual Adult Dose for Seizure Prophylaxis
Initial dose: 7.5 mg orally 3 times a day
Maintenance dose: May increase by no more than 7.5 mg orally every week
Maximum dose: 90 mg/day
Usual Pediatric Dose for Seizure Prophylaxis
9 to 12 years:
-Initial dose: 7.5 mg orally 2 times a day
-Maintenance dose: May increase by no more than 7.5 mg orally every week
-Maximum dose: 60 mg/day
12 years or older:
-Initial dose: 7.5 mg orally 3 times a day
-Maintenance dose: May increase by no more than 7.5 mg orally every week
-Maximum dose: 90 mg/day

Drug contraindications

Hypersensitivity to clorazepate or any component of the formulation; acute narrow-angle glaucoma

Documentation of allergenic cross-reactivity for benzodiazepines is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty

Canadian labeling: Additional contraindications (not in US labeling): Myasthenia gravis

Side effects

Frequency not defined
Cardiovascular: Hypotension
Central nervous system: Anxiety, ataxia, confusion, depression, dizziness, drowsiness, dysarthria, fatigue, headache, insomnia, irritability, memory impairment, nervousness, slurred speech
Dermatologic: Skin rash
Endocrine & metabolic: Decreased libido
Gastrointestinal: Constipation, decreased appetite, diarrhea, increased appetite, nausea, vomiting, xerostomia
Hepatic: Increased serum transaminases, jaundice
Neuromuscular & skeletal: Tremor
Ophthalmic: Blurred vision, diplopia

Alcohol (Ethyl), Alizapride, Azelastine (Nasal), Blonanserin, Bosentan, Brexanolone, Brimonidine (Topical), Bromopride, Bromperidol, Buprenorphine, Cannabidiol, Cannabis, Chlormethiazole,
Chlorphenesin Carbamate, CloZAPine, CNS Depressants, CYP3A4 Inducers (Moderate), CYP3A4 Inducers (Strong), Dabrafenib, Deferasirox, Dimethindene (Topical), Doxylamine, Dronabinol,
Droperidol, Enzalutamide, Erdafitinib, Esketamine, Flunitrazepam, Fosamprenavir, Kava Kava,
HydrOXYzine, Ivosidenib, Lemborexant, Lofexidine, Magnesium Sulfate, Melatonin, Mitotane,
Methadone, Methotrimeprazine, MetyroSINE, Minocycline (Systemic), Nabilone, OLANZapine,
Opioid Agonists, Orphenadrine, Oxomemazine, OxyCODONE, Paraldehyde, Perampanel,
Piribedil, Pramipexole, Ritonavir, ROPINIRole, Rotigotine, Rufinamide, Saquinavir, Sarilumab,
Selective Serotonin Reuptake Inhibitors, Siltuximab, Sodium Oxybate, Suvorexant, Zolpidem, Teduglutide, Tetrahydrocannabinol, Tetrahydrocannabinol and Cannabidiol, Thalidomide,
Theophylline Derivatives, Tobacco (Smoked), Tocilizumab, Trimeprazine, Yohimbine

Alerts

Clorazepate may be habit-forming. Never share clorazepate with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it. Selling or giving away this medicine is against the law

The sedative effects of clorazepate may last longer in older adults. Accidental falls are common in elderly patients who take benzodiazepines. Use caution to avoid falling or accidental injury while you are taking clorazepate

Do not drink alcohol. Dangerous side effects could occur

Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, or death. Reserve use for patients for whom alternative therapies are inadequate and limit use to lowest possible dose and shortest possible duration. Monitor for signs or symptoms of respiratory depression and sedation

Points of recommendation

You should not use clorazepate if you have narrow-angle glaucoma

Clorazepate can cause birth defects. Do not use if you are pregnant

Do not stop using clorazepate suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using clorazepate

Some people have thoughts about suicide when taking a medicine like clorazepate. Stay alert to changes in your mood or symptoms. Report any new or worsening symptoms to your doctor.

To make sure clorazepate is safe for you, tell your doctor if you have:
-liver or kidney disease
-mood problems or depression
-a history of suicidal thoughts or actions
-if you use a narcotic (opioid) medication

Clorazepate is not approved for use by anyone younger than 9 years old

While using clorazepate, you may need frequent blood tests. Your liver function may also need to be checked

Call your doctor if your symptoms do not improve, or if they get worse

Clorazepate is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription

Pregnancy level

HAVE NOT BEEN ESTABLISHED

Not available. An increased risk of congenital malformations associated with the use of minor tranquilizers during the first trimester of pregnancy has been suggested in several studies

Breast feeding warning

enters breast milk; do not nurse

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