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CLORAZEPATE
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Clorazepate is a water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. Studies in healthy men have shown that clorazepate dipotassium has depressant effects on the central nervous system. Clorazepate is a prodrug since orally administered it is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug. Nordiazepam positively modulates GABAA receptors to produce anxiolytic and anticonvulsant effects.
Clorazepate:
https://drugs.ncats.io/drug/D51WO0G0L4
Clorazepate is a benzodiazepine. 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. Clorazepate may be habit-forming. Never share clorazepate with another person, especially someone with a history of drug abuse or addiction. Clorazepate can cause birth defects in an unborn baby. Do not use clorazepate without your doctor's consent if you are pregnant. Some people have thoughts about suicide when taking a medicine like clorazepate.
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/017105s076lbl.pdf
| Maximum Dosage: | |
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| Prescribers Digital Reference | |
Prescribers Digital Reference Tranxene Drug Summary: https://www.pdr.net/drug-summary/Tranxene-clorazepate-dipotassium-1708 | |
| Adults: | 60 mg/day PO for anxiety; 90 mg/day PO for acute alcohol withdrawal or partial seizures. |
| Geriatric: | 60 mg/day PO for anxiety; 90 mg/day PO for acute alcohol withdrawal or partial seizures. |
| Adolescents: | 60 mg/day PO for anxiety; 90 mg/day PO for partial seizures. |
| Children: | 9 to 12 years: 60 mg/day PO for partial seizures; safety and efficacy for the treatment of anxiety have not been established. |
| Children: | Less than 9 years: Safety and efficacy have not been established; off label use for seizures reported in literature in children as young as 3 years. |
| Infants: | Safety and efficacy have not been established. |
| Neonates: | Safety and efficacy have not been established. |
| Duration: Is a prodrug for Desmethyldiazepam which is responsible for most of the therapeutic effects. Has a long half life, with the addition of Desmethyldiazepam as the main metabolite, which makes it much longer. | |||
| Route | Onset | Duration | After Effects |
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| Tripsit Factsheets | |||
Clorazepate Basic Information: http://drugs.tripsit.me/clorazepate | |||
| All ROAs: | 20-80 minutes | 8-12 hours | 1-8 hours |
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| Avoid: All other CNS depressants. | |||
Aliases:
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| Effects: Anxiolytic, Sedative, Muscle Relaxant, Amnesia, Dystaxia, Hypnotic. | |||
| Side Effects: |
| Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. |
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| RxList |
Tranxene (clorazepate dipotassium): https://www.rxlist.com/tranxene-drug/patient-images-side-effects.htm |
| Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself. |
Call your doctor at once if you have:
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Common side effects may include:
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| This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. |
Pediatric:
Appropriate studies have not been performed on the relationship of age to the effects of clorazepate in children younger than 9 years of age.Safety and efficacy have not been established.
Geriatric:
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of clorazepate in the elderly. However, elderly patients are more likely to have unwanted effects (eg, severe drowsiness, dizziness, confusion, clumsiness, or unsteadiness) and kidney, liver, or heart problems, which may require caution and an adjustment in the dose for patients receiving clorazepate.Other Medical Problems:
Make sure you tell your doctor if you have any other medical problems, especially:
- Alcohol abuse, or history of
- Depression, history of
- Drug abuse or dependence, or history of
- Lung or breathing problems (eg, respiratory depression)
- Mental health problems, history of - Use with caution. May make these conditions worse
- Glaucoma, narrow angle - Should not be used in patients with this condition
- Kidney disease
- Liver disease - Use with caution. The effects may be increased because of slower removal of the medicine from the body
Clorazepate (Oral Route):
https://www.mayoclinic.org/drugs-supplements/clorazepate-oral-route/description/drg-20072306
Breastfeeding:Summary of Use During Lactation:
Clorazepate is excreted into breastmilk and appears to accumulate in the serum of breastfed infants.Because the half-life of clorazepate and its active metabolite are long, timing breastfeeding with respect to the dose is of little or no benefit in reducing infant exposure.
Other agents may be preferred, especially while nursing a newborn or preterm infant.Drug Levels:
Clorazepate is a prodrug of nordiazepam (desmethyldiazepam) which is the primary active metabolite of diazepam.Alternate Drugs to Consider:
- (Sedative) Lorazepam
- Oxazepam
- (Seizure Disorder) Carbamazepine
- Divalproex
- Gabapentin
- Lamotrigine
- Oxcarbazepine
- Phenytoin
- Valproic Acid
Clorazepate Drug Levels and Effects:
https://www.ncbi.nlm.nih.gov/books/NBK501210/
| Black Box Warnings: |
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Tranxene SD, Tranxene T-Tab (clorazepate) (Rx): https://reference.medscape.com/drug/tranxene-sd-tranxene-t-tab-clorazepate-342901 |
| Concomitant use of benzodiazepines and opioids may result in profound respiratory depression, coma, and death; administer concomitantly when there are no alternative options; limit dosages and durations to minimum required; monitor for signs and symptoms of respiratory depression and sedation |
Liver:
Therapy with clorazepate is not associated with serum aminotransferase elevations, and cases of clinically apparent liver injury from clorazepate have been reported but are very rare.
Clorazepate Hepatotoxicity:
Clorazepate, as with other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from clorazepate is extremely rare. A few only partially convincing case reports of acute hepatocellular injury from clorazepate have been reported. Rare instances of drug induced liver injury have been reported with other benzodiazepines, such as chlordiazepoxide, diazepam, flurazepam, triazolam, and alprazolam. In benzodiazepine related cases of acute liver injury, the latency has ranged from a few weeks to 6 months; the typical pattern of liver enzyme elevations has been cholestatic or mixed, but instances of hepatocellular patterns have also been reported. The injury is usually mild to moderate in severity and self-limited. Fever and rash have not been described nor has autoantibody formation.D Likelihood score: D (possible but rare cause of clinically apparent liver injury).
Clorazepate Overview:
https://www.ncbi.nlm.nih.gov/books/NBK548330/
Important Information:
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.
Clorazepate may impair your thinking or reactions. Avoid driving or operating machinery until you know how clorazepate will affect you. Dizziness or severe drowsiness can cause falls or other accidents.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.
Interactions:
Drug Interactions (446) Alcohol/Food Interactions (2) Disease Interactions (10)
What other drugs will affect Clorazepate?
Taking clorazepate with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death. Ask your doctor before taking a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression, or seizures.Other drugs may interact with clorazepate, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
A total of 446 drugs are known to interact with Clorazepate.
- 27 major drug interactions
- 386 moderate drug interactions
- 33 minor drug interactions
Clorazepate Drug Information:
https://www.drugs.com/mtm/clorazepate.html
Drugs.com Clorazepate Monograph:
https://www.drugs.com/monograph/clorazepate-dipotassium.html
Drugs.com Gen-Xene Overview:
https://www.drugs.com/cons/gen-xene.html
Clorazepate is an unusually long-lasting benzodiazepine.
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