Tranxilene

Tranxilene Uses, Dosage, Side Effects, Food Interaction and all others data.

A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions.

Clorazepate is a member of the group of drugs called benzodiazepines. Pharmacologically, clorazepate has the characteristics of the benzodiazepines. It has depressant effects on the central nervous system. The primary metabolite, nordiazepam, quickly appears in the blood stream. Studies in healthy men have shown that clorazenate has depressant effects on the central nervous system. Since orally administered clorazepate dipotassium is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug.

Trade Name Tranxilene
Generic Clorazepic acid
Clorazepic acid Other Names Chlorazepate, Clorazepate, Clorazepic acid
Type
Formula C16H11ClN2O3
Weight Average: 314.723
Monoisotopic: 314.045819935
Protein binding

The protein binding of nordiazepam in plasma is high (97-98%).

Groups Approved, Illicit
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Tranxilene
Tranxilene

Uses

Tranxilene is a benzodiazepine used to treat anxiety, partial seizures, and alcohol withdrawal.

For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Also used as adjunctive therapy in the management of partial seizures and for the symptomatic relief of acute alcohol withdrawal.

Tranxilene is also used to associated treatment for these conditions: Acute Alcohol Withdrawal, Generalized Anxiety Disorder (GAD), Partial-Onset Seizures, Acute Anxiety

How Tranxilene works

Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Toxicity

Oral LD50 in rats is 1320 mg/kg. In monkeys, oral LD50 exceed 1600 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.

Food Interaction

  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Elimination Route

Rapidly absorbed following oral administration (bioavailability is 91%).

Half Life

The serum half-life is about 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours.

Elimination Route

The drug is metabolized in the liver and excreted primarily in the urine.

Innovators Monograph

You find simplified version here Tranxilene

*** Taking medicines without doctor's advice can cause long-term problems.
Share