NOTE: This drug is discontinued in the US

Prazepam is an oral benzodiazepine used for the management of symptoms associated with anxiety disorders and for short-term amelioration of the symptoms of anxiety or anxiety associated with depression.

Shorter-duration benzodiazepines are often preferable to prazepam in the treatment of anxiety, particularly in the elderly or patients with liver disease, because prazepam produces an active metabolite with a prolonged half-life. Prazepam was approved by the FDA in 1976.

The Centrax product was discontinued by the manufacturer in 1996; the FDA subsequently withdrew the NDA for this drug after market removal.

Indications:

• Anxiety

Centrax is a prescription benzodiazepine drug, also known as prazepam in its generic form, that is used to treat symptoms of anxiety. Centrax is also an anticonvulsant, sedative, and skeletal muscle relaxant drug. Like other benzodiazepines, Centrax is intended only for short-term use. Centrax is usually only prescribed to a patient for a few weeks. Short-term use helps reduce the risk of addiction and dependence that can occur with benzodiazepines. Side effects of Centrax can include fatigue, lethargy, clumsiness, coordination problems and difficulty thinking.

Multi-Substance Centrax (Prazepam) Overdose:
According to a CNN report, the number of benzodiazepine overdose deaths has risen significantly in recent years; however, an additional drug is almost always involved. Benzodiazepines were involved in around 30% of prescription drug overdose deaths in 2013, according to the Centers for Disease Control and Prevention. Researchers and medical professionals believe that people are using drugs like Centrax in riskier ways, which is contributing to overdose deaths. This includes taking higher doses than prescribed, and dangerously mixing them with other prescription drugs, illicit drugs, and alcohol. The risk of an overdose when something like Centrax is combined with another sedative is quite high.

Prazepam is a benzodiazepine derivative and is indicated to treat symptoms of anxiety. Benzodiazepines are used to treat severe incapacitating symptoms or symptoms leading to an extreme suffering for the patient. Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation. Prazepam is a prodrug for N-desmethyl-diazepam, which is responsible for the therapeutic effects of prazepam. Prazepam was discontinued in USA.

Prazepam:
https://drugs.ncats.io/drug/Q30VCC064M

What Centraxis and what it is used for:
Centrax is a tranquilliser containing the active ingredient prazepam.

• It belongs to a group of medicines called benzodiazepines. Benzodiazepines affect chemical activity in the brain and may help to reduce anxiety and stress.
• It is used for short term relief of severe or disabling anxiety or when anxiety is causing great distress.
• The overall length of your treatment should not be more than 4 to 6 weeks including a period where the dose is gradually reduced.

It is not suitable for children and adolescents under 18 years.

Uses:
In the human body this long-acting drug converts into desmethyldiazepam, which is called a metabolite. Desmethyldiazepam is the major metabolite of diazepam and also a metabolite of clorazepate dipotassium and chlordiazepoxide. Some researchers believe this metabolite produces the main drug effects of prazepam and that prazepam should therefore be considered a prodrug (meaning the substance itself has little drug value but that within the body it converts into another substance that is beneficial). Prazepam resembles oxazepam both in chemistry and in its effects.

Prazepam is used medically to relieve anxiety and is considered as effective as alprazolam and lorazepam for that purpose even though they are much stronger drugs than prazepam. One study found prazepam to work better than diazepam for treating anxiety, although diazepam is about twice as potent. A comparison with chlordiazepoxide showed mixed results; chlordiazepoxide produced faster general betterment of anxiety, but prazepam was more effective at improving particular symptoms. Prazepam has also been used successfully for treatment of depression and crankiness. The drug has been used to help alcoholics withdraw from alcohol.

Some scientists have wondered if the drug improves mood simply by helping patients to get better sleep; researchers investigating that question concluded that the drug does have antianxiety qualities causing the improvement.

What should my health care professional know before I take prazepam?

They need to know if you have any of these conditions:

• An alcohol or drug abuse problem
• Depression or psychosis
• Kidney disease
• Liver disease
• Lung disease or breathing difficulties
• Myasthenia gravis
• Parkinson's disease
• Porphyria
• Shortness of breath
• Snoring
• Suicidal thoughts
• An unusual or allergic reaction to prazepam, other benzodiazepines, foods, dyes, or preservatives
• Pregnant or trying to get pregnant
• Breast-feeding

Precautions:

It should be avoided in the following conditions:

• Patients allergic to prazepam or other similar drugs, such as:
  • Diazepam
  • Bromazepam
  • Lorazepam
  • Nitrazepam
  • Others
  • Contact your doctor immediately if you are experiencing symptoms of an allergy, such as:
    • Skin rash
    • Itching of the skin
    • Swelling of the face
    • Swelling of the tongue
    • Difficulty breathing
• Patients with liver damage
• In patients with myasthenia gravis (autoimmune neuromuscular disease)
• In patients with trouble breathing

Special Precautions:

• Chronic pulmonary insufficiency
• Elderly or debilitated patients
• Muscle weakness, impaired liver or kidney function
• Drowsiness may affect skilled tasks
• Monitor cardio-respiratory function when used for deep sedation
• Patients with personality disorders or organic brain changes
• Pregnancy and lactation
• History of alcohol or drug addiction due to risk of depression.

Resp depression and hypotension with parenteral admin, therefore this route should only be used when facilities for reversing resp depression are available. May precipitate suicide or aggressive behavior, not used alone to treat depression or anxiety associated with depression.

Centrax with food and drink:
Do not drink any alcohol whilst you are taking Centrax, as alcohol increases the effects of this medicine.

Elderly Patients:
Centrax may cause the muscles to feel relaxed or weak, therefore elderly patients taking Centrax are more at risk of falling, which may lead to hip fractures. Elderly patients should therefore take care when moving around if they experience any muscles problems.

Pregnancy:
Centrax is not recommended during pregnancy and in women of childbearing potential not using birth control. If you are pregnant, think you may be pregnant or are planning to have a baby ask your doctor or pharmacist for advice before taking this medicine. If you do become pregnant while taking this medicine, your doctor will advise you of the risks involved and may advise you to stop taking the tablets. Occasionally, your doctor may assess your condition and it may be necessary to give you Centrax during late pregnancy or during labour. In these cases babies may have a low body temperature, floppiness, withdrawal symptoms, breathing and feeding difficulties.

Breast-feeding:
Do not breast-feed while taking Centrax, as the drug may pass into breast milk.

Duration of treatment:
Duration of treatment should be as short as possible (see "Posology and Method of Administration") and should not exceed 8-12 weeks, including the dose withdrawal phase. If the treatment is to be extended beyond this period, the situation should be re-evaluated.

Amnesia:
Benzodiazepines can cause anterograde amnesia which generally occurs within a few hours after ingestion of the product. As a consequence, in order to minimise this risk, patients need to be sure that they will have 7 to 8 hours of uninterrupted sleep following intake of the medicinal product (see also section "Indesirable effects")

Prazepam

Duration: Benzodiazepine dervative. Has all the normal benzodiazepine-like quality (Anxiolytic/anticonvulsant/sedative/Skeletal muscle relaxant) It is also a prodrug for Desmethyldiazepam which is responsible for most if not all of the effects of Prazepam.
Route	Onset	Duration	After Effects
Tripsit Factsheets
Prazepam Basic Information: http://drugs.tripsit.me/prazepam
All ROAs:	45-120 minutes	8-20 hours	8-24 hours
Effects: Anxiolytic, Anticonvulsant, Sedative, Skeletal Muscle Relaxant
Avoid: All other CNS depressants, and Cimetidine

What Prazepam EG looks like and contents of the pack:

• Prazepam EG 10 mg tablets are scoredblue tabletsand are available in Aluminium/PVCblister packs of 20, 30, 40, 50 and 60 tablets.The tablet can be divided into equal halves.
• Prazepam EG 20 mg tablets are scored white tablets and are available inAluminium/PVCblisterpacks of 20, 50 and 60 tablets. The tablet can be divided into equal halves.
• Prazepam EG 15 mg/ml oral drops, solution is availablein 20 ml dropper containers. 30 drops of the solution correspond with 1 ml and thus 15 mg prazepam.

Prazepam Chemical Safety Information

Chemical Safety Summary:
INCHEM
Prazepam: http://www.inchem.org/documents/pims/pharm/pim680.htm
Main risks and target organs:
Central nervous system, causing depression of respiration and consciousness.
Summary of clinical effects:
Central nervous system (CNS) depression and coma, or paradoxical excitation, but deaths are rare when benzodiazepines are taken alone. Deep coma and other manifestations of severe CNS depression are rare. Sedation, somnolence, diplopia, dysarthria, ataxia and intellectual impairment are the most common adverse effects of benzodiazepines. Overdose in adults frequently involves co- ingestion of other CNS depressants, which act synergistically to increase toxicity. Elderly and very young children are more susceptible to the CNS depressant action. Intravenous administration of even therapeutic doses of benzodiazepines may produce apnoea and hypotension. Dependence may develop with regular use of benzodiazepines, even in therapeutic doses for short periods. If benzodiazepines are discontinued abruptly after regular use, withdrawal symptoms may develop. The amnesia produced by benzodiazepines can have medico-legal consequences.

• Prazepam is only found in individuals that have used or taken this drug.
• It is a benzodiazepine that is used in the treatment of anxiety disorders.
• Belongs to the class of organic compounds known as 1,4-benzodiazepines.
• It is a schedule IV drug in the U.S.
• Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system.

  Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.

Prazepam:
http://www.t3db.ca/toxins/T3D3054

Alternate Chemical Names:

• DEMETRIN
• W-4020
• PRAZEPAM
• CENTRAX
• PRAZEPAMUM
• CENTRAX
• pubchem compound: 4890
• rxcui: 8627
• chembl: CHEMBL969
• drugbank: 01588
• chemidplus: 2955-38-6

Prazepam Drug Record:
https://www.dgidb.org/drugs/PRAZEPAM

Trade names:

Common trade names include:

• Centrac
• Centrax
• Demetrin
• Lysanxia
• Mono Demetrin
• Pozapam
• Prasepine
• Prazene
• Reapam
• Trepidan

Trade names vary depending on the country:

• Austria: Demetrin
• Belgium: Lysanxia
• France: Lysanxia
• Germany: Demetrin, Mono Demetrin
• Greece: Centrac
• Ireland: Centrax
• Italy: Prazene, Trepidan
• Macedonia: Demetrin, Prazepam
• Netherlands: Reapam
• Portugal: Demetrin
• South Africa: Demetrin
• Switzerland: Demetrin
• Thailand: Pozapam, Prasepine

• A benzodiazepine derivative drug
• Developed in the 1960s
• It has anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.
• It's a prodrug for desmethyldiazepam which is responsible for the therapeutic effects of prazepam.
• Desmethyldiazepam, an active metabolite, has a very long half-life of 29 to 224 hours, which contributes to the therapeutic effects of prazepam.
• Indicated for the short-term treatment of anxiety.

  After short-term therapy, the dose is usually gradually tapered-off to reduce or avoid any withdrawal or rebound effects.

• Side effects of prazepam are less profound than with other benzodiazepines.

Excessive drowsiness and with longer-term use, drug dependence, are the most common side effects of prazepam.