Premazepam is a benzodiazepine derivative. It is a partial agonist

Partial agonist

Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...

 of benzodiazepine

Benzodiazepine

A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...

 receptors and has been shown to possess both anxiolytic

Anxiolytic

An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

 and sedative

Sedative

A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....

 properties in human subjects.

Properties

The initial doses of premazepam given to human test subjects demonstrated similar psychological test results to those produced by diazepam. It was also demonstrated that initial dosing with premazepam produces similar sedative effects as compared with diazepam, although psychomotor impairments are greater with premazepam than with diazepam after initial dosing. However, with repeated dosing for more than one day premazepam causes less sedation and less psychomotor impairment than diazepam

Diazepam

Diazepam , first marketed as Valium by Hoffmann-La Roche is a benzodiazepine drug. Diazepam is also marketed in Australia as Antenex. It is commonly used for treating anxiety, insomnia, seizures including status epilepticus, muscle spasms , restless legs syndrome, alcohol withdrawal,...

. Premazepam possesses sedative

Sedative

A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....

 and anxiolytic

Anxiolytic

An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

 properties. Premazepam produces more slow wave and less fast wave EEG

EEG

EEG commonly refers to electroencephalography, a measurement of the electrical activity of the brain.EEG may also refer to:* Emperor Entertainment Group, a Hong Kong-based entertainment company...

 changes than diazepam. Tests have shown that 7.5 mg of premazepam is approximately equivalent to 5 mg of diazepam

Diazepam

Diazepam , first marketed as Valium by Hoffmann-La Roche is a benzodiazepine drug. Diazepam is also marketed in Australia as Antenex. It is commonly used for treating anxiety, insomnia, seizures including status epilepticus, muscle spasms , restless legs syndrome, alcohol withdrawal,...

.

Pharmacology

Premazepam is a pyrrolodiazepine benzodiazepine and acts as a partial agonist at benzodiazepine receptors. The mean time taken to reach peak plasma levels is 2 hours and the mean half life of pramazepam in humans is 11.5 hours. About 90% of the drug is excreted in unchanged form. Of the remaining 10% of the drug none of the metabolites showed any pharmacological activity. Thus premazepam produces no active metabolites in humans.

See also

• Benzodiazepine
  Benzodiazepine
  A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
  
  
• Benzodiazepine dependence
  Benzodiazepine dependence
  Benzodiazepine dependence or benzodiazepine addiction is a condition during which a person is dependent on benzodiazepine drugs. Dependence can be either a psychological dependence, physical dependence, or a combination of the two...
  
  
• Benzodiazepine withdrawal syndrome
  Benzodiazepine withdrawal syndrome
  Benzodiazepine withdrawal syndrome—often abbreviated to benzo withdrawal—is the cluster of symptoms which appear when a person who has taken benzodiazepines long term and has developed benzodiazepine dependence stops taking benzodiazepine drug or during dosage reductions...
  
  
• Long term effects of benzodiazepines
  Long term effects of benzodiazepines
  The long-term effects of benzodiazepines include drug dependence as well as the possibility of adverse effects on cognitive function, physical health, and mental health. There are significant risks associated with the long-term use of benzodiazepines. However, not all people experience problems...