Imidazenil
Encyclopedia
Imidazenil is an anxiolytic
drug which is derived from the benzodiazepine
family, and is most closely related to other imidazobenzodiazepines such as midazolam
, flumazenil
and bretazenil
.
Imidazenil is a GABAA partial agonist
with an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant
and anxiolytic
effects, yet without any notable sedative
or amnestic effects. In fact, imidazenil blocks the sedative effects of diazepam
, yet without lowering the convulsion threshold, and so potentially could be a more flexible antidote than the antagonist flumazenil
which is commonly used to treat benzodiazepine overdose
at present.
This unusual profile of effects makes imidazenil potentially a very useful drug. In animal studies it has been shown to be an effective anxiolytic and strong anticonvulsant, yet without many of the side effects associated with other benzodiazepines; it does not produce tolerance or dependence
, reverses the amnestic effects of conventional benzodiazepines, and does not potentiate the effects of alcohol.
Imidazenil has not yet been developed commercially for use in humans, however it has been suggested as a safe and effective treatment for anxiety
, a potent yet non-sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agent
s, and as a novel treatment for schizophrenia
.
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
drug which is derived from the benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
family, and is most closely related to other imidazobenzodiazepines such as midazolam
Midazolam
Midazolam is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potent anxiolytic,...
, flumazenil
Flumazenil
Flumazenil is a benzodiazepine antagonist available for injection only, and the only benzodiazepine receptor antagonist on the market today.It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by...
and bretazenil
Bretazenil
Bretazenil is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the benzodiazepine antagonist flumazenil, although its effects are somewhat different...
.
Imidazenil is a GABAA 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...
with an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
and anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
effects, yet without any notable sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
or amnestic effects. In fact, imidazenil blocks the sedative effects 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,...
, yet without lowering the convulsion threshold, and so potentially could be a more flexible antidote than the antagonist flumazenil
Flumazenil
Flumazenil is a benzodiazepine antagonist available for injection only, and the only benzodiazepine receptor antagonist on the market today.It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by...
which is commonly used to treat benzodiazepine overdose
Benzodiazepine overdose
Benzodiazepine overdose describes the ingestion of one of the drugs in the benzodiazepine class in quantities greater than are recommended or generally practiced. Death as a result of benzodiazepines is uncommon but does occasionally happen. Deaths after hospital admission are considered to be low...
at present.
This unusual profile of effects makes imidazenil potentially a very useful drug. In animal studies it has been shown to be an effective anxiolytic and strong anticonvulsant, yet without many of the side effects associated with other benzodiazepines; it does not produce tolerance or dependence
Physical dependence
Physical dependence refers to a state resulting from chronic use of a drug that has produced tolerance and where negative physical symptoms of withdrawal result from abrupt discontinuation or dosage reduction...
, reverses the amnestic effects of conventional benzodiazepines, and does not potentiate the effects of alcohol.
Imidazenil has not yet been developed commercially for use in humans, however it has been suggested as a safe and effective treatment for anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
, a potent yet non-sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agent
Nerve agent
Nerve agents are a class of phosphorus-containing organic chemicals that disrupt the mechanism by which nerves transfer messages to organs...
s, and as a novel treatment for schizophrenia
Schizophrenia
Schizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
.