Ethyl loflazepate
Encyclopedia
Ethyl loflazepate is a drug which is a benzodiazepine
derivative. It possesses anxiolytic
, anticonvulsant
, sedative
and skeletal muscle relaxant properties. In animal studies it was found to have low toxicity, although in rats evidence of pulmonary phospholipidosis occurred with pulmonary foam cells developing with long-term use of very high doses. Its elimination half-life is 51 hours - 103 hours. It's mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite
which is stronger than the parent compound. Ethyl loflazepate was designed to be a prodrug
for descarboxyloflazepate, it's active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure
or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation
and ataxia
. Hypotonia
may also occur in severe cases. These symptoms occur much more frequently and severely in children. Death from therapeutic maintenance doses of ethyl loflazepate taken for 2 – 3 weeks has been reported in 3 elderly patients. The cause of death was asphyxia
due to benzodiazepine toxicity. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.
Ethyl loflazeplate is commercialized in Mexico
, although is not very used, under the trade name Victan. It's officially approved for the following conditions:
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
derivative. It possesses anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
, 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...
, sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and skeletal muscle relaxant properties. In animal studies it was found to have low toxicity, although in rats evidence of pulmonary phospholipidosis occurred with pulmonary foam cells developing with long-term use of very high doses. Its elimination half-life is 51 hours - 103 hours. It's mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite
Active metabolite
- Prodrugs :Sometimes drugs are formulated deliberately so they will break down inside the body to form the active drug, these are called prodrugs. The reason for this may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better...
which is stronger than the parent compound. Ethyl loflazepate was designed to be a prodrug
Prodrug
A prodrug is a pharmacological substance administered in an inactive form. Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation. The rationale behind the use of a prodrug is generally for absorption, distribution, metabolism, and...
for descarboxyloflazepate, it's active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure
Renal failure
Renal failure or kidney failure describes a medical condition in which the kidneys fail to adequately filter toxins and waste products from the blood...
or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation
Psychomotor agitation
Psychomotor agitation is a series of unintentional and purposeless motions that stem from mental tension and anxiety of an individual. This includes pacing around a room, wringing one's hands, pulling off clothing and putting it back on and other similar actions...
and ataxia
Ataxia
Ataxia is a neurological sign and symptom that consists of gross lack of coordination of muscle movements. Ataxia is a non-specific clinical manifestation implying dysfunction of the parts of the nervous system that coordinate movement, such as the cerebellum...
. Hypotonia
Hypotonia
Hypotonia is a state of low muscle tone , often involving reduced muscle strength. Hypotonia is not a specific medical disorder, but a potential manifestation of many different diseases and disorders that affect motor nerve control by the brain or muscle strength...
may also occur in severe cases. These symptoms occur much more frequently and severely in children. Death from therapeutic maintenance doses of ethyl loflazepate taken for 2 – 3 weeks has been reported in 3 elderly patients. The cause of death was asphyxia
Asphyxia
Asphyxia or asphyxiation is a condition of severely deficient supply of oxygen to the body that arises from being unable to breathe normally. An example of asphyxia is choking. Asphyxia causes generalized hypoxia, which primarily affects the tissues and organs...
due to benzodiazepine toxicity. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.
Ethyl loflazeplate is commercialized in Mexico
Mexico
The United Mexican States , commonly known as Mexico , is a federal constitutional republic in North America. It is bordered on the north by the United States; on the south and west by the Pacific Ocean; on the southeast by Guatemala, Belize, and the Caribbean Sea; and on the east by the Gulf of...
, although is not very used, under the trade name Victan. It's officially approved for the following conditions:
- AnxietyAnxietyAnxiety 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,...
- Post-trauma anxiety
- Anxiety associated with severe neuropathic pain.
- Generalized anxiety disorder (GAD)
- Anxiety "crisis"
- Delirium tremensDelirium tremensDelirium tremens is an acute episode of delirium that is usually caused by withdrawal from alcohol, first described in 1813...