Temazepam (anxiolytic): Uses, Characteristics And Adverse Effects
Benzodiazepines are a group of medications that slow down the central nervous system and decrease neuronal excitation.
Although there are different types, these drugs are mainly used as anxiolytics, hypnotics and muscle relaxants. Temazepam is an example of a benzodiazepine used to help you fall asleep and reduce nighttime awakenings.
In this article we explain what temazepam is what are its main characteristics and clinical uses, its mechanism of action, and the side effects, interactions and contraindications that we must take into account when using this medication.
Temazepam is a drug from the benzodiazepine group used mainly in the treatment of insomnia and serious or disabling sleep disorders. This medication is also used in anxiety disorders, since in addition to having hypnotic effects, it has an anxiolytic and sedative action. Its half-life is approximately 10 hours, making it appropriate for treating maintenance insomnia.
This compound was patented in 1962, and marketed for medical use in 1969 under the name “Restoril.” In 1982 it was approved by the Food and Drug Administration (FDA), and currently there are several pharmaceutical companies that manufacture it in generic form.
In studies carried out in sleep laboratories, it has been proven that temazepam significantly reduces the number of nocturnal awakenings, although it has a distorting effect on normal sleep patterns. Typically, this medication is administered orally and the effects begin sixty minutes later, lasting up to eight hours in total.
The prescription and consumption of benzodiazepines is widespread in the population , especially among older people. And although temazepam is a relatively safe and effective drug, its consumption quickly generates tolerance to its hypnotic and anxiolytic effects, which causes the dose to have to be increased. Typically, prescribing guidelines limit the use of these types of medications to two to four weeks, due to tolerance and dependence issues.
Because benzodiazepines can be abused, their use should be avoided by people in certain high-risk groups, such as people with a history of dependence on alcohol or other drugs, people with emotional problems, and patients with serious mental disorders.
Mechanism of action
Temazepam, like many other similar benzodiazepines, acts as a gamma-aminobutyric acid (GABA) modulator and is capable of causing a variety of effects including: sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.
GABA is considered the main inhibitory neurotransmitter in the human body. When this neurotransmitter binds to GABAA receptors found in neuronal synapses, chloride ions are conducted across the cell membranes of neurons through an ion channel in the receptors. With sufficient chloride ions, the membrane potentials of the associated local neurons become hyperpolarized, making it more difficult or less likely for action potentials to fire, resulting in less excitation of neurons
Although the main pharmacological activity of temazepam is to increase the effect of the neurotransmitter GABA, in animal studies (specifically, in rats) it has also been proven that the drug triggers the release of vasopressin in the paraventricular nucleus of the hypothalamus and decreases the release of vasopressin. adrenocorticotropic hormone under stress conditions.
As with other benzodiazepines, temazepam produces central nervous system depressant effects when coadministered with other medications that also produce this depressant effect, such as barbiturates, alcohol, opiates, tricyclic antidepressants, non-selective inhibitors of the MAO, phenothiazines and other antipsychotics, muscle relaxants, antihistamines and anesthetics.
Administration of theophylline or aminophylline has been shown to reduce the sedative effects of temazepam and other benzodiazepines Unlike many other benzodiazepines, pharmacokinetic interactions involving cytochrome P450 have not been observed with temazepam.
Furthermore, temazepam does not show a significant interaction with cytochrome CYP3A4 inhibitors, and oral contraceptives may decrease the effectiveness of this medication and accelerate its elimination half-life. On the other hand, the use of temazepam should be avoided, if possible, in people with these conditions:
Side effects
The consumption of temazepam is not free of possible side effects and adverse reactions The most common and those that share the vast majority of benzodiazepines are related to depression of the central nervous system and include: drowsiness, sedation, drunkenness, dizziness, fatigue, ataxia, headache, lethargy, impairment of memory and learning.
There may also be impaired motor functions and coordination, slurred speech, decreased physical performance, emotional numbness, decreased alertness, muscle weakness, blurred vision, and poor concentration. Rarely, a state of euphoria has been reported after taking temazepam. In addition, cases of retrograde amnesia and respiratory depression have been reported at high doses.
In a 2009 meta-analysis A 44% increase in the rate of mild infections, such as pharyngitis and sinusitis, was found in people who had taken temazepam or other hypnotic medications compared to those who took a placebo.
On the other hand, cases of hyperhidrosis, hypotension, burning eyes, increased appetite, changes in libido, hallucinations, fainting, nystagmus, vomiting, pruritus, gastrointestinal disorders, nightmares, palpitations and paradoxical reactions such as restlessness, aggression, violence, overstimulation and agitation (in less than 0.5% of cases).
