Benzodiazepines are the pharmacological group that the population accesses most easily and frequently, without the need for there to be a linked pathology that indicates their use.
How many times have we heard that someone around us uses Noctamid or Ortfidal to be able to sleep at night? These two drugs are part of the benzodiazepine family and, together with trankimazin, are the most used. However, we must know the peculiarities of benzodiazepines and when deciding to take them, we must follow a doctor’s instructions, since they can generate rapid dependence and tolerance.
If you want to know this pharmacological group so present in our lives, know what it should be used for and what its indications should be, keep reading this Psychology-Online article: Benzodiazepines: what they are, mechanism of action and classification.
Benzodiazepines: what are they?
What are benzodiazepines? Benzodiazepines are the family of psychotropic drugs par excellence against treatment for anxiety. Although there are also types of benzodiazepines classified in the group of hypnotics, since at high doses they have a hypnotic-sedative effect. Its discovery in the early sixties was a great advance for the treatment of anxiety, because the drug of choice for anxiety disorders was barbiturates, a high-risk pharmacological group due to the short distance between a safe dose and a toxic dose. Therefore, they quickly became the first choice drug for anxiety disorders and also used as a hypnotic drug.
This pharmacological group has the property of relaxing to the person who takes it and although its main action is against anxiety, its use is also applied as a muscle relaxant, hypnotic-sedative and anticonvulsant. However, although it is a pharmacological group that works very well, like all drugs, benzodiazepines have side effects and risks that the person should be aware of. Benzodiazepines are a very safe pharmacological group, however if their administration is prolonged, can cause dependence and tolerance.
Its administration tends to be orallyHowever, in the face of very high agitation or anxiety attacks, it might be advisable to use its intravenous administration, because it acts more quickly in the body.
Benzodiazepines: mechanism of action
What are benzodiazepines used for? How do they work? Benzodiazepines act on the GABA receptor (gamma-amino butyric acid), a neurotransmitter that has the function of creating a relaxation, tranquilizing and/or calming effect in our brain, reducing the transmission of nervous impulses between our cells.
The neurotransmitter GABA has a inhibitory effect in our body, that is, it causes cells slow down of communication between them or that they stop transmitting information. A large part of our neurons, almost half, respond to this receptor, which means that after increasing its action in the brain with the drug, the GABA receptor causes a relaxing effect on our entire body, generating a depressant effect in it. For this reason, there is a reduction in the and induces an increase in muscle relaxation and hypnotic.
Benzodiazepines: classification
The classification of benzodiazepines is assigned based on two concepts: the onset of action and the elimination half-life.
Benzodiazepines: classification according to onset
The onset of action refers to the time elapsed since the drug is administered. until it reaches its maximum concentration. This temporal variable will depend on the pharmaceutical form in which it is made, the route of administration, the lipid solubility of the drug, that is, the ability of the drug to cross the blood-brain barrier, so that the drug can exert its action, and the time that it takes. It takes until the drug crosses said barrier. The classification based on this variable distinguishes 3 types of benzodiazepines.
Types of benzodiazepines according to initiation
- Quick start: the maximum concentration of the drug appears within one hour.
- Intermediate start: The maximum concentration of the drug appears between one and two hours.
- Slow start: The maximum concentration of the drug appears in two hours or more.
Benzodiazepines: classification according to half-life
On the other hand, the elimination half-life, that is, the time that elapses until the drug is expelled of the body, will depend on the metabolization of the drug, its lipid solubility, the presence of active metabolites and the proportion of body fat. Among the temporal variability of elimination, 3 types of benzodiazepines have been established.
Types of benzodiazepines according to half-life
- Short: The elimination period of the drug is equal to or less than six hours.
- Intermediate: The elimination period of the drug is between six and twenty-four hours.
- Prolonged: The elimination period of the drug is equal to or greater than twenty-four hours.
Let’s take a closer look at their classification and which benzodiazepines are part of each type.
Short-lived benzodiazepines
As we have previously indicated, benzodiazepines with a short half-life remain in our body. six hours or less. Their advantage is that they are the group of benzodiazepines with the fastest acting, which is why they are frequently used for specific symptoms, such as the appearance of, to treat or as momentary muscle relaxants, however they are not used for the treatment long-term anxiety.
The big problem with this group is that as it has a short half-life, the effect of the drug fades away soon and therefore, the person has the need to want to maintain the effects of this, consuming the drug again, which is why they tend to to generate dependency problems in the long term if its consumption is not regulated by a doctor. This is one of the side effects or risks of benzodiazepines. In this group we can find different types of benzodiazepines, also taking into account the onset of action.
Types of short-lived benzodiazepines
- Short half-life benzodiazepines with rapid onset of action: midazolam, brotizolam, clothiazepam and bentazepam.
- Short half-life benzodiazepines with intermediate onset of action: triazolam and loprazolam.
- Short half-life benzodiazepines with slow onset of action: zolpidem and zopiclone.
Intermediate-life benzodiazepines
Intermediate-life benzodiazepines have an acting half-life of between six and twenty-four hours, thereby favoring the reduction of the potential for abuse, because its effects are longer over time. In this group we can find different types of benzodiazepines, also taking into account the onset of action.
Types of half-life benzodiazepines
- Intermediate half-life benzodiazepines with rapid onset of action: temazepam.
- Intermediate half-life benzodiazepines with intermediate onset of action: flunitrazepam, lormatazepam, nitrazepam, alprazolam, bromazepam and halazepam.
- Intermediate half-life benzodiazepines with slow onset of action: oxazepam.
Long-acting benzodiazepines
Long-lived benzodiazepines maintain an elimination half-life of more than twenty-four hourstherefore they are very suitable for long term anxiety treatment. As an advantage, it should be noted that the drug remains stable in the body for a long period of time, which can lead to its greatest drawback in the same way that the drug accumulates in the blood, potentially reaching blood levels of toxicity and/or cause more side effects. In this group we can find different types of benzodiazepines, also taking into account the onset of action.
Types of long-lived benzodiazepines
- Benzodiazepines with a long half-life with rapid onset of action: clorazepate, flurazepam and tetrazepam.
- Long half-life benzodiazepines with intermediate onset of action: chlordiazepoxide, clobazam, clonazepam, medazepam and quazepam.
- Long half-life benzodiazepines with slow onset of action: prazepam and ketazolam.
Benzodiazepines and alcohol
Regarding the administration of benzodiazepines, it is necessary to take into account the possible dangers when interacting with other substances. A question that patients frequently ask is: Can you mix benzodiazepines and alcohol? The answer is no. It is very dangerous to mix benzodiazepines and alcohol. Alcohol inhibits the liver enzymes responsible for biotransformation, that is, transforming the drug substances. The consequence of this inhibition is that the concentrations of these substances increase. Therefore, if we take benzodiazepines and alcohol together, the alcohol will make the action of the drug greater.
On the other hand, both substances share the main effect, since they are depressants. Therefore, the effect is enhanced.
The consequences of mixing benzodiazepines and alcohol can be drowsiness, loss of balance, decreased heart rate, difficulty breathing and loss of consciousnessamong other.
This article is merely informative, at Psychology-Online we do not have the power to make a diagnosis or recommend a treatment. We invite you to go to a psychologist to treat your particular case.
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