Diazepam is a medication of the benzodiazepine group. It acts on the central nervous system with anxiolytic, sedative and anticonvulsant effects. It is long-acting and its use is widespread in anxiety disorders, epileptic seizures and febrile disorders or as a muscle relaxant.
How does diazepam work?
Diazepam is a central nervous system depressant, that is, it decreases the activity of neuronal circuits. It acts mainly in the limbic system, thalamus and hypothalamus. This depressing action is due to Diazepam potentiates the action of an inhibitory neurotransmitter called gamma-aminobutyric acid (GABA).
Neurotransmitters are chemical substances that participate in neuronal communication, connecting some neurons with others and facilitating the transmission of signals necessary for the correct functioning of the nervous system. In other words, when a neuron receives a signal, it transmits it to the next by releasing a neurotransmitter. This produces two changes in the second neuron:
- Activation. If the neurotransmitter is exciter or activator, making the signal continue to be transmitted.
- Inhibition. If the neurotransmitter is inhibitory, causing the transmission of the signal to cease.
Therefore, diazepam, along with other benzodiazepines, will have a depressant or inhibitory action of the central nervous system by promoting the action of the GABA neurotransmitter . The levels of this neurotransmitter are abnormally low in some psychiatric disorders such as depression, anxiety and epilepsy, from which the anxiolytic and anticonvulsant effects of benzodiazepines such as diazepam can be deduced.
Diazepam is a long-acting benzodiazepine , its half-life is about 30-60 hours. It can be administered in different ways:
- Oral route , with very rapid absorption. In medicines used orally, it must be borne in mind that the action is not instantaneous since it begins when the drug is absorbed in the digestive system, mainly in the stomach and first tracts of the intestine.
- Rectal route , useful in the form of microenemas (liquid solution that is administered rectally). It is a very used form in pediatric convulsions given its rapid action.
- Intravenous route , with a very fast action, approximately 5 minutes after adminsitration.
- Intramuscular route , less and less used since absorption is slow when administered through this route.
Once in the blood it is widely redistributed throughout the tissues. It crosses the blood-brain barrier that separates the nervous system from the rest of the body , hence it can be used for disorders of the nervous system such as anxiety or epilepsy. It also crosses the placental barrier reaching fetal tissues, a fact that must be taken into account if administered in pregnant women and during breastfeeding, since it also reaches breast milk.
The metabolism of diazepam is mainly hepatic, so care must be taken in its administration along with other medications of hepatic metabolism or alcohol, or in patients with some type of liver disease, such as cirrhosis or liver failure.
Indications of diazepam
- Treatment of anxiety : it is mainly used orally, with different doses depending on the age of the patient and the degree of anxiety. If it is very intense, you can resort to intravenous administration.
- Treatment of abstinence. It can be caused by an addiction to alcohol or by addiction to benzodiazepines. The intravenous route is used, sometimes high doses are necessary in the first days of abstinence. It also appears in the treatment of delirium tremens , a condition that appears in severe cases of withdrawal from ethyl alcohol that leads to hallucinations and other distortions of reality.
- Muscle relaxant: it is used orally or intravenously for muscle contractions of different nature. Included here are those pathologies that occur with reflex contractures, in which the muscle remains contracted continuously due to a defense mechanism of the same. A characteristic example is renal colic, in which the abdominal muscles are reflexively contracted, or the torticollis.
- Anticonvulsant: benzodiazepines are one of the groups of drugs known as antiepileptics, used effectively in the treatment of epilepsy . They are also used in non-epileptic seizures, such as in febrile seizures or in drug-induced seizures. In this case rectal administration may be useful, especially in childhood febrile seizures.
- In medical procedures that require sedation , such as an endoscopy, due to its hypnotic effect .