Oxazepam: What It Is And How It Works

Oxazepam is a short-acting benzodiazepine used to combat different anxiety scenarios in addition to helping to overcome withdrawal symptoms in alcoholics.

Before delving into the characteristics of this drug, we must know a little the pathology for which its action is directed.

The anxiety

Anxiety can be a normal emotion or a psychiatric disorder depending on the intensity and impact on the patient.

In normal situations, anxiety is a component of normal mental activity that participates in defense mechanisms and allows the body to adjust to stressful situations.

What happens is that this situation becomes pathological when limits are exceeded, nullifying or hindering adaptation to the stressful situation.

The feeling of anxiety can be described as the experience of a feeling of threat, of tense expectation of the future and of alteration of the psychosomatic balance in the absence of real danger.

When under the effects of anxiety, the patient suffers different simultaneous feelings such as:

• Fear
• Apprehension
• Anguish in the face of something “threatening”
• Irritability

Which, together, gives rise to various symptoms such as:

• Sweating
• Palpitations
• Insomnia
• Headaches
• Fatigue

What is an anxiolytic drug?

Drugs used to combat anxiety, such as oxazepam or lorazepam, are called anxiolytic drugs. These, theoretically, alleviate or suppress the anxiety syndrome without producing sedation or sleep.

Normally in small doses they are capable of producing anxiolysis, but as the dose is increased, sedative effects appear, coma and can even lead to death from intoxication.

In addition to these two terms, anxiety and anxiolytic drugs, we will look in more detail at the following characteristics of oxazepam:

• Mechanism of action.
• Pharmacokinetics.
• Pharmacokinetic actions.
• Adverse reactions.

Mechanism of action of Oxazepam

Oxazepam is a short-acting drug for the treatment of anxiety. To achieve its anxiolytic action, this drug has two complementary mechanisms.

• Facilitates the transmission of GABA.
  • GABA is a neurotransmitter with the ability to inhibit or reduce neuronal activity, therefore, when oxazepam binds to the GABA A receptor, a change will occur in it that will lead to a better binding with the neurotransmitter, enhancing its inhibitory capacity.
• It binds to specific sites of the GABA-BZD receptor complex.
  • This complex has several domains: α1, ß2, γ2. It is important to achieve the selectivity of these receptors to separate the hypnotic action from the anxiolytic, specifically, for anxiolysis, the receptor involved is BZ2 (ω2).

Pharmacokinetics

Oxazepam, in general, like the other benzodiazepines, is well absorbed orally. It is also bound in a high percentage to plasma proteins, so care must be taken as it can interact with other drugs that have these characteristics.

It is important to know that it undergoes hepatic metabolism, since it can interact with other drugs that are metabolized in this way.

As it only undergoes a reaction for its metabolism, it is useful in geriatric patients, since at this age the functionality of the liver is usually diminished. By requiring fewer metabolic reactions, patients at this age will clear it more easily.

Pharmacological actions

Depending on the characteristics of the benzodiazepines, one action or the other can develop, or even both at the same time. Oxazepam has mainly anxiolytic and anticonvulsant actions.

Anxiolytic action is characteristic of the BZ2 receptor. Binding to this complex triggers actions that decrease anxiety and aggressiveness. We have to distinguish between healthy people taking oxazepam and patients with anxiety:

• In healthy people : At therapeutic doses it does not alter the performance of physical or mental exercises. At higher doses they can cause drowsiness, lethargy, ataxia and muscle weakness.
• In patients with anxiety : Oxazepam relieves both subjective tension and subjective symptoms, but is not very effective in situations of panic, phobias and non-neurotic anxiety.

In addition to these effects, they can also produce effects on aggressiveness, memory, the cardiovascular and respiratory systems, depressing them, and decreases the ability to speak and express themselves.

Adverse reactions

The adverse effects of oxazepam derive from a long action.  They especially affect the central nervous system:

• Sedation
• Ataxia (difficulty coordinating movements)
• Anterograde amnesia
• Dysarthria
• Tolerance-dependency