Anxiolytics

Anxiolytics are drugs used to quell anxiety disorders, insomnia and physical problems related to the state of excessive apprehension and agitation. There are several classes of substances that have such activity, here’s what they are and how they act.

What are they

Anxiolytics are defined as all those drugs with calming and relaxing effects on the central nervous system, used in the treatment of anxiety disorders and somatic problems associated with them (insomnia, tachycardia, excessive sweating, muscle and mental tension, etc.).

Like the other substances generally used in psychiatry, anxiolytics are defined as “psychotropic drugs” because their priority action is carried out at the brain level (through the modulation of the activity of well-defined nervous areas and circuits), determining clinical effects primarily at the psychoemotional and behavioral level.

These medicines are widely used all over the world, well proven by decades of use on millions of people, and generally considered effective and safe, when taken on prescription and monitored by a licensed health professional (family doctor, psychiatrist, etc.).

Not infrequently, unfortunately, anxiolytics are subject to improper use, being used in contexts where they do not find specific indication or by people in which they could be contraindicated, in excessive doses or for too prolonged periods, exposing to the risk of side effects and / or unfavorable interactions with other drugs or substances of abuse (drugs and alcohol) possibly taken. A behavior that must be absolutely avoided.

Let’s see how an anxiolytic works, in the context of which therapies it is prescribed, what consequences it can have on the psychological tension and quality of life of those who take it and why it is important to respect the doctor’s instructions on dosage, times and methods of use.

How they work

There are different categories of drugs with an anxiolytic effect that they exert through different mechanisms of action. In general, they all act by influencing the electrical activity of certain brain areas – those involved in the origin of anxiety, depression and sleep disorders – but exert their effect by modulating the action of different neurotransmitters.

What are they?

The main classes of anxiolytic drugs are:

  • benzodiazepines
  • GABArgic non-benzodiazepines
  • Azapironi
  • SSRI antidepressants (selective serotonin reuptake inhibitors).

The active ingredients belonging to the first two groups (benzodiazepines, non-benzodiazepine GABAergics) all act, albeit in a slightly diversified way, binding to gamma-aminobutyric acid (GABA) receptors – a neurotransmitter that has the function of lowering the level of activity of nerve cells – enhancing their inhibitory action.

Substances belonging to the other two groups (azapyrones and SSRI antidepressants) interfere with another neurotransmitter system: serotonin.

A separate mention deserve barbiturates, compounds widely used in the past as sedatives and hypnotics that, given their poor safety, have been replaced, since the sixties, by benzodiazepines. Currently, barbiturates are used only as antiepileptics and anesthetics, while they are generally not expected to be administered in patients suffering from anxiety disorders.

Who cares what

Each class of anxiolytic drugs has different uses, summarized here and explained in detail below.

Benzodiazepines Anxiety reduction and sleep induction Useful to control acute anxiety and to counteract insomnia, preferably for short periods
GABAergic non-benzodiazepines Sleep induction/regulation Useful to promote falling asleep and to counteract insomnia associated with anxiety
Azapironi Anxiolytic and antidepressant effect Useful to control anxiety especially if associated with depressive manifestations
SSRI antidepressants Antidepressant and sedative effect Useful to control anxiety especially if associated with depressive manifestations

Benzodiazepines. It is the class of anxiolytic drugs still most widely used in the treatment of anxiety, especially in the acute / initial or occasional phase, but also in the medium-long term. In addition to anxiety disorders and insomnia, the following are used:

  • in people with panic disorder or obsessive-compulsive disorder
  • when temporary sedation is required to facilitate a medical procedure
  • for muscle relaxant purposes in muscle spasms.

The numerous molecules belonging to this group exert their two main therapeutic effects – anxiety reduction and sleep induction – in somewhat different proportions depending on the specific activity on GABA receptors and the duration of action. Therefore, some benzodiazepines are more effective in alleviating anxiety and related physical symptoms, while others are more suitable for the pharmacological treatment of sleep disorders.

Benzodiazepines have the disadvantage of inducing addiction, resulting in a gradual loss of efficacy after a few weeks of use and the need to increase the dosage to achieve the same therapeutic effect (but with greater side effects). This tolerance towards the pharmacological action tends to induce physical dependence: for this reason, in general, treatments with anxiolytics of this class are preferably short-lived, intermittent or “as needed” (if the need is not too frequent or prolonged).

GABAergic not benzodiazepines. The drugs belonging to this group, which includes different categories of molecules recently introduced in medicine (cyclopyrroles, imidazopyridine, pyrazolopyrimidines), are particularly suitable as sleep inducers / regulators, as in relation to this activity they have the advantage, compared to benzodiazepines, of not causing addiction (resulting, therefore, also associated with a lower risk of abuse).

Azapironi. Of this class, in Italy, there is currently a single molecule on the market, buspirone, with both anxiolytic and antidepressant effects. As an anxiolytic, buspirone achieves its effectiveness more gradually than benzodiazepines (3-4 weeks): for this reason, it is a drug less indicated in cases that need a rapid anti-anxiety effect, but it is more suitable in long-term treatment and in elderly patients (as it induces less daytime sleepiness and less muscle weakness than other anxiolytics).

SSRI antidepressants. The drugs of this group can combine their main antidepressant action with a sedative effect, which has proved useful in particular forms of anxiety (obsessive-compulsive disorder and panic disorder) and in depressive forms with a strong anxious component. In general, higher doses than those expected in the treatment of depression are required to achieve the anxiolytic effect, but in the majority of patients SSRI therapy remains well tolerated.

Effects

Putting aside barbiturates, the most important adverse effects are given by benzodiazepines. The real side disorders are generally due to an accentuation of the therapeutic effects (excessive sedation, daytime sleepiness, muscle weakness, lightheadedness, mental confusion and difficulty concentrating, pressure drop and dizziness).

The side effects of benzodiazepines may be greater and less predictable in adolescents and the elderly: two age groups in which treatment should be initiated under strict medical supervision and at the lowest dose, to be increased gradually (if well tolerated) until the desired clinical effect is achieved.

Although they can become severe when alcohol or other sedative drugs are taken at the same time, these side effects of benzodiazepine therapies can be controlled by changing the dose of the drug in use or by using other molecules of the same group (after medical evaluation and appropriate therapeutic review).

The biggest problem is, however, represented by the tendency of benzodiazepines to cause addiction, especially towards the hypnotic action, and physical dependence, consisting in the immediate appearance of serious psychological discomfort and physical symptoms at the suspension of the drug, which generates the feeling of “not being able to do without it anymore”.

To avoid the typical problems of benzodiazepine “withdrawal crisis” and the return of anxiety to amplified levels (rebound), when it is considered appropriate to interrupt a treatment in progress for a few consecutive weeks, it is necessary to plan together with the doctor the gradual reduction of the dosage taken, up to completely discontinuing the drug. Generally, this phase takes a couple of weeks, but the period may be longer if you were taking a high dose of benzodiazepines.

There are much fewer side effects on the cognitive level, mental fatigue and muscle weakness, as well as the risk of addiction and physical dependence, associated with the use of non-benzodiazepine GABAergic anxiolytics and buspirone.

With SSRI antidepressants, on the other hand, at the beginning of therapy there may be a worsening of anxious symptoms or difficulty falling asleep. This happens because these drugs have an “activating” action, which makes them particularly effective against depressive manifestations, but which can be temporarily counterproductive in those who are already “activated” by anxiety disorders. For this reason, SSRIs are often combined with a benzodiazepine in the first weeks of therapy, which is then discontinued when the anti-anxiety effect of SSRIs has stabilized.

SSRIs should be used with great caution in adolescents because symptoms apparently referable to an anxiety disorder and associated insomnia could actually be manifestations of the onset of an undiagnosed bipolar disorder, which would inevitably be worsened by treatment with antidepressants. For this reason, SSRIs (as well as any other psychotropic drug), should be taken by adolescents only after a thorough psychological / psychiatric evaluation and carefully respecting what is prescribed by the doctor.

In this regard, it should be remembered that all anxiolytics are medicines for which a medical prescription is mandatory and which should only be used under the strict supervision of the attending physician. Any careless behavior or abuse exposes you to the risk not only of experiencing side effects, but also of seeing anxiety disorders worsen rather than improve, greatly complicating subsequent treatment and the restoration of a good quality of life.

Natural remedies

When anxiety disorders and / or insomnia are mild and you do not want to resort immediately to a pharmacological treatment, you can try to take advantage of the calming properties of some plants and plant extracts, in use for decades in popular tradition and in natural medicine.

Among the herbal remedies useful to counteract anxiety and insomnia (with variable effectiveness from person to person), we can include the extracts of: passionflower (Passiflora incarnata), valerian (Valeriana officinalis), escolzia (Eschscholtzia californica), lemon balm (Melissa officinalis). The trusted pharmacist will be able to indicate the most suitable for the individual case and the correct administration methods depending on the formulations (tablets, drops, sachets or infusion preparations).

The intake of these natural remedies in the form of herbal teas and infusions can be particularly effective if the moment of their preparation is structured as a sort of “ritual” in which, through simple and slow gestures that interrupt the routine, time and attention are dedicated to themselves, carving out a space for reflection and relaxation. A calm and pleasant background music can further facilitate the removal of negative thoughts and psychological tension, amplifying the anti-anxiety and calming effect of plant active ingredients.

Joycelyn Elders is the author and creator of EmpowerEssence, a health and wellness blog. Elders is a respected public health advocate and pediatrician dedicated to promoting general health and well-being.

The blog covers a wide range of topics related to health and wellness, with articles organized into several categories.

Leave a Reply

Your email address will not be published. Required fields are marked *