flurazepam

Flurazepam is a hypnotic drug that has anxiolytic, sedative, anticonvulsant and muscle relaxant properties. From a chemical point of view, flurazepam is a benzodiazepine.

Indications

For what it uses

Flurazepam - Chemical Structure

The use of flurazepam is indicated for the treatment of short-term insomnia.

Treated insomnia may be related to anxiety.

Warnings

It is important to know that flurazepam - as, indeed, all benzodiazepines - is indicated for the treatment of insomnia only when it becomes a serious and debilitating disorder for the individual.

Flurazepam should be administered with caution in elderly and debilitated patients. In these cases, a reduction in the dose of drug administered may be necessary.

Since flurazepam has muscle relaxant properties, in elderly patients there may be an increased risk of falls and subsequent fractures.

In patients with chronic respiratory failure or liver failure, a reduction in the administered dose may be necessary.

Flurazepam should not be used in patients with spinal or cerebellar ataxia.

Extreme caution should be used when administering benzodiazepines in patients with a history of alcohol and drug abuse.

Alcohol consumption should be avoided during treatment with flurazepam.

Flurazepam should not be used in children.

Flurazepam may impair the ability to drive and use machines.

Patients who make repeated use of flurazepam may experience tolerance. That is, there may be a decrease in the hypnotic effects induced by the flurazepam itself.

Interactions

The sedative action of flurazepam can be increased by concomitant alcohol intake .

The central nervous system depressive effect induced by flurazepam may be increased by concomitant administration of drugs, such as:

Barbiturates ;
Antipsychotics ;
Other hypnotic, sedative and anxiolytic drugs;
Antidepressant drugs;
Anticonvulsant drugs;
Antihypertensive drugs.

The concomitant administration of flurazepam and theophylline or aminophylline can reduce the sedative effect induced by flurazepam.

Concomitant administration of flurazepam and opioid analgesics may lead to an increase in euphoria and psychic dependence.

The concomitant administration of flurazepam and hydantoins and barbiturates used in the treatment of epilepsy may cause an increase in toxicity and side effects induced by the flurazepam itself.

Rifampicin (an antibiotic) is able to increase the elimination rate of flurazepam.

Flurazepam should not be administered concomitantly with cimetidine, omeprazole (drugs used to reduce acid secretion of the stomach) or disulfiram (a drug used to treat alcoholism), as these drugs reduce the elimination of flurazepam, thus enhancing the 'action.

Side effects

Treatment with flurazepam can cause various types of side effects, although not all patients experience them.

The main side effects that may occur during flurazepam therapy are listed below.

Psychiatric disorders

Treatment with flurazepam may cause:

Emotional poverty;
Confusion;
Hallucinations;
Depression.

Furthermore, the drug can cause paradoxical symptoms, such as anxiety, sleep disorders, insomnia, nightmares, agitation and restlessness, irritability, aggression, delusions, emotional disturbances, suicidal ideation and behavior.

Addiction

Flurazepam can lead to the development of physical and mental dependence. The risk of developing dependence is directly proportional to the dose of drug administered and to the duration of the treatment.

Patients who have abused alcohol and drugs are at greater risk of developing addiction.

Once physical dependence is established, abrupt termination of treatment causes withdrawal symptoms. These symptoms are:

Depression;
derealization;
depersonalization;
Anxiety;
Confusion;
Nervousness;
Restlessness;
Irritability;
Hallucinations;
Epileptic shocks;
Rebound insomnia;
Mood changes;
Sweating;
Diarrhea;
Headache;
Muscle pains;
Hypersensitivity and intolerance to sounds (hyperacusis);
Hypersensitivity to light and physical contact.

It is therefore recommended to gradually stop the treatment.

Rebound symptoms

Once the treatment with flurazepam is finished, so-called rebound symptoms can arise. That is, the symptoms (insomnia and anxiety) that had made it necessary to take flurazepam recur in an aggravated form.

Sometimes these symptoms may be accompanied by restlessness and mood swings.

The rebound symptoms appear more easily when the therapy is stopped abruptly, therefore the gradual suspension of the treatment is recommended.

Amnesia

Treatment with flurazepam may cause anterograde amnesia. The development of this type of amnesia can occur after hours of taking the drug, so patients - after taking the drug - should have an uninterrupted sleep of at least 8 hours.

Memory can be compromised if the patient wakes up at the time of maximum activity of the drug.

Blood and lymphatic system disorders

Flurazepam therapy can cause disorders of the blood cell production system (hemolymphopoietic system). These disorders can cause leukopenia (decrease in white blood cells in the blood), agranulocytosis (decrease in blood levels of granulocytes), thrombocytopenia (reduction in the number of platelets in the blood circulation) and pancytopenia (ie reduction in the number of all blood cells) .

Nervous system disorders

Treatment with flurazepam can cause changes in the sense of taste, drowsiness, ataxia, dizziness, headache, decreased alertness and extrapyramidal disorders.

Eye disorders

After taking flurazepam, visual disturbances may arise, such as - for example - diplopia (double vision).

Hepatobiliary disorders

Flurazepam therapy may cause changes in liver enzyme levels in the bloodstream and may promote the onset of jaundice.

Other side effects

Other side effects that may occur following treatment with flurazepam are:

Allergic reactions in sensitive subjects;
Hypotension;
Respiratory depression, especially at night;
Nausea;
Abdominal pains;
Skin eruptions;
Fatigue;
Muscle weakness;
Urinary retention;
Changes in libido.

Overdose

Generally, taking an overdose of flurazepam should not create life-threatening hazards for patients, unless other substances have been taken at the same time that can depress the central nervous system, including alcohol.

Overdose can occur in both mild and severe form.

The symptoms that occur in the case of mild overdosage are:

lightheadedness;
Confusion;
Lethargy.

In case of severe overdosage, however, the symptoms that can occur are:

Dysarthria;
Changes in vision;
Dystonia;
hypotonia;
Ataxia;
Respiratory depression;
Hypotension.

Very rarely, coma and death can occur.

In the event of an overdose of flurazepam vomiting should be induced within an hour of taking the drug if the patient is conscious, or - if the patient is unconscious - gastric lavage should be performed. The administration of activated charcoal may also be useful.

The pharmacological treatment consists in administering a competitive antagonist of benzodiazepines, flumazenil .

In any case, if you suspect you have taken an overdose of medication, you must contact a doctor immediately and go to the nearest hospital.

Action mechanism

Flurazepam - like all benzodiazepines - works by stimulating the GABA (γ-aminobuttiric acid) system, otherwise called the GABAergic system.

GABA is the main inhibitory neurotransmitter of the brain and performs its biological functions by binding to its specific receptors: GABA-A, GABA-B and GABA-C.

A binding site for benzodiazepines is present on the GABA-A receptor.

Flurazepam - as a benzodiazepine - binds to this site and activates the receptor, thus promoting the cascade of inhibitory signals induced by GABA.

Mode of Use - Posology

Flurazepam is available for oral administration as hard capsules.

The capsules should be taken whole with a little water just before bedtime.

The dosage of flurazepam must be established by the doctor on an individual basis, depending on the severity of the insomnia and the patient's response to therapy.

Generally, the dose of flurazepam administered ranges from 15 mg to a maximum of 60 mg a day.

The treatment can last from a few days up to a maximum of four weeks, including the period of gradual interruption.

In elderly patients, patients with liver and / or kidney disease and in patients with chronic pulmonary insufficiency may need to reduce the dose of the drug administered.

Pregnancy and breastfeeding

The use of the drug by pregnant women is not recommended, except in the case where the doctor does not consider it absolutely necessary.

The administration of flurazepam during the last periods of pregnancy or during labor can cause the following side effects in the fetus or newborn:

Irregularity in the fetal heart rate;
Hypothermia;
hypotonia;
Respiratory depression;
Possibility of development of physical dependence and withdrawal symptoms in the post-natal period.

Because benzodiazepines are excreted in breast milk, flurazepam should not be taken by mothers who are breast-feeding.