Flurazepam

ATC CodeN05CD01
CAS number17617-23-1
PUB number3393
Drugbank IDDB00690
Empirical formulaC21H23ClFN3O
Molar mass (g·mol−1)387,878
Physical statesolid
Density (g·cm−3)1,2
Melting point (°C)79,5
Boiling point (°C)551,4
Solubility0.009582 mg/mL

Basics

Flurazepam is an active ingredient that is used to treat sleep disorders. It belongs to the group of benzodiazepines, which have a calming and sleep-promoting effect. Flurazepam is a long-acting benzodiazepine. It has a rapid onset of action and is based on binding to the GABA receptors. Like all other benzodiazepines, flurazepam can also be addictive. Flurazepam is also often abused as a narcotic. It is usually present in medicines as flurazepam hydrochloride. It is white, crystalline and very easily soluble in water. Dream times remain unaffected when taking flurazepam.

Graphic structural formula of the active substance flurazepam

Effect

Flurazepam works by shortening the sleep onset latency, i.e. the time it takes to fall asleep, and reducing the waking phases. It binds to the GABA-A receptors in the brain and increases the effect of gamma-aminobutyric acid (GABA) there. Furthermore, there is also an increased influx of chloride ions, which leads to the cell becoming unexcitable and thus triggers the desired calming effect. An important factor is that benzodiazepines have no effect without GABA. This is not the case with barbiturates, although there is a higher risk of respiratory depression with barbiturates. If flurazepam is taken for longer than 2 weeks, a habituation effect occurs, which means that the dose has to be increased to achieve the same effect. This habituation effect is the reason for the dependence potential of flurazepam.

Flurazepam is absorbed from the gastrointestinal tract within 30 minutes. The half-life, i.e. the time the body needs to excrete half of the active substance, is 2.3 hours on average.

Dosage

Always take flurazepam exactly as described in the package leaflet or as advised by your doctor.

The usual recommended starting dose is 15 mg daily, but this can be increased to 30 mg daily if necessary. In general, the dosage should be kept as low as possible.

In older patients, the daily dose should NOT exceed 15 mg .

Side effects

The following side effects may occur:

Frequent:

  • dampened emotions
  • abnormal drowsiness
  • reduced attention
  • movement coordination disorders
  • dizziness
  • headaches
  • taste disturbances
  • Impairment of memory
  • Muscle weakness, which leads to an increased risk of falling and therefore an increased risk of fractures in older people
  • Tiredness

Occasional:

  • Discomfort in the gastrointestinal tract
  • Nausea
  • Skin reactions
  • Changes in sexual behavior

Rarely:

  • Hypersensitivity reactions
  • visual disturbances
  • Low blood pressure
  • Respiratory depression
  • urinary retention

Very rare:

  • Jaundice
  • elevated liver enzymes

Frequency unknown:

  • Blood disorders (e.g. thrombocytopenia, leukopenia,...)
  • confusion
  • hallucinations
  • addiction
  • Withdrawal symptoms
  • depression
  • Psychiatric and paradoxical reactions
  • suicidal thoughts
  • extrapyramidal diseases
  • risk of falling
  • memory lapses

Like other benzodiazepines, flurazepam can be addictive.

Flurazepam can increase depression, provoke suicidal thoughts, cause sensory illusions and memory problems .

Interactions

Interactions may occur if the following medicines are taken at the same time:

  • Sleeping pills, sedatives and anesthetics
  • painkillers
  • anxiolytics
  • anti-epileptic drugs
  • Allergy medication (antihistamines)
  • neuroleptics
  • antidepressants
  • Medication against HIV
  • Opioids - life-threatening breathing difficulties can occur, which can lead to death
  • Muscle relaxants - there may be an increased risk of falls
  • Cimetidine and omeprazole can increase the effect of flurazepam
  • Antibiotics of the macrolide type such as erythromycin can increase the effect of flurazepam
  • Contraceptives (the 'pill') can increase the effect of flurazepam
  • Rifampicin can weaken the effect of flurazepam
  • 4-Hydroxybutanoic acid - life-threatening respiratory depression may occur
  • Alcohol

Contraindications

Flurazepam must NOT be taken in the following cases:

  • in case of allergy to flurazepam or other benzodiazepines
  • in case of myasthenia gravis
  • in the case of existing or previous dependence on medication, alcohol or drugs
  • severe respiratory disorders
  • severe liver damage
  • for muscle and movement disorders
  • acute poisoning with alcohol, sleeping pills, painkillers or psychotropic drugs

Age restriction

Flurazepam should NOT be used under the age of 18 .

In older patients, the dose should be as low as possible because there may be an increased risk of falls and, as a result, bone fractures.

Pregnancy & breastfeeding

Pregnancy

Flurazepam should only be used during pregnancy after consultation with your doctor.

In the first trimester of pregnancy, an increased risk of malformation was discussed in earlier studies. More recent studies have not been able to confirm this connection.

In the 2nd and 3rd trimester of pregnancy, short-term use of flurazepam is acceptable. However, prolonged regular use can trigger serious symptoms in the newborn (temperature regulation disorders, drinking difficulties, low blood pressure, etc.). In addition, severe withdrawal symptoms can occur in newborns, such as seizures.

In the case of benzodiazepine dependence in pregnant women, withdrawal during pregnancy should be avoided at all costs, as this can lead to severe withdrawal symptoms that are harmful to the unborn child. Delivery should always take place in a clinic with a neonatology unit.

Breastfeeding

Flurazepam should only be used during breastfeeding after consultation with your doctor . If flurazepam is taken regularly over a longer period, breastfeeding should be discontinued as flurazepam passes into breast milk.

Thomas Hofko

Thomas Hofko



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