How diazepam works
Diazepam is a drug from the benzodiazepine group and as such has anxiety-relieving, sedative, muscle-relaxing and antispasmodic effects.
The active substance influences the nerve cells in the brain stem and the limbic system – a functional unit of the brain that is essentially responsible for a person’s state of mind. Diazepam enhances the inhibitory effect of a transmitter substance (gamma-aminobutyric acid) and thus reduces the excitability of the cells.
This relieves anxiety and tension and provides emotional calming. At the same time, emotional impairment has a lesser effect on the autonomic nervous system, which controls vital functions such as heartbeat, blood pressure, breathing and digestion.
Absorption, breakdown and excretion
This produces degradation products that are also effective (active metabolites) and are slowly excreted in the urine. The half-life of diazepam – i.e. the period of time after which about half of the active substance has been excreted – is approximately 48 hours.
To prevent the active substance from accumulating in the body, the dosage prescribed by the doctor must be strictly adhered to!
When is diazepam used?
The areas of application (indications) of diazepam are:
- for premedication (preparation for anesthesia) before diagnostic or surgical procedures
- Conditions with increased muscle tension (e.g. status epilepticus = persistent epileptic seizure)
- Sleep problems
How diazepam is used
Diazepam tablets and diazepam drops are taken with a glass of water either before a meal or some time after. Diazepam suppositories are inserted into the anus, and rectal tubes are emptied into the anus according to the product information.
An evening intake is half an hour before bedtime. The drug should not be taken on a full stomach, because otherwise the onset of action is delayed. It also helps to avoid side effects such as fatigue and lack of concentration the next morning.
What are the side effects of diazepam?
Side effects are dose-dependent and occur mainly at the beginning of treatment. The main adverse effects include daytime sleepiness and drowsiness with impaired alertness and responsiveness.
Other possible side effects include drowsiness, dizziness, confusion, gait and movement disorders, headache, and temporary memory lapses.
Prolonged or repeated use of diazepam may decrease its effectiveness. With prolonged use of high doses, temporary disturbances such as slowed or slurred speech, visual disturbances, and unsteadiness of movement and gait are also possible.
What should be considered when using diazepam?
Contraindications
In certain other cases, use is recommended only when absolutely necessary and after a careful risk-benefit assessment, such as acute intoxication with alcohol or other centrally depressant substances, severe liver damage, severe respiratory failure, and narrow-angle glaucoma (a form of glaucoma).
Drug interactions
Grapefruit juice increases the absorption of diazepam in the intestine and decreases its breakdown.
Simultaneous use of diazepam and other centrally depressant drugs (such as sleeping pills, some painkillers, anesthetics, etc.) increases the sleep-inducing and respiratory depressant effect.
The effect of drugs that reduce muscle tension (muscle relaxants) may be enhanced by diazepam. The degradation of diazepam may be accelerated by phenobarbital and phenytoin (anti-epilepsy drugs), which shortens its duration of action.
If you are newly prescribed other medications in addition to diazepam (including over-the-counter preparations), inform your doctor to be on the safe side.
Diazepam withdrawal symptoms
Diazepam can lead to mental and physical dependence if used for a long time. When stopping therapy, withdrawal symptoms such as sleep disturbances, increased dreaming, anxiety and tension, and inner restlessness may therefore occur.
Children and adolescents
Diazepam may be administered to infants as young as six months of age if indicated.
Pregnancy and lactation
Studies on several thousand pregnancies under diazepam therapy showed no evidence of malformations of the embryo. Nevertheless, to be on the safe side, diazepam should not be used during pregnancy.
Single doses during breastfeeding (e.g. for acute antiepileptic treatment) are possible. In this case, a break from breastfeeding is not necessary. In the case of continuous administration, attention must be paid to side effects in the infant such as sedation, weakness in drinking and weight loss.
How to obtain medicines with the active ingredient diazepam
Preparations containing diazepam require a prescription in Germany, Austria and Switzerland, and are therefore only available from pharmacies on prescription.
How long has diazepam been known?
Diazepam was developed by pharmacist and chemist Leo Henry Sternbach in New Jersey when he was researching the chemical group of benzodiazepines. Before that, in 1957, he had already succeeded in producing substances in his laboratory that turned out to be highly effective drugs for sedation.
What you should also know about diazepam
Therefore, during treatment with diazepam, driving ability and ability to work with machines may be impaired.