Tetrazepam

Tetrazepam belongs to the group of benzodiazepines and has a muscle-relaxing, sedative, anxiolytic, sleep-inducing and anticonvulsant effect. In April 2013, the European Medicines Agency (EMA) recommended that the drug be withdrawn from the market because it can cause severe skin reactions and therefore the risk of the drug outweighs the benefit. According to the EMA, tetrazepam is no longer available in the European Union. Tetrazepam should not be discontinued suddenly and medical advice should be sought. As with other medicines from the benzodiazepine group, there is also a risk of dependence with tetrazepam.

Tetrazepam is used as a muscle relaxant, especially for seizures or chronic pain caused by muscle tension. There are more suitable drugs from the benzodiazepine group for use as a sedative, anxiolytic or sleep-inducing medication.

Tetrazepam acts on the GABA-A receptors and increases the effect of the neurotransmitter GABA when it is present. This receptor binding results in an increased influx of chloride ions, which in turn leads to an increased electrical voltage in the cell (hyperpolarization). This effect protects the cell from overexcitation. Tetrazepam is GABA-dependent, which means that tetrazepam can only work if GABA binds to the same receptor, i.e. they must bind to the receptor at the same time. The advantage of this is that the risk of respiratory depression, i.e. respiratory arrest due to muscle paralysis, is reduced compared to drugs used in the past. Tetrazepam leads relatively quickly to habituation, which can lead to dependence.

Tetrazepam is absorbed via the gastrointestinal tract and is 83-87% bound to plasma proteins after ingestion by tablet. The maximum plasma concentration is reached after 1.5-2 hours. Tetrazepam is metabolized in the liver and excreted almost exclusively via the kidneys. A steady-state condition is reached after approx. 3 days, which means that the full effect is only achieved after a constant intake of the drug for 3 days.

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

The dose is generally increased gradually at the beginning in order to achieve the optimum effect. The usual dose for adults is 50 mg per day. If the desired effect is not achieved, the dosage can be slowly increased up to 400 mg per day (for severe convulsions).

The following side effects may occur:

Frequent:

• Speech and movement disorders
• Nausea and vomiting

Occasional:

• Allergic skin reactions

Rarely:

• Diarrhea or constipation

Very rare:

• Profuse salivation
• Dry mouth
• Increased thirst
• Urinary disorders
• menstrual disorders
• Decreased sex drive

It can also lead to

• memory lapses
• impaired reaction time
• dizziness
• fatigue
• muscle flaccidity
• low blood pressure
• liver cell damage
• bile stasis
• hypersensitivity reactions
• severe skin reactions (DRESS syndrome, Stevens-Johnson syndrome, or toxic epidermal necrolysis)
• lack of emotion
• reduced alertness
• headaches
• double vision
• delusions
• fits of rage
• mental disorders
• and inappropriate behavior.

In older patients, there may also be an increased risk of falls. In children and older people, aggressive behavior, states of agitation, hallucinations, difficulty falling asleep and sleeping through the night can occur. Tetrazepam therapy can cause an existing depression to recur.

There is a risk of developing an addiction to tetrazepam. The higher the dose or the duration of treatment, the higher the risk of dependence. This already applies to therapeutic applications. After four weeks at the latest, it should be checked whether treatment with tetrazepam is still necessary.

Interactions may occur with the following medicines:

• with other medicines from the benzodiazepine group, as the risk of withdrawal symptoms may be increased.
• with medicines containing alcohol, as this can increase drowsiness.

Effects and side effects may be increased with the following medicines:

• medicines containing morphine
• medicines from the barbiturate group
• H1-sedating antihistamines
• sleeping pills, anticonvulsants, anesthetics and anxiolytics that do not belong to the benzodiazepine group
• neuroleptics
• certain medicines to lower blood pressure
• medicines for muscle relaxation
• medicines containing the active ingredients cisapride, cimetidine or omeprazole
• medicines containing the active ingredient clozapine, as these can cause a risk of collapse with respiratory and/or circulatory arrest.

Interactions may occur with the following medicines:

• Antihypertensives
• beta-blockers (for the treatment of high blood pressure and certain heart diseases)
• heart-strengthening medicines (cardiac glycosides)
• blood coagulants
• Medicines for the treatment of blood sugar
• H2 receptor blockers (for allergies or nausea)
• Contraceptive medicines ("the pill")

Taking tetrazepam together with alcohol can lead to increased drowsiness and increase the risk of dependence on tetrazepam.

Tetrazepam should not be taken:

• if you are allergic to tetrazepam
• severe breathing difficulties
• in forms of muscle weakness
• severe liver dysfunction

Caution should be exercised with:

• nervous disorders with gait instability, balance or speech disorders
• intoxication with alcohol, sleeping pills or painkillers
• medicines for the treatment of mental and emotional disorders (antidepressants)
• impaired liver function
• impaired kidney function

Approved from the age of 2. Only used in children and adolescents if absolutely necessary.

During pregnancy, tetrazepam should only be administered very carefully and after strict consideration of the risk-benefit aspect. It should be noted that only very few experience reports are available.

Tetrazepam should not be used during breastfeeding as it passes into breast milk. If taken for more than 2 days, breastfeeding should be discontinued.