How tetrazepam works
Due to its chemical structure, tetrazepam belongs to the benzodiazepine group, but in the literature it is often listed among the centrally acting muscle relaxants. This is because its muscle-relaxing, antispasmodic effect – compared with that of other benzodiazepines – is much more pronounced.
The human nervous system has various messenger substances (neurotransmitters) that can have an activating or inhibiting effect. Normally, they are in balance and ensure an appropriate response to external circumstances such as rest or stress.
One of these neurotransmitters – GABA (gammaaminobutyric acid) – has an inhibitory effect on the nervous system as soon as it binds to its docking sites (receptors). Tetrazepam enhances the effect of this substance, resulting in muscle relaxation and sedation.
Absorption, degradation and excretion
When was tetrazepam used?
The indications for the use of tetrazepam included:
- Muscle tension, especially as a result of diseases of the spine or the joints near the axis
- @ Spastic syndromes with pathologically increased muscle tension of any cause
How tetrazepam was used
The active substance was used mainly in the form of tablets and drops. The dosage at the beginning of therapy was 50 milligrams per day. It could then be slowly increased up to 400 milligrams daily.
The dose had to be reduced in children, elderly patients, and patients with liver or kidney dysfunction.
Increases and decreases in the dose always had to be gradual with tetrazepam, that is, gradually over a period of several weeks.
What are the side effects of tetrazepam?
Occasionally (in 0.1 to one percent of those treated), allergic skin reactions and muscle weakness occurred. Even more rarely, severe skin reactions (reason for withdrawal from the market), menstrual irregularities in women, and decreased sexual desire (libido) occurred.
Severe skin reactions can occur unpredictably and suddenly even after years of taking tetrazepam.
Another possible side effect is a reversal of action (paradoxical tetrazepam action): Although the active ingredient is supposed to have the opposite effect, it can also paradoxically trigger activation of the nervous system and, as a result, states of agitation with anxiety, sleep disturbances, aggression, and muscle spasms.
What was to be considered when taking tetrazepam?
Contraindications
Tetrazepam should not be used in:
- Hypersensitivity to the active substance or to any of the other components of the medication
- decompensated respiratory insufficiency (respiratory failure)
- Sleep apnea syndrome
Drug interactions
Tetrazepam may increase the effect of other centrally acting or depressant drugs (including psychotropic drugs, analgesics, sleeping pills, allergy medications). The sedative effect of alcohol is also enhanced by tetrazepam, so alcohol consumption is discouraged during use.
Simultaneous use of cisapride (increases intestinal motility), omeprazole (“stomach protector”), and cimetidine (heartburn medicine) may prolong the effect of tetrazepam. This also applies to neostigmine (agent against increased muscle tone).
Traffic ability and operation of machines
The active ingredient tetrazepam significantly limits the ability to react. Therefore, patients have been advised against operating heavy machinery or actively participating in road traffic after taking the drug.
Age Limitation
Tetrazepam is contraindicated in children under one year of age.
Pregnancy and lactation
These are states of weakness in the newborn with weakness in drinking, slowed breathing rate, decreased pulse, lack of oxygen, and muscle weakness. Instead, switch to better studied medications:
Ibuprofen and diclofenac (up to 30 weeks of gestation) represented well-tested alternatives in this regard. If necessary, the better-studied diazepam could also be used for a short time.
Like all benzodiazepines, tetrazepam passes into breast milk. During lactation, therefore, the drug was contraindicated or weaning was required. Even for treatment lasting one to two days, the manufacturer recommended that breastfeeding be discontinued until approximately 48 hours after the last dose, and that milk be pumped and discarded.
How to receive medications with tetrazepam
The active ingredient is also not commercially available in Switzerland.
How long has tetrazepam been known?
Tetrazepam has been known as a drug from the group of so-called benzodiazepines for a relatively long time. Initially, the drug was used to calm and relieve anxiety.
Soon, the muscle-relaxing effect of the active ingredient was also recognized. For a long time, tetrazepam was therefore successfully used for painful muscle tension – until the rare risk of serious skin reactions was discovered.