Synonyms

diazepam

    definition

    Diazepam is often better known under one of its trade names: Valium ® . It belongs to the group of benzodiazepines, which in turn are among the psychotropic drugs, so they are characterized by an influence on the central nervous system ( CNS ).
    Diazepam is used inter alia for the treatment of anxiety disorders, for premedication (before surgery) and for the interruption of seizures in epilepsy.

    effect

    Valium ® is a benzodiazepine . It works:

    • anxiolytic ( anxiolytic )
    • anticonvulsant (anticonvulsant)
    • muscle relaxant (muscle relaxing)
    • sedative to hypnotic ( damping )

    Valium acts on the group of GABA receptors in the brain that sit on the surface of nerve cells. Here it leads to a damping of the nerve cell.

    The half-life of Valium® is up to 48 hours. Therefore, nowadays, especially when used in patients who are not in inpatient treatment, more active ingredients from the same group, but with a shorter half-life are used. The problem of the long half-life is above all the overhang. This means that the effect of the tablet lingers for a long time. If, for example, she was taken in the afternoon or evening of the previous day, those affected are often still very tired and sleepy the following morning.

    Diazepam is used in the case of arousal and anxiety, alcohol withdrawal syndrome and acute epileptic seizure. Sleep disorders are also used, with benzodiazepines having a lower risk of overhang being preferred because of the long half-life.

    indication

    Benzodiazepines in general are often referred to as tranquilizers, so tranquilizers. They are used inter alia for the treatment of anxiety disorders. They also find application in sleep disorders, with the use of short-acting benzodiazepines such as triazolam, since Valium ® ( diazepam ) has a much too long half-life for this indication and would lead to overhang, ie fatigue, well into the next day,
    Furthermore, Valium ® is often given for premedication, ie before surgery, so here you make use of its anxiolytic and sedating component.
    Also used as anticonvulsant (Greek / Latin for seizures) Valium ®, but not as a standard drug. This is related to the strong addictive potential that benzodiazepines generally possess. It is used here rather in acute seizures to break through the spasms to get the patient out of immediate danger.

    pharmacology

    The fact that Valium ® - unlike most other benzodiazepines - is converted during its degradation to substances that do not lose their efficacy through this conversion, it has a relatively long half life of about 40 hours. This makes it one of the long-acting benzodiazepines. Short-acting, for example, triazolam or midazolam, among the medium-acting effective include, inter alia, oxazepam and lorazepam (trade name: Tavor ® ).

    dependence

    Benzodiazepines have a strong dependency potential. Therefore, they should usually not be given for more than a 3-6 week period.
    Withdrawal symptoms of dependency can be manifest among other things in the form of anxiety, hypersensitivity and hallucinations.

    Can I buy Valium® over the counter?

    Valium ® is one of the psychotropic drugs. It contains the active substance diazepam. This is a drug from the group of benzodiazepines. Valium ® can not be purchased without a prescription. This is mainly due to the fact that the active substance has a strong effect and can have dangerous consequences for patients who have not been instructed in the application. For example, active participation in road traffic should no longer occur once the drug has been taken. If taken in higher doses, you may experience extreme drowsiness and respiratory disorders.

    A combination with absorbing substances such as alcohol or sleeping pills is prohibited because of the danger of life-threatening interactions. With prolonged intake, there is a development of dependence.

    Valium® and Alcohol Is this acceptable?

    No - As the benzodiazepine group has a strong depressant effect on GABA receptors in the brain, the combination with alcohol is contraindicated. This is because alcohol and benzodiazepines act on the same receptor type in the brain, a subtype of the GABA receptor. The binding of alcohol degradation products or active ingredients such as diazepam to these receptors leads to an increased influx of ions into the relevant nerve cell. This causes the cell to become less active, it comes to a damping of the central nervous system. Since alcohol and diazepam have a very similar effect, when administered at the same time, there is a marked increase in the effect of both substances.

    It can lead to respiratory disorders to respiratory arrest and comatose states. An overdose of benzodiazepines and alcohol can be fatal. The amount of an overdose varies greatly from person to person. The combination of benzodiazepines and sleeping pills or other substances that attenuate are also contraindicated.

    withdrawal

    Benzodiazepines are a very effective drug, especially for the treatment of acute anxiety or agitation. Disadvantage of this drug group, however, is their high dependence potential.

    The dependence can develop after a short time and also at a normal dose. Many patients therefore suffer from benzodiazepine dependence, often even without being aware of it. Dependence is psychic and physical. It comes with the withdrawal so to physical and mental withdrawal symptoms.

    Due to the high risk of dependence development, the intake of Valium ® and co should usually be limited to a few weeks. However, this is often not the case in practice. If there has been a development of dependency, it must be discussed with the person concerned, how it can go on. As a rule, if the underlying disease allows it, withdrawal should be the goal. The principle here is not to discontinue the drug completely from one day to the next, but to slowly creep out, thus reducing the dose more and more. Depending on the dose, you can reduce it relatively quickly at the beginning. For example, the dose is reduced at weekly intervals.

    However, especially at the end of the affected people show some pronounced withdrawal symptoms, so that the reduction should be very slow here.

    The goal is the permanent and complete discontinuation of the drug. Symptoms of withdrawal include anxiety, restlessness, mood swings, nightmares, sleep disturbances, sweating, loss of appetite, nausea, visual disturbances such as ocular fibrillation or blurred vision, changes in the sense of smell and taste, hypersensitivity to light and noise, tinnitus, tremor (trembling of the hands ), Palpitations and blood pressure increase . The severe withdrawal symptoms include hallucinations, the fear or persuasion to be followed, seizures and a delirium.

    side effects

    Common side effects of Valium ® include severe daytime tiredness, prolonged reaction time (dangerous on the road !), Dizziness, gait disturbances, muscle weakness, difficulty concentrating, headache, confusion, and the occurrence of temporary memory lapses.

    Especially in the elderly, taking Valium ® can lead to a so-called paradoxical reaction. The patients are not calmed by the drug, but are very restless, agitated and anxious.

    mechanism of action

    Valium ® ( diazepam ) works on a receptor in the brain. This receptor sits on nerve cells and regulates the influx of chloride ions into the cell through its coupling to a channel.
    Such channels are needed because the cell is otherwise quite impermeable to ions of any kind. Only by the presence of pumps, channels and receptors ( which are often coupled to channels ) can ions thus pass from the cell interior to the outside or from outside into the cell interior. If this were not the case and the ions could follow their gradient ( ie from the place of the higher to the lower concentration of their own ), the cell would shrink or burst through the subsequent osmotic (balancing) water flow and thus become inoperative.
    The receptor to which Valium ® (diazepam) binds is called the GABA receptor. GABA ( gamma-aminobutyric acid ) is a neurotransmitter. He is the ligand for this receptor. That is, when GABA binds, the receptor undergoes a conformational change, and the channel that belongs to the receptor complex becomes permeable to chloride ions for a few milliseconds. Since the chloride concentration outside the cell is much higher than inside, so in this short phase of the open channel chloride ions flow into the cell interior. Chloride ions are simply negatively charged. So the cell gets a more negative potential through its influx.
    If you delve a little deeper into cell physiology, a regularity is that a cell becomes more active whenever its potential becomes more positive. The normal resting potential of a cell is in the range between -60 and -80 mV ( millivolts ). When the negative or positive ion influx outflows, the potential of the cell approaches 0 ( depolarization ). Once it has reached a certain threshold, an action potential is created and the cell is energized, ie active. The other way around, however, is the influx of negative charge, as in the case of the GABA receptor. Chloride ions flow in, so the potential of the cell becomes even more negative. The cell is hyperpolarized. This makes them even less excitable, so it would take a lot more "effort" to put them into an active state.
    What is the effect of Valium ® ? It binds to the GABA receptor and alters its conformation so that it becomes even more receptive to the binding of its ligand GABA. So it comes faster and easier to a hyperpolarizing chloride influx and the cell becomes more excitable.


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