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Benzodiazepine drugs

The benzodiazepine Listen ( BZD ) are a class of organic compounds containing a cycle benzene fused to a diazepine . Also classified as benzodiazepine thienodiazepines , which unlike having a benzene cycle have a thiophene cycle .

They are a class of drugs psychotropic , colloquially called anxiolytics, used in the medical treatment of anxiety , the insomnia , the psychomotor agitation , the convulsions , the spasms , or in the context of alcohol withdrawal syndrome . They are mainly used as anxiolytics , less for their hypnotic properties , where nearby molecules called nonbenzodiazepinesthey are preferred for their short action and less conducive to residual morning effects. They also have three other effects: antiepileptics , amnesia and muscle relaxants .

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Chemistry

The fully systematic (IUPAC) name for the nucleus of the benzodiazepine group (CAS 12794-10-4) is 2,3-diazabicyclo[5.4.0]undeca-3,5,7,9,11pentaene. The different drugs have varying substituents on this basic skeleton.

Pharmacology:

1- Pharmacodynamics

The GABA is the major neurotransmitter inhibitor central nervous system . Its fixation on its receptors induces an influx of chloride ions which hyperpolarizes the neuron membrane . Benzodiazepines bind to a site related to that of GABA, and have the effect of enhancing the effects following their activation by it or another agonist (such as alcohol ). Specifically, these products have an amplifying action on the GABA-A -alpha-1, 2, 3 and 5 9 receptor subtypes . They do not demonstrate selectivity for certain subtypes rather than others 10. Only certain related products have a more selective action, such as zolpidem (alpha-1 receptors) 11 and etifoxine (alpha-2 and 3 receptors) 12 , thus giving them a specifically hypnotic or anxiolytic profile, respectively.

We speak of a positive allosteric modulator effect . For the same amount of GABA, the frequency of opening of the ion channel will be greater, which will allow the passage of more negatively charged chloride ions and ipso facto a stronger inhibition. Unlike barbital , benzodiazepines are not GABA agonists and do not activate this channel of inhibition directly. They only reinforce its natural activity, which limits the risks of overdose 13 .

2 – Pharmacokinetics

Benzodiazepines share many pharmacokinetic characteristics.

Most of them have a distribution and a rapid absorption (<90 min) ( diazepam , alprazolam , etc.) 14 , while others, for different reasons, have a delay of action, and a half – longer elimination life.

Some benzodiazepines are excreted unchanged in the urine, and others undergo biotransformation and catabolization by enzymes in the P450 subgroup such as CYP 3A4 15 .

Benzodiazepines are generally distinguished according to their elimination half-life. They thus have different indications; anxiolytics with a short half-life are generally intended to treat insomnia while preserving sleep by limiting the residual effect 16 , grand epilepticus, or transient anxiety states, while molecules with a longer half-life are mainly intended to treat anxiety on a daily basis (for a limited time), to treat withdrawal (alcohol, benzodiazepines, opiates). These benzodiazepines generally have active metabolites which also have a long half-life.

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BENZODIAZEPINES IN CLINICAL PRACTICE ( Lifetime ):

General

BZDs are classified in terms of their elimination half-life. Short-acting BZDs have a median elimination half-life of 1-12 hours, intermediate-acting BZDs have an average elimination half-life of 12-40 hours, and long-acting BZDs have an average elimination half-life of 40-250 hours. As noted earlier, 5 half-lives are generally necessary for an agent to be eliminated from the body, making the number of hours that a drug is in the body considerably longer. The table lists various BZDs and their characteristics.

General risks

All the general risks linked to the use of benzodiazepine are well known and appear in the

Summary of Product Characteristics (MA) for each of them [8]. Thus, the use of benzodiazepines

can lead to:

– anterograde amnesia (loss of memory of recent events), which can occur at therapeutic doses. The risk increases in proportion to the dose;

– an impairment of psychomotor functions which may occur within hours of taking it;

– a syndrome associating, to varying degrees, behavioral and memory disorders and a

altered state of consciousness. The following effects may be observed: worsening of

insomnia, nightmares, restlessness, nervousness, delusions, hallucinations, confusional dream state,

psychotic symptoms, disinhibition with impulsivity, euphoria, irritability, anterograde amnesia and suggestibility.

This syndrome can be accompanied by disorders potentially dangerous for others and for themselves

such as unusual behavior for the patient, violent behavior, especially if those around him

attempts to hinder the patient’s activity.

These demonstrations require the cessation of treatment [8]. If it is impossible to stop treatment completely,

a decrease in dosage may, in some cases, cause the disorder to regress.

– tolerance characterized by a progressive decrease in the therapeutic effect for the same

dose administered for several weeks. Tolerance can lead to increased

doses to achieve the desired effect;

–  an addiction. Any treatment with benzodiazepines and related drugs, especially

prolonged use, can lead to a state of physical and mental drug dependence.

Various factors seem to favor the onset of dependence: the duration of treatment, the dose and

history of other drug and non-drug dependencies, including alcoholism.

Drug dependence can occur at therapeutic doses and / or in patients without factor

of particular risk.

The combination of several benzodiazepines may, whatever the indication, increase the risk of

drug dependence .

abuse of benzodiazepine products :

Although some people may have a genetic tendency to become addicted to drugs, there is little doubt that environmental factors also play a significant role. Some of the more common environmental influences are low socioeconomic status, unemployment, and peer pressure.

Risks linked to association with other products:

Alcohol enhances the sedative effect of benzodiazepines and related drugs.

Combination with other central nervous system depressants increases central depression and

impaired alertness. The association with morphine derivatives (analgesics, cough suppressants and substitution treatment for drug dependence on opiates) also increases the risk of depression

respiratory, possibly fatal.

Benzodiazepine Abuse Treatment

– Benzodiazepine Abuse Treatment Self-Care at Home

Drug abusers often deny their problem by playing down the extent of their drug use or blaming job or family stress. The most important thing that can be done at home is to recognize that there may be a problem and to seek help.

– Awareness of the signs and symptoms of abuse help with recognition.

– The next step is to try to obtain help for the person. This can be done either through your doctor or by contacting many of the drug abuse help lines in your community.

– Medical Treatment

Acute toxicity: The treatment required usually depends on what drugs were taken and how much. Often, you need only a period of evaluation in a hospital emergency department:

– If the drugs were taken within the previous 1-2 hours, the doctor may consider gastric lavage. With this procedure, a large tube is placed directly into your stomach through the mouth or nose. Large volumes of water can then be pushed into the stomach in an attempt to wash out the pill fragments. This is not used often and only if you are known to have swallowed other potentially more lethal medications.

– A single dose of activated charcoal is recommended for people who come to the emergency department within 4 hours of taking drugs. This acts to prevent absorption of the medication. It is a black powder that is mixed with water and given to you to drink. Side effects can include nausea, vomiting, and abdominal cramps.

– There is an antidote to counteract the toxic effects of benzodiazepines called flumazenil (or Romazicon). This reverses the sedative effect of benzodiazepines. It is, however, usually reserved for severe poisoning, because it can cause withdrawal and seizures in people who are chronic benzodiazepine abusers, and also may require repeated administrations, with careful monitoring, due to its fairly short duration of action.

Chronic abuse:

The treatment of chronic abuse can usually be done at home with the help of your doctor or in specific drug rehabilitation centers. The first step consists of gradual reduction of benzodiazepines to prevent withdrawal and seizures. This is often much easier than the prolonged recovery phase in which the person attempts to stay drug-free. In addition to the medical care, someone abusing these drugs often requires social support and help in finding housing and employment. The involvement of family and friends can be very helpful in this difficult stage.

Somes answers of Dr. Sarah Coscas, psychiatrists-addictologist to users of benzodiazepines:

– Is Atarax a substitute product?

It is not a substitute but it is a very good anxiolytic which is not addictive.

– I have been on laroxyl, nozinan, temesta since 1980, 3 times a day. What risk for my husband?

There is a risk of dependence on temesta because it contains benzodiazepines. It should not be prescribed for more than three months.

– I am 64 years old, I have been on lysanxia 10 in the evening for 15 years. I have been in depression since May with an additional 1 stresam morning and evening and a seroplex5 in the evening. When I am better my doctor will stop lysanxia What to do for withdrawal? I’m afraid of lack.

Weaning is possible but you have to go at your own pace.

­- Can you stop a drug overnight? My doctor does not want me to stop Lexomil and Seroplex 10 without his advice or gradually?

Both drugs should be stopped gradually and on medical advice.

– Can valium give joint pain?

Yes, at the time of weaning.

– Are benzodiazepines carcinogenic?

No, no study has proven it.

– Can herbal medicines for anxiety help?

Some patients are sensitive to it in this case they are effective but not for everyone.

– For almost 1 year and a half, I have been taking one VERATRAN 10 MG tablet. Is it dangerous?

No, but the indication of this prescription must be reviewed.

– Which benzodiazepine has the longest lifespan?

It is lysanxia.

– What about the effects of benzodiazepines on libido?

There is no direct effect demonstrated.

– Why don’t we directly prescribe drugs with a longer half-life?

Because we can look for a mechanism of action with the short half-life.

– What is the difference between Lysanxia and Lexomyl? Do they belong to the same class and cause the same addictive addiction?

They belong to the family of benzodiazepines. Same risk of addiction.

– What is the best noctamide medication? Can it replace zolpidem 2 in the evening and a seresta 50?

This treatment can be compared to benzodiazepines, the risk of dependence persists.

– How can we enter the center to detoxify from taking anxiety and hypnotics in high doses for years. What criteria are required?

It is essential to evaluate the indication for hospitalization which will be scheduled in the event of dependence, if ambulatory withdrawal is impossible or if there have already been seizures.

– From what dosage is the deroxat active? Can osteopathy help with withdrawal?

Deroxat is an antidepressant, it is active from 20 mg. The stop must be discussed by a doctor and progressive.

– In which category do we place stresan? I have been assured that it is not addictive. Is it true?

It is an anxiolytic and not a benzodiazepine. It is not addictive but the way of taking the treatment can be addictive

– I have been taking seropram for 15 years and I continue at the rate of half a tablet per day for fear of plunging back into depression. Is it worse than if I took lexomil instead? Which has the most detrimental effect on memory. Besides, can these two products cause tremors?

No, they do not have the same effect, seropram can be taken long term in small doses to prevent depression. It can cause tremors like lexomil.

 – have been in menopause since October 2012. I take 3 lexomil and 1 seroplex per day. Will i gain weight?

No, it is a rare side effect. The weight gain will certainly be due to menopause.

What do you think of STABLON for anxiety?

It is little prescribed.

– How to stop an antidepressant?

It varies depending on the antidepressants. Stop after the symptoms of depression have disappeared for 6 months.

– I have been on valium 10 mg in the evening for neuropathy of charcot marie tooth, since 1993. Is it dangerous? Is there any other medication for muscle cramps and pain related to the disease other than benzodiazepines?

In neurological indications, the benefit prevails over the side effects.

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