Tag Archives: Sedative

Effects of Benzodiazepine

Sedative and Euphoric Effects of Benzodiazepine

BenzodiazepineBenzodiazepines are drugs that have been used in hospitals to curb pain, as anti-anxiety and for sedation. However these drugs are can be abused as they are rewarding in higher doses. For this reason many people have used these drugs for all the wrong reasons. What happens when you take these drugs depends on the dosage. When used as prescribed the work as anti-anxiety and for sedation but when abused they result in even more grave side effects.

Benzodiazepines are glycoproteins with an affinity for benzodiazepine receptors which act as specific binding sites for gamma aminobutyric acid shortly known as GABA. The GABA is the major inhibitory neurotransmitter in the CNS. Many scientists have proposed various action mechanisms but despite all these proposed action mechanisms, the exact sites and mechanisms of actions of these drugs is still a mystery unraveled.

The mechanism of action of these drugs is often based on this belief that these drugs affect CNS by interacting with a macromolecular protein complex in the neuronal membrane which includes GABAa receptors, high-affinity benzodiazepine receptors and chloride channels. The scientists are still working to find more about the mechanisms of action of benzodiazepines in the CNS but until now we can dwell more on their effects in the body and how to safely use them.

Occupation of the benzodiazepine receptor increases the affinity of the GABAa receptor for GABA. GABA potentiates the direct opening of the chloride ion channel, allowing an increased influx of chloride into the neuron. The inward shift of chloride ions hyperpolarizes and stabilizes the membrane, resulting in a net inhibitory effect on neuronal firing. Benzodiazepines alone have little effect on chloride ion channel permeability and depend upon the presence of GABA in the synapse for their actions.

Some of benzodiazepines are very similar in their chemical structures but their potency differs greatly and so is the rate of absorption and other pharmacological parameters. The potency of a benzodiazepine is correlated with its affinity for its binding site, the benzodiazepine receptor. In therapeutic use, the benzodiazepines, while differing in potency, have similar pharmacologic profiles.

It is believed that there are different types of benzodiazepine receptors in different areas of the CNS which produce the various pharmacological actions of the drugs. As the dose of benzodiazepine is increased, anxiolytic effects are first produced, followed by anticonvulsant effects, a reduction in muscle tonus, and finally sedation and hypnosis.

Clinically, benzodiazepines are used in the management of anxiety disorders, insomnia, seizure disorders, skeletal muscle spasticity, alcohol withdrawal, panic disorder and as premedicants prior to surgical or diagnostic procedures. Benzodiazepines have also been used in the management of nausea and vomiting associated with emetogenic cancer chemotherapy.

When taken benzodiazepines get widely spread in the body and accumulate preferentially in lipid rich areas such as the CNS and adipose tissue. The more lipophilic agents have the fastest rates of absorption and onset of clinical effects. Benzodiazepines and their metabolites are highly bound to plasma proteins. Steady state plasma concentrations of benzodiazepines and their metabolites are reached after about 5 elimination half-lives, typically, a few days to 2 weeks after initiation of therapy. The higher the concentrations of benzodiazepines   in the plasma the higher their sedative and euphoric effects. For sedative purposes the concentrations of benzodiazepine in the plasma are much lower than the concentrations of benzodiazepine in plasma that would evoke euphoric effects. This shows that that a person may have euphoric feelings after using higher doses of benzodiazepine than the doses needed for sedative purposes. However, the higher the doses of benzodiazepines the danger it beckons for higher doses may result in intoxication or even delirium which is characterized by ataxia, amnesia, stupor, impaired consciousness, nystagmus.

Mortality hazards of the use of Benzodiazepine

The benzodiazepines are clinically useful but that does not mean that they are free from any side effects. The use of benzodiazepines within the prescribed doses foe sedation and sleeping disorders may give relief and a reason to celebrate but as I have written earlier, these drugs are prone to abuse and as commonly abuse of any drug will always give rise to undesired effects. Though it has not been perceived to be as dangerous as other drugs of abuse such as opioids and ‘bath salts’ that can cause death instantly due to overdose, the side effects of benzodiazepine can lead to death in one way or another. These side effects include; dependency, withdrawal, rebound symptoms, daytime sedation, confusion, cognitive deficits, ataxia, dysarthria, diplopia, and vertigo. The use of benzodiazepines have been linked to motor vehicle accidents especially in the elderly. Benzodiazepines are often used in patients undergoing dialysis for their sedation effects. However a study done in japan where these drugs were used widely in dialysis patients showed that benzodiazepine use may be associated with an increased mortality risk.

Benzodiazepine increased rise of falls in Elderly

BenzodiazepineBenzodiazepine has also been found to increase falls in the elderly leading major fractures. The long term use of these drugs is also associated with nocturnal falls and still the elderly still fall victims. Rise in falls is one of the problems that can be linked to the effects of the drug on the elderly.

Finally, you need more information to stay away from dependence on alcohol and drugs as these have crippled societies and that is why here at AWAREmed we are dedicated to finding the best solutions to addiction and dependence on substances. Dr. Dalal Akoury (MD) is always in the mood of helping any patient to be addiction free. Do not hesitate to call on her for help in managing any sort of chronic pain or any type of addiction as well as other diseases.

Sedative and Euphoric Effects of Benzodiazepine

Facebooktwitterpinterestlinkedin

Sedatives and Chronic Pain Treatment

Sedatives and Chronic Pain Treatment

What are sedatives?

SedativesSedatives refers to the drugs which when administered to a patient, they reduce tension and anxiety and cause sedation. They are drugs which cause calmness when taken by the patient. In chronic pain treatment, these drugs are administered with a purpose to kill the pain that the patient is experiencing. This is not a common medication though and it will only be made available to the public if the clinical trials have shown that the benefits of using the drug seemingly outweigh its adverse risks.

How are sedatives administered?

Sedatives are administered to patients in many ways. The mode in which the sedation is given will though be determined by the area on which the pain is being experienced. The modes through which sedation can be administered include:-

ü  Through inhalation- through nose

ü  Through mouth (oral)

ü  Under the tongue

ü  Or sometimes administered intravenously i.e. through the veins.

Is sedation helpful in pain relief?

Yes. Sedation is a medication that has been specifically developed to help people who are experiencing pain. This medication works by calming the nervous system and hence making the patient not to feel any pain. Sometime when you are experiencing chronic pain, it may be difficult for you to concentrate on anything or even have sleep. Sedation in this case can prove helpful to you.

Does sedation cure chronic pain?

There has been confusion in many people who use sedation and think they are treating pain. Sedation is not a curative medication for pain, but it is only meant to help the patient by providing temporary relief from pain.

Under what circumstances will sedation be important?

As earlier mentioned, these medicines should only be used when prescribed by a doctor, because they are known to be habit forming. This will make them less effective the next time you will need to use them.

This medication is normally in most cases prescribed to the patients who are experiencing difficulties in sleep. This is because it is very difficult for a person experiencing severe pain to get any sleep. In this case, the doctor will prescribe sedative medication which will help the patient in killing the pain and consequently the patient gets sleep.

Are there thing I should avoid when under sedation treatment?

Yes. Sedation if not well taken care of can be hazardous. Depending with the level of sedation, (e.g. Deep sedation) taking of other drugs like alcohol as this may cause extreme drowsiness and this can reduce breathing and if intense, death may occur.

When you will also want to stop taking sedation medication E.g. for sleep aid, do not stop abruptly. Instead discuss it with your doctor to be advised on how to gradually withdraw. The abrupt stoppage may subject you to withdrawal symptoms.

Which are the types of sedation?

The type of sedation medication to be administered to the patient will be determined by the doctor when the patient visits the doctor. This choice will though be based of the intended effect of the sedative in terms of intensity. The following are the common types of sedative medication:-

  • Minimal sedation – when this sedation is administered, the patients respond normally to verbal communications since this is a light sedative medication. Sometimes this method may though impair cognitive function and coordination, breathing in unaffected.
  • Moderate sedation – this is also referred to as cognitive sedation and the patient remains conscious and an respond purposefully to verbal commands either alone or by light simulation.
  • Deep sedation – if this type of sedation is administered to a patient, the patient cannot be easily aroused but responds to painful simulation. The patient may require assistance to breath.
  • General Anesthesia this is normally a very serious sedation treatment and its intensity is high. The patient cannot be aroused even by inducing pain on him/her. Breathing ability may completely be impaired.

Does sedation have any side effects?

SedativesAlmost all drugs, prescribed or over the counter will have some side effects. In this case, sedation is no exception. Some of the powerful sedation medicines have very high chances of causing addiction to the patient, especially if they are abused. Apart from the risk of addition, these drugs may also sometimes produce unpleasant reaction to the patient. It is important to note that the reaction that results from different patients when they take a given drug is quite different and hence it is vital after you see a negative reaction to the drug you see your doctor as soon as possible.

Is sedation same as opioids treatment?

Not really. As mentioned earlier, sedation refers to the medication which is normally given to the pain experiencing patient in order to bring about calmness. On the other hand, opioids are curative mediations which are given to pain experiencing patient with aim of not just giving them a temporal relief from the pain but to get them a permanent solution to the pain. Therefore, in simple terms the difference between the two is that opioids are medications that cure pain while sedatives are medications meant to calm or cool down the pain. Both medications should be administered by a qualified physician though, to avoid risks of addiction.

Sedatives and Chronic Pain Treatment

Facebooktwitterpinterestlinkedin