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