자넥스 주요성분 - 벤조디아제핀 정리 (영어)

BZD [Benzodiazepine] - Downer

며칠 전에 병원 실습에서 교수님이 벤조에 대한 질문을 했는데, 벤조가 가장 많이 쓰이는 부분만 쏙 빼놓고 이야기함. 벤조는 불안 증세를 보이는 환자에게 가장 많이 쓰이는 약이다. 미국에서 살면 자넥스(Xanax)라는 이름의 약을 많이 들어봤을 것이다. 이 자넥스의 주요성분이 바로 벤조디아제핀이다. 어떻게 이게 기억이 안났지? 띠로리..ㅠㅠ

 

벤조디아제핀은 Downer라고도 불리는데, 이유는 중추신경계를 억누르는 역할을 하기 때문이다. 뇌에서 글루타메이트(Glutamate)가 많이 나오면 우리가 불안함을 느끼게 되는데, 이것이 분비되는 것을 억제시켜주기 때문이란다.

 

 

불안증세를 보이는 환자에게 많이 쓰이는 XANAX

 

하지만 나는 이 용도 말고 나머지 마이너한 세 개 경우; 발작(seizure), 불면증(insomnia), 마취(anesthesia)에 대해서만 말함.ㅠ 나중에 다시 물어보면 안까먹어야지. 벤조에 대하여 공부한 것을 정리해둔다.

MOA

GABAa enhancer - Ast as a central nervous system depressant

  • Brain cells = Neurons. Sends and receive a signal through neurotransmitter like Glutamate and GABA.

  • Neuron --> gets stimulated --> release nuerotransmitter such as Glutamate/GABA --> binds to other Neuron --> Depolarizes --> release another neurotransmitter from that Neuron

    • Excitatory neuron = Glutamate

    • Inhibitory neuron = GABA - GABA receptor (Ligan-gated ion channel) releases Cl- ion. when the cell becomes more Negative - Inactivates neuron

  • Psychiatric disorders = Too much excitatory NT release at once [Anxtiey, Panic attack] 

  • Neurological disorders = Too much inhibitory NT release at once [seizures, epilepsy] 

  • BZD decreases excitatory signals --> enhancing the effect of inhibitory neuron

  • BZD bind to GABAa receptor and increases intracellular Cl- level. 

    • Barbiturates also bind to GABAa receptor. It tends to open channels longer and unlike BZDs they can open this channel in absence of GABA

Indication

anxiolytic, anticonvulsant, hypnotic, anesthetic, and treat withdrawal syndromes

Drugs

Long-acting BZDs

Short-acting BZD

Diazepam (Valium)

Midazolam (Versed)

Chlordiazepoxide (Librium)

Alprazolam (Xanax)

 

Lorazepam (Ativan) 

 

Oxazepam (Alepam)

 

Temazepam (Restoril)

Use of BZD

  • Anxiety disorder - panic attack

  • Status Epilepticus - 5 mins of seizure, multiple seizures without returning to normal in-between 

  • Anesthesia - depress the function of the nervous system

  • Insomnia - depress the function of the nervous system [it decreases REM sleep]

  • Withdrawal symptoms - decrease severity on alcohol withdrawal symptoms

  • Muscle spasm - cerebral palsy (뇌성마비)

Side effects

  • Drowsiness, decreased concentration, decreased problem-solving abilities and decreased reaction time

  • Causes "Paradoxical stimulation in the brain" - fast speech, excitement, restlessness

    • in this case, we can use competitive antagonist for BZDs called Flumazenil

Contraindication

  • Anything that makes the nervous system depressed such as alcohol, barbiturates, and anti-histamines

Clinical pearls

  • Should not take BZDs before driving, avoid activities that require mental alertness

  • With chronic use, will develop tolerance. It would decreases BZDs effect. Can lead to addiction due to habit-forming and dependence

Z-drugs are not benzodiazepine but similar. It acts on a subunit of the benzodiazepine receptor family BZ1. Zolpidem has no anticonvulsant or muscle-relaxant properties but has only a hypnotic effect. 

Z-Drugs 

Zolpidem (Ambien)

Zopilcon (Imovane)

Zaleplon (Sonata)


참고자료

사진: https://www.theguardian.com/society/2018/feb/09/reduces-people-zombies-uk-readers-xanax-misuse

약학지식: http://www.osmosis.org/

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