(From Lippincott’s, by Brian Buschman)
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Benzadiazopenes are the most used sedative/hypnotic because they are safer than others. Benzadiazopenes bind to a receptor that is attached to the GABA receptors which when bound increases the affinity that the receptor has for GABA. Therefore benzadiazopenes increase Cl- conductance and cause hyperpolarization.
Benzadiazopenes are distributed all over the body (lipophillic) and are mostly metabolized by the liver. They can cause withdrawal effects and can potentate the effects of EtOH.
Hypnotic agents include:
1) Flurazepam which is a long-acting benzadiazopene causing little rebound insomnia. The longer the half-life the less the rebound insomnia (in general).
2) Temazepam has a slow onset but a medium half-life.
3) Triazolam is a short acting benzadiazopene. It is used to help people get to sleep but is short enough it does little to keep them asleep.
Sedative agents include:
1) Diazepam which is used for anxiety disorders that require long term treatment, muscle spasm, EtOH addition and it is the DOC for gran mal seizures.
2) Alprazolam is the DOC for panic disorder.
3) Clonazepam is used for epilepsy other than gran mal (use diazepam).
4) EtOH addiction can be partially treated with chlordiazepoxide, dorazepine, diazepam or oxazepam.
Flumazenil is a short acting GABA antagonist used with OD of benzadiazopenes.
Barbs mess up the Na+/K+ transport in membranes which leads to interference of the mesencephalic activating system. At low doses they produce sedation and at higher doses hypnosis and anesthesia. OD causes depression of any CNS function. They also induce P-450 systems.
Thiopental has a very short action and s useful in induction of anesthesia.
Phenobarbital is used long-term in tonic-clonic seizures, status epilepticus and eclampsia.
Sedative hypnotics include pentobarbital, secobarbital and amobarbital but have been replaced by the safer benzadiazopenes flurazepam, temazepam and triazolam.
Barbs are very addictive and cause withdrawal symptoms. With OD life support may be necessary and alkalization (increased pH) of the urine helps increase elimination.
Zolpidem is a hypnotic that has no tolerance or withdrawal and only slight rebound insomnia. It is selective for hypnosis.
Buspirone is the DOC for GAD. Buspirone has a slow onset of action but works well on anxiety without much of the other benzo effects.
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