What factors may affect the absorption and distribution of sedative-hypnotic drugs? What is the clinical significance thereof?

Lipophilic is the factor that plays the most important role in absorption and the time extent the drug will have an effect on the CNS. Drugs that has a low lipophilicy has a slow onset of effect because of the inability to cross the blood brain barrier. The more lipophilic the more effective the drug will be.

What is meant by redistribution and what is the significance thereof?

Redistribution happens when a drug is taken up into the circulation and transported to other tissue/parts of the body.

How are the BDs metabolized? Name the various steps in the process.

BD’s are metabolized by hepatic microsomal enzymes using 3 steps. (1) Dealkylation (2) Oxidation

(3) Conjugation

Which BDs are converted to active metabolites? What is the significance thereof?

Diazepam, Clorazepate, Prazepam, chloordiasepoksied and ketasolam. The ability to form active metabolites increases the effective time of medication.

Which BDs are not dependent on the cytochrome P450 oxidative enzymes for metabolism? What are the advantages thereof?

Oxazepam, Lorazepam, Temazepam, Lormetazepam. This medication is used when the patient’s cyto P450 activity is insufficient.

What is enzyme induction? Which of the sedative hypnotic drugs are known for this?. What is the clinical significance of enzyme induction?

Enzyme induction is when the enzymes is induced which will cause and increased metabolism of the drug. The drug concentration in the systemic circulation is less and will have a decrease in the therapeutic effect of the drug.