LUNE HUGGETT

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Lune' Huggett 31913377 Blog #3

2 Mar 2021, 18:12 Publicly Viewable

1. Absorption and distribution of drugs are affected the most by lipid solubility. Lipid solubility helps sedative-hypnotic drugs to be absorbed into the central nervous system. This factor is responsible for how fast the sedative-hypnotic drugs start working. The clinical significance of this is that the more lipophilic a drug is, the faster and better it is absorbed into the patients system. 

2. Redistribution of drugs is when a lipid soluble drug is distributed to the organs of the body and is then distributed again into the fat and tissue. Redistribution is done to lengthen the action of the drug. 

3. The metabolism of BDs happen via biotransformation by hepatic enzymes and in 3 steps: 

  • Dealkylation 
  • Oxidation 
  • Conjugation

4. The benzodiazepines that are converted to active metabolites are:

  • Diazepam
  • Prazepam 
  • Chlorazepate 

By converting BDs to active metabolites, you lengthen the duration of action of the drug. 

5. The BDs that are not dependent on the cytochrome P450 oxidative enzymes are: 

  • Oxazepam 
  • Lorazepam 
  • Temazepam 

These drugs are not metabolised by the CYP450 enzymes. It is therefore the preferred drug for patients with decreased CYP450 enzyme activity.

6. Enzyme induction is when a drug causes an increase in the production of specific enzymes that betters the metabolism of that drug. A drug that causes this include: phenobarbital. Enzyme induction decreases the amount of drugs in the patient's circulation which causes the therapeutic effect to be decreased.