Diazepam Pharmacology

Diazepam has numerous dosage forms. There are rectal, injectable, and oral formulations of the drug that are commonly used in clinical practice.

Diazepam has 2 major metabolic pathways. It is broken down primarily by CYP3A4 and CYP2C19, leaving open the potential for numerous drug interactions. I discuss this further in the podcast.

Diazepam is on the Beers list because it has a tendency to accumulate in the geriatric patient population and cause adverse effects like sedation, confusion, and falls.

Respiratory depression, coma, and death are significantly more likely in overdose situations where opioids are used in combination with benzodiazepines like diazepam.

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Fluoxetine Pharmacology

Fluoxetine is an SSRI used in the management of depression, anxiety, OCD, PTSD, and other psychiatric conditions.

Fluoxetine has a very long half-life which can impact clinical management. I discuss how this matters in this podcast episode.

Fluoxetine inhibits CYP2D6 which can alter the concentrations of many drugs.

Prodrugs like codeine and tamoxifen can have their effects reduced because of fluoxetine. I explain this further in the episode.

By inhibiting CYP2D6 concentrations of many drugs can be raised by the use of fluoxetine.

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Buspirone Pharmacology

Buspirone is an anti-anxiety medication that has the potential of having some serotonin agonist activity.

Buspirone has a very high first-pass metabolism. This means that the body breaks much of the medication down prior to it getting into the systemic circulation.

Buspirone is broken down by CYP3A4, so concomitant use with inhibitors or inducers can alter its concentrations

Buspirone should not be used as needed as this medication takes a while to start to show benefit.

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Benzodiazepine Pharmacology

Benzodiazepines act by enhancing the effect of GABA, an inhibitory neurotransmitter.

Benzodiazepines can cause confusion, sedation, and respiratory depression.

There are many potential indications for benzodiazepines. They can be used in anxiety, status epilepticus, insomnia, and alcohol withdrawal amongst other things.

There is a boxed warning for the use of opioids with benzodiazepines. The primary risk of the combination is respiratory depression.