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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Zolpidem Pharmacology

Zolpidem enhances the action of GABA which is an inhibitor neurotransmitter.

Zolpidem metabolism can be impacted by the use of CYP3A4 inhibitors. Concentrations can rise on account of this potential interaction.

It is important to remember to go slowly when tapering off zolpidem. Particularly in patients who have been on the drug for a long time or those who are on higher doses.

Abnormal sleeping behaviors like sleep-walking, eating, or driving have been reported with zolpidem.

Remember that CNS depressant drug interactions can happen with zolpidem. Take note of any other sedating medications prior to starting zolpidem.

I discuss important drug interactions on the podcast, be sure to check out my latest project which is a 200+ page book on managing drug interactions in primary care.

Be sure to check out our free Top 200 study guide – a 31 page PDF that is yours for FREE!

Doxepin Pharmacology

Doxepin is under the class of tricyclic antidepressants. It can inhibit the reuptake of serotonin and norepinephrine.

In addition to the serotonin and norepinephrine reuptake inhibition mechanism, doxepin also has antihistamine type effects.

Because of the anticholinergic activity of doxepin, it is recommended to avoid this medication in the elderly, particularly at high doses.

Be aware that anticholinergics like doxepin can reduce the benefit of dementia medications.

CYP2D6 is an important enzyme in the metabolism of doxepin and drugs like bupropion that inhibit CYP2D6 can increase the concentrations of doxepin.

I discuss important drug interactions on the podcast, be sure to check out my latest project which is a 200+ page book on managing drug interactions in primary care.

Be sure to check out our free Top 200 study guide – a 31 page PDF that is yours for FREE!

Atomoxetine Pharmacology

Atomoxetine is a norepinephrine reuptake inhibitor that can be used in the management of ADHD.

Atomoxetine is a non-controlled substance option for patients seeking this alternative to traditional stimulants.

CYP2D6 is an important enzyme in the breakdown of atomoxetine.

CYP2D6 inhibition or poor metabolizers via CYP2D6 can lead to higher concentrations of atomoxetine and put our patients at greater risk for adverse effects.

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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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Methylphenidate Pharmacology

Methylphenidate has an FDA approved indication for ADHD. In this podcast episode, I cover the pharmacology, adverse effects, kinetics, and drug interaction.

Because methylphenidate has stimulant type effects, it can raise blood pressure and heart rate.

Weight, blood pressure, and pulse are important monitoring parameters in patients taking a stimulant type medication like methylphenidate.

There are numerous dosage forms of methylphenidate which can help accommodate many different patients’ needs.

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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.

Clozapine Pharmacology

Clozapine Pharmacology

On this episode, I discuss clozapine pharmacology. This drug has multiple mechanisms of action: Dopamine blockade, anticholinergic activity, and alpha blocking activity all contribute to the complexity of this drug.

Smoking cessation can significantly increase the concentrations of clozapine. This is because smoking can induce CYP1A2. Listen to the podcast for more details on how this can impact our patients clinically.

Clozapine has 5 boxed warnings. I discuss them all in this podcast. The most well-known boxed warning is for agranulocytosis.

Because clozapine has alpha blocking activity, it can cause orthostasis. We need to monitor for this.

Clozapine can cause QTc prolongation. Keep an eye out for other medications that the patient may be taking that can also cause this. Examples include: amiodarone, ondansetron, quinolones, and macrolides

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Trazodone Pharmacology

Trazodone pharmacology is complex. It can inhibit serotonin reuptake, block histamine receptors, and possibly have alpha-blocking activity.

Side effects of trazodone include sedation, dizziness, and dry mouth. Rarely, priapism may occur. I’ve seen this nugget come up on pharmacology exams!

While trazodone is classified as antidepressant, it is often used to help manage insomnia.

Trazodone can possibly prolong the QT interval. Risk of other medications and patient specific parameters should be considered.

Trazodone concentrations can be increased with the use of CYP3A4 inhibitors and reduced with 3A4 inducers.

Be sure to check out our free Top 200 study guide – a 31 page PDF that is yours for FREE!