Asenapine Pharmacology

Asenapine is an atypical antipsychotic that acts as an antagonist at multiple receptors, including dopamine D2 and serotonin 5-HT2A, contributing to its antipsychotic and mood-stabilizing effects.

Adverse effects of asenapine include somnolence, dizziness, and extrapyramidal symptoms.

Because asenapine is significantly metabolized by CYP1A2, inhibitors or inducers of these enzymes can affect its plasma concentrations.

Co-administration with other CNS depressants may increase the risk of sedation and impaired cognitive or motor function.

Asenapine can prolong the QT interval, so caution is advised when used with other medications that affect cardiac conduction.

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Loxapine Pharmacology

Loxapine is a first-generation (typical) antipsychotic with dopamine D2 receptor antagonism as its primary mechanism, though it also has affinity for serotonin 5-HT2A receptors, making its pharmacology somewhat atypical.

Loxapine is available in multiple formulations, including oral capsules and an inhalation powder, the latter approved specifically for acute agitation in patients with schizophrenia or bipolar I disorder.

Sedation and extrapyramidal symptoms (EPS), including dystonia, akathisia, and parkinsonism, are common adverse effects due to its potent dopamine blockade in the nigrostriatal pathway.

Orthostatic hypotension can occur with loxapine due to its alpha-1 adrenergic blockade, requiring monitoring in elderly patients or those on antihypertensives.

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Fluphenazine Pharmacology

Fluphenazine is a high-potency typical antipsychotic that primarily acts as a dopamine D2 receptor antagonist in the mesolimbic pathway, reducing positive symptoms of schizophrenia.

Extrapyramidal symptoms (EPS), such as dystonia, akathisia, and parkinsonism, are common due to potent D2 blockade in the nigrostriatal pathway.

Neuroleptic malignant syndrome (NMS), though rare, is a life-threatening adverse effect characterized by rigidity, hyperthermia, altered mental status, and autonomic instability.

CYP2D6 inhibitors (e.g., fluoxetine, paroxetine) can increase fluphenazine plasma concentrations, potentially raising the risk of toxicity and side effects.

Concomitant use of fluphenazine with CNS depressants (e.g., alcohol, benzodiazepines) can enhance sedation and respiratory depression.

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Top 200 Drugs – Medications 166-170

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On this episode of the Top 200 Drugs podcast from Real Life Pharmacology, we cover Percocet, Epogen, quetiapine, glimepiride, and tirzepatide. These are drugs 166-170.

Percocet is a combination analgesic. It contains acetaminophen and oxycodone. Pay attention to acetaminophen intake from all sources when patients are on this medication.

Epogen (epoetin alfa) stimulates the production of red blood cells. This medication can be useful in treating anemia.

Quetiapine (Seroquel) is an antipsychotic. It is often used in patients with hallucinations and delusions associated with Parkinson’s disease because it has a lower potential to block dopamine receptors compared to other antipsychotics.

Glimepiride is a sulfonylurea. This medication stimulates the release of insulin which can help lower blood sugars in diabetes.

Tirzepatide (Mounjaro) is a combination GIP and GLP-1 receptor agonist that can be used for weight loss and the treatment of diabetes.

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Risperidone Pharmacology Podcast

On this episode, I discuss risperidone pharmacology, adverse effects, monitoring, and common indications.

There are numerous drug interactions that I discuss in this podcast episode. CYP2D6 inhibitors may increase drug concentrations.

Risperidone increases prolactin more than most 2nd generation antipsychotics. This can lead to sexual adverse effects.

QTC prolongation is a concern with all antipsychotics like risperidone. We can monitor EKG to monitor for this risk.

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