Ketoconazole Pharmacology

Ketoconazole is an imidazole antifungal that works by inhibiting fungal cytochrome P450 14α-demethylase, an enzyme essential for ergosterol synthesis, which disrupts fungal cell membrane integrity.

Common adverse effects of ketoconazole include nausea, vomiting, abdominal pain, and elevated liver enzymes, with hepatotoxicity being a notable concern.

Ketoconazole carries a boxed warning for severe hepatotoxicity, including cases of liver failure and death, and should not be used as a first-line treatment for fungal infections when other safer antifungals are available.

Another boxed warning highlights ketoconazole’s potential to prolong the QT interval, increasing the risk for life-threatening ventricular arrhythmias such as torsades de pointes.

Ketoconazole is a strong inhibitor of CYP3A4 and can cause significant drug interactions by increasing serum concentrations of medications metabolized by this pathway, including statins, certain benzodiazepines, and some antiarrhythmic.

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Lotrisone (Clotrimazole/Betamethasone) Pharmacology

Lotrisone is a topical cream that contains a combination of clotrimazole, an antifungal, and betamethasone dipropionate, a corticosteroid.

It is used to treat fungal skin infections such as athlete’s foot, jock itch, and ringworm that also involve inflammation or itching.

Clotrimazole works by disrupting the fungal cell membrane, while betamethasone reduces redness, swelling, and itching.

Lotrisone should not be used on the face, groin, or underarms for extended periods due to the risk of skin thinning and other steroid-related side effects.

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Clotrimazole Pharmacology

On this podcast episode, I discuss Clotrimazole pharmacology, adverse effects, indications, administration, and much more.

Clotrimazole is an imidazole antifungal that exerts its pharmacological effect by inhibiting the synthesis of ergosterol, an essential component of fungal cell membranes. This inhibition compromises membrane integrity, leading to leakage of cellular contents and ultimately fungal cell death.

Clotrimazole is primarily used topically due to poor systemic absorption when administered via the skin or mucous membranes, which limits systemic side effects.

When clotrimazole is used intravaginally or orally in lozenge form, localized concentrations are sufficient to treat mucocutaneous infections without significant systemic exposure.

Pay attention when clotrimazole is used frequently to treat Candida infections as corticosteroids, immunosuppression, and antibiotics may increase the risk of this type of infection.

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Gentamicin Pharmacology Podcast Episode 311

On this podcast episode, I discuss gentamicin pharmacology, adverse effects, monitoring, drug interactions and much more!

Drug monitoring is critical with gentamicin. Trough and peak concentrations can guide therapy and identify someone at risk of toxicity.

Nephrotoxicity is a major concern with gentamicin. There are numerous nephrotoxic agents that can increase this risk. I discuss them on the podcast.

Ototoxicity is another risk associated with gentamicin. Loop diuretics like furosemide can increase this risk. Learn more on this podcast episode.

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Levofloxacin Pharmacology Podcast Episode 309

On this podcast episode, I discuss levofloxacin pharmacology, adverse effects, boxed warnings, interactions, and much more.

Levofloxacin is well known to cause QTc prolongation and many drugs can increase this risk such as antiarrhythmics, citalopram, antipsychotics, and many more.

Binding interactions are important when discussing levofloxacin pharmacology. Calcium, iron, magnesium, and many other cations can block the absorption of this medication.

I discuss tendon rupture in relation to levofloxacin use and what factors may increase the risk of this rare adverse effect.

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Tamoxifen Pharmacology Podcast

On this podcast episode, I discuss tamoxifen pharmacology, adverse effects, drug interaction, and much more.

Tamoxifen is converted to a more active compound in the body by CYP2D6.

CYP2D6 inhibitors such as paroxetine, fluoxetine, or bupropion can essentially reduce the effectiveness of tamoxifen.

Hot flashes are a common adverse effect of tamoxifen and I discuss a few pharmacologic options to manage this adverse effect.

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Clindamycin Pharmacology Podcast

On this podcast episode, I discuss clindamycin pharmacology, adverse effects, drug interactions, and much more!

Clindamycin (oral administration) can cause esophageal irritation and it is recommended to take this medication with a full glass of water.

C. Diff risk and frequent dosing are two of the biggest downsides to using clindamycin to manage infections.

Clindamycin has good activity against many gram-positive organisms like Staph and Strep as well as anaerobic activity.

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Cefuroxime Pharmacology Podcast

On this episode, I discuss cefuroxime pharmacology, adverse effects, drug interaction, pharmacokinetics, and much more.

Cefuroxime is a 2nd generation cephalosporin that binds Penicillin-binding proteins and prevents bacterial cell wall synthesis.

Medications that create a higher pH in the stomach such as antacids can ultimately reduce the concentrations of cefuroxime.

Cefuroxime is primarily eliminated by the kidney. Dose adjustments are recommended for patients with a CrCL less than 30 mls/min.

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Minocycline Pharmacology Podcast

Minocycline is a tetracycline antibiotic. I discuss pharmacology, adverse effects, and drug interactions.

Minocycline can cause sun sensitivity. Be sure to educate patients about this risk.

Metal cations like iron, zinc, calcium, and magnesium can bind minocycline and reduce the oral absorption of the medication.

Tooth discoloration is a possible adverse effect if minocycline is given to pediatric patients. I discuss it further in this episode.

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Cephalexin (Keflex) Pharmacology Podcast

On this podcast episode, I discuss cephalexin pharmacology, adverse effects, drug interactions, and much more!

Penicillin allergies and cross-reactivity are common questions with regard to the use of cephalexin and I discuss this briefly in the podcast episode.

Cephalexin is a first-generation cephalosporin with its primary sweet spot being gram-positive bacteria like Staph and Strep species.

Warfarin, probenecid, zinc, and a couple of others are potential medications that can interact with cephalexin. I discuss this further in this podcast episode.

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