Cefepime Pharmacology

Cefepime is a fourth-generation cephalosporin antibiotic with broad-spectrum activity against both gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. It works by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins, leading to cell lysis and death.

Clinically, cefepime is commonly used in hospital settings for serious infections such as pneumonia, febrile neutropenia, urinary tract infections, skin infections, and intra-abdominal infections. It’s typically administered intravenously, with doses often ranging from 1 to 2 grams every 8 to 12 hours depending on the indication and renal function.

From a pharmacokinetic standpoint, cefepime is primarily renally eliminated, so dose adjustments are required in patients with impaired kidney function. Failure to reduce the dose appropriately can lead to neurotoxicity — one of the key adverse effects associated with cefepime — manifesting as encephalopathy, confusion, myoclonus, or seizures, particularly in elderly or renally impaired patients.

Common side effects include gastrointestinal upset and rash. Cefepime has relatively limited drug interactions, though concurrent nephrotoxic agents can increase the risk of renal injury.

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Piperacillin/Tazobactam Pharmacology

Zosyn (piperacillin/tazobactam) is a broad-spectrum β-lactam/β-lactamase inhibitor combination used widely in hospitals. Piperacillin covers gram-positive, gram-negative, and anaerobic bacteria, while tazobactam helps protect against β-lactamase breakdown. It is commonly used for pneumonia, intra-abdominal infections, skin and soft tissue infections, and febrile neutropenia. An important pharmacology pearl for exams is understanding that Pseudomonas, but it doesn’t cover MRSA.

The drug is renally eliminated, so dosing adjustments are needed in kidney impairment. Many institutions use extended or prolonged infusions to maximize time above the MIC, which can improve efficacy. Standard dosing is 3.375 g to 4.5 g every 6–8 hours, with modifications for dialysis patients.

Adverse effects include hypersensitivity, gastrointestinal upset, electrolyte imbalances like hypokalemia, and blood count changes with prolonged therapy. A key clinical concern is nephrotoxicity risk, especially when used with vancomycin. Monitoring renal function and electrolytes are important.

Methotrexate and probenecid are two medications that can interact with Zosyn. Concentrations of Zosyn can be increased when these medications are used in combination.

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Ciprofloxacin Pharmacology Podcast

On this podcast, I cover ciprofloxacin pharmacology. Ciprofloxacin is one of the most widely recognized fluoroquinolone antibiotics and has been on the market for decades. Because of its broad utility, it often comes up in practice, but it also carries significant adverse effect concerns and boxed warnings that pharmacists and prescribers need to keep in mind.

From a pharmacology standpoint, ciprofloxacin works by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes that are essential for bacterial DNA replication, transcription, and repair. This action gives ciprofloxacin bactericidal activity against a variety of gram-negative organisms, including E. coli, Klebsiella, Enterobacter, and Pseudomonas aeruginosa. It also has some gram-positive activity, though it is generally not the best choice for strep infections.

Ciprofloxacin comes in multiple dosage forms, including oral tablets, oral suspension, and intravenous formulations, which makes it flexible across care settings. I discuss the conversion of IV and PO formulations.

Pharmacokinetics are important to consider. Ciprofloxacin is primarily renally eliminated, so dose adjustments are necessary in patients with impaired kidney function. Distribution into tissues is generally good, but it has limited activity in the lungs against Streptococcus pneumoniae, which is why it is not a first-line option for community-acquired pneumonia.

Adverse effects are a major concern. The fluoroquinolone class carries multiple boxed warnings. Ciprofloxacin has been associated with tendon rupture, peripheral neuropathy, CNS effects such as agitation or seizures, and exacerbation of myasthenia gravis. More recent warnings include the risk for aortic aneurysm and hypoglycemia or hyperglycemia, particularly in older adults or those with comorbidities. On top of these boxed warnings, ciprofloxacin can also prolong the QT interval and cause GI upset.

Drug interactions are another big factor in practice. Ciprofloxacin is a CYP1A2 inhibitor, which can raise levels of drugs like theophylline, tizanidine, and clozapine. It also interacts with polyvalent cations such as calcium, magnesium, iron, and aluminum, which can dramatically reduce its absorption—sometimes by more than 50%. This is a common reason for treatment failure if counseling isn’t provided.

From a dosing perspective, ciprofloxacin is usually given 250–750 mg orally twice daily or 400 mg IV every 8–12 hours depending on the indication and severity of infection. Renal dosing adjustments are needed as kidney function declines.

In summary, ciprofloxacin is a powerful antibiotic when used appropriately. It remains an option for urinary tract infections, complicated intra-abdominal infections, and some cases of hospital-acquired pneumonia, but its use must be balanced with the potential for significant adverse effects and interactions. For pharmacists, educating patients on drug interactions, counseling about boxed warnings, and ensuring correct dosing in renal impairment are some of the most valuable interventions when ciprofloxacin shows up on a medication list.

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Itraconazole Pharmacology

In this episode, we break down itraconazole—a potent antifungal with a lot of baggage. If you’re a pharmacist, clinician, or student who needs to understand how this drug works and why it can be tricky to use, this episode is for you.

We start with the basics. Itraconazole blocks 14α-demethylase, an enzyme fungi need to make their cell membranes. That disruption kills or slows the fungus. It works against tough bugs like Aspergillus, Histoplasma, and Blastomyces, plus common skin infections.

Side effects? Nausea, liver enzyme elevations, and more seriously, heart failure. Yes, itraconazole has a black box warning for worsening or causing congestive heart failure. If your patient has heart issues, think twice.

Drug interactions are everywhere. Itraconazole is a strong CYP3A4 inhibitor. It can raise levels of drugs like statins, benzos, calcium channel blockers, and immunosuppressants—sometimes to dangerous levels. Don’t co-prescribe without checking.

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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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