Oseltamivir Pharmacology

Oseltamivir is an antiviral agent that is indicated for the treatment and prophylaxis of influenza.

It is important to remember that oseltamivir is cleared at least in part by the kidney and dose adjustments should be made based upon kidney function.

There is a low potential that oseltamivir could contribute to psych issues like delirium.

Probenecid has the potential to raise the concentrations of oseltamivir.

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Dolutegravir

Dolutegravir is an integrase inhibitor that is used in the management of HIV infection/

Carbamazepine along with other enzyme inducers can substantially lower the concentrations of dolutegravir.

Dolutegravir can potentially increase blood sugars, this should be closely monitored in our patients with diabetes.

CNS adverse effects like insomnia and dizziness can happen with dolutegravir.

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Medroxyprogesterone Acetate Injection Pharmacology

On this podcast episode, I cover medroxyprogesterone acetate injection pharmacology (DMPA or Depo-Provera)

Medroxyprogesterone acetate injection is given every three months for the prevention of pregnancy.

Medroxyprogesterone acetate has a boxed warning for its risk of causing low bone mineral density.

Classic enzyme inducers can cause lower concentrations of medroxyprogesterone which can potentially lead to contraceptive failure.

Examples of enzyme inducers that can lower concentrations of medroxyprogesterone include carbamazepine, phenytoin, rifampin, and some agents used in the management of HIV.

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Budesonide Formoterol Pharmacology

Budesonide and Formoterol Pharmacology

Budesonide/formoterol inhalation is sold under the brand name Symbicort.

Budesonide/formoterol is a combination agent that is used in the management of COPD and asthma.

Budesonide/formoterol is a combination of an inhaled corticosteroid and long-acting beta-agonist.

GINA guidelines now allow for the use of budesonide/formoterol in the management of acute asthma exacerbation.

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Benztropine Pharmacology

Benztropine Pharmacology

Benztropine is a highly anticholinergic medication that is primarily used for movement disorders.

Antipsychotics can cause extrapyramidal adverse effects that can help be managed with benztropine.

Because benztropine is highly anticholinergic, it can cause dry eyes, dry mouth, urinary retention, constipation and contribute to falls and confusion, particularly in our elderly population.

While benztropine is classified as an anti-Parkinson’s agent, it is rarely used for that indication as it has a high incidence of anticholinergic adverse effects (particularly at the doses that are required for benefit).

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Budesonide Pharmacology (Oral and Rectal Formulations)

Budesonide is a corticosteroid that can be given orally or rectally for management of Crohn’s disease or ulcerative colitis.

Because budesonide has a high first pass metabolism, the relative impact of systemic effects may be less than other steroids like prednisone.

Remember that CYP3A4 inhibitors can increase the concentrations of budesonide. I discuss this further on the podcast.

Different dosage forms of budesonide (oral versus rectal) can be used for different reasons. The site of the inflammation in Ulcerative colitis can determine which dosage form is most appropriate.

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Cimetidine Pharmacology

Cimetidine blocks histamine 2 receptors which can suppress acid production and reduce symptoms of heartburn.

One of the major downsides to cimetidine is that it has a ton of drug interactions. I discuss many of the common ones in this episode.

Cimetidine is one of a few drugs that has the potential to cause gynecomastia. I discuss the mechanism of this adverse effect in this episode.

Phenytoin concentrations can rise due to the use of cimetidine. I discuss this in the drug interactions section of this episode.

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Clopidogrel Pharmacology

Clopidogrel is an antiplatelet agent that is often used in combination with aspirin to help reduce the risk of an MI.

The risk of bleed is a high priority with the use of clopidogrel. Patients must be monitored for signs and symptoms of bleeding and bruising.

Clopidogrel is a prodrug that is converted to its active metabolite by CYP2C19.

Fluconazole can inhibit CYP2C19 which may reduce the effectiveness of clopidogrel.

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Sulfasalazine Pharmacology

Sulfasalazine is a medication that can be used for diseases like rheumatoid arthritis, Crohn’s disease, and Ulcerative Colitis.

Because sulfasalazine can cause GI upset, this is a major reason why we try to break up the dose and give it multiple (at least two) times per day.

LFT and CBC monitoring are recommended with sulfasalazine due to its low potential to cause liver dysfunction, aplastic anemia, and agranulocytosis.

Sulfasalazine can impair folic acid absorption and lead to potential deficiency. A patient deficient in folic acid is at higher risk for developing anemia.

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Cholestyramine Pharmacology

On this episode, I discuss the pharmacology of cholestyramine.

Cholestyramine was originally developed as an agent to manage cholesterol, but has fallen out of favor for some of the more effective agents like statins.

Cholestyramine is notorious for binding drug interactions. It can reduce concentrations of drugs like amiodarone, digoxin, oral contraceptives, immunosuppressive and many more!

In patients with chronic diarrhea, cholestyramine is occasionally used off label to help manage symptoms because it tends to have constipating effects.

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