Real Life Pharmacology - Pharmacology Education for Health Care Professionals

On this episode, I discuss the pharmacology of oral semaglutide. It is a GLP-1 agonist that is the first one in the class to have an oral formulation. There is a recommended dose titration with oral semaglutide that can take a month or two to get therapeutic doses. I disucss this further in this episode. The most common adverse effect of oral semaglutide is nausea. Oral semaglutide is dosed once d...

Patients with G6PD deficiency who are taking probenecid are at increased risk for hemolytic anemia. In a patient taking probenecid, they need to have adequate kidney function for the drug to work. GI upset is likely the most common adverse effect of probenecid. It can be given with food. Probenecid can raise the concentrations of many common antibiotics like penicillins and cephalosporins. Remembe...

Nicotine replacement therapy is an important tool in helping our patients quit smoking. There are lots of clinical pearls involving the pharmacology of nicotine patches and I explore them in this episode. Nicotine patches differ from the gum and other acute relief forms in that they are intended to provide a consistent level of nicotine in the body. The initial dosing of nicotine patches is depend...

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 antic...

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 great...

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 fluo...

Metoprolol is a beta-blocker commonly used in the management of hypertension, heart failure, and atrial fibrillation. There is an extended release dosage form and immediate release dosage form with metoprolol. The advantage of the extended release product is that it doesn’t require as frequent dosing. Metoprolol is selective for beta-1 receptors. It is less likely to interact with asthma med...

Mometasone is an inhaled corticosteroid and a nasal corticosteroid. The inhaled steroid is called Asmanex by brand name and the nasal version is Nasonex. Nasonex is primarily used in the management of allergic rhinitis and can help with nasal congestion type symptoms. Remember that nasal mometasone takes a little while to have its full effect. It can take up to a week or two to provide its maximum...

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 ar...

Cilostazol has antiplatelet and vasodilatory effects. Because of this, it can manage symptoms of intermittent claudication. GI upset, headache, and edema are common adverse effects associated with the use of cilostazol. Cilostazol is recommended to be given on an empty stomach. In patients with heart failure, cilostazol use is contraindicated. CYP3A4 interactions are prevalent with cilostazol. Inh...

Metronidazole (Flagyl) is an antibiotic that is used for various infections. Metronidazole can certainly cause GI upset like most antibiotics, but uniquely may also cause a metallic taste. Metronidazole is also rarely associated with CNS changes and can induce the potential for peripheral neuropathy. Patients should avoid alcohol with the use of metronidazole and this is on account for the possibi...

Testosterone replacement is primarily utilized in patients with hypogonadism. I discuss testosterone pharmacology, adverse effects, and drug interactions on this podcast episode. Testosterone is a controlled substance because it is most often diverted for its potential to build muscle in athletes for competitive sports. There is cardiovascular risks associated with the use of testosterone. Testost...

Morphine has opioid agonist activity that can cause respiratory depression and death in overdose. Morphine-6-glucuronide is the metabolite that can accumulate and cause CNS toxicity in renal failure. Be aware of CNS depressants that may enhance the effect of morphine and other opioids. Some examples of CNS depressants include gabapentin, benzodiazepines, older antihistamine, skeletal muscle relaxa...

Prasugrel is a P2Y12 inhibitor that is used in the setting of ACS. Be aware of patients who may be taking over the counter medications that can increase their bleed risk while taking prasugrel. Prasugrel is on the Beers list and in general, should be avoided in most situations for patients who are 75 years of age or older. Morphine has the potential to impact antiplatelet agents like prasugrel and...

Mirabegron is a beta-3 agonist that can help relax bladder smooth muscle and manage symptoms of overactive bladder. Mirabegron inhibits CYP2D6 which can negatively impact the effectiveness of tamoxifen. I discuss this in greater detail in the podcast. Tramadol and codeine effectiveness can be impacted by mirabegron. Be aware of this when using this medication. By inhibiting CYP2D6, mirabegron can...

Erythromycin uniquely has some potential benefit in the setting of gastroparesis. Azithromycin you will likely not see used for this indication. Erythromycin binds the 50s subunit and ultimately prevents protein synthesis which is necessary for bacteria to grow and replicate. QTc prolongation is a risk with all macrolide antibiotics (erythromycin included). By inhibiting CYP3A4, erythromycin can b...

Naloxone is a life saving drug that can help manage an opioid overdose situation. Naloxone blocks opioids receptors so opioid agonists cannot bind there. One of the biggest risks with opioid overdose includes respiratory depression. Naloxone can help reduce the risk of this if administered in a timely manner. IV naloxone will have the quickest physiological onset of action, but nasal naloxone may...

Prochlorperazine has several potential mechanisms of action. It can block dopamine and alpha receptors as well as have anticholinergic effects. Prochlorperazine is classified as an antipsychotic and antiemetic. It is very seldom used as an antipsychotic in clinical practice and more used for its antiemetic effects. Because of the anticholinergic activity of prochlorperazine, there is potential for...

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 b...

Ondansetron (Zofran) is a medication used for nausea and vomiting. In this episode, I lay out the pharmacology, adverse effects, drug interactions and more! Ondansetron has been reported to increase the risk of serotonin syndrome. I discuss this further on the podcast. Ondansetron can exacerbate QTc prolongation. Keep an eye out for patients who may have risk factors or be on other medications tha...

On this episode “Acyclovir Pharmacology” I discuss the mechanism of action, important monitoring parameters, and drug interactions with acyclovir. I discuss why acyclovir has to be dosed so many times per day. Acyclovir can inhibit CYP1A2 which can impact a few drugs. I discuss a couple of those examples on this podcast episode. GI effects are one of the more common side effects of acy...

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 prim...

Celecoxib is easy to remember as its mechanism of action is “COX”-2 Inhibition. This can result in result in reduced prostaglandin formation and help with pain and inflammation. Kidney function is important to monitor in our patient on celecoxib. It is especially important in patients taking ACE inhibitors, ARBs, and/or diuretics. While GI bleed may be less likely with celecoxib compar...

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...

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. Be sure to...