Prasugrel Pharmacology

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 make them less effective. Be sure this is clinically considered prior to using morphine with prasugrel.

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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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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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Heparin Pharmacology

Heparin Pharmacology

Heparin is an interesting drug with a lot of unique clinical quirks. This drug ultimately inhibits the formation of fibrin. Fibrin is an essential component of a blood clot.

Because heparin has blood thinning effects, it is critical to assess a patient’s bleed risk. Look out for other agents that may increase the risk of bleeding. Examples include; NSAIDs, antiplatelet agents, and other anticoagulants.

One classic test question about heparin that often comes up is the reversal agent. Protamine can be used to help reverse the effects of heparin.

Heparin-induced thrombocytopenia is a critical adverse effect to understand. I discuss both subtypes on the podcast and let you know what to look out for.

Rarer side effects of heparin include hyperkalemia and osteoporosis (only with long term use).

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Ezetimibe Pharmacology

Ezetimibe Pharmacology

On this episode, I discuss ezetimibe pharmacology. Ezetimibe works by inhibiting Niemann-Pick C1-Like1 (NPC1L1) transporter. This transporter aids in cholesterol absorption so by blocking it, we can reduce cholesterol levels (and LDL) in the bloodstream.

Ezetimibe is usually very well tolerated. Diarrhea, myopathy, and elevations in LFT’s are adverse effects that have been reported but do not occur at high rates.

Ezetimibe is dosed at 10 mg once daily. This is a nice advantage because this is a starting dose and the usual treatment dose.

With the most recent cholesterol guideline updates, I do expect ezetimibe to be utilized a little more than it used to be. They place more emphasis on a target LDL and getting patients to goal.

Statins are going to be used first line for cholesterol and ezetimibe will be an add on therapy to consider. They don’t, unfortunately, lower cholesterol as much as high-intensity statins do.

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Rivaroxaban Pharmacology

Rivaroxaban is a factor 10a inhibitor that inhibits clot formation and thins the blood.

Rivaroxaban needs to be monitored for bleed risk. Checking periodic CBC can help us assess if hemoglobin and hematocrit are remaining stable.

Enzyme inducers like rifampin, St. John’s Wort, and carbamazepine can reduce concentrations and increase the risk of treatment failure.

NSAIDs and antiplatelet medications can significantly increase the risk of bleed with rivaroxaban.

Rivaroxaban should not be used with dual P-glycoprotein and CYP3A4 inhibitors. Examples include ketoconazole, itraconazole, and ritonavir.

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Hydralazine Pharmacology

Hydralazine Pharmacology

Hydralazine Pharmacology

Hydralazine works as a direct vasodilator. It primarily works on the arterioles versus the venous system.

Hydralazine can cause a unique adverse reaction. It can cause a Lupus type syndrome that can result in fever, myopathy and symptoms that mimic arthritis.

I discuss drug interactions with hydralazine and how you need to be aware of certain medications that can have additive effects and also those that can oppose the effects of the drug.

One of the downsides to using hydralazine is that patients don’t like to take it as often as it requires. It is typically dosed three to four times per day.

Orthostasis is a risk with any drug that reduces blood pressure and hydralazine is no different.

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Aspirin Pharmacology

Aspirin Pharmacology

On this episode of the Real Life Pharmacology Podcast, I discuss aspirin pharmacology.

The two most common adverse effects with aspirin are GI upset and increasing the risk for bleeding and bruising.

A commonly asked test question about aspirin is whether it can be used in pediatrics and what risk we encounter if we use it.

Another rare effect with aspirin is tinnitus which I discuss further on this episode.

It is critical to pay attention to other medications that can thin the blood in a patient taking aspirin. Examples include anticoagulants like warfarin, apixaban, rivaroxaban; antiplatelets like clopidogrel or prasugrel; or NSAIDs.

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Clonidine Pharmacology

Clonidine is classified as an antihypertensive. Clonidine pharmacology involves having agonist activity at central alpha 2 receptors. This leads to lower sympathetic outflow and a reduction in blood pressure.

Clonidine has numerous reported uses in addition to its antihypertensive effect. It can potentially be used for ADHD, menopausal type symptoms, and opioid withdrawal.

Clonidine has historically been on the Beers’ list of drugs as it can cause some CNS side effects like sedation, dizziness, and rarely delirium.

Clonidine is unique in the antihypertensive class as it does have a patch formulation.

Because of the blood pressure lowering effect of clonidine, we have to be aware of patients who report dizziness. Monitoring is critical.

Clonidine can also lower heart rate and contribute to dry mouth. Keep an eye out for drugs that can have a cumulative effect on these symptoms.

Drugs like beta-blockers, non-DHP CCB’s, and digoxin can all have a cumulative effect with clonidine and lower pulses. Monitoring is important.

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Loop Diuretics Pharmacology

On this episode, I cover common loop diuretics. They include furosemide, torsemide, and bumetanide.

Loop diuretics are potent agents that can help in the management of heart failure and ascites.

Loops diuretics help promote the loss of excessive fluid through the urine.

A common patient complaint from loop diuretics is that they can cause frequent urination. Because of this, we typically dose these drugs earlier in the day.

Kidney function and electrolyte monitoring is critical with the use of loop diuretics.

Enjoy the episode!

Be sure to check out our free Top 200 study guide – a 31 page PDF that is yours for FREE!