Bisoprolol (Zebeta) Pharmacology

On this episode, I discuss bisoprolol (Zebeta) pharmacology, adverse effects, drug interactions, and other important clinical pearls.

Bisoprolol is a beta-1 selective antagonist that can be used for atrial fibrillation, angina, and other cardiovascular indications.

It is important to remember that bisoprolol and other beta-blockers are not considered first-line agents for hypertension alone.

Beta-receptor selectivity does start to disappear with bisoprolol as you get to higher dosages. I discuss this further in the podcast.

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Rosuvastatin Pharmacology

On this episode, I discuss rosuvastatin pharmacology, adverse effects, drug interactions and pharmacokinetics.

Rosuvastatin is a hydrophilic statin which differs from some of the most commonly used statins like simvastatin and atorvastatin.

Rosuvastatin is minimally affected by CYP3A4 drug interactions so that is a small potential advantage over simvastatin and atorvastatin.

At dosages of 20-40 mg, rosuvastatin is considered a high intensity statin and can bring down LDL by over 50%.

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Propranolol Pharmacology

On this episode, I discuss propranolol pharmacology, adverse reactions, and important drug interactions you should know.

Propranolol (Inderal) is a non-selective beta-blocker. There are many indications for it including hypertension, tachycardia, atrial fibrillation, post-MI, chronic stable angina, essential tremors, migraine prophylaxis, esophageal varices, performance anxiety disorder, lithium-induced tremor, psychotic induced akathisia, and thyroid storm.

Propranolol blocks beta-1 receptors that are commonly referred to as the cardiac receptors and beta-2 receptors that are in the lungs. Albuterol is a beta-2 agonist meaning that propranolol can block its effects. This may lead to bronchospasms and worsening of respiratory conditions. This is one of the major issues when using a non-selective beta-blocker vs a selective one.

Other adverse effects include a drop in blood pressure and pulse. Fatigue is also seen in many geriatric patients so it is important to be titrating them up slowly. If you notice patients increasing caffeine intake, starting a stimulant, or experiencing new depression symptoms that can be a sign of fatigue. Sexual dysfunction has also been seen in patients taking propranolol. Propranolol may mask symptoms of hypoglycemia. Closely monitor patients that are taking insulin and/or sulfonylureas. Abrupt discontinuation can increase the risk for acute coronary syndromes, especially if the patient is already at risk. Make sure that the medication is taken consistently and there aren’t periods of multiple missed doses.

Propranolol comes in multiple dosage forms that have been mixed up. When dispensing or administering take extra caution that the medication is correct.

Propranolol is a weak CYP1A2 inhibitor that could increase concentrations of tizanidine or theophylline. Propranolol also gets broken down by CYP1A2. Medications that inhibit this enzyme can increase the concentration of propranolol. Examples of these are ciprofloxacin and fluvoxamine. Inducers of CYP1A2 can reduce concentrations. These are rifampin, carbamazepine, and phenobarbital. A unique CYP1A2 inducer is smoking tobacco. Medications can cause additive effects when it comes to blood pressure and pulse. Be careful with any blood pressure-lowering medications including antihypertensives, PDE5 inhibitors (sildenafil), and Parkinson’s medications (Sinemet). Drugs that can lower pulse include centrally acting alpha 2 antagonists (clonidine) and acetylcholinesterase inhibitors (donepezil, rivastigmine).

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

Study Materials For Pharmacists and Students

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Cilostazol Pharmacology

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. Inhibitors of CYP3A4 can increase the concentrations of cilostazol.

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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.

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