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June 21, 2021

Calcium Channel Blockers (Mechanism of Action)

💊 Calcium channel blockers (CCBs) are used in the treatment of many cardiovascular conditions including hypertension and angina. They are divided into subclasses, non-dihydropyridines, and dihydropyridines and differ by their pharmacokinetic properties, clinical uses, response, and selectivity. ⁠ ⁠ 💊 The name of this class, calcium channel blockers, hints at its mechanism of action – inhibits the entry of calcium into cells of the cardiac and peripheral vascular smooth muscles. ⁠ ⁠ 🗒️ Calcium entry into L-type channels of cardiac and peripheral vascular cells is needed for them to contract or constrict more strongly. ⁠ ⁠ 🗒️ By blocking calcium entry, calcium channel blockers cause:⁠ 👉🏻 peripheral vascular smooth muscle relaxation (decreases blood pressure)⁠ 👉🏻 decreased myocardial contractility (decrease myocardial demand making them effective in angina)⁠ 👉🏻 decrease heart rate and conduction velocity (useful in arrhythmias). ⁠

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Entresto® (Sacubitril/Valsartan)

📖 Angiotensin receptor-neprilysin inhibitors (ARNI) is a new class of heart failure medications. ⁠

☝🏻 The first drug in this class is Entresto® (sacubitril/valsartan). It is a combination medication comprised of a neprilysin inhibitor (sacubitril) and an angiotensin II receptor blocker (valsartan). ⁠

💊 Sacubitril is a prodrug that inhibits neprilysin thus preventing it from breaking down natriuretic peptides. This mechanism leads to an increase in vasodilation and diuresis as levels of natriuretic peptides rise. ⁠

💊 Valsartan directly blocks angiotensin II receptors inhibiting angiotensin II from binding onto the receptors and causing vasoconstriction and aldosterone release.⁠

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Pharmacokinetics in Pregnancy

🤰🏻 Choosing an effective yet safe antibiotic during pregnancy requires you to weigh the risks and benefits. It can often be a gray area based on limited clinical studies in pregnant patients. ⁠⠀
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Some tips include:⁠⠀
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👉🏻 Only using antibiotics when no other treatment options are available ⁠⠀
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👉🏻 Avoid prescribing antibiotics during the first trimester if possible. ⁠⠀
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👉🏻 Chose a safe medication with available clinical studies that have been tested in pregnancy⁠⠀
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👉🏻 Dose at the lowest possible amount proven effective.⁠⠀

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