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June 21, 2021

Calcium Channel Blockers (Mechanism of Action)

๐Ÿ’Š 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. โ  โ  ๐Ÿ’Š The name of this class, calcium channel blockers, hints at its mechanism of action โ€“ inhibits the entry of calcium into cells of the cardiac and peripheral vascular smooth muscles. โ  โ  ๐Ÿ—’๏ธ Calcium entry into L-type channels of cardiac and peripheral vascular cells is needed for them to contract or constrict more strongly. โ  โ  ๐Ÿ—’๏ธ By blocking calcium entry, calcium channel blockers cause:โ  ๐Ÿ‘‰๐Ÿป peripheral vascular smooth muscle relaxation (decreases blood pressure)โ  ๐Ÿ‘‰๐Ÿป decreased myocardial contractility (decrease myocardial demand making them effective in angina)โ  ๐Ÿ‘‰๐Ÿป decrease heart rate and conduction velocity (useful in arrhythmias). โ 

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Entrestoยฎ (Sacubitril/Valsartan)

๐Ÿ“– Angiotensin receptor-neprilysin inhibitors (ARNI) is a new class of heart failure medications. โ 
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โ˜๐Ÿป The first drug in this class is Entrestoยฎ (sacubitril/valsartan). It is a combination medication comprised of a neprilysin inhibitor (sacubitril) and an angiotensin II receptor blocker (valsartan). โ 
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๐Ÿ’Š 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. โ 
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๐Ÿ’Š Valsartan directly blocks angiotensin II receptors inhibiting angiotensin II from binding onto the receptors and causing vasoconstriction and aldosterone release.โ 
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Pharmacokinetics in Pregnancy

๐Ÿคฐ๐Ÿป 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. โ โ €
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Some tips include:โ โ €
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๐Ÿ‘‰๐Ÿป Only using antibiotics when no other treatment options are available โ โ €
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๐Ÿ‘‰๐Ÿป Avoid prescribing antibiotics during the first trimester if possible. โ โ €
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๐Ÿ‘‰๐Ÿป Chose a safe medication with available clinical studies that have been tested in pregnancyโ โ €
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๐Ÿ‘‰๐Ÿป Dose at the lowest possible amount proven effective.โ โ €

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