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Amlodipine

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Summary
Common uses
Hypertension0, Stable angina0, Vasospastic angina0
Pharmacy
Starting dose
2.5-5 mg PO once daily; titrate to 10 mg/d
Preparations
2.5, 5, 10 mg tablets; 1 mg/mL oral suspension
US FDA Max
10 mg/d
Pharmacology
Routes
Oral
Onset
BP effect within 24 hours; full effect at 1-2 weeks (long half-life)
Duration
24 hours
Half-life
30-50 hours[1]
Bioavailability
64-90% (oral; not affected by food)[1]
Pregnancy
Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Amlodipine is a dihydropyridine calcium channel blocker that selectively inhibits L-type voltage-gated calcium channels in vascular smooth muscle, producing peripheral arterial vasodilation with minimal direct cardiac effect.0 The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Norvasc (amlodipine besylate), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019787s055lbl.pdf