pharmacopeia
GET
/api/v1/drug/amlodipine
2D structure
3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN
InChIKey HTIQEAQVCYTUBX-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites.

Calcium ChannelCytochrome P450 3AL-Calcium Channel Receptor

Indications

Sourced from openFDA
  • Amlodipine besylate tablets are calcium channel blocker and may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of: •Hypertension ( 1.1 ) о Amlodipine besylate tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.ICD-10: I10

Contraindications

Sourced from openFDA
  • Known sensitivity to amlodipine ( 4 ) Amlodipine besylate tablets are contraindicated in patients with known sensitivity to amlodipine.contraindicated

Dosage & administration

Sourced from openFDA

•Adult recommended starting dose: 5 mg once daily with maximum dose 10 mg once daily. ( 2.1 ) о Small, fragile, or elderly patients, or patients with hepatic insufficiency may be started on 2.5 mg once daily. ( 2.1 ) •Pediatric starting dose: 2.5 mg to 5 mg once daily. ( 2.2 ) Important Limitation : Doses in excess of 5 mg daily have not been studied in pediatric patients. ( 2.2 ) 2.1 Adults The usual initial antihypertensive oral dose of amlodipine besylate tablet is 5 mg once daily and the maximum dose is 10 mg once daily. Small, fragile, or elderly patients, or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used when adding amlodipine besylate tablet to other antihypertensive therapy. Adjust dosage according to blood pressure goals. In general, wait 7 to 14 days between titration steps. Titrate more rapidly, however, if clinically warranted, provided the patient is assessed frequently. Angina The recommended dose for chronic stable or vasospastic angina is 5 to 10 mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency. Most patients will require 10 mg for adequate effect. Coronary artery disease The recommended dose range for patients with coronary artery disease is 5 to 10 mg once daily. In clinical studies, the majority of patients required 10 mg [see CLINICAL STUDIES (14.4) ] . 2.2 Children The effective antihypertensive oral dose in pediatric patients ages 6 to 17 years is 2.5 mg to 5 mg once daily.

Warnings & precautions

Sourced from openFDA

Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis. However, acute hypotension is unlikely. ( 5.1 ) Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of amlodipine, particularly in patients with severe obstructive coronary artery disease. ( 5.2 ) Titrate slowly in patients with severe hepatic impairment. ( 5.3 ) 5.1 Hypotension Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis. Because of the gradual onset of action, acute hypotension is unlikely. 5.2 Increased Angina or Myocardial Infarction Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of amlodipine, particularly in patients with severe obstructive coronary artery disease. 5.3 Patients with Hepatic Failure Because amlodipine besylate is extensively metabolized by the liver and the plasma elimination half-life (t 1/2 ) is 56 hours in patients with impaired hepatic function, titrate slowly when administering amlodipine besylate to patients with severe hepatic impairment.

Adverse reactions

Sourced from openFDA

Most common adverse reaction to amlodipine is edema which occurred in a dose related manner. Other adverse experiences not dose related but reported with an incidence >1.0% are fatigue, nausea, abdominal pain, and somnolence. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc. at 1-800-399-2561 or www.lupinpharmaceuticals.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Amlodipine has been evaluated for safety in more than 11,000 patients in U.S. and foreign clinical trials. In general, treatment with amlodipine was well-tolerated at doses up to 10 mg daily. Most adverse reactions reported during therapy with amlodipine were of mild or moderate severity. In controlled clinical trials directly comparing amlodipine (N=1730) at doses up to 10 mg to placebo (N=1250), discontinuation of amlodipine because of adverse reactions was required in only about 1.5% of patients and was not significantly different from placebo (about 1%). The most commonly reported side effects more frequent than placebo are reflected in the table below. The incidence (%) of side effects that occurred in a dose related manner are as follows: Amlodipine Placebo 2 .

Use in specific populations

Sourced from openFDA

Pediatric: Effect on patients less than 6 years old is not known. ( 8.4 ) Geriatric: Start dosing at the low end of the dose range. ( 8.5 ) 8.1 Pregnancy Risk Summary The limited available data based on post-marketing reports with amlodipine use in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled hypertension in pregnancy [see Clinical Considerations] . In animal reproduction studies, there was no evidence of adverse developmental effects when pregnant rats and rabbits were treated orally with amlodipine maleate during organogenesis at doses approximately 10 and 20-times the maximum recommended human dose (MRHD), respectively. However for rats, litter size was significantly decreased (by about 50%) and the number of intrauterine deaths was significantly increased (about 5-fold). Amlodipine has been shown to prolong both the gestation period and the duration of labor in rats at this dose [see Data]. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S.

Overdosage

Sourced from openFDA

Overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia. In humans, experience with intentional overdosage of amlodipine is limited. Single oral doses of amlodipine maleate equivalent to 40 mg amlodipine/kg and 100 mg amlodipine/kg in mice and rats, respectively, caused deaths. Single oral amlodipine maleate doses equivalent to 4 or more mg amlodipine/kg or higher in dogs (11 or more times the maximum recommended human dose on a mg/m 2 basis) caused a marked peripheral vasodilation and hypotension. If massive overdose should occur, initiate active cardiac and respiratory monitoring. Frequent blood pressure measurements are essential. Should hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids. If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output. As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit.

Approval history

Sourced from openFDA
  • Jul 31, 1992NDANDA019787Viatris
  • Mar 3, 1995NDANDA020364Sandoz
  • Jan 30, 2004NDANDA021540Pharmacia
  • Jun 20, 2007NDANDA021990Novartis
  • Sep 26, 2007NDANDA022100Cosette
  • Apr 30, 2009NDANDA022314Novartis
  • Jul 23, 2010NDANDA200175Cosette
  • Jul 8, 2019NDANDA211340Azurity

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
431,545 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue26,1696.1%
  2. 2Diarrhoea22,8325.3%
  3. 3Nausea22,6045.2%
  4. 4Dyspnoea21,5845.0%
  5. 5Drug Ineffective20,3854.7%
  6. 6Dizziness18,3724.3%
  7. 7Headache17,0674.0%
  8. 8Off Label Use17,0223.9%
  9. 9Pain16,3073.8%
  10. 10Asthenia14,8633.4%
  11. 11Vomiting14,4963.4%
  12. 12Fall14,4553.3%
  13. 13Hypertension13,8873.2%
  14. 14Death13,6003.2%
  15. 15Malaise13,4853.1%

Literature

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Recent PubMed references pinned to Amlodipine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 717 ClinicalTrials.gov registrations naming Amlodipine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Amlodipine work?
Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites.
What is Amlodipine used for?
According to FDA labeling, Amlodipine carries indications including: Amlodipine besylate tablets are calcium channel blocker and may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of: •Hypertension ( 1.1 ) о Amlodipine besylate tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Amlodipine?
Amlodipine is classified as Dihydropyridine derivatives, Calcium Channel Blocker, Dihydropyridine Calcium Channel Blocker, Calcium Channel Antagonists, Cytochrome P450 3A Inhibitors, L-Calcium Channel Receptor Antagonists, Coronary Arterial Vasodilation, Decreased Blood Pressure.
What are the brand names for Amlodipine?
Amlodipine is marketed under brand names including Azor, Caduet, Consensi, Exforge, Exforge HCT, Katerzia, Lotrel, Norliqva.
What are the contraindications for Amlodipine?
Amlodipine labeling lists contraindications including: Known sensitivity to amlodipine ( 4 ) Amlodipine besylate tablets are contraindicated in patients with known sensitivity to amlodipine.. Always consult the full prescribing information and a clinician.
Note. Data for amlodipine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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