Amlodipine
Identification
- Summary
Amlodipine is a calcium channel blocker used to treat hypertension and angina.
- Brand Names
- Amlobenz, Azor, Caduet, Dafiro, Exforge, Exforge Hct, Katerzia, Lotrel, Norliqva, Norvasc, Prestalia, Tribenzor, Twynsta, Viacoram
- Generic Name
- Amlodipine
- DrugBank Accession Number
- DB00381
- Background
Amlodipine, initially approved by the FDA in 1987, is a popular antihypertensive drug belonging to the group of drugs called dihydropyridine calcium channel blockers. Due to their selectivity for the peripheral blood vessels, dihydropyridine calcium channel blockers are associated with a lower incidence of myocardial depression and cardiac conduction abnormalities than other calcium channel blockers 5.
Amlodipine is commonly used in the treatment of high blood pressure and angina. Amlodipine has antioxidant properties and an ability to enhance the production of nitric oxide (NO), an important vasodilator that decreases blood pressure 3. The option for single daily dosing of amlodipine is an attractive feature of this drug Label.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 408.876
Monoisotopic: 408.145199627 - Chemical Formula
- C20H25ClN2O5
- Synonyms
- (RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
- 3-Ethyl 5-methylester, (±)-2-[(2-aminoethoxy)methyl]-4-(o-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate
- Amlodipine
- Amlodipine free base
- Amlodipino
- Amlodipinum
Pharmacology
- Indication
Amlodipine may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of the following conditions Label:
• Hypertension
• Coronary artery disease
• Chronic stable angina
• Vasospastic angina (Prinzmetal’s or Variant angina)
• Angiographically documented coronary artery disease in patients without heart failure or an ejection fraction < 40%
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to prevent Cardiovascular events Combination Product in combination with: Rosuvastatin (DB01098) •••••••••••• ••••• •••• •••••••••••••• •••• ••••••• •••••••••••• Treatment of Chronic stable angina pectoris •••••••••••• ••••••••••• •••••• Used in combination to manage Chronic stable angina pectoris Combination Product in combination with: Rosuvastatin (DB01098) •••••••••••• ••••• ••••••• •••••••••••• Used in combination to manage Chronic stable angina pectoris Combination Product in combination with: Atorvastatin (DB01076) •••••••••••• Used in combination to manage Coronary artery disease Combination Product in combination with: Atorvastatin (DB01076) •••••••••••• •••••••••••••••• •••••••••• ••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
General pharmacodynamic effects
Amlodipine has a strong affinity for cell membranes, modulating calcium influx by inhibiting selected membrane calcium channels. This drug's unique binding properties allow for its long-acting action and less frequent dosing regimen 1, Label.
Hemodynamic effects
After the administration of therapeutic doses of amlodipine to patients diagnosed with hypertension, amlodipine causes vasodilation, which results in a reduction of supine and standing blood pressure. During these blood pressure reductions, there are no clinically significant changes in heart rate or plasma catecholamine levels with long-term use. Acute intravenous administration of amlodipine reduces arterial blood pressure and increases heart rate in patients with chronic stable angina, however, chronic oral administration of amlodipine in clinical studies did not cause clinically significant alterations in heart rate or blood pressures in patients diagnosed with angina and normal blood pressure. With long-term, once daily oral administration, antihypertensive effectiveness is maintained for at least 24 hours Label.
Electrophysiologic effects
Amlodipine does not change sinoatrial (SA) nodal function or atrioventricular (AV) conduction in animals or humans. In patients who were diagnosed with chronic stable angina, the intravenous administration of 10 mg of amlodipine did not cause clinically significant alterations A-H and H-V conduction and sinus node recovery time after cardiac pacing. Patients administered amlodipine with concomitant beta-blockers produced similar results. In clinical trials in which amlodipine was given in combination with beta-blockers to patients diagnosed with hypertension or angina, no adverse effects on electrocardiographic parameters were noted. In clinical studies comprised of angina patients alone, amlodipine did not change electrocardiographic intervals or produce high degrees of AV block Label.
Effects on angina
Amlodipine relieves the symptoms of chest pain associated with angina. In patients diagnosed with angina, daily administration of a single amlodipine dose increases total exercise time, the time to angina onset, and the time to 1 mm ST-segment depression on ECG studies, decreases anginal attack frequency, and decreases the requirement for nitroglycerin tablets 9.
- Mechanism of action
Mechanism of action on blood pressure
Amlodipine is considered a peripheral arterial vasodilator that exerts its action directly on vascular smooth muscle to lead to a reduction in peripheral vascular resistance, causing a decrease in blood pressure. Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle. Experimental studies imply that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites, located on cell membranes. The contraction of cardiac muscle and vascular smooth muscle are dependent on the movement of extracellular calcium ions into these cells by specific ion channels. Amlodipine blocks calcium ion influx across cell membranes with selectivity. A stronger effect of amlodipine is exerted on vascular smooth muscle cells than on cardiac muscle cells Label. Direct actions of amlodipine on vascular smooth muscle result in reduced blood pressure 9.
Mechanism of action in angina
The exact mechanism by which amlodipine relieves the symptoms of angina have not been fully elucidated to this date, however, the mechanism of action is likely twofold:
Amlodipine has a dilating effect on peripheral arterioles, reducing the total peripheral resistance (afterload) against which the cardiac muscle functions. Since the heart rate remains stable during amlodipine administration, the reduced work of the heart reduces both myocardial energy use and oxygen requirements 9.
Dilatation of the main coronary arteries and coronary arterioles, both in healthy and ischemic areas, is another possible mechanism of amlodipine reduction of blood pressure. The dilatation causes an increase in myocardial oxygen delivery in patients experiencing coronary artery spasm (Prinzmetal's or variant angina) and reduces coronary vasoconstriction caused by smoking 9.
Target Actions Organism AVoltage-dependent L-type calcium channel subunit alpha-1C inhibitorHumans AVoltage-dependent T-type calcium channel subunit alpha-1I inhibitorHumans UVoltage-dependent N-type calcium channel subunit alpha-1B inhibitorHumans UVoltage-dependent L-type calcium channel subunit beta-1 inhibitorHumans UVoltage-dependent calcium channel subunit alpha-2/delta-3 inhibitorHumans UCarbonic anhydrase 1 inhibitorHumans USphingomyelin phosphodiesterase inhibitorHumans UVoltage-dependent N-type calcium channel inhibitorHumans - Absorption
Amlodipine absorbed slowly and almost completely from the gastrointestinal tract. Peak plasma concentrations are achieved 6-12 hours after oral administration. The estimated bioavailability of amlodipine is 64-90%. Steady-state plasma amlodipine levels are achieved after 7-8 days of consecutive daily dosing. Absorption is not affected by food Label.
- Volume of distribution
- Protein binding
- Metabolism
Amlodipine is heavily (approximately 90%) converted to inactive metabolites via hepatic breakdown with 10% of the parent compound and 60% of the metabolites found excreted in the urine. Ex vivo studies have shown that about 93% of the circulating drug is bound to plasma proteins in hypertensive patients Label. Characteristics that add to amlodipine's unique pharmacologic profile include nearly complete absorption, late-peak plasma concentrations, high bioavailability, and slow hepatic breakdown 2.
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- Route of elimination
Elimination from the plasma occurs in a biphasic with a terminal elimination half-life of about 30–50 hours. Steady-state plasma levels of amlodipine are reached after 7-8 days of consecutive daily dosing Label. Amlodipine is 10% excreted as unchanged drug in the urine. Amlodipine can be initiated at normal doses in patients diagnosed with renal failure 9, Label.
- Half-life
The terminal elimination half-life of about 30–50 hours Label.
Plasma elimination half-life is 56 hours in patients with impaired hepatic function, titrate slowly when administering this drug to patients with severe hepatic impairment Label.
- Clearance
Total body clearance (CL) has been calculated as 7 ± 1.3 ml/min/kg (0.42 ± 0.078 L/ h/kg) in healthy volunteers 5, 6.
Elderly patients show a reduced clearance of amlodipine with an AUC (area under the curve) increase of about 40–60%, and a lower initial dose may be required Label.
- Adverse Effects
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- Toxicity
Acute oral toxicity (LD50): 37 mg/kg (mouse) MSDS.
Overdose
An overdose of amlodipine could result in a high degree of peripheral vasodilatation with a possibility of reflex tachycardia. Significant and prolonged hypotension leading to shock and fatal outcomes have been reported Label.
Carcinogenesis, mutagenesis, impairment of fertility
Rats and mice treated with amlodipine maleate in the diet on a long-term basis for up to 2 years demonstrated no evidence of a carcinogenic effect of the drug. For the mouse, the highest dose was comparable to the maximum recommended human dose of 10 mg amlodipine per day. For the rat, the highest dose was measured to be about twice the maximum recommended human dose Label.
Mutagenicity studies using amlodipine maleate showed no drug-related gene or chromosomal effects Label.
There was no impact on the fertility of rats given oral amlodipine maleate (males for 64 days and females for 14 days before mating) at doses up to 10 mg amlodipine/kg/day (8 times the maximum recommended human dose) Label.
Use in pregnancy
The safety of amlodipine in human pregnancy or lactation has not been proven. Amlodipine is therefore considered a pregnancy category C drug 9. Use amlodipine only if the potential benefit justifies the potential risk Label.
Use in nursing
Discontinue when administering amlodipine Label.
- Pathways
Pathway Category Amlodipine Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Natriuretic peptides A --- (A;A) AA allele Effect Directly Studied Patients with this genotype have increased risk of adverse cardiovascular outcomes with diuretics. Details
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide The risk or severity of adverse effects can be increased when Amlodipine is combined with Abaloparatide. Abametapir The serum concentration of Amlodipine can be increased when it is combined with Abametapir. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Amlodipine. Acarbose The risk or severity of hypoglycemia can be increased when Amlodipine is combined with Acarbose. Acebutolol Amlodipine may increase the arrhythmogenic activities of Acebutolol. - Food Interactions
- Avoid grapefruit products.
- Avoid natural licorice.
- Take with or without food. The absorption is unaffected by food.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Amlodipine benzoate XD75TQ8A2P 1239916-29-0 RVPCEXXEUXIPEO-UHFFFAOYSA-N Amlodipine besylate 864V2Q084H 111470-99-6 ZPBWCRDSRKPIDG-UHFFFAOYSA-N Amlodipine camsylate 0V8DBY3260 652969-01-2 UXKMFEPPKJZDAR-STOWLHSFSA-N Amlodipine maleate CQ27G2BZJM 88150-47-4 TZNOWAJJWCGILX-BTJKTKAUSA-N Amlodipine mesylate 291Y33EZHA 246852-12-0 MUVFCHUBATVFPP-UHFFFAOYSA-N Amlodipine mesylate monohydrate FAS0DJC51V 440358-84-9 LGWOIMCQWJLZIT-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Aforbes (Merck) / Agen (Zentiva) / Aken (Kendrick Farmaceutica) / Amcard (Apex Pharma Ltd) / Amdepin (Cadila Pharmaceuticals) / Amdipin (Laboratorios Lafrancol) / Amilostad / Amlocard (AWD (Germany)) / Amlod / Amlodine (Sumitomo Pharmaceuticals) / Amlodipin / Amlodipin-Mepha 5/10 (Mepha Pharma AG) / Amlodipine 5 (PT KALBE FARMA Tbk) / Amlodis (Eczacibasi (Turkey)) / Amlong (Micro Labs) / Amlopin (Lek) / Amlopine (Berlin) / Amlostin (Discovery Pharmaceuticals) / Amlosun (Sun Pharmaceutical) / Amlovas (Macleods Pharmaceuticals Ltd) / Amlovasc (Dr. Reddy's Laboratories) / Amlozek (Adamed) / Amvaz (Reddy (Malaysia)) / Asomex (Emcure Pharmaceuticals) / Atecard-AM (Alembic Ltd) / Camlodin (Square) / Cardilopina / Coroval (Sandoz (Argentina)) / Dailyvasc (Xeno Pharmaceuticals) / Istin / Lama (Stadmed Private Limited) / Lodip (TIME Pharmaceuticals) / Lodopin (Merck Pakistan) / Lopin (Edruc Ltd) / Nelod (The Kemiko Pharmaceuticals Ltd) / Nopidin (Ad-din Pharmaceuticals Ltd) / Nordip / Perivasc / Pharex Amlodipine (PHAREX HealthCorp) / Tenox (Krka)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Amlodipine Tablet 2.5 mg Oral TEVA Canada Limited 2010-03-02 Not applicable Canada Act Amlodipine Tablet 10 mg Oral TEVA Canada Limited 2009-07-10 Not applicable Canada Act Amlodipine Tablet 5 mg Oral TEVA Canada Limited 2009-07-10 Not applicable Canada Amlodipine Tablet 5 mg Oral Meliapharm Inc 2011-04-08 2014-06-25 Canada Amlodipine Tablet 5 mg Oral Sivem Pharmaceuticals Ulc 2012-06-12 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Accel-amlodipine Tablet 5 mg Oral Accel Pharma Inc 2010-03-05 2016-10-19 Canada Accel-amlodipine Tablet 10 mg Oral Accel Pharma Inc 2010-03-05 2016-10-19 Canada Accel-amlodipine Tablet 2.5 mg Oral Accel Pharma Inc Not applicable Not applicable Canada Ach-amlodipine Tablet 2.5 mg Oral Accord Healthcare Inc 2018-11-05 Not applicable Canada Ach-amlodipine Tablet 10 mg Oral Accord Healthcare Inc 2018-11-05 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ALAMUT Amlodipine (10 MG) + Ramipril (10 MG) Capsule Oral So.Se.Pharm S.R.L. Societa' Di Servizio Per L'industria Farmaceutica Ed Affini 2016-01-12 Not applicable Italy ALAMUT Amlodipine (5 MG) + Ramipril (10 MG) Capsule Oral So.Se.Pharm S.R.L. Societa' Di Servizio Per L'industria Farmaceutica Ed Affini 2016-01-12 Not applicable Italy ALAMUT Amlodipine (5 MG) + Ramipril (2.5 MG) Capsule Oral So.Se.Pharm S.R.L. Societa' Di Servizio Per L'industria Farmaceutica Ed Affini 2016-01-12 Not applicable Italy ALAMUT Amlodipine (10 MG) + Ramipril (5 MG) Capsule Oral So.Se.Pharm S.R.L. Societa' Di Servizio Per L'industria Farmaceutica Ed Affini 2016-01-12 Not applicable Italy ALAMUT Amlodipine (5 MG) + Ramipril (5 MG) Capsule Oral So.Se.Pharm S.R.L. Societa' Di Servizio Per L'industria Farmaceutica Ed Affini 2016-01-12 Not applicable Italy - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Hypertenipine Amlodipine besylate (2.5 mg/1) + Arginine (90 mg/1) Kit Oral Physician Therapeutics Llc 2011-07-07 Not applicable US
Categories
- ATC Codes
- C09BB13 — Benazepril and amlodipine
- C09BB — ACE inhibitors and calcium channel blockers
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09BB — ACE inhibitors and calcium channel blockers
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C07FB — Beta blocking agents and calcium channel blockers
- C07F — BETA BLOCKING AGENTS, OTHER COMBINATIONS
- C07 — BETA BLOCKING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09XA — Renin-inhibitors
- C09X — OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09BX — ACE inhibitors, other combinations
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09DX — Angiotensin II receptor blockers (ARBs), other combinations
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09BX — ACE inhibitors, other combinations
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DX — Angiotensin II receptor blockers (ARBs), other combinations
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09XA — Renin-inhibitors
- C09X — OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09BB — ACE inhibitors and calcium channel blockers
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C07FB — Beta blocking agents and calcium channel blockers
- C07F — BETA BLOCKING AGENTS, OTHER COMBINATIONS
- C07 — BETA BLOCKING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C07FB — Beta blocking agents and calcium channel blockers
- C07F — BETA BLOCKING AGENTS, OTHER COMBINATIONS
- C07 — BETA BLOCKING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09DX — Angiotensin II receptor blockers (ARBs), other combinations
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C08CA — Dihydropyridine derivatives
- C08C — SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- C09BX — ACE inhibitors, other combinations
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C09DX — Angiotensin II receptor blockers (ARBs), other combinations
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C08GA — Calcium channel blockers and diuretics
- C08G — CALCIUM CHANNEL BLOCKERS AND DIURETICS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- C08CA — Dihydropyridine derivatives
- C08C — SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
- C08 — CALCIUM CHANNEL BLOCKERS
- C — CARDIOVASCULAR SYSTEM
- C09DB — Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- C09D — ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- C10BX — Lipid modifying agents in combination with other drugs
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C09BB — ACE inhibitors and calcium channel blockers
- C09B — ACE INHIBITORS, COMBINATIONS
- C09 — AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- ACE Inhibitors and Calcium Channel Blockers
- Agents causing hyperkalemia
- Angiotensin II Antagonists and Calcium Channel Blockers
- Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- Antianginal Agents
- Antiarrhythmic agents
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Bradycardia-Causing Agents
- Calcium Channel Blockers
- Calcium Channel Blockers (Dihydropyridine)
- Calcium Channel Blockers and Diuretics
- Calcium-Regulating Hormones and Agents
- Cardiovascular Agents
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (moderate)
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (weak)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dihydropyridine Derivatives
- Dihydropyridines
- Hypotensive Agents
- Membrane Transport Modulators
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Pyridines
- Selective Calcium Channel Blockers With Mainly Vascular Effects
- Vasodilating Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridines and derivatives
- Sub Class
- Hydropyridines
- Direct Parent
- Dihydropyridinecarboxylic acids and derivatives
- Alternative Parents
- Chlorobenzenes / Aryl chlorides / Dicarboxylic acids and derivatives / Vinylogous amides / Methyl esters / Enoate esters / Amino acids and derivatives / Azacyclic compounds / Dialkyl ethers / Dialkylamines show 7 more
- Substituents
- Alpha,beta-unsaturated carboxylic ester / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxylic acid derivative show 25 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- ethyl ester, primary amino compound, methyl ester, monochlorobenzenes, dihydropyridine (CHEBI:2668)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1J444QC288
- CAS number
- 88150-42-9
- InChI Key
- HTIQEAQVCYTUBX-UHFFFAOYSA-N
- InChI
- InChI=1S/C20H25ClN2O5/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21/h5-8,17,23H,4,9-11,22H2,1-3H3
- IUPAC Name
- 3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
- SMILES
- CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC
References
- Synthesis Reference
- US4572909
- General References
- Nayler WG, Gu XH: The unique binding properties of amlodipine: a long-acting calcium antagonist. J Hum Hypertens. 1991 Aug;5 Suppl 1:55-9. [Article]
- van Zwieten PA: Amlodipine: an overview of its pharmacodynamic and pharmacokinetic properties. Clin Cardiol. 1994 Sep;17(9 Suppl 3):III3-6. [Article]
- Fares H, DiNicolantonio JJ, O'Keefe JH, Lavie CJ: Amlodipine in hypertension: a first-line agent with efficacy for improving blood pressure and patient outcomes. Open Heart. 2016 Sep 28;3(2):e000473. doi: 10.1136/openhrt-2016-000473. eCollection 2016. [Article]
- Flynn JT, Nahata MC, Mahan JD Jr, Portman RJ: Population pharmacokinetics of amlodipine in hypertensive children and adolescents. J Clin Pharmacol. 2006 Aug;46(8):905-16. doi: 10.1177/0091270006289844. [Article]
- Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003. [Article]
- Faulkner JK, McGibney D, Chasseaud LF, Perry JL, Taylor IW: The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol. 1986 Jul;22(1):21-5. [Article]
- FDA Approved Drug Products: Amlodipine Oral Tablets [Link]
- FDA Approved Drug Products: Amlodipine Oral Suspension [Link]
- Apo amlodipine tablets, MedSafe NZ [File]
- External Links
- Human Metabolome Database
- HMDB0005018
- KEGG Drug
- D07450
- KEGG Compound
- C06825
- PubChem Compound
- 2162
- PubChem Substance
- 46507214
- ChemSpider
- 2077
- BindingDB
- 50088383
- 17767
- ChEBI
- 2668
- ChEMBL
- CHEMBL1491
- Therapeutic Targets Database
- DAP000139
- PharmGKB
- PA448388
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Amlodipine
- FDA label
- Download (270 KB)
- MSDS
- Download (74.5 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Disability Free Survival / Elderly / Healthy Subjects (HS) / Independent Living 1 4 Completed Not Available Hypertension 1 4 Completed Basic Science Genetics Hypertension / Hypertension 1 4 Completed Basic Science Syndrome, Metabolic 1 4 Completed Diagnostic Hypertension / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Synthon pharmaceuticals inc
- Actavis totowa llc
- Alkem laboratories ltd
- Amneal pharmaceuticals ny llc
- Apotex inc
- Aurobindo pharma ltd
- Caraco pharmaceutical laboratories ltd
- Dr reddys laboratories ltd
- Gedeon richter usa inc
- Genpharm inc
- Glenmark generics ltd
- Invagen pharmaceuticals inc
- Lek pharmaceuticals dd
- Lupin ltd
- Matrix laboratories ltd
- Mutual pharmacal co
- Mylan laboratories inc
- Orchid healthcare
- Ranbaxy laboratories ltd
- Roxane laboratories inc
- Teva pharmaceuticals usa inc
- Torrent pharmaceuticals ltd
- Upsher smith laboratories inc
- Vintage pharmaceuticals llc
- Watson laboratories inc
- Wockhardt ltd
- World gen llc
- Zydus pharmaceuticals usa inc
- Pfizer inc
- Dr reddys laboratories inc
- Packagers
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Amneal Pharmaceuticals
- Apotex Inc.
- AQ Pharmaceuticals Inc.
- Arrow Pharm Malta Ltd.
- A-S Medication Solutions LLC
- Aurobindo Pharma Ltd.
- Beijing Second Pharmaceutical Co. Ltd.
- Blu Pharmaceuticals LLC
- Breckenridge Pharmaceuticals
- Bryant Ranch Prepack
- Cadila Healthcare Ltd.
- Camber Pharmaceuticals Inc.
- Caraco Pharmaceutical Labs
- Cardinal Health
- Chemical Works Of Gedeon Richter Ltd.
- Cobalt Pharmaceuticals Inc.
- Comprehensive Consultant Services Inc.
- Corepharma LLC
- Coupler Enterprises Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Direct Pharmaceuticals Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Glenmark Generics Ltd.
- Greenstone LLC
- H.E. Butt Grocery Co.
- Heartland Repack Services LLC
- InvaGen Pharmaceuticals Inc.
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Letco Medical Inc.
- Lupin Pharmaceuticals Inc.
- Major Pharmaceuticals
- Medisca Inc.
- Medvantx Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Norwich Pharmaceuticals Inc.
- Novartis AG
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pfizer Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Promius Pharma
- Qualitest
- Rebel Distributors Corp.
- Redpharm Drug
- Remedy Repack
- Roxane Labs
- Sandhills Packaging Inc.
- Secan Pharmaceuticals Inc.
- Solco Healthcare US LLC
- Southwood Pharmaceuticals
- Stat Rx Usa
- Stat Scripts LLC
- Synthon Pharmaceuticals Inc.
- Teva Pharmaceutical Industries Ltd.
- Torrent Pharmaceuticals
- Tya Pharmaceuticals
- UDL Laboratories
- US Pharmaceutical Group
- USL Pharma Inc.
- Va Cmop Dallas
- Vangard Labs Inc.
- Warner Lambert Company LLC
- Wockhardt Ltd.
- Zydus Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet, coated Oral 5 mg Tablet Oral 6.940 mg Tablet Oral 5. mg Tablet Oral 500000 mg Tablet Oral 5.000 mg Capsule Oral Tablet Oral 7.5 MG Tablet Oral Tablet Oral 13.87 MG Tablet Oral 13.9 MG Tablet Oral 13868 MG Tablet Oral 14 MG Tablet Oral 6.943 mg Tablet Oral 6.95 MG Tablet Oral 6934 MG Tablet Oral 7 MG Tablet Oral 10 mg/1 Tablet Oral 2.5 mg/1 Tablet Oral 5 mg/1 Tablet, coated Oral 10 mg Tablet, film coated Oral 2.5 mg Tablet, film coated Oral 5 mg Capsule, liquid filled Oral 10 mg Capsule, liquid filled Oral 5 mg Tablet Oral 13.88 mg Tablet, effervescent 1.25 mg Tablet, effervescent 2.5 mg Tablet, effervescent 5 mg Tablet Tablet Oral 10.0 mg Tablet Oral 5.0 mg Tablet, film coated Oral 10 MG Capsule, coated Oral Tablet, coated Oral 2.5 mg Tablet, coated Oral 250000 mg Tablet Oral 10.00 mg Tablet Oral 5.00 mg Tablet Oral 12.500 mg Tablet, film coated Oral Tablet Oral Tablet, film coated Oral 6.93 mg Tablet Oral 6.9350 mg Tablet Oral 10 mg Tablet Oral 5 mg Tablet, coated Oral Tablet, film coated Oral 5 MG/160MG Tablet Oral 150.000 mg Capsule, gelatin coated Oral Tablet Oral 5 MG Tablet Oral 2.500 mg Tablet, film coated Oral 10.00 mg Tablet, film coated Oral 5.00 mg Tablet, effervescent 10 mg Tablet, effervescent Tablet Oral 6.93 MG Kit Oral Tablet Oral 160.000 mg Suspension Oral 1 mg/1mL Tablet, effervescent Oral Tablet Oral 40.000 mg Tablet, delayed release Oral Tablet, multilayer, extended release Oral Capsule Oral 5.000 mg Capsule Oral 5.000 mg Tablet, coated Solution Oral 1 mg/1mL Tablet Oral 1000000 mg Tablet, soluble Oral 5 mg Tablet, orally disintegrating Oral 10 mg Tablet, orally disintegrating Oral 5 mg Solution Oral 1 mg / mL Tablet Oral 6.930 mg Tablet Oral 6.900 mg Tablet Oral 10 MG Tablet, film coated Oral 5 mg Tablet, film coated Oral 10 mg Tablet, multilayer Oral Tablet, coated Oral 5 mg Capsule, liquid filled Oral Tablet Oral 2.5 mg - Prices
Unit description Cost Unit Amlodipine besylate powder 9.99USD g Lotrel 10-40 mg capsule 5.21USD capsule Lotrel 10-20 mg capsule 4.8USD capsule Lotrel 5-40 mg capsule 4.37USD capsule Lotrel 5-20 mg capsule 4.13USD capsule Lotrel 5-10 mg capsule 3.91USD capsule Lotrel 2.5-10 mg capsule 3.83USD capsule Norvasc 10 mg tablet 3.16USD tablet Amlodipine besylate 10 mg tablet 2.42USD tablet Norvasc 2.5 mg tablet 2.36USD tablet Norvasc 5 mg tablet 2.36USD tablet Norvasc 10 mg Tablet 2.14USD tablet Amlodipine besylate 2.5 mg tablet 1.76USD tablet Amlodipine besylate 5 mg tablet 1.76USD tablet Norvasc 5 mg Tablet 1.44USD tablet Amlodipine 10 mg Tablet 1.03USD tablet Apo-Amlodipine 10 mg Tablet 1.03USD tablet Co Amlodipine 10 mg Tablet 1.03USD tablet Gd-Amlodipine 10 mg Tablet 1.03USD tablet Jamp-Amlodipine 10 mg Tablet 1.03USD tablet Mylan-Amlodipine 10 mg Tablet 1.03USD tablet Novo-Amlodipine 10 mg Tablet 1.03USD tablet Phl-Amlodipine 10 mg Tablet 1.03USD tablet Pms-Amlodipine 10 mg Tablet 1.03USD tablet Ran-Amlodipine 10 mg Tablet 1.03USD tablet Ratio-Amlodipine 10 mg Tablet 1.03USD tablet Sandoz Amlodipine 10 mg Tablet 1.03USD tablet Amlodipine 5 mg Tablet 0.7USD tablet Apo-Amlodipine 5 mg Tablet 0.7USD tablet Co Amlodipine 5 mg Tablet 0.7USD tablet Gd-Amlodipine 5 mg Tablet 0.7USD tablet Jamp-Amlodipine 5 mg Tablet 0.7USD tablet Mylan-Amlodipine 5 mg Tablet 0.7USD tablet Novo-Amlodipine 5 mg Tablet 0.7USD tablet Phl-Amlodipine 5 mg Tablet 0.7USD tablet Pms-Amlodipine 5 mg Tablet 0.7USD tablet Ran-Amlodipine 5 mg Tablet 0.7USD tablet Ratio-Amlodipine 5 mg Tablet 0.7USD tablet Sandoz Amlodipine 5 mg Tablet 0.7USD tablet Phl-Amlodipine 2.5 mg Tablet 0.35USD tablet Pms-Amlodipine 2.5 mg Tablet 0.35USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2170278 No 1999-08-03 2014-08-10 Canada US6162802 No 2000-12-19 2017-12-19 US US5969156 Yes 1999-10-19 2017-01-08 US US6294197 Yes 2001-09-25 2017-12-18 US US5559111 Yes 1996-09-24 2019-01-21 US US6395728 No 2002-05-28 2019-07-08 US US6828339 No 2004-12-07 2022-11-20 US US5616599 Yes 1997-04-01 2016-10-25 US US6455574 No 2002-09-24 2018-08-11 US US8101599 No 2012-01-24 2023-05-16 US US8475839 Yes 2013-07-02 2023-11-16 US US8613949 No 2013-12-24 2029-12-21 US US8618174 No 2013-12-31 2021-11-15 US US8183295 No 2012-05-22 2023-05-16 US US7846961 No 2010-12-07 2029-10-05 US US6696481 No 2004-02-24 2023-04-15 US US9662315 No 2017-05-30 2030-02-28 US US10350171 No 2019-07-16 2038-06-14 US US10695329 No 2020-06-30 2037-10-16 US US9408837 No 2016-08-09 2030-02-28 US US10799453 No 2020-10-13 2039-04-11 US US10894039 No 2021-01-19 2037-10-06 US US10925835 No 2021-02-23 2038-06-14 US US10952998 No 2021-03-23 2037-10-06 US US10945960 No 2021-03-16 2038-06-14 US US10959991 No 2021-03-30 2037-10-06 US US11253474 No 2021-02-24 2041-02-24 US US11364230 No 2017-10-06 2037-10-06 US US11458095 No 2021-02-24 2041-02-24 US US11471409 No 2017-10-06 2037-10-06 US US11484498 No 2017-10-06 2037-10-06 US US11701326 No 2017-10-06 2037-10-06 US US11723866 No 2021-02-24 2041-02-24 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 199-201 https://www.chemicalbook.com/ChemicalProductProperty_US_CB4127875.aspx boiling point (°C) 527.2 https://www.lookchem.com/Amlodipine-besylate/ water solubility slightly soluble in water FDA label logP 3.00 AUSTIN,RP ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.0074 mg/mL ALOGPS logP 2.22 ALOGPS logP 1.64 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 19.12 Chemaxon pKa (Strongest Basic) 9.45 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 99.88 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 108.64 m3·mol-1 Chemaxon Polarizability 42.31 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9479 Blood Brain Barrier - 0.7744 Caco-2 permeable - 0.5468 P-glycoprotein substrate Substrate 0.9102 P-glycoprotein inhibitor I Inhibitor 0.8564 P-glycoprotein inhibitor II Non-inhibitor 0.8473 Renal organic cation transporter Non-inhibitor 0.803 CYP450 2C9 substrate Non-substrate 0.8627 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6967 CYP450 1A2 substrate Inhibitor 0.538 CYP450 2C9 inhibitor Inhibitor 0.514 CYP450 2D6 inhibitor Non-inhibitor 0.7626 CYP450 2C19 inhibitor Inhibitor 0.5871 CYP450 3A4 inhibitor Inhibitor 0.8608 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6642 Ames test Non AMES toxic 0.7605 Carcinogenicity Non-carcinogens 0.8568 Biodegradation Not ready biodegradable 0.9791 Rat acute toxicity 2.5396 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8302 hERG inhibition (predictor II) Inhibitor 0.8411
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 200.975386 predictedDarkChem Lite v0.1.0 [M-H]- 200.21031 predictedDeepCCS 1.0 (2019) [M+H]+ 200.231886 predictedDarkChem Lite v0.1.0 [M+H]+ 202.75047 predictedDeepCCS 1.0 (2019) [M+Na]+ 200.592686 predictedDarkChem Lite v0.1.0 [M+Na]+ 210.77263 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1C
- Uniprot ID
- Q13936
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1C
- Molecular Weight
- 248974.1 Da
References
- Bodi I, Mikala G, Koch SE, Akhter SA, Schwartz A: The L-type calcium channel in the heart: the beat goes on. J Clin Invest. 2005 Dec;115(12):3306-17. doi: 10.1172/JCI27167. [Article]
- Tang L, Gamal El-Din TM, Swanson TM, Pryde DC, Scheuer T, Zheng N, Catterall WA: Structural basis for inhibition of a voltage-gated Ca(2+) channel by Ca(2+) antagonist drugs. Nature. 2016 Sep 1;537(7618):117-121. doi: 10.1038/nature19102. Epub 2016 Aug 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1I
- Uniprot ID
- Q9P0X4
- Uniprot Name
- Voltage-dependent T-type calcium channel subunit alpha-1I
- Molecular Weight
- 245100.8 Da
References
- Lin M, Aladejebi O, Hockerman GH: Distinct properties of amlodipine and nicardipine block of the voltage-dependent Ca2+ channels Cav1.2 and Cav2.1 and the mutant channels Cav1.2/dihydropyridine insensitive and Cav2.1/dihydropyridine sensitive. Eur J Pharmacol. 2011 Nov 16;670(1):105-13. doi: 10.1016/j.ejphar.2011.08.005. Epub 2011 Sep 2. [Article]
- Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
- Inoue Y, Hisatome I, Tsuboi M, Ahmmed GU, Yatsuhashi T, Uchida K, Yamanouchi Y, Santo Y, Miake J, Tanaka Y, Hamada T, Watanabe M, Igawa O, Yoshida A, Shigemasa C, Makita N, Sato R: Effects of amlodipine on native cardiac Na+ channels and cloned alpha-subunits of cardiac Na+ channels. Arzneimittelforschung. 1999 May;49(5):394-7. doi: 10.1055/s-0031-1300433. [Article]
- Ozawa Y, Hayashi K, Kobori H: New Generation Calcium Channel Blockers in Hypertensive Treatment. Curr Hypertens Rev. 2006 May 1;2(2):103-111. doi: 10.2174/157340206776877370. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1B
- Uniprot ID
- Q00975
- Uniprot Name
- Voltage-dependent N-type calcium channel subunit alpha-1B
- Molecular Weight
- 262493.84 Da
References
- Furukawa T, Nukada T, Suzuki K, Fujita Y, Mori Y, Nishimura M, Yamanaka M: Voltage and pH dependent block of cloned N-type Ca2+ channels by amlodipine. Br J Pharmacol. 1997 Jul;121(6):1136-40. [Article]
- Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. [Article]
- Miyashita Y, Furukawa T, Kamegaya E, Yoshii M, Nukada T: A region of N-type Ca(2+) channel critical for blockade by the dihydropyridine amlodipine. Eur J Pharmacol. 2010 Apr 25;632(1-3):14-22. doi: 10.1016/j.ejphar.2010.01.006. Epub 2010 Jan 22. [Article]
- Murakami M, Nakagawasai O, Fujii S, Kameyama K, Murakami S, Hozumi S, Esashi A, Taniguchi R, Yanagisawa T, Tan-no K, Tadano T, Kitamura K, Kisara K: Antinociceptive action of amlodipine blocking N-type Ca2+ channels at the primary afferent neurons in mice. Eur J Pharmacol. 2001 May 11;419(2-3):175-81. [Article]
- Ogihara T, Kano T, Kakinuma C: Evaluation of the inhibitory effect of dihydropyridines on N-type calcium channel by virtual three-dimensional pharmacophore modeling. Arzneimittelforschung. 2009;59(6):283-8. doi: 10.1055/s-0031-1296398. [Article]
- Qu YL, Sugiyama K, Ohnuki T, Hattori K, Watanabe K, Nagatomo T: Comparison of binding affinities of omega-conotoxin and amlodipine to N-type Ca2+ channels in rat brain. Zhongguo Yao Li Xue Bao. 1998 Mar;19(2):97-100. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
- Gene Name
- CACNB1
- Uniprot ID
- Q02641
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit beta-1
- Molecular Weight
- 65712.995 Da
References
- Furukawa T, Nukada T, Suzuki K, Fujita Y, Mori Y, Nishimura M, Yamanaka M: Voltage and pH dependent block of cloned N-type Ca2+ channels by amlodipine. Br J Pharmacol. 1997 Jul;121(6):1136-40. [Article]
- Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. [Article]
- Miyashita Y, Furukawa T, Kamegaya E, Yoshii M, Nukada T: A region of N-type Ca(2+) channel critical for blockade by the dihydropyridine amlodipine. Eur J Pharmacol. 2010 Apr 25;632(1-3):14-22. doi: 10.1016/j.ejphar.2010.01.006. Epub 2010 Jan 22. [Article]
- Murakami M, Nakagawasai O, Fujii S, Kameyama K, Murakami S, Hozumi S, Esashi A, Taniguchi R, Yanagisawa T, Tan-no K, Tadano T, Kitamura K, Kisara K: Antinociceptive action of amlodipine blocking N-type Ca2+ channels at the primary afferent neurons in mice. Eur J Pharmacol. 2001 May 11;419(2-3):175-81. [Article]
- Ogihara T, Kano T, Kakinuma C: Evaluation of the inhibitory effect of dihydropyridines on N-type calcium channel by virtual three-dimensional pharmacophore modeling. Arzneimittelforschung. 2009;59(6):283-8. doi: 10.1055/s-0031-1296398. [Article]
- Qu YL, Sugiyama K, Ohnuki T, Hattori K, Watanabe K, Nagatomo T: Comparison of binding affinities of omega-conotoxin and amlodipine to N-type Ca2+ channels in rat brain. Zhongguo Yao Li Xue Bao. 1998 Mar;19(2):97-100. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated ion channel activity
- Specific Function
- The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Acts as a regulatory subunit for P/Q-t...
- Gene Name
- CACNA2D3
- Uniprot ID
- Q8IZS8
- Uniprot Name
- Voltage-dependent calcium channel subunit alpha-2/delta-3
- Molecular Weight
- 123010.22 Da
References
- Furukawa T, Nukada T, Suzuki K, Fujita Y, Mori Y, Nishimura M, Yamanaka M: Voltage and pH dependent block of cloned N-type Ca2+ channels by amlodipine. Br J Pharmacol. 1997 Jul;121(6):1136-40. [Article]
- Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. [Article]
- Miyashita Y, Furukawa T, Kamegaya E, Yoshii M, Nukada T: A region of N-type Ca(2+) channel critical for blockade by the dihydropyridine amlodipine. Eur J Pharmacol. 2010 Apr 25;632(1-3):14-22. doi: 10.1016/j.ejphar.2010.01.006. Epub 2010 Jan 22. [Article]
- Murakami M, Nakagawasai O, Fujii S, Kameyama K, Murakami S, Hozumi S, Esashi A, Taniguchi R, Yanagisawa T, Tan-no K, Tadano T, Kitamura K, Kisara K: Antinociceptive action of amlodipine blocking N-type Ca2+ channels at the primary afferent neurons in mice. Eur J Pharmacol. 2001 May 11;419(2-3):175-81. [Article]
- Ogihara T, Kano T, Kakinuma C: Evaluation of the inhibitory effect of dihydropyridines on N-type calcium channel by virtual three-dimensional pharmacophore modeling. Arzneimittelforschung. 2009;59(6):283-8. doi: 10.1055/s-0031-1296398. [Article]
- Qu YL, Sugiyama K, Ohnuki T, Hattori K, Watanabe K, Nagatomo T: Comparison of binding affinities of omega-conotoxin and amlodipine to N-type Ca2+ channels in rat brain. Zhongguo Yao Li Xue Bao. 1998 Mar;19(2):97-100. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea.
- Gene Name
- CA1
- Uniprot ID
- P00915
- Uniprot Name
- Carbonic anhydrase 1
- Molecular Weight
- 28870.0 Da
References
- Puscas I, Gilau L, Coltau M, Pasca R, Domuta G, Baican M, Hecht A: Hypotensive effect of calcium channel blockers is parallel with carbonic anhydrase I inhibition. Clin Pharmacol Ther. 2000 Oct;68(4):443-9. [Article]
- Puscas L, Gilau L, Coltau M, Pasca R, Domuta G, Baican M, Hecht A: Calcium channel blockers reduce blood pressure in part by inhibiting vascular smooth muscle carbonic anhydrase I. Cardiovasc Drugs Ther. 2000 Oct;14(5):523-8. [Article]
- Puscas I, Coltau M, Baican M, Pasca R, Domuta G, Hecht A: Vasoconstrictive drugs increase carbonic anhydrase I in vascular smooth muscle while vasodilating drugs reduce the activity of this isozyme by a direct mechanism of action. Drugs Exp Clin Res. 2001;27(2):53-60. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sphingomyelin phosphodiesterase activity
- Specific Function
- Converts sphingomyelin to ceramide. Also has phospholipase C activities toward 1,2-diacylglycerolphosphocholine and 1,2-diacylglycerolphosphoglycerol. Isoform 2 and isoform 3 have lost catalytic ac...
- Gene Name
- SMPD1
- Uniprot ID
- P17405
- Uniprot Name
- Sphingomyelin phosphodiesterase
- Molecular Weight
- 69751.3 Da
References
- Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Muhle C, Terfloth L, Groemer TW, Spitzer GM, Liedl KR, Gulbins E, Tripal P: Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One. 2011;6(8):e23852. doi: 10.1371/journal.pone.0023852. Epub 2011 Aug 31. [Article]
- Identification of New Functional Inhibitors of Acid Sphingomyelinase Using a Structure-Property-Activity Relation Model [File]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1B gives rise to N-type calcium currents.
- Specific Function
- Voltage-gated calcium channel activity
Components:
Name | UniProt ID |
---|---|
Voltage-dependent N-type calcium channel subunit alpha | A0A024R8I1 |
Voltage-dependent N-type calcium channel subunit alpha-1B | Q00975 |
References
- Miyashita Y, Furukawa T, Kamegaya E, Yoshii M, Nukada T: A region of N-type Ca(2+) channel critical for blockade by the dihydropyridine amlodipine. Eur J Pharmacol. 2010 Apr 25;632(1-3):14-22. doi: 10.1016/j.ejphar.2010.01.006. Epub 2010 Jan 22. [Article]
- Godfraind T: Discovery and Development of Calcium Channel Blockers. Front Pharmacol. 2017 May 29;8:286. doi: 10.3389/fphar.2017.00286. eCollection 2017. [Article]
- Furukawa T, Nukada T, Suzuki K, Fujita Y, Mori Y, Nishimura M, Yamanaka M: Voltage and pH dependent block of cloned N-type Ca2+ channels by amlodipine. Br J Pharmacol. 1997 Jul;121(6):1136-40. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [Article]
- Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
- Flockhart Table of Drug Interactions [Link]
- Amlodipine FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Limited in vitro data support this enzyme action.
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Data supporting this enzyme action are limited to in vitro studies in addition studies performed with rabbits.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Katoh M, Nakajima M, Shimada N, Yamazaki H, Yokoi T: Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52. [Article]
- Shah MB, Wilderman PR, Pascual J, Zhang Q, Stout CD, Halpert JR: Conformational adaptation of human cytochrome P450 2B6 and rabbit cytochrome P450 2B4 revealed upon binding multiple amlodipine molecules. Biochemistry. 2012 Sep 18;51(37):7225-38. doi: 10.1021/bi300894z. Epub 2012 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- There are contradictory data available on this enzyme action. Some studies suggest this drug is a CYP3A5 substrate, while others suggest it does not have a role in amlodipine metabolism.
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
- Bhatnagar V, Garcia EP, O'Connor DT, Brophy VH, Alcaraz J, Richard E, Bakris GL, Middleton JP, Norris KC, Wright J, Hiremath L, Contreras G, Appel LJ, Lipkowitz MS: CYP3A4 and CYP3A5 polymorphisms and blood pressure response to amlodipine among African-American men and women with early hypertensive renal disease. Am J Nephrol. 2010;31(2):95-103. doi: 10.1159/000258688. Epub 2009 Nov 12. [Article]
- Lu Y, Zhong H, Tang Q, Huang Z, Jing N, Smith J, Miao R, Li Y, Yuan H: Construction and verification of CYP3A5 gene polymorphisms using a Saccharomyces cerevisiae expression system to predict drug metabolism. Mol Med Rep. 2017 Apr;15(4):1593-1600. doi: 10.3892/mmr.2017.6214. Epub 2017 Feb 17. [Article]
- Zhang YP, Zuo XC, Huang ZJ, Cai JJ, Wen J, Duan DD, Yuan H: CYP3A5 polymorphism, amlodipine and hypertension. J Hum Hypertens. 2014 Mar;28(3):145-9. doi: 10.1038/jhh.2013.67. Epub 2013 Jul 18. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Floyd JS, Kaspera R, Marciante KD, Weiss NS, Heckbert SR, Lumley T, Wiggins KL, Tamraz B, Kwok PY, Totah RA, Psaty BM: A screening study of drug-drug interactions in cerivastatin users: an adverse effect of clopidogrel. Clin Pharmacol Ther. 2012 May;91(5):896-904. doi: 10.1038/clpt.2011.295. Epub 2012 Mar 14. [Article]
- Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Data of this enzyme action are limited and are based on results of in vitro studies.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Augustin M, Schoretsanitis G, Grunder G, Haen E, Paulzen M: How to Treat Hypertension in Venlafaxine-Medicated Patients-Pharmacokinetic Considerations in Prescribing Amlodipine and Ramipril. J Clin Psychopharmacol. 2018 Oct;38(5):498-501. doi: 10.1097/JCP.0000000000000929. [Article]
- Ma B, Prueksaritanont T, Lin JH: Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Krasulova K, Holas O, Anzenbacher P: Influence of Amlodipine Enantiomers on Human Microsomal Cytochromes P450: Stereoselective Time-Dependent Inhibition of CYP3A Enzyme Activity. Molecules. 2017 Nov 3;22(11):1879. doi: 10.3390/molecules22111879. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Krasulova K, Holas O, Anzenbacher P: Influence of Amlodipine Enantiomers on Human Microsomal Cytochromes P450: Stereoselective Time-Dependent Inhibition of CYP3A Enzyme Activity. Molecules. 2017 Nov 3;22(11):1879. doi: 10.3390/molecules22111879. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4. Pharm Res. 2000 Oct;17(10):1189-97. [Article]
- Darvari R, Boroujerdi M: Concentration dependency of modulatory effect of amlodipine on P-glycoprotein efflux activity of doxorubicin--a comparison with tamoxifen. J Pharm Pharmacol. 2004 Aug;56(8):985-91. doi: 10.1211/0022357043941. [Article]
- Kuzuya T, Kobayashi T, Moriyama N, Nagasaka T, Yokoyama I, Uchida K, Nakao A, Nabeshima T: Amlodipine, but not MDR1 polymorphisms, alters the pharmacokinetics of cyclosporine A in Japanese kidney transplant recipients. Transplantation. 2003 Sep 15;76(5):865-8. doi: 10.1097/01.TP.0000084873.20157.67. [Article]
- Kim KA, Park PW, Park JY: Effect of ABCB1 (MDR1) haplotypes derived from G2677T/C3435T on the pharmacokinetics of amlodipine in healthy subjects. Br J Clin Pharmacol. 2007 Jan;63(1):53-8. doi: 10.1111/j.1365-2125.2006.02733.x. Epub 2006 Jul 21. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55