U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C20H25ClN2O5.C6H6O3S
Molecular Weight 567.053
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMLODIPINE BESYLATE

SMILES

CCOC(=O)C1=C(COCCN)NC(=C(C1c2ccccc2Cl)C(=O)OC)C.c1ccc(cc1)S(=O)(=O)O

InChI

InChIKey=ZPBWCRDSRKPIDG-UHFFFAOYSA-N
InChI=1S/C20H25ClN2O5.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h5-8,17,23H,4,9-11,22H2,1-3H3;1-5H,(H,7,8,9)

HIDE SMILES / InChI

Molecular Formula C20H25ClN2O5
Molecular Weight 408.8766
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula C6H6O3S
Molecular Weight 158.1764
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular mooth muscle cells than on cardiac muscle cells. Amlodipine is indicated for the treatment of hypertension and coronary artery disease.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
NORVASC

Approved Use

Amlodipine besylate tablets USP 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 USP 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. •Coronary Artery Disease (1.2) о Chronic Stable Angina о Vasospastic Angina (Prinzmetal's or Variant Angina) о Angiographically Documented Coronary Artery Disease in patients without heart failure or an ejection fraction < 40% 1.1 Hypertension Amlodipine besylate tablets USP 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. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including amlodipine besylate. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program's Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy. Amlodipine besylate tablets USP may be used alone or in combination with other antihypertensive agents. 1.2 Coronary Artery Disease (CAD) Chronic Stable Angina Amlodipine besylate tablets USP are indicated for the symptomatic treatment of chronic stable angina. Amlodipine besylate tablets USP may be used alone or in combination with other antianginal agents. Vasospastic Angina (Prinzmetal's or Variant Angina) Amlodipine besylate tablets USP are indicated for the treatment of confirmed or suspected vasospastic angina. Amlodipine besylate tablets USP may be used as monotherapy or in combination with other antianginal agents. Angiographically Documented CAD In patients with recently documented CAD by angiography and without heart failure or an ejection fraction <40%, amlodipine besylate tablets USP are indicated to reduce the risk of hospitalization for angina and to reduce the risk of a coronary revascularization procedure.

Launch Date

7.1254082E11
Primary
NORVASC

Approved Use

Amlodipine besylate tablets USP 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 USP 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. •Coronary Artery Disease (1.2) о Chronic Stable Angina о Vasospastic Angina (Prinzmetal's or Variant Angina) о Angiographically Documented Coronary Artery Disease in patients without heart failure or an ejection fraction < 40% 1.1 Hypertension Amlodipine besylate tablets USP 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. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including amlodipine besylate. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program's Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy. Amlodipine besylate tablets USP may be used alone or in combination with other antihypertensive agents. 1.2 Coronary Artery Disease (CAD) Chronic Stable Angina Amlodipine besylate tablets USP are indicated for the symptomatic treatment of chronic stable angina. Amlodipine besylate tablets USP may be used alone or in combination with other antianginal agents. Vasospastic Angina (Prinzmetal's or Variant Angina) Amlodipine besylate tablets USP are indicated for the treatment of confirmed or suspected vasospastic angina. Amlodipine besylate tablets USP may be used as monotherapy or in combination with other antianginal agents. Angiographically Documented CAD In patients with recently documented CAD by angiography and without heart failure or an ejection fraction <40%, amlodipine besylate tablets USP are indicated to reduce the risk of hospitalization for angina and to reduce the risk of a coronary revascularization procedure.

Launch Date

7.1254082E11
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.3 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3 μg/L
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.9 μg/L
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10.4 μg/L
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3.5 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10.5 ng/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
114 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
187 μg × h/L
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
238 μg × h/L
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
464 μg × h/L
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
169 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
214 ng × h/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
48 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
36 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
37 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
41 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
47 h
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AMLODIPINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
AMLODIPINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
75 mg single, oral (mean)
Overdose
Dose: 75 mg
Route: oral
Route: single
Dose: 75 mg
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: Hypertension
Age Group: 42 years
Sex: F
Population Size: 1
Sources:
Disc. AE: Sinus tachycardia, Metabolic acidosis...
AEs leading to
discontinuation/dose reduction:
Sinus tachycardia (1 patient)
Metabolic acidosis (1 patient)
Hypocalcemia (1 patient)
Sources:
10 mg 1 times / day steady, oral (min)
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 1250
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 1250
Sources:
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (1.5%)
Sources:
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 268
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 268
Sources:
DLT: Edema, Dizziness...
Dose limiting toxicities:
Edema (10.8%)
Dizziness (3.4%)
Flushing (2.6%)
Palpitation (4.5%)
Sources:
2.5 mg 1 times / day steady, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy, adult
n = 275
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 275
Sources:
DLT: Edema, Dizziness...
Dose limiting toxicities:
Edema (1.8%)
Dizziness (1.1%)
Flushing (0.7%)
Palpitation (0.7%)
Sources:
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 296
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 296
Sources:
DLT: Edema, Dizziness...
Dose limiting toxicities:
Edema (3%)
Dizziness (3.4%)
Flushing (1.4%)
Palpitation (1.4%)
Sources:
5.6 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.6 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.6 mg, 1 times / day
Sources:
unhealthy, adult
n = 231
Health Status: unhealthy
Condition: Hypertension, Pregnancy
Age Group: adult
Sex: F
Population Size: 231
Sources:
Other AEs: Neonatal disorder NOS...
Other AEs:
Neonatal disorder NOS (11 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Hypocalcemia 1 patient
Disc. AE
75 mg single, oral (mean)
Overdose
Dose: 75 mg
Route: oral
Route: single
Dose: 75 mg
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: Hypertension
Age Group: 42 years
Sex: F
Population Size: 1
Sources:
Metabolic acidosis 1 patient
Disc. AE
75 mg single, oral (mean)
Overdose
Dose: 75 mg
Route: oral
Route: single
Dose: 75 mg
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: Hypertension
Age Group: 42 years
Sex: F
Population Size: 1
Sources:
Sinus tachycardia 1 patient
Disc. AE
75 mg single, oral (mean)
Overdose
Dose: 75 mg
Route: oral
Route: single
Dose: 75 mg
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: Hypertension
Age Group: 42 years
Sex: F
Population Size: 1
Sources:
Headache 1.5%
Disc. AE
10 mg 1 times / day steady, oral (min)
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 1250
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 1250
Sources:
Edema 10.8%
DLT
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 268
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 268
Sources:
Flushing 2.6%
DLT
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 268
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 268
Sources:
Dizziness 3.4%
DLT
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 268
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 268
Sources:
Palpitation 4.5%
DLT
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 268
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 268
Sources:
Flushing 0.7%
DLT
2.5 mg 1 times / day steady, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy, adult
n = 275
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 275
Sources:
Palpitation 0.7%
DLT
2.5 mg 1 times / day steady, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy, adult
n = 275
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 275
Sources:
Dizziness 1.1%
DLT
2.5 mg 1 times / day steady, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy, adult
n = 275
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 275
Sources:
Edema 1.8%
DLT
2.5 mg 1 times / day steady, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy, adult
n = 275
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 275
Sources:
Flushing 1.4%
DLT
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 296
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 296
Sources:
Palpitation 1.4%
DLT
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 296
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 296
Sources:
Edema 3%
DLT
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 296
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 296
Sources:
Dizziness 3.4%
DLT
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 296
Health Status: unhealthy
Condition: Hypertension
Age Group: adult
Sex: unknown
Population Size: 296
Sources:
Neonatal disorder NOS 11 patient
5.6 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.6 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.6 mg, 1 times / day
Sources:
unhealthy, adult
n = 231
Health Status: unhealthy
Condition: Hypertension, Pregnancy
Age Group: adult
Sex: F
Population Size: 231
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
moderate [IC50 11.3 uM]
no [IC50 >133 uM]
no [IC50 >133 uM]
no [IC50 >133 uM]
no [IC50 >133 uM]
no
strong [Ki 0.13 uM]
strong [Ki 1.95 uM]
strong
weak [IC50 57 uM]
weak
weak
weak
weak
yes (co-administration study)
Comment: A prospective study in renal transplant patients (N=11) showed on an average of 40% increase in trough cyclosporine levels when concomitantly treated with amlodipine.
Page: (Label 2) 24
yes [IC50 22 uM]
yes [Inhibition 2 uM]
yes
yes
yes
yes (co-administration study)
Comment: A prospective study in healthy Chinese volunteers (N=9) with CYP3A5 expressers showed a 2.5-to 4-fold increase in tacrolimus exposure when concomitantly administered with amlodipine.
Page: (Label 2) 24
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
likely
major
major
yes (co-administration study)
Comment: Co-administration of the moderate CYP3A inhibitor diltiazem increases the exposure to amlodipine 1.6-fold., Erythromycin co-administration in healthy volunteers did not significantly change amlodipine systemic exposure.
Page: (ClinPharm) 21, 26, (Label 2) 23
yes
yes (pharmacogenomic study)
Comment: Following administration of amlodipine, blood pressure in all patients decreased. The magnitude of the change in blood pressure varied among patients. Individuals with the CYP3A5*1/*3 polymorphism exhibited the highest change in blood pressure, followed by CYP3A5*4, CYP3A5*1/*1, and CYP3A5*6
yes
yes (pharmacogenomic study)
Comment: Amlodipine pharmacokinetics was affected by the genetic polymorphisms of the ABCB1 gene in humans.
Tox targets
PubMed

PubMed

TitleDatePubMed
A double-blind evaluation of the effect of amlodipine on ambulatory blood pressure.
1991
Low Dose Combination Therapy vs. High Dose Monotherapy in the Management of Hypertension.
1999 Nov
Role of nitric oxide in the control of cardiac oxygen consumption in B(2)-kinin receptor knockout mice.
1999 Oct
[Effects of calcium antagonists on atherosclerosis progression and intima media thickness].
2000
Amlodipine besylate induced acute interstitial nephritis.
2000 Aug
Motor and electrographic response of refractory experimental status epilepticus in rats and effect of calcium channel blockers.
2000 Feb
Restenosis and clinical outcome in patients treated with amlodipine after angioplasty: results from the Coronary AngioPlasty Amlodipine REStenosis Study (CAPARES).
2000 Mar 1
Differential effect of chronic inhibition of calcium channel and angiotensin II type 1-receptor on aldosterone synthesis in spontaneously hypertensive rats.
2000 Oct
[Extrapyramidal reactions after epidural droperidol].
2000 Oct
Haemodynamic and metabolic effects of rilmenidine in hypertensive patients with metabolic syndrome X. A double-blind parallel study versus amlodipine.
2000 Oct
Nephrotoxicity of high- and low-osmolar contrast media. The protective role of amlodipine in a rat model.
2000 Sep
Nebivolol vs amlodipine as first-line treatment of essential arterial hypertension in the elderly.
2002
Double-blind, placebo-controlled crossover comparison of five classes of antihypertensive drugs.
2002 Apr
Synergistic effect of nicorandil and amlodipine on mitochondrial function during isoproterenol-induced myocardial infarction in rats.
2002 Jan
Combination therapy of amlodipine/benazepril versus monotherapy of amlodipine in a practice-based setting.
2002 Jun
[Amlodipine-induced acute hepatitis].
2002 Jun-Jul
Arterial hypertension with brachydactyly in a 15-year-old boy.
2003 Aug
The effect of nonsteroidal anti-inflammatory drugs on blood pressure in patients treated with different antihypertensive drugs.
2003 Jan-Feb
VALUE trial: Long-term blood pressure trends in 13,449 patients with hypertension and high cardiovascular risk.
2003 Jul
Effects of the selective aldosterone blocker eplerenone versus the calcium antagonist amlodipine in systolic hypertension.
2003 May
Amlodipine reduces cyclosporin-induced hyperuricaemia in hypertensive renal transplant recipients.
2003 Oct
Synergistic effect of nicorandil and amlodipine on lysosomal hydrolases during experimental myocardial infarction in rats.
2003 Sep
Platelet morphology and plasma indices of platelet activation in essential hypertension: effects of amlodipine-based antihypertensive therapy.
2004
Amlodipine and carvedilol prevent cytotoxicity in cortical neurons isolated from stroke-prone spontaneously hypertensive rats.
2004 Apr
Acute renal failure and hepatotoxicity associated with roxithromycin.
2004 Apr
Comparison of antihypertensive effects of an angiotensin-converting enzyme inhibitor, a calcium antagonist and a diuretic in patients with hypertension not controlled by angiotensin receptor blocker monotherapy.
2005 Apr
Exercise-related syncope induced by vasodilator therapy in an elderly hypertensive patient.
2005 Feb
Clinic blood pressure responses to two amlodipine salt formulations, adipate and besylate, in adult Korean patients with mild to moderate hypertension: a multicenter, randomized, double-blind, parallel-group, 8-week comparison.
2005 Jun
Prediction of genotoxicity of chemical compounds by statistical learning methods.
2005 Jun
Effect of food on the bioavailability of amlodipine besylate/atorvastatin calcium combination tablet.
2006 Oct
Results of a comparative, phase III, 12-week, multicenter, prospective, randomized, double-blind assessment of the efficacy and tolerability of a fixed-dose combination of telmisartan and amlodipine versus amlodipine monotherapy in Indian adults with stage II hypertension.
2007 Dec
Improved attainment of blood pressure and cholesterol goals using single-pill amlodipine/atorvastatin in African Americans: the CAPABLE trial.
2008 Jan
Synergistic effect of amlodipine and atorvastatin on blood pressure, left ventricular remodeling, and C-reactive protein in hypertensive patients with primary hypercholesterolemia.
2008 Mar
Amlodipine improves endothelial function and metabolic parameters in patients with hypertension.
2009 Mar 20
Patents

Sample Use Guides

Adult recommended starting dose: 5 mg once daily with maximum dose 10 mg once daily. Small, fragile, or elderly patients, or patients with hepatic insufficiency may be started on 2.5 mg once daily. Pediatric starting dose: 2.5 mg to 5 mg once daily. Important Limitation: Doses in excess of 5 mg daily have not been studied.
Route of Administration: Oral
amlodipine was effective against A. castellanii and B. mandrillaris at 250μM
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:03:24 UTC 2021
Edited
by admin
on Fri Jun 25 21:03:24 UTC 2021
Record UNII
864V2Q084H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AMLODIPINE BESYLATE
EMA EPAR   HSDB   ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
IMPRIDA-HCT COMPONENT AMLODIPINE BESILATE
Brand Name English
IMPRIDA COMPONENT AMLODIPINE BESILATE
Brand Name English
3,5-PYRIDINEDICARBOXYLIC ACID, 2-((2-AMINOETHOXY)METHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-, 3-ETHYL 5-METHYL ESTER, (+/-)-, MONOBENZENESULPHONATE
Common Name English
NORVASC
Brand Name English
AMLODIPINE BESYLATE [ORANGE BOOK]
Common Name English
AMLODIPINE BENZENESULFONATE [MI]
Common Name English
AMLODIPINE BESYLATE [EMA EPAR VETERINARY]
Common Name English
AMLODIPINE BESYLATE COMPONENT OF ONDUARP
Brand Name English
AMLODIPINE BESILATE COMPONENT OF DAFIRO-HCT
Brand Name English
DAFIRO COMPONENT AMLODIPINE BESILATE
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF AMTURNIDE
Common Name English
EXFORGE HCT COMPONENT AMLODIPINE BESYLATE
Common Name English
AMLODIPINE BESYLATE [USP-RS]
Common Name English
AMLODIPINE BESYLATE [VANDF]
Common Name English
3-ETHYL 5-METHYL 2-(2-AMINOETHOXYMETHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYLPYRIDINE-3,5-DICARBOXYLATE MONOBENZENESULPHONATE
Systematic Name English
AMTURNIDE COMPONENT AMLODIPINE BESYLATE
Common Name English
AMLODIPINE BESYLATE COMPONENT OF TEKAMLO
Common Name English
AMLODIPINE (AS BESILATE)
Common Name English
3-ETHYL 5-METHYL (+/-)-2-((2-AMINOETHOXY)METHYL)-4-(O-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-3,5-PYRIDINEDICARBOXYLATE, MONOBENZENESULPHONATE
Common Name English
EXFORGE COMPONENT AMLODIPINE BESYLATE
Brand Name English
AMLODIPINE BESILATE
EP   JAN   MART.   WHO-DD  
Common Name English
LODIPRESSIN
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF AZOR
Common Name English
AMLODIPINE BESILATE COMPONENT OF EXFORGE
Brand Name English
CONSENSI COMPONENT AMLODIPINE BESYLATE
Brand Name English
AZOR COMPONENT AMLODIPINE BESYLATE
Common Name English
UK-48,340-26
Code English
TWYNSTA COMPONENT AMLODIPINE BESYLATE
Common Name English
AMLODIPINE BESYLATE COMPONENT OF TRIBENZOR
Brand Name English
AMLODIPINE BESILATE [MART.]
Common Name English
AMLESSA COMPONENT AMLODIPINE BESYLATE
Common Name English
ANTACAL
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF TWYNSTA
Common Name English
3-ETHYL 5-METHYL (+/-)-2-((2-AMINOETHOXY)METHYL)-4-(O-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-3,5-PYRIDINEDICARBOXYLATE, MONOBENZENESULFONATE
Common Name English
TEKAMLO COMPONENT AMLODIPINE BESYLATE
Common Name English
AMLODIPINE BESILATE COMPONENT OF EXFORGE-HCT
Brand Name English
3,5-PYRIDINEDICARBOXYLIC ACID, 2-((2-AMINOETHOXY)METHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-, 3-ETHYL 5-METHYL ESTER, (+/-)-, MONOBENZENESULFONATE
Common Name English
AMLODIPINE BESYLATE [USP MONOGRAPH]
Common Name English
EXFORGE COMPONENT AMLODIPINE BESILATE
Brand Name English
AMLODIPINE BESYLATE [USAN]
Common Name English
COPALIA COMPONENT AMLODIPINE BESYLATE
Brand Name English
EXFORGE-HCT COMPONENT AMLODIPINE BESILATE
Brand Name English
CADUET COMPONENT AMLODIPINE BESYLATE
Brand Name English
ONDUARP COMPONENT AMLODIPINE BESYLATE
Brand Name English
AMLODIPINE BESYLATE [EMA EPAR]
Common Name English
AMLODIPINE BESYLATE [USP]
Common Name English
AMLOR
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF CONSENSI
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF COPALIA
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF EXFORGE HCT
Common Name English
MONOPINA
Brand Name English
AMLODIPINE BESYLATE COMPONENT OF CADUET
Brand Name English
DAFIRO-HCT COMPONENT AMLODIPINE BESILATE
Brand Name English
TRIBENZOR COMPONENT AMLODIPINE BESYLATE
Brand Name English
AMLODIPINE BESILATE [JAN]
Common Name English
LOTREL COMPONENT AMLODIPINE BESYLATE
Common Name English
NSC-758922
Code English
AMLODIPINE BESYLATE COMPONENT OF LOTREL
Common Name English
AMLODIPINE BESYLATE COMPONENT OF EXFORGE
Brand Name English
AMLODIPINE BESILATE [EP MONOGRAPH]
Common Name English
AMLODIPINE BESILATE COMPONENT OF IMPRIDA-HCT
Brand Name English
AMLODIPINE BESILATE [WHO-DD]
Common Name English
AMLODIPINE BESYLATE [HSDB]
Common Name English
AMLODIPINE BESILATE COMPONENT OF DAFIRO
Brand Name English
UK-48340-26
Code English
ISTIN
Brand Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS DAFIRO (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS COPALIA (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS ONDUARP (WITHDRAWN: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS IMPRIDA (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
NCI_THESAURUS C333
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA VETERINARY ASSESSMENT REPORTS LODIPRESSIN [REFUSED]
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS EXFORGE-HCT (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS EXFORGE (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS TWYNSTA (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS DAFIRO-HCT (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS IMPRIDA-HCT (WITHDRAWN: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
EMA ASSESSMENT REPORTS COPALIA-HCT (AUTHORIZED: HYPERTENSION)
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C28820
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
USP_CATALOG
1029501
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY USP-RS
MERCK INDEX
M1757
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY Merck Index
PUBCHEM
60496
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
FDA UNII
864V2Q084H
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
ChEMBL
CHEMBL1491
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
RXCUI
104416
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY RxNorm
CAS
111470-99-6
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
DRUG BANK
DBSALT001054
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
EPA CompTox
111470-99-6
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
EVMPD
SUB12864MIG
Created by admin on Fri Jun 25 21:03:24 UTC 2021 , Edited by admin on Fri Jun 25 21:03:24 UTC 2021
PRIMARY
Related Record Type Details
ENANTIOMER -> RACEMATE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
USP
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
EP
PARENT -> SALT/SOLVATE
ENANTIOMER -> RACEMATE
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IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ACTIVE MOIETY