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

Details

Stereochemistry RACEMIC
Molecular Formula C20H25ClN2O5.C6H10O4
Molecular Weight 555.018
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMLODIPINE ADIPATE

SMILES

CCOC(=O)C1=C(COCCN)NC(=C(C1c2ccccc2Cl)C(=O)OC)C.C(CCC(=O)O)CC(=O)O

InChI

InChIKey=BGXVCBNVNUORTP-UHFFFAOYSA-N
InChI=1S/C20H25ClN2O5.C6H10O4/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;7-5(8)3-1-2-4-6(9)10/h5-8,17,23H,4,9-11,22H2,1-3H3;1-4H2,(H,7,8)(H,9,10)

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 C6H10O4
Molecular Weight 146.1414
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
The unique binding properties of amlodipine: a long-acting calcium antagonist.
1991 Aug
A randomized, placebo-controlled, double-blind comparison of amlodipine and atenolol in patients with essential hypertension.
1992 Oct
Effects of amlodipine on myocardial infarction, infarct expansion, and ventricular geometry in the rat.
1992 Sep
Effects of antihypertensive drugs on peritoneal vessels in hypertensive dogs with mild renal insufficiency.
2003
Arterial hypertension with brachydactyly in a 15-year-old boy.
2003 Aug
Biochemical changes on the cardioprotective effect of nicorandil and amlodipine during experimental myocardial infarction in rats.
2003 Dec
VALUE trial: Long-term blood pressure trends in 13,449 patients with hypertension and high cardiovascular risk.
2003 Jul
Effects of amlodipine on ischemia after percutaneous transluminal coronary angioplasty: secondary results of the Coronary Angioplasty Amlodipine Restenosis (CAPARES) Study.
2003 Jun
Effects of the selective aldosterone blocker eplerenone versus the calcium antagonist amlodipine in systolic hypertension.
2003 May
Heterogeneous effect of calcium antagonists on leg oedema: a comparison of amlodipine versus lercanidipine in hypertensive patients.
2003 Oct
Amlodipine reduces cyclosporin-induced hyperuricaemia in hypertensive renal transplant recipients.
2003 Oct
Better renoprotective effect of angiotensin II antagonist compared to dihydropyridine calcium channel blocker in childhood.
2003 Oct
Synergistic effect of nicorandil and amlodipine on lysosomal hydrolases during experimental myocardial infarction in rats.
2003 Sep
Comparative efficacy and safety of nisoldipine extended-release (ER) and amlodipine (CESNA-III study) in African American patients with hypertension.
2003 Sep
Antiproteinuric efficacy of losartan in comparison with amlodipine in non-diabetic proteinuric renal diseases: a double-blind, randomized clinical trial.
2003 Sep
Platelet morphology and plasma indices of platelet activation in essential hypertension: effects of amlodipine-based antihypertensive therapy.
2004
Irbesartan: a review of its use in hypertension and in the management of diabetic nephropathy.
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
Effect of slow-release indapamide and perindopril compared with amlodipine on 24-hour blood pressure and left ventricular mass in hypertensive patients of African ancestry.
2004 May
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
Prediction of genotoxicity of chemical compounds by statistical learning methods.
2005 Jun
Efficacy and tolerability of combination therapy with valsartan plus hydrochlorothiazide compared with amlodipine monotherapy in hypertensive patients with other cardiovascular risk factors: the VAST study.
2005 May
An economic evaluation of the 2003 European Society of Hypertension-European Society of Cardiology guidelines for the management of mild-to-moderate hypertension in Greece.
2005 Sep
Indapamide sustained release: a review of its use in the treatment of hypertension.
2006
Angiotensin-converting enzyme (ACE) inhibitor-associated angioedema of the stomach and small intestine: a case report.
2006 Dec
The effect of different antihypertensive drugs on cavernous tissue in experimental chronic renal insufficiency.
2006 Jul-Aug
Effect of stealthy liposomal topotecan plus amlodipine on the multidrug-resistant leukaemia cells in vitro and xenograft in mice.
2006 Jun
Pharmacoeconomic consequences of amlodipine besylate therapy in patients undergoing PTCA.
2006 Mar
Beneficial effects of combined benazepril-amlodipine on cardiac nitric oxide, cGMP, and TNF-alpha production after cardiac ischemia.
2006 May
A novel stealth liposomal topotecan with amlodipine: apoptotic effect is associated with deletion of intracellular Ca2+ by amlodipine thus leading to an enhanced antitumor activity in leukemia.
2006 May 15
Effect of food on the bioavailability of amlodipine besylate/atorvastatin calcium combination tablet.
2006 Oct
Incidence and predictors of angioedema in elderly hypertensive patients at high risk for cardiovascular disease: a report from the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT).
2006 Sep
Two multicenter, 8-week, randomized, double-blind, placebo-controlled, parallel-group studies evaluating the efficacy and tolerability of amlodipine and valsartan in combination and as monotherapy in adult patients with mild to moderate essential hypertension.
2007 Apr
G1 cell cycle arrest by amlodipine, a dihydropyridine Ca2+ channel blocker, in human epidermoid carcinoma A431 cells.
2007 Apr 1
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
Dysgeusia with amlodipine--a case report.
2007 Feb
Differential effects of dihydropyridine calcium antagonists on doxorubicin-induced nephrotoxicity in rats.
2007 Feb 28
Fibroblast apoptosis precedes cardiomyocyte mass reduction during left ventricular remodeling in hypertensive rats treated with amlodipine.
2007 Jun
Antihypertensive efficacy of amlodipine and losartan after two 'missed' doses in patients with mild to moderate essential hypertension.
2007 Nov-Dec
Antihypertensive efficacy of the oral direct renin inhibitor aliskiren as add-on therapy in patients not responding to amlodipine monotherapy.
2007 Oct
Comparison of monotherapy versus combination antihypertensive therapy in elderly patients with essential hypertension.
2008 Apr-May
Improved attainment of blood pressure and cholesterol goals using single-pill amlodipine/atorvastatin in African Americans: the CAPABLE trial.
2008 Jan
Vildagliptin, a novel dipeptidyl peptidase IV inhibitor, has no pharmacokinetic interactions with the antihypertensive agents amlodipine, valsartan, and ramipril in healthy subjects.
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
Effects of amlodipine, captopril, and bezafibrate on oxidative milieu in rats with fatty liver.
2008 Mar
Amlodipine inhibits cell proliferation via PKD1-related pathway.
2008 May 2
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 Sat Jun 26 15:44:55 UTC 2021
Edited
by admin
on Sat Jun 26 15:44:55 UTC 2021
Record UNII
3I0OF3W3E4
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AMLODIPINE ADIPATE
Common Name English
3,5-PYRIDINEDICARBOXYLIC ACID, 2-((2-AMINOETHOXY)METHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-, 3-ETHYL 5-METHYL ESTER, HEXANEDIOATE (1:1)
Systematic Name English
AMLODIPINE ADIPATE [WHO-DD]
Common Name English
CJ 11828
Code English
CJ-11828
Code English
3,5-PYRIDINEDICARBOXYLIC ACID, 2-((2-AMINOETHOXY)METHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-, 3-ETHYL 5-METHYL ESTER, COMPD. WITH HEXANEDIOIC ACID (1:1)
Systematic Name English
Code System Code Type Description
FDA UNII
3I0OF3W3E4
Created by admin on Sat Jun 26 15:44:56 UTC 2021 , Edited by admin on Sat Jun 26 15:44:56 UTC 2021
PRIMARY
PUBCHEM
9850652
Created by admin on Sat Jun 26 15:44:56 UTC 2021 , Edited by admin on Sat Jun 26 15:44:56 UTC 2021
PRIMARY
CAS
526216-43-3
Created by admin on Sat Jun 26 15:44:56 UTC 2021 , Edited by admin on Sat Jun 26 15:44:56 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE