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Details

Stereochemistry RACEMIC
Molecular Formula C20H25ClN2O5.CH4O3S
Molecular Weight 504.982
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMLODIPINE MESYLATE

SMILES

CS(O)(=O)=O.CCOC(=O)C1=C(COCCN)NC(C)=C(C1C2=C(Cl)C=CC=C2)C(=O)OC

InChI

InChIKey=MUVFCHUBATVFPP-UHFFFAOYSA-N
InChI=1S/C20H25ClN2O5.CH4O3S/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;1-5(2,3)4/h5-8,17,23H,4,9-11,22H2,1-3H3;1H3,(H,2,3,4)

HIDE SMILES / InChI

Molecular Formula CH4O3S
Molecular Weight 96.106
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C20H25ClN2O5
Molecular Weight 408.876
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

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

1992
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

1992
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
24-hour blood pressure control with the once-daily calcium antagonist amlodipine.
1991
A randomized, placebo-controlled, double-blind comparison of amlodipine and atenolol in patients with essential hypertension.
1992 Oct
[The effect of amlodipine, nifedipine and perindopril on insulin sensitivity and blood lipid of patients with essential hypertension].
1998 Mar
Low Dose Combination Therapy vs. High Dose Monotherapy in the Management of Hypertension.
1999 Nov
Effect of indomethacin on blood pressure in elderly people with essential hypertension well controlled on amlodipine or enalapril.
2000 Nov
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
Syncope following oral chloroquine administration in a hypertensive patient controlled on amlodipine.
2002 Apr
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
Is psychosis exacerbated by modafinil?
2002 Mar
Reversible ageusia induced by losartan: a case report.
2002 May
Severity of hypertension affects improved resistance artery endothelial function by angiotensin-converting enzyme inhibition.
2002 May
The effects of antihypertensive agents on the survival rate of polycystic kidney disease in Han:SPRD rats.
2002 Nov
Amlodipine and carvedilol prevent cytotoxicity in cortical neurons isolated from stroke-prone spontaneously hypertensive rats.
2004 Apr
Calcium channel blockades exhibit anti-inflammatory and antioxidative effects by augmentation of endothelial nitric oxide synthase and the inhibition of angiotensin converting enzyme in the N(G)-nitro-L-arginine methyl ester-induced hypertensive rat aorta: vasoprotective effects beyond the blood pressure-lowering effects of amlodipine and manidipine.
2005 Aug
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
Indapamide sustained release: a review of its use in the treatment of hypertension.
2006
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
Comparison of monotherapy versus combination antihypertensive therapy in elderly patients with essential hypertension.
2008 Apr-May
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 inhibits cell proliferation via PKD1-related pathway.
2008 May 2
Patents

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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 Dec 15 16:38:51 GMT 2023
Edited
by admin
on Fri Dec 15 16:38:51 GMT 2023
Record UNII
291Y33EZHA
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AMLODIPINE MESYLATE
Common Name English
AMLODIPINE MESILATE
WHO-DD  
Common Name English
AMLODIPINE (AS MESILATE)
Common Name English
3,5-PYRIDINEDICARBOXYLIC ACID, 2-((2-AMINOETHOXY)METHYL)-4-(2-CHLOROPHENYL)-1,4-DIHYDRO-6-METHYL-, 3-ETHYL 5-METHYL ESTER METHANESULFONATE (1:1)
Common Name English
Amlodipine mesilate [WHO-DD]
Common Name English
Code System Code Type Description
SMS_ID
100000089571
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
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EVMPD
SUB22129
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
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CAS
246852-12-0
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
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DRUG BANK
DBSALT001964
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
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PUBCHEM
10300874
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
PRIMARY
FDA UNII
291Y33EZHA
Created by admin on Fri Dec 15 16:38:51 GMT 2023 , Edited by admin on Fri Dec 15 16:38:51 GMT 2023
PRIMARY
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PARENT -> SALT/SOLVATE
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ACTIVE MOIETY