amlodipine indications/contra

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 183 88150-42-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • amlodipine
  • amlopres
  • racemic amlodipine
  • amlodipine besylate
  • amlodipine besilate
  • amlodipine maleate
  • amlodipine mesylate
  • amlodipine mesilate
A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.
  • Molecular weight: 408.88
  • Formula: C20H25ClN2O5
  • CLOGP: 3.43
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 99.88
  • ALOGS: -4.74
  • ROTB: 10

Drug dosage:

DoseUnitRoute
5 mg O

Approvals:

DateAgencyCompanyOrphan
July 31, 1992 FDA PFIZER

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 5991.97 25.02 1806 16914 29308 3337831
Hypotension 4540.96 25.02 1643 17077 47871 3319268
Toxicity to various agents 2497.54 25.02 1055 17665 45999 3321140
Intentional overdose 2366.22 25.02 755 17965 14470 3352669
Overdose 2212.54 25.02 883 17837 33095 3334044
Drug hypersensitivity 2009.93 25.02 836 17884 34844 3332295
Acute kidney injury 1649.93 25.02 805 17915 48878 3318261
Shock 1636.31 25.02 475 18245 6462 3360677
Oedema peripheral 1612.17 25.02 708 18012 33653 3333486
Dizziness 1478.45 25.02 864 17856 75648 3291491
Suicide attempt 1390.12 25.02 513 18207 15334 3351805
Bradycardia 1357.55 25.02 511 18209 16158 3350981
Drug interaction 1315.40 25.02 678 18042 46134 3321005
Blood pressure inadequately controlled 1295.65 25.02 287 18433 1133 3366006
Blood pressure increased 1245.17 25.02 520 18200 21710 3345429
Metabolic acidosis 1176.42 25.02 390 18330 8388 3358751
Gingival hypertrophy 1070.06 25.02 213 18507 418 3366721
Hypertension 990.04 25.02 526 18194 37940 3329199
Angioedema 782.76 25.02 335 18385 14800 3352339
Headache 747.94 25.02 611 18109 91369 3275770
Dyspnoea 744.72 25.02 639 18081 102295 3264844
Syncope 739.95 25.02 379 18341 25254 3341885
Fall 725.21 25.02 502 18218 58381 3308758
Blood pressure decreased 694.76 25.02 300 18420 13536 3353603
Pulmonary oedema 670.12 25.02 280 18440 11631 3355508
Malaise 645.62 25.02 487 18233 64690 3302449
Orthostatic hypotension 619.41 25.02 210 18510 4826 3362313
Loss of consciousness 596.22 25.02 339 18381 27808 3339331
Cardiac arrest 551.70 25.02 319 18401 27000 3340139
Joint swelling 537.93 25.02 268 18452 16789 3350350

Pharmacologic Action:

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SourceCodeDescription
ATC C08CA01 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
ATC C07FB07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
ATC C07FB12 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
ATC C07FB13 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
ATC C08GA02 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
CALCIUM CHANNEL BLOCKERS AND DIURETICS
Calcium channel blockers and diuretics
ATC C09BB03 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
ATC C09BB04 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
ATC C09BB07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
ATC C09BX01 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors, other combinations
ATC C09BX03 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors, other combinations
ATC C09DB01 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB04 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB05 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DX01 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists, other combinations
ATC C09DX03 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists, other combinations
ATC C09XA53 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
Renin-inhibitors
ATC C09XA54 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
Renin-inhibitors
ATC C10BX03 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
ATC C10BX07 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
ATC C10BX09 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
ATC C10BX11 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
ATC C10BX14 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175421 Dihydropyridine Calcium Channel Blocker
FDA Chemical/Ingredient N0000007556 Dihydropyridines
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35620 vasodilator agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Prinzmetal angina indication 87343002
Angina pectoris indication 194828000
Cerebrovascular accident indication 230690007 DOID:6713
Primary Prevention of Coronary Heart Disease indication
Myocardial Infarction Prevention indication
Anuria contraindication 2472002 DOID:2983
Alcoholism contraindication 7200002
Hyperkalemia contraindication 14140009
Jaundice contraindication 18165001
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Obstruction of bile duct contraindication 30144000 DOID:13580
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Hypothyroidism contraindication 40930008 DOID:1459
Angioedema contraindication 41291007 DOID:1558
Hypokalemia contraindication 43339004
Diabetes mellitus type 2 contraindication 44054006 DOID:9352
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Chronic idiopathic constipation contraindication 82934008
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:2527
Disorder of connective tissue contraindication 105969002 DOID:65
Disorder of muscle contraindication 129565002 DOID:423
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Hemorrhagic cerebral infarction contraindication 230706003
Disease of liver contraindication 235856003 DOID:409
Rhabdomyolysis contraindication 240131006
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Surgical procedure contraindication 387713003
Breastfeeding (mother) contraindication 413712001
Traumatic injury contraindication 417746004
Azotemia contraindication 445009001
Head and Neck Angioedema contraindication
Hemodialysis with High-Flux Membrane contraindication
Severe Aortic Valve Stenosis contraindication
Intestinal Angioedema contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.0 Basic
pKa2 1.55 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE TEKAMLO NOVARTIS N022545 Aug. 26, 2010 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
EQ 5MG BASE TEKAMLO NOVARTIS N022545 Aug. 26, 2010 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
EQ 10MG BASE AMTURNIDE NOVARTIS N200045 Dec. 21, 2010 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
EQ 5MG BASE AMTURNIDE NOVARTIS N200045 Dec. 21, 2010 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
EQ 10MG BASE CADUET PFIZER N021540 Jan. 30, 2004 RX TABLET ORAL 6455574 Aug. 11, 2018 TREATMENT OF HYPERTENSION AND HYPERLIPIDEMIA WITH A SINGLE COMPOSITION
EQ 2.5MG BASE CADUET PFIZER N021540 July 29, 2004 RX TABLET ORAL 6455574 Aug. 11, 2018 TREATMENT OF HYPERTENSION AND HYPERLIPIDEMIA WITH A SINGLE COMPOSITION
EQ 5MG BASE CADUET PFIZER N021540 Jan. 30, 2004 RX TABLET ORAL 6455574 Aug. 11, 2018 TREATMENT OF HYPERTENSION AND HYPERLIPIDEMIA WITH A SINGLE COMPOSITION
EQ 10MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 6696481 April 15, 2023 TREATMENT OF HYPERTENSION
EQ 2.5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 6696481 April 15, 2023 TREATMENT OF HYPERTENSION
EQ 5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 6696481 April 15, 2023 TREATMENT OF HYPERTENSION
EQ 10MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 7846961 Oct. 5, 2029 TREATMENT OF HYPERTENSION
EQ 2.5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 7846961 Oct. 5, 2029 TREATMENT OF HYPERTENSION
EQ 5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL 7846961 Oct. 5, 2029 TREATMENT OF HYPERTENSION

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL Jan. 21, 2018 NEW PRODUCT
EQ 2.5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL Jan. 21, 2018 NEW PRODUCT
EQ 5MG BASE PRESTALIA MARINA BIOTECH N205003 Jan. 21, 2015 RX TABLET ORAL Jan. 21, 2018 NEW PRODUCT

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel BLOCKER Ki 7 WOMBAT-PK CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER WOMBAT-PK CHEMBL
Voltage-dependent calcium channel gamma-1 subunit Ion channel Ki 7.20 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.65 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 5.87 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.58 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 5.36 DRUG MATRIX
Carbonic anhydrase 1 Enzyme WOMBAT-PK
Aldehyde oxidase Enzyme IC50 5.26 WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 4.51 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 5.27 CHEMBL
Potassium channel subfamily K member 2 Ion channel IC50 6.40 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 5.63 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 5.10 CHEMBL
Voltage-dependent calcium channel subunit alpha-2/delta-1 Ion channel Ki 7.20 WOMBAT-PK
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel Ki 8.70 CHEMBL

External reference:

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IDSource
DB00381 DRUGBANK_ID
4020813 VUID
N0000148333 NUI
C0051696 UMLSCUI
6981 IUPHAR_LIGAND_ID
D00615 KEGG_DRUG
1J444QC288 UNII
5729 INN_ID
246852-12-0 SECONDARY_CAS_RN
4020813 VANDF
N0000006268 NDFRT
N0000148333 NDFRT
27341 MMSL
003672 NDDF
17767 RXNORM
d00689 MMSL
108537001 SNOMEDCT_US
386864001 SNOMEDCT_US
173594 MMSL
CHEMBL1491 ChEMBL_ID
2162 PUBCHEM_CID
CHEMBL1200402 ChEMBL_ID
CHEMBL1200984 ChEMBL_ID
D017311 MESH_DESCRIPTOR_UI
CHEBI:2668 CHEBI
06X PDB_CHEM_ID
6UB PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Amlodipine Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0100 TABLET 2.50 mg ORAL ANDA 16 sections
Amlodipine Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0101 TABLET 5 mg ORAL ANDA 16 sections
Amlodipine Besylate HUMAN PRESCRIPTION DRUG LABEL 1 0054-0102 TABLET 10 mg ORAL ANDA 16 sections
Norvasc HUMAN PRESCRIPTION DRUG LABEL 1 0069-1520 TABLET 2.50 mg ORAL NDA 17 sections
Norvasc HUMAN PRESCRIPTION DRUG LABEL 1 0069-1530 TABLET 5 mg ORAL NDA 17 sections
Norvasc HUMAN PRESCRIPTION DRUG LABEL 1 0069-1540 TABLET 10 mg ORAL NDA 17 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2150 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2160 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2170 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2180 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2190 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2250 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2260 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2270 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2960 TABLET, FILM COATED 2.50 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2970 TABLET, FILM COATED 2.50 mg ORAL NDA 19 sections
Caduet HUMAN PRESCRIPTION DRUG LABEL 2 0069-2980 TABLET, FILM COATED 2.50 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0364 CAPSULE 10 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0379 CAPSULE 10 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0384 CAPSULE 5 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0404 CAPSULE 2.50 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0405 CAPSULE 5 mg ORAL NDA 19 sections
Lotrel HUMAN PRESCRIPTION DRUG LABEL 2 0078-0406 CAPSULE 5 mg ORAL NDA 19 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0488 TABLET, FILM COATED 5 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0489 TABLET, FILM COATED 10 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0490 TABLET, FILM COATED 5 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0491 TABLET, FILM COATED 10 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0559 TABLET, FILM COATED 5 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0560 TABLET, FILM COATED 5 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0561 TABLET, FILM COATED 10 mg ORAL NDA 18 sections