diltiazem Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, diltiazem derivatives 897 42399-41-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • (+)-Diltiazem
  • dilzem
  • d-Diltiazem
  • d-cis-Diltiazem
  • diltiazem hydrochloride
  • diltiazem malate
  • diltiazem
  • diltiazem HCl
A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
  • Molecular weight: 414.52
  • Formula: C22H26N2O4S
  • CLOGP: 3.65
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 59.08
  • ALOGS: -4.39
  • ROTB: 7

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.24 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 19.30 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 38 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 4.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.18 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 1982 FDA VALEANT INTL

FDA Adverse Event Reporting System (Female)

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 704.44 10.25 1155 94986 144765 46445156
Atrial fibrillation 584.13 10.25 881 95260 102709 46487212
Cardiac failure congestive 272.75 10.25 591 95550 91159 46498762
Bradycardia 224.96 10.25 451 95690 65847 46524074
Rheumatoid arthritis 202.62 10.25 122 96019 240093 46349828
Hypotension 192.59 10.25 967 95174 231622 46358299
Off label use 190.20 10.25 306 95835 379535 46210386
Drug ineffective 189.80 10.25 738 95403 677100 45912821
Maternal exposure during pregnancy 151.55 10.25 17 96124 102532 46487389
Dyspnoea 137.47 10.25 1642 94499 513906 46076015
Exposure during pregnancy 130.89 10.25 31 96110 108181 46481740
Nodal rhythm 113.17 10.25 60 96081 1665 46588256
Sedation complication 112.13 10.25 78 96063 3567 46586354
Creatinine renal clearance decreased 109.13 10.25 100 96041 6820 46583101
Toxicity to various agents 107.33 10.25 775 95366 210991 46378930
Treatment failure 102.54 10.25 32 96109 93055 46496866
Neutropenia 99.50 10.25 89 96052 143115 46446806
Cardiac arrest 92.34 10.25 400 95741 89999 46499922
Atrioventricular block complete 91.72 10.25 95 96046 7532 46582389
Nerve injury 87.36 10.25 93 96048 7612 46582309
Febrile neutropenia 84.03 10.25 45 96096 94582 46495339
Orthostatic hypotension 83.86 10.25 168 95973 24490 46565431
Dyspnoea exertional 81.19 10.25 258 95883 50031 46539890
Fluid retention 77.10 10.25 256 95885 50790 46539131
Synovitis 76.85 10.25 16 96125 61059 46528862
Atrioventricular block second degree 76.26 10.25 63 96078 3736 46586185
Heart rate increased 75.65 10.25 330 95811 74461 46515460
Chronic obstructive pulmonary disease 74.90 10.25 275 95866 57358 46532563
Poisoning 73.01 10.25 115 96026 13879 46576042
Gastrointestinal haemorrhage 71.22 10.25 332 95809 77041 46512880
Pemphigus 70.81 10.25 6 96135 45268 46544653
International normalised ratio increased 68.92 10.25 233 95908 46650 46543271
Sinus bradycardia 67.44 10.25 110 96031 13672 46576249
Chest pain 67.29 10.25 605 95536 175719 46414202
Oedema peripheral 65.62 10.25 557 95584 159149 46430772
Atrioventricular block first degree 63.74 10.25 71 96070 6115 46583806
Therapeutic product effect incomplete 62.59 10.25 42 96099 78111 46511810
Cardiogenic shock 62.27 10.25 117 96024 16267 46573654
Drug intolerance 58.10 10.25 136 96005 146913 46443008
Labile blood pressure 56.06 10.25 38 96103 1665 46588256
Product use issue 55.38 10.25 68 96073 94576 46495345
Contraindicated product administered 55.12 10.25 50 96091 79897 46510024
Systemic lupus erythematosus 54.98 10.25 33 96108 65147 46524774
Pulmonary congestion 54.16 10.25 104 96037 14695 46575226
Abortion spontaneous 53.75 10.25 12 96129 43634 46546287
Rash 53.57 10.25 473 95668 356039 46233882
Leukopenia 53.04 10.25 38 96103 68305 46521616
Therapeutic product effect decreased 50.85 10.25 57 96084 82544 46507377
Injection site erythema 50.77 10.25 47 96094 74380 46515541
Heart rate decreased 50.50 10.25 162 95979 31561 46558360
Atrial flutter 48.86 10.25 76 96065 9072 46580849
Alopecia 48.21 10.25 172 95969 162242 46427679
Hand deformity 47.98 10.25 7 96134 34567 46555354
Pulmonary arterial hypertension 47.42 10.25 139 96002 25789 46564132
Fall 46.60 10.25 943 95198 328154 46261767
Pneumonia 46.45 10.25 1057 95084 375263 46214658
Dizziness 46.09 10.25 969 95172 339445 46250476
Product use in unapproved indication 45.67 10.25 72 96069 90201 46499720
Product complaint 45.47 10.25 86 96055 12015 46577906
Malignant neoplasm progression 44.28 10.25 41 96100 64885 46525036
Cardiac disorder 43.17 10.25 192 95949 43666 46546255
Suspected suicide 42.13 10.25 50 96091 4611 46585310
Coronary artery disease 42.12 10.25 159 95982 33593 46556328
Blood calcium decreased 42.04 10.25 97 96044 15576 46574345
Palpitations 40.55 10.25 335 95806 94924 46494997
Pericardial haemorrhage 40.40 10.25 30 96111 1521 46588400
Supraventricular tachycardia 39.94 10.25 86 96055 13184 46576737
Medication error 39.72 10.25 147 95994 30764 46559157
Asthenia 39.68 10.25 878 95263 310197 46279724
Pyrexia 39.63 10.25 494 95647 348308 46241613
Renal failure 39.38 10.25 382 95759 113212 46476709
Acute generalised exanthematous pustulosis 39.32 10.25 70 96071 9335 46580586
Sedation 39.23 10.25 120 96021 22790 46567131
Hepatic enzyme increased 37.02 10.25 70 96071 81717 46508204
Hypoxia 36.88 10.25 207 95934 51631 46538290
Foetal exposure during pregnancy 36.77 10.25 9 96132 30738 46559183
Angina pectoris 36.67 10.25 130 96011 26645 46563276
Pulmonary hypertension 36.51 10.25 159 95982 35834 46554087
Respiratory arrest 36.32 10.25 152 95989 33664 46556257
Hyperkalaemia 35.10 10.25 201 95940 50508 46539413
Drug interaction 34.58 10.25 599 95542 202495 46387426
White blood cell count decreased 33.86 10.25 118 96023 112113 46477808
Nodal arrhythmia 33.83 10.25 25 96116 1258 46588663
Inhibitory drug interaction 33.76 10.25 30 96111 1965 46587956
Joint swelling 33.74 10.25 202 95939 165871 46424050
Presyncope 33.72 10.25 119 96022 24335 46565586
Arthropathy 33.70 10.25 78 96063 84622 46505299
Infusion related reaction 33.59 10.25 102 96039 101106 46488815
Pain in jaw 33.36 10.25 162 95979 38210 46551711
Intentional self-injury 33.29 10.25 5 96136 24161 46565760
Balance disorder 33.08 10.25 237 95904 64284 46525637
Musculoskeletal stiffness 33.07 10.25 98 96043 97895 46492026
Blood pressure systolic increased 32.98 10.25 132 96009 28655 46561266
C-reactive protein abnormal 32.77 10.25 3 96138 21267 46568654
Nephrolithiasis 32.76 10.25 145 95996 32906 46557015
Thrombocytopenia 32.49 10.25 142 95999 126439 46463482
Oedema 32.46 10.25 243 95898 66828 46523093
Torsade de pointes 32.35 10.25 75 96066 12079 46577842
Pulseless electrical activity 32.12 10.25 55 96086 7112 46582809
Injection site pain 32.10 10.25 113 96028 107039 46482882
Premature delivery 31.74 10.25 4 96137 22065 46567856
Bezoar 31.59 10.25 25 96116 1394 46588527
Arthralgia 31.12 10.25 546 95595 364057 46225864
Atrioventricular block 30.17 10.25 52 96089 6759 46583162
Respiratory tract congestion 29.93 10.25 75 96066 12689 46577232
Body tinea 28.74 10.25 20 96121 915 46589006
Pulmonary oedema 28.72 10.25 192 95949 50913 46539008
Pregnancy 28.69 10.25 10 96131 27127 46562794
Myocardial infarction 28.59 10.25 317 95824 97211 46492710
Suicidal ideation 28.48 10.25 45 96096 56337 46533584
Glossodynia 27.98 10.25 30 96111 44343 46545578
General physical health deterioration 27.84 10.25 133 96008 115636 46474285
Neutrophil count decreased 26.68 10.25 30 96111 43396 46546525
Ventricular tachycardia 26.42 10.25 86 96055 16881 46573040
Bunion operation 26.33 10.25 18 96123 800 46589121
Product residue present 26.17 10.25 36 96105 3846 46586075
Pancytopenia 25.94 10.25 89 96052 84969 46504952
Intentional product use issue 25.84 10.25 43 96098 52737 46537184
Blood pressure diastolic decreased 25.81 10.25 76 96065 14135 46575786
Cognitive disorder 25.39 10.25 146 95995 36737 46553184
Erythromelalgia 25.28 10.25 10 96131 137 46589784
Transfusion 25.22 10.25 72 96069 13159 46576762
Depressed level of consciousness 25.12 10.25 176 95965 47393 46542528
Injection site pruritus 24.92 10.25 27 96114 39716 46550205
Arrhythmia 24.69 10.25 139 96002 34702 46555219
Alveolitis 24.45 10.25 28 96113 2485 46587436
Seizure 24.29 10.25 151 95990 122903 46467018
Sinus arrhythmia 24.11 10.25 21 96120 1339 46588582
Fluid overload 23.79 10.25 115 96026 27070 46562851
Cardioactive drug level increased 23.60 10.25 25 96116 2034 46587887
Gouty tophus 23.54 10.25 10 96131 166 46589755
Sinus arrest 23.45 10.25 23 96118 1708 46588213
Hepatic ischaemia 23.41 10.25 14 96127 492 46589429
Arteriovenous fistula occlusion 23.17 10.25 12 96129 317 46589604
Colon gangrene 23.01 10.25 5 96136 4 46589917
Death 22.99 10.25 876 95265 334672 46255249
Muscle relaxant therapy 22.97 10.25 9 96132 120 46589801
Mucosal inflammation 22.79 10.25 28 96113 38948 46550973
Erythrodermic psoriasis 22.72 10.25 17 96124 872 46589049
Syncope 22.71 10.25 322 95819 104481 46485440
Blue toe syndrome 22.31 10.25 12 96129 343 46589578
Premature baby 22.26 10.25 5 96136 18107 46571814
Drug hypersensitivity 21.78 10.25 362 95779 243463 46346458
Bladder prolapse 21.71 10.25 23 96118 1871 46588050
C-reactive protein increased 21.69 10.25 56 96085 58534 46531387
Vasoplegia syndrome 21.69 10.25 18 96123 1074 46588847
Rectal prolapse 21.53 10.25 21 96120 1549 46588372
Injection site swelling 21.51 10.25 31 96110 40296 46549625
Epilepsy 21.48 10.25 11 96130 23727 46566194
Blood pressure inadequately controlled 21.33 10.25 35 96106 4371 46585550
Heart rate irregular 21.09 10.25 85 96056 18506 46571415
Rectal haemorrhage 21.06 10.25 143 95998 38112 46551809
BRASH syndrome 21.03 10.25 8 96133 98 46589823
Hospitalisation 20.90 10.25 211 95930 63174 46526747
Cardioversion 20.85 10.25 18 96123 1134 46588787
Nephroangiosclerosis 20.83 10.25 9 96132 156 46589765
Unevaluable event 20.50 10.25 164 95977 46011 46543910
Depression 20.37 10.25 238 95903 169866 46420055
Psoriasis 20.27 10.25 88 96053 78516 46511405
Cerebellar syndrome 20.22 10.25 30 96111 3435 46586486
Cardiac pacemaker insertion 20.13 10.25 31 96110 3668 46586253
Coagulopathy 19.74 10.25 83 96058 18416 46571505
Renal pain 19.52 10.25 38 96103 5423 46584498
Status epilepticus 19.01 10.25 3 96138 13976 46575945
Posterior reversible encephalopathy syndrome 18.97 10.25 4 96137 15137 46574784
Bone marrow failure 18.77 10.25 20 96121 29649 46560272
Thermal burn 18.74 10.25 35 96106 4842 46585079
Prinzmetal angina 18.32 10.25 14 96127 741 46589180
Stent placement 18.24 10.25 29 96112 3527 46586394
Multiple sclerosis relapse 18.23 10.25 37 96104 42088 46547833
Stomatitis 17.89 10.25 76 96065 68221 46521700
Cerebrovascular accident 17.89 10.25 300 95841 100739 46489182
Inappropriate schedule of product administration 17.87 10.25 71 96070 64942 46524979
Anuria 17.85 10.25 58 96083 11373 46578548
Injection site reaction 17.51 10.25 46 96095 47803 46542118
Impaired quality of life 17.41 10.25 27 96114 3215 46586706
Drug resistance 17.35 10.25 7 96134 17361 46572560
Hepatorenal syndrome 17.35 10.25 20 96121 1788 46588133
Sleep disorder 17.11 10.25 45 96096 46750 46543171
Stupor 17.09 10.25 28 96113 3492 46586429
Cytomegalovirus infection 17.04 10.25 8 96133 18136 46571785
Fear of eating 17.02 10.25 10 96131 340 46589581
Disease progression 17.01 10.25 114 96027 91186 46498735
Oxygen therapy 16.91 10.25 20 96121 1837 46588084
Blood pressure increased 16.88 10.25 360 95781 126306 46463615
Blood loss anaemia 16.73 10.25 47 96094 8510 46581411
Limb injury 16.70 10.25 81 96060 19093 46570828
Myopathy 16.61 10.25 48 96093 8833 46581088
Extrasystoles 16.34 10.25 33 96108 4836 46585085
Peak expiratory flow rate abnormal 16.33 10.25 7 96134 119 46589802
Metabolic acidosis 16.28 10.25 136 96005 38644 46551277
Drug-induced liver injury 16.16 10.25 17 96124 25351 46564570
Electrocardiogram QT shortened 16.11 10.25 7 96134 123 46589798
Leukaemoid reaction 16.11 10.25 8 96133 193 46589728
Urticaria 16.10 10.25 160 95981 117732 46472189
Aggression 15.94 10.25 14 96127 22730 46567191
Catheter site erythema 15.83 10.25 29 96112 3954 46585967
Cardiac ablation 15.71 10.25 16 96125 1243 46588678
Psoriatic arthropathy 15.71 10.25 32 96109 36347 46553574
Distributive shock 15.68 10.25 11 96130 510 46589411
Acute lung injury 15.59 10.25 16 96125 1255 46588666
Sinus node dysfunction 15.52 10.25 30 96111 4259 46585662
Sopor 15.41 10.25 11 96130 19817 46570104
Forced expiratory volume decreased 15.27 10.25 33 96108 5071 46584850
Atrioventricular dissociation 15.25 10.25 8 96133 217 46589704
Heart rate abnormal 15.19 10.25 26 96115 3361 46586560
Catheter site haemorrhage 15.16 10.25 23 96118 2686 46587235
Histoplasmosis 15.06 10.25 18 96123 1672 46588249
Red blood cell sedimentation rate increased 14.97 10.25 15 96126 22874 46567047
Productive cough 14.92 10.25 165 95976 50550 46539371
Carbon dioxide increased 14.80 10.25 15 96126 1159 46588762
Exposure via ingestion 14.75 10.25 26 96115 3441 46586480
Pain 14.70 10.25 818 95323 476130 46113791
Activated partial thromboplastin time prolonged 14.63 10.25 39 96102 6850 46583071
Dialysis 14.61 10.25 50 96091 10066 46579855
Hepatotoxicity 14.59 10.25 18 96123 24991 46564930
Pulmonary embolism 14.56 10.25 148 95993 108437 46481484
Anion gap abnormal 14.52 10.25 9 96132 338 46589583
Infection susceptibility increased 14.38 10.25 20 96121 2159 46587762
Respiratory rate increased 14.38 10.25 54 96087 11379 46578542
Disturbance in attention 14.28 10.25 27 96114 31533 46558388
Pericarditis 14.19 10.25 17 96124 23910 46566011
Lower gastrointestinal haemorrhage 14.11 10.25 40 96101 7280 46582641
Cardiac monitoring 13.97 10.25 4 96137 18 46589903
Intra-abdominal haematoma 13.93 10.25 17 96124 1614 46588307
Poor quality sleep 13.69 10.25 65 96076 15188 46574733
Hypertrophic cardiomyopathy 13.68 10.25 15 96126 1269 46588652
Humidity intolerance 13.68 10.25 9 96132 375 46589546
Total lung capacity decreased 13.67 10.25 14 96127 1095 46588826
Oxygen saturation decreased 13.60 10.25 209 95932 68955 46520966
Unresponsive to stimuli 13.59 10.25 113 96028 32061 46557860
Inflammation 13.58 10.25 53 96088 48728 46541193
Renal necrosis 13.55 10.25 5 96136 56 46589865
Nasal congestion 13.46 10.25 155 95986 47958 46541963
Acute myocardial infarction 13.42 10.25 112 96029 31812 46558109
Wrong technique in product usage process 13.38 10.25 62 96079 54360 46535561
Injection site urticaria 13.37 10.25 4 96137 11963 46577958
Anaphylactic reaction 13.36 10.25 60 96081 53052 46536869
Bundle branch block left 13.36 10.25 36 96105 6363 46583558
Arrhythmogenic right ventricular dysplasia 13.31 10.25 4 96137 22 46589899
Sebaceous gland infection 13.29 10.25 6 96135 116 46589805
Acute myeloid leukaemia 13.28 10.25 8 96133 15770 46574151
Sinoatrial block 13.25 10.25 12 96129 806 46589115
Plasma cell myeloma 13.25 10.25 47 96094 44431 46545490
Incision site haemorrhage 13.24 10.25 10 96131 520 46589401
Caesarean section 13.18 10.25 9 96132 16594 46573327
Wound 12.90 10.25 45 96096 42757 46547164
Injection site inflammation 12.85 10.25 23 96118 3079 46586842
Haemodialysis 12.83 10.25 45 96096 9172 46580749
Discomfort 12.80 10.25 51 96090 46619 46543302
Liver disorder 12.74 10.25 37 96104 37209 46552712
Brain natriuretic peptide increased 12.71 10.25 29 96112 4621 46585300
Arteriospasm coronary 12.70 10.25 25 96116 3596 46586325
Osteonecrosis of jaw 12.64 10.25 33 96108 34369 46555552
Rhabdomyolysis 12.63 10.25 137 96004 41772 46548149
Metastases to liver 12.62 10.25 13 96128 19572 46570349
Muscle spasticity 12.47 10.25 4 96137 11436 46578485
Hypochromic anaemia 12.32 10.25 15 96126 1420 46588501
Metastases to central nervous system 12.09 10.25 4 96137 11217 46578704
Bladder disorder 12.05 10.25 37 96104 7041 46582880
Injection site rash 11.99 10.25 9 96132 15804 46574117
Exercise tolerance decreased 11.91 10.25 28 96113 4549 46585372
Duodenal polyp 11.88 10.25 5 96136 81 46589840
Migraine 11.79 10.25 90 96051 69936 46519985
Erythema 11.78 10.25 215 95926 142605 46447316
Night sweats 11.74 10.25 24 96117 27226 46562695
No adverse event 11.71 10.25 34 96107 34197 46555724
Bronchitis 11.58 10.25 293 95848 105686 46484235
Blister 11.48 10.25 50 96091 44581 46545340
Accidental exposure to product 11.45 10.25 16 96125 21065 46568856
Abnormal behaviour 11.42 10.25 16 96125 21042 46568879
Catheter site discharge 11.40 10.25 17 96124 1955 46587966
Upper gastrointestinal haemorrhage 11.35 10.25 66 96075 16672 46573249
Electrocardiogram QRS complex shortened 11.34 10.25 8 96133 374 46589547
Mitral valve incompetence 11.30 10.25 72 96069 18780 46571141
Fibrous histiocytoma 11.26 10.25 9 96132 509 46589412
Ill-defined disorder 11.24 10.25 24 96117 26803 46563118
Mental status changes 11.24 10.25 124 96017 37964 46551957
CREST syndrome 11.21 10.25 8 96133 381 46589540
Electrocardiogram U wave present 11.20 10.25 5 96136 94 46589827
Asthma 11.18 10.25 257 95884 91285 46498636
Pneumocystis jirovecii pneumonia 11.16 10.25 9 96132 15239 46574682
Polyneuropathy 11.14 10.25 5 96136 11639 46578282
Ventricular fibrillation 11.06 10.25 50 96091 11446 46578475
Catheter site inflammation 11.06 10.25 10 96131 670 46589251
Retroperitoneal haemorrhage 11.00 10.25 20 96121 2710 46587211
Brain oedema 10.97 10.25 6 96135 12472 46577449
Blood pressure decreased 10.96 10.25 172 95969 56987 46532934
Metastases to bone 10.81 10.25 12 96129 17464 46572457
Contusion 10.81 10.25 246 95895 87241 46502680
Coronary artery occlusion 10.80 10.25 39 96102 8063 46581858
Hyperbilirubinaemia 10.77 10.25 4 96137 10434 46579487
Intestinal ischaemia 10.69 10.25 35 96106 6890 46583031
Cough 10.68 10.25 578 95563 229671 46360250
Seasonal allergy 10.67 10.25 55 96086 13279 46576642
Palmar-plantar erythrodysaesthesia syndrome 10.63 10.25 16 96125 20435 46569486
Live birth 10.59 10.25 4 96137 10326 46579595
Atrial appendage closure 10.57 10.25 3 96138 13 46589908
Blood count abnormal 10.54 10.25 68 96073 17810 46572111
Aortic stenosis 10.54 10.25 26 96115 4356 46585565
Multiple sclerosis 10.54 10.25 22 96119 24769 46565152
Fracture 10.54 10.25 11 96130 16460 46573461
Hepatic haematoma 10.49 10.25 8 96133 422 46589499
Malignant melanoma 10.43 10.25 4 96137 10230 46579691
Condition aggravated 10.39 10.25 406 95735 244646 46345275
Jaundice 10.35 10.25 28 96113 28817 46561104
Renal injury 10.33 10.25 43 96098 9498 46580423
Gastrointestinal disorder 10.30 10.25 76 96065 59500 46530421
Enlarged uvula 10.28 10.25 5 96136 115 46589806
Gravitational oedema 10.27 10.25 12 96129 1088 46588833
Orthopnoea 10.25 10.25 31 96110 5849 46584072

FDA Adverse Event Reporting System (Male)

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
Bradycardia 390.35 10.59 556 57933 64970 29829019
Atrial fibrillation 316.65 10.59 670 57819 107454 29786535
Completed suicide 290.64 10.59 616 57873 98876 29795113
Cardiac failure congestive 143.92 10.59 426 58063 83981 29810008
Hypotension 135.33 10.59 758 57731 199807 29694182
Off label use 134.63 10.59 174 58315 249116 29644873
Cardiac arrest 86.58 10.59 385 58104 92465 29801524
Febrile neutropenia 61.07 10.59 71 58418 106622 29787367
Atrial flutter 60.83 10.59 104 58385 14177 29879812
Dyspnoea 59.76 10.59 947 57542 332348 29561641
Drug ineffective 59.62 10.59 405 58084 339982 29554007
International normalised ratio increased 58.02 10.59 215 58274 47524 29846465
Atrioventricular block complete 56.42 10.59 76 58413 8401 29885588
Atrioventricular block 54.23 10.59 69 58420 7213 29886776
Myocardial infarction 50.88 10.59 419 58070 125206 29768783
Pyrexia 46.84 10.59 360 58129 294129 29599860
Product use in unapproved indication 46.68 10.59 45 58444 73648 29820341
Dizziness 43.18 10.59 575 57914 194334 29699655
Chronic obstructive pulmonary disease 41.98 10.59 190 58299 45936 29848053
Incision site pain 41.28 10.59 33 58456 1971 29892018
Poisoning 40.93 10.59 77 58412 11305 29882684
Prinzmetal angina 39.80 10.59 24 58465 905 29893084
Atrioventricular block first degree 37.86 10.59 51 58438 5637 29888352
Syncope 36.96 10.59 288 58201 84615 29809374
Nodal arrhythmia 36.35 10.59 22 58467 835 29893154
Neutropenia 36.26 10.59 129 58360 128411 29765578
Drug interaction 35.59 10.59 567 57922 199001 29694988
Arterial spasm 34.71 10.59 12 58477 116 29893873
Gastrointestinal haemorrhage 34.11 10.59 279 58210 83167 29810822
Coronary artery disease 32.75 10.59 187 58302 49525 29844464
Nodal rhythm 32.71 10.59 25 58464 1398 29892591
Cardioplegia 31.44 10.59 6 58483 0 29893989
Chest pain 30.71 10.59 358 58131 117269 29776720
Exposure via ingestion 30.06 10.59 31 58458 2580 29891409
Cardiogenic shock 29.52 10.59 86 58403 16775 29877214
Oedema peripheral 29.38 10.59 326 58163 105506 29788483
Angina unstable 28.88 10.59 70 58419 12240 29881749
Tetany 28.28 10.59 18 58471 748 29893241
Heart rate decreased 27.56 10.59 97 58392 20897 29873092
Angina pectoris 26.40 10.59 121 58368 29397 29864592
Red blood cells urine positive 25.83 10.59 23 58466 1594 29892395
Serotonin syndrome 24.58 10.59 3 58486 17888 29876101
Suspected suicide 23.61 10.59 30 58459 3131 29890858
Medication error 23.44 10.59 92 58397 20880 29873109
General physical health deterioration 23.32 10.59 108 58381 99836 29794153
Pancytopenia 22.88 10.59 87 58402 84965 29809024
Blood glucose increased 22.63 10.59 201 58288 61329 29832660
Fluid retention 22.01 10.59 102 58387 24896 29869093
Pulmonary arterial hypertension 21.93 10.59 53 58436 9248 29884741
Product use issue 21.88 10.59 35 58454 45981 29848008
Influenza virus test positive 21.02 10.59 8 58481 104 29893885
Treatment failure 21.00 10.59 22 58467 34657 29859332
Mycotic allergy 20.68 10.59 9 58480 168 29893821
Discharge 20.35 10.59 8 58481 114 29893875
Chondrocalcinosis 19.99 10.59 10 58479 259 29893730
Neutrophil count decreased 19.53 10.59 33 58456 42421 29851568
White blood cell count decreased 19.41 10.59 91 58398 83856 29810133
Injury 19.37 10.59 89 58400 21642 29872347
Atrioventricular block second degree 19.16 10.59 27 58462 3113 29890876
Cerebrovascular accident 18.72 10.59 247 58242 83230 29810759
Myocardial ischaemia 18.57 10.59 75 58414 17242 29876747
Acquired haemophilia 18.47 10.59 14 58475 773 29893216
Electrocardiogram QRS complex shortened 18.40 10.59 8 58481 149 29893840
Thrombocytopenia 18.35 10.59 175 58314 136869 29757120
Mite allergy 18.32 10.59 9 58480 224 29893765
Rheumatoid arthritis 18.06 10.59 33 58456 41164 29852825
Intentional product use issue 18.01 10.59 27 58462 36413 29857576
Atrial thrombosis 17.57 10.59 20 58469 1861 29892128
Malignant neoplasm progression 17.53 10.59 77 58412 72210 29821779
Nephrogenic systemic fibrosis 17.52 10.59 31 58458 4340 29889649
Ventricular fibrillation 17.40 10.59 67 58422 15071 29878918
Pneumocystis jirovecii pneumonia 17.13 10.59 6 58483 17114 29876875
Ischaemic hepatitis 17.03 10.59 18 58471 1541 29892448
Eczema infected 16.97 10.59 5 58484 27 29893962
Gallbladder polyp 16.70 10.59 9 58480 273 29893716
Palpitations 16.35 10.59 117 58372 33456 29860533
Hepatic function abnormal 16.33 10.59 36 58453 41909 29852080
Skin tightness 16.32 10.59 20 58469 2012 29891977
Spirometry abnormal 16.23 10.59 9 58480 289 29893700
Toxic optic neuropathy 15.71 10.59 12 58477 670 29893319
Blood urea increased 15.65 10.59 110 58379 31271 29862718
Protein urine present 15.57 10.59 31 58458 4744 29889245
Lymphocyte count decreased 15.50 10.59 76 58413 18979 29875010
Vitiligo 15.44 10.59 12 58477 688 29893301
Pacemaker generated rhythm 15.30 10.59 5 58484 40 29893949
BRASH syndrome 15.19 10.59 5 58484 41 29893948
Psychotic disorder 14.98 10.59 12 58477 21503 29872486
Hypoxia 14.94 10.59 151 58338 47703 29846286
Toxicity to various agents 14.89 10.59 452 58037 176731 29717258
Pericardial haemorrhage 14.79 10.59 23 58466 2895 29891094
Mesothelioma 14.76 10.59 10 58479 462 29893527
Blood pressure immeasurable 14.64 10.59 13 58476 898 29893091
Cardiac disorder 14.50 10.59 130 58359 39763 29854226
Blood pressure systolic decreased 14.49 10.59 26 58463 3681 29890308
Renal injury 14.38 10.59 53 58436 11676 29882313
Agranulocytosis 14.35 10.59 13 58476 21929 29872060
Product dose omission issue 14.03 10.59 113 58376 91518 29802471
Infection 14.02 10.59 92 58397 77982 29816007
Sinus arrest 13.92 10.59 16 58473 1504 29892485
Device capturing issue 13.65 10.59 3 58486 3 29893986
Subacute cutaneous lupus erythematosus 13.60 10.59 11 58478 668 29893321
Rectal fissure 13.48 10.59 8 58481 293 29893696
Dust allergy 13.44 10.59 9 58480 408 29893581
Sepsis 13.44 10.59 203 58286 146192 29747797
Angina bullosa haemorrhagica 13.42 10.59 5 58484 61 29893928
Fear 13.34 10.59 49 58440 10776 29883213
Ventricular tachycardia 13.31 10.59 86 58403 23776 29870213
Epilepsy 13.13 10.59 12 58477 20157 29873832
Heart rate irregular 13.07 10.59 53 58436 12206 29881783
Anuria 12.97 10.59 47 58442 10269 29883720
Aortic stenosis 12.86 10.59 26 58463 4022 29889967
Bronchopulmonary aspergillosis 12.83 10.59 4 58485 12280 29881709
Cardiospasm 12.79 10.59 3 58486 5 29893984
Eosinophilic pleural effusion 12.73 10.59 7 58482 221 29893768
Blood pressure inadequately controlled 12.67 10.59 20 58469 2550 29891439
Mast cell degranulation present 12.61 10.59 5 58484 73 29893916
Arrhythmia 12.52 10.59 109 58380 33060 29860929
Antiacetylcholine receptor antibody positive 12.46 10.59 4 58485 30 29893959
Septic shock 12.43 10.59 73 58416 63534 29830455
Hyperbilirubinaemia 12.37 10.59 9 58480 16933 29877056
Encephalopathy 12.24 10.59 28 58461 32177 29861812
Osteonecrosis of jaw 12.21 10.59 11 58478 18607 29875382
Product residue present 12.06 10.59 20 58469 2658 29891331
Drug resistance 11.93 10.59 13 58476 20120 29873869
Anticoagulation drug level above therapeutic 11.77 10.59 16 58473 1783 29892206
Abnormal behaviour 11.70 10.59 20 58469 25603 29868386
Emotional distress 11.51 10.59 61 58428 15704 29878285
Conjunctivitis allergic 11.44 10.59 9 58480 525 29893464
Rhabdomyolysis 11.41 10.59 181 58308 63399 29830590
Labyrinthitis 11.39 10.59 11 58478 846 29893143
Cardioactive drug level increased 11.37 10.59 15 58474 1624 29892365
Right ventricular failure 11.31 10.59 38 58451 7998 29885991
Anhedonia 11.27 10.59 39 58450 8330 29885659
Dyspnoea exertional 11.15 10.59 112 58377 35318 29858671
Blood pressure diastolic decreased 11.11 10.59 32 58457 6199 29887790
Iron binding capacity total increased 11.11 10.59 4 58485 44 29893945
Arteriospasm coronary 11.06 10.59 19 58470 2599 29891390
Transaminases increased 11.00 10.59 18 58471 23439 29870550
Lung adenocarcinoma stage IV 10.91 10.59 5 58484 106 29893883
Lower gastrointestinal haemorrhage 10.79 10.59 37 58452 7867 29886122
Unevaluable event 10.75 10.59 102 58387 31683 29862306
Shock 10.75 10.59 79 58410 22780 29871209
Infectious mononucleosis 10.69 10.59 8 58481 433 29893556
Tooth injury 10.68 10.59 10 58479 740 29893249
Inner ear disorder 10.62 10.59 6 58483 200 29893789

Pharmacologic Action:

SourceCodeDescription
ATC C05AE03 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Muscle relaxants
ATC C08DB01 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH DIRECT CARDIAC EFFECTS
Benzothiazepine derivatives
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175566 Calcium Channel Blocker
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:38215 calcium channel blockers

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Atrial fibrillation indication 49436004 DOID:0060224
Paroxysmal supraventricular tachycardia indication 67198005
Prinzmetal angina indication 87343002
Angina pectoris indication 194828000
Anal fissure off-label use 30037006
Supraventricular arrhythmia off-label use 72654001
Diastolic heart failure off-label use 418304008 DOID:9775
Hyperkalemia contraindication 14140009
Ventricular tachycardia contraindication 25569003
Complete atrioventricular block contraindication 27885002
Acute cerebrovascular insufficiency contraindication 29322000
Sick sinus syndrome contraindication 36083008 DOID:13884
Immunosuppression contraindication 38013005
Angioedema contraindication 41291007 DOID:1558
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Lown-Ganong-Levine syndrome contraindication 55475008 DOID:13087
Aortic valve stenosis contraindication 60573004 DOID:1712
Wolff-Parkinson-White pattern contraindication 74390002 DOID:384
Transplantation contraindication 77465005
Chronic idiopathic constipation contraindication 82934008
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Kidney disease contraindication 90708001 DOID:557
Disorder of connective tissue contraindication 105969002 DOID:65
Second degree atrioventricular block contraindication 195042002
Decompensated cardiac failure contraindication 195111005
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Left ventricular cardiac dysfunction contraindication 429589006
Hemodialysis with High-Flux Membrane contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.63 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
120MG DILTIAZEM HYDROCHLORIDE GLENMARK PHARMS LTD A212317 March 22, 2021 RX CAPSULE, EXTENDED RELEASE ORAL Sept. 26, 2021 COMPETITIVE GENERIC THERAPY
60MG DILTIAZEM HYDROCHLORIDE GLENMARK PHARMS LTD A212317 March 22, 2021 RX CAPSULE, EXTENDED RELEASE ORAL Sept. 26, 2021 COMPETITIVE GENERIC THERAPY
90MG DILTIAZEM HYDROCHLORIDE GLENMARK PHARMS LTD A212317 March 22, 2021 RX CAPSULE, EXTENDED RELEASE ORAL Sept. 26, 2021 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER IC50 7.32 WOMBAT-PK CHEMBL
Voltage-dependent calcium channel gamma-1 subunit Ion channel IC50 6.10 WOMBAT-PK
Cytochrome P450 3A4 Enzyme IC50 5.74 DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 4.02 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR Ki 5.62 PDSP
Multidrug resistance protein 1 Transporter IC50 4.37 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.91 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.76 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1S Ion channel Ki 6.42 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.35 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel BLOCKER IC50 4.68 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 4.52 CHEMBL
Voltage-gated L-type calcium channel Ion channel Ki 7.80 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel IC50 7.34 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 7.27 CHEMBL
Potassium voltage-gated channel subfamily C member 1 Unclassified BLOCKER IC50 4 IUPHAR
Potassium voltage-gated channel subfamily A member 7 Unclassified BLOCKER IC50 4.20 IUPHAR
5-hydroxytryptamine receptor 3A Ion channel BLOCKER IC50 5.26 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1F Unclassified BLOCKER IC50 4 IUPHAR

External reference:

IDSource
4020128 VUID
N0000179650 NUI
D00616 KEGG_DRUG
33286-22-5 SECONDARY_CAS_RN
4018817 VANDF
4019722 VANDF
4020128 VANDF
C0012373 UMLSCUI
CHEBI:101278 CHEBI
C9F PDB_CHEM_ID
39186 PUBCHEM_CID
CHEMBL23 ChEMBL_ID
CHEMBL1697 ChEMBL_ID
CHEMBL1200805 ChEMBL_ID
DB00343 DRUGBANK_ID
D004110 MESH_DESCRIPTOR_UI
2298 IUPHAR_LIGAND_ID
3433 INN_ID
EE92BBP03H UNII
203211 RXNORM
1547 MMSL
4604 MMSL
d00045 MMSL
000711 NDDF
004514 NDDF
007237 NDDF
12218006 SNOMEDCT_US
372793000 SNOMEDCT_US
59941008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0318 TABLET, FILM COATED 30 mg ORAL ANDA 18 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0319 TABLET, FILM COATED 60 mg ORAL ANDA 18 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0320 TABLET, FILM COATED 90 mg ORAL ANDA 18 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0321 TABLET, FILM COATED 120 mg ORAL ANDA 18 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0771 TABLET, COATED 30 mg ORAL NDA 21 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0772 TABLET, COATED 60 mg ORAL NDA 21 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0791 TABLET, COATED 90 mg ORAL NDA 21 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0792 TABLET, COATED 120 mg ORAL NDA 21 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0795 CAPSULE, COATED, EXTENDED RELEASE 120 mg ORAL NDA 14 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0796 CAPSULE, COATED, EXTENDED RELEASE 180 mg ORAL NDA 14 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0797 CAPSULE, COATED, EXTENDED RELEASE 240 mg ORAL NDA 14 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0798 CAPSULE, COATED, EXTENDED RELEASE 300 mg ORAL NDA 14 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0799 CAPSULE, COATED, EXTENDED RELEASE 360 mg ORAL NDA 14 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2045 TABLET, EXTENDED RELEASE 120 mg ORAL NDA 25 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2046 TABLET, EXTENDED RELEASE 180 mg ORAL NDA 25 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2047 TABLET, EXTENDED RELEASE 240 mg ORAL NDA 25 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2048 TABLET, EXTENDED RELEASE 300 mg ORAL NDA 25 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2049 TABLET, EXTENDED RELEASE 360 mg ORAL NDA 25 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2050 TABLET, EXTENDED RELEASE 420 mg ORAL NDA 25 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2612 CAPSULE, EXTENDED RELEASE 120 mg ORAL NDA 23 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2613 CAPSULE, EXTENDED RELEASE 180 mg ORAL NDA 23 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2614 CAPSULE, EXTENDED RELEASE 240 mg ORAL NDA 23 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2615 CAPSULE, EXTENDED RELEASE 300 mg ORAL NDA 23 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2616 CAPSULE, EXTENDED RELEASE 360 mg ORAL NDA 23 sections
TIAZACEXTENDED RELEASE HUMAN PRESCRIPTION DRUG LABEL 1 0187-2617 CAPSULE, EXTENDED RELEASE 420 mg ORAL NDA 23 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2918 CAPSULE, EXTENDED RELEASE 360 mg ORAL ANDA 20 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-6060 CAPSULE, EXTENDED RELEASE 60 mg ORAL ANDA 20 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-6090 CAPSULE, EXTENDED RELEASE 90 mg ORAL ANDA 20 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-6120 CAPSULE, EXTENDED RELEASE 120 mg ORAL ANDA 20 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-1171 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 24 sections