calcitriol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Vitamin D analogues/derivatives 466 32222-06-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rocaltrol
  • calcitriol
  • Dihydroxyvitamin D3
  • topitriol
  • 1,25-dihydroxyvitamin D3
The physiologically active form of vitamin D. It is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (CALCIFEDIOL). Its production is stimulated by low blood calcium levels and parathyroid hormone. Calcitriol increases intestinal absorption of calcium and phosphorus, and in concert with parathyroid hormone increases bone resorption.
  • Molecular weight: 416.65
  • Formula: C27H44O3
  • CLOGP: 6.04
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 3
  • TPSA: 60.69
  • ALOGS: -4.80
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
1 mcg O
1 mcg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 61 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.25 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.31 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 11 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 17, 1978 FDA VALIDUS PHARMS

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
Recalled product 1059.89 11.57 216 23790 1172 56266889
Hypocalcaemia 689.20 11.57 305 23701 28455 56239606
Hypercalcaemia 475.35 11.57 227 23779 25184 56242877
Milk-alkali syndrome 227.20 11.57 54 23952 644 56267417
Peritonitis bacterial 180.35 11.57 70 23936 4663 56263398
Calciphylaxis 161.39 11.57 56 23950 2711 56265350
Blood calcium decreased 157.86 11.57 108 23898 23661 56244400
Tetany 150.06 11.57 47 23959 1645 56266416
Blood parathyroid hormone increased 132.49 11.57 49 23957 2856 56265205
Shunt stenosis 122.80 11.57 31 23975 482 56267579
Rheumatoid arthritis 115.25 11.57 14 23992 382590 55885471
Arteriovenous fistula site complication 114.05 11.57 29 23977 465 56267596
Blood calcium abnormal 105.44 11.57 33 23973 1152 56266909
Nephrocalcinosis 97.61 11.57 30 23976 985 56267076
Nephrogenic systemic fibrosis 92.98 11.57 43 23963 4422 56263639
Peritonitis 87.68 11.57 65 23941 16137 56251924
Hypoparathyroidism 83.72 11.57 24 23982 616 56267445
Hypercalciuria 82.13 11.57 20 23986 266 56267795
Shunt occlusion 80.73 11.57 23 23983 577 56267484
Renal failure 74.54 11.57 153 23853 110347 56157714
Chronic kidney disease 71.61 11.57 89 23917 41967 56226094
Blood calcium increased 68.65 11.57 43 23963 8111 56259950
Aplasia pure red cell 66.82 11.57 34 23972 4308 56263753
Acute kidney injury 65.15 11.57 238 23768 240525 56027536
Drug ineffective 63.03 11.57 193 23813 918796 55349265
Renal impairment 59.49 11.57 116 23890 80597 56187464
Systemic lupus erythematosus 50.80 11.57 8 23998 180070 56087991
Peritoneal dialysis complication 50.04 11.57 19 23987 1191 56266870
Infusion related reaction 49.31 11.57 14 23992 208917 56059144
Drug intolerance 48.91 11.57 26 23980 264792 56003269
Synovitis 48.24 11.57 6 24000 161299 56106762
Kidney transplant rejection 47.98 11.57 27 23979 4186 56263875
Hyperparathyroidism secondary 47.63 11.57 19 23987 1360 56266701
Glossodynia 47.27 11.57 5 24001 152453 56115608
Treatment failure 47.10 11.57 8 23998 170384 56097677
Contraindicated product administered 46.79 11.57 11 23995 186275 56081786
Blood creatinine increased 45.97 11.57 104 23902 80087 56187974
Completed suicide 45.30 11.57 3 24003 133830 56134231
Skin induration 44.61 11.57 23 23983 2995 56265066
Joint swelling 44.60 11.57 35 23971 289765 55978296
Arthropathy 44.42 11.57 15 23991 200260 56067801
Hyperphosphataemia 43.63 11.57 20 23986 2015 56266046
Renal transplant 41.63 11.57 17 23989 1293 56266768
Skin hypertrophy 40.47 11.57 22 23984 3188 56264873
Chronic kidney disease-mineral and bone disorder 39.64 11.57 11 23995 250 56267811
Hyperparathyroidism tertiary 39.32 11.57 7 23999 15 56268046
Blood phosphorus increased 37.73 11.57 20 23986 2756 56265305
Therapeutic product effect decreased 37.04 11.57 13 23993 169439 56098622
Anaemia 36.83 11.57 217 23789 267294 56000767
Hungry bone syndrome 33.76 11.57 8 23998 94 56267967
Brown tumour 33.72 11.57 7 23999 42 56268019
Hyperparathyroidism 33.34 11.57 18 23988 2574 56265487
Hospitalisation 32.11 11.57 87 23919 74913 56193148
Pulmonary renal syndrome 30.71 11.57 10 23996 397 56267664
Acute myocardial infarction 30.49 11.57 50 23956 30343 56237718
Pericarditis 30.34 11.57 5 24001 108918 56159143
Muscle spasms 29.95 11.57 127 23879 137244 56130817
Dialysis 29.69 11.57 28 23978 9674 56258387
Hypervitaminosis D 29.64 11.57 7 23999 81 56267980
Alopecia 29.39 11.57 50 23956 293408 55974653
Skin tightness 28.71 11.57 19 23987 3936 56264125
Pain 28.66 11.57 166 23840 663018 55605043
Hepatic enzyme increased 28.55 11.57 19 23987 171365 56096696
Fungal peritonitis 28.37 11.57 10 23996 507 56267554
Septic shock 27.48 11.57 72 23934 60763 56207298
Skin fibrosis 26.73 11.57 11 23995 853 56267208
Nephrolithiasis 26.69 11.57 53 23953 37282 56230779
Parathyroidectomy 26.53 11.57 8 23998 246 56267815
Peritoneal dialysis 26.17 11.57 9 23997 424 56267637
Lower respiratory tract infection 24.75 11.57 9 23997 114785 56153276
Hypervolaemia 24.51 11.57 42 23964 26416 56241645
Sinusitis 24.39 11.57 29 23977 197552 56070509
Metabolic alkalosis 23.91 11.57 15 23991 2836 56265225
Wound 23.64 11.57 15 23991 138789 56129272
End stage renal disease 23.37 11.57 20 23986 6091 56261970
Discomfort 23.23 11.57 16 23990 141745 56126316
Swelling 22.96 11.57 42 23964 239729 56028332
Haemodialysis 22.92 11.57 23 23983 8568 56259493
Abdominal discomfort 22.80 11.57 53 23953 277221 55990840
Anti-erythropoietin antibody positive 22.78 11.57 8 23998 401 56267660
Coagulation test abnormal 21.69 11.57 9 23997 713 56267348
Blood urea increased 21.56 11.57 38 23968 24435 56243626
Product use issue 21.21 11.57 29 23977 186012 56082049
Maternal exposure during pregnancy 20.18 11.57 31 23975 189522 56078539
Arthralgia 19.83 11.57 129 23877 501540 55766521
Blood potassium increased 19.52 11.57 30 23976 17231 56250830
Diabetic foot 19.29 11.57 10 23996 1317 56266744
Azotaemia 18.81 11.57 15 23991 4143 56263918
Hypertension 18.52 11.57 172 23834 244106 56023955
Hypoglycaemia 18.39 11.57 59 23947 55756 56212305
Vascular parkinsonism 18.30 11.57 5 24001 107 56267954
Calcinosis 17.93 11.57 11 23995 1999 56266062
Rash 17.41 11.57 131 23875 492916 55775145
Arrhythmia 17.37 11.57 43 23963 35040 56233021
Irritable bowel syndrome 17.26 11.57 4 24002 68454 56199607
Intentional overdose 17.13 11.57 4 24002 68113 56199948
Impaired healing 16.79 11.57 8 23998 86833 56181228
Drug hypersensitivity 16.65 11.57 185 23821 275020 55993041
Parathyroid disorder 16.64 11.57 7 23999 574 56267487
Daydreaming 16.60 11.57 6 24000 327 56267734
Alveolar bone resorption 16.58 11.57 4 24002 51 56268010
Haemoglobin decreased 16.02 11.57 105 23901 134032 56134029
Diffuse alopecia 15.98 11.57 7 23999 634 56267427
Electrolyte imbalance 15.88 11.57 28 23978 18005 56250056
Asthenia 15.78 11.57 219 23787 342754 55925307
Urine calcium increased 15.74 11.57 4 24002 64 56267997
Off label use 15.54 11.57 157 23849 556023 55712038
Mental status changes 15.54 11.57 43 23963 37458 56230603
Paraesthesia 15.49 11.57 102 23904 130412 56137649
Staphylococcal infection 15.45 11.57 43 23963 37575 56230486
Renal tubular necrosis 15.43 11.57 21 23985 10807 56257254
Anti-neutrophil cytoplasmic antibody positive vasculitis 15.42 11.57 11 23995 2572 56265489
Product supply issue 15.40 11.57 9 23997 1497 56266564
Blood magnesium decreased 15.39 11.57 22 23984 11852 56256209
Sepsis 15.23 11.57 107 23899 139733 56128328
Arteriovenous fistula thrombosis 15.20 11.57 5 24001 205 56267856
Drug abuse 15.08 11.57 5 24001 67605 56200456
Papillary thyroid cancer 14.92 11.57 10 23996 2114 56265947
Gastrointestinal haemorrhage 14.85 11.57 68 23938 75883 56192178
Therapeutic product effect incomplete 14.82 11.57 14 23992 106017 56162044
Bone pain 14.71 11.57 51 23955 50134 56217927
Hypersensitivity 14.63 11.57 58 23948 256350 56011711
Nephropathy toxic 14.43 11.57 18 23988 8509 56259552
Hypocalcaemic seizure 13.81 11.57 3 24003 23 56268038
Cerebral infarction 13.80 11.57 30 23976 22475 56245586
Nephrotic syndrome 13.79 11.57 14 23992 5286 56262775
Unresponsive to stimuli 13.77 11.57 37 23969 31688 56236373
Iron deficiency 13.57 11.57 15 23991 6241 56261820
Simple partial seizures 13.57 11.57 6 24000 555 56267506
Urosepsis 13.50 11.57 25 23981 16691 56251370
Gingival hypertrophy 13.15 11.57 8 23998 1432 56266629
Urinary tract infection 12.90 11.57 158 23848 240355 56027706
Vomiting 12.81 11.57 290 23716 497938 55770123
Encapsulating peritoneal sclerosis 12.79 11.57 5 24001 339 56267722
Cardio-respiratory arrest 12.71 11.57 52 23954 55269 56212792
Catarrh 12.40 11.57 5 24001 368 56267693
International normalised ratio increased 12.25 11.57 44 23962 43997 56224064
Cerebral calcification 12.14 11.57 4 24002 165 56267896
Cardiac arrest 11.83 11.57 70 23936 86244 56181817
Incision site impaired healing 11.74 11.57 4 24002 183 56267878
Suicide attempt 11.69 11.57 5 24001 57831 56210230
Suicidal ideation 11.66 11.57 5 24001 57737 56210324
Bloody peritoneal effluent 11.58 11.57 3 24003 52 56268009

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
Appendicolith 269.87 13.06 112 21131 5619 31670482
Appendicitis 223.31 13.06 122 21121 11343 31664758
Peritonitis bacterial 196.09 13.06 90 21153 5762 31670339
Hypocalcaemia 157.33 13.06 125 21118 21853 31654248
Cardiogenic shock 150.96 13.06 123 21120 22285 31653816
Shunt stenosis 136.52 13.06 40 21203 693 31675408
Stress 133.51 13.06 120 21123 24821 31651280
Blood parathyroid hormone increased 133.33 13.06 46 21197 1376 31674725
Hypercalcaemia 129.87 13.06 93 21150 13907 31662194
Arteriovenous fistula site complication 129.15 13.06 34 21209 388 31675713
Shunt occlusion 123.06 13.06 38 21205 793 31675308
Blood phosphorus increased 110.90 13.06 56 21187 4426 31671675
Ascites 102.87 13.06 132 21111 40881 31635220
Abdominal distension 98.25 13.06 144 21099 50540 31625561
Nephrocalcinosis 91.70 13.06 28 21215 562 31675539
Recalled product 79.30 13.06 22 21221 310 31675791
Ventricular fibrillation 74.92 13.06 77 21166 18771 31657330
General physical health deterioration 73.78 13.06 204 21039 113231 31562870
Multiple organ dysfunction syndrome 71.85 13.06 148 21095 68055 31608046
Nephrogenic systemic fibrosis 71.25 13.06 40 21203 3915 31672186
Hypercalciuria 67.20 13.06 19 21224 288 31675813
Peritonitis 67.12 13.06 66 21177 15261 31660840
Peritoneal dialysis complication 66.96 13.06 29 21214 1615 31674486
Aplasia pure red cell 64.70 13.06 43 21200 5694 31670407
Abdominal pain 61.47 13.06 226 21017 145726 31530375
Vomiting 60.49 13.06 303 20940 223670 31452431
Chronic kidney disease 58.36 13.06 97 21146 37878 31638223
Drug hypersensitivity 54.71 13.06 138 21105 72461 31603640
Drug ineffective 54.59 13.06 115 21128 395458 31280643
Sepsis 53.99 13.06 223 21020 151706 31524395
Mean platelet volume increased 53.60 13.06 18 21225 495 31675606
Hyperparathyroidism secondary 53.15 13.06 24 21219 1477 31674624
Hospitalisation 51.15 13.06 107 21136 49700 31626401
Hyperparathyroidism 48.66 13.06 21 21222 1159 31674942
Constipation 48.03 13.06 187 21056 123804 31552297
Hypervolaemia 47.71 13.06 60 21183 18191 31657910
Zoonotic bacterial infection 45.37 13.06 10 21233 49 31676052
Hyponatraemia 41.43 13.06 126 21117 73673 31602428
Ventricular hyperkinesia 41.21 13.06 12 21231 203 31675898
Hypochromasia 41.03 13.06 13 21230 296 31675805
Mycobacterium marinum infection 40.98 13.06 13 21230 297 31675804
Calciphylaxis 40.40 13.06 18 21225 1073 31675028
Right atrial enlargement 39.96 13.06 12 21231 227 31675874
Nephrectomy 39.61 13.06 16 21227 747 31675354
Mycobacterium test positive 38.05 13.06 13 21230 377 31675724
Mitral valve thickening 34.37 13.06 12 21231 372 31675729
Tendon calcification 32.83 13.06 8 21235 65 31676036
Blood calcium decreased 32.77 13.06 36 21207 9458 31666643
Lung diffusion test decreased 32.68 13.06 13 21230 583 31675518
Hyperphosphataemia 31.65 13.06 20 21223 2429 31673672
Blood creatinine increased 30.99 13.06 130 21113 88948 31587153
Febrile neutropenia 30.89 13.06 22 21221 121827 31554274
Nausea 29.30 13.06 325 20918 307622 31368479
Haemoglobin decreased 28.59 13.06 150 21093 112525 31563576
Narrow anterior chamber angle 28.50 13.06 8 21235 118 31675983
Left ventricular enlargement 27.71 13.06 12 21231 668 31675433
Calcinosis 27.42 13.06 12 21231 685 31675416
Skin induration 27.05 13.06 17 21226 2045 31674056
Carotid arteriosclerosis 26.93 13.06 16 21227 1741 31674360
Completed suicide 26.70 13.06 14 21229 91500 31584601
Shunt infection 26.42 13.06 7 21236 82 31676019
Hypertensive heart disease 26.18 13.06 17 21226 2164 31673937
Left atrial enlargement 26.06 13.06 12 21231 773 31675328
Hypophosphatasia 25.40 13.06 6 21237 42 31676059
Anti-erythropoietin antibody positive 24.96 13.06 12 21231 852 31675249
Blood uric acid increased 23.47 13.06 25 21218 6345 31669756
Peripheral arterial occlusive disease 23.40 13.06 23 21220 5310 31670791
Skin fibrosis 23.15 13.06 12 21231 1001 31675100
Haemodialysis 23.09 13.06 31 21212 10014 31666087
Chronic kidney disease-mineral and bone disorder 23.03 13.06 9 21234 385 31675716
Blood urea increased 22.71 13.06 56 21187 28956 31647145
Skin tightness 22.27 13.06 15 21228 2029 31674072
Renal transplant 22.27 13.06 14 21229 1685 31674416
Blood iron decreased 22.04 13.06 21 21222 4669 31671432
Granuloma 21.73 13.06 17 21226 2900 31673201
Joint contracture 21.51 13.06 14 21229 1789 31674312
Hypophosphataemia 20.68 13.06 27 21216 8487 31667614
Hypervitaminosis D 20.53 13.06 4 21239 9 31676092
Haematocrit decreased 20.41 13.06 55 21188 30006 31646095
Blood chloride increased 20.22 13.06 16 21227 2775 31673326
Renal transplant failure 20.15 13.06 11 21232 1019 31675082
Dry mouth 19.99 13.06 48 21195 24410 31651691
Skin hypertrophy 19.75 13.06 15 21228 2450 31673651
Bronchiolitis 19.66 13.06 16 21227 2888 31673213
Lymphocyte count decreased 19.61 13.06 43 21200 20606 31655495
Proteinuria 19.56 13.06 38 21205 16725 31659376
Toxicity to various agents 18.62 13.06 61 21182 181426 31494675
Red cell distribution width increased 17.71 13.06 20 21223 5414 31670687
Interstitial granulomatous dermatitis 17.56 13.06 6 21237 174 31675927
Electrocardiogram T wave inversion 17.54 13.06 13 21230 2047 31674054
Milk-alkali syndrome 17.30 13.06 8 21235 520 31675581
Porphyria acute 17.20 13.06 7 21236 333 31675768
Obstruction 17.14 13.06 13 21230 2119 31673982
Interstitial lung disease 17.03 13.06 10 21233 61393 31614708
Parathyroidectomy 16.99 13.06 5 21238 88 31676013
Hungry bone syndrome 16.93 13.06 5 21238 89 31676012
Blood 1,25-dihydroxycholecalciferol decreased 16.85 13.06 3 21240 3 31676098
Hepatic cyst infection 16.81 13.06 4 21239 29 31676072
Lens dislocation 16.34 13.06 5 21238 101 31676000
Fibrosis 15.74 13.06 13 21230 2396 31673705
Blood erythropoietin decreased 15.63 13.06 3 21240 6 31676095
Intestinal prolapse 15.61 13.06 5 21238 118 31675983
Pyelonephritis 15.42 13.06 19 21224 5637 31670464
Arteriovenous fistula occlusion 14.94 13.06 5 21238 136 31675965
Kidney transplant rejection 14.53 13.06 21 21222 7261 31668840
Bone deformity 14.44 13.06 4 21239 56 31676045
Rheumatoid arthritis 14.41 13.06 7 21236 47802 31628299
Reticulocyte count abnormal 14.31 13.06 3 21240 11 31676090
Blood alkaline phosphatase decreased 14.14 13.06 8 21235 794 31675307
Arthralgia 14.11 13.06 53 21190 151371 31524730
Zoonosis 14.11 13.06 3 21240 12 31676089
Cardiac arrest 14.04 13.06 105 21138 88957 31587144
Mucosal inflammation 13.96 13.06 3 21240 34424 31641677
Renal cyst 13.59 13.06 22 21221 8394 31667707
Potentiating drug interaction 13.57 13.06 16 21227 4537 31671564
Serum ferritin increased 13.50 13.06 18 21225 5774 31670327
Insomnia 13.47 13.06 27 21216 94809 31581292
Product use issue 13.41 13.06 11 21232 56748 31619353
Arteriovenous fistula site infection 13.25 13.06 4 21239 77 31676024
Azotaemia 13.18 13.06 16 21227 4676 31671425
Diastolic dysfunction 13.09 13.06 17 21226 5318 31670783

FDA Adverse Event Reporting System (Geriatric)

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
Hypocalcaemia 454.35 11.22 287 37053 44572 70846532
Hypercalcaemia 449.03 11.22 259 37081 34126 70856978
Recalled product 388.56 11.22 92 37248 856 70890248
Peritonitis bacterial 343.04 11.22 142 37198 9042 70882062
Appendicolith 293.32 11.22 111 37229 5569 70885535
Shunt stenosis 258.68 11.22 71 37269 1241 70889863
Arteriovenous fistula site complication 234.72 11.22 61 37279 856 70890248
Milk-alkali syndrome 213.26 11.22 60 37280 1153 70889951
Appendicitis 205.00 11.22 121 37219 16612 70874492
Shunt occlusion 186.70 11.22 56 37284 1359 70889745
Blood parathyroid hormone increased 166.19 11.22 63 37277 3174 70887930
Calciphylaxis 161.88 11.22 63 37277 3410 70887694
Peritonitis 140.86 11.22 114 37226 26045 70865059
Cardiogenic shock 140.43 11.22 131 37209 36176 70854928
Blood phosphorus increased 133.18 11.22 67 37273 6703 70884401
Nephrocalcinosis 116.51 11.22 39 37301 1362 70889742
Nephrogenic systemic fibrosis 116.43 11.22 59 37281 5993 70885111
Rheumatoid arthritis 111.29 11.22 12 37328 291793 70599311
Chronic kidney disease 99.78 11.22 141 37199 60916 70830188
Hospitalisation 97.43 11.22 164 37176 82404 70808700
Drug ineffective 95.84 11.22 222 37118 939530 69951574
Blood calcium decreased 94.46 11.22 95 37245 28751 70862353
Peritoneal dialysis complication 90.82 11.22 37 37303 2259 70888845
Ascites 88.94 11.22 141 37199 67406 70823698
Aplasia pure red cell 86.85 11.22 52 37288 7322 70883782
Sepsis 80.40 11.22 297 37043 244248 70646856
Tetany 77.94 11.22 33 37307 2221 70888883
Stress 77.53 11.22 133 37207 67833 70823271
Hyperparathyroidism secondary 77.14 11.22 34 37306 2524 70888580
Multiple organ dysfunction syndrome 74.89 11.22 172 37168 108343 70782761
Abdominal distension 74.56 11.22 168 37172 104501 70786603
Drug hypersensitivity 71.11 11.22 300 37040 262159 70628945
Completed suicide 69.55 11.22 17 37323 227118 70663986
Ventricular fibrillation 68.80 11.22 78 37262 27033 70864071
Hypercalciuria 66.60 11.22 20 37320 487 70890617
Drug abuse 58.89 11.22 5 37335 147251 70743853
Skin induration 57.74 11.22 33 37307 4262 70886842
Chronic kidney disease-mineral and bone disorder 57.10 11.22 19 37321 651 70890453
Hyperparathyroidism 56.56 11.22 29 37311 3018 70888086
Blood creatinine increased 55.88 11.22 184 37156 142817 70748287
General physical health deterioration 54.99 11.22 258 37082 235773 70655331
Hypervolaemia 52.41 11.22 83 37257 39623 70851481
Vomiting 52.01 11.22 508 36832 592603 70298501
Renal impairment 50.79 11.22 179 37161 143758 70747346
Synovitis 50.03 11.22 5 37335 129223 70761881
Hyperphosphataemia 49.96 11.22 30 37310 4246 70886858
Drug intolerance 49.02 11.22 29 37311 225658 70665446
Renal transplant 48.05 11.22 24 37316 2364 70888740
Infusion related reaction 47.91 11.22 22 37318 197512 70693592
Joint swelling 47.73 11.22 38 37302 253173 70637931
Skin hypertrophy 47.62 11.22 30 37310 4622 70886482
Zoonotic bacterial infection 46.22 11.22 10 37330 59 70891045
Hungry bone syndrome 45.30 11.22 12 37328 182 70890922
Renal failure 45.00 11.22 208 37132 188862 70702242
Mycobacterium marinum infection 43.11 11.22 14 37326 444 70890660
Kidney transplant rejection 42.52 11.22 38 37302 9923 70881181
Blood calcium increased 41.78 11.22 36 37304 8957 70882147
Calcinosis 41.70 11.22 21 37319 2104 70889000
Mean platelet volume increased 41.46 11.22 17 37323 1055 70890049
Abdominal pain 41.44 11.22 315 37025 341812 70549292
Ventricular hyperkinesia 41.24 11.22 12 37328 261 70890843
Blood calcium abnormal 40.95 11.22 18 37322 1327 70889777
Treatment failure 40.00 11.22 13 37327 144129 70746975
Parathyroidectomy 39.87 11.22 11 37329 196 70890908
Hyponatraemia 39.48 11.22 178 37162 159909 70731195
Skin fibrosis 39.48 11.22 18 37322 1447 70889657
Hyperparathyroidism tertiary 39.24 11.22 7 37333 11 70891093
Haemodialysis 39.11 11.22 47 37293 17319 70873785
Hypoparathyroidism 38.94 11.22 16 37324 998 70890106
Right atrial enlargement 38.79 11.22 12 37328 324 70890780
Skin tightness 38.06 11.22 27 37313 5063 70886041
Intentional overdose 37.61 11.22 4 37336 98431 70792673
Contraindicated product administered 37.60 11.22 12 37328 134600 70756504
Blood urea increased 37.60 11.22 78 37262 45831 70845273
Brown tumour 37.45 11.22 8 37332 44 70891060
Mitral valve thickening 36.38 11.22 12 37328 400 70890704
Mycobacterium test positive 36.12 11.22 12 37328 409 70890695
Arthralgia 35.24 11.22 141 37199 503249 70387855
Arthropathy 34.42 11.22 18 37322 150039 70741065
Hypochromasia 34.17 11.22 13 37327 661 70890443
Tendon calcification 33.82 11.22 9 37331 139 70890965
Toxicity to various agents 33.57 11.22 97 37243 382075 70509029
End stage renal disease 33.42 11.22 35 37305 11098 70880006
Dialysis 32.66 11.22 43 37297 17359 70873745
Systemic lupus erythematosus 32.42 11.22 7 37333 101895 70789209
Alopecia 32.39 11.22 34 37306 198456 70692648
Hand deformity 31.82 11.22 4 37336 86478 70804626
Hypervitaminosis D 31.63 11.22 8 37332 100 70891004
Sinusitis 31.11 11.22 26 37314 169169 70721935
Peripheral arterial occlusive disease 30.78 11.22 28 37312 7481 70883623
Hepatic enzyme increased 30.28 11.22 23 37317 156967 70734137
Left ventricular enlargement 29.92 11.22 12 37328 703 70890401
Blood uric acid increased 29.76 11.22 30 37310 9099 70882005
Constipation 29.74 11.22 231 37109 252207 70638897
Glossodynia 29.51 11.22 5 37335 86482 70804622
Febrile neutropenia 29.06 11.22 39 37301 204279 70686825
Therapeutic product effect decreased 28.82 11.22 20 37320 142998 70748106
Suicide attempt 28.49 11.22 4 37336 79506 70811598
Left atrial enlargement 28.42 11.22 13 37327 1053 70890051
Acute myocardial infarction 27.74 11.22 93 37247 72794 70818310
Narrow anterior chamber angle 27.72 11.22 8 37332 169 70890935
Shunt infection 27.72 11.22 8 37332 169 70890935
Hypertensive heart disease 27.51 11.22 20 37320 3896 70887208
Nephrectomy 27.36 11.22 15 37325 1788 70889316
Anti-erythropoietin antibody positive 26.74 11.22 11 37329 688 70890416
Cardiac arrest 26.40 11.22 159 37181 159675 70731429
Diabetic foot 26.36 11.22 18 37322 3176 70887928
Proteinuria 25.34 11.22 51 37289 29323 70861781
Fungal peritonitis 25.25 11.22 12 37328 1060 70890044
Hypophosphatasia 25.13 11.22 6 37334 58 70891046
Pulmonary renal syndrome 25.10 11.22 10 37330 576 70890528
Peritoneal dialysis 25.01 11.22 11 37329 812 70890292
Hypophosphataemia 24.17 11.22 36 37304 16290 70874814
Anaemia 24.13 11.22 321 37019 403102 70488002
Suicidal ideation 23.79 11.22 4 37336 69592 70821512
Joint contracture 23.77 11.22 15 37325 2317 70888787
Lung diffusion test decreased 23.55 11.22 12 37328 1233 70889871
Pain 23.43 11.22 215 37125 628601 70262503
Carotid arteriosclerosis 23.23 11.22 15 37325 2412 70888692
Haemoglobin decreased 23.19 11.22 186 37154 204973 70686131
Product use issue 22.99 11.22 37 37303 179900 70711204
Pericarditis 22.87 11.22 8 37332 84697 70806407
Rash 21.50 11.22 169 37171 510393 70380711
Therapeutic product effect incomplete 21.33 11.22 19 37321 119863 70771241
Azotaemia 20.85 11.22 23 37317 7730 70883374
Renal cyst 20.58 11.22 30 37310 13315 70877789
Blood erythropoietin decreased 20.42 11.22 4 37336 13 70891091
Swelling 20.33 11.22 43 37297 188496 70702608
High density lipoprotein decreased 20.18 11.22 17 37323 4102 70887002
Hypersensitivity 19.67 11.22 59 37281 229753 70661351
Renal transplant failure 19.61 11.22 12 37328 1756 70889348
Helicobacter infection 19.47 11.22 3 37337 55653 70835451
Hepatic cyst infection 19.15 11.22 6 37334 169 70890935
Hypertension 19.14 11.22 239 37101 295794 70595310
Arteriovenous fistula site infection 18.92 11.22 6 37334 176 70890928
Nausea 18.90 11.22 584 36756 851504 70039600
Arteriovenous fistula occlusion 18.86 11.22 8 37332 541 70890563
Arteriovenous fistula thrombosis 18.81 11.22 8 37332 544 70890560
Cerebral calcification 18.57 11.22 6 37334 187 70890917
Metabolic alkalosis 18.16 11.22 16 37324 4100 70887004
Gastrointestinal haemorrhage 18.00 11.22 129 37211 137279 70753825
Pulmonary calcification 17.91 11.22 7 37333 383 70890721
Acute kidney injury 17.62 11.22 349 36991 474275 70416829
Haematocrit decreased 17.48 11.22 68 37272 57190 70833914
Blood chloride increased 17.48 11.22 17 37323 4936 70886168
Blood potassium increased 17.40 11.22 42 37298 27284 70863820
Vascular parkinsonism 17.40 11.22 5 37335 104 70891000
Interstitial granulomatous dermatitis 17.36 11.22 6 37334 231 70890873
Blood alkaline phosphatase decreased 17.32 11.22 11 37329 1718 70889386
Mucosal inflammation 17.32 11.22 7 37333 67843 70823261
Bronchiolitis 17.18 11.22 15 37325 3799 70887305
Electrolyte imbalance 16.80 11.22 41 37299 26820 70864284
Urosepsis 16.54 11.22 38 37302 23911 70867193
Serum ferritin increased 16.51 11.22 22 37318 8983 70882121
Lens dislocation 16.23 11.22 5 37335 133 70890971
Fatigue 16.04 11.22 322 37018 823997 70067107
Psoriatic arthropathy 16.03 11.22 7 37333 64764 70826340
Granuloma 15.99 11.22 20 37320 7675 70883429
Nephrogenic anaemia 15.83 11.22 14 37326 3604 70887500
Encapsulating peritoneal sclerosis 15.63 11.22 8 37332 829 70890275
Neutropenia 15.55 11.22 76 37264 257080 70634024
Coagulation test abnormal 15.47 11.22 9 37331 1201 70889903
Asthma 15.27 11.22 25 37315 120768 70770336
Hypocalcaemic seizure 15.27 11.22 4 37336 58 70891046
Bloody peritoneal effluent 15.23 11.22 5 37335 164 70890940
Blood iron decreased 15.17 11.22 26 37314 13235 70877869
Irritable bowel syndrome 15.17 11.22 4 37336 50846 70840258
Staphylococcal infection 15.16 11.22 62 37278 53342 70837762
Refractory cytopenia with unilineage dysplasia 15.09 11.22 8 37332 892 70890212
Complications of transplanted kidney 14.93 11.22 17 37323 5917 70885187
Pyelonephritis 14.88 11.22 31 37309 18258 70872846
Drug reaction with eosinophilia and systemic symptoms 14.79 11.22 6 37334 58007 70833097
Diffuse alopecia 14.48 11.22 7 37333 642 70890462
Cognitive disorder 14.44 11.22 7 37333 60949 70830155
Alveolar bone resorption 14.41 11.22 4 37336 73 70891031
Nephrolithiasis 14.28 11.22 56 37284 47267 70843837
Zoonosis 14.28 11.22 3 37337 15 70891089
Low turnover osteopathy 14.11 11.22 10 37330 1872 70889232
Musculoskeletal stiffness 14.07 11.22 36 37304 147724 70743380
Graft thrombosis 13.97 11.22 6 37334 418 70890686
Anti-erythropoietin antibody 13.82 11.22 3 37337 18 70891086
Parathyroid tumour benign 13.82 11.22 7 37333 710 70890394
Urine protein/creatinine ratio increased 13.81 11.22 8 37332 1060 70890044
Obstruction 13.80 11.22 13 37327 3628 70887476
Unresponsive to stimuli 13.74 11.22 59 37281 51872 70839232
Peripheral swelling 13.68 11.22 71 37269 236492 70654612
Electrocardiogram T wave inversion 13.66 11.22 15 37325 5016 70886088
Blood 1,25-dihydroxycholecalciferol decreased 13.55 11.22 3 37337 20 70891084
Blister 13.47 11.22 20 37320 100506 70790598
Cardio-respiratory arrest 13.46 11.22 95 37245 100582 70790522
Injection site pain 13.38 11.22 26 37314 117593 70773511
Gangrene 13.28 11.22 19 37321 8290 70882814
Intentional product use issue 13.28 11.22 27 37313 120115 70770989
Nasopharyngitis 13.24 11.22 66 37274 222140 70668964
Hypoglycaemia 13.18 11.22 90 37250 94274 70796830
Lumbar vertebral fracture 13.15 11.22 16 37324 5971 70885133
Hepatocellular injury 13.06 11.22 4 37336 46087 70845017
Peritoneal cloudy effluent 13.00 11.22 5 37335 262 70890842
Injection site reaction 12.96 11.22 5 37335 49847 70841257
Wound 12.89 11.22 20 37320 98712 70792392
Cardiac valve disease 12.80 11.22 15 37325 5383 70885721
Lymphocyte count decreased 12.72 11.22 51 37289 43488 70847616
Growth retardation 12.71 11.22 9 37331 1683 70889421
Coma 12.58 11.22 18 37322 91826 70799278
Sleep disorder 12.51 11.22 11 37329 69861 70821243
Stomatitis 12.48 11.22 31 37309 128480 70762624
Urticaria 12.46 11.22 44 37296 163005 70728099
Blood triglycerides increased 12.28 11.22 30 37310 19634 70871470
Fibrosis 12.28 11.22 14 37326 4880 70886224
Infarction 12.14 11.22 13 37327 4229 70886875
Fibromyalgia 12.12 11.22 5 37335 47869 70843235
Potentiating drug interaction 12.08 11.22 18 37322 8146 70882958
Angina pectoris 12.06 11.22 54 37286 48329 70842775
Bone deformity 11.99 11.22 5 37335 324 70890780
Breast induration 11.83 11.22 3 37337 38 70891066
Neutrophil count decreased 11.82 11.22 16 37324 83540 70807564
Weight increased 11.73 11.22 77 37263 242254 70648850
Sedation 11.64 11.22 5 37335 46726 70844378
Intestinal prolapse 11.63 11.22 4 37336 152 70890952
Electrocardiogram ST segment elevation 11.59 11.22 17 37323 7587 70883517
Dyslalia 11.55 11.22 7 37333 1007 70890097
Fanconi syndrome acquired 11.50 11.22 10 37330 2517 70888587
Bone pain 11.40 11.22 55 37285 50767 70840337
Blood parathyroid hormone abnormal 11.38 11.22 5 37335 368 70890736
Oxygen saturation decreased 11.37 11.22 28 37312 116401 70774703
Malignant neoplasm progression 11.33 11.22 30 37310 121709 70769395
Medullary thyroid cancer 11.31 11.22 4 37336 165 70890939
Apparent mineralocorticoid excess 11.29 11.22 3 37337 46 70891058
Paraesthesia oral 11.25 11.22 25 37315 15392 70875712

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A11CC04 ALIMENTARY TRACT AND METABOLISM
VITAMINS
VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO
Vitamin D and analogues
ATC D05AX03 DERMATOLOGICALS
ANTIPSORIATICS
ANTIPSORIATICS FOR TOPICAL USE
Other antipsoriatics for topical use
FDA CS M0004229 Cholecalciferol
MeSH PA D050071 Bone Density Conservation Agents
MeSH PA D002120 Calcium Channel Agonists
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018977 Micronutrients
MeSH PA D014662 Vasoconstrictor Agents
MeSH PA D014815 Vitamins
FDA EPC N0000175908 Vitamin D3 Analog
CHEBI has role CHEBI:24621 hormones
CHEBI has role CHEBI:25212 metabolites
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:38807 calcium channel agonists
CHEBI has role CHEBI:38808 calcium channel modulators
CHEBI has role CHEBI:50646 antiosteoporotic
CHEBI has role CHEBI:50733 Dietary Supplement
CHEBI has role CHEBI:50748 antipsoriatic drug
CHEBI has role CHEBI:50846 Immunologic factor
CHEBI has role CHEBI:75771 Mus musculus metabolites
CHEBI has role CHEBI:77746 Homo sapiens metabolite

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypophosphatemia indication 4996001
Hypocalcemia indication 5291005
Renal osteodystrophy indication 16726004 DOID:13068
Hypoparathyroidism indication 36976004 DOID:11199
Plaque psoriasis indication 200965009
Hyperparathyroidism Secondary to Chronic Renal Failure indication
Hypocalcemia from End-Stage Renal Disease with Dialysis indication
Neonatal hypocalcemic tetany off-label use 18442000
Vitamin D deficiency off-label use 34713006
Rickets off-label use 41345002 DOID:10609
Familial x-linked hypophosphatemic vitamin D refractory rickets off-label use 82236004
Vitamin D Dependent Rickets off-label use
Hyperphosphatemia contraindication 20165001 DOID:0050459
Hypervitaminosis D contraindication 27712000 DOID:9971
Sarcoidosis contraindication 31541009 DOID:11335
Hypercalcemia contraindication 66931009 DOID:12678
Kidney disease contraindication 90708001 DOID:557
Kidney stone contraindication 95570007
Arteriosclerosis obliterans contraindication 361133006 DOID:5160
Hypercalcemia associated with Sarcoidosis contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.7 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3MCG/GM VECTICAL GALDERMA LABS LP N022087 Jan. 23, 2009 RX OINTMENT TOPICAL July 17, 2023 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vitamin D3 receptor Nuclear hormone receptor AGONIST EC50 8.40 WOMBAT-PK CHEMBL
Vitamin D 25-hydroxylase Enzyme WOMBAT-PK
Vitamin D-binding protein Secreted Kd 7.62 CHEMBL
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial Enzyme WOMBAT-PK
Vitamin D3 receptor Transcription factor Ki 10.30 CHEMBL
Vitamin D3 receptor Transcription factor Ki 10.60 CHEMBL
Vitamin D3 receptor Transcription factor EC50 10.30 CHEMBL
Vitamin D3 receptor Nuclear hormone receptor Kd 10.15 CHEMBL
Vitamin D3 receptor A Nuclear hormone receptor EC50 8.26 CHEMBL
Vitamin D3 receptor Nuclear hormone receptor EC50 7 CHEMBL

External reference:

IDSource
4017800 VUID
N0000146161 NUI
D00129 KEGG_DRUG
152323 RXNORM
4017800 VANDF
4021906 VANDF
C0006674 UMLSCUI
CHEBI:17823 CHEBI
VDX PDB_CHEM_ID
CHEMBL846 ChEMBL_ID
D002117 MESH_DESCRIPTOR_UI
DB00136 DRUGBANK_ID
5280453 PUBCHEM_CID
C118756 MESH_SUPPLEMENTAL_RECORD_UI
2779 IUPHAR_LIGAND_ID
4393 INN_ID
FXC9231JVH UNII
1311 MMSL
42410 MMSL
4324 MMSL
d03126 MMSL
001017 NDDF
259333003 SNOMEDCT_US
68206008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0007 CAPSULE 0.25 ug ORAL ANDA 22 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0007 CAPSULE 0.25 ug ORAL ANDA 22 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0054-3120 SOLUTION 1 ug ORAL ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0054-3120 SOLUTION 1 ug ORAL ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7352 CAPSULE, LIQUID FILLED 0.25 ug ORAL ANDA 26 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7352 CAPSULE, LIQUID FILLED 0.25 ug ORAL ANDA 26 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7353 CAPSULE, LIQUID FILLED 0.50 ug ORAL ANDA 26 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0093-7353 CAPSULE, LIQUID FILLED 0.50 ug ORAL ANDA 26 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 0143-9728 INJECTION 1 ug INTRAVENOUS ANDA 24 sections
Vectical HUMAN PRESCRIPTION DRUG LABEL 1 0299-2012 OINTMENT 3 ug TOPICAL NDA 26 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-831 INJECTION 1 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-831 INJECTION 1 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-931 INJECTION 1 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-931 INJECTION 1 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-932 INJECTION 2 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17478-932 INJECTION 2 ug INTRAVENOUS ANDA 23 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17856-0723 CAPSULE 0.25 ug ORAL ANDA 21 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 17856-3120 SOLUTION 1 ug ORAL ANDA 25 sections
CALCITRIOL HUMAN PRESCRIPTION DRUG LABEL 1 23155-662 CAPSULE 0.25 ug ORAL ANDA 21 sections
CALCITRIOL HUMAN PRESCRIPTION DRUG LABEL 1 23155-663 CAPSULE 0.50 ug ORAL ANDA 21 sections
Rocaltrol HUMAN PRESCRIPTION DRUG LABEL 1 30698-143 CAPSULE, GELATIN COATED 0.25 ug ORAL NDA 24 sections
Rocaltrol HUMAN PRESCRIPTION DRUG LABEL 1 30698-144 CAPSULE, GELATIN COATED 0.50 ug ORAL NDA 24 sections
Rocaltrol HUMAN PRESCRIPTION DRUG LABEL 1 30698-911 SOLUTION 1 ug ORAL NDA 24 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 43353-034 CAPSULE 0.25 ug ORAL ANDA 26 sections
CALCITRIOL HUMAN PRESCRIPTION DRUG LABEL 1 43353-138 CAPSULE 0.25 ug ORAL NDA authorized generic 26 sections
Rocaltrol HUMAN PRESCRIPTION DRUG LABEL 1 43353-633 CAPSULE, GELATIN COATED 0.25 ug ORAL NDA 22 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 43353-998 CAPSULE, LIQUID FILLED 0.25 ug ORAL ANDA 25 sections
calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 45802-608 OINTMENT 3 ug TOPICAL NDA 25 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 51407-169 CAPSULE, LIQUID FILLED 0.25 ug ORAL ANDA 24 sections
Calcitriol HUMAN PRESCRIPTION DRUG LABEL 1 51407-169 CAPSULE, LIQUID FILLED 0.25 ug ORAL ANDA 24 sections