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

Stem definitionDrug idCAS RN
Vitamin D analogues/derivatives 130 41294-56-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alfacalcidol
  • 1alpha-Hydroxycholecalciferol
  • alfarol
  • alphacalcidol
  • einsalpha
  • alpha-calcidol
  • 1-hydroxycholecalciferol
  • Molecular weight: 400.65
  • Formula: C27H44O2
  • CLOGP: 8.24
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 2
  • TPSA: 40.46
  • ALOGS: -5.39
  • ROTB: 6

Drug dosage:

DoseUnitRoute
1 mcg O
1 mcg P
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 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) 71 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 0.82 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 48.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1978 YEAR INTRODUCED

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
Muscle spasticity 406.60 15.15 161 14305 17023 50573635
Respiratory disorder 349.89 15.15 173 14293 31014 50559644
Ear pain 338.55 15.15 164 14302 28119 50562539
Night sweats 332.01 15.15 171 14295 33403 50557255
Body temperature increased 316.75 15.15 162 14304 31179 50559479
Lower respiratory tract infection 154.83 15.15 162 14304 95039 50495619
Urticaria 150.36 15.15 185 14281 129376 50461282
Insomnia 128.08 15.15 200 14266 174665 50415993
Hypocalcaemia 127.38 15.15 85 14381 26731 50563927
Back pain 111.73 15.15 214 14252 219816 50370842
Abdominal pain upper 102.67 15.15 172 14294 159137 50431521
Sinusitis 94.12 15.15 172 14294 170386 50420272
Hypercalcaemia 89.73 15.15 65 14401 23287 50567371
Pruritus 89.60 15.15 228 14238 283340 50307318
Upper respiratory tract inflammation 87.99 15.15 31 14435 2358 50588300
Peripheral swelling 86.26 15.15 185 14281 205751 50384907
Osteonecrosis of jaw 82.77 15.15 71 14395 32455 50558203
Hepatic function abnormal 80.45 15.15 70 14396 32611 50558047
Drug ineffective 78.21 15.15 72 14394 819261 49771397
Renal impairment 78.05 15.15 102 14364 75559 50515099
Spinal compression fracture 77.20 15.15 47 14419 12609 50578049
Fatigue 71.30 15.15 59 14407 707542 49883116
Shunt stenosis 67.53 15.15 17 14449 398 50590260
Vomiting 62.13 15.15 278 14188 460480 50130178
Asthenia 57.69 15.15 211 14255 318831 50271827
Diarrhoea 54.15 15.15 319 14147 588157 50002501
Rash 52.34 15.15 255 14211 437216 50153442
Joint swelling 50.13 15.15 169 14297 245117 50345541
Drug intolerance 47.75 15.15 4 14462 219100 50371558
Drug hypersensitivity 42.18 15.15 10 14456 251000 50339658
Blood parathyroid hormone increased 41.64 15.15 19 14447 2835 50587823
Product dose omission issue 41.05 15.15 3 14463 183835 50406823
Incorrect route of product administration 38.10 15.15 36 14430 18630 50572028
Atypical femur fracture 37.21 15.15 21 14445 4895 50585763
Hyperuricaemia 35.44 15.15 20 14446 4660 50585998
Interstitial lung disease 34.93 15.15 58 14408 53118 50537540
Abdominal discomfort 33.82 15.15 12 14454 231629 50359029
Alopecia 33.62 15.15 14 14452 245033 50345625
Cardiac failure 32.52 15.15 69 14397 75971 50514687
Toxoplasmosis 32.50 15.15 13 14453 1404 50589254
Shunt occlusion 32.32 15.15 10 14456 506 50590152
Enteritis infectious 31.94 15.15 14 14452 1901 50588757
Cerebral infarction 31.92 15.15 35 14431 21569 50569089
Lymph node palpable 31.20 15.15 7 14459 98 50590560
Nausea 31.17 15.15 101 14365 705297 49885361
Iron deficiency anaemia 29.74 15.15 30 14436 16804 50573854
Arthropathy 29.19 15.15 5 14461 157901 50432757
Tetany 27.52 15.15 12 14454 1609 50589049
Large intestine polyp 27.22 15.15 20 14446 7312 50583346
Gastroenteritis 26.52 15.15 33 14433 23248 50567410
Treatment failure 26.24 15.15 4 14462 137633 50453025
Headache 25.88 15.15 239 14227 506296 50084362
Milk-alkali syndrome 25.65 15.15 9 14457 676 50589982
Osteomyelitis 24.37 15.15 31 14435 22322 50568336
Beta 2 microglobulin urine increased 24.11 15.15 5 14461 47 50590611
Glossodynia 22.87 15.15 3 14463 115566 50475092
Anaemia 22.49 15.15 136 14330 252320 50338338
Calciphylaxis 21.96 15.15 12 14454 2626 50588032
Haemodialysis complication 21.89 15.15 6 14460 197 50590461
Anxiety 21.51 15.15 12 14454 177594 50413064
Enterocolitis viral 21.49 15.15 6 14460 211 50590447
Rheumatoid arthritis 21.38 15.15 16 14450 202534 50388124
Oncocytoma 21.16 15.15 4 14462 22 50590636
Death 21.10 15.15 38 14428 325341 50265317
Toxicity to various agents 20.92 15.15 18 14448 212481 50378177
Nephrogenic anaemia 20.70 15.15 10 14456 1695 50588963
Periodontitis 20.27 15.15 12 14454 3057 50587601
Immunosuppressant drug level increased 20.22 15.15 12 14454 3070 50587588
Enterocolitis 20.17 15.15 16 14450 6551 50584107
Platelet count decreased 20.15 15.15 69 14397 100657 50490001
Pneumonia aspiration 19.27 15.15 33 14433 30971 50559687
Product monitoring error 18.76 15.15 11 14455 2753 50587905
Peripheral arterial occlusive disease 18.70 15.15 12 14454 3525 50587133
Immobilisation syndrome 18.64 15.15 5 14461 151 50590507
Infusion related reaction 18.41 15.15 13 14453 169544 50421114
Wound 18.17 15.15 4 14462 105790 50484868
Premature rupture of membranes 18.16 15.15 13 14453 4567 50586091
Neuropsychiatric lupus 18.07 15.15 5 14461 170 50590488
Pharyngitis 17.10 15.15 23 14443 17480 50573178
Blood albumin decreased 17.09 15.15 20 14446 13216 50577442
Precocious puberty 17.03 15.15 5 14461 211 50590447
Discomfort 16.89 15.15 5 14461 108375 50482283
Hypophosphataemia 16.73 15.15 16 14450 8398 50582260
Community acquired infection 16.66 15.15 3 14463 12 50590646
Musculoskeletal stiffness 16.56 15.15 8 14458 128473 50462185
Neurosis 16.37 15.15 5 14461 242 50590416
Colon cancer 16.29 15.15 16 14450 8675 50581983
Cystitis 16.29 15.15 38 14428 44526 50546132
Hungry bone syndrome 16.21 15.15 4 14462 86 50590572
Liver disorder 16.16 15.15 34 14432 37188 50553470
Colitis microscopic 16.10 15.15 14 14452 6506 50584152
Calculus urinary 16.03 15.15 7 14459 941 50589717
Retinal haemorrhage 15.90 15.15 12 14454 4569 50586089
Oesophageal mucosal tear 15.65 15.15 3 14463 18 50590640
Autoimmune pancytopenia 15.64 15.15 4 14462 100 50590558
Hepatic enzyme increased 15.62 15.15 10 14456 137370 50453288

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
Shunt stenosis 120.68 18.04 28 6968 561 29566970
Hypocalcaemia 113.56 18.04 67 6929 20598 29546933
Shunt occlusion 79.85 18.04 21 6975 715 29566816
Oesophageal perforation 65.24 18.04 18 6978 737 29566794
Immunosuppressant drug level increased 59.93 18.04 27 6969 4738 29562793
Soft tissue mass 58.84 18.04 16 6980 620 29566911
Multimorbidity 56.22 18.04 15 6981 540 29566991
Osteonecrosis of jaw 47.94 18.04 36 6960 16474 29551057
Hepatic function abnormal 45.28 18.04 51 6945 39208 29528323
Transplant failure 41.78 18.04 18 6978 2838 29564693
Superinfection 40.82 18.04 16 6980 1985 29565546
Upper respiratory tract inflammation 40.41 18.04 15 6981 1605 29565926
Renal impairment 39.83 18.04 70 6926 81263 29486268
Oesophageal carcinoma 39.56 18.04 20 6976 4527 29563004
Procalcitonin abnormal 39.17 18.04 10 6986 302 29567229
Aplasia pure red cell 36.01 18.04 20 6976 5471 29562060
Myocardial ischaemia 35.89 18.04 30 6966 15998 29551533
Labelled drug-drug interaction medication error 34.16 18.04 26 6970 12133 29555398
Anti-erythropoietin antibody negative 32.67 18.04 8 6988 203 29567328
Neuromyopathy 32.63 18.04 11 6985 888 29566643
Inflammatory marker increased 31.52 18.04 16 6980 3651 29563880
Calciphylaxis 31.35 18.04 11 6985 1001 29566530
Encephalomalacia 30.46 18.04 10 6986 743 29566788
Hypercalcaemia 28.81 18.04 24 6972 12735 29554796
C-reactive protein increased 28.29 18.04 43 6953 44220 29523311
Drug ineffective 27.91 18.04 27 6969 363143 29204388
Lung consolidation 26.75 18.04 16 6980 5027 29562504
Retinopathy hypertensive 26.08 18.04 7 6989 258 29567273
Cardiomegaly 25.23 18.04 23 6973 13753 29553778
Device related sepsis 24.75 18.04 12 6984 2483 29565048
Drug level increased 24.41 18.04 26 6970 18761 29548770
PO2 decreased 24.02 18.04 10 6986 1449 29566082
Interstitial lung disease 23.60 18.04 46 6950 57672 29509859
Drug interaction 22.29 18.04 99 6897 197286 29370245
Cerebral infarction 21.78 18.04 28 6968 24647 29542884
Extraskeletal ossification 20.97 18.04 4 6992 29 29567502
Rales 20.96 18.04 16 6980 7494 29560037
Lymphocyte count increased 20.60 18.04 11 6985 2783 29564748
Fatigue 20.55 18.04 27 6969 316794 29250737
Immune thrombocytopenia 20.28 18.04 16 6980 7861 29559670
PCO2 decreased 19.86 18.04 9 6987 1599 29565932
Hepatosplenomegaly neonatal 19.82 18.04 4 6992 40 29567491
Bradycardia foetal 19.80 18.04 6 6990 343 29567188
Monocyte count increased 19.76 18.04 12 6984 3874 29563657
Myeloperoxidase deficiency 19.47 18.04 4 6992 44 29567487
Nail discolouration 18.43 18.04 7 6989 797 29566734
Hyperkalaemia 18.26 18.04 43 6953 61349 29506182
Acute kidney injury 18.23 18.04 116 6880 265151 29302380
Disseminated intravascular coagulation 18.14 18.04 23 6973 19957 29547574

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 207.32 12.98 139 19386 41614 64437593
Shunt stenosis 177.53 12.98 45 19480 1022 64478185
Muscle spasticity 154.62 12.98 83 19442 16586 64462621
Ear pain 127.89 12.98 85 19440 25051 64454156
Osteonecrosis of jaw 125.94 12.98 101 19424 39724 64439483
Upper respiratory tract inflammation 121.41 12.98 45 19480 3737 64475470
Respiratory disorder 117.21 12.98 93 19432 36018 64443189
Hepatic function abnormal 116.15 12.98 119 19406 64194 64415013
Night sweats 115.22 12.98 92 19433 35954 64443253
Hypercalcaemia 110.83 12.98 85 19440 31331 64447876
Shunt occlusion 106.55 12.98 31 19494 1196 64478011
Body temperature increased 103.38 12.98 87 19438 36579 64442628
Renal impairment 98.23 12.98 159 19366 134858 64344349
Drug ineffective 86.16 12.98 77 19448 840170 63639037
Spinal compression fracture 82.57 12.98 53 19472 14722 64464485
Fatigue 81.14 12.98 65 19460 748665 63730542
Oesophageal perforation 63.34 12.98 20 19505 1021 64478186
Blood parathyroid hormone increased 61.04 12.98 26 19499 3108 64476099
Lower respiratory tract infection 60.20 12.98 105 19420 94509 64384698
Interstitial lung disease 55.21 12.98 103 19422 97629 64381578
Aplasia pure red cell 51.59 12.98 30 19495 6984 64472223
Immunosuppressant drug level increased 50.63 12.98 30 19495 7229 64471978
Cerebral infarction 50.15 12.98 62 19463 40982 64438225
Soft tissue mass 49.29 12.98 16 19509 893 64478314
Multimorbidity 43.68 12.98 15 19510 997 64478210
Hyperuricaemia 41.34 12.98 30 19495 10161 64469046
Drug intolerance 39.82 12.98 5 19520 187987 64291220
Platelet count decreased 39.45 12.98 126 19399 167585 64311622
Urticaria 37.72 12.98 114 19411 147203 64332004
Insomnia 37.24 12.98 138 19387 197698 64281509
Procalcitonin abnormal 36.63 12.98 10 19515 305 64478902
Transplant failure 35.47 12.98 19 19506 3775 64475432
Product dose omission issue 35.04 12.98 8 19517 194739 64284468
Oesophageal carcinoma 34.13 12.98 20 19505 4723 64474484
Peripheral arterial occlusive disease 34.01 12.98 23 19502 6964 64472243
Anaemia 33.85 12.98 213 19312 378467 64100740
Drug hypersensitivity 33.55 12.98 15 19510 237800 64241407
Gastroenteritis 33.30 12.98 43 19482 29668 64449539
Cardiac failure 32.54 12.98 101 19424 132272 64346935
Diarrhoea 32.27 12.98 347 19178 722357 63756850
Calciphylaxis 32.13 12.98 17 19508 3295 64475912
Disseminated intravascular coagulation 31.94 12.98 44 19481 32304 64446903
Completed suicide 31.90 12.98 14 19511 224400 64254807
Large intestine polyp 31.12 12.98 26 19499 10811 64468396
Enteritis infectious 30.68 12.98 16 19509 3012 64476195
Superinfection 29.59 12.98 17 19508 3869 64475338
Tetany 29.48 12.98 14 19511 2158 64477049
Nausea 29.02 12.98 131 19394 785669 63693538
Back pain 28.39 12.98 150 19375 250021 64229186
Anti-erythropoietin antibody negative 28.11 12.98 8 19517 285 64478922
Labelled drug-drug interaction medication error 28.03 12.98 34 19491 22028 64457179
Lymph node palpable 28.00 12.98 7 19518 150 64479057
Weight increased 27.75 12.98 15 19510 213333 64265874
Hungry bone syndrome 27.53 12.98 7 19518 161 64479046
Atypical femur fracture 26.61 12.98 17 19508 4681 64474526
Incorrect route of product administration 26.55 12.98 34 19491 23264 64455943
Neuromyopathy 25.49 12.98 11 19514 1357 64477850
Toxoplasmosis 25.01 12.98 13 19512 2431 64476776
Hyperhidrosis 24.86 12.98 4 19521 124916 64354291
Encephalomalacia 24.44 12.98 10 19515 1081 64478126
Decreased appetite 24.34 12.98 157 19368 281132 64198075
Hypophosphataemia 24.33 12.98 26 19499 14694 64464513
Hyperphosphataemia 24.03 12.98 15 19510 3966 64475241
Beta 2 microglobulin urine increased 23.93 12.98 6 19519 130 64479077
Pruritus 23.83 12.98 169 19356 312231 64166976
Inflammatory marker increased 23.69 12.98 20 19505 8431 64470776
Iron deficiency anaemia 23.47 12.98 31 19494 21858 64457349
Periodontitis 23.43 12.98 15 19510 4144 64475063
Enterocolitis viral 23.17 12.98 7 19518 308 64478899
Liver disorder 22.68 12.98 50 19475 53301 64425906
Treatment failure 22.67 12.98 4 19521 116812 64362395
Pneumonia aspiration 22.38 12.98 53 19472 59218 64419989
Osteomyelitis 22.10 12.98 34 19491 27553 64451654
Myocardial ischaemia 22.01 12.98 31 19494 23220 64455987
Immobilisation syndrome 21.51 12.98 7 19518 394 64478813
Abdominal pain upper 21.26 12.98 107 19418 174923 64304284
Enterocolitis 21.24 12.98 22 19503 11996 64467211
Abdominal discomfort 20.69 12.98 15 19510 182307 64296900
Pharyngitis 20.47 12.98 27 19498 19012 64460195
Immune thrombocytopenia 20.42 12.98 24 19501 15042 64464165
Retinopathy hypertensive 20.42 12.98 7 19518 463 64478744
Milk-alkali syndrome 20.30 12.98 9 19516 1184 64478023
Oncocytoma 19.86 12.98 4 19521 30 64479177
Premature rupture of membranes 19.85 12.98 13 19512 3731 64475476
C-reactive protein increased 19.36 12.98 68 19457 94841 64384366
Haemodialysis complication 19.14 12.98 6 19519 299 64478908
Chronic gastritis 19.04 12.98 12 19513 3228 64475979
Anxiety 18.97 12.98 20 19505 202629 64276578
Nephrogenic anaemia 18.75 12.98 12 19513 3313 64475894
Sinusitis 18.28 12.98 90 19435 145838 64333369
Neuropsychiatric lupus 18.20 12.98 5 19520 156 64479051
Vomiting 18.13 12.98 250 19275 550867 63928340
Arthropathy 18.06 12.98 7 19518 120960 64358247
Nephrotic syndrome 17.79 12.98 18 19507 9549 64469658
Intentional overdose 17.63 12.98 3 19522 89941 64389266
Rash 17.59 12.98 214 19311 458335 64020872
Peritonitis 17.52 12.98 29 19496 24994 64454213
Death 17.44 12.98 81 19444 482624 63996583
Depression 17.26 12.98 18 19507 183273 64295934
Skin erosion 17.08 12.98 12 19513 3864 64475343
Lung consolidation 17.05 12.98 16 19509 7742 64471465
Infusion related reaction 16.82 12.98 15 19510 164452 64314755
Colon cancer 16.78 12.98 20 19505 12719 64466488
Therapeutic product effect decreased 16.69 12.98 7 19518 115344 64363863
Alopecia 15.91 12.98 16 19509 165674 64313533
PO2 decreased 15.82 12.98 10 19515 2703 64476504
Haemorrhage subcutaneous 15.81 12.98 12 19513 4349 64474858
Oesophageal mucosal tear 15.78 12.98 3 19522 16 64479191
Injection site pain 15.74 12.98 7 19518 111401 64367806
Pneumonia bacterial 15.67 12.98 21 19504 15014 64464193
Shunt aneurysm 15.62 12.98 3 19522 17 64479190
Hyperkalaemia 15.35 12.98 66 19459 101063 64378144
Protein urine present 15.12 12.98 16 19509 8940 64470267
Hypothyroidism 15.08 12.98 36 19489 40421 64438786
Precocious puberty 15.04 12.98 5 19520 301 64478906
Premature delivery 15.02 12.98 23 19502 18566 64460641
Idiopathic pulmonary fibrosis 14.99 12.98 11 19514 3789 64475418
Hypotension 14.92 12.98 62 19463 380912 64098295
Pemphigoid 14.87 12.98 19 19506 12967 64466240
Community acquired infection 14.51 12.98 3 19522 26 64479181
Syncope 14.26 12.98 16 19509 157619 64321588
Pneumonia 14.22 12.98 243 19282 559333 63919874
Pyelonephritis acute 14.09 12.98 12 19513 5122 64474085
Device related sepsis 14.04 12.98 12 19513 5143 64474064
Feeling abnormal 13.89 12.98 12 19513 133590 64345617
Myeloperoxidase deficiency 13.87 12.98 3 19522 33 64479174
Colitis microscopic 13.85 12.98 14 19511 7418 64471789
Neurosis 13.82 12.98 5 19520 387 64478820
Calculus urinary 13.81 12.98 8 19517 1849 64477358
Aortic dissection 13.63 12.98 10 19515 3442 64475765
Gastric cancer 13.53 12.98 13 19512 6480 64472727
Dermatophytosis of nail 13.51 12.98 4 19521 164 64479043
Concomitant disease aggravated 13.40 12.98 17 19508 11525 64467682
Sepsis 13.34 12.98 117 19408 230224 64248983
Stag horn calculus 13.33 12.98 4 19521 172 64479035
Marasmus 13.03 12.98 6 19519 862 64478345

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A11CC03 ALIMENTARY TRACT AND METABOLISM
VITAMINS
VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO
Vitamin D and analogues
ATC M05BB06 MUSCULO-SKELETAL SYSTEM
DRUGS FOR TREATMENT OF BONE DISEASES
DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
Bisphosphonates, combinations
MeSH PA D050071 Bone Density Conservation Agents
CHEBI has role CHEBI:50646 antiosteoporotic

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

DiseaseRelationSNOMED_IDDOID
Renal osteodystrophy indication 16726004 DOID:13068
Hypoparathyroidism indication 36976004 DOID:11199
Hyperparathyroidism indication 66999008 DOID:13543
Neonatal hypocalcemia indication 268846006




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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vitamin D3 receptor Nuclear hormone receptor AGONIST WOMBAT-PK KEGG DRUG
Sodium-dependent noradrenaline transporter Transporter Ki 6 DRUG MATRIX

External reference:

IDSource
D01518 KEGG_DRUG
12062 RXNORM
C0044410 UMLSCUI
CHEBI:31186 CHEBI
M9B PDB_CHEM_ID
CHEMBL1601669 ChEMBL_ID
DB01436 DRUGBANK_ID
C008088 MESH_SUPPLEMENTAL_RECORD_UI
5282181 PUBCHEM_CID
4489 INN_ID
URQ2517572 UNII
003501 NDDF
11984007 SNOMEDCT_US
329325000 SNOMEDCT_US

Pharmaceutical products:

None