levothyroxine indications/contra

Stem definitionDrug idCAS RN
2646 51-48-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • levothyroxine sodium anhydrous
  • levothyroxine sodium pentahydrate
  • L-Thyroxine
  • thyroxin sodium
  • thyroxine sodium
  • levothyroxine sodium
  • tetraiodothyronine
  • thyroxine
  • levothyroxine
  • levothyroxin natrium
  • T4
  • levothyroxine sodium hydrate
The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.
  • Molecular weight: 776.87
  • Formula: C15H11I4NO4
  • CLOGP: 3.51
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 3
  • TPSA: 92.78
  • ALOGS: -4.94
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.15 mg O
0.15 mg P

Approvals:

DateAgencyCompanyOrphan
Aug. 21, 2000 FDA STEVENS J

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood thyroid stimulating hormone increased 1692.27 22.42 296 5711 1095 3378757
Completed suicide 1441.44 22.42 466 5541 30648 3349204
Blood thyroid stimulating hormone abnormal 706.47 22.42 107 5900 97 3379755
Product substitution issue 665.66 22.42 187 5820 7413 3372439
Fatigue 661.24 22.42 386 5621 106854 3272998
Hyperthyroidism 636.91 22.42 148 5859 2686 3377166
Hypothyroidism 594.22 22.42 162 5845 5727 3374125
Product quality issue 557.74 22.42 223 5784 26512 3353340
Drug ineffective 482.48 22.42 326 5681 115764 3264088
Alopecia 464.76 22.42 178 5829 18808 3361044
Thyroid function test abnormal 440.54 22.42 85 5922 585 3379267
Palpitations 431.78 22.42 169 5838 18914 3360938
Drug interaction 408.91 22.42 213 5794 46599 3333253
Toxicity to various agents 379.37 22.42 203 5804 46851 3333001
Blood thyroid stimulating hormone decreased 378.73 22.42 75 5932 600 3379252
Drug hypersensitivity 339.05 22.42 172 5835 35508 3344344
Weight increased 310.90 22.42 148 5859 26592 3353260
Nausea 289.08 22.42 252 5755 129393 3250459
Hypotension 286.25 22.42 172 5835 49342 3330510
Overdose 282.98 22.42 150 5857 33828 3346024
Feeling abnormal 282.75 22.42 140 5867 27385 3352467
Headache 281.01 22.42 215 5792 91765 3288087
Therapeutic response unexpected 280.55 22.42 88 5919 5080 3374772
Malaise 276.16 22.42 186 5821 64991 3314861
Dizziness 253.76 22.42 188 5819 76324 3303528
Foetal exposure during pregnancy 233.71 22.42 103 5904 15448 3364404
Intentional overdose 226.08 22.42 100 5907 15125 3364727
Asthenia 223.49 22.42 164 5843 65501 3314351
Rash 221.25 22.42 168 5839 70653 3309199
Insomnia 218.34 22.42 129 5878 35769 3344083

Pharmacologic Action:

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SourceCodeDescription
ATC H03AA01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
THYROID THERAPY
THYROID PREPARATIONS
Thyroid hormones
FDA EPC N0000175945 l-Thyroxine
FDA Chemical/Ingredient N0000007632 Thyroxine

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Goiter indication 3716002 DOID:12176
Hashimoto thyroiditis indication 21983002 DOID:7188
Hypothyroidism indication 40930008 DOID:1459
Myxedema indication 43153006 DOID:11634
Hyperlipidemia indication 55822004 DOID:1168
Congenital hypothyroidism indication 190268003
Malignant tumor of thyroid gland indication 363478007 DOID:1781
Diagnostic Test for Thyroid Dysfunction indication
Myocardial infarction contraindication 22298006 DOID:5844
Thyrotoxic crisis contraindication 29028009 DOID:12837
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Conduction disorder of the heart contraindication 44808001
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Osteoporosis contraindication 64859006 DOID:11476
Diabetes mellitus contraindication 73211009 DOID:9351
Hypopituitarism contraindication 74728003 DOID:9406
Angina pectoris contraindication 194828000
Osteopenia contraindication 312894000
Primary adrenocortical insufficiency contraindication 373662000 DOID:13774
Disorder of coronary artery contraindication 414024009
Myxedema coma off-label use 21263006

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.08 acidic
pKa2 6.63 acidic
pKa3 8.6 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.025MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.05MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.075MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.088MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.112MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.125MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.137MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.15MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.175MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.1MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.2MG **See current Annual Edition, 1.8 Description of Special Situations, Levothyroxine Sodium LEVOXYL KING PHARMS N021301 May 25, 2001 RX TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE
0.3MG **Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons** LEVOXYL KING PHARMS N021301 May 25, 2001 DISCN TABLET ORAL 7101569 Oct. 2, 2023 METHOD OF USE OF ADMINISTERING LEVOTHYROXINE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Thyroid hormone receptor beta Nuclear hormone receptor AGONIST IC50 8.52 IUPHAR CHEMBL
Thyroid hormone receptor alpha Nuclear hormone receptor AGONIST UNKNOWN IUPHAR
THAP domain-containing protein 1 Unclassified WOMBAT-PK
Transthyretin Secreted IC50 4.98 CHEMBL
Bile acid receptor Nuclear hormone receptor IC50 5.10 CHEMBL
Thyroid hormone receptor beta Transcription factor IC50 7.46 CHEMBL

External reference:

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IDSource
DB00451 DRUGBANK_ID
2635 IUPHAR_LIGAND_ID
4017826 VUID
N0000179290 NUI
C0079691 UMLSCUI
D01010 KEGG_DRUG
CHEMBL559 ChEMBL_ID
054I36CPMN UNII
453 INN_ID
55-03-8 SECONDARY_CAS_RN
CHEMBL42115 ChEMBL_ID
4022126 VANDF
N0000007632 NDFRT
N0000020132 NDFRT
73187006 SNOMEDCT_US
d00278 MMSL
38076006 SNOMEDCT_US
005896 NDDF
710809001 SNOMEDCT_US
10582 RXNORM
004881 NDDF
CHEMBL1624 ChEMBL_ID
CHEMBL2103741 ChEMBL_ID
5819 PUBCHEM_CID
D013974 MESH_DESCRIPTOR_UI
CHEBI:6446 CHEBI
T44 PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1341 TABLET 0.03 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1342 TABLET 0.05 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1343 TABLET 0.08 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1344 TABLET 0.09 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1345 TABLET 0.10 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1346 TABLET 0.11 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1347 TABLET 0.13 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1349 TABLET 0.15 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1350 TABLET 0.18 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1351 TABLET 0.20 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1352 TABLET 0.30 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1370 TABLET 0.03 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1371 TABLET 0.05 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1372 TABLET 0.08 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1373 TABLET 0.09 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1374 TABLET 0.10 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1375 TABLET 0.11 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1376 TABLET 0.13 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1377 TABLET 0.15 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1378 TABLET 0.18 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1379 TABLET 0.20 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1380 TABLET 0.30 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-1638 TABLET 0.14 mg ORAL NDA 11 sections
UNITHROID HUMAN PRESCRIPTION DRUG LABEL 1 0527-1639 TABLET 0.14 mg ORAL NDA 11 sections
LEVOTHYROXINE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 16590-302 TABLET 0.10 mg ORAL NDA 11 sections
LEVOTHYROXINE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 16590-403 TABLET 0.05 mg ORAL NDA 11 sections
LEVOTHYROXINE SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 16590-977 TABLET 0.11 mg ORAL NDA 11 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-748 TABLET 0.03 mg ORAL NDA 10 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-749 TABLET 0.05 mg ORAL NDA 10 sections
Levothyroxine Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-750 TABLET 0.08 mg ORAL NDA 10 sections