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Levothyroxine sodium

pharmaceutical raw materials
Levothyroxine sodium structure

Levothyroxine sodium 

structure
  • CAS No:

    55-03-8

  • Formula:

    C15H12I4NNaO4

  • Chemical Name:

    Levothyroxine sodium

  • Synonyms:

    Levothyroxine sodium;Sodium 4-O-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-L-tyrosine;(S)-2-Amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propionic Acid odium;(s)-2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propionic acid sodium salt;sodium (s)-2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propionate;L-THYROXINE SODIUM ANHYDROUS;Levothyroxine Sdium;levothyroxine sodium anhydrous

  • Categories:

    Active Pharmaceutical Ingredients  >  Hormones and the Endocrine System

Description

Levothyroxine sodium  is White Solid


Levothyroxine Sodium is the sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.|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.


On August 14, 1997, the FDA declared levothyroxine sodium tablets a “new drug.” On February 15, 2017, the FDA approved levothyroxine sodium (brand name: Tirosint-SOL, developed by IBSA Pharma Inc.) oral solution for hypothyroidism and pituitary thyroid-stimulating hormone (TSH) suppression. Subsequently, the FDA approved two changes to the labeling of levothyroxine sodium (Tirosint-SOL, IBSA). The first change was for use in combination with a proton pump inhibitor (PPI). The second adjustment was the timing of levothyroxine sodium administration. The approved labeling changes were based on the results of two clinical studies that found no interaction between levothyroxine sodium and PPIs, and the same results were shown when administered 15 minutes and 30 minutes before breakfast. This led to the approval to label levothyroxine sodium as the only FDA-approved LT4 therapy that does not have label interactions with PPIs and can be taken 15 minutes before breakfast.


ChEBI: The sodium salt of L-thyoxine. It is used as replacement therapy in the treatment of hypothyroidism.


Levothyroxine sodium,O-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-2-tyrosinemonosodium salt, hydrate (Synthroid, Letter, Levoxine,Levoid), is the sodium salt of the levo isomer of thyroxine,which is an active physiological principle obtained from thethyroid gland of domesticated animals used for food by humans.It is also prepared synthetically. The salt is a light yellow,tasteless, odorless powder. It is hygroscopic but stablein dry air at room temperature. It is soluble in alkali hydroxides,1:275 in alcohol, and 1:500 in water, to give a pH ofabout 8.9.

Levothyroxine sodium Basic Attributes

800.87

798.668579

200-221-4

9J765S329G

TSCA listed

DTXSID10209941

C888

Off-white to light yellow

2937909000

Characteristics

141.76000

powder

d420 2.381

207-210 (dec.)(lit.)

576.3ºC at 760 mmHg

302.3ºC

cell culture medium: 0.1 mg/mL

2-8°C

D20 -4.4° (c = 3 in 70% ethanol)

Keep in dark place,Inert atmosphere,2-8°C

Safety Information

II

6.1(a)

2811

3

22-24/25

YP2833760

P201, P202, P260, P264, P270, P281, P308+P313, P314, P405, P501

H361

2811

|Danger|H361 (94.23%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P260, P264, P270, P281, P308+P313, P314, P405, and P501|Aggregated GHS information provided by 52 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|Warning|H302 (89.47%): Harmful if swallowed [Warning Acute toxicity, oral]|P260, P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P314, P322, P330, P363, and P501|Aggregated GHS information provided by 20 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H361 (25%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|Aggregated GHS information provided by 4 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

3,5,3',5'-Tetraiodothyronine

Levothyroxine sodium Use and Manufacturing

Uses

One of the thyroid hormones involved in the maintenance of metabolic homeostasis. Synthesized and stored as amino acid residues of thyroglobulin, the major protein component of the thyroid follicular colloid. Synthesis and secretion are regulated by the pituitary hormone (TSH). Deiodinated in peripheral tissues to the active metabolite, liothyronine. The D-form has very little activity as a thyroid hormone, but has been used to treat hyperlipidemia.

L-Tyrosine, O-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-, sodium salt (1:1): INACTIVE

Computed Properties

Molecular Weight:888.93
Hydrogen Bond Donor Count:7
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:5
Exact Mass:888.7215
Monoisotopic Mass:888.7215
Topological Polar Surface Area:101
Heavy Atom Count:30
Complexity:426
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:7
Compound Is Canonicalized:Yes

Material

Drug Function and Efficacy

1. Increase the effect of anticoagulants; 2. Increase the level of phenytoin sodium in the blood; 3. The metabolism is accelerated by anticonvulsants (such as carbamazepine and phenytoin sodium), and it can be replaced from plasma proteins; 4. The dosage of cardiac glycosides needs to be adjusted when used with cardiac glycosides; 5. Increase the effect of sympathomimetic drugs; 6. Increase the sensitivity of catecholamine receptors, thereby increasing the response of tricyclic antidepressants; 7. The absorption is reduced by the influence of cholestyramine, and the dosage of levothyroxine sodium needs to be increased when oral contraceptives are used at the same time.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • AZICO BIOPHORE INDIA PVT LTD

    United States United States
    Active
  • EXCELLA GMBH AND CO KG

    United States United States
    Active
  • VALARY LAB PRIVATE LIMITED

    India India
    Active

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