Liothyronine

Very slightly soluble

In water, 3.958 mg/l at 37 °C.

Soluble in dilute alkalies with the formation of a brownish, water-soluble, sodium salt. Insoluble in propylene glycol.

11.4 [ug/mL] (The mean of the results at pH 7.4)

Warning

H315 (98.9%): Causes skin irritation [Warning Skin corrosion/irritation]

P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 174 reports by companies from 10 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

Hays MT; J Clin Endocrinol 63: 527 (1970). Absorption of triiodothyronine in man.

Surks MI, et al; J Clin Invest 52: 805 (1973). Determination of iodothyronine absorption and conversion to L-thyroxine (T4) to L-triiodothyronine (T3) using a rate turnover technique.

Commercially available liothyronine sodium tablets should be stored in tight containers at a temperature less than 40 °C, preferably between 15-30 °C. Commercially available liothyronine sodium injection should be stored at 2-8 °C. /Liothyronine sodium/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

USE OF PROPRANOLOL IN CONJUNCTION WITH REPLACEMENT THERAPY HAS BEEN REPORTED TO DECR RISK OF ARRHYTHMIA & ANGINA...

THYROID COMPOUNDS THAT PRODUCE HYPERMETABOLIC STATE (LIOTHYRONINE...) INCR RATE OF DECAY OF VITAMIN K-DEPENDENT CLOTTING FACTORS, & IN PRESENCE OF ORAL ANTICOAGULANTS /EG, WARFARIN/, NORMAL COMPENSATION BY INCR SYNTHESIS IS PREVENTED.

THERE IS CONSIDERABLE CLINICAL EVIDENCE THAT A PATIENT'S THYROID STATE AFFECTS RESPONSE TO TRICYCLIC ANTIDEPRESSANT DRUGS. ADDITION OF LIOTHYRONINE (25 UG/DAY) MAY PREVENT RELATIVELY LONG LAG TIME THAT OCCURS BEFORE CLINICAL EFFECTIVENESS OF TRICYCLIC ANTIDEPRESSANTS IS OBSERVED.

CHOLESTYRAMINE MAY CAUSE CLINICALLY SIGNIFICANT DECR IN ABSORPTION OF THYROID HORMONE WHEN THESE DRUGS ARE GIVEN SIMULTANEOUSLY. /THYROID HORMONE/

For more Interactions (Complete) data for LIOTHYRONINE (16 total), please visit the HSDB record page.

The hormones, T₄ and T₃, are tyrosine-based hormones produced by the thyroid gland. Iodine is an important component in their synthesis. The major form of thyroid hormone in the blood is thyroxine (T₄). This is converted to the more active liothyronine form by deiodinases in peripheral tissues. Liothyronine acts on the body to increase the basal metabolic rate, affect protein synthesis and increase the body's sensitivity to catecholamines (such as adrenaline). The thyroid hormones are essential to proper development and differentiation of all cells of the human body. To various extents T₄ and T₃ regulate protein, fat and carbohydrate metabolism. Their most pronounced effect is on how human cells use energetic compounds. The thyroid hormone derivatives bind to the thyroid hormone receptors initially to initiate their downstream effects.

UNTOWARD EFFECTS OF OVERDOSES OF THYROID HORMONES INCL TACHYCARDIA...ANGINA PECTORIS, HYPERTENSION...HYPERKINESIS...GI DISTURBANCES, & HYPOADRENOCORTICISM. ...MAY CAUSE ALLERGIC REACTIONS. /THYROID HORMONES/

FRANKLY TOXIC DOSES INDUCE UNPLEASANT BUT TRANSIENT SYMPTOMS THAT RESEMBLE THYROTOXICOSIS (THYROID STORM). SIGNS & SYMPTOMS INCL PALPITATIONS, RAPID & IRREGULAR PULSE, HEADACHE, TREMORS, NERVOUSNESS, INSOMNIA, DELIRIUM, DIAPHORESIS, HYPERPYREXIA, VOMITING (SOMETIMES UNCONTROLLABLE), COLLAPSE & COMA. /THYROID/

LOW TOXICITY @ NORMAL DOSAGE.

Benchmark Dataset for the Liver Toxicity Knowledge Base (LTKB)

liothyronine

Triostat®

Thyroid agents

Not Applicable

no-DILI-concern

IN RATS EXOPHTHALMOS HAS BEEN PRODUCED /BY USE OF LIOTHYRONINE/. IN RABBITS INTRAOCULAR PRESSURE HAS BEEN REDUCED 4 MM HG BY SUBCONJUNCTIVAL INJECTION OF TRIIODOTHYRONINE...

Four pregnant New Zealand white rabbits received intramuscular triiodothyronine (Liothyronine; T3) at 125 ug/kg on days 25 and 26 of gestation. Another group of 6 rabbits served as controls. Maternal and fetal plasma-free T3, thyroxine (T4), and glucose concentration, as well as fetal liver glycogen content, were evaluated on day 27 of gestation. In T3-treated rabbits, maternal and fetal plasma-free T3 concentration was higher than in controls. T3 treatment resulted in fetal hyperglycemia and depletion of fetal liver glycogen content.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

STATE OF DEFICIENCY: WHEN THERE IS A DEFICIENCY OF IODINE IN RAT THYROID... THE RATIO OF THYROXINE TO TRIIODOTHYRONINE DECREASES FROM 4:1 TO 1:3.

STATE OF DEFICIENCY: IN ABSENCE OF...TRIIODOTHYRONINE, GROWTH IS DEFICIENT, PARTICULARLY AT YOUNGER AGES.

Liothyronine presents a very large binding to plasma proteins and around 99.7% of the administered dose can be found bound. Liothyronine is found to be bound to thyroxine-binding globulin, thyroxine-binding prealbumin and albumin. It is important to consider that only the little unbound portion of liothyronine is metabolically active.

In hormonal replacement, liothyronine is more potent and present a faster action when compared to levothyroxine but the time of action is significantly shorter. The type of treatment needs to be well evaluated as the fast correction of thyroid hormones in certain diseases presents additional risks such as heart failure. The onset of activity is observed a few hours after administration and the maximum effect is observed after 2-3 days. Treatment with liothyronine has been shown to produce normal plasma levels of T3 hormone but to have no effect on the T4 plasma concentration.

Liothyronine replaces endogenous thyroid hormone and then exerts its physiologic effects by controlling DNA transcription and protein synthesis. This effect on DNA is obtained by the binding of liothyronine to the thyroid receptors attached to DNA. Exogenous liothyronine exerts all the normal effects of the endogenous thyroid T3 hormone. Hence, it increases energy expenditure, accelerates the rate of cellular oxidation stimulating growth, maturation, and metabolism of the body tissues, aids in myelination of nerves and development of synaptic processes in the nervous system and enhances carbohydrate and protein metabolism.

LIOTHYRONINE IS ONLY LOOSELY BOUND TO PLASMA PROTEINS & HENCE DOES NOT ELEVATE PLASMA BOUND IODINE SIGNIFICANTLY...PBI MAY ACTUALLY BE LOWERED, BECAUSE OF HOMEOSTATIC DECR IN THYROXINE RELEASE FROM THYROID GLAND.

TRIIODOTHYRONINE INCR METABOLIC RATE & OXYGEN CONSUMPTION OF ANIMAL TISSUES.

Liothyronine is mainly metabolized in the liver where it is deiodinated to diiodothyronine and monoiodothyronine followed by conjugation with glucuronides and sulfates. One of the formed metabolites formed by the conjugation and decarboxylation is tiratricol. The iodine released by the metabolism of liothyronine is later taken and used within the thyroid cells.

THE LIVER CONJUGATES THYROXINE & TRIIODOTHYRONINE WITH GLUCURONIC & SULFURIC ACIDS THROUGH THE PHENOLIC HYDROXYL GROUP, & EXCRETES THESE CONJUGATES & SMALL AMT OF FREE COMPOUNDS IN THE BILE.

Triiodothyronine has known human metabolites that include (2S,3S,4S,5R)-6-[4-[4-[(2S)-2-amino-2-carboxyethyl]-2,6-diiodophenoxy]-2-iodophenoxy]-3,4,5-trihydroxyoxane-2-carboxylic acid.

Half Life: 2.5 days

06LU7C9H1V

LIOTHYRONINE

Established Pharmacologic Class [EPC] - l-Triiodothyronine

Chemical Structure [CS] - Triiodothyronine

Liothyronine is a l-Triiodothyronine.

Thyroid hormones are well absorbed orally. From these hormones, liothyronine is almost completely absorbed and it does not present changes in the absorption rate due to concomitant administration of food.liothyronin Multiple administration of 50 mcg of liothyronine provided a maximal plasma concentration of total T3 of 346 ng/dL in about 2.5 hours with an AUC of 4740 ng.h/dL.

The main elimination of thyroid hormones is known to be done via the kidneys from which less than 2.5% of the excreted drug is represented by the unchanged drug. This elimination route is reduced with age. A portion of the metabolic products of liothyronine is excreted to the bile and gut where they can be part of enterohepatic recirculation.

The reported volume of distribution of liothyronine is reported to be of 0.1-0.2 L/kg.

There are no reports obtaining this value specifically.

WHILE TRIIODOTHYRONINE IS MUCH LESS FIRMLY BOUND /TO PROTEIN THAN IS THYROXINE/, THE QUANTITY THAT IS FREE IS STILL SMALL PERCENTAGE OF TOTAL.

THE DAILY SECRETION OF /TRIIODOTHYRONINE/ IN NORMAL MAN IS APPROXIMATELY...25 UG.

THERAP CAT: Thyroid hormone; THERAP CAT (VET): Thyroid hormone.

Used as replacement or supplemental therapy in patients with hypothyroidism of any etiology, except transient hypothyrodism during the recovery phase of subacute thyroiditis.

Formation from diiodothyronine: Roche et al., Biochem Biophys Acta 11, 215 (1953). Isoln from thyroid gland and synthesis: Gross, Pitt-Rivers, Biochem J 53, 645 (1953); Roche et al., Bull Soc Chim France 4, 462 (1957); Plati, Wenner, U.S. pat 2,784,222 (1957 to Hoffmann-La Roche); Pitt-Rivers, Gross, U.S. pat 2,823,164 (1958 to Nat Res Dev Corp); Razdan, Wetherill, U.S. pat 2,993,928 (1961 to Glaxo).

LIOTHYRONINE SODIUM, USP (CYTOMEL), IS...DESIGNATION FOR SALT OF L-TRIIODOTHYRONINE. ...ALSO IS MARKETED AS TABLETS CONTAINING 5, 25, & 50 UG. KITS FOR PREPN OF POWDER FOR INJECTION ARE AVAILABLE FROM MFR. /LIOTHYRONINE SODIUM/

ORAL TABLETS 5, 25, & 50 MCG; INJECTION: POWDER (FOR SOLN) 114 UG/ML. NOT COMMERCIALLY AVAILABLE; MFR WILL SUPPLY KIT UPON REQUEST.,.

/SODIUM SALT LIOTHYRONINE IS/ COMMONLY USED FORM. /LIOTHYRONINE SODIUM/.

...TRIIODOTHYRONINE REPRESENTS RELATIVELY MINOR FRACTION (ABOUT 5%) /OF ORGANIC IODINE/.

IN DOGS & MAN IT HAS APPROX 2,500 TIMES THE ORAL POTENCY OF OFFICIAL THYROID PREPN.

Possesses 5 times the activity of L-thyroxine.