Diotroxin

Diotroxin Uses, Dosage, Side Effects, Food Interaction and all others data.

Liothyronine is a thyroidal hormone T3 which is normally produced by the thyroid gland in a ratio 4:1 when compared with T4: T3. Liothyronine is the active form of thyroxine which is composed in a basic chemical structure by a tyrosine with bound iodine. The exogenous liothyronine product was developed by King Pharmaceuticals and FDA approved in 1956.

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.

Diotroxin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Diotroxin
Generic	Levothyroxine Sodium + Liothyronine
Type
Therapeutic Class
Manufacturer
Available Country	South Africa
Last Updated:	September 19, 2023 at 7:00 am

Uses

Liothyronine is a thyroid hormone replacement therapy used to treat hypothyroidism, to suppress TSH, and to help in the diagnosis of hyperthyroidism.

Liothyronine is officially approved for the following indications:

Replacement therapy in primary (thyroidal), secondary (pituitary) and tertiary (hypothalamic) congenital or acquired hypothyroidism.
As an adjunct therapy to surgery and radioiodine in the management of thyroid cancer.
As a diagnostic agent in suppression tests for mild hyperthyroidism or thyroid gland autonomy.

In general terms, exogenous liothyronine is used to replace insufficient hormonal production and restore T3 plasma levels.

The lack of liothyronine can be presented as a pale and puffy face, coarse, brittle hair, dry skin, croaky voice and constipation as well as irregular periods, drowsiness, and lethargy.

Liothyronine should never be used in the suppression of benign nodules and nontoxic diffuse goiter in iodine-sufficient patients nor in the treatment of hyperthyroidism during the recovery phase of subacute thyroiditis.

Diotroxin is also used to associated treatment for these conditions: Autonomy of thyroid gland, Hyperthyroidism, Hypothyroidism, Myxedema coma, Thyroid Cancers, Euthyroid Goitre, Myxedema pre-coma, Supplemental or replacement therapy

How Diotroxin works

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.

Toxicity

The reported oral LD50 of liothyronine in the rat is higher than 4540 mg/kg. When overdosage is registered, symptoms of hyperthyroidism are reported as well as confusion, disorientation, cerebral embolism, seizure, shock, coma, and death. The symptoms of overdose can be presented immediately or several days after overdose ingestion. In an overdose state, reduce the dose of liothyronine and do supportive treatment.

There are no reports studying the carcinogenic, and mutagenic potential nor on the effects of liothyronine on fertility.

Volume of Distribution

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

Elimination Route

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.

Half Life

The half-life of liothyronine is reported to be between 1 and 2 days.

Clearance

There are no reports obtaining this value specifically.

Elimination Route

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.