Overview
Levothyroxine is a synthetically produced form of thyroxine, a major endogenous hormone secreted by the thyroid gland. Also known as L-thyroxine or the brand name product Synthroid, levothyroxine is used primarily to treat hypothyroidism, a condition where the thyroid gland is no longer able to produce sufficient quantities of the thyroid hormones T (tetraiodothyronine or thyroxine) and T (triiodothyronine or Liothyronine), resulting in diminished down-stream effects of these hormones. Without sufficient quantities of circulating thyroid hormones, symptoms of hypothyroidism begin to develop such as fatigue, increased heart rate, depression, dry skin and hair, muscle cramps, constipation, weight gain, memory impairment, and poor tolerance to cold temperatures. In response to Thyroid Stimulating Hormone (TSH) release by the pituitary gland, a normally functioning thyroid gland will produce and secrete T, which is then converted through deiodination (by type I or type II 5′-deiodinases) into its active metabolite T. While T is the major product secreted by the thyroid gland, T exerts the majority of the physiological effects of the thyroid hormones; T and T have a relative potency of ~1:4 (T4:T3). T and T act on nearly every cell of the body, but have a particularly strong effect on the cardiac system. As a result, many cardiac functions including heart rate, cardiac output, and systemic vascular resistance are closely linked to thyroid status. Prior to the development of levothyroxine, Thyroid, porcine or desiccated thyroid, used to be the mainstay of treatment for hypothyroidism. However, this is no longer recommended for the majority of patients due to several clinical concerns including limited controlled trials supporting its use. Desiccated thyroid products contain a ratio of T4 to T3 of 4.2:1, which is significantly lower than the 14:1 ratio of secretion by the human thyroid gland. This higher proportion of T3 in desiccated thyroid products can lead to supraphysiologic levels of T3 which may put patients at risk of thyrotoxicosis if thyroid extract therapy is not adjusted according to the serum TSH.
Background
Levothyroxine is a synthetically produced form of thyroxine, a major endogenous hormone secreted by the thyroid gland. Also known as L-thyroxine or the brand name product Synthroid, levothyroxine is used primarily to treat hypothyroidism, a condition where the thyroid gland is no longer able to produce sufficient quantities of the thyroid hormones T (tetraiodothyronine or thyroxine) and T (triiodothyronine or Liothyronine), resulting in diminished down-stream effects of these hormones. Without sufficient quantities of circulating thyroid hormones, symptoms of hypothyroidism begin to develop such as fatigue, increased heart rate, depression, dry skin and hair, muscle cramps, constipation, weight gain, memory impairment, and poor tolerance to cold temperatures. In response to Thyroid Stimulating Hormone (TSH) release by the pituitary gland, a normally functioning thyroid gland will produce and secrete T, which is then converted through deiodination (by type I or type II 5′-deiodinases) into its active metabolite T. While T is the major product secreted by the thyroid gland, T exerts the majority of the physiological effects of the thyroid hormones; T and T have a relative potency of ~1:4 (T4:T3). T and T act on nearly every cell of the body, but have a particularly strong effect on the cardiac system. As a result, many cardiac functions including heart rate, cardiac output, and systemic vascular resistance are closely linked to thyroid status. Prior to the development of levothyroxine, Thyroid, porcine or desiccated thyroid, used to be the mainstay of treatment for hypothyroidism. However, this is no longer recommended for the majority of patients due to several clinical concerns including limited controlled trials supporting its use. Desiccated thyroid products contain a ratio of T4 to T3 of 4.2:1, which is significantly lower than the 14:1 ratio of secretion by the human thyroid gland. This higher proportion of T3 in desiccated thyroid products can lead to supraphysiologic levels of T3 which may put patients at risk of thyrotoxicosis if thyroid extract therapy is not adjusted according to the serum TSH.
Indication
Levothyroxine is indicated as replacement therapy in primary (thyroidal), secondary (pituitary) and tertiary (hypothalamic) congenital or acquired hypothyroidism. It is also indicated as an adjunct to surgery and radioiodine therapy in the management of thyrotropin-dependent well-differentiated thyroid cancer.
Associated Conditions
- Edematous Fibrosclerotic Panniculopathy (Cellulite)
- Hypothyroidism
- Localized Adiposity
- Myxedema coma
- Euthyroid Goitre
- Thyrotropin dependent Well-Differentiated Thyroid Cancer
Clinical Trials
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Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2023/09/14 | Phase 3 | Completed | |||
2023/04/21 | Phase 2 | Completed | |||
2023/04/07 | Phase 2 | Completed | |||
2023/02/03 | Phase 2 | Active, not recruiting | |||
2022/09/02 | Phase 2 | Recruiting | |||
2022/06/09 | Phase 2 | Completed | |||
2022/05/23 | N/A | Completed | OMER B ABDELBASIT | ||
2022/05/12 | Phase 4 | Completed | Federico II University | ||
2022/04/07 | Phase 3 | Recruiting | Fondazione IRCCS Istituto Nazionale dei Tumori, Milano | ||
2022/03/11 | N/A | Recruiting |
FDA Drug Approvals
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Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
A-S Medication Solutions | 50090-6880 | ORAL | 0.112 mg in 1 1 | 11/8/2023 | |
Mylan Pharmaceuticals Inc. | 0378-1811 | ORAL | 112 ug in 1 1 | 8/31/2020 | |
Mylan Pharmaceuticals Inc. | 0378-1800 | ORAL | 25 ug in 1 1 | 8/31/2020 | |
NorthStar RxLLC | 72603-664 | ORAL | 100 ug in 1 1 | 4/15/2025 | |
REMEDYREPACK INC. | 70518-3208 | ORAL | 50 ug in 1 1 | 6/2/2025 | |
Major Pharmaceuticals | 0904-6956 | ORAL | 0.15 mg in 1 1 | 2/4/2020 | |
IBSA Pharma Inc. | 71858-0105 | ORAL | 13 ug in 1 mL | 11/30/2023 | |
Bryant Ranch Prepack | 63629-2094 | ORAL | 300 ug in 1 1 | 7/23/2020 | |
A-S Medication Solutions | 50090-5661 | ORAL | 50 ug in 1 1 | 7/23/2020 | |
NuCare Pharmaceuticals,Inc. | 68071-4866 | ORAL | 100 ug in 1 1 | 2/17/2021 |
EMA Drug Approvals
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Approved Product | Authorization Holder | Status | Issued Date |
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No EMA approvals found for this drug. |
HSA Drug Approvals
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No HSA approvals found for this drug. |
NMPA Drug Approvals
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PPB Drug Approvals
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Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
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TGA Drug Approvals
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Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
LEVOTHYROXINE SCP levothyroxine sodium 50 microgram un-coated tablet blister pack | 374936 | Medicine | A | 12/23/2022 | |
OROXINE levothyroxine sodium 100 microgram tablet blister pack | 125499 | Medicine | A | 5/17/2006 | |
LEVOTHOX levothyroxine sodium 88 microgram tablet bottle | 363989 | Medicine | A | 7/25/2022 | |
ELTROXIN levothyroxine sodium 25 microgram tablet bottle | 206944 | Medicine | A | 5/19/2014 | |
ELTROXIN levothyroxine sodium 112 microgram tablet bottle | 206967 | Medicine | A | 5/19/2014 | |
LEVOTHYROXINE GH levothyroxine sodium 75 microgram tablet bottle pack | 365690 | Medicine | A | 3/31/2023 | |
LEVOTHYROXINE LUP levothyroxine sodium 25 microgram un-coated tablet blister pack | 374926 | Medicine | A | 12/23/2022 | |
ELTROXIN levothyroxine sodium 150 microgram tablet bottle | 206946 | Medicine | A | 5/19/2014 | |
LEVOTHYROXINE LUP levothyroxine sodium 100 microgram un-coated tablet blister pack | 374929 | Medicine | A | 12/23/2022 | |
APO-LEVOTHYROXINE levothyroxine sodium 150 microgram un-coated tablet blister pack | 374924 | Medicine | A | 12/23/2022 |