Tìm theo
Liotrix
Các tên gọi khác (2) :
  • Levothyroxine sodium - liothyronine sodium mixt
  • Thyrolar
Hormon thượng thận và những chất tổng hợp thay thế
Thuốc Gốc
Small Molecule
CAS: 8065-29-0
ĐG : Forest Pharmaceuticals , http://www.forestpharm.com
CTHH: C30H21I7N2Na2O8
PTK: 1471.8072
Liotrix is a synthetically derived thyroid hormone replacement preparation. It consists of levothyroxine sodium (thyroxine, T4) and liothyronine sodium (triiodothyronine, T3) in a 4 to 1 ratio by weight. Liotrix was developed when it was believed that serum levels of both T4 and T3 were maintained by direct thyroidal secretion. It is now known that the thyroid gland secretes approximately ten times more T4 than T3 and that 80% of serum T3 is derived from deiodination of T4 in peripheral tissues. Administration of levothyroxine alone is sufficient for maintaining serum T4 and T3 levels in most patients and combination hormone replacement therapy generally offers no therapeutic advantage. In fact, administration of T3 may result in supratherapeutic levels of T3.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C30H21I7N2Na2O8
Phân tử khối
1471.8072
Monoisotopic mass
1471.440608948
InChI
InChI=1S/C15H11I4NO4.C15H12I3NO4.2Na/c16-8-4-7(5-9(17)13(8)21)24-14-10(18)1-6(2-11(14)19)3-12(20)15(22)23;16-9-6-8(1-2-13(9)20)23-14-10(17)3-7(4-11(14)18)5-12(19)15(21)22;;/h1-2,4-5,12,21H,3,20H2,(H,22,23);1-4,6,12,20H,5,19H2,(H,21,22);;/q;;2*+1/p-2/t2*12-;;/m00../s1
InChI Key
InChIKey=LKYWLLWWYBVUPP-XOCLESOZSA-L
IUPAC Name
disodium (2S)-2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoate (2S)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoate
Traditional IUPAC Name
disodium levothyroxine(1-) liothyronine(1-)
SMILES
[Na+].[Na+].N[C@@H](CC1=CC(I)=C(OC2=CC(I)=C(O)C=C2)C(I)=C1)C([O-])=O.N[C@@H](CC1=CC(I)=C(OC2=CC(I)=C(O)C(I)=C2)C(I)=C1)C([O-])=O
logP
3.73
pKa (strongest acidic)
0.27
pKa (Strongest Basic)
9.43
PSA
95.61 Å2
Refractivity
137.63 m3·mol-1
Polarizability
49.04 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Thyroid hormone drugs are natural or synthetic preparations containing T4 or T3 or both. T4 and T3 are produced in the human thyroid gland by the iodination and coupling of the amino acid tyrosine. Liotrix is a synthetic preparation of T4 and T3 in a 4:1 weight-based ratio. These hormones enhance oxygen consumption by most tissues of the body and increase the basal metabolic rate and the metabolism of carbohydrates, lipids and proteins. Thus, they exert a profound influence on every organ system in the body and are of particular importance in the development of the central nervous system.
Cơ Chế Tác Dụng : Liotrix is a synthetically derived thyroid hormone replacement preparation. It consists of levothyroxine sodium (thyroxine, T4) and liothyronine sodium (triiodothyronine, T3) in a 4 to 1 ratio by weight. Liotrix was developed when it was believed that serum levels of both T4 and T3 were maintained by direct thyroidal secretion. It is now known that the thyroid gland secretes approximately ten times more T4 than T3 and that 80% of serum T3 is derived from deiodination of T4 in peripheral tissues. Administration of levothyroxine alone is sufficient for maintaining serum T4 and T3 levels in most patients and combination hormone replacement therapy generally offers no therapeutic advantage. In fact, administration of T3 may result in supratherapeutic levels of T3. The hormones, T4 and T3, are tyrosine-based hormones produced by the thyroid gland. Iodine is an important component in their synthesis. The major secreted form of thyroid hormone is T4. T4 is converted T3, the more active thyroid hormone, by deiodinases in peripheral tissues. T3 acts in the body to increase basal metabolic rate, alter protein synthesis and increase the body's sensitivity to catecholamines (such as adrenaline). Thyroid hormones are essential for proper development and differentiation of all cells of the human body. T4 and T3 regulate protein, fat and carbohydrate metabolism to varying extents. The most pronounced effect of the hormones is in altering how human cells use energetic compounds. The thyroid hormone derivatives bind to the thyroid hormone receptors initially to initiate their downstream effects.
Dược Động Học :

▧ Route of Elimination :
Thyroid hormones are primarily eliminated by the kidneys.
Độc Tính : Hypermetabolic state indistinguishable from thyrotoxicosis of endogenous origin. Symptoms of thyrotoxicosis include weight loss, increased appetite, palpitations, nervousness, diarrhea, abdominal cramps, sweating, tachycardia, increased pulse and blood pressure, cardiac arrhythmias, tremors, insomnia, heat intolerance, fever, and menstrual irregularities.
Chỉ Định : May be used to treat primary, secondary or tertiary hypothyroidism. May also be used to suppress thyroid stimulating hormone (TSH) secretion in patients with simple (nontoxic) goiter, subacute or chronic lymphocytic thyroiditis multinodular goiter, and in the management of thyroid cancer. May be used in conjunction with other antithyroid agents to treat thyrotoxicosis to prevent goitrogenesis and hypothyroidism. May also be used for differential diagnosis of suspected mild hyperthyroidism or thyroid gland autonomy.
Tương Tác Thuốc :
  • Calcium Acetate Calcium salts such as calcium acetate may diminish the therapeutic effect of thyroid products such as liotrix. Separate the doses of the thyroid product and the oral calcium supplement by at least 4 hours. Monitor for decreased therapeutic effects of thyroid products if an oral calcium supplement is initiated/dose increased, or increased effects if an oral calcium supplement is discontinued/dose decreased.
  • Cholestyramine The resin, cholestyramine, decreases the absorption of the thyroid hormone, liotrix.
  • Colestipol The resin, colestipol, decreases the absorption of the thyroid hormone, liotrix.
  • Digoxin The thyroid hormone, liotrix, decreases the effect of digoxin.
  • Warfarin Liotrix may contribute to the anticoagulant effect of warfarin by increasing the metabolism of vitamin K-dependent clotting factors. Monitor for changes in prothrombin time and anticoagulant effects if liotrix is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral - 100 mcg/25 mcg
Tablet - Oral - 12.5 mcg/3.1 mcg
Tablet - Oral - 150 mcg/37.5 mcg
Tablet - Oral - 25 mcg/6.25 mcg
Tablet - Oral - 50 mcg/12.5 mcg
Dữ Kiện Thương Mại
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01583
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=71371
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506203
ChemSpider
http://www.chemspider.com/Chemical-Structure.64467.html
PharmGKB
http://www.pharmgkb.org/drug/PA164748036
RxList
http://www.rxlist.com/cgi/generic/liot.htm
Drugs.com
http://www.drugs.com/cdi/liotrix.html
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