Tìm theo
L-Carnitine
Các tên gọi khác (18 ) :
  • (-)-Carnitine
  • (-)-L-Carnitin
  • (-)-L-Carnitine
  • (R)-Carnitine
  • (S)-Carnitine
  • 3-Carboxy-2-hydroxy-N,N,N-trimethyl-1-propanaminium
  • 3-Carboxy-2-hydroxy-N,N,N-trimethyl-1-propanaminium hydroxide, inner salt
  • Carnicor
  • Carnitene
  • Carnitine
  • Carnitor
  • Karnitin
  • L-Carnitine
  • Levocarnitin
  • Levocarnitina
  • Lévocarnitine
  • Levocarnitinum
  • Vitamin bt
Vitamin
Thuốc Gốc
Small Molecule
CAS: 541-15-1
ATC: A16AA01
ĐG : McLaren Medical , http://www.mclarenmedical.com
CTHH: C7H15NO3
PTK: 161.1989
Constituent of striated muscle and liver. It is used therapeutically to stimulate gastric and pancreatic secretions and in the treatment of hyperlipoproteinemias. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
161.1989
Monoisotopic mass
161.105193351
InChI
InChI=1S/C7H15NO3/c1-8(2,3)5-6(9)4-7(10)11/h6,9H,4-5H2,1-3H3/t6-/m1/s1
InChI Key
InChIKey=PHIQHXFUZVPYII-ZCFIWIBFSA-N
IUPAC Name
(3R)-3-hydroxy-4-(trimethylazaniumyl)butanoate
Traditional IUPAC Name
L-carnitine
SMILES
C[N+](C)(C)C[C@H](O)CC([O-])=O
Độ tan chảy
195-198
Độ hòa tan
2500 mg/mL
logP
-4.9
logS
-1.6
pKa (strongest acidic)
4.2
pKa (Strongest Basic)
-3.6
PSA
60.36 Å2
Refractivity
63.49 m3·mol-1
Polarizability
16.93 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
pKa
3.8
Dược Lực Học : Levocarnitine is a carrier molecule in the transport of long chain fatty acids across the inner mitochondrial membrane. It also exports acyl groups from subcellular organelles and from cells to urine before they accumulate to toxic concentrations. Lack of carnitine can lead to liver, heart, and muscle problems. Carnitine deficiency is defined biochemically as abnormally low plasma concentrations of free carnitine, less than 20 µmol/L at one week post term and may be associated with low tissue and/or urine concentrations. Further, this condition may be associated with a plasma concentration ratio of acylcarnitine/levocarnitine greater than 0.4 or abnormally elevated concentrations of acylcarnitine in the urine. Only the L isomer of carnitine (sometimes called vitamin BT) affects lipid metabolism. The "vitamin BT" form actually contains D,L-carnitine, which competitively inhibits levocarnitine and can cause deficiency. Levocarnitine can be used therapeutically to stimulate gastric and pancreatic secretions and in the treatment of hyperlipoproteinemias.
Cơ Chế Tác Dụng : Constituent of striated muscle and liver. It is used therapeutically to stimulate gastric and pancreatic secretions and in the treatment of hyperlipoproteinemias. [PubChem] Levocarnitine can be synthesised within the body from the amino acids lysine or methionine. Vitamin C (ascorbic acid) is essential to the synthesis of carnitine. Levocarnitine is a carrier molecule in the transport of long chain fatty acids across the inner mitochondrial membrane. It also exports acyl groups from subcellular organelles and from cells to urine before they accumulate to toxic concentrations. Only the L isomer of carnitine (sometimes called vitamin BT) affects lipid metabolism. Levocarnitine is handled by several proteins in different pathways including carnitine transporters, carnitine translocases, carnitine acetyltransferases and carnitine palmitoyltransferases.
Dược Động Học :
▧ Absorption :
Absolute bioavailability is 15% (tablets or solution). Time to maximum plasma concentration was found to be 3.3 hours.
▧ Volume of Distribution :
The steady state volume of distribution (Vss) of an intravenously administered dose, above endogenous baseline levels, was calculated to be 29.0 +/- 7.1L. However this value is predicted to be an underestimate of the true Vss.
▧ Protein binding :
None
▧ Metabolism :
After oral administration L-carnitine which is unabsorbed is metabolized in the gastrointestinal tract by bacterial microflora. Major metabolites include trimethylamine N-oxide and [3H]-gamma-butyrobetaine.
▧ Route of Elimination :
Following a single intravenous dose, 73.1 +/- 16% of the dose was excreted in the urine during the 0-24 hour interval. Post administration of oral carnitine supplements, in addition to a high carnitine diet, 58-65% of the administered radioactive dose was recovered from urine and feces in 5-11 days.
▧ Half Life :
17.4 hours (elimination) following a single intravenous dose.
▧ Clearance :
Total body clearance was found to be a mean of 4L/h.
Độc Tính : LD50 > 8g/kg (mouse, oral). Adverse effects include hypertension, fever, tachycardia and seizures.
Chỉ Định : For treatment of primary systemic carnitine deficiency, a genetic impairment of normal biosynthesis or utilization of levocarnitine from dietary sources, or for the treatment of secondary carnitine deficiency resulting from an inborn error of metabolism such as glutaric aciduria II, methyl malonic aciduria, propionic acidemia, and medium chain fatty acylCoA dehydrogenase deficiency. Used therapeutically to stimulate gastric and pancreatic secretions and in the treatment of hyperlipoproteinemias. Parenteral levocarnitine is indicated for the prevention and treatment of carnitine deficiency in patients with end-stage renal disease.
Liều Lượng & Cách Dùng : Injection - Intravenous - 200mg/mL
Liquid - Oral
Solution - Intravenous
Solution - Oral - 1g/10mL
Tablet - Oral
Tablet - Oral - 330mg
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