Trometamol, molecular formula c4h11no3, white crystalline or powder. MP 171-172 ℃, BP 219-220 ℃ / 1.3 kPa, soluble in ethanol and water, slightly soluble in ethyl acetate, benzene, insoluble in diethyl ether, carbon tetrachloride, corrosive effect on copper and aluminum, irritant. Trometamol as a non sodium amino buffer base. In body fluids can react with water while making it less available. For metabolic acidemia, but also for respiratory acidemia, and would be ideal for comparison in patients with metabolic acidemia complicated by acute respiratory acidemia.
Introduction to compounds
essential information
Chinese Name: trometamol;
Chinese aliases: trihydroxymethylaminomethane; 2-amino-2 - (hydroxymethyl) - 1,3-propanediol; Ammonium bradyruvate; 2-amino-2-hydroxymethyl-1,3-propanediol; Chorismate; Tris (hydroxymethyl) aminomethane;
Name in English: trometamol
English aliases: 8vte 1L; Tham-E； thamset； THAM； riladyl； Talatrol； 1,3-Propanediol, 2-amino-2-（hydroxymethyl）-； Trizma； TRISMAT； TRIS； Tromethamine； Pehanorm；
CAS number: 77-86-1
MDL number: mfcd00004679
EINECS number: 201-064-4
RTECS number: ty2900000
BRN number: 741883
PubChem number: 24899961
Molecular formula: c4h11no3
Structural formula:
MW: 121.13500
Accurate mass: 121.07400
PSA：86.71000
Physicochemical properties
Appearance and characteristics: white crystalline powder
Density: 1353 g / cm3
MP: 167-172 ° C (lit.)
B.P.: 219-220 ° C10 mm Hg (lit.)
Flash point: 219-220 ° C / 10 mm
Refractive index: 1.531
Water solubility: 550 g / L (25 º C)
Stability: stable Incompatible with bases, strong oxidizing agents. Protect from moisture.
Storage conditions: 2-8 º C
security information
Customs Code: 29221980
WGK Germany：2
Risk category code: R36 / 37 / 38
Safety note: s26-s36-s37 / 39
RTECS number: ty2900000
Danger marker: Xi
toxicology data
acute toxicity
LD50 of rat caliber: 5900 mg / kg; Intravenous LD50 in rats: 1800 mg / kg; LC50: 1210 mg / kg intravenous in mice; Rabbit caliber LD50: 1 mg / kg;
Molecular structural data
1. Molar refractive index: 28.68
2. Molar volume (cm / mol): 90.8
3. Isospecific volume (90.2k): 265.6
4. Surface tension (dyne / cm): 73.2
5. Polarizability (10 cm): 11.37
Computational chemistry data
1. Reference values (xlogp) calculated for hydrophobic parameters: - 2.9
2. Number of hydrogen bond donors: 4
3. Number of hydrogen bond acceptors: 4
4. Number of rotatable chemical bonds: 3
5. Number of tautomers: None
6. Topology molecular polar surface area 86.7
7. Number of heavy atoms: 8
8. Surface charge: 0
9. Complexity: 54
10. Number of isotopic atoms: 0
11. Determining the number of atomic stereocenters: 0
12. Uncertain number of atomic stereocenters: 0
13. Determining the number of chemical bond stereocenters: 0
14. Uncertain number of chemically bonded stereocenters: 0
15. Number of covalent bond units: 1
synthetic method
1. Taken by reduction or catalytic hydrogenation of the corresponding nitro compound.
2. Available nitromethane acts with 3 mol formaldehyde to produce trihydroxymethylnitromethane, which is reduced back to trihydroxymethylaminomethane.
purpose
1. Fosfomycin intermediates, also used as sulfurization enhancers, cosmetics (creams, lotions), mineral oils, paraffin emulsifiers, biological buffers.
2. To be used as acid gas absorbents, formulation buffers, surfactants, emulsifiers and enhancers. Also used in organic synthesis.
Licensing standards
Pinyin Name: andingsanchun
Name in English: tpometamolum
Book title: h1-119
Standard No.: ws1-87 (b) - 89
[C4H11NO3=121.14]
This product is 2-amino-2-hydroxymethyl-1,3-propanediol. Contains c4h11no3 not less than 99.0% as calculated on a dry basis.
character
This article is white crystalline; Odourless, mildly sweet and bitter.
This product is freely soluble in water and is dissolved in ethanol.
Melting point the melting point of this product (Appendix P 13) is 168-172 ° C.
identify
(1) Take 2 ml of potassium periodate solution (0.05 → 10), add 1 drop of nitric acid, mix, add 5 mg of this product, shake, and add 5 drops of silver nitrate ts, i.e., show white turbidity.
(2) Take 0.2 g, add 1 ml to dissolve, add 1 ml of salicylaldehyde saturated solution 1 ml with glacial acetic acid 2 drops, i.e., yellow color.
inspect
Alkalinity take 1 g of this sample and dissolve by adding 20 ml of water to make the assay according to law (Appendix P 33), pH should be 10.0-11.5.
Take 1 g of nickel salt, add 10 ml to dissolve, add 1 ml of ammonia test solution with butanedione oxime test solution 2 ml, and allow to stand 10 minutes, as developed, with standard nickel solution (accurately weigh nickel ammonium sulfate 0.6730 g, into a 1000 ml measuring flask, add appropriate amounts to dissolve and dilute to volume, and shake. Accurately take 10 ml, into a 100 ml measuring flask, dilute to volume with water, and shake) 1.5 ml of a control made with the same method, not deeper (0.0015%).
Loss on drying a sample, dried at 80 ℃ to a constant weight, shall not lose more than 0.6% of its weight (Appendix P 40).
Residue on ignition 对 1g of this substance, and as per law inspection (Appendix P 42) residue on residue shall not exceed 0.1%.
Heavy metals take the residue remaining under the item on residue on ignition, as checked by law (Annex P 38, 2nd law), and contain heavy metals not to exceed 20 parts per million.
Content determination
Take about 0.25 g, accurately weighed, add 80 ml to dissolve, add 2 to 3 drops of methyl red indicator solution, titrate with hydrochloric acid (0.1 mol / L), i.e. Each 1 ml aliquot of HCl (0.1 mol / L) is equivalent to 12.11 mg of c4h11no3.
Role and use
Acid base balance regulating drugs. For acute respiratory, metabolic acidemia.
usage and dosage
Premedication plus glucose injection diluted as 3.6% solution was administered intravenously. Dosage was used at their discretion.
be careful
It is contraindicated in patients with chronic respiratory acidemia and renal acidemia.
Storage
Shade, keep tightly.
pharmacological action
Trometamol is a sodium free amino buffered base that combines with H2CO3 in body fluids to produce bicarbonate. So it can buffer acid but also reduce CO2 tension, has the double effect of correcting acute respiratory acidosis and metabolic acidosis, its effect is faster and stronger than sodium bicarbonate. At pH 7.4, there is only 75% dissociation of THAM, and its undissociated part has high lipid solubility, is easily permeable to the blood-brain barrier and cell membrane, rapidly acts as a buffer acid base in the cell, thus can function simultaneously inside and outside the cell. In addition, this product was quickly eliminated in urine (50% - 70% excretion within 24 h) in its original form, taking h and water, so there was still alkalinized urine and osmotic diuretic effect.
Pharmacokinetic
It can function as soon as 30-40 min after administration, is not metabolized in the body, and is excreted as the crude drug with urine, which is about 60% excreted daily.
indication
For acute metabolic acidosis and acute respiratory acidosis. Because sodium is not available, it is particularly useful in patients with heart failure combined with acidosis. It is useful for hypothermic anesthesia, shock, and rescue of cardiac arrest. Ischemic intracellular acidosis can be treated with this drug after organ transplantation.
contraindication
It is contraindicated in patients with chronic respiratory acidemia and renal acidemia.
Usage
Intravenous drip: estimated with the following formula: 3.64% tham (ML number) = [normal CO2 binding (50%) - measured CO2 binding (vol%)] × zero point six × Body weight (kg). A 7.28% solution will be diluted with an equal volume of 5% - 10% dextrose solution to obtain a 3.64% solution, which can be administered first 1 / 2 to 1 / 3, and later on depending on the condition, and in the emergency situation, a 3.64% solution, 2 ml / kg to 3 ml / kg, can be administered intravenously over 1 h to 2 h. 1 repeat in severe cases.
Adverse effects
This product can cause hypoglycemia, hypotension, nausea, vomiting, and can also depress respiration or even stop breathing.
matters needing attention
Generally, for infusion with a 3.64% solution, a 7.28% solution (i.e., a 0.6m solution) can be used after dilution with an equal volume of 5% - 10% dextrose injection prior to clinical use, and water restricted patients can receive a direct infusion of a 7.28% solution.
Do not spill outside the vein when injecting so as not to cause local necrosis.
May produce a significant reduction in alveolar ventilation, so when used for respiratory acidosis, simultaneous oxygen administration is necessary.
The acidity can often be corrected within 30-40 minutes after injection, and it also improves in 4-6 hours.
Excessive dosing and too rapid infusion should be avoided.
Interactions
① When combined with ACTH, ACTH, and androgens, hypernatremia and edema may occur.
② In combination with amphetamine, quinidine, the latter two reduced by renal excretion. Susceptibility to toxic effects; Alkalinize urine and affect renal excretion of ephedrine, so the dose of ephedrine should be reduced when combined.
③ In combination with anticoagulants such as warfarin, m-cholinesterase drugs, H2 receptor antagonists such as ranitidine, etc., the latter decrease in absorption.
④ Coadministration with calcium containing medicines, milk and dairy products may cause milk alkali syndrome.
⑤ In combination with potassium depleting diuretics, increased risk of developing hypochloremic alkalosis.
⑥ Increased oral absorption of levodopa.
⑦ Increased renal excretion of salicylic acid preparations; Increased sodium load increases renal excretion of lithium, so when combined with lithium, the lithium dose should be adjusted as appropriate.
⑧ The combination of the two is not advocated since alkalinized urine inhibits the conversion of meth oate to formaldehyde, thereby inhibiting its therapeutic effect.
Expert commentary
This product is an amino buffered base without sodium, which combines with H2CO3 in body fluids to generate bicarbonate. So he can buffer acid but also reduce CO2 tension, has the double effect of correcting acute respiratory acidosis and metabolic acidosis, and its effect is faster and stronger than sodium hydrogen carbonate. Clinically used for acute metabolic and acute respiratory acidosis. Generally, it is instilled with 3.64% solution, and those with limited moisture can be instilled with 7.28% solution directly intravenously, but excessive dosage and too fast instillation should be avoided. It should be used with caution in those with renal insufficiency and contraindicated in those without.