Is methimazole water soluble?
Is methimazole water soluble?
Solubility : Soluble in DMSO (23 mg/ml at 25° C), ethanol (23 mg/ml at 25° C), chloroform (~222.22 mg/ml), water (~200 mg/ml), and methanol.
Is Carbimazole soluble in water?
Solubility (25°C)
| In vitro | DMSO | 38 mg/mL (204.04 mM) |
|---|---|---|
| Ethanol | 15 mg/mL (80.54 mM) | |
| Water | Insoluble |
What is the MOA of methimazole?
Methimazole prevents iodine and peroxidase from their normal interactions with thyroglobulin to form T4 and T3. This action decreases thyroid hormone production. Methimazole also interferes with the conversion of T4 to T3. Since T3 is more potent than T4, this also reduces the activity of thyroid hormones.
What is methimazole derived from?
Methimazole, 1-methyl-2-imidazolthiol (25.2. 5), is synthesized by reacting aminoacetic aldehyde diethylacetal with methylisothiocyanate and subsequent hydrolysis of the acetal group of the resulting disubstituted urea derivative 25.2.
How is methimazole metabolized?
Methimazole is rapidly and extensively metabolized by the liver, mainly via the CYP450 and FMO enzyme systems.
What class is methimazole?
Methimazole is a member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. It has a role as an antithyroid drug.
What is the difference between methimazole and Carbimazole?
Carbimazole has a higher molecular weight than methimazole, so 5 mg of carbimazole is equivalent to 3 mg of methimazole. The starting dose for carbimazole is 5 mg every 8 to 12 hours.
What class of drug is Carbimazole?
Carbimazole and propylthiouracil belong to a group (class) of medicines called thionamides. Thionamides have similar actions on the thyroid gland.
When do you hold methimazole?
Stop methimazole if the count is less than 1000 per ml. Treat fever or any apparent infections with intravenous antibiotics.
What is the indication of methimazole?
In the United States, methimazole is indicated for the treatment of hyperthyroidism in patients with Graves’ disease or toxic multinodular goiter for whom thyroidectomy or radioactive iodine therapy are not appropriate treatment options.
Where is Carbimazole absorbed?
Carbimazole (CBZ) is immediately metabolized in serum to methimazole (MMI), and it has been calculated that 10 mg of CBZ yields 6 mg of MMI. All the antithyroid drugs are rapidly and almost completely absorbed from the gastrointestinal tract, with peak serum concentrations at 1 or 2 h.
What is the name of the compound with the formula methimazole?
Methimazole Description. Methimazole, USP (1-methylimidazole-2-thiol) is a white, crystalline substance that is freely soluble in water. It differs chemically from the drugs of the thiouracil series primarily because it has a 5- instead of a 6-membered ring.
What is the difference between thiouracil and methimazole?
It differs chemically from the drugs of the thiouracil series primarily because it has a 5- instead of a 6-membered ring. Each tablet contains 5 or 10 mg (43.8 or 87.6 μmol) Methimazole, an orally administered antithyroid drug.
What does methimazole do to the thyroid?
Methimazole. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).
How is methimazole absorbed in the body?
Methimazole is rapidly absorbed from the GI tract following oral administration with peak plasma concentrations occurring within about 1 hour. Methimazole readily crosses the placenta and is distributed into milk in concentrations approximately equal to those in maternal serum. The drug is excreted in urine.
