Molecular Formula | C9H10Cl3N3O |
Molar Mass | 282.55 |
Melting Point | 215-217℃ |
Solubility | ≥ 14.1 mg/mL in DMSO, ≥ 17.17 mg/mL in EtOH with ultrasonic and warming, ≥ 50.6 mg/m |
Appearance | Solid |
Color | white |
Merck | 14,4561 |
Storage Condition | Inert atmosphere,Room Temperature |
Use | This product is for scientific research only and shall not be used for other purposes. |
UN IDs | 3249 |
WGK Germany | 3 |
RTECS | CY1481000 |
HS Code | 2925294500 |
Hazard Class | 6.1(b) |
Packing Group | III |
Toxicity | LD50 in mice: 165 mg/kg orally (Coward) |
pharmacological effects | guanfacine hydrochloride is a central antihypertensive drug, and its pharmacological effects are similar to clonine. It is a central α2 receptor activator, which activates the central α2 receptor, reduces peripheral sympathetic nerve activity, and causes blood pressure to drop. The antihypertensive effect of this drug is weaker than that of clonine. Therefore, the dose is 7~10 times larger than that of clonine, and the sedative effect of the central nervous system is also weak, and the action site may be different from clonine. |
pharmacokinetics | guanfacine hydrochloride is absorbed quickly and completely by oral administration. the antihypertensive effect reaches a peak 6 hours after oral administration and lasts for more than 24 hours. The oral half-life is 21 h. Therefore, the drug is more easily distributed to various tissues, so the drug concentration in the blood is low, and the plasma protein binding rate is low. Most drugs are metabolized in the body. The main metabolites are 3-hydroxy derivatives and oxidized thiol uric acid derivatives, 80% metabolites are excreted by the kidneys. |
indications | guanfacine hydrochloride is suitable for the treatment of patients with moderate and severe hypertension. Can be used alone or in combination with diuretics. The antihypertensive effect is similar to that of clonine, with an average effective rate of 70%. |
adverse reactions | guanfacine hydrochloride common adverse reactions include dry mouth, lethargy, orthostatic hypotension and constipation. Sudden withdrawal of long-term medication also has withdrawal syndrome, which is manifested as headache, mental tension, palpitations, tremor and elevated blood pressure. Discontinuation syndrome usually occurs within 2~7 days after withdrawal. |
usage and dosage | oral administration for adults: start once a day, 0.5~1 mg each time. Take it before bed. According to the blood pressure, the dose is increased by 2mg/d, once taken. Taking this drug does not produce drug resistance. |
biological activity | Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with antihypertensive effect. |
Target | Value |