GUANABENZ ACETATE

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H301：삼키면 유독함

• 예방조치문구

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P301+P310：삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

GUANABENZ ACETATE 화학적 특성, 용도, 생산

• 용도

  antihypertensive

• 일반 설명

  Guanabenz acetate, [(2,6-dichlorobenzylidene)amino]guanidine monoacetate (Wytensin), is acentral 2-adrenergic agonist that reduces the release of norepinephrinefrom the neuron when stimulated. The effect ofthe drug results in decreased sympathetic tone in the heart,kidneys, and peripheral blood vessels. The drug does not produceorthostatic hypotension.

• 생물학적 활성

  α 2 -adrenergic agonist and IGRS (imidazoline I 2 binding site) selective ligand.

• Pharmacokinetics

  The oral bioavailability of guanabenz is 70 to 80%. Following an oral dose, the hypotensive effect of guanabenz begins within 1 hour, peaks within 2 to 7 hours, and is diminished within 6 to 8 hours. It has an elimination half-life averaging 4 to 14 hours. The blood pressure response can persist for at least 12 hours. Following IV dosing, guanabenz is distributed into the CNS, with brain concentrations 3 to 70 times higher than concurrent plasma concentrations. Guanabenz is approximately 90% bound to plasma proteins. In patients with hepatic or renal impairment, its elimination half-life may be prolonged.
  Guanabenz is metabolized principally by hydroxylation to its inactive metabolite, 4-hydroxyguanabenz, which is eliminated in the urine as its glucuronide (major) and sulfate conjugates. Guanabenz and its inactive metabolites are excreted principally in urine, with approximately 70 to 80% of its oral dose excreted in urine within 24 hours and approximately 10–30% in feces via enterohepatic cycling. Approximately 40% of an oral dose of guanabenz is excreted in urine as 4-hydroxyguanabenz and its glucuronide, and less than 5% is excreted unchanged. The remainder is excreted as unidentified metabolites and their conjugates.

• Clinical Use

  Overall, the therapeutic applications for guanabenz are similar to those of clonidine and other α2-adrenergic agonists. One advantage for guanabenz is its once-a-day dosing schedule. Guanabenz has been used in diabetic patients with hypertension without adverse effect on the control of or therapy for diabetes, and it has been effective in hypertensive patients with chronic obstructive pulmonary disease, including asthma, chronic bronchitis, or emphysema. Guanabenz has been used alone or in combination with naltrexone in the management of opiate withdrawal in patients physically dependent on opiates and undergoing detoxification. Guanabenz also has been used as an analgesic in a limited number of patients with chronic pain

• 부작용

  Overall, the frequency of adverse effects produced by guanabenz is similar to that produced by clonidine and the other α2-adrenergic agonists, but the incidence is lower. As with the other centrally active sympatholytics (e.g., clonidine), abrupt withdrawal of guanabenz may result in rebound hypertension, but the withdrawal syndrome symptoms appear to be less severe.

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