장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴(노출되어도 특정 표적장기 독성을 일으키지 않는다는 결정적인 노출경로가 있다면 노출경로를 기재)
특정 표적장기 독성 - 1회 노출
구분 1
위험
P260, P264, P270, P307+P311, P321,P405, P501
예방조치문구:
P210
열·스파크·화염·고열로부터 멀리하시오 - 금연 하시오.
P260
분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P310
삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P311
의료기관(의사)의 진찰을 받으시오.
NFPA 704
0
2
0
Tapentadol Hydrochloride C화학적 특성, 용도, 생산
개요
Agonism of the MOR is a common strategy for moderate to severe
pain intervention. Opioid drugs, such as morphine, that modulate this
receptor have demonstrated efficacy in acute situations; however, chronic
conditions, particularly those of neuropathic or inflammatory etiology,
suffer from inadequate pain management with this treatment. With a
narrow therapeutic window, traditional MOR agonists flirt with side
effects at optimal analgesia, and prolonged use increases the potential
for physical dependency. Since extensive efforts to design activators of
MOR have failed to dissociate the undesirable adverse effects from the
analgesic properties, the focus has been on enhancing the analgesic
efficacy through a dual mechanism of action. Tapentadol hydrochloride
brings this concept to fruition; MOR agonism is coupled with noradrenaline reuptake inhibition in a combinatory contribution to analgesia. Compared to morphine, it is about 50-fold less potent for MOR (Ki = 100 nM
for tapentadol versus 2 nM for morphine). The Ki for inhibition of noradrenaline reuptake was 500 nM while reuptake of serotonin was only
weakly inhibited (Ki = 2.5μM). Despite its lower affinity for MOR, the
dual mechanism has provided an efficacious profile in both acute and
chronic conditions with fewer side effects.
화학적 성질
Light Brown Solid
용도
A novel, centrally acting oral analgesic with a dual mode of action that has demonstrated efficacy in preclinical and clinical models of pain relief.
Clinical Use
Tapentadol was approved by the FDA in November 2008 for the
treatment of moderate to severe acute pain. It is a centrally acting
analgesic that acts as both an agonist at the l-opiod receptor and
as a norepinephrine re-uptake inhibitor, allowing it to have
efficacy similar to potent narcotic analgesics but without their side
effects. The drug was developed by Grunenthal and Johnson & Johnson and was marketed starting in 2009.
부작용
The common adverse effects of tapentadol were nausea, vomiting, somnolence, dizziness, and itching. As with all opioid medications, constipation was also an issue. Tapentadol is contraindicated in patients taking monoamine oxidase inhibitors because of the potential for adverse cardiovascular events due to additive effects on norepinephrine levels. As with other MOR agonists, it is also contraindicated in patients with paralytic ileus. In patients with a history of epilepsy or seizure, tapentadol may induce seizures. Since tapentadol causes somnolence, its combination with other sleep aids could dangerously affect breathing. Similarly, patients with existing breathing or lung problems are cautioned about using tapentadol. Furthermore, patients with past or present substance abuse or drug addiction should consult the doctor prior to use since physical dependency and addiction is a risk with tapentadol. Alcohol should be avoided due to the potential additive effect on CNS depression.
