Tapentadol Hydrochloride

한글명:Tapentadol Hydrochloride

카스 번호175591-09-0

상품명:Tapentadol Hydrochloride

CBNumberCB71565532

분자식C14H24ClNO

포뮬러 무게257.81

MOL 파일175591-09-0.mol

화학적 성질

녹는점	178-194°C
인화점	9℃
저장 조건	-20°C Freezer, Under Inert Atmosphere
용해도	DMF: 20 mg/ml; DMSO: 25 mg/ml; Ethanol: 20 mg/ml; PBS (pH 7.2): 10 mg/ml
물리적 상태	A neat solid

위험 및 안전 성명

위험품 표기

F,T

위험 카페고리 넘버

11-23/24/25-39/23/24/25

안전지침서

7-16-36/37-45

유엔번호(UN No.)

UN1230 - class 3 - PG 2 - Methanol, solution

WGK 독일

NFPA 704:

	0
2		0

그림문자(GHS)

Tapentadol Hydrochloride 화학적 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 (K_i = 100 nM for tapentadol versus 2 nM for morphine). The K_i for inhibition of noradrenaline reuptake was 500 nM while reuptake of serotonin was only weakly inhibited (K_i = 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.

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