트라마돌

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H301：삼키면 유독함

  H336：졸음 또는 현기증을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

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

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

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

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P321：(…) 처치를 하시오.

  P330：입을 씻어내시오.

  P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

트라마돌 화학적 특성, 용도, 생산

• 화학적 성질

  Light Yellow Oil

• 용도

  Tramadol is thought to produce analgesia by two distinct actions. First, it has agonist activity at the MOP and KOP receptors. Tramadol itself is a prodrug, with most of its analgesia mediated by a metabolite – O-desmethyltramadol – that has a 200-fold higher affinity for the MOP receptor. I t is metabolised by cytochrome P450 (CYP2D6 and CYP3A4), and its potency is therefore affected by a patient's CYP genetics, with rapid and poor metabolisers.
  S econd, it enhances the descending inhibitory systems in the spinal cord by inhibiting noradrenaline reuptake and releasing serotonin from nerve endings. It is available in immediate- and sustained-release oral preparations and for parenteral administration. I ts use is contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs). Caution must also be exercised in hepatic impairment as its clearance is reduced to a much greater extent than morphine and related agents.

• 일반 설명

  Tramadol (Ultram) is an analgesic agent with multiple mechanismsof action. It is a weak μ-agonist with approximately30% of the analgesic effect antagonized by the opioid antagonistnaloxone. Used at recommended doses, it has minimaleffects on respiratory rate, heart rate, blood pressure, or GItransit times. Structurally, tramadol resembles codeine with the B, D, and E ring removed. The manufacturer states thatpatients allergic to codeine should not receive tramadol, becausethey may be at increased risk for anaphylactic reactions. Tramadol is synthesized and marketed as the racemicmixture of two (the [2S, 3S] [-] and the [2R, 3R] [+]) of thefour possible enantiomers. The (+) enantiomer is about30 times more potent than the (—) enantiomer; however,racemic tramadol shows improved tolerability.Neurotransmitter reuptake inhibition is also responsible forsome of the analgesic activity with the (—) enantiomer primarilyresponsible for norepinephrine reuptake and the (+)enantiomer responsible for inhibiting serotonin reuptake. Like codeine, tramadol is O-demethylated viaCYP2D6 to a more potent opioid agonist having 200-foldhigher affinity for the opioid receptor than the parent compound.Tramadol was initially marketed as nonaddictive, anda 3-year follow up study showed that the abuse potential isvery low, but not zero. Most abusers of tramadol have abusedopioid drugs in the past. Both enantiomers of tramadoland the major O-demethylated metabolite are proconvulsive,and tramadol should not be used in patients with a lowseizurethreshold including patients with epilepsy.

• Mechanism of action

  Fentanyl is a μ agonist with approximately 80 times greater potency than morphine. Fentanyl has been used in combination with nitrous oxide for “ balanced” anesthesia and in combination with droperidol for “ neurolepalgesia.” The advantages of fentanyl over morphine for anesthetic procedures are its shorter duration of action (1–2 hours) and the fact that it does not cause histamine release on intravenous injection.

• Pharmacokinetics

  The analgesic activity of tramadol is attributed to a synergistic effect caused by the opioid activity of the (+)-isomer and the neurotransmitter reuptake blocking effect of the (–)-isomer. The (+)-isomer possesses weak μ opioid agonist activity equivalent to approximately 1/3,800 that of morphine. The O-desmethyl metabolite (CYP2D6) of (±)-tramadol has improved μ opioid activity equivalent to 1/35 that of morphine. Affinity for both δ and κ receptors is improved. Despite its higher opioid potency, the contribution of O-desmethlytramedol to the overall analgesic effect has been questioned but not well studied. Individuals who lack CYP2D6 or are taking a CYP2D6 inhibitor have a reduced effect to tramadol. The fact that naloxone causes a decrease in the analgesic potency of tramadol argues strongly for an opioid component to the analgesic activity. (–)-T ramadol possesses only 1/20 the opioid activity of its (+)-isomer, but it has good activities for inhibition of norepinephrine (Ki = 0.78 μM) and serotonin (Ki = 0.99 μM) reuptake. Tramadol's neurotransmitter reuptake activity is approximately 1/20 that of imipramine, a tricyclic antidepressant agent that is used widely in pain management. Although none of the individual pharmacological activities of tramadol is impressive, they interact to give a synergistic analgesic effect that is clinically useful.
  Tramadol has been used in Europe since the 1980s and was introduced to the U.S. market in 1995. The drug is nonaddicting and, thus, is not a scheduled agent. In addition, tramadol does not cause respiratory depression or constipation.

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