• 한국임상약학회지
• /
• 제21권1호
• /
• pp.36-38
• /
• 2011

We report an unusual case of respiratory depression and prolonged apnea after the second dose of 100-mg intravenous tramadol. Due to continuous pain at foley catheter keep site, intravenous tramadol was administered to the patient. Soon after the second dose of tramadol injection, the patient became apneic. The patient did not respond to verbal command and started exhibiting oxygen desaturation. The patient was quickly treated with 100% oxygen, and it took 4 hours for the spontaneous respiration to return to regular. This case report demonstrates that even two doses of tramadol administered intravenously may manifest as sudden and prolonged apnea. Respiratory depression with tramadol has been reported in patients with impaired renal functions and Cytochrome P(CYP) 2D6 gene duplication.

• Biomolecules & Therapeutics
• /
• 제31권2호
• /
• pp.168-175
• /
• 2023

Tramadol is an opioid analog used to treat chronic and acute pain. Intradermal injections of tramadol at hundreds of millimoles have been shown to produce a local anesthetic effect. We used the whole-cell patch-clamp technique in this study to investigate whether tramadol blocks the sodium current in HEK293 cells, which stably express the pain threshold sodium channel Na_v1.7 or the cardiac sodium channel Na_v1.5. The half-maximal inhibitory concentration of tramadol was 0.73 mM for Na_v1.7 and 0.43 mM for Na_v1.5 at a holding potential of -100 mV. The blocking effects of tramadol were completely reversible. Tramadol shifted the steady-state inactivation curves of Na_v1.7 and Na_v1.5 toward hyperpolarization. Tramadol also slowed the recovery rate from the inactivation of Na_v1.7 and Na_v1.5 and induced stronger use-dependent inhibition. Because the mean plasma concentration of tramadol upon oral administration is lower than its mean blocking concentration of sodium channels in this study, it is unlikely that tramadol in plasma will have an analgesic effect by blocking Na_v1.7 or show cardiotoxicity by blocking Na_v1.5. However, tramadol could act as a local anesthetic when used at a concentration of several hundred millimoles by intradermal injection and as an antiarrhythmic when injected intravenously at a similar dose, as does lidocaine.

• 한국임상수의학회지
• /
• 제29권3호
• /
• pp.226-232
• /
• 2012

본 연구는 승용말에 detomidine과 tramadol을 정맥 투여한 후 진정 및 진통 효과를 평가하기 위하여 실시되었다. 여섯 마리의 승용말에 각각 detomidine (10 ${\mu}g/kg$), tramadol (2 mg/kg) 및 detomidine/tramadol 병용 (각 10 ${\mu}g/kg$과 2 mg/kg) 투여하였다. 심박수, 호흡수, 직장체온, 간접동맥혈압, 위장관 운동에서 detomidine과 detomidine/tramadol 병용은 큰 차이를 보이지 않았다. 진정효과는 detomidine, detomidine/tramadol 병용 투여 후 5분에 관찰되기 시작하였으나, detomidine 및 detomidine/tramadol 병용간 유의한 진정효과의 차이는 나타나지 않았다. Detomidine과 detomidine/tramadol 병용은 투여 후 50분까지 유사한 진통효과를 나타내었으나, detomidine/tramadol 병용이 더 긴 진통효과를 나타내었다. Detomidine의 투여 후 혈당 수치가 투여 후 60분까지 증가하였으나, detomidine/tramadol 병용 투여 후의 혈당 수치는 증가하지 않았다. Tramadol과 detomidine/tramadol 병용 투여된 한 마리가 투여 5분 이내에 흥분된 행동을 보였다. 이상의 결과로부터 detomidine/tramadol 병용 투여가 기립상태에서 말의 간단한 외과적 처치와 진단을 위하여 유용하게 이용될 수 있을 것으로 판단된다.

• 한국임상수의학회지
• /
• 제27권6호
• /
• pp.668-673
• /
• 2010

본 연구는 tramadol과 medetomidine이 개에서 isoflurane의 최소폐포농도에 미치는 영향에 대해 알아보고자 하였다. Isoflurane의 최소폐포농도는 1 ml의 생리식염수(control), $2{\mu}g$/kg의 medetomidine (M2), 4 mg/kg의 tramadol (T4), $2{\mu}g$/kg medetomidine과 4 mg/kg tramadol (M2T4)의 투여 네 가지 경우에 따라 측정되었다. 실험 중 심박수, 혈압, 호흡수, 호기말 이산화탄소분압, 혈중산소포화도, 체온을 측정하였다. M2, T4, M2T4 투여 후 isoflurane의 최소 폐포농도는 각각 $0.81{\pm}0.17%$, $0.81{\pm}0.14%$, $0.62{\pm}0.13%$로 대조군$1.13{\pm}0.19%$ 에 비해서 낮았다. 심박수는 M2, T4, M2T4 투여 시 낮았고 혈압은 M2T4투여 시에만 유의적으로 높았다. Tramadol 과 medetomidine의 투여 및 두 약물의 혼합투여는 isoflurane의 최소폐포농도를 유의적으로 낮추었다. 특히 tramadol과 medetomidine의 혼합투여는 마취제의 절감효과와 심혈관계에 있어 변화가 적기 때문에 전마취제로서 유용하게 사용될 수 있을 것이다.

• The Korean Journal of Physiology and Pharmacology
• /
• 제14권3호
• /
• pp.191-198
• /
• 2010

The effects of different doses of tramadol on analgesia and electroencephalographic (EEG) spectralparameters were compared in rats. Saline or tramadol 5, 10, 20 or 40 mg/kg was administered. The degree of analgesia was evaluated by tail-flick latency, and the degree of seizure was measured using numerical seizure score (NSS). Additionally, band powers, median power frequency and spectral edge frequency 95 were measured to quantify the EEG response. All doses of tramadol produced spike-wave discharge. Tramadol significantly and dose-dependently increased the analgesia, but these effects did not correspond with the changes in the EEG spectral parameters. NSS significantly increased in the Tramadol 20 and 40 mg/kg treatment groups compared to the Control and TRA5 groups, and two rats given 40 mg/kg had convulsions. In conclusion, tramadol dose-dependently increased the analgesic effect, and the 10 mg/kg dose appears to be a reliable clinical dose for analgesia in rats, but dose-dependent increases in analgesia and seizure severity did not correlate with EEG spectral parameters.

• The Korean Journal of Pain
• /
• 제14권2호
• /
• pp.150-155
• /
• 2001

Background: Tramadol is known to be a weak opioid. However, it has also been shown that tramadol is an effective norepinephrine and serotonin uptake blocker, which may be effective in the treatment of neuropathic pain. The present study was undertaken in order to assess the antinociceptive action of tramadol and to investigate possible antinociceptive mechanisms by using antagonists in an animal neuropathic pain models in rats. Methods: Rats were prepared with tight ligation at the left 5 and 6th lumbar spinal nerves (Kim and Chung's neuropathic pain model). The antinociceptive effects of tramadol (10, 20, and 50 mg/kg i.p.) in rats with neuropathic pain were assessed. Additionally, following coadministration of antagonists such as naloxone (1 mg/kg i.p.), yohimbine (1 mg/kg i.p.) and ritanserin (1 mg/kg i.p.) with 50 mg/kg of tramadol, the responses to mechanical and thermal stimuli were measured over a two-hour period. Results: Tramadol displayed potent antinociceptive effects in a dose-dependent manner on rats with neuropathic pain (P < 0.05). The effects of tramadol were inhibited by coadministered naloxone and yohimbine in rats with mechanical and thermal allodynia, respectively (P < 0.05). However, there were no significant changes in the pain behaviors in the case of ritanserin. Conclusions: Tramadol showed significant antinociceptive effects in rats with regards to neuropathic pain against both mechanical and thermal allodynia. The antinociceptive effect on the mechanical stimuli is medicated via an opioid receptor. However, it appears that the antinociceptive effects on thermal allodynia are mediated via a noradrenalin receptor vice a serotonergic receptor.

• The Korean Journal of Pain
• /
• 제11권1호
• /
• pp.54-59
• /
• 1998

Background: Tramadol administered epidurally is known to have one-thirtieth the potency of morphine for treatment of pain following abdominal surgery. We designed a prospective, randomized, controlled study to evaluate the analgesic efficacy and safety of combined epidural infusion of bupivacaine and tramadol with 2-day infusor as ompared to bupivacaine and morphine combined epidural infusion. Methods: Sixty healthy women scheduled for Cesarean delivery were assigned randomly in double- blind fashion: Group 1 (n=20) were given a mixture of morphine 10 mg(1 ml), 0.5% bupivacaine 40 ml and normal saline(NS) 40 ml; Group 2(n=20) a mixture of tramadol 300 mg(6 ml), 0.5% bupivacaine 40 ml and NS 54 ml; Group 3(n=20) or a mixture of tramadol 500 mg(10 ml), 0.5% bupivacaine 50 ml and NS 50 ml, of continuous dose via epidural route following 1% lidocaine 6 ml as bolus dose for 48 hours postoperatively. We evaluated the analgesic efficacy and side effects of these three groups using visual analogue pain scale (VAPS) and verbal rating scale (VRS). Results: VAPS of group 1 and 3 were lower than group 2, and VAPS of group 1 was lower than group 3(12, 24, 36, 48 hours). VRS of group 1 and 3 were lower than group 2 (12, 24, 36 hours). There were incidences of pruritus was 16 patients in group 1. Conclusions: Tramadol does possess the analgesia effect of morphine, but has the added analgesia following increment. Further research to determine the most effective administration method and reguired dosage of tramadol is further needed.

• 분석과학
• /
• 제31권3호
• /
• pp.107-111
• /
• 2018

Currently, ultraviolet-visible spectrophotometry and titration methods are used for assay tests of tramadol hydrochloride injection and raw material in the Korean Pharmacopoeia XI (KP XI). Titration has also been used in the British Pharmacopoeia (BP 2013) for the assay test of tramadol hydrochloride, and the HPLC assay for tramadol hydrochloride raw material has been used in the United States Pharmacopeia (USP 39). In this study, we developed an alternative HPLC assay method for tramadol hydrochloride injection that is up to date and specific, and employs the same method as tramadol hydrochloride capsules. Validation of the HPLC method was conducted to determine linearity, precision, accuracy, system suitability, and robustness. The linearity of the calibration curves in the desired concentration range was good ($r^2$ > 0.9999). RSDs of intra-day precision obtained were 0.05-0.08 % and inter-day precision obtained were 0.08-0.19 %. Accuracy was obtained with recoveries in the range of 98.16 % and 100.90 %. As a result of the system's suitability, the RSD of both retention time and the peak area obtained were 0.07 %. The values of the plate number and tailing factor of tramadol hydrochloride obtained were 7076 and 1.16, respectively. Because of the intermediate precision and robustness of the developed assay, it is expected to become a valuable tool for revising the Korean Pharmacopoeia (KP XI).

• 한국임상수의학회지
• /
• 제33권6호
• /
• pp.325-331
• /
• 2016

This study investigated the antinociceptive effect of epidural tramadol with bupivacaine in 36 healthy Beagle dogs. The dogs were divided into 6 groups; 1) C (control), 2) B (0.5% bupivacaine 0.1 mL/kg), 3) BT0.5 (0.5% bupivacaine 0.1 mL/kg + tramadol 0.5 mg/kg), 4) BT1 (0.5% bupivacaine 0.1 mL/kg + tramadol 1 mg/kg), 5) BT2 (0.5% bupivacaine 0.1 mL/kg + tramadol 2 mg/kg), 6) BT3 (0.5% bupivacaine 0.1 mL/kg + tramadol 3 mg/kg). The epidural injection was performed under isoflurane inhalation, after then, nociceptive block and motor block scores were assessed with physiologic parameters (HR, RR, RT, MAP). BT groups showed significantly longer antinociceptive time than C and B, while motor block time of BT groups were not different from B except BT3. Durations of total nociceptive block of BT2 ($60.83{\pm}19.08min$) and BT3 ($74.17{\pm}8.61min$) were significantly longer than those of BT0.5 ($33.33{\pm}8.76min$) and BT1 ($37.50{\pm}19.43min$), but there was no significant difference between BT2 and BT3. Durations of total motor block in all groups were less than 20 minutes although that of BT3 was significantly longer than B. There were no significant differences in HR, RR, RT, MAP among groups. Consequently, epidural administration of tramadol (2 mg/kg) with 0.5% bupivacaine (0.1 mL/kg) can be used safely and effectively in dogs.

• Journal of Yeungnam Medical Science
• /
• 제37권4호
• /
• pp.329-331
• /
• 2020

Negative myoclonus (NM) is a shock-like jerky involuntary movement caused by a sudden, brief interruption of tonic muscle contraction. NM is observed in patients diagnosed with epilepsy, metabolic encephalopathy, and drug toxicity and in patients with brain lesions. A 55-year-old man presented with NM in both his arms and neck. He has taken medications containing tramadol at a dose of 80-140 mg/day for 5 days due to common cold. He had no history of seizures. Acute lesions were not observed during magnetic resonance imaging, and abnormal findings in his laboratory tests were not noted. His NM resolved completely after the discontinuation of tramadol and the oral administration of clonazepam. Our case report suggests that tramadol can cause NM in patients without seizure history or metabolic disorders, even within its therapeutic dose.