Arch Pharm (Weinheim). 1992 Nov;325(11):733-9.
[Synthesis of enantiomerically pure 6,10-epoxybenzocycloocten-7-amines with CNS activity]

[Article in German]

Wunsch B, Zott M, Hofner G.

Institut fur Pharmazie und Lebensmittelchemie, Universitat Munchen.

In an oxa-Pictet-Spengler reaction the methyl (S)-phenyllactate 6 and methyl levulinate (7a) are condensed to the 2-benzopyrans cis-8a and trans-8a, which react with CH3I to yield the dimethyl ethers cis-9a and trans-9a. Cis-9a and trans-9a can be separated by medium pressure liquid chromatography. In the subsequent Dieckmann-Cyclisation cis-9a is transformed to the laevorotatory beta-ketoester (-)-10a, while the dextrorotatory enantiomer (+)-10a is obtained from trans-9a after C-3-epimerisation. With Eu(hfc)3 the ketone (-)-11, prepared by saponification and decarboxylation of (-)-10a, proves to be enantiomerically pure. By reductive amination, ketone (-)-11 is transformed to the amines (-)-12a and (-)-12b. Symptoms typical for central damping are caused after i.p. application of (-)-12a and (-)-12b to mice. In the mouse writhing-test (-)-12a HCl affords an ED50-value of 7.0 mg/kg, comparable with the ED50-value of tramadol.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1485838&dopt=Abstract tramadol Ultram




Dermatol Surg. 2004 Feb;30 Suppl 2:253-6.
Sentinel node biopsy in melanoma of the trunk and the extremities in tumescent local anesthesia.

Eichhorn K, Renner R, Frithjof Haustein U.

University Hospital Leipzig, Department of Dermatology, Dermatologic Surgery Unit, Leipzig, Germany.

BACKGROUND. : The sentinel node biopsy (SNB) of axilla and groin is a common staging procedure and can be done in both general anesthesia and local anesthesia. OBJECTIVE. : To investigate the efficacy of tumescent local anesthesia (TLA) as a widely used type of local anesthesia in dermatologic surgery for the SNB of axilla and groin. METHOD. : From 1999 to 2002, 195 patients underwent a SNB of axilla or groin. A 0.1% tumescent solution with prilocaine was used. In cases in which local anesthesia did not produce complete analgesia, there was additional medication using Midazolam and Tramadol. RESULTS. : In 74.9% of the patients, TLA was sufficient as the sole method. In 25.1%, sedation became necessary. Additional medication was required for 31.9% of the patients with SNB in the axilla and for 17.3% with SNB in the groin; 26.6% of the patients with SNB of both axillas and 25% with SNB of the axilla and the groin received additional medication using Midazolam. Two patients with a SNB of the axilla received a combination of Midazolam and Tramadol. CONCLUSION. : SNB of the axilla and the groin in TLA is a good alternative to other anesthetic techniques, for example, general anesthesia or infiltration anesthesia.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14871218&dopt=Abstract tramadol Ultram [PubMed - in process]




Klin Wochenschr. 1991;69 Suppl 26:84-8.
[Arousal in various analgosedation schedules]

[Article in German]

Lierz P, Hoffmann P, Schockenhoff B.

Abteilung fur Anasthesiologie und operative Intensivmedizin, Allgemeines Krankenhaus Hamburg-Barmbek.

The patterns of recovery of patients who received seven different analgesic and sedative treatments were investigated with regard to the time at which the subjects awoke. For observations of the neurologic status, we developed a special score. The analgesic and sedative therapies were given at three various doses. The combination of fentanyl/midazolam, alfentanil/midazolam and ketamine/flunitrazepam showed the best results. Piritramid/promethazine, pethidine/flunitrazepam, pethidine/promethazine and tramadol/methohexital required more time for awakening. On the basis of these results, we prefer to use the combination of fentanyl/midazolam, alfentanil/midazolam and ketamine/flunitrazepam to judge all patients' neurologic scores.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1687605&dopt=Abstract tramadol Ultram




Biull Eksp Biol Med. 1991 Feb;111(2):126-8.
[The effect of microinjections of morphine and tramadol into the locus coeruleus on the nociceptive responses of the spinal cord neurons and on shifts in the arterial pressure]

[Article in Russian]

Kolchin VV, Zaitsev AA.

Morphine and tramadol produces selective inhibition of the spinal noxious-evoked activity, but does not change blood pressure reactions. Antinociception was reversed by this structure injection of the naloxone. These data suggest that locus coeruleus realized the pain-relief effect of the opiate drugs.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1854949&dopt=Abstract tramadol Ultram




Acta Physiol Hung. 1991;77(2):173-8.
Relationship between the antitussic and analgesic activity of substances.

Nosal'ova G, Strapkova A, Korpas J.

Department of Pathophysiology and Pharmacology, Faculty of Medicine, Comenius University, Sklabinska, Czechoslovakia.

The authors studied relationship between the antitussic and analgesic activity of substances. The antitussic effect of codeine, tilidine, tramadol and pentazocine has been studied in nonanesthetized healthy cats. The drugs except tilidine, were administered intraperitoneally in a dose of 10 mg/kg body weight. Tilidine was administered intramuscularly in the same dose. Cough induced in nonanesthetized cats by mechanical irritation of laryngopharyngeal and tracheobronchial areas was evaluated by changes of the lateral tracheal pressure. A significant decrease of the subsequent cough parameters was observed after the application of codeine, tilidine, tramadol and pentazocine. Naloxone given 5 min before the application of the drug has not prevented the cough-suppressing effect due to codeine. Naloxone alone administered in a dose of 1 mg/kg body weight has not significantly influenced the experimentally-induced cough reflex in nonanesthetized cats.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1927541&dopt=Abstract tramadol Ultram