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Results for “Tilidine”

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Double blind study with nefopam, tilidine and placebo, for postoperative pain suppression.

A double-blind study involving 101 patients was done to assess the efficacy of parenteral nefopam (0.66 mg/kg) for postoperative pain suppression, in comparison to tilidine (1.67 mg/kg) or placebo. The difference in painfree duration for both active drugs compared to placebo is significant, but no significant difference was present between them; although tilidine was a little longer acting. At no moment a significant difference was present in the pain score of the patients receiving one of both active drugs. Only minor changes of blood pressure, heart rate and respiratory frequency were seen and marked side effects were not present in any of the patients.

Adolescent↗

[Comparison of diflunisal and tilidine in tumor pain].

In an open study in patients with tumour-induced pain the analgetic effects of the prostaglandin-inhibiting compound diflunisal and the centrally-acting analgetic tilidine N were compared. A dosage of 1 g diflunisal was found to be equivalent to 50 drops of tilidine N and to be subjectively well-tolerated. In the pain-relieving therapy of tumour patients diflunisal appears to offer a genuine alternative to centrally-acting analgetics.

Aged↗

[Long-term treatment of chronic pain with tilidine-naloxone. An analysis of 50 patients with chronic pain conditions of non-malignant origin].

METHOD: 50 patients with incurable chronic pain states were treated for a period of between six months and 14 years (median: 31 months) with tilidine-naloxone, and the results of tumor recorded. Amelioration of pain was achieved in an average of 60.7% of the cases. The 16 patients of this series suffering from neuropathic pain who received a somewhat lower dose responded equally as well (60.3% amelioration) as the overall group. In 24 patients suffering from pain, the daily dose remained unchanged throughout the course of treatment, had to be increased in 19, and was reduced in seven patients. In two patients, acceptable side-effects were indicated; in no case were there any signs of drug-induced organic damage. CONCLUSIONS: The results show that tilidine-naloxone is a highly effective opioid analgesic with a remarkably favorable benefit-risk ratio for use in long-term treatment.

Adult↗

GLC determination of tilidine, nortilidine, and bisnortilidine in biological fluids with a nitrogen-sensitive detector.

A sensitive and specific GLC method is described to determine therapeutic levels of tilidine and its two main metabolites, nortilidine and bisnortilidine, in plasma and urine. The method involves the extraction of the compounds and an internal standard with cyclohexane from alkalinized samples, followed by back-extraction into 1 N HCl. The hydrochloric acid solution is evaporated to dryness. After liberation of the free bases with ammonia, the residue is subjected to GLC analysis with a nitrogen-phosphorus detector and a 1.8-m (6-ft) glass column packed with 1% CRS 101 and 1.5% LAC-4-R-886 on Gas Chrom Q. Sensitivity in plasma and urine is approximately 1 ng/ml for a 5-ml sample.

Adult↗

A comparison of the stimulus effects of codeine in rhesus monkeys under the contingencies of a two lever discrimination task and a cross self-administration paradigm: tests of generalization to pentazocine, buprenorphine, tilidine, and different doses of codeine.

The stimulus effects of codeine were assessed in three monkeys trained to perform first under the contingencies of a cross self-administration paradigm and then under a two lever discrimination task. Codeine-trained monkeys generalized to pentazocine, buprenorphine, and codeine under both procedures in doses different from the training dose. Codeine-trained monkeys did not generalize to tilidine. These results indicate that monkeys do not behave in a qualitatively different way when presented with the study drugs under both contingencies. However, there were marked quantitative differences between the generalization effects of doses of pentazocine, buprenorphine, and codeine to doses other than that used in training between the two paradigms. Much higher doses of codeine and pentazocine, but not of buprenorphine, were necessary for inducing generalization effects in the two lever task than in the cross self-administration procedure. The possible reasons for these quantitative differences are discussed. It is concluded that the cross self-administration procedure is more sensitive for the assessment of opioid-like stimulus properties of drugs than the two lever discrimination task.

Animals↗

[Analog computer analysis of radioactivity kinetics in man following oral administration of tilidine HCl-14C].

Models for studying the absorption and elimination kinetics of 14-C labelled DL-Ethyl-trans-2-dimethylamino-1-phenyl-cyclohex-3-ene-trans-1-carboxylate-hydrochloride (Tilidine - HCl, Valoron) are developed, based on the concentration vs. time of radioactivity in the plasma following a single oral administration in man. For this purpose, the average concentration values in the plasma of 3 healthy adults, as given by Vollmer and Poisson [12] were employed. 1. Two three-compartment-models were developed which simulate with sufficient accuracy the 14-C-Valoron concentration curve in the plasma. 2. Computer analysis enables one to determine the distribution of 14-C-Valoron among the intra- and extravasal compartments and the half life for absorption t1/2 equals 0.57 h, for transport from plasma into the extravasal compartment t1/2 equals 3.31 h, for resorption t1/2 equals 4.11 h, for elimination with feces t1/2 equals 29.5 h and for elimination in urine t1/2 equals 8.75 h. 3. The use of two different models allows one to draw conclusions concerning the participation of parenchymatous organs in storage and elimination. 4. The probable radioactivity curve is calculated for repeated oral application of 14-C-Valoron in 8 hours intervals.

Administration, Oral↗

Spectrophotometric determination of tilidine using bromocresol green and bromophenol blue.

A spectrophotometric method is described for the determination of tilidine in its dosage forms (injection, drops, suppositories). The method is based on ion-pair extraction with chloroform at pH 3.5 using bromocresol green or bromophenol blue as the ion-pairing reagents. The spectrophotometric measurements are carried out at the absorption maxima at 415 and 411 nm, respectively.

Bromcresol Green↗

The respiratory effects of tilidine hydrochloride.

A standard 50-mg dose of tilidine hydrochloride (Valoron) was administered to 20 patients in the postoperative phase of open-heart surgery. No significant change in respiratory status, as measured by arterial blood gas analysis, was demonstrated with this dosage.

Acid-Base Equilibrium↗

High-performance liquid chromatographic determination of tilidine in pharmaceutical dosage forms.

A reversed-phase high performance liquid chromatographic method for the determination of tilidine in bulk drug and its liquid and solid dosage forms is described. The method uses reversed-phase column RP-8 with methanol -0.2% water solution of ammonium carbonate (75:25,v/v) as the mobile phase and UV detector. The time taken for separation is 6.17 min. The response is linear up to 3.6 mmol/l, with recovery levels ranging from 98.2 to 101.2%. The present method is rapid, simple and reproducible.

Chromatography, High Pressure Liquid↗

[Tilidin (Valoron) abuse. Results of an enquiry of drug consumers (author's transl)].

Contrary to previous clinical reports tilidin (Valoron), valuable as a strong analgesic, can replace opiates in young people addicted to them. In the drug scene, therefore, Valoron - very often through irresponsible medical prescription - has become a substitute for opiates. The results of an enquiry about Valoron abuse in 44 opiate addicts are reported. Four cases of isolated Valoron addiction are included which were indistinguishable from the typical career of an opium addict. Further cases of Valoron abuse, estimated at 600, have been mentioned to us, partly by name and partly by number. Doctors and pharmacists are urgently advised to treat Valoron with the same caution prescribed for opiates by the Betäubungsmittelgesetz (= Narcotics Act).

Adolescent↗

[Tilidine as an analgesic in combination anesthesia].

In 2446 "insufflation anesthesias" the usefulness of Tilidine as an analgesic has been established. The preferred combinations were with Methohexital, Dehydrobenzperidol, Nitrous oxide, Succinyl and Diallyl-Nortoxiferine.

Adjuvants, Anesthesia↗