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PubMedDate not supplied

Disposition of tilidine in a fatal poisoning in man.

A fatal intoxication due to the ingestion of tilidine, a narcotic analgesic, in conjunction with ethanol, is described. Tilidine and its two active metabolites, nortilidine and bisnortilidine, were identified and quantitated in the biological fluids and tissues by thin-layer chromatography (TLC), gas-liquid chromatography with sensitive nitrogen-phosphorus detection (GLC/NPD) and gas-liquid chromatography with mass spectrometric detection (GC/MS). The toxicological results are compared with previously reported 14C-tilidine tissue distributions in rats following oral administration and limited tissue data in a previously reported human fatality. In the present case, the death was attributed to the combined central nervous system-depressing effects of ethanol and tilidine.

Adult↗
PubMed1976

[Premedication with valoron (Tilidin) in internal laparoscopy].

Apart from sufficient experience on the part of the examining physician and adequate technical apparatus, proper premedication can facilitate the procedures for both patient and physician considerably. The paper reports on experience gained in 500 laparoscopies carried out under conditions which were deviated slightly from those hitherto recommended in the literature. The analgesic employed was Tilidine (in Germany: Valoron), and Diazepam was used as a sedative; both of these substances were given intravenously, the vein was kept open for the entire course of the examination. The Tilidine dose was normally 50-100 mg, but under exceptional circumstances as much as 150 mg. Tilidine showed good analgesic effectiveness and tolerance; no case or nausea or vomiting and no sign of respiratory depression of effects on smooth muscle were observed under the conditions stated. The fact that Tilidine is not subject to the restrictions imposed by the German narcotics law is also seen as an advantage. The Diazepam dose was 5-30 mg. Apart from its sedative effect Diazepam also diminishes the tonus of skeletal muscle (important in laparoscopy) and has a relatively long time of elimination (20-48 h). In addition to these two substances, 10-20 ccm of 1% Lidocaine solution with Epinephrine additive was given as a local anaesthetic. The investigators' experience with the above premedication procedure was found to be convincingly positive.

Anesthesia, Local↗
PubMed1982

The influence of tilidine and prazepam on withdrawal reflex, skin resistance reaction and pain rating in man.

Pain rating, withdrawal reflex and skin resistance reaction upon electrical skin stimuli were studied on 15 male volunteers under placebo, tilidine and prazepam. Tilidine (Valoron) is an orally applicable narcotic analgesic, with a mode of pain relief presumably similar to morphine; the tranquilizer prazepam (Demetrin) belongs to the benzodiazepine group. Significant reduction in all measured reaction amplitudes was found under tilidine, whereas prazepam reduced significantly only the skin resistance reaction. The relative drug-induced changes in reaction amplitudes, related to the corresponding placebo value, were independent of stimulus intensity for all investigated reactions. Therefore, fitted power functions re = a . Sn between reaction amplitudes re and stimulus intensity S showed a decrease in parameter a under the investigated drugs, whereas the exponent n remained constant. High correlations between parameters a and corresponding reciprocal threshold currents could be shown for all reactions measured. Furthermore the drug-induced changes of withdrawal reflex amplitude and of subjective estimation were found to be correlated over subjects. In contrast, no correlations were found between variations in skin resistance reaction and magnitude estimation due to the selected drugs, i.e., the influence of the drugs on the sensory component of pain sensation and on the skin resistance reaction were independent effects.

Analgesia↗
PubMed1975

[The effect of tilidine on left-ventricular function of the human heart (author's transl)].

The effect of tilidine (Valoron, 1.5 mg/kg) on left-ventricular function was measured in ten patients undergoing diagnostic cardiac catheterization. In the course of thirty minutes after administration there was a small fall in systemic arterial pressure, decrease in cardiac output, cardiac index and stroke volume, as well as a change in the isovolumetric inotropic state. Haemodynamic and inotropic changes were small in amount, varying between 3.4 and 14.5% of basal values. This study indicates that tilidine, while having a powerful analgesic effect, has only a mild contractility-inhibiting action. Tilidine is thus a useful alternative as an analgesic in cardiac pain.

Adult↗
PubMedDate not supplied

In vitro adsorption of tilidine HCl by activated charcoal.

In vitro studies were carried out in order to determine the adsorption of tilidine HCl, a narcotic analgesic, by activated charcoal (max. adsorption capacity 185.5 mg/g of charcoal). The path of the adsorption isotherms at pH 1.2 and 7.5 suggests that the in vivo adsorption of tilidine HCl may be increased when the drug passes from the stomach to the intestine, unless the intestinal content exerts a displacing effect. Nevertheless, the adsorption was dependent on the quantity of activated charcoal used, becoming more complete when the quantity of activated charcoal was increased. The effects of additives on the adsorption capacity of activated charcoal were also investigated in vitro. Ethanol, sorbitol and sucrose significantly reduced drug adsorption, while cacao powder, milk and starch had no effect on tilidine adsorption. At an acid pH, Federa Activated Charcoal significantly adsorbed more drug than either Norit A or Activated Charcoal Merck.

Adsorption↗
PubMed1976

Action of tilidine hydrochloride and morphine hydrochloride on ventilatory control in normal subjects.

The action of tilidine hydrochloride and morphine hydrochloride on the ventilatory response to inhaled carbon dioxide has been assessed in 10 normal volunteers. In doses of 50 mg and 100 mg given intravenously, tilidine hydrochloride induced less respiratory depression than 10 mg of morphine given intravenously. Side effects were not different or troublesome with either drug. Depending on its relative pain-relieving property, tilidine hydrochloride may have advantages over morphine as an analgesic.

Adult↗
PubMed1978

Gas-chromatographic determination of nanogram amounts of enantiomers of nortilidine, a main metabolite of tilidine, in biological specimens.

We report a specific and sensitive method for determination of the individual optical isomers of nortilidine, a main metabolite of tilidine, with the aid of a nitrogen-sensitive detector. With N-trifluoroacetyl-L-leucyl chloride as chiral reagent, the diastereomeric derivatives of the nortilidine enantiomers could be separated and quantified in the nanogram range. Under these conditions, the enantiomers of bisnortilidine, another main metabolite of tilidine, were also separated. Investigations in rats with the enantiomers of tilidine and nortilidine indicated that no racemization occurs during N-demethylation in the organism. After oral and intravenous administration of 50 mg of tilidine.HCI to a human volunteer, identical concentrations of nortilidine enantiomers were found in the plasma.

Animals↗
PubMed1978

[Effects of tilidin and naloxone on pulmonary function (author's transl)].

The respiratory depressant effect of tilidine (valoron) was investigated in anaesthetized patients. One hundred mg of tilidine had a slight respiratory depressant effect which was without importance in awake subjects. The respiratory depression caused by tilidine could be antagonized by naloxone while the analgesic effect was maintained. This suggests a dissociation of the mechanisms responsible for the respiratory and the analgesic actions.

Adolescent↗
PubMed1976

A comparison of tilidine hydrochloride and morphine in the treatment of postoperative pain.

Intramuscular injections of 10 mg morphine or 100 mg tilidine hydrochloride were administered in a double-blind fashion and in random order to 40 patients after minor surgical operations. The therapeutic effect of each analgesic was assessed by comparing the severity of pain immediately postoperatively with that 1, 2, 3 and 4 hours after injection of the relevant analgesic. Tilidine and morphine relieved pain to a similar degree. Within the limits of the protocol followed, morphine appeared superior to tilidine in some tests. No major side-effects occurred.

Adult↗
PubMed1975

An evaluation of tilidine hydrochloride in the treatment of pain requiring immediate analgesia.

Problems relating to analgesia in various situations are briefly discussed. A simple working classification for analgesic administration is given. The results of a trial, in which 50 mg of a new analgesic, tilidine, was given sublingually, are presented. The drug was evaluated in cases where immediate analgesia was indicated. The majority of patients had injuries to the hand or head. It was found that tilidine provided a marked analgesic effect in 27 of the 30 patients. The onset of action was rapid, 25 of the 30 patients obtaining complete relief within 6 minutes. It is concluded that tilidine is a powerful analgesic, with a rapid onset of action when it is give in the sublingual drop form. Moreover, it is a drug of choice, in this form, for acute, moderately severe situations (those which require immediate analgesia, but where opinates are not thought to be necessary).

Acute Disease↗
PubMed1976

A death case involving tilidine.

A fatal poisoning case due to the combination of a relative overdose of barbiturates (600 mg daily) and 750 mg of tilidine is reported. The concentrations of barbiturates and tilidine with its metabolites were determined in blood, liver, and urine.

Adult↗
PubMed1986

Intrathecal injection of codeine, buprenorphine, tilidine, tramadol and nefopam depresses the tail-flick response in rats.

The effect of intrathecal (i.t.) injection of the analgesic agents, codeine, buprenorphine, tilidine and one of its metabolites, nortilidine, tramadol and nefopam, was determined in the tail-flick test performed on rats. ED50 values were derived from the dose-response lines. The relative potency ranking established from the ED50 values is buprenorphine (0.4 nM) greater than nortilidine (29 nM) = tramadol (26 nM) = nefopam (34 nM) greater than codeine (42 nM) greater than tilidine (118 nM). An i.t. injection of the opiate antagonist, naloxone (5 micrograms), prevented the antinociceptive effect of all analgesic agents administered at the highest dose tested. It is concluded that these analgesic agents, like morphine, exert their effect at least in part through a spinal site of action.

Analgesics↗
PubMedDate not supplied

Comparison of a GLC-NPD method with a GLC-MS-SIM procedure for the determination of tilidine and its metabolites in plasma.

A gas liquid chromatographic method with nitrogen-phosphorus detection (GLC-NPD) is compared to a GLC-mass spectrometric determination employing selected ion monitoring (GLC-MS-SIM). These two methods of gas chromatographic separation were shown to be suitable for therapeutic monitoring of tilidine, nortilidine, and bisnortilidine in patients. The pharmacokinetic profile of tilidine was also studied in three normal humans after a single oral dose. Pharmacokinetic parameters such as Cmax, tmax, (t1/2) beta, AUC, AUMC, Vd beta, Cltot, beta, and MRT are derived from model independent pharmacokinetic techniques.

Absorption↗
PubMed1976

Respiratory depressant action of tilidine during N2O + O2 anaesthesia.

The respiratory depressant actions of pethidine and tilidine during anaesthesia were compared in 18 surgical patients anaesthetized with N2O + O2 after thiopental induction. Five minutes after thiopental, 0.5 mg/kg pethidine or 1.5 mg/kg tilidine were each given intravenously to six patients, the remaining six patients serving as controls. Minute ventilation, respiratory rate, end-tidal CO2 and PCO2 from arterialized venous blood were measured up to 30 min. Pethidine caused the following maximal changes: V -0.98 +/- 0.24 (s.e. mean) 1/min, rate -5.5 +/- 0.7/min, CO2ET + 0.7 +/- 0.1 vol % and PCO2 + 5.7 +/- 1.1 mm Hg. These changes occurred within 10 min of the injection.

Adult↗
PubMed1982

Involvement of the median raphe nucleus in antinociception induced by morphine, buprenorphine and tilidine in the rat.

1 Antinociception induced by three analgesics with differing profiles of activity, morphine, buprenorphine and tilidine, have been evaluated in the hot plate and paw pressure tests after administration by the subcutaneous route and directly into the median raphe nucleus in the conscious rat. 2 Behavioural and neurological effects of the three analgesics were also assessed. 3 The typical profiles of antinociceptive activity induced by the three analgesics were qualitatively similar after either route of administration. Morphine induced naloxone-sensitive dose-dependent effects in both tests. Buprenorphine showed naloxone-sensitive effects with a bell-shaped dose-response curve in the thermal test but dose-dependent activity in the pressure test. Tilidine induced naloxone-sensitive dose-dependent effects in the thermal test but demonstrated naloxone-insensitive activity in the paw pressure test. 4 The behavioural and neurological effects of the analgesics in the dose range used would not have affected the animals' ability to respond to the nociceptive stimuli. 5 The results suggest that the median raphe could participate in drug-induced antinociception. The mechanisms by which this might occur are discussed.

Analgesics↗
PubMed1992

Comparative study of tilidine-naloxone and pentazocine in knee and hip osteoarthritis.

Fifty patients, twenty-five suffering from severe knee osteoarthritis and twenty-five from acute hip osteoarthritis, received pentazocine or a new preparation of tilidine-naloxone for a period of 2 weeks, in a double-blind study. The two drugs were found to have the same efficacy and tolerance in both diseases with a minor but not statistically significant superiority for tilidine-naloxone. Similar quantities of drugs were taken over the study period, while patients were allowed to take as many as 8 capsules per day to relieve pain. There were quite equivalent side-effects and no marked changes in laboratory tests.

Aged↗
PubMed1989

Pharmacokinetics of tilidine and metabolites in man.

Tilidine is a prodrug from which the active metabolite nortilidine is formed by demethylation. The pharmacokinetics of tilidine (T), nortilidine (NT) and bisnortilidine (BNT) were studied in nine healthy subjects following single intravenous (10 min infusion) and oral 50 mg T-HCl dose as well as following multiple 50 mg T-HCl oral doses. Systemic availability of the parent substance was 6% and of the active metabolite NT 99%. The terminal half-life of NT was 3.3 h following single oral administration, 4.9 h following intravenous administration and 3.6 h following multiple dosing. Following intravenous infusion, concentrations of unchanged substance were found which were 30 times higher than following oral administration. BNT was eliminated with half-lives of 5 h after oral administration and 6.9 h after intravenous administration. Renal elimination of unchanged substance was 1.6% of the dose following intravenous administration and less than 0.1% of the dose following oral administration. Approximately 3% were recovered in urine as NT and 5% as BNT following both routes of administration.

Administration, Oral↗
PubMed1986

[Initial experience with preorally administered dipotassium clorazepate and tilidine-naloxone in extracorporeal shockwave lithotripsy].

After 70 treatments with extracorporeal shock wave lithotripsy (ESWL), using a combination of dipotassiumclorazepate p.o. 12 h before treatment and tilidin-naloxon 45 min before ESWL, 56 patients reported to be painfree or only minor, well-tolerable pain. Informed consent was obtained in all patients for this pilot study, leaving the possibility of further pain medication. 7 patients asked for an additional analgesic (fentanyl) and another 7 patients required a sedative (midazolam). No further anesthesiologic procedures were necessary. Nausea was observed in one patient as a possible side-effect of tilidin. To confirm these preliminary results, a prospective randomized study is currently conducted.

Administration, Oral↗