Pharmacokinetics and Pharmacodynamics of Pentazocine in Children

Abstract

Pharmacokinetics and ventilatory effects of a single intravenous dose of 0.5 mg/kg of pentazocine were studied in ten children aged 4 to 8 years after ophthalmic surgery. Elimination half-life (mean +/- S.D.) was 3.0 +/- 1.5 hr and clearance 21.8 +/- 5.9 ml/min./kg. The values for Vc, Vss and V beta were 0.73 +/- 0.21, 4.0 +/- 1.2 and 5.3 +/- 2.1 l/kg, respectively. The pharmacokinetic parameters were similar to those of adults. After administration of pentazocine decrease in ventilatory rate and oxygen saturation and increase in end-tidal carbon dioxide were relatively fast and steep. Oxygen saturation of four patients decreased below 90% and in one patient the decrease did not recover instantly and additional oxygen was given for 2 min. No patient needed assisted ventilation. Only clinically insignificant changes in heart rate and mean arterial pressure were observed. The duration of analgesia was 164 +/- 59 min. No serious side-effects appeared.

Pharmacokinetic/Pharmacodynamic Modeling and Simulation of the Analgesic Effects of Pentazocine Using Perioperative Real-World Data

“…Therefore, we assumed no difference in the PTZ PKs between the intraoperative and postoperative periods and developed a PPK model. The obtained PPK parameters were within the range of the previously reported values, 12,30,31) which we considered valid for the simulations of 40-80 kg body weight. In addition, Ritschel et al calculated the distribution and clearance volume for a patient weighing 95.5 kg, 30) which was the same as the previously reported PK data and our PPK data.…”

“…Pentazocine (PTZ) is widely used for pain control in Japan, acts on central μ-and κ-opioid receptors, 6,7) and produces analgesic effects by inhibiting the stimulus conduction system. 8,9) As a result, morphine-like side effects, such as nausea, dizziness, headache, insomnia, increased blood pressure, and decreased respiratory rate, [10][11][12] are observed. Moreover, fatal PTZ overdose and abuse have been reported, and some studies revealed that the entry point for people who fall into inappropriate self-injection is medical in origin.…”

A randomized controlled trial comparing Pentazocine and Chamomilla recutita for labor pain relief

“…The pain relief after 2 h with Pentazocine, as compared with placebo, was slightly better as shown in Figure 1. Pentazocine has a half life of 2e3 h 27,28 and usually takes 2 h to have its maximum effect on reduced sensitivity to pain stimuli (Table 3).…”

Effects of Pentazocine on perioperative myocardial injury of elderly hypertensive patients

“…Recently, it has been found that several anesthetics, especially opioids, have myocardial protective effects, and pentazocine as a partial agonist of opioid receptors may also have myocardial protective effects [3][4], a nding that may be effective in reducing the occurrence of intraoperative circulatory and respiratory adverse events in patients, but studies on the use of pentazocine as a myocardial protective drug are currently limited to laboratory trials or human However, the use of pentazocine as a cardioprotective agent has been limited to laboratory trials or human extracorporeal circulation (CPB) procedures, with minimal exploration of its use in patients undergoing non-cardiovascular procedures. In this study, we investigated the intraoperative management of pentazocine in elderly hypertensive patients undergoing THR, observed intraoperative hemodynamic changes and recorded intraoperative adverse cardiovascular events, and compared preoperative and 24-h postoperative plasma troponin (cTnI) concentrations to investigate whether pentazocine could reduce perioperative myocardial injury in elderly hypertensive noncardiac surgery patients and thus exert a protective effect on myocardium.…”