Pharmacokinetics of Intravenous Procaine Infusion in Humans

Seifen, Astride B.; Ferrari, A; Seifen, Ernst; Thompson, Dola S.; Chapman, John

doi:10.1097/00132586-198010000-00012

Cited by 4 publications

(6 citation statements)

References 0 publications

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“…The major difference between drugs was that the increase in ITI increased the maximum level of responding for cocaine but not for procaine. This is consistent with the shorter duration of action of procaine (JavaJd et al 1978;Seifen et al 1979). Except at the highest dose, the direct effects of procaine to suppress responding seem to have dissipated within 15 min.…”

Section: Discussionsupporting

confidence: 79%

Comparison of the reinforcing efficacy of cocaine and procaine in rhesus monkeys responding under a progressive-ratio schedule

Woolverton

1995

Psychopharmacology

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Rhesus monkeys (n = 5) were prepared with chronic IV catheters and trained to lever press under a PR schedule of drug injection. The schedule consisted of five components, each made up of four trials (i.e., 20 trials total). Each trial within a component had the same response requirement. The response requirement in the first component was 120/trial and doubled in successive components to a maximum of 1920 in the fifth. A trial ended with an injection or the expiration of a 12-min limited hold (LH). The inter-trial interval (ITI) was 15 or 30 min. Following an injection or expiration of the LH, all stimulus lights were extinguished and responding had no consequence for the remainder of the trial. A session ended when either all 20 injections were self-administered or the response requirement was not met within the LH for two consecutive trials. The number of injections/session and responses/session increased with dose for cocaine (0.012-0.1 mg/kg per injection) and procaine (0.12-2.0 mg/kg per injection) at both ITI values. At the 15-min ITI, responding decreased again at higher doses in some monkeys with cocaine and in all monkeys with procaine. At maximum, cocaine maintained significantly more injections and responses/session when the ITI was 30 min than when it was 15 min. In contrast, the increase in ITI did not increase the maximum maintained by procaine. Cocaine was approximately 10-fold more potent than procaine and maintained at maximum significantly more injections and responses than procaine when ITI was 30 min but not when the ITI was 15 min.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionsupporting

confidence: 79%

Comparison of the reinforcing efficacy of cocaine and procaine in rhesus monkeys responding under a progressive-ratio schedule

Woolverton

1995

Psychopharmacology

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“…The in vitro investigation s support the hypothesis of an inhibition of the reaction through interaction of the local anesthetic with the substrate.The dose of pro caine under ECC conditions was first of all calculated empirically from the necessary rate of infusio n for an equal pressure o f perfusion and a measurable increase of resistan ce of the erythrocytes against osmotic and mechanic stress. This lies between 1.5 and 2 mg/kg/min and corresponds with the recently published pharma cokinetic data for achieving a steady state with the infusion of procaine within 20 minute s(18) . In order to atta in an exact determination of the effect of procaine on Plase A under our clinical conditions (ECC, hypothermia) in the sense of a dose-effect relationship, further pharmacokineti c investigation s are necessary.R ef erences 1 Addo nizio , VP , J.f : Strauss, Li -Feng Chang, CA .…”

supporting

confidence: 86%

“…At the end of the cooling period an average of 35 mgjkg procaine had been applied. From this, a concentration of about I mmol/ml can be calculated under the assumption of an initially only intravasal distribution of procaine (18). The Plase activity which was determined is compared in Fig.…”

Section: Re Sult Smentioning

confidence: 99%

Phospholipase A Activation Following Extracorporeal Circulation and its Blockade by Procaine

Olthoff¹,

Kunze²,

Rüstow³

1983

Thorac cardiovasc Surg

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The phospholipase A activity of human plasma was investigated in the course of operations with the aid of extracorporeal circulation. After an initial increase following heparin application, there is a continuous rise up to the end of perfusion and a decrease to normal values 30 minutes after the end of perfusion and the application of protamine. Procaine is suitable for the inhibition of the increased phospholipase A activity. In accordance with in vitro determinations of an effective dose of 1 mmol/ml, corresponding concentrations were attained with an infusion rate of 1.5-2 mg/kg/min. In a second series of investigations, a significantly smaller phospholipase A activation in the course of perfusion was detectable through the addition of procaine.

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“…In the present study, local anesthetics blocked DA uptake as effectively as cocaine in concentrations of 100-1000 µM. At these concentrations, sodium channel effects would be expected to become increasingly prominent (Karlsson 1973;O'Brien et al 1979;Seifen et al 1979;Kuhnert et al 1986;Nunes de Moraes et al 1998;Tsai et al 1998;Yoko-yama et al 1998).…”

Section: Discussionmentioning

confidence: 53%

“…We chose the local anesthetics cocaine, procaine, dimethocaine, chloroprocaine and tetracaine, all of which have been reported to function as positive reinforcers Balster 1979, 1982;Johanson 1980) and to bind the DAT in rats and monkeys (Ritz et al 1987;Wilcox et al 1999). Moreover, with the exception of tetracaine, these local anesthetics have similar pharmacokinetic profiles (Seifen et al 1979;Kuhnert et al 1986;Lamas et al 1995), i.e., they are relatively short-acting compounds. Therefore, differences in reinforcing effects could be more reliably attributed to pharmacodynamic, rather than the pharmacokinetic, differences between the drugs.…”

Section: Introductionmentioning

confidence: 99%

On the relationship between the dopamine transporter and the reinforcing effects of local anesthetics in rhesus monkeys: practical and theoretical concerns

et al. 2000

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The potency of local anesthetics as positive reinforcers is likely related to their potency as DA uptake inhibitors. Variation in their effectiveness as positive reinforcers was not a function of differences in effectiveness as DA uptake blockers, but may be related to relative potency over the concentrations that are achieved in vivo. Effects at sodium channels may limit the reinforcing effects of local anesthetics.

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Pharmacokinetics of Intravenous Procaine Infusion in Humans

Cited by 4 publications

References 0 publications

Comparison of the reinforcing efficacy of cocaine and procaine in rhesus monkeys responding under a progressive-ratio schedule

Comparison of the reinforcing efficacy of cocaine and procaine in rhesus monkeys responding under a progressive-ratio schedule

Phospholipase A Activation Following Extracorporeal Circulation and its Blockade by Procaine

On the relationship between the dopamine transporter and the reinforcing effects of local anesthetics in rhesus monkeys: practical and theoretical concerns

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