Pharmacokinetics of Intravenous Procaine Infusion in Humans

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

doi:10.1213/00000539-197909000-00007

Cited by 28 publications

(12 citation statements)

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“…In our patients, using a two-cornpartment pharmacokinetic model, procaine had a distribution and an elimination halflife of 2 and 15 minutes, respectively. These values obtained during hypothermia correspond favorably to the 2.5 and 7.7 minutes by Seifen and co-workers (19) at normothermia.…”

Section: Discussionsupporting

confidence: 86%

“…No components of Bretschneider's solution other than procaine will cross the blood/brain barrier in the time interval studied. Procaine has abrief half-life and a limited degree of distribution and tissue uptake (19). In our patients, using a two-cornpartment pharmacokinetic model, procaine had a distribution and an elimination halflife of 2 and 15 minutes, respectively.…”

Section: Discussionmentioning

confidence: 76%

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Cerebral Blood Flow during Early Cardiopulmonary Bypass in Man. Effect of Procaine in Cardioplegic Solutions

Henriksen¹,

Di²,

Ih³

et al. 1986

Thorac cardiovasc Surg

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Cerebral blood flow (CBF), plasma procaine concentrations, and somatosensory evoked potentials (SSEP) were recorded in 2 groups of patients in whom either a high-procaine cardioplegic solution (Bretschneider's n = 29), or a low-procaine cardioplegic solution (St. Thomas', n = 13) was used. In the Bretschneider's group, marked changes in CBF occurred (p less than 0.001). Mean CBF was 27 (range 18 to 51) ml/(100 g X min) between sternotomy and the onset of extracorporeal circulation (ECC). A mean of 6 minutes after the onset of ECC, and before the administration of Bretschneider's cardioplegic solution, CBF increased to 39 ml/(100 g X min). After administration of the cardioplegic solution, CBF decreased significantly within the first 15 minutes, and then gradually increased to a mean of 68 (range 43 to 108) ml/(100 g X min). Cerebral blood flow was 45 ml/(100 g X min) just after ECC was stopped. Marked plasma procaine concentrations, up to 100 mg/l, were reached just after the infusion of Bretschneider's solution. The flow was significantly reduced (p less than 0.015) in patients with plasma procaine greater than or equal to 10 mg/l, when compared to patients with plasma procaine values less than 10 mg/l. In the St. Thomas' cardioplegic solution group the same reduction in CBF did not occur (p less than 0.02). Despite the depressant effect of procaine on CBF in the Bretschneider group, a consistent brain hyperperfusion was observed in all patients during hypothermic ECC if their blood pressure was sufficient to produce hyperemia. In rats (n = 6), during normothermia without extracorporeal circulation, the effect of procaine was much more pronounced. The CBF fell from a mean resting level of 108 ml/(100 g X min) to 68 and 54 ml/(100 g X min) after 15 and 35 minutes, respectively, of continuous infusion of Bretschneider's solution. The flow returned to the resting level about 40 minutes after termination of the infusion.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 76%

Cerebral Blood Flow during Early Cardiopulmonary Bypass in Man. Effect of Procaine in Cardioplegic Solutions

Henriksen¹,

Di²,

Ih³

et al. 1986

Thorac cardiovasc Surg

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“…2b,c). Furthermore, cellular esterase/amidases are unlikely to explain the lack of cellular labeling or weak behavioral activity of A-NK-amide; precedent examples from the literature on local anesthetics show that amidation is correlated with increased in vivo stability (procainamide, lidocaine) over that of procaine444546.…”

Section: Discussionmentioning

confidence: 99%

A Clickable Analogue of Ketamine Retains NMDA Receptor Activity, Psychoactivity, and Accumulates in Neurons

Emnett¹,

Li²,

Jiang³

et al. 2016

Sci Rep

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Ketamine is a psychotomimetic and antidepressant drug. Although antagonism of cell-surface NMDA receptors (NMDARs) may trigger ketamine’s psychoactive effects, ketamine or its major metabolite norketamine could act intracellularly to produce some behavioral effects. To explore the viability of this latter hypothesis, we examined intracellular accumulation of novel visualizable analogues of ketamine/norketamine. We introduced an alkyne “click” handle into norketamine (alkyne-norketamine, A-NK) at the key nitrogen atom. Ketamine, norketamine, and A-NK, but not A-NK-amide, showed acute and persisting psychoactive effects in mice. This psychoactivity profile paralleled activity of the compounds as NMDAR channel blockers; A-NK-amide was inactive at NMDARs, and norketamine and A-NK were active but ~4-fold less potent than ketamine. We incubated rat hippocampal cells with 10 μM A-NK or A-NK-amide then performed Cu2+ catalyzed cycloaddition of azide-Alexa Fluor 488, which covalently attaches the fluorophore to the alkyne moiety in the compounds. Fluorescent imaging revealed intracellular localization of A-NK but weak A-NK-amide labeling. Accumulation was not dependent on membrane potential, NMDAR expression, or NMDAR activity. Overall, the approach revealed a correlation among NMDAR activity, intracellular accumulation/retention, and behavioral effects. Thus, we advance first generation chemical biology tools to aid in the identification of ketamine targets.

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“…shot of 25 till 50 mg Procaine to reach a systemic action. The pure Procaine infusion was firstly described by SEIFEN et al [37,38] and was mostly used as a continuous treatment in cases of acute pancreatitis [39][40][41] and for epidural anesthesia in infants, children and risk patients, which underlines the low toxicity of the substance [42][43][44][45][46][47][48][49]. O´DONNELL et al reported about the use of procaine infusion to block the cardiac nerves [50].…”

Section: The Procaine-infusion -The Logic Following Of Other Parentermentioning

confidence: 99%

The Procaine-Base-Infusion: a Review after twenty Years of Use

Oettmeier¹,

Reuter²

2017

J Med - Clin Res & Rev

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The highly-dosed infusion with Procaine-HCl with sodium-bicarbonate as additive was firstly published twenty years ago. The method advanced to a routine in many centers for pain treatment, rehabilitation and natural medicine. The aim of the procedure is the systemic use of the various pharmacological features of Procaine, especially to inhibit pain and inflammation, for vasodilatation, anti-oxidation and to harmonize the vegetative nervous system. On one hand shall the addition of sodium-bicarbonate balance the common latent pH-decrease in the periphery. On the other hand also the degradation products of Procaine (DAE and PABA) have a systemic effect. For the safety of the patients and to improve the success rate of the method it was shown that the classic Procaine-Base-infusion should be only realized on the base of a prior acid-base-diagnostic.

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Pharmacokinetics of Intravenous Procaine Infusion in Humans

Cited by 28 publications

References 0 publications

Cerebral Blood Flow during Early Cardiopulmonary Bypass in Man. Effect of Procaine in Cardioplegic Solutions

Cerebral Blood Flow during Early Cardiopulmonary Bypass in Man. Effect of Procaine in Cardioplegic Solutions

A Clickable Analogue of Ketamine Retains NMDA Receptor Activity, Psychoactivity, and Accumulates in Neurons

The Procaine-Base-Infusion: a Review after twenty Years of Use

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