Pharmacokinetics and Clinical Effects of Scopolamine in Caesarean Section Patients

Quinolones are synthetic broad-spectrum antibiotics with good oral absorption and excellent bioavailability. Due to the chemical functions found on their nucleus (a carboxylic acid function at the 3-position, and in most cases a basic piperazinyl ring (or another N-heterocycle) at the 7-position, and a carbonyl oxygen atom at the 4-position) quinolones bind metal ions forming complexes in which they can act as bidentate, as unidentate and as bridging ligand, respectively. In the polymeric complexes in solid state, multiple modes of coordination are simultaneously possible. In strongly acidic conditions, quinolone molecules possessing a basic side nucleus are protonated and appear as cations in the ionic complexes. Interaction with metal ions has some important consequences for the solubility, pharmacokinetics and bioavailability of quinolones, and is also involved in the mechanism of action of these bactericidal agents. Many metal complexes with equal or enhanced antimicrobial activity compared to the parent quinolones were obtained. New strategies in the design of metal complexes of quinolones have led to compounds with anticancer activity. Analytical applications of complexation with metal ions were oriented toward two main directions: determination of quinolones based on complexation with metal ions or, reversely, determination of metal ions based on complexation with quinolones.

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“…Moreover, the synthesized complexes also showed high potency against some fluoroquinolone-resistant strains of H. pylori. [50].…”

Section: Consequences and Applications Of Metal-quinolone Complexamentioning

confidence: 99%

Metal Complexes of Quinolone Antibiotics and Their Applications: An Update

2013

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“…In the absence of critical No Observed Adverse Effect Levels (NOAELs) for either atropine or scopolamine, we estimated the Acute Reference Doses (ARfDs) departing from the lowest recommended paediatric and/or obstetric therapeutic doses, i.e. 10 µg kg –1 BM for atropine (Honkavaara and Pyykkö ; Mirakhur and Jones, ) and 5 µg kg –1 BM for scopolamine (Pihlajamaki et al ., ). Both alkaloids act as the antagonists of muscarinic receptors.…”

Section: Introductionmentioning

confidence: 97%

Acute effects of a low‐dose atropine/scopolamine mixture as a food contaminant in human volunteers

Perharič

Juvan

Stanovnik

2012

J of Applied Toxicology

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To verify the assumptions in our previous risk assessment of an atropine/scopolamine mixture in buckwheat flour, we performed a randomized, double-blind, placebo-controlled cross-over study in 20 healthy, adult volunteers. The volunteers ingested a traditional Slovenian buckwheat meal, made of boiled buckwheat flour to which alkaloids were added. In addition to the placebo they ingested 0.12/0.10, 0.37/0.29, 1.22/0.95, 3.58/2.81 and 12.10/9.50 µg kg(-1) body mass (BM) of the atropine/scopolamine mixture. The changes in body temperature, heart rate, salivary and sweat secretion, pupil size, near-point vision and subjective symptoms were recorded regularly for 4 h after the ingestion. Decreased salivary and sweat secretion, increased heart rate and pupil size and reduced near-point vision accompanied by characteristic subjective symptoms were observed at 12.10/9.50 µg kg(-1) BM. At doses of 0.37/0.29 and 1.22/0.95 µg kg(-1) BM, a significant decrease in the heart rate was noted, which we consider to be a critical effect of a low-dose exposure to the atropine/scopolamine mixture. Although this did not have any clinical relevance in our subjects, it may have serious implications if it occurred in people with pre-existent cardiac conditions or those on medications that may cause bradycardia. No significant changes in the observed end points were noted at 0.12/0.10 µg kg(-1) BM. We estimate that the NOAEL (No Observed Adverse Effect Level) for the atropine/scopolamine mixture lies between the lower two administered doses. Applying the uncertainty factor of 10, we propose a new provisional Acute Reference Doses (ARfDs) of the mixture, i.e. 0.01 µg kg(-1) BM for each alkaloid, and a further refinement using higher-tier approaches.

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“…Whilst the lack of effects of the scopolamine patch on cognition will be of interest to users of the patch for travel sickness, these findings do suggest that the effective dose of scopolamine available through the patch is too low to represent a viable antidepressant mechanism. Although blood scopolamine levels were not measured in this study, previous studies suggest that the peak plasma concentration of scopolamine achieved by the patch (~100 pg/mL reached after 8 h) is much lower than that induced by oral (~350 pg/mL 50 min post-injection of 0.6 mg tablet) or intravenous scopolamine (~18 ng/mL serum concentration within minutes of 4.0 μg/kg dose) (Renner et al, 2005;Pihlajamäki et al, 1986). These findings should be interpreted in the context of the modest sample size and with the caveat that healthy volunteer models may be less sensitive than patient samples to detect the antidepressant effects of scopolamine.…”

Section: Discussionmentioning

confidence: 78%

Overnight transdermal scopolamine patch administration has no clear effect on cognition and emotional processing in healthy volunteers

et al. 2018

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There has been increasing interest in the antidepressant effects of the muscarinic cholinergic receptor antagonist scopolamine. Here we assess, for the first time, whether a transdermal scopolamine patch is sufficient to induce changes in cognition that are consistent with the reported cognitive and antidepressant effects of scopolamine. A scopolamine or placebo patch was administered to healthy volunteers [n=33] for 17h in a double-blind, between-subject procedure. There was no clear effect of scopolamine patch on emotional cognition, verbal or working memory, suggesting that the effective dose of scopolamine available through the patch is too low to represent a viable antidepressant mechanism.

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Pharmacokinetics and Clinical Effects of Scopolamine in Caesarean Section Patients

Cited by 22 publications

References 8 publications

Metal Complexes of Quinolone Antibiotics and Their Applications: An Update

Metal Complexes of Quinolone Antibiotics and Their Applications: An Update

Acute effects of a low‐dose atropine/scopolamine mixture as a food contaminant in human volunteers

Overnight transdermal scopolamine patch administration has no clear effect on cognition and emotional processing in healthy volunteers

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