Absorption of ipecac alkaloids in emergency patients

Moran, Donald M.; Crouch, Dennis J.; Finkle, Bryan S.

doi:10.1016/s0196-0644(84)80332-7

Cited by 21 publications

(6 citation statements)

References 9 publications

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“…Unfortunately, emetine absorption from oral ipecac displays considerable inter-patient variation [14]. Some patients may not absorb sufficient emetine or alkaloids to be therapeutically effective.…”

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Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses

Bleasel

Peterson

2020

Pharmaceuticals

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The COVID-19 coronavirus is currently spreading around the globe with limited treatment options available. This article presents the rationale for potentially using old drugs (emetine, other ipecac alkaloids or analogues) that have been used to treat amoebiasis in the treatment of COVID-19. Emetine had amongst the lowest reported half-maximal effective concentration (EC 50 ) from over 290 agents screened for the Middle East respiratory syndrome (MERS) and severe acute respiratory syndrome (SARS) coronaviruses. While EC 50 concentrations of emetine are achievable in the blood, studies show that concentrations of emetine can be almost 300 times higher in the lungs. Furthermore, based on the relative EC 50 s of emetine towards the coronaviruses compared with Entamoeba histolytica, emetine could be much more effective as an anti-coronavirus agent than it is against amoebiasis. This paper also discusses the known side effects of emetine and related compounds, how those side effects can be managed, and the optimal method of administration for the potential treatment of COVID-19. Given the serious and immediate threat that the COVID-19 coronavirus poses, our long history with emetine and the likely ability of emetine to reach therapeutic concentrations within the lungs, ipecac, emetine, and other analogues should be considered as potential treatment options, especially if in vitro studies confirm viral sensitivity.

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confidence: 99%

“…First, blood levels varied between studies. One study reported the range [14] of levels achieved, while another recorded the mean [9], with the midpoint of the range and the mean being very different. This initially indicated that emetine could be very useful, with a blood concentration/IC 50 ratio of approximately 8 (see Table 1).…”

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confidence: 99%

Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses

Bleasel

Peterson

2020

Pharmaceuticals

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“…Previously performed human pharmacokinetics studies on 1 and 2 showed that after oral administration of 30 mL ipecac syrup (11.4-13.9 mg of 1; 23.4-45.0 mg of 2), all patients presented rapidly detectable plasma levels of 1 and 2 in highly variable extents among individuals [42,43]. The maximum plasmatic concentration (C max ) of 2 was about two times higher than 1, and data suggest extensive distribution and possible tissue accumulation for both alkaloids [42][43][44][45]. These reports have important implications concerning ipecac chronic abuse and regarding the here described hERG blocking cardiotoxicity potential.…”

Section: Resultsmentioning

confidence: 99%

hERG Channel Blocking Ipecac Alkaloids Identified by Combined In Silico – In Vitro Screening

et al. 2016

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Human ether-a-go-go-related gene channel blocking is associated with QT interval prolongation and increased risk of potentially fatal arrhythmias. As natural products keep increasing in popularity, there is an urgent need for studies assessing human ether-a-go-go-related gene channel-related cardiotoxic risks. We selected 49 plant species based on the results of a pharmacophore-based virtual screening campaign, in parallel with a literature data survey concerning highly consumed herbal medicines with reported cardiac liabilities. Lead-like enhanced extracts were prepared, an initial in vitro screening was performed at 100 µg/mL by voltage clamp on Xenopus oocytes, and five human ether-a-go-go-related gene channel blocking extracts were identified. In accordance to the six virtually predicted alkaloids, the root extract of Carapichea ipecacuanha inhibited human ether-a-go-go-related gene channel currents by 32.5 %. A phytochemical workflow resulted in the isolation and identification of five out of the six virtually predicted alkaloids. All isolates blocked human ether-a-go-go-related gene channel currents to different extents. The major ipecac constituents emetine (1) and cephaeline (2) showed IC50 values of 21.4 and 5.3 µM, respectively, measured by whole-cell patch clamp in HEK293 cells. This is the first report on human ether-a-go-go-related gene channel blockers from C. ipecacuanha. Its roots and rhizomes are used to produce different pharmacopeial ipecac preparations that are mainly used as emetics for poisoning treatment. Our findings raise further questions regarding the safety and over-the-counter appropriateness of these herbal products.

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“…In the USA it is widely used in adults (Moran et al, 1984) and has also been similarly recommended in Australia (Lett et al, 1977). It works by irritating the gastric mucosa but is also absorbed in varying degrees (Moran et al, 1984) to produce a central effect as well (Weaver & Griffith, 1969). It clearly cannot be used in unresponsive patients or those who are uncooperative.…”

Section: Syrup Of Ipecacmentioning

confidence: 99%

Drug abuse and the accident and emergency department.

Redmond

1985

Emergency Medicine Journal

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Absorption of ipecac alkaloids in emergency patients

Cited by 21 publications

References 9 publications

Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses

Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses

hERG Channel Blocking Ipecac Alkaloids Identified by Combined In Silico – In Vitro Screening

Drug abuse and the accident and emergency department.

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