The present clinical study describes gastrointestinal myiasis in horses caused due to infection with Gasterophilus intestinalis. All horses were successfully treated by gastric lavage with liquid ...paraffin followed by inj. Ivermectin, inj. Flunixin meglumine and liver supplement. Keywords: Bot fly; dipterous fly; equine; Gasterophilus intestinalis
Ivermectin mass drug administration to humans or livestock is a potential vector control tool for malaria elimination. Racemic ivermectin is composed of two components, namely a major component (> ...80%; ivermectin B
), which has an ethyl group at C-26, and a minor component (< 20%; ivermectin B
), which has a methyl group at C-26. There is no difference between the efficacy of ivermectin B
and ivermectin B
efficacy in nematodes, but only ivermectin B
has been reported to be lethal to snails. The ratios of ivermectin B
and B
ratios in ivermectin formulations and tablets can vary between manufacturers and batches. The mosquito-lethal effects of ivermectin B
and ivermectin B
have never been assessed. As novel ivermectin formulations are being developed for malaria control, it is important that the mosquito-lethal effects of individual ivermectin B
and ivermectin B
compounds be evaluated.
Racemic ivermectin, ivermectin B
or ivermectin B
, respectively, was mixed with human blood at various concentrations, blood-fed to Anopheles dirus sensu stricto and Anopheles minimus sensu stricto mosquitoes, and mortality was observed for 10 days. The ivermectin B
and B
ratios from commercially available racemic ivermectin and marketed tablets were assessed by liquid chromatography-mass spectrometry.
The results revealed that neither the lethal concentrations that kills 50% (LC
) nor 90% (LC
) of mosquitoes differed between racemic ivermectin, ivermectin B
or ivermectin B
for An. dirus or An. minimus, confirming that the individual ivermectin components have equal mosquito-lethal effects. The relative ratios of ivermectin B
and B
derived from sourced racemic ivermectin powder were 98.84% and 1.16%, respectively, and the relative ratios for ivermectin B
and B
derived from human oral ivermectin tablets were 98.55% and 1.45%, respectively.
The ratio of ivermectin B
and B
does not influence the Anopheles mosquito-lethal outcome, an ideal study result as the separation of ivermectin B
and B
components at scale is cost prohibitive. Thus, variations in the ratio of ivermectin B
and B
between batches and manufacturers, as well as potentially novel formulations for malaria control, should not influence ivermectin mosquito-lethal efficacy.
•Ivermectin, an FDA-approved anti-parasitic agent, was found to be an inhibitor of SARS-CoV-2 replication in the laboratory.•Ivermectin may be effective for the treatment of early-onset mild COVID-19 ...in adult patients.•Early viral clearance of SARS-CoV-2 was observed in ivermectin treated patients.•Remission of fever, cough and sore throat did not differ among treatment groups. No severe adverse event was observed.•Larger trials will be needed to confirm these preliminary findings.
Ivermectin, a US Food and Drug Administration-approved anti-parasitic agent, was found to inhibit severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication in vitro. A randomized, double-blind, placebo-controlled trial was conducted to determine the rapidity of viral clearance and safety of ivermectin among adult SARS-CoV-2 patients. The trial included 72 hospitalized patients in Dhaka, Bangladesh, who were assigned to one of three groups: oral ivermectin alone (12 mg once daily for 5 days), oral ivermectin in combination with doxycycline (12 mg ivermectin single dose and 200 mg doxycycline on day 1, followed by 100 mg every 12 h for the next 4 days), and a placebo control group. Clinical symptoms of fever, cough, and sore throat were comparable among the three groups. Virological clearance was earlier in the 5-day ivermectin treatment arm when compared to the placebo group (9.7 days vs 12.7 days; p = 0.02), but this was not the case for the ivermectin + doxycycline arm (11.5 days; p = 0.27). There were no severe adverse drug events recorded in the study. A 5-day course of ivermectin was found to be safe and effective in treating adult patients with mild COVID-19. Larger trials will be needed to confirm these preliminary findings.
SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of ...the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy against SARS-CoV-2. Plasma and lung ivermectin concentrations vs. time profiles in cattle were used to determine the apparent plasma to lung tissue partition coefficient of ivermectin. This coefficient, together with a simulated geometric mean plasma profile of ivermectin from a published population pharmacokinetic model, was utilized to develop a minimal physiologically-based pharmacokinetic (mPBPK) model. The mPBPK model accurately described the simulated ivermectin plasma concentration profile in humans. The mPBPK model was also used to simulate human lung exposure to ivermectin after 12, 30, and 120 mg oral doses. The simulated ivermectin lung exposures reached a maximum concentration of 772 ng/mL, far less than the estimated 1750 ng/mL IC
reported for ivermectin against SARS-CoV-2 in vitro. Further studies of ivermectin either reformulated for inhaled delivery or in combination with other antivirals with differing mechanisms of action is needed to assess its therapeutic potential.
The 2015 Nobel Prize in Physiology or Medicine has been awarded to William C. Campbell, Satoshi Omura, and Youyou Tu for the discovery of avermectins and artemisinin, respectively, therapies that ...revolutionized the treatment of devastating parasite diseases. With the recent technological advances, a New Golden Age of natural products drug discovery is dawning.
The 2015 Nobel Prize in Physiology or Medicine has been awarded to William C. Campbell, Satoshi Omura, and Youyou Tu for the discovery of avermectins and artemisinin, respectively, therapies that revolutionized the treatment of devastating parasite diseases. With the recent technological advances, a new Golden Age of natural products drug discovery is dawning.
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•CMC-g-PRSG nanocarriers are prepared from two compounds from natural materials.•Such nanocarriers can improve the affinity and light stability of pesticides on leaf.•AVM@CMC-g-PRSG ...maintains high insecticidal activity and improves biological safety.
The increasing world-wide demand for food has prompted the development of efficient and environmentally friendly pesticide formulations. In this article, we have prepared CMC-g-PRSG carrier based on two compounds from natural materials carboxymethyl cellulose (CMC) and rosin (RS). The model pesticide avermectin (AVM) was encapsulated through hydrophobic interaction, and self-assembled to form nanopesticide AVM@CMC-g-PRSG with an average particle size of 167 nm. The prepared nanopesticide displays enhanced dispersibility and stability of AVM in water, and can effectively adhere to the leaves to prevent loss. The release rate of AVM encapsulated in the nanocarrier can be controlled by adjusting pH, and AVM half-life under ultraviolet radiation shows a 3-fold increase allowing control of pests for prolonged periods of time in practical applications. Biological safety tests showed that AVM@CMC-g-PRSG effectively reduces the toxicity of AVM to aquatic animals. Therefore, the cheap and degradable carrier CMC-g-PRSG can improve the effect of hydrophobic pesticides.
Ivermectin has powerful antitumor effects, including the inhibition of proliferation, metastasis, and angiogenic activity, in a variety of cancer cells. This may be related to the regulation of ...multiple signaling pathways by ivermectin through PAK1 kinase. On the other hand, ivermectin promotes programmed cancer cell death, including apoptosis, autophagy and pyroptosis. Ivermectin induces apoptosis and autophagy is mutually regulated. Interestingly, ivermectin can also inhibit tumor stem cells and reverse multidrug resistance and exerts the optimal effect when used in combination with other chemotherapy drugs.
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•Ivermectin effectively suppresses the proliferation and metastasis of cancer cells and promotes cancer cell death at doses that are nontoxic to normal cells.•Ivermectin shows excellent efficacy against conventional chemotherapy drug-resistant cancer cells and reverses multidrug resistance.•Ivermectin combined with other chemotherapy drugs or targeted drugs has powerful effects on cancer.•The structure of crosstalk centered on PAK1 kinase reveals the mechanism by which ivermectin regulates multiple signaling pathways.•Ivermectin has been used to treat parasitic diseases in humans for many years and can quickly enter clinical trials for the treatment of tumors.
Ivermectin is a macrolide antiparasitic drug with a 16-membered ring that is widely used for the treatment of many parasitic diseases such as river blindness, elephantiasis and scabies. Satoshi ōmura and William C. Campbell won the 2015 Nobel Prize in Physiology or Medicine for the discovery of the excellent efficacy of ivermectin against parasitic diseases. Recently, ivermectin has been reported to inhibit the proliferation of several tumor cells by regulating multiple signaling pathways. This suggests that ivermectin may be an anticancer drug with great potential. Here, we reviewed the related mechanisms by which ivermectin inhibited the development of different cancers and promoted programmed cell death and discussed the prospects for the clinical application of ivermectin as an anticancer drug for neoplasm therapy.
S2k‐Leitlinie: Rosazea Clanner‐Engelshofen, Benjamin M.; Bernhard, Dominik; Dargatz, Sonja ...
Journal der Deutschen Dermatologischen Gesellschaft,
August 2022, 2022-08-00, 20220801, Letnik:
20, Številka:
8
Journal Article
Recenzirano
Odprti dostop
Zusammenfassung
Die vorliegende aktualisierte und auf S2k‐Niveau angehobene Leitlinie befasst sich mit der Diagnostik und der Therapie der Rosazea, bei welcher es sich um eine häufige, ...chronisch‐entzündliche Hauterkrankung handelt, die meist das Gesicht betrifft. Der Verlauf der Rosazea ist initial durch rezidivierende Erytheme, Teleangiektasien sowie Flushing gekennzeichnet. Später überwiegt die entzündliche Komponente, wobei es zu persistierenden Erythemen mit follikulären Papeln, Papulopusteln und Pusteln kommt. Die Bildung von Phymen, die meist an den Akren auftreten, stellt dabei die schwerste Ausprägung der Erkrankung dar. Zur Behandlung empfiehlt die interdisziplinäre Leitlinienkommission, die aus Vertretern der Deutschen Dermatologischen Gesellschaft (DDG), des Berufsverbandes der Deutschen Dermatologen (BVDD), der Deutschen Ophthalmologischen Gesellschaft (DOG), der Gesellschaft für Dermopharmazie (GD), der Schweizerischen Gesellschaft für Dermatologie und Venerologie (SGDV) und der Deutschen Rosazea Hilfe e. V. besteht, neben der Meidung von Triggerfaktoren, die topische Anwendung der Wirkstoffe Metronidazol, Azelainsäure oder Ivermectin. Zur symptomatischen Behandlung persistierender zentrofazialer Erytheme können zudem die Vasokonstriktoren Brimonidin oder Oxymetazolin topisch angewandt werden. Bei therapieresistenten sowie bei schweren Formen der Rosacea papulopustulosa wird eine systemische Therapie empfohlen. Hierfür ist niedrigdosiertes Doxycyclin das Präparat der 1. Wahl. Alternativ kann niedrigdosiertes Isotretinoin empfohlen werden. Für die okulären Rosazea kann neben einer Lidrandhygiene die topische Behandlung mit Ciclosporin‐haltigen Augentropfen, Azithromycin, Ivermectin oder Metronidazol empfohlen werden.
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