Tolerability, Safety, and Pharmacokinetics of Ivermectin After Nasal Application in Healthy Adult Subjects.
Nasal epithelium is the site of infection for SARS‐CoV2 viruses, with interactions of the viral spike protein with the ACE2 receptor of the host cell. Molecular docking studies have shown that ivermectin shields the spike protein and thereby prevents binding to ACE2. Nasal application of high doses...
| Publicado en: | Journal of Clinical Pharmacology Vol. 66; no. 1; pp. 1 - 18 |
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| Autores principales: | , , , , , |
| Formato: | research tables/charts randomized controlled trial Journal Article |
| Publicado: |
Wiley-Blackwell
Jan2026
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=191106126&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 191106126 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 00912700 5WH jtl: Journal of Clinical Pharmacology issn: 00912700 maglogo: Y pubinfo: dt: Jan2026 vid: 66 iid: 1 pid: 480 pub: Wiley-Blackwell place: Malden, Massachusetts artinfo: ui: 191106126 191106126 191106126 10.1002/jcph.70137 191106126 ppf: 1 ppct: 17 formats: tig: atl: Tolerability, Safety, and Pharmacokinetics of Ivermectin After Nasal Application in Healthy Adult Subjects. aug: au: Wissel, Stefan Wissel, Philipp Rischer, Matthias Häberlein, Felix Riethmüller‐Winzen, Hilde Häberlein, Hanns affil: HWI Pharma Services GmbH, Rülzheim, Germany sug: subj: Drug Tolerance Patient Safety Antibiotics, Macrolide Pharmacokinetics Administration, Intranasal Clinical Trials Antibiotics, Macrolide Administration and Dosage Human Male Female Adult Middle Age Germany Romania Prospective Studies Randomized Controlled Trials Double-Blind Studies Rhinorrhea Sneezing Body Weight Electrocardiography Blood Pressure Heart Rate Body Temperature Funding Source Adult: 19-44 years Middle Aged: 45-64 years Male Female ab: Nasal epithelium is the site of infection for SARS‐CoV2 viruses, with interactions of the viral spike protein with the ACE2 receptor of the host cell. Molecular docking studies have shown that ivermectin shields the spike protein and thereby prevents binding to ACE2. Nasal application of high doses of ivermectin could be the right therapeutic approach in the treatment and prevention of COVID‐19. Tolerability, safety, and pharmacokinetics of ivermectin, administered nasally as 5% microsuspension (F004), were investigated in a randomized, double‐blind, parallel‐groups, placebo‐controlled phase 1 study in 28 healthy adults. Bioavailability of a single dose of 14 mg ivermectin was determined with AUC0–tT of 1701.1 ng/mL h (AUC0–∞ of 2382.7 ng/mL h, calculated), Cmax of 96.2 ng/mL, Tmax of 4.4 h, and T1/2 of 59.9 h. Following 42 mg/day multiple dose (3 × 14 mg every 6 h) administered nasally over 5 days, AUC0‐∞ of 2194.4 ng/mL h was analyzed, and 96% of ivermectin concentrations were still measurable 12 h after the last dose. F004 was safe in this study and well‐tolerated. Nine (F004 group) and three (placebo group) of 28 subjects reported 14 symptoms, including a few systemic but mainly local nasal adverse events (AE). The number of subjects reporting AE decreased continuously after both F004 and placebo treatment. All subjects recovered fully with no AE recorded at the end of the study. Nasal examination showed stable patterns of nasal mucosal grading, mucosal bleeding, and crusting of the mucosa. Nasally administered ivermectin is well tolerated in high concentrations and could provide systemic therapeutic benefits in addition to local effects. pubtype: Academic Journal doctype: research tables/charts randomized controlled trial Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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