Source: Medicines and Medical Devices Safety Authority (NZ) Revision Year: 2020 Publisher: Novartis New Zealand Limited, PO Box 99102, Newmarket, Auckland 1149, New Zealand
Pharmacotherapeutic group: ophthalmologicals; Antiallergics
ATC Code: S01GX05
Lodoxamide trometamol is a mast cell stabiliser that inhibits the in vivo Type-I, IgEmediated (immediate) hypersensitivity reaction. Lodoxamide inhibits the increase in cutaneous vascular permeability that is associated with reagin or IgE and antigenmediated reactions.
In vitro studies have demonstrated the ability of lodoxamide to stabilise rodent mast cells and prevent antigen-stimulated release of histamine. In addition, lodoxamide prevents the release of other mast cell inflammatory mediators (i.e. SRS-A, slowreacting substances of anaphylaxis, also known as the peptido-leukotrienes) and inhibits eosinophil chemotaxis. Although lodoxamide’s precise mechanism of action is unknown, the drug has been reported to prevent calcium influx into mast cells upon antigen stimulation.
Lodoxamide has no intrinsic vasoconstrictor, antihistaminic, cyclo-oxygenase inhibition or other anti-inflammatory activity.
The disposition of 14C-lodoxamide was studied in six healthy adult volunteers receiving a 3 mg (50 μCi) oral dose of lodoxamide. Urinary excretion was the major route of elimination (83%). The elimination half-life of 14C-lodoxamide was estimated from urinary excretion data to be 8.5 hours.
The administration of Lomide Eye Drops to twelve healthy adult volunteers (one drop in each eye four times per day for ten days) resulted in only 3 plasma samples (from a total of 108) with detectable levels of lodoxamide (level of detection 2.5 ng/mL). It is, therefore, possible that minute amounts of lodoxamide might be absorbed systemically in some patients.
Studies in animals have not shown evidence of an increased occurrence of fetal damage.
Reproduction studies with lodoxamide trometamol administered orally to rats and rabbits in doses of 100 mg/kg/day produced no evidence of developmental toxicity. There are no or a limited amount of data from the use of Lomide Eye Drops in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. Because animal reproductive studies are not always predictive of human response, Lomide Eye Drops should only be used in pregnancy if clearly needed.
No evidence of impairment of reproductive function was shown in laboratory animal studies. There are no data available on the effect of lodoxamide on fertility in humans.
A long-term study with lodoxamide trometamol in rats (two-year oral administration) showed no neoplastic or tumourigenic effects at doses up to 100 mg/kg/day (more than 5,000 times the proposed human clinical dose).
No evidence of mutagenicity or genetic damage was seen in assays for gene mutations and chromosomal damage. In the BALB/c-3T3 Cells Transformation Assay, some increase in the number of transformed foci was seen at high concentrations.
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