Where can I get more information (LamISIL)?
Your pharmacist can provide more information about Tineal.
How to take Tineal
- Before you start the treatment, read the manufacturer's printed information leaflet from ins >
Generic Name: Tineal hydrochloride Dosage Form: tablet
Medically reviewed by Drugs.com. Last updated on Dec 1, 2019.
Some people taking Tineal have developed severe liver damage leading to liver transplant or death.
Call your doctor at once if you have symptoms of liver damage, such as nausea, upper stomach pain, vomiting, loss of appetite, tiredness, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes). These events can occur whether or not you have ever had liver problems before.
Side effects of Tineal
Tineal appears to be a relatively safe drug. Side effects, usually minor, arise occasionally. Serious side effects occur rarely. Routine blood test monitoring is not considered necessary .
Adverse reactions to Tineal may include:
Is Tineal safe to take if I'm pregnant or breastfeeding?
There are no adequate studies in pregnant women. Since nail fungus treatment can be delayed until after pregnancy there is no reason to use oral Tineal during pregnancy.
Breastfeeding mothers should not use oral Tineal because Tineal passes into breast milk.
Before taking this medicine
You should not use Tineal if you are allergic to it, or if you have:
To make sure Tineal is safe for you, tell your doctor if you have ever had:
weak immune system (caused by disease or by using certain medicine); or
It is not known whether Tineal will harm an unborn baby. You should wait until after your pregnancy to start treating your nail or scalp infection with Tineal. Tell your doctor if you are pregnant or plan to become pregnant during treatment.
Tineal can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.
Tineal interferes with ergosterol biosynthesis, and thereby with the formation of the fungal cell membrane. It is absorbed from the gastrointestinal tract and undergoes extensive metabolism in the liver ( t½ 14 h). Tineal is used topically for dermatophyte infections of the skin and orally for infections of hair and nails where the site, e.g. hair, severity or extent of the infection renders topical use inappropriate (see pp. 270–271 ). Treatment may need to continue for several weeks. Tineal may cause nausea, diarrhoea, dyspepsia, abdominal pain, headaches and cutaneous reactions.
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The most frequently reported adverse events observed in the 3 U.S./Canadian placebo-controlled trials are listed in the Table 1. The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia, and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. Changes in the ocular lens and retina have been reported following the use of Tineal tablets in controlled trials. The clinical significance of these changes is unknown. In general, the adverse events were mild, transient, and did not lead to discontinuation from study participation. Table 1. Most frequently reported adverse events observed in the 3 U.S./Canadian placebo-controlled trials
Tineal tablets are contraindicated in patients with:
- Chronic or active liver disease
- History of allergic reaction to oral Tineal because of the risk of anaphylaxis
There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that Lamisil Tablets not be initiated during pregnancy.
Oral reproduction studies have been performed in rabbits and rats at doses up to 300 mg/kg/day and have revealed no evidence of impaired fertility or harm to the fetus due to Tineal.
Animal Toxicology And/Or Pharmacology
A wide range of in vivo studies in mice, rats, dogs, and monkeys, and in vitro studies using rat, monkey, and human hepatocytes suggest that peroxisome proliferation in the liver is a rat-specific finding. However, other effects, including increased liver weights and APTT, occurred in dogs and monkeys at doses giving Css trough levels of the parent Tineal 2-3x those seen in humans at the MRHD. Higher doses were not tested.
Tineal, an allylamine antifungal, inhibits biosynthesis of ergosterol, an essential component of fungal cell membrane, via inhibition of squalene epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of squalene but not due to ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Tineal hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown.
Tineal has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections:
Trichophyton mentagrophytes Trichophyton rubrum
The following in vitro data are available, but their clinical significance is unknown. In vitro, Tineal exhibits satisfactory MIC's against most strains of the following microorganisms; however, the safety and efficacy of Tineal in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials:
Candida albicans Epidermophyton floccosum Scopulariopsis brevicaulis
Carcinogenesis, Mutagenesis, Impairment of Fertility
In a 28-month oral carcinogenicity study in rats, an increase in the incidence of liver tumors was observed in males at the highest dose tested, 69 mg/kg/day (2 times the MRHD based on AUC comparisons of the parent Tineal); however, even though dose-limiting toxicity was not achieved at the highest tested dose, higher doses were not tested.
The results of a variety of in vitro (mutations in E. coli and S. typhimurium , DNA repair in rat hepatocytes, mutagenicity in Chinese hamster fibroblasts, chromosome aberration, and sister chromat >in vivo (chromosome aberration in Chinese hamsters, micronucleus test in mice) genotoxicity tests gave no evidence of a mutagenic or clastogenic potential.
Oral reproduction studies in rats at doses up to 300 mg/kg/day (12 times the MRHD based on BSA comparisons) did not reveal any specific effects on fertility or other reproductive parameters. Intravaginal application of Tineal hydrochloride at 150 mg/day in pregnant rabbits did not increase the incidence of abortions or premature deliveries nor affect fetal parameters.
Tineal is well absorbed after oral administration, but it undergoes significant “first-pass” metabolism and its resulting apparent bioavailability is only 45%. 190,191 It is metabolized to ten metabolites by at least seven different CYP enzymes, the most important apparently being CYP2C9, CYP1A2, and CYP3A4. 192 Tineal binds extensively to plasma proteins. 193 Of note, it distributes extensively to poorly perfused tissues (i.e., skin and ungual bed). 189 Tineal is extensively metabolized by the liver and 15 metabolites have been identified. 189