the Pharmacokinetics and Safety of Tiamulin

Q: the Pharmacokinetics and Safety of Tiamulin

Hello： The pharmacokinetics of Terbinafine show that it can reach a peak plasma concentration of 0.97 micrograms per milliliter (μg/ml) within 2 hours. <br>For toenail infections excluding the big toe, especially in young individuals with normal nail growth rates, the treatment d

Could you please provide more details about your question regarding Lamisil?

1.
The pharmacokinetic properties of Terbinafine (the active ingredient in Lamisil) include absorption, metabolism, and excretion.
Terbinafine is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 2 hours after oral administration.
It is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, and has a half-life of about 36 hours.
The drug is excreted mainly in the urine, with less than 1% of the dose being eliminated unchanged.
2.
Safety data for Terbinafine includes information on carcinogenicity, genotoxicity, and shelf life.
Terbinafine has not been shown to be carcinogenic in animal studies.
It has also demonstrated no significant genotoxic effects in various in vitro and in vivo assays.
The shelf life of Terbinafine is typically 24 months when stored under recommended conditions.

Da Xiong, 20~29 year old female. Ask Date: 2010/03/21

Dr. Hou Fangmin reply Pharmacology

Hello: The pharmacokinetics of Terbinafine show that it can reach a peak plasma concentration of 0.97 micrograms per milliliter (μg/ml) within 2 hours.
For toenail infections excluding the big toe, especially in young individuals with normal nail growth rates, the treatment duration can be less than 3 months.
Most other nail fungal infections require a treatment period of 3 months.
In the early stages of treatment, the rate of nail growth can be monitored; for patients with slow nail growth, treatment may need to extend beyond 3 months.
Optimal clinical improvement in symptoms after curing onychomycosis may take several months after discontinuation of the medication, as this is the time required for healthy nail growth.
This medication is metabolized by the liver and excreted by the kidneys.
There is limited data regarding its potential carcinogenicity.
The shelf life for the topical formulation is 4 years, while the oral formulation is 3 years.
The most common side effects include gastrointestinal discomfort (bloating, loss of appetite, nausea, mild abdominal pain, diarrhea) or skin reactions (rash and urticaria); there have been no life-threatening side effects reported or severe enough to necessitate discontinuation of the drug.
The aforementioned benign skin reactions should be distinguished from allergic reactions, which are rare but require cessation of the medication.
Due to hepatic metabolism and renal excretion, patients with severe liver or kidney impairment (creatinine clearance less than 50 mL/min or serum creatinine greater than 3000 micromoles per liter) should use a lower dosage.
It is advised that pregnant women avoid using this medication, and those taking it orally should not breastfeed.
I have attached a file for your reference.
Wishing you peace and happiness.

Reply Date: 2010/03/21

More Info

Tiamulin, a pleuromutilin antibiotic, is primarily used in veterinary medicine to treat bacterial infections in livestock and poultry. Its pharmacokinetics and safety profile are essential for understanding its therapeutic use and potential risks.

1. Pharmacokinetics of Tiamulin
Absorption: Tiamulin is well-absorbed after oral administration, with peak plasma concentrations typically occurring within 1 to 3 hours. The bioavailability can be influenced by the formulation and the presence of food, which may enhance absorption.

Distribution: Once absorbed, tiamulin is widely distributed throughout the body. It has a high volume of distribution, indicating extensive tissue binding. Tiamulin can penetrate various tissues, including lung, liver, and kidney, which is beneficial for treating infections in these areas.

Metabolism: Tiamulin undergoes hepatic metabolism, primarily through oxidation and conjugation processes. The liver plays a crucial role in its biotransformation, and the metabolites formed are generally less active than the parent compound.
Excretion: The elimination half-life of tiamulin varies but is typically around 6 to 12 hours in animals. It is primarily excreted through the urine and feces, with a significant portion being eliminated as metabolites. Renal function can influence the excretion rate, and adjustments may be necessary in cases of renal impairment.

2. Safety Profile of Tiamulin
Carcinogenicity: Current data on the carcinogenic potential of tiamulin is limited. Long-term studies in animals have not conclusively demonstrated a carcinogenic effect. However, as with any drug, it is essential to use it judiciously and according to guidelines to minimize potential risks.

Genotoxicity: Tiamulin has been evaluated for genotoxic effects, and studies have shown that it does not exhibit significant mutagenic properties. Nevertheless, it is always prudent to consider the potential for adverse effects when using any antibiotic, especially in food-producing animals.

Expiration Date: The effective shelf life of tiamulin varies depending on the formulation and storage conditions. Generally, it is advisable to adhere to the expiration date provided by the manufacturer, which is typically around 2 to 3 years from the date of manufacture when stored properly. After the expiration date, the efficacy and safety of the drug cannot be guaranteed.

Conclusion
In summary, tiamulin exhibits favorable pharmacokinetic properties, including good absorption, extensive tissue distribution, and effective metabolism and excretion. Its safety profile indicates a low risk of carcinogenicity and genotoxicity, making it a viable option for treating bacterial infections in veterinary medicine. However, as with any medication, it is crucial to follow prescribed guidelines and monitor for any adverse effects during treatment. Always consult with a veterinarian or a medical professional for specific recommendations and concerns regarding the use of tiamulin in clinical practice.

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