Tinidazole

Tinidazole is an antiparasitic and antimicrobial drug used to treat various infections caused by protozoal and bacterial pathogens. It belongs to the group of nitroimidazoles.

Tinidazole is used to treat conditions such as:

1. Trichomoniasis (infection caused by the protozoan Trichomonas vaginalis), most commonly seen as a genitourinary infection in women and men.
2. Amoebiasis (an infection caused by the amoeba Entamoeba histolytica), which can affect the intestines and cause a variety of intestinal symptoms.
3. Bacterial infections such as bacterial vaginosis and gastrointestinal infections caused by Clostridium difficile.

Tinidazole is also sometimes used in combination with other medicines to treat infections such as Helicobacter pylori, which can lead to stomach and duodenal ulcers.

The dosage and duration of tinidazole administration usually depend on the type and severity of the infection, as well as on the doctor's recommendations. Patients should strictly follow the doctor's instructions and complete the full course of treatment, even if symptoms disappear before completion, to prevent the possibility of recurrence of the infection.

Indications Tinidazole

Tinidazole is used to treat various infections caused by protozoal and bacterial pathogens. The main indications for the use of tinidazole include the following infections:

1. Trichomoniasis: An infection caused by the protozoan Trichomonas vaginalis, which most commonly occurs as a genitourinary infection in women and men.
2. Amoebiasis: An infection caused by the amoeba Entamoeba histolytica, which can affect the intestines and cause a variety of intestinal symptoms.
3. Bacterial Vaginosis: A disruption of the balance of bacteria in the vagina that can cause a variety of uncomfortable symptoms in women, such as odor, itching, and discharge.
4. Gastrointestinal infections: Certain bacterial infections of the gastrointestinal tract, including infections caused by Clostridium difficile.
5. Other infections: Tinidazole may also be used in combination with other medicines to treat infections such as Helicobacter pylori, which can lead to stomach and duodenal ulcers.

Release form

Tinidazole is available in the form of film-coated tablets containing 500 mg of active substance. Tablets are packed in contoured cell packs, each of which may contain 4 tablets.

Pharmacodynamics

Tinidazole is a nitroimidazole antiprotozoal agent with a broad spectrum of activity, including against pathogenic protozoa (e.g. Trichomonas vaginalis, Entamoeba histolytica, Giardia duodenalis) and a wide range of clinically important anaerobic bacteria (e.g. Bacteroides fragilis, Clostridium difficile), as well as the microaerophilic bacterium Helicobacter pylori. Within sensitive protozoa and bacterial cells, tinidazole is reduced to cytotoxic intermediates that covalently bind to DNA, causing irreversible damage. Tinidazole has a bioavailability of 100%, a volume of distribution of 50.7 L, binds minimally to plasma proteins (12%), has a plasma half-life of 12.3 hours, and is predominantly metabolized in the liver (approximately 63%). Dose adjustment does not appear to be required based on race, gender, or renal function. Data on the distribution of tinidazole in patients with severe hepatic impairment are not available; therefore, the use of tinidazole in patients with severe hepatic impairment (Child-Pugh class C) is not recommended. Clinical studies have shown that tinidazole is effective in the treatment of trichomoniasis, giardiasis, amoebiasis and amebic liver abscess, providing overall cure rates of more than 90%.

The most commonly reported side effects include bitter taste, nausea, abdominal discomfort, anorexia, vomiting and fatigue. The recommended dosage of tinidazole is a single dose of 2 g for the treatment of trichomoniasis and giardiasis and 2 g/day for 3-5 days for amoebiasis.

This information emphasizes the importance of tinidazole as a promising agent for the treatment of trichomoniasis, giardiasis, amoebiasis and amebic liver abscess. Additional clinical studies are needed to evaluate the use of tinidazole against anaerobic bacteria and H. Pylori.

Pharmacokinetics

Tinidazole pharmacokinetics describes how the drug interacts with the body, passes through the body, and how the body metabolizes and excretes it. Here are the main aspects of tinidazole pharmacokinetics:

1. Absorption: Tinidazole is usually well absorbed from the gastrointestinal tract after oral administration. Food may increase its absorption, so it is recommended to take tinidazole with meals.
2. Metabolism: Tinidazole is metabolized in the liver. The main metabolite is hydroxytinidazole, which also has activity against protozoa and bacteria.
3. Distribution: Tinidazole is widely distributed throughout the tissues and organs of the body, including the intestines, liver, kidneys, lungs and urogenital organs. It may penetrate the placental barrier and be excreted in breast milk.
4. Excretion: Tinidazole is mainly excreted from the body through the kidneys in the form of metabolites. About 60-70% of the dose is excreted through the urine, the rest - through the intestine.
5. Half-life: The half-life of tinidazole is about 12-14 hours, allowing it to be taken throughout the day given this decomposition time.
6. Concentration: Tinidazole may reach maximum blood concentrations about 2-4 hours after administration.
7. Dosage and regimen: The dosage and regimen of tinidazole may vary depending on the type of infection, severity of disease, and other factors. It is usually taken orally as tablets or suspension, and the frequency of administration may vary from once a day to several times a day.

Dosing and administration

The method of use and dosage of tinidazole depends on the type of infection, its severity, and your doctor's recommendations. Tinidazole is usually taken orally, with food, to reduce the possibility of stomach side effects. Here are general recommendations for route of administration and dosage:

1. Trichomoniasis: A single dose of 2 g tinidazole (4 500 mg tablets) at one time is usually prescribed for the treatment of trichomoniasis in adult women and men.
2. Amoebiasis: For the treatment of amoebiasis, adult dosage may range from 1.5 to 2 g (3 to 4 500 mg tablets) per day for 3 to 5 days.
3. Bacterial vaginosis: A single dose of 2 g tinidazole (4 500 mg tablets) is usually prescribed to treat bacterial vaginosis.
4. Gastrointestinal Infections: For the treatment of gastrointestinal infections, the dosage is usually 2 g (4 500 mg tablets) daily for 3 to 5 days.

For children, the dosage is determined individually based on their weight and health status, and is usually about half the adult dose.

Use Tinidazole during pregnancy

Tinidazole is contraindicated for use in the first trimester of pregnancy. In subsequent periods of pregnancy and during breastfeeding, use is possible only under strict indications, when the expected benefit to the mother exceeds the potential risk to the fetus or child.

Contraindications

Tinidazole is contraindicated in the following cases:

1. Individual intolerance or allergy to tinidazole or other nitroimidazole derivatives. Patients with known allergy to metronidazole or other drugs of this class may be contraindicated with tinidazole due to possible cross-allergy.
2. First trimester of pregnancy. In accordance with the general guidelines for the use of medicinal products during pregnancy, the use of tinidazole in the first trimester of pregnancy should be limited due to the lack of sufficient safety data.
3. Period of lactation. Tinidazole penetrates into breast milk, which may pose a potential risk to a nursing child. It is recommended to avoid the use of tinidazole during breastfeeding or discontinue breastfeeding during treatment and for a certain period after its termination.

These contraindications are based on the pharmacological properties of tinidazole and the general principles of its use. Before starting treatment, it is important to carefully read the instructions for use of the drug and consult a doctor to take into account all potential risks and limitations.

Side effects Tinidazole

Tinidazole is usually well tolerated, but like any medication, it can cause side effects in some patients. Some of the possible side effects of tinidazole include:

1. Gastrointestinal disorders: The most common side effects are nausea, vomiting, diarrhea, constipation, abdominal bloating and dyspepsia. These symptoms are usually easily tolerated and go away after completion of treatment.
2. Headache and dizziness: Some patients may experience headache, dizziness, or a feeling of weakness while taking tinidazole.
3. Allergic reactions: In rare cases, an allergic reaction to tinidazole may develop, manifested as skin rash, itching, urticaria, facial edema or difficulty breathing. In case of allergic reactions you should immediately stop taking the drug and consult a doctor.
4. Changes in blood: In rare cases, tinidazole may cause a temporary decrease in the number of white blood cells, platelets and other blood elements. This may lead to symptoms such as increased fatigue, susceptibility to infections, or bleeding.
5. Other side effects: Other possible side effects of tinidazole include changes in taste, vaginal irritation in women, and changes in measures of liver function.

Overdose

Tinidazole overdose may lead to worsening of side effects described earlier, such as nausea, vomiting, diarrhea, headache, dizziness and others. In case of overdose it is recommended to seek medical attention.

The physician may recommend symptomatic therapy aimed at eliminating unwanted manifestations. This may include symptomatic treatment of gastrointestinal disorders, administration of infusion solutions to restore water-electrolyte balance, and other supportive measures depending on the severity of symptoms.

Interactions with other drugs

Tinidazole may interact with other medicines, which may alter their effectiveness, increase the risk of side effects, or cause other undesirable effects. Below are some known interactions of tinidazole with other drugs:

1. Alcohol: Alcohol intake during tinidazole treatment may cause acute disulfiram-like reactions such as nausea, vomiting, dizziness, pulse, headaches, etc. Therefore, it is recommended to avoid alcohol and products containing alcohol while taking tinidazole.
2. Antimicrobials: Interactions may occur with other antibiotics or antiparasitic agents, which may increase or decrease their effectiveness. For example, the combination of tinidazole with ampicillin or amoxicillin may result in decreased efficacy of the latter.
3. Anticoagulants: Tinidazole may increase the effect of anticoagulants (drugs that reduce blood clotting), such as warfarin, which may increase the risk of bleeding. When combined with such drugs, it is recommended to regularly monitor blood clotting parameters and adjust the dosage of anticoagulants if necessary.
4. Phenytoin and warfarin: Tinidazole may increase the blood levels of these drugs, which may lead to an increase in their toxic effects.
5. Lithium: Tinidazole may increase lithium levels in the blood, which may lead to increased lithium toxicity.

Before starting tinidazole or making changes to your treatment regimen, it is important to consult your doctor or pharmacist to avoid potential interactions with other medicines.

Storage conditions

Storage conditions for tinidazole may vary depending on the form of release and the manufacturer of the drug. However, it is generally recommended to store tinidazole according to the following recommendations:

1. Temperature: The product should be stored at room temperature, between 15 and 30 degrees Celsius.
2. Light: It is recommended that most forms of tinidazole be stored in a light-protected area to avoid exposure to direct sunlight.
3. Humidity: Storage of tinidazole in a place with low humidity is preferred to avoid damage to tablets or capsules from moisture.
4. Packaging: The drug should be stored in the original package or container to avoid exposure to external factors.
5. Additional instructions: It is important to follow the instructions on the package and the manufacturer's directions regarding storage conditions, as they may vary slightly from drug to drug.

It is important to avoid storing the drug in areas accessible to children or pets, and to avoid storage in humid or hot places, as this may affect the stability of the drug.