Metronidazole  Tablets  500 mg   10 tab.  Pharmacological action

Metronidazole belongs to the group of antimicrobial drugs. The drug has high anaerobic activity. Has antiprotozoal and antibacterial effects.

Pharmacodynamics

The mechanism of action of Metronidazole is associated with a change in the DNA structure of pathogenic microorganisms that are sensitive to the action of the drug. These include:

• Trichomonas vaginalis;
• Entamoeba histolytica;
• Gardnerella vaginalis;
• Lamblia spp. ;
• Bacteroides spp. ;
• Fusobacterium spp. ;
• Veillonella spp. ;
• Clostridium spp. ;
• Peptostreptococcus spp. ;
• Eubacter spp. ;
• Peptococcus spp. ;
• Helicobacter pylori.

Aerobic and facultative anaerobic microorganisms exhibit resistance to the drug. Metronidazole has the ability to enhance the effect of radiation therapy on tumor formations.

Pharmacokinetics

Metronidazole is well absorbed orally. Evenly distributed in tissues and biological fluids of the body. The bioavailability of the drug is about 80%.The drug penetrates the BBB and the placental barrier. Binds to blood proteins by 20%. Metabolized in the liver. The half-life of Metronidazole is 8 hours. Most of the drug is excreted in the urine, the remainder in feces.

Indications for use of Metronidazole

Indications for prescribing Metronidazole depend on the form of release of the drug.Among the main diseases for which the drug is used are:

• urethritis;
• cystitis;
• vaginitis;
• dysentery;
• giardiasis;
• chronic form of alcoholism;
• prevention of infectious diseases in the postoperative period;
• peptic ulcer of the stomach or duodenum, as well as gastritis associated with Helicobacter pylori;
• acne;
• long-term non-healing wounds;
• trophic ulcers;
• demodicosis;
• amebiasis;
• stomatitis.

The dosage, form of release of the drug, frequency of use and duration of treatment are determined individually. The speed of recovery is influenced by the type of disease, its severity and the general condition of the body. There are general therapeutic recommendations for taking Metronidazole. These include:

1. The drug in tablet form is taken orally during or after meals.A single dosage varies from 250 to 500 mg. On average, the drug is taken 2-3 times a day.
2. Vaginal suppositories, tablets and gel are used intravaginally. The prescribed dosage is 500 mg 1–2 times a day. The average duration of treatment is 10 days. During therapy, it is recommended to abstain from sexual intercourse.
3. The dosage of ointment and gel for external use is selected individually.The course of treatment can last 3–9 weeks.

Contraindications

Metronidazole is not recommended for use in the following conditions:

• individual intolerance to the components of the drug;
• liver failure;
• lactation period;
• diseases of the central nervous system;
• leukopenia.

The drug is prescribed with caution during pregnancy and in case of renal failure. The dosage and frequency of taking the drug are selected individually.

Side effects of Metronidazole

The following side effects may occur while taking Metronidazole:

• nausea;
• stool instability;
• dry mouth;
• vomiting;
• appetite disturbance;
• stomatitis;
• dizziness;
• headache;
• impaired consciousness and coordination;
• emotional lability;
• hallucinations;
• weakness, increased fatigue;
• sleep disturbance;
• urticaria;
• Quincke's edema;
• candidiasis;
• cystitis;
• urinary incontinence.

The appearance of any of the above symptoms requires stopping the medication and consulting a doctor.

Overdose

Exceeding the therapeutic dosage of Metronidazole contributes to the appearance of overdose symptoms. These include:

• nausea;
• vomiting;
• convulsions;
• weakness;
• headache.

If these signs appear, it is recommended to stop taking the drug and consult a doctor. In severe cases of overdose, hospitalization is required. There is no specific antidote. To relieve the above symptoms, symptomatic therapy is used.

Interaction

Metronidazole enhances the effect of indirect anticoagulants.This is diagnosed by detecting an increase in prothrombin formation time.

The combined use of Metronidazole with ethanol contributes to the occurrence of side effects. Therefore, during treatment it is necessary to stop drinking alcohol.

Metronidazole contributes to the appearance of various neurological symptoms when prescribed together with Disulfiram.

The metabolism of Metronidazole slows down when it interacts with Cimetidine. Due to increased levels of the antimicrobial drug in the body, side effects may occur.

The simultaneous administration of Metronidazole with non-depolarizing muscle relaxants is not recommended.

Sulfonamides increase the antimicrobial activity of Metronidazole.

The combination of Metronidazole with Amoxicillin is not recommended for use in pediatric practice.

 

Children

Metronidazole is used in pediatric practice.The dosage is determined according to the age of the child:

• up to 1 year, 125 mg per day is prescribed;
• from 2 to 4 years, use 250 mg of Metronidazole per day;
• For children 5–8 years old, the daily dose of the drug is 375 mg;
• over the age of 8 years, 500 mg of Metronidazole per day is prescribed;
• Medications for external use are prescribed to children over 12 years of age.

Metronidazole during pregnancy and lactation

In the first trimester of pregnancy, taking Metronidazole is contraindicated. At a later date, the drug can be prescribed, but only if there are strict indications and under the supervision of a doctor. Due to the fact that the active substance of the drug penetrates into biological fluids, the use of Metronidazole is contraindicated during lactation.

Metronidazole and alcohol

The combined use of Metronidazole with alcoholic beverages is strictly prohibited. This is due to the fact that this combination can lead to side effects. These include a sharp drop in blood pressure, headache, dizziness, weakness, and fatigue.


 

What is metronidazole.

Metronidazole is a powerful antibiotic and antiprotozoal drug used to combat a wide range of bacterial and protozoal infections. It is available in various forms, including tablets, creams, and intravenous solutions.

What is metronidazole used for?

Metronidazole is used for several diseases, including:

Bacterial Infections: Metronidazole is particularly effective against anaerobic bacteria that thrive in environments deprived of oxygen.These bacteria are responsible for a number of infections, including but not limited to:

• Bacterial vaginosis: A common vaginal infection characterized by the overgrowth of certain bacteria in the vagina, leading to symptoms such as abnormal vaginal discharge, itching and foul odor.
• Intra-abdominal infections .Metronidazole is often used in combination with other antibiotics to treat abdominal infections such as peritonitis and abscesses.

Protozoal infections : Metronidazole is highly effective against a variety of protozoa, which are single-celled microorganisms that can cause serious infections:

• Trichomoniasis: A sexually transmitted infection caused by the parasite Trichomonas vaginalis, resulting in symptoms such as vaginal discharge and itching in women and urethral discharge in men.
• Giardiasis : an intestinal infection caused by the parasite Giardia lamblia, resulting in diarrhea, abdominal cramps and other gastrointestinal symptoms.
• Amebiasis: An infection caused by the amoeba Entamoeba histolytica, which can affect the intestines and liver, leading to symptoms such as dysentery and liver abscesses.

Infections of teeth and oral cavity .Metronidazole is sometimes prescribed in combination with other antibiotics to treat dental and oral infections, especially those involving anaerobic bacteria. This may include conditions such as dental abscesses and periodontal disease.

Helicobacter pylori infection: Metronidazole is part of a treatment regimen for Helicobacter pylori infection, a bacterial infection associated with stomach ulcers and gastritis.When used in combination with other antibiotics, it helps kill bacteria, promoting the healing of stomach ulcers.

Inflammatory bowel disease (IBD): In some cases, metronidazole may be prescribed to treat IBD symptoms such as Crohn's disease and ulcerative colitis. It is believed to help reduce inflammation in the gut and control certain symptoms during flare-ups.

Other uses: Metronidazole can be used in the treatment of other conditions such as rosacea, a chronic skin condition, where it can help reduce the inflammation and redness associated with the condition.

What is the mechanism of action of metronidazole.

The mechanism of action of metronidazole is unique and is primarily based on its ability to destroy and interfere with the DNA and metabolic processes of certain microorganisms.

• Activation of microorganisms . Metronidazole is administered in an inactive form and does not exhibit antimicrobial properties until absorbed by susceptible microorganisms such as bacteria and protozoa.Once inside the microorganism, metronidazole undergoes chemical transformation under the action of cellular enzymes.
• Formation of reactive forms . Transformed metronidazole generates reactive species, including nitroradicals, inside microbial cells. These reactive species are highly toxic and unstable molecules.
• DNA damage .One of the main targets of metronidazole is the DNA inside microbial cells. The reactive substances produced by metronidazole cause serious damage to the DNA structure. They cause DNA strand breaks and interfere with replication and repair processes.
• Suppression of DNA synthesis: Metronidazole disrupts the synthesis of new DNA molecules in microbial cells.This prevents microorganisms from replicating their genetic material, which is critical for their survival and reproduction.
• Metabolic disorders . Metronidazole also interferes with the metabolic processes of microorganisms. This impairs their ability to generate energy through the tricarboxylic acid (TCA) cycle, a key metabolic pathway.This disruption of energy production further weakens microorganisms.
• Toxic effects: Accumulation of DNA damage and metabolic disturbances lead to toxic effects on microbial cells. These effects include inhibition of cell division, disruption of cell membranes, and general cellular dysfunction.
• Death of microorganisms .The combined effects of metronidazole on DNA and metabolism ultimately lead to the death of microorganisms. This antimicrobial effect is particularly effective against anaerobic microorganisms that are sensitive to metronidazole due to their unique metabolic pathways.

What is the dosage of metronidazole.

Dosage may vary depending on the specific disease being treated, the age, weight and general health of the patient, and the form of the medication (oral, topical, intravenous, etc.). It is extremely important to follow the prescribed dosage and instructions from your healthcare professional to ensure safe and effective use of metronidazole.

Bacterial vaginosis :

• Oral tablets: The usual adult dose is 500 mg twice daily for 7 days. Alternatively, a single dose of 2 grams may be administered as a one-time treatment.
• Vaginal gel: A healthcare professional may prescribe a 0.75% concentration of metronidazole vaginal gel, which is inserted into the vagina once a day for 5 days.

Trichomoniasis :

• The typical adult dose is 2 grams (g) PO once or 250 mg three times daily for 7 days.

Anaerobic infections (intra-abdominal, gynecological, skin and soft tissue, etc.) :

• The dosage for adults is usually 500 to 750 mg orally every 6 to 8 hours. For severe infections, the dosage may be increased to 1 gram every 6 hours.

Giardiasis :

• For adults and children over 3 years of age, the usual dose is 250 mg orally three times daily for 5 to 7 days.

Amebiasis :

• The recommended dose for adults is usually 750 mg to 1 gram orally three times daily for 5 to 10 days, followed by treatment of luminal (intestinal) amoebiasis as needed.

Infection Helicobacter pylori :

• As part of combination therapy for H. pylori eradication, metronidazole is often prescribed at a dose of 500–750 mg twice daily for 7 days along with other antibiotics and acid-suppressing drugs.

Rosacea :

• For topical treatment of rosacea, metronidazole is available as a cream, gel or lotion.Typically, a thin layer is applied to the affected area of ​​skin once or twice daily as directed by your doctor.

What are the side effects of metronidazole.

Although metronidazole is very effective, like all medicines, it can potentially cause side effects in some people. It is very important to be aware of these side effects and discuss them with your doctor before and during treatment.

Common side effects :

• Nausea and vomiting . Gastrointestinal disorders are one of the most common side effects of metronidazole. This may include nausea, vomiting, and a metallic taste in the mouth.
• Diarrhea . Some people may experience diarrhea as a side effect of metronidazole.
• Headache . Headaches are another relatively common side effect.
• Loss of appetite : Metronidazole may cause a temporary loss of appetite or feeling of fullness.
• Metallic taste in the mouth.
• Dry mouth.
• Changes in taste sensations.

Less common side effects :

• Dizziness . Some people may feel dizzy or lightheaded.
• Effects on the nervous system: In rare cases, metronidazole may affect the central nervous system, resulting in symptoms such as confusion, irritability, or hallucinations.
• Dark Urine: Metronidazole may cause dark urine.
• Peripheral neuropathy .Long-term use of metronidazole, especially in high doses, can rarely lead to peripheral neuropathy, which is accompanied by tingling or numbness of the extremities.
• Allergic reactions . Although allergic reactions to metronidazole are relatively rare, they can be serious. Symptoms may include hives, rash, itching, swelling of the face, lips or tongue, and difficulty breathing.Seek immediate medical attention if you experience any of these symptoms.

It is important to note that most people taking metronidazole do not experience serious side effects.

What precautions should you take when taking metronidazole?

When using metronidazole, it is important to take certain precautions to ensure its safe and effective use. The following precautions may help minimize risks and optimize treatment.

• Prescription only: Metronidazole is available with a prescription. Always use it under the direction and supervision of a qualified healthcare professional.Do not self-medicate or share your medicine with others.
• Medical history . Tell your doctor your complete medical history, including any allergies, liver disease, kidney disease, blood disorders, and nervous system disorders. This information can help determine appropriate dosage and monitor potential risks.
• Pregnancy and breastfeeding .If you are pregnant, planning to become pregnant, or breastfeeding, discuss the risks and benefits of metronidazole with your doctor. In some cases, alternative medications may be recommended.
• Avoiding alcohol . Metronidazole can cause a disulfiram-like reaction when combined with alcohol, resulting in severe nausea, vomiting and headache.Avoid drinking alcohol during treatment with metronidazole and for at least 48 hours after your last dose.
• Allergy . If you have a known allergy to metronidazole or similar medications (such as tinidazole), tell your doctor right away. Allergic reactions can be serious and may require alternative treatments.
• Driving and operating machinery: Metronidazole may cause dizziness and drowsiness in some people. If you experience these side effects, avoid driving or operating heavy machinery until you are sure you can do so safely.
• Take the full course: Complete the entire prescribed course of metronidazole, even if your symptoms improve before you take all the medications.Stopping treatment early may result in persistent infection or development of drug resistance.

What drugs interact with metronidazole.

Metronidazole may interact with other medicines, which may either affect their effectiveness or cause unwanted side effects.Tell your doctor about all the medications and supplements you take to avoid potential interactions.

• Alcohol . Combining metronidazole with alcohol can lead to a disulfiram-like reaction. This reaction includes symptoms such as severe nausea, vomiting, headache and a general feeling of discomfort. Even small amounts of alcohol can cause this reaction.
• Warfarin (Coumadin) : Metronidazole may increase the effects of the blood thinning drug warfarin, increasing the risk of bleeding.
• Lithium: Metronidazole may increase lithium blood levels, potentially leading to lithium toxicity.
• Phenytoin (Dilantin) and other anticonvulsants .Metronidazole may change the metabolism of anticonvulsants such as phenytoin, resulting in changes in their blood levels.
• Cimetidine (Tagamet) : Cimetidine, an acid-reducing drug, may increase your blood levels of metronidazole.
• Anticoagulants and antiplatelet agents .Metronidazole may increase the risk of bleeding when taken with anticoagulants (eg, heparin) and antiplatelet agents (eg, aspirin).
• Disulfiram (Antabuse) : Disulfiram is a medicine used to treat alcohol dependence. When combined with metronidazole, it may increase the risk of a disulfiram-like reaction (similar to the reaction seen with alcohol).

Toxicity

In cases of overdose or long-term use of high doses, metronidazole can lead to toxicity, causing neurological symptoms such as seizures, peripheral neuropathy and liver toxicity. It is very important to follow the prescribed dosage and seek medical attention if you suspect an overdose.

Frequently asked questions (FAQ)

Question: Can I drink alcohol while taking metronidazole?

Answer: No, you should avoid drinking alcohol while taking metronidazole as it can cause severe nausea and vomiting.

Question: Is metronidazole safe during pregnancy?

Answer: It is recommended that you consult your healthcare provider if you are pregnant or plan to become pregnant because the safety of metronidazole during pregnancy has not been fully established.

Question: What are the common side effects of metronidazole.

Answer: Common side effects include nausea and a metallic taste in the mouth.Allergic reactions and neurological symptoms are rare but should be reported to your doctor.

Question: How does metronidazole work?

Answer: Metronidazole destroys the DNA of microorganisms, which leads to their death. It is particularly effective against anaerobic bacteria and protozoa.

Question: Can metronidazole interact with other medications?

Answer: Yes, metronidazole may interact with other medications, potentially affecting their effectiveness or causing adverse reactions. Tell your doctor about all the medications and supplements you take.

Question: What precautions should be taken when using metronidazole.

Answer: If you are pregnant, avoid drinking alcohol and use metronidazole with caution if you have liver disease.

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