Metronidazole-Akos bottles of 500 mg, 100 ml (metronidazole)

Release form

Infusion solution 0.5% transparent, with a greenish tint.

Packaging

100 ml - dark glass bottles (1) - packs of cardboard.

Pharmacological action

Antimicrobial, antiprotozoal.

Derived 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotamicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (P. bivia, P. buccae, P. disiens) and some gram-positive organisms Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). IPC for these strains is 0, 125–6.25 μg / ml.

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of resistance to metronidazole).

Aerobic microorganisms and some anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against regular aerobes.

Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like effect), stimulates reparative processes.

Pharmacokinetics

Absorption is high, oral bioavailability is at least 80%. It has high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretion, seminal fluid, breast milk passes through the BBB and the placental barrier. The distribution volume in adults is approximately 0.55 l / kg, in newborns - 0.54-0.81 l / kg. Cmax with oral administration is achieved after 1-3 hours and ranges from 6 to 40 μg / ml, depending on the dose. Plasma protein binding is 10–20%. With the on / in the introduction of 500 mg for 20 min Cmax in serum after 1 h - 35.2 μg / ml, after 4 hours - 33.9 μg / ml, after 8 hours - 25.7 μg / ml Cmin with subsequent administration - 18 mcg / ml. The time to reach Cmax is 30–60 min, the therapeutic concentration is maintained for 6–8 hours. With normal bile formation, the concentration of metronidazole in bile after iv administration can significantly exceed the plasma concentration.

About 30-60% of metronidazole is metabolized in the body by hydroxylation, oxidation and glucuronidation. The main metabolite (2-hydroxymetronidazole) also has an antiprotozoal and antimicrobial effect.

T1 / 2 with normal liver function - 8 hours (6 to 12 hours), with alcoholic liver damage - 18 hours (10 to 29 hours) in newborns born with a gestational age of 28-30 weeks - about 75 hours, 32 –35 weeks - 35 hours and 36–40 weeks - 25 hours, respectively. It is excreted by the kidneys 60–80% (20% unchanged), through the intestines - 6-15%. Renal clearance - 10.2 ml / min. In patients with impaired renal function after repeated administration, cumulation of metronidazole in serum may be observed (therefore, in patients with severe renal failure, the frequency of administration should be reduced). Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis, it is excreted in small quantities.

Indications

Protozoal infections: extraintestinal amoebiasis, including amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis, hyardiasis, balantidiasis, giardiasis, cutaneous leishmaniasis, trichomonas vaginitis.

Infections caused by Bacteroides spp. (including B.fragilis, B.distasonis, B.ovatus, B.thetaiotaomicron, B.vulgatus): infections of bones and joints, infections of the central nervous system, including meningitis, brain abscess, bacterial endocarditis, pneumonia, empyema and lung abscess.

Infections caused by Bacteroides species, including the B.fragilis group, Clostridium, Peptococcus and Peptostreptococcus species: infections of the abdominal cavity (peritonitis, liver abscess), infections of the pelvic organs (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, vaginal fornix infections after surgery), skin and soft tissue infections.

Infections caused by Bacteroides spp., including the B.fragilis group, and Clostridium spp.

Pseudomembranous colitis (associated with the use of antibiotics).

Gastritis or duodenal ulcer associated with Helicobacter pylori, alcoholism.

Prevention of postoperative complications (especially interventions on the colon, periorectal region, appendectomy, gynecological surgery).

Radiation therapy of patients with tumors - as a radiosensitizing agent in cases where tumor resistance is due to hypoxia in the tumor cells.

Contraindications

hypersensitivity, leukopenia (including a history), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of high doses), I trimester of pregnancy, breast-feeding.

Precautions - in the II and III trimesters of pregnancy, renal / liver failure.

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy with caution - in the second and third trimesters of pregnancy.

During lactation, it is recommended to stop breastfeeding.

Composition

1 ml1 vial

metronidazole 5 mg 500 mg

Excipients: sodium chloride, citric acid monohydrate, sodium hydrogen phosphate, water for injection.

Side effects of the digestive system: diarrhea, anorexia, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

From the nervous system: dizziness, impaired coordination of movements, ataxia, confusion, irritability, depression, irritability, weakness, insomnia, headache, cramps, hallucinations, peripheral neuropathy.

Allergic reactions: urticaria, skin rash, flushing of the skin, nasal congestion, fever, arthralgia.

From the genitourinary system: dysuria, cystitis, polyuria, urinary incontinence, candidiasis, staining of urine in red-brown color.

Local reactions: thrombophlebitis (pain, redness, or swelling at the injection site).

Other: neutropenia, leukopenia, flattening of the T wave on the ECG.

Drug Interaction

Metronidazole is not recommended for mixed administration with other drugs.

Increases the effect of indirect anticoagulants, leading to an increase in the time of prothrombin formation.

Ethanol intolerance is similar to disulfiram. Concomitant use with disulfiram can lead to the development of various neurological symptoms (interval between appointment - at least 2 weeks).

Cimetidine inhibits the metabolism of metronidazole, which may increase its serum concentration and increase the risk of side effects.

Simultaneous administration of drugs, stimulating enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, resulting in a decrease in its plasma concentration.

When co-administered with lithium, plasma concentrations of the latter and the development of intoxication symptoms may increase.

It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).

Sulfanylamides enhance the antimicrobial action of metronidazole.

overdose

There is no overdose on the drug.

Treatment: metronidazole and major metabolites are rapidly removed by hemodialysis (T1 / 2 reduced to 2.6 h). Peritoneal dialysis is excreted in small quantities.

Storage conditions

In a dry, dark place.

Keep out of the reach of children.

Expiration

2 years.

Do not use after the expiry date stated on the package.

prescription

pharmacies terms of prescription



Metronidazole-Akos bottles of 500 mg, 100 ml (metronidazole) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Metronidazole-Akos bottles of 500 mg, 100 ml - Sale. PayPal accept. Free shipping florida. Fast international shipping.