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information about product

METRONIDAZOLE
(Metranidazole 0,5% Intravenous solution for injection)

The trading (patented) name of a preparation - METRONIDAZOLE
The international name–
Metranidazole
ATC-Code – J01XD01


STRUCTURE AND THE FORM OF RELEASE
1 litre of a solution contains
Metronidazole ........... 5g
Sodium Chloride......7.9g
Monosubstituted Sodium Phosphate2H2Ξ......0.355g
Disubstituted Sodium Phosphate......0.162g
Citric Acid......0.229g
Other ingredients: water for injection.
100 ml of solution in plastic PVC containers.

Definition
Clear Liquid, Colourless or with yellowish-greenish shade.

PHARMACOLOGICAL GROUPE
Antibacterial means with antimicrobial activity, derivative of nytroimidazole.

PHARMACOLOGICAL EFFECT
Antibacterial and antimicrobial preparation, derivative of 5- intorimidazole. It’s effect lies in the biochemical reduction of 5-nitrogroups with intercellular transporting proteins of anaerobic microorganisms and protozoa. The reduced 5-nitrogroups interacts from DNA cells of microorganisms, inhibting the synthesis of their nucleic acids, which leads to the destruction of bacteria
The preparation is active towards: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp.; anaerobic bacteria; Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens), Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. MPK for these culture is 0,125-6,25 mkg/ml.
In combination with amoxicillin it reveals activity towards Helicobacter pylori (amoxicillin suppresses the development of resistance towards metronidazole).
Anaerobic microorganisms and optional anaerobes are settled in the preparation, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergeticaly with antibiotics, which are effective towards aerobes.
The preparation increases the sensitivity of tumors towards radiation, and has disulfurized effect, stimulates reparation processes.

PHARMACOKINETICS
ABSORPTION
After 20 minutes intravenous administration of 500 mg Cmax in the blood serum becomes 35.2 mkg/ml in an hour, 25.7 mkg/ml in 8 hours, 33.9 mkg/ml in 4 hours; Cmin during continuous introduction – 18 mkg/ml.
During intravenous administration Cmax is attained in 30-60 minutes, therapeutic concentration is preserved about 6-8 hours
During normal gall-formation the concentration of metronidazole in gall after intravenous injection can considerably exceed in plasma.
ALLOCATION
Combined with plasma proteins – 10-20%. Vd with adults – 0.55 l/kg, with infants – 0.54-0.81 l/kg.
Metronidazol possesses high penetrating/ infiltrating ability. Reaches to bactericidal concentration in lungs, kidney, liver, brain, skin, spinal fluid, gall, saliva, amniotic fluid, abscess cavity; vaginal secretion, seminal fluid, pectoral milk. Penetrates through hematoencephalic barrier and passes through placental barrier.
METABOLISM
Metabolizes (about 30-60%) by means of hydro-oxidization, oxidation, glucosidation
Basic metabolite – 2 oximetronidazole – has antibacterial and antimicrobial effect.
DEDUCTION
Is moved out/deducted through kidneys (60-80%), 20% - in immutable form, deducted through intestine 6-15%. T1/2 is deducted in 8 hours (6-12 hours). Renal clearance – 10.2 ml/min.

SIDE-EFFECTS

– Bacterial infections (extra-intestinal amebiasis /including liver abscess/, intestinal amebiasis, trichomoniasis, balantidiasis, lambliasis (girardiasis), cutaneous [dermal] leishmaniasis, Trichomonas vaginata, Trichomonas urethritis;
– infections causing Bacteroides spp., including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus (infections of bones and joints, infections of CNS/ including meningitis, brain abscess/ bacterial endocarditis, pneumonia, empyema and abscess in lungs);
– infections causing Bacteroides spp. (including Bacteroides fragilis), Clostridium spp., Peptococcus spp., Peptostreptococcus spp. (infections of abdominal cavity/ peritonitis, liver abscess/, infections of genitals endomiometritis, abscess of Fallopian tube and ovary, infections of fornix [vault] of vagina after surgical operation, infections of skin and soft tissues;
– sepsis, causing Bacteroides spp. (including Bacteroides fragilis) and Clostridium spp.;
– pseudo-membranous colitis(in result of using antibiotics).
– gastritis or ulcer of duodenum in result of Helicobacter pylori;
– prophylaxis of post-operational infection (especially after operation on colon, near rectal tract, appendectoma after gynaecological operations).

DOSAGE
Recommended for intravenous drop injection to adults and children above 12 years initial dosage being 0,5-1g (injection duration being 30-40 min). Then adminsitred 500 mg in every 8 hours with rate up to 5 ml/min. If after the first 2-3 injections endurance is satisfactory then it could be passed to flow injection. The course of treatment is 7 days. If necessary the treatment through intravenous administration is prolonged. Maximum daily dosage is 4 g. According to indications it could be followed by supporting administration in the dosage of 400 mg - 3 times a day.
For children under 12 it is prescribed in the same scheme for only single use in the dosage of 7,5 mg/kg
During suppurative-septic diseases usually 1 course of treatment is implemented.
For prophylactic purposes the preparation is prescribed as an injection for adults and children above 12 in the dosage of 0,5-1 g a day before the operation, on the day of operation and on the day following the operation – 1,5 g a day (500 mg in every 8 hours) After 1-2 days intravenous supporting therapy starts. For patients with chronic renal deficiency and the quantity of ciratinine less than 30 ml/min maximum daily dose is 1 gr.

SIDE-EFFECTS
Digestion system: nausea; vomit(ing), diarea, intestinal colic, constipation,
metallic taste in the mouth, dryness in the mouth, glossitis, stomatitis, pancreatitis
Nervous system: dizziness; hypotaxia (incoordination), ataxy, mental confusion, irritability, depression, heightened excitability, weakness, insomnia, headaches, cramps, hallucination, peripheral neuropathy.
Urinary tract: dysuria, cystitis, polyuria, enuresis, red-brown urine;
Allergic reactions; skin rash, nettle-rash, skin hyperemia, fever, stuffiness in nose, arthralgia.
Local reactions, during intravenous injection – trombophlebitis (pain, reddening, hydropic syndrome).
ΟStrong/ durable candidosis, leuko(cyto)penia, peaking of T-wave on ECG

CONTRAINDICATION

– leuko(cyto)penia (including anamnesis);
– Organic affection of Central nervous system (CNS)
– epilepsy;
– hepatic deficiency (on using the preparation in higher doses;
– pregnancy (I term);
– lactation (breast-feed);
– hypersensitivity towards the preparation.

PREGNANCY AND LACTATION
The preparation is contra-indicated for usage in the 1 st term of pregnancy and during breast feeding. The preparation must be prescribed cautiously in the II and III terms of pregnancy.

OVERDOSAGE
Data regarding overdosage is missing.

SPECIAL INDICATIONS

It should be taken into consideration that during the usage of the preparation the use of ethanol is contra-indicated, as since development of disulfiram reaction is possible (spastic pains on the abdomen, nausea, vomiting, headache, sudden rush of blood to face).
During long term therapy hematological indicators should be controlled.
If neurological symptoms will be developed the usage of the preparation should be terminated.
During the treatments of Trichomonas vaginata at females, Trichomonas urethritis at man it is necessary to abstain from sexual life. Simultaneous treatment of sexual partners is obligatory. The treatment should be continued during menstruation. After the treatment of trichomoniasis control analysis should be hold in 3 regular/ periodic cycles before and after menstruation. /
After the treatment of lambliosis (girardiasis) (if the symptoms remain) after 3-4 weeks it is necessary to hold 3 analysis of faeces by few day intervals (in some successfully treated patients permanent lactose and could remain for few weeks or months looking like lambliosis).
The preparation can immobilize thryponem and cause unfavorable test of Nelson/
It is not recommended to combine with nondepolarizing muscle relaxants nondepolarizing miorelaxers (i.e. vecuronium bromide)/
USAGE IN PAEDIATRICS
It is not recommended to use the preparation in combination with amoxicyline for patients under 18.

MEDICINAL INTERACTION
During simultaneous usage of Metronidazole with indirect anticoagulant it is noted that the time for the development of protromine is extended./
During simultaneous usage of Metronidazole – ACOS with preparations of lithium salts increase of lithium concentration in blood plasma as well as development of intoxication symptoms are possible.
During simultaneous usage with cymeditine inhybation of Metronidazole metabolism is noted, which could lead to increase of Metronidazole concentration in plasma and increase of the risk of side effects./
Sulphanilamids amplifies/enlarges the antimicrobial effect of Metronidazole.
During simultaneous usage with enthanol disulfiram reactions are noted.
PHARMACEUTICAL EFFECT Intravenous administration of Metronidazole with other medicinal preparations is not recommended.

STORAGE CONDITIONS AND SHELF LIFE
The preparation should be stored in a place protected from light at room temperature. Expiry date of the intravenous solution is 2 years

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