Doxef - instructions for use, dose, side effects, contraindications

Active substanceCefpodoximeCefpodoxime

Similar drugsTo uncover

Doxef

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Lupine Co., Ltd. India

Sephpotek®

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Nobel Ilach Sanayi Ve Tidjaret A.Sh. Turkey

Dosage form: & nbspfilm coated tablets

Composition:

Composition per 1 tablet:

1 tablet, film-coated, contains:

dosage of 100 mg

active ingredient: cefpodoxime proxetil (in terms of cefpodoxime) - 100,0 mg;

auxiliary substances: carmellose calcium - 72,05 mg; lactose monohydrate 9.00 mg; hypromellose - 6.75 mg; sodium lauryl sulfate - 4.50 mg; magnesium stearate 2.25 mg;

film shell: opadray white 03-A-28718 - 5.62 mg.

dosage of 200 mg

active ingredient: cefpodoxime proxetil (in terms of cefpodoxime) - 200,0 mg;

auxiliary substances: carmellose calcium - 144.11 mg; lactose monohydrate - 18,0 mg; hypromellose - 13.50 mg; sodium lauryl sulfate 9.00 mg; magnesium stearate - 4.50 mg;

film shell: opadray white 03-A-28718 - 11.25 mg.

Description:

Dosage 100 mg: Round, biconvex tablets coated with a film coating, white or almost white, engraved "100" on one side. On the cross-section the nucleus is from white to almost white.

Dosage 200 mg: Round biconvex tablets coated with a film shell, white or almost white, engraved "200" on one side. On the transverse cut the core from white to almost white.

Pharmacotherapeutic group:Antibiotic-cephalosporin

ATX: & nbsp

J.01.D.D.13 Cefpodoxime

Pharmacodynamics:

Cefpodoxime is a semisynthetic broad-spectrum antibiotic of the third generation cephalosporin group. Cefpodoxime - a prodrug, the active metabolite of which is cefpodoxime. The bactericidal activity of cefpodoxime is due to the suppression of the synthesis of peptidoglycans at the ribosomal level in the bacterial cell walls.

Cefpodoxime is active against the following Gram-positive bacteria

Usually sensitive

Aerobic Gram-positive microorganisms:

Staphylococcus aureus (methicillin-sensitive strains)

Streptococcus pneumoniae

Streptococcus pyogenes

Aerobic Gram-negative microorganisms:

Haemophilus influenzae

Neisseria gonorrhoeae

Proteus mirabilis

Intermediate sensitivity (possible acquired resistance)

Aerobic Gram-positive microorganisms:

Staphylococcus aureus

Staphylococcus epidermidis

Staphylococcus haemolyticus

Staphylococcus hominis

Staphylococcus saprophyticus

Staphylococcus pneumoniae (strains with intermediate sensitivity to penicillin)

Aerobic Gram-negative microorganisms:

Citrobacter freundii

Enterobacter cloacae

Escherichia coli

Klebsiella pneumoniae

Moraxella catarrhalis

Serratia marcescens

Resistant microorganisms

Aerobic Gram-positive microorganisms:

Enterobacter spp.

Staphylococcus aureus (methicillin-sensitive strains)

Streptococcus pneumoniae (penicillin-sensitive strains)

Aerobic Gram-negative microorganisms:

Morganella morganii

Pseudomonas aeruginosa

Other microorganisms

Chlamydia spp.

Chlamydophila spp.

Legionella pneumophila

Mycoplasma spp.

Cefpodoxime is also active against Acinetobacter spp. (including Acinetobacter baumannii), Citrobacter spp., (including Enterobacter cloacae and Enterobacter aerogenes), However, for these species, the effectiveness of the action is largely determined by the developing resistance to cefpodoxime.

With respect to anaerobes, it shows little activity, including a significant proportion of species Yersinia spp. (including Yersinia enterocolitica), Peptococcus spp., Peptosterptococcus spp.

Cefpodoxime is inactive for methicillin-resistant strains Staphylococcus spp., Streptococcus spp. (groups D), Enterococcus spp., Serratia spp., Pseudomonas spp. (at t.h.), Corynebacterium spp. (groups J and TO), Listeria monocytogenes, Clostridium difficile, Bacteroides spp.

General mechanisms of development of resistance of cefpodoxime as well as other cephalosporin antibiotics are due to changes in membrane permeability or modification of penicillin-binding proteins (PBP), production of beta-lactamase, and inhibition of access and penetration of drug molecule in the target area.

The threshold values of MIC of cefpodoxim are listed below for various bacterial pathogens:

Pathogens	Sensitivity	Resistance
	(mg / L)	(mg / L)
Enterobacteriaceae *	≤ 1	> 1
Streptococcus pneumoniae	≤0,25	>0,5
Haemophilus influenzae	≤0,25	>0,5

* Only uncomplicated urinary tract infections.

Pharmacokinetics:

Ceppodoxime is a prodrug that is absorbed from the gastrointestinal tract (GIT) and hydrolyzed in the small intestine to the active metabolite, cefpodoxime.

After taking 100 to 400 mg of the drug through 2.0-3.0 hours, a concentration of 1.2-4.5 mg / L is achieved, which is therapeutic. The volume of distribution is about 32 liters.

Absolute bioavailability is 50%. Cefpodoxime binds to blood serum proteins (up to 40%), kidneys in unchanged form displays about 80% of the dose with a half-life (T1 / 2) of 2.1 to 3.9 hours.

In patients with impaired renal function, excretion decreases: with creatinine clearance of 50-80 ml / min, T1 / 2 averages 3.5 hours; with a creatinine clearance of 30-40 ml / min, T1 / 2 is 5.9 hours; at 5-29 ml / min - 9.8 hours.

In elderly people, including with broncho-pulmonary infection, there is a slight lengthening 1m and concentration of cefpodoxim in the blood, but not requiring dose adjustment, except for patients with reduced renal function.

Indications:

Infections caused by susceptible to cefpodoxim pathogens:

- Infections of the upper and lower respiratory tract: tonsillitis, pharyngitis, acute sinusitis, acute bronchitis, pneumonia, exacerbation of chronic bronchitis (including in smokers and persons over 65 years of age);

- uncomplicated urinary tract infections (cystitis);

- uncomplicated gonorrhea in women (gonorrheal urethritis, gonorrheal cervicitis), anorectal infection in women caused by sensitive Neisseria gonorrhoeae;

- infections of the skin and soft tissues.

Sensitivity of antibiotics in vitro varies depending on the geographic region and over time, so when choosing antibacterial therapy local resistance information should be considered.

Contraindications:

- Hypersensitivity to cefpodoxime and to any of the components of the drug, other cephalosporins;

- severe hypersensitivity reactions to other β-lactam antibiotics (penicillins, monobactams and carbapenems) in the anamnesis;

- breast-feeding;

- children's age till 12 years;

- hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:Not severe hypersensitivity reactions to other β-lactam antibiotics (penicillins, monobactams and carbapenems), pollinosis, bronchial asthma (see section "Special instructions"); pregnancy, chronic colitis, renal failure, joint use with "loop" diuretics and other nephrotoxic drugs.

Pregnancy and lactation:Studies in animals have not revealed teratogenic or embryotoxic effects of cefpodoxime. However, due to a lack of clinical experience during pregnancy, the Doxef drug, especially during the first trimester of pregnancy, should be used with caution, comparing the potential benefit to the mother and the possible risk to the fetus.

Cefpodoxime penetrates into breast milk in small amounts. The safety of the drug Doxef for children with breastfeeding has not been established. You can not exclude the effect of cefpodoxim on a child who is breastfeeding when it is used by the mother in therapeutic doses and the risk of diarrhea, fungal infections of the mucous membranes and hypersensitivity reactions in the child. It is necessary to stop breastfeeding or stop / refrain from cefpodoxime therapy, taking into account the benefits of breastfeeding for the baby and the benefits of therapy for the mother.

Dosing and Administration:

Inside, with food. It is necessary to drink the preparation with a sufficient amount of liquid (1 glass of water).

For adults and children over 12 years of age in the following doses:

Indications for use	Dosing	Duration admission
Tonsillitis and pharyngitis	100 mg every 12 hours	5-10 days
Pneumonia	200 mg every 12 hours	14 days
Acute maxillary sinusitis Exacerbation of chronic bronchitis	200 mg every 12 hours	10 days
uncomplicated gonorrhea in women (gonorrheal urethritis, gonorrheal cervicitis), anorectal infection in women caused by Neisseria gonorrhoeae	200 mg	Once
Infections of the skin and soft tissues	200 mg every 12 hours	7-14 days
Uncomplicated urinary tract infections (cystitis)	100 mg every 12 hours	7 days

Renal failure: with creatinine clearance (CK) above 40 ml / min / 1.73 m² correction of the dose is not required; with SC 10-39 ml / min / 1.73 m² - single dose every 24 hours; with QC less than 10 - single dose every 48 hours.

Patients on hemodialysis - a single dose after each procedure of hemodialysis. Hepatic failure: dose adjustment is not required.

Side effects:

According to the World Health Organization (WHO), undesirable effects are classified according to the frequency of their development: very often (≥1 / 10); often (1/10-1/100); infrequently (1 / 100-1 / 1000); rarely (1 / 1000-1 / 10000); very rarely (<1/10000), the frequency is unknown (the frequency can not be determined based on the available data).

Infectious and parasitic diseases:

Often: fungal superinfections.

From the side of the blood and lymphatic system:

Infrequent: thrombocytosis (reversible after treatment);

Rarely: hemolytic anemia, eosinophilia, agranulocytosis, lymphocytosis, anemia, leukopenia, neutropenia, leukocytosis, thrombocytopenia.

From the immune system:

Rarely: allergic reactions, incl. Quincke's edema, anaphylactic reactions, bronchospasm, anaphylactic shock.

From the side of metabolism and nutrition:

Often: anorexia.

From the nervous system:

Infrequent: headache, paresthesia, dizziness.

From the organ of hearing:

Infrequent: noise in the ears.

From the gastrointestinal tract:

Often: a feeling of heaviness in the stomach, nausea, vomiting, flatulence, diarrhea.

Rarely: pseudomembranous colitis, acute pancreatitis.

From the liver and bile ducts:

Infrequently: increased activity of "liver" transaminases, an increase in the concentration of bilirubin.

Rarely: acute hepatitis.

From the side of the rut and subcutaneous tissues:

Infrequently: erythema, skin rash, hives, purpura, itching.

Rarely: erythema multiforme (including Stephen-Johnson syndrome), Lyell's syndrome.

From the side of the kidneys and urinary tract:

Rarely: increased concentration of creatinine and urea, acute renal failure.

Common violations:

Infrequently: asthenia, fatigue and malaise.

Overdose:

Symptoms: nausea, vomiting, discomfort in the epigastric region, diarrhea. In case of overdose, especially in patients with impaired renal function, encephalopathy, as a rule, is reversible with a decrease in cefpodoxime in the blood plasma.

Treatment: in case of an overdose of the drug, excretion of cefpodoxime from the body is performed with hemodialysis or peritoneal dialysis, especially if the kidney function is impaired.

Interaction:

Simultaneous use of the drug with diuretics, aminoglycosides, polymyxin B, ethacrynic acid increases the concentration of the drug in the blood, prolongs the half-life (T1 / 2), increases nephrotoxicity.

Nonsteroidal anti-inflammatory drugs (NSAIDs) slow the excretion of cephalosporins by the kidneys, increasing the risk of bleeding.

Blockers of H2-histamine receptors reduce bioavailability due to changes in the pH of the stomach. Antacids in high doses (sodium hydrogen carbonate, aluminum hydroxide) reduce the absorption.It is necessary to take these drugs with an interval of 2-3 hours.

Probenecid reduces the excretion of cephalosporins.

Ceppodoxime enhances the effects of indirect anticoagulants (suppressing the intestinal microflora and reducing the prothrombin index).

It is recommended to monitor the international normalized relationship (INR) during and shortly after the joint application of the drug with indirect anticoagulants.

When used simultaneously with other bactericidal antibiotics, synergism is manifested, with bacteriostatic (macrolides, chloramphenicol, tetracyclines) - antagonism.

Special instructions:

Recommended exercise extreme care when using the drug DOKSEF patients with allergic reactions of any kind in history (e.g., hay fever, bronchial asthma), as these patients are at increased risk of severe hypersensitivity reactions (see "With caution"). Use DOKSEF patients with known sensitivity to cephalosporin or hypersensitivity reactions to other β-lactam antibiotics (penicillins, monobactams and carbapenems) history contraindicated (see. The section "Contraindications").

Doxef should not be used in children younger than 12 years (see "Contraindications").

Pseudomembranous colitis caused by Clostridium difficile , can appear both on the background of long-term use, and 2-3 weeks after the cessation of treatment; is manifested by diarrhea, leukocytosis, fever, abdominal pain (sometimes accompanied by discharge with mucous masses of blood and mucus). If these phenomena occur in mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin inwards Metronidazole. Do not use drugs that inhibit the intestinal motility.

It is necessary to carry out careful monitoring of kidney function when applying Doxefa concomitantly with drugs with nephrotoxicity. It is necessary to avoid simultaneous application of Doxef and "loop diuretics". Care should also be taken with pregnancy, chronic colitis, renal failure (see "With caution").

In patients with impaired renal function, correction of the dosing regimen is necessary depending on the value of the CC (see the section "Dosing and Administration").

When treating the drug, false-positive results of the determination of glucose in urine can be noted (glucosuria is recommended to be determined only by enzyme method).

Doxef is not the main antibiotic for the treatment of staphylococcal pneumonia, nor should it be used in the treatment of atypical pneumonia caused by bacteria of the type Legionella, Mycoplasma and Chlamydia.

As with other β-lactam antibiotics, prolonged use of Doxefa may lead to the development of neutropenia, very rarely - agranulocytosis. It is required to conduct blood counts monitoring, with neutropenia the therapy is suspended. In some patients, a positive direct Coombs test is possible during treatment.

Continued use of cefpodoxime may lead to an overgrowth of resistant microorganisms.

Effect on the ability to drive transp. cf. and fur:

At the time of taking the drug, due to the risk of dizziness and other undesirable reactions, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 100 mg, 200 mg.

Packaging:

10 tablets in a blister of aluminum foil Al / Al.

For 1 or 2 blisters in a cardboard box together with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004285

Date of registration:10.05.2017

Expiration Date:10.05.2022

The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India

Manufacturer: & nbsp

LUPIN, Ltd. India

Representation: & nbspLUPIN LIMITEDLUPIN LIMITED

Information update date: & nbsp15.06.2017

Illustrated instructions

Instructions

Doxef (Doxcef)