SOFTIN [Cefotaxime] 1 g Powder for the preparation of a solution for IM administration
SOFTIN
instructions for the medical use of the medicinal
product
Tradename
Softin, Софтин
International
non-proprietary name or generic name
Cefotaxime, Цефотоксим
Composition
Each vial contains:
Cefotaxime (as cefotaxime sodium)
1 g.
Solvent ampoule:
Lidocaine 1%.
Dosage form
Powder for preparation of solution for injection.
Antibiotic,
cephalosporin.
Pharmacological properties
Pharmacodynamics
III generation cephalosporin
antibiotic for parenteral administration. It has a bactericidal effect. The
mechanism of action is associated with a violation of the synthesis of
mucopeptide of the cell wall of microorganisms. Possesses a wide spectrum of
antimicrobial action.
The drug is active against
gram-positive and gram-negative microorganisms resistant to other antibiotics:
Staphylococcus spp. (including Staphylococcus aureus, including strains that
form penicillinase, excluding strains resistant to methicillin), Staphylococcus
epidermidis (excluding strains resistant to methicillin), Streptococcus
pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococci) Streptococcus
agalactiae (group B streptococci), Enterococcus spp., Enterobacter spp.,
Escherichia coli, Haemophilus influenzae (including strains that form
penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis spp.
(including Klebsiella pneumoniae, Klebsiella oxytoca), Morganella morganii,
Neisseria gonorrhoeae (including strains that form penicillinase),
Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathium
spp., Erysipelothrix rhusiopathium spp. ... (including Clostridium
perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris,
Providencia spp. (including Providencia rettgeri), Serratia spp., some strains
of Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including
some strains of Bacteroides fragilis), Fusobacterium spp. (including
Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.
Intermittently affects some strains
of Pseudomonas aeruginosa, Acinetobacter spp., Helicobacter pylori, Bacteroides
fragilis, Clostridium difficile.
Resistant to most
beta-lactamases of gram-positive and gram-negative microorganisms.
After i / m administration in
doses of 500 mg and 1 g, Tmax is 0.5 h, Cmax is 11 and 21 μg / ml,
respectively.
Plasma protein binding -
30-50%. Bioavailability is 90-95%. Therapeutic concentrations are achieved in
most tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids
(synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of
the body. Vd - 0.25-0.39 l / kg.
T1 / 2 with intramuscular
injection - 1-1.5 hours. Excreted by the kidneys: 20-36% - unchanged, the rest
- in the form of metabolites (15-25% - in the form of pharmacologically active
deacetylcefotaxime and 20-25% - in as 2 inactive metabolites).
In chronic renal failure and
in the elderly, T1 / 2 increases by 2 times. T1 / 2 in newborns - 0.75-1.5
hours, in premature newborns (body weight less than 1500 g) increases to 4.6
hours; in children weighing more than 1500 g - 3.4 hours.
Indications for use
After i / m
administration in doses of 500 mg and 1 g, Tmax is 0.5 h, Cmax is 11 and 21 μg / ml, respectively.
Plasma protein
binding - 30-50%. Bioavailability is 90-95%. Therapeutic concentrations are
achieved in most tissues (myocardium, bones, gallbladder, skin, soft tissues)
and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal
fluid) of the body. Vd - 0.25-0.39 l / kg.
T1 / 2 with
intramuscular injection - 1-1.5 hours. Excreted by the kidneys: 20-36% -
unchanged, the rest - in the form of metabolites (15-25% - in the form of
pharmacologically active deacetylcefotaxime and 20-25% - in as 2 inactive
metabolites).
In chronic renal
failure and in the elderly, T1 / 2 increases by 2 times. T1 / 2 in newborns -
0.75-1.5 hours, in premature newborns (body weight less than 1500 g) increases
to 4.6 hours; in children weighing more than 1500 g - 3.4 hours.
For forms containing
lidocaine as a solvent:
- hypersensitivity to
cefotaxime and other cephalosporins;
- hypersensitivity to
lidocaine or other local anesthetic of the amide type;
- intracardiac
blockade without an established pacemaker;
- severe heart
failure;
- chronic renal
failure;
- pregnancy;
- intravenous
administration;
- children's age up
to 2.5 years (for intramuscular injection).
Method of administration and dosage
Intramuscularly.
The dose and
frequency of administration should be determined by the severity of the
infection, the sensitivity of the pathogen and the condition of the patient.
Adults and children
over 12 years old and weighing 50 kg or more: for infections of mild and
moderate severity - 1 g every 12 hours.
In severe infections,
the dose can be increased to 12 g per day, divided into 3 or 4 administrations.
For infections caused
by Pseudomonasspp., The daily dose should be more than 6 g.
Children under 12
years old and weighing up to 50 kg: the usual dose is 100-150 mg /
kg / day, divided into 2-4 injections. For very severe infections, the dose may
be increased to 200 mg / kg / day.
Newborn: 50 mg / kg / day,
divided into 2-4 injections. For severe infections, a dose of 150-200 mg / kg /
day, divided into 2-4 injections.
With gonorrhea: 1 g once.
For the prevention of
infections before surgery (from 30 to 90 minutes before the start of the
operation) 1 g is administered.
With renal failure. In cases where
creatinine clearance is less than 10 ml / min, it is necessary to reduce the
dose. After the introduction of the initial single dose, the daily dose should
be halved without changing the frequency of administration, i.e. instead of 1 g
every 12 hours - 0.5 g every 12 hours, instead of 1 g every 8 hours - 0.5 g
every 8 hours, instead of 2 g every 8 hours - 1 g every 8 hours, etc. Further
dose adjustment may be required depending on the course of the infection and
the general condition of the patient.
Rules for the
preparation of solutions
Powder Softin 1 g is
dissolved in 4 ml of 1% lidocaine solvent. The solution is administered only
intramuscularly.
Special instructions and precautions
In the first weeks of treatment, pseudomembranous
colitis may occur, manifested by severe, prolonged diarrhea. At the same time,
they stop taking the drug and prescribe adequate therapy, including vancomycin
or metronidazole.
Patients with a history of allergic reactions to
penicillins may have an increased sensitivity to cephalosporin antibiotics.
When treating with the drug for more than 10 days, it
is necessary to control the picture of peripheral blood.
During treatment, alcohol should not be consumed,
since effects similar to the action of disulfiram are possible (flushing of the
face, cramps in the abdomen and in the stomach, nausea, vomiting, headache,
lowering blood pressure, tachycardia, shortness of breath).
Influence on the
ability to drive vehicles and mechanisms
Application during pregnancy and during breastfeeding
Contraindicated for use during pregnancy.
If it is necessary to use the drug during lactation, breastfeeding should be
discontinued.
Interaction with other medicinal products
Aminoglycoside antibiotics,
diuretics - derivatives of ethacrynic acid and other diuretics (furosemide)
increase the risk of nephrotoxicity when used simultaneously with cefotaxime.
When combined with indirect
anticoagulants, synergism develops.
Combined use with nifedipine
increases the bioavailability of cefotaxime by 70%.
Probenecid blocks the tubular
secretion of cefotaxime and lengthens its half-life.
Pharmaceutically incompatible
with solutions of other antibiotics in the same syringe, administered separately.
Side effect
From the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal pain, dysbiosis,
pseudomembranous enterocolitis, hepatitis, liver dysfunction.
From the nervous
system: headache, dizziness,
convulsions, reversible encephalopathy, fatigue, weakness.
From the urinary
system: impaired renal function,
oliguria, interstitial nephritis.
On the part of biochemical parameters: an increase in the level of
hepatic transaminases, lactate dehydrogenase, alkaline phosphatase and
bilirubin, the concentration of urea nitrogen and creatinine.
From the
peripheral blood: hemolytic anemia,
leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis,
hypocoagulation.
Local reactions: phlebitis, soreness along the vein, soreness and infiltration at the
site of intramuscular injection.
Others: superinfection (vaginal and oral candidiasis). When treating infections
caused by spirochetes, complications such as Herxheimer's reaction can occur.
This can lead to fever, chills, headache, and joint pain.
If any of the side effects indicated in the instructions are
aggravated, or you notice any other side effects not listed in the
instructions, inform your doctor.
Symptoms: convulsions,
encephalopathy (if administered in high doses, especially in patients with
renal failure), tremor, neuromuscular irritability.
Treatment: symptomatic
therapy, there is no specific antidote.
Store in a dry and
dark place, at a temperature not exceeding 25°C.
Keep out of the reach
of children!
2 years. Do not use
after the expiration date printed on the package.
Vacation conditions
Dispensed by prescription.
Release form
1 bottle of powder
and 1 ampoule of 4 ml lidocaine solution with instructions for medical use in a
cardboard box.