ROKINOL [Chloramphenicol] 1 g Powder for preparing a solution for I.M. / I.V. injection
ROKINOL
instructions for the medical use of the medicinal
product
Tradename
Rokinol, Рокинол
International
non-proprietary name or generic name
Chloramphenicol, Хлорамфеникол
Composition
Each bottle contains:
Active substance: chloramphenicol (as chloramphenicol sodium succinate) 1 g.
Dosage form
Powder for preparation of
solution for injection.
Antibiotic.
Pharmacodynamics
A bacteriostatic antibiotic with a broad spectrum of
action, disrupts the process of protein synthesis in a microbial cell at the
stage of transfer of t-RNA amino acids to ribosomes. Effective against strains
of bacteria resistant to penicillins, tetracyclines, sulfonamides.
Active against gram-positive and gram-negative
bacteria: Escherichia coli, Shigella boydii, Shigella dysenteriae, Shigella
flexneri, Shigella sonnei, Salmonella spp. (including Salmonella typhi,
Salmonella paratyphi), Staphylococcus spp., Streptococcus spp. (including
Streptococcus pneumoniae), Neisseria meningitidis Neisseria gonorrhoeae, a
number of strains Proteus spp., Burkholderia pseudomallei, Rickettsia spp.,
Treponema spp., Leptospira spp., Chlamydia spp. (including Chlamydia
trachomatis), Coxiella burnetii, Ehrlichia canis, Bacteroides fragilis,
Klebsiella pneumoniae, Haemophilus influenzae.
Does not affect acid-fast bacteria (including
Mycobacterium tuberculosis), anaerobes, methicillin-resistant strains of
staphylococci, Acinetobacter spp., Enterobacter spp., Serratia marcescens,
indole-positive strains Proteus spp. Pseudomonas aeruginosa spp .; protozoa and
mushrooms.
Resistance of microorganisms develops slowly.
Pharmacokinetics
Absorption
- 90% (fast and almost complete). Bioavailability - 70% after i / m
administration. Communication with plasma proteins - 50-60%, in premature
infants - 32%.
Tmax
after intravenous administration - 1-1.5 hours. Vd - 0.6-1 l / kg.
It
penetrates well into body fluids and tissues. Its highest concentrations are
found in the liver and kidneys. Up to 30% of the administered dose is found in
bile. Cmax in the cerebrospinal fluid is determined 4–5 hours after a single
oral administration and can reach, in the absence of meninges inflammation,
21–50% of the Cmax in plasma and 45–89% in the presence of meninges
inflammation. Passes through the placental barrier, the concentration in the
serum of the fetus can be 30-80% of that in the mother's blood. Penetrates into
breast milk.
The
main amount (90%) is metabolized in the liver. In the intestine, under the
influence of intestinal bacteria, it is hydrolyzed to form inactive
metabolites.
It
is excreted within 24 hours by the kidneys - 90% (by glomerular filtration -
5-10% unchanged, by tubular secretion in the form of inactive metabolites -
80%), through the intestines - 1-3%. T1 / 2 of the drug from blood plasma in
adults - 1.5-3.5 hours, with impaired renal function - 3-11 hours.
T1
/ 2 in children from 1 month to 16 years - 3-6.5 hours, in newborns from 1 to 2
days - 24 hours or more (it especially varies in children with low birth
weight), 10-16 days - 10 h.
Poorly
excreted during hemodialysis.
Infectious and
inflammatory diseases caused by sensitive microorganisms, incl. brain abscess,
typhoid fever, paratyphoid fever, salmonellosis (mainly generalized forms),
dysentery, brucellosis, tularemia, Q fever, meningococcal infection,
rickettsioses (including typhus, trachoma, Rocky Mountain spotted fever),
inguinal and lymphogranuloses , ehrlichiosis, urinary tract infections,
purulent wound infection, purulent peritonitis, biliary tract infections.
Hypersensitivity to
chloramphenicol and other amphenicol, inhibition of hematopoiesis, blood
diseases, acute intermittent porphyria; skin diseases (psoriasis, eczema,
fungal infections); hepatic and / or renal failure; deficiency of
glucose-6-phosphate dehydrogenase; pregnancy and the period of breastfeeding.
Method of administration and dosage
I / V or I / M.
The daily dose depends on the age and weight of the
patient and the type and severity of the infection.
Adults — 1 g per injection 2-3 times a day. In severe
forms of infections (including typhoid fever, peritonitis) in a hospital, it is
possible to increase the dose to 3-4 g / day.
The maximum daily dose is 4 g.
Children - under the control of the concentration of
the drug in serum depending on age: infants and older - 12.5 mg / kg (base)
every 6 hours or 25 mg / kg (base) every 12 hours, in severe infections
(bacteremia, meningitis) - up to 75-100 mg / kg (base) / day.
Solutions are prepared just before injection.
For intravenous administration, the contents of a 1 g
bottle are in 5 ml of 5 or 40% glucose solution or water for injection.
Patients suffering from diabetes, the drug is administered in a solution of
sodium chloride 0.9%. Injected intravenously slowly over 3-5 minutes.
When administered intramuscularly, the volume of the
solvent is usually 2-3 ml per 1 g of the antibiotic. As a solvent for the drug
used in / m, 0.25–0.5% solutions of novocaine can be used. Injected deeply
intramuscularly.
The average duration of treatment is 8-10 days.
Special instructions and precautions
Chloramphenicol
is not used in newborns, because development of "gray syndrome" is
possible (flatulence, nausea, hypothermia, gray-blue skin color, progressive
cyanosis, dyspnea, cardiovascular failure).
Use with
caution in patients who have previously received treatment with cytostatic
drugs or radiation therapy.
With the
simultaneous intake of alcohol, a disulfiram-like reaction may develop
(hyperemia of the skin, tachycardia, nausea, vomiting, reflex cough,
convulsions).
In the
course of treatment, systematic monitoring of the peripheral blood picture is
necessary.
It is
unacceptable for the uncontrolled prescription of chloramphenicol and its use
for mild forms of infectious processes, especially in pediatric practice.
Use with
caution in elderly patients in order to avoid exacerbation of chronic diseases.
Before
the introduction, it is necessary to conduct a test for the tolerability of the
drug, provided there are no contraindications to conduct.
Influence on the ability to drive
vehicles and mechanisms
It should be used with caution by persons driving
vehicles or working with other mechanisms, due to the risk of developing
possible adverse reactions from the nervous system.
Application during pregnancy and during breastfeeding
Contraindicated for use during pregnancy
and during breastfeeding.
Interaction with other medicinal products
Suppresses the enzyme system of cytochrome P450,
therefore, with simultaneous use with phenobarbital, phenytoin, indirect
anticoagulants, a weakening of the metabolism of these drugs is noted, a
slowdown in excretion and an increase in their concentration in plasma.
Reduces the antibacterial effect of penicillins and
cephalosporins.
With simultaneous use with erythromycin, clindamycin,
lincomycin, a mutual weakening of the action is noted due to the fact that
chloramphenicol can displace these drugs from the bound state or prevent them
from binding with the 50S subunit of bacterial ribosomes.
Simultaneous administration with drugs that inhibit
hematopoiesis (sulfonamides, cytostatics), affecting the metabolism in the
liver, with radiation therapy increases the risk of side effects.
When administered with oral hypoglycemic drugs, an
increase in their action is noted (due to the suppression of metabolism in the
liver and an increase in their concentration in plasma).
Myelotoxic drugs increase the manifestations of
hematotoxicity.
The simultaneous long-term use of chloramphenicol with
oral contraceptives containing estrogen - can lead to a decrease in the
reliability of contraception and an increase in the frequency of sudden
bleeding.
Side effect
From the digestive system: nausea, vomiting, diarrhea,
dysbiosis, glossitis, stomatitis.
From the nervous system: psychomotor disorders, depression, confusion,
peripheral neuritis, optic neuritis, visual and auditory hallucinations,
decreased visual acuity and hearing, headache.
From the side of hematopoietic organs: reticulocytopenia,
leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia, aplastic
anemia, agranulocytosis.
Allergic reactions: skin rash, angioedema.
Others: secondary fungal infection, collapse (in children under 1 year of age).
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: Possible
increased side effects.
Treatment: hemosorption,
symptomatic therapy.
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.
Dispensed by
prescription.
Release form
1 bottle with instructions for use in a cardboard box.