Merkacin (Amikacin)
Pharmaceutical Form
Solution for intramuscular, intravenous injection
COMPOSITION
One ml contains
Amicacin (as sulfate) 100 mg or 500 mg
THERAPEUTIC INDICATIONS
Treatment of infectious and inflammatory severe
diseases caused by microorganisms sensitive to Mercacin and also by
microorganisms resistant to other aminoglycosides:
- Abdominal cavity infections (including
peritonitis);
- Septic endocarditis;
- Sepsis;
- Infections of CNS (including meningitis);
- Infections of upper airways (bronchitis,
pneumonia, pleural empyema, abscess of lungs);
- suppurative infections of skin and soft
tissues (including infected burns, infected ulcers and pressure sores of
different genesis);
- frequently recurrent infection of urinogenital tracts (pyelonephritis,
cystitis, urethritis, prostatitis, gonorrhea);
- infections of bile-excreting tracts;
- infections of bones and joints (including. osteomyelitis);
- wound infection and post-operative infections.
CONTRAINDICATIONS
Mercacin is contraindicated in the following
cases:
- Hypersensitization to drug ingredients, and
also to other antibiotics of aminoglycoside;
- Severe renal impairment;
- Cochlear neuritis;
- Pregnancy.
LIMITS TO ADMINISTRATION
The drug should be applied with cautious on the
following cases: myasthenia, parkinsonism, botulism (aminoglycosides may cause
disbalance of neuromuscular transmission that results in further attenuation
of skeletal muscles), dehydratation, and renal insufficiency. It is also
should be used with cautious in infants (especially in premature newborns) and
in elderly patients.
ADVERSE REACTIONS
Effects on CNS and peripheral nervous system:
headache, somnolence, disbalance of neuromuscular transmission (apnoea),
neurotoxicity (muscular twitching, sensation of numbness, tingling, epileptic
seizures).
Effects on blood formation system: anemia,
leukopenia, granulocytopenia, thrombocytopenia.
Effects on digestive system: nausea, vomiting, increase in activity of hepatic
transminases, hyperbilirubinemia.
Effects on urinary tracts system: oliguria,
proteinuria, microhematuria; rarely renal impairment.
Effects on sense organs: ototoxicity (hearing
impairment, vestibular and labyrinthine disturbances, irreversible deafness),
toxic action on vestibular apparatus (discoordination of movements, dizziness,
nausea, vomiting).
Allergic reaction: skin eruption, pruritus, skin hyperemia, fever; rarely
angioedema.
DOSAGE AND ADMINISTRATION
The dosage regime has been established
individually depending on body weight, severity and localization of infection
and pathogen sensitivity.
Doses of 5 mg/kg every 8 h or 7.5 mg/kg every
12 h for 10-12 days are prescribed in adults and adolescences IM, IV as
stream introduction for 2 minutes or as drop-by-drop introduction.
The maximum dose for adults is up to 15 mg/kg a
day, but not more than 1.5 g a day. The initial dose for infants is 10 mg/kg,
then 7.5 mg/kg every 12 h for 7-10 days.
The recommended dose for premature newborns
is 7.5 mg/kg every 12 h.
In case of infections of respiratory tracts,
bacteremia, septicemia, complicated infections of urinogenital tracts, intra-infections
and febrile granulopenia: 15 mg/kg once daily IV for adults and 20 mg/kg for
infants older 4 weeks.
In case of bacterial infections of urinary
tracts (not complicated): 250 mg every 12 h; the additional dose of 3-5 mg/kg
may be prescribed following hemodialysis.
IV injection may be as stream
introduction for 2 minutes or as drop-by-drop introduction for 30-60 minutes
(in infants 1-2 h).
The appropriate dose is diluted with 100-200 ml
of sterile solvent. Amicacin concentration in solution for IV injection should
be less than 5 mg/kg. The following solvents are recommended to use for
preparation of solutions for IV injection:
- 5% glucose solution for injection;
- 5% glucose solution and 0.2% sodium chloride
solution for injection;
- 5% glucose solution and 0.45% sodium chloride
solution for injection;
- 0.9% sodium chloride solution for injection;
- Ringer's lactated solution for injection.
Prepare solution immediately before usage.
As other aminoglycosides Mercacin should not be
injected concomitantly with other agents.
As other drug for parenteral injection
Mercacin should be inspected for particular matter or staining before usage!
The treatment duration is 3-7 days when injected
IV and is 7-10 days when injected IM.
If therapeutical effect has not been appeared in
3-5 days since the first injection administration should be discontinued and
pathogen sensitivity to amicacin should be checked once again.
It not recommended administering the drug once a
day for patients with renal impairment (creatinin clearance < 50 ml/min),
dosage regime should be adjusted in this case. The drug is generally
prescribed 2 times a day determining amicacin serum concentrations. Total dose
in compare with usual dose have been decreased by increasing in dosing
interval.
5-7.5 mg/kg every 4-6 h may be required for patients with burns due to their
shorter T1/2 (1-1.5 h).
OVERDOSAGE
Symptoms: ataxia, dizziness, micturition
disorders, loss of appetite, nausea, vomiting, ring in ears, hearing loss,
respiratory impairment.
Treatment: hemodialysis or peritoneal dialysis, anticholinesterase drugs,
calcium salts, artificial pulmonary ventilation and symptomatic therapy is
applied for reversal of blockade of neuromuscular transmission and its
aftermath.
DRUG INTERACTION
Mercacin demonstrates synergetic action with
carbenicylin, benzylpenicillin and cephalosporins (co-administration with
beta-lactams may decrease in aminoglycoside efficacy in patients with severe
chronic renal impairment).
Co-administration with cephalosporin B,
vancomycin, methoxyflurane, enflurane, NSAID, radiopaque contrast agents,
cephalotome, cyclosporine, cisplatin, polymyxins, nalidixic acid may result in
onset of nephrotoxic action.
Mercacin enhances action of neuromuscular
relaxants.
Methoxyflurane, polymyxins for parenteral introduction, capreomycin and other
agents blocking neuromuscular transmission (halogenated anesthetics, opioid
analgesics), citrated hemotransfusion increases the risk of respiratory
standstill (especially during intraperitoneal introduction of Mercacin).
Parenteral introduction of indometacin increases the risk of toxic action of
aminoglycosides (increases in T1/2 and decreases in clearance).
Amicacin reduces efficacy of drugs for treatment
of myasthenia.
Pharmaceutical incompatibility
Mercacin in a solution is incompatible with
penicillins, heparin, cephalosporins, capreomycin, amphotericin B,
hydrochlorothiazide, erythromycin, nitrofurantoin, and thiopentone; and also
with vitamins of group B and C, tetracycline and potassium chloride depending
on concentration and composition of solution.
WARNINGS
Patients receiving Mercacin are to be monitored
taking into consideration potential ototoxicity and nephrotoxicity of
aminoglycosides.
It is not recommended administering the drug
over 14 days, since the safety of its application over this period has not
been established.
In case of onset of ototoxicity (tinnitus,
dizziness, hearing impairment) or nephrotoxicity the dug should be
discontinued or dosage adjustment should be done.
It is not recommended concomitant or sequential
administering with other aminoglycosides and also with other neurotoxic and
nephrotoxic agents.
Elderly age and state of dehydration are also
the risk factors of toxic effects.
Aminoglycosides should be applied with cautious
in patients with muscular disturbances such as myastenia gravis or
parkinsonism since this group of antibiotics may have enhance muscular
weakness due to potential neuromuscular relaxant effect on neuromuscular
transmission.
Mercacin administration may be associated with
colonization of non-sensitive microorganisms as with other antibiotics that
requires prescription of appropriate treatment.
It is recommended to determine amicacin serum
concentrations to prevent exceeding of amicacin limit during treatment.
Amicacin plasma concentration should be less 25 mcg/ml (therapeutical
concentration is 15-25 mcg/ml).
It is necessary to control the function of
acoustic nerve and vestibular apparatus not less than once a week during
treatment.
The risk of ototoxicity and nephrotoxicity has
been increased in patients with renal impairment, when applied high doses and
in prolong administration. It is recommended to monitor renal function (creatinin
serum concentrations and creatinin clearance).
Decrease the dosage or withdraw the drug in case
of unsatisfactory results of audimetry.
It is recommended to take more liquid for
patients with infectious and inflammatory diseases of urinary tracts.
Sodium bisulfite which is a part of the drug may
cause the development of allergic reactions (even anaphylactic) especially in
patients with allergic anamnesis.
PREGNANCY AND LACTATION
Mercacin may be applied during pregnancy and
lactation only if there are vital indications. Amicacin has penetrated through
the placenta and may have influence on fetus; therefore a patient should be
informed of potential risk to fetus.
Breast-feeding should be ceased if it is
necessary to use Mercacin during lactation.
USE IN PEDIATRICS
As all aminoglycosides, Mercacin should be
applied with cautious in infants and premature newborns since their urinary
tracts system has not been completely matured.
DOSAGE FORM
Solution for IM and IV injection is supplied in
a vial at a dosage of 100 mg/2 ml or 250 mg/2 ml or 500 mg/2 ml.
One vial is in a carton box with a leaflet.
SALES TERMS:
Sold under prescription.
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