Description and composition of Lupika injection
Lupika injection is an aminoglycoside antibiotic used for the treatment of susceptible bacterial infections. It contains Amikacin as its active ingredient. It also contains inactive ingredients called excipients in sufficient quantities.
It has broad spectrum of activity against both gram positive and gram negative bacteria.
Pharmacology of Lupika injection
Lupika injection is a semi-synthetic aminoglycoside antibiotic active against a broad spectrum of gram-negative organisms, including pseudomonas and some gram-positive
Organisms (especially Staphylococcus aureus). It elicits its pharmacological effect by irreversibly binding to the 30S ribosomal subunit of the bacterial cell thereby inhibiting the protein synthesis.
Though bacteriostatic, it exhibits a dose-dependent bactericidal effect. It also possesses a post-antibiotic effect which continues to suppress susceptible bacteria after serum levels of the drug have fallen.
Amikacin, like other aminoglycosides are positively charged, therefore, they are not absorbed when given orally.
Absorption is rapid following intramuscular administration attaining peak plasma levels in about an hour. The tmax following IV dosing is about 30 minutes.
Amikacin is found in body tissues and fluids. It crosses the placenta but does not readily penetrate the CSF. It substantially penetrates the blood-brain barrier in cases of meningitis.
It has a volume of distribution of 0.25 L/ kg and a plasma protein binding of 11%. Excretion is principally via urine (94-98 %) and the plasma half-life is 2-3 hours
Uses of Lupika injection
Lupika injection is used for short-term treatment of serious infections caused by susceptible gram-negative organisms such as Pseudomonas, Proteus, Serratia, Enterobacter, Klebsiella and Acinetobacter species and Escherichia coli;
It is also used for the treatment of infections caused by susceptible Staphylococcus species especially in patients allergic to other antibiotics or in cases of mixed staphylococcal/ Gram-negative infections.
Dosage of Lupika injection
Adult dosage
Adult and Child >12 years old with normal renal function (CrCl 250 mL/min)
Infections due to susceptible organisms, by IM or slow IV injection (2-3 minutes) or IV infusion (30-60 minutes), 15 mg/kg daily in one or two divided doses for 7-10 days; not exceeding max. 1.5 g/day
Urinary tract infections (other than pseudomonas infections), 7.5 mg/kg/day in two equally divided doses (equiv. to 250 mg twice daily in adults). May administer with a urinary alkalinising agent to enhance the activity of amikacin
Elderly: Dosages should be adjusted based on renal function status
Child dosage
Infections due to susceptible organisms
Child 4 weeks to 12 years old with normal renal function By IM or slow IV infusion, 15-20 mg/kg daily in one or two divided doses
Neonate with normal renal function By IM injection or IV infusion (1-2 hours), 10 mg/kg as an initial loading dose, followed by 7.5 mg/kg 12 hourly; not exceeding total daily dose of 15 mg/kg.
Dosage in renal impairment
Modify dosages by giving amikacin at prolonged intervals or by giving reduced doses at fixed intervals based on serum creatinine or creatinine clearance values.
NOTE:
Patients should be well hydrated during amikacin therapy.
Safety for treatment periods which are longer than 14 days has not been established
Renal, auditory, and vestibular functions should be monitored, as well as serum amikacin levels especially during prolonged therapy.
Stop and reevaluate therapy if there is no definite clinical response within 3 to 5 days.
Side effects of Lupika injection
Neurotoxicity with clinical features such as vestibular and permanent bilateral auditory ototoxicity, skin rash, drug fever, headache, paraesthesia, tremor, nausea and vomiting, eosinophilia, arthralgia, anaemia, hypotension and hypomagnesaemia.
Blindness and retinal infarction following intravitreous administration; Potentially fatal effects include nephrotoxicity, neuromuscular blockade and respiratory paralysis.
Clostridium difficile-induced colitis.
Contraindications
Hypersensitivity to amikacin or other aminoglycosides or other ingredients in the formulation
Myasthenia gravis (as aminoglycosides may impair neuromuscular transmission)
Concurrent use with other neurotoxic, ototoxic or nephrotoxic drugs.
Precautions to take while on Lupika injection
Patients with pre-existing hearing loss or vestibular damage (increased risk of ototoxicity; monitor closely)
Disorders affecting muscular function e.g. parkinsonism (aminoglycosides may aggravate muscle weakness due to their potential curare-like effect on the neuromuscular junction)
Renal impairment (increased risk of nephrotoxicity & ototoxicity; monitor closely)
As with other antibiotics, the use of amikacin may result in overgrowth of non-susceptible organisms Premature infants and neonates (due to their immature renal function) Pregnancy and lactation
Drugs interactions with Lupika injection
Neurotoxic, ototoxic or nephrotoxic agents such as bacitracin, cisplatin, amphotericin B, ciclosporin, tacrolimus, cefaloridine, paromomycin, viomycin, polymyxin B, colistin, vancomycin, and other aminoglycosides (Additive toxicity following concurrent use contraindicated).
High-ceiling diuretics such as frusemide and ethacrynic acid (Enhanced ototoxicity of amikacin. Concurrent use contraindicated).
Cefalosporins (Increased serum creatinine levels and risk of nephrotoxicity).
Indomethacin (Potential to increase plasma concentration of amikacin in neonates); Bisphosphonates (Increased risk of hypocalcaemia following concurrent use).
Anaesthetic or muscle relaxants such as ether, halothane, tubocurarine, suxamethonium, decamethonium, atracurium, rocuronium and vecuronium (Increased risk of neuromuscular blockade and consequently respiratory depression.
Alternative classes of antibiotics should be used during anaesthesia but if aminoglycosides must be used, close monitoring is advised and appropriate facilities for mechanical respiratory assistance made available).
Recommendations on the use of Lupika injection in pregnancy and breastfeeding
Lupika injection rapidly crosses the placenta to the fetal circulation. However, no report of congenital abnormalities has been linked amikacin use in pregnancy.
There is a risk of auditory or vestibular nerve damage if used during 2nd and 3rd trimesters of pregnancy and so should be avoided unless essential.
Monitoring of serum level is essential when used during pregnancy.
Amikacin is excreted into breast milk in low concentrations. It is considered compatible with pregnancy.
Administration of Lupika injection
For intramuscular or intravenous injection.
Dosage is identical for both routes of administration. For single use in one patient only. Discard any unused portion. Obtains patient’s pre-treatment bodyweight for the calculation of correct dosage.
To be administered separately according to the recommended dose and route; not to be premixed with other drugs
Patient’s renal function should be monitored before and during treatment
For most infections the intramuscular route is preferred, but in life-threatening infections, or in patients in whom intramuscular injection is not feasible, the intravenous route, either slow bolus (2 to 3 minutes) or infusion (0.25% over 30 minutes) may be used.
Compartible diluents for intravenous use are: Normal saline or 5% Dextrose in Water for Injection.
Following dilution, the solution must be used as soon as possible and not stored.
Nursing action
IV infusion: For adults, add 500 mg amikacin to 100-200 mL of IV fluid e.g. 0.9% Sodium chloride or 5% Dextrose water.
For paediatrics, the volume of diluent to be used varies depending on the recommended dosage of amikacin – Amikacin injection is for single use only. Discard any unused portion
Amikacin solution may darken from colourless to pale yellow, but this does not indicate loss of potency
Amikacin shows incompatibility with some drugs including penicillins, cephalosporins, amphotericin, chlorothiazide sodium, nitrofurantoin sodium, thiopentone sodium, warfarin sodium and depending on the composition of the excipients, tetracyclines and vitamins.
They should not be physically mixed in the same syringes or infusion bottles prior to administration.