Nemeclox Ampicillin and Cloxacillin Capsules and Powder

NEMECLOX
PHARMACOLOGICAL FORM

NEMECLOX CAPSULES: PURPLE AND BLACK CAPSULES PRESENTED IN TROPICANIZED BLISTERS.

NEMECLOX POWDER FOR ORAL SUSPENSION PRESENTED AS DRY POWDER IN 100ML BOTTLES.

 

QUALITATIVE AND QUANTITATIVE COMPOSITION

Nemeclox capsules 500mg contains 250mg Ampicillin and 250mg cloxacillin per capsule.

Nemeclox powder for oral suspension 250mg/5mI contains 125mg ampicIllin and 125mg cloxacillin.

 

DESCRIPTION

Both ampicillin and cloxacillin is semisynthetic antibiotic substances derived from the basis penicillin nucleus, 6-aminopenicillenic acid. Chemically ampicillin Is (25.5R,6R) 6—((12R)-2-amino, 2-phenylacelylamine), 3-3dimethyl-7-oxo-4-thia-1-azabicyclo (3.2.0) heptane-2-carboxylic acid.

The molecular formular is C10N12O5S and the molecular weight is 349.41 g/mol.
Chemically cloxacillin is (2S,5R,6R)-6({3-(2-chlorophenyl) 5-methyl-oxazole-4-carbonyl}amino)-3.3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0) heptane-2-carboxykic acid. The molecular formular is C10H12CIN2O2S and the molecular weight is 435.88g/mol.

 

PHARMACOLOGICAL CLASSIFICATION

B-lactam antibiotics.

 

PHARMACOLOGICAL ACTION

Pharmacokinetics

Absorption: Both ampiclllin and cloxacillin are gastric acid stable and is well absorbed from the gastrointestinal tract.

Distribution: They are giving peak serum levels (Tmax) about 2 hours after dosing.
As there is a linear dose/response in peak serum level after oral administration of both components, doubling the dose virtually doubles the peak serum levels.

Elimination: Both components are excreted primarily by the kidneys by glomerular filtration and tubular secretion.

Bile: Bile concentrations of both ampicillin and cloxacillin vary from 3-48 times the serum concentration, according to the condition of the biliary tract.

Pharmacodynamic
Both ampicillin and cloxaclilin act by inhibiting the formation of peptidoglycan cross-links in the bacterial cell wall. The β-lactam molety (functional group) of ampicillin binds to the enzyme, known as transpeptidasses that links the peptidoglycan molecules in bacteria, which weakens the cell wall of the bacterium results into cytolysis or death due to osmotic pressure. In addition, the build-up of peptidoglycan precursors triggers the activation of bacterial cell wall hydrolases and autolysis, which further digest the bacteria’s existing peptidoglycan.

Ampicillin is bactericidal at low concentrations and is clinically effective not only against the gram-positive organisms usually susceptible to penicillin G but also against a variety of gram-negative organisms.

Cloxacillin is used against staphylococci that produce beta-lactamase, due to its larger R chain which does’t allow the beta-lactamases to bind.

In vitro studies have demonstrated the susceptibility of most strains of the following organisms:

Gram-Positive: strains of alpha-and beta-hemolytlc streptococci, streptococcus pneumoniae, those strains of staphylococci, which do not produce penicillnase, Clostridium sp. Baclllius anthracis, Corynebacterium xeroses, and most strains of enterococci.

Gram-Negative: Haemophilus influezae, Neisseria gonorrhoeae and N. Meninggitides, Proteus mirabilis, and many strains of salmonella (including S.typhosa), Shigella, and/Escherichia coli.

 

INDICATIONS AND USAGE

The use of this antibiotic may lead to the appearance of resistant strains of organisms and sensitivity testing should, therefore, be carried out wherever possible, to ensure the appropriateness of the therapy.

 

CONTRAINDICATION

Known allergy to penicillin or cephalosporin. Cases of cross sensitivity have been reported on babies born of hypersensitive mothers in the neonatal period.

 

DOSAGE AND ADMINISTRATION

Children 2-10 years: 250-500mg (5-10ml of 250 mg/5mI syrup) every 6 hours.

Children up to 2 years: 250 mg (5ml of 250 mg/5mI syrup) every 6 hours.

Adults: 500mg 6hourly.

 

ADVERSE REACTIONS

Allergic reactions: exfoliative dermatitis, other skin rashes, interstitial nephritis and vasculitis may occur.

Generalized sensitivity reaction: urticaria, fever, joint pains and eosinophilia can develop within a few hours to several weeks after starting treatment.

Others: A sore mouth or tongue and a black hairy tongue, increase in liver enzyme values, diarrhoea, nausea and heartburn and anaphylactic reactions.

 

DRUG INTERACTIONS

Allopurinol: Increased possibility of skin rash when Nemeclox co-administrated with allopurinol.

Oral Contraceptives: Nemeclox may decrease the efficacy of estrogen-containing oral contraceptives when co-administrated Nemeclox with oral contraceptives.

Probenecid: Higher Nemeclox serum levels can be achieved in patients with normal renal function by the concurrent administration of a renal blocking agent such as probenecid.

In adults, a dose of 500mg of probenecid q.d.s. will result in 1.5-2 fold increase in Nemeclox serum levels.

 

WARNING

When administered to a patient with penicillin allergy anaphylactic shock may occur. Adrenaline, corticosteroids and antihistamines should be used to treat anaphylaxis.

The oral dosage forms are not recommended for chronic, severe, or deep-seated infections such as subacute bacterial endocarditis, meningitis or syphilis.

 

PRECAUTIONS

Precaution should be taken when high doses are given to patients with renal impairment (because of the risk of neurotoxicity) or congestive heart failure. Renal and haematological systems should be monitored during prolonged and high dose therapy.
Precaution should be taken when treating patients with syphilis, as the Jarisch-Herxheimer reaction may occur shortly after starting treatment. This reaction, manifesting as fever, chills, headache and reactions at the site of the lesion, can be dangerous in cardiovascular syphilis or where there is a serious risk of increased local damage such as with optic atrophy.

Nemeclox contains cloxacillin sodium, therefore disturbances of blood electrolytes may follow the administration of large doses.

 

OVERDOSES

In case of overdosage, discontinue medication, treat symptomatically and institute supportive measures as required.

 

STORAGE

Store below 25°C in dry place. Protect from light.

 

SHAKE WELL BEFORE USE

Keep bottle tightly closed and out of reach children.

 

PRESENTATION

Bottle of 100ml

Capsules 500mg

 

Manufactured by

NEMEL PHARMACEUTICAL INDUSTRY LIMITED

No. 4a/4b Medical Road, Phase VI,

Trans-Ekulu, Enugu, Nigeria.

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