ULTRAMOX Capsule Ref.[50559] Active ingredients: Amoxicillin

Source: Marketing Authorisation Holder  Publisher: Oethmaan Biosims (PTY) Ltd., 207A Sherwood House, Greenacres Office Park, c/o Victory and Rustenburg Roads, Victory Park, Johannesburg 2195

5.1. Pharmacodynamic properties

Pharmacological classification: A 20.1.2 Penidllins.

Pharmacological action

(a) Bacteriology

(i) Spectrum

Amoxycillin is a penicillinase-susceptible penicillin and is, therefore, contra-indicated in infections caused by penicillinase-producing organisms. ULTRAMOX exhibits in vitro, and in experimental animals in vivo, bactericidal activity against a wide range of Gram-negative and Gram-positive organisms including:

Gram-positive bacteria: Gram-negative bacteria:
Staphylococcus aureus (penicillin-sensitive) Neisseria gonorrhoeae
Streptococcus pyogenesNeisseria meningitidis
Streptococcus viridansHaemophilus influences
Streptococcus faecalisBordetella pertussis
Diplococcus pneumoniaeEscherichia coli
Corynebacterium speciesSalmonella typhi
Clostridium speciesSalmonella species
Bacillus anthracisShigella species
 Brucella suedes
 Proteus mirabilis

(ii) Bactericidal

In Vitro: ULTRAMOX exerts a more rapid bactericidal action than other beta-lactam antibiotics against susceptible Escherichia coli. At similar inhibitory concentrations, ULTRAMOX results in a greater degree of bacterial cell lysis than other beta-lactam antibiotics against susceptible E. coll.

In Vivo: ULTRAMOX has been shown to exert greater therapeutic activity than ampicillin at similar blood levels in certain experimental infections.

(b) Absorption

ULTRAMOX is extremely well absorbed orally. mAfter oral administration, there is no significant difference between the peak serum levels in fasting and non-fasting subjects. The presence of food does not interfere with the absorption of ULTRAMOX. ULTRAMOX may, therefore, be taken with meals. There is a linear/dose response in peak serum levels after oral administration.

(c) Distribution

i) Sputum: The concentration of amoxycillin in sputum does not decrease as occurs with ampicill in as purulence subsides.

ii) Bile: ULTRAMOX is present in bile obtained from a common bile duct drain of a healthy gall-bladder, however binary levels are lower when the gall-bladder is diseased and absent in the presence of binary tract obstruction.

iii) Urine: The average concentration of ULTRAMOX in urine collected during the first six hours after a 250 mg oral dose, is 580 pg/ml

iv) CSF: There is insufficient evidence at present to show that ULTRAMOX penetrates into the cerebra-spinal fluid in therapeutic quantities and it should, therefore, not be used in the treahnent of cerebra-spinal infections.

(d) Excretion

i) Renal: Approximately 60% of an oral dose of ULTRAMOX is excreted unchanged in the active form into the urine within six hours.

ii) Biliary: Avariable percentage of ULTRAMOX is excreted into the bile.

(e) Probenecid

Even higher ULTRAMOX serum levels may be achieved after oral administration to patients with normal renal function, by the simultaneous administration of a renal blocking agent such as probenecid. Probenecid should not be given in the presence of abnormal renal function.

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