PENBRITIN 250 (capsules); PENBRITIN 500 (capsules); PENBRITIN S (syrup); PENBRITIN SF (syrup forte); PENBRITIN 250 I (injection); PENBRITIN 500 I (injection); PENBRITIN 1000 I (injection)

INDICATIONS CONTRA-INDICATIONS DOSAGE SIDE-EFFECTS PREGNANCY OVERDOSE IDENTIFICATION PATIENT INFORMATION

PENBRITIN 250 (capsules)
PENBRITIN 500 (capsules)
PENBRITIN S (syrup)
PENBRITIN SF (syrup forte)
PENBRITIN 250 I (injection)
PENBRITIN 500 I (injection)
PENBRITIN 1000 I (injection)

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

PENBRITIN 250 (capsules)
PENBRITIN 500 (capsules)
PENBRITIN S (syrup)
PENBRITIN SF (syrup forte)
PENBRITIN 250 I (injection)
PENBRITIN 500 I (injection)
PENBRITIN 1000 I (injection)

COMPOSITION:

Penbritin 250	–	Capsules each containing ampicillin trihydrate B.P. equivalent to 250 mg ampicillin.
Penbritin 500	–	Capsules each containing ampicillin trihydrate B.P. equivalent to 500 mg ampicillin.
Penbritin S	–	Syrup containing ampicillin trihydrate B P. equivalent to 125 mg ampicillin in each 5 mL of reconstituted syrup. Contains sodium benzoate 0,1272% m/m as a preservative.
Penbritin SF	–	Syrup containing ampicillin trihydrate B P, equivalent to 250 mg ampicillin in each 5 mL of reconstituted syrup. Contains sodium benzoate 0,1272% m/m as a preservative.
Penbritin 250 I	–	Vials each containing ampicillin sodium B.P. equivalent to 250 mg ampicillin.
Penbritin 500 I	–	Vials each containing ampicillin sodium B.P. equivalent to 500 mg ampicillin.
Penbritin 1000 I	–	Vials each containing ampicillin sodium B.P. equivalent to 1 g ampicillin.

PHARMACOLOGICAL CLASSIFICATION:
A.20.1.2 Penicillins.

PHARMACOLOGICAL ACTION
Penbritin is a semi-synthetic penicillin derived from the nucleus 6-amino-penicillanic acid.
Penbritin is bactericidal at low concentration against a wide range of both Gram-positive and Gram-negative bacteria.

Chemistry:
Ampicillin is 6-(D(-) alpha-aminophenylacetamido) -penicillanic acid. The sodium salt of ampicillin is used in the preparation of the parenteral dosage forms, while ampicillin trihydrate is used in the preparation of the oral dosage forms.

Bacteriology:
Penbritin is a broad spectrum bactericidal antibiotic.
Gram-positive bacteria
Penbritin is active against non-penicillinase producing staphylococci, haemolytic and non-haemolytic streptococci, Diplococcus pneumoniae, Clostridia spp. and Streptococcus faecalis.
Gram-negative bacteria
Penbritin is active against all the common Gram-negative organisms including the Gram-negative cocci (Neisseria spp.), H. influenzae, Proteus mirabilis and many strains of Brucellae, Salmonellae, Shigellae and E. coli.

Absorption and excretion:
Penbritin is acid-stable and well-absorbed from the gastrointestinal tract. Penbritin should be taken ½ - 1 hour before meals.
The administration of double or higher doses results in a directly proportionate increase in serum concentration.
When the meninges are inflamed the C.S.F. level is approximately 20% of the simultaneous serum level.
The biliary, concentration is approximately 3 - 48 times the serum level. 30% of an oral dose is excreted into the urine within six hours. In patients with severely impaired renal function urinary Penbritin levels fall but therapeutically significant urine levels are still maintained.

Probenecid:
For patients with normal renal function higher Penbritin serum levels may be achieved by the simultaneous use of a renal blocking agent such as probenecid. In adults a dose of 0,5 g four times daily results in a 1½ to 2 fold increase in Penbritin serum levels.

INDICATIONS
Respiratory tract and other systemic infections.
Bronchitis.
Urinary tract infections.
Gonorrhoea.
Gastro-intestinal infections.
Enteric fever.
Severe infections.
Meningitis (children). N.B. Meningitis should be treated with parenteral, preferably I.V. ampicillin.

CONTRA-INDICATIONS
Allergy to penicillins is an absolute contra-indication to the use of Penbritin.

DOSAGE AND DIRECTIONS FOR USE
Adults:

INDICATION		DOSAGE	ROUTE	DURATION OF TREATMENT
RESPIRATORY TRACT AND OTHER SYSTEMIC INFECTIONS	Moderate	250-500 mg 6 hourly	Oral	5-10 days
	Severe	500 mg 6 hourly	I.M.	5-10 days
BRONCHITIS	Normal Therapy	250 mg 6 hourly	Oral	7 days or more
	High Dosage	1 g 6 hourly	Oral	7-14 days
		500 mg 6 hourly	I.M.	7-14 days
URINARY TRACT INFECTIONS	Lower	500 mg 8 hourly	Oral	7-10 days
	Upper	500 mg - l g 8 hourly	Oral	10 days or more
		500 mg 6 hourly	I.M.	10 days or more
GONORRHOEA		3,5g + 1 g Probenecid	Oral	As a single dose
ENTERIC FEVER	Acute	1-2g 6 hourly	Oral	14-21 days
	Carriers	1-2g 6 hourly	Oral	4-12 weeks
SEVERE INFECTIONS	Septicaemia, Peritonitis, Bacterial- endocarditis, Osteomyelitis	500 mg* 4-6 times daily	I.M. or I.V.	1-6 weeks
MENINGITIS (Children)		150-300 mg/kg/day	I.V.	First 48 hours
		100 mg/kg/day	I.M.	2 weeks
GASTRO-INTESTINAL INFECTIONS		500-750 mg 6 -8 hourly	Oral	7 days

* Much higher doses (up to 12 g daily in adults) may be safely given.
In severe infections doses may be safely increased or given by injection.

Paediatric:
Oral
Dosage based on age:

0 - 2 years:	62,5 mg 6 hourly
2 - 5 years:	125 mg 6 hourly
5 - 10 years:	125-250 mg 6 hourly

Dosage based on body weight:

Up to 5 kg:	200 mg daily in four divided doses.
5 - 25 kg:	25-50 mg/kg daily in four divided doses.
Over 25 kg:	adult dose.

Parenteral:
Intramuscular Dosage based on body weight.

Directions for use:
Injectable Shake the vial immediately after adding the sterile diluent. Always use freshly prepared solutions.

Intramuscular:
250 mg, 500 mg, 1 g - add, 1,5 - 2 mL Water for Injections BP.

Intravenous:
Dissolve the contents of a vial in the specified volume of Water for Injections BP.

250 mg:	5,0 mL,
500 mg:	10,0 mL,
l g:	20,0 mL.

Administer by slow injection over a period of three to four minutes.
Alternatively, if fluids are being given by intravenous infusion, the solution may be injected slowly into the drip tubing.

Intravenous infusion:
Penbritin is compatible with the commonly used intravenous infusion fluids. Solutions should be used within four to eight hours. See notes on stability.

Intraperitoneal:

Dialysis:	50 mg per litre of dialysate.
Therapeutic:	Dissolve 500 mg in 10 mL Water for Injections BP.

Intrapleural:
Dissolve 500 mg in 5 - 10 mL Water for Injections BP.

Intra-articular:
50 - 100 mg/mL of Water for Injections BP. or 0,5% lignocaine hydrochloride BP. to make up to volume of 2,5 mL.

Sub-conjunctival:
Dissolve 100 mg in 0,5 mL Water for Injections BP.

Stability and compatibility:
Injectable solution. Only freshly prepared solutions should be used.
Intravenous infusions. Penbritin is compatible with the commonly used intravenous fluids. The periods of stability at room temperature are shown in table 1

Table 1: Period of stability of Penbritin intravenous infusion solutions at room temperature.

N. saline	24 hours
5% Dextrose	3 hours
Dextrose saline	3 hours
M/6 Sodium lactate	6 hours
Ringer’s solution	24 hours
1,4% Sodium bicarbonate	4 hours

Penbritin should not be added to infusion bottles containing Dextran 40 Injection B P but may be injected into the drip tubing of such an infusion.

Blood and plasma: A dilute solution (i.e. 500 mg dissolved in 20 mL Water for Injections BP) should be injected slowly into the drip tubing rather than added to the infusion bottle.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Allergic reactions may occur, presenting as a pruritic skin rash, an erythematous skin reaction or urticaria. In this event, withdrawal of Penbritin and administration of an antihistamine will suffice in most cases. Should a serious anaphylactic reaction occur, Penbritin should be discontinued and the patient treated with the usual agents: (adrenaline, corticosteroids and antihistamines.)
Treatment with Penbritin may give rise to a maculopapular rash during therapy or within a few days after completion thereof.
The incidence of maculopapular rash is especially high in patients suffering from infectious mononucleosis.
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 therapy.

IDENTIFICATION:

Penbritin 250	–	Black and red gelatine capsules with “Penbritin 250”imprinted in white.
Penbritin 500	–	Black and red gelatine capsules with “Penbritin 500”imprinted in white.
Penbritin S	–	Bottles containing powder for the preparation of 100 mL fruit-flavoured syrup.
Penbritin SF	–	Bottles containing powder for the preparation of 100 mL fruit-flavoured syrup.
Penbritin 250 I	–	White powder. Clear solution.
Penbritin 500 I	–	White powder. Clear solution.
Penbritin 1000 I	–	White powder. Clear solution.

PRESENTATION:

Penbritin 250	–	(Black-Red) capsules printed with “Penbritin 250” in canisters of 20, 100 and 500.
Penbritin 500	–	(Black-Red) capsules printed with “Penbritin 500”in canisters of 20, 100 and 500.
Penbritin S	–	Fruit flavoured syrup containing ampicillin trihydrate B.P. equivalent to 125 mg ampicillin per 5 mL in 100 mL bottles.
Penbritin SF	–	Fruit flavoured syrup containing ampicillin trihydrate B.P. equivalent to 250 mg ampicillin per 5 mL in 100 mL bottles.
Penbritin 250 I	–	Ampicillin sodium B.P. equivalent to 250 mg ampicillin per vial.
Penbritin 500 I	–	Ampicillin sodium B.P. equivalent to 500 mg ampicillin per vial.
Penbritin 1000 I	–	Ampicillin sodium B.P. equivalent to 1 g ampicillin per vial.

STORAGE INSTRUCTIONS:
Penbritin presentations should be stored in a cool (below 25°C), dry place.
Keep out of reach of children.

REGISTRATION NUMBERS:

Penbritin 250	:	A.594 (Act 101/1965)
Penbritin 500	:	A.600 (Act 101/1965)
Penbritin S	:	A.597 (Act 101/1965)
Penbritin SF	:	A.596 (Act 101/1965)
Penbritin 250 I	:	A.598 (Act 101/1965)
Penbritin 500 I	:	A.817 (Act 101/1965)
Penbritin 1000 I	:	A.818 (Act 101/1965)

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Beecham Pharmaceuticals (Pty) Ltd.
6 Carey Street, Wynberg Ext. 6, Johannesburg 2090

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
6/03/1986.

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Penbritin and the BRL logo are trademarks
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