Bicillin L-A

New Zealand - English - Medsafe (Medicines Safety Authority)

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Active ingredient:
Benzathine benzylpenicillin tetrahydrate 442 mg/mL (1,200,000U/2.3mL)
Available from:
Pfizer New Zealand Limited
INN (International Name):
Benzathine benzylpenicillin tetrahydrate 442 mg/mL (1,200,000U/2.3mL)
Dosage:
1,200,000 U/2.3 mL
Pharmaceutical form:
Suspension for injection
Composition:
Active: Benzathine benzylpenicillin tetrahydrate 442 mg/mL (1,200,000U/2.3mL) Excipient: Carmellose sodium Lecithin Methyl hydroxybenzoate Povidone Propyl hydroxybenzoate Sodium citrate dihydrate Water for injection
Units in package:
Cartridge, glass, 2 mL
Class:
Prescription
Prescription type:
Prescription
Manufactured by:
Sandoz GmbH
Therapeutic indications:
Intramuscular benzathine benzylpenicillin is indicated in the treatment of infections due to penicillin-sensitive micro-organisms that are susceptible to the low and very prolonged serum levels common to this particular dosage form. Therapy should be guided by bacteriological studies (including sensitivity tests) and by clinical response. The following infections will usually respond to adequate dosage of intramuscular benzathine benzylpenicillin: · Streptococcal infections (Group A - without bacteraemia). Mild-to-moderate infections of the upper respiratory tract (eg., pharyngitis). · Venereal infections - Syphilis, yaws, bejel and pinta.
Product summary:
Package - Contents - Shelf Life: Syringe, glass, Pre-filled 2.3 mL in cardboard carton - 10 dose units - 48 months from date of manufacture stored at 2° to 8°C (Refrigerate, do not freeze) 2 months not refrigerated stored at or below 30°C. Do not return to refrigerated storage.
Authorization number:
TT50-3592/1
Authorization date:
1996-03-20

New Zealand Consumer Medicine Information

BICILLIN L-A

Bicillin® L-A

Benzathine benzylpenicillin tetrahydrate

Consumer Medicine Information

What is in this leaflet

This leaflet answers some common

questions about Bicillin L-A. It does

not contain all the available

information. It does not take the

place of talking to your doctor or

pharmacist.

All medicines have risks and

benefits. Your doctor has weighed

the risks of you receiving Bicillin L-

A against the benefits they expect it

will have for you.

If you have any questions about

receiving this medicine, ask your

doctor or pharmacist.

Keep this leaflet.

You may need to read it again.

What Bicillin L-A is

used for

Bicillin L-A is used to treat

infections in different parts of the

body caused by bacteria. Bicillin L-

A is also used to prevent certain

infections such as rheumatic fever.

Bicillin L-A will not work against

infections caused by viruses such as

colds or flu.

Bicillin belongs to the group of

penicillin antibiotics. It works by

killing bacteria or preventing their

growth. This particular type of

Bicillin is called Bicillin L-A

because it is long-acting. It is

supplied in a syringe for once-only

use.

Your doctor may have prescribed

Bicillin L-A for another purpose.

Ask your doctor if you have any

questions about why Bicillin L-A

has been prescribed for you.

This medicine is available only with

a doctor's prescription.

Before you are given

Bicillin L-A

When you must not be given

it:

Do not have Bicillin L-A if you

have an allergy to:

any medicine containing

benzathine benzylpenicillin

any of the ingredients listed at the

end of this leaflet

any other similar medicines such

as other penicillin antibiotics

cephalosporins. You may have an

increased chance of being allergic

to Bicillin L-A if you are allergic

to cephalosporins.

If you are not sure, check with your

pharmacist.

Some of the symptoms of an allergic

reaction may include:

shortness of breath

wheezing or difficulty breathing

swelling of the face, lips, tongue,

throat, or other parts of the body

rash, itching or hives on the skin

chills and fever, joint pain,

weakness or feeling faint.

Do not have Bicillin L-A if the

expiry date on the pack has passed

or if the packaging is torn or shows

signs of tampering.

If it is expired or damaged, Bicillin

L-A should be returned to the

pharmacist for disposal.

If you are not sure whether you

should be given this medicine, talk

to your doctor.

Before you are given it

Tell your doctor if you have

allergies to any other medicines,

foods, preservatives or dyes.

Tell your doctor if you have or

have had any of the following

medical conditions:

asthma

hives

hay fever

kidney or liver disease.

Tell your doctor if you are

pregnant or plan to become

pregnant or are breast-feeding.

Your doctor can discuss with you the

risks and benefits involved.

If you have not told your doctor

about any of the above, tell them

before you are given Bicillin L-A.

Taking other medicines

Tell your doctor if you are taking

any other medicines, including

medicines you buy without a

prescription from a pharmacy,

supermarket or health food shop.

Some medicines may interfere with

Bicillin L-A. These include:

Tetracycline antibiotics

Probenecid.

These medicines may affect how

well it works. You may need to take

different amounts of your medicine

BICILLIN L-A

or you may need to take different

medicines.

Your doctor or pharmacist has more

information on medicines to be

careful with or avoid while being

given this medicine.

How Bicillin L-A is

given

Follow all directions given to you

by your doctor or pharmacist

carefully.

They may differ from the

information contained in this leaflet.

Bicillin L-A is usually only given by

a doctor, pharmacist or nurse. It is

injected into a muscle. For adults

this is usually the buttocks. With

small children it may be the thigh. It

must not be injected near an artery or

nerve. If the injection is repeated, a

new site must be chosen.

How much to be given

Your doctor will decide what dose

and how many times you will receive

Bicillin L-A. This depends on your

infection and other factors, such as

your weight.

How long to be given it

Sometimes only a single dose of

Bicillin L-A is needed for the

treatment or prevention of certain

infections.

While you are being

given Bicillin L-A

Things you must do

Tell your doctor if the symptoms of

your infection do not improve

within a few days, or if they

become worse.

If you develop itching with swelling

or skin rash or difficulty breathing

after you have been given Bicillin

L-A, contact your doctor

immediately as these are symptoms

of an allergic reaction.

Tell your doctor or pharmacist if

you develop severe diarrhoea, even

if it occurs several weeks after you

have stopped receiving Bicillin L-

A.

Diarrhoea may mean that you have a

serious condition affecting your

bowel. You may need urgent

medical care.

Do not take any diarrhoea

medicine without first checking

with your doctor.

If you get a sore white mouth or

tongue after you have been given

Bicillin L-A, tell your doctor. Also

tell your doctor if you get vaginal

itching or discharge.

This may mean you have a fungal

infection called thrush. Sometimes

the use of Bicillin L-A allows fungi

to grow and the above symptoms to

occur. Bicillin L-A does not work

against fungi.

If you are about to be started on

any new medicine, remind your

doctor and pharmacist that you

are being given Bicillin L-A.

Tell any doctors, dentists or

pharmacists who treat you that

you have been given Bicillin L-A.

If you are going to have surgery,

tell the surgeon or anaesthetist that

you are being given this medicine.

It may affect other medicines used

during surgery.

If you become pregnant while you

are being given this medicine, tell

your doctor immediately.

If you are about to have any blood

or urine tests, tell your doctor that

you are being given this medicine.

Bicillin L-A may affect the results of

some tests, including tests measuring

glucose (sugar) in the urine.

Keep all of your doctor's

appointments so that your progress

can be checked.

Things to be careful of

Contact your doctor immediately

if:

you experience any symptoms of

an allergy

you have severe pain in the

muscle where your Bicillin L-A

injection was given.

Be careful driving or operating

machinery until you know how

Bicillin L-A affects you.

Bicillin L-A generally does not cause

any problems with your ability to

drive a car or operate machinery.

However, as with many other

medicines, Bicillin L-A may cause

dizziness, drowsiness, or tiredness in

some people.

In case of overdose

If you are given too much

(overdose)

It is unlikely that you will receive an

overdose as Bicillin L-A as it is most

likely to be given to you under the

supervision of your doctor.

Immediately telephone your doctor

or the National Poisons Centre

(telephone 0800 POISON or 0800

764 766), or go to accident and

emergency at your nearest

hospital, if you think that you or

anyone else may have been given

too much Bicillin L-A. Do this even

if there are no signs of discomfort

or poisoning.

Symptoms of an overdose may

include seizures and/or unusual

muscle movement, for example,

waves of rippling along the muscle.

You may need urgent medical

attention.

BICILLIN L-A

Side Effects

Tell your doctor or pharmacist as

soon as possible if you do not feel

well while you are being given

Bicillin L-A.

This medicine helps most people

with certain bacterial infections, but

it may have unwanted side effects in

some people.

All medicines can have side effects.

Sometimes they are serious, most of

the time they are not. You may need

medical attention if you get some of

the side effects.

If you are over 65 years of age you

may have an increased chance of

getting side effects.

Do not be alarmed by the following

list of side effects. You may not

experience any of them.

Ask your doctor or pharmacist any

questions you may have.

Tell your doctor if you notice any

of the following and they worry

you:

feeling anxious, nervous or

experience tremors

sleepiness or tiredness

nausea or vomiting

excessive or abnormal sweating

muscle or joint pain

oral thrush - white, furry, sore

tongue and mouth

vaginal thrush - sore and itchy

vagina and / or vaginal discharge.

Tell your doctor as soon as possible

if you notice any of the following:

stomach cramps

fast or irregular heartbeat

frequent infections (symptoms

such as fever, severe chills, sore

throat or mouth ulcers)

swollen glands in the neck,

armpit or groin

bleeding or bruising more easily

than normal

blood in stool

weakness of muscles

numbness, tingling or weakness

of the arms and legs

injection site reaction, which may

include pain, irritation, swelling,

redness, or bruising

impotence or persistent painful

erection of the penis which occurs

without sexual arousal

blurred vision, blindness.

The above list includes serious side

effects that may require medical

attention.

Tell your doctor immediately or go

to accident and emergency at your

nearest hospital if you notice any of

the following:

severe blisters and bleeding in the

lips, eyes, mouth, nose or genitals

itchy spots accompanied by fever

and feeling unwell

allergic reaction e.g. shortness of

breath, wheezing or difficulty

breathing, swelling of the face,

lips, tongue or other parts of the

body, rash, itching or hives on the

skin

severe agitation, confusion and

hallucinations

heart attack, symptoms may

include chest or shoulder pain,

tightness of chest, shortness of

breath

rapid, shallow breathing, cold,

clammy skin, a rapid, weak pulse,

dizziness, weakness and fainting

stroke (collapse, numbness or

weakness of the arms or legs,

headache, dizziness and

confusion, visual disturbance,

difficulty swallowing, slurred

speech and loss of speech)

seizures, fits or convulsions

severe diarrhoea, usually with

blood and mucus, stomach pain,

fever. This may occur during

treatment or several weeks after

treatment with Bicillin L-A

kidney disease, with blood in the

urine or pass little or no urine.

The above list includes very serious

side effects. You may need urgent

medical attention or hospitalisation

You may not experience any of them.

Some people may get other side

effects whilst receiving Bicillin L-A.

Do not take any diarrhoea

medicine without first checking

with your doctor.

Tell your doctor if you notice

anything else that is making you

feel unwell, even if it is not on this

list.

Ask your doctor or pharmacist if you

do not understand anything in this

list.

After being given

Bicillin L-A

Storage

Bicillin L-A is usually stored by your

doctor or pharmacist.

If you are storing Bicillin L-A, keep

it where young children cannot reach

Bicillin L-A must be kept in a

refrigerator (2-8°C). Do not keep it in

the door of the refrigerator, or the

freezer.

Bicillin L-A may be stored outside of

refrigerated storage but below 30°C,

for a single period of up to 2 months,

prior to expiry. The date the product

is placed outside of refrigerated

storage and stored below 30°C

should be written in the space

provided on the carton. After storage

outside of refrigeration, the product

cannot be returned to refrigerated

storage and should be discarded.

Disposal

Your doctor, pharmacist or nurse

should dispose of the Bicillin L-A

syringe and any leftover contents

after use. Do not handle or re-use the

syringe.

BICILLIN L-A

Further information

This is not all the information that is

available on Bicillin L-A. If you have

any more questions or are not sure

about anything, ask your doctor or

pharmacist.

Product description

What it looks like

Bicillin L-A is supplied as a prefilled

syringe containing a thick white

liquid in packs of 10 syringes.

Ingredients

Bicillin L-A 1,200,000 Units/2.3 mL

syringe contains 1,200,000 Units

equivalent to 1016.6 mg of the active

ingredient, benzathine

benzylpenicillin tetrahydrate in 2.3

It also contains the following inactive

ingredients:

sodium citrate

carmellose sodium

lecithin

povidone

methyl hydroxybenzoate

propyl hydroxybenzoate

water for injections.

Sponsor Details

Bicillin L-A is supplied in New

Zealand by:

Pfizer New Zealand Limited

P O Box 3998

Auckland 1140

New Zealand

Toll Free Number: 0800 736 363

Date of Preparation

This leaflet was revised on 27

September 2019.

® Registered Trademark

© Copyright

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NEW ZEALAND DATA SHEET

1. PRODUCT NAME

BICILLIN L-A

Benzathine Benzylpenicillin 1,200,000 Units/2.3 mL suspension for injection

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

BICILLIN L-A contains benzathine benzylpenicillin (the benzathine salt of benzylpenicillin)

in aqueous suspension

1,200,000

Units/2.3

pre-filled

syringe,

containing

Benzathine

benzylpenicillin

tetrahydrate 1016.6 mg/2.3 mL.

Excipient(s) with known effect

Methyl hydroxybenzoate

Propyl hydroxybenzoate

For the full list of excipients, see section 6.1 LIST OF EXCIPIENTS.

3. PHARMACEUTICAL FORM

Suspension for injection pre-filled syringe with needle.

BICILLIN L-A in the disposable pre-filled syringe formulation is a viscous and opaque white

suspension.

4. CLINICAL PARTICULARS

4.1 Therapeutic indications

Intramuscular benzathine benzylpenicillin is indicated in the treatment of infections due to

penicillin-sensitive micro-organisms that are susceptible to the low and very prolonged serum

levels common to this particular dosage form. Therapy should be guided by bacteriological

studies (including sensitivity tests) and by clinical response.

The following infections will usually respond to adequate dosage of intramuscular benzathine

benzylpenicillin:

Streptococcal infections (Group A - without bacteraemia). Mild-to-moderate infections of

the upper respiratory tract (e.g. pharyngitis).

Venereal infections - Syphilis, yaws, bejel and pinta.

Medical conditions in which benzathine benzylpenicillin therapy is indicated as prophylaxis:

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Rheumatic fever and/or chorea - Prophylaxis with benzathine benzylpenicillin has proven

effective in preventing recurrence of these conditions. It has also been used as follow-up

prophylactic therapy for rheumatic heart disease and acute glomerulonephritis.

4.2 Dose and method of administration

Dose

Use a concentration of 442 mg/mL when measuring part doses. The quantity of benzathine

benzylpenicillin is based on 1,200 Units/mg potency.

Streptococcal (Group A) upper respiratory infections (for example, pharyngitis)

A single injection of 1,200,000 Units for adults.

A single injection of 900,000 Units for older children.

A single injection of 300,000 to 600,000 Units for infants and for children under 27 kg.

Venereal infections

Syphilis - Primary, secondary and latent - 2,400,000 Units) (1-dose). Late (tertiary including

neurosyphilis) – 2,400,000 Units at 7-day intervals for three doses.

Congenital (with normal CSF) - under 2 years of age: 50,000 Units/kg body weight; ages 2-

12 years; adjust dosage based on adult dosage schedule.

Yaws, bejel and pinta - 1,200,000 Units (single injection).

Prophylaxis - for rheumatic fever and glomerulonephritis

The dosing recommendation for benzathine penicillin G is 1,200,000 units for patients

weighing

20 kg and 600,000 units for patients weighing <20 kg, every 4 weeks, except in

patients considered to be at high risk, for whom 3 weekly administration is recommended.

Method of Administration

Because of the high concentration of suspended material in this product, the needle may be

blocked if the injection is not made at a slow, steady rate.

Administer by DEEP, INTRAMUSCULAR INJECTION in the upper, outer quadrant of the

buttock. In infants and small children, the midlateral aspect of the thigh may be preferable.

When doses are repeated, vary the injection site.

Method of administration is the same as with conventional syringe. Remove needle cover by

grasping it securely; twist and pull. Introduce needle into patient, aspirate by pulling back

slightly on the plunger, and inject.

Discard any unused portion.

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4.3 Contraindications

BICILLIN L-A is contraindicated in patients who have had previous experience of a major

allergy or anaphylaxis to a cephalosporin or penicillin.

Hypersensitivity to any of the excipients.

4.4 Special warnings and precautions for use

Allergic Reactions

Serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported

in patients on penicillin therapy. Although anaphylaxis is more frequent following parenteral

therapy, it has occurred in patients on oral penicillins. These reactions are more apt to occur

in individuals with a history of sensitivity to multiple allergens. There have been well-

documented reports of individuals with a history of penicillin hypersensitivity reactions who

have

experienced

severe

hypersensitivity

reactions

when

treated

with

cephalosporin.

Before therapy

with a penicillin, careful inquiry should be made

concerning previous

hypersensitivity reactions to penicillins, cephalosporins and other allergens. BICILLIN L-A

should

given

with

caution

patients

have

previously

experienced

signs

symptoms of allergy associated with a cephalosporin or penicillin. If an allergic reaction

occurs, the drug should be discontinued and the patient treated with the usual agents, e.g.

pressor amines, antihistamines and corticosteroids. Severe anaphylactoid reactions require

emergency treatment with adrenaline. Oxygen and intravenous corticosteroids and airway

management, including intubation, should also be administered as indicated.

Penicillin should be used with caution in individuals with histories of significant allergies

and/or asthma. Whenever allergic reactions occur, penicillin should be withdrawn unless, in

the opinion of the physician, the condition being treated is life-threatening and amenable only

to penicillin therapy.

Severe Cutaneous Adverse Reactions

Severe cutaneous adverse reactions (SCAR), such as Stevens-Johnson syndrome (SJS), toxic

epidermal

necrolysis

(TEN),

drug

reaction

with

eosinophilia

systemic

symptoms

(DRESS), and acute generalised exanthematous pustulosis (AGEP) have been reported in

patients taking beta-lactam antibiotics. When SCAR is suspected, BICILLIN L-A should be

discontinued immediately and an alternative treatment should be considered.

Administration Precautions

Do not inject intravenously or admix with other intravenous solutions.

There have been

reports of inadvertent intravenous administration of benzathine which has been associated

with

cardiorespiratory

arrest

death

(see

section

DOSE

METHOD

ADMINISTRATION).

Inadvertent intravascular administration, including inadvertent direct intra-arterial injection

injection

immediately

adjacent

arteries,

BICILLIN

other

penicillin

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preparations has resulted in severe neurovascular damage, including transverse myelitis with

permanent paralysis, gangrene requiring amputation of digits and more proximal portions of

extremities, and necrosis and sloughing at and surrounding the injection site consistent with

the diagnosis of Nicolau syndrome. Such severe effects have been reported following

injections into the buttock, thigh and deltoid areas. Other serious complications of suspected

intravascular administration which have been reported include immediate pallor, mottling or

cyanosis of the extremity, both distal and proximal to the injection site, followed by bleb

formation; severe oedema requiring anterior and/or posterior compartment fasciotomy in the

lower extremity.

Severe effects and complications following accidental intravascular administration have most

often occurred in infants and small children. Prompt consultation with an appropriate

specialist is indicated if any evidence of compromise of the blood supply occurs at, proximal

to, or distal to the site of injection (see sections 4.3 CONTRAINDICATIONS and 4.2 DOSE

AND METHOD OF ADMINISTRATION).

Injection into or near a nerve may result in permanent neurological damage

. Quadriceps

femoris fibrosis and atrophy have been reported following repeated intramuscular injections

of penicillin preparations into the anterolateral thigh.

Antibiotic-associated Pseudomembranous Colitis

Antibiotic-associated pseudomembranous colitis has been reported with many antibiotics

including penicillin. Treatment with antibacterial agents alters the normal flora of the colon

leading to overgrowth of

C. difficile

C. difficile

produces toxins A and B which contribute to the development of

Clostridium

difficile

associated diarrhea (CDAD). Hypertoxin producing strains of

C. difficile

cause

increased morbidity and mortality, as these infections can be refractory to antimicrobial

therapy and may require colectomy. CDAD must be considered in all patients who present

with diarrhea following antibacterial use. Careful medical history is necessary since CDAD

has been reported to occur over two months after the administration of antibacterial agents.

The severity of the colitis may range from mild to life-threatening. It is important to consider

this diagnosis in patients who develop diarrhoea or colitis in association with antibiotic use

(this may occur up to several weeks after cessation of antibiotic therapy). Mild cases usually

respond to drug discontinuation alone. However, in moderate to severe cases, appropriate

therapy with a suitable oral antibacterial agent effective against

C. difficile

should be

considered. Fluids, electrolytes and protein replacement should be provided when indicated.

Drugs which delay peristalsis, e.g. opiates and diphenoxylate with atropine (Lomotil) may

prolong and/or worsen the condition and should not be used.

Non-susceptible Organisms and Superinfections

Prolonged use of antibiotics may promote the overgrowth of non-susceptible organisms,

including fungi. Should superinfection occur, appropriate measures should be taken.

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Streptococcal Infections

In streptococcal infections, therapy must be sufficient to eliminate the organism otherwise the

sequelae of streptococcal disease may occur. Cultures should be taken following completion

of treatment to determine whether streptococci have been eradicated.

Blood and Kidney Function Tests

In prolonged therapy with penicillin and particularly with high-dosage schedules, periodic

evaluation of the renal and haematopoietic systems is recommended.

Fluids, electrolytes and protein replacement therapy should be provided when indicated.

Paediatric Use

See sections 4.1 THERAPEUTIC INDICATIONS and 4.2 DOSE AND METHOD OF

ADMINISTRATION.

Geriatric Use

Clinical studies of benzylpenicillin did not include sufficient numbers of subjects aged 65 and

over to determine whether they respond differently from younger subjects. Other reported

clinical experience has not identified differences in responses between the elderly and

younger patients. In general, dose selection for an elderly patient should be cautious, usually

starting at the low end of the dosing range, reflecting the greater frequency of decreased

hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. This

drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to

this

drug

greater

patients

with

impaired

renal

function

(see

section

PHARMACOKINETIC PROPERTIES). Because elderly patients are more likely to have

decreased renal function, care should be taken in dose selection, and it may be useful to

monitor renal function.

Effects on Laboratory Tests

Penicillins may interfere with:

- Urinary glucose test

- Coomb's tests

- Tests for urinary or serum proteins

- Tests which use bacteria e.g. Guthrie test.

Penicillins can interfere with the copper sulphate reagent method of testing for glycosuria,

resulting in falsely elevated or falsely decreased readings. Such interference does not occur

with the glucose oxidase method.

4.5 Interaction with other medicines and other forms of interaction

Tetracycline may antagonise the bactericidal effect of penicillin and concurrent use of these

drugs should be avoided.

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The rate of excretion of the penicillins is decreased by concomitant administration of

probenecid which prolongs, as well as increases, blood levels of the penicillins.

Penicillins

reduce

excretion

methotrexate

thereby

increasing

risk

methotrexate toxicity.

4.6 Fertility, pregnancy and lactation

Pregnancy

Human experience with penicillins during pregnancy has not shown any evidence of adverse

effects on the fetus. There are, however, no adequate and well-controlled studies in pregnant

women showing conclusively that harmful effects of these drugs on the fetus can be

excluded. BICILLIN L-A should be used during pregnancy only if clearly needed.

Breast-feeding

Penicillin can be detected in breast milk with the potential for hypersensitivity reactions (e.g.

drug rashes) or gastrointestinal disorders (e.g. diarrhoea or candidosis) in the breast-fed

infant. Consequently, breastfeeding might have to be discontinued.

Fertility

No long-term animal studies have been conducted with this drug.

4.7 Effects on ability to drive and use machines

During treatment with BICILLIN L-A undesirable effects may occur (e.g. allergic reactions,

dizziness, seizures which may influence the ability to drive and use machines. Patients should

be cautious when driving or operating machinery.

4.8 Undesirable effects

As with other penicillins, untoward reactions of the sensitivity phenomena are likely to occur,

particularly in individuals who have previously demonstrated hypersensitivity to penicillins

or in those with a history of allergy, asthma, hay fever, or urticaria.

The following adverse reactions have been reported:

General: Hypersensitivity reactions including the following: skin eruptions (maculopapular to

exfoliative dermatitis), urticaria, laryngeal oedema, fever, eosinophilia, other serum sickness-

like

reactions

(including

chills,

fever,

oedema,

arthralgia

prostration),

anaphylactic/anaphylactoid reaction (including shock and death).

Fever and eosinophilia may frequently be the only reaction observed.

Gastrointestinal: Pseudomembranous colitis. Onset of pseudomembranous colitis symptoms

may occur during or after antibacterial treatment (see section 4.4 SPECIAL WARNINGS

AND PRECAUTIONS FOR USE).

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Haematologic: Haemolytic anaemia, leucopenia, thrombocytopenia

Neurologic: Neuropathy

Urogenital: Nephropathy, acute interstitial nephritis

As with other treatments for syphilis, the Jarisch-Herxheimer reaction has been reported.

The following adverse events have been temporally associated with parenteral administration

of benzylpenicillin:

Body as a Whole: Hypersensitivity reactions including allergic vasculitis, pruritus, fatigue,

asthenia, pain, aggravation of existing disorder, headache, and Nicolau syndrome.

Cardiovascular:

Cardiac

arrest,

hypotension,

tachycardia,

palpitations,

pulmonary

hypertension,

pulmonary

embolism,

vasodilation,

vasovagal

reaction,

cerebrovascular

accident, syncope.

Gastrointestinal: Nausea, vomiting, blood in stool, intestinal necrosis.

Haematological: Lymphadenopathy.

Injection Site: Injection site reactions including pain, inflammation, lump, abscess, necrosis,

oedema,

haemorrhage,

cellulitis,

hypersensitivity,

atrophy,

ecchymosis,

skin

ulcer.

Neurovascular reactions including warmth, vasospasm, pallor, mottling, gangrene, numbness

of the extremities, cyanosis of the extremities, and neurovascular damage.

Metabolic: Elevated BUN, creatinine, and SGOT.

Musculoskeletal:

Joint

disorder,

periostitis,

exacerbation

arthritis,

myoglobinuria,

rhabdomyolysis.

Nervous System: Nervousness, tremors, dizziness, somnolence, confusion, anxiety, euphoria,

transverse myelitis, seizures, coma. A syndrome manifested by a variety of CNS symptoms

such as severe agitation with confusion, visual and auditory hallucinations, and a fear of

impending

death

(Hoigne's

syndrome),

been

reported

after

administration

benzylpenicillin

procaine

and,

less

commonly,

after

injection

combination

benzylpenicillin benzathine and benzylpenicillin procaine. Other symptoms associated with

this

syndrome,

such

psychosis,

seizures,

dizziness,

tinnitus,

cyanosis,

palpitations,

tachycardia, and/or abnormal perception in taste, also may occur.

Respiratory: Hypoxia, apnoea, dyspnoea.

Skin and Other Subcutaneous Tissue Disorders: Diaphoresis.

Severe

cutaneous

adverse

reactions,

including

Stevens-Johnson

syndrome

(SJS),

toxic

epidermal

necrolysis

(TEN),

drug

reaction

with

eosinophilia

systemic

symptoms

(DRESS), and acute generalised exanthematous pustulosis (AGEP) have been reported in

beta-lactam antibiotics.

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Special Senses: Blurred vision, blindness.

Urogenital: Neurogenic bladder, haematuria, proteinuria, renal failure, impotence, priapism.

Reporting of Suspected Adverse Reactions

Reporting suspected adverse reactions after authorisation of the medicine is important. It

allows

continued

monitoring

benefit/risk

balance

medicine.

Healthcare

professionals

asked

report

suspected

adverse

reactions

https://nzphvc.otago.ac.nz/reporting/.

4.9 Overdose

Penicillin in overdosage has the potential to cause neuromuscular hyperirritability and

convulsive seizures. This is particularly so if the penicillin is given to patients with renal

failure.

For advice on the management of overdose, please contact the National Poisons Centre on

0800 POISON (0800 764 766).

5. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Benzylpenicillin exerts a bactericidal action against penicillin-sensitive micro-organisms

during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell-

wall peptidoglycan, rendering the cell wall osmotically unstable. It is not active against the

penicillinase-producing bacteria or against organisms resistant to beta-lactams because of

alterations in the penicillin-binding proteins.

following

in-vitro

data

available

clinical

significance

unknown.

Benzylpenicillin exerts high in vitro activity against Staphylococci (except penicillinase-

producing strains), Streptococci (Groups A, C, G, H, L and M) and Pneumococci. Other

organisms

sensitive

benzylpenicillin

are:

Neisseria

gonorrhoea

Corynebacterium

diphtheria

Bacillus

anthracis

Clostridia

spp,

Actinomyces

bovis

Streptobacillus

moniliformis

Listeria monocytogenes

and Leptospira spp.

Treponema pallidum

is extremely

sensitive to the bactericidal action of benzylpenicillin.

5.2 Pharmacokinetic properties

Intramuscular benzathine benzylpenicillin is absorbed very slowly into the bloodstream from

the intramuscular site and converted by hydrolysis to benzylpenicillin. This combination of

hydrolysis and slow absorption results in blood serum levels much lower but much more

prolonged than other parenteral penicillins.

Intramuscular administration of 225 mg of benzathine benzylpenicillin in adults results in

blood levels of 22.5 to 37.5 nanogram per mL, which are maintained for 4 to 5 days. Similar

blood levels may persist for 10 days following administration of 450 mg and for 14 days

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following administration of 900 mg. Blood concentrations of 2.25 nanogram per mL may

still be detectable 4 weeks following administration of 900 mg.

Approximately 60% of benzylpenicillin is bound to serum protein. The drug is distributed

throughout the body tissues in widely varying amounts. Highest levels are found in the

kidneys with lesser amounts in the liver, skin and intestines. Benzylpenicillin penetrates into

all other tissues and the spinal fluid to a lesser degree.

With normal kidney function, the drug is excreted rapidly by tubular excretion. In neonates

and young infants and in individuals with impaired kidney function, excretion is considerably

delayed.

5.3 Preclinical safety data

Carcinogenesis and Mutagenesis

No long-term animal studies have been conducted with this drug.

6. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Carmellose sodium

Sodium citrate

Water for injection

Lecithin

Povidone

Methyl hydroxybenzoate

Propyl hydroxybenzoate.

6.2 Incompatibilities

Not known.

6.3 Shelf life

48 months from date of manufacture stored at 2° to 8°C.

BICILLIN L-A may be stored below 30

C, for a single period of up to 2 months, prior to

expiry. The date the product is placed outside of refrigerated storage and stored below 30

should be written in the space provided on the carton. After storage outside of refrigeration,

the product should be discarded and cannot be returned to refrigerated storage.

6.4 Special precautions for storage

Refrigerate, do not freeze.

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6.5 Nature and contents of container

BICILLIN L-A is supplied as follows:

2.3 mL pre-filled glass syringe, containing 1,200,000 Units benzathine benzylpenicillin

tetrahydrate, equivalent to 1016.6 mg; pack of 10 syringes.

6.6 Special precautions for disposal and other handling

Single dose injection. Use a single dose unit in one patient on one occasion only. Discard any

unused portion.

Any unused medicine or waste material should be disposed of in accordance with local

requirements.

7. MEDICINE SCHEDULE

Prescription medicine.

8. SPONSOR

Pfizer New Zealand Limited,

PO Box 3998

Auckland, New Zealand, 1140

Toll Free Number: 0800 736 363

9. DATE OF FIRST APPROVAL

01 November 2012

10. DATE OF REVISION OF THE TEXT

18 December 2019

Registered Trademark

SUMMARY TABLE OF CHANGES

Section changed

Summary of new information

4.4, 4.8

Safety update to add Nicolau Syndrome

4.8, 6.1, 10

Minor editorial changes.

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