Consumer medicine information

Bicillin L-A

Benzathine benzylpenicillin tetrahydrate

BRAND INFORMATION

Brand name

Bicillin L-A

Active ingredient

Benzathine benzylpenicillin tetrahydrate

Schedule

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
if you have had an allergic reaction to cephalosporins if you are not sure, check with your pharmacist
You may have an increased chance of being allergic to Bicillin L-A if you are allergic to cephalosporins.

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 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. It should not be injected in front and to the side of the thigh.

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.

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 Poisons Information Centre (telephone 13 11 26) for advice, or go to the Emergency department at the 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.

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.

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 the Emergency department 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 it.

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 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 should be discarded and cannot be returned to refrigerated storage.

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.

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 or 5 and 10 syringes*.

*Not all pack sizes are available.

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 mL.

Bicillin L-A 600,000 Units/1.17 mL syringe contains 600,000 Units equivalent to 517 mg of the active ingredient, benzathine benzylpenicillin tetrahydrate in 1.17 mL.

It also contains the following inactive ingredients:

sodium citrate
carmellose sodium
lecithin
povidone
methyl hydroxybenzoate
propyl hydroxybenzoate
water for injections.

Manufacturer

Bicillin L-A is supplied by:

Pfizer Australia Pty Ltd
ABN 50 008 422 348
Level 17, 151 Clarence Street
Sydney NSW 2000
Toll Free Number: 1800 675 229
[email protected]

Australian Registration Number:

Bicillin L-A 1,200,000 Units/2.3 mL, AUST R 147169

Bicillin L-A 600,000 Units/1.17 mL, AUST R 293456.

® Registered Trademark

This leaflet was revised in January 2021.

Published by MIMS March 2021

BRAND INFORMATION

Brand name

Bicillin L-A

Active ingredient

Benzathine benzylpenicillin tetrahydrate

Schedule

1 Name of Medicine

Benzathine benzylpenicillin tetrahydrate.

2 Qualitative and Quantitative Composition

Bicillin L-A contains benzathine benzylpenicillin (the benzathine salt of benzylpenicillin) in aqueous suspension.
600,000 Units/1.17 mL pre-filled syringe, containing benzathine benzylpenicillin tetrahydrate 517 mg/1.17 mL.
1,200,000 Units/2.3 mL 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.

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:

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

Dosage.

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. Following an acute attack, benzathine benzylpenicillin (parenteral) may be given in doses of 1,200,000 Units once a month or 600,000 Units every 2 weeks.

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. Administration in the anterolateral thigh is not recommended due to the adverse effects observed (see Section 4.4 Special Warnings and Precautions for Use), and vascularity of this region. 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.

4.3 Contraindications

Previous hypersensitivity reaction to any of the penicillins.

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 a cephalosporin. Before therapy with a penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins and other allergens. 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 and 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 and death.
Inadvertent intravascular administration, including inadvertent direct intra-arterial injection or injection immediately adjacent to arteries, of Bicillin L-A and other penicillin 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 (also known as livedoid dermatitis or embolia cutis medicamentosa). 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.

Do not inject into or near a nerve.

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. Because of these adverse effects and the vascularity of this region, administration in the anterolateral thigh is not recommended.

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 Clostridioides difficile.
C. difficile produces toxins A and B which contribute to the development of Clostridioides difficile associated diarrhoea (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 diarrhoea 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.

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.

Use in the elderly.

Bicillin L-A is known to be mainly excreted by the kidney, the risk of toxic reactions to this drug may be greater in patients with impaired renal function (see Section 5.2 Pharmacokinetic Properties). It may be useful to monitor renal function in elderly patients.

Paediatric use.

(See Section 4.1 Therapeutic Indications; Section 4.2 Dose and Method of Administration.)

Effects on laboratory tests.

Penicillins can interfere with the copper sulfate reagent method of testing for glycosuria, resulting in falsely elevated or falsely decreased readings. Such interference does not occur with the glucose oxidase method.

Other.

Bicillin L-A contains approximately 0.11 mEq of sodium per 600,000 units of benzylpenicillin (approximately 2.59 mg of sodium per 600,000 units of benzylpenicillin) and approximately 0.22 mEq of sodium per 1,200,000 units of benzylpenicillin (approximately 5.17 mg of sodium per 1,200,000 units of benzylpenicillin).

4.5 Interactions with Other Medicines and Other Forms of Interactions

Tetracyclines may antagonise the bactericidal effect of penicillin and concurrent use of these drugs should be avoided.
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.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category A)
Category A - Drugs which have been taken by a large number of pregnant women and women of child-bearing age without any proven increase in the frequency of malformations or other direct or indirect harmful effects on the fetus having been observed.
Although generally considered to be safe, Bicillin L-A should be used during pregnancy only if clearly needed.
Soluble benzylpenicillin (the hydrolysate of benzathine benzylpenicillin) is excreted in breast milk. The effect on the infant, if any, is not known. Caution should be used when Bicillin L-A is administered to a nursing woman.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (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 with Bicillin L-A during post-marketing experience:

Skin and other subcutaneous tissue disorders.

Stevens-Johnson syndrome (SJS) and drug reaction with eosinophilia and systemic symptoms (DRESS) (see Section 4.4 Special Warnings and Precautions for Use).
The following adverse reactions have been reported with parenteral benzylpenicillin (the active moiety in Bicillin L-A):

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 and prostration), and anaphylactic/ anaphylactoid reaction (including shock and death); severe cutaneous adverse reactions (SCAR), such as toxic epidermal necrolysis (TEN) and acute generalised exanthematous pustulosis (AGEP) (see Section 4.4 Special Warnings and Precautions for Use).
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).

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 benzathine benzylpenicillin (the active moiety of Bicillin L-A):

Body as a whole.

Hypersensitivity reactions (including allergic vasculitis, pruritus, fatigue, asthenia, and pain), aggravation of existing disorder, headache, Nicolau syndrome (also known as livedoid dermatitis or embolia cutis medicamentosa) (see Section 4.4 Special Warnings and Precautions for Use, Administration precautions).

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, and 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 of 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), has been reported after administration of benzylpenicillin procaine and, less commonly, after injection of the combination of benzylpenicillin benzathine and benzylpenicillin procaine. Other symptoms associated with this syndrome, such as 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.

Special senses.

Blurred vision, blindness.

Urogenital.

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

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.

4.9 Overdose

There have been no reported overdoses with Bicillin L-A. Penicillin in overdosage has the potential to cause neuromuscular hyperirritability and convulsive seizures. This is particularly so if the penicillin is given intravenously or to patients with renal failure.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

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.
The following in-vitro data are available but the clinical significance is 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 to benzylpenicillin are: Neisseria gonorrhoea, Corynebacterium diphtheriae, Bacillus anthracis, Clostridia spp, Actinomyces bovis, Streptobacillus moniliformis, Listeria monocytogenes and Leptospira spp. Treponema pallidum is extremely sensitive to the bactericidal action of benzylpenicillin.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

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 following administration of 900 mg. Blood concentrations of 2.25 nanogram per mL may still be detectable 4 weeks following administration of 900 mg.

Distribution.

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.

Excretion.

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

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Sodium citrate, water for injections, lecithin, carmellose sodium, povidone, methyl hydroxybenzoate, propyl hydroxybenzoate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store at 2 to 8°C. Refrigerate, do not freeze.
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°C 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.

6.5 Nature and Contents of Container

Bicillin L-A is supplied as follows:
1.17 mL pre-filled glass syringe, containing 600,000 Units benzathine benzylpenicillin tetrahydrate, equivalent to 517 mg; *packs of 5 and 10 syringes.
2.3 mL pre-filled glass syringe, containing 1,200,000 Units benzathine benzylpenicillin tetrahydrate, equivalent to 1016.6 mg; *packs of 5 and 10 syringes.
*Not all pack sizes available.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Benzathine benzylpenicillin occurs as a white or almost white powder. It is very slightly soluble in water, freely soluble in dimethylformamide and in formamide, slightly soluble in ethanol (96 per cent).

Chemical structure.

Bicillin L-A (sterile benzathine benzylpenicillin suspension) is chemically designated as (2S,5R,6R)-3,3-dimethyl- 7-oxo-6-(2-phenylacetamido)- 4-thia-1-azabicyclo[3.2.0] heptane-2-carboxylic acid compound with N,N'-dibenzylethylenediamine (2:1), tetrahydrate.
Chemical Formula: (C₁₆H₁₈N₂O₄S)₂.C₁₆H₂₀N₂.4H₂O.
Molecular Weight: 981.18.

CAS number.

41372-02-5.

7 Medicine Schedule (Poisons Standard)

Schedule 4 - Prescription Only Medicine.

Log in

Consumer medicine information

Bicillin L-A

Benzathine benzylpenicillin tetrahydrate

Keep track of your medicines

BRAND INFORMATION