Consumer medicine information

Cilicaine Syringe 1.5

Procaine benzylpenicillin (procaine penicillin)

BRAND INFORMATION

Brand name

Cilicaine Syringe 1.5

Active ingredient

Procaine benzylpenicillin (procaine penicillin)

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Cilicaine Syringe 1.5.

What is in this leaflet

This leaflet answers some common questions about CILICAINE SYRINGE 1.5. 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 being given CILICAINE SYRINGE 1.5 against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What CILICAINE SYRINGE 1.5 is used for

CILICAINE SYRINGE 1.5 is an antibiotic belonging to the group of antibiotics known as penicillins. The active ingredient in CILICAINE SYRINGE 1.5 is procaine benzylpenicillin (procaine penicillin).

CILICAINE SYRINGE 1.5 is used to treat infections in different parts of the body caused by bacteria. It works by killing the bacteria that are causing the infection. It will not work against infections caused by viruses such as colds or the flu.

Ask your doctor if you have any questions about why this medicine has been prescribed for you. Your doctor may have prescribed it for another reason.

This medicine is available only with a doctor's prescription.

Before you are given CILICAINE SYRINGE 1.5

When you must not be given it

Do not receive CILICAINE SYRINGE 1.5 if you have an allergy to:

  • any medicine containing procaine benzylpenicillin
  • any other penicillin medicines
  • any of the ingredients listed at the end of this leaflet

You must tell your doctor if you have had an allergic reaction to cephalosporins. You may have an increased chance of being allergic to CILICAINE SYRINGE 1.5 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 or other parts of the body
  • rash, itching or hives on the skin

Tell your doctor if you have suffered from any other allergic reactions in the past due to use of penicillin.

Do not receive this medicine if you are pregnant. It may affect your developing baby if you take it during pregnancy.

Do not breast-feed if you are taking this medicine. Your doctor will discuss with you the risks and benefits of being given CILICAINE SYRINGE 1.5 during pregnancy and when you are breastfeeding.

Do not receive this medicine after the expiry date printed on the pack or if the packaging is torn or shows signs of tampering.

If you are not sure whether you should start taking this medicine, talk to your doctor.

Before you are given it

Tell your doctor or nurse if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor if you are taking probenecid, a medicine used to treat gout.

If you take the oral contraceptive pill, talk to your doctor or nurse about the need to use additional contraception whilst being given CILICAINE SYRINGE 1.5. Some antibiotics may decrease the effectiveness of some birth control pills, though this has not been shown in CILICAINE SYRINGE 1.5.

If you have not told your doctor about any of the above, tell them before you are given CILICAINE.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you get without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and CILICAINE SYRINGE 1.5 may interfere with each other. These include:

You may need different amounts of your medicines, or you may need to take different medicines.

Your doctor and nurse have more information on medicines to be careful with or avoid whilst you are receiving CILICAINE SYRINGE 1.5.

How you are given CILICAINE SYRINGE 1.5

CILICAINE SYRINGE 1.5 is given as a deep injection into a large muscle.

CILICAINE SYRINGE 1.5 must only be given by a doctor or nurse.

How much you are given

The usual dose is:

Adults
1.5 g daily for two to five days.

For the treatment of gonorrhoea or syphilis:

1 g daily for 7 to 14 days or up to 4.8 g as a single session treatment usually administered with probenecid.

Children
1/4 or 1/2 adult dose is usually sufficient for children under 3 or over 3 years of age, respectively.

How long to use it for

Your doctor will tell you how long you will be given CILICAINE SYRINGE 1.5 injections for.

The whole course must be given. Do not stop receiving CILICAINE SYRINGE 1.5 even if you feel better.

Your infection and symptoms may return.

If you forget to be given it

If you have forgotten about your next CILICAINE SYRINGE 1.5 injection, go to your doctor as soon as you remember and then go back to your normal visits.

If you are given too much (overdose)

As this medicine is given to you by a doctor or nurse it is unlikely that you will receive too much.

Immediately telephone your doctor or the Poisons Information Centre (telephone 13 11 26) for advice, or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have been given too much CILICAINE SYRINGE 1.5. Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

While you are using CILICAINE SYRINGE 1.5

Things you must do

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are currently receiving CILICAINE SYRINGE 1.5.

Tell any other doctors, dentists and pharmacists who treat you that you are receiving this medicine.

If your symptoms do not improve within few days, or if they become worse, tell your doctor.

If you develop any form of skin rash and/or itching or difficulty in breathing while using CILICAINE SYRINGE 1.5, contact your doctor immediately.

If you develop severe diarrhoea tell your doctor immediately. Do this even if it occurs several weeks after you have stopped using CILICAINE SYRINGE 1.5.

If you become pregnant while receiving this medicine, tell your doctor immediately.

If you are about to have any blood tests, tell your doctor that you are being given this medicine. It may interfere with the results of some tests.

Tell your doctor if you have not received this medicine as it was prescribed. Otherwise your doctor may think that it was not effective and change your treatment unnecessarily.

Keep all of your doctor's appointments so that your progress can be checked.

Things you must not do

Do not use CILICAINE SYRINGE 1.5 to treat any other complaints unless your doctor tells you to.

Do not give your medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage without checking with your doctor.

Things to be careful of

Tell your doctor if you get vaginal itching or discharge, sore mouth or tongue. This is due to a fungal infection called thrush. Sometimes use of this medicine allows fungi to grow, as CILICAINE SYRINGE 1.5 is ineffective against fungi.

If you get diarrhoea, nausea or vomiting, tell your doctor. Do this even if it occurs several weeks after receiving your last CILICAINE SYRINGE 1.5 injection.

Be careful driving or operating machinery until you know how CILICAINE SYRINGE 1.5 affects you. CILICAINE SYRINGE 1.5 generally does not affect your ability to drive a car or operate machinery. However, as with many other medicines, CILICAINE SYRINGE 1.5 may also cause dizziness, drowsiness and/or tiredness in some people.

may be added as needed.

Side effects

Tell your doctor or nurse as soon as possible if you do not feel well while you are taking CILICAINE SYRINGE 1.5.

This medicine helps most people, but it may have unwanted side effects in a few 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.

Do not be alarmed by the following lists of side effects. You may not experience any of them.

Ask your doctor or nurse to answer any questions you may have.

Side effects reported by some people using CILICAINE SYRINGE 1.5 include:

  • diarrhoea
  • nausea & vomiting
  • skin rash
  • difficulty in breathing

Tell your doctor or nurse if you notice anything that is making you feel unwell.

Other side effects not listed above may also occur in some people.

After receiving CILICAINE SYRINGE 1.5

Storage

The syringes will be kept on the hospital ward or in the pharmacy. Keep the syringes in the pack until it is time to take them.

Store CILICAINE SYRINGE 1.5 between 2 and 8 degrees Celsius.

Product description

What it looks like

CILICAINE SYRINGE 1.5 is a slightly viscous white suspension with a faint odour characteristic of penicillin.

Ingredients

CILICAINE SYRINGE 1.5 contains 1.5 mg of procaine benzylpenicillin (procaine penicillin) as the active ingredient.

The syringes also contain the following inactive ingredients:

  • polysorbate 80
  • sodium citrate
  • water for injections

CILICAINE SYRINGE 1.5 syringe injection is preservative free.

Distributor

CILICAINE SYRINGE 1.5 is distributed in Australia by:

Alphapharm Pty Ltd
Level 1, 30 The Bond
30-34 Hickson Road
Millers Point NSW 2000
www.mylan.com.au

This leaflet was prepared in September 2020.

AUST R 288818

cilicaine-syringe-1.5_cmi\Sep20/00

Published by MIMS November 2020

BRAND INFORMATION

Brand name

Cilicaine Syringe 1.5

Active ingredient

Procaine benzylpenicillin (procaine penicillin)

Schedule

S4

 

1 Name of Medicine

Procaine benzylpenicillin (procaine penicillin).

2 Qualitative and Quantitative Composition

Each Cilicaine Syringe 1.5 injection suspension contains 1.5 g of procaine benzylpenicillin (as procaine penicillin) as the active ingredient.
The solution in Cilicaine Syringe 1.5 is sterile.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Cilicaine Syringe 1.5 injection suspension is a slightly viscous white suspension, free of excessive aeration, that has a faint odour characteristic of penicillin.

4 Clinical Particulars

4.1 Therapeutic Indications

Treatment of moderately severe infections due to penicillin sensitive organisms. Therapy should be guided by bacteriological studies, including sensitivity tests, and also by clinical response.
Infections which usually respond to adequate dosage are:
group A streptococcal infections including:
upper respiratory tract infections, skin and skin structure infections and scarlet fever;
pneumococcal infections of the respiratory tract;
susceptible staphylococcal infections; most gonococcal infections; syphilis, fusospirochaetosis (Vincent's gingivitis and pharyngitis).
Cilicaine Syringe 1.5 must be administered by the intramuscular route only (see Section 4.2 Dose and Method of Administration).

4.2 Dose and Method of Administration

For use by intramuscular injection only.
Before injecting the dose, aspirate to be sure that the needle is not in a blood vessel (the syringe is designed to facilitate easy aspiration before injection). If blood appears, withdraw and inject in another site.

Adults.

A common dose of procaine benzylpenicillin (procaine penicillin) is 1.5 g daily for two to five days, the fourth and fifth doses being dependent on the severity of the infection.

Gonorrhoea.

Uncomplicated infection with sensitive gonococci: dosage regimen varies according to treatment plan. Doses may be 1 g daily for one to two weeks, or up to 4.8 g as a single session treatment, usually administered with probenecid.

Syphilis.

Often a 10 to 14 day course of procaine benzylpenicillin (procaine penicillin) 1 g/day.

Use in children.

Dose should be adjusted according to age and weight.

Newborn and premature infants.

Crystalline penicillin given at intervals of 8 or 12 hours is more suitable for more serious infections.

Children under 3 years.

¼ adult dose is usually sufficient.

Children over 3 years.

½ adult dose is usually sufficient.

4.3 Contraindications

Known hypersensitivity to penicillins or procaine.

4.4 Special Warnings and Precautions for Use

Identified precautions.

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 penicillin. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or history of sensitivity to multiple allergens. There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins. Before initiating therapy with any penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillin, cephalosporins or other allergens. If an allergic reaction occurs, Cilicaine Syringe 1.5 should be discontinued and the appropriate therapy instituted. Serious anaphylactoid reactions require immediate emergency treatment with adrenaline. Oxygen, intravenous steroids, and airway management, including intubation, should also be administered as indicated.
Antibiotic associated pseudomembranous colitis has been reported with many antibiotics including this drug. A toxin produced with Clostridium difficile appears to be the primary cause. 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 Clostridium 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 may prolong and/or worsen the condition and should not be used.
As with any antibiotic, overgrowth with non-susceptible organisms may occur. If noted, appropriate measures must be taken. Streptococcal infections should be treated for a minimum of 10 days, and cultures should be taken at completion of treatment to confirm that Streptococci have been eradicated.
Inadvertent intravascular administration, including inadvertent direct intra-arterial injection or injection immediately adjacent to arteries, 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. 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. The above described severe effects and complications have most often occurred in infants and small children.
Quadriceps femoris fibrosis and atrophy have been reported following repeated intramuscular injections of penicillin preparations into the anterolateral thigh.
Injection into or near a nerve may result in permanent neurological damage.
In prolonged therapy with penicillin, and particularly with high dosage schedules, periodic evaluation of the renal and haematopoietic systems is recommended.

Brugada syndrome.

The procaine component of Cilicaine Syringe 1.5 has been associated with the unmasking of Brugada syndrome. Cilicaine Syringe 1.5 should be avoided in patients with known Brugada syndrome. Care should be exercised in patients with suspected cardiac conduction abnormalities.

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, Cilicaine Syringe 1.5 should be discontinued immediately and an alternative treatment should be considered.

Use in the elderly.

No data available.

Paediatric use.

See Section 5.2 Pharmacokinetic Properties.

Effects on laboratory tests.

Interference with laboratory tests.

Studies using procaine benzylpenicillin (procaine penicillin), ampicillin or carbenicillin indicate that penicillins can interfere with urinary glucose determinations using cupric sulphate (e.g. Benedict's solution, Clinitest). In high concentrations, penicillins can cause false positive results in these tests for urinary glucose. Glucose oxidase tests for urinary glucose (e.g. Clinistix, Tes-tape) are reportedly not affected by the presence of penicillins.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Bacteriostatic drugs, such as tetracyclines, may antagonise the bactericidal effect of penicillin. Concurrent use of these drugs should be avoided.
Concurrent administration of probenecid and penicillin will result in increased blood concentrations by reducing tubular excretion of penicillin.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category A)
Human experience with penicillins during pregnancy has not shown any positive 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.
The drug is excreted in breast milk in concentrations lower than plasma levels. As safety to newborn infants has not been established, it is not recommended for breastfeeding mothers unless the benefits outweigh any potential risk.

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)

Very common.

Gastrointestinal effects like diarrhoea, nausea and vomiting; skin rash; difficulty in breathing.

Common.

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).

Rare.

Anaphylactic shock occurs rarely.
Other adverse effects have generally been associated with large intravenous doses of more than 10 million units of benzylpenicillin per day. These adverse effects include haemolytic anaemia, leucopenia, thrombocytopenia, neuropathy and nephropathy. These are rare reactions usually only occurring with large doses.
Some patients being treated for syphilis may experience a Jarisch-Herxheimer reaction shortly after starting treatment with Cilicaine Syringe 1.5.
Extreme anxiety and a sensation of impending death has been reported after intramuscular injection of aqueous procaine benzylpenicillin (procaine penicillin) however patients show no major abnormal physical signs. Some develop hallucinations, disorientation, tachycardia, acute depersonalisation or frank psychotic behaviour. Patients may be regarded as hysterical by anyone not aware of this clinical entity. It is thought these attacks are due to the procaine. They are usually self limiting, subsiding in 15 to 30 minutes. These 'procaine reactions' have been attributed to accidental intravascular administration. They are not allergic reactions.

Skin and other subcutaneous tissue disorders.

Severe cutaneous adverse reactions, including 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 beta-lactam antibiotics.

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

Cilicaine Syringe 1.5 has the potential to cause neuromuscular hyperirritability or convulsive seizures.

Treatment.

Management of overdosage should include monitoring of electrolyte balance, cardiovascular status and renal function. Penicillins are not readily removed by dialysis.
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 is a bactericidal antibiotic, producing its effect on penicillin sensitive microorganisms during the stage of active multiplication through inhibition of biosynthesis of cell wall mucopeptides.

Microbiology.

Procaine benzylpenicillin (procaine penicillin) is effective against benzylpenicillin sensitive organisms including:
Gram positive cocci including Streptococci (groups A, C, G, H, L and M), non-beta-lactamase producing Staphylococci, Pneumococci, and anaerobic Streptococci.
Gram positive bacilli including Corynebacterium diphtheriae, Bacillus anthracis, Clostridia sp. (Cl. tetani, Cl. perfringens).
Gram negative cocci including Neisseria meningitidis, N. gonorrhoeae.
Gram negative bacilli are generally resistant.
Treponema pallidum and leptospirae are sensitive to benzylpenicillin.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

The procaine salt has low solubility and is administered intramuscularly as a suspension of crystalline procaine benzylpenicillin (procaine penicillin). These particles dissolve slowly after administration, so that absorption from the injection site takes place over a prolonged period. Because absorption continues for up to 24 hours, injection may be given only once or twice daily, or as an initial treatment. A peak serum level is reached in about 2 hours.

Distribution.

About 60% of benzylpenicillin is bound to serum proteins. 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 into the cerebro-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 delayed considerably.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

The injection suspension also contains the following inactive ingredients: sodium citrate dihydrate, polysorbate 80 and water for injections.

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.

6.5 Nature and Contents of Container

Container type: syringe (glass type I clear).
The syringes are disposable.
Pack size: 5.
Some strengths, pack sizes and/or pack types may not be marketed.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking it to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Chemical name: 2-diethylaminoethyl 4-aminobenzoate (6R)-(2-phenylacetamido) penicillinate monohydrate.
Molecular formula: C13H20N2O2,C16H18N2O4S,H2O.
Molecular weight: 588.7.

Physical and chemical properties.

Procaine benzylpenicillin (procaine penicillin) is a white crystalline powder. It is slightly soluble in water (1 in 250 or 4.0 - 4.5 mg/mL), soluble in 96% alcohol (1 in 30 or 3.33 mg/mL) and chloroform (1 in 60), slightly soluble in acetone and fixed oils. A 0.33% aqueous suspension has a pH of 5.0 to 7.5.

CAS number.

6130-64-9.

7 Medicine Schedule (Poisons Standard)

S4 (Prescription Only Medicine).

Summary Table of Changes