Consumer medicine information

Cilicaine Syringe

Procaine benzylpenicillin (procaine penicillin)

BRAND INFORMATION

Brand name

Cilicaine Syringe 1.5 Suspension for injection

Active ingredient

Procaine benzylpenicillin (procaine penicillin)

Schedule

S4

 

Consumer medicine information (CMI) leaflet

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

What is in this leaflet

This leaflet answers some common questions about CILICAINE. It does not contain all the available information. It does not take place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of using CILICAINE against the benefits this medicine is expected to have for you.

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

Keep this leaflet with your medicine.

You may need to read it again.

What is CILICAINE used for

The name of your medicine is CILICAINE syringe injection.

CILICAINE is a type of antibiotic and belongs to the group of medicines called penicillins. It contains a penicillin, as an active ingredient, which is called Procaine benzylpenicillin (procaine penicillin).

CILICAINE syringe injection is available as a 1.5 gram disposable syringe with sterile swabs.

CILICAINE 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.

Your doctor may have prescribed this medicine for another purpose.

Ask your doctor if you have any questions about why CILICAINE has been prescribed for you.

CILICAINE is only available with a doctor’s prescription.

Before using it

When you must not be given it

Do not use CILICAINE if you have ever had an allergic reaction to:

  • CILICAINE syringe injection or any other penicillin.
  • Any of the other ingredients in CILICAINE 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 if you are allergic to cephalosporins.

Some of the symptoms of an allergic reaction may include skin rash and itching. Other reactions may include nausea, vomiting and diarrhoea.

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

You must also tell your doctor if:

  1. You are allergic to any other medicines, foods, dyes or preservatives.
  2. You are pregnant or intend to become pregnant.
  3. You are breast-feeding or plan to breast feed.
    Like most medicines, CILICAINE is not recommended in pregnancy and during breast-feeding. Your doctor will discuss the possible risks and benefits of using CILICAINE during pregnancy and breast-feeding.

When you must not be given it

Do not use CILICAINE if:

  • the packaging shows sign of tampering or the seal is broken.
  • the expiry date printed on the pack has passed.
    The medication may have no effect at all, or worse, it may give an entirely unexpected effect if you use it after the expiry date.

Taking other medicines

Tell your doctor (or pharmacist) if you are taking any other medicines including probenecid, a medicine used to treat gout.

This includes any that you buy without a prescription from a pharmacy, supermarket or health food shop.

Some medicines may affect the way others work. Your doctor or pharmacist can tell you what to do when CILICAINE is given with other medicines.

Talk to your doctor about the need for an additional method of contraception while on a course of CILICAINE.

Some antibiotics may decrease the effectiveness of some birth control pills, although this has not been shown with CILICAINE.

How much is given

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

CILICAINE must only be given by a doctor or nurse.

How much to inject

The usual dose is:

Adults: 1.5 g daily for two to five days.
For the treatment of Gonorrhoea or Syphilis a dose of 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 under 3 or over 3 years, respectively.

How long to use it for

Your doctor will tell you how long the course of CILICAINE will last. The whole course must be given. Do not cease CILICAINE even if you feel better.

Your infection and symptoms may return.

If you forget to take it

If you forget to go for CILICAINE administration, go to your doctor as soon as you remember and then go back to your normal visits.

If you take too much (overdose)

Telephone your doctor or Poisons Information Centre (phone 13 11 26) if you think that you or anyone else may have been given too much CILICAINE.

Do this even if there are no signs of discomfort or poisoning.

Keep the telephone numbers of these places handy.

While you are using it

Things you must do

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, 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.

If you become pregnant while you are using this medicine tell your doctor.

If you have to get any blood or urine tests done tell your doctor and nurse that you are using CILICAINE.

Tell all your doctor(s), dentist and pharmacist(s) who are treating you that you are on a course of CILICAINE.

Tell your doctor if you feel that this medicine is not helping your condition.

Tell your doctor if, for any reason, it has not been used exactly as prescribed.

Otherwise, your doctor may think that it was not effective and change your treatment unnecessarily.

Things you must not do

Do not cease your CILICAINE course until it is finished, even if you feel better.

Your infection and symptoms may not clear completely and it may return.

Do not administer this medicine to anyone else even if their symptoms seem similar to yours.

Do not use CILICAINE to treat other conditions unless your doctor tells you.

Your doctor has prescribed CILICAINE especially for you and your condition. If you use it for another condition, it may not work or make the condition worse.

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 is ineffective against fungi.

If you get diarrhoea, nausea or vomiting, tell your doctor.

Take care while driving or operating machinery until you know how CILICAINE affects you.

CILICAINE generally does not affect your ability to drive a car or operate machinery. However, as with many other medicines, CILICAINE may also cause dizziness, drowsiness and/or tiredness in some people.

Side Effects

Tell your doctor or pharmacist if you do not feel well while you are using CILICAINE.

CILICAINE helps most people with infections but it may have some unwanted side effects in a few people.

Side effects reported by some people using CILICAINE include:

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

CILICAINE may cause other side effects.

If you have any other side effects, check with your doctor.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

While using it

Storage

Keep CILICAINE syringe injection where young children cannot reach it.

A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Store CILICAINE syringe 2 - 8°C. DO NOT FREEZE.

Do not leave CILICAINE syringe in the car or on windowsills.

Heat can destroy some medicines.

Disposal

If your doctor tells you to stop using CILICAINE or it has passed its expiry date, ask your pharmacist what to do with any CILICAINE syringe left over.

Product Description

What it looks like

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

Ingredients

Active ingredient:

Procaine benzylpenicillin (procaine penicillin) 1.5 g per 3.4 mL.

Inactive ingredients:

Polysorbate 80, sodium citrate, and water for injections. CILICAINE 1.5 syringe injection is preservative free.

Australian Registration number:
CILICAINE 1.5 syringe injection
AUST R 288818.

Sponsor

Aspen Pharma Pty Ltd
34-36 Chandos Street
St Leonards NSW 2065
Australia

This leaflet was revised in June 2017


BRAND INFORMATION

Brand name

Cilicaine Syringe 1.5 Suspension for injection

Active ingredient

Procaine benzylpenicillin (procaine penicillin)

Schedule

S4

 

1 Name of Medicine

Procaine benzylpenicillin (procaine penicillin).

6.7 Physicochemical Properties

Its chemical name is 2-diethylaminoethyl 4-aminobenzoate (6R)-(2-phenylacetamido) penicillinate monohydrate with an empirical formula of C13H20N2O2,C16H18N2O4S,H2O and a molecular weight of 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.

Chemical structure.


CAS number.

6130-64-9.

2 Qualitative and Quantitative Composition

Cilicaine Syringe 1.5 injection contains 1.5 g of procaine benzylpenicillin (procaine penicillin) in 3.4 mL. It is a sterile buffered aqueous suspension.

Note.

1 unit = 1 microgram of pure procaine benzylpenicillin (procaine penicillin).

Excipients.

Sodium citrate dihydrate, polysorbate 80 and water for injections.

3 Pharmaceutical Form

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

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 the following.
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

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.
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 cerebrospinal 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 delayed considerably.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

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). Procaine benzylpenicillin (procaine penicillin) must be administered by the intramuscular route only (see Section 4.2 Dose and Method of Administration).

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, procaine benzylpenicillin (procaine penicillin) 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 (Lomotil), may prolong and/or worsen the condition and should not be used.
As with any antibiotic, overgrowth with nonsusceptible 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 has been associated with the unmasking of Brugada syndrome. Cilicaine 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, procaine penicillin 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 the penicillins during pregnancy has not shown any positive evidence of adverse effects on the foetus. There are, however, no adequate and well controlled studies in pregnant women showing conclusively that harmful effects of these drugs on the foetus 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.

4.8 Adverse Effects (Undesirable Effects)

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.

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.
Extreme anxiety and a sensation of impending death has been reported after intramuscular injection of aqueous procaine benzylpenicillin (procaine penicillin), but 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.

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. (Cilicaine syringes are 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 regimens vary 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.

4.7 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.

4.9 Overdose

Cilicaine 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).

7 Medicine Schedule (Poisons Standard)

S4.

6 Pharmaceutical Particulars

6.1 List of Excipients

See Section 2 Qualitative and Quantitative Composition.

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

Cilicaine syringe should be stored at 2°C to 8°C. (Refrigerate. Do not freeze.)

6.5 Nature and Contents of Container

Cilicaine syringe 1.5 g is available in disposable syringes (containing sterile buffered aqueous suspension): 5's (with 5 sterile skin swabs).

6.6 Special Precautions for Disposal

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

Summary Table of Changes