Consumer medicine information

Lincomycin SXP

Lincomycin

BRAND INFORMATION

Brand name

Lincomycin SXP

Active ingredient

Lincomycin

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Lincomycin SXP.

What is in this leaflet

Please read this leaflet carefully before you start using LINCOMYCIN SXP. This leaflet answers some common questions about LINCOMYCIN SXP. 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 using LINCOMYCIN SXP against the benefits it is expected to have for you. Use LINCOMYCIN SXP as instructed and follow the advice given in this leaflet.

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

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

What LINCOMYCIN SXP is used for

LINCOMYCIN SXP is an antibiotic used to treat serious infections in different parts of the body caused by certain bacteria. LINCOMYCIN SXP works by killing or stopping the growth of bacteria causing your infection.

The specific infections for which LINCOMYCIN SXP is used include: ear, throat and lung infections; skin infections; bone and joint infections; and infections of the blood.

LINCOMYCIN SXP will not work against viral infections such as colds or flu.

Your doctor may have prescribed LINCOMYCIN SXP for another reason.

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

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

LINCOMYCIN SXP is not addictive.

Before you use LINCOMYCIN SXP

Some information is provided below. However, always talk to your doctor if you have concerns or questions about your treatment.

When you must not use LINCOMYCIN SXP

Do not use LINCOMYCIN SXP if:

  1. you have an allergy to:
  • clindamycin or lincomycin
  • any of the other ingredients listed at the end of this leaflet
    (see 'Product Description')
Symptoms of an allergic reaction may include skin rash, itching or difficulty in breathing, wheezing or coughing (anaphylactic reactions). If you are not sure if you have or have had an allergic reaction to LINCOMYCIN SXP , check with your doctor.
  1. the packaging is torn or shows signs of tampering
  2. the expiry date (EXP) printed on the label has passed
  3. you are breast-feeding
LINCOMYCIN SXP may pass into the breast-milk so alternatives should be discussed with your doctor.

LINCOMYCIN SXP is not to be given to a newborn baby.

If you are not sure about the use of LINCOMYCIN SXP, talk to your doctor.

Before you start treatment with LINCOMYCIN SXP

Tell your doctor if:

  1. you are pregnant or intend to become pregnant.
Your doctor will discuss the risks and benefits of using LINCOMYCIN SXP during pregnancy.
  1. your child to be treated was born premature.
  2. you have or have ever had any of the following conditions:
  • asthma
  • any gastrointestinal (stomach or gut) problems
  • any liver or kidney disease.
  1. you have ever had any other health problems or medical conditions.
  2. you have any allergies to any other medicines or any other substances such as foods, preservatives or dyes.

If you have not told your doctor or pharmacist about any of the above, do so before you start taking LINCOMYCIN SXP.

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. LINCOMYCIN SXP should not be given with erythromycin since these two medicines may interact.

  • LINCOMYCIN SXP should not be given with certain medicines due to physical incompatibility with LINCOMYCIN SXP. These include kanamycin, novobiocin and phenytoin.
  • Interference between LINCOMYCIN SXP and neuromuscular blocking medicines (muscle-relaxing medicines) may occur

Your doctor or pharmacist can tell you what to do if you are already taking any of these medicines. They also have a more complete list of medicines to be careful with or avoid while using LINCOMYCIN SXP.

Ask your doctor or pharmacist if

How to use LINCOMYCIN SXP

LINCOMYCIN SXP is administered by an infusion into a vein or an injection into a muscle. Do not administer this medicine to yourself.

How much to use

The dose and frequency of LINCOMYCIN SXP that your doctor prescribes for you depends on your medical condition.

How long to use LINCOMYCIN SXP

Your doctor will continue giving you LINCOMYCIN SXP for as long as your condition requires.

If a dose is missed

If a dose of LINCOMYCIN SXP is missed, the next dose should be given at the normal time it is due.

If you are given too much (overdose)

Your doctor will ensure that you receive the correct dose of LINCOMYCIN SXP.

Never administer this medicine to yourself.

Immediately telephone your doctor or Poisons Information Centre (in Australia; tel 13 11 26, or in New Zealand; tel 0800 POISON or 0800 764 766), for advice, or go to Accident and Emergency (Casualty) at your nearest hospital if you think that you or anyone else may have been given too much LINCOMYCIN SXP. Do this even if there are no signs of discomfort or poisoning.

You may need urgent medical attention. Keep the telephone numbers for these services handy. Have the LINCOMYCIN SXP box or this leaflet available to give details if needed.

While using LINCOMYCIN SXP

Things you must do

Advise your doctor immediately if you notice any unusual symptoms.

If you are about to start taking any new medicines, tell your doctor or pharmacist that you are taking LINCOMYCIN SXP.

Tell all doctors, dentists and pharmacists who are treating you that you are being treated with LINCOMYCIN SXP.

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

If you get severe diarrhoea, tell your doctor, pharmacist or nurse immediately. Do this even if it occurs several weeks after LINCOMYCIN SXP has been stopped. 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 while taking or soon after stopping LINCOMYCIN SXP, tell your doctor. Also tell your doctor if you get vaginal itching or discharge. This may mean you have a fungal/ yeast infection called thrush. Sometimes the use of LINCOMYCIN SXP allows fungi/yeast to grow and the above symptoms to occur. LINCOMYCIN SXP does not work against fungi/yeast.

If you become pregnant while you are taking LINCOMYCIN SXP , tell your doctor.

If you are about to start taking any new medicines, tell your doctor and pharmacist that you are taking LINCOMYCIN SXP.

Tell all doctors, dentists and pharmacists who are treating you that you are taking LINCOMYCIN SXP. you are not sure if you are taking any of these medicines

Side effects

Check with your doctor as soon as possible if you have any concerns while using LINCOMYCIN SXP , even if you do not think your concerns are connected with the medicine or are not listed in this leaflet.

All medicines can have side effects and LINCOMYCIN SXP may have unwanted side effects in a few people.

Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Do not be alarmed by this list of possible side effects. You may not experience any of them. Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are using LINCOMYCIN SXP.

While being treated with LINCOMYCIN SXP

Tell your doctor if you notice any of the following and they worry you:

  • oral thrush - white, furry, sore tongue and mouth
  • vaginal thrush - sore and itchy vagina and/or discharge
  • sore mouth or tongue
  • nausea and/or vomiting
  • diarrhoea
  • skin rash
  • ringing in the ears
  • dizziness
  • pain or swelling at the injection site

If these effects do not go away or they are worrying to you, tell your doctor.

Tell your doctor immediately or go to Accident and Emergency (Casualty) at your nearest hospital if you experience any of the following:

  • allergic type reactions e.g. skin rash, itching and difficulty breathing, wheezing or coughing (anaphylactic reactions)
  • severe diarrhoea
  • severe stomach pains

LINCOMYCIN SXP can also cause: changes in blood cells, lowering of blood pressure.

After finishing treatment with LINCOMYCIN SXP

Tell your doctor immediately if you notice any of the following side effects, particularly if they occur several weeks after stopping treatment with LINCOMYCIN SXP:

  • severe abdominal cramps or stomach cramps
  • watery and severe diarrhoea, which may also be bloody
  • fever, in combination with one or both of the above

These are rare but serious side effects. LINCOMYCIN SXP can cause bacteria which is normally present in the bowel and normally harmless, to multiply and cause the above symptoms. Therefore, you may need urgent medical attention.

However, this side effect is rare.

Do not take any diarrhoea medicine without first checking with your doctor.

Some people may get other side effects while taking LINCOMYCIN SXP.

Tell your doctor if you notice any other effects.

This is not a complete list of all possible side effects. Some people may get other side effects while being treated with LINCOMYCIN SXP.

After treatment with LINCOMYCIN SXP

Storage

Normally your doctor will get your LINCOMYCIN SXP from the hospital pharmacy or their consulting rooms. If however, you do take your LINCOMYCIN SXP from the pharmacy to your doctor, it is important to store your LINCOMYCIN SXP in a safe place away from light and away from heat (below 25°C).

Do not leave your LINCOMYCIN SXP in a car.

If for any reason you take your LINCOMYCIN SXP home, always ensure that it is stored in a place where children cannot reach it. Do not freeze LINCOMYCIN SXP.

Disposal

If your doctor stops treating you with LINCOMYCIN SXP , your hospital pharmacist will dispose of any unused medicine.

The expiry date is printed on the carton. Do not use LINCOMYCIN SXP after this date has passed.

Product Description

What LINCOMYCIN SXP looks like

LINCOMYCIN SXP is a clear, colourless or almost colourless solution in a glass vial.

Identification

LINCOMYCIN SXP can be identified by the Australian Register Number:

300 mg/mL vial AUST R 281299

600 mg/2 mL vial: AUST R 281302

Ingredients

The active ingredient in LINCOMYCIN SXP is lincomycin hydrochloride. Each 1 mL vial contains lincomycin hydrochloride equivalent to 300 mg of lincomycin.

Each 2 mL vial contains lincomycin hydrochloride equivalent to 600 mg of lincomycin.

LINCOMYCIN SXP also contains benzyl alcohol and water for injections.

Supplier

LINCOMYCIN SXP is supplied in Australia by:

Southern XP Pty Ltd
Unit 5/118 Church Street
Hawthorn VIC 3122

Sponsor:

Southern XP IP Pty Ltd
Unit 5/118 Church Street
Hawthorn VIC 3122

This leaflet was prepared in August 2022.

Published by MIMS October 2022

BRAND INFORMATION

Brand name

Lincomycin SXP

Active ingredient

Lincomycin

Schedule

S4

 

Notes

Distributed by Southern XP Pty Ltd

1 Name of Medicine

Lincomycin hydrochloride monohydrate.

2 Qualitative and Quantitative Composition

Each 1 mL injection contains 340.2 mg lincomycin hydrochloride monohydrate equivalent to 300.0 mg lincomycin.
Each 2 mL injection contains 680.4 mg lincomycin hydrochloride monohydrate equivalent to 600.0 mg lincomycin.
Contains no excipients with a known effect.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Clear, colorless to slightly yellow solution, having a slight odour, essentially free from visible particulate matter.

4 Clinical Particulars

4.1 Therapeutic Indications

Lincomycin SXP is indicated in the treatment of serious infections due to susceptible strains of gram-positive aerobes such as streptococci, pneumococci and staphylococci.
Its use should be reserved for penicillin-allergic patients or other patients for whom, in the judgement of the physician, a penicillin is inappropriate. Because of the risk of colitis (see Section 4.4 Special Warnings and Precautions for Use), before selecting lincomycin the physician should consider the nature of infection and the suitability of less toxic alternatives (e.g. erythromycin).
Lincomycin injection has been demonstrated to be effective in the treatment of staphylococcal infections resistant to other antibiotics and susceptible to lincomycin. Staphylococcal strains resistant to lincomycin injection have been recovered; culture and susceptibility studies should be done in conjunction with lincomycin injection therapy. In the case of macrolides, partial but not complete cross resistance may occur. The drug may be administered concomitantly with other antimicrobial agents with which it is compatible when indicated (see Section 4.4 Special Warnings and Precautions for Use).
The specific infections for which Lincomycin SXP is indicated are as follows.
Upper respiratory infections including tonsillitis, pharyngitis, otitis media, sinusitis, scarlet fever and as adjuvant therapy for diphtheria. Effectiveness in the treatment of mastoiditis would be anticipated.
Lower respiratory infections including acute and chronic bronchitis and pneumonia.
Skin and skin structure infections including cellulitis, furuncles, abscesses, impetigo, acne and wound infections. Conditions such as erysipelas, lymphadenitis, paronychia (panaritium), mastitis and cutaneous gangrene should, if caused by susceptible organisms, respond to lincomycin therapy.
Bone and joint infections including osteomyelitis and septic arthritis.
Septicaemia and endocarditis. Selected cases of septicaemia and/or endocarditis due to susceptible organisms have responded well to lincomycin. However, bactericidal drugs are often preferred for these infections.
Bacillary Dysentery. Although Shigella is resistant to lincomycin in vitro (MIC approximately 200-400 microgram/mL), lincomycin has been effective in its treatment due to the very high levels of lincomycin attained in the bowel (approximately 3000-7000 microgram/gram of stool).

4.2 Dose and Method of Administration

Note.

If significant diarrhoea occurs during therapy, this antibiotic should be discontinued (see Section 4.4 Special Warnings and Precautions for Use).
Lincomycin injection is incompatible with novobiocin, kanamycin and phenytoin.
With beta-haemolytic streptococcal infections, treatment should continue for at least 10 days to diminish the likelihood of subsequent rheumatic fever or glomerulonephritis.
Product is for single use in one patient only. Discard any residue.

Intramuscular.

Adults.

Serious infections.

600 mg (2 mL) intramuscularly every 24 hours.

More serious infections.

600 mg (2 mL) intramuscularly every 12 hours or more often, as determined by the severity of the infection.
Children over 1 month of age.

Serious infections.

One intramuscular injection of 10 mg/kg/day.

More serious infections.

One intramuscular injection of 10 mg/kg every 12 hours or more often.

Intravenous.

Intravenous doses are given on the basis of 1 g lincomycin injection diluted in not less than 100 mL of appropriate solution and infused over a period of not less than one hour.

Note.

Severe cardiopulmonary reactions have occurred when this drug has been given at greater than the recommended concentration and rate.
Adults.

Serious infections.

600 mg to 1 g given every 8-12 hours.

More severe infections.

The above doses may be increased. In life-threatening situations, daily intravenous doses of as much as 8 g have been given.
Children over 1 month of age. Depending on the severity of the infection, 10-20 mg/kg/day may be infused in divided doses as described in Table 1.
These doses may be repeated as often as required to the limit of the maximum recommended daily dose of 8 g.
The following infusion solutions have been found to be physically compatible with lincomycin injection: Glucose Intravenous Infusion 5%, Glucose Intravenous Infusion 10%, Sodium Chloride 0.9% and Glucose 5% Intravenous Infusion, Sodium Chloride 0.9% and Glucose 10% Intravenous Infusion, Compound Sodium Lactate Intravenous Infusion, Sodium Lactate 1/6 Molar and Dextran 70 Intravenous Infusion.
Please note that these compatibility determinations are physical observations only, not chemical determinations. Adequate clinical evaluation of the safety and efficacy of these combinations has not been performed.

Patients with diminished renal function.

When lincomycin injection therapy is required in individuals with severe impairment of renal function, an appropriate dose is 25 to 30% of that recommended for patients with normal renal function.

4.3 Contraindications

This drug is contraindicated in patients previously found to be hypersensitive to lincomycin or clindamycin. It is not indicated in the treatment of minor bacterial infections or viral infections.
Lincomycin is not indicated in the newborn.

4.4 Special Warnings and Precautions for Use

Lincomycin should not be injected IV as a bolus but should be infused as described (see Section 4.2 Dose and Method of Administration).

Risk of colitis.

The use of lincomycin can lead to the development of severe colitis. Fatalities have been reported. Therefore, lincomycin injection should be reserved for serious infections where less toxic antimicrobial agents are inappropriate (see Section 4.1 Therapeutic Indications). It should not be used in patients with non-bacterial infections such as most upper respiratory tract infections.
A toxin produced by 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 the use of antibiotics, including parenteral lincomycin. Symptoms may occur up to several weeks after cessation of antibiotic therapy.
Mild cases of pseudomembranous colitis 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.
Review of experience to date suggests that a subgroup of older patients with associated severe illness may tolerate diarrhoea less well. When lincomycin injection is indicated in these patients, they should be carefully monitored for change in bowel frequency.
Clostridium difficile associated diarrhoea (CDAD) has been reported with use of nearly all antibacterial agents, including lincomycin, and may range in severity from mild diarrhoea to fatal colitis. 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 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 antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.
Lincomycin injection should be prescribed with caution in individuals with a history of gastrointestinal disease, particularly colitis.

Allergies.

Lincomycin injection, like any drug, should be used with caution in patients with a history of asthma or significant allergies.

Hypersensitivity reactions.

Hypersensitivity reactions (such anaphylactic reaction, angioedema and serum sickness) have been reported, some of these in patients known to be sensitive to penicillin. If an allergic reaction should occur, the drug should be discontinued and the usual agents (adrenalin, corticosteroids, antihistamines) should be available for emergency treatment.
Severe hypersensitivity reactions, including anaphylactic reactions and severe cutaneous adverse reactions (SCAR) such as Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), acute generalised exanthematous pustulosis (AGEP), and erythema multiforme (EM) have been reported in patients receiving lincomycin therapy. If an anaphylactic reaction or severe skin reaction occurs, lincomycin should be discontinued and appropriate therapy should be initiated (see Section 4.8 Adverse Effects (Undesirable Effects)).

Superinfections.

The use of antibiotics occasionally results in overgrowth of non-susceptible organisms - particularly yeasts. Should superinfections occur, appropriate measures should be taken. When patients with pre-existing monilial infections require lincomycin injection therapy, concomitant antimonilial treatment should be given.

Monitoring.

During prolonged lincomycin injection therapy, periodic liver function and renal studies and blood counts should be performed.

Meningitis.

Although lincomycin appears to diffuse into cerebrospinal fluid, levels of lincomycin in the CSF may be inadequate for the treatment of meningitis. Thus, the drug should not be used in the treatment of meningitis.

Incompatibilities.

Lincomycin injection is incompatible with novobiocin, kanamycin and phenytoin.

Use in hepatic impairment.

In patients with impaired hepatic or renal function, the serum half-life of lincomycin is increased. Consideration should be given to decreasing the frequency and dose of lincomycin administered in patients with impaired hepatic or liver function.
Since adequate data are not yet available in patients with pre-existing liver disease, its use in such patients is not recommended at this time unless special clinical circumstances so indicate.

Use in renal impairment.

See Section 4.4 Special Warnings and Precautions for Use, Use in hepatic impairment.

Use in the elderly.

No data available.

Paediatric use.

Lincomycin injection contains benzyl alcohol which is associated with severe adverse effects, including fatal "Gasping Syndrome", in paediatric patients. The minimum amount of benzyl alcohol at which toxicity may occur is unknown. The risk of benzyl alcohol toxicity depends on the quantity administered and the liver and kidneys' capacity to detoxify the chemical. Premature and low birth weight infants may be more likely to develop toxicity.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Lincomycin injection has been shown to have neuromuscular blocking properties that may enhance the action of other neuromuscular blocking agents. Therefore, it should be used with caution in patients receiving such agents.
Antagonism has been demonstrated between lincomycin and erythromycin in vitro. Because of possible clinical significance, these two drugs should not be administered concurrently.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category A)
In humans, lincomycin crosses the placenta and results in cord serum levels about 25% of the maternal serum levels. No significant accumulation occurs in the amniotic fluid. There is limited data on the use of lincomycin in pregnant women. The progeny of 302 patients treated with lincomycin at various stages of pregnancy showed no increases in congenital anomalies or delayed development compared to a control group for up to 7 years after birth. Lincomycin should be used during pregnancy only if clearly needed. Lincomycin is not indicated in the newborn (see Section 4.3 Contraindications). Benzyl alcohol can cross the placenta (see Section 4.4 Special Warnings and Precautions for Use, Paediatric use).
No embryo fetal toxicity was observed in rats dosed with 10% lincomycin in the diet (equivalent to 5000 mg/kg/day) during organogenesis.
 Lincomycin injection has been reported to appear in breast milk in ranges of 0.5 to 2.4 microgram/mL. It should not, therefore, be used during lactation unless alternative arrangements can be made for feeding the baby.

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)

Adverse reactions are listed according to the following categories:
Very common: ≥ 1/10; Common: ≥ 1/100 to < 1/10; Uncommon: ≥ 1/1,000 to < 1/100; Rare: ≥ 1/10,000 to < 1/1,000; Very rare: < 1/10,000; Not known: cannot be estimated from available data.

Infections and infestations.

Uncommon: Vaginal infection. Not known: Pseudomembranous colitis, Clostridium difficile colitis.

Gastrointestinal disorders.

Common: Diarrhoea, vomiting, nausea. Rare: Stomatitis. Not known: Enterocolitis (see Section 4.4 Special Warnings and Precautions for Use), oesophagitisa, glossitis, abdominal discomfort.

Blood and lymphatic system disorders.

Not known: Pancytopenia, agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenic purpura.

Immune system disorders.

Not known: Anaphylactic reaction, angioedema, serum sickness (see Section 4.4 Special Warnings and Precautions for Use).

Skin and subcutaneous tissue disorders.

Uncommon: Rash, urticaria. Rare: Pruritus. Not known: Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalised exanthematous pustulosis, erythema multiforme, dermatitis bullous, dermatitis exfoliative, anal pruritus.

Hepatobiliary disorders.

Not known: Jaundice, liver function test abnormal, transaminases increased.

Renal and urinary disordersb.

Not known: Renal impairment, oliguria, proteinuria, azotaemia.

Cardiac disorders.

Not known: Cardio-respiratory arrestc.

Vascular disorders.

Not known: Hypotensiond, thrombophlebitise.

Ear and labyrinth disorders.

Not known: Vertigo, tinnitus.

General disorders and administration site conditions.

Not known: Injection site abscess sterilef, injection site indurationf, injection site painf, injection site irritationf.
a Reported with oral preparations.
b No direct relationship of lincomycin to renal damage has been established.
c Rare instances have been reported after too rapid intravenous administration.
d Following parenteral administration, particularly after too rapid administration.
e Reported with intravenous injection. This reaction can be minimised by avoidance of indwelling intravenous catheters.
f Reported with intramuscular injection. These reactions can be minimised by deep intramuscular injection.

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

The minimal toxic or lethal dose is not well established. At therapeutic doses, the primary toxic effects may involve the gastrointestinal tract and may include severe diarrhoea and pseudomembranous colitis that may result in death. Rapid administration of large doses has resulted in ventricular dysrhythmias, hypotension and cardiac arrest. Dermatitis, nephrotoxicity, hepatotoxicity, and various haematological abnormalities are toxic effects that occur less frequently.
No specific antidote is known. Support respiratory and cardiac function. In cases of overdose, drug levels of lincomycin are not clinically useful. However, monitoring serum concentrations in patients with markedly reduced renal and hepatic function may be indicated during high-dose therapy. Monitor full blood count in patients with significant exposure as lincomycin may produce abnormalities of the haematopoietic system. Because lincomycin may cause hepatotoxicity, monitor liver function tests in patients with significant exposure.
Haemodialysis and peritoneal dialysis are not effective in removing lincomycin from the serum.
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.

Microbiology. In vitro studies indicate that the following organisms are usually sensitive to concentrations achieved normally in the serum following recommended doses: Staphylococcus aureus, Staphylococcus epidermidis, beta-haemolytic Streptococcus, Streptococcus viridans, Streptococcus pneumoniae, Clostridium tetani, Clostridium perfringens, Corynebacterium diphtheriae.

Note.

The drug is not active against most strains of Enterococcus faecalis, nor against Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae or other gram-negative organisms or yeasts. Some strains of Clostridium perfringens and strains of some less common human pathogens of Clostridia may be lincomycin-resistant. Depending on the sensitivity of the organism and concentration of the antibiotic, it may be either bactericidal or bacteriostatic. Cross resistance has not been demonstrated with penicillin, chloramphenicol, ampicillin, cephalosporins or the tetracyclines. Despite chemical differences, lincomycin injection exhibits antibacterial activity similar but not identical to the macrolide antibiotics (e.g. erythromycin). Some cross-resistance (with erythromycin) including a phenomenon known as dissociated cross-resistance or macrolide effect has been reported. Microorganisms have not developed resistance to lincomycin injection rapidly when tested by in vitro or in vivo methods. Staphylococci develop resistance to lincomycin injection in a slow step-wise manner based on in vitro serial subculture experiments. Studies indicated that lincomycin injection does not share antigenicity with penicillin compounds.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

Lincomycin injection is absorbed rapidly after a 500 mg oral dose, reaching peak serum levels of 2-3 microgram/mL in 2 to 4 hours, which then diminish to approximately 1 microgram/mL in a further 4-8 hours. Doubling the dose increases but does not double the peak serum levels. Food in the stomach reduces total absorption as well as peak serum levels.

Distribution.

Significant levels have been demonstrated in the majority of body tissues. Although the drug is not present in significant amounts in the spinal fluid of normal volunteers, it has been demonstrated in the spinal fluid of one patient with pneumococcal meningitis.

Metabolism.

The excretion of lincomycin in urine and bile does not account for all the administered dose and a substantial proportion of the drug appears to be inactivated in the body, presumably in the liver.
The biological half-life, after oral, intramuscular or intravenous administration is 5.4 ± 1.0 hours.

Excretion.

Urinary recovery of drug in a 24-hour period ranges from 1.0 to 31 percent (mean: 4.0) after a single oral dose of 500 mg. Bile is an important route of excretion.
Intramuscular administration of a single dose of 600 mg produces a peak serum level of approximately 9-11.5 microgram/mL at 30 minutes with detectable levels persisting for 24 hours. Urinary excretion after this dose ranges from 1.8 to 24.8 percent (mean: 17.3).
The intravenous infusion over a 2-hour interval of 600 mg of lincomycin injection in 500 mL of 5 percent glucose in water yields therapeutic levels for 14 hours. Urinary excretion ranges from 4.9 to 30.3 percent (mean: 13.8).
Haemodialysis and peritoneal dialysis do not effectively remove lincomycin from the blood.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Benzyl alcohol 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 below 25°C. Protect from light. Do not freeze.

6.5 Nature and Contents of Container

Clear type 1 glass ampoules - packs of 5 ampoules/carton.

6.6 Special Precautions for Disposal

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

6.7 Physicochemical Properties

Lincomycin hydrochloride monohydrate consists mainly of methyl 6,8-dideoxy-6-[[[(2S,4R)-1-methyl-4-propylpyrrolidin-2-yl]carbonyl] amino]-1-thio-D-erythro-α-D-galacto-octopyranoside (lincomycin) hydrochloride monohydrate.
Lincomycin hydrochloride monohydrate is the monohydrated salt of lincomycin, a substance produced by the growth of a member of the lincolnensis group of Streptomyces lincolnensis (fam. Streptomycetaceae). It is a white, or practically white, crystalline powder and is odourless or has a faint odour. Its solutions are acid and are dextrorotatory. Lincomycin injection is freely soluble in water, soluble in dimethylformamide and very slightly soluble in acetone. The sum of the contents of lincomycin hydrochloride and lincomycin B hydrochloride is 96.0 per cent to 102.0 per cent (anhydrous substance).
The maximum content of lincomycin B hydrochloride is 5.0 per cent (anhydrous substance).
Lincomycin Injection is a clear, colourless or almost colourless solution, practically free from particles. pH - 3.0 to 5.5. pKa - 7.6. Octanol/Water Partition Coefficient log Kow = 0.20.

Chemical structure.


CAS number.

7179-49-9.

7 Medicine Schedule (Poisons Standard)

S4 Prescription Medicine.

Summary Table of Changes