Ceftal 500 mg Coated Tablets

Ireland - English - HPRA (Health Products Regulatory Authority)

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Active ingredient:
Cefuroxime
Available from:
Rowex Ltd
ATC code:
J01DC; J01DC02
INN (International Name):
Cefuroxime
Dosage:
500 milligram(s)
Pharmaceutical form:
Coated tablet
Prescription type:
Product subject to prescription which may not be renewed (A)
Therapeutic area:
Second-generation cephalosporins; cefuroxime
Authorization status:
Marketed
Authorization number:
PA0711/101/003
Authorization date:
2006-10-13

Package leaflet: Information for the patient

Ceftal 250 mg Coated Tablets

Ceftal 500 mg Coated Tablets

cefuroxime

Read all of this leaflet carefully before you start taking this medicine because it contains

important information for you.

Keep this leaflet. You may need to read it again.

If you have any further questions, ask your doctor or pharmacist.

This medicine has been prescribed for you only. Do not pass it on to others. It may harm them,

even if their signs of illness are the same as yours.

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side

effects not listed in this leaflet. See section 4.

What is in this leaflet

What Ceftal is and what it is used for

What you need to know before you take Ceftal

How to take Ceftal

Possible side effects

How to store Ceftal

Contents of the pack and other information

1.

What Ceftal is and what it is used for

Ceftal is an antibiotic used in adults and children. It works by killing bacteria that cause infections.

It belongs to a group of medicines called

cephalosporins

Ceftal is used to treat infections of:

the throat

sinus

middle ear

the lungs or chest

the urinary tract

the skin and soft tissues.

Ceftal can also be used:

to treat Lyme disease (an infection spread by parasites called ticks).

2.

What you need to know before you take Ceftal

Do not take Ceftal:

if you are allergic

to cefuroxime, to

any cephalosporin antibiotics

or any of the other

ingredients of this medicine (listed in section 6)

if you have ever had a severe allergic (hypersensitive) reaction to any other type of

beta-lactam antibiotic (penicillins, monobactams and carbapenems).

If you think this applies to you,

don’t take Ceftal

until you have checked with your doctor.

Warnings and precautions

Talk to your doctor, pharmacist or nurse before using Ceftal.

Ceftal

is not recommended for children aged under 3 months

, as the safety and effectiveness

are not known in this age group.

You must look out for certain symptoms, such as allergic reactions, fungal infections (such as

candida

) and severe diahorrea (

pseudomembranous colitis

) while you are taking Ceftal. This will

reduce the risk of any problems. See ‘Conditions you need to look out for’ in Section 4.

If you need a blood test

Ceftal can affect the results of a test for blood sugar levels, or a blood screen called the

Coombs test

If you need a blood test:

Tell the person taking the sample

that you are taking Ceftal.

Other medicines and Ceftal

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicine.

This includes medicines you can obtain without a prescription.

Medicines used to

reduce the amount of acid in your stomach

(e.g.

antacids

used to treat

heartburn

) can affect how Ceftal works.

Probenecid

Oral anticoagulants

Tell your doctor or pharmacist

if you are taking any medicine like this.

Pregnancy, breast-feeding and fertility

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask

your doctor or pharmacist for advice before taking this medicine.

Your doctor will consider the benefit of treating you with Ceftal against the risk to your baby.

Driving and using machines

Ceftal can make you dizzy

and have other side effects that make you less alert.

Don’t drive or use machines

if you do not feel well.

Ceftal coated

tablets contain aspartame and sodium.

250 mg:

This medicine contains 0.3 mg aspartame in each coated tablet.

500 mg:

This medicine contains 0.4 mg aspartame in each coated tablet.

Aspartame is a source of phenylalanine. It may be harmful if you have phenylketonuria (PKU), a

rare genetic disorder in which phenylalanine builds up because the body cannot remove it

properly. This medicine contains less than 1 mmol sodium (23 mg) per coated tablet, that is to say

essentially ‘sodium-free’.

3.

How to take Ceftal

Always take this medicine exactly as your doctor or pharmacist has told you

. Check with your

doctor or pharmacist if you are not sure.

Take Ceftal after food.

This will help to make the treatment more effective.

Swallow Ceftal tablets with some water.

The recommended dose is:

Adults

The usual dose of Ceftal is 250 mg to 500 mg twice daily depending on the severity and type of

infection.

Use in children and adolescents

The usual dose of Ceftal is 10 mg/kg (to a maximum of 125 mg) to 15 mg/kg (to a maximum of

250 mg) twice daily depending on:

the severity and type of infection.

Ceftal

is not recommended for children aged under 3 months

, as the safety and effectiveness are

not known in this age group.

Depending on the illness or how you or your child responds to treatment, the initial dose may be

changed or more than one course of treatment may be needed.

Patients with kidney problems

If you have a kidney problem, your doctor may change your dose.

Talk to your doctor

if this applies to you.

If you take more Ceftal than you should

If you take too much Ceftal you may have neurological disorders, in particular you may be

more

likely to have fits (seizures).

Don't delay. Contact your doctor or your nearest hospital emergency department

immediately

. If possible, show them the Ceftal pack.

If you forget to take Ceftal

Don't take a double dose to make up for a forgotten dose

. Just take your next dose at the usual

time.

If you stop taking Ceftal

Don’t stop Ceftal without advice.

It is important that you take the full course of Ceftal.

Don’t stop unless your doctor advises you to

– even if you are feeling better. If you don't complete the full course of treatment, the infection may

come back.

If you have any further questions on the use of this medicine, ask your doctor or pharmacist.

4.

Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them.

Conditions you need to look out for

A small number of people taking Ceftal get an allergic reaction or potentially serious skin reaction.

Symptoms of these reactions include:

severe allergic reaction

. Signs include

raised and itchy rash

swelling

, sometimes of the face or

mouth causing

difficulty in breathing

skin rash,

which may

blister

, and looks like

small targets

(central dark spot surrounded by a

paler area, with a dark ring around the edge).

a widespread rash

with

blisters

peeling skin.

(These may be signs of

Stevens-Johnson

syndrome

toxic epidermal necrolysis

fungal infections.

Medicines like Ceftal can cause an overgrowth of yeast (

Candida

) in the body

which can lead to fungal infections (such as thrush). This side effect is more likely if you take

Ceftal for a long time.

severe diarrhoea (Pseudomembranous colitis).

Medicines like Ceftal can cause inflammation of

the colon (large intestine), causing severe diarrhoea, usually with blood and mucus, stomach pain,

fever.

Jarisch-Herxheimer reaction.

Some patients may get a high temperature (fever), chills,

headache, muscle pain and skin rash while being treated with Ceftal for Lyme disease. This is

known as the

Jarisch-Herxheimer reaction.

Symptoms usually last a few hours or up to one day.

Contact a doctor or nurse immediately if you get any of these symptoms.

Common side effects

These may affect

up to 1 in 10

people:

fungal infections (such as

Candida

headache

dizziness

diarrhoea

feeling sick

stomach pain.

Common side effects that may show up in blood tests:

an increase in a type of white blood cell (

eosinophilia

an increase in liver enzymes.

Uncommon side effects

These may affect

up to 1 in 100

people:

being sick

skin rashes.

Uncommon side effects that may show up in blood tests:

a decrease in the number of blood platelets (cells that help blood to clot)

a decrease in the number of white blood cells

positive Coomb’s test.

Other side effects

Other side effects have occurred in a very small number of people, but their exact frequency is

unknown:

severe diarrhoea (

pseudomembranous colitis

allergic reactions

skin reactions (including severe)

high temperature (

fever

yellowing of the whites of the eyes or skin

inflammation of the liver (

hepatitis

Side effects that may show up in blood tests:

red blood cells destroyed too quickly (

haemolytic anaemia).

Reporting of side effects

If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side

effects not listed in this leaflet. You can also report side effects directly via HPRA Pharmacovigilance,

Earlsfort Terrace, IRL - Dublin 2; Tel: +353 1 6764971; Fax: +353 1 6762517. Website: www.hpra.ie;

E-mail: medsafety@hpra.ie. By reporting side effects you can help provide more information on the

safety of this medicine.

5.

How to store Ceftal

Keep this medicine out of the sight and reach of children.

Do not use this medicine after the expiry date which is stated on the label and carton after EXP. The

expiry date refers to the last day of that month.

Store in the original packaging in order to protect from moisture.

This medicine does not require any special temperature storage conditions.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to

throw away medicines you no longer use. These measures will help protect the environment.

6.

Contents of the pack and other information

What Ceftal contains

The active substance is cefuroxime.

Ceftal 250 mg contains 300.72 mg of cefuroxime axetil per coated tablet equivalent to 250 mg of

cefuroxime.

Ceftal 500 mg contains 601.44 mg of cefuroxime axetil per coated tablet (equivalent to 500 mg of

cefuroxime).

The other ingredients (excipients) are: sodium laurylsulfate, copovidone, croscarmellose sodium

(E468), magnesium stearate (E470B), anhydrous colloidal silicon dioxide (E551), mannitol

(E421), microcrystalline cellulose (E460), crospovidone (E1202) and talc (E553B), mannitol

(E421), soluble (potato) starch, titanium dioxide (E171) and aspartame (E951).

What Ceftal

looks like and contents of the pack

Ceftal tablets are coated.

Ceftal 250 mg coated tablets are white to slightly yellowish, biconvex, oblong tablets scored on both

sides.

Ceftal 500 mg coated tablets are white to slightly yellowish, biconvex, oblong tablets.

Ceftal 250 mg coated tablets are available in carton boxes with blister(s) tear-off or strips containing 8,

10, 12, 14 and 24 coated tablets.

Ceftal 500 mg coated tablets are available in carton boxes with blister(s) tear-off or strips containing 6,

8, 10, 12, 14 and 24 coated tablets.

Not all pack sizes may be marketed.

Marketing Authorisation Holder and Manufacturer

Marketing Authorisation Holder

Rowex Ltd., Bantry, Co. Cork, Ireland.

Manufacturer

Sandoz GmbH, Biochemiestrasse 10, 6250 Kundl, Austria.

This medicinal product is authorised in the Member States of the EEA under the following

names:

Austria

Ceforoxim Hexal 250 mg – Filmtabletten

Ceforoxim Hexal 500 mg – Filmtabletten

Ireland

Ceftal 250 mg Coated Tablets

Ceftal 500 mg Coated Tablets

Italy

CEFUROXIMA SANDOZ

CEFUROXIMA SANDOZ

CEFUROXIMA SANDOZ

Netherlands

CEFUROXIMAXETIL 125, omhulde tabletten 125 mg

CEFUROXIMAXETIL 250, omhulde tabletten 250 mg

CEFUROXIMAXETIL 500, omhulde tabletten 500 mg

This leaflet is last revised in 05/2019.

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Summary of Product Characteristics

1 NAME OF THE MEDICINAL PRODUCT

Ceftal 500 mg Coated Tablets

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Each 500 mg coated tablet contains 601.44 mg cefuroxime (as axetil).

Excipients with known effect:

Each coated tablet contains 0.4 mg aspartame (E951).

For the full list of excipients, see section 6.1.

3 PHARMACEUTICAL FORM

Coated tablets

White to slightly yellowish, biconvex, oblong tablets

4 CLINICAL PARTICULARS

4.1 Therapeutic Indications

Ceftal is indicated for the treatment of the infections listed below in adults and children from the age of 3 months (see sections

4.4 and 5.1).

- Acute streptococcal tonsillitis and pharyngitis.

- Acute bacterial sinusitis.

- Acute otitis media.

- Acute exacerbations of chronic bronchitis.

- Cystitis

- Pyelonephritis.

- Uncomplicated skin and soft tissue infections.

- Treatment of early Lyme disease.

Consideration should be given to official guidance on the appropriate use of antibacterial agents.

4.2 Posology and method of administration

Posology

The usual course of therapy is seven days (may range from five to ten days).

Table 1. Adults and children (≥40 kg)

Indication

Dosage

Acute tonsillitis and pharyngitis, acute bacterial sinusitis

250 mg twice daily

Acute otitis media

500 mg twice daily

Acute exacerbations of chronic bronchitis

500 mg twice daily

Cystitis

250 mg twice daily

Pyelonephritis

250 mg twice daily

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Uncomplicated skin and soft tissue infections

250 mg twice daily

Lyme disease

500 mg twice daily for 14 days (range of 10 to 21 days)

Table 2. Children (<40 kg)

Indication

Dosage

Acute tonsillitis and pharyngitis, acute bacterial sinusitis

10 mg/kg twice daily to a maximum of 125 mg twice daily

Children aged two years or older with otitis media or,

where appropriate, with more severe infections

15 mg/kg twice daily to a maximum of 250 mg twice daily

Cystitis

15 mg/kg twice daily to a maximum of 250 mg twice daily

Pyelonephritis

15 mg/kg twice daily to a maximum of 250 mg twice daily for 10 to 14

days

Uncomplicated skin and soft tissue infections

15 mg/kg twice daily to a maximum of 250 mg twice daily

Lyme disease

15 mg/kg twice daily to a maximum of 250 mg twice daily for 14 days

(10 to 21 days)

There is no experience of using Ceftal in children under the age of 3 months.

Renal impairment

The safety and efficacy of cefuroxime axetil in patients with renal failure have not been established.

Cefuroxime is primarily excreted by the kidneys. In patients with markedly impaired renal function it is recommended that the

dosage of cefuroxime should be reduced to compensate for its slower excretion. Cefuroxime is effectively removed by dialysis.

Table 3. Recommended doses for Ceftal in renal impairment

Creatinine clearance

T

1/2

(hrs)

Recommended dosage

≥30 mL/min/1.73 m

1.4–2.4

no dose adjustment necessary (standard dose of 125 mg to 500 mg given twice daily)

10-29 mL/min/1.73 m

standard individual dose given every 24 hours

<10 mL/min/1.73 m

16.8

standard individual dose given every 48 hours

Patients on haemodialysis

2–4

a further standard individual dose should be given at the end of each dialysis

Hepatic impairment

There are no data available for patients with hepatic impairment. Since cefuroxime is primarily eliminated by the kidney, the

presence of hepatic dysfunction is expected to have no effect on the pharmacokinetics of cefuroxime.

Method of administration

Oral use

Ceftal tablets should be taken after food for optimum absorption.

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

Patients with known hypersensitivity to cephalosporin antibiotics.

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History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins,

monobactams and carbapenems).

4.4 Special warnings and precautions for use

Hypersensitivity reactions

Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactam antibiotics

because there is a risk of cross-sensitivity. As with all beta-lactam antibacterial agents, serious and occasionally fatal

hypersensitivity reactions have been reported. In case of severe hypersensitivity reactions, treatment with cefuroxime must be

discontinued immediately and adequate emergency measures must be initiated.

Before beginning treatment, it should be established whether the patient has a history of severe hypersensitivity reactions to

cefuroxime, to other cephalosporins or to any other type of beta-lactam agent. Caution should be used if cefuroxime is given

to patients with a history of non-severe hypersensitivity to other beta-lactam agents.

Jarisch-Herxheimer reaction

The Jarisch-Herxheimer reaction has been seen following cefuroxime axetil treatment of Lyme disease. It results directly from

the bactericidal activity of cefuroxime axetil on the causative bacteria of Lyme disease, the spirochaete Borrelia burgdorferi.

Patients should be reassured that this is a common and usually self-limiting consequence of antibiotic treatment of Lyme

disease (see section 4.8).

Overgrowth of non-susceptible microorganisms

As with other antibiotics, use of cefuroxime axetil may result in the overgrowth of Candida. Prolonged use may also result in

the overgrowth of other non-susceptible microorganisms (e.g. enterococci and Clostridium difficile), which may require

interruption of treatment (see section 4.8).

Antibacterial agent–associated pseudomembranous colitis have been reported with nearly all antibacterial agents, including

cefuroxime and may range in severity from mild to life threatening. This diagnosis should be considered in patients with

diarrhoea during or subsequent to the administration of cefuroxime (see section 4.8). Discontinuation of therapy with

cefuroxime and the administration of specific treatment for Clostridium difficile should be considered. Medicinal products that

inhibit peristalsis should not be given (see section 4.8).

Interference with diagnostic tests

The development of a positive Coomb's Test associated with the use of cefuroxime may interfere with cross matching of blood

(see section 4.8).

As a false negative result may occur in the ferricyanide test, it is recommended that either the glucose oxidase or hexokinase

methods are used to determine blood/plasma glucose levels in patients receiving cefuroxime axetil.

Ceftal contains aspartame and sodium

Aspartame is a source of phenylalanine. It may be harmful to patients with phenylketonuria (PKU). Neither non-clinical nor

clinical data are available to assess aspartame use in infants below 12 weeks of age.

This medicine contains less than 1 mmol sodium (23 mg) per coated tablet, that is to say essentially 'sodium-free'.

4.5 Interaction with other medicinal products and other forms of interactions

Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil compared with that of the fasting

state and tend to cancel the effect of enhanced absorption after food.

Cefuroxime is excreted by glomerular filtration and tubular secretion. Concomitant use of probenecid is not recommended.

Concurrent administration of probenecid significantly increases the peak concentration, area under the serum concentration

time curve and elimination half-life of cefuroxime.

Concomitant use with oral anticoagulants may give rise to increased INR.

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4.6 Fertility, pregnancy and lactation

Pregnancy

There are limited data from the use of cefuroxime in pregnant women. Studies in animals have shown no harmful effects on

pregnancy, embryonal or foetal development, parturition or postnatal development. Ceftal should be prescribed to pregnant

women only if the benefit outweighs the risk.

Breastfeeding

Cefuroxime is excreted in human milk in small quantities. Adverse effects at therapeutic doses are not expected, although a risk

of diarrhoea and fungus infection of the mucous membranes cannot be excluded. Breastfeeding might have to be

discontinued due to these effects. The possibility of sensitisation should be taken into account. Cefuroxime should only be

used during breastfeeding after benefit/risk assessment by the physician in charge.

Fertility

There are no data on the effects of cefuroxime axetil on fertility in humans. Reproductive studies in animals have shown no

effects on fertility.

4.7 Effects on ability to drive and use machines

No studies on the effects on the ability to drive and use machines have been performed. However, as this medicine may cause

dizziness, patients should be warned to be cautious when driving or operating machinery.

4.8 Undesirable effects

The most common adverse reactions are Candida overgrowth, eosinophilia, headache, dizziness, gastrointestinal disturbances

and transient rise in liver enzymes.

The frequency categories assigned to the adverse reactions below are estimates, as for most reactions suitable data (for

example from placebo-controlled studies) for calculating incidence were not available. In addition the incidence of adverse

reactions associated with cefuroxime axetil may vary according to the indication.

Data from large clinical studies were used to determine the frequency of very common to rare undesirable effects. The

frequencies assigned to all other undesirable effects (i.e. those occurring at <1/10,000) were mainly determined using

post-marketing data and refer to a reporting rate rather than true frequency. Placebo-controlled trial data were not available.

Where incidences have been calculated from clinical trial data, these were based on drug-related (investigator assessed) data.

Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.

Treatment related adverse reactions, all grades, are listed below by MedDRA body system organ class, frequency and grade of

severity. The following convention has been utilised for the classification of frequency: 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 and not known (cannot be

estimated from the available data).

System organ

class

Common

Uncommon

Not known

Infections and infestations

Candida

overgrowth

Clostridium difficile overgrowth

Blood and lymphatic system disorders

eosinophilia

positive Coomb’s test,

thrombocytopenia,

leukopenia (sometimes

profound)

haemolytic anaemia

Immune system disorders

drug fever, serum sickness,

anaphylaxis, Jarisch-Herxheimer

reaction

Nervous system disorders

headache,

dizziness

Gastrointestinal disorders

diarrhoea,

nausea,

abdominal

vomiting

pseudomembranous colitis

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System organ

class

Common

Uncommon

Not known

pain

Hepatobiliary disorders

transient

increases of

hepatic

enzyme

levels

jaundice (predominantly

cholestatic), hepatitis

Skin and subcutaneous tissue disorders

skin rashes

urticaria, pruritus, erythema

multiforme, Stevens-Johnson

syndrome, toxic epidermal

necrolysis (exanthematic

necrolysis) (see Immune system

disorders), angioneurotic oedema

Description of selected adverse reactions

Cephalosporins as a class tend to be absorbed onto the surface of red cells membranes and react with antibodies directed

against the drug to produce a positive Coombs’ test (which can interfere with cross-matching of blood) and very rarely

haemolytic anaemia.

Transient rises in serum liver enzymes have been observed which are usually reversible.

Paediatric population

The safety profile for cefuroxime axetil in children is consistent with the profile in adults.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation 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 via HPRA Pharmacovigilance, Earlsfort Terrace, IRL - Dublin 2; Tel: +353 1 6764971; Fax: +353 1 6762517.

Website: www.hpra.ie; E-mail: medsafety@hpra.ie.

4.9 Overdose

Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can

occur if the dose is not reduced appropriately in patients with renal impairment (see sections 4.2 and 4.4).

Serum levels of cefuroxime can be reduced by haemodialysis and peritoneal dialysis.

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: antibacterials for systemic use, second-generation cephalosporins, ATC-Code: J01DC02

Mechanism of action

Cefuroxime axetil undergoes hydrolysis by esterase enzymes to the active antibiotic, cefuroxime.

Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the

interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.

Mechanism of resistance

Bacterial resistance to cefuroxime may be due to one or more of the following mechanisms:

hydrolysis by beta-lactamases; including (but not limited to) by extended-spectrum beta-lactamases (ESBLs), and AmpC

enzymes that may be induced or stably derepressed in certain aerobic Gram-negative bacteria species;

reduced affinity of penicillin-binding proteins for cefuroxime;

outer membrane impermeability, which restricts access of cefuroxime to penicillin binding proteins in Gram-negative

bacteria;

bacterial efflux pumps.

Organisms that have acquired resistance to other injectable cephalosporins are expected to be resistant to cefuroxime.

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Depending on the mechanism of resistance, organisms with acquired resistance to penicillins may demonstrate reduced

susceptibility or resistance to cefuroxime.

Cefuroxime axetil breakpoints

Minimum inhibitory concentration (MIC) breakpoints established by the European Committee on Antimicrobial Susceptibility

Testing (EUCAST) are as follows:

Microorganism

Breakpoints (mg/L)

Enterobacteriaceae

1, 2

≤8

>8

Staphylococcus spp.

Note

Note

Streptococcus A, B, C and G

Note

Note

Streptococcus pneumoniae

≤0.25

>0.5

Moraxella catarrhalis

≤0.125

>4

Haemophilus influenzae

≤0.125

>1

Non-species related breakpoints

1

The cephalosporin breakpoints for Enterobacteriaceae will

detect all clinically important resistance mechanisms (including

ESBL and plasmid mediated AmpC). Some strains that produce

beta-lactamases are susceptible or intermediate to 3rd or 4th

generation cephalosporins with these breakpoints and should

be reported as found, i.e. the presence or absence of an ESBL

does not in itself influence the categorization of susceptibility. In

many areas, ESBL detection and characterization is

recommended or mandatory for infection control purposes.

Uncomplicated UTI (cystitis) only (see section 4.1).

Susceptibility of staphylococci to cephalosporins is inferred

from the methicillin susceptibility except for ceftazidme and

cefixime and ceftibuten, which do not have breakpoints and

should not be used for staphylococcal infections.

The beta-lactam susceptibility of beta-haemolytic streptococci

groups A, B, C and G is inferred from the penicillin susceptibility.

insufficient evidence that the species in question is a good

target for therapy with the drug.

An MIC with a comment but without an accompanying S or

R-categorization may be reported.

S=susceptible, R=resistant

Microbiological susceptibility

The prevalence of acquired resistance may vary geographically and with time for selected species and local information on

resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local

prevalence of resistance is such that the utility of cefuroxime axetil in at least some types of infections is questionable.

Cefuroxime is usually active against the following microorganisms in vitro.

Commonly susceptible species

Gram-positive aerobes:

Staphylococcus aureus (methicillin-susceptible)*

Coagulase negative staphylococcus (methicillin susceptible)

Streptococcus pyogenes

Streptococcus agalactiae

Gram-negative aerobes:

Haemophilus influenzae

Haemophilus parainfluenzae

Moraxella catarrhalis

Spirochaetes:

Borrelia burgdorferi

Microorganisms for which acquired resistance may be a problem

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Gram-positive aerobes:

Streptococcus pneumoniae

Gram-negative aerobes:

Citrobacter freundii

Enterobacter aerogenes

Enterobacter cloacae

Escherichia coli

Klebsiella pneumoniae

Proteus mirabilis

Proteus spp. (other than P. vulgaris)

Providencia spp.

Gram-positive anaerobes:

Peptostreptococcus spp.

Propionibacteriumspp.

Gram-negative anaerobes:

Fusobacterium spp.

Bacteroides spp.

Inherently resistant microorganisms

Gram-positive aerobes:

Enterococcus faecalis

Enterococcus faecium

Gram-negative aerobes:

Acinetobacter spp.

Campylobacter spp.

Morganella morganii

Proteus vulgaris

Pseudomonas aeruginosa

Serratia marcescens

Gram-negative anaerobes:

Bacteroides fragilis

Others:

Chlamydia spp.

Mycoplasma spp.

Legionella spp.

* All methicillin-resistant S. aureus are resistant to cefuroxime.

5.2 Pharmacokinetic properties

Absorption

After oral administration cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal

mucosa and blood to release cefuroxime into the circulation. Optimum absorption occurs when it is administered shortly after

a meal.

Following administration of cefuroxime axetil tablets peak serum levels (2.9 μg/mL for a 125 mg dose, 4.4 μg/mL for a 250 mg

dose, 7.7 μg/mL for a 500 mg dose and 13.6 μg/mL for a 1000 mg dose) occur approximately 2.4 hours after dosing when

taken with food. The pharmacokinetics of cefuroxime is linear over the oral dosage range of 125 to 1000 mg. No accumulation

of cefuroxime occurred following repeat oral doses of 250 to 500 mg.

Distribution

Protein binding has been stated as 33 to 50% depending on the methodology used. Following a single dose of cefuroxime

axetil 500 mg tablet to 12 healthy volunteers, the apparent volume of distribution was 50 L (CV%=28%). Concentrations of

cefuroxime in excess of the minimum inhibitory levels for common pathogens can be achieved in the tonsilla, sinus tissues,

bronchial mucosa, bone, pleural fluid, joint fluid, synovial fluid, interstitial fluid, bile, sputum and aqueous humor. Cefuroxime

passes the blood-brain barrier when the meninges are inflamed.

Biotransformation

Cefuroxime is not metabolised.

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Elimination

The serum half-life is between 1 and 1.5 hours. Cefuroxime is excreted by glomerular filtration and tubular secretion. The renal

clearance is in the region of 125 to 148 mL/min/1.73 m

Special patient populations

Gender

No differences in the pharmacokinetics of cefuroxime were observed between males and females.

Elderly

No special precaution is necessary in the elderly patients with normal renal function at dosages up to the normal maximum of

1 g per day. Elderly patients are more likely to have decreased renal function; therefore, the dose should be adjusted in

accordance with the renal function in the elderly (see section 4.2).

Paediatric population

In older infants (aged >3 months) and in children, the pharmacokinetics of cefuroxime are similar to that observed in adults.

There is no clinical trial data available on the use of cefuroxime axetil in children under the age of 3 months.

Renal impairment

The safety and efficacy of cefuroxime axetil in patients with renal failure have not been established.

Cefuroxime is primarily excreted by the kidneys. Therefore, as with all such antibiotics, in patients with markedly impaired renal

function (i.e. C1cr <30 mL/minute) it is recommended that the dosage of cefuroxime should be reduced to compensate for its

slower excretion (see section 4.2). Cefuroxime is effectively removed by dialysis.

Hepatic impairment

There are no data available for patients with hepatic impairment. Since cefuroxime is primarily eliminated by the kidney, the

presence of hepatic dysfunction is expected to have no effect on the pharmacokinetics of cefuroxime.

PK/PD relationship

For cephalosporins, the most important pharmacokinetic-pharmacodynamic index correlating with in vivo efficacy has been

shown to be the percentage of the dosing interval (%T) that the unbound concentration remains above the minimum inhibitory

concentration (MIC) of cefuroxime for individual target species (i.e. %T>MIC).

5.3 Preclinical safety data

Non-clinical data reveal no special hazard for humans based on studies of safety pharmacology, repeated dose toxicity,

genotoxicity and toxicity to reproduction and development. No carcinogenicity studies have been performed; however, there is

no evidence to suggest carcinogenic potential.

Gamma glutamyl transpeptidase activity in rat urine is inhibited by various cephalosporins, however the level of inhibition is

less with cefuroxime. This may have significance in the interference in clinical laboratory tests in humans.

6 PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Sodium laurylsulfate, copovidone

Croscarmellose sodium (E468)

Magnesium stearate (E470B)

Colloidal anhydrous silica (E551)

Granulated mannitol (E421)

Microcrystalline cellulose (E460)

Crospovidone (E1202)

Talc (E553B)

Mannitol (E421)

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Soluble starch (potato)

Titanium dioxide (E171)

Aspartame (E951)

6.2 Incompatibilities

Not applicable

6.3 Shelf life

Al/Al strip: 3 years

Al/Al blister: 3 years

6.4 Special precautions for storage

Al/Al strip: Store in the original packaging in order to protect from moisture

Al/Al blister: Store in the original packaging in order to protect from moisture

This medicinal product does not require any special temperature storage conditions

6.5 Nature and contents of container

Al/Al strip packaging

Al/Al blister packaging

Pack sizes:

125 mg: 8, 10, 12, 14, 24 tablets

250 mg: 8, 10, 12, 14, 24 tablets

500 mg: 6, 8, 10, 12, 14, 24 tablets

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

7 MARKETING AUTHORISATION HOLDER

Rowex Ltd

Newtown

Bantry

Co. Cork

Ireland

8 MARKETING AUTHORISATION NUMBER

PA0711/101/003

9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

Date of first authorisation: 13 October 2006

Date of last renewal: 26 January 2010

10 DATE OF REVISION OF THE TEXT

October 2019

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