Phenoxymethylpenicillin 125mg/5ml Oral Solution
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Phenoxymethylpenicillin 125 mg/5mL Oral Solution
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
5 ml of reconstituted syrup contain:
Phenoxymethylpenicillin potassium equivalent to phenoxymethylpenicillin 125 mg For a full list of excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Powder for oral solution
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Phenoxymethylpenicillin potassium is an orally active penicillin indicated for treatment of mild to moderately severe infections associated with microorganisms whose susceptibility to penicillin is within the range of serum levels attained with the dosage form.
Phenoxymethylpenicillin should not be used for serious infections because absorption can be unpredictable and plasma concentrations variable.
Lower respiratory tract: pneumonia, bronchitis
Upper respiratory tract: bacterial pharyngitis, otitis media
Others: skin and soft tissues infections, scarlatina, erysipelas, Vincent’s gingivitis, prophylaxis of rheumatic fever/or choreaand pneumococcal infection prophylaxis in asplenia or patients with sickle cell disease.
Consideration should be given to official guidance on the appropriate use of antibacterial agents.
4.2 Posology and method of administration
Posology
The dose will depend upon the severity, type and site of infection. In general the treatment must be continued 2-3 days after improvement of the symptoms.
To avoid late complications (rheumatic fever), infections with P-haemolytic streptococci should be treated for 10 days.
The treatment of acute otitis media with penicillin V should be limited to 5 days. However, 5-10 days treatment may be recommended in patients with potential for complications.
For children
Up to 1 year of age: 62.5 mg every 6 hours 1-5 years of age: 125 mg every 6 hours 6-12 years of age: 250 mg every 6 hours
For adults (including elderly)
250-500 mg every 6 hours
Prevention of recurrence of rheumatic fever/ chorea: 250mg twice daily on a continuing basis
Prevention of pneumococcal infection in asplenia or sickle cell disease:
Adult: 500mg every 12 hours
Child under 5 years: 125mg every 12 hours
Child 6-12 years: 250mg every 12 hours
Elderly
The dosage should be reduced if renal function is markedly impaired.
Special dosage:
Administer with caution in the presence of markedly impaired renal function due to the increased risk of encephalopathy. As a safe dosage may be lower than usually recommended.
The elimination of phenoxymethylpenicillin potassium is reduced in case of renal insufficiency. The dose interval should be adjusted to every 8 hours to 12 hours according to the severity of renal impairment.
Dosage adjustment may be necessary in patients with impaired liver function when they also have renal failure. In this situation the liver may be a major excretion route.
The recommended dose is to be taken about half an hour before meals or 2 hours after food, as ingestion of Phenoxymethylpenicillin with meals slightly reduces the absorption of the drug.
Method of Administration
For instructions on dilution of the product before administration, see section 6.6.
4.3 Contraindications
Phenoxymethylpenicillin potassium should not be given to patients with a history of penicillin hypersensitivity. Penicillin or any of the excipients contained in the product and should be used with caution in patients with known histories of allergy.
Attention should be paid to possible cross-sensitivity with other beta-lactam antibiotics e.g. cephalosporms. Severe acute infections should not be treated with phenoxymethylpenicillin.
4.4 Special warnings and precautions for use
Penicillin should be used with caution in individuals with histories of significant allergies and/or asthma.
All degrees of hypersensitivity, including fatal anaphylaxis, have been observed with oral penicillin. Cross sensitivity may occur with cephalosporins and other beta lactam antibiotics. These reactions are more likely to occur in individuals with a history of sensitivity to penicillins, cephalosporins and other allergens.
Enquiry should be made for such a history before therapy with a penicillin begins. If any allergic reaction occurs, the drug should be discontinued and the patient treated with the usual agents (e.g. adrenaline and other pressor amines, antihistamines and corticosteroids).
Oral therapy should not be relied upon in patients with severe illness, or with nausea, vomiting, gastric dilation, cardiospasm, achalasia or intestinal hypermotility.
Occasionally, patients do not absorb therapeutic amounts of orally administered penicillin.
Streptococcal infections should be treated for a minimum of 10 days, and post therapy cultures should be performed to confirm the eradication of the organisms.
Prolonged use of antibiotics may promote the overgrowth of non-susceptible organisms, including fungi. If super-infection occurs, appropriate measures should be taken.
Caution should be used when treating patients with a history of antibiotic-associated colitis.
Severe empyema, bacteraemia, pericarditis, meningitis and arthritis should not be treated with phenoxymethylpenicillin during the acute phase.
Patients with a past history of rheumatic fever receiving continuous prophylaxis may harbour penicillin-resistant organisms. In these patients, the use of another prophylactic agent should be considered.
Oral penicillin should not be used as adjunctive prophylaxis for genito - urinary instrumentation or surgery, lower intestinal tract surgery, sigmoidoscopy and child birth.
4.5 Interaction with other medicinal products and other forms of interaction
Probenecid delays the elimination of penicillin through the kidneys and thus prolongs its action.
Phenoxymethylpenicillin reduces the excretion of the cytotoxic drug, methotrexate thereby increasing the risk of toxicity.
Avoid concomitant administration with bacteriostatic antibiotics such as tetracycline, erythromycin, chloramphenicol and sulphonamides because it can diminish the effect of phenoxymethylpenicillin potassium.
In case of simultaneous administration of phenoxymethylpenicillin and oral contraceptives, the hormonal contraception can lose its efficacy. Patients should be advised to use additional forms of contraceptive precautions while taking phenoxymethylpenicillin.
The simultaneous administration of guar gum diminishes the absorption of penicillins.
Aminoglycosides: Neomycin is reported to reduce the absorption of phenoxymethylpenicillin.
Anticoagulants: Penicillins may interfere with anticoagulant control.
Sulfinpyrazone: Excretion of penicillins reduced by sulfinpyrazone.
Typhoid vaccine (oral): Penicillins may inactivate oral typhoid vaccine if ingested concomitantly.
4.6 Fertility, pregnancy and lactation
Pregnancy:
Animal studies with phenoxymethylpenicillin potassium have shown no teratogenic effects. Phenoxymethylpenicillin potassium has been in extensive clinical use and suitability in human pregnancy has been well documented in clinical studies.
However, as with other drugs, caution should be exercised when prescribing to pregnant patients.
Breast-feeding
Breast feeding is not contraindicated with phenoxymethylpenicillin potassium. Trace quantities of phenoxymethylpenicillin potassium can be detected in breast milk. While adverse effects are apparently rare, two potential problems exist for nursing infant:
- modification of bowel flora
- direct effects on the infant such as allergy/sensitization
Caution should therefore be exercised when prescribing for the nursing mother.
4.7 Effects on ability to drive and use machines
None known.
4.8 Undesirable effects
|
System Organ Class |
Frequency |
Adverse Event |
|
Immune system disorders |
Common |
Allergic reactions (typically manifest as skin reactions (See Skin and subcutaneous disorders). |
|
Rare |
Severe allergic reactions causing angioedema, laryngeal oedema, anaphylaxis | |
|
Not known |
Urticaria, fever, arthralgia (joint pains), rashes, serum sickness like reactions, haemolytic anaemia and interstitial nephritis, chills and oedema | |
|
Renal and urinary disorders |
Very rare |
Interstitial nephritis |
|
Uncommon |
Nephropathy (usually associated with high doses of parenteral penicillin) | |
|
Hepatobiliary disorders |
Very Rare |
Cholestatic jaundice and hepatitis |
|
Gastro-intestinal tract |
Common |
Nausea and/or vomiting, abdominal pains, severe and persistent diarrhoeas, soft stools |
|
Not known |
Sore mouth and black hairy tongue (discolouration of tongue) |
|
Blood and lymphatic |
Very rare |
changes in blood counts, |
|
system disorders |
including, neutropenia, leucopenia, eosinophilia,thrombocytopenia, haemolytic anaemia. | |
|
Not known |
Coagulation disorders (including prolongation of bleeding time and defective platelet function), neuropathy, and nephropathy (usually associated with high doses of parenteral penicillin) | |
|
Skin and subcutaneous |
Common |
Urticarial, erythematous or |
|
tissue |
mobilliform rash and pruritus | |
|
disorders |
Rare |
Exfoliative dermatitis, |
|
Nervous system disorders |
Not known |
Central nervous system toxicity, including convulsions , has been reported, especially following high doses or in severe renal impairment. Paraesthesia has been reported with prolonged use. Neuropathy (usually associated with high doses of parenteral penicillin) |
|
Infections and infestations |
Not known |
Pseudomembranous colitis |
Hypersensitivity
Although reactions have been reported much less frequently after oral than after parenteral therapy, it should be remembered that all degrees of hypersensitivity, including fatal anaphylaxis, have been observed with oral penicillin.
Pseudomembranous colitis requires immediate attention and treatment with an appropriate antibiotherapy (i.e. vancomycin).
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 the yellow card scheme at www.mhra.gov.uk/yellowcard.
4.9 Overdose
Cases of intended or accidental overdosage should be brought under medical supervision for symptomatic treatment. It is advisable to monitor blood levels in patients with renal malfunction.
Symptoms: A large oral overdose of penicillin may cause nausea, vomiting, stomach pain, diarrhoea, and rarely, major motor seizures. If other symptoms are present, consider the possibility of an allergic reaction. Hyperkalaemia may result from over dosage, particularly for patients with renal insufficiency.
Management: No specific antidote is known. Symptomatic and supportive therapy is recommended. Activated charcoal with a cathartic, such as sorbitol may hasten drug elimination. Penicillin may be removed by haemodialysis.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Beta lactamase sensitive penicillins ATC Code: J01CE02 Mechanism of action:
Phenoxymethylpenicillin potassium is a beta lactam antibiotic with bactericidal action against Gram-positive bacteria and Gram-negative cocci. Its antimicrobial action is similar to that of benzylpenicillin. Phenoxymethylpenicillin potassium is usually active against the following organisms:
Gram-positive aerobes and anaerobes including
Bacillus anthracis Clostridium perfringens Clostridium tetani Corynebacterium diphtheriae Erysipelothrix rhusiopathiae Listeria mono cyto genes Peptostreptococcus spp.
Streptococcus agalactiae (Group B)
Streptococcus pneumoniae Streptococcus pyogenes (Group A}
Gram-negative including Neisseria meningitides Neisseria gonorrhoeae
Phenoxymethylpenicillin potassium is inactivated by penicillinase and other beta lactamases.
Phenoxymethylpenicillin binds to penicillin-binding proteins located on the inner membrane of the bacterial cell wall. Phenoxymethylpenicillin binds to and inactivates these proteins resulting in weakening of the bacterial cell wall and lysis.
5.2 Pharmacokinetic properties
Absorption:
Phenoxymethylpenicillin is stable under acidic conditions so it can be administered by oral route. Phenoxymethylpenicillin is rapidly, but incompletely absorbed after oral administration and the absorption level is around 60%. The simultaneous administration of food slightly decreases the peak plasma concentration of phenoxymethylpenicillin, but does not appear to affect the extent of absorption. Peak plasma concentrations are reached in about 45 minutes. The peak plasma concentration increases approximately in proportion with increased doses.
Distribution:
Phenoxymethylpenicillin passes into the tissues (volume of distribution about 0.2 l.kg-1 of body weight. The plasma protein binding is about 80%.
Biotransformation:
Phenoxymethylpenicillin is partially metabolised to inactive penicilloic acid by hydrolysis of the lactam ring. This metabolism occurs in the liver.
Elimination:
About 40% of the dose is eliminated in the urine either as under unchanged or as penicilloic acid in the first 10 hours after oral administration. The plasma half-life of phenoxymethylpenicillin is about 45 minutes. It is however extended in case of renal insufficiency.
5.3 Preclinical safety data
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of this SPC.
6.1 List of excipients
The excipients in the syrup: sodium saccharin, citric acid, sodium citrate, sucrose, banana flavour, preservative:
E 211: sodium benzoate colouring agent:
El 27 Erythrosine
6.2 Incompatibilities
None known.
6.3 Shelf life
The shelf life of the product is 36 months.
6.4 Special precautions for storage
Do not store above 25oC.Keep the container tightly closed.
Store the reconstituted solution preferably in a refrigerator (2-8°C).
Phenoxymethylpenicillm Potassium solution should be kept out of reach and sight of children.
6.5 Nature and contents of container
The product comes in amber coloured glass bottles of 60 ml and 100 ml fitted with ROPP caps.
Not all pack sizes may be marketed.
6.6 Special precautions for disposal
The reconstituted syrup should be used within 7 days.
7 MARKETING AUTHORISATION HOLDER
Special Concept Development (UK) Limited,
Unit 1-7 Colonial Way,
Watford, Hertfordshire,
WD24 4YR United Kingdom.
8 MARKETING AUTHORISATION NUMBER(S)
PL 36722/0063
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
02/11/2010
10 DATE OF REVISION OF THE TEXT
13/05/2016