URANTOIN/NITROFURANTOIN 100MG TABLETS

Active substance: NITROFURANTOIN

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
URANTOIN/Nitrofurantoin 100mg Tablets

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Nitrofurantoin BP 100.00 mg

3

PHARMACEUTICAL FORM
Tablet

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Treatment of and prophylaxis against acute or recurrent uncomplicated pyelitis
or lower urinary tract infection proven to be due to B. coli, Staph. aureus or
Strep. faecalis - either spontaneous or following surgical procedures. The drug
should be used as a second line choice for acute attacks.

4.2

Posology and method of administration
Adults:

Uncomplicated acute urinary tract infections:
50 mg t.i.d. for 3 days.
Severe chronic recurrence: 100 mg t.i.d. for 7 days.
Long term suppression: 100 mg once a day or 2.4 mg/kg/day if treatment

duration less than 3 months and 50 mg once a day or 1.2 mg/kg/day if
treatment duration more than 3 months.
For prophylaxis: 50 mg t.i.d. for duration of procedure and 3 days thereafter.
Special groups (uncomplicated acute lower UTI):
Children:

1.2-2.4 mg/kg/day.

Elderly:

50 mg b.i.d.

Route of administration: Oral

4.3

Contraindications
Hypersensitivity to the drug or other nitrofurans. Renal dysfunction with a
creatinine clearance of less than 60/ml/min or elevated serum creatinine.
Patients with porphyria
Infants below 3 months of age. Pregnant patients at term.

4.4

Special warnings and precautions for use
Nitrofurantoin is not effective for the treatment of parenchymal infections of
unilaterally non-functioning kidney. A surgical cause for infections should be
excluded in recurrent or severe cases. Nitrofurantoin should be used with
caution in renal dysfunction where creatinine clearance is between 60 ml and
90 ml, anaemia, diabetes, debilitating conditions, vitamin B (particularly
folate) deficiency, or patients likely to have G-6-PD or other erythrocyte
enzyme deficiency, pulmonary disease, hepatic dysfunctions, neurological
disorders and allergic diathesis. Superinfection with fungal or non-susceptible
organisms can occur in prolonged therapy.
Acute, subacute or chronic pulmonary reactions have been observed in
patients treated with nitrofurantoin. If these reactions occur, nitrofurantoin
should be discontinued and appropriate measures taken. Reports have cited
pulmonary reactions as a contributing cause of death. Chronic pulmonary
reactions (diffuse interstitial pneumonitis or pulmonary fibrosis, or other) can
develop insidiously. These reactions occur rarely and generally in patients
receiving therapy for six months or longer. Chronic pulmonary reactions may
occur more commonly in elderly patients. Close monitoring of the pulmonary
condition of patients receiving long-term therapy is warranted and requires
that the benefits of therapy be weighed against potential risks.

Hepatic reactions, including cholestatic jaundice and chronic active hepatitis,
occur rarely. Fatalities have been reported. Cholestatic jaundice is generally
associated with short-term therapy (usually up to two weeks). Chronic active
hepatitis is generally associated with long-term therapy (usually after six
months); the onset may be insidious, and patients should be monitored
periodically for changes in liver function. If hepatitis occurs, the drug should
be withdrawn immediately and appropriate measures taken.
Drug rashes, pyrexia and hepatitis associated with nitrofurantoin therapy have
been reported. The hepatitis is of an allergic type and may be associated with
lymphocyte sensitisation. Bronchospasm and/or dyspnoea, cough and
occasionally chest pain has been reported. These symptoms have sometimes
been associated with pulmonary infiltration or pleural effusion which is
usually transitory.
Ten percent of black patients and a variable percentage of ethnic groups of
Mediterranean, Near Eastern and Asian origin, suffer from a deficiency of
glucose-6-phosphate dehydrogenase in their blood cells. In such people,
nitrofurantoin, in common with many other therapeutic agents, may cause
haemolysis. This enzyme deficiency is extremely rare in Caucasians. Any
sign of haemolysis is an indication to discontinue the drug. Haemolysis ceases
when the drug is withdrawn.
Discontinue treatment with nitrofurantoin if otherwise unexplained
pulmonary, hepatotoxic, haemolytic or neurologic symptoms occur.
For long-term treatment beyond one month, monitor patient closely for
appearance of haematological, hepatic, pulmonary or neurological symptoms
and other evidence of toxicity.

4.5

Interaction with other medicinal products and other forms of interaction
Increased absorption with food and anticholinergic drugs. Decreased
absorption with magnesium trisilicate. Increased metabolism of phenytoin.
Decreased renal excretion of nitrofurantoin by probenecid and sulfinyprazone.
Decreased antibacterial activity by carbonic anhydrase inhibitors, urine
alkalinisation and barbiturates. Antibacterial antagonism by quinolone antiinfectives. Interference with urinary estimations of glucose by clinitest (but
not by clinistix) method.

4.6

Pregnancy and lactation

Based on animal reproduction studies and clinical experience in humans over
many
years, there is no evidence of any teratogenic effects of nitrofurantoin on the
foetus. Caution should be exercised whilst breast feeding an infant known or
suspected to have any erythrocyte enzyme deficiency as nitrofurantoin is
detected in trace amounts in breast milk. However, the maternal side-effects
may adversely affect the course of the pregnancy. The drug should be used at
the lowest effective dose as appropriate for the specific indication only after
careful assessment of benefits against potential risks.

4.7

Effects on ability to drive and use machines
None stated.

4.8

Undesirable effects
Respiratory: Acute, subacute or chronic pulmonary reactions may occur.
Acute pulmonary reactions are commonly manifested by fever, chills, cough,
chest pain, dyspnoea, pulmonary infiltration with consolidation or pleural
effusion on X-ray and eosinophilia. Acute reactions usually occur within the
first week of treatment and are reversible with cessation of therapy.
Resolution is often dramatic.
In subacute pulmonary reactions, fever and eosinophilia occur less often than
in the acute form. Upon cessation of therapy, recovery may require several
months. If the symptoms are not recognised as being drug-related and therapy
is not stopped, they may become more severe.
Chronic pulmonary reactions may occur in patients who have received
continuous therapy for six months or more. Chronic pulmonary reactions may
occur more commonly in elderly patients. Malaise, dyspnoea on exertion,
cough and altered pulmonary function are common manifestations which can
occur insidiously. Radiological and histological findings of diffuse interstitial
pneumonitis or fibrosis, or both, are also common manifestations of the
chronic pulmonary reactions. Fever is rarely prominent. The severity of
chronic pulmonary reactions and their degree of resolution appear to be related
to the duration of therapy after the first clinical signs appear. Pulmonary
function may be impaired permanently, even after cessation of therapy. The
risk is greater when chronic pulmonary reactions are not recognised early.
Gastrointestinal: Nausea and anorexia have been reported. Emesis, abdominal
pain and diarrhoea are less common gastrointestinal reactions. These reactions
may be minimised by taking the drug with food or milk or by adjustment of
dosage. Hepatic reactions including cholestatic jaundice and chronic active
hepatitis occur rarely.

Hypersensitivity: Exfoliative dermatitis and erythema multiforme (including
Stevens-Johnson syndrome) have been reported rarely.
Allergic skin reactions manifesting as angioneurotic oedema, maculopapular,
erythematous or eczematous eruptions, urticaria, rash, pruritus have occurred.
Lupuslike syndrome associated with pulmonary reactions to nitrofurantoin has
been reported.
Other hypersensitivity reactions include anaphylaxis, sialadenitis, pancreatitis,
drug fever and arthralgia.
Haematological: Agranulocytosis, leucopenia, granulocytopenia, haemolytic
anaemia, megaloblastic anaemia and eosinophilia have occurred. Cessation of
therapy has generally returned the blood picture to normal. Aplastic anaemia
has been reported rarely.
Neurological: Peripheral neuropathy, which may become severe or irreversible
has occurred but has usually been associated with severed renal impairment
and/or prolonged therapy. Less frequent reactions, of unknown causal
relationship are nystagmus, vertigo, dizziness, asthenia, headache and
drowsiness. Should numbness or tingling occur in any part of the body,
treatment should be discontinued.
Miscellaneous: Transient alopecia has been reported.
As with other antimicrobial agents superinfections by resistant organisms such
as Pseudomonas may occur. However, these are limited to the genito-urinary
tract because suppression of normal bacterial flora does not occur elsewhere in
the body.

4.9

Overdose
Symptoms and signs of overdosage include gastric irritation, nausea and
vomiting. There is no known specific antidote. Nitrofurantoin can be
haemodialysed. Treatment is by induction of emesis or by gastric lavage in
recent ingestion. Full blood count, liver function tests and pulmonary function
should be monitored. A high fluid intake should be maintained to promote
urinary excretion of the drug.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Nitrofurantoin is bactericidal in vitro to most gram-positive and gram-negative
urinary tract pathogens and minimum inhibitory concentrations have been
reported to range from 4 to 100 micrograms per millilitre. It is most active in
acid urine and when the pH exceeds 8 most of the anti-bacterial activity is lost.
Nitrofurantoin is thought to act by interfering with bacterial enzymes involved
in carbohydrate metabolism.

5.2

Pharmacokinetic properties
Nitrofurantoin is readily absorbed from the gastro-intestinal tract and from
25% to 60% is bound to plasma proteins. The plasma half-life is
approximately 20 minutes.
Nitrofurantoin diffuses across the placenta and low concentrations appear in
the foetal circulation and have been detected in milk.
About 40% of a dose is excreted in the urine as Nitrofurantoin.

5.3

Preclinical safety data
Not applicable.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose
Maize starch
Pregelatinised maize starch
Sodium starch glycollate
Magnesium stearate
Purified water

6.2

Incompatibilities
None stated.

6.3

Shelf life
36 months.

6.4

Special precautions for storage
Store below 25°C in a dry place in well closed containers.
Protect from light.

6.5

Nature and contents of container
High density polystyrene containers with polythene lids and/or polypropylene
containers with polypropylene or polythene lids.
Pack sizes: 28, 30, 50, 56, 60, 84, 100, 250, 500 & 1000.
250 micron green rigid PVC pharmaceutical grade.
20 micron hard-tempered aluminium foil, coated on the dull side with 6-7 gsm
heat-seal lacquer and printed on the bright side.
Pack sizes: 28, 30, 50, 56, 60, 84, 100, 250, 500 & 1000.

6.6

Special precautions for disposal
Not applicable.

7

MARKETING AUTHORISATION HOLDER
Chelonia Healthcare Limited
Boumpoulinas 11, 3rd Floor
NICOSIA
CYPRUS
P.C. 1060

CYPRUS

8

MARKETING AUTHORISATION NUMBER(S)
PL 33414/0070

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
12/01/2009

10

DATE OF REVISION OF THE TEXT
12/01/2009

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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