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OMEPRAZOL UNIVERSAL FARMA 20 MG GASTRO-RESISTANT CAPSULES.

Active substance(s): OMEPRAZOLE

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SUMMARY OF PRODUCT CHARACTERISTICS
1

NAME OF THE MEDICINAL PRODUCT
Omeprazol Universal Farma 20 mg, gastro-resistant capsules

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each capsule contains 20mg omeprazole
Excipients: Sucrose, etc
For a full list of excipients, see section 6.1

3

PHARMACEUTICAL FORM
Gastro-resistant capsules
Hard gelatin capsules, opaque yellow cap and body

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Omeprazole capsules are indicated for:
Adults:
• Treatment of duodenal ulcers
• Prevention of relapse of duodenal ulcers
• Treatment of gastric ulcers
• Prevention of relapse of gastric ulcers
• In combination with appropriate antibiotics, Helicobacter pylori (H. pylori)
eradication in peptic ulcer disease
• Treatment of NSAID-associated gastric and duodenal ulcers
• Prevention of NSAID-associated gastric and duodenal ulcers in patients at
risk
• Treatment of reflux oesophagitis
• Long-term management of patients with healed reflux esophagitis
• Treatment of symptomatic gastro-esophageal reflux disease
• Treatment of Zollinger-Ellison syndrome
• gastric and duodenal ulcers
Paediatric use
Children over 1 year of age and ≥10kg:
• Treatment of reflux oesophagitis.
• Symptomatic treatment of heartburn and acid regurgitation in gastroesophageal reflux disease.

Children and adolescents over 4 years of age:
In combination with antibiotics in treatment of duodenal ulcer caused by H.
pylori.

4.2

Posology and method of administration
Posology in adults
Treatment of duodenal ulcers
The recommended dose in patients with an active duodenal ulcer is
Omeprazole 20mg once daily. In most patients healing occurs within two
weeks. For those patients who may not be fully healed after the initial course,
healing usually occurs during a further two weeks treatment period. In patients
with poorly responsive duodenal ulcer Omeprazole 40mg once daily is
recommended and healing is usually achieved within four weeks.
Prevention of relapse of duodenal ulcers
For the prevention of relapse of duodenal ulcer in H. pylori negative patients
or when H. pylori eradication is not possible the recommended dose is
Omeprazole 20mg once daily. In some patients a daily dose of 10mg may be
sufficient. In case of therapy failure, the dose can be increased to 40mg.
Treatment of gastric ulcers
The recommended dose is Omeprazole 20mg once daily. In most patients
healing occurs within four weeks. For those patients who may not be fully
healed after the initial course, healing usually occurs during a further four
weeks treatment period. In patients with poorly responsive gastric ulcer
Omeprazole 40mg once daily is recommended and healing is usually achieved
within eight weeks.
Prevention of relapse of gastric ulcers
For the prevention of relapse in patients with poorly responsive gastric ulcer
the recommended dose is Omeprazole 20mg once daily. If needed the dose can
be increased to Omeprazole 40mg once daily.
H. pylori eradication in peptic ulcer disease
For the eradication of H. pylori the selection of antibiotics should consider the
individual patient’s drug tolerance, and should be undertaken in accordance
with national, regional and local resistance patterns and treatment guidelines.
• Omeprazole 20mg + clarithromycin 500mg + amoxicillin 1,000mg, each
twice daily for one week, or
• Omeprazole 20mg + clarithromycin 250mg (alternatively 500mg) +
metronidazole 400mg (or 500mg or tinidazole 500mg), each twice daily
for one week or
• Omeprazole 40mg once daily with amoxicillin 500mg and metronidazole
400mg (or 500mg or tinidazole 500mg), both three times a day for one
week.
In each regimen, if the patient is still H. pylori positive, therapy may be
repeated.
Treatment of NSAID-associated gastric and duodenal ulcers

For the treatment of NSAID-associated gastric and duodenal ulcers, the
recommended dose is Omeprazole 20mg once daily. In most patients healing
occurs within four weeks. For those patients who may not be fully healed after
the initial course, healing usually occurs during a further four weeks treatment
period.
Prevention of NSAID-associated gastric and duodenal ulcers in patients at
risk
For the prevention of NSAID-associated gastric ulcers or duodenal ulcers in
patients at risk (age >60, previous history of gastric and duodenal ulcers,
previous history of upper GI bleeding) the recommended dose is Omeprazole
20mg once daily.
Treatment of reflux esophagitis
The recommended dose is Omeprazole 20mg once daily. In most patients
healing occurs within four weeks. For those patients who may not be fully
healed after the initial course, healing usually occurs during a further four
weeks treatment period.
In patients with severe esophagitis Omeprazole 40mg once daily is
recommended and healing is usually achieved within eight weeks.
Long-term management of patients with healed reflux esophagitis
For the long-term management of patients with healed reflux esophagitis the
recommended dose is Omeprazole 10mg once daily. If needed, the dose can be
increased to Omeprazole 20-40mg once daily.
Treatment of symptomatic gastro-esophageal reflux disease
The recommended dose is Omeprazole 20mg daily. Patients may respond
adequately to 10mg daily, and therefore individual dose adjustment should be
considered.
If symptom control has not been achieved after four weeks treatment with
Omeprazole 20mg daily, further investigation is recommended.
Treatment of Zollinger-Ellison syndrome
In patients with Zollinger-Ellison syndrome the dose should be individually
adjusted and treatment continued as long as clinically indicated. The
recommended initial dose is Omeprazole 60mg daily. All patients with severe
disease and inadequate response to other therapies have been effectively
controlled and more than 90% of the patients maintained on doses of
Omeprazole 20-120mg daily. When dose exceed Omeprazole 80mg daily, the
dose should be divided and given twice daily.
Posology in children
Children over 1 year of age and ≥ 10 kg
Treatment of reflux esophagitis
Symptomatic treatment of heartburn and acid regurgitation in gastroesophageal reflux disease
The posology recommendations are as follows:
Age
Weight
Posology
≥ 1 year of age
10-20 kg
10mg once daily. The dose can be increased
to 20mg once daily if needed

≥ 2 years of age

> 20 kg

20mg once daily. The dose can be increased
to 40mg once daily if needed

Reflux esophagitis: The treatment time is 4-8 weeks.
Symptomatic treatment of heartburn and acid regurgitation in gastroesophageal reflux disease: The treatment time is 2–4 weeks. If symptom
control has not been achieved after 2–4 weeks the patient should be
investigated further.
Children and adolescents over 4 years of age
Treatment of duodenal ulcer caused by H. pylori
When selecting appropriate combination therapy, consideration should be
given to official national, regional and local guidance regarding bacterial
resistance, duration of treatment (most commonly 7 days but sometimes up to
14 days), and appropriate use of antibacterial agents.
The treatment should be supervised by a specialist.
The posology recommendations are as follows:
Weight
Posology
15–30 kg
Combination with two antibiotics: Omeprazole 10mg,
amoxicillin 25mg/kg body weight and clarithromycin
7.5mg/kg body weight are all administrated together two times
daily for one week.
31–40 kg
Combination with two antibiotics: Omeprazole 20mg,
amoxicillin 750mg and clarithromycin 7.5mg/kg body weight
are all administrated two times daily for one week.
> 40 kg
Combination with two antibiotics: Omeprazole 20mg,
amoxicillin 1g and clarithromycin 500mg are all administrated
two times daily for one week.
Special populations
Impaired renal function
Dose adjustment is not needed in patients with impaired renal function (see
section 5.2).
Impaired hepatic function
In patients with impaired hepatic function a daily dose of 10–20mg may be
sufficient (see section 5.2).
Elderly (> 65 years old)
Dose adjustment is not needed in the elderly (see section 5.2).
Method of administration
It is recommended to take Omeprazole capsules in the morning, preferably
without food, swallowed whole with half a glass of water. The capsules must
not be chewed or crushed.
For patients with swallowing difficulties and for children who can drink or
swallow semi-solid food
Patients can open the capsule and swallow the contents with half a glass of
water or after mixing the contents in a slightly acidic fluid e.g., fruit juice or
applesauce, or in non-carbonated water. Patients should be advised that the

dispersion should be taken immediately (or within 30 minutes) and always be
stirred just before drinking and rinsed down with half a glass of water.
Alternatively patients can suck the capsule and swallow the pellets with half a
glass of water. The enteric-coated pellets must not be chewed.

4.3

Contraindications
Hypersensitivity to omeprazole, substituted benzimidazoles or to any of the
excipients.
Omeprazole like other proton pump inhibitors (PPIs) must not be used
concomitantly with nelfinavir (see section 4.5).

4.4

Special warnings and precautions for use
In the presence of any alarm symptom (e.g. significant unintentional weight
loss, recurrent vomiting, dysphagia, haematemesis or melena) and when
gastric ulcer is suspected or present, malignancy should be excluded, as
treatment may alleviate symptoms and delay diagnosis.
Co-administration of atazanavir with proton pump inhibitors is not
recommended (see section 4.5). If the combination of atazanavir with a proton
pump inhibitor is judged unavoidable, close clinical monitoring (e.g. virus
load) is recommended in combination with an increase in the dose of
atazanavir to 400mg with 100mg of ritonavir; omeprazole 20mg should not be
exceeded.
Omeprazole, as all acid-blocking medicines, may reduce the absorption of
vitamin B12 (cyanocobalamin) due to hypo- or achlorhydria. This should be
considered in patients with reduced body stores or risk factors for reduced
vitamin B12 absorption on long-term therapy.
Omeprazole is a CYP2C19 inhibitor. When starting or ending treatment with
omeprazole, the potential for interactions with drugs metabolised through
CYP2C19 should be considered. An interaction is observed between
clopidogrel and omeprazole (see section 4.5). The clinical relevance of this
interaction is uncertain. As a precaution, concomitant use of omeprazole and
clopidogrel should be discouraged.
Some children with chronic illnesses may require long-term treatment
although it is not recommended.
Omeprazole 20mg capsules contain sucrose. Patients with rare hereditary
problems of fructose intolerance, glucose-galactose malabsorption or sucraseisomaltase insufficiency should not take this medicine.
Treatment with proton pump inhibitors may lead to slightly increased risk of
gastrointestinal infections such as Salmonella and Campylobacter (see section
5.1).
As in all long-term treatments, especially when exceeding a treatment period
of 1 year, patients should be kept under regular surveillance.
Proton pump inhibitors, especially if used in high doses and over long
durations (>1 year), may modestly increase the risk of hip, wrist and spine

fracture, predominantly in the elderly or in presence of other recognised risk
factors. Observational studies suggest that proton pump inhibitors may
increase the overall risk of fracture by 10–40%. Some of this increase may be
due to other risk factors. Patients at risk of osteoporosis should receive care
according to current clinical guidelines and they should have an adequate
intake of vitamin D and calcium.
Hypomagnesaemia
Severe hypomagnesaemia has been reported in patients treated with PPIs like
omeprazole for at least three months, and in most cases for a year. Serious
manifestations of hypomagnesaemia such as fatigue, tetany, delirium,
convulsions, dizziness and ventricular arrhythmia can occur but they may
begin insidiously and be overlooked. In most affected patients,
hypomagnesaemia
improved
after
magnesium
replacement
and
discontinuation of the PPI.
For patients expected to be on prolonged treatment or who take PPIs with
digoxin or drugs that may cause hypomagnesaemia (e.g., diuretics), health
care professionals should consider measuring magnesium levels before
starting PPI treatment and periodically during treatment.

4.5

Interaction with other medicinal products and other forms of interaction
Effects of omeprazole on the pharmacokinetics of other active substances
Active substances with pH dependent absorption
The decreased intragastric acidity during treatment with omeprazole might
increase or decrease the absorption of active substances with a gastric pH
dependent absorption.
Nelfinavir, atazanavir
The plasma levels of nelfinavir and atazanavir are decreased in case of coadministration with omeprazole.
Concomitant administration of omeprazole with nelfinavir is contraindicated
(see section 4.3). Co-administration of omeprazole (40mg once daily) reduced
mean nelvinavir exposure by ca. 40% and the mean exposure of the
pharmacologically active metabolite M8 was reduced by ca. 75 –90%. The
interaction may also involve CYP2C19 inhibition.
Concomitant administration of omeprazole with atazanavir is not
recommended (see section 4.4). Concomitant administration of omeprazole
(40mg once daily) and atazanavir 300mg/ritonavir 100mg to healthy volunteers
resulted in a 75% decrease of the atazanavir exposure. Increasing the
atazanavir dose to 400mg did not compensate for the impact of omeprazole on
atazanavir exposure. The co-administration of omeprazole (20mg once daily)
with atazanavir 400mg/ritonavir 100mg to healthy volunteers resulted in a
decrease of approximately 30% in the atazanavir exposure as compared to
atazanavir 300mg/ritonavir 100mg once daily.
Digoxin
Concomitant treatment with omeprazole (20mg daily) and digoxin in healthy
subjects increased the bioavailability of digoxin by 10%. Digoxin toxicity has
been rarely reported. However caution should be exercised when omeprazole is

given at high doses in elderly patients. Therapeutic drug monitoring of digoxin
should be then be reinforced.
Clopidogrel
In a crossover clinical study, clopidogrel (300mg loading dose followed by
75mg/day) alone and with omeprazole (80mg at the same time as clopidogrel)
were administered for 5 days. The exposure to the active metabolite of
clopidogrel was decreased by 46% (Day 1) and 42% (Day 5) when clopidogrel
and omeprazole were administered together. Mean inhibition of platelet
aggregation (IPA) was diminished by 47% (24 hours) and 30% (Day 5) when
clopidogrel and omeprazole were administered together. In another study it
was shown that administering clopidogrel and omeprazole at different times
did not prevent their interaction that is likely to be driven by the inhibitory
effect of omeprazole on CYP2C19. Inconsistent data on the clinical
implications of this PK/PD interaction in terms of major cardiovascular events
have been reported from observational and clinical studies.
Other active substances
The absorption of posaconazole, erlotinib, ketoconazol and itraconazol is
significantly reduced and thus clinical efficacy may be impaired. For
posaconazol and erlotinib concomitant use should be avoided.
Active substances metabolised by CYP2C19
Omeprazole is a moderate inhibitor of CYP2C19, the major omeprazole
metabolising enzyme. Thus, the metabolism of concomitant active substances
also metabolised by CYP2C19, may be decreased and the systemic exposure
to these substances increased. Examples of such drugs are R-warfarin and
other vitamin K antagonists, cilostazol, diazepam and phenytoin.
Cilostazol
Omeprazole, given in doses of 40mg to healthy subjects in a cross-over study,
increased Cmax and AUC for cilostazol by 18% and 26% respectively, and
one of its active metabolites by 29% and 69% respectively.
Phenytoin
Monitoring phenytoin plasma concentration is recommended during the first
two weeks after initiating omeprazole treatment and, if a phenytoin dose
adjustment is made, monitoring and a further dose adjustment should occur
upon ending omeprazole treatment.
Unknown mechanism
Saquinavir
Concomitant administration of omeprazole with saquinavir/ritonavir resulted in
increased plasma levels up to approximately 70% for saquinavir associated
with good tolerability in HIV-infected patients.
Tacrolimus
Concomitant administration of omeprazole has been reported to increase the
serum levels of tacrolimus. A reinforced monitoring of tacrolimus
concentrations as well as renal function (creatinine clearance) should be
performed, and dosage of tacrolimus adjusted if needed.
Effects of other active substances on the pharmacokinetics of omeprazole
Inhibitors CYP2C19 and/or CYP3A4

Since omeprazole is metabolised by CYP2C19 and CYP3A4, active substances
known to inhibit CYP2C19 or CYP3A4 (such as clarithromycin and
voriconazole) may lead to increased omeprazole serum levels by decreasing
omeprazole’s rate of metabolism. Concomitant voriconazole treatment resulted
in more than doubling of the omeprazole exposure. As high doses of
omeprazole have been well-tolerated adjustment of the omeprazole dose is not
generally required. However, dose adjustment should be considered in patients
with severe hepatic impairment and if long-term treatment is indicated.
Inducers of CYP2C19 and/or CYP3A4
Active substances known to induce CYP2C19 or CYP3A4 or both (such as
rifampicin and St John’s wort) may lead to decreased omeprazole serum levels
by increasing omeprazole’s rate of metabolism.

4.6

Fertility, pregnancy and lactation
Results from three prospective epidemiological studies (more than 1000
exposed outcomes) indicate no adverse effects of omeprazole on pregnancy or
on the health of the foetus/newborn child. Omeprazole can be used during
pregnancy.
Omeprazole is excreted in breast milk but is not likely to influence the child
when therapeutic doses are used.

4.7

Effects on ability to drive and use machines
Omeprazole is not likely to affect the ability to drive or use machines. Adverse
drug reactions such as dizziness and visual disturbances may occur (see
section 4.8). If affected, patients should not drive or operate machinery.

4.8

Undesirable effects
The most common side effects (1-10% of patients) are headache, abdominal
pain, constipation, diarrhoea, flatulence and nausea/vomiting.
The following adverse drug reactions have been identified or suspected in the
clinical trials programme for omeprazole and post-marketing. None was found
to be dose-related. Adverse reactions listed below are classified according to
frequency and System Organ Class (SOC). Frequency categories are defined
according to the following convention: Very common (>1/10),Common
(>1/100,
<1/10),Uncommon
(>1/1,000,
<1/100),Rare
(>1/10,000,
<1/1,000),Very rare (<1/10,000), Not known (cannot be estimated from the
available data).
SOC/frequency

Adverse reaction

Blood and lymphatic system disorders
Rare:
Leukopenia, thrombocytopenia
Very rare:
Agranulocytosis, pancytopenia
Immune system disorders

Rare:

Hypersensitivity reactions e.g. fever,
angioedema and anaphylactic reaction/shock

Metabolism and nutrition disorders
Rare:
Hyponatraemia
Not known:
Hypomagnesaemia (see section 4.4)
Psychiatric disorders
Uncommon:
Rare:
Very rare:

Insomnia
Agitation, confusion, depression
Aggression, hallucinations

Nervous system disorders
Common:
Headache
Uncommon:
Dizziness, paraesthesia, somnolence
Rare:
Taste disturbance
Eye disorders
Rare:

Blurred vision

Ear and labyrinth disorders
Uncommon:
Vertigo
Respiratory, thoracic and mediastinal disorders
Rare:
Bronchospasm
Gastrointestinal disorders
Common:
Abdominal pain, constipation, diarrhoea,
flatulence, nausea/vomiting
Rare:
Dry mouth, stomatitis, gastrointestinal
candidiasis
Hepatobiliary disorders
Uncommon:
Rare:
Very rare:

Increased liver enzymes
Hepatitis with or without jaundice
Hepatic failure, encephalopathy in patients with
pre-existing liver disease

Skin and subcutaneous tissue disorders
Uncommon:
Dermatitis, pruritus, rash, urticaria
Rare:
Alopecia, photosensitivity
Very rare:
Erythema multiforme, Stevens-Johnson
syndrome, toxic epidermal necrolysis (TEN)
Musculoskeletal and connective tissue disorders
Uncommon:
Fracture of the hip, wrist or spine (see section
4.4)
Rare:
Arthralgia, myalgia
Very rare:
Muscular weakness
Renal and urinary disorders

Rare:

Interstitial nephritis

Reproductive system and breast disorders
Very rare:
Gynaecomastia
General disorders and administration site conditions
Uncommon:
Malaise, peripheral oedema
Rare:
Increased sweating
Paediatric population
The safety of omeprazole has been assessed in a total of 310 children aged 0 to
16 years with acid-related disease. There are limited long term safety data
from 46 children who received maintenance therapy of omeprazole during a
clinical study for severe erosive esophagitis for up to 749 days. The adverse
event profile was generally the same as for adults in short- as well as in longterm treatment. There are no long term data regarding the effects of
omeprazole treatment on puberty and growth.

4.9

Overdose
There is limited information available on the effects of overdoses of
omeprazole in humans. In the literature, doses of up to 560mg have been
described, and occasional reports have been received when single oral doses
have reached up to 2,400mg omeprazole (120 times the usual recommended
clinical dose). Nausea, vomiting, dizziness, abdominal pain, diarrhoea and
headache have been reported. Also apathy, depression and confusion have
been described in single cases.
The symptoms described have been transient, and no serious outcome has
been reported. The rate of elimination was unchanged (first order kinetics)
with increased doses. Treatment, if needed, is symptomatic.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Pharmacotherapeutic group: Proton pump inhibitors, ATC code: A02B C 01
Mechanism of action
Omeprazole, a racemic mixture of two enantiomers reduces gastric acid
secretion through a highly targeted mechanism of action. It is a specific
inhibitor of the acid pump in the parietal cell. It is rapidly acting and provides
control through reversible inhibition of gastric acid secretion with once daily
dosing.
Omeprazole is a weak base and is concentrated and converted to the active
form in the highly acidic environment of the intracellular canaliculi within the
parietal cell, where it inhibits the enzyme H+ K+-ATPase - the acid pump.
This effect on the final step of the gastric acid formation process is dosedependent and provides for highly effective inhibition of both basal acid
secretion and stimulated acid secretion, irrespective of stimulus.
Pharmacodynamic effects

All pharmacodynamic effects observed can be explained by the effect of
omeprazole on acid secretion.
Effect on gastric acid secretion
Oral dosing with omeprazole once daily provides for rapid and effective
inhibition of daytime and night-time gastric acid secretion with maximum
effect being achieved within 4 days of treatment. With omeprazole 20mg, a
mean decrease of at least 80% in 24-hour intragastric acidity is then
maintained in duodenal ulcer patients, with the mean decrease in peak acid
output after pentagastrin stimulation being about 70% 24 hours after dosing.
Oral dosing with omeprazole 20mg maintains an intragastric pH of ≥ 3 for a
mean time of 17 hours of the 24-hour period in duodenal ulcer patients.
As a consequence of reduced acid secretion and intragastric acidity,
omeprazole dose-dependently reduces/normalizes acid exposure of the
esophagus in patients with gastro-esophageal reflux disease.
The inhibition of acid secretion is related to the area under the plasma
concentration-time curve (AUC) of omeprazole and not to the actual plasma
concentration at a given time.
No tachyphylaxis has been observed during treatment with omeprazole.
Effect on H. pylori
H. pylori is associated with peptic ulcer disease, including duodenal and
gastric ulcer disease. H. pylori is a major factor in the development of gastritis.
H. pylori together with gastric acid are major factors in the development of
peptic ulcer disease. H. pylori is a major factor in the development of atrophic
gastritis which is associated with an increased risk of developing gastric
cancer.
Eradication of H. pylori with omeprazole and antimicrobials is associated
with, high rates of healing and long-term remission of peptic ulcers.
Dual therapies have been tested and found to be less effective than triple
therapies. They could, however, be considered in cases where known
hypersensitivity precludes use of any triple combination.
Other effects related to acid inhibition
During long-term treatment gastric glandular cysts have been reported in a
somewhat increased frequency. These changes are a physiological
consequence of pronounced inhibition of acid secretion, are benign and appear
to be reversible.
Decreased gastric acidity due to any means including proton pump inhibitors,
increases gastric counts of bacteria normally present in the gastrointestinal
tract. Treatment with acid-reducing drugs may lead to slightly increased risk
of gastrointestinal infections such as Salmonella and Campylobacter.
Paediatric use
In a non-controlled study in children (1 to 16 years of age) with severe reflux
esophagitis, omeprazole at doses of 0.7 to 1.4mg/kg improved esophagitis
level in 90% of the cases and significantly reduced reflux symptoms. In a
single-blind study, children aged 0–24 months with clinically diagnosed
gastro-esophageal reflux disease were treated with 0.5, 1.0 or 1.5mg
omeprazole/kg. The frequency of vomiting/regurgitation episodes decreased
by 50% after 8 weeks of treatment irrespective of the dose.

Eradication of H. pylori in children
A randomised, double blind clinical study (Héliot study) concluded that
omeprazole in combination with two antibiotics (amoxicillin and
clarithromycin), was safe and effective in the treatment of H. pylori infection
in children age 4 years old and above with gastritis: H. pylori eradication rate:
74.2% (23/31 patients) with omeprazole + amoxicillin + clarithromycin versus
9.4% (3/32 patients) with amoxicillin + clarithromycin. However, there was
no evidence of any clinical benefit with respect to dyspeptic symptoms. This
study does not support any information for children aged less than 4 years.

5.2

Pharmacokinetic properties
Absorption
Omeprazole is acid labile and is administered orally as enteric-coated granules
in capsules. Absorption of omeprazole is rapid, with peak plasma levels
occurring approximately 1-2 hours after dose. Absorption of omeprazole takes
place in the small intestine and is usually completed within 3-6 hours.
Concomitant intake of food has no influence on the bioavailability. The
systemic availability (bioavailability) from a single oral dose of omeprazole is
approximately 40%. After repeated once-daily administration, the
bioavailability increases to about 60%.
Distribution
The apparent volume of distribution in healthy subjects is approximately 0.3
l/kg body weight. Omeprazole is 97% plasma protein bound.
Metabolism
Omeprazole is completely metabolised by the cytochrome P450 system (CYP).
The major part of its metabolism is dependent on the polymorphically
expressed CYP2C19, responsible for the formation of hydroxyomeprazole, the
major metabolite in plasma. The remaining part is dependent on another
specific isoform, CYP3A4, responsible for the formation of omeprazole
sulphone. As a consequence of high affinity of omeprazole to CYP2C19, there
is a potential for competitive inhibition and metabolic drug-drug interactions
with other substrates for CYP2C19. However, due to low affinity to CYP3A4,
omeprazole has no potential to inhibit the metabolism of other CYP3A4
substrates. In addition, omeprazole lacks an inhibitory effect on the main CYP
enzymes.
Approximately 3% of the Caucasian population and 15-20% of Asian
populations lack a functional CYP2C19 enzyme and are called poor
metabolisers. In such individuals the metabolism of omeprazole is probably
mainly catalysed by CYP3A4. After repeated once-daily administration of 20
mg omeprazole, the mean AUC was 5 to 10 times higher in poor metabolisers
than in subjects having a functional CYP2C19 enzyme (extensive
metabolisers). Mean peak plasma concentrations were also higher, by 3 to 5
times. These findings have no implications for the posology of omeprazole.
Excretion
The plasma elimination half-life of omeprazole is usually shorter than one hour
both after single and repeated oral once-daily dosing. Omeprazole is
completely eliminated from plasma between doses with no tendency for

accumulation during once-daily administration. Almost 80% of an oral dose of
omeprazole is excreted as metabolites in the urine, the remainder in the faeces,
primarily originating from bile secretion.
The AUC of omeprazole increases with repeated administration. This increase
is dose-dependent and results in a non-linear dose-AUC relationship after
repeated administration. This time- and dose dependency is due to a decrease
of first pass metabolism and systemic clearance probably caused by an
inhibition of the CYP2C19 enzyme by omeprazole and/or its metabolites (e.g.
the sulphone).
No metabolite has been found to have any effect on gastric acid secretion.
Special populations
Impaired hepatic function
The metabolism of omeprazole in patients with liver dysfunction is impaired,
resulting in an increased AUC. Omeprazole has not shown any tendency to
accumulate with once daily dosing.
Impaired renal function
The pharmacokinetics of omeprazole, including systemic bioavailability and
elimination rate, are unchanged in patients with reduced renal function.
Elderly
The metabolism rate of omeprazole is somewhat reduced in elderly subjects
(75-79 years of age).
Paediatric patients
During treatment with the recommended doses to children from the age of 1
year, similar plasma concentrations were obtained as compared to adults. In
children younger than 6 months, clearance of omeprazole is low due to low
capacity to metabolise omeprazole.

5.3

Preclinical safety data
Gastric ECL-cell hyperplasia and carcinoids, have been observed in life-long
studies in rats treated with omeprazole. These changes are the result of
sustained hypergastrinaemia secondary to acid inhibition. Similar findings
have been made after treatment with H2-receptor antagonists, proton pump
inhibitors and after partial fundectomy. Thus, these changes are not from a
direct effect of any individual active substance.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Capsules content:
Sugar spheres (consisting of maize starch and sucrose)
Sodium laurilsulfate
Disodium phosphate, anhydrous.
Mannitol
Hypromellose 6 cP
Macrogol 6000

Talc
Polysorbate 80
Titanium dioxide (E 171)
Methacrylic Acid-ethylacrylate copolymer (1:1)
The gelatin capsule consists of:
Gelatin
Quinoline yellow (E 104)
Titanium dioxide (E 171)

6.2

Incompatibilities
Not applicable

6.3

Shelf life
3 years

6.4

Special precautions for storage
Aluminium/Aluminium blister pack: Store in the original package to protect
from moisture.
HDPE bottle: Keep the bottle tightly closed to protect from moisture.

6.5

Nature and contents of container
Aluminium/Aluminium blister:
Pack sizes: 7, 14, 15, 28, 30, 50, 56, and 60 capsules; 100, 140, 280 and 500
capsules (for hospital use only)
HDPE bottle with plastic stopper (polypropylene) containing silicagel:
Pack sizes: 5, 7, 14, 15, 28, 30, 50, 56, 60 and 100 capsules and 500 capsules
(for hospital use only)
Not all pack sizes may be marketed.

6.6

Special precautions for disposal
No special requirements

7

MARKETING AUTHORISATION HOLDER
UNIVERSAL FARMA, S.L.
Gran Vía Carlos III, 98, 7th floor
08028 Barcelona
Spain

8

MARKETING AUTHORISATION NUMBER(S)
PL 19706/0001

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
30/10/2007

10

DATE OF REVISION OF THE TEXT
29/10/2012

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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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