ANTRA ® Omeprazole

ANTRA ® is a drug based on Omeprazole.

THERAPEUTIC GROUP: Antireflux - Antiulcer - Inhibitors of the acid pump

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications ANTRA ® Omeprazole

ANTRA is used in common clinical practice in the treatment of diseases of the gastro-intestinal tract associated with gastric hyperacidosis.

Duodenal ulcers, gastric ulcers and reflux esophagitis, peptic ulcer from H.Pylori, ulcers and erosive gastropathies associated with prolonged use of non-steroidal anti-inflammatory drugs, functional dyspepsia and Zollinger-Ellison syndrome, represent the most common therapeutic indications associated with therapy with ANTRA ®

In pediatric age instead, for patients over 2 years, this medicine can be used in the treatment of gastroesophageal reflux oesophagitis, for periods not exceeding two months.

Mechanism of action ANTRA ® Omeprazole

ANTRA ® is a drug based on omeprazole, the active ingredient in the category of proton pump inhibitors.

Its therapeutic action is due to the ability to act selectively on the H + / K + ATPase pump, involved in the regulation of acid secretion of the gastric contents, through the formation of a covalent bond with a cysteine present in its active domain.

This type of irreversible inhibition guarantees an antacid effect, which is manifested by a reduction of the intragastric acidity of 80% and which lasts even for 24 hours, time necessary for the parietal cell of the stomach, to regenerate new effective proton pumps.

From the pharmacokinetic point of view, the oral intake of omeprazole is followed by a duodenal absorption, which guarantees the achievement of the maximum plasma concentration in about 3 - 6 hours, with a bioavailability of at most 35% of the total dose taken .

Through the blood, bound to the plasma proteins, the omeprazole, reaches the gastric canaliculi, where a pH that is around 2, therefore strongly acid, allows the activation of the active principle, which can then act freely on the parietal cells of the stomach, which express the gastric proton pump.

After its activity, and following a hepatic metabolism induced by the CYP2C19 isoform, the hydroxylated form of omeprazole is mainly excreted in the urine.

Studies carried out and clinical efficacy

1. FARMACOGENOMICA AND OMEPRAZOLE

The presence of particular polymorphisms of the enzyme CYP2C19, involved in the metabolism of omeprazole, have been associated not only to a reduction in the therapeutic efficacy of the same, but also to the reappearance of the symptomatology, once the therapy has been suspended.

2. LONG-TERM OMEPRAZOLE

Prolonged use of proton pump inhibitors is a therapy that is routinely used to control gastric acidity in those patients who require controlled therapy. Statistical studies have shown that this therapeutic protocol can be fundamentally effective and safe, highlighting in particular patients at risk, the onset of Clostridium infections with relative diarrhea.

3. OMEPRAZOLO AND BONE METABOLISM

Prolonged omeprazole therapy has been partly associated with the appearance of bone lesions. The molecular study of this metabolism has shown how the active principle can exert an activating action on osteoblasts with an osteopetrosic effect, probably responsible for fractures.

Method of use and dosage

ANTRA ® 10 -20 mg modified-release hard capsules of omeprazole:

in most cases, an effective treatment is obtained by administering 20 mg of omeprazole per day, preferably taken in the morning with a glass of water, for about 2 - 4 weeks.

The treatment may be subject to variations, both from the point of view of the duration and of the doses used, based on the therapeutic needs of the patient.

In this case the medical supervision useful for establishing the correct therapeutic procedure is of fundamental importance, after a careful evaluation of the patient's physiopathological conditions.

In the treatment of gastric ulcer associated with H.Pylori, omeprazole should be combined with an antibiotic useful for the eradication of this pathogen.

In any case, therapy with omeprazole must be monitored for the duration of the treatment by your doctor.

For pediatric patients, treatment with ANTRA ® should be started in a hospital setting, under the close supervision of a hospital pediatrician.

ANTRA ® Omeprazole warnings

The administration of ANTRA ® should be preceded by a careful check-up of the patient, the purpose of which is to diagnose gastric ulcers of malignant origin in advance.

This need becomes a requirement, since the therapy with omeprazole could mask some of the symptoms and signs associated with malignant diseases, delaying the diagnosis and the therapeutic approach.

Given the hepatic metabolism and subsequent renal excretion, the administration of ANTRA ® should be done with particular care, in patients with reduced liver and kidney function.

Dizziness, sleepiness, dizziness and headache could reduce the patient's perceptive and reactive abilities, making it dangerous to use machinery and drive vehicles.

PREGNANCY AND BREASTFEEDING

The total absence of both toxicological and pharmacokinetic studies on the intake of omeprazole during pregnancy does not allow us to establish the safety profile of ANTRA ®, thus discouraging the use of this medicine both during pregnancy and in the subsequent stage of breastfeeding.

Interactions

As is known, omeprazole is metabolized by the cytochrome p450, therefore it is able to interfere with the normal absorption of drugs such as warfarin and vitamin K antagonists, phenytoin, diazepam and tacrolimus, normally metabolized by the same enzyme.

On the contrary, the absence of interactions with antibiotics such as metronidazole and amoxiciliin, allows synergistic therapy in the treatment of the eradication of Helicobacter Pylori.

The antacid action induced by omeprazole could reduce the absorption of particular drugs that require particularly acid pH.

ANTRA ® Omeprazole Contraindications

ANTRA ® is against indicated in patients with known hypersensitivity to the active ingredient or to one of its excipients, and during the period of pregnancy and lactation.

Undesirable effects - Side effects

Therapy with ANTRA has proved to be very well tolerated, with clinically little relevant side effects and usually limited to the period of administration.

The most documented adverse reactions involve the gastrointestinal tract with diarrhea, constipation, nausea / vomiting, flatulence, the central nervous system with headache, drowsiness, dizziness and vertigo.

Endocrine, hepatic and renal diseases were rarer with impaired function of these organs.

Prolonged intake of proton pump inhibitors may be associated with the appearance of clinically insignificant gastric cysts and opportunistic pathogens.