Omeprazole: instructions for use,contraindications, indications, dosage, side effects

Update: October 2018

Omeprazole – a popular drug from the group of organotropic
gastrointestinal agents used in the treatment of inflammatory –
destructive diseases of the digestive system. Renders
active inhibitory effect on the production of hydrochloric acid in
terminal stage of its synthesis. Omeprazole is standard
scheme of complex treatment of peptic ulcer.

Фармакологическая группа: Входит в группу ингибиторов
proton pump.

The composition of the drug, release form, price

  • Main substance: Omeprazole
  • Auxiliary substances: Glycerin, nipagin, gelatin, nipazol,
    sodium lauryl sulfate, titanium dioxide, purified water, E 129
    (dye).

Omeprazole is available in opaque solid capsules of 10, 20,
40 mg, consisting of 2 parts: one part is red and the second is
white. The contents of the capsules are spherical pellets.
white or light beige.

10 capsules in a cell contour packaging, 1, 2, 3
Packing in a carton box. Also available in polymer
the bank.

Price:

  • 10 mg № 28: 65-82 rubles;
  • 20 mg number 10: 29-30 rubles;
  • 20 mg № 20: 41-42 rubles;
  • 40 mg № 28: 131-154 rubles.

pharmachologic effect

Omeprazole is an active anti-ulcer drug.
the action of inhibiting the enzyme H + / K + -adenosine triphosphate
(ATP) -phase.

The action of omeprazole is associated with inhibition of the activity of the indicated
enzyme, another name for which is the proton pump. Deactivation
enzyme occurs in the parietal cells of the stomach: blocked
transfer of hydrogen ions necessary for the implementation of the terminal
stages of the synthesis of hydrochloric acid.

Omeprazole is a prodrug, i.e. acts as
active metabolite. Under the influence of the acidic environment of the tubules
gastric parietal cells omeprazole for 2-4 minutes
biotransformed into sulfenamide, which reacts
blocking membrane H + / K + – adenosine triphosphate (ATP) -phase,
connecting to the enzyme through a disulfide bridge.

This mechanism of action explains the high selectivity
drug against parietal cells – it is in them
the medium required for the conversion of omeprazole into an active metabolite.
In this case, sulfenamide is not absorbed, since it is
cation.

  • Omeprazole has a suppressive effect on secretion as
    basal and stimulated salt food irritant
    acid.
  • Inhibits pepsin production and reduces total secretion
    stomach.
  • In addition, omeprazole has gastroprotective activity.
    obscure mechanism.

Does not affect the formation of the internal factor Castle and
on the speed of passage of the food mass through the stomach in
duodenum; does not affect histamine and
acetylcholine receptors.

The microgranules in the capsules are coated with a thin shell,
the gradual release of which results in:

  • to the beginning of the action of the drug about 60 minutes after
    reception
  • reaching therapeutic maximum after 120 minutes
  • the effect of omeprazole persists for a day or more
  • inhibition of half of the maximum gastric secretion in the background
    reception 20 мг омепразола продолжается в течение суток.

Thus, a single dose of omeprazole during the day
quickly and effectively inhibits daytime and nighttime secretion of salt
acid. Inhibitory effect becomes maximal after 4 days
from the start of treatment. In patients with ulcerative lesions of the gastrointestinal mucosa
taking 20 mg of omeprazole leads to the maintenance of the pH inside the stomach inside the
for 17 hours. Прекращение reception омепразола приводит к
recovery of gastric secretory activity after 3-5 days.

Pharmacokinetics

It has high absorption. Bioavailability reaches 30-40%,
increases in older people, and when liver failure
comes to 100%. The drug has high lipophilicity,
as a result, it easily enters the parietal cells. Enters into
communication with plasma proteins (albumin and acid
alpha1-glycoprotein) up to 90-95%.

The half-life of about 0.5-1 h, increases to 3 h at
liver failure. Clearance – 500-600 ml / min.
Metabolized in the liver almost fully, forming 6
inactive metabolites. Inhibits CYP2C19 isoenzyme. About 70-80
% of the drug is excreted by the kidneys, and 20-30% by bile.

Chronic renal failure, advanced age leads to
reduce the rate of elimination of omeprazole in proportion to the decrease
Creatine clearance rate.

Indications for use Omeprazole

  • Gastropathy during treatment with NSAIDs;
  • Peptic ulcer and duodenal ulcer, including
    including caused by Helicobacter pylori. Assigned as
    anti-relapse treatment and in the acute phase.
  • Reflux esophagitis, including a form of erosive nature.
  • Conditions occurring with hypersecretion of gastric juice:
    • polyendocrine adenomatosis;
    • Zollinger – Ellison syndrome;
    • gastrointestinal ulcers on the background of stress;
    • systemic mastocytosis.

Contraindications

Caution is advised to a group of patients with renal or
hepatic insufficiency. In the instructions for use of omeprazole
the absolute contraindications to treatment are indicated:

  • Pregnancy;
  • Lactation;
  • Childhood;
  • Hypersensitivity.

Application, dosage

Капсулы предназначены для reception внутрь целиком. Usually their
taken in the morning before meals, without chewing and drinking water. Omeprazole
can be taken simultaneously with food.

Exacerbation of YABZH and 12-perstroy intestine, gastropathy on the background of NSAIDs,
reflux esophagitis

  • on 20 mg of omeprazole once a day.
  • тяжелая форма reflux esophagitisа: 40 мг омепразола однократно в
    day.

A course of treatment:

  • duodenal ulcer: 2-4 weeks, can be extended
    up to 4-5 weeks;
  • ЯБЖ, reflux esophagitis, поражения ЖКТ на фоне терапии НПВС: 4-8
    weeks.

Patients who are not sensitive to other anti-ulcer drugs

  • по 40 мг омепразола в day. The course of treatment of ulcerative lesions
    The duodenum is 4 weeks old,
  • ЯБЖ и reflux esophagitisа – 8 weeks.

The use of omeprazole for the treatment of patients with insufficiency
liver function:

Доза снижается до 10-20 мг препарата однократно в day. With
severe forms – the daily dose should not exceed 20 mg. Have
patients with renal disease and elderly people do not adjust dose
required.

Other

  • Zollinger syndrome – Elisson: 60 mg daily, permissible
    increasing the dose to 80-120 mg (in this case, it is divided into 2
    reception).
  • Prevention of peptic ulcer exacerbations: 10 mg once a day.
    day.
  • Eradication of the bacterium Helicobacter pylori: 20 mg of omeprazole 2
    once a day (with parallel etiotropic therapy).

Side effect

  • Digestive organs: abdominal pain, diarrhea or constipation, nausea
    and vomiting, flatulence. Rarely increased hepatic activation
    enzymes, there is a perversion of taste, stomatitis, dry mucous membranes
    mouth Have пациентов с тяжелыми патологиями печени возможно развитие
    hepatitis A.
  • Нервная система: With сопутствующих соматических заболеваниях в
    severe form of dizziness, headaches, depressive
    condition, arousal. Have пациентов с тяжелыми патологиями печени
    encephalopathy is possible.
  • Musculoskeletal system: rarely develop myasthenia,
    arthralgia, myalgia.
  • Hematopoietic system: rarely – leukopenia, agranulocytosis,
    thrombocytopenia, pancytopemia.
  • Skin: in rare cases – itching or rash,
    photosensitization, exudative erythema multiforme,
    alopecia.
  • Allergic reactions: angioedema, urticaria,
    fever, bronchospasm, anaphylactic shock.
  • Other: редко возможны нарушения зрения, отеки конечностей,
    malaise, increased sweating, gynecomastia, formation
    reversible benign gastric glandular cysts
    with long-term treatment.

Drug interactions

  • Reduces the absorption of iron salts, ampicillin esters,
    Itraconazole and ketoconazole.
  • May increase blood concentrations of the following drugs:
    diazepam, indirect anticoagulants, phenytoin,
    clarithromycin. Data groups of drugs
    metabolized in the liver by the cytochrome CYP2C19 enzyme,
    which is inhibited by omeprazole.

special instructions

Before use, oncopathology of the gastrointestinal tract is necessarily excluded,
because omeprazole can erase symptoms and delay
way of making the correct diagnosis.

Overdose

There is confusion, drowsiness, blurred vision,
dry mouth, nausea, arrhythmia, tachycardia, headache
pain. There is no specific antidote, the treatment is symptomatic.

Omeprazole — аналоги:

Аналоги Omeprazoleа — лосек, омез, хелицид, зероцид, ромесек,
gastrosol, bioprazole, demeprazole, lomac, chrismel, zolser, omegast,
Omezol, Zerocide, Omitox, Omepar, Zhelizol, Pepticum, Omipix,
Promez, Pepicum, Rishek, Romsek, Soprati, Ulthop, Cisagast, Helol,
orthanol

Other drugs proton pump inhibitors include:

  • Pantoprazole-based drugs – sanpraz, nolpaza,
    kontrolik, peptazol.
  • Esomeprazole – Nexium.
  • Lansoprazol preparations – lanzap, lansofed, helicol, lansotop,
    epicure, lantsid.
  • On the basis of rabeprazole – zolispan, parite, zulbeks, ontime,
    Hayrabesol, rabodek.
  •  Orthanol

10 mg. 14 pcs 100 r.

40 mg. 14 pcs 200 r.

  • Omez

10 mg. 10 pcs 70 r.

20 mg. 30 pieces 190 r.

  • Haveльтоп

10 mg. 14 pcs. 112 rub.

20 mg. 14 pcs. 150 rub.

  • Losek map

10 mg. 14 pcs 230-270 p.

  • Gastrosol

20 mg. 14 pcs 80 r.

20 mg. 28 pcs 160 r.

Автор: врач-гигиенист, эпидемиолог

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