Lansoprazol

General characteristics. Structure:

Active ingredient: 15 mg or 30 mg of a lansoprazol in 1 capsule.

Antiulcerous drug.

Pharmacological properties:

Pharmacodynamics. Blocks a final mode of formation of hydrochloric acid. In tubules of covering cells of a stomach it is transformed to an active form — sulfonamide, it is irreversible interacting with the H+-K+-Atfazy SH groups (the proton pump). Reduces basal and stimulated (food, Pentagastrinum, insulin) secretion and volume of a secret. Speed and degree of inhibition of secretion of hydrochloric acid are dozozavisimy: after reception of 15 and 30 mg of pH begins to increase in 1–2 and 2–3 h, and secretion goes down to 80–97%, respectively. Recovery of activity of H+-K+-Atfazy happens to a half-cycle of 30-48 h. Average daily value рН a gastric juice increases to 2,9 (the preservation time percent рН> 3 makes 47,6).

After the reception termination the level of acid remains lower than 50% basal during 39 h, ricochet increase in secretion (is not noted). At patients with Zollinger's syndrome — Ellisona acts more for a long time. Oppresses production of pepsin (pepsinogen level in blood serum increases). Has gastroprotektivny effect: increase in oxygenation of a mucous membrane, increase in secretion of bicarbonates. Suppresses Helicobacter pylori growth (MPK makes 0,78–6,25 mg/l), promotes education in a mucous membrane of specific IgA to these bacteria, increases antikhelikobakterny activity of other drugs. Reduces a blood stream in antral department of a stomach, the gatekeeper and a bulb of a duodenum on average by 17%, slows down motor эвакуаторную function of a stomach. Oppression of secretion is followed by increase in number of nitrozobakteriya and increase in concentration of nitrates in a gastric secret. Increases concentration of gastrin in blood serum for 50–100% (level of gastrin reaches the plateau in 2 months of treatment and is returned to reference values after the termination of a course of treatment). Provides more bystry healing and weakening of symptoms at a duodenum ulcer (85% of duodenal ulcers begin to live in 4 weeks of treatment at a dose of 30 mg/days). It is effective at therapy of stomach ulcer and a duodenum, resistant to H2 blockers. Frequency of recuring of round ulcers after treatment makes 55–62%. At a reflux esophagitis full treatment by the end of 8 weeks of reception (30 mg/days) is noted at 88,7%.

Causes a hyperplasia of enterokhromafinopodobny (ECL-) cells, increases the frequency of a metaplasia of an epithelium of a mucous membrane of a stomach and formation of adenoma in intersticial fabric of seed plants at introduction of high doses of a lansoprazol an experimental animal.

Некислотоустойчив therefore it is applied, as a rule, in the form of the granules having the acid resisting covering interfering destruction in a stomach. Almost it is completely soaked up from a small intestine and comes to a system blood stream. Against the background of cirrhosis absorption is slowed down. Absolute bioavailability makes not less than 80%, decreases by 50% after meal (the anti-secretory effect is weakened).

Pharmacokinetics. After intake of 30 mg of a lansoprazol of Cmax  (0,75–1,15 mg/l) is defined by 1,5–2,2 h (on average — in 1,7 h), time of achievement of Cmax  at reception is less in the morning, than at reception in the evening. In the range of doses from 15 to 60 mg the pharmacokinetics is linear — concentration in plasma are proportional to a dose, parameters are constant and cumulation does not happen. Linkng with proteins of plasma — 97–99% (at concentration from 0,05–5,0 mkg/ml). Well gets into fabrics, in particular, in obkladochny cells of a stomach. Distribution volume — 0,5 l/kg. T1/2  healthy examinees of 1,5 h, at elderly patients have 1,9–2,9 h, patients with an abnormal liver function have 3,2–7,2 h and is shortened at a renal failure. Sulphone - and oxyderivatives is metabolized in a liver with the participation of fermental system of P450 cytochrome with education sulfinil-. It is excreted in the form of two main inactive metabolites with bile (2/3) and with urine (the renal failure significantly does not influence the speed and size of excretion).

Indications to use:

Not ulcer dyspepsia, peptic ulcer of a stomach and duodenum, benign stomach ulcer, erosive and ulcer esophagitis, reflux esophagitis, Zollingera-Ellison's syndrome, Helicobacter pylori infection (the combined treatment).

Route of administration and doses:

Inside, in the morning. Not ulcer dyspepsia: 15–30 mg/days during 2–4 weeks. Duodenum ulcer: 30 mg/days during 2–4 weeks. Stomach ulcer: 30–60 mg/days during 4–8 weeks.

Erosive and ulcer esophagitis: 30–60 mg/days during 4–8 weeks. Reflux esophagitis: 30 mg/days — 4 weeks.

Zollinger's syndrome — Ellisona: in individually picked up dose providing the level of a basal kislotoproduktion 10 mmol/h are lower.

Helicobacter pylori infection: on 30 mg 2 times a day as a part of various schemes of the combined antikhelikobakterny therapy.

Features of use:

Use at pregnancy and feeding by a breast. It is contraindicated in the I trimester. In II and III trimesters it is possible if the expected advantage of therapy exceeds potential risk for a fruit.

Category of action on a fruit on FDA — B. For the period of treatment it is necessary to stop breastfeeding.

Before the beginning and after the end of therapy endoscopic control for an exception of malignant new growths is obligatory (лансопразол can mask symptoms and delay establishment of the diagnosis).

With care apply at patients with the lowered function of a liver and at patients of advanced age (treatment begin with half doses, gradually increasing them to recommended, but no more than 30 mg/days).

At simultaneous use with antacids it is necessary to appoint them 1 h to or in 1–2 h after reception of a lansoprazol.

Side effects:

From bodies of a GIT: diarrhea; less often — increase or a loss of appetite, nausea, abdominal pains; seldom — a lock; in some cases — nonspecific ulcer colitis, GIT candidiasis, increase in activity of liver enzymes (ALT, nuclear heating plant, ShchF, gamma глутамилтрансфераза, a lactate dehydrogenase) and bilirubin.

From a nervous system and sense bodys: headache; seldom — feeling of an indisposition, dizziness, drowsiness, a depression, alarm.

From respiratory system: seldom — a severe cough, pharyngitis, rhinitis, an inflammation or an upper respiratory tract infection.

From cardiovascular system and blood: seldom — thrombocytopenia (with hemorrhagic manifestations); in some cases — anemia.

From integuments: in some cases — a photosensitization, a mnogoformny erythema, an alopecia.

Allergic reactions: skin rash.

Others: seldom — a grippopodobny syndrome, a mialgiya.

Interaction with other medicines:

Lowers (for 10%) clearance of theophylline.

Sukralfat reduces bioavailability by 30% (the interval 30–40 min. between receptions of these drugs is necessary).

The antacids containing алгелдрат and magnesium hydroxide at a concomitant use with lansoprazoly can reduce absorption of the last.

Can change pH-dependent absorption of the medicines relating to groups of weak acids (delay) and the bases (acceleration).

Slows down absorption of ampicillin, digoxin, a ketokonazol, cyanocobalamine, iron salts.

Interaction with the drugs which are metabolized with the participation of fermental system of P450 cytochrome is possible.

Let's combine with antipyrine, diazepam, an ibuprofen, indometacin, peroral contraceptives, Phenytoinum, Prednisolonum, propranolol, warfarin.

Contraindications:

Hypersensitivity, malignant new growths of a GIT, pregnancy (especially I trimester), feeding by a breast.

Restrictions to use. An abnormal liver function, age up to 18 years (safety and efficiency at these patients is studied insufficiently), advanced age.

Overdose:

Symptoms: are not described (the single dose in a dose of 600 mg was not followed by clinical manifestations of overdose).

Treatment: observation, performing the supporting and symptomatic therapy is recommended. The hemodialysis is inefficient.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules of 15 mg and 30 mg. On 10 capsules in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.