Omez D 30 capsules — Made in India — Free Delivery

Name: Omez D 30 capsules — Made in India — Free Delivery
Brand: Dr. Reddy's
Price: 21.8785 USD
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Brand: Dr. Reddy's
Product Code: Omez D
Availability: In Stock

$21.88

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Description

Pharmacological properties

Pharmacodynamics. Omeprazole is an antisecretory antiulcer agent that reduces spontaneous and stimulated gastric secretion due to inhibition of the n + / k + -atphase (proton pump), which is necessary for the transport of hydrogen ions. suppresses the final phase of basal and stimulated release of hydrochloric acid, regardless of the nature of the stimulus.

Domperidone is a dopamine receptor antagonist, prokinetic. Practically does not penetrate the BBB. Increases the duration of peristaltic contractions of the antrum of the stomach and duodenum, the rate of stomach release, increases the tone of the lower esophageal sphincter. Does not affect digestive secretion. It has an antiemetic effect, which is a combination of gastrokinetic action and antagonism to dopamine receptors in the chemoreceptor trigger zone outside the BBB.

Pharmacokinetics

Omeprazole. Omeprazole is rapidly absorbed. Cmax is achieved within 1-2 hours after oral administration of the preparation. The absorption of omeprazole occurs in the small intestine and is usually completed within 3-6 hours. Simultaneous food intake does not affect the bioavailability of omeprazole. The bioavailability of a single oral dose of the preparation is about 40%. With repeated use in the 1 time per day regimen, bioavailability increases to 60%.

The volume of distribution in healthy volunteers is about 0.3 l / kg of body weight. Omeprazole binds to plasma proteins by 97%.

Omeprazole is completely metabolized by the cytochrome P450 (CYP) system, mainly with the participation of CYP 2C19, which is responsible for the formation of hydroxyomeprazole as the main metabolite of omeprazole in blood plasma. The sulfone derivative of omeprazole is formed with the participation of another isoform, namely CYP 3A4. Due to the high affinity of omeprazole for CYP 2C19, competitive inhibition of the metabolism of other substrates by this isoform is possible. However, the affinity of omeprazole for CYP 3A4 is low; therefore, omeprazole cannot inhibit the metabolization of other CYP 3A4 substrates. However, omeprazole does not inhibit the main enzymes of the cytochrome P450 system.

T1 / 2 of omeprazole from blood plasma both with single and multiple doses - 1 hour. Omeprazole is completely excreted from the blood plasma in the period between taking the next doses. When applied once a day, there was no tendency to accumulation of the preparation. About 80% of the dose of omeprazole that enters the body is excreted in the urine as metabolites. The rest is excreted in the feces due to secretion in the bile.

With repeated use, the AUC for omeprazole increases. This increase is dose dependent and the relationship is not linear. The time and dose dependence is a consequence of a decrease in first-pass metabolism and systemic clearance, probably due to inhibition of CYP 2C19 by omeprazole and / or its metabolites (eg sulfone). Omeprazole metabolites do not affect gastric acid secretion.

Domperidone. After oral administration on an empty stomach, domperidone is rapidly absorbed. Cmax in blood plasma is reached within 30-60 minutes. The low absolute bioavailability of domperidone (about 15%) after oral administration is due to significant first-pass metabolism in the intestinal wall and liver. Although the bioavailability of domperidone increases in healthy volunteers when taken with food, patients with gastrointestinal complaints should take the preparation 15-30 minutes before meals. The reduced acidity of gastric contents interferes with the absorption of domperidone.

Bioavailability after oral administration is reduced with previous administration of cimetidine and sodium bicarbonate. If domperidone is used after a meal, the maximum absorption time is somewhat delayed, and the AUC increases.

Domperidone after oral administration does not accumulate and does not induce its own metabolism. Cmax in blood plasma 90 minutes after administration at a dose of 30 mg daily for 2 weeks is practically the same as after taking the first dose (21 ng / ml versus 18 ng / ml). Domperidone binds to blood plasma proteins by 91–93%.

Domperidone is rapidly and extensively metabolized in the liver by hydroxylation and N-dealkylation.

With urine and feces, 31 and 66% of the dose taken orally are excreted. An insignificant part of the preparation is excreted unchanged (10% with feces and 1% with urine). T½ from blood plasma after a single dose in healthy volunteers is 7-9 hours. This period is lengthened in patients with severe renal failure.

Indications

Functional dyspepsia, delayed evacuation of stomach contents and gastroparesis, reflux esophagitis, gastric ulcer and duodenal ulcer; in the schemes of helicobacter pylori eradication in the presence of gastroesophageal reflux.

Application

Take the capsules whole, without opening or chewing. the recommended dose depends on the course of the disease and is set individually. the average recommended dose for adults and children over the age of 12 is 1 capsule 2-3 times a day 30 minutes before meals with a glass of water. if necessary, the dose can be increased by a doctor to 2 capsules 2 times a day. the course of treatment is 4–8 weeks.

In eradication schemes, 2 capsules 2 times a day in combination with antibacterial agents.

Contraindications

Hypersensitivity to domperidone, omeprazole or other components of the preparation. prolactin-secretory tumor of the pituitary gland (prolactinoma). gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the stomach or intestines. severe or moderate impairment of liver and / or kidney function. the simultaneous use of ketoconazole, erythromycin or other potent inhibitors of cyp 3a4, preparations that lengthen the q – t interval, such as fluconazole, voriconazole, clarithromycin, amiodarone, telithromycin (see special instructions, interaction). simultaneous reception with atazanavir.

Side effects

Adverse reactions, information about which are given below, are classified by organs and systems and by frequency of occurrence: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥1 / 1000 and 1/100 ), rare (? 1/10 000 and 1/1000), very rare (1/10 000) and the frequency is unknown (the frequency cannot be determined from the available data).

From the immune system: rarely - angioedema; hypersensitivity reactions, including anaphylaxis, anaphylactic shock; fever; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis.

On the part of the skin and its appendages: infrequently - skin rash, itching, dermatitis, urticaria; rarely - alopecia, photosensitivity; very rarely - erythema multiforme.

Mental disorders: infrequently - anxiety; rarely - agitation, confusion, depression; very rarely - aggression, hallucinations; frequency unknown - nervousness.

From the nervous system: infrequently - headache, dizziness, paresthesia, drowsiness, insomnia; frequency unknown - convulsions, extrapyramidal reactions, irritability, agitation, akathisia, vertigo.

From the side of the cardiovascular system: very rarely - ventricular arrhythmias; frequency is unknown - lengthening of the Q – T interval, peripheral edema, palpitations, violation of the frequency and rhythm of heart contractions.

From the side of the organ of vision: rarely - blurred vision; frequency unknown - oculogyric crisis.

From the respiratory system: rarely - bronchospasm.

From the digestive tract: often - abdominal pain, constipation, diarrhea, flatulence; rarely - dry mouth, stomatitis, gastrointestinal candidiasis, taste perversion; frequency unknown - intestinal colic, regurgitation, change in appetite, change in taste, nausea, vomiting, heartburn, colitis, thirst.

From the side of the musculoskeletal system: rarely - arthralgia, myalgia; very rarely - muscle weakness; frequency unknown - leg pain.

From the hepatobiliary system: rarely - hepatitis with or without jaundice; very rarely - liver failure, encephalopathy in patients with pre-existing liver disease.

From the urinary system: rarely - interstitial nephritis; frequency unknown - urinary retention, dysuria, frequent urination.

Reproductive system disorders: infrequently - galactorrhea, pain in the area of the mammary glands; the frequency is unknown - gynecomastia, amenorrhea, increased prolactin levels, decreased or lack of libido, irregular menstrual cycle, breast edema, impaired lactation.

Metabolic disorders: rarely - hyponatremia; very rarely - hypomagnesemia.

From the side of the blood: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia.

Laboratory indicators: the frequency is unknown - an increase in the level of ALT, AST and CS, an increase in the content of prolactin in the blood serum.

Other disorders: infrequently - asthenia, malaise, peripheral edema; rarely - increased sweating; frequency unknown - conjunctivitis, lethargy.

Special instructions

When combined with domperidone, antacids or antisecretory preparations should be taken after meals, but should not be taken concomitantly with domperidone. patients who do not feel discomfort after eating and who have to constantly take domperidone for 2 weeks should consult a doctor. patients with nausea and vomiting lasting 48 hours should see a doctor.

In studies of interaction with the oral form of ketoconazole, a prolongation of the Q – T interval was noted. Although the value of this study is not clearly established, an alternative treatment should be chosen if antifungal therapy with ketoconazole is indicated (see INTERACTIONS).

Domperidone should be used with caution in patients with risk factors for prolongation of the Q – T interval, including hypokalemia, severe hypomagnesemia, organic heart disease, and in patients with mild hepatic and / or renal impairment.

If there is an ulcer or there is a suspicion of it, or one of such symptoms as a significant decrease in body weight that cannot be explained, vomiting, dysphagia, vomiting with blood or melena, the malignant process should be excluded, since treatment with omeprazole can mask its symptoms and delay determination of the diagnosis.

The preparation contains lactose, sucrose, so the preparation should not be used in patients with lactose intolerance, galactosemia and malabsorption of glucose / galactose, fructose, sucrose-isomaltose.

Domperidone can lead to an increase in prolactin levels, which causes galactorrhea in women and gynecomastia in men.

In patients with pheochromocytoma, when using domperidone, a hypertensive crisis may occur.

Patients should be informed that the preparation is not recommended as a remedy for motion sickness.

Consider the following information on the risk of developing complications of cardiovascular disease associated with preparations containing domperidone:

- some epidemiological studies have shown that domperidone may be associated with an increased risk of serious ventricular arrhythmias or sudden cardiac death;

- The risk of serious ventricular arrhythmias or sudden cardiac death may be higher in patients over the age of 60 or with oral administration of the preparation at doses above 30 mg / day.

Domperidone should be administered to adults and children at the lowest effective dose.

The risk-benefit ratio of domperidone remains favorable.

Omeprazole may reduce the absorption of cyanocobalamin. This should be borne in mind when the preparation is prescribed for a long time to patients with a reduced content of vitamin B12 in the body or in case of impaired absorption of vitamin B12 in the gastrointestinal tract.

The ability to influence the reaction rate when driving or working with other mechanisms. During treatment with the preparation, special care must be taken when driving vehicles and / or when working with potentially dangerous machinery.

Use during pregnancy and lactation. Do not use for pregnant women. If necessary, the appointment of the preparation, breastfeeding should be discontinued.

Children. The preparation is used to treat children aged 12 years and older and weighing at least 35 kg.

Interactions

Domperidone. anticholinergic preparations can neutralize the antidispeptic effect of domperidone.

Antacids and antisecretory preparations should not be taken concomitantly with domperidone, as they reduce its bioavailability after oral administration.

The main pathway of metabolic transformations of domperidone occurs with the participation of the isoenzyme CYP 3A4 of the cytochrome P450 system, therefore, with the simultaneous use of domperidone and preparations that significantly inhibit this isoenzyme, an increase in the level of domperidone in the blood plasma is possible.

Concomitant use with ketoconazole, erythromycin or other potential inhibitors of CYP 3A4 can lead to prolongation of the Q – T interval.

With the simultaneous use of domperidone at a dose of 10 mg 4 times a day and ketoconazole at a dose of 200 mg 2 times a day, an increase in the Q – T interval is noted by an average of 9.8 ms (from 1.2 to 17.5 ms individually). With the simultaneous use of domperidone at a dose of 10 mg 4 times a day and erythromycin at a dose of 500 mg 3 times a day, an increase in the Q – T interval is noted by an average of 9.9 ms (from 1.6 to 14.3 ms individually). In the equilibrium state, with such an interaction, Cmax and AUC for domperidone increases by about 3 times. In these studies, monotherapy with domperidone at a dose of 10 mg 4 times a day led to an increase in the Q – T interval by 1.6 ms (study of interaction with ketoconazole) and by 2.5 ms (study of interaction with erythromycin). Monotherapy with ketoconazole (200 mg 2 times a day) led to an increase in the Q – T interval by 3.8 ms, and monotherapy with erythromycin (500 mg 3 times a day) - by 4.9 ms.

Potent CYP 3A4 inhibitors with which domperidone is not recommended: azole antifungals such as fluconazole *, itraconazole * and voriconazole *; macrolide antibiotics such as clarithromycin * and erythromycin; HIV protease inhibitors such as amprenavir, atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir, and saquinavir; calcium antagonists such as diltiazem and verapamil; amiodarone *; amrepitant; nefazodone; telithromycin * (* prolong the Q – Tc interval). Domperidone can be combined with antipsychotics, the effect of which it enhances; dopaminergic agonists (bromocriptine, L-dopa), the undesirable peripheral actions of which - indigestion, nausea, vomiting - it suppresses without neutralizing the main properties.

Omeprazole. A decrease in acidity in the stomach during the use of omeprazole can alter the absorption of preparations for which this process is pH-dependent. With the simultaneous use of omeprazole with nelfinavir, atazanavir, the concentration of the latter in the blood plasma decreases. The combined use of omeprazole with nelfinavir is contraindicated. The use of omeprazole at a dose of 40 mg once a day reduces the content of nelfinavir by an average of 40%, and its pharmacologically active metabolite M8 by 75–90%. Another interaction mechanism is possible through CYP 2C19.

The combined use of omeprazole with atazanavir is contraindicated. With the simultaneous use of omeprazole at a dose of 40 mg once a day and atazanavir 300 mg / ritonavir 100 mg in healthy volunteers, the effect of atazanavir is reduced by 75%. Increasing the dose of atazanavir to 400 mg does not compensate for this effect of omeprazole. With the combined use of omeprazole at a dose of 20 mg once a day and atazanavir 400 mg / ritonavir 100 mg in healthy volunteers, the effect of atazanavir is reduced by about 30%.

Increases in serum levels of other antiretroviral agents such as saquinavir have been reported. There are also other antiretroviral preparations, the levels of which in blood plasma remained unchanged when used concomitantly with omeprazole.

The combined use of omeprazole at a dose of 20 mg 1 time per day with digoxin in healthy volunteers increases the bioavailability of digoxin by 10%. Although no toxic effects of digoxin have been reported in such cases, caution should be exercised when using high doses of omeprazole with digoxin in the elderly.

In a crossover clinical study, with the simultaneous use of clopidogrel (loading dose of 300 mg, and then 75 mg / day) with omeprazole (80 mg with simultaneous administration) for 5 days, the effect of the active metabolite of clopidogrel decreased by 46% (1st day) and by 42% (2nd day). Platelet aggregation decreased by 47% after 24 hours and by 30% on the 5th day. In another clinical study, it was shown that taking clopidogrel and omeprazole at different times does not prevent this interaction, which is probably due to inhibition of CYP 2C19 caused by the preparation.

The use of omeprazole significantly reduces the absorption of posaconazole, erlotinib, ketoconazole and itraconazole, as a result of which the clinical efficacy of these preparations may decrease.

Omeprazole inhibits CYP 2C19, the main omeprazole metabolizing enzyme. Thus, the metabolism of concomitant preparations also metabolized by CYP 2C19, such as diazepam, phenytoin, warfarin (R-warfarin) or other vitamin K antagonists and cilostazol, may be slowed down. Monitoring of patients taking phenytoin is recommended; it may also be necessary to reduce the dose of phenytoin. However, the simultaneous use of 20 mg of omeprazole per day did not change the concentration of phenytoin in the blood plasma of patients who used this preparation for a long time. Monitoring of the international normalized ratio is recommended in patients who are using warfarin or other vitamin K antagonists; dose reduction of warfarin (or other vitamin K antagonist) may be required. The simultaneous use of 20 mg of omeprazole per day, however, did not change the coagulation time in patients who used warfarin for a long time.

Omeprazole is also partially metabolized by CYP 3A4, but does not suppress this enzyme. Thus, omeprazole does not affect the metabolism of preparations that are metabolized by CYP 3A4, such as cyclosporine, lidocaine, quinidine, estradiol, erythromycin, and budesonide. An increase in the level of methotrexate has been reported in some patients while taking it with proton pump inhibitors. If it is necessary to use methotrexate in high doses, consideration should be given to temporarily discontinuing omeprazole.

The simultaneous use of omeprazole with tacrolimus can lead to an increase in the concentration of tacrolimus in the blood plasma. At the beginning or after treatment with the preparation, it is recommended to monitor the concentration of tacrolimus in the blood plasma.

With the simultaneous use of omeprazole and inhibitors of CYP 2C19 and CYP 3A4 (for example, clarithromycin and voriconazole), an increase in the content of omeprazole in the blood plasma is possible due to a decrease in the metabolism of the latter. The combined use of voriconazole and omeprazole doubles the effects of the latter. Since such an increase in the content of omeprazole is quite acceptable, usually no dose adjustment is required, except in patients with severe hepatic impairment or in the case of a long course of treatment.

Preparations that induce CYP 2C19, CYP 3A4, or both enzymes (eg rifampicin) can lead to a decrease in the level of omeprazole in the blood plasma by accelerating its metabolism.

Overdose

Overdose due to the action of domperidone. symptoms: agitation, impaired consciousness, convulsions, disorientation, drowsiness, extrapyramidal disorders.

Treatment: gastric lavage, intake of activated charcoal, cholinergic receptor blockers to eliminate extrapyramidal disorders. In the event of extrapyramidal reactions, anticholinergic preparations and preparations are used to treat parkinsonism.

Overdose due to the action of omeprazole. Symptoms: nausea, vomiting, dizziness, abdominal pain, flatulence, diarrhea, headache, tachycardia, apathy, depression, confusion. All symptoms are transient. The excretion rate remains unchanged regardless of the dose (primary kinetics).

Treatment: symptomatic.

Storage conditions

In a dry, dark place at temperatures up to 25 ° C.

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