Imodium Express lyophilisate pills 2mg, 10pcs

Product description

Imodium® (Imodium®) is the world’s No. 1 brand for stopping diarrhea among loperamide-based products (by sales in monetary terms).

Composition

1 tablet contains:

Active ingredient:

loperamide hydrochloride 2 mg;

Auxiliary substances:  

gelatin – 5.863 mg,

mannitol-4.397 mg,

aspartame-0.75 mg,

mint flavor-0.3 mg,

sodium bicarbonate-0.375 mg,

purified water-136.315 mg (removed during lyophilization).

Clinical Pharmacology

Pharmacodynamics : Loperamide binds to opioid receptors in the intestinal wall and inhibits the release of acetylcholine and prostaglandins, thus slowing down peristalsis and increasing the time of passage of contents through the intestine. Increases the tone of the anal sphincter, thereby reducing fecal incontinence and the urge to defecate. As a result of a clinical study, data were obtained that the antidiarrheal effect occurs within one hour after taking a single dose (4 mg). Pharmacokinetics: Most of loperamide is absorbed in the intestine, but due to active presystemic metabolism, the systemic bioavailability is approximately 0.3%. Data from preclinical studies indicate that loperamide is a P – glycoprotein substrate. The binding of loperamide to plasma proteins (mainly albumin) is 95%. Loperamide is mainly metabolized in the liver, conjugated and excreted in the bile. Oxidative N-demethylation is the main route of loperamide metabolism and is mainly carried out with the participation of an inhibitor of the CYP3A4 and CYP2C8 isoenzymes. Due to active presystemic metabolism, the concentration of unchanged loperamide in blood plasma is negligible. In humans, the average half-life of loperamide is 11 hours, ranging from 9 to 14 hours. Unchanged loperamide and its metabolites are mainly excreted in the faeces. Pharmacokinetic studies in children have not been conducted. It is expected that the pharmacokinetics of loperamide and its interaction with other drugs will be similar to those in adults.

Indications

Acute and chronic diarrhea( diarrhea); regulation of stool in patients with ileostoma

Use during pregnancy and lactation

Use during pregnancy There is no evidence that loperamide has a teratogenic or embryotoxic effect. Imodium Express is contraindicated during the first trimester of pregnancy. During the II-III trimesters of pregnancy, Imodium® Express can only be used after consultation with your doctor. The drug can be Use during breast-feedingmultiple amounts of loperamide can enter breast milk, so Imodium ® Express is not recommended to be taken during breastfeeding.

Contraindications

-acute dysentery and other gastrointestinal infections (caused, including Salmonella spp., Shigella spp., Campylobacter spp. ); – intestinal obstruction (including if necessary, avoid suppression of peristalsis);- diverticulosis;- acute ulcerative colitis;- pseudomembranous enterocolitis (diarrhea caused by taking antibiotics); – I trimester of pregnancy— – lactation (breastfeeding);— children under 6 years of age;- hypersensitivity to loperamide and / or other components of the drug.

Side effects

Adverse reactions are undesirable events for which a proven causal relationship with the use of loperamide should be considered based on a comprehensive assessment of the available information about the adverse event. In some cases, it is quite difficult to reliably establish a causal relationship between taking loperamide and the occurrence of these symptoms. In addition, since clinical trials are conducted in different settings, the frequency of adverse reactions in clinical trials of one drug cannot be directly compared with the frequency of adverse reactions in clinical trials of another drug and may not reflect the frequency of adverse reactions in clinical practice. According to clinical studies, adverse reactions observed in ≥1% of patients taking Imodium® for acute diarrhea: headache, constipation, flatulence, nausea, vomiting. Adverse reactions observed in patients with Adverse reactions observed in ≥1% of patients taking Imodium® for chronic diarrhea: dizziness, flatulence, constipation, nausea. Adverse reactions observed in patients with

Interaction

According to preclinical studies, loperamide is a P-glycoprotein substrate. With the simultaneous use of loperamide (a single dose of 16 mg) and quinidine or ritonavir, which are P-glycoprotein inhibitors, the concentration of loperamide in blood plasma increased 2-3 times. The clinical significance of the described pharmacokinetic interaction with P-glycoprotein inhibitors when using loperamide at the recommended doses is unknown. Simultaneous use of loperamide (a single dose of 4 mg) and itraconazole, an inhibitor of the CYP3A4 isoenzyme and P-glycoprotein, resulted in a 3-4-fold increase in the concentration of loperamide in blood plasma. In the same study, the use of an inhibitor of the CYP2C8 isoenzyme, gemfibrozil, led to an increase in the concentration of loperamide in blood plasma by approximately 2 times. When using a combination of itraconazole and gemfibrozil, the peak concentration of loperamide in blood plasma increased by 4 times, and the total concentration-by 13 times. This increase was not associated with the effect on the central nervous system, which was assessed by psychomotor tests (i. e. subjective assessment of drowsiness and digital character replacement test). Concomitant use of loperamide (a single dose of 16 mg) and ketoconazole, a CYP3A4 inhibitor and P-glycoprotein, resulted in a fivefold increase in the concentration of loperamide in blood plasma. This increase was not associated with an increase in the pharmacodynamic effect estimated by pupil size. With simultaneous oral use of desmopressin, the concentration of desmopressin in blood plasma increased by 3 times, probably due to a slowdown in gastrointestinal motility. It is expected that drugs with similar pharmacological properties can enhance the effect of loperamide, and drugs that increase the rate of passage through the gastrointestinal tract can reduce the effect of loperamide.

How to take, course of use and dosage

Inside. The tablet is placed on the tongue, within a few seconds it dissolves, after which it is swallowed with saliva, without drinking water. Adults and children over 6 years of age:

• Acute diarrhea: the initial dose is 2 tablets (4 mg) for adults and 1 tablet (2 mg) for children, then 1 tablet (2 mg) after each act of defecation in case of loose stools.
• Chronic diarrhea: the initial dose is 2 tablets (4 mg) per day for adults and 1 tablet (2 mg) for children; further, the initial dose should be adjusted so that the frequency of a normal chair was 1-2 times a day, which is usually achieved with a maintenance dose of 1 to 6 tablets (2-12 mg) per day.

The maximum daily dose should not exceed 6 tablets (12 mg); the maximum daily dose in children is calculated based on body weight (3 tablets per 20 kg of body weight of the child), but should not exceed 6 tablets (12 mg). If the stool is normalized or if there is no stool for more than 12 hours, the drug is canceled. Use in children: Do not use Imodium® in children under 6 years of age. Use in elderly patients: No dose adjustment is required in the treatment of elderly patients. Use in patients with impaired renal function: No dose adjustment is required in the treatment of patients with impaired renal function. Use in patients with impaired liver function: Although pharmacokinetic data are not available in patients with hepatic insufficiency, Imodium® should be used with caution in such patients due to delayed presystemic metabolism (see section “Special instructions”). INSTRUCTIONS FOR USE Since freeze-dried tablets are quite fragile, do not push them through the foil to avoid damage. In order to remove the tablet from the blister, follow these steps: take the foil by the edge and completely remove it from the cell where the tablet is located; gently push down from the bottom and remove the tablet from the package.

Overdose

Symptoms. In case of overdose (including relative overdose due to impaired liver function), urinary retention, paralytic intestinal obstruction, signs of central nervous system (CNS) depression may occur: stupor, impaired coordination, drowsiness, miosis, muscle hypertonus, respiratory depression. Children may be more sensitive to the effects of loperamide on the central nervous system than adults. Therapy. If symptoms of overdose occur, naloxone can be used as an antidote. Since the duration of action of loperamide is longer than that of naloxone (1-3 hours), repeated use of naloxone may be required. Therefore, it is necessary to carefully monitor the patient’s condition for at least 48 hours in order to detect signs of possible CNS depression in a timely manner.

Special instructions

Treatment of diarrhea with Imodium® is only symptomatic. In cases where it is possible to determine the cause of diarrhea, appropriate therapy should be carried out. Patients with diarrhea, especially children, may experience fluid and electrolyte loss.In such cases, it is necessary to carry out appropriate replacement therapy (replenishment of fluid and electrolytes). Imodium ® freeze-dried tablets contain a source of phenylalanine. Admission to patients with phenylketonuria is contraindicated. If there is no effect after 2 days of treatment, it is necessary to stop taking the drug, clarify the diagnosis and exclude the infectious genesis of diarrhea. AIDS patients taking Imodium® to treat diarrhea should stop taking the drug at the first sign of bloating. There have been isolated reports of constipation with an increased risk of developing toxic megacolon in patients with AIDS and infectious colitis of viral and bacterial etiology who were treated with loperamide. Although there are no data on the pharmacokinetics of loperamide in patients with hepatic insufficiency, Imodium® should be used with caution in such patients due to delayed presystemic metabolism, since this can lead to relative overdose and toxic damage to the central nervous system. If the medicine has become unusable or the expiration date has expired, do not throw it into the sewage system or on the street! Place the medicine in a plastic bag and put it in the trash can. These measures will help protect the environment!

Form of production

White or almost white, round lyophilized tablets.

Storage conditions

Store at a temperature of 15 to 30 °C. Keep out of reach of children.

Active ingredient

Loperamide

Dosage form

Tablets