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Imodium
Imodium is a medicine that has a depressing effect on the function of peristalsis.
Indications of the imodium
It is shown for elimination of such violations:
- treatment of symptoms of acute diarrhea (for children from 12 years old, as well as adults);
- treatment of signs of acute types of diarrhea that occurs due to IBS (for adults over 18 years of age) provided that the doctor prescribes a primary diagnosis.
Pharmacodynamics
Loperamide hydrochloride is synthesized with opiate endings on the walls of the intestine. With this action, the process of releasing PG as well as acetylcholine is inhibited, as a result of which the translational peristalsis is reduced and the period of passage of foods along the digestive tract is prolonged, and with it the capacity of the intestinal walls to absorb liquids is increased.
The active component of the drug increases the tone of the anal sphincter, which reduces the incontinence of the stool along with the urge to empty the intestine.
Pharmacokinetics
A large number of orally consumed loperamide is absorbed into the intestine, but intensive metabolic processes during the first passage provide only 0.3% of the systemic bioavailability of the substance.
The test data of the substance in rats relative to the distribution parameters demonstrated that it has a strong affinity for the intestinal walls, mainly with subsequent synthesis with endings within the longitudinal layer of the musculature. The synthesis of the component with the protein is 95%, mainly it binds to albumins. Preclinical information demonstrates that loperamide is a substrate of the P-glycoprotein.
Extraction of loperamide almost all occurs in the liver. Here it is mainly conjugated, and then excreted together with bile. Oxidative process of N-demethylation is the main way of substance metabolism, which is carried out mainly with the help of elements CYP3A4, and also CYP2C8. Since the first hepatic pass at it is very intense, the plasma index of unchanged drugs remains rather low.
The half-life of the substance in humans is about 11 hours (range within 9-14 hours). The unchanged component with its decay products is mainly excreted with feces.
Contraindications
Among the contraindications of drugs:
- strong intolerance to loperamide hydrochloride, and in addition to any of the other elements of the drug;
- children age less than 12 years;
- in the presence of an acute form of dysentery, which is characterized by high fever, as well as blood in the stool;
- in the acute stage of ulcerative colitis or with pseudomembranous form of colitis, which are associated with the use of antibiotics having a wide range of effects;
- with the bacterial form of enterocolitis provoked by microbes from the genus Salmonella, Shigella or Campylobacter.
It is not recommended to use Imodium when there is a risk that when the function of peristalsis is suppressed, serious complications develop among the patient, including intestinal obstruction, and megacolon (together with the toxic form of this pathology).
When flatulence, constipation or intestinal obstruction is required, it is necessary to immediately abolish the use of drugs.
Side effects of the imodium
When eliminating the acute form of diarrhea, the following adverse reactions can be developed that were identified during clinical trials:
- organs of the National Assembly: development of severe headaches; more rarely - the appearance of dizziness;
- organs of the digestive system: flatulence, nausea, constipation; less - discomfort in the abdomen, abdominal pains, dry mouth mucous membranes, dyspepsia, and in addition pain in the upper abdomen;
- subcutaneous tissue and skin: the appearance of rashes.
In the course of postmarketing studies, the following negative reactions were identified:
- organs of the immune system: hypersensitivity reactions are observed singly, among them anaphylactic (anaphylaxis including), as well as anaphylactoid manifestations;
- organs of the National Assembly: there are single problems with coordination, suppression or loss of consciousness, a feeling of drowsiness or stupor, hypertension develops;
- visual organs: in isolated situations miosis develops;
- organs of the digestive system: occasionally begins blockage of the intestine (in some cases even in a paralytic form), and in addition a megacolon (sometimes in a toxic form);
- subcutaneous tissue and skin: seldom there are bullous eruptions, urticaria, Quincke edema, pruritus, and in addition, polyiform erythema, Lyell or Stevens-Johnson syndromes;
- urinary system and kidneys: the urinary retention period develops singly;
- general disorders: in single moments severe fatigue occurs.
Dosing and administration
The medicine is not used at the initial stage of therapy for severe diarrhea, which is accompanied by a decrease in water-electrolyte indices. In such cases, loss of fluid is recommended to be compensated by using substitution treatment (oral or parenteral methods).
Capsules are consumed with water.
To eliminate the symptoms of acute diarrhea in children aged 12 and adults, the initial dosage is 2 capsules (4 mg), and then one capsule (2 mg) should be taken with each subsequent liquid stool. The standard size of daily dosage is 6-8 mg (or 3-4 capsules). During the day in the treatment of acute diarrhea, it is allowed to take no more than 12 mg of medication (ie, 6 capsules).
When eliminating the symptoms of acute diarrhea that have arisen because of the development of IBS, the initial dose for adults (when given by the doctor of the initial diagnosis) is 4 mg (2 capsules), after which it is necessary to drink the first capsule every time a loose stool or according to the prescription treating doctor. A day is allowed to drink no more than 6 capsules (dosage of 12 mg).
In the absence of improvement during 48 hours (acute form of diarrhea) after the use of drugs, it is recommended to cancel the medicine.
Overdose
In case of an overdose (including a conditional excess of the dose due to a disorder of the hepatic function), it is possible to develop symptoms of CNS suppression - such as coordination disorder, stupor, miosis, suppression of respiratory function, and muscle toning. In addition, urinary retention or signs similar to intestinal obstruction may develop.
Children may have increased sensitivity to the effects on the central nervous system.
When developing an overdose, an immediate consultation with the doctor is required. When signs of violation appear, it is allowed to use naloxone as an antidote. Since the duration of Imodium exposure exceeds the period of action of naloxone (1-3 hours), the latter can be re-assigned. To detect possible suppression of the central nervous system, it is necessary to carefully monitor the patient's condition for at least 48 hours.
Interactions with other drugs
There are data on the interaction with drugs that have similar pharmacological characteristics. Children should not be prescribed medications with Imodium, which have an overwhelming effect on the function of the central nervous system.
Preclinical tests demonstrate that loperamide is a substrate of the P-glycoprotein. With the combined use of loperamide (16 mg) with P-glycoprotein substance inhibitors (such as ritonavir or quinidine), the plasma index of loperamide doubled / tripled. The clinical significance of this interaction in case of using the recommended dosages of loperamide remains unknown.
The combination of loperamide (single dose of 4 mg) with itraconazole, and in addition inhibitor of the element CYP3A4, as well as P-glycoprotein 3-4 times increases the plasma index of loperamide. During the same test, the inhibitor of the CYP2C8 element (gemfibrozil) increased the active drug level by about half.
Combined use with itraconazole, as well as gemfibrozil four times increased the peak plasma index of loperamide, and 13 times the AUC. This increase is not related to the CNS action, determined by psychomotor testing.
A single dose (16 mg) of loperamide coupled with ketoconazole, an inhibitor of the CYP3A4 element, as well as the P-glycoprotein, allows a 5-fold increase in the level of loperamide within the blood plasma. This indicator is not associated with increased pharmacodynamic properties, the determination was made using papillomimetry.
Taking medication in combination with oral desmopressin leads to an increase in the latter's indices inside the plasma (3-fold). Most likely, this is due to a slowdown in the motility of the gastrointestinal tract.
There is an opinion that drugs that have a similar medicinal effect are capable of increasing the properties of loperamide, but drugs that accelerate the passage of food inside the gastrointestinal tract, on the contrary, can weaken its effectiveness.
Attention!
To simplify the perception of information, this instruction for use of the drug "Imodium" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.