Descrizione Clinica
Diarrea Loperamide hexal 15cps 2mg Sandoz
LOPERAMIDE HEXAL 2 MG RIGID CAPSULES OTHER MEDICINAL PRODUCTS
active ingredients
Each capsule contains: Active Ingredient: loperamide hydrochloride 2 mg equal to loperamide 1,8 mg For full list of excipients, see paragraph 6.1.Excellent
Excipients: lactose, corn starch, magnesium stearate, talc Body of the capsule: gelatin, iron oxide black (E172), titanium dioxide (E171) Cover: gelatin, iron oxide black (E172), iron oxide yellow (E172), blue license (E131), titanium oxide (E171)Therapeutic indications
LOPERAMIDE HEXAL is suitable for treating acute and chronic diarrhea. After ileostomy it allows to decrease the number and volume of the discharges and to increase the consistency.Contraindications
Hypersensitivity to the active ingredient or any of the excipients listed in paragraph 6.1. Loperamide Hydrochloride should not be used in children under 2 years of age. Loperamide Hydrochloride should not be used as primary therapy: either in patients with acute dysentery, characterized by blood in feces and high fever or in patients with acute ulcerative colitis or in patients with bacterial enterocoliti caused by invasive organisms, including Salmonella, Shigella and Campilobacter or in patients with pseudomembranous colitis associated with the use of broad spectrum antibiotics. Loperamide hydrochloride should not be used when inhibition of peristalsis should be avoided due to the possible risk of significant sequels, including ileo, megacolon and toxic megacolon. Loperamide hydrochloride should be interrupted immediately if stipsis, abdominal distension or ileum develop.Dosage
Adults and children aged between 6 and 17 The medicine should be taken with some liquid. Acute diarrhea The initial dose is 2 capsules for adults and 1 capsule for children; 1 capsule after each subsequent evacuation of unformed feces (molli). Chronic diarrhea You can almost always get a normal defecation with a dose adapted to each patient. The initial dose is 2 capsules per day for adults and 1 capsule for children. This initial dose is adapted until 1 or 2 evacuation of feces formed per day, which is generally possible with a maintenance dose of 1 – 6 capsules (2 mg – 12 mg) per day. Attention: for adults the maximum daily dose in case of acute and chronic diarrhea is 8 capsules (16 mg). For children the dose must be related to body weight (3 capsules/20 Kg) but should not exceed a maximum of 8 capsules per day. Decrease the dose just obtained the normalization of the feces; discontinue treatment in case of stipsi. Children under 6 years Loperamide Hexal 2mg rigid capsules should not be used in children under 6 years. Seniors In the elderly, dose adjustment is not necessary. Renal Compromise In patients with renal impairment, dose adjustment is not necessary. Epathetic Comprogation Despite data is not available of pharmacokinetics in patients with liver impairment, loperamide hydrochloride should be used with caution in these patients due to reduced first-pass metabolism (see paragraph 4.4 "Special warnings and precautions of use"). Caution: do not use for more than 2 days.Conservation
This medicine does not require any special condition of conservation.Warnings
The treatment of diarrhea with loperamide hydrochloride is only symptomatic. Whenever a basic etiology can be determined, specific treatment should be given when appropriate. In patients with diarrhea, especially in children, depletion of liquids and electrolytes may occur. In these cases, the most important countermeasure is the administration of adequate replacement therapy based on liquids and electrolytes. Loperamide Hydrochloride should not be given to children from 2 to 6 years of age without prescription and medical supervision. In acute diarrhea, if an improvement of clinical symptomatology is not observed within 48 hours, the administration of hydrochloride loperamide must be interrupted and patients should be advised to consult the doctor. Patients with AIDS treated with loperamide hydrochloride for diarrhea must stop therapy at the first signs of abdominal distension. In patients with AIDS with infectious colitis caused by viral and bacterial pathogens treated with loperamide hydrochloride, isolated cases of stipsis were reported with an increase in the risk of toxic megacolons. Although no pharmacokinetic data is available in patients with impairment of liver function, in such patients loperamide hydrochloride should be used with caution, due to the reduction of first-pass metabolism. Patients with liver dysfunction must be carefully monitored for signs of toxicity to the central nervous system (SNC). Heart events have been reported including the extension of the QT and peak twists in association with overdose. Some cases were fatal (see paragraph 4.9). Patients should not exceed the recommended dose and/or do not protract the duration of therapy. Loperamide Hexal contains lactose, therefore patients with rare hereditary problems of galactose intolerance, lactase deficiency or glucose–galactose disease syndrome should not take this medicine.Interactions
Non-clinical data have shown that loperamide is a substrate of P–glycoprotein. Concurrent administration of loperamide (in a single dose of 16 mg) with chinidine or ritonavir, both P–glycoprotein inhibitors, showed an increase of 2 to 3 times of plasma levels of loperamide. The clinical relevance of this drug interaction with P–glycoprotein inhibitors, when loperamide is administered to recommended dosages, is not known. Concurrent administration of loperamide (in a single dose of 4 mg) and itraconazole, a inhibitor of CYP3A4 and P–glycoprotein, showed an increase of 3 to 4 times of plasma concentrations of loperamide. In the same study the gemfibrozil, a CYP2C8 inhibitor, increased the plasma concentrations of loperamide by about 2 times. The combination of itraconazole and gemfibrozil showed a 4-time increase in plasma levels of loperamide peak and a 13-time increase in total plasma exposure. These increases were not associated with effects on the central nervous system (SNC), as detected by psychomotor tests (e.g. subjective drowsiness and the test of substitution of symbols and digits – Digit Symbol Substitution Test). Concurrent administration of loperamide (in a single dose of 16 mg) and ketoconazole, a inhibitor of CYP3A4 and P–glycoprotein, has resulted in a 5-fold increase in plasma concentrations of loperamide. This increase was not associated with an increase in pharmacodynamic effects, as detected by the pupillometry. Concurrent treatment with oral desmopressin resulted in an increase of 3 times of plasma concentrations of desmopressin, presumably due to a slowdown in gastrointestinal motility. Possible interactions can occur with: drugs that slow intestinal peristalsis (e.g. anti-linergics), as the effects of loperamide can be enhanced. Treatment with substances with similar pharmacological properties can enhance the effect of loperamide and drugs that accelerate intestinal transit can decrease its effect. We do not recommend the concomitant use of cytochrome inhibitors CYP 450 and glycoprotein inhibitors P.Effects
Adults and children aged ≥12 years The safety of loperamide hydrochloride was assessed in 3076 adults and children aged ≥12 years who participated in 31 controlled and uncontrolled clinical trials with loperamide hydrochloride used for treating diarrhea. Of these, 26 studies were on acute diarrhea (N=2755) and 5 on chronic diarrhea (N=321). The adverse reactions to the drug (ADR) reported most commonly (i.e. with an incidence ≥1%) during clinical studies with loperamide hydrochloride for the treatment of acute diarrhea were: constipation (2.7%), flatulence (1.7%), headache (1.2%) and nausea (1.1%). In clinical studies for the treatment of chronic diarrhea, ADR reported more commonly (i.e. with an incidence ≥1%) were: flatulence (2.8%), constipation (2.2%), nausea (1.2%) and dizziness (1.2%). The data contained in Table 1 represent the results of 3076 adults and children aged ≥12 years who participated in 31 controlled and uncontrolled clinical trials with loperamide hydrochloride used for treating diarrhea. Of these, 26 studies were on acute diarrhea (N=2755) and 5 on chronic diarrhea (N=321). The frequency categories in Table 1 are defined in accordance with the following Convention: very common (≥ 1/10), common (≥ 1/100, Table 1 Frequency of adverse reactions to the drug reported with the use of loperamide hydrochloride during clinical studies in adults and children aged ≥12 years| Classification for systems and organs | Indication | |
| Acute diarrhea (N=2755) | Chronic diarrhea (N=321) | |
| Diseases of the nervous system | ||
| Cefa | Town | Not common |
| Heads | Not common | Town |
| Gastrointestinal diseases | ||
| Stitching, nausea, flatulence | Town | Town |
| Abdominal pain, abdominal malaise, dry mouthfeel | Not common | Not common |
| Pain from the upper part of the abdomen, vomit | Not common | |
| Dispepsia | Not common | |
| Abdominal distension | Rare | |
| Pathologies of skin and subcutaneous tissue | ||
| Rash | Not common | |
Overdosing
Synonyms In case of overdose (including relative overdose, due to hepatic dysfunction) depression of the SNC may occur (stupor, coordination abnormalities, drowsiness, myosis, muscle hypertonia and respiratory depression), urinary and ileum retention. Children can be more sensitive to the effects of the central nervous system than adults. Therefore it is recommended to keep the product outside of their scope because in cases of erroneous administration in children under 4 years of age, for absolute overdose (intentional intake of excessive doses) or relative (for accumulation in the blood of non-metabolized drug, while administered to the correct doses), stipsi can be manifested and, as for many other drugs (e.g. mid-phamidic) in the barrier of sleepymaturity. In this case the patient must be kept under careful observation for 48 hours in order to highlight a possible depression of the central nervous system. In patients who have ingested excessive doses of loperamide hydrochloride heart events have been observed such as extension of the QT range, point torsions, other severe ventricular arrhythmias, cardiac arrest and syncope (see paragraph 4.4). Fatal cases have also been reported. Treatment Measures in case of overdose: gastric lavender, vomiting, clisma or laxative administration If overdose symptoms arise, naloxone can be administered as an antidote. Since the duration of loperamide action is more extensive than that of naloxone (from 1 to 3 hours), repeated treatment with naloxone can be indicated. Therefore, the patient must be monitored carefully for at least 48 hours, in order to detect a possible depression of the SNC.Although there are no indications that loperamide hydrochloride possesses teratogenic or embryotoxic properties, the expected therapeutic benefits should be assessed compared to the potential risks before administering loperamide hydrochloride during pregnancy, especially during the first trimester. Small amounts of loperamide can appear in human breast milk. Therefore loperamide hydrochloride is not recommended during lactation.
Source: Farmadati
