Loperamide Hydrochloride (Page 2 of 5)

Dehydration

Fluid and electrolyte depletion often occur in patients who have diarrhea. In such cases, administration of appropriate fluid and electrolytes is very important. The use of loperamide hydrochloride capsules does not preclude the need for appropriate fluid and electrolyte therapy.

Gastrointestinal Disorders

In general, loperamide hydrochloride capsules should not be used when inhibition of peristalsis is to be avoided due to the possible risk of significant sequelae including ileus, megacolon and toxic megacolon. Loperamide hydrochloride capsules must be discontinued promptly when constipation, abdominal distention or ileus develop.

Treatment of diarrhea with loperamide hydrochloride capsules is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate (or when indicated).

Patients with AIDS treated with loperamide hydrochloride capsules for diarrhea should have therapy stopped at the earliest signs of abdominal distention. There have been isolated reports of toxic megacolon in AIDS patients with infectious colitis from both viral and bacterial pathogens treated with loperamide hydrochloride.

Variability in Pediatric Response

Loperamide hydrochloride capsules should be used with special caution in pediatric patients because of the greater variability of response in this age group. Dehydration, particularly in pediatric patients less than 6 years of age, may further influence the variability of response to loperamide hydrochloride capsules. Loperamide hydrochloride capsules are contraindicated in pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions.

PRECAUTIONS

General

Allergic Reactions

Extremely rare allergic reactions including anaphylaxis and anaphylactic shock have been reported.

Hepatic Impairment

The effects of hepatic impairment on the pharmacokinetics of loperamide have not been studied. Use loperamide hydrochloride capsules with caution in such patients because the systemic exposure to loperamide may be increased due to reduced metabolism. Monitor patients with hepatic impairment closely for signs of central nervous system (CNS) toxicity.

Renal Impairment

No pharmacokinetic data are available in patients with renal impairment. Since it has been reported that the majority of the drug is metabolized and metabolites or the unchanged drug are excreted mainly in the feces, dosage adjustments in patients with renal impairment are not required.

Geriatric Use

No formal studies have been conducted to evaluate the pharmacokinetics of loperamide in elderly subjects. However, in two studies that enrolled elderly patients, there were no major differences in the drug disposition in elderly patients with diarrhea relative to young patients.

In general, elderly patients may be more susceptible to drug-associated effects on the QT interval. Avoid loperamide hydrochloride capsules in elderly patients taking drugs that can result in prolongation of the QT interval (for example, Class IA or III antiarrhythmics) or in patients with risk factors for Torsades de Pointes (see WARNINGS).

Information for Patients

Advise patients:

  • to take loperamide hydrochloride capsules at the prescribed dosage. Use of a higher than prescribed dosage is not recommended (see WARNINGS). Report to a healthcare facility if you or someone you are caring for taking loperamide hydrochloride capsules experiences a fainting episode, a rapid or irregular heartbeat or becomes unresponsive.
  • with acute diarrhea, that if clinical improvement is not observed in 48 hours, discontinue loperamide hydrochloride capsules and contact their healthcare provider.
  • to contact their healthcare provider if they see blood in their stools, or if they develop a fever or abdominal distention.
  • to use caution when driving a car or operating machinery, as tiredness, dizziness, or drowsiness may occur in the setting of diarrheal syndromes treated with loperamide hydrochloride capsules (see ADVERSE REACTIONS).
  • to tell their healthcare provider about all the medications they are taking, including prescription and over-the-counter medications, vitamins and herbal supplements, especially if they take Class 1A (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmics, antipsychotics (e.g., chlorpromazine, haloperidol, thioridazine, ziprasidone), antibiotics (e.g., moxifloxacin), or any other drug known to prolong the QT interval (e.g., pentamidine, levomethadyl acetate, methadone).

Drug Interactions

Effects of Other Drugs on Loperamide

Concomitant use of loperamide hydrochloride capsules with inhibitors of CYP3A4 (e.g., itraconazole) or CYP2C8 (e.g., gemfibrozil) or inhibitors of P-glycoprotein (e.g., quinidine, ritonavir) can increase exposure to loperamide. The increased systemic exposure to loperamide may increase a risk for cardiac adverse reactions especially in patients who are taking multiple CYP enzyme inhibitors, or in patients with underlying cardiac conditions (see WARNINGS). Monitor patients for cardiac adverse reactions.

CYP3A4 Inhibitors

Itraconazole

Concomitant administration of multiple doses of 100 mg itraconazole twice daily, an inhibitor of both CYP3A4 and P-glycoprotein, with a single 4 mg dose of loperamide hydrochloride increased the peak plasma concentration and the systemic exposure to loperamide by 2.9-fold and 3.8-fold, respectively.

CYP2C8 Inhibitors

Gemfibrozil

When a single 4 mg dose of loperamide hydrochloride was coadministered with 600 mg gemfibrozil, a strong inhibitor of CYP2C8, on day 3 of a 5-day treatment with gemfibrozil twice daily, the mean peak plasma concentration and the systemic exposure to loperamide was increased by 1.6-fold and 2.2-fold, respectively.

CYP3A4 and CYP2C8 Inhibitors

When multiple doses of both 100 mg itraconazole and 600 mg gemfibrozil twice daily were administered with a single 4 mg dose of loperamide hydrochloride, the mean peak plasma concentration and the systemic exposure to loperamide was increased by 4.2-fold and 12.6-fold, respectively.

P-glycoprotein Inhibitors

Concomitant administration of a 16 mg single dose of loperamide hydrochloride with a 600 mg single dose of quinidine or ritonavir, both of which are P-glycoprotein inhibitors, resulted in a 2- to 3-fold increase in loperamide plasma concentrations. Due to the potential for enhanced CNS adverse reactions when loperamide is coadministered with quinidine and with ritonavir, caution should be exercised when loperamide hydrochloride capsules are administered at the recommended dosages (2 mg, up to 16 mg maximum daily dose) with P-glycoprotein inhibitors.

Effects of Loperamide on Other Drugs

Saquinavir

When a single 16 mg dose of loperamide hydrochloride is coadministered with a 600 mg single dose of saquinavir, loperamide decreased saquinavir exposure by 54%, which may be of clinical relevance due to reduction of therapeutic efficacy of saquinavir. The effect of saquinavir on loperamide is of less clinical significance. Therefore, when loperamide hydrochloride capsules are given with saquinavir, the therapeutic efficacy of saquinavir should be closely monitored.

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