لوپرامید
Loperamide Hcl (Imodium)
لوپرامید

نام ژنریک

Loperamide

شکل دارویی

اشكال دارويي:


Tablet: 2mg


Capsule: 2mg


Solution: 1 mg/5ml

موارد مصرف

موارد و مقدار مصرف ‌


الف) اسهال حاد غير اختصاصي:


بزرگسالان و كودكان بزرگتر از 12 سال: در ابتدا mg 4 خوراكي مصرف مي‌شود و پس از هر بار دفع اسهالي، ‌mg 2 استفاده مي‌شود. حداكثر دوز روزانه mg 16 مي‌باشد.


كودكان 12-8 ساله: در روز اول mg 2 خوراكي سه بار در روز مصرف مي‌شود.


كودكان 8-5 ساله: در روز اول mg 2 خوراكي دو بار در روز مصرف مي‌شود.


كودكان 5-2 ساله: در روز اول mg 1 خوراكي سه بار در روز مصرف مي‌شود.


دوز نگهدارنده يك سوم تا يك دوم مقدار مصرف اوليه است (mg/kg 0.1 پس از هر بار دفع اسهال) كه نبايد از دوز روز اول تجاوز نمايد. در صورت عدم بهبودي پس از 48 ساعت، دارو بايد قطع شود.


ب) اسهال مزمن:


بزرگسالان: در ابتدا mg 4 خوراكي و سپس mg 2 پس‌از هر بار دفع اسهالي تا رفع اسهال مصرف مي‌شود. دوز بايد بر اساس پاسخ هر فرد تعيين شود.


در صورت مصرف شدن mg 16 در روز براي حداقل 10 روز، ‌دارو را قطع كنيد.


كودكان: mg/kg 0.24-0.08 در روز در 2 تا 3 دوز منقسم مصرف مي‌شود.


مكانيسم اثر


اثر ضد اسهال: دارو بطور مستقيم بر انتهاهاي عصبي موجود در مخاط روده اثر نموده و حركات روده را كاهش مي‌دهد. به اثرات ضد پريستالتيك اين دارو تحمل ايجاد نمي‌شود.


ترشح آب و الكتروليت‌ها نيز ممكن است با مكانيسم ناشناخته‌اي مهار شود. هر چند لوپراميد از نظر شيميايي شبيه اوپيوئيدها است، ‌اما وابستگي فيزيكي در انسان ايجاد نمي‌كند. اين دارو اثر ضد درد ندارد.

موارد منع مصرف

تداخل دارويي


مصرف همزمان لوپراميد با ضد دردهاي اوپيوئيد ممكن است باعث ايجاد يبوست شديد شود.

موارد قابل توجه

-

تداخل دارویی

عوارض جانبي


اعصاب مركزي: ‌سرگيجه، خواب آلودگي، خستگي.


دستگاه گوارش:‌ درد شكمي، ‌اتساع شكم، ناراحتي شكم، يبوست، خشكي دهان، تهوع، ‌استفراغ.


پوست: واكنشهاي ازدياد حساسيت، بثورات پوستي.


مسموميت و درمان


تظاهرات باليني: يبوست، تحريك گوارشي، تضعيف CNS.


درمان: در صورت مصرف در چند ساعت اخير، ذغال فعال تجويز مي‌شود يا مي‌توان از شستشوي معده استفاده و پس از آن ذغال فعال تجويز نمود. بيمار بايد از نظر تضعيف تنفس پايش شود. در صورت بروز تضعيف تنفسي، نالوكسون تجويز مي‌شود.

مکانیزم اثر

عوارض جانبي


اعصاب مركزي: ‌سرگيجه، خواب آلودگي، خستگي.


دستگاه گوارش:‌ درد شكمي، ‌اتساع شكم، ناراحتي شكم، يبوست، خشكي دهان، تهوع، ‌استفراغ.


پوست: واكنشهاي ازدياد حساسيت، بثورات پوستي.


مسموميت و درمان


تظاهرات باليني: يبوست، تحريك گوارشي، تضعيف CNS.


درمان: در صورت مصرف در چند ساعت اخير، ذغال فعال تجويز مي‌شود يا مي‌توان از شستشوي معده استفاده و پس از آن ذغال فعال تجويز نمود. بيمار بايد از نظر تضعيف تنفس پايش شود. در صورت بروز تضعيف تنفسي، نالوكسون تجويز مي‌شود.

فارماكوكینتیك

موارد منع مصرف و احتياط


موارد منع مصرف: بچه‌هاي زير 2 سال، حساسيت به دارو، بيماراني كه در آنها يبوست خطرناك است؛ همچنين مصرف OTC دارو در بيماراني كه تب بالاي 38.3 درجه سانتگراد يا مدفوع خوني دارند، ‌ممنوع است.


موارد احتياط: ‌بيماري كبدي.

سایر اطلاعات

طبقه‌بندي فارماكولوژيك: مشتق پيپريدين.


طبقه‌بندي درماني: ضد اسهال.


طبقه‌بندي مصرف در بارداري: رده C


نامهاي تجاري : Apo - Loperamide


ملاحظات اختصاصي


پس از تجويز دارو از راه لوله بيني ـ معدي، ‌لوله را با آب شستشو دهيد.


در صورت بروز اسهال شديد، وضعيت آب و الكتروليت‌هاي بيمار را كنترل كنيد.


در صورت ابتلاي بيمار به اختلال کبدي، بيمار را از نظر سميت CNS كنترل كنيد؛ زيرا متابوليسم عبور اول دارو ممكن است كاهش يابد.


نكات قابل توصيه به بيمار


نبايد دارو را بيش از دوز مجاز مصرف نمود.


از كار با ماشين آلات و رانندگي بايد پرهيز نمود تا زماني كه اثرات دارو بر CNS مشخص شود.


در صورت عدم بهبودي طي 48 ساعت و بروز تب، پزشك را مطلع كنيد.


در صورت سياه يا خوني شدن مدفوع پزشك را مطلع كنيد.


مصرف در كودكان: دارو براي كودكان 2 ساله و بزرگتر تأييد شده است، هر چند كودكان كم سن به عوارض جانبي ممكن است حساس تر باشند.


مصرف در شيردهي: ترشح دارو در شير مشخص نيست. بايد با احتياط مصرف شود.

Loperamide Hcl (Imodium)

IMODIUM®
(loperamide hydrochloride),

DRUG DESCRIPTION

IMODIUM® (loperamide hydrochloride), 4-(p-chlorophenyl)-4-hydroxy-N, N-dimethyl- a, a-diphenyl-1-piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal for oral use.

IMODIUM (loperamide hydrochloride) structural formula illustration

IMODIUM® (loperamide hcl) is available in 2mg capsules.

The inactive ingredients are: Lactose, cornstarch, talc, and magnesium stearate. IMODIUM® (loperamide hcl) capsules contain FD&C Yellow No. 6.

What are the possible side effects of loperamide?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking loperamide and call your doctor at once if you have a serious side effect such as:

  • stomach pain or bloating;
  • ongoing or worsening diarrhea;
  • diarrhea that is watery or bloody; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes...

Read All Potential Side Effects and See Pictures of Imodium »

What are the precautions when taking loperamide hcl (Imodium)?

Before taking loperamide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: stomach/abdominal pain without diarrhea, bowel obstruction (e.g., ileus, megacolon, abdominal distention).

The rapidly dissolving tablets may contain aspartame or phenylalanine. If you have phenylketonuria (PKU) or any other condition that requires you to restrict your intake of aspartame or phenylalanine, consult your doctor or pharmacist regarding the safe use of...

Read All Potential Precautions of Imodium »

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

IMODIUM® (loperamide hydrochloride) is indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. IMODIUM® (loperamide hcl) is also indicated for reducing the volume of discharge from ileostomies.

DOSAGE AND ADMINISTRATION

(1 capsule = 2 mg)

Patients should receive appropriate fluid and electrolyte replacement as needed.

Acute Diarrhea

Adults: The recommended initial dose is 4mg (two capsules) followed by 2 mg (one capsule) after each unformed stool. Daily dose should not exceed 16mg (eight capsules). Clinical improvement is usually observed within 48 hours.

Children: In children 2 to 5 years of age (20 kg or less), the non-prescription liquid formulation (IMODIUM® (loperamide hcl) A-D 1 mg/5 mL) should be used; for ages 6 to 12, either IMODIUM® (loperamide hcl) Capsules or IMODIUM® (loperamide hcl) A-D Liquid may be used. For children 2 to 12 years of age, the following schedule for capsules or liquid will usually fulfill initial dosage requirements:

Recommended First Day Dosage Schedule

Two to five years: 1 mg t.i.d. (3mg daily dose) (13 to 20 kg) Six to eight years: 2 mg b.i.d. (4mg daily dose) (20 to 30 kg) Eight to twelve years: 2mg t.i.d. (6mg daily dose) (greater than 30 kg)

Recommended Subsequent Daily Dosage

Following the first treatment day, it is recommended that subsequent IMODIUM® (loperamide hcl) doses (1 mg/10 kg body weight) be administered only after a loose stool. Total daily dosage should not exceed recommended dosages for the first day.

Chronic Diarrhea

Children: Although IMODIUM® (loperamide hcl) has been studied in a limited number of children with chronic diarrhea; the therapeutic dose for the treatment of chronic diarrhea in a pediatric population has not been established.

Adults: The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool until diarrhea is controlled, after which the dosage of IMODIUM® (loperamide hcl) should be reduced to meet individual requirements. When the optimal daily dosage has been established, this amount may then be administered as a single dose or in divided doses.

The average daily maintenance dosage in clinical trials was 4 to 8 mg (two to four capsules). A dosage of 16 mg (eight capsules) was rarely exceeded. If clinical improvement is not observed after treatment with 16 mg per day for at least 10 days, symptoms are unlikely to be controlled by further administration. IMODIUM® (loperamide hcl) administration may be continued if diarrhea cannot be adequately controlled with diet or specific treatment.

Children under 2 Years

The use of IMODIUM (loperamide hcl) in children under 2 years is not recommended. There have been rare reports of paralytic ileus associated with abdominal distention. Most of these reports occurred in the setting of acute dysentery, overdose, and with very young children less than two years of age.

Elderly

No formal pharmacokinetic studies were conducted in elderly subjects. However, there were no major differences reported in the drug disposition in elderly patients with diarrhea relative to young patients. No dosage adjustment is required for the elderly.

Renal Impairment

No pharmacokinetic data are available in patients with renal impairment. Since the metabolites and the unchanged drug are mainly excreted in the feces, no dosage adjustment is required for patients with renal impairment (see PRECAUTIONS section).

Hepatic Impairment

Although no pharmacokinetic data are available in patients with hepatic impairment, IMODIUM (loperamide hcl) should be used with caution in such patients because of reduced first pass metabolism. (see PRECAUTIONS).

HOW SUPPLIED

Capsules - each capsule contains 2 mg of loperamide hydrochloride. The capsules have a light green body and a dark green cap with "JANSSEN" imprinted on one segment and "IMODIUM" on the other segment. IMODIUM® (loperamide hcl) capsules are supplied in bottles of 100.

NDC 50458-400-10.........(100 CAPSULES)

Store at 15°-25°C (59°-77°F).

Janssen Pharmaceutica Inc. Revised September 1996, July 1998. FDA Rev date: 10/21/2005

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Clinical Trial Data

The adverse effects reported during clinical investigations of IMODIUM® (loperamide hydrochloride) are difficult to distinguish from symptoms associated with the diarrheal syndrome. Adverse experiences recorded during clinical studies with IMODIUM® (loperamide hcl) were generally of a minor and self-limiting nature. They were more commonly observed during the treatment of chronic diarrhea.

The adverse events reported are summarized irrespective of the causality assessment of the investigators.

1) Adverse events from 4 placebo-controlled studies in patients with acute diarrhea The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on loperamide hydrochloride as on placebo, are presented in the table below.

  Acute Diarrhea
Loperamide
Hydrochloride
Placebo
No. of treated patients 231 236
Gastrointestinal AE%
Constipation

2.6%

0.8%

The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on loperamide hydrochloride, were: dry mouth, flatulence, abdominal cramp and colic.

2) Adverse events from 20 placebo-controlled studies in patients with chronic diarrhea

The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on loperamide hydrochloride as on placebo, are presented below in the table below.

  Chronic Diarrhea
Loperamide
Hydrochloride
Placebo
No. of treated patients 285 277
Gastrointestinal AE%
Constipation

5.3%

0.0%
Central and peripheral
nervous system AE%

Dizziness

1.4%

0.7%

The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on loperamide hydrochloride were: nausea, vomiting, headache, meteorism, abdominal pain, abdominal cramp and colic.

3) Adverse events from seventy-six controlled and uncontrolled studies in patients with acute or chronic diarrhea

The adverse events with an incidence of 1.0% or greater in patients from all studies are given in the table below.

  Acute Diarrhea Chronic Diarrhea All Studiesa
No. of treated patients 1913 1371 3740
Gastrointestinal AE%
Nausea 0.7% 3.2% 1.8%
Constipation 1.6% 1.9% 1.7%
Abdominal cramps 0.5% 3.0% 1.4%
a. All patients in all studies, including those in which it was not specified if the adverse events occurred in patients with acute or chronic diarrhea.

Post -marketing experience

The following adverse events have been reported:

Skin and subcutaneous tissue disorders

Rash, pruritus, urticaria, angioedema, and extremely rare cases of bullous eruption including erythema multiforme, Stevens-Johnson syndrome and Toxic Epidermal Necrolysis have been reported with use of IMODIUM (loperamide hcl) .

Immune system disorders

Isolated occurrences of allergic reactions and in some cases severe hypersensitivity reactions including anaphylactic shock and anaphylactoid reactions have been reported with the use of IMODIUM (loperamide hcl) .

Gastrointestinal disorders

Dry mouth, abdominal pain, distention or discomfort, nausea, vomiting, flatulence, dyspepsia, constipation, paralytic ileus, megacolon, including toxic megacolon (see CONTRAINDICATIONS and WARNINGS).

Renal and urinary disorders

Urinary retention

Nervous system disorders

Drowsiness, dizziness

General disorders and administrative site conditions

Tiredness

A number of the adverse events reported during the clinical investigations and post- marketing experience with loperamide are frequent symptoms of the underlying diarrheal syndrome (abdominal pain/discomfort, nausea, vomiting, dry mouth, tiredness, drowsiness, dizziness, constipation, and flatulence). These symptoms are often difficult to distinguish from undesirable drug effects.

Drug Abuse And Dependence

Abuse

A specific clinical study designed to assess the abuse potential of loperamide at high doses resulted in a finding of extremely low abuse potential.

Dependence

Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented signs of morphine withdrawal. However, in humans, the naloxone challenge pupil test, which when positive indicates opiate-like effects, performed after a single high dose, or after more than two years of therapeutic use of IMODIUM® (loperamide hydrochloride), was negative. Orally administered IMODIUM® (loperamide hcl) (loperamide formulated with magnesium stearate) is both highly insoluble and penetrates the CNS poorly.

Read the Imodium (loperamide hcl) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Nonclinical data have shown that loperamide is a P-glycoprotein substrate. Concomitant administration of loperamide (16 mg single dose) with a 600 mg single dose of either quinidine, or ritonavir, both of which are P-glycoprotein inhibitors, resulted in a 2- to 3- fold increase in loperamide plasma levels. Due to the potential for enhanced central effects when loperamide is coadministered with quinidine and with ritonavir, caution should be exercised when loperamide is administered at the recommended dosages (2 mg, up to 16 mg maximum daily dose) with P-glycoprotein inhibitors.

When a single 16-mg dose of loperamide 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 is given with saquinavir, the therapeutic efficacy of saquinavir should be closely monitored.

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

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 IMODIUM® (loperamide hcl) does not preclude the need for appropriate fluid and electrolyte therapy.

In general, IMODIUM (loperamide hcl) 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. IMODIUM (loperamide hcl) must be discontinued promptly when constipation, abdominal distention or ileus develop.

Treatment of diarrhea with IMODIUM (loperamide hcl) 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 IMODIUM (loperamide hcl) 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. {ref EDMS-PSDB-2564186, pg 12}

IMODIUM® (loperamide hcl) should be used with special caution in young children because of the greater variability of response in this age group. Dehydration, particularly in younger children, may further influence the variability of response to IMODIUM® (loperamide hcl) .

PRECAUTIONS

General

Extremely rare allergic reactions including anaphylaxis and anaphylactic shock have been reported. In acute diarrhea, if clinical improvement is not observed in 48 hours, the administration of IMODIUM® (loperamide hydrochloride) should be discontinued and patients should be advised to consult their physician. Although no pharmacokinetic data are available in patients with hepatic impairment, IMODIUM (loperamide hcl) should be used with caution in such patients because of reduced first pass metabolism. Patients with hepatic dysfunction should be monitored closely for signs of CNS toxicity. 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 is excreted mainly in the feces, dosage adjustments in patients with renal impairment are not required. 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.

Carcinogenesis, mutagenesis, impairment of fertility

In an 18-month rat study with oral doses up to 40 mg/kg/day (21 times the maximum human dose of 16 mg/day, based on a body surface area comparison), there was no evidence of carcinogenesis.

Loperamide was not genotoxic in the Ames test, the SOS chromotest in E. coli, the dominant lethal test in female mice, or the mouse embryo cell transformation assay.

Fertility and reproductive performance was evaluated in rats using oral doses of 2.5, 10, and 40 mg/kg/day in one study, and 1, 5, 10, 20, and 40 mg/kg/day (females only) in a second study. Oral administration of 20 mg/kg/day (approximately 11 times the human dose based on a body surface area comparison) and higher produced strong impairment of female fertility. Treatment of female rats with up to 10 mg/kg/day p.o. (approximately 5 times the human dose based on a body surface area comparison) had no effect on fertility. Treatment of male rats with 40 mg/kg/day p.o. (approximately 21 times the human dose based on a body surface area comparison) produced impairment of male fertility, whereas administration of up to 10 mg/kg/day (approximately 5 times the human dose based on a body surface area comparison) had no effect.

Pregnancy

Teratogenic Effects Pregnancy Category C

Teratology studies have been performed in rats using oral doses of 2.5, 10, and 40 mg/kg/day, and in rabbits using oral doses of 5, 20, and 40 mg/kg/day. These studies have revealed no evidence of impaired fertility or harm to the fetus at doses up to 10 mg/kg/day in rats (5 times the human dose based on body surface area comparison) and 40 mg/kg/day in rabbits (43 times the human dose based on body surface area comparison). Treatment of rats with 40 mg/kg/day p.o. (21 times the human dose based on a body surface area comparison) produced marked impairment of fertility. The studies produced no evidence of teratogenic activity. There are no adequate and well-controlled studies in pregnant women. Loperamide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Non-teratogenic Effects

In a peri- and post-natal reproduction study in rats, oral administration of 40 mg/kg/day produced impairment of growth and survival of offspring.

Nursing Mothers

Small amounts of loperamide may appear in human breast milk. Therefore, IMODIUM (loperamide hcl) is not recommended during breast-feeding.

Pediatric Use

See the "WARNINGS" Section for information on the greater variability of response in this age group.

In case of accidental overdosage of IMODIUM® by children, see "OVERDOSAGE" Section for suggested treatment.

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

In cases of overdosage, (including relative overdose due to hepatic dysfunction), urinary retention, paralytic ileus and CNS depression may occur. Children may be more sensitive to CNS effects than adults. Clinical trials have demonstrated that a slurry of activated charcoal administered promptly after ingestion of loperamide hydrochloride can reduce the amount of drug which is absorbed into the systemic circulation by as much as ninefold. If vomiting occurs spontaneously upon ingestion, a slurry of 100 gms of activated charcoal should be administered orally as soon as fluids can be retained.

If vomiting has not occurred, gastric lavage should be performed followed by administration of 100 gms of the activated charcoal slurry through the gastric tube. In the event of overdosage, patients should be monitored for signs of CNS depression for at least 24 hours.

If symptoms of overdose occur, naloxone can be given as an antidote. If responsive to naloxone, vital signs must be monitored carefully for recurrence of symptoms of drug overdose for at least 24 hours after the last dose of naloxone.

In view of the prolonged action of loperamide and the short duration (one to three hours) of naloxone, the patient must be monitored closely and treated repeatedly with naloxone as indicated. Since relatively little drug is excreted in the urine, forced diuresis is not expected to be effective for IMODIUM® (loperamide hydrochloride) overdosage.

In clinical trials an adult who took three 20mg doses within a 24 hour period was nauseated after the second dose and vomited after the third dose. In studies designed to examine the potential for side effects, intentional ingestion of up to 60 mg of loperamide hydrochloride in a single dose to healthy subjects resulted in no significant adverse effects.

CONTRAINDICATIONS

IMODIUM (loperamide hcl) is contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients.

IMODIUM (loperamide hcl) is contraindicated in patients with abdominal pain in the absence of diarrhea.

IMODIUM (loperamide hcl) is not recommended in infants below 24 months of age.

IMODIUM (loperamide hcl) should not be used as the primary therapy:

- in patients with acute dysentery, which is characterized by blood in stools and high fever,

- in patients with acute ulcerative colitis,

- in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter,

- in patients with pseudomembranous colitis associated with the use of broad- spectrum antibiotics.

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

In vitro and animal studies show that IMODIUM® (loperamide hydrochloride) acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency.

In man, IMODIUM® (loperamide hcl) prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Clinical studies have indicated that the apparent elimination half-life of loperamide in man is 10.8 hours with a range of 9.1 - 14.4 hours. Plasma levels of unchanged drug remain below 2 nanograms per mL after the intake of a 2mg capsule of IMODIUM® (loperamide hcl) . Plasma levels are highest approximately five hours after administration of the capsule and 2.5 hours after the liquid. The peak plasma levels of loperamide were similar for both formulations. Elimination of loperamide mainly occurs by oxidative N-demethylation. Cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, are thought to play an important role in loperamide N-demethylation process since quercetin (CYP2C8 inhibitor) and ketoconazole (CYP3A4 inhibitor) significantly inhibited the N- demethylation process in vitro by 40% and 90%, respectively. In addition, CYP2B6 and CYP2D6 appear to play a minor role in loperamide N-demethylation. Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces. In those patients in whom biochemical and hematological parameters were monitored during clinical trials, no trends toward abnormality during IMODIUM® (loperamide hcl) therapy were noted. Similarly, urinalyses, EKG and clinical ophthalmological examinations did not show trends toward abnormality.

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

Patients should be advised to check with their physician if their diarrhea does not improve in 48 hours or if they note blood in their stools, develop a fever or develop abdominal distention.

Tiredness, dizziness, or drowsiness may occur in the setting of diarrheal syndromes treated with IMODIUM (loperamide hcl) . Therefore, it is advisable to use caution when driving a car or operating machinery. (see ADVERSE REACTIONS).

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

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PATIENT INFORMATION

Patients should be advised to check with their physician if their diarrhea does not improve in 48 hours or if they note blood in their stools, develop a fever or develop abdominal distention.

Tiredness, dizziness, or drowsiness may occur in the setting of diarrheal syndromes treated with IMODIUM (loperamide hcl) . Therefore, it is advisable to use caution when driving a car or operating machinery. (see ADVERSE REACTIONS).

Last reviewed on RxList: 3/18/2008
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Imodium Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

LOPERAMIDE - ORAL

(low-PAIR-uh-mide)

COMMON BRAND NAME(S): Imodium, Kaopectate 1-D, Maalox Anti-Diarrheal, Pepto Diarrhea Control

USES: This medication is used to treat sudden diarrhea (including traveler's diarrhea). It works by slowing down the movement of the gut. This decreases the number of bowel movements and makes the stool less watery. Loperamide is also used to reduce the amount of discharge in patients who have undergone an ileostomy. It is also used to treat on-going diarrhea in people with inflammatory bowel disease.

Loperamide treats only the symptoms, not the cause of the diarrhea (e.g., infection). Treatment of other symptoms and the cause of the diarrhea should be determined by your doctor.

Do not use in children younger than 6 years unless directed by your doctor. This medication should not be used in infants younger than 24 months.

HOW TO USE: If you are using the over-the-counter product to self-treat, read all the directions on the product package before taking this medication. If your doctor has prescribed this medication, follow your doctor's directions and the directions on your prescription label. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth, usually after each loose stool, or as directed by your doctor. Dosage is based on your condition and response to therapy. In children, dosage is also based on age and weight. Adults should not use more than 8 milligrams in 24 hours if self-treating, or 16 milligrams if under a doctor's direction.

If you are taking the chewable tablet, take this medication on an empty stomach. The chewable tablets should be chewed thoroughly before swallowing.

If you are using the rapidly dissolving tablets, dry your hands before opening the blister pack to carefully remove a tablet. Do not push the tablet through the blister pack. Place the tablet on the tongue, allow it to dissolve completely, then swallow it with saliva. Do not crush, split, or break the tablet before taking it. Do not remove the tablet from the blister pack until just before taking. No water is needed to take this medication.

Diarrhea can cause a serious loss of body water (dehydration). Drink plenty of fluids and minerals (electrolytes) to replace what is lost. Tell your doctor immediately if you develop signs of dehydration (e.g., extreme thirst, decreased urination, muscle cramps, weakness, fainting). You may also need to change to a bland diet during this time to reduce irritation to your stomach/intestines. Consult your doctor or pharmacist for more information.

Tell your doctor if your diarrhea does not improve after 2 days, if your condition worsens, or if you develop new symptoms. If you develop blood in the stool, fever, or an uncomfortable fullness/swelling of the stomach/abdomen, or if you think you may have a serious medical problem, seek immediate medical attention.

If you are taking this medication under your doctor's direction for ongoing diarrhea, tell your doctor if your diarrhea continues after 10 days of treatment.

Disclaimer

Imodium Consumer (continued)

SIDE EFFECTS: Dizziness, drowsiness, tiredness, or constipation may occur. If any of these effects persist or worsen, contact your doctor promptly.

If your doctor has prescribed this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Stop taking this medication and seek immediate medical attention if any of these unlikely but serious side effects occur: severe constipation/nausea/vomiting, stomach/abdominal pain, uncomfortable fullness of the stomach/abdomen.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the Imodium (loperamide hcl) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before taking loperamide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: stomach/abdominal pain without diarrhea, bowel obstruction (e.g., ileus, megacolon, abdominal distention).

The rapidly dissolving tablets may contain aspartame or phenylalanine. If you have phenylketonuria (PKU) or any other condition that requires you to restrict your intake of aspartame or phenylalanine, consult your doctor or pharmacist regarding the safe use of this medicine.

Antibiotics may rarely cause a severe intestinal condition (Clostridium difficile-associated diarrhea) due to a type of resistant bacteria. Symptoms include: persistent diarrhea, abdominal or stomach pain/cramping, or blood/mucus in your stool. This condition may occur weeks after antibiotic treatment has stopped. This medication may make this condition worse. Do not use this anti-diarrhea product, especially after recent antibiotic use, if you have the above symptoms without talking with your doctor first.

This medication should not be used without seeing your doctor first if you have certain medical conditions. These symptoms/conditions may require other treatment before you can use this medication safely. Before using this medication, tell your doctor or pharmacist your medical history, especially of: black/tarry stool, blood/mucus in your stool, high fever, HIV infection/AIDS, liver problems, certain stomach/intestinal infections (e.g., Salmonella, Shigella), certain type of bowel disease (acute ulcerative colitis).

This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Avoid alcoholic beverages.

Caution is advised when using this drug in children because they may be more sensitive to the effects of the drug, especially the drowsiness effect. Children are at higher risk for dehydration. (See also Uses, How to Use sections.)

During pregnancy, this medication should be used only if clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk but is unlikely to have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.

Disclaimer

Imodium Consumer (continued)

DRUG INTERACTIONS: If you are taking this medication under your doctor's direction, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.

This drug should not be used with the following medication because a very serious interaction may occur: pramlintide.

If you are currently using the medication listed above, tell your doctor or pharmacist before starting loperamide.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: recent/current antibiotic use, drugs that can cause constipation (e.g., anticholinergics such as belladonna/scopolamine/benztropine, antispasmodics such as glycopyrrolate/oxybutynin, potent narcotic pain medicines such as morphine, certain antihistamines such as diphenhydramine, tricyclic antidepressants such as amitriptyline), cholestyramine, quinidine, ritonavir, saquinavir.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: difficult urination, slowed breathing, deep sleep.

NOTES: If your doctor has prescribed this medication for you, do not share it with others.

MISSED DOSE: If you are taking this drug on a regular schedule (not "as needed") and you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature away from light and moisture. Refer to storage information printed on the bottle for the exact temperature range. If you have any questions about storage, ask your pharmacist. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised December 2011. Copyright(c) 2011 First Databank, Inc.

Imodium Patient Information Including Side Effects

Brand Names: Diamode, Imodium A-D, Imodium A-D EZ Chews, Imodium A-D New Formula, Kao-Paverin, Kaopectate 1-D, Maalox Anti-Diarrheal

Generic Name: loperamide (Pronunciation: loe PER a mide)

What is loperamide (Imodium)?

Loperamide slows the rhythm of digestion so that the small intestines have more time to absorb fluid and nutrients from the foods you eat.

Loperamide is used to treat diarrhea. Loperamide is also used to reduce the amount of stool in people who have an ileostomy (re-routing of the bowel through a surgical opening in the stomach).

Loperamide may also be used for purposes not listed in this medication guide.

Loperamide 2 mg-GG

white, imprinted with GG 530

Loperamide 2 mg-MYL

brown, imprinted with MYLAN 2100

Loperamide 2 mg-TEV

dark brown/light brown, imprinted with 93 311

What are the possible side effects of loperamide?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking loperamide and call your doctor at once if you have a serious side effect such as:

  • stomach pain or bloating;
  • ongoing or worsening diarrhea;
  • diarrhea that is watery or bloody; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Less serious side effects may include:

  • dizziness;
  • drowsiness, tired feeling;
  • constipation;
  • mild stomach pain; or
  • mild skin rash or itching.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Imodium (loperamide hcl) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about loperamide?

You should not use this medication if you are allergic to loperamide, or if you have stools that are bloody, black, or tarry, or if you have diarrhea that is caused by taking an antibiotic.

Before taking loperamide, tell your doctor if you have a fever, mucus in your stools, a history of liver disease, or if you are taking an antibiotic.

Drink plenty of liquids while you are taking loperamide.

It may take up to 48 hours before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 10 days of treatment.

Loperamide may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Side Effects Centers

Imodium Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking loperamide?

You should not use this medication if you are allergic to loperamide, or if you have:

  • stools that are bloody, black, or tarry; or
  • if you have diarrhea that is caused by taking an antibiotic.

Ask a doctor or pharmacist if it is safe for you to take this medicine if you have:

  • a fever;
  • mucus in your stools;
  • a history of liver disease; or
  • if you are taking an antibiotic.

FDA pregnancy category C. It is not known whether loperamide will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Loperamide can pass into breast milk and may harm a nursing baby. You should not breast-feed while you are using loperamide.

Do not give this medicine to a child without medical advice.

How should I take loperamide?

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.

Take loperamide with a full glass of water. Drink extra water while you are taking this medication to keep from getting dehydrated.

Loperamide is usually taken at the first sign of diarrhea, and again if diarrhea comes back. The first dose of loperamide is usually twice as much as the following doses. Do not take this medication more than 3 times in 24 hours without your doctor's advice.

The loperamide chewable tablet must be chewed before swallowing.

Shake the oral suspension (liquid) well just before you measure a dose. Measure the liquid with a special dose measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose measuring device, ask your pharmacist for one.

Immodium A-D Liquid and New Immodium A-D Liquid contain two different strengths of loperamide. If you switch from using one brand to using the other, follow the dosing instructions carefully. Immodium A-D Liquid also contains a small amount of alcohol, but New Immodium A-D Liquid does not.

It may take up to 48 hours before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 10 days of treatment.

Store at room temperature away from moisture and heat. Do not freeze liquid loperamide.

Side Effects Centers

Imodium Patient Information including If I Miss a Dose

What happens if I miss a dose?

Since loperamide is taken as needed, you may not be on a dosing schedule. If you are taking the medication regularly, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include dizziness, drowsiness, urinating less than usual, severe stomach cramps or bloating, and vomiting.

What should I avoid while taking loperamide?

Loperamide may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Avoid becoming overheated or dehydrated during exercise and in hot weather. Follow your doctor's instructions about the type and amount of liquids you should drink.

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you are taking an antibiotic and you have diarrhea that is watery or has blood in it, call your doctor. Do not use loperamide to stop the diarrhea unless your doctor has told you to.

What other drugs will affect loperamide?

Tell your doctor about all other medicines you use, especially saquinavir (Invirase).

This list is not complete and other drugs may interact with loperamide. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about loperamide.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 5.01. Revision date: 3/31/2011.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

Healthwise

Side Effects Centers

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