Loperamide (Capsules) Instructions for Use
ATC Code
A07DA03 (Loperamide)
Active Substance
Loperamide (Rec.INN registered by WHO)
Clinical-Pharmacological Group
Symptomatic antidiarrheal drug
Pharmacotherapeutic Group
Antidiarrheal, intestinal anti-inflammatory/antimicrobial agents; agents that reduce gastrointestinal motility
Pharmacological Action
Antidiarrheal agent. It reduces the tone and motility of the intestinal smooth muscle, apparently by binding to opioid receptors in the intestinal wall.
It inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the transit time of intestinal contents.
It increases the tone of the anal sphincter. The effect occurs rapidly and lasts for 4-6 hours.
Pharmacokinetics
After oral administration, the absorption of loperamide is about 40%; it undergoes intensive first-pass metabolism in the liver.
A small amount of unchanged loperamide enters the systemic circulation. It does not cross the blood-brain barrier.
It is metabolized in the liver.
The elimination half-life (T1/2) is 9-14 hours. It is excreted in the bile with feces as conjugated metabolites; a small portion is excreted in the urine.
Indications
Symptomatic treatment of acute and chronic diarrhea of various origins (including allergic, emotional, drug-induced, radiation-induced; due to changes in diet and food composition, due to malabsorption and metabolic disorders; as an adjunctive agent in diarrhea of infectious origin). Regulation of bowel movements in patients with ileostomy.
ICD codes
| ICD-10 code | Indication |
| A09 | Other and unspecified gastroenteritis and colitis of infectious origin |
| K59.1 | Functional diarrhea |
| K91.4 | Dysfunction following colostomy and enterostomy |
| ICD-11 code | Indication |
| 1A40.Z | Infectious gastroenteritis or colitis, unspecified |
| DD91.2 | Functional diarrhea |
| DD93.Y | Other specified functional gastrointestinal disorders in infants, toddlers and school-age children |
| DD9Z | Functional gastrointestinal disorders, unspecified |
| DE12 | Dysfunction or complications associated with external stoma of the digestive system |
| DE12.0 | Dysfunction of colostomy or enterostomy |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Capsules
For adults with acute diarrhea, the initial dose is 4 mg, then 2 mg after each bowel movement in case of loose stools. For chronic diarrhea, the initial dose is 2 mg, and the maintenance dose is adjusted so that the stool frequency is 1-2 times per day (2-12 mg/day).
The maximum daily dose for adults is 12 mg.
For children aged 4-8 years: 1 mg 3-4 times/day for 3 days; for children aged 9-12 years: 2 mg 4 times/day for 5 days.
Adverse Reactions
From the digestive system: abdominal pain, bloating, nausea, constipation, dry mouth.
From the central nervous system: increased fatigue, drowsiness, dizziness.
Allergic reactions: skin rash.
Contraindications
Intestinal obstruction; constipation, abdominal distension, subileus, acute dysentery (as monotherapy), acute ulcerative colitis, pseudomembranous colitis caused by the use of broad-spectrum antibiotics; children under 4 years of age, first trimester of pregnancy, hypersensitivity to loperamide.
Use in Pregnancy and Lactation
Contraindicated in the first trimester of pregnancy. In the second and third trimesters of pregnancy, Loperamide can be prescribed in cases where the expected therapeutic benefit for the mother outweighs the potential risk to the fetus.
Since a small amount of loperamide is detected in breast milk, use during breastfeeding is not recommended.
Use in Hepatic Impairment
Use with caution in patients with impaired liver function, in hepatic insufficiency.
Pediatric Use
Contraindicated in children under 4 years of age.
Special Precautions
Use with caution in hepatic insufficiency.
Should not be used in clinical situations where inhibition of intestinal peristalsis is required.
If there is no effect after 2 days of using loperamide, the diagnosis should be clarified and an infectious origin of diarrhea should be excluded.
Use with caution in patients with impaired liver function.
In case of loperamide overdose, naloxone is used as an antidote.
Drug Interactions
It is believed that concomitant use of cholestyramine may reduce the effectiveness of loperamide.
Concomitant use with co-trimoxazole, ritonavir increases the bioavailability of loperamide, which is due to inhibition of its first-pass metabolism in the liver.
In case of loperamide overdose, naloxone is used as an antidote.
Storage Conditions
Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.
Dispensing Status
Over-the-Counter
Important Safety Information
This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Capsules 2 mg: 10, 20, 30, or 40 pcs.
Marketing Authorization Holder
Obnovlenie Pfc, JSC (Russia)
Dosage Form
 |
Loperamide Renewal | Capsules 2 mg: 10, 20, 30, or 40 pcs. |
Dosage Form, Packaging, and Composition
Capsules hard gelatin, size #4, with a white body and a blue cap; capsule contents are a white or almost white powder.
| 1 capsule | |
| Loperamide hydrochloride | 2 mg |
Excipients: lactose monohydrate (milk sugar), corn starch, talc, magnesium stearate, colloidal silicon dioxide (aerosil).
Hard gelatin capsule[capsule body composition: titanium dioxide (E171), gelatin; capsule cap composition: titanium dioxide (E171), iron oxide yellow (E172), patent blue V (E131), gelatin].
10 pcs. – blister packs (1, 2, 3, or 4) – cardboard cartons.
Capsules 2 mg: 10, 20, 22, or 30 pcs.
Marketing Authorization Holder
Aliym, JSC (Russia)
Dosage Form
|
Loperamide-Alium | Capsules 2 mg: 10, 20, 22, or 30 pcs. |
Dosage Form, Packaging, and Composition
Capsules hard gelatin, size #3, with a grey body and a dark green cap; capsule contents are a white or white with a yellowish tint powder.
| 1 capsule | |
| Loperamide hydrochloride | 2 mg |
Excipients: microcrystalline cellulose type 101, corn starch, magnesium stearate, croscarmellose sodium.
Capsule body composition: titanium dioxide, iron oxide black, brilliant black, gelatin.
Capsule cap composition: titanium dioxide, quinoline yellow, patent blue V, sunset yellow FCF, brilliant black, gelatin.
10 pcs. – blister packs (1) – cardboard cartons.
10 pcs. – blister packs (2) – cardboard cartons.
10 pcs. – blister packs (3) – cardboard cartons.
11 pcs. – blister packs (2) – cardboard cartons.
Capsules 2 mg: 4, 6, 7, 8, 10, 12, 14, 16, 18, 20, 21, 24, 28, 30, 35, 36, 40, 42, 50, or 60 pcs.
Marketing Authorization Holder
Velpharm, LLC (Russia)
Manufactured By
Velpharm, LLC (Russia)
Or
Velpharm-M, LLC (Russia)
Packaging and Quality Control Release
VELPHARM-M, LLC (Russia)
Dosage Form
|
Loperamide Velpharm | Capsules 2 mg: 4, 6, 7, 8, 10, 12, 14, 16, 18, 20, 21, 24, 28, 30, 35, 36, 40, 42, 50, or 60 pcs. |
Dosage Form, Packaging, and Composition
Capsules gelatin, size #4 yellow; capsule contents are a white or white with a yellowish tint powder.
| 1 capsule | |
| Loperamide hydrochloride | 2 mg |
Excipients: lactose monohydrate (milk sugar), corn starch, colloidal silicon dioxide (aerosil), talc, magnesium stearate.
Capsule composition: titanium dioxide, quinoline yellow, sunset yellow FCF, gelatin.
4 pcs. – blister packs (1) – cardboard cartons.
4 pcs. – blister packs (2) – cardboard cartons.
4 pcs. – blister packs (3) – cardboard cartons.
4 pcs. – blister packs (4) – cardboard cartons.
4 pcs. – blister packs (5) – cardboard cartons.
4 pcs. – blister packs (6) – cardboard cartons.
6 pcs. – blister packs (1) – cardboard cartons.
6 pcs. – blister packs (2) – cardboard cartons.
6 pcs. – blister packs (3) – cardboard cartons.
6 pcs. – blister packs (4) – cardboard cartons.
6 pcs. – blister packs (5) – cardboard cartons.
6 pcs. – blister packs (6) – cardboard cartons.
7 pcs. – blister packs (1) – cardboard cartons.
7 pcs. – blister packs (2) – cardboard cartons.
7 pcs. – blister packs (3) – cardboard cartons.
7 pcs. – blister packs (4) – cardboard cartons.
7 pcs. – blister packs (5) – cardboard cartons.
7 pcs. – blister packs (6) – cardboard cartons.
10 pcs. – blister packs (1) – cardboard cartons.
10 pcs. – blister packs (2) – cardboard cartons.
10 pcs. – blister packs (3) – cardboard cartons.
10 pcs. – blister packs (4) – cardboard cartons.
10 pcs. – blister packs (5) – cardboard cartons.
10 pcs. – blister packs (6) – cardboard cartons.
10 pcs. – polymer jars (1) – cardboard cartons.
20 pcs. – polymer jars (1) – cardboard cartons.
30 pcs. – polymer jars (1) – cardboard cartons.
40 pcs. – polymer jars (1) – cardboard cartons.
50 pcs. – polymer jars (1) – cardboard cartons.
60 pcs. – polymer jars (1) – cardboard cartons.
4 pcs. – blister packs (200) – cardboard containers (for hospitals).
6 pcs. – blister packs (200) – cardboard containers (for hospitals).
7 pcs. – blister packs (200) – cardboard containers (for hospitals).
10 pcs. – blister packs (200) – cardboard containers (for hospitals).
![Loperamide [Capsules] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Loperamide [Capsules] 2")