Loperamide

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Enterobene, Imodium, Loperamid, Normakut; Belgium: Imodium, Loperamide; Bulgaria: Diarostad, Imodium, Imomed, Lopedium, Stoperan, Vacontil; Cyprus: Imodium, Loperamide, Loperium; Czech Republic: Imodium, Loperon; Denmark: Imodium, Imolope, Loperamid, Propiden; Estonia: Imodium, Lopedium, Loperamid, Loperamide; Finland: Imocur, Imodium, Lopex; France: Altocel, Arestal, Diaretyl, Dyspagon, Ercestop, Imodium, Indiaral, Loperamide, Peracel; Germany: Aperamid, Duralopid, Endialop, Imodium, Lop-Dia, Lopa, Lopedium, Loperamid, Loperhö; Greece: Imodium, Neo-Enteroseptol, Neo-Septol, Rheostop; Hungary: Imodium, Lopedium; Ireland: Arret 2, Diareze, Imodium; Italy: Dissenten, Imodium, Lopemid, Loperyl, Tebloc; Latvia: Imodium, Lopedium, Loperamid, Loperamide, Roko; Lithuania: Imodium, Loperamide, Loperamidum, Lopedium; Luxembourg: D-Stop, Dyspagon, Imodium, Lopedium, Loperamid, Loperamide; Malta: Imodium, Loperamide, Loperan; Netherlands: Arestal, Diacure, Imodium, Kruidvat Diarreeremmer, Loperamide, Trekpleister Diarreeremmer; Poland: Dissenten, Imodium, Laremid, Loperamid, Stoperan; Portugal: Dyspagon, Imodium, Loperamida, Lopitum, Loride; Romania: Imodium, Lopedium, Loperamid, Loperamidum, Loprid, Neo-Enteroseptol; Slovakia: Imodium, Loperamid; Slovenia: Seldiar; Spain: Diarfin, Elissan, Fortasec, Imodium, Loperamida, Loperan, Loperkey, Protector, Salvacolina; Sweden: Dimor, Imodium, Loperamid, Primodium; UK: Diocalm, Imodium, Loperamide.

North America

Canada: Diarr-Eze, Diarrhea Relief, Imodium, Loperacap, Loperamide; USA: Imodium, Loperamide.

Latin America

Argentina: Colifilm, Custey, Dotalsec, Elcoman, Excelentia Antidiarreico, Ionet, Lansek A, Lefa Enteril L, Loperamida, Minicam, Nodiar, Normasec, Plexol, Plorinoc, Regulane, Suprasec, Viltar; Brazil: Imosec, Loperin, Magnostase; Mexico: Acanol, Acqta, Apo-Pera, Biolid, Cryoperacid, Deroser, Diaperol, Exclefin, Hurplex, Imodium, Lomidal, Lomotil, LOP, Loperamida, Nodiamex, Permidal, Pramidal, Rediarin, Top-Dal.

Asia

Japan: Beltessa, Cagudalin, Clalet, Fussen, Lonbanin, Lopecald, Lopejust, Lopemic, Lopemin, Lopena, Loperamide, Loperan, Loperanil, Loseramin, Miropin, Rospolia, Taipemin.

Drug combinations

Loperamide and Neomycin

Loperamide and Simethicone

Chemistry

Loperamide Hydrochloride: C~29~H~33~ClN~2~O~2~ HCl. Mw: 513.50. (1) 1-Piperidinebutanamide, 4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-, monohydrochloride; (2) 4-(p-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutyramide monohydrochloride. CAS-34552-83-5; CAS-53179-11-6 (loperamide)(1975).

Pharmacologic Category

Antidiarrhea Agents. (ATC-Code: A07DA03).

Mechanism of action

Acts directly on circular and longitudinal intestinal muscles, through opioid receptor, to inhibit peristalsis and prolong transit time. Reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss. Demonstrates antisecretory activity. Increases tone on anal sphincter.

Therapeutic use

Treatment of chronic diarrhea associated with inflammatory bowel disease. Acute nonspecific diarrhea. Increased volume of ileostomy discharge.

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies.

Unlabeled use

Cancer treatment-induced diarrhea (e.g. irinotecan-induced). Chronic diarrhea caused by bowel resection.

Contraindications

Hypersensitivity to loperamide or any component of the formulation. Abdominal pain without diarrhea. Children <2 years. Avoid use as primary therapy in acute dysentery, acute ulcerative colitis, bacterial enterocolitis, pseudomembranous colitis.

Warnings and precautions

Rare cases of anaphylaxis and anaphylactic shock reported. GI effects (abdominal pain, constipation, or ileus) might develop. Use with caution in hepatic impairment. Use with caution in treatment of AIDS patients. Cases of toxic megacolon occurred in AIDS patients with infectious colitis. Use with caution in young children (response may be variable due to dehydration). Should not be used if diarrhea is accompanied by high fever or blood in stool, or when inhibition of peristalsis is undesirable or dangerous.

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