Loperamide (R 18 553) was compared with placebo in a double-blind crossover study of 21 patients with chronic diarrhoea caused by ileocolic disease or resection. Eighteen patients completed the trial. At a median daily dose of 6 mg the new antidiarrhoeal preparation was found to be superior to placebo in controlling chronic diarrhoea. The frequency and weight of stools significantly decreased, ...

The adenosine triphosphate-binding cassette transporter P-glycoprotein (ABCB1/Abcb1a) restricts at the blood-brain barrier (BBB) brain distribution of many drugs. ABCB1 may be involved in drug-drug interactions (DDIs) at the BBB, which may lead to changes in brain distribution and central nervous system side effects of drugs. Positron emission tomography (PET) with the ABCB1 substrates (R)-[(11...

BACKGROUND Peripheral opioid receptor targeting has been well established as a novel target in clinical pain management for acute and chronic peripheral inflammatory pain. The physiochemical properties of the peripheral mu-opioid receptor agonist, loperamide HCl, limit the use of the free drug as an analgesic or anti-inflammatory agent, particularly for dermal delivery across intact skin. OBJ...

Capsaicin produces thermal allodynia in animals and humans by acting as an agonist at vanilloid receptor subtype 1 [VR1; also known as transient receptor potential vanilloid type 1 (TRPV1)]. VR1 receptors are widely distributed in the periphery (e.g., on primary afferent neurons). These studies examined the ability of loperamide (0.1-1 mg/kg s.c.; a micro-opioid agonist that is peripherally sel...

P-glycoprotein (P-gp) and CYP3A (cytochrome P450 3A, generally; Cyp3a, rodent enzyme) in the intestine can attenuate absorption of orally administered drugs. While some suggest that P-gp enhances intestinal metabolism by CYP3A/Cyp3a during absorption of a dual substrate, others suggest that P-gp reduces the metabolism in the intestine when substrates are at subsaturating concentrations. Hence, ...

Pycnocycla spinosa Decne. ex Boiss. var. spinosa (Fam. Umbelliferae) is an essential oil-containing wild plant growing in central part of Iran. Hydroalcoholic extract of Pycnocycla spinosa has antispasmodic and antidiarrheal activity. The aim of this study was to further investigate antidiarrheal and small intestinal transit effect of P. spinosa extract for a comparison with loperamide and dicy...

Loperamide is the most commonly used antidiarrhoeal medication in the UK. We report a serious and hitherto undocumented adverse effect of chronic use in a 45-year-old man with inflammatory bowel disease. He presented to the endocrine clinic with fatigue and low libido; biochemical assessment revealed hypogonadism and adrenal insufficiency without any elevated adrenocorticotropic hormone. When s...

Pycnocycla spinosa Decne. ex Boiss. var. spinosa (Fam. Umbelliferae) is an essential oil-containing wild plant growing in central part of Iran. Hydroalcoholic extract of Pycnocycla spinosa has antispasmodic and antidiarrheal activity. The aim of this study was to further investigate antidiarrheal and small intestinal transit effect of P. spinosa extract for a comparison with loperamide and dicy...

Background: Loperamide is used as an antidiarrheal drug and is available over-the-counter. It cannot pass the blood-brain barrier and it does not have a considerable abuse potential. It can lead to dangerous cardiac arrhythmia.Case Report: Herein, we report a 35-year-old man with a 13-year history of abusing opioids who had undergone detoxification for four times during this period. He underwen...

Eluxadoline, an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist developed for the treatment of diarrhea-predominant irritable bowel syndrome, normalizes gastrointestinal (GI) transit and defecation under conditions of novel environment stress or post-inflammatory altered GI function. Furthermore, compared to loperamide, which is used to treat non-specific ...