All Topics  
Loperamide

 

 
   Email Print
   Bookmark   Link
 

 

Loperamide
 
 
  Topics Loperamide Topic Home

Loperamide, a synthetic piperidine
Piperidine

Piperidine is an organic compound with the molecular formula 5NH. This heterocyclic compound amine consists of a six-membered ring containing five methylene units and one nitrogen atom....
 derivative, is a drug
Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
 effective against diarrhea
Diarrhea

In medicine, diarrhea, also spelled diarrhoea , is characterized by frequent loose or liquid bowel movements. The spelling of "diarrhea" is an appropriation of the Greek "diarrhoia" meaning "a flowing through." ....
 resulting from gastroenteritis
Gastroenteritis

Gastroenteritis is inflammation of the gastrointestinal tract, involving both the stomach and the small intestine and resulting in acute diarrhea....
 or inflammatory bowel disease
Inflammatory bowel disease

In medicine, inflammatory bowel disease is a group of inflammation conditions of the colon and small intestine. The major types of IBD are Crohn's disease and ulcerative colitis.....
. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor and Pepto Diarrhea Control. It was discovered at Janssen Pharmaceutica
Janssen Pharmaceutica

Janssen Pharmaceutica, is a pharmaceutical company based in Beerse, in the Campine region of the province of Antwerp , Belgium. The company was established in 1953 by Paul Janssen....
 in 1969.

ramide is an opioid
Opioid

An opioid is a chemical substance that has a morphine-like action in the body. The main use is for analgesia. These agents work by binding to opioid receptors, which are found principally in the central nervous system and the gastrointestinal tract....
 receptor agonist and acts on the µ-opioid receptors
Mu Opioid receptor

The ? opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins....
 in the myenteric plexus large intestines; it does not affect the central nervous system
Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
 like other opioids.

It works by decreasing the activity of the myenteric plexus, which decreases the motility of the circular and longitudinal smooth muscle
Smooth muscle

Smooth muscle is a type of non-striated muscle, found within the tunica media layer of large and small arteries and veins, the urinary bladder, uterus, male and female reproductive tracts, gastrointestinal tract, respiratory tract, the ciliary muscle, and iris of the eye....
s of the intestinal wall.






Discussion
Ask a question about 'Loperamide'
Start a new discussion about 'Loperamide'
Answer questions from other users
Full Discussion Forum



Encyclopedia


Loperamide, a synthetic piperidine
Piperidine

Piperidine is an organic compound with the molecular formula 5NH. This heterocyclic compound amine consists of a six-membered ring containing five methylene units and one nitrogen atom....
 derivative, is a drug
Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
 effective against diarrhea
Diarrhea

In medicine, diarrhea, also spelled diarrhoea , is characterized by frequent loose or liquid bowel movements. The spelling of "diarrhea" is an appropriation of the Greek "diarrhoia" meaning "a flowing through." ....
 resulting from gastroenteritis
Gastroenteritis

Gastroenteritis is inflammation of the gastrointestinal tract, involving both the stomach and the small intestine and resulting in acute diarrhea....
 or inflammatory bowel disease
Inflammatory bowel disease

In medicine, inflammatory bowel disease is a group of inflammation conditions of the colon and small intestine. The major types of IBD are Crohn's disease and ulcerative colitis.....
. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor and Pepto Diarrhea Control. It was discovered at Janssen Pharmaceutica
Janssen Pharmaceutica

Janssen Pharmaceutica, is a pharmaceutical company based in Beerse, in the Campine region of the province of Antwerp , Belgium. The company was established in 1953 by Paul Janssen....
 in 1969.

Mode of action

Loperamide is an opioid
Opioid

An opioid is a chemical substance that has a morphine-like action in the body. The main use is for analgesia. These agents work by binding to opioid receptors, which are found principally in the central nervous system and the gastrointestinal tract....
 receptor agonist and acts on the µ-opioid receptors
Mu Opioid receptor

The ? opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins....
 in the myenteric plexus large intestines; it does not affect the central nervous system
Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
 like other opioids.

It works by decreasing the activity of the myenteric plexus, which decreases the motility of the circular and longitudinal smooth muscle
Smooth muscle

Smooth muscle is a type of non-striated muscle, found within the tunica media layer of large and small arteries and veins, the urinary bladder, uterus, male and female reproductive tracts, gastrointestinal tract, respiratory tract, the ciliary muscle, and iris of the eye....
s of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex
Gastrocolic reflex

The gastrocolic reflex or gastrocolic response is one of a number of physiological reflexes controlling the motility, or peristalsis, of the gastrointestinal tract....
.

Loperamide molecules do not cross the blood-brain barrier
Blood-brain barrier

The blood-brain barrier is a metabolic or cellular structure in the central nervous system that restricts the passage of various chemical substances and microscopic objects between the bloodstream and the neural tissue itself, while still allowing the passage of substances essential to metabolism function ....
 in significant amounts, and, thus, it has no analgesic
Analgesic

An analgesic is any member of the diverse group of Medication used to relieve pain . The word analgesic derives from Greek an- and algos ....
 properties. Any that do cross the blood-brain barrier are quickly exported from the brain by P-glycoprotein
P-glycoprotein

P-glycoprotein is a well-characterized ABC-transporter of the Multidrug_resistance/Transporter_associated_with_antigen_processing subfamily. P-gp is also called ABCB1, ATP-binding cassette sub-family B member 1, MDR1, and PGY1....
 (Pgp), also known as multidrug resistance protein (MDR1). Tolerance in response to long-term use has not been reported.

However, loperamide can cause physical dependence
Physical dependence

Physical dependence refers to a state resulting from chronic use of a drug that has produced Tolerance and where negative physical symptoms of withdrawal result from abrupt discontinuation or dosage reduction....
. Symptoms of opiate withdrawal have been observed in patients abruptly discontinuing long-term therapy with loperamide. For this reason, the drug was briefly classified as a Schedule V controlled substance upon its introduction.

Contraindication
Contraindication

In medicine, a contraindication is a condition or factor that increases the risks involved in using a particular medication, carrying out a medical procedure, or engaging in a particular activity....
s

Treatment should be avoided in the presence of fever
Fever

Fever is a frequent medical sign that describes an increase in internal body temperature to levels above normal. Fever is most accurately characterized as a temporary elevation in the body's thermoregulatory set-point, usually by about 1?2 ?C ....
 or if the stool is bloody. Treatment is not recommended for patients that could suffer detrimental effects from rebound constipation
Constipation

Constipation, costiveness, or irregularity, is a condition of the digestive system in which a person experiences hard feces that are difficult to expel....
. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as E. coli O157:H7
Escherichia coli O157:H7

Escherichia coli O157:H7 is an enterohemorrhagic strain of the Bacteria Escherichia coli and a cause of foodborne illness. Infection often leads to bloody diarrhea, and occasionally to kidney failure, especially in young children and elderly people....
 or salmonella
Salmonella

Salmonella is a genus of rod-shaped Gram-negative enterobacteriaceae that causes typhoid fever, paratyphoid fever, and the foodborne illness salmonellosis....
, loperamide is contraindicated.

Crossing the blood-brain barrier


Concurrent administration of P-glycoprotein inhibitors such as quinidine
Quinidine

Quinidine is a pharmaceutical Medication that acts as a class I antiarrhythmic agent in the heart. It is a stereoisomer of quinine, originally derived from the bark of the cinchona tree....
 with loperamide has been found to produce respiratory depression, indicative of central opioid action.

Side-effects

Side-effects can include drowsiness, constipation, abdominal pain or discomfort, dry mouth, fatigue, and, in rare cases, toxic megacolon
Toxic megacolon

Toxic megacolon is a life-threatening complication of other intestinal conditions. It is characterized by a very dilated Colon , accompanied by abdominal distension , and sometimes fever, abdominal pain, or Shock ....
, mild euphoria, and mild stimulation (at high doses).

See also

  • Gastroenteritis
    Gastroenteritis

    Gastroenteritis is inflammation of the gastrointestinal tract, involving both the stomach and the small intestine and resulting in acute diarrhea....
  • Traveler's diarrhea
    Traveler's diarrhea

    Traveler's diarrhea or traveller's diarrh?a , abbreviated to TD, is the most common illness affecting travelers. Traveler's diarrhea is defined as three or more unformed stools in 24 hours passed by a traveler, commonly accompanied by abdominal cramps, nausea, and bloating....


External links