LOMOTIL TABLET

Product Information

Registration Status: Active

LOMOTIL TABLET is approved to be sold in Singapore with effective from 1991-01-29. It is marketed by JOHNSON & JOHNSON PTE LTD, with the registration number of SIN05364P.

This product contains Atropine 0.025mg, and Diphenoxylate 2.5mg in the form of TABLET. It is approved for ORAL use.

This product is manufactured by PHARMACIA LTD in UNITED KINGDOM.

It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.

Atropine
Diphenoxylate

Description

An alkaloid, originally from Atropa belladonna, but found in other plants, mainly solanaceae. [PubChem]

Indication

For the treatment of poisoning by susceptible organophosphorous nerve agents having anti-cholinesterase activity (cholinesterase inhibitors) as well as organophosphorous or carbamate insecticides.

Mechanism of Action

Atropine binds to and inhibit muscarinic acetylcholine receptors, producing a wide range of anticholinergic effects.

Pharmacokinetics

Absorption
Atropine is rapidly and well absorbed after intramuscular administration. Atropine disappears rapidly from the blood and is distributed throughout the various body tissues and fluids.
Distribution
Metabolism
Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver. From 13 to 50% is excreted unchanged in the urine.
Elimination

Toxicity

Oral, mouse: LD50 = 75 mg/kg. Symptoms of overdose includes widespread paralysis of parasympathetically innervated organs. Dry mucous membranes, widely dilated and nonresponsive pupils, tachycardia, fever and cutaneous flush are especially prominent, as are mental and neurological symptoms. In instances of severe intoxication, respiratory depression, coma, circulatory collapse and death may occur.

Active Ingredient/Synonyms

(+-)-Atropine | (+-)-Hyoscyamine | (+,-)-Tropyl tropate | (±)-atropine | (±)-hyoscyamine | (3-Endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl tropate | [(1S,5R)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl] 3-hydroxy-2-phenyl-propanoate | 8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 3-hydroxy-2-phenylpropanoate | 8-Methyl-8-azabicyclo[3.2.1]oct-3-yl tropate | Atropin | Atropina | Atropine | Atropinum | dl-Hyoscyamine | dl-tropyltropate | Mydriasine | Tropine tropate | Atropine |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.


Description

A meperidine congener used as an antidiarrheal, usually in combination with atropine. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II.

Indication

For as adjunctive therapy in the management of diarrhea

Mechanism of Action

Diphenoxylate is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Diphenoxylate has a direct effect on circular smooth muscle of the bowel, that conceivably results in segmentation and prolongation of gastrointestinal transit time. The clinical antidiarrheal action of diphenoxylate may thus be a consequence of enhanced segmentation that allows increased contact of the intraluminal contents with the intestinal mucosa.

Pharmacokinetics

Absorption
90%
Distribution
Metabolism
Hepatic
Elimination

Toxicity

Coma, dry skin and mucous membranes, enlarged pupils of the eyes, extremely high body temperature, flushing, involuntary eyeball movement, lower than normal muscle tone, pinpoint pupils, rapid heartbeat, restlessness, sluggishness, suppressed breathing

Active Ingredient/Synonyms

1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-isonipecotic acid ethyl ester | 2,2-Diphenyl-4-(4-carbethoxy-4-phenylpiperidino)butyronitrile | 4-Ethoxycarbonyl-alpha,alpha,4-triphenyl-1-piperidinebutyronitrile | Difenossilato | Difenoxilato | Diphenoxylatum | Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylate | Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylisonipecotate | Diphenoxylate |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank