Dosage Forms
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral | 2.,5 mg |
| Solution | Oral | |
| Liquid | Oral | |
| Tablet | Oral | |
| Tablet | 2.5 mg/0.025mg | |
| Solution | Oral | 0.5 mg/mL |
| Tablet | Oral | 25 mcg |
| Tablet | Oral | 0.,025 mg |
Prices
| Unit description | Cost | Unit |
|---|---|---|
| Lomotil 2.5-0.025 mg/5ml Liquid 60ml Bottle | 30.86USD | bottle |
| Lomotil 2.5-0.025 mg tablet | 1.4USD | tablet |
| Lomotil tablet | 1.,12USD | tablet |
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Patents Not Available
Properties
State Solid Experimental Properties Predicted Properties
| Property | Value | Source |
|---|---|---|
| Water Solubility | 0.00146 mg/mL | ALOGPS |
| logP | 5.,74 | ALOGPS |
| logP | 5.88 | ChemAxon |
| logS | -5.5 | ALOGPS |
| pKa (Strongest Basic) | 8.5 | ChemAxon |
| Physiological Charge | 1 | ChemAxon |
| Hydrogen Acceptor Count | 3 | ChemAxon |
| Hydrogen Donor Count | 0 | ChemAxon |
| Polar Surface Area | 53.,33 Å2 | ChemAxon |
| Rotatable Bond Count | 9 | ChemAxon |
| Refractivity | 146.76 m3·mol-1 | ChemAxon |
| Polarizability | 51.,1 | ChemAxon |
| Rule of Five | No | ChemAxon |
| Ghose Filter | No | ChemAxon |
| Veber’s Rule | No | ChemAxon |
| MDDR-like Rule | Yes | ChemAxon |
Predicted ADMET Features
| Property | Value | Probability |
|---|---|---|
| Human Intestinal Absorption | + | 0.,9903 |
| Blood Brain Barrier | + | 0.9592 |
| Caco-2 permeable | + | 0.5316 |
| P-glycoprotein substrate | Substrate | 0.7094 |
| P-glycoprotein inhibitor I | Inhibitor | 0.7045 |
| P-glycoprotein inhibitor II | Inhibitor | 0.7845 |
| Renal organic cation transporter | Inhibitor | 0.5967 |
| CYP450 2C9 substrate | Non-substrate | 0.,8333 |
| CYP450 2D6 substrate | Non-substrate | 0.5667 |
| CYP450 3A4 substrate | Non-substrate | 0.5988 |
| CYP450 1A2 substrate | Non-inhibitor | 0.6827 |
| CYP450 2C9 inhibitor | Inhibitor | 0.6701 |
| CYP450 2D6 inhibitor | Inhibitor | 0.6461 |
| CYP450 2C19 inhibitor | Inhibitor | 0.51 |
| CYP450 3A4 inhibitor | Inhibitor | 0.,5797 |
| CYP450 inhibitory promiscuity | High CYP Inhibitory Promiscuity | 0.817 |
| Ames test | Non AMES toxic | 0.8482 |
| Carcinogenicity | Non-carcinogens | 0.839 |
| Biodegradation | Not ready biodegradable | 0.9805 |
| Rat acute toxicity | 3.3423 LD50, mol/kg | Not applicable |
| hERG inhibition (predictor I) | Weak inhibitor | 0.,7969 |
| hERG inhibition (predictor II) | Inhibitor | 0.592 |
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties., (23092397)
Spectra
Mass Spec (NIST) Not Available Spectra
Targets
Kind Protein Organism Humans Pharmacological action
Yes
Actions
Agonist
General Function Voltage-gated calcium channel activity Specific Function Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone…, Gen-Namn för OPRM1 Uniprot ID P35372 Uniprot Namn Mu-typen opioid receptor Molekylvikt 44778.855 Da
- Chen X, Ji ZL, Chen YZ: TTD: Terapeutiska Målet Databasen. Nukleinsyror Res.2002 Jan 1;30(1):412-5.
- Baker de: Loperamid: en farmakologisk granskning. Rev Gastroenterol Disorder. 2007;7 Suppl 3:S11-8.
- Corazziari E: opioidligands roll i irritabelt tarmsyndrom. Kan J Gastroenterol. 1999 Mar;13 Suppl a:71A-75A.
- Coupar IM: den peristaltiska reflexen i rat ileum: bevis för funktionella Mu-och delta-opiatreceptorer., J Pharm Pharmacol. 1995 Augusti;47(8):643-6.
- De Luca A, Coupar IM: Difenoxin och loperamid: studier av möjliga mekanismer för intestinal antisekretorisk verkan. Naunyn Schmiedebergs Arch Pharmacol. 1993 Feb;347(2):231-7.
Kind protein Organism människor farmakologisk verkan
okänd
åtgärder
Agonist
allmän funktion Opioid receptoraktivitet specifik funktion g-protein kopplad receptor som fungerar som receptor för endogena enkefaliner och för en delmängd av andra opioider., Ligandbindning orsakar en konformationsändring som utlöser signalering via guanine n… Gen Namn OPRD1 Uniprot ID P41143 Uniprot Namn Delta-typen opioid receptor Molekylvikt 40368.235 Da
- Coupar IM: Den peristaltiska reflexen i råtta ileum: bevis för funktionell mu – och delta-opiatreceptorer. J Pharm Pharmacol. 1995 Augusti;47(8):643-6.,
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läkemedel som skapades den 13 juni 2005 07: 24 / uppdaterad den 02 November 2020 21: 01