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 |
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
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…, Genet Navn OPRM1 Uniprot ID P35372 Uniprot Navn Mu-type opioid reseptor molekylvekt 44778.855 Da
- Chen X, Ji ZL, Chen YZ: TTD: Terapeutiske Målet Database. Nukleinsyrer Res. 2002 Jan 1;30(1):412-5.
- Baker DE: Loperamide: en medisinsk vurdering. Rev Gastroenterol Disorder Lucy Hale Og. 2007;7 Suppl 3:S11-8.
- Corazziari E: Rolle av opioid-ligander i den irritabel tarm-syndrom. Kan J Gastroenterol. 1999 Mar;13 Suppl EN:71A-75A.
- Coupar IM: Den peristaltic refleks i rotte huden: bevis for funksjonell mu – og delta-opiat-reseptorer., J Pharm Epidemiologically. 1995 Aug;47(8):643-6.
- De Luca A, Coupar IM: Difenoxin og loperamide: studier på mulige mekanismer av intestinal antisecretory handling. Naunyn Schmiedebergs Arch Epidemiologically. 1993 Feb;347(2):231-7.
Type Protein Organismen Mennesker Farmakologiske virkningen
Ukjent
Handlinger
Agonist
Generell Funksjon Opioid reseptor aktivitet Bestemt Funksjon G-protein koblet reseptor som fungerer som reseptor for endogene enkephalins og for en undergruppe av andre opioider., Ligand binding fører til at en konformasjon endring som utløser signalering via guanin n… Genet Navn OPRD1 Uniprot ID P41143 Uniprot Navn Delta-type opioid reseptor molekylvekt 40368.235 Da
- Coupar IM: Den peristaltic refleks i rotte huden: bevis for funksjonell mu – og delta-opiat-reseptorer. J Pharm Epidemiologically. 1995 Aug;47(8):643-6.,
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Bedøve opprettet på juni 13, 2005 07:24 / Oppdatert November 02, 2020 21:01