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 Navn OPRM1 Uniprot-ID P35372 Uniprot Navn Mu-type opioidreceptor Molekylær Vægt 44778.855 Da
- Chen X, Ji ZL, Chen YZ: TTD: Terapeutiske Mål Database. 2002 Jan 1;30(1):412-5.
- Baker de: Loperamid: en farmakologisk gennemgang. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8.
- Cora..iari E: rolle af opioidligander i det irritable tarmsyndrom. Kan J Gastroenterol. 1999 Mar; 13 Suppl a: 71A-75A.
- Coupar im: den peristaltiske refleks i rotte ileum: bevis for funktionelle mu – og delta-opiatreceptorer., J Pharm Pharmacol. 1995 August;47 (8): 643-6.
- De Luca A, Coupar im: Difeno .in og Loperamid: undersøgelser af mulige mekanismer for intestinal antisekretorisk virkning. Naunyn Schmiedebergs Arch Pharmacol. 1993 Feb; 347 (2): 231-7.
Slags Protein Organisme Mennesker Farmakologiske indsats
Ukendt
Handlinger
Agonist
Generelle Funktion Opioid receptor aktivitet Bestemt Funktion G-protein koblet receptor, der fungerer som receptor for endogen enkephalins og for en delmængde af andre opioider., Ligandbinding forårsager en konformationsændring, der udløser signalering via guanin n… Gen Navn OPRD1 Uniprot-ID P41143 Uniprot Navn Delta-type opioidreceptor Molekylær Vægt 40368.235 Da
- Coupar IM: Den peristaltiske refleks i rat ileum: beviser for funktionelle mu – og delta-opiat-receptorer. J Pharm Pharmacol. 1995 August;47 (8): 643-6.,
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Drug oprettet den 13 juni 2005 07:24 / Opdateret den 02 November, 2020 21:01