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…, Nazwa genu OPRM1 UniProt ID P35372 Nazwa Uniprot receptor opioidowy typu Mu Masa cząsteczkowa 44778.855 Da
- Chen X, Ji zl, Chen YZ: TTD: baza celów terapeutycznych. Nucleic Acids Res.2002 Jan 1;30(1):412-5.
- Baker DE: Loperamide: przegląd farmakologiczny. Rev Gastroenterol Disord. 2007; 7 Suppl 3: S11-8.
- Corazziari E: rola ligandów opioidowych w zespole jelita drażliwego. Can J Gastroenterol. 1999 Mar; 13 Suppl a: 71A-75A.
- Coupar IM: the peristaltic reflex in the rat ileum: evidence for functional mu-and delta-opiate receptors., J Pharm Pharmacol. 1995 Aug; 47 (8): 643-6.
- De Luca A, Coupar IM: Difenoxin and loperamide: studies on possible mechanisms of jelites antisecretory action. Naunyn Schmiedebergs Arch. 1993 Feb;347(2):231-7.
rodzaj białka organizm człowieka działanie farmakologiczne
nieznany
działania
agonista
Ogólna funkcja aktywność receptora opioidowego specyficzna funkcja receptor sprzężony z białkiem G, który działa jako receptor endogennych enkefalin i podgrupy innych opioidów., Wiązanie ligandu powoduje zmianę konformacji, która wyzwala sygnalizację przez guaninę N… Nazwa genu OPRD1 UniProt ID P41143 Nazwa Uniprot receptor opioidowy typu Delta Masa cząsteczkowa 40368.235 Da
- Coupar IM: odruch perystaltyczny w jelitach szczura: dowody na funkcjonalne receptory opioidowe mu i delta. J Pharm Pharmacol. 1995 Aug; 47 (8): 643-6.,
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Drug created on June 13, 2005 07: 24 / Updated on November 02, 2020 21:01