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…, Nombre del gen OPRM1 UniProt ID P35372 nombre de UniProt Mu-tipo receptor opioide peso Molecular 44778.855 Da
- Chen X, Ji ZL, Chen YZ: TTD: base de datos terapéutica de la blanco. Nucleic Acids Res. 2002 Jan 1;30 (1): 412-5.
- Baker DE: Loperamida: una revisión farmacológica. Rev Gastroenterol Disord. 2007; 7 Suppl 3: S11-8.
- Corazziari e: papel de los ligandos opioides en el síndrome del intestino irritable. Can J Gastroenterol. 1999 Mar;13 Suppl A:71a-75A.
- Coupar IM: the peristaltic reflex in the rat ieon: evidence for functional mu – and delta-opiate receptors., J Pharm Pharmacol. 1995 Aug; 47(8): 643-6.
- De Luca a, Coupar IM: Difenoxina y loperamida: estudios sobre posibles mecanismos de acción antisecretora intestinal. Naunyn Schmiedebergs Arch Pharmacol. 1993 Feb;347 (2): 231-7.
tipo de proteína organismo humano acción farmacológica
Desconocido
acciones
agonista
función General actividad del receptor opioide función específica receptor acoplado a proteína G que funciona como receptor de encefalinas endógenas y para un subconjunto de otros opioides., La Unión del ligando causa un cambio de conformación que desencadena la señalización a través de la guanina n… Gene Name OPRD1 UniProt ID P41143 UniProt Name Delta-type opioid receptor peso Molecular 40368.235 Da
- Coupar IM: the peristaltic reflex in the rat ieon: evidence for functional mu – and delta-opiate receptors. J Pharm Pharmacol. 1995 Aug; 47(8): 643-6.,
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de Drogas creado el 13 de junio de 2005 07:24 / Actualizado 02 de noviembre de 2020, 21:01