gabapentin enacarbil
Description
Name: gabapentin enacarbil
Type: small molecule
Groups: approved
Indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Accession Number: DB08872 ( DB08872)
Description: Gabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Structure:
Prescription Products:
Generic Prescription Products: Not Available
Over the Counter Products: Not Available
Prescription Products:
International Brands
Brand Names
Brand Mixtures
Categories
Type: small molecule
Groups: approved
Indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Accession Number: DB08872 ( DB08872)
Description: Gabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Structure:
Prescription Products:
| Name | Dosage | Strength | Route | Marketing Start | Marketing End | Country |
| Horizant | tablet, extended release | 600 mg/1 | oral | 01-05-2013 | US | |
| Horizant | tablet, extended release | 300 mg/1 | oral | 01-05-2013 | US |
Generic Prescription Products: Not Available
Over the Counter Products: Not Available
Prescription Products:
| Name | Dosage | Strength | Route | Marketing Start | Marketing End | Country |
| Horizant | tablet, extended release | 600 mg/1 | oral | 01-05-2013 | US | |
| Horizant | tablet, extended release | 300 mg/1 | oral | 01-05-2013 | US |
International Brands
- No Brands
Brand Names
- No Brands
Brand Mixtures
| Brand Name | Ingredients |
|---|---|
| Horizant | gabapentin enacarbil |
| Horizant | gabapentin enacarbil |
| Brand Name | Ingredients |
|---|---|
| Horizant | gabapentin enacarbil |
| Horizant | gabapentin enacarbil |
Categories
- No Category
Pharmacology
Indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Pharmacodynamics: Not Available
Mechanism of action: Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Absorption: Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
Volume of distribution:
Protein binding: Gabapentin plasma protein binding is less than 3%.
Metabolism: Not Available
Route of elimination: Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
Half life: The elimination half-life of gabapentin is 5.1 to 6.0 hours.
Clearance: Not Available
Toxicity: Most common adverse reactions are headache, dizziness, and somnolence.
Affected organisms
SNP Mediated Adverse Drug Reactions
Pharmacodynamics: Not Available
Mechanism of action: Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Absorption: Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
Volume of distribution:
- The volume of distribution is 76L.
Protein binding: Gabapentin plasma protein binding is less than 3%.
Metabolism: Not Available
Route of elimination: Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
Half life: The elimination half-life of gabapentin is 5.1 to 6.0 hours.
Clearance: Not Available
Toxicity: Most common adverse reactions are headache, dizziness, and somnolence.
Affected organisms
- Not Available
SNP Mediated Adverse Drug Reactions
- Not Available
Pharmacoeconomics
Manufacturers:
Packagers:
Dosage forms
Prices
Patents
- Not Available
Packagers:
- Not Available
Dosage forms
| Form | Route | Strength |
|---|---|---|
| Tablet, extended release | oral | 300 mg/1 |
| Tablet, extended release | oral | 600 mg/1 |
| Form | Route | Strength |
|---|---|---|
| Tablet, extended release | oral | 300 mg/1 |
| Tablet, extended release | oral | 600 mg/1 |
Prices
| Unit description | Cost | Unit |
|---|
| Unit description | Cost | Unit |
|---|
Patents
| Country | Patent Number | Approved | Expires (estimated) |
|---|
Interactions
Drug Interactions
Food Interactions:
| Drug | Interaction |
|---|---|
| Azelastine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine. |
| Baclofen | The risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil. |
| Brimonidine | Brimonidine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Buprenorphine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine. |
| Doxylamine | Doxylamine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Dronabinol | Dronabinol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Droperidol | Droperidol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Ethanol | Ethanol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Hydrocodone | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone. |
| Hydroxyzine | Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Lorazepam | The risk or severity of adverse effects can be increased when Lorazepam is combined with gabapentin enacarbil. |
| Magnesium Sulfate | Magnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Methotrimeprazine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. |
| Metyrosine | gabapentin enacarbil may increase the sedative activities of Metyrosine. |
| Minocycline | Minocycline may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Mirtazapine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. |
| Nabilone | Nabilone may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Orphenadrine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. |
| Paraldehyde | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. |
| Paroxetine | The risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Paroxetine. |
| Perampanel | Perampanel may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Pramipexole | gabapentin enacarbil may increase the sedative activities of Pramipexole. |
| Ropinirole | gabapentin enacarbil may increase the sedative activities of Ropinirole. |
| Rotigotine | gabapentin enacarbil may increase the sedative activities of Rotigotine. |
| Rufinamide | The risk or severity of adverse effects can be increased when Rufinamide is combined with gabapentin enacarbil. |
| Sodium oxybate | Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Suvorexant | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. |
| Tapentadol | Tapentadol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Thalidomide | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide. |
| Zolpidem | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem. |
| Drug | Interaction |
|---|---|
| Azelastine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine. |
| Baclofen | The risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil. |
| Brimonidine | Brimonidine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Buprenorphine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine. |
| Doxylamine | Doxylamine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Dronabinol | Dronabinol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Droperidol | Droperidol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Ethanol | Ethanol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Hydrocodone | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone. |
| Hydroxyzine | Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Lorazepam | The risk or severity of adverse effects can be increased when Lorazepam is combined with gabapentin enacarbil. |
| Magnesium Sulfate | Magnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Methotrimeprazine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. |
| Metyrosine | gabapentin enacarbil may increase the sedative activities of Metyrosine. |
| Minocycline | Minocycline may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Mirtazapine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. |
| Nabilone | Nabilone may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Orphenadrine | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. |
| Paraldehyde | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. |
| Paroxetine | The risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Paroxetine. |
| Perampanel | Perampanel may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Pramipexole | gabapentin enacarbil may increase the sedative activities of Pramipexole. |
| Ropinirole | gabapentin enacarbil may increase the sedative activities of Ropinirole. |
| Rotigotine | gabapentin enacarbil may increase the sedative activities of Rotigotine. |
| Rufinamide | The risk or severity of adverse effects can be increased when Rufinamide is combined with gabapentin enacarbil. |
| Sodium oxybate | Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Suvorexant | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. |
| Tapentadol | Tapentadol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil. |
| Thalidomide | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide. |
| Zolpidem | gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem. |
Food Interactions:
- No food effects.
Taxonomy
Kingdom: Not Available
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
substituent:
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
- Not Available
substituent:
- Not Available
References
Synthesis Reference: 1. Cundy KC, Branch R, Chernov-Rogan T, Dias T, Estrada T, Hold K, Koller K, Liu X, Mann A, Panuwat M, Raillard SP, Upadhyay S, Wu QQ, Xiang JN, Yan H, Zerangue N, Zhou CX, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. Epub 2004 May 14.
General Reference: # Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15146029
External Links:
ATC Codes:
AHFS Codes:
MSDS: Download
General Reference: # Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15146029
External Links:
| Resource | Link |
|---|---|
| RxList | http://www.rxlist.com/horizant-drug.htm |
| Drugs.com | http://www.drugs.com/sfx/gabapentin-enacarbil-side-effects.html |
| Resource | Link |
|---|---|
| RxList | http://www.rxlist.com/horizant-drug.htm |
| Drugs.com | http://www.drugs.com/sfx/gabapentin-enacarbil-side-effects.html |
ATC Codes:
- Not Available
AHFS Codes:
- Not Available
MSDS: Download