- Automobiles & Motorcycles
- Beauty & Personal Care
- Business Services
- Chemicals
- Construction & Real Estate
- Consumer Electronics
- Electrical Equipment & Supplies
- Electronic Components & Supplies
- Energy
- Environment
- Excess Inventory
- Fashion Accessories
- Food & Beverage
- Furniture
- Gifts & Crafts
- Hardware
- Health & Medical
- Home & Garden
- Home Appliances
- Lights & Lighting
- Luggage, Bags & Cases
- Machinery
- Measurement & Analysis Instruments
- Mechanical Parts & Fabrication Services
- Minerals & Metallurgy
- Office & School Supplies
- Packaging & Printing
- Rubber & Plastics
- Security & Protection
- Service Equipment
- Shoes & Accessories
- Sports & Entertainment
- Telecommunications
- Textiles & Leather Products
- Timepieces, Jewelry, Eyewear
- Tools
- Toys & Hobbies
- Transportation
Pregabalin - LiverTox
Pregabalin - LiverTox
OVERVIEW
Introduction
Pregabalin is an inhibitor of neuronal activity used for therapy of painful neuropathy and as an anticonvulsant. Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare.
Pregabalin - LiverTox
OVERVIEW
Introduction
Pregabalin is an inhibitor of neuronal activity used for therapy of painful neuropathy and as an anticonvulsant. Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare.
Background
Pregabalin (pre gab' a lin) is a structural analogue of gamma-aminobutyric acid (GABA) but is novel in its activity, having no effects on GABA-A or GABA-B receptors. Instead, the neuronal activity of pregabalin appears to be mediated by its binding to the alpha-2-delta subunit of the presynaptic voltage-gated calcium channel which leads to a decrease in release of neuroexcitatory neurotransmitters by hyperexcited neurons. Pregabalin has been shown to be effective in reducing neuropathic pain from diabetic and postherpetic neuropathy and is an effective anticonvulsant. Pregabalin was approved for use in the United States in . Current indications include diabetic and post-herpetic neuropathy and as adjunctive therapy of partial onset seizures. Pregabalin is also used for fibromyalgia and off-label for generalized anxiety disorders and migraine. Pregabalin is available in capsules in varying concentrations from 25 to 300 mg under the brand name of Lyrica. The recommended initial dose for neuropathic pain is 50 to 75 mg two to three times daily, the maximum dose being 300 mg daily. Higher doses are used in treating seizures. The dose should be increased and tapered gradually. The most common side effects of pregabalin are dose related and include peripheral edema, weight gain, dizziness, somnolence, confusion, headache, blurred vision, tremor and ataxia. Rare but potentially severe adverse events include depression, suicidal ideation and behaviors, angioedema, and hypersensitivity reactions.
Hepatotoxicity
Limited data is available on the hepatotoxicity of pregabalin. In prelicensure clinical trials in diabetic neuropathy and epilepsy, therapy with pregabalin was not associated with an increased frequency of serum aminotransferase elevations or liver toxicity. Since its approval and more wide scale use, however, pregabalin has been linked to rare instances of clinically apparent liver injury. Most cases were mild and frequently without jaundice. The latency to onset of injury was short, symptoms of liver injury arising within 3 to 14 days. Both cholestatic and hepatocellular patterns of injury have been reported. Signs of hypersensitivity (fever, rash, eosinophilia) and autoimmunity were not present. Some cases have been severe and associated with marked jaundice and prolongation of the prothrombin time, but all cases ultimately resolved after the medication was stopped without evidence of residual injury.
Likelihood score: C (probable rare cause of clinically apparent liver injury).
Mechanism of Injury
The low rate of significant hepatotoxicity from pregabalin may be due to its minimal hepatic metabolism and rapid urinary excretion. The injury is clearly idiosyncratic and either immunologic or metabolic causes are possible.
Outcome and Management
The case reports of hepatic injury due to pregabalin were followed by complete recovery without evidence of residual or chronic injury. There is no information about cross reactivity with other compounds having similar structure (gabapentin).
Drug Class: Anticonvulsants
Background
Pregabalin (pre gab' a lin) is a structural analogue of gamma-aminobutyric acid (GABA) but is novel in its activity, having no effects on GABA-A or GABA-B receptors. Instead, the neuronal activity of pregabalin appears to be mediated by its binding to the alpha-2-delta subunit of the presynaptic voltage-gated calcium channel which leads to a decrease in release of neuroexcitatory neurotransmitters by hyperexcited neurons. Pregabalin has been shown to be effective in reducing neuropathic pain from diabetic and postherpetic neuropathy and is an effective anticonvulsant. Pregabalin was approved for use in the United States in . Current indications include diabetic and post-herpetic neuropathy and as adjunctive therapy of partial onset seizures. Pregabalin is also used for fibromyalgia and off-label for generalized anxiety disorders and migraine. Pregabalin is available in capsules in varying concentrations from 25 to 300 mg under the brand name of Lyrica. The recommended initial dose for neuropathic pain is 50 to 75 mg two to three times daily, the maximum dose being 300 mg daily. Higher doses are used in treating seizures. The dose should be increased and tapered gradually. The most common side effects of pregabalin are dose related and include peripheral edema, weight gain, dizziness, somnolence, confusion, headache, blurred vision, tremor and ataxia. Rare but potentially severe adverse events include depression, suicidal ideation and behaviors, angioedema, and hypersensitivity reactions.
Hepatotoxicity
Limited data is available on the hepatotoxicity of pregabalin. In prelicensure clinical trials in diabetic neuropathy and epilepsy, therapy with pregabalin was not associated with an increased frequency of serum aminotransferase elevations or liver toxicity. Since its approval and more wide scale use, however, pregabalin has been linked to rare instances of clinically apparent liver injury. Most cases were mild and frequently without jaundice. The latency to onset of injury was short, symptoms of liver injury arising within 3 to 14 days. Both cholestatic and hepatocellular patterns of injury have been reported. Signs of hypersensitivity (fever, rash, eosinophilia) and autoimmunity were not present. Some cases have been severe and associated with marked jaundice and prolongation of the prothrombin time, but all cases ultimately resolved after the medication was stopped without evidence of residual injury.
Further reading:Where to find high purity 1,3-dimethylurea?
Likelihood score: C (probable rare cause of clinically apparent liver injury).
Mechanism of Injury
The low rate of significant hepatotoxicity from pregabalin may be due to its minimal hepatic metabolism and rapid urinary excretion. The injury is clearly idiosyncratic and either immunologic or metabolic causes are possible.
Outcome and Management
The case reports of hepatic injury due to pregabalin were followed by complete recovery without evidence of residual or chronic injury. There is no information about cross reactivity with other compounds having similar structure (gabapentin).
Contact us to discuss your requirements of cas -80-4. Our experienced sales team can help you identify the options that best suit your needs.
Drug Class: Anticonvulsants
CAS--50-8 - Uses, DMF, Dossier, Manufacturer ...
96
PharmaCompass offers a list of Pregabalin API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Pregabalin manufacturer or Pregabalin supplier for your needs.
Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Pregabalin manufacturer or Pregabalin supplier.
PharmaCompass also assists you with knowing the Pregabalin API Price utilized in the formulation of products. Pregabalin API Price is not always fixed or binding as the Pregabalin Price is obtained through a variety of data sources. The Pregabalin Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.
For more information, please visit -31-2.
If you are interested in sending in a Guest Blogger Submission,welcome to write for us!
Comments
0