Pregabalin

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Lyrica; Belgium: Lyrica; Czech Republic: Lyrica; Denmark: Lyrica; Estonia: Lyrica; Finland: Lyrica; France: Lyrica; Germany: Lyrica; Greece: Lyrica; Hungary: Lyrica; Ireland: Lyrica; Italy: Lyrica; Latvia: Lyrica; Lithuania: Lyrica; Luxembourg: Lyrica; Malta: Lyrica; Netherlands: Lyrica; Poland: Lyrica; Portugal: Lyrica; Romania: Lyrica; Slovakia: Lyrica; Slovenia: Lyrica; Spain: Lyrica; Sweden: Lyrica; UK: Lyrica.

North America

Canada: Lyrica; USA: Lyrica.

Latin America

Argentina: Axual, Balfibro, Gavin, Lyrica, Plenica, Prebanal; Mexico: Lyrica.

Asia

Japan: Lyrica.

Drug combinations

Chemistry

Pregabalin: C~8~H~17~NO~2~. Mw: 159.23. (S)-3-(Aminomethyl)-5-methylhexanoic acid. CAS-148553-50-9. (1997).

Pharmacologic Category

Anticonvulsants, Miscellaneous. Fibromyalgia Agents. (ATC-Code: N03AX16).

Mechanism of action

Binds to α~2~-δ-subunit of voltage-gated calcium channels within CNS, inhibiting excitatory neurotransmitter release. Exerts antinociceptive and anticonvulsant activity. Decreases symptoms of painful peripheral neuropathies and, as adjunctive therapy in partial seizures, decreases frequency of seizures.

Therapeutic use

Management of pain associated with diabetic peripheral neuropathy. Management of postherpetic neuralgia. Adjunctive therapy for partial-onset seizure disorder in adults. Management of fibromyalgia.

Pregnancy and lactiation implications

Increased incidence of fetal abnormalities, particularly skeletal malformations, observed in animal studies. Male-mediated teratogenicity observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Use only when potential benefit to mother outweighs possible risk to fetus. Not recommended during lactation.

Unlabeled use

Contraindications

Hypersensitivity to pregabalin or any component of the formulation.

Warnings and precautions

Angioedema reported, may be life-threatening (use with caution in history of angioedema episodes). Concurrent use with other drugs known to cause angioedema (e.g. ACEIs) may increase risk. May cause CNS depression. Hypersensitivity reactions, including skin redness, blistering, hives, rash, dyspnea, and wheezing reported. May decrease platelet count. May cause mild prolongation of PR interval (use with caution in underlying AV block). Associated with increases in CPK and rare cases of rhabdomyolysis. Visual disturbances, such as blurred vision, decreased acuity and visual field changes, associated with therapy. Use may be associated with weight gain and peripheral edema (effect on weight gain/edema may be additive to thiazolidinedione antidiabetic agent particularly in prior cardiovascular disease). Use with caution in CHF, hypertension, or diabetes (weight gain and/or peripheral edema may occur). Use with caution in renal impairment. Effects with other sedative drugs or ethanol may be potentiated. Increased incidence of hemangiosarcoma noted in animal studies (unknown significance in humans). Therapy should be withdrawn gradually.

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