II. Indications
- Anticonvulsant
- Adjunct for partial-onset Seizures
- Neuropathic Pain Management
III. Mechanism
- Lipophilic (greater diffusion across blood brain barrier)
- Binds alpha2-delta1 subunit of Central Nervous System voltage-gated Calcium channels
- GABA Receptor Agonist, but does not bind GABA Receptors or Benzodiazepine receptors
IV. Dosing: Adults - Chronic Neuropathic Pain (Diabetic Neuropathy, Postherpetic Neuralgia, Fibromyalgia)
- Regular Release
- Start 50 mg orally three times daily or 75 mg orally twice daily
- May start at 25 mg orally three times daily to maximize tolerability
- May increase after 1 week to 100 mg orally three times daily or 150 mg orally twice daily
- Maximum dose: 300 mg (Diabetic Neuropathy), 450 mg (Fibromyalgia), 600 mg/day (Postherpetic Neuralgia)
- Start 50 mg orally three times daily or 75 mg orally twice daily
- Extended Release (Pregabalin XR, Lyrica CR)
- Stopping
- Taper off agent over 1 week or more
- Avoid stopping abruptly due to withdrawal symptoms
V. Dosing: Partial Seizures
- Adult
- Start 50 mg orally three times daily or 75 mg orally twice daily
- Maximum: 600 mg/day
- Child (over age 1 month)
- Weight > 30 kg
- Start 2.5 mg/kg/day divided 2-3 times per day
- Titrate as needed to 10 mg/kg/day in divided doses (maximum 600 mg/day)
- Weight <30 kg
- Start 3.5 mg/kg/day divided 3 times per day
- Titrate as needed to 14 mg/kg/day in divided doses (maximum 600 mg/day)
- Weight > 30 kg
VI. Metabolism
- Decrease Pregabalin dosing in Creatinine Clearance <60 ml/min
VII. Safety
- Unknown Safety in Lactation
- First trimester use linked to possible birth defects
VIII. Adverse effects
- Common adverse effects
- Severe but uncommon adverse effects
- Other adverse effects
- Risk of Abuse
- Gabapentin and Pregabalin (Lyrica) are abused by patients on Opiates to potentiate CNS Opiate effects
- More than one quarter of Opiate patients have abused Gabapentin
- Pregabalin (Lyrica) is more potent with faster onset and has higher abuse potential than Gabapentin
- Smith (2012) Br J Gen Pract 62(601):406-7 +PMID:22867659 [PubMed]
- Cardiovascular Events
- Single retrospective EHR chart review associated Gabapentin and Pregabalin with cardiovascular events
- Higher quality confirmatory studies are needed
- Pan (2022) Cardiovasc Diabetol 21(1):170 +PMID: 36050764 [PubMed]
IX. Resources
X. References
- (2022) Presc Lett, Resource #361206, Antiseizure Medications
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 56-7
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
Images: Related links to external sites (from Bing)
Related Studies
| pregabalin (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| PREGABALIN 100 MG CAPSULE | Generic | $0.07 each |
| PREGABALIN 150 MG CAPSULE | Generic | $0.08 each |
| PREGABALIN 20 MG/ML SOLUTION | Generic | $0.12 per ml |
| PREGABALIN 200 MG CAPSULE | Generic | $0.09 each |
| PREGABALIN 225 MG CAPSULE | Generic | $0.09 each |
| PREGABALIN 25 MG CAPSULE | Generic | $0.07 each |
| PREGABALIN 300 MG CAPSULE | Generic | $0.10 each |
| PREGABALIN 50 MG CAPSULE | Generic | $0.07 each |
| PREGABALIN 75 MG CAPSULE | Generic | $0.08 each |
| lyrica (on 3/15/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| LYRICA 100 MG CAPSULE | Generic | $0.07 each |
| LYRICA 150 MG CAPSULE | Generic | $0.08 each |
| LYRICA 200 MG CAPSULE | Generic | $0.09 each |
| LYRICA 225 MG CAPSULE | Generic | $0.09 each |
| LYRICA 300 MG CAPSULE | Generic | $0.10 each |
| LYRICA 50 MG CAPSULE | Generic | $0.07 each |
| LYRICA 75 MG CAPSULE | Generic | $0.08 each |
Ontology: pregabalin (C0657912)
| Definition (NCI_NCI-GLOSS) | A drug used to treat nerve pain caused by diabetes or herpes zoster infection and certain types of seizures. It is being studied in the prevention and treatment of nerve pain in the hands and feet of cancer patients given chemotherapy. Pregabalin is a type of anticonvulsant. |
| Definition (NCI) | A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation. |
| Concepts | Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) |
| MSH | C080245 |
| SnomedCT | 415159003, 415160008 |
| LNC | LP61621-6, MTHU021880 |
| English | 3-(Aminomethyl)-5-methyl-hexanoic Acid, 3-Isobutyl GABA, pregabalin (medication), PREGABALIN, pregabalin [Chemical/Ingredient], (S+)-3-isobutyl GABA, 3-(aminomethyl)-5-methylhexanoic acid, (R-)-3-isobutyl GABA, (S)-3-(aminomethyl)-5-methylhexanoic acid, Pregabalin (product), Pregabalin (substance), Pregabalin, 3-isobutyl GABA, pregabalin |
| Spanish | pregabalina (producto), pregabalina (sustancia), pregabalina |
Ontology: Lyrica (C1570232)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C080245 |
| English | Lyrica, Pfizer brand of pregabalin |
