(pregabalin · DailyMed)
PREGALIN
PREGABALIN USP
What it does
Pregabalin is a medication used to treat nerve pain and certain types of seizures. It helps calm overactive nerves in the brain.
Commonly used for: nerve pain (neuropathic pain), seizures (epilepsy), anxiety disorders
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
Medicine sourcing is available in Kenya only. We don't sell or dispense medicines - licensed pharmacies do.
Sourcing - Kenya onlyRegistration & product details
Source: Rwanda Food and Drugs Authority · fetched 2026-06-02 06:15:19 · updated 2026-09-14 02:30:15
Drug Interactions
65Pharmacodynamic Warnings
Pregabalin appears in TABLE 11: Drugs with CNS depressant effects
Severe (7)
Antiepileptics - decreases absorption
Iron chelators (dexrazoxane) might decrease the absorption of antiepileptics (fosphenytoin, phenytoin). Avoid.
Antiepileptics - decreases exposure
Lumacaftor is predicted to decrease the exposure to antiepileptics (carbamazepine, fosphenytoin, phenobarbital, phenytoin, primidone). Avoid.
Antiepileptics - decreases concentration
St John’s wort is predicted to decrease the concentration of antiepileptics (fosphenytoin, phenobarbital, phenytoin, primidone). Avoid.
Antiepileptics - increases risk of overheating and dehydration
Hydroxyzine potentially increases the risk of overheating and dehydration when given with antiepileptics (zonisamide). Avoid in children.
Antiepileptics - increases risk of overheating and dehydration
Haloperidol potentially increases the risk of overheating and dehydration when given with antiepileptics (zonisamide). Avoid in children.
Antiepileptics - decreases absorption
Dexrazoxane might decrease the absorption of antiepileptics (fosphenytoin, phenytoin). Avoid.
Antiepileptics - increases risk of overheating and dehydration
Oxybutynin potentially increases the risk of overheating and dehydration when given with antiepileptics (zonisamide). Avoid in children.
Moderate (25)
Antiepileptics - increases concentration
Intravenous chloramphenicol increases the concentration of antiepileptics (fosphenytoin, phenytoin) and antiepileptics (fosphenytoin, phenytoin) affect the concentration of intravenous chloramphenicol
Antiepileptics - decreases concentration
Diazoxide decreases the concentration of antiepileptics (fosphenytoin, phenytoin) and antiepileptics (fosphenytoin, phenytoin) are predicted to decrease the effects of diazoxide. Monitor concentration
Antiepileptics - increases concentration
Disulfiramincreasestheconcentrationofantiepileptics (fosphenytoin,phenytoin).Monitorconcentrationandadjust dose.rStudy →AlsoseeTABLE12p.1520
Antiepileptics - increases concentration
Fluorouracilincreasestheconcentrationofantiepileptics (fosphenytoin,phenytoin).Monitorconcentrationandadjust dose.rAnecdotal 1xidneppA|snoitcaretnI A1 https://www.facebook.c (Books-Courses-Medic
Antiepileptics - decreases concentration
Folates are predicted to decrease the concentration of antiepileptics (fosphenytoin, phenobarbital, phenytoin, primidone). Monitor concentration and adjust dose.
Unknown (33)
Antiepileptics - increases risk of overheating and dehydration
Acetazolamide potentially increases the risk of overheating and dehydration when given with antiepileptics (zonisamide). Avoid in children.
Antiepileptics - increases risk of visual disturbances
Alcohol potentially increases the risk of visual disturbances when given with antiepileptics (retigabine).
Antiepileptics - decreases exposure
Enzalutamide is predicted to slightly decrease the exposure to antiepileptics (brivaracetam).
Antiepileptics - decreases exposure
Apalutamidepotentiallydecreasestheexposureto antiepileptics(valproate).nTheoretical
Antiepileptics - increases concentration
Capecitabine increases the concentration of antiepileptics (fosphenytoin, phenytoin).
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: class
About this medicine
Pregabalin is a medication used to treat nerve pain and certain types of seizures. It helps calm overactive nerves in the brain.
What it treats
- nerve pain (neuropathic pain)
- seizures (epilepsy)
- anxiety disorders
How it works
Pregabalin works by reducing the number of signals sent by nerves to the brain, which helps decrease pain and seizure activity.
Who it's for
Pregabalin is suitable for adults and some children who have nerve pain or epilepsy.
Drug class
Antiepileptics
Cautions
- • Be careful if you are taking other medications that can cause drowsiness or slow down brain activity.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Pregabalin
BNF-referencedPregabalin is an anticonvulsant medication that is structurally related to gamma-aminobutyric acid (GABA). It is primarily used for the management of epilepsy, neuropathic pain, and generalized anxiety disorder. Pregabalin modulates the release of excitatory neurotransmitters by binding to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, which contributes to its antiseizure and analgesic effects. It does not interact directly with GABA receptors but may enhance GABAergic activity indirectly.
Indications
- Epilepsy
- Neuropathic pain
- Generalized anxiety disorder
Dosage
Adults: The usual starting dose is 150 mg daily, divided into two or three doses. The dose may be increased to a maximum of 600 mg daily based on clinical response and tolerability. Refer to the BNF for specific dosing adjustments in
Mechanism of action
Pregabalin binds presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system. This binding modulates the release of several excitatory neurotransmitters, including glutamate, substance P, norepinephrine, and calcitonin gene-related peptide. By preventing the trafficking of the alpha2-delta subunit from the dorsal root ganglia to the spinal dorsal horn, pregabalin contributes to its anticonvulsant and analgesic effects.
Pharmacodynamics
Pregabalin increases the density of GABA transporters in cultured neurons but does not bind directly to GABA-A, GABA-B, or benzodiazepine receptors. It does not affect dopamine, serotonin, or opiate receptors, nor does it modulate sodium channels or cyclooxygenase activity. Its primary action is through the inhibition of excitatory neurotransmitter release, which helps in controlling seizures and alleviating neuropathic pain.
Pharmacokinetics
Pregabalin is rapidly absorbed after oral administration, with peak plasma concentrations usually reached within 1 hour. It has a bioavailability of approximately 90%, and its plasma concentration does not significantly change with increasing doses. Pregabalin is not extensively metabolized; it is primarily excreted unchanged in the urine. The elimination half-life is about 6 hours, and dose adjustments may be necessary in patients with renal impairment.
Adverse effects
- Dizziness
- Somnolence
- Dry mouth
- Edema
- Weight gain
- Blurred vision
- Difficulty concentrating
- Euphoria
- Depression
- Angioedema
Interactions
- CNS depressants may enhance the sedative effects of pregabalin
- Concurrent use with opioids may increase the risk of respiratory depression
- Antiepileptic drugs may have additive effects
Precautions
- Use with caution in patients with a history of substance abuse
- Monitor for signs of angioedema, especially in patients with a history of angioedema
- Caution in patients with renal impairment, as dosage adjustments may be necessary
Pregnancy
Pregabalin is classified as category C. Animal studies have shown adverse effects, and there are no well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
Pregabalin is excreted in breast milk. The effects on a nursing infant are unknown, and caution is advised when administering to nursing mothers.
Storage
Store at room temperature, away from moisture and heat. Keep out of reach of children.
Formulations
- Capsules: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg
- Oral solution: 20 mg/mL
- Chewable tablets: 50 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Pregabalin
PubChem CID 5486971Molecular formula: C8H17NO2
Mechanism of action
Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models. By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action. Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors. Pregabalin is an anticonvulsant that is structurally related to the inhibitory CNS neurotransmitter gamma-aminobutyric acid (GABA). Pregabalin also has demonstrated analgesic activity. Although pregabalin was developed as a structural analog of GABA, the drug does not bind directly to GABA-A, GABA-B, or benzodiazepine receptors; does not augment GABA-A responses in cultured neurons; and does not alter brain concentrations of GABA in rats or affect GABA uptake or degradation. However, in cultured neurons, prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport. Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissues. ... In vitro, pregabalin reduces the calcium-dependent release of several neurotransmitters, including glutamate, norepinephrine, and substance P, possibly by modulation of calcium channel function. Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. Pregabalin is a potent ligand for the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system that exhibits potent anticonvulsant, analgesic, and anxiolytic activity in a range of animal models. ... Potent binding to the alpha-2-delta site reduces depolarization-induced calcium influx with a consequential modulation in excitatory neurotransmitter release. Pregabalin has no demonstrated effects on GABAergic mechanisms. ... For more Mechanism of Action (Complete) data for PREGABALIN (6 total), please visit the HSDB record page.
Pharmacodynamics
Although the structure of pregabalin is similar to gamma-aminobutyric acid (GABA), it does not bind to GABA receptors. Instead, it binds the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system. Pregabalin does not modulate dopamine receptors, serotonin receptors, opiate receptors, sodium channels or cyclooxygenase activity.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.
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- EVOGAB 150MG CAPSULES · Pharmevo
- EVOGAB 75MG CAPSULES · Pharmevo