Generic
Pregabalin
208 brands available in the market
At a glance
Pregabalin is used for neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury, and as adjunctive therapy for partial-onset seizures. It is a structural derivative of GABA that binds to the α2-δ subunit of calcium channels, reducing neurotransmitter release.
Description
Pregabalin is a structural derivative of the inhibitory neurotransmitter GABA. It does not bind directly to GABAA, GABAB, or benzodiazepine receptors. Pregabalin binds with high affinity to the α2-δ site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissues, which may be involved in its anti-nociceptive and antiseizure effects.
Indications
- Neuropathic pain associated with diabetic peripheral neuropathy
- Postherpetic neuralgia
- Adjunctive therapy for partial-onset seizures (1 month and older)
- Fibromyalgia
- Neuropathic pain associated with spinal cord injury
Therapeutic class
Adjunct anti-epileptic drugs, Primary anti-epileptic drugs
Pharmacological class
α2-δ Calcium Channel Ligand
Pharmacology
Pregabalin binds with high affinity to the α2-δ subunit of voltage-gated calcium channels in CNS tissues. It modulates calcium channel activity and reduces the release of several neurotransmitters including glutamate, norepinephrine, serotonin, and dopamine, producing analgesic and anticonvulsant effects.
Mechanism of action
Relieves pain and seizures by modulating calcium channels and reducing neurotransmitter release.
Dosage
Adult Dose (Oral):
- Diabetic neuropathy: 50 mg three times daily initially; increase to 100 mg three times daily within 1 week; max 300 mg/day
- Postherpetic neuralgia: 150 mg/day initially; increase to 300 mg/day; max 600 mg/day
- Fibromyalgia: 150 mg/day initially; maintenance 300-450 mg/day
- Spinal cord injury: 150 mg/day initially; 300-600 mg/day
- Partial seizures: 150 mg/day initially; 300 mg/day; max 600 mg/day
- CR tablet: 165 mg once daily; increase to 330 mg/day; max 660 mg/day
Renal Impairment Dose: CrCl 30-<60: 75 mg/day (max 300 mg/day); CrCl 15-<30: 25-50 mg/day (max 150 mg/day); CrCl <15: 25 mg/day (max 75 mg/day)
Administration
- May be taken with or without food; take at a fixed time
- CR tablet should be taken after an evening meal; swallow whole, do not split, crush, or chew
- Taper gradually over at least 1 week when discontinuing
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Dizziness
- Somnolence
- Dry mouth
- Edema
- Blurred vision
- Weight gain
- Thinking abnormal (difficulty with concentration/attention)
Precautions & warnings
- May affect driving ability; do not drive if drowsy or dizzy
- Discontinue if angioedema (swelling of throat, head, neck) occurs
- Discontinue if hypersensitivity reactions (hives, dyspnea) occur
- Risk of suicidal thoughts or behavior; monitor
- Respiratory depression may occur with concomitant CNS depressants or underlying respiratory impairment
Contraindications
- Hypersensitivity to pregabalin or any component
Drug interactions
- Lorazepam: Effects potentiated
- Opiates and benzodiazepines: Additive CNS depressant effects
- ACE inhibitors: Increased risk of angioedema
- Thiazolidinediones: Increased risk of weight gain and peripheral edema
Food interactions
Alcohol with Pregabalin may cause excessive drowsiness.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; small amounts detected in breast milk; due to potential risk of tumorigenicity, breastfeeding is not recommended.
Pediatric use
Safety and effectiveness established for partial-onset seizures in pediatric patients 1 month and older; not established for other indications.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment based on CrCl; consult your doctor.
Hepatic Impairment: Safe in liver disease; no dose adjustment needed; consult your doctor.
Overdose effects
Overdose: Reduced consciousness, depression/anxiety, confusional state, agitation, seizures, heart block; no specific antidote; emesis or gastric lavage, supportive care, monitoring of vital signs.
Storage conditions
Store in a cool and dry place (below 30°C), protected from light and moisture; keep out of reach of children.
Chemical structure
Pregabalin