Pregabalin 300mg

Product Overview

Generic Name: Pregabalin

Brand Name: Lyrica®, Lyrica CR®

Drug Class: Gabapentinoids / Anticonvulsant

DEA Schedule: C-V (Schedule V Controlled Substance) [citation:9]

FDA Initial Approval: 2004 [citation:3]

Pregabalin was originally developed as an anti-epileptic drug and later found effective for multiple neuropathic pain conditions. It is structurally analogous to the inhibitory neurotransmitter GABA but does not directly bind to GABA receptors [citation:2].

Available Strengths & Forms

Formulation	Available Strengths
Immediate-Release Capsules [citation:1]	25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg
Oral Solution [citation:3]	20 mg/mL
Extended-Release Tablets (Lyrica CR) [citation:4]	82.5 mg, 165 mg, 330 mg

FDA-Approved Indications [citation:1][citation:6]

• Diabetic Peripheral Neuropathy: Management of neuropathic pain associated with diabetic peripheral neuropathy
• Postherpetic Neuralgia: Management of neuropathic pain following shingles
• Fibromyalgia: Management of fibromyalgia in adults
• Partial-Onset Seizures: Adjunctive therapy for partial-onset seizures in patients 17 years and older
• Spinal Cord Injury: Management of neuropathic pain associated with spinal cord injury

Off-Label Uses: Generalized anxiety disorder (GAD), social anxiety disorder, bipolar disorder, insomnia, and other chronic pain conditions not sanctioned by the FDA [citation:2].

Mechanism of Action [citation:2][citation:7]

Pregabalin binds with high affinity and selectivity to the α2-δ subunit of voltage-gated calcium channels (VGCCs) in the central nervous system. This binding reduces calcium influx at nerve terminals, which in turn decreases the release of excitatory neurotransmitters including glutamate, norepinephrine, substance P, and calcitonin gene-related peptide [citation:2].

Key characteristics of pregabalin’s mechanism:

• Does not directly bind to GABA-A or GABA-B receptors
• No known activity at serotonin, opiate, sodium channels, or dopamine receptors
• Does not modify cyclooxygenase activity [citation:2]
• Only modulates excitatory neurotransmitter release in “hyper-excited” neurons, restoring them to normal physiological state [citation:7]

This novel mechanism of action is believed to confer pregabalin’s analgesic, anticonvulsant, and anxiolytic properties [citation:7].

Dosage Recommendations by Indication [citation:1][citation:9]

Important Administration Notes:

• Take with or without food, consistently the same way each day
• Swallow capsules whole; do not crush or chew [citation:4]
• When discontinuing, taper gradually over a minimum of 1 week
• Adjust dose in patients with renal impairment (primarily renally excreted)

licensierad

*For postherpetic neuralgia, doses up to 600 mg/day may be used in patients tolerating 300 mg/day with ongoing pain after 2-4 weeks [citation:1].

Dosage in Renal Impairment [citation:1][citation:9]

Since pregabalin is eliminated primarily by renal excretion (unchanged drug), dose adjustment is required based on creatinine clearance (CLcr).

Indication	Starting Dose	Maximum Dose	Frequency
Diabetic Peripheral Neuropathy	50 mg TID (150 mg/day)	100 mg TID (300 mg/day)	Three times daily
Postherpetic Neuralgia	75 mg BID or 50 mg TID (150 mg/day)	150 mg BID or 100 mg TID (300 mg/day)*	Two or three times daily
Fibromyalgia	75 mg BID (150 mg/day)	225 mg BID (450 mg/day)	Two times daily
Partial-Onset Seizures (Adjunctive)	150 mg/day	600 mg/day	Two or three times daily
Spinal Cord Injury Pain	75 mg BID (150 mg/day)	300 mg BID (600 mg/day)	Two times daily

Creatinine Clearance (CLcr)	Total Daily Dose	Dose Regimen
≥ 60 mL/min	150-600 mg/day	BID or TID
30–60 mL/min	75-300 mg/day	BID or TID
15–30 mL/min	25-150 mg/day	QD or BID
< 15 mL/min	25-75 mg/day	QD

Hemodialysis patients: Take a supplemental dose immediately following every 4-hour hemodialysis treatment [citation:1].

Pharmacokinetics [citation:2]

Parameter	Information
Absorption	Linear and dose-proportional; absorbed in small intestine and proximal colon
Time to peak (Tmax) – IR	0.7–1.5 hours
Time to peak (Tmax) – CR	8 hours (range: 5–12 hours)
Volume of distribution	0.5 L/kg
Plasma protein binding	None (0%)
Metabolism	Negligible hepatic metabolism; does not induce or inhibit CYP450 enzymes
Elimination	Primarily renal (unchanged drug)
Elimination half-life	6.3 hours (normal renal function)

Contraindications [citation:1][citation:6]

BOXED WARNINGS & Serious Warnings

Common Side Effects [citation:3]

• Very Common (>10%): Dizziness, drowsiness (somnolence)
• Common (1-10%): Peripheral edema (swelling in hands/feet), weight gain, dry mouth, blurred vision, trouble concentrating, increased appetite, constipation, nausea, fatigue

Serious Side Effects (Seek Immediate Medical Attention) [citation:3]

• Weak or shallow breathing, blue-colored skin, lips, fingers, toes (respiratory depression)
• Confusion, extreme drowsiness, or weakness
• Vision problems
• Swelling in hands or feet, rapid weight gain (especially with diabetes or heart problems)
• Easy bruising, unusual bleeding
• Unexplained muscle pain, tenderness, or weakness (especially with fever or malaise)
• Angioedema: Swelling of face, mouth, tongue, throat
• Suicidal thoughts or behavior

Drug Interactions [citation:1][citation:3]

Primary interaction concerns:

• Opioids and CNS depressants: Additive CNS depression, increased risk of respiratory depression, sedation, and death [citation:3][citation:8]
• Angioedema-associated drugs (ACE inhibitors): May increase risk of developing angioedema
• Gabapentin: Concomitant use not studied; no dosing recommendations available [citation:1]

Notable advantage: Pregabalin does not induce or inhibit cytochrome P450 enzymes, resulting in fewer drug-drug interactions compared to many other anticonvulsants [citation:2].

Pregnancy, Breastfeeding & Fertility [citation:5][citation:10]

Pregnancy: Some (but not all) studies show taking pregabalin during pregnancy may slightly increase the chance of birth defects. High dose folic acid (5 mg/day) is recommended. Do not stop abruptly without medical advice, as seizures can harm mother and baby [citation:5].

Breastfeeding: Pregabalin passes into breast milk in small amounts, but breastfed babies rarely experience side effects. Monitor for changes in feeding, unusual sleepiness, irritability, constipation, or diarrhea [citation:5].

Fertility: There is no evidence that pregabalin affects fertility in men or women [citation:5].

Overdose

Signs of overdose: Excessive sedation, confusion, agitation, restlessness, seizures, respiratory depression, coma [citation:3].

Treatment: Supportive care. No specific antidote. Hemodialysis may remove pregabalin from the blood.

Emergency: Call Poison Control (1-800-222-1222) or 911 immediately if overdose is suspected.

Storage

• Store at room temperature (59-86°F / 15-30°C)
• Protect from light and moisture
• Keep in a secure location out of reach of children

Legal Status (United States)

Pregabalin is a Schedule V (C-V) controlled substance [citation:9]. This classification reflects its potential for abuse and physical dependence, though lower than Schedule IV substances.

Educational Summary

Pregabalin is a gabapentinoid anticonvulsant used for neuropathic pain (diabetic neuropathy, postherpetic neuralgia, spinal cord injury), fibromyalgia, and partial-onset seizures. It binds to α2-δ subunits of voltage-gated calcium channels, reducing excitatory neurotransmitter release. Available in 25-300 mg capsules, typical starting doses range from 150-300 mg/day depending on indication, up to 600 mg/day for seizures and spinal cord injury pain. Key contraindications: hypersensitivity. Serious warnings: angioedema, suicidal ideation, respiratory depression (especially with CNS depressants/opioids). Withdrawal: taper over ≥1 week. Pregnancy: high dose folic acid recommended. Renally dosed. Schedule V controlled substance.

Note: This information is for pharmaceutical educational and pharmacy reference purposes only. Pregabalin is a prescription-only medication. This content does not constitute medical advice. Always follow the official prescribing information and the physician’s prescription. If you or someone you know is experiencing an overdose or severe side effects, call emergency services immediately.