Ruibeihu Pregabalin Sustained-release Tablets

1. Indications and Usage
Neuropathic Pain: Indicated as adjunctive therapy for adult patients with postdiabetic peripheral neuropathy (pDPN), postherpetic neuralgia (PHN), fibromyalgia, and spinal cord injury (SCI)-related neuropathic pain.
Epilepsy: Indicated as adjunctive treatment for partial-onset seizures in patients aged 4 years and older.
2. Dosage and Administration
Route of Administration: Oral administration.
Recommended Dosage:
pDPN/PHN: Start at 165 mg once daily. The dose may be increased to 330 mg once daily within one week. The maximum recommended dose is 330 mg once daily (660 mg once daily for PHN).
Fibromyalgia: The recommended dose range is 330 mg to 495 mg once daily.
Partial-onset Seizures: Dosing depends on age, renal function, and concomitant medications.
Administration Details: Must be taken with food (preferably after dinner). The tablet must be swallowed whole and must not be divided, crushed, or chewed.
Discontinuation: Must be tapered gradually over at least 1 week to minimize withdrawal symptoms.
3. Mechanism of Action
Calcium Channel Modulation: Pregabalin binds to the α2δ subunit of voltage-gated calcium channels in the central nervous system.
Neurotransmitter Inhibition: This binding reduces calcium influx, leading to decreased release of excitatory neurotransmitters (such as glutamate, norepinephrine, and substance P) involved in pain transmission and neuronal hyperexcitability.
4. Safety and Warnings
Angioedema and Hypersensitivity: Discontinue immediately if facial, oral, or laryngeal edema or severe skin eruptions occur.
Driving and Machinery: May cause dizziness and somnolence; patients should avoid driving or operating hazardous machinery until the effect is known.
Cardiac Failure: May cause or exacerbate peripheral edema; use with caution in patients with a history of congestive heart failure (NYHA class II-IV).
Suicidal Behavior: Monitor for depression or changes in mood and behavior, particularly when used as an antiepileptic drug.
5. Adverse Reactions
Most Common Adverse Reactions: Dizziness, somnolence, ataxia, confusion, peripheral edema, dry mouth, weight gain, blurred vision, and constipation.
6. Drug Interactions
CNS Depressants: Concomitant use with ethanol, lorazepam, or opioids (e.g., oxycodone) may enhance CNS depression and cognitive impairment.
Thiazolidinediones: May cause additive effects leading to increased weight gain and peripheral edema.
Renal Excretion: No significant pharmacokinetic interactions are expected as pregabalin is primarily excreted unchanged in the urine.
7. Pharmaceutical Information
Composition: Active ingredient: Pregabalin.
Appearance: White to off-white, oval-shaped film-coated tablets.
Packaging: Available in blister packs (e.g., 8 or 30 tablets per pack).
Storage: Store at controlled room temperature; protect from moisture.