pregabalin capsules CV

Action

Unclear. Binds with high affinity to CNS alpha₂-delta site (auxiliary subunit of voltage-gated calcium channels), possibly resulting in antinociceptive and antiseizure effects.

Availability

Capsules: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg

Indications and dosages

➣ Adjunct for partial-onset seizures in adults

Adults: Initially, 75 mg P.O. b.i.d. or 50 mg P.O. t.i.d.; may increase to maximum of 600 mg P.O. daily given in divided doses based on response and tolerance

➣ Neuropathic pain related to diabetic peripheral neuropathy

Adults: Initially, 50 mg P.O. t.i.d. in patients with creatinine clearance of at least 60 ml/minute; may increase to maximum of 100 mg P.O. t.i.d. within 1 week based on efficacy and tolerance

➣ Postherpetic neuralgia

Adults: Initially, 75 mg P.O. b.i.d., or 50 mg P.O. t.i.d. in patients with creatinine clearance of at least 60 ml/minute; may increase to maximum of 300 mg P.O. daily within 1 week based on efficacy and tolerance. Tolerant patients who don't obtain sufficient pain relief after 2 to 4 weeks of 300 mg daily may receive up to 300 mg b.i.d. or 200 mg t.i.d. Reserve dosages above 300 mg daily for patients with ongoing pain who tolerate 300 mg daily.

➣ Fibromyalgia

Adults: Initially, 75 mg P.O. b.i.d. in patients with creatinine clearance of at least 60 ml/minute; may increase to 150 mg P.O. b.i.d. within 1 week based on efficacy and tolerance. If patient doesn't obtain sufficient benefit at 300 mg daily, dosage may be increased further to 225 mg b.i.d. Dosages above 450 mg daily aren't recommended.

Dosage adjustment

• Renal impairment

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• abnormal creatinine clearance

• concurrent use of thiazolidinedione antidiabetics

• history of angioedema episode

• concurrent use of drugs associated with angioedema (such as angiotensin-converting enzyme inhibitors)

• elderly patients

• children (safety and efficacy not established).

Administration

• Give with or without food.

• To discontinue drug, withdraw gradually over at least 1 week to reduce risk of increased seizure frequency in patients with history of seizure disorders.

Adverse reactions

CNS: dizziness, somnolence, euphoria, balance disorder, abnormal thinking, asthenia, neuropathy, ataxia, vertigo, confusion, incoordination, abnormal gait, tremor, amnesia, nervousness, headache, speech disorder, twitching, myoclonus, fatigue, feeling drunk, hypertonia, hypoesthesia, paresthesia, lethargy, anxiety, disorientation, depression, depersonalization, stupor

EENT: abnormal or blurred vision, diplopia, nystagmus, conjunctivitis, sinusitis, otitis media, tinnitus, pharyngolaryngeal pain

GI: vomiting, constipation, flatulence, abdominal distention, gastroenteritis, dry mouth

GU: urinary incontinence, urinary frequency, decreased libido, anorgasmia, erectile dysfunction

Metabolic: hypoglycemia, fluid retention

Musculoskeletal: back pain, myasthenia, arthralgia, muscle spasms

Respiratory: dyspnea, bronchitis

Skin: ecchymosis, pruritus

Other: increased appetite, weight gain, edema, peripheral edema, accidental injury, pain, chest pain, infection, allergic reaction, angioedema, hypersensitivity reactions including anaphylactoid reactions (rare)

Interactions

Drug-drug. Gabapentin: slight decrease in pregabalin rate of absorption

Lorazepam, oxycodone: exacerbated effects on cognitive and gross motor functioning

Drug-diagnostic tests. Serum glucose: decreased level

Drug-behaviors. Alcohol use: exacerbated effects on cognitive and gross motor functioning

Patient monitoring

See Monitor patient closely for hypersensitivity reaction and angioedema; if these effects occur, discontinue drug and begin emergency measures immediately.

• Know that patients with history of drug or alcohol abuse may be more likely to misuse or abuse drug.

Patient teaching

• Instruct patient to take drug with or without food.

See Teach patient to recognize signs and symptoms of angioedema and to discontinue drug and seek immediate medical care if these arise.

See Inform patient that drug may cause hypersensitivity reactions, such as wheezing, dyspnea, rash, hives, and blisters. Advise patient to discontinue drug and seek medical care if these reactions occur.

• Inform patient that drug may cause weight gain and edema.

• Advise patient to avoid driving and other hazardous activities until drug's effects on vision and alertness are known.

• Caution patient to avoid alcohol while taking drug.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.