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All about: Pregabalin

Big Image Pronouncation: (preh-GAB-ah-lin)
Class: Anticonvulsant

Trade Names:
Lyrica
- Capsules 25 mg
- Capsules 50 mg
- Capsules 75 mg
- Capsules 100 mg
- Capsules 150 mg
- Capsules 200 mg
- Capsules 225 mg
- Capsules 300 mg

Mechanism of Action

Pharmacology

Mechanism of pregabalin's antinociceptice and antiseizure effects is unknown. Effects may be related to high affinity binding to alpha 2 -delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissue.

Pharmacokinetics

Absorption

Well absorbed after oral administration; bioavailability more than 90%. T max within 1.5 hr. Steady state achieved within 24 to 48 hr.

Distribution

Vd is approximately 0.5 L/kg. Substrate for system L transporter (transports large amino acids across blood brain barrier.

Metabolism

Negligible metabolism.

Elimination

T ½ is about 6 hr. Largely eliminated by renal excretion; 90% excreted unchanged in urine.

Special Populations

Renal Function Impairment

Cl nearly proportional to Ccr.

Elderly

Renal Cl decreases as result of age-related decline in renal function.

Indications and Usage

Management of neuropathic pain associated with diabetic peripheral neuropathy; adjunctive therapy for adults with partial-onset seizures; management of postherpetic neuralgia.

Contraindications

Standard considerations.

Dosage and Administration

Neuropathic Pain Associated with Diabetic Peripheral Neuropathy
Adults

PO Initial: 50 mg tid increased to 300 mg/day within 1 wk based on efficacy and tolerability (max, 300 mg/day).

Epilepsy
Adults

PO Initial: 75 mg bid or 50 mg tid increased to max dose of 300 mg bid or 200 mg tid.

Postherpetic Neuralgia
Adults

PO Initial: 75 mg bid or 50 mg tid increased to 300 mg/day within 1 wk based on efficacy and tolerability. May increase up to 300 mg bid or 200 mg tid if necessary and tolerated (max, 600 mg/day).

Discontinuation

Taper over 1 wk.

Dosage Adjustment for Renal Impairment
Adults

Ccr 60 mL/min or greater: total daily dose range 150 to 600 mg/day administered bid or tid; Ccr 30 to 59 mL/min: total daily dose range 75 to 300 mg/day administered bid or tid; Ccr 15 to 29 mL/min: total daily dose range 25 to 150 mg administered once or twice daily; Ccr less than 15 mL/min: total daily dose range 25 to 75 mg/day administered once daily.

Patients on hemodialysis

Maintenance doses based on Ccr as recommended plus a supplemental post-hemodialysis dose administered after each 4 hr of hemodialysis as follows: if maintenance dose 25 mg once daily, post-dialysis dose is 25 or 50 mg; if maintenance dose is 25 to 50 mg once daily, post-dialysis dose is 50 or 75 mg; if maintenance dose 75 mg once daily, post-dialysis dose is 100 or 150 mg.

Storage/Stability

Store capsules at controlled room temperature (59° to 86°F).

Drug Interactions

CNS depressants (eg, alcohol, lorazepam, oxycodone)

Additive effects on cognitive and gross motor function have been seen. Avoid alcohol.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Abnormal thinking, amnesia, anxiety, asthenia, ataxia, confusion, depersonalization, dizziness, euphoria, abnormal gait, headache, hypertonia, hypesthesia, incoordination, decreased libido, myoclonus, nervousness, neuropathy, nystagmus, paresthesia, somnolence, speech disorder, stupor, tremor, twitching, vertigo (at least 1%).

Dermatologic

Pruritus (at least 1%).

EENT

Abnormal vision, blurred vision, conjunctivitis, diplopia, eye disorder (at least 1%).

GI

Abdominal pain, constipation, dry mouth, flatulence, gastroenteritis, vomiting (at least 1%).

Genitourinary

Anorgasmia, impotence, urinary frequency, urinary incontinence (at least 1%).

Lymphatic

Ecchymosis (at least 1%).

Metabolic-Nutritional

Edema, hypoglycemia, peripheral edema, weight gain (at least 1%).

Musculoskeletal

Arthralgia, back pain, myasthenia (at least 1%).

Respiratory

Bronchitis, dyspnea (at least 1%).

Miscellaneous

Accidental injury, allergic reaction, increased appetite, chest pain, face edema, flu-syndrome, infection, pain (at least 1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Because of age-related renal impairment, dosage adjustment is recommended.

Renal Function

Dose reduction recommended.

Hazardous Tasks

May cause dizziness and drowsiness.

Congestive heart failure

Use with caution in patients with NYHA Class III or IV cardiac status.

Creatine kinase elevations

Has been reported. Discontinue pregabalin if myopathy is diagnosed or suspected or if markedly elevated creatine kinase levels occur.

Decreased platelet count

Clinically significant decreases in platelets (20% below baseline and less than 150 x 103/mcL) have been documented.

ECG changes

Mild PR interval prolongation (3 to 6 msec) has been reported; these changes were not associated with an increased risk of PR increases greater than 25% from baseline, on-treatment PR intervals greater than 200 msec, or increased risk of second or third degree block.

Peripheral edema

Has been reported, more frequently in patients taking pregabalin and a thiazolidinedione antidiabetic agent. Use caution with coadministration.

Ophthalmological effects

Reduction in visual acuity, visual field changes, and funduscopic changes have been reported.

Weight gain

Has been reported.

Overdosage

Symptoms

None known.

Patient Information

  • Explain name, dose, action, and potential side effects of drug.
  • Advise patient or caregiver to read the Patient Information leaflet before starting therapy and with each refill.
  • Instruct patient with epilepsy to continue to take other medications for seizures unless advised otherwise by health care provider.
  • Advise patient or caregiver that medication will usually be started at a low dose and then increased as tolerated until maximum benefit has been obtained.
  • Instruct patient or caregiver to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
  • Advise patient to take without regard to meals but to take with food if stomach upset occurs.
  • Advise patient or caregiver that if medication needs to be discontinued it will be slowly withdrawn over a period of 1 wk or more unless safety concerns (eg, rash) require a more rapid withdrawal.
  • Instruct patient to immediately report unexplained muscle pain, tenderness, or weakness, especially if accompanied by general body discomfort or fever.
  • Caution patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
  • Advise patient that pregabalin may cause visual changes, edema (swelling in feet and/or ankles), and weight gain and to notify health care provider if any of these occur.
  • Caution patient to avoid alcohol, opiates, and other CNS depressants while taking pregabalin because of risk of additive CNS impairment and depressant effects.
  • Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
  • Instruct women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
  • Instruct patient with seizures to notify health care provider if seizures worsen or if new types of seizures occur.
  • Advise patient with epilepsy to carry identification (eg, Medic Alert ) indicating medication usage and epilepsy.
  • Advise patient not to take any prescription or OTC medications, dietary supplements, or herbal preparations unless advised by health care provider.
  • Advise patient or caregiver that follow-up visits and lab tests may be required to monitor therapy and to keep appointments.

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