Professional Information

Pregabalin

Pronouncation: (pre-GA-ba-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

Pharmacology

Feedback for Pregabalin

As a treatment for...	Avg User Ratings [?]
Neuralgia	2 comments Rate it!	9.3
Generalized Anxiety Disorder	8 comments Rate it!	9.2
Migraine Prevention	2 comments Rate it!	8.5

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Mechanism of pregabalin's antinociceptive 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 h. Steady state achieved within 24 to 48 h.

Distribution

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

Metabolism

Negligible metabolism.

Elimination

The t _½ is about 6 h. Largely eliminated by renal excretion; 90% excreted unchanged in urine.

Special Populations

Renal Function Impairment

Cl nearly proportional to CrCl.

Gender/Race

Pharmacokinetics do not seem to be affected by gender or race.

Indications and Usage

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

Unlabeled Uses

Treatment of generalized anxiety disorder.

Contraindications

Standard considerations.

Dosage and Administration

Neuropathic Pain Associated With Diabetic Peripheral Neuropathy
Adults

PO Initial: 50 mg 3 times daily increased to 100 mg 3 times daily within 1 wk based on efficacy and tolerability (max, 300 mg/day).

Partial-Onset Seizures
Adults

PO Initial: 75 mg twice daily or 50 mg 3 times daily increased to max dose of 300 mg twice daily or 200 mg 3 times daily.

Postherpetic Neuralgia
Adults

PO Initial: 75 mg twice daily or 50 mg 3 times daily increased to 300 mg/day within 1 wk based on efficacy and tolerability. If relief is insufficient after 2 to 4 weeks, may increase up to 300 mg twice daily or 200 mg 3 times daily if necessary and tolerated (max, 600 mg/day).

Fibromyalgia
Adults

PO Initial: 75 mg twice daily increased to 150 mg twice daily within 1 wk based on efficacy and tolerability. Patients not experiencing sufficient benefit may further increase the dose to 225 mg twice daily (max, 450 mg/day).

Discontinuation

Taper over 1 wk.

Dosage Adjustment for Renal Function Impairment
Adults

CrCl greater than 60 mL/min: total daily dose range 150 to 600 mg/day administered twice daily or 3 times daily; CrCl 30 to 60 mL/min: total daily dose range 75 to 300 mg/day administered twice daily or 3 times daily; CrCl 15 to 30 mL/min: total daily dose range 25 to 150 mg administered once or twice daily; CrCl less than 15 mL/min: total daily dose range 25 to 75 mg/day administered once daily.

Patients on hemodialysis

Maintenance doses based on CrCl as recommended plus a supplemental posthemodialysis dose administered after each 4 h of hemodialysis as follows: if maintenance dose 25 mg once daily, postdialysis dose is 25 or 50 mg; if maintenance dose is 25 to 50 mg once daily, postdialysis dose is 50 or 75 mg; if maintenance dose is 50 to 75 mg once daily, postdialysis dose is 75 or 100 mg; if maintenance dose is 75 mg daily, postdialysis dose is 100 to 150 mg.

Storage/Stability

Store capsules at 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

Dizziness (45%); somnolence (28%); ataxia (20%); headache (14%); tremor (11%); abnormal thinking, balance disorder, neuropathy (9%); abnormal gait, fatigue (8%); asthenia, confusion, euphoria, increased appetite, speech disorder (7%); amnesia, disturbances in attention, incoordination (6%); twitching (5%); amnesia, memory impairment, myoclonus, vertigo (4%); abnormal feeling, hypoesthesia (3%); anxiety, depression, disorientation, drunk feeling, lethargy, nervousness (2%); depersonalization, hypertonia (at least 1%).

Dermatologic

Pruritus (at least 1%).

EENT

Blurred vision, diplopia (12%); abnormal vision (5%); pharyngolaryngeal pain (3%); eye disorder, vertigo (2%); conjunctivitis, otitis media, tinnitus (at least 1%).

GI

Dry mouth (15%); constipation (10%); increased appetite (6%); flatulence, vomiting (3%); distension (2%); gastroenteritis (at least 1%); diarrhea, nausea (postmarketing).

Genitourinary

Urinary incontinence (2%); anorgasmia, impotence, urinary frequency, urinary incontinence (at least 1%).

Hematologic-Lymphatic

Ecchymosis (at least 1%).

Hypersensitivity

Hypersensitivity, including blisters, dyspnea, hives, rash, skin redness, and wheezing (postmarketing).

Metabolic-Nutritional

Peripheral edema, weight gain (16%); edema (6%); hypoglycemia (3%).

Musculoskeletal

Back pain, muscle spasm (4%); leg cramps, myalgia (at least 1%); arthralgia, myasthenia (1%).

Respiratory

Sinusitis (7%); bronchitis, dyspnea (3%).

Miscellaneous

Infection (14%); accidental injury (11%); pain (5%); chest pain (4%); face edema (3%); flu syndrome (2%); abdominal pain, allergic reaction, fever (at least 1%); angioedema, including swelling of face, mouth, and neck (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Because of age-related renal function impairment, dosage adjustment may be needed.

Renal Function

Dose reduction recommended.

Hazardous Tasks

May cause dizziness and drowsiness.

Antiepileptic drug withdrawal

Withdraw gradually (over at least 1 wk) to minimize potential of increased seizure frequency in patients with seizure disorders. Upon abrupt or rapid discontinuation, insomnia, nausea, headache, and diarrhea have been reported.

CHF

Use with caution in patients with New York Heart Association class III or IV cardiac status.

Creatine kinase elevations

Have 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 × 103/mcL) have been documented.

ECG changes

Mild PR interval prolongation (3 to 6 msec) has been reported; the mean changes difference was not associated with an increased risk of PR increase more than 25% from baseline, on-treatment PR more than 200 msec, or increased risk of second- or third-degree AV 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

Advise patient or caregiver to read the patient information leaflet before starting therapy and to reread 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 max 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 patient with seizures to notify health care provider if seizures worsen or if new types of seizures occur.
Advise patient with epilepsy to carry medical identification (eg, card, bracelet) indicating medication usage and epilepsy.