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
| ||||||||||||
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 ImpairmentCl nearly proportional to CrCl.
Gender/RacePharmacokinetics 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 NeuropathyAdults
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 SeizuresAdults
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 NeuralgiaAdults
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).
FibromyalgiaAdults
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).
DiscontinuationTaper over 1 wk.
Dosage Adjustment for Renal Function ImpairmentAdults
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 hemodialysisMaintenance 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.
 |
Link to Page |  |
Print Page |  |
Email Page |  | Add to List |
More Pregabalin resources:
Pregabalin - Includes detailed dosage instructions.
Generalized Anxiety Disorder, Migraine Prevention, Persisting Pain -- Shingles, Diabetic Nerve Damage, Fibromyalgia, Pain, Neuralgia, Epilepsy
