- Capsules 25 mg
- Capsules 50 mg
- Capsules 75 mg
- Capsules 100 mg
- Capsules 150 mg
- Capsules 200 mg
- Capsules 225 mg
- Capsules 300 mg
- Oral solution 20 mg/mL
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.
Well absorbed after oral administration; bioavailability is more than 90%. T max occurs within 1.5 h. Steady state was achieved within 24 to 48 h.
Vd is approximately 0.5 L/kg. Substrate for system L transporter, which is responsible for the transport of large amino acids across the blood brain barrier.
The half-life is 6.3 h. Largely eliminated by renal excretion; 90% excreted unchanged in urine. Mean renal Cl is approximately 67 to 80.9 mL/min.
Special PopulationsRenal Function Impairment
Cl is nearly proportional to CrCl. Plasma concentrations reduced by approximately 50% following a 4-h hemodialysis treatment.Elderly
Oral Cl tends to decrease with increasing age. Dose reduction may be required in patients who have age-related renal impairment.Children
Pharmacokinetics have not been studied.Gender
Pharmacokinetics do not seem to be affected by gender.Race
Pharmacokinetics do not seem to be affected by 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.
Treatment of generalized anxiety disorder.
Dosage and AdministrationNeuropathic Pain Associated With Diabetic Peripheral Neuropathy
PO 50 mg 3 times daily initially, increased to 100 mg 3 times daily within 1 wk based on efficacy and tolerability (max, 300 mg/day).Partial-Onset Seizures
PO 75 mg twice daily or 50 mg 3 times daily initially, increased to 150 to 600 mg/day divided 2 or 3 times daily based on efficacy and tolerability (max, 600 mg/day).Postherpetic Neuralgia
PO 75 mg twice daily or 50 mg 3 times daily initially, increased to 150 mg twice daily or 100 mg 3 times daily within 1 wk based on efficacy and tolerability. If relief is insufficient after 2 to 4 wk, may increase up to 300 mg twice daily or 200 mg 3 times daily.Fibromyalgia
PO 75 mg twice daily initially, increased to 150 mg twice daily within 1 wk based on efficacy and tolerability. Patients not experiencing sufficient benefit may further increase the dosage to 225 mg twice daily (max, 450 mg/day).Dosage Adjustment for Renal Function Impairment
CrCl 60 mL/min or greater: total daily dose range of 150 to 600 mg/day administered twice daily or 3 times daily; CrCl 30 to 60 mL/min: total daily dose range of 75 to 300 mg/day administered twice daily or 3 times daily; CrCl 15 to 30 mL/min: total daily dose range of 25 to 150 mg administered once or twice daily; CrCl less than 15 mL/min: total daily dose range of 25 to 75 mg/day administered once daily.Hemodialysis patients
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.
- May be given with or without food.
- When discontinuing, taper gradually over a minimum of 1 wk.
Store at 59° to 86°F. Use the oral solution within 45 days of first opening the bottle.
Drug InteractionsACE inhibitors (eg, captopril)
Coadministration of these agents may increase the risk of swelling and hives. The patient's health care provider should be contacted immediately, if these signs occur.CNS depressants (eg, alcohol, lorazepam, oxycodone)
Additive effects on cognitive and gross motor function have been seen. Avoid alcohol.Thiazolidinediones (eg, pioglitazone)
Both pregabalin and thiazolidinediones may cause weight gain and/or fluid retention, possibly exacerbating or leading to heart failure. Use with caution. Monitor the patient. If an interaction is suspected, it may be necessary to adjust the dose of one or both agents.
Dizziness (45%); somnolence (28%); ataxia (20%); headache (14%); tremor (11%); abnormal thinking, balance disorder, neuropathy (9%); abnormal gait, fatigue (8%); asthenia, confusion, euphoria, speech disorder (7%); amnesia, disturbances in attention, incoordination (6%); twitching (5%); memory impairment, myoclonus, vertigo (4%); abnormal feeling, hypesthesia (3%); anxiety, depression, disorientation, drunk feeling, lethargy (2%); depersonalization, hypertonia, paresthesia, stupor (at least 1%); nervousness (1%).
Blurred vision, diplopia (12%); abnormal vision (5%); pharyngolaryngeal pain (3%); eye disorder (2%); conjunctivitis, nystagmus, otitis media, tinnitus (at least 1%).
Dry mouth (15%); constipation (10%); increased appetite (7%); flatulence, vomiting (3%); abdominal distension (2%); abdominal pain, gastroenteritis (at least 1%); diarrhea, nausea (postmarketing).
Urinary incontinence (2%); anorgasmia, impotence, libido decreased, urinary frequency (at least 1%).
Peripheral edema, weight gain (16%); edema (6%); face edema, fluid retention, hypoglycemia (3%).
Arthralgia (6%); back pain, muscle spasm (4%); leg cramps, myalgia, myasthenia (at least 1%).
Sinusitis (7%); bronchitis, dyspnea (3%).
Infection (14%); pain (5%); chest pain (4%); flu syndrome (2%); allergic reaction, ecchymosis, fever, pruritus (at least 1%); angioedema, hypersensitivity (postmarketing).
Monitor for emergence or worsening of depression, suicidal thoughts or behavior, or any unusual changes in behavior. Monitor for weight gain and/or fluid retention, possibly exacerbating or leading to heart failure. Carefully evaluate patients for a history of drug abuse and observe them for signs of pregabalin misuse or abuse (eg, development of tolerance, dose escalation, drug-seeking behavior).
Category C .
Safety and efficacy not established.
Because of age-related renal function impairment, dosage adjustment may be needed.
Hypersensitivity reactions (including skin redness, blisters, hives, rash, dyspnea, and wheezing) have been reported shortly after initiation of pregabalin.
Dose reduction recommended.
May cause dizziness and drowsiness, which may impair the ability to preform tasks such as driving or operating machinery.
Has been reported during initial and long-term treatment.
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 × 10 3 /mcL) have been documented.
Withdrawal symptoms may occur suggestive of physical dependence.
Discontinuation of therapy
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.
Reduction in visual acuity, visual field changes, and funduscopic changes have been reported.
Has been reported. Occurs more frequently in patients taking pregabalin and a thiazolidinedione antidiabetic agent.
PR interval prolongation
PR interval prolongation (3 to 6 msec) has been reported; the mean change 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.
Suicidal behavior and ideation
May increase the risk of suicidal thoughts or behavior. This was observed as early as 1 week after starting treatment and persisted for the duration of treatment.
Has been reported.
None well documented.
- Advise patient or caregiver to read the Medication Guide 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.
- Advise patients that concomitant treatment with pregabalin and a thiazolidinedione antidiabetic agent may lead to an additive effect on edema and weight gain. For patients with preexisting cardiac conditions, this may increase the risk of heart failure.
- 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.
- Advise patients that the drug may increase the risk of suicidal thoughts and behavior and to be alert for the emergence or worsening of symptoms of depression.
- Advise patients that pregabalin may cause angioedema, with swelling of the face, mouth (lip, gum, and tongue), and neck (larynx and pharynx) that can lead to life-threatening respiratory compromise. Instruct patients to discontinue pregabalin and immediately seek medical care if they experience these symptoms.
- Advise patients that pregabalin has been associated with hypersensitivity reactions (eg, blisters, dyspnea, hives, rash, wheezing). Instruct patients to discontinue pregabalin and seek medical care immediately if they experience these symptoms.
- Counsel patients, their caregivers, and families that antilepileptic drugs, including pregabalin, may increase the risk of suicidal thoughts and behavior and advise them of the need to be alert for the emergence or worsening of symptoms of depression; any unusual changes in mood or behavior; or the emergence of suicidal thoughts, behavior, or thoughts about self-harm. Immediately report behaviors of concern to health care providers.
- Instruct patients to notify health care provider if they become pregnant or intend to become pregnant during therapy, and to notify their health care provider if they are breast-feeding or intend to breast-feed during therapy.
- Encourage patients to enroll in the NAAED Pregnancy Registry if they become pregnant. This registry is collecting information about the safety of antiepileptic drugs during pregnancy. To enroll, patients can call the toll-free number 1-888-233-2334.
- Inform men being treated with pregabalin who plan to father a child of the potential risk of male-mediated teratogenicity.
- Instruct patients with diabetes to pay particular attention to skin integrity while being treated with pregabalin.
Copyright © 2009 Wolters Kluwer Health.
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