The overall safety profile in adolescents was similar to that observed in adults with fibromyalgia. Safety and effectiveness in pediatric patients below the age of 1 month have not been established. The youngest subject evaluated was 3 months of age; use in patients 1 month to less than 3 months of age is supported by additional pharmacokinetic analyses.
A no-effect dose was not established. In controlled clinical studies of LYRICA in neuropathic pain associated with diabetic peripheral neuropathy, patients were 65 to 74 years of age, and 73 patients were 75 years of age or older.
In controlled clinical studies of LYRICA in neuropathic pain associated with postherpetic neuralgia, patients were 65 to 74 years of age, and patients were 75 years of age or older. In controlled clinical studies of LYRICA in epilepsy, there were only 10 patients 65 to 74 years of age, and 2 patients who were 75 years of age or older. No overall differences in safety and efficacy were observed between these patients and younger patients. Although the adverse reaction profile was similar between the two age groups, the following neurological adverse reactions were more frequent in patients 65 years of age or older: dizziness, vision blurred, balance disorder, tremor, confusional state, coordination abnormal, and lethargy.
Because LYRICA is eliminated primarily by renal excretion, adjust the dose for elderly patients with renal impairment [see Dosage and Administration 2. LYRICA is eliminated primarily by renal excretion and dose adjustment is recommended for adult patients with renal impairment [see Dosage and Administration 2.
In clinical studies, following abrupt or rapid discontinuation of LYRICA, some patients reported symptoms including insomnia, nausea, headache or diarrhea [see Warnings and Precautions 5. In the postmarketing experience, in addition to these reported symptoms there have also been reported cases of anxiety and hyperhidrosis.
Seizures and heart block have also been reported. If indicated, elimination of unabsorbed drug may be attempted by emesis or gastric lavage; observe usual precautions to maintain the airway. General supportive care of the patient is indicated including monitoring of vital signs and observation of the clinical status of the patient. Pregabalin is described chemically as S aminomethyl methylhexanoic acid.
The molecular formula is C 8 H 17 NO 2 and the molecular weight is The chemical structure of pregabalin is:. Pregabalin is a white to off-white, crystalline solid with a pK a1 of 4. It is freely soluble in water and both basic and acidic aqueous solutions. LYRICA pregabalin Capsules are administered orally and are supplied as imprinted hard-shell capsules containing 25, 50, 75, , , , , and mg of pregabalin, along with lactose monohydrate, cornstarch, and talc as inactive ingredients.
The capsule shells contain gelatin and titanium dioxide. In addition, the orange capsule shells contain red iron oxide and the white capsule shells contain sodium lauryl sulfate and colloidal silicon dioxide. Colloidal silicon dioxide is a manufacturing aid that may or may not be present in the capsule shells.
The imprinting ink contains shellac, black iron oxide, propylene glycol, and potassium hydroxide. LYRICA pregabalin binds with high affinity to the alpha 2 -delta site an auxiliary subunit of voltage-gated calcium channels in central nervous system tissues.
Although the mechanism of action of pregabalin has not been fully elucidated, results with genetically modified mice and with compounds structurally related to pregabalin such as gabapentin suggest that binding to the alpha 2 -delta subunit may be involved in pregabalin's anti-nociceptive and antiseizure effects in animals.
Evidence from other animal models of nerve damage and persistent pain suggest the anti-nociceptive activities of pregabalin may also be mediated through interactions with descending noradrenergic and serotonergic pathways originating from the brainstem that modulate pain transmission in the spinal cord. However, in cultured neurons prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport.
Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. Pregabalin is well absorbed after oral administration, is eliminated largely by renal excretion, and has an elimination half-life of about 6 hours. Following repeated administration, steady state is achieved within 24 to 48 hours.
Multiple-dose pharmacokinetics can be predicted from single-dose data. However, administration of pregabalin with food has no clinically relevant effect on the total absorption of pregabalin. Therefore, pregabalin can be taken with or without food. Pregabalin does not bind to plasma proteins. The apparent volume of distribution of pregabalin following oral administration is approximately 0. Pregabalin is a substrate for system L transporter which is responsible for the transport of large amino acids across the blood brain barrier.
Although there are no data in humans, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkeys. In addition, pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. Pregabalin undergoes negligible metabolism in humans. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in urine, accounted for 0.
In preclinical studies, pregabalin S-enantiomer did not undergo racemization to the R-enantiomer in mice, rats, rabbits, or monkeys. Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6. Mean renal clearance was estimated to be Because pregabalin is not bound to plasma proteins this clearance rate indicates that renal tubular reabsorption is involved. Pregabalin elimination is nearly proportional to creatinine clearance CLcr [see Dosage and Administration 2.
In population pharmacokinetic analyses of the clinical studies in various populations, the pharmacokinetics of LYRICA were not significantly affected by race Caucasians, Blacks, and Hispanics.
Population pharmacokinetic analyses of the clinical studies showed that the relationship between daily dose and LYRICA drug exposure is similar between genders. Pregabalin clearance is nearly proportional to creatinine clearance CLcr. Dosage reduction in patients with renal dysfunction is necessary. Pregabalin is effectively removed from plasma by hemodialysis. For patients on hemodialysis, dosing must be modified [see Dosage and Administration 2. Pregabalin oral clearance tended to decrease with increasing age.
This decrease in pregabalin oral clearance is consistent with age-related decreases in CLcr. Reduction of pregabalin dose may be required in patients who have age-related compromised renal function [see Dosage and Administration 2.
Pediatric Patients 3 months to less than 17 years of age. Pregabalin pharmacokinetics were evaluated in pediatric patients 3 months to less than 17 years of age with partial-onset seizures at dose levels of 2. Following oral administration, pregabalin reaches peak plasma concentration at 0. A weight-based dosing regimen is necessary to achieve pregabalin exposures in pediatric patients 1 month to less than 17 years of age similar to those observed in adults treated for partial-onset seizures at effective doses [see Dosage and Administration 2.
The relationship is similar in pediatric and adult subjects. Therefore, an increase in the metabolism of coadministered CYP1A2 substrates e. The drug interaction studies described in this section were conducted in healthy adults, and across various patient populations. The pharmacokinetic interactions of pregabalin and gabapentin were investigated in 12 healthy subjects following concomitant single-dose administration of mg pregabalin and mg gabapentin and in 18 healthy subjects following concomitant multiple-dose administration of mg pregabalin every 8 hours and mg gabapentin every 8 hours.
Gabapentin pharmacokinetics following single- and multiple-dose administration were unaltered by pregabalin coadministration. The extent of pregabalin absorption was unaffected by gabapentin coadministration, although there was a small reduction in rate of absorption.
Multiple-dose administration of pregabalin mg twice a day in healthy subjects had no effect on the rate and extent of lorazepam single-dose pharmacokinetics and single-dose administration of lorazepam 1 mg had no effect on the steady-state pharmacokinetics of pregabalin. Multiple-dose administration of pregabalin mg twice a day in healthy subjects had no effect on the rate and extent of oxycodone single-dose pharmacokinetics.
Single-dose administration of oxycodone 10 mg had no effect on the steady-state pharmacokinetics of pregabalin. Multiple-dose administration of pregabalin mg twice a day in healthy subjects had no effect on the rate and extent of ethanol single-dose pharmacokinetics and single-dose administration of ethanol 0.
Phenytoin, carbamazepine, valproic acid, and lamotrigine. Steady-state trough plasma concentrations of phenytoin, carbamazepine and carbamazepine 10,11 epoxide, valproic acid, and lamotrigine were not affected by concomitant pregabalin mg three times a day administration.
Population pharmacokinetic analyses in patients treated with pregabalin and various concomitant medications suggest the following:. A no-effect dose for induction of hemangiosarcomas in mice was not established. Pregabalin was not mutagenic in bacteria or in mammalian cells in vitro , was not clastogenic in mammalian systems in vitro and in vivo , and did not induce unscheduled DNA synthesis in mouse or rat hepatocytes.
These included decreased sperm counts and sperm motility, increased sperm abnormalities, reduced fertility, increased preimplantation embryo loss, decreased litter size, decreased fetal body weights, and an increased incidence of fetal abnormalities.
Effects on sperm and fertility parameters were reversible in studies of this duration 3—4 months. The low dose in this study produced a plasma exposure approximately 9 times that in humans receiving the MRD. A no-effect dose for female reproductive toxicity in rats was not established.
Skin lesions ranging from erythema to necrosis were seen in repeated-dose toxicology studies in both rats and monkeys. The etiology of these skin lesions is unknown. The more severe dermatopathies involving necrosis were associated with pregabalin exposures as expressed by plasma AUCs of approximately 3 to 8 times those achieved in humans given the MRD.
No increase in incidence of skin lesions was observed in clinical studies. A no-effect dose for ocular lesions was not established.
Similar lesions were not observed in lifetime carcinogenicity studies in two strains of mice or in monkeys treated for 1 year. The efficacy of the maximum recommended dose of LYRICA for the management of neuropathic pain associated with diabetic peripheral neuropathy was established in three double-blind, placebo-controlled, multicenter studies with three times a day dosing, two of which studied the maximum recommended dose.
Patients were enrolled with either Type 1 or Type 2 diabetes mellitus and a diagnosis of painful distal symmetrical sensorimotor polyneuropathy for 1 to 5 years. The patients had a minimum mean baseline pain score of greater than or equal to 4 on an point numerical pain rating scale ranging from 0 no pain to 10 worst possible pain. The baseline mean pain scores across the two studies ranged from 6. Patients were permitted up to 4 grams of acetaminophen per day as needed for pain, in addition to pregabalin.
Patients recorded their pain daily in a diary. There was no evidence of a greater effect on pain scores of the mg three times a day dose than the mg three times a day dose, but there was evidence of dose dependent adverse reactions [see Adverse Reactions 6.
For a range of levels of improvement in pain intensity from baseline to study endpoint, Figure 1 shows the fraction of patients achieving that level of improvement. Some patients experienced a decrease in pain as early as Week 1, which persisted throughout the study. For various levels of improvement in pain intensity from baseline to study endpoint, Figure 2 shows the fraction of patients achieving that level of improvement.
The efficacy of LYRICA for the management of postherpetic neuralgia was established in three double-blind, placebo-controlled, multicenter studies. These studies enrolled patients with neuralgia persisting for at least 3 months following healing of herpes zoster rash and a minimum baseline score of greater than or equal to 4 on an point numerical pain rating scale ranging from 0 no pain to 10 worst possible pain.
Seventy-three percent of patients completed the studies. The baseline mean pain scores across the 3 studies ranged from 6 to 7. For various levels of improvement in pain intensity from baseline to study endpoint, Figure 3 shows the fraction of patients achieving that level of improvement.
For various levels of improvement in pain intensity from baseline to study endpoint, Figure 4 shows the fraction of patients achieving those levels of improvement. For various levels of improvement in pain intensity from baseline to study endpoint, Figure 5 shows the fraction of patients achieving that level of improvement. The efficacy of LYRICA as adjunctive therapy for partial-onset seizures in adult patients was established in three week, randomized, double-blind, placebo-controlled, multicenter studies.
Patients were enrolled who had partial-onset seizures with or without secondary generalization and were not adequately controlled with 1 to 3 concomitant antiepileptic drugs AEDs. Patients taking gabapentin were required to discontinue gabapentin treatment 1 week prior to entering baseline. During an 8-week baseline period, patients had to experience at least 6 partial-onset seizures with no seizure-free period exceeding 4 weeks. The mean duration of epilepsy was 25 years in these 3 studies and the mean and median baseline seizure frequencies were Approximately half of the patients were taking 2 concurrent AEDs at baseline.
Table 11 shows median baseline seizure rates and median percent reduction in seizure frequency by dose. In the first study E1 , each daily dose was divided into two equal doses twice a day dosing. In the second study E2 , each daily dose was divided into three equal doses three times a day dosing. In the third study E3 , the same total daily dose was divided into two equal doses for one group twice a day dosing and three equal doses for another group three times a day dosing.
While the three times a day dosing group in Study E3 performed numerically better than the twice a day dosing group, this difference was small and not statistically significant.
The following figure displays responder rate by dose for two of the studies. Subset evaluations of the antiseizure efficacy of LYRICA showed no clinically important differences as a function of age, gender, or race. The efficacy of LYRICA as adjunctive therapy in partial-onset seizures was established in a week, randomized, double-blind, placebo-controlled, multicenter study in pediatric patients 4 years to less than 17 years of age with partial-onset seizures with or without secondary generalization.
The mean duration of epilepsy was 6 years and the mean and median baseline seizure frequencies were 57 and 18 seizures per month, respectively. Administration of each daily dose was divided into two equal doses twice a day dosing.
Because of higher weight-normalized clearance in patients with body weight less than 30 kg [see Clinical Pharmacology Table 12 shows median baseline seizure rates, median percent change from baseline in seizure rates, and percent difference relative to placebo derived from the primary analysis model by dose. While the 2. The following figure displays responder rate by dose:. The efficacy of LYRICA as adjunctive therapy in partial-onset seizures was established in a day, randomized, double-blind, placebo-controlled, multicenter study in children 1 month to less than 4 years of age with partial-onset seizures with or without secondary generalization.
The youngest patient evaluated was 3 months of age. During a to hour baseline video electroencephalogram EEG , patients had to experience at least 2 partial-onset seizures. The mean duration of epilepsy at baseline was 1. Administration of each daily dose was divided into three equal doses three times a day dosing. The primary endpoint was the hour partial-onset seizure rate based on the comparison of the baseline video EEG to a repeat 48—72 hour video EEG performed at the end of 14 days of double-blind treatment.
Table 13 shows median baseline seizure rates, median percent change from baseline in seizure rates, and percent difference relative to placebo derived from the primary analysis model by dose.
The efficacy of LYRICA for management of fibromyalgia was established in one week, double-blind, placebo-controlled, multicenter study F1 and one six-month, randomized withdrawal study F2. Studies F1 and F2 enrolled patients with a diagnosis of fibromyalgia using the American College of Rheumatology ACR criteria history of widespread pain for 3 months, and pain present at 11 or more of the 18 specific tender point sites.
The studies showed a reduction in pain by visual analog scale. Patients were enrolled with a minimum mean baseline pain score of greater than or equal to 4 on an point numeric pain rating scale and a score of greater than or equal to 40 mm on the mm pain visual analog scale VAS. The baseline mean pain score in this trial was 6.
Responders to placebo in an initial one-week run-in phase were not randomized into subsequent phases of the study. There was no evidence of a greater effect on pain scores of the mg daily dose than the mg daily dose, but there was evidence of dose-dependent adverse reactions [see Adverse Reactions 6. The results are summarized in Figure 9 and Table For various levels of improvement in pain intensity from baseline to study endpoint, Figure 9 shows the fraction of patients achieving that level of improvement.
The figure is cumulative. But another study did not find pregabalin to be any more effective than a placebo a treatment with no active drug for treating symptoms of opiate withdrawal. But it may be used off-label to treat this condition. With RLS, you experience twitchiness and discomfort occurs in your legs, typically after going to bed.
A clinical study found that pregabalin the active drug in Lyrica was more effective than a placebo in treating the symptoms of RLS. The study also found that Lyrica was less likely to cause worsening of symptoms over time compared with pramipexole Mirapex. A review of seven clinical trials found pregabalin the active drug in Lyrica to be effective for treating sleep problems related to GAD. If you have questions about treatment for sleep issues, including the Lyrica dosage for sleep that may be right for you, talk with your doctor.
Lyrica is FDA-approved for treating partial onset seizures in children ages 1 month and older. Clinical studies have found Lyrica to be effective for treating partial onset seizures in children ages 1 month and older. Lyrica is a brand-name medication that contains the active drug pregabalin.
This active drug is also available as a generic medication. A generic medication is an exact copy of the active drug in a brand-name medication. The generic is considered to be as safe and effective as the original drug. Generics tend to cost less than brand-name drugs.
They can tell you if it comes in forms and strengths that can be used for your condition. Lyrica can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Lyrica.
These lists do not include all possible side effects. For more information about the possible side effects of Lyrica, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome. Most of these side effects may go away within a few days or a couple of weeks. Call your doctor right away if you have serious side effects. The only condition that Lyrica is approved to treat in children is partial onset seizures in those ages 1 month and older.
In clinical trials , the most common side effects seen in children taking Lyrica were:. You may wonder how often certain side effects occur with this drug. As with most drugs, some people can have an allergic reaction after taking Lyrica. Symptoms of a mild allergic reaction can include:. A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:. Call your doctor right away if you have an allergic reaction to Lyrica, as the reaction could become severe.
Lyrica can cause weight gain in some people. Across clinical studies involving adults with different conditions:. The researchers noted that the risk of weight gain from Lyrica appeared to be related to higher dosages and how long a person took the drug for.
Lyrica may also cause swelling in your feet, hands, and legs, which can contribute to weight gain. Lyrica may cause sleepiness in some people. In clinical trials involving adults with different conditions:. Sleepiness was also reported in clinical trials of children taking Lyrica. Because Lyrica can make you sleepy or dizzy, it can affect your ability to drive or operate machinery. For this reason, you should avoid these and other potentially dangerous activities until you know how Lyrica affects you.
Talk with your doctor about when it may be safe for you to do these activities again. It was noted in clinical studies that some people experienced an increase or decrease in their libido sex drive while taking Lyrica. They can help determine the cause and discuss the best treatment for you. Blurry vision could occur while taking Lyrica. Call your doctor if you experience any changes in your vision while taking Lyrica. Your doctor may decide to monitor your vision more frequently.
Lyrica belongs to a class of medications called antiepileptic drugs AEDs. As with other AEDs, Lyrica may raise your risk for suicidal thoughts and behaviors. Lyrica may also increase your risk for new or worsening depression and other unusual changes in your behavior or mood. But in clinical trials of people taking other AEDs:. If you have new or worsening depression or thoughts of suicide while taking Lyrica, talk with your doctor right away. They may recommend that you switch to a different medication to treat your condition.
Your doctor may also recommend other ways to help lower your suicidal thoughts or behaviors. Regardless of the condition that Lyrica is being used to treat, its manufacturer recommends adjusting the dosage for people with kidney problems. If you have kidney problems, talk with your doctor for more details. Typically, your doctor will start you on a low dosage. Your doctor will ultimately prescribe the smallest dosage that provides the desired effect.
The following information describes dosages that are commonly used or recommended. But be sure to take the dosage your doctor prescribes for you.
The capsules are available in the following strengths:. Lyrica is also available as a liquid solution that you take by mouth. But this form of Lyrica is only available in one strength: 20 mg per milliliter.
The recommended starting dosage for diabetic nerve pain in adults is mg of Lyrica per day. This is taken as 50 mg three times per day. After 1 week, your doctor may increase your dosage to mg three times per day a total of mg per day.
This is the maximum dosage for treating diabetic nerve pain. Your doctor will adjust your dosage as needed based on how well the drug is working for you and any side effects that you may experience. For treating fibromyalgia in adults, the recommended starting dosage of Lyrica is mg per day.
This is taken as 75 mg twice per day. After 1 week, your doctor may increase your dosage to mg twice per day a total of mg per day. Whether or not your dosage is increased will depend on how well the drug is working for you and any side effects that you may experience. This is the maximum dosage for treating fibromyalgia. The recommended starting dosage of Lyrica for adults with nerve pain after shingles is mg per day.
This can be taken as 75 mg twice per day or 50 mg three times per day. After 1 week, your doctor may increase your dosage to one of the two recommended dosages.
Both options equal a total of mg to mg:. After 2 to 4 weeks of taking mg daily, your doctor may increase your dosage to the maximum of mg daily. This can either be taken as mg twice per day or mg three times per day. For treating nerve pain from a spinal cord injury , the recommended starting dosage of Lyrica is mg per day.
This is taken either as 50 mg three times per day or 75 mg twice per day. This is divided into two or three doses per day. For example, if a child weighs 32 kg about 70 pounds [lb] , the recommended starting dosage would be 80 mg total per day.
This could be taken as 40 mg twice daily. It could also be split into three doses per day such as 30 mg in the morning and afternoon, and 20 mg at night. The maximum dosage for children in this weight range is 10 mg per kg of body weight daily, with a maximum of mg per day. This dosage should be divided into two or three doses per day. For example, if a child weighs 20 kg about 44 lb , the recommended starting dosage would be 70 mg total per day.
This could be taken as 35 mg twice per day. It could also be split into three doses per day such as 20 mg in the morning and afternoon, and 10 mg at night. The maximum dosage for children in this weight range is 14 mg per kg of body weight daily.
For children ages 1 month to younger than 4 years, this should be divided into three doses per day. For children ages 4 years and older, this may be divided into two or three doses per day. Then, take your next dose as its regular time. This could raise your risk for side effects. This can include setting an alarm on your phone or downloading a reminder app. A kitchen timer can also work. Lyrica is meant to be used as a long-term treatment. You may wonder how Lyrica compares with other medications that are prescribed for similar uses.
Here, we look at how Lyrica and gabapentin are alike and different. Lyrica belongs to a drug class called antiepileptic drugs AEDs. Lyrica contains the active drug pregabalin. Gabapentin is also an AED.
Gabapentin is approved for use in children ages 3 years and older. But this form of Lyrica is only available in one strength: 20 mg of the drug per milliliter mL of liquid.
Gabapentin comes in three forms: capsules, tablets, and a liquid solution. All are taken by mouth. Gabapentin is available in the following strengths:. Lyrica and gabapentin have some similar side effects and others that vary.
Below are examples of these side effects. These lists contain examples of serious side effects that can occur with either Lyrica or gabapentin, as well as serious side effects that both drugs may share. But studies have found both Lyrica and gabapentin to be effective for nerve pain after shingles and for partial onset seizures.
According to estimates on GoodRx. Lyrica is a brand-name drug. Brand-name medications usually cost more than generics. Gabapentin is a generic drug. Other drugs are available that can treat your condition. Some may be a better fit for you than others. They can tell you about other medications that may work well for you. Note: Some of the drugs listed here are used off-label to treat these specific conditions.
Examples of other drugs that may be used to treat diabetic nerve pain include:. Examples of other drugs that may be used to treat fibromyalgia include:. Error Email field is required. Error Include a valid email address. To provide you with the most relevant and helpful information and to understand which information is beneficial, we may combine your e-mail and website usage information with other information we have about you.
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