Save up to 80% by drug discount in your pharmacy with "Pharmacy Near Me - National Drug Discount Card"
You can scan QR Code(just open camera on your phone/scan by application) from the image on prescription drug discount card to save it to your mobile phone. Or just click on image if you're on mobile phone.
| Product NDC Code | 68382-607 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Drug Name | Gabapentin |
||||||||
| Type | Generic | ||||||||
| Pharm Class | Decreased Central Nervous System Disorganized Electrical Activity [PE] | ||||||||
| Active Ingredients |
|
||||||||
| Route | ORAL | ||||||||
| Dosage Form | TABLET | ||||||||
| RxCUI drug identifier | 1806380, 1806382 |
||||||||
| Application Number | ANDA203934 | ||||||||
| Labeler Name | Zydus Pharmaceuticals USA Inc. | ||||||||
| Packages |
|
||||||||
| Check if available Online | Get Medication Prices online with Discount |
Drug abuse and dependence
Information about whether the drug is a controlled substance, the types of abuse that can occur with the drug, and adverse reactions pertinent to those types of abuse.9 DRUG ABUSE AND DEPENDENCE The abuse and dependence potential of gabapentin has not been evaluated in human studies.
Overdosage of gabapentin
Information about signs, symptoms, and laboratory findings of acute ovedosage and the general principles of overdose treatment.10 OVERDOSAGE Signs of acute toxicity in animals included ataxia, labored breathing, ptosis, sedation, hypoactivity, or excitation. Acute oral overdoses of gabapentin have been reported. Symptoms include double-vision, tremor, slurred speech, drowsiness, altered mental status, dizziness, lethargy, and diarrhea. Fatal respiratory depression has been reported with gabapentin overdose, alone and in combination with other central nervous system (CNS) depressants. Gabapentin can be removed by hemodialysis. Hemodialysis has been performed in overdose cases reported, and it may be indicated by the patient's clinical state or in patients with significant renal impairment.
Adverse reactions
Information about undesirable effects, reasonably associated with use of the drug, that may occur as part of the pharmacological action of the drug or may be unpredictable in its occurrence. Adverse reactions include those that occur with the drug, and if applicable, with drugs in the same pharmacologically active and chemically related class. There is considerable variation in the listing of adverse reactions. They may be categorized by organ system, by severity of reaction, by frequency, by toxicological mechanism, or by a combination of these.6 ADVERSE REACTIONS The most common adverse reaction (greater than or equal to 5% and twice placebo) is dizziness. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Zydus Pharmaceuticals (USA) Inc. at 1- 877-993-8779 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 359 patients with neuropathic pain associated with postherpetic neuralgia have received gabapentin at doses up to 1,800 mg daily during placebo-controlled clinical studies. In clinical trials in patients with postherpetic neuralgia, 9.7% of the 359 patients treated with gabapentin and 6.9% of 364 patients treated with placebo discontinued prematurely due to adverse reactions. In the gabapentin treatment group, the most common reason for discontinuation due to adverse reactions was dizziness. Of gabapentin-treated patients who experienced adverse reactions in clinical studies, the majority of those adverse reactions were either "mild" or "moderate". Table 4 lists all adverse reactions, regardless of causality, occurring in at least 1% of patients with neuropathic pain associated with postherpetic neuralgia in the gabapentin group for which the incidence was greater than in the placebo group. Table 4 Treatment-Emergent Adverse Reaction Incidence in Controlled Trials in Neuropathic Pain Associated with Postherpetic Neuralgia (Events in at Least 1% of all Gabapentin-Treated Patients and More Frequent Than in the Placebo Group) Body System – Preferred Term Gabapentin N = 359 % Placebo N = 364 % Ear and Labyrinth Disorders Vertigo 1.4 0.5 Gastrointestinal Disorders Diarrhea Dry mouth Constipation Dyspepsia 3.3 2.8 1.4 1.4 2.7 1.4 0.3 0.8 General Disorders Peripheral edema Pain 3.9 1.1 0.3 0.5 Infections and Infestations Nasopharyngitis Urinary tract infection 2.5 1.7 2.2 0.5 Investigations Weight increased 1.9 0.5 Musculoskeletal and Connective Tissue Disorders Pain in extremity Back pain 1.9 1.7 0.5 1.1 Nervous System Disorders Dizziness Somnolence Headache Lethargy 10.9 4.5 4.2 1.1 2.2 2.7 4.1 0.3 In addition to the adverse reactions reported in Table 4 above, the following adverse reactions with an uncertain relationship to gabapentin were reported during the clinical development for the treatment of postherpetic neuralgia. Events in more than 1% of patients but equally or more frequently in the gabapentin-treated patients than in the placebo group included blood pressure increase, confusional state, gastroenteritis viral, herpes zoster, hypertension, joint swelling, memory impairment, nausea, pneumonia, pyrexia, rash, seasonal allergy, and upper respiratory infection. 6.2 Postmarketing and Other Experience with other Formulations of Gabapentin In addition to the adverse experiences reported during clinical testing of gabapentin, the following adverse experiences have been reported in patients receiving other formulations of marketed gabapentin. These adverse experiences have not been listed above and data are insufficient to support an estimate of their incidence or to establish causation. The listing is alphabetized: angioedema, blood glucose fluctuation, breast enlargement, bullous pemphigoid, elevated creatine kinase, elevated liver function tests, erythema multiforme, fever, hyponatremia, jaundice, movement disorder, Stevens-Johnson syndrome. Adverse events following the abrupt discontinuation of gabapentin immediate release have also been reported. The most frequently reported events were anxiety, insomnia, nausea, pain and sweating. There are postmarketing reports of life-threatening or fatal respiratory depression in patients taking gabapentin with opioids or other central nervous system (CNS) depressants, or in the setting of underlying respiratory impairment.
| 1.4 | 0.5 | |
| 3.3 2.8 1.4 1.4 | 2.7 1.4 0.3 0.8 | |
| 3.9 1.1 | 0.3 0.5 | |
| 2.5 1.7 | 2.2 0.5 | |
| 1.9 | 0.5 | |
| 1.9 1.7 | 0.5 1.1 | |
| 10.9 4.5 4.2 1.1 | 2.2 2.7 4.1 0.3 |
gabapentin Drug Interactions
Information about and practical guidance on preventing clinically significant drug/drug and drug/food interactions that may occur in people taking the drug.7 DRUG INTERACTIONS In vitro studies were conducted to investigate the potential of gabapentin to inhibit the major cytochrome P450 enzymes (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4) that mediate drug and xenobiotic metabolism using isoform selective marker substrates and human liver microsomal preparations. Only at the highest concentration tested (171 mcg/mL; 1mM) was a slight degree of inhibition (14% to 30%) of isoform CYP2A6 observed. No inhibition of any of the other isoforms tested was observed at gabapentin concentrations up to 171 mcg/mL (approximately 15 times the C max at 3,600 mg/day). Gabapentin is not appreciably metabolized nor does it interfere with the metabolism of commonly coadministered antiepileptic drugs. The drug interaction data described in this section were obtained from studies involving healthy adults and adult patients with epilepsy. An increase in gabapentin AUC values have been reported when administered with hydrocodone. ( 7.6 ) An increase in gabapentin AUC values have been reported when administered with morphine. ( 7.7 ) An antacid containing aluminum hydroxide and magnesium hydroxide reduced the bioavailability of gabapentin immediate release by about approximately 20%, but by only 5% when gabapentin was taken 2 hours after antacids. It is recommended that gabapentin be taken at least 2 hours following antacid administration. ( 7.10 ) 7.1 Phenytoin In a single (400 mg) and multiple dose (400 mg three times daily) study of gabapentin immediate release in epileptic patients (N=8) maintained on phenytoin monotherapy for at least 2 months, gabapentin had no effect on the steady-state trough plasma concentrations of phenytoin and phenytoin had no effect on gabapentin pharmacokinetics. 7.2 Carbamazepine Steady-state trough plasma carbamazepine and carbamazepine 10, 11 epoxide concentrations were not affected by concomitant gabapentin immediate release (400 mg three times daily; N=12) administration. Likewise, gabapentin pharmacokinetics were unaltered by carbamazepine administration. 7.3 Valproic Acid The mean steady-state trough serum valproic acid concentrations prior to and during concomitant gabapentin immediate release administration (400 mg three times daily; N=17) were not different and neither were gabapentin pharmacokinetic parameters affected by valproic acid. 7.4 Phenobarbital Estimates of steady-state pharmacokinetic parameters for phenobarbital or gabapentin immediate release (300 mg three times daily; N=12) are identical whether the drugs are administered alone or together. 7.5 Naproxen Coadministration of single doses of naproxen (250 mg) and gabapentin immediate release (125 mg) to 18 volunteers increased gabapentin absorption by 12% to 15%. Gabapentin immediate release had no effect on naproxen pharmacokinetics. The doses are lower than the therapeutic doses for both drugs. The effect of coadministration of these drugs at therapeutic doses is not known. 7.6 Hydrocodone Coadministration of gabapentin immediate release (125 mg and 500 mg) and hydrocodone (10 mg) reduced hydrocodone C max by 3% and 21%, respectively, and AUC by 4% and 22%, respectively. The mechanism of this interaction is unknown. Gabapentin AUC values were increased by 14%; the magnitude of the interaction at other doses is not known. 7.7 Morphine When a single dose (60 mg) of controlled-release morphine capsule was administered 2 hours prior to a single dose (600 mg) of gabapentin immediate release in 12 volunteers, mean gabapentin AUC values increased by 44% compared to gabapentin immediate release administered without morphine. The pharmacokinetics of morphine were not affected by administration of gabapentin immediate release 2 hours after morphine. The magnitude of this interaction at other doses is not known. 7.8 Cimetidine Cimetidine 300 mg decreased the apparent oral clearance of gabapentin by 14% and creatinine clearance by 10%. The effect of gabapentin immediate release on cimetidine was not evaluated. This decrease is not expected to be clinically significant. 7.9 Oral Contraceptives Gabapentin immediate release (400 mg three times daily) had no effect on the pharmacokinetics of norethindrone (2.5 mg) or ethinyl estradiol (50 mcg) administered as a single tablet, except that the C max of norethindrone was increased by 13%. This interaction is not considered to be clinically significant. 7.10 Antacid (containing aluminum hydroxide and magnesium hydroxide) An antacid containing aluminum hydroxide and magnesium hydroxide reduced the bioavailability of gabapentin immediate release by about approximately 20%, but by only 5% when gabapentin immediate release was taken 2 hours after the antacid. It is recommended that gabapentin be taken at least 2 hours following the antacid (containing aluminum hydroxide and magnesium hydroxide) administration. 7.11 Probenecid Gabapentin immediate release pharmacokinetic parameters were comparable with and without probenecid, indicating that gabapentin does not undergo renal tubular secretion by the pathway that is blocked by probenecid. 7.12 Drug/Laboratory Test Interactions False positive readings were reported with the Ames-N-Multistix SG ® dipstick test for urine protein when gabapentin was added to other antiepileptic drugs; therefore, the more specific sulfosalicylic acid precipitation procedure is recommended to determine the presence of urine protein.
Clinical pharmacology
Information about the clinical pharmacology and actions of the drug in humans.12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism of action by which gabapentin exerts its analgesic action is unknown but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Gabapentin prevents pain-related responses in several models of neuropathic pain in rats and mice (e.g., spinal nerve ligation models, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formulin test), but does not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase). The relevance of these models to human pain is not known. Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but it does not modify GABA A or GABA B radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. In radioligand binding assays at concentrations up to 100 μM, gabapentin did not exhibit affinity for a number of other receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine; alpha 1, alpha 2, or beta adrenergic; adenosine A1 or A2; cholinergic, muscarinic, or nicotinic; dopamine D1 or D2; histamine H1; serotonin S1 or S2; opiate mu, delta, or kappa; cannabinoid 1; voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem; or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A20-alpha-benzoate. Gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin. In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels. However, functional correlates of gabapentin binding, if any, remain to be elucidated. It is hypothesized that gabapentin antagonizes thrombospondin binding to α2δ-1 as a receptor involved in excitatory synapse formation and suggested that gabapentin may function therapeutically by blocking new synapse formation. 12.2 Pharmacodynamics No pharmacodynamic studies have been conducted with gabapentin. 12.3 Pharmacokinetics Absorption Gabapentin is absorbed from the proximal small bowel by a saturable L-amino transport system. Gabapentin bioavailability is not dose proportional; as the dose is increased, bioavailability decreases. When gabapentin (1,800 mg once daily) and gabapentin immediate release (600 mg three times a day) were administered with high fat meals (50% of calories from fat), gabapentin has a higher C max and lower AUC at steady state compared to gabapentin immediate release (Table 5). Time to reach maximum plasma concentration (T max ) for gabapentin is 8 hours, which is about 4 hours to 6 hours longer compared to gabapentin immediate release. Table 5 Mean ± SD Steady-State Pharmacokinetics for Gabapentin and Gabapentin Immediate Release in Healthy Subjects under high-fat high calorie fed state (Day 5, n = 21) $ T max is presented as median (range); * relative to most recent dose Pharmacokinetic Parameter (Mean ± SD) Gabapentin 1,800 mg QD (3 x 600 mg) Gabapentin Immediate Release 600 mg TID AUC0-24 (μg hr/mL) 132.8 ± 34.7 141.3 ± 29.8 C max (μg/mL) 9.59 ± 2.33 8.54 ± 1.72 C min (μg/mL) 1.84 ± 0.65 2.6 ± 0.78 T max (hr) $ 8 (3 to 12) 2 (1 to 5)* Do not use once-daily gabapentin tablets interchangeably with other gabapentin products because of differing pharmacokinetic profiles that affect frequency of administration. Gabapentin should be taken with evening meals. If it is taken on an empty stomach, the bioavailability will be substantially lower. Administration of gabapentin with food increases the rate and extent of absorption of gabapentin compared to the fasted state. C max of gabapentin increases 33% to 84% and AUC of gabapentin increases 33% to 118% with food depending on the fat content of the meal. Gabapentin should be taken with food . Distribution Gabapentin is less than 3% bound to plasma proteins. After 150 mg intravenous administration, the mean ± SD volume of distribution is 58 ± 6 L. Elimination Gabapentin is eliminated by renal excretion as unchanged drug. In patients with normal renal function given gabapentin immediate release 1,200 to 3,000 mg/day, the drug elimination half-life (t 1/2 ) was 5 hours to 7 hours. Elimination kinetics do not change with dose level or multiple doses. Metabolism Gabapentin is not appreciably metabolized in humans. Excretion Gabapentin elimination rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance. In elderly patients and patients with impaired renal function, plasma clearance is reduced. Gabapentin can be removed from plasma by hemodialysis. Dosage adjustment in patients with compromised renal function is necessary. In patients undergoing hemodialysis, gabapentin should not be administered [see Dosage and Administration ( 2.2 )]. 12.4 Special Populations Renal Insufficiency As renal function decreases, renal and plasma clearances and the apparent elimination rate constant decrease, while C max and t 1/2 increase. In patients (N=60) with creatinine clearance of at least 60, 30 to 59 or less than 30 mL/min, the median renal clearance rates for a 400 mg single dose of gabapentin immediate release were 79, 36 and 11 mL/min, respectively, and the median t 1/2 values were 9.2, 14, and 40 hours, respectively. Dosage adjustment is necessary in patients with impaired renal function [see Dosage and Administration ( 2.2 )]. Hemodialysis In a study in anuric adult subjects (N=11), the apparent elimination half-life of gabapentin on nondialysis days was about 132 hours; during dialysis the apparent half-life of gabapentin was reduced to 3.8 hours. Hemodialysis thus has a significant effect on gabapentin elimination in anuric subjects. Gabapentin should not be administered in patients undergoing hemodialysis. Alternative formulations of gabapentin products should be considered in patients undergoing hemodialysis. Elderly Apparent oral and renal clearances of gabapentin decrease with increasing age, although this may be related to the decline in renal function with age. Reductions in gabapentin dose should be made in patients with age-related compromised renal function [see Dosage and Administration ( 2.2 )]. Hepatic Impairment Because gabapentin is not metabolized, studies have not been conducted in patients with hepatic impairment. Pediatrics The pharmacokinetics of gabapentin have not been studied in patients less than 18 years of age. Gender Although no formal study has been conducted to compare the pharmacokinetics of gabapentin in men and women, it appears that the pharmacokinetic parameters for males and females are similar and there are no significant gender differences. Race Pharmacokinetic differences due to race have not been studied. Because gabapentin is primarily renally excreted and there are no important racial differences in creatinine clearance, pharmacokinetic differences due to race are not expected.
| 132.8 ± 34.7 | 141.3 ± 29.8 | |
| 9.59 ± 2.33 | 8.54 ± 1.72 | |
| 1.84 ± 0.65 | 2.6 ± 0.78 | |
| 8 (3 to 12) | 2 (1 to 5)* | |
Mechanism of action
Information about the established mechanism(s) of the drugÕs action in humans at various levels (for example receptor, membrane, tissue, organ, whole body). If the mechanism of action is not known, this field contains a statement about the lack of information.12.1 Mechanism of Action The mechanism of action by which gabapentin exerts its analgesic action is unknown but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Gabapentin prevents pain-related responses in several models of neuropathic pain in rats and mice (e.g., spinal nerve ligation models, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formulin test), but does not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase). The relevance of these models to human pain is not known. Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but it does not modify GABA A or GABA B radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. In radioligand binding assays at concentrations up to 100 μM, gabapentin did not exhibit affinity for a number of other receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine; alpha 1, alpha 2, or beta adrenergic; adenosine A1 or A2; cholinergic, muscarinic, or nicotinic; dopamine D1 or D2; histamine H1; serotonin S1 or S2; opiate mu, delta, or kappa; cannabinoid 1; voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem; or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A20-alpha-benzoate. Gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin. In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels. However, functional correlates of gabapentin binding, if any, remain to be elucidated. It is hypothesized that gabapentin antagonizes thrombospondin binding to α2δ-1 as a receptor involved in excitatory synapse formation and suggested that gabapentin may function therapeutically by blocking new synapse formation.
Pharmacodynamics
Information about any biochemical or physiologic pharmacologic effects of the drug or active metabolites related to the drugÕs clinical effect in preventing, diagnosing, mitigating, curing, or treating disease, or those related to adverse effects or toxicity.12.2 Pharmacodynamics No pharmacodynamic studies have been conducted with gabapentin.
Pharmacokinetics
Information about the clinically significant pharmacokinetics of a drug or active metabolites, for instance pertinent absorption, distribution, metabolism, and excretion parameters.12.3 Pharmacokinetics Absorption Gabapentin is absorbed from the proximal small bowel by a saturable L-amino transport system. Gabapentin bioavailability is not dose proportional; as the dose is increased, bioavailability decreases. When gabapentin (1,800 mg once daily) and gabapentin immediate release (600 mg three times a day) were administered with high fat meals (50% of calories from fat), gabapentin has a higher C max and lower AUC at steady state compared to gabapentin immediate release (Table 5). Time to reach maximum plasma concentration (T max ) for gabapentin is 8 hours, which is about 4 hours to 6 hours longer compared to gabapentin immediate release. Table 5 Mean ± SD Steady-State Pharmacokinetics for Gabapentin and Gabapentin Immediate Release in Healthy Subjects under high-fat high calorie fed state (Day 5, n = 21) $ T max is presented as median (range); * relative to most recent dose Pharmacokinetic Parameter (Mean ± SD) Gabapentin 1,800 mg QD (3 x 600 mg) Gabapentin Immediate Release 600 mg TID AUC0-24 (μg hr/mL) 132.8 ± 34.7 141.3 ± 29.8 C max (μg/mL) 9.59 ± 2.33 8.54 ± 1.72 C min (μg/mL) 1.84 ± 0.65 2.6 ± 0.78 T max (hr) $ 8 (3 to 12) 2 (1 to 5)* Do not use once-daily gabapentin tablets interchangeably with other gabapentin products because of differing pharmacokinetic profiles that affect frequency of administration. Gabapentin should be taken with evening meals. If it is taken on an empty stomach, the bioavailability will be substantially lower. Administration of gabapentin with food increases the rate and extent of absorption of gabapentin compared to the fasted state. C max of gabapentin increases 33% to 84% and AUC of gabapentin increases 33% to 118% with food depending on the fat content of the meal. Gabapentin should be taken with food . Distribution Gabapentin is less than 3% bound to plasma proteins. After 150 mg intravenous administration, the mean ± SD volume of distribution is 58 ± 6 L. Elimination Gabapentin is eliminated by renal excretion as unchanged drug. In patients with normal renal function given gabapentin immediate release 1,200 to 3,000 mg/day, the drug elimination half-life (t 1/2 ) was 5 hours to 7 hours. Elimination kinetics do not change with dose level or multiple doses. Metabolism Gabapentin is not appreciably metabolized in humans. Excretion Gabapentin elimination rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance. In elderly patients and patients with impaired renal function, plasma clearance is reduced. Gabapentin can be removed from plasma by hemodialysis. Dosage adjustment in patients with compromised renal function is necessary. In patients undergoing hemodialysis, gabapentin should not be administered [see Dosage and Administration ( 2.2 )].
| 132.8 ± 34.7 | 141.3 ± 29.8 | |
| 9.59 ± 2.33 | 8.54 ± 1.72 | |
| 1.84 ± 0.65 | 2.6 ± 0.78 | |
| 8 (3 to 12) | 2 (1 to 5)* | |
Contraindications
Information about situations in which the drug product is contraindicated or should not be used because the risk of use clearly outweighs any possible benefit, including the type and nature of reactions that have been reported.4 CONTRAINDICATIONS Gabapentin tablet is contraindicated in patients with demonstrated hypersensitivity to the drug or its ingredients. Gabapentin tablet is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients. ( 4 )
Description
General information about the drug product, including the proprietary and established name of the drug, the type of dosage form and route of administration to which the label applies, qualitative and quantitative ingredient information, the pharmacologic or therapeutic class of the drug, and the chemical name and structural formula of the drug.11 DESCRIPTION Gabapentin tablet contains gabapentin, a gamma-aminobutyric acid (GABA) analogue, as the active pharmaceutical ingredient. Gabapentin's chemical name is 1-(aminomethyl)cyclohexaneacetic acid; with a molecular formula of C 9 H 17 NO 2 and a molecular weight of 171.24 g/mol. Gabapentin chemical structural formula is: Gabapentin, USP is a white to off-white, crystalline powder with a pKa1 of 3.7 and a pKa2 of 10.7. It is freely soluble in water and in alkaline and acidic solutions. The log of the partition coefficient (n-octanol/ 0.05M phosphate buffer) at pH 7.4 is -1.25. Each gabapentin tablet intended for oral administration contains 300 mg or 600 mg of gabapentin. In addition, each tablet contains the following inactive ingredients: copovidone, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polyethylene oxide, povidone, talc and titanium dioxide. Image
Dosage and administration
Information about the drug product’s dosage and administration recommendations, including starting dose, dose range, titration regimens, and any other clinically sigificant information that affects dosing recommendations.2 DOSAGE AND ADMINISTRATION Gabapentin tablet should be titrated to an 1,800 mg dose taken orally, once-daily with the evening meal. Gabapentin tablets should be swallowed whole. Do not crush, split or chew the tablets. ( 2.1 ) If gabapentin dose is reduced, discontinued, or substituted with an alternative medication, this should be done gradually over a minimum of 1 week or longer (at the discretion of the prescriber). ( 2.1 ) Renal impairment: Dose should be adjusted in patients with reduced renal function. Gabapentin tablet should not be used in patients with CrCl less than 30 or in patients on hemodialysis. ( 2.2 ) 2.1 Postherpetic Neuralgia Once-daily gabapentin tablets are not interchangeable with other gabapentin products. Titrate gabapentin tablet to an 1,800 mg dose taken orally once daily with the evening meal. Gabapentin tablets should be swallowed whole. Do not split, crush, or chew the tablets. If gabapentin dosing is reduced, discontinued, or substituted with an alternative medication, this should be done gradually over a minimum of one week or longer (at the discretion of the prescriber). In adults with postherpetic neuralgia, gabapentin therapy should be initiated and titrated as follows: Table 1 Gabapentin Recommended Titration Schedule Day 1 Day 2 Days 3 to 6 Days 7 to 10 Days 11 to 14 Day 15 Daily Dose 300 mg 600 mg 900 mg 1,200 mg 1,500 mg 1,800 mg 2.2 Patients with Renal Impairment In patients with stable renal function, creatinine clearance (C Cr ) can be reasonably well estimated using the equation of Cockcroft and Gault: For females C Cr =(0.85)(140-age)(weight)/[(72)(S Cr )] For males C Cr =(140-age)(weight)/[(72)(S Cr )] where age is in years, weight is in kilograms and S Cr is serum creatinine in mg/dL. The dose of gabapentin should be adjusted in patients with reduced renal function, according to Table 2. Patients with reduced renal function must initiate gabapentin at a daily dose of 300 mg. Gabapentin should be titrated following the schedule outlined in Table 1. Daily dosing in patients with reduced renal function must be individualized based on tolerability and desired clinical benefit. Table 2 Gabapentin Tablet Dosage Based on Renal Function Once-daily dosing Creatinine Clearance (mL/min) Gabapentin Tablet Dose (once daily with evening meal) ≥ 60 1,800 mg 30 to 60 600 mg to 1,800 mg < 30 Gabapentin tablet should not be administered patients receiving hemodialysis Gabapentin tablet should not be administered
| Daily Dose | 300 mg | 600 mg | 900 mg | 1,200 mg | 1,500 mg | 1,800 mg |
| Creatinine Clearance (mL/min) | Gabapentin Tablet Dose (once daily with evening meal) |
| ≥ 60 | 1,800 mg |
| 30 to 60 | 600 mg to 1,800 mg |
| < 30 | Gabapentin tablet should not be administered |
| patients receiving hemodialysis | Gabapentin tablet should not be administered |
Dosage forms and strengths
Information about all available dosage forms and strengths for the drug product to which the labeling applies. This field may contain descriptions of product appearance.3 DOSAGE FORMS AND STRENGTHS Tablets: 300 mg and 600 mg ( 3 )
Indications and usage
A statement of each of the drug products indications for use, such as for the treatment, prevention, mitigation, cure, or diagnosis of a disease or condition, or of a manifestation of a recognized disease or condition, or for the relief of symptoms associated with a recognized disease or condition. This field may also describe any relevant limitations of use.1 INDICATIONS AND USAGE Gabapentin tablet is indicated for the management of postherpetic neuralgia. Once-daily gabapentin tablets are not interchangeable with other gabapentin products because of differing pharmacokinetic profiles that affect the frequency of administration. Gabapentin tablet is indicated for the management of Postherpetic Neuralgia (PHN). Important Limitation Once-daily gabapentin tablets are not interchangeable with other gabapentin products because of differing pharmacokinetic profiles that affect the frequency of administration (see Warnings and Precautions).
Spl product data elements
Usually a list of ingredients in a drug product.gabapentin gabapentin GABAPENTIN GABAPENTIN CELLULOSE, MICROCRYSTALLINE COPOVIDONE K25-31 HYPROMELLOSE 2208 (100000 MPA.S) HYPROMELLOSE 2910 (6 MPA.S) MAGNESIUM STEARATE POLYETHYLENE GLYCOL 6000 POLYETHYLENE GLYCOL 7000000 POVIDONE K90 TALC TITANIUM DIOXIDE WHITE TO OFF-WHITE 608 gabapentin gabapentin GABAPENTIN GABAPENTIN CELLULOSE, MICROCRYSTALLINE COPOVIDONE K25-31 HYPROMELLOSE 2208 (100000 MPA.S) HYPROMELLOSE 2910 (6 MPA.S) MAGNESIUM STEARATE POLYETHYLENE GLYCOL 6000 POLYETHYLENE GLYCOL 7000000 POVIDONE K90 TALC TITANIUM DIOXIDE WHITE TO OFF-WHITE 607
Carcinogenesis and mutagenesis and impairment of fertility
Information about carcinogenic, mutagenic, or fertility impairment potential revealed by studies in animals. Information from human data about such potential is part of the warnings field.13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Gabapentin was given in the diet to mice at 200, 600, and 2,000 mg/kg/day and to rats at 250, 1,000 and 2,000 mg/kg/day for 2 years. A statistically significant increase in the incidence of pancreatic acinar cell adenoma and carcinomas was found in male rats receiving the high dose; the no-effect dose for the occurrence of carcinomas was 1,000 mg/kg/day. Peak plasma concentrations of gabapentin in rats receiving the high dose of 2,000 mg/kg/day were more than 10 times higher than plasma concentrations in humans receiving 1,800 mg per day and in rats receiving 1,000 mg/kg/day peak plasma concentrations were more than 6.5 times higher than in humans receiving 1,800 mg/day. The pancreatic acinar cell carcinomas did not affect survival, did not metastasize and were not locally invasive. The relevance of this finding to carcinogenic risk in humans is unclear. Studies designed to investigate the mechanism of gabapentin-induced pancreatic carcinogenesis in rats indicate that gabapentin stimulates DNA synthesis in rat pancreatic acinar cells in vitro and, thus, may be acting as a tumor promoter by enhancing mitogenic activity. It is not known whether gabapentin has the ability to increase cell proliferation in other cell types or in other species, including humans. Mutagenesis Gabapentin did not demonstrate mutagenic or genotoxic potential in 3 in vitro and 4 in vivo assays. It was negative in the Ames test and the in vitro HGPRT forward mutation assay in Chinese hamster lung cells; it did not produce significant increases in chromosomal aberrations in the in vitro Chinese hamster lung cell assay; it was negative in the in vivo chromosomal aberration assay and in the in vivo micronucleus test in Chinese hamster bone marrow; it was negative in the in vivo mouse micronucleus assay; and it did not induce unscheduled DNA synthesis in hepatocytes from rats given gabapentin. Impairment of Fertility No adverse effects on fertility or reproduction were observed in rats at doses up to 2,000 mg/kg (approximately 11 times the maximum recommended human dose on an mg/m 2 basis).
Nonclinical toxicology
Information about toxicology in non-human subjects.13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Gabapentin was given in the diet to mice at 200, 600, and 2,000 mg/kg/day and to rats at 250, 1,000 and 2,000 mg/kg/day for 2 years. A statistically significant increase in the incidence of pancreatic acinar cell adenoma and carcinomas was found in male rats receiving the high dose; the no-effect dose for the occurrence of carcinomas was 1,000 mg/kg/day. Peak plasma concentrations of gabapentin in rats receiving the high dose of 2,000 mg/kg/day were more than 10 times higher than plasma concentrations in humans receiving 1,800 mg per day and in rats receiving 1,000 mg/kg/day peak plasma concentrations were more than 6.5 times higher than in humans receiving 1,800 mg/day. The pancreatic acinar cell carcinomas did not affect survival, did not metastasize and were not locally invasive. The relevance of this finding to carcinogenic risk in humans is unclear. Studies designed to investigate the mechanism of gabapentin-induced pancreatic carcinogenesis in rats indicate that gabapentin stimulates DNA synthesis in rat pancreatic acinar cells in vitro and, thus, may be acting as a tumor promoter by enhancing mitogenic activity. It is not known whether gabapentin has the ability to increase cell proliferation in other cell types or in other species, including humans. Mutagenesis Gabapentin did not demonstrate mutagenic or genotoxic potential in 3 in vitro and 4 in vivo assays. It was negative in the Ames test and the in vitro HGPRT forward mutation assay in Chinese hamster lung cells; it did not produce significant increases in chromosomal aberrations in the in vitro Chinese hamster lung cell assay; it was negative in the in vivo chromosomal aberration assay and in the in vivo micronucleus test in Chinese hamster bone marrow; it was negative in the in vivo mouse micronucleus assay; and it did not induce unscheduled DNA synthesis in hepatocytes from rats given gabapentin. Impairment of Fertility No adverse effects on fertility or reproduction were observed in rats at doses up to 2,000 mg/kg (approximately 11 times the maximum recommended human dose on an mg/m 2 basis).
Laboratory tests
Information on laboratory tests helpful in following the patient’s response to the drug or in identifying possible adverse reactions. If appropriate, information may be provided on such factors as the range of normal and abnormal values expected in the particular situation and the recommended frequency with which tests should be performed before, during, and after therapy.5.6 Laboratory Tests Clinical trial data do not indicate that routine monitoring of clinical laboratory procedures is necessary for the safe use of gabapentin. The value of monitoring gabapentin blood concentrations has not been established.
Package label principal display panel
The content of the principal display panel of the product package, usually including the product’s name, dosage forms, and other key information about the drug product.PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Gabapentin Tablets, 300 mg 90 Tablets NDC 68382-608-16 Rx only Zydus Gabapentin Tablets, 600 mg 90 Tablets NDC 68382-607-16 Rx only Zydus 300 mg 600 mg
Spl unclassified section
Information not classified as belonging to one of the other fields. Approximately 40% of labeling with effective_time between June 2009 and August 2014 have information in this field.Manufactured by: Zydus Lifesciences Ltd. Ahmedabad, India. Distributed by: Zydus Pharmaceuticals (USA) Inc. Pennington, NJ 08534 Rev.: 09/23
Manufactured by: Zydus Lifesciences Ltd. Ahmedabad, India. Distributed by: Zydus Pharmaceuticals (USA) Inc. Pennington, NJ 08534 Rev.: 09/23 This Medication Guide has been approved by the U.S. Food and Drug Administration.
gabapentin: Information for patients
Information necessary for patients to use the drug safely and effectively, such as precautions concerning driving or the concomitant use of other substances that may have harmful additive effects.17 PATIENT COUNSELING INFORMATION Advise patients of the availability of a Medication Guide, and instruct them to read the Medication Guide prior to taking gabapentin tablets. Advise patients that once-daily gabapentin tablets are not interchangeable with other formulations of gabapentin. Advise patients to take gabapentin only as prescribed. Gabapentin may cause dizziness, somnolence, and other signs and symptoms of CNS depression. Advise patients not to drive or operate other complex machinery until they have gained sufficient experience on gabapentin to gauge whether or not it adversely affects their mental and/or motor performance. Advise patients who require concomitant treatment with morphine to tell their prescriber if they develop signs of CNS depression such as somnolence. If this occurs the dose of gabapentin or morphine should be reduced accordingly. Advise patients that if they miss a dose of gabapentin to take it with food as soon as they remember. If it is almost time for the next dose, just skip the missed dose and take the next dose at the regular time. Do not take two doses at the same time. Advise patients that if they take too much gabapentin, to call their healthcare provider or poison control center, or go to the nearest emergency room right away. Suicidal Thoughts and Behavior Advise patients, their caregivers, and families that AEDs, including gabapentin, the active ingredient in gabapentin tablet, may increase the risk of suicidal thoughts and behavior and should be advised 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. Behaviors of concern should be reported immediately to healthcare providers [see Warnings and Precautions ( 5.1 )]. Respiratory Depression Inform patients about the risk of respiratory depression. Include information that the risk is greatest for those using concomitant central nervous system (CNS) depressants (such as opioid analgesics) or in those with underlying respiratory impairment. Teach patients how to recognize respiratory depression and advise them to seek medical attention immediately if it occurs [see Warnings and Precautions (5.2)]. Dosing and Administration Gabapentin is not interchangeable with other gabapentin products because of differing pharmacokinetic profiles that affect the frequency of administration. The safety and effectiveness of gabapentin in patients with epilepsy has not been studied. Advise patients that gabapentin should be taken orally once-daily with the evening meal. Gabapentin tablets should be swallowed whole. Do not split, crush, or chew the tablets [see Dosage and Administration (2.1)]. Pregnancy Advise patients to notify their healthcare provider if they become pregnant or intend to become pregnant during treatment with gabapentin tablets. Advise patients that there is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to gabapentin tablets during pregnancy [see Use in Specific Populations (8.1)] . ® is the registered trademark of its owner. Medication Guide available at www.zydususa.com/medguides or call 1-877-993-8779.
Spl medguide
Information about the patient medication guide that accompanies the drug product. Certain drugs must be dispensed with an accompanying medication guide. This field may contain information about when to consult the medication guide and the contents of the medication guide.MEDICATION GUIDE Gabapentin (gab" a pen' tin) Tablets Read this Medication Guide before you start taking gabapentin and each time you get a refill. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or treatment. If you have any questions about gabapentin, ask your healthcare provider or pharmacist. What is the most important information I should know about gabapentin? Do not stop taking gabapentin without first talking with your healthcare provider. Stopping gabapentin suddenly can cause serious problems. Like other antiepileptic drugs, gabapentin, the active ingredient in gabapentin tablet, may cause suicidal thoughts or actions in a very small number of people, about 1 in 500. However, it is not known if gabapentin is safe and effective in people with seizure problems (epilepsy). Therefore, gabapentin tablet should not be used in place of other gabapentin products. Call a healthcare provider right away if you have any of these symptoms, especially if they are new, worse, or worry you: thoughts about suicide or dying attempts to commit suicide serious breathing problems new or worse depression new or worse anxiety feeling agitated or restless panic attacks trouble sleeping (insomnia) new or worse irritability acting aggressive, being angry, or violent acting on dangerous impulses an extreme increase in activity and talking (mania) other unusual changes in behavior or mood How can I watch for early symptoms of suicidal thoughts and actions? Pay attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings. Keep all follow-up visits with your healthcare provider as scheduled. Call your healthcare provider between visits as needed, especially if you are worried about symptoms. Serious breathing problems Serious breathing problems can occur when gabapentin is taken with other medicines that can cause severe sleepiness or decreased awareness, or when it is taken by someone who already has breathing problems. Watch for increased sleepiness or decreased breathing when starting gabapentin or when the dose is increased. Get help right away if breathing problems occur. Do not stop taking gabapentin without first talking with your healthcare provider. Stopping gabapentin suddenly can cause serious problems. What is gabapentin? Gabapentin is a prescription medicine used in adults, 18 years and older, to treat: pain from damaged nerves (neuropathic pain) that follows healing of shingles (a painful rash that comes after a herpes zoster infection). It is not known if gabapentin is safe and effective in people with seizure problems (epilepsy). It is not known if gabapentin is safe and effective in children under 18 years of age with postherpetic pain. Gabapentin tablet is not interchangeable with other gabapentin products. Who should not take gabapentin? Do not take gabapentin tablet if you are allergic to gabapentin or any of the ingredients in gabapentin tablet. See the end of this Medication Guide for a complete list of ingredients in gabapentin tablet. What should I tell my healthcare provider before taking gabapentin? Before taking gabapentin, tell your healthcare provider if you: have or have had depression, mood problems or suicidal thoughts or behavior have breathing problems have seizures have kidney problems or get kidney dialysis are pregnant or plan to become pregnant. It is not known if gabapentin can harm your unborn baby. Tell your healthcare provider right away if you become pregnant while taking gabapentin. You and your healthcare provider will decide if you should take gabapentin while you are pregnant. If you become pregnant while taking gabapentin, talk to your healthcare provider about registering with the North American Antiepileptic Drug (NAAED) Pregnancy Registry. The purpose of this registry is to collect information about the safety of antiepileptic drugs, including gabapentin, the active ingredient in gabapentin tablet, during pregnancy. You can enroll in this registry by calling 1-888-233-2334. are breastfeeding or plan to breastfeed. Gabapentin passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby during treatment with gabapentin. Tell your healthcare provider about all the medicines you take including prescription and non-prescription medicines, vitamins or herbal supplements. Especially tell your healthcare provider if you take any opioid pain medicine (such as oxycodone), or medicines for anxiety (such as lorazepam) or insomnia (such as zolpidem). You may have a higher chance for dizziness, sleepiness or serious breathing problems if these medicines are taken with gabapentin. Taking gabapentin with certain other medicines can cause side effects or affect how well they work. Do not start or stop other medicines without talking to your healthcare provider. Know the medicines you take. Keep a list of them and show it to your healthcare provider and pharmacist when you get a new medicine. How should I take gabapentin? Take gabapentin exactly as prescribed. Your healthcare provider will tell you how much gabapentin to take and when to take it. Take gabapentin at the same time each day. Do not change your dose or stop taking gabapentin without talking with your healthcare provider. If you stop taking gabapentin suddenly, you may experience side effects. Talk with your healthcare provider about how to stop gabapentin slowly. Take gabapentin with food one time each day with your evening meal. Take gabapentin tablets whole. Do not split, crush, or chew gabapentin tablets before swallowing. Your healthcare provider may change your dose of gabapentin. Do not change your dose of gabapentin without talking to your healthcare provider. If you miss a dose, take it as soon as you remember with food. If it is almost time for your next dose, just skip the missed dose. Take the next dose at your regular time. Do not take two doses at the same time. If you take too much gabapentin, call your healthcare provider or poison control center, or go to the nearest emergency room right away. If you are taking an antacid containing aluminum hydroxide and magnesium hydroxide, it is recommended that gabapentin be taken at least 2 hours following administration of the antacid. What should I avoid while taking gabapentin? Do not drink alcohol or take other medicines that make you sleepy or dizzy while taking gabapentin without first talking to your healthcare provider. Taking gabapentin with alcohol or medicines that cause sleepiness or dizziness may make your sleepiness or dizziness worse. Do not operate heavy machines or do other dangerous activities until you know how gabapentin affects you. Gabapentin can slow your thinking and motor skills. What are the possible side effects of gabapentin? The most common side effect of gabapentin is: dizziness Tell your healthcare provider about any side effect that bothers you or that does not go away. These are not all the possible side effects of gabapentin. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. How should I store gabapentin tablets? Store gabapentin tablets at 20°C to 25°C (68°F to 77°F). Gabapentin tablets come in child-resistant bottles of 90's. Keep gabapentin and all medicines out of the reach of children. General information about the safe and effective use of gabapentin Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use gabapentin for a condition for which it was not prescribed. Do not give gabapentin to other people, even if they have the same symptoms you have. It may harm them. This Medication Guide summarizes the most important information about gabapentin. If you would like more information, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about gabapentin that is written for health professionals. Please address all medical inquiries to, [email protected] or Tel.: 1-877-993-8779. What are the ingredients in gabapentin tablet? Active ingredient: gabapentin, USP Inactive ingredients: copovidone, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polyethylene oxide, povidone, talc and titanium dioxide. Medication Guide available at www.zydususa.com/medguides or call 1-877-993-8779.
Clinical studies
This field may contain references to clinical studies in place of detailed discussion in other sections of the labeling.14 CLINICAL STUDIES The efficacy of gabapentin for the management of postherpetic neuralgia was established in a double-blind, placebo-controlled, multicenter study. This study enrolled patients between the age of 21 to 89 with postherpetic neuralgia persisting for at least 6 months following healing of herpes zoster rash and a minimum baseline pain intensity score of at least 4 on an 11-point numerical pain rating scale ranging from 0 (no pain) to 10 (worst possible pain). This 11-week study compared gabapentin 1,800 mg once daily with placebo. A total of 221 and 231 patients were treated with gabapentin or placebo, respectively. The study treatment including titration for all patients comprised a 10-week treatment period followed by 1-week of dose tapering. Double-blind treatment began with titration starting at 300 mg/day and titrated up to a total daily dose of 1,800 mg over 2 weeks, followed by 8 weeks fixed dosing at 1,800 mg once daily, and then 1 week of dose tapering. During the 8-week stable dosing period, patients took 3 active or placebo tablets each night with the evening meal. During baseline and treatment, patients recorded their pain in a daily diary using an 11-point numeric pain rating scale. The mean baseline pain score was 6.6 and 6.5 for gabapentin and placebo-treated patients, respectively. Treatment with gabapentin statistically significantly improved the endpoint mean pain score from baseline. For various degrees of improvement in pain from baseline to study endpoint, Figure 1 shows the fraction of patients achieving that degree of improvement. The figure is cumulative, so that patients whose change from baseline is, for example, 50%, are also included at every level of improvement below 50%. Patients who did not complete the study were assigned 0% improvement. Figure 1: Percent of Patients Achieving Various Levels of Pain Relief Image
Geriatric use
Information about any limitations on any geriatric indications, needs for specific monitoring, hazards associated with use of the drug in the geriatric population.8.5 Geriatric Use The total number of patients treated with gabapentin in controlled clinical trials in patients with postherpetic neuralgia was 359, of which 63% were 65 years of age or older. The types and incidence of adverse events were similar across age groups except for peripheral edema, which tended to increase in incidence with age. Gabapentin is known to be substantially excreted by the kidney. Reductions in gabapentin dose should be made in patients with age-related compromised renal function [see Dosage and Administration ( 2.2 )] .
Nursing mothers
Information about excretion of the drug in human milk and effects on the nursing infant, including pertinent adverse effects observed in animal offspring.8.2 Lactation Risk Summary Gabapentin is present in human milk following oral administration. Adverse effects on the breastfed infant have not been reported. There are no data on the effects of the drug on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for gabapentin and any potential adverse effects on the breastfed infant from gabapentin or from the underlying maternal condition.
Pediatric use
Information about any limitations on any pediatric indications, needs for specific monitoring, hazards associated with use of the drug in any subsets of the pediatric population (such as neonates, infants, children, or adolescents), differences between pediatric and adult responses to the drug, and other information related to the safe and effective pediatric use of the drug.8.4 Pediatric Use The safety and effectiveness of gabapentin in the management of postherpetic neuralgia in patients less than 18 years of age has not been studied.
Pregnancy
Information about effects the drug may have on pregnant women or on a fetus. This field may be ommitted if the drug is not absorbed systemically and the drug is not known to have a potential for indirect harm to the fetus. It may contain information about the established pregnancy category classification for the drug. (That information is nominally listed in the teratogenic_effects field, but may be listed here instead.)8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to gabapentin, including gabapentin, during pregnancy. Encourage women who are taking gabapentin during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling the toll free number 1-888-233-2334 or visiting https://www.aedpregnancyregistry.org/. Risk Summary Available data from published prospective and retrospective cohort studies, and case reports over decades of use with gabapentin during pregnancy have not identified a drug-associated risk of major birth defects. The available data are insufficient to evaluate a drug-associated risk of miscarriage and other maternal or fetal outcomes. In nonclinical studies in mice, rats, and rabbits, gabapentin was developmentally toxic (increased fetal skeletal and visceral abnormalities, and increased embryofetal mortality) when administered to pregnant animals at doses similar to those used clinically (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data When pregnant mice received oral doses of gabapentin (1,000 or 3,000 mg/kg/day, approximately 3 to 8 times the maximum recommended dose of 1,800 mg on a mg/m 2 basis) during the period of organogenesis, embryofetal toxicity (increased incidences of skeletal variations) was observed. The no effect level was 500 mg/kg/day, representing approximately the maximum recommended human dose [MRHD] on a mg/m 2 basis. When rats were dosed prior to and during mating, and throughout gestation, pups from all dose groups (500, 1,000 and 2,000 mg/kg/day) were affected. These doses are equivalent to approximately 3 to 11 times the MRHD on a mg/m 2 basis. There was an increased incidence of hydroureter and/or hydronephrosis in rats in a study of fertility and general reproductive performance at 2,000 mg/kg/day with no effect at 1,000 mg/kg/day, in a teratology study at 1,500 mg/kg/day with no effect at 300 mg/kg/day, and in a perinatal and postnatal study at all doses studied (500, 1,000 and 2,000 mg/kg/day). The doses at which the effects occurred are approximately 3 to 11 times the maximum recommended dose of 1,800 mg on a mg/m 2 basis; the no-effect doses were approximately 5 times (Fertility and General Reproductive Performance study) and approximately equal to (Teratogenicity study) the MRHD on a mg/m 2 basis. Other than hydroureter and hydronephrosis, the etiologies of which are unclear, the incidence of malformations was not increased compared to controls in offspring of mice, rats, or rabbits given doses up to 8 times (mice), 10 times (rats), or 16 times (rabbits) the human daily dose on a mg/m 2 basis. When pregnant rabbits were treated with gabapentin during the period of organogenesis, an increase in embryofetal mortality was observed at 60, 300, and 1,500 mg/kg/day (0.6 to 16 times the MRHD on a mg/m 2 basis). In a published study, gabapentin (400 mg/kg/day) was administered by intraperitoneal injection to neonatal mice during the first postnatal week, a period of synaptogenesis in rodents (corresponding to the last trimester of pregnancy in humans). Gabapentin caused a marked decrease in neuronal synapse formation in brains of intact mice and abnormal neuronal synapse formation in a mouse model of synaptic repair. Gabapentin has been shown in vitro to interfere with activity of the α2δ subunit of voltage-activated calcium channels, a receptor involved in neuronal synaptogenesis. The clinical significance of these findings is unknown.
Use in specific populations
Information about use of the drug by patients in specific populations, including pregnant women and nursing mothers, pediatric patients, and geriatric patients.8 USE IN SPECIFIC POPULATIONS Elderly: Reductions in gabapentin dose should be made in patients with age-related compromised renal function. ( 8.5 ) Renal impairment: Dosage adjustment is necessary for patients with impaired renal function. ( 8.7 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to gabapentin, including gabapentin, during pregnancy. Encourage women who are taking gabapentin during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling the toll free number 1-888-233-2334 or visiting https://www.aedpregnancyregistry.org/. Risk Summary Available data from published prospective and retrospective cohort studies, and case reports over decades of use with gabapentin during pregnancy have not identified a drug-associated risk of major birth defects. The available data are insufficient to evaluate a drug-associated risk of miscarriage and other maternal or fetal outcomes. In nonclinical studies in mice, rats, and rabbits, gabapentin was developmentally toxic (increased fetal skeletal and visceral abnormalities, and increased embryofetal mortality) when administered to pregnant animals at doses similar to those used clinically (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data When pregnant mice received oral doses of gabapentin (1,000 or 3,000 mg/kg/day, approximately 3 to 8 times the maximum recommended dose of 1,800 mg on a mg/m 2 basis) during the period of organogenesis, embryofetal toxicity (increased incidences of skeletal variations) was observed. The no effect level was 500 mg/kg/day, representing approximately the maximum recommended human dose [MRHD] on a mg/m 2 basis. When rats were dosed prior to and during mating, and throughout gestation, pups from all dose groups (500, 1,000 and 2,000 mg/kg/day) were affected. These doses are equivalent to approximately 3 to 11 times the MRHD on a mg/m 2 basis. There was an increased incidence of hydroureter and/or hydronephrosis in rats in a study of fertility and general reproductive performance at 2,000 mg/kg/day with no effect at 1,000 mg/kg/day, in a teratology study at 1,500 mg/kg/day with no effect at 300 mg/kg/day, and in a perinatal and postnatal study at all doses studied (500, 1,000 and 2,000 mg/kg/day). The doses at which the effects occurred are approximately 3 to 11 times the maximum recommended dose of 1,800 mg on a mg/m 2 basis; the no-effect doses were approximately 5 times (Fertility and General Reproductive Performance study) and approximately equal to (Teratogenicity study) the MRHD on a mg/m 2 basis. Other than hydroureter and hydronephrosis, the etiologies of which are unclear, the incidence of malformations was not increased compared to controls in offspring of mice, rats, or rabbits given doses up to 8 times (mice), 10 times (rats), or 16 times (rabbits) the human daily dose on a mg/m 2 basis. When pregnant rabbits were treated with gabapentin during the period of organogenesis, an increase in embryofetal mortality was observed at 60, 300, and 1,500 mg/kg/day (0.6 to 16 times the MRHD on a mg/m 2 basis). In a published study, gabapentin (400 mg/kg/day) was administered by intraperitoneal injection to neonatal mice during the first postnatal week, a period of synaptogenesis in rodents (corresponding to the last trimester of pregnancy in humans). Gabapentin caused a marked decrease in neuronal synapse formation in brains of intact mice and abnormal neuronal synapse formation in a mouse model of synaptic repair. Gabapentin has been shown in vitro to interfere with activity of the α2δ subunit of voltage-activated calcium channels, a receptor involved in neuronal synaptogenesis. The clinical significance of these findings is unknown. 8.2 Lactation Risk Summary Gabapentin is present in human milk following oral administration. Adverse effects on the breastfed infant have not been reported. There are no data on the effects of the drug on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for gabapentin and any potential adverse effects on the breastfed infant from gabapentin or from the underlying maternal condition. 8.4 Pediatric Use The safety and effectiveness of gabapentin in the management of postherpetic neuralgia in patients less than 18 years of age has not been studied. 8.5 Geriatric Use The total number of patients treated with gabapentin in controlled clinical trials in patients with postherpetic neuralgia was 359, of which 63% were 65 years of age or older. The types and incidence of adverse events were similar across age groups except for peripheral edema, which tended to increase in incidence with age. Gabapentin is known to be substantially excreted by the kidney. Reductions in gabapentin dose should be made in patients with age-related compromised renal function [see Dosage and Administration ( 2.2 )] . 8.6 Hepatic Impairment Because gabapentin is not metabolized, studies have not been conducted in patients with hepatic impairment. 8.7 Renal Impairment Gabapentin is known to be substantially excreted by the kidney. Dosage adjustment is necessary in patients with impaired renal function . Gabapentin should not be administered in patients with CrCL between 15 and 30 or in patients undergoing hemodialysis [see Dosage and Administration ( 2.2 )] .
How supplied
Information about the available dosage forms to which the labeling applies, and for which the manufacturer or distributor is responsible. This field ordinarily includes the strength of the dosage form (in metric units), the units in which the dosage form is available for prescribing, appropriate information to facilitate identification of the dosage forms (such as shape, color, coating, scoring, and National Drug Code), and special handling and storage condition information.16 HOW SUPPLIED/STORAGE AND HANDLING Gabapentin Tablets, 300 mg are white to off-white, oval, film-coated tablets debossed with "608" on one side and plain on the other side and are supplied as follows: NDC 68382-608-16 in bottle of 90 tablets with child-resistant closure NDC 68382-608-05 in bottle of 500 tablets NDC 68382-608-77 in unit-dose blister cartons of 100 (10 x 10) unit dose tablets Gabapentin Tablets, 600 mg are white to off-white, oval, beveled edge film coated tablets debossed with "607" on one side and plain on the other side and are supplied as follows: NDC 68382-607-16 in bottle of 90 tablets with child-resistant closure NDC 68382-607-05 in bottle of 500 tablets NDC 68382-607-77 in unit-dose blister cartons of 100 (10 x 10) unit dose tablets Storage Store at 20° C to 25°C (68° F to 77°F); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF) [See USP Controlled Room Temperature]. Keep out of reach of children.
Disclaimer: Do not rely on openFDA or Phanrmacy Near Me to make decisions regarding medical care. While we make every effort to ensure that data is accurate, you should assume all results are unvalidated. Source: OpenFDA, Healthporta Drugs API