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ACTIVE-PAC with Gabapentin
Overview
What is ACTIVE-PAC with Gabapentin?
Gabapentin capsules, USP are supplied as imprinted hard shell capsules containing 100 mg, 300 mg, and 400 mg of gabapentin USP.
The inactive ingredients for the capsules are calcium carbonate, calcium sulfate dihydrate, glyceryl behenate, and pregelatinized starch. The capsule shell contains gelatin, titanium dioxide, sodium lauryl sulfate, yellow iron oxide (300 mg and 400 mg) and red iron oxide (400 mg). The imprinting ink contains shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, strong ammonia solution, black iron oxide, potassium hydroxide, and purified water.
Gabapentin is described as 1-(aminomethyl)cyclohexaneacetic acid with a molecular formula of CHNO and a molecular weight of 171.24. The structural formula of gabapentin is:
Gabapentin is a white to off-white crystalline solid with a pK of 3.7 and a pK of 10.7. It is freely soluble in water and both basic and acidic aqueous solutions. The log of the partition coefficient (n-octanol/0.05M phosphate buffer) at pH 7.4 is -1.25.
What does ACTIVE-PAC with Gabapentin look like?
What are the available doses of ACTIVE-PAC with Gabapentin?
Sorry No records found.
What should I talk to my health care provider before I take ACTIVE-PAC with Gabapentin?
Sorry No records found
How should I use ACTIVE-PAC with Gabapentin?
For temporary relief of pain associated with minor cuts, scrapes and minor skin irritations.
Apply directly to effected area. Do not use more than four times per day.
What interacts with ACTIVE-PAC with Gabapentin?
Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.
What are the warnings of ACTIVE-PAC with Gabapentin?
Array
Suicidal Behavior and Ideation
Antiepileptic drugs (AEDs), including gabapentin, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. Patients treated with any AED for any indication should be monitored for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior.
Pooled analyses of 199 placebo-controlled clinical trials (mono- and adjunctive therapy) of 11 different AEDs showed that patients randomized to one of the AEDs had approximately twice the risk (adjusted Relative Risk 1.8, 95% CI:1.2, 2.7) of suicidal thinking or behavior compared to patients randomized to placebo. In these trials, which had a median treatment duration of 12 weeks, the estimated incidence rate of suicidal behavior or ideation among 27,863 AED-treated patients was 0.43%, compared to 0.24% among 16,029 placebo-treated patients, representing an increase of approximately one case of suicidal thinking or behavior for every 530 patients treated. There were four suicides in drug-treated patients in the trials and none in placebo-treated patients, but the number is too small to allow any conclusion about drug effect on suicide.
The increased risk of suicidal thoughts or behavior with AEDs was observed as early as one week after starting drug treatment with AEDs and persisted for the duration of treatment assessed. Because most trials included in the analysis did not extend beyond 24 weeks, the risk of suicidal thoughts or behavior beyond 24 weeks could not be assessed.
The risk of suicidal thoughts or behavior was generally consistent among drugs in the data analyzed. The finding of increased risk with AEDs of varying mechanisms of action and across a range of indications suggests that the risk applies to all AEDs used for any indication. The risk did not vary substantially by age (5 to 100 years) in the clinical trials analyzed. shows absolute and relative risk by indication for all evaluated AEDs.
The relative risk for suicidal thoughts or behavior was higher in clinical trials for epilepsy than in clinical trials for psychiatric or other conditions, but the absolute risk differences were similar for the epilepsy and psychiatric indications.
Anyone considering prescribing gabapentin or any other AED must balance the risk of suicidal thoughts or behavior with the risk of untreated illness. Epilepsy and many other illnesses for which AEDs are prescribed are themselves associated with morbidity and mortality and an increased risk of suicidal thoughts and behavior. Should suicidal thoughts and behavior emerge during treatment, the prescriber needs to consider whether the emergence of these symptoms in any given patient may be related to the illness being treated.
Patients, their caregivers, and families should be informed that AEDs increase the risk of suicidal thoughts and behavior and should be advised of the need to be alert for the emergence or worsening of the signs and 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.
| Indication | Placebo Patients with Events Per 1000 Patients | Drug Patients with Events Per 1000 Patients | Relative Risk: Incidence of Events in Drug Patients/Incidence in Placebo Patients | Risk Difference: Additional Drug Patients with Events Per 1000 Patients |
|---|---|---|---|---|
| Epilepsy | 1.0 | 3.4 | 3.5 | 2.4 |
| Psychiatric | 5.7 | 8.5 | 1.5 | 2.9 |
| Other | 1.0 | 1.8 | 1.9 | 0.9 |
| Total | 2.4 | 4.3 | 1.8 | 1.9 |
Neuropsychiatric Adverse Events—Pediatric Patients 3 to 12 years of age
Gabapentin use in pediatric patients with epilepsy 3 to 12 years of age is associated with the occurrence of central nervous system related adverse events. The most significant of these can be classified into the following categories: 1) emotional lability (primarily behavioral problems), 2) hostility, including aggressive behaviors, 3) thought disorder, including concentration problems and change in school performance, and 4) hyperkinesia (primarily restlessness and hyperactivity). Among the gabapentin-treated patients, most of the events were mild to moderate in intensity.
In controlled trials in pediatric patients 3 to 12 years of age, the incidence of these adverse events was: emotional lability 6% (gabapentin-treated patients) vs 1.3% (placebo-treated patients); hostility 5.2% vs 1.3%; hyperkinesia 4.7% vs 2.9%; and thought disorder 1.7% vs 0%. One of these events, a report of hostility, was considered serious. Discontinuation of gabapentin treatment occurred in 1.3% of patients reporting emotional lability and hyperkinesia and 0.9% of gabapentin-treated patients reporting hostility and thought disorder. One placebo-treated patient (0.4%) withdrew due to emotional lability.
Withdrawal Precipitated Seizure, Status Epilepticus
Antiepileptic drugs should not be abruptly discontinued because of the possibility of increasing seizure frequency.
In the placebo-controlled studies in patients > 12 years of age, the incidence of status epilepticus in patients receiving gabapentin was 0.6% (3 of 543) versus 0.5% in patients receiving placebo (2 of 378). Among the 2074 patients > 12 years of age treated with gabapentin across all studies (controlled and uncontrolled) 31 (1.5%) had status epilepticus. Of these, 14 patients had no prior history of status epilepticus either before treatment or while on other medications. Because adequate historical data are not available, it is impossible to say whether or not treatment with gabapentin is associated with a higher or lower rate of status epilepticus than would be expected to occur in a similar population not treated with gabapentin.
Tumorigenic Potential
In standard preclinical lifetime carcinogenicity studies, an unexpectedly high incidence of pancreatic acinar adenocarcinomas was identified in male, but not female, rats. (See ). The clinical significance of this finding is unknown. Clinical experience during gabapentin's premarketing development provides no direct means to assess its potential for inducing tumors in humans.
In clinical studies in adjunctive therapy in epilepsy comprising 2085 patient-years of exposure in patients > 12 years of age, new tumors were reported in 10 patients (2 breast, 3 brain, 2 lung, 1 adrenal, 1 non-Hodgkin's lymphoma, 1 endometrial carcinoma ), and preexisting tumors worsened in 11 patients (9 brain, 1 breast, 1 prostate) during or up to 2 years following discontinuation of gabapentin. Without knowledge of the background incidence and recurrence in a similar population not treated with gabapentin, it is impossible to know whether the incidence seen in this cohort is or is not affected by treatment.
Sudden and Unexplained Death in Patients With Epilepsy
During the course of premarketing development of gabapentin 8 sudden and unexplained deaths were recorded among a cohort of 2203 patients treated (2103 patient-years of exposure).
Some of these could represent seizure-related deaths in which the seizure was not observed, e.g., at night. This represents an incidence of 0.0038 deaths per patient-year. Although this rate exceeds that expected in a healthy population matched for age and sex, it is within the range of estimates for the incidence of sudden unexplained deaths in patients with epilepsy not receiving gabapentin (ranging from 0.0005 for the general population of epileptics to 0.003 for a clinical trial population similar to that in the gabapentin program, to 0.005 for patients with refractory epilepsy). Consequently, whether these figures are reassuring or raise further concern depends on comparability of the populations reported upon to the gabapentin cohort and the accuracy of the estimates provided.
What are the precautions of ACTIVE-PAC with Gabapentin?
Information for Patients
Patients should be instructed to take gabapentin only as prescribed.
Patients, their caregivers, and families should be counseled that AEDs, including gabapentin, 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.
Patients should be advised that gabapentin may cause dizziness, somnolence and other symptoms and signs of CNS depression. Accordingly, they should be advised neither to drive a car nor to operate other complex machinery until they have gained sufficient experience on gabapentin to gauge whether or not it affects their mental and/or motor performance adversely.
Patients who require concomitant treatment with morphine may experience increases in gabapentin concentrations. Patients should be carefully observed for signs of CNS depression, such as somnolence, and the dose of gabapentin or morphine should be reduced appropriately (see ).
Patients should be encouraged to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry if they become pregnant. This registry is collecting information about the safety of antiepileptic drugs during pregnancy. To enroll, patients can call the toll free number 1-888-233-2334 (see ).
Laboratory Tests
Clinical trials data do not indicate that routine monitoring of clinical laboratory parameters is necessary for the safe use of gabapentin. The value of monitoring gabapentin blood concentrations has not been established. Gabapentin may be used in combination with other antiepileptic drugs without concern for alteration of the blood concentrations of gabapentin or of other antiepileptic drugs.
Drug Interactions
Phenytoin:
Carbamazepine:
Valproic Acid:
Phenobarbital:
Naproxen:
Hydrocodone:
max
max
Morphine:
PRECAUTIONS
Cimetidine:
Oral Contraceptive:
max
Antacid (Maalox):
*
*
*
Effect of Probenecid:
Drug/Laboratory Tests Interactions
Because false positive readings were reported with the Ames N-Multistix SG dipstick test for urinary protein when gabapentin was added to other antiepileptic drugs, the more specific sulfosalicylic acid precipitation procedure is recommended to determine the presence of urine protein.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Gabapentin was given in the diet to mice at 200, 600, and 2000 mg/kg/day and to rats at 250, 1000, and 2000 mg/kg/day for 2 years. A statistically significant increase in the incidence of pancreatic acinar cell adenomas and carcinomas was found in male rats receiving the high dose; the no-effect dose for the occurrence of carcinomas was 1000 mg/kg/day. Peak plasma concentrations of gabapentin in rats receiving the high dose of 2000 mg/kg were 10 times higher than plasma concentrations in humans receiving 3600 mg per day, and in rats receiving 1000 mg/kg/day peak plasma concentrations were 6.5 times higher than in humans receiving 3600 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 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.
Gabapentin did not demonstrate mutagenic or genotoxic potential in three
and four assays. It was negative in the Ames test and the HGPRT forward mutation assay in Chinese hamster lung cells; it did not produce significant increases in chromosomal aberrations in the Chinese hamster lung cell assay; it was negative in the chromosomal aberration assay and in the micronucleus test in Chinese hamster bone marrow; it was negative in the mouse micronucleus assay; and it did not induce unscheduled DNA synthesis in hepatocytes from rats given gabapentin.
No adverse effects on fertility or reproduction were observed in rats at doses up to 2000 mg/kg (approximately 5 times the maximum recommended human dose on a mg/m basis).
Pregnancy
Pregnancy Category C: Gabapentin has been shown to be fetotoxic in rodents, causing delayed ossification of several bones in the skull, vertebrae, forelimbs, and hindlimbs. These effects occurred when pregnant mice received oral doses of 1000 or 3000 mg/kg/day during the period of organogenesis, or approximately 1 to 4 times the maximum dose of 3600 mg/day given to epileptic patients on a mg/m basis. The no-effect level was 500 mg/kg/day or approximately ½ of the human dose on a mg/m basis.
When rats were dosed prior to and during mating, and throughout gestation, pups from all dose groups (500, 1000 and 2000 mg/kg/day) were affected. These doses are equivalent to less than approximately 1 to 5 times the maximum human dose on a mg/m basis. There was an increased incidence of hydroureter and/or hydronephrosis in rats in a study of fertility and general reproductive performance at 2000 mg/kg/day with no effect at 1000 mg/kg/day, in a teratology study at 1500 mg/kg/day with no effect at 300 mg/kg/day, and in a perinatal and postnatal study at all doses studied (500, 1000 and 2000 mg/kg/day). The doses at which the effects occurred are approximately 1 to 5 times the maximum human dose of 3600 mg/day on a mg/m basis; the no-effect doses were approximately 3 times (Fertility and General Reproductive Performance study) and approximately equal to (Teratogenicity study) the maximum human dose on a mg/m 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 50 times (mice), 30 times (rats), and 25 times (rabbits) the human daily dose on a mg/kg basis, or 4 times (mice), 5 times (rats), or 8 times (rabbits) the human daily dose on a mg/m basis.
In a teratology study in rabbits, an increased incidence of postimplantation fetal loss occurred in dams exposed to 60, 300, and 1500 mg/kg/day, or less than approximately 1/4 to 8 times the maximum human dose on a mg/m basis. There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
To provide information regarding the effects of in utero exposure to gabapentin capsules, physicians are advised to recommend that pregnant patients taking gabapentin capsules enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry. This can be done by calling the toll free number 1-888-233-2334, and must be done by patients themselves. Information on the registry can also be found at the website http://www.aedpregnancyregistry.org/.
Use in Nursing Mothers
Gabapentin is secreted into human milk following oral administration. A nursed infant could be exposed to a maximum dose of approximately 1 mg/kg/day of gabapentin. Because the effect on the nursing infant is unknown, gabapentin should be used in women who are nursing only if the benefits clearly outweigh the risks.
Pediatric Use
Safety and effectiveness of gabapentin in the management of postherpetic neuralgia in pediatric patients have not been established.
Effectiveness as adjunctive therapy in the treatment of partial seizures in pediatric patients below the age of 3 years has not been established (see ).
Geriatric Use
The total number of patients treated with gabapentin in controlled clinical trials in patients with postherpetic neuralgia was 336, of which 102 (30%) were 65 to 74 years of age, and 168 (50%) were 75 years of age and older. There was a larger treatment effect in patients 75 years of age and older compared with younger patients who received the same dosage. Since gabapentin is almost exclusively eliminated by renal excretion, the larger treatment effect observed in patients ≥75 years may be a consequence of increased gabapentin exposure for a given dose that results from an age-related decrease in renal function. However, other factors cannot be excluded. The types and incidence of adverse events were similar across age groups except for peripheral edema and ataxia, which tended to increase in incidence with age.
Clinical studies of gabapentin in epilepsy did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and dose should be adjusted based on creatinine clearance values in these patients (see , , and sections).
What are the side effects of ACTIVE-PAC with Gabapentin?
Postherpetic Neuralgia
The most commonly observed adverse events associated with the use of gabapentin in adults, not seen at an equivalent frequency among placebo-treated patients, were dizziness, somnolence, and peripheral edema.
In the 2 controlled studies in postherpetic neuralgia, 16% of the 336 patients who received gabapentin and 9% of the 227 patients who received placebo discontinued treatment because of an adverse event. The adverse events that most frequently led to withdrawal in gabapentin-treated patients were dizziness, somnolence, and nausea.
Incidence in Controlled Clinical Trials
Table 3
Other events in more than 1% of patients but equally or more frequent in the placebo group included pain, tremor, neuralgia, back pain, dyspepsia, dyspnea, and flu syndrome. There were no clinically important differences between men and women in the types and incidence of adverse events. Because there were few patients whose race was reported as other than white, there are insufficient data to support a statement regarding the distribution of adverse events by race.
| Body System/Preferred Term | Gabapentin N=336 % | PlaceboN=227 % |
|---|---|---|
| Asthenia | 5.7 | 4.8 |
| Infection | 5.1 | 3.5 |
| Headache | 3.3 | 3.1 |
| Accidental injury | 3.3 | 1.3 |
| Abdominal pain | 2.7 | 2.6 |
| Diarrhea | 5.7 | 3.1 |
| Dry mouth | 4.8 | 1.3 |
| Constipation | 3.9 | 1.8 |
| Nausea | 3.9 | 3.1 |
| Vomiting | 3.3 | 1.8 |
| Flatulence | 2.1 | 1.8 |
| Peripheral edema | 8.3 | 2.2 |
| Weight gain | 1.8 | 0.0 |
| Hyperglycemia | 1.2 | 0.4 |
| Dizziness | 28.0 | 7.5 |
| Somnolence | 21.4 | 5.3 |
| Ataxia | 3.3 | 0.0 |
| Thinking abnormal | 2.7 | 0.0 |
| Abnormal gait | 1.5 | 0.0 |
| Incoordination | 1.5 | 0.0 |
| Amnesia | 1.2 | 0.9 |
| Hypesthesia | 1.2 | 0.9 |
| Pharyngitis | 1.2 | 0.4 |
| Rash | 1.2 | 0.9 |
| Amblyopia | 2.7 | 0.9 |
| Conjunctivitis | 1.2 | 0.0 |
| Diplopia | 1.2 | 0.0 |
| Otitis media | 1.2 | 0.0 |
Epilepsy
The most commonly observed adverse events associated with the use of gabapentin in combination with other antiepileptic drugs in patients > 12 years of age, not seen at an equivalent frequency among placebo-treated patients, were somnolence, dizziness, ataxia, fatigue, and nystagmus. The most commonly observed adverse events reported with the use of gabapentin in combination with other antiepileptic drugs in pediatric patients 3 to 12 years of age, not seen at an equal frequency among placebo-treated patients, were viral infection, fever, nausea and/or vomiting, somnolence, and hostility (see ).
Approximately 7% of the 2074 patients > 12 years of age and approximately 7% of the 449 pediatric patients 3 to 12 years of age who received gabapentin in premarketing clinical trials discontinued treatment because of an adverse event. The adverse events most commonly associated with withdrawal in patients > 12 years of age were somnolence (1.2%), ataxia (0.8%), fatigue (0.6%), nausea and/or vomiting (0.6%), and dizziness (0.6%). The adverse events most commonly associated with withdrawal in pediatric patients were emotional lability (1.6%), hostility (1.3%), and hyperkinesia (1.1%).
Incidence in Controlled Clinical Trials
Table 4
The prescriber should be aware that these figures, obtained when gabapentin was added to concurrent antiepileptic drug therapy, cannot be used to predict the frequency of adverse events in the course of usual medical practice where patient characteristics and other factors may differ from those prevailing during clinical studies. Similarly, the cited frequencies cannot be directly compared with figures obtained from other clinical investigations involving different treatments, uses, or investigators. An inspection of these frequencies, however, does provide the prescribing physician with one basis to estimate the relative contribution of drug and nondrug factors to the adverse event incidences in the population studied.
Other events in more than 1% of patients >12 years of age but equally or more frequent in the placebo group included: headache, viral infection, fever, nausea and/or vomiting, abdominal pain, diarrhea, convulsions, confusion, insomnia, emotional lability, rash, acne.
Among the treatment-emergent adverse events occurring at an incidence of at least 10% of gabapentin-treated patients, somnolence and ataxia appeared to exhibit a positive dose-response relationship.
The overall incidence of adverse events and the types of adverse events seen were similar among men and women treated with gabapentin. The incidence of adverse events increased slightly with increasing age in patients treated with either gabapentin or placebo. Because only 3% of patients (28/921) in placebo-controlled studies were identified as nonwhite (black or other), there are insufficient data to support a statement regarding the distribution of adverse events by race.
Table 5
Other events in more than 2% of pediatric patients 3 to 12 years of age but equally or more frequent in the placebo group included: pharyngitis, upper respiratory infection, headache, rhinitis, convulsions, diarrhea, anorexia, coughing, and otitis media.
| Body System/Adverse Event | Gabapentin N=543 % | Placebo N=378 % |
|---|---|---|
| Body As A Whole | ||
| Fatigue | 11.0 | 5.0 |
| Weight Increase | 2.9 | 1.6 |
| Back Pain | 1.8 | 0.5 |
| Peripheral Edema | 1.7 | 0.5 |
| Cardiovascular | ||
| Vasodilatation | 1.1 | 0.3 |
| Digestive System | ||
| Dyspepsia | 2.2 | 0.5 |
| Mouth or Throat Dry | 1.7 | 0.5 |
| Constipation | 1.5 | 0.8 |
| Dental Abnormalities | 1.5 | 0.3 |
| Increased Appetite | 1.1 | 0.8 |
| Hematologic and Lymphatic Systems | ||
| Leukopenia | 1.1 | 0.5 |
| Musculoskeletal System | ||
| Myalgia | 2.0 | 1.9 |
| Fracture | 1.1 | 0.8 |
| Nervous System | ||
| Somnolence | 19.3 | 8.7 |
| Dizziness | 17.1 | 6.9 |
| Ataxia | 12.5 | 5.6 |
| Nystagmus | 8.3 | 4.0 |
| Tremor | 6.8 | 3.2 |
| Nervousness | 2.4 | 1.9 |
| Dysarthria | 2.4 | 0.5 |
| Amnesia | 2.2 | 0.0 |
| Depression | 1.8 | 1.1 |
| Thinking Abnormal | 1.7 | 1.3 |
| Twitching | 1.3 | 0.5 |
| Coordination Abnormal | 1.1 | 0.3 |
| Respiratory System | ||
| Rhinitis | 4.1 | 3.7 |
| Pharyngitis | 2.8 | 1.6 |
| Coughing | 1.8 | 1.3 |
| Skin and Appendages | ||
| Abrasion | 1.3 | 0.0 |
| Pruritus | 1.3 | 0.5 |
| Urogenital System | ||
| Impotence | 1.5 | 1.1 |
| Special Senses | ||
| Diplopia | 5.9 | 1.9 |
| Amblyopia | 4.2 | 1.1 |
| Laboratory Deviations | ||
| WBC Decreased | 1.1 | 0.5 | Body System/Adverse Event | Gabapentin N=119% | Placebo N=128 % |
| Body As A Whole | ||
| Viral Infection | 10.9 | 3.1 |
| Fever | 10.1 | 3.1 |
| Weight Increase | 3.4 | 0.8 |
| Fatigue | 3.4 | 1.6 |
| Digestive System | ||
| Nausea and/or Vomiting | 8.4 | 7.0 |
| Nervous System | ||
| Somnolence | 8.4 | 4.7 |
| Hostility | 7.6 | 2.3 |
| Emotional Lability | 4.2 | 1.6 |
| Dizziness | 2.5 | 1.6 |
| Hyperkinesia | 2.5 | 0.8 |
| Respiratory System | ||
| Bronchitis | 3.4 | 0.8 |
| Respiratory Infection | 2.5 | 0.8 |
Other Adverse Events Observed During All Clinical Trials
Clinical Trials in Adults and Adolescents (Except Clinical Trials in Neuropathic Pain)
Gabapentin has been administered to 4717 patients > 12 years of age during all adjunctive therapy clinical trials (except clinical trials in patients with neuropathic pain), only some of which were placebo-controlled. During these trials, all adverse events were recorded by the clinical investigators using terminology of their own choosing. To provide a meaningful estimate of the proportion of individuals having adverse events, similar types of events were grouped into a smaller number of standardized categories using modified COSTART dictionary terminology. These categories are used in the listing below. The frequencies presented represent the proportion of the 4717 patients > 12 years of age exposed to gabapentin who experienced an event of the type cited on at least one occasion while receiving gabapentin. All reported events are included except those already listed in , those too general to be informative, and those not reasonably associated with the use of the drug.
Events are further classified within body system categories and enumerated in order of decreasing frequency using the following definitions: frequent adverse events are defined as those occurring in at least 1/100 patients; infrequent adverse events are those occurring in 1/100 to 1/1000 patients; rare events are those occurring in fewer than 1/1000 patients.
Body As A Whole:
Frequent:
Infrequent:
Rare:
Cardiovascular System:
Frequent:
Infrequent:
Rare:
Digestive System:
Frequent:
Infrequent:
Rare:
Endocrine System:
Rare:
Hematologic and Lymphatic System:
Frequent:
Infrequent:
Rare:
Musculoskeletal System:
Frequent:
Infrequent:
Rare:
Nervous System:
Frequent:
Infrequent:
Rare:
Respiratory System:
Frequent:
Infrequent:
Rare:
Dermatological:
Infrequent:
Rare:
Urogenital System:
Infrequent:
Rare:
Special Senses:
Frequent:
Infrequent:
Rare:
Clinical trials in Pediatric Patients With Epilepsy
Adverse events occurring during epilepsy clinical trials in 449 pediatric patients 3 to 12 years of age treated with gabapentin that were not reported in adjunctive trials in adults are:
Body as a Whole:
Digestive System:
Hemic and Lymphatic System:
Nervous System:
Psychobiologic Function:
Respiratory System:
Clinical Trials in Adults With Neuropathic Pain of Various Etiologies
Safety information was obtained in 1173 patients during double-blind and open-label clinical trials including neuropathic pain conditions for which efficacy has not been demonstrated. Adverse events reported by investigators were grouped into standardized categories using modified COSTART IV terminology. Listed below are all reported events except those already listed in and those not reasonably associated with the use of the drug.
Events are further classified within body system categories and enumerated in order of decreasing frequency using the following definitions: frequent adverse events are defined as those occurring in at least 1/100 patients; infrequent adverse events are those occurring in 1/100 to 1/1000 patients; rare events are those occurring in fewer than 1/1000 patients.
Body as a Whole:
Infrequent:
Rare:
Cardiovascular System:
Infrequent:
Rare:
Digestive System:
Infrequent:
Rare:
Endocrine System:
Infrequent:
Hemic and Lymphatic System:
Infrequent:
Rare:
Metabolic and Nutritional:
Infrequent:
Rare:
Musculoskeletal:
Infrequent:
Rare:
Nervous System:
Frequent:
Infrequent:
Rare:
Respiratory System:
Infrequent:
Rare:
Skin and Appendages:
Infrequent:
Rare:
Special Senses:
Infrequent:
Rare:
Urogenital System:
Infrequent:
Rare:
Postmarketing and Other Experience
In addition to the adverse experiences reported during clinical testing of gabapentin, the following adverse experiences have been reported in patients receiving 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 hypertrophy, erythema multiforme, elevated liver function tests, fever, hyponatremia, jaundice, movement disorder, Stevens-Johnson syndrome.
Adverse events following the abrupt discontinuation of gabapentin have also been reported. The most frequently reported events were anxiety, insomnia, nausea, pain and sweating.
What should I look out for while using ACTIVE-PAC with Gabapentin?
Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.
What might happen if I take too much ACTIVE-PAC with Gabapentin?
A lethal dose of gabapentin was not identified in mice and rats receiving single oral doses as high as 8000 mg/kg. Signs of acute toxicity in animals included ataxia, labored breathing, ptosis, sedation, hypoactivity, or excitation.
Acute oral overdoses of gabapentin up to 49 grams have been reported. In these cases, double vision, slurred speech, drowsiness, lethargy and diarrhea were observed. All patients recovered with supportive care.
Gabapentin can be removed by hemodialysis. Although hemodialysis has not been performed in the few overdose cases reported, it may be indicated by the patient’s clinical state or in patients with significant renal impairment.
How should I store and handle ACTIVE-PAC with Gabapentin?
Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Protect from light and moisture. [see USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP.Store the unit-dose blister packages in the carton until contents have been used.Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01Gabapentin capsules, USP are supplied as follows:100 mg capsules;White hard gelatin capsules printed with “137” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-137-02 Non Child Resistant Cap NDC 62756-137-03Bottles of 500: Non Child Resistant Cap NDC 62756-137-05Bottles of 1000: Non Child Resistant Cap NDC 62756-137-04Unit dose 50's: NDC 62756-137-01300 mg capsules;Yellow hard gelatin capsules printed with “138” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-138-02 Non Child Resistant Cap NDC 62756-138-03Bottles of 500: Non Child Resistant Cap NDC 62756-138-05Bottles of 1000: Non Child Resistant Cap NDC 62756-138-04Unit dose 50's: NDC 62756-138-01400 mg capsules;Orange hard gelatin capsules printed with “139” on cap and body; available in:Bottles of 100: Child Resistant Cap NDC 62756-139-02 Non Child Resistant Cap NDC 62756-139-03Bottles of 500: Non Child Resistant Cap NDC 62756-139-05Bottles of 1000: Non Child Resistant Cap NDC 62756-139-04Unit dose 50's: NDC 62756-139-01
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
The mechanism 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). In particular, gabapentin prevents pain-related responses in several models of neuropathic pain in rats or mice (e.g. spinal nerve ligation models, streptozocin-induced diabetes model, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formalin test). Gabapentin did not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase, acetic acid abdominal constriction test, footpad heat irradiation test). The relevance of these models to human pain is not known.
The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. Gabapentin exhibits antiseizure activity in mice and rats in both the maximal electroshock and pentylenetetrazole seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). The relevance of these models to human epilepsy is not known.
Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABA or GABA radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. Gabapentin was tested in radioligand binding assays at concentrations up to 100 µM and did not exhibit affinity for a number of other common 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 A 20-alpha-benzoate. Furthermore, gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin.
In vitro
Non-Clinical Toxicology
Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.In vitro
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.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
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Interactions
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