Active-Pac

Drug overview for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol):

Generic name: GABAPENTIN/LIDOCAINE HCL/MENTHOL (gab-uh-PEN-tin)
Drug class: Anticonvulsants
Therapeutic class: Central Nervous System Agents

Gabapentin is an anticonvulsant structurally related to the inhibitory CNS neurotransmitter gamma -aminobutyric acid (GABA); the drug also possesses analgesic activity. Gabapentin enacarbil is a prodrug of gabapentin.

Conventional (immediate-release) preparations of gabapentin are used in the management of seizure disorders. Conventional preparations also may be used in the treatment of postherpetic neuralgia (PHN). Gabapentin also is commercially available as a gastroretentive tablet formulation (Gralise(R)) for once-daily administration in the treatment of PHN.

Because of differences in pharmacokinetic properties, gabapentin gastroretentive tablets are not interchangeable with other gabapentin preparations. Gabapentin enacarbil, a prodrug of gabapentin, is commercially available as an extended-release tablet formulation (Horizant(R)) for once-daily administration in the treatment of PHN or primary restless legs syndrome. Because of differences in pharmacokinetic properties, gabapentin enacarbil extended-release tablets are not interchangeable with other gabapentin preparations.

DRUG IMAGES

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The following indications for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol) have been approved by the FDA:

Indications:
None.

Professional Synonyms:
None.

The following drug interaction information is available for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol):

Contraindicated
Severe
Moderate

There are 0 contraindications.

There are 3 severe interactions. These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.

Drug Interaction	Drug Names
Sodium Oxybate/Agents that May Cause Respiratory Depression SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Oxybate by itself may be associated with severe somnolence or respiratory depression. Concurrent use with other CNS depressants may further increase the risk for respiratory depression or loss of consciousness.(1-3) CLINICAL EFFECTS: Concurrent use of sodium oxybate and sedative hypnotics or alcohol may further increase the risk for profound sedation, respiratory depression, coma, and/or death.(1,2) Fatalities have been reported.(3) PREDISPOSING FACTORS: Based upon FDA evaluation of deaths in patients taking sodium oxybate, risk factors may include: use of multiple drugs which depress the CNS, more rapid than recommended oxybate dose titration, exceeding the maximum recommended oxybate dose, and prescribing for unapproved uses such as fibromyalgia, insomnia or migraine. Note that in oxybate clinical trials for narcolepsy 78% - 85% of patients were also receiving concomitant CNS stimulants.(1-3) PATIENT MANAGEMENT: Avoid use of concomitant opioids, benzodiazepines, sedating antidepressants, sedating antipsychotics, general anesthetics, or muscle relaxants, particularly when predisposing risk factors are present. If combination use is required, dose reduction or discontinuation of one or more CNS depressants should be considered. If short term use of an opioid or general anesthetic is required, consider interruption of sodium oxybate treatment.(1,2) Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. Consider this risk when using concurrently with other agents that may cause CNS depression.(4) Discuss naloxone with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing naloxone to patients prescribed medicines to treat OUD or opioid analgesics (such as those taking CNS depressants) who are at increased risk of opioid overdose and when a patient has household members/close contacts at risk for accidental overdose.(5) DISCUSSION: The FDA evaluated sodium oxybate postmarket fatal adverse event reports from the FDA Adverse Event Reporting System(AERS)and from the manufacturer. Although report documentation was not always optimal or complete, useful information was obtained. Factors which may have contributed to fatal outcome: concomitant use of one or more drugs which depress the CNS, more rapid than recommended oxybate dose titration, exceeding the maximum recommended oxybate dose, and prescribing for unapproved uses such as fibromyalgia, insomnia or migraine. Many deaths occurred in patients with serious psychiatric disorders such as depression and substance abuse. Other concomitant diseases may have also contributed to respiratory and CNS depressant effects of oxybate.(3)	LUMRYZ, LUMRYZ STARTER PACK, SODIUM OXYBATE, XYREM, XYWAV
Gabapentinoids/Opioids (Cough & Cold) SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Opioid-induced reduction in GI motility may increase the absorption of gabapentin and pregabalin.(1) Gabapentin and pregabalin may reverse opioid-induced tolerance of respiratory depression.(2) Concurrent use may result in profound sedation, respiratory depression, coma, and/or death.(3) CLINICAL EFFECTS: Concurrent use of opioids may result in elevated levels of and toxicity from gabapentin and pregabalin, including profound sedation, respiratory depression, coma, and/or death.(1-7) PREDISPOSING FACTORS: Patients who are elderly, are taking other CNS depressants, have decreased renal function, and/or have conditions that reduce lung function (e.g. Chronic Obstructive Pulmonary Disease [COPD]) may be at a higher risk of this interaction. PATIENT MANAGEMENT: Avoid prescribing opioid-including cough medications for patients taking CNS depressants.(8) If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. If starting a gabapentinoid with an opioid analgesic, prescribe a lower initial dose of the gabapentinoid than indicated in the absence of an opioid and titrate based upon clinical response. If an opioid analgesic is indicated in a patient already taking a gabapentinoid, prescribe a lower dose of the opioid and titrate based upon clinical response.(1) Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. Consider this risk when using concurrently with other agents that may cause CNS depression.(9) Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.(1) DISCUSSION: In a study in 12 healthy males, administration of a single dose of morphine (60 mg sustained release) increased the area-under-curve (AUC) of a single dose of gabapentin (600 mg) by 44%.(1,3,4) There were no affects on the pharmacokinetics of morphine.(1,3,4) The combination of gabapentin plus morphine increased pain tolerance over the combination of morphine plus placebo. Side effects were not significantly different between morphine plus placebo and morphine plus gabapentin.(1) A retrospective, case-control study of opioid users in Ontario, Canada between August 1, 1997 and December 31, 2013 who died of an opioid-related cause matched cases to up to 4 controls who also used opioids. Use of gabapentin in the 120 days prior to death resulted in a significant increase in odds of opioid-related death (OR 1.99, CI=1.61-2.47, p<0.001), compared to opioid use alone. Use of moderate dose (900 mg to 1,799 mg daily) or high dose (>= 1,800 mg daily) gabapentin increased the odds of opioid-related death 60% compared to opioid use without gabapentin. Review of gabapentin prescriptions from calendar year 2013 found that 46% of gabapentin users received at least 1 opioid prescription.(3) Among 49 case reports submitted to FDA over a 5 year period (2012-2017), 12 people died from respiratory depression with gabapentinoids. Two randomized, double-blind, placebo-controlled clinical trials in healthy people, three observational studies, and several studies in animals were reviewed. A trial showed that using pregabalin alone and using it with an opioid pain reliever can depress breathing function. Three observational studies showed a relationship between gabapentinoids given before surgery and respiratory depression occurring after surgery. Several animal studies also showed that pregabalin plus opioids can depress respiratory function.(7) A retrospective cohort study evaluated the risk of mortality among Medicare beneficiaries aged 65 and older who were taking gabapentin with or without concurrent use of opioids. All-cause mortality in gabapentin users compared to duloxetine users was 12.16 per 1,000 person years vs. 9.94 per 1,000 person years, respectively. Adjusted for covariates, the risk of all-cause mortality among gabapentin users on high-dose opioids was more than double the control group (hazard ratio (HR) 2.03, CI=1.19-3.46).(10)	HYCODAN, HYDROCODONE-CHLORPHENIRAMNE ER, HYDROCODONE-HOMATROPINE MBR, HYDROMET, PROMETHAZINE-CODEINE, TUXARIN ER
Long-acting Bupivacaine/Local Anesthetics SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) CLINICAL EFFECTS: Concurrent or use of local anesthetics with 96 hours of use of long-acting bupivacaine may result in neurologic and cardiovascular toxicity. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also result in methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) PREDISPOSING FACTORS: Use of additional agents that are associated with methemoglobinemia may further increase the risk of methemoglobinemia.(1) Patients who are at increased risk of developing methemoglobinemia include those with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.(1) PATIENT MANAGEMENT: Avoid the use of other local anesthetics within 96 hours following the administration of long-acting bupivacaine. In patients for whom use is required, monitor for neurologic and cardiovascular effects. Also monitor for methemoglobinemia with use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine.(1,2) Non-liposomal bupivacaine may be administered in the same syringe as bupivacaine liposomal or injected immediately before bupivacaine liposomal as long as the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1) DISCUSSION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposome bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally. Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)	BUPIVACAINE LIPOSOME, EXPAREL, XARACOLL, ZYNRELEF

There are 3 moderate interactions. The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.

Drug Interaction	Drug Names
Gabapentin/Aluminum; Magnesium-Containing Compounds SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Aluminum or magnesium containing products may reduce the bioavailability of gabapentin.(1) CLINICAL EFFECTS: Simultaneous administration of aluminum or magnesium containing products and gabapentin may result in decreased absorption of gabapentin by 20% and reduce its clinical effectiveness.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: If the use of both medications is unavoidable, it is recommended that gabapentin be taken at least 2 hours following the administration of aluminum or magnesium containing products.(1) DISCUSSION: In 16 subjects, Maalox reduced the bioavailability of gabapentin by about 20%. The reduction was only 5% when gabapentin was administered 2 hours after the Maalox dose. It is for this reason that the manufacturer of gabapentin recommends that it be taken at least 2 hours after the administration of aluminum or magnesium containing products.(1)	ALUMINUM CHLORIDE, ALUMINUM HYDROXIDE, CHOLINE MAGNESIUM TRISALICYLAT, CLENPIQ, KAOLIN, MAGNESIUM CHLORIDE, MAGNESIUM CITRATE, MAGNESIUM OXIDE, MAGNESIUM SULFATE, SOD SULF-POTASS SULF-MAG SULF, SUFLAVE, SUPREP, SUTAB
Gabapentinoids/Opioids (IR & ER) SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Opioid-induced reduction in GI motility may increase the absorption of gabapentin and pregabalin.(1) Gabapentin and pregabalin may reverse opioid-induced tolerance of respiratory depression.(2) Concurrent use may result in profound sedation, respiratory depression, coma, and/or death.(3) CLINICAL EFFECTS: Concurrent use of opioids may result in elevated levels of and toxicity from gabapentin and pregabalin, including profound sedation, respiratory depression, coma, and/or death.(1-7) PREDISPOSING FACTORS: Patients who are elderly, are taking other CNS depressants, have decreased renal function, and/or have conditions that reduce lung function (e.g. Chronic Obstructive Pulmonary Disease [COPD]) may be at a higher risk of this interaction. PATIENT MANAGEMENT: Limit prescribing opioid analgesics and gabapentinoids to patients for whom alternatives are inadequate.(1) If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. If starting a gabapentinoid with an opioid analgesic, prescribe a lower initial dose of the gabapentinoid than indicated in the absence of an opioid and titrate based upon clinical response. If an opioid analgesic is indicated in a patient already taking a gabapentinoid, prescribe a lower dose of the opioid and titrate based upon clinical response.(1) Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. Consider this risk when using concurrently with other agents that may cause CNS depression.(8) Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.(1) Discuss naloxone with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing naloxone to patients prescribed medicines to treat OUD or opioid analgesics (such as those taking CNS depressants) who are at increased risk of opioid overdose and when a patient has household members/close contacts at risk for accidental overdose.(9) DISCUSSION: In a study in 12 healthy males, administration of a single dose of morphine (60 mg sustained release) increased the area-under-curve (AUC) of a single dose of gabapentin (600 mg) by 44%.(1,3,4) There were no affects on the pharmacokinetics of morphine.(1,3,4) The combination of gabapentin plus morphine increased pain tolerance over the combination of morphine plus placebo. Side effects were not significantly different between morphine plus placebo and morphine plus gabapentin.(1) A retrospective, case-control study of opioid users in Ontario, Canada between August 1, 1997 and December 31, 2013 who died of an opioid-related cause matched cases to up to 4 controls who also used opioids. Use of gabapentin in the 120 days prior to death resulted in a significant increase in odds of opioid-related death (OR 1.99, CI=1.61-2.47, p<0.001), compared to opioid use alone. Use of moderate dose (900 mg to 1,799 mg daily) or high dose (>= 1,800 mg daily) gabapentin increased the odds of opioid-related death 60% compared to opioid use without gabapentin. Review of gabapentin prescriptions from calendar year 2013 found that 46% of gabapentin users received at least 1 opioid prescription.(3) Among 49 case reports submitted to FDA over a 5 year period (2012-2017), 12 people died from respiratory depression with gabapentinoids. Two randomized, double-blind, placebo-controlled clinical trials in healthy people, three observational studies, and several studies in animals were reviewed. A trial showed that using pregabalin alone and using it with an opioid pain reliever can depress breathing function. Three observational studies showed a relationship between gabapentinoids given before surgery and respiratory depression occurring after surgery. Several animal studies also showed that pregabalin plus opioids can depress respiratory function.(7) A retrospective cohort study evaluated the risk of mortality among Medicare beneficiaries aged 65 and older who were taking gabapentin with or without concurrent use of opioids. All-cause mortality in gabapentin users compared to duloxetine users was 12.16 per 1,000 person years vs. 9.94 per 1,000 person years, respectively. Adjusted for covariates, the risk of all-cause mortality among gabapentin users on high-dose opioids was more than double the control group (hazard ratio (HR) 2.03, CI=1.19-3.46).(10)	ACETAMIN-CAFF-DIHYDROCODEINE, ACETAMINOPHEN-CODEINE, APADAZ, ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, BELBUCA, BELLADONNA-OPIUM, BENZHYDROCODONE-ACETAMINOPHEN, BRIXADI, BUPRENORPHINE, BUPRENORPHINE HCL, BUPRENORPHINE-NALOXONE, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTORPHANOL TARTRATE, BUTRANS, CARISOPRODOL-ASPIRIN-CODEINE, CODEINE PHOSPHATE, CODEINE SULFATE, CONZIP, DEMEROL, DIHYDROCODEINE BITARTRATE, DILAUDID, DIPHENOXYLATE-ATROPINE, DISKETS, DSUVIA, DURAMORPH, ENDOCET, FENTANYL, FENTANYL CITRATE, FENTANYL CITRATE-0.9% NACL, FENTANYL CITRATE-D5W, FENTANYL CITRATE-STERILE WATER, FENTANYL CITRATE-WATER, FENTANYL-BUPIVACAINE-0.9% NACL, FENTANYL-BUPIVACAINE-NACL, FENTANYL-ROPIVACAINE-0.9% NACL, FENTANYL-ROPIVACAINE-NACL, FIORICET WITH CODEINE, HYDROCODONE BITARTRATE, HYDROCODONE BITARTRATE ER, HYDROCODONE-ACETAMINOPHEN, HYDROCODONE-IBUPROFEN, HYDROMORPHONE ER, HYDROMORPHONE HCL, HYDROMORPHONE HCL-0.9% NACL, HYDROMORPHONE HCL-D5W, HYDROMORPHONE HCL-NACL, HYDROMORPHONE HCL-WATER, HYSINGLA ER, INFUMORPH, LEVORPHANOL TARTRATE, LOMOTIL, MEPERIDINE HCL, MEPERIDINE HCL-0.9% NACL, METHADONE HCL, METHADONE HCL-0.9% NACL, METHADONE HCL-NACL, METHADONE INTENSOL, METHADOSE, MITIGO, MORPHINE SULFATE, MORPHINE SULFATE ER, MORPHINE SULFATE-0.9% NACL, MORPHINE SULFATE-NACL, MOTOFEN, MS CONTIN, NALBUPHINE HCL, NALOCET, NUCYNTA, NUCYNTA ER, OLINVYK, OPIUM TINCTURE, OXYCODONE HCL, OXYCODONE HCL ER, OXYCODONE HYDROCHLORIDE, OXYCODONE-ACETAMINOPHEN, OXYCONTIN, OXYMORPHONE HCL, OXYMORPHONE HCL ER, PENTAZOCINE-NALOXONE HCL, PERCOCET, PRIMLEV, PROLATE, QDOLO, REMIFENTANIL HCL, ROXICODONE, ROXYBOND, SUBLOCADE, SUBOXONE, SUFENTANIL CITRATE, TRAMADOL HCL, TRAMADOL HCL ER, TRAMADOL HCL-ACETAMINOPHEN, TREZIX, ULTIVA, XTAMPZA ER, ZUBSOLV
Gabapentinoids/Benzodiazepines SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Concurrent use may result in profound sedation, respiratory depression, coma, and/or death.(1-3) CLINICAL EFFECTS: Concurrent use of benzodiazepines may result in elevated levels of and toxicity from gabapentin and pregabalin, including profound sedation, respiratory depression, coma, and/or death.(1-3) PREDISPOSING FACTORS: Patients who are elderly, are taking other CNS depressants, have decreased renal function, and/or have conditions that reduce lung function (e.g. Chronic Obstructive Pulmonary Disease [COPD]) may be at a higher risk of this interaction. PATIENT MANAGEMENT: Limit prescribing benzodiazepines and gabapentinoids to patients for whom alternatives are inadequate.(1) If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. If starting a gabapentinoid with an benzodiazepine, prescribe a lower initial dose of the gabapentinoid than indicated in the absence of an opioid and titrate based upon clinical response. If a benzodiazepine is indicated (other than an indication of epilepsy) in a patient already taking a gabapentinoid, prescribe a lower dose of the benzodiazepine and titrate based upon clinical response.(1) Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.(1) DISCUSSION: Clinical trials have shown no pharmacokinetic interaction between pregabalin (300 mg BID) and lorazepam (1 mg single dose).(2) Among 49 case reports submitted to FDA over a 5 year period (2012-2017), 12 people died from respiratory depression with gabapentinoids. Two randomized, double-blind, placebo-controlled clinical trials in healthy people, three observational studies, and several studies in animals were reviewed. A trial showed that using pregabalin alone and using it with an opioid pain reliever can depress breathing function. Three observational studies showed a relationship between gabapentinoids given before surgery and respiratory depression occurring after surgery. Several animal studies also showed that pregabalin plus opioids can depress respiratory function. Benzodiazepines are expected to have a similar effect when used with gabapentinoids.(1)	ALPRAZOLAM, ALPRAZOLAM ER, ALPRAZOLAM INTENSOL, ALPRAZOLAM ODT, ALPRAZOLAM XR, ATIVAN, BYFAVO, CHLORDIAZEPOXIDE HCL, CHLORDIAZEPOXIDE-AMITRIPTYLINE, CHLORDIAZEPOXIDE-CLIDINIUM, CLOBAZAM, CLONAZEPAM, CLORAZEPATE DIPOTASSIUM, DIAZEPAM, DORAL, ESTAZOLAM, FLURAZEPAM HCL, HALCION, KLONOPIN, LIBRAX, LORAZEPAM, LORAZEPAM INTENSOL, LOREEV XR, MIDAZOLAM, MIDAZOLAM HCL, MIDAZOLAM HCL-0.8% NACL, MIDAZOLAM HCL-0.9% NACL, MIDAZOLAM HCL-D5W, MIDAZOLAM HCL-NACL, MIDAZOLAM-0.9% NACL, MIDAZOLAM-NACL, MKO (MIDAZOLAM-KETAMINE-ONDAN), NAYZILAM, ONFI, OXAZEPAM, QUAZEPAM, RESTORIL, SYMPAZAN, TEMAZEPAM, TRIAZOLAM, VALIUM, VALTOCO, XANAX, XANAX XR

The following contraindication information is available for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol):

Overview
Contraindicated
Severe
Moderate

Drug contraindication overview.

No enhanced Contraindications information available for this drug.

There are 0 contraindications.

There are 7 severe contraindications. Adequate patient monitoring is recommended for safer drug use.

Severe List
Chronic kidney disease stage 3A (moderate) GFR 45-59 ml/min
Chronic kidney disease stage 3B (moderate) GFR 30-44 ml/min
Chronic kidney disease stage 4 (severe) GFR 15-29 ml/min
Chronic kidney disease stage 5 (failure) GFr<15 ml/min
Chronic obstructive pulmonary disease
Respiratory depression
Suicidal ideation

There are 2 moderate contraindications. Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.

Moderate List
Depression
Kidney disease with likely reduction in glomerular filtration rate (GFr)

The following adverse reaction information is available for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol):

Overview
Severe
Less Severe

Adverse reaction overview.

No enhanced Common Adverse Effects information available for this drug.

There are 41 severe adverse reactions.

More Frequent	Less Frequent
Ataxia Nystagmus	Altered mental status Depression Dermatitis due to topical drug Dyspnea Hostility Memory impairment Mood changes

Rare/Very Rare
Abnormal hepatic function tests Acute cognitive impairment Acute respiratory failure Anaphylaxis Angioedema Bradycardia Bronchospastic pulmonary disease Bullous pemphigoid Cardiac arrhythmia CNS toxicity Cyanosis DRESS syndrome Drug dependence Eosinophilia Erythema multiforme Eyelid edema Headache disorder Hypersensitivity drug reaction Hyponatremia Hypotension Irritability Jaundice Lymphadenopathy Methemoglobinemia Multiple organ failure Respiratory depression Rhabdomyolysis Seizure disorder Stevens-johnson syndrome Suicidal ideation Syncope Unconsciousness

Rare/Very Rare

Abnormal hepatic function tests
Acute cognitive impairment
Acute respiratory failure
Anaphylaxis
Angioedema
Bradycardia
Bronchospastic pulmonary disease
Bullous pemphigoid
Cardiac arrhythmia
CNS toxicity
Cyanosis
DRESS syndrome
Drug dependence
Eosinophilia
Erythema multiforme
Eyelid edema
Headache disorder
Hypersensitivity drug reaction
Hyponatremia
Hypotension
Irritability
Jaundice
Lymphadenopathy
Methemoglobinemia
Multiple organ failure
Respiratory depression
Rhabdomyolysis
Seizure disorder
Stevens-johnson syndrome
Suicidal ideation
Syncope
Unconsciousness

There are 65 less severe adverse reactions.

More Frequent	Less Frequent
Dizziness Drowsy Fatigue Peripheral edema Sedation	Acute bacterial otitis media Back pain Blanching of skin Blurred vision Constipation Cough Diarrhea Diplopia Dry throat Dysarthria Edema Erythema General weakness Hyperkinesis Malaise Nausea Pharyngitis Pruritus of skin Skin rash Stinging of skin Toxic amblyopia Tremor Urticaria Viral infection Vomiting Weight gain Xerostomia

Rare/Very Rare
Accidental fall Acute cognitive impairment Agitation Anorexia Apprehension Behavioral disorders Blurred vision Concentration difficulty Conjunctivitis Dizziness Drowsy Dyspepsia Erectile dysfunction Euphoria Fever Gynecomastia Headache disorder Hyperglycemia Hyperhidrosis Increased creatine kinase level Insomnia Libido changes Muscle fasciculation Nervousness Pain Rhinitis Sensation of cold Sensation of warmth Skin rash Symptoms of anxiety Tinnitus Tremor Vomiting

Rare/Very Rare

Accidental fall
Acute cognitive impairment
Agitation
Anorexia
Apprehension
Behavioral disorders
Blurred vision
Concentration difficulty
Conjunctivitis
Dizziness
Drowsy
Dyspepsia
Erectile dysfunction
Euphoria
Fever
Gynecomastia
Headache disorder
Hyperglycemia
Hyperhidrosis
Increased creatine kinase level
Insomnia
Libido changes
Muscle fasciculation
Nervousness
Pain
Rhinitis
Sensation of cold
Sensation of warmth
Skin rash
Symptoms of anxiety
Tinnitus
Tremor
Vomiting

The following precautions are available for ACTIVE-PAC (gabapentin/lidocaine hcl/menthol):

Pediatric
Pregnant
Lactation
Geriatric

No enhanced Pediatric Use information available for this drug.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

Although there are no adequate and controlled studies to date in pregnant women, gabapentin and gabapentin enacarbil have been shown to cause developmental toxicity when administered to pregnant animals during the period of organogenesis at doses similar to or lower than those used clinically. Such effects include skeletal abnormalities, hydroureter and hydronephrosis, and increased embryofetal mortality. In addition, abnormal or decreased synaptic formation was observed in neonatal mice exposed to intraperitoneal injections of gabapentin during the first postnatal week (corresponding to the last trimester of pregnancy in humans); the clinical importance of these findings is not known.

Gabapentin and gabapentin enacarbil should be used during pregnancy only when the potential benefits justify the possible risks to the fetus. Women who become pregnant while receiving gabapentin should be encouraged to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 888-233-2334; registry information also is available on the website at https://www.aedpregnancyregistry.org.

Gabapentin is distributed into milk following oral administration. Because of the potential for serious adverse reactions to gabapentin in nursing infants, the drug should be administered to nursing women only if the potential benefits justify the risk to the infant. The manufacturer of gabapentin enacarbil states that a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

No enhanced Geriatric Use information available for this drug.