Gabapentin enacarbil
Looking up MedlinePlus…
From MedlinePlus, U.S. National Library of Medicine
Dosing in kidney impairment
Recommended Dosage for Renal Impairment Dosing of HORIZANT is adjusted in accordance with renal function, as represented by creatinine clearance [see Clinical Pharmacology ] . Target dose regimens are listed in Table 1 and Table 2. [See table below.] [See table below.] 300 mg every other day in AM. Increase to 300 mg once daily in AM if needed None <15 on hemodialysis None 300 mg following every dialysis.
Increase to 600 mg following every dialysis if needed None In patients with stable renal function, CrCl can be estimated using the equation of Cockcroft and Gault: for males: CrCl = (140-age)(weight)/[(SCr)] for females: CrCl =(140-age)(weight)/[(SCr)] where age is in years, weight is in kilograms, and SCr is serum creatinine in mg/dL.
| Creatinine Clearance (mL/min) | Target Dose Regimen |
|---|---|
| ≥60 | 600 mg per day |
| 30 – 59 | Start at 300 mg per day and increase to 600 mg as needed |
| 15 – 29 | 300 mg per day |
| <15 | 300 mg every other day |
| <15 on hemodialysis | Not recommended |
| Creatinine Clearance (mL/min) | Titration | Maintenance | Tapering |
|---|---|---|---|
| ≥60 | 600 mg in AM for 3 days | 600 mg twice daily | 600 mg in AM for 1 week |
| 30 – 59 | 300 mg in AM for 3 days | 300 mg twice daily. Increase to 600 mg twice daily as needed Based on tolerability and efficacy | Reduce current maintenance dose to once daily in AM for 1 week |
| 15 – 29 | 300 mg in AM on Day 1 and Day 3 | 300 mg in AM. Increase to 300 mg twice daily if needed | If taking 300 mg twice daily, reduce to 300 mg once daily in AM for 1 week. If taking 300 mg once daily, no taper needed. |
| <15 | None | 300 mg every other day in AM. Increase to 300 mg once daily in AM if needed | None |
| <15 on hemodialysis | None | 300 mg following every dialysis. Increase to 600 mg following every dialysis if needed | None |
Preparation and administration
Dosage and Administration Overview Tablets should be swallowed whole and should not be cut, crushed, or chewed. Tablets should be taken with food. HORIZANT is not substitutable with other gabapentin products because of differing pharmacokinetic profiles [ see Warnings and Precautions ].
Drug interactions
Check gabapentin enacarbil against a medication listLabel text (1 paragraph)
Gabapentin enacarbil is released faster from HORIZANT Extended-Release tablets in the presence of alcohol. Consumption of alcohol is not recommended when taking HORIZANT [see Clinical Pharmacology (12.3) ] . Morphine: HORIZANT taken in conjunction with morphine causes increased somnolence/sedation, dizziness, and nausea when compared with either drug alone [see Clinical Pharmacology (12.3) ].
Contraindications
None. None. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
E*Likelihood score E*: Unproven but suspected cause of liver injury.
Gabapentin enacarbil is a long acting form of gabapentin that is used for restless leg syndrome and for painful postherpetic neuropathy. Gabapentin enacarbil and gabapentin are associated with a low rate of transient serum enzyme elevations during treatment and with rare instances of clinically apparent liver injury.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of HORIZANT in pregnant women. In nonclinical studies in rats and rabbits, administration of gabapentin enacarbil was developmentally toxic when administered to pregnant animals at doses and gabapentin exposures greater than those used clinically [see Data ] . Postmarketing data suggest that extended gabapentin use with opioids close to delivery may increase the risk of neonatal withdrawal versus opioids alone.
Although there is at least one report of neonatal withdrawal syndrome in an infant exposed to gabapentin alone during pregnancy, there are no comparative epidemiologic studies evaluating this association. Therefore, whether exposure to gabapentin alone late in pregnancy may cause withdrawal signs and symptoms is not known [see Clinical Considerations ]. In the US 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. The background risk of major birth defects and miscarriage for the indicated population is unknown.
Clinical Considerations Fetal/Neonatal Adverse Reactions Neonatal withdrawal syndrome has been reported in newborns exposed to gabapentin in utero for an extended period of time when also exposed to opioids close to delivery. Neonatal withdrawal signs and symptoms reported have included tachypnea, vomiting, diarrhea, hypertonia, irritability, sneezing, poor feeding, hyperactivity, abnormal sleep pattern, and tremor. Reported signs and symptoms that may also be related to withdrawal include tongue thrusting, wandering eye movements while awake, back arching, and continuous extremity movements.
Observe neonates exposed to HORIZANT and opioids for signs and symptoms of neonatal withdrawal and manage accordingly. Data Animal data When pregnant rats were administered gabapentin enacarbil (oral doses of 200, 1,000, or 5,000 mg/kg/day) throughout the period of organogenesis, embryofetal mortality was increased at the 2 highest doses and fetal body weights were decreased at the high dose. The no-effect dose for embryofetal developmental toxicity in rats (200 mg/kg/day) represents approximately 2 times the gabapentin exposure associated with the maximum recommended human dose (MRHD) of 1,200 mg/day gabapentin enacarbil on an area under the curve (AUC) basis.
When pregnant rabbits were administered gabapentin enacarbil (oral doses of 200, 500, or 2,500 mg/kg/day) throughout the period of organogenesis, embryofetal mortality was…
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
Not the price at the counterThese are not what a patient pays at the pharmacy counter. They are what pharmacies, health plans, and government buyers pay, before manufacturer rebates. A patient's cost depends on their insurance (copay, coinsurance, or deductible) or the pharmacy's cash price.