This portion of the website is intended for Healthcare Professionals.

For moderate to severe primary RLS

Move forward with HORIZANT PROdrug technology

HORIZANT provides dose-proportional and extended gabapentin exposure in RLS patients1,2

See how HORIZANT works

Discover the role of PROdrug technology in the mechanism of absorption of HORIZANT

 
how conventional gabapentin is absorbed

How conventional gabapentin is absorbed

Conventional gabapentin is thought to absorb in the upper small intestine via a low-capacity transporter2

This absorption pathway may become saturated, limiting the amount of drug that reaches systemic circulation, making it difficult to find the proper dose, and leading to other pharmacokinetic deficiencies.2,3

How HORIZANT is absorbed

HORIZANT absorbs throughout the entire intestinal tract1,2

The PROdrug technology in HORIZANT conjugates a molecule to gabapentin that is recognized by high-capacity nutrient transporters distributed throughout the intestinal tract, including the small intestine and colon.1,2

This absorption pathway does not become saturated at clinically relevant doses, enabling a greater proportion of the dose of drug to reach systemic circulation.2

As HORIZANT is transported from the intestinal tract into circulation, it is converted by endogenous enzymes in the enterocytes into gabapentin.1,2

To further discusss HORIZANT's absorption, request a Rep visit.

HORIZANT is not interchangeable with other gabapentin products.

The clinical significance of the pharmacokinetic profile of HORIZANT is unknown.

how Horizant is absorbed

HORIZANT has twice the bioavailability of conventional gabapentin

HORIZANT provides dose-proportional and extended exposure2

In a pharmacokinetic study of healthy adults, gabapentin bioavailability from HORIZANT was twice that of conventional gabapentin.2

Horizant vs gabapentin bioavailability

HORIZANT is not interchangeable with other gabapentin products.

Pharmacokinetic Study DesignThe pharmacokinetics of HORIZANT were compared with those of conventional gabapentin in a crossover study of the same healthy adults. Patients (N=12) were randomized to 3 different treatment sequences, each receiving 3 doses: a 626-mg gabapentin-equivalent dose of HORIZANT* with food, a 626-mg gabapentin-equivalent dose of HORIZANT without food, and a 600-mg dose of conventional gabapentin without food. Patients had a 7-day washout period between doses. Data for fasted state is not available as HORIZANT prescribing information states that it should be taken with food.2*The molecular weight of HORIZANT is approximately 2 times that of gabapentin: two 600-mg doses of HORIZANT contain about 626 mg of gabapentin.2

The clinical significance of these results has not been determined.

The absorption of HORIZANT through the entire intestinal tract enables dose-proportional, extended gabapentin exposure*

Approximate equimolar doses in the same healthy adults2

Horizant vs gabapentin absorption through the intestinal tract*HORIZANT data for 626-mg-equivalent dose taken with food; gabapentin data for 600-mg dose taken without food. The molecular weight of HORIZANT is nearly 2 times that of gabapentin: two 600-mg doses of HORIZANT contain approximately 626 mg of gabapentin.2

The clinical significance of these results has not been determined.

target icon

Relief for a range of RLS symptoms

See the Benefits
beaker icon

Get HORIZANT samples and information

Request a Rep Visit

VIEW INDICATION AND FULL IMPORTANT SAFETY INFORMATION

  • Effects on DrivingHORIZANT may cause significant driving impairment. The duration of driving impairment after starting therapy is unknown. Patients should not drive until they have enough experience on HORIZANT to know if it impairs their driving. Patients’ ability to assess their driving competence and degree of somnolence caused by HORIZANT can be imperfect.
  • Somnolence/Sedation and DizzinessHORIZANT causes somnolence/sedation and dizziness. Patients should not drive or operate other complex machinery until they have enough experience on HORIZANT to know if it impairs their ability to perform these tasks.

Important Safety Information for HORIZANT® (gabapentin enacarbil) Extended-Release Tablets

INDICATIONS:

HORIZANT® (gabapentin enacarbil) Extended-Release Tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults. HORIZANT is not recommended for patients who are required to sleep during the daytime and remain awake at night.

HORIZANT® (gabapentin enacarbil) Extended-Release Tablets are indicated for the management of postherpetic neuralgia (PHN) in adults.

IMPORTANT SAFETY INFORMATION

WARNINGS AND PRECAUTIONS

Effects on Driving

HORIZANT may cause significant driving impairment. The duration of driving impairment after starting therapy is unknown. Patients should not drive until they have enough experience on HORIZANT to know if it impairs their driving. Patients’ ability to assess their driving competence and degree of somnolence caused by HORIZANT can be imperfect.

Somnolence/Sedation and Dizziness

HORIZANT causes somnolence/sedation and dizziness. Patients should not drive or operate other complex machinery until they have enough experience on HORIZANT to know if it impairs their ability to perform these tasks.

Lack of Interchangeability With Gabapentin

HORIZANT is not interchangeable with other gabapentin products because of differing pharmacokinetic profiles. The same dose of HORIZANT results in different plasma concentrations of gabapentin relative to other gabapentin products. The safety and effectiveness of HORIZANT in patients with epilepsy have not been studied.

Suicidal Behavior and Ideation

HORIZANT is a prodrug of gabapentin, an antiepileptic drug (AED). AEDs increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. As a prodrug of gabapentin, HORIZANT also increases this risk. 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. Anyone considering prescribing HORIZANT must balance the risk of suicidal thoughts or behavior with the risk of untreated illness.

Patients, caregivers, and families should be informed that HORIZANT increases 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 of self-harm. Behaviors of concern should be reported immediately to healthcare providers.

Drug Reaction With Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity

Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), also known as multiorgan hypersensitivity, has been reported in patients taking antiepileptic drugs, including gabapentin. HORIZANT is a prodrug of gabapentin. Some of these events have been fatal or life-threatening. DRESS typically, although not exclusively, presents with fever, rash, and/or lymphadenopathy, in association with other organ system involvement, such as hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis sometimes resembling an acute viral infection. Eosinophilia is often present. Because this disorder is variable in its expression, other organ systems not noted here may be involved.

It is important to note that early manifestations of hypersensitivity, such as fever or lymphadenopathy, may be present even though rash is not evident. If such signs or symptoms are present, the patient should be evaluated immediately. HORIZANT should be discontinued if an alternative etiology for the signs or symptoms cannot be established.

Discontinuation of HORIZANT

When discontinuing HORIZANT, patients with RLS receiving 600 mg or less once daily can discontinue the drug without tapering. If the recommended dose is exceeded, the dose should be reduced to 600 mg daily for 1 week prior to discontinuation to minimize the potential of withdrawal seizure.

In patients with PHN receiving HORIZANT twice daily, the dose should be reduced to once daily for 1 week prior to discontinuation to minimize the potential of withdrawal seizure.

Tumorigenic Potential

In an oral carcinogenicity study, gabapentin enacarbil increased the incidence of pancreatic acinar cell adenoma and carcinoma in male and female rats. The clinical significance of this finding is unknown.

ADVERSE REACTIONS

The most common adverse reactions for patients with RLS (incidence >10% and at least 2 times the rate of placebo) were somnolence/sedation and dizziness.

The most common adverse reactions for patients with PHN (incidence >10% and greater than placebo) were dizziness, somnolence, and headache.

DRUG INTERACTIONS

Gabapentin enacarbil is released faster from HORIZANT Extended-Release tablets in the presence of alcohol. Consumption of alcohol is not recommended when taking HORIZANT.

HORIZANT taken in conjunction with morphine causes increased somnolence/sedation, dizziness, and nausea.

USE IN SPECIAL POPULATIONS

Pregnancy and Lactation

Pregnancy Category C. There are no adequate and well-controlled studies with HORIZANT in pregnant women. In nonclinical studies in rat and rabbits, administration of gabapentin enacarbil was developmentally toxic when administered to pregnant animals at doses and gabapentin exposures greater than those used clinically. HORIZANT should be used during pregnancy only if potential benefit justifies potential risk to fetus.

It is not known whether gabapentin derived from HORIZANT is secreted in human milk; however, gabapentin is secreted into human milk following oral administration of gabapentin products. Because of the potential for adverse reactions in nursing infants from HORIZANT, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness of HORIZANT in pediatric patients have not been studied.

Geriatric Use

Clinical trials of HORIZANT for the treatment of RLS did not include a sufficient number of patients 65 years and older to determine whether they respond differently from younger individuals. Because elderly patients are more likely to have a decreased renal function, the frequency of dosing may need to be adjusted based on calculated creatinine clearance in these patients.

Renal Impairment

Gabapentin is known to be almost exclusively excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with impaired renal function. The dose of HORIZANT should be adjusted in patients with renal impairment based upon creatinine clearance. HORIZANT is not recommended for treatment of RLS in patients receiving hemodialysis.

For additional safety information, consult the HORIZANT full Prescribing Information here.

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.

This site is intended for US residents only.

HORIZANT is a registered trademark of Arbor Pharmaceuticals, LLC.

© 2018 Arbor Pharmaceuticals, LLC. All rights reserved. July 2018. PP-HOR-US-0287