NEURONTIN^® Indication

NEURONTIN^® is indicated for the treatment of neuropathic pain which includes diabetic pain, post-herpetic neuralgia, and trigeminal neuralgia¹

NEURONTIN^® Mode of Action

The clinical potential of NEURONTIN^® may be attributable to its pharmacological profile, including:

• NEURONTIN^® exerts its effect by central mechanisms¹
• NEURONTIN^® has a high affinity to binding sites related with alpha-2-delta subunits of voltage- gated calcium channels at the level of the spinal cord¹
• NEURONTIN^® exerts its anti-neuralgic effect predominantly by central mechanisms and particularly at spinal cord level¹

NEURONTIN^®: Proven efficacy in patients with neuropathic pain.^1,2

NEURONTIN^®: Proven efficacy in patients with neuropathic pain.^1,2

NEURONTIN® demonstrated significant pain relief in patients with various neuropathic pain syndromes (including post-herpetic neuralgia and painful diabetic neuropathy) vs placebo.^1,2*

Allodynia: Change from baseline¹

>50% reduction in pain: Gabapentin – 23%; Placebo – 15%.

Shooting pain: Change from baseline¹

>50% reduction in pain: Gabapentin – 32%; Placebo – 24%.

Burning Pain: Change from Baseline¹

>50% reduction in pain: Gabapentin – 26%; Placebo – 17%.

Adapted from Serpell M, et al. Pain. 2002

* A double-blind, randomised, placebo-controlled 8-week study was conducted to evaluate the efficacy and safety of gabapentin in the treatment of neuropathic pain, using doses up to 2400 mg/day. The study used a novel design that was symptom- rather than syndrome-based; an approach that aimed to reflect the realities of clinical practice. Participants had a wide range of neuropathic pain syndromes, with at least two of the following symptoms: allodynia, burning pain, shooting pain, or hyperalgesia. Patients were randomised to gabapentin (n=153) or placebo (n=152). Gabapentin was given in three divided doses, initially titrated to 900 mg/day over 3 days, followed by two further increases, to a maximum of 2400 mg/day if required by the end of week 5.

>50% reduction in pain: Gabapentin – 23%; Placebo – 15%.

Hyperalgesia: Change from Baseline¹

NEURONTIN^® provided effective treatment in painful diabetic neuropathy in a randomized, double-blind study compared to placebo.^3*

NEURONTIN^® provided significant reduction in weekly mean pain score in patients with painful diabetic neuropathy in a randomized, double-blind study versus placebo.^3*

Weekly mean pain score as measured on an 11-Point Likert Scale from 0 (no pain) to 10 (worst possible pain).

Adapted from Backonja M, et al. 1998.

NEURONTIN^® improved sleep disturbance due to painful diabetic neuropathy in a randomized, double-blind study vs placebo.^3*

Adapted from Backonja M, et al.1998.

Weekly mean sleep interference scores as rated on a 11-Point Likert scale that described how pain had interfered with the patient’s sleep during the past 24 hours, from 0 (did not interfere) to 10 (unable to sleep due to pain).

*A randomized, double-¬blind, placebo-¬controlled, 8-¬week trial, 165 patients were enrolled who had a 1-¬ to 5-¬year history of pain attributed to diabetic neuropathy and a minimum 40-¬mm pain score on the Short-¬Form McGill Pain Questionnaire visual analogue scale. The primary efficacy measure was daily pain severity as measured on an 11-¬point Likert scale. Secondary measures included sleep interference scores, the Short-¬ Form McGill Pain Questionnaire scores, Patient Global Impression of Change and Clinical Global Impression of Change, the Short Form–36 Quality of Life Questionnaire scores, and the Profile of Mood States results.

NEURONTIN^® Safety & Tolerability

NEURONTIN^® was generally well-tolerated with adverse events being of mild or moderate intensity.^1,2

Adverse effects observed during NEURONTIN^® treatment usually resolve within 3-5 days after treatment onset.1

The most common adverse events with NEURONTIN® include dizziness and somnolence³

Adapted from Backonja M, et al. 1998.

*Data in number (%).²

†Data was calculated using the Fisher exact test.²

Following oral administration, peak plasma gabapentin concentrations are observed within 2 to 3 hours. The elimination half-life of gabapentin is independent of dose and averages 5 to 7 hours.⁴

NEURONTIN^®: Dosing and Administration

The starting dose is 900 mg/day given in three equally divided doses, and increased if necessary, based on response, up to a maximum dose of 3600 mg/day. Therapy should be initiated by titrating the dose¹

* Recommended for adults and adolescents ≥12 years.

NEURONTIN^®: Recommended as a first-line treatment option for peripheral neuropathic pain.^2,3,4

Neurontin main clinical information in patients with neuropathic pain

Neurontin clinical information is on its efficacy in patients with various neuropathic pain syndromes, including pain relief and the improvement of sleep disturbance.^1,2

ABBREVIATED PRESCRIBING INFORMATION

Note: Please refer to the full prescribing information before prescribing

NEURONTIN^®

Content: Gabapentin

Indication: Adjunctive therapy in the treatment of partial seizures with and without secondary generalization in adults and children aged 3 years and older. Treatment of neuropathic pain which includes diabetic pain, post-herpetic neuralgia, and trigeminal neuralgia.

Dosage: Dose reduction, discontinuation, or substitution with an alternative medication should be done gradually over a minimum of 1 week. Epilepsy Adults Effective dosing range of 900 mg/day to 1800 mg/day. Initially 300 mg three times a day on Day 1; or 300 mg once a day on Day 1, 300 mg two times a day on Day 2, and 300 mg three times a day on Day 3. Thereafter, dose can be increased in three equally divided doses up to a maximum of 1800 mg/day. Maximum time between doses in the three times a day schedule should not exceed 12 hours to prevent breakthrough convulsions. Pediatric patients aged 3 to 12 years Starting dose should range from 10 to 15 mg/kg/day given in three equally divided doses, and the effective dose reached by upward titration over a period of approximately 3 days. The effective dose in patients aged 5 years and older is 25 to 35 mg/kg/day given in three equally divided doses and the effective dose in patients aged 3 to less than 5 years is 40 mg/kg/day given in three equally divided doses. Doses up to 50 mg/kg/day have been well tolerated, and the maximum time interval between doses should not exceed 12 hours. Neuropathic pain in adults Starting dose is 900 mg/day given in three equally divided doses, and increased if necessary, based on response, up to a maximum dose of 3600 mg/day. Initiate therapy by taking 300 mg once a day on Day 1, 300 mg two times a day on Day 2, and 300 mg three times a day on Day 3.

Administration: Take orally with or without food.

Contraindications: Hypersensitivity to gabapentin or the product’s components.

Special Precautions: Abrupt withdrawal in epileptic patients may precipitate status epilepticus. Dizziness and somnolence, confusion, loss of consciousness, and mental impairment reported, exercise caution until patient is familiar with the potential effects of the drug. Increased systemic concentration with opioids. Monitor for signs of central nervous system (CNS) depression (eg somnolence, sedation, respiratory depression). Suicidal ideation and behavior reported. Emotional lability (primarily behavioral problems), hostility, thought disorder, and hyperkinesia reported in pediatric patients with epilepsy 3-12 years of age. Severe, life-threatening, systemic hypersensitivity reactions such as drug rash with eosinophilia and systemic symptoms (DRESS) reported. Anaphylaxis reported. Abuse and dependence reported, carefully evaluate patients for a history of drug abuse and monitor for possible signs of abuse. Severe respiratory depression, patients with concomitant use of CNS depressants, compromised respiratory function, respiratory or neurological disease, renal impairment, and the elderly may be at a higher risk. Increased risk of CNS depression and death when concomitantly used with opioids or other CNS depressants. Pregnancy and Lactation, gabapentin crosses the human placenta and is excreted in breast milk. Gabapentin should be used during pregnancy only if the potential benefit to the mother clearly outweighs the potential risk to the fetus. Do not drive a car or operate potentially dangerous machinery until it is known that the medication does not affect ability to engage in these activities.

Adverse reactions: Abdominal pain, back pain, fatigue, fever, headache, viral infection; vasodilation; constipation, dental abnormalities, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea and/or vomiting; leukopenia, decreased White Blood Cells; peripheral edema, increased weight; fracture, myalgia; amnesia, ataxia, confusion, abnormal coordination, depression, dizziness, dysarthria, emotional lability, insomnia, nervousness, nystagmus, somnolence, abnormal thinking, tremor, twitching; coughing, pharyngitis, rhinitis; abrasion, acne, pruritus, rash; amblyopia, diplopia; impotence; asthenia, malaise, facial edema; hypertension; flatulence, anorexia, gingivitis; purpura; arthralgia; vertigo, hyperkinesia; increased, decreased, or absent reflexes; paresthesia, anxiety, hostility; pneumonia, urinary tract infection, visual disturbances, bronchitis, respiratory infection

Drug Interactions: Increased systemic concentration with morphine. Increased risk of central nervous system (CNS) depression and death when concomitantly used with opioids or other CNS depressants. Reduced bioavailability with antacids containing aluminum and magnesium, take gabapentin 2 hours following antacid administration. Slight decrease in renal excretion with cimetidine. False-positive readings with the Ames N-Multistix SG dipstick test. To determine urinary protein, the more specific sulfosalicylic acid precipitation procedure is recommended.

Presentation and Packing: Capsules in blister packs 300 mg x 100’s, 400 mg x 100’s. Capsules in bottles 300 mg x 100’s, 400 mg x 100’s.

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