Neurontin (Gabapentin). Dosage, Side Effects, Interactions
Gabapentin is an antiepileptic (anticonvulsant) and is used to treat seizure disorders such as epilepsy and nerve pain (neuropathy). The effect of gabapentin is based on inhibition of glutamatergic transmission of excitation and blockade of central calcium channels.
- Adjunctive therapy in adults and children 6 years and older with partial seizures with and without secondary generalization
- Monotherapy in adults and adolescents 12 years and older with partial onset seizures with and without secondary generalization.
- peripheral neuropathic pain
- painful diabetic neuropathy
- postherpetic neuralgia
- Gabapentin is available on the market in the form of hard capsules, film-coated tablets and as an oral solution.
How Neurontin (Gabapentin) works
Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) and prevents the uncontrolled excitation of the nerve cells in the brain and thus increases the seizure threshold. The underlying mechanism has not yet been fully elucidated. Gabapentin probably increases the release of GABA, which inhibits the transmission of stimuli from nerve cell to nerve cell.
- After oral administration, peak plasma concentrations of gabapentin are reached within 2 to 3 hours
- Gabapentin is not bound to plasma proteins
- Gabapentin is not metabolised in humans, nor does the active substance induce enzyme induction of hepatic mixed-function oxidases responsible for drug metabolism
- Gabapentin is eliminated exclusively renally unchanged
- The elimination half-life of gabapentin is dose-independent and averages 5 to 7 hours.
Dosage of Neurontin (Gabapentin)
Long-term therapy is generally necessary for epilepsy . The doctor treating you determines the dosage based on individual tolerability and effectiveness. The total daily dose should be divided into 3 individual doses. In order to avoid the occurrence of recurrences, the interval between 2 consecutive doses should not be greater than 12 hours.
Adults and youth 12 years and older
The effective dose is between 900 and 3,600 mg/day. Treatment can be initiated by dose escalation (Day 1: 300 mg once daily, Day 2: 300 mg twice daily, Day 3: 300 mg three times daily) or with 3 divided doses of 300 mg each on Day 1. Depending on patient response and individual tolerability, the daily dose can then be increased in 300 mg increments every 2 to 3 days up to a maximum dose of 3,600 mg gabapentin per day. Doses up to 4,800 mg/day have been well tolerated in clinical studies.
Children from 6 to 12 years
The starting dose should be 10 to 15 mg/kg/day, the effective dose being achieved by escalating over a period of about 3 days. The effective dose of gabapentin in children (6 to 12 years) is 25 to 35 mg/kg/day, while doses up to 50 mg/kg/day have been shown to be well tolerated in a long-term clinical study.
Peripheral neuropathic pain
Treatment can be initiated by up-titration (Day 1: 300 mg once daily, Day 2: 300 mg twice daily, Day 3: 300 mg three times daily). Alternatively, the starting dose can be 900 mg/day in 3 equal divided doses. Thereafter, depending on patient response and individual tolerability, the daily dose can be increased in 300 mg increments every 2 to 3 days up to a maximum dose of 3,600 mg/day. In the treatment of peripheral neuropathic pain, a treatment duration of more than 5 months is not recommended due to the lack of corresponding clinical studies.
Elderly patients (over 65 years)
Dose adjustment may be required in elderly patients due to age-related decline in renal function. Somnolence, peripheral edema, and asthenia may be more common in elderly patients.
Impaired kidney function
Dose adjustment based on creatinine clearance (ml/min) is recommended in patients with renal impairment. Corresponding dosage recommendations can be found in the product information.
Discontinuation of therapy with gabapentin
If gabapentin has to be discontinued, it should be done gradually over at least 1 week, regardless of the indication.
Side effects of Neurontin (Gabapentin)
Very common side effects (≥ 1/10) include:
- Viral infections
- Somnolence, dizziness, ataxia
- Exhaustion, fever
Common side effects (≥1/100 to <1/10) include:
- Pneumonia , respiratory tract infections, urinary tract infections , other infections, otitis media
- Loss of appetite, increased appetite
- Hostility, confusion and emotional lability, depression , anxiety, nervousness, thought disorders
- Seizures, hyperkinesia, dysarthria, amnesia, tremor, insomnia, headache
- Abnormal sensations such as paraesthesia, hypoesthesia, coordination disorders, nystagmus, increased, weakened or absent reflexes
- Visual disorders, such as amblyopia, diplopia
- hypertension , vasodilation
- Dyspnoea, bronchitis, pharyngitis, cough, rhinitis
- Vomiting, nausea, dental abnormalities, gingivitis, diarrhea, abdominal pain, dyspepsia, constipation, dry mouth and throat, flatulence
- Facial oedema, purpura (most commonly described as bruising secondary to physical trauma), rash, pruritus, acne
- Arthralgia, myalgia, back pain, muscle twitching
- peripheral and generalized edema, abnormal gait, asthenia, pain, malaise, influenza syndrome
- decreased number of white blood cells
- weight gain
- accidental injuries, broken bones, abrasions
- Morphine ► AUC of gabapentin increased
- Antacids containing magnesium or aluminum ► Reduced bioavailability of gabapentin ► It is therefore recommended to take gabapentin no earlier than 2 hours after taking such an antacid
Hypersensitivity to the active substance
There are no adequate data from the use of gabapentin in pregnant women. Animal studies have shown reproductive toxicity. Gabapentin should not be used during pregnancy unless the potential benefit to the mother clearly outweighs the risk to the foetus.
Gabapentin is excreted in breast milk. Because effects on the breastfed infant cannot be excluded, caution should be exercised when administering gabapentin to nursing mothers.
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