Gabapentin is an anti-epileptic (anticonvulsant) to treat seizure disorders such as epilepsy and nerve pain (neuropathies). The effect of gabapentin is based on the inhibition of glutamatergic impulse transmission and a blockade of central calcium channels.
Gabapentin – indications
The indication for the use of Gabapentin 300mg is in epilepsy. The substance can be used as adjunctive therapy in partial seizures with or without secondarily generalized seizures in adults and children over 6 years of age.
In addition, gabapentin can be used as monotherapy for partial seizures with or without secondary seizures in adults and adolescents over 12 years of age. Gabapentin can also be used in the treatment of peripheral neuropathic pain associated with painful diabetic neuropathy.
How long it stays in the body?
The bioavailability of gabapentin depends on the dose administered and decreases with increasing dose (0.4 g dose is 25% lower than 0.1 g dose); in the usually recommended doses, it is about 60%. Food does not affect the speed and degree of absorption.
After oral administration, maximum serum concentrations are reached after 3 hours for a single dose or 2 hours for multiple dosing. In the case of administration 3 times/day, the steady-state (i.e., the state in which the rate of drug entry into the body equals the rate of its elimination) is established after 24-48 h and is maintained throughout the treatment period.
Gabapentin is not bound to plasma proteins. The biological half-life is 5-7 h. It is mainly excreted in the urine, which accounts for 80% of the administered dose, and 20% in the feces.
Neurontin can cause several side effects. The most common of these are dizziness and drowsiness (extreme tiredness). It could affect your ability to drive and operate the equipment safely.t
In addition to dizziness and drowsiness, other side effects of Neurontin include:
- Allergic reaction
- Swelling of the feet
- Behavioral changes, especially in children between the ages of 3 and 12.
- Severe side effects
In rare cases, Neurontin causes life-threatening side effects, including:
- Suicidal thinking or behavior
- Sudden and unexplained death due to epilepsy (SUDEP)
Treatment of Neuropathic Pain in adults 18 years of age and older. Efficacy and safety in patients under the age of 18 have not been established.
Hypersensitivity to gabapentin or ancillary components of the drug.
Use as monotherapy for partial seizures in children under 12 years of age.
Use as an additional agent in treating partial seizures with and without secondary generalization in children under the age of 3 years.
Risks due to gabapentin
Gabapentin crosses the placenta. With the use of gabapentin, congenital malformations of the fetus and adverse pregnancy outcomes have been reported; however, there is no adequate report of the use of the drug in lactating or pregnant women and thus cannot conclude anything solid.
In experiments on animals, it showed the toxicity of the drug to the fetus. The potential risk to humans is unknown. Therefore gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus.
Gabapentin – precautions
Gabapentin may increase the frequency of seizures or the emergence of new types of seizures in some patients. There are also difficulties stopping additional anti-epileptic drugs (when therapy is ineffective) and switching to gabapentin monotherapy. There are insufficient data on the safety of gabapentin use for a long time, i.e., over 36 weeks, and its use in people over 65 years of age.
People with renal insufficiency should use drugs with gabapentin with caution. It is often necessary to modify the dose level. Gabapentin should be discontinued when acute pancreatitis develops.
Gabapentin is excreted in breast milk; its effect on a nursing child is unknown; therefore, during breastfeeding, Neurontin® should be prescribed only if it advantages the mother that overcomes the risks.
Influence on Driving
Gabapentin shows little influence while driving or using machines as it affects the central nervous system and can cause sleepiness, day drowsiness, or other similar symptoms. These side effects can be equally harmful even in small amounts in patients who drive or use machines.
In animal studies, no effect of gabapentin on fertility was noted.
Abrupt discontinuation of Gabapentin 300mg or a rapid dose reduction can cause serious side effects. If you have side effects or want to stop or reduce your medication, talk to your doctor first. The consequences of cancellation may include Convulsions, Status epilepticus, Behavioral changes.