Gabapentin (Neurontin)

A GABA analogue.

Potentiates GABA activity indirectly, and partly through its interaction with voltage sensitive calcium channels.

Used to relieve treat seizures, pain, neuropathic pain, postherpetic neuralgia, and hot flashes.

Reduces severity of withdrawal symptoms of opioid analgesics, such as heroin, morphine, oxycodone, and benzodiazepines.

Effective in prevention of frequent migraine headaches, and nystagmus.

Commonly prescribed for chronic pain, mood and anxiety disorders, and sleep problems, in addition to seizure prophylaxis.

Useful for the treatment of alcohol dependence.

Its use prevents heavy drinking and promotes alcohol abstinence among patients with alcohol use disorder and the history of alcohol withdrawal symptoms.

Can help patients with post-operative chronic pain and nerve pain associated with spinal cord injury.

May be effective in reducing pain and spasticity in multiple sclerosis and useful to treating complex regional pain syndrome.

May help deepen sleep, and reducing arousals during the night.

Not effective as a mood-stabilizing treatment for bipolar disorder, anxiety disorders, obsessive-compulsive disorder, depression, weight gain or tinnitus.

Most common side effects include: dizziness, drowsiness, and peripheral edema.

Side effects more common in the elderly and with higher doses.

Children 3–12 years of age are susceptible to mild-to-moderate mood swings, hostility, concentration problems, and hyperactivity.

Should be used carefully in patients with renal impairment due to possible drug accumulation.

Associated with an increased risk of suicidal acts or violent deaths.

Should not be discontinued abruptly after long term use.

Abrupt or over rapid withdrawal may provoke a withdrawal syndrome, and gradual reduction over a period of weeks or months helps minimize such risks.

Side effects upon discontinuation of gabapentin include insomnia, restlessness, agitation, anxiety, disorientation, confusion, light sensitivity, diaphoresis, headaches, palpitations, hypertension, chest pain, seizures, and flu-like symptoms.

Overdoses in individuals can manifest as drowsiness, blurred vision, slurred speech and somnolence or coma.

Approximately 1% of the general population has misused gabapentin for recreation purposes, self medication, or intentional self harm, either alone, or in combination with other substances.

Pregabalin is more potent, absorbs faster and has greater bioavailability.

A gamma-aminobutyric acid agent utilized in neurologic and psychiatric disorders.

Commonly prescribed for neuropathic pain and can be associated with sedation and ataxia.

Oral gabapentin (1200-3600 mg/d for 4-12 weeks) for patients with moderate or severe neuropathic pain from postherpetic neuralgia (PHN) or painful diabetic neuropathy (PDN) is associated with pain reduction of at least 50% in 14% to 17% more patients than placebo.

Has dose dependent exposure because of saturable absorption and high interpatient variability is a result of low capacity nutrient transporters in the small intestine which become saturated, at cinically relevant doses.

As a result of pharmakinetic limitations the drug is delivered multiple times per day to provide therapeutic efficacy.

Does not impair balance.

Effective in the management of hot flashes.

Has few adverse effects at ow to moderate dose, although adverse effects of sedation and dizziness may occur at higher doses.

Does not seem to have drug abuse potential.

There is growing evidence of misuse and overdoses with gabapentin and it is involved in almost 10% of overdose deaths: in almost 90% of fatal overdoses in which gabapentin is detected, opioids are also involved.

Gabapentin encarbil an investigatory prodrug that activley absorbed by high capacity nutrient transporters in the small and large bowel and is converted to gabapentin with less variability among patients and with dose proportional exposure.

The anti-epileptic drugs gabapentin and pregabalin are ligands of the subunits of neuronal voltage gated calcium channels which reduce neuronal excitability.
Gabapentin and pregabalin are recommended for the treatment of neuropathic pain.
Pregabalin is effective in demonstrated in trials of pain from fibromyalgia.
Trials of ineuropathic pain conditions the number of patients needed to be treated to achieve 50% reduction was  7.7 for pregabalin and 7.2 patients for gabapentin.
Post mortem toxicology studies detected gabapentin in almost 1 in 10 US overdose deaths between 2019 in 2020, and about half of the cases, the drug was a cause of death (CDC).
About 90% of the above causes of death involved opioids, primarily illicit fentanyl, and 83% of the deaths occurred among adults age 35 to 54 years.

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