GABAPENTIN (Neurontin): What is used for?

What is Gabapentin?

Gabapentin is an active ingredient used for the treatment of partial epileptic seizures with or without secondary generalization and in neuropathic pain.

The brand names of Gabapentin in United States are: Neurontin, Gralise, Gabarone, Fanatrex.

Gabapentin Mechanism of Action (MOA)

It reduces the release of monoamino neurotransmitters and increases the exchange of GABA in various brain areas.

Therapeutic Indications and Posology of Gabapentin

Oral use.

– In monotherapy or combined, in partial epileptic seizures with or without secondary generalization in adults and children >12 years.
Start, 900 mg/day in 3 doses; maintenance, up to 3,600 mg/day in 3 doses.

– In children ‚Č• 6 years in combined therapy in partial seizures with or without secondary generalization.
Effective dose 25-35 mg/kg/day in 3 doses.

– Peripheral neuropathic pain.
Initial, 900 mg/day in 3 doses; maintenance, max. 3,600 mg/day in 3 doses.

Renal insufficiency: daily dose (in 3 doses) of: 600-1,800 mg if Clcr = 50-79 ml/min; 300-900 mg if Clcr = 30-49 ml/min; 150*-600 mg if Clcr= 15-29 ml/min; 150*-300 mg if Clcr < 15 ml/min.
Note: * = Administer 300 mg/48 h.

Haemodialysis: loading dose 300-400 mg followed by 200-300 mg after each 4 h of haemodialysis.

Mode of administration 

Oral use.
Administer with or without food and swallow whole with sufficient intake of liquid (a glass of water).

Contraindications of Gabapentin

Hypersensitivity.

Warnings and precautions with Gabapentin

  • Kidney failure.
  • Elderly.
  • Mixed crises including absences.
  • Gradually stop treatment in at least one week.
  • Assess the benefit/risk of prolonged therapy in children and adolescents.
  • Possibility of suicidal thoughts and behaviors.
  • Stop if you develop acute pancreatitis.
  • Risk of drug eruption with eosinophilia and systemic symptoms (s. DRESS), if fever or lymphadenopathy appears, evaluate the patient and if an alternative etiology for these symptoms is not established, discontinue treatment.Risk of falls, confusion, loss of consciousness, progressive mental damage.
  • Abuse and dependence, monitoring.
  • May cause anaphylaxis, if symptoms of anaphylaxis appear, discontinue treatment.
  • Greater risk of presenting respiratory depression in respiratory and neurological diseases, in renal insufficiency, and concomitant with opioids, control for signs of CNS depression.

Renal insufficiency

Caution. Kidney failure: daily dose (in 3 doses) of: 600-1,800 mg if Clcr = 50-79 ml/min; 300-900 mg if Clcr = 30-49 ml/min; 150 (1) -600 mg if Clcr = 15-29 ml/min; 150 (1) -300 mg if Clcr < 15 ml/min. (1) Administer 300 mg/48 h.

Haemodialysis: loading dose 300-400 mg followed by 200-300 mg after each 4 h of haemodialysis.

Interactions with Gabapentin

  • Decreased bioavailability (to administer 2 h later) by: antacids.
  • Increased AUC with: morphine.
  • Lab: false + in the semi-quantitative determination of total proteins in urine with the analysis of test strips.

Pregnancy and Gabapentin

Animal studies have shown reproductive toxicity.
The potential risk in humans is unknown.
It should not be used during pregnancy unless the benefit to the mother is clearly greater than the potential risk to the fetus.

Breastfeeding

Gabapentin is excreted in breast milk.
Not knowing the possible effect on infants, during lactation should be administered with caution.
Gabapentin should only be used during lactation if the benefits to the mother clearly outweigh the potential risks to the baby.

Effects on driving ability

Gabapentin acts on the central nervous system and can produce: drowsiness, dizziness, visual alterations and decreased ability to react.
These effects, as well as the disease itself, make it advisable to be cautious when driving vehicles or operating dangerous machinery, especially until each patient’s particular sensitivity to the medication has been established.

Adverse reactions and side effects of Gabapentin

Viral infection, pneumonia, respiratory infection, urinary tract infection, infection, otitis media.
Leukopenia; anorexia, increased appetite.
Hostility, confusion and emotional instability, depression, anxiety, nervousness, abnormal thinking.
Drowsiness, dizziness, ataxia, convulsions, hyperkinesia, dysarthria, amnesia, tremor, insomnia, headache, sensations such as paresthesia, hypoesthesia, abnormal coordination, nystagmus, increase/decrease/absence of reflexes.
Visual alterations such as amblyopia, diplopia.
Vertigo.
High blood pressure, vasodilatation.
Dyspnea, bronchitis, pharyngitis, cough, rhinitis; vomiting, nausea, dental anomalies, gingivitis, diarrhea, abdominal pain, dyspepsia, constipation, dry mouth or throat, flatulence; facial edema, rash, itching, acne.
Arthralgia, myalgia, back pain, spasms; impotence; fatigue, fever, peripheral or generalized edema, abnormal gait, asthenia, pain, malaise, flu syndrome.
Decrease in leukocytes, weight gain.
Accidental injuries, fracture, abrasion.
Repetitive depression.
After the evaluation of pharmacovigilance data has been observed: dysphagia.

‚≠ź‚≠ź‚≠ź‚≠ź‚≠ź VIDEO OF GABAPENTIN/NEURONTIN (DRUG)

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII:6CW7F3G59X
ChemIDplus
DrugPortal
NCI Thesaurus: C1108

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