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DRUGS & SUPPLEMENTS
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Gabapentin
What is the dose of the medication you are taking? |
Gabapentin uses
Pharmacological action
Gabapentin is an antiepileptic drug. Chemical structure is similar to GABA fulfilling the function of the inhibitory neurotransmitter in the CNS. It is believed that the mechanism of action of Gabapentin is different from other anticonvulsants acting through GABA synapses. In in vitro studies showed that Gabapentin is characterized by the presence of a new peptide binding sites in the brain tissues of rats, including the hippocampus and cerebral cortex, which may be relevant to the anticonvulsant activity of Gabapentin and its derivatives. Gabapentin in clinically relevant concentrations is not associated with other conventional drugs and neurotransmitter receptors in the brain.
The final mechanism of action of Gabapentin is not defined.
Pharmacokinetics
Gabapentin is absorbed from the gastrointestinal tract. After oral administration of Gabapentin Cmax in plasma achieved within 2-3 hours. The absolute bioavailability of approximately 60%. Taking of this medication in conjunction with food (including a high-fat) does not affect the pharmacokinetics of Gabapentin.
Gabapentin is not bound to plasma proteins and has Vd 57.7 l.
Gabapentin is excreted only by the kidneys. Signs of biotransformation of Gabapentin in the human body were not found.
Gabapentin is removed from plasma by hemodialysis.
The concentrations of Gabapentin in the plasma of children were similar to those of adults.
Why is Gabapentin prescribed?
Treatment of neuropathic pain in adults over the age of 18 years; monotherapy of partial seizures with secondary generalization and without its fot children and adults older than 12 years; as an adjunct in the treatment of partial seizures with secondary generalization and without its for adults and children aged 3 years and older.
Dosage and administration
Dosing regimen of Gabapentin is individual, depending on the indications and treatment regimens.
Gabapentin side effects, adverse reactions
CNS and peripheral nervous system: amnesia, ataxia, confusion, impaired coordination, depression, dizziness, dysarthria, nervous hyperexcitability, nystagmus, drowsiness, impaired thinking, tremor, muscle cramps, amblyopia, diplopia, hyperkinesia, strengthening, weakening or absence of reflexes, paresthesia, anxiety, hostility, impaired gait.
Digestive system: change in staining of teeth, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in liver function tests.
Hemopoietic system: leucopenia, decrease the number of leukocytes, thrombocytopenic purpura.
Respiratory system: rhinitis, pharyngitis, cough, pneumonia.
Musculoskeletal system: myalgia, arthralgia, bone fractures.
Cardiovascular: hypertension, manifestations of vasodilation.
Urinary system: urinary tract infections, urinary incontinence.
Allergic reactions: erythema multiforme, Stevens-Johnson syndrome.
Dermatological reactions: maceration of the skin, acne, itching, rash.
Other: back pain, fatigue, peripheral edema, impotence, fatigue, malaise, swelling of the face, increase in body weight, accidental injury, asthenia, flu-like syndrome, fluctuations in blood glucose in children - a viral infection, otitis media.
Gabapentin contraindications
Hypersensitivity to Gabapentin.
Using during pregnancy and breastfeeding
Adequate and well-controlled studies on the safety of Gabapentin during pregnancy and lactation in humans has not been conducted. If necessary use Gabapentin during pregnancy and lactation patients should carefully weigh the potential benefits of therapy for the mother and the potential risk to the fetus or infant.
Gabapentin is excreted in breast milk. When this drug used in the lactation period, the character of the action of Gabapentin on the infant is not defined.
Category effects on the fetus by FDA - C.
Special instructions
Abrupt discontinuation of therapy by anticonvulsant drugs in patients with partial seizures may provoke a convulsive status. If necessary to reduce the dose of Gabapentin, to cancel or replace it with an alternative means it should be phased over a minimum of 1 week.
Gabapentin is not an effective drug for treatment of absence seizures.
For patients with impaired renal function and patients in hemodialysis it requires correction of dosing regimen. Elderly patients may require correction of the dosing regimen of Gabapentin due to the fact that such patients may decrease renal clearance.
The efficacy and safety of neuropathic pain treatment in patients under age 18 is not defined.
During the period of treatment it is necessary to avoid taking alcohol.
Prior to determining individual response to treatment the patient should refrain from potentially dangerous activities coupled with the need to focus and improve the speed of psychomotor reactions.
Gabapentin drug interactions
Simultaneous administration of Gabapentin with:
Gabapentin in case of emergency / overdose
There was reported an acute overdose while taking 49 g of Gabapentin. Symptoms: double vision, slurred speech, drowsiness, lethargy, diarrhea.
Treatment: maintenance therapy, hemodialysis.
Gabapentin pharmaceutical active ingredients containing related brand and generic drugs:
Gabapentin available forms, composition, doses:
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.