Gabapentin in the structure similar to
GABA, but its mechanism of action differs from other drugs that interact with
GABA receptors (valproate, barbiturates, benzodiazepines, inhibitors of
GABA-transaminase inhibitors capture GABA agonists GABA and GABA prodrugs
forms), and therapeutic concentrations are not associated with the following
receptors (GABA A subtypes, and b-, benzodiazepine, glutamate, glycine, and
PM-methyl-B-aspartate). In studies of the labeled gabapentin in vitro to
identify new peptide receptors in the brain tissue of rats, including the
neocortex and hippocampus, which may mediate the anticonvulsant activity of
gabapentin and its derivatives (structure and function gabapentin ovyh
receptors is not fully explored). You easy to Order Gabapentin Online
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Pharmacokinetics Gabapentin 300 mg:
Absorption – fast. Bioavailability is
not proportional to dose: as the dose is reduced and is at a dose of 300 mg –
60% at 1600 mg – 30%, respectively. Absolute bioavailability – 60% (capsules).
Pisha, including with a big fat no effect on pharmacokinetics. TSmah – 2-4
hours, plasma concentrations are proportional to dose. Smah – 2.4 micrograms /
ml when used in doses of 300 mg every 8 hours and 5.50 mcg / ml – a dose of 400
mg. AUC, respectively – 24.8 micrograms / ml / h and 33.3 micrograms / ml / hr.
Passes through the BBB, enters into breast milk. The volume of distribution –
57.7 liters. In patients with epilepsy concentration in CSF is approximately
20% of the corresponding CM drug in plasma. Relationship to plasma proteins –
is very low (less than 5%). Practically not metabolized, does not induce
oxidative enzymes with mixed functions involved in the metabolism of drugs. Also
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Excreted by the kidneys. Derivation
from plasma has a linear dependence. T1 / 2 – an average of 5-7 h does not
depend on the dose (at a dose of 300 mg – 5.2 hours, at a dose of 400 mg / -6.1
h). The rate constant of elimination, clearance from the plasma and renal
clearance of gabapentin is directly proportional to spacecraft. Removed during
hemodialysis. Clearance of gabapentin from the plasma is reduced in the elderly
and patients with impaired renal function, T1 / 2 for CC less than 30 ml / min
– 52 h. The pharmacokinetics did not change when you reapply.
Indications
Gabapentin 300 mg:
Epilepsy: partial seizures with
secondary generalization, and without her children and adults over age 12
(monotherapy), partial seizures with secondary generalization and without
adults (extra HP)-resistant form of epilepsy in children older than 3 years
(extra HP). Neuropathy in patients older than 18 years of age (treatment) (Gabapentin COD).
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