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The anticonvulsant drug. Gabapentin is structurally similar to c neurotransmitter gamma-aminobutyric cellulitis acid (GABA), but its mechanism of action differs from that of certain other drugs that interact with GABA-receptors, including valproate, barbiturates, benzodiazepines, GABA-transaminase inhibitors, inhibitors capture GABA, GABA agonists, and prodrugs of GABA. He does not have the properties of GABA-ergic and does not affect the metabolism of the capture and GABA. Preliminary studies have shown that gabapentin is associated with α2-δ-subunit of voltage-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms of action of gabapentin cellulitis for neuropathic pain are: reduction of glutamate-dependent neuronal cell death, increased synthesis cellulitis of GABA, inhibition of monoamine neurotransmitter release.
Gabapentin at clinically relevant concentrations, does not bind to receptors or other drugs commonly neurotransmitter receptors including GABAA, GABAB, benzodiazepine, glutamate, glycine, or N-methyl-D-aspartate (NMDA). Unlike phenytoin, carbamazepine and gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuate the effects of glutamate NMDA receptor agonists in some tests in vitro, but only at concentrations greater than 100 micromoles, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.
Indications epilepsy: monotherapy or in combination therapy for the treatment of partial seizures, including cellulitis proceeding with secondary cellulitis generalization in adults cellulitis and children over the age of 12 years, treatment cellulitis of neuropathic pain in adults.
When partial seizures as monotherapy or used as an aid in adults and children over 12 years of age, treatment is initiated with a dose of 300 mg 1 time / day and gradually increase it to 900 mg / day: day 1 - 300 mg 1 time / day, in Day 2 - 300 mg 2 times / day for 3 days - 300 mg 3 times / day. Subsequently possible to further increase the dose. The dose is Konvalisa 900-1200 mg / day. The maximum dose - 3.6 g / day in 3 divided doses equal doses with an interval of 8 hours
Neuropathic pain medication prescribed for adults in a daily dose of 1 300 mg 1 time / day, in two day - 300 mg 2 times / day for 3 days - 300 mg 3 times / day. With intense pain Konvalis be administered from day 1, 300 mg 3 times / day. Depending on the effectiveness of the dose can be gradually increased, but not more than 3.6 g / day.
For patients with impaired renal function, the daily dose is: with CC 50-79 ml / min - 600-1800 mg / day, 30-49 ml / min - 300-900 mg / day, 15-29 ml / min - 300 - 600 mg / day, less than 15 ml / min - 300 mg on alternate days or daily.
For patients on hemodialysis, the initial dose is 300 mg Konvalisa. An additional dose of 300 mg after each 4-hour hemodialysis session. On a day when hemodialysis is not carried out, Konvalis not appointed.
With the Musculoskeletal System: arthralgia, back pain, nail fragility, myalgia.
CNS and peripheral nervous system: dizziness, hyperkinesia, strengthening, weakening or absence of tendon reflexes, paresthesia, anxiety, hostility, amnesia, ataxia, confusion, impaired coordination, depression, cellulitis dysarthria, emotional lability, insomnia, nystagmus, drowsiness, cellulitis impaired thinking, tremor, muscle twitching, impaired vision, amblyopia, diplopia. cellulitis
Interactions with other drugs
With simultaneous use of gabapentin and morphine (as morphine took about 2 hours to gabapentin), an increase in mean AUC of gabapentin by 44% compared with monotherapy cellulitis gabapentin, accompanied by an increase in pain threshold (KHOLODOVA pressor test). The clinical significance of this change is not set, the pharmacokinetics cellulitis of morphine is not changed. Adverse effects of morphine during coadministration with gabapentin did not differ from those of morphine in conjunction cellulitis with receiving placebo.
Simultaneous use of gabapentin with antacids containing aluminum and magnesium, followed by reduction of gabapentin bioavailability by approximately 20%. Therefore, it is recommended to take Konvalis no earlier than 2 hours after antacids.
Konvalis cellulitis should be used during cellulitis pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus, as data on the use of the drug in pregnant women are not available.
During cellulitis treatment Konvalisom possible false-positive results in the determination of protein in the urine by Lakme
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