Farm group Gabapentin 100 mg:
antiepileptic drugs.
Farmdeystvie Gabapentin 100 mg:
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 gabapentinovyh receptors is not fully explored).
Pharmacokinetics Gabapentin 100 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. 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 100 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).
Contraindications Gabapentin 100 mg:
Hypersensitivity. With caution. Pregnancy, lactation, renal insufficiency.
Dosage: Orally, regardless of the meal. Epilepsy. Adults and children over the age of 12 years: initial dose – 300 mg 3 times a day on the first day, the effective dose – 900-3600 mg / day. The maximum daily dose – 3600 mg (for 3 equal doses). Maximum interval between administration of doses in the appointment of the drug 3 times a day should not exceed 12 h. Perhaps the appointment of the following scheme (phase titration). At a dose of 900 mg: first day – 300 mg 1 time per day, in the second – 300 mg 2 times a day, a third – 300 mg 3 times a day at a dose of 1200 mg: 400 mg 1 time a day, 400 mg 2 times a day, 400 mg 3 times daily in the first, second and third days, respectively. Children aged 3-12 years: Effective dose – 25-35 mg / kg / day. in 3 equal acceptance. Titrate dose to effective possible within 3 days: 10 mg / kg / day. – On the first day, 20 mg / kg / day. – Second, and 30 mg / kg / day. on the third. In the long-term clinical trial of tolerability at doses of 40-50 mg / kg / day. was good. Possible appointment to the scheme: if body weight 17-25 kg – 600 mg / day., Respectively, at 26-36 kg – 900 mg / day. At 37-50 kg – 1200 mg / day. At 51-72 kg – 1800 mg / day. Neuropathy in adults: initial dose – 300 mg 3 times a day, if necessary, gradually increase the dose to a maximum of 3600 mg / day. Patients with impaired renal function: with CC greater than 60 ml / min – 400 mg 3 times daily, with CC from 30 to 60 ml / min – 300 mg 2 times a day, with CC from 15 to 30 ml / min – 300 mg 1 time per day, with CC of less than 15 ml / min – 300 mg every other day. Patients on hemodialysis who had not previously received gabapentin, are encouraged to nominate a saturating dose of 300-400 mg, then 200-300 mg every 4 hours of hemodialysis.
Side Effects Gabapentin 100 mg:
From the CCC: Symptoms of vasodilation. When used in combination with other antiepileptic drugs – increased blood pressure. From the digestive system: dyspepsia, rarely – nausea, vomiting, abdominal pain, increased appetite, it is extremely rare – dry mouth or throat, constipation or diarrhea, pancreatitis, increased activity of liver trans-called. When used in combination with other antiepileptic drugs – flatulence, anorexia, gingivitis. From the musculoskeletal system: rarely – myalgia, arthralgia. When used in combination with other antiepileptic drug – a pain in the back. The nervous system: drowsiness, dizziness, ataxia, nystagmus (dose-related), fatigue, tremor, dysarthria, increased nervous excitability, rarely – headache, amnesia, depression, very rarely – thought disorder, confusion, tics, paresthesia (a dose-dependent ), fatigue, malaise, hyperkinesia; gain, hypo-or areflexia, anxiety and hostility. When used in combination with other antiepileptic drugs – insomnia. Part of the respiratory system: rarely – rhinitis, pharyngitis. When used in combination with other antiepileptic drugs – cough and pneumonia. From the urogenital system: the extremely rare – incontinence. When used in combination with other antiepileptic drugs – reduced potency, urinary tract infection. From the senses: visual disturbances (diplopia, amblyopia), ringing in the ears. For part of the blood: a very rare – leukopenia. Allergic reactions: seldom – skin rash, itching, fever, erythema multiforme exudative (including Stevens-Johnson syndrome). Other: purpura, weight gain, it is extremely rare – peripheral edema, discoloration of the enamel of teeth, acne, facial edema, fluctuations in blood glucose in diabetic patients. When used in combination with other antiepileptic drugs – increased fragility of bones.
Overdose Gabapentin 100 mg:
Symptoms: dizziness, diarrhea, diplopia, impaired speech, drowsiness, lethargy. Treatment: symptomatic, hemodialysis (with severe chronic renal failure).
Interaction Gabapentin 100 mg:
Possible joint application with other antiepileptic drugs (phenytoin, carbamazepine, valproic acid, phenobarbital), with oral contraceptive drugs (containing norethindrone and / or ethinyl estradiol), drugs that block tubular secretion (reduced excretion of gabapentin by the kidneys). Antacids (containing A13 + and Mg2 +) reduce the bioavailability of gabapentin by about 20% (recommended for 2 hours after taking an antacid). Myelotoxicity drugs – strengthening gematotoksichnosti (leukopenia).
Special instructions Gabapentin 100 mg:
If necessary, reduce the dose of medication to cancel or replace it with an alternative drug should be gradual over a minimum of 1 week. Abrupt discontinuation of antiepileptic drug therapy in patients with epilepsy can cause status epilepticus. Ineffective for the treatment of absansnyh seizures. During pregnancy, only applies if the alleged benefits to the mother justifies the potential risk to the fetus (may slow fetal growth in excess of therapeutic dose of 3600 mg in terms of mg / sq. M). Excreted in breast milk. Its effect on infants breast-fed, it is unclear why to use in breastfeeding women should only if the benefits to the mother clearly outweighs the risk. Safety and efficacy of gabapentin use in children younger than 3 years as an adjunctive therapy for epilepsy in children under the age of 12 years as a single agent is not installed. Safety and efficacy of the treatment of neuropathy in patients under age 18 is not installed. In the case of adults drowsiness, ataxia, dizziness, fatigue, nausea and / or vomiting, weight gain, and sleepiness in children, hyperkinesia and animosity should stop treatment and consult with your doctor. During the period of treatment must be careful when driving vehicles and occupation of other potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions.
