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dosage form Capsules size №0, yellow; contents of capsules — amorphous or crystalline powder white or white with a slightly yellowish tint. Composition gabapentin300 mg
Composition Gelatin Capsules: titanium dioxide, gelatin, iron oxide yellow. pharmachologic effect Anticonvulsants. Gabapentin is structurally similar to c neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from that of some other drugs that interact with GABA-receptors, including valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA, agonists GABA and prodrugs of GABA. It has no GABA-ergic properties and no effect on the capture and metabolism of GABA. Preliminary studies showed that gabapentin binds to alpha2-gamma subunit of the voltage-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the onset of neuropathic pain. Other mechanisms of action of gabapentin for neuropathic pain are: reduction of glutamate-dependent neuronal death, increasing the synthesis of GABA, inhibition of monoamine neurotransmitter release group.
Gabapentin at clinically relevant concentrations, does not bind to other receptors or neurotransmitters common drugs, including GABAA receptors, GABAB, benzodiazepine, glutamate, glycine, or N-methyl-D-aspartate (NMDA). Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partial agonist effects attenuated NMDA glutamate receptors in some tests in vitro, but only at a concentration of more than 100 micromoles, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitter in vitro Pharmacokinetics Suction
After oral administration, Cmax of gabapentin in plasma achieved in 2-3 hours. The bioavailability of gabapentin is not proportional to the dose, as by increasing the dose is reduced. Absolute bioavailability when taking gabapentin capsules is approximately 60%. Simultaneous food intake, including with a high content of fat, it has no effect on pharmacokinetics.
Pharmacokinetics does not change with repeated use; Css plasma can be predicted on the basis of the results of a single dose. Gabapentin is almost bound to plasma proteins (<3%), Vd is about 57.7 liters.
It is not subjected to metabolism. It does not induce hepatic oxidative enzymes mixed function involved in the metabolism of drugs.
T1 / 2 is not dependent on the dose and averages 5-7 hours.
Displays only the kidneys unchanged.
Pharmacokinetics in special clinical situations
It is found that the plasma concentration of gabapentin in children between the ages of 4 and 12 are generally similar to those in adults.
Clearance from plasma gabapentin reduced in the elderly and in patients with impaired renal function. The constant rate of excretion, clearance from the plasma and renal clearance are directly proportional to QC. Gabapentin is removed from plasma by hemodialysis. Side effects In the treatment of neuropathic pain
From the digestive system: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain.
From the central and peripheral nervous system: gait disturbance, amnesia, ataxia, confusion, dizziness, hypesthesia, somnolence, abnormal thinking, tremor, amblyopia.
The respiratory system: dyspnea, pharyngitis.
Dermatological reactions: skin rash.
Other: asthenic syndrome, flu-like symptoms, headache, infections, pain of various localization, peripheral edema, weight gain.
In the treatment of partial seizures
Cardio-vascular system: vasodilation symptoms decrease or increase in blood pressure.
From the digestive system: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea and / or vomiting.
From hemopoiesis system: purpura (often described as her bruises, occurred when a physical injury), leukopenia.
From the Musculoskeletal System: arthralgia, back pain, increased fragility of nails, myalgia.
From the central and peripheral nervous system: dizziness, hyperkinesia, strengthening, weakening or absence of tendon reflexes, paresthesia, anxiety, hostility, amnesia, ataxia, confusion, incoordination, depression, dysarthria, emotional lability, insomnia sale Properties prescription Special conditions Cancelling Konvalis or replace it with an alternative means should be gradual, at least for a week.
If you have symptoms of acute pancreatitis, drug treatment should be discontinued immediately.
During treatment Konvalisom possible false positive results in the determination of protein in the urine with litmus paper. In such cases it is necessary to confirm the result using another method of analysis.
In patients with diabetes is sometimes necessary to change the dose of hypoglycemic drugs.
Effects on ability to drive vehicles and management mechanisms
During treatment, patients should refrain from driving and performing work that requires attention and speed of psychomotor reactions. testimony — Epilepsy: monotherapy or in combination therapy for the treatment of partial seizures, including proceeding with secondary generalization in adults and children over the age of 12 years;
— Treatment of neuropathic pain in adults. Contraindications — Acute pancreatitis;
— Children up to age 12 years;
— Hypersensitivity to gabapentin and other ingredients.
Precautions should be used drug in renal failure Dosage When partial seizures with monotherapy or used as an aid in adults and children over 12 years of age are treated with a dose of 300 mg 1 time / and gradually increase it to 900 mg /: 1 day — 300 mg 1 time / on day 2 — 300 mg 2 to 3 day — 300 mg 3 subsequently possible to further increase the dose. Generally, the dosage is 900-1200 mg Konvalisa / maximum dose -. 3.6 g / in 3 doses equal doses every 8 hours In neuropathic pain medication prescribed for adults on Day 1 at a dose of 300 mg 1 time / day in 2 — 300 mg 2 on 3 day — 300 mg 3 When intense pain Konvalis can be administered on day 1, 300 mg of 3, depending on the effectiveness of the dose can be gradually increased, but not more than 3.6 g / for patients with impaired renal function daily dose of: QC at 50-79 ml / min — 600-1800 mg / 30-49 ml / min — 300-900 mg / 15-29 ml / min — 300-600 mg / less than 15 ml / min — 300 mg every day or daily. For patients on hemodialysis, the initial dose is 300 mg Konvalisa. Additional dose of 300 mg after each 4-hour hemodialysis session. On the day when the hemodialysis is not carried out, Konvalis not appointed