Convalis 300mg Capsules N50
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Active ingredients
Gabapentin
Release form
Capsules
Composition
1 capsule contains: Active substance: gabapentin 300 mg. Adjuvants: lactose monohydrate - 0.066 g, pregelatinized corn starch - 0.03 g, talc - 0.003 g, magnesium stearate - 0.001 g. Composition of hard gelatin capsules: titanium dioxide - 2%, dye iron oxide yellow - 0.6286%, gelatin - up to 100%.
Pharmacological effect
Gabapentin is similar in structure to the neurotransmitter GABA; however, its mechanism of action differs from that of some other drugs that interact with GABA receptors, including valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA inhibitors, GABA agonists, and pro-GABA pro-GABA inhibitors, and GABA inhibitors, and GABA inhibitors; has GABA-ergic properties and does not affect the seizure and metabolism of GABA. Preliminary research suggests that gabapentin is associated with the α2-δ-subunit of potential-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: reducing glutamate-dependent neuronal death, increasing GABA synthesis, suppressing the release of the neurotransmitters of the monoamine group. At clinically relevant concentrations, gabapentin does not bind to other receptors, including the GABAA, GABAB, benzodiazepine, glutamate, glycine or N-methyl-d-acparta receptors. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin has partially attenuated the effects of the glutamate receptor agonist N-methyl-d-aspartate in some in vitro tests, but only at a concentration of more than 100 mcmol / l, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters in vitro.
Pharmacokinetics
Absorption and distribution After ingestion of Cmax gabapentin in plasma is achieved in 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Bioavailability is not proportional to the dose, because with increasing doses, it decreases. Food, including with a high fat content, does not affect the pharmacokinetics. The pharmacokinetics do not change with repeated use. Css in plasma can be predicted based on the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%) and has a Vd of 57.7 l. Metabolism and elimination of T1 / 2 from plasma does not depend on the dose and averages 5-7 hours.Excreted exclusively by the kidneys in unchanged form, is not exposed to metabolism. The drug does not induce mixed function liver oxidative enzymes involved in drug metabolism. Plasma gabarenta of plasma decreases in elderly patients and patients with impaired renal function. The rate constant of elimination, plasma clearance and renal clearance are directly proportional to QC. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended.
Indications
- Epilepsy: in adults and children over 12 years of age - as monotherapy or as part of combination therapy for the treatment of partial epileptic seizures, including occurring with secondary generalization; - For the treatment of neuropathic pain in adults.
Contraindications
- Acute pancreatitis; - Children's age up to 12 years; - Lactase deficiency, lactose intolerance, glucose-galactose malabsorption; - Hypersensitivity to the drug and / or its components. With caution should be prescribed for renal failure.
Use during pregnancy and lactation
There are insufficient data on the use of gabapentin in pregnant women. Do not use the drug during pregnancy, if the potential benefit to the mother does not exceed the possible risk to the fetus. The drug penetrates into breast milk, the effect on babies during breastfeeding is unknown, therefore during breastfeeding, the drug should be used only in those cases where the potential benefit for the mother from taking the drug clearly exceeds the potential risk to the infant.
Dosage and administration
The drug is taken orally, regardless of the meal, without chewing and squeezing the required amount of fluid. Monotherapy and the use of Convalis as an adjuvant for the treatment of partial epileptic seizures in children over 12 years old and adults. 900 mg / day (the first day - 300 mg 1 time / day, the second - 300 mg 2 times / day, the third - 300 mg 3 times / day). Subsequently, the dose may be increased. Typically, the dose of Convalis is 900-1200 mg / day. The maximum dose - 3600 mg / day, divided into three equal doses after 8 hours.The maximum interval between doses of the drug should not exceed 12 hours in order to avoid renewed seizures. Neuropathic pain in adults Begin treatment with a dose of 300 mg on the first day, then: 600 mg (300 mg 2 times) on the second day, 900 mg (300 mg 3 times) - on the third day. With intense pain, Convalis can be applied from the first day to 300 mg 3 times / day. Depending on the effect, the dose can be gradually increased, but not more than 3600 mg / day. In patients with impaired renal function (with a CC of 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with a CC of 30-49 ml / min - 300-900 mg / day, with CC 15-29 ml / min - 300-600 mg / day, with CC less than 15 ml / min - 300 mg every other day or daily. In patients on hemodialysis, the initial dose Convalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On the days when dialysis is not performed, Convalis is not used.
Side effects
When treating neuropathic pain. From the digestive system: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain. On the side of the central nervous system: gait disturbance, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, impaired thinking , tremor. From the respiratory system: shortness of breath, pharyngitis. From the skin: skin rash. From the senses: amblyopia. Others: asthenic syndrome, flu-like syndrome, headache, infectious diseases, pain of different localization, lane spherical edema, weight gain. When treating partial seizures On the side of the cardiovascular system: symptoms of vasodilation, increased or decreased blood pressure. On the part of the digestive system: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or pharynx, nausea, vomiting. From the blood system: purpura (most often it was described as bruises resulting from physical trauma), leukopenia. From the musculoskeletal system: arthralgia, back pain, increased th brittle bones, mialgiya.So CNS: dizziness, hyperkinesia; strengthening, weakening or absence of tendon reflexes, paresthesia, anxiety, hostility, amnesia, ataxia, confusion, incoordination, depression,dysarthria, emotional lability, insomnia, nystagmus, drowsiness, impaired thinking, tremor, muscle fibrillation. On the respiratory system: pneumonia, cough, pharyngitis, rhinitis. On the skin side: abrasions, acne, itchy skin, skin rash. On the part of the urinary Systems: urinary tract infection. Genital system: impotence. Sensory organs: visual impairment, amblyopia, diplopia. Others: asthenic syndrome, swelling of the face, fatigue, fever, headache, viral infection, peripheral edema, increased ma sy tela.Pri comparison tolerability at doses of 300 and 3600 mg / day dose dependency marked phenomena such as dizziness, ataxia, somnolence, paresthesia and nistagm.Postregistratsionny experience primeneniyaVozmozhnye cases sudden unexplained deaths not related to gabapentin treatment. The following adverse events can occur during gabapentin treatment: various allergic reactions, acute renal failure, abnormal liver function, pancreas, breast volume increase, gynecomastia, hallucinations, movement disorders (myoclonus, discenisia, dystonia), palpitations, thrombocytopenia, noise in tinnitus, urination disorders. After abrupt withdrawal of gabapentin therapy, the following side effects were most often noted: anxiety, insomnia, nausea, pain of various l otsalization and sweating. If any of the side effects indicated in the instructions are aggravated or other side effects are noted that are not indicated in the instructions, you should inform your doctor.
Overdose
Symptoms: with a single dose of 49 g of gabapentin dizziness, diplopia, speech disorder, drowsiness, dysarthria, diarrhea were observed. A lethal dose of gabapentin when administered orally is established in mice and rats treated with the drug in doses of 8000 mg / kg. Signs of acute toxicity in animals included ataxia, shortness of breath, ptosis, hypoactivity, or agitation. Treatment: symptomatic therapy. Hemodialysis may be indicated in patients with severe renal insufficiency.
Interaction with other drugs
When gabapentin and morphine were taken simultaneously, when morphine was taken 2 hours before gabapptin, an increase in the average AUC gabapentin was observed by 44% compared with gabapentin monotherapy, which was associated with an increase in the pain threshold (cold pressor test).The clinical significance of this change has not been established, and the pharmacokinetic characteristics of morphine did not change. Side effects of morphine when administered jointly with gabapentin did not differ from those of morphine taken together with placebo. Interactions between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine were not observed. The pharmacokinetics of gabapentin in the equilibrium state are the same in healthy people and patients receiving other anticonvulsant drugs. Simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinyl estradiol was not accompanied by changes in the pharmacokinetics of both components. by 20%. In this regard, the drug should be taken no earlier than 2 hours after taking antacids. Pimetidin slightly reduces renal excretion of gabapentin. Ethanol and agents acting on the central nervous system can increase the side effects of gabapentin from the central nervous system. Simultaneous administration of naproxen with gabapentin increases absorption of the latter , while gabapentin does not affect naproxen pharmacokinetic parameters. Simultaneous use of gabapentin with hydrocodone leads to a decrease in pharmacokinetic parameters (Cmax and AUC) hydro Odon and increased AUC of gabapentin.
special instructions
When analyzing urine for total protein using the Ames N-Multistix SG test system, a false positive result is possible. It is necessary to confirm the result obtained using another method of analysis. In patients with diabetes mellitus, it is sometimes necessary to change the dose of hypoglycemic drugs. If there is evidence of acute pancreatitis, treatment with the drug should be stopped. The drug should be changed or replaced with an alternative means gradually, at least over a week. Abrupt cessation of anticonvulsant therapy in patients with partial convulsions may provoke the development of convulsions. There may be an increased risk of suicides and suicidal thoughts. With the aim of early detection of behavioral disorders that may be harbingers of suicidal thoughts and actions,It is recommended to monitor the mental state of patients. Impact on the ability to drive vehicles and control mechanisms. During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require high concentration of attention and psychomotor speed.