Convalis capsules 300mg, No. 50

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, incl. proceeding with secondary generalization;

for the treatment of neuropathic pain in adults.

The drug is taken orally, regardless of food intake, without chewing and drinking the required amount of liquid.

Monotherapy and use of Konvalis as an adjuvant for the treatment of partial epileptic seizures in children over 12 years of age and adults

Treatment begins with a dose of 300 mg 1 time / day and gradually increases to 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. Usually the dose of Konvalis is 900-1200 mg / day. The maximum dose is 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 the resumption of seizures.

Neuropathic pain in adults

Treatment begins 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. In case of intense pain, KonvalisЃ can be used from the first day, 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 CC 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with CC 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 of Konvalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On days when dialysis is not performed, KonvalisЃ is not used.

Capsules size No. 0, yellow; the contents of the capsules are white or yellowish crystalline powder.

1 caps.

gabapentin 300 mg

Excipients: lactose monohydrate - 66 mg, pregelatinized corn starch - 30 mg, talc - 3 mg, magnesium stearate - 1 mg.

acute pancreatitis;

children under 12 years of age;

lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

hypersensitivity to the drug and / or its components.

Precautions should be taken in renal failure.

pharmachologic effect

Gabapentin is structurally similar to the neurotransmitter GABA, but 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 uptake inhibitors, GABA agonists, and non-GABA prodrugs possesses GABA-ergic properties and does not affect the uptake and metabolism of GABA.

Preliminary studies indicate that gabapentin binds to the ? 2 - ? subunit of voltage-gated calcium channels and inhibits calcium ion flux, which plays an important role in neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, and inhibition of the release of monoamine group neurotransmitters. Gabapentin at clinically relevant concentrations does not bind to other receptors, including the GABAA, GABAB, benzodiazepine, glutamate, glycine, or N-methyl-d-acid receptors. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin 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 ?mol / l, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.

Pharmacokinetics

Absorption and distribution

After oral administration, Cmax of gabapentin in plasma is achieved after 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Bioavailability is not proportional to dose. with increasing dose, it decreases. Food, incl. with a high fat content, has no effect on pharmacokinetics.

Pharmacokinetics does not change with repeated use. Plasma Css can be predicted from 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 liters.

Metabolism and excretion

T1 / 2 from plasma does not depend on the dose and averages 5-7 hours. It is excreted exclusively by the kidneys in unchanged form, it is not metabolized. The drug does not induce mixed liver oxidative enzymes involved in drug metabolism.

The clearance of gabapentin from plasma is reduced in elderly patients and patients with impaired renal function. The rate constant of elimination, plasma clearance and renal clearance are directly proportional to CC. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended.

Side effect

When treating neuropathic pain

From the digestive system: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain.

From the side of the central nervous system: gait disturbance, amnesia, ataxia, confusion, dizziness, hypesthesia, drowsiness, impaired thinking, tremor.

From the respiratory system: shortness of breath, pharyngitis.

On the part of the skin: skin rash.

From the senses: amblyopia.

Others: asthenic syndrome, flu-like syndrome, headache, infectious diseases, pain of various localization, peripheral edema, weight gain.

In the treatment of partial seizures

From the side of the cardiovascular system: symptoms of vasodilation, increase or decrease in blood pressure.

From the digestive system: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea, vomiting.

From the side of the blood system: purpura (most often it was described as bruising resulting from physical injury), leukopenia.

From the musculoskeletal system: arthralgia, back pain, increased fragility of bones, myalgia.

From the side of the central nervous system: dizziness, hyperkinesis; strengthening, weakening or absence of tendon reflexes, paresthesia, anxiety, hostility, amnesia, ataxia, confusion, impaired coordination of movements, depression, dysarthria, emotional lability, insomnia, nystagmus, drowsiness, impaired thinking, tremor, muscle fibrillation.

From the respiratory system: pneumonia, cough, pharyngitis, rhinitis.

On the part of the skin: abrasions, acne, itching of the skin, skin rash.

From the urinary system: urinary tract infection.

From the reproductive system: impotence.

From the senses: visual impairment, amblyopia, diplopia.

Others: asthenic syndrome, facial edema, fatigue, fever, headache, viral infection, peripheral edema, weight gain.

When comparing the tolerability of the drug in doses of 300 and 3600 mg / day, a dose-dependence of such phenomena as dizziness, ataxia, drowsiness, paresthesia and nystagmus was noted.

Post-registration experience of application

Potential sudden unexplained deaths are not associated with gabapentin treatment. During treatment with gabapentin, the following undesirable effects can be observed: various allergic reactions, acute renal failure, impaired liver function, pancreas, an increase in the volume of the mammary glands, gynecomastia, hallucinations, movement disorders (myoclonus, dyskenia, dystonia), palpitations, thrombocytopenia, noise in tinnitus, urinary disorders.

After abrupt withdrawal of gabapentin therapy, the following side effects were most often observed: anxiety, insomnia, nausea, pain of various localization and sweating.

If any of the side effects indicated in the instructions are aggravated or other side effects not indicated in the instructions are noted, you must inform your doctor about it.

Application during pregnancy and lactation

There are insufficient data on the use of gabapentin in pregnant women. You should not use the drug during pregnancy if the potential benefit to the mother does not outweigh the potential risk to the fetus.

The drug passes into breast milk, the effect on children during breastfeeding is unknown, therefore, during breastfeeding, the drug should be used only if the potential benefit to the mother from taking the drug clearly outweighs the potential risk to the baby.

Application for impaired renal function

The drug should be prescribed with caution in case of renal failure.

In patients with impaired renal function (with CC 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with CC 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 of Konvalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On days when dialysis is not performed, Konvalis is not used.

Application in children

The use of the drug is contraindicated in children under 12 years of age.

special instructions

When testing urine for total protein using the Ames N-Multistix SGЃ test system, a false positive result is possible. It is necessary to confirm the obtained result using another method of analysis.

Patients with diabetes mellitus sometimes need to change the dose of hypoglycemic drugs.

If signs of acute pancreatitis appear, treatment with the drug should be discontinued.

The drug should be withdrawn or replaced with an alternative remedy gradually, at least over a week. Abrupt discontinuation of anticonvulsant therapy in patients with partial seizures can provoke the development of seizures.

There may be an increased risk of suicide and suicidal thoughts. In order to early detection of behavioral disorders that may be harbingers of suicidal thoughts and actions, it is recommended to monitor the mental state of patients.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: with a single dose of 49 g of gabapentin, dizziness, diplopia, speech impairment, drowsiness, dysarthria, diarrhea were observed. The lethal oral dose of gabapentin was established in mice and rats treated with the drug at doses of 8000 mg / kg. Signs of acute toxicity in animals included ataxia, shortness of breath, ptosis, hypoactivity, or agitation.

Treatment: carrying out symptomatic therapy. Patients with severe renal insufficiency may be indicated for hemodialysis.

Drug interactions

With the simultaneous administration of gabapentin and morphine, when morphine was taken 2 hours before taking gabapeptin, there was an increase in the mean AUC value of gabapentin 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. The side effects of morphine when taken together with gabapentin did not differ from those when taking morphine together with placebo.

Interactions between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine have not been observed. The steady state pharmacokinetics of gabapentin are similar in healthy individuals and in patients receiving other anticonvulsants.

The simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinyl estradiol was not accompanied by changes in the pharmacokinetics of both components.

Antacids containing aluminum or magnesium reduce the bioavailability of gabapentin by about 20%. In this regard, the drug should be taken no earlier than 2 hours after taking antacids.

Pimetidine slightly reduces renal excretion of gabapentin.

Ethanol and CNS agents may increase the CNS side effects of gabapentin.

With the simultaneous appointment of naproxen with gabapentin, the absorption of the latter increases, while gabapentin does not affect the pharmacokinetic parameters of naproxen.

The simultaneous use of gabapentin with hydrocodone leads to a decrease in the pharmacokinetic parameters (Cmax and AUC) of hydrocodone and an increase in the AUC of gabapentin.