Convalis 300 mg, 50 pcs.

1 capsule contains:

active substance :

gabapentin - 0.3 g

excipients :

 lactose monohydrate - 0.066 g,

Pregelatinized corn starch - 0.030 g,

talc - 0.003 g,

magnesium stearate - 0.001 g.

Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (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 transcriptase inhibitors, GABA receptor inhibitors, GABA transaminases and prodrug forms of GABA: it does not have GABAergic properties and does not affect the uptake and metabolism of GABA.

Preliminary studies suggest that gabapentin binds to the α2-δ subunit of voltage-gated 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: a decrease in glutamate-dependent death of neurons, an increase in GABA synthesis, and suppression of the release of neurotransmitters of the monoamine group.

Clinically significant concentrations of gabapentin do not bind to receptors of other common drugs or neurotransmitters, including GABAA, GABAA, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate 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 μmol / L, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neutron transmitters in vitro.

For the treatment of neuropathic pain in adults. 

Data on the use of the drug in pregnant women are not available, so Convalis should be used during pregnancy only if the expected benefit to the mother outweighs the possible risk to the fetus.

The drug is excreted in breast milk, and its effect on the breast-fed baby is unknown. Therefore, if necessary, the use of the drug should abandon breastfeeding.

• acute pancreatitis;
• children under 12 years old;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• hypersensitivity to the drug and / or its components.

Use for impaired renal function

With caution, the drug should be prescribed for renal failure.

In patients with impaired renal function (with KK 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with KK 30-49 ml / min - 300-900 mg / day, with KK 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 Convalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On days when dialysis is not performed, Convalis is not used.

Use in children

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

Pregnancy and lactation

Data on the use of the drug in pregnant women are not available, so Convalis should be used during pregnancy only if the expected benefit to the mother outweighs the possible risk to the fetus.

The drug is excreted in breast milk, and its effect on the breast-fed baby is unknown. Therefore, if necessary, the use of the drug should abandon breastfeeding.

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

Monotherapy and the use of Konvalis as an adjuvant for the treatment of partial epileptic seizures in children over 12 years old 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 Convalis 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 recurrence 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. With intense pain, Convalis can be used from the first day at 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 KK 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with KK 30-49 ml / min - 300-900 mg / day, with KK 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 Convalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On days when dialysis is not performed, Convalis is not used.

With the simultaneous administration of gabapentin and morphine, when morphine was taken 2 hours before taking gabapeptin, an increase in the average AUC of 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; the pharmacokinetic characteristics of morphine have not changed. Side effects of morphine when taken together with gabapentin did not differ from those when taking morphine in conjunction with placebo.

The interaction between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine was not observed. The pharmacokinetics of gabapentin in equilibrium are the same in healthy people and 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 the renal excretion of gabapentin.

Ethanol and agents acting on the central nervous system can enhance the side effects of the central nervous system gabapentin.

With the simultaneous administration 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 (C _max  and AUC) of hydrocodone and an increase in AUC of gabapentin.

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

Monotherapy and the use of Konvalis as an adjuvant for the treatment of partial epileptic seizures in children over 12 years old 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 Convalis 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 recurrence 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. With intense pain, Convalis can be used from the first day at 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 KK 50-79 ml / min), the daily dose of the drug is 600-1800 mg / day, with KK 30-49 ml / min - 300-900 mg / day, with KK 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 Convalis is 300 mg. An additional post-hemodialysis dose is 300 mg after each 4-hour hemodialysis session. On days when dialysis is not performed, Convalis is not used.

Symptoms: with a single dose of 49 g of gabapentin, dizziness, diplopia, speech impairment, drowsiness, dysarthria, diarrhea were observed. The lethal dose of gabapentin when administered 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. Patients with severe renal failure may be shown hemodialysis.

In the treatment of neuropathic pain

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

From the side of the central nervous system: impaired gait, 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 sensory organs: amblyopia.

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

In the treatment of partial seizures

From the cardiovascular system: symptoms of vasodilation, increased or decreased blood pressure.

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

On the part of the blood system: purpura (most often it was described as bruising arising from physical trauma), leukopenia.

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

From the side of the central nervous system: dizziness, hyperkinesis; amplification, 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.

From the skin: abrasions, acne, itching of the skin, skin rash.

From the urinary system: urinary tract infection.

From the reproductive system: impotence.

From the sensory organs: impaired vision, amblyopia, diplopia.

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

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

Post-Registration Application Experience

Possible cases of sudden unexplained death are not associated with gabapentin treatment. During the treatment with gabapentin, the following adverse events can be observed: various allergic reactions, acute renal failure, impaired liver, pancreas, increased mammary gland volume, gynecomastia, hallucinations, motor disorders (myoclonus, dyskinesia, dystonia), heartbeat, thrombocytopenia, noise in ears, urination disorders.

After abrupt discontinuation 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 specified in the instructions are aggravated or other side effects are noted that are not listed in the instructions, you should inform your doctor.

Capsules