Neurontin, 100 pcs., 600 mg, film-coated tablets

Neurontin®

In the treatment of neuropathic pain

From the body as a whole:

at least 1% - accidental injuries, asthenia, back pain, flu-like syndrome, headache, infection, pain of various localizations, peripheral edema, weight gain.

From the digestive system:

at least 1% - constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain.

From the central nervous system and peripheral nervous system:

at least 1% - gait disturbance, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, impaired thinking, tremor.

From the respiratory system:

at least 1% - shortness of breath, pharyngitis;

Dermatological reactions:

at least 1% - skin rash.

From the senses:

at least 1% - amblyopia.

In the treatment of partial seizures

Neurontin is most often used in combination with other anticonvulsants, so it was not possible to determine which drug was causing the side effects (if any).

From the body as a whole:

at least 1% - asthenia, general malaise, facial swelling, fatigue, fever, headache, viral infection, peripheral edema, weight gain.

From the cardiovascular system:

at least 1% - symptoms of vasodilation or arterial hypertension.

From the digestive system:

at least 1% - flatulence, anorexia, gingivitis, abdominal pain, constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or pharynx, nausea and/or vomiting.

From the hematopoietic system:

at least 1% - purpura (most often it was described as bruising that occurred as a result of physical trauma), leukopenia.

From the musculoskeletal system:

at least 1% - arthralgia, back pain, fractures, myalgia.

From the central nervous system and peripheral nervous system:

at least 1% - dizziness, hyperkinesis, increased, weakened or absent reflexes, paresthesia, anxiety, hostility, amnesia, ataxia, confusion, impaired coordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremor, muscle twitching.

From the respiratory system:

at least 1% - pneumonia, cough, pharyngitis, rhinitis.

Dermatological reactions:

at least 1% - abrasions, acne, skin itching, skin rash.

From the urinary system:

at least 1% - urinary tract infection, impotence.

From the senses:

at least 1% - visual impairment, amblyopia, diplopia.

These side effects were mild or moderate.

No new or unexpected side effects were observed during monotherapy. When comparing the tolerability of the drug at doses of 300 mg/day and 3.6 g/day, a dose dependence of such phenomena as dizziness, ataxia, drowsiness, paresthesia and nystagmus was noted.

The following are side effects that have been observed in children

with adjunctive therapy with an incidence of approximately 2% or higher compared with placebo.

From the body as a whole:

viral infection, fever, weight gain, fatigue.

From the digestive system:

nausea and/or vomiting.

From the central nervous system and peripheral nervous system:

drowsiness, hostility, emotional lability, dizziness, hyperkinesia.

From the respiratory system:

bronchitis, respiratory infection.

Other:

in more than 2% of children (incidence in the placebo group was similar or higher) - included pharyngitis, upper respiratory tract infections, headache, rhinitis, cramps, diarrhea, anorexia, cough and otitis media.

Side effects that most often required discontinuation of the drug

used as an adjuvant therapy - drowsiness, ataxia, dizziness, fatigue, nausea and/or vomiting; as monotherapy - dizziness, nervousness, weight gain, nausea and/or vomiting and drowsiness.

Adverse events that most often led to drug discontinuation in children

- drowsiness, hyperkinesia and hostility.

Post-registration experience of use

There have been cases of sudden unexplained death, the connection of which with gabapentin treatment has not been established. Other undesirable effects are acute renal failure, allergic reactions (including urticaria, angioedema), alopecia, fluctuations in blood glucose levels in patients with diabetes, chest pain, increased activity of liver enzymes, exudative erythema multiforme (including . Stevens-Johnson syndrome), hallucinations, movement disorders (choreoathetosis, dyskinesia and dystonia), palpitations, pancreatitis, thrombocytopenia, tinnitus, urinary incontinence, hepatitis and jaundice.

After abrupt cancellation

Neurontin therapy most often causes anxiety, insomnia, nausea, pain of various localizations and sweating.

NEURONTIN

special instructions

Suicidal ideation and behavior
Antiepileptic drugs, including gabapentin, may increase the risk of suicidal ideation or behavior. A meta-analysis of randomized placebo-controlled trials of antiepileptic drugs demonstrated a small increase in the risk of suicidal ideation and behavior. The mechanism for increasing the risk of developing suicidal ideation is unknown, but for gabapentin it cannot be excluded. Therefore, patients receiving these drugs should be closely monitored for new or worsening depression, the emergence of suicidal thoughts or behavior, and any changes in behavior. Patients or their caregivers should seek medical attention if signs of suicidal thoughts or behavior occur.

Acute pancreatitis

If acute pancreatitis develops while taking gabapentin, the possibility of discontinuing the drug should be assessed.

Convulsions ("oo" syndrome).

As with other antiepileptic drugs, gabapentin may cause an increase in the frequency of seizures or the appearance of a different type of seizure.

As with other anticonvulsants, attempts to discontinue all concomitant antiepileptic drugs in order to initiate gabapentin monotherapy in cases of treatment refractory in patients taking multiple anticonvulsants are generally unsuccessful.

Gabapentin is not thought to be effective for primary generalized seizures, such as absence seizures, and may even worsen such seizures in some patients. In this regard, gabapentin should be used with caution in patients with mixed seizures, including absence seizures.

Elderly patients

Systematic studies have not been conducted in patients aged 65 years and older taking gabapentin. In a double-blind study of gabapentin for neuropathic pain, patients aged 65 years and older had a higher incidence of somnolence, peripheral edema, and asthenia compared with patients aged <65 years. Apart from these results, clinical examination of this group of patients showed that their side effect profile did not differ from the rest.

Children

The effect of long-term therapy (more than 36 weeks) with gabapentin on the learning ability, intelligence and development of the child has not been sufficiently studied. The ratio of possible risks and benefits should be assessed when prescribing long-term therapy. Abuse and addiction. The post-marketing surveillance database contains reports of cases of drug abuse and dependence. As with any drug that affects the central nervous system, clinicians should carefully review patients' drug abuse history and monitor patients for possible signs of gabapentin abuse (eg, drug seeking, development of resistance to gabapentin therapy, inappropriate dosage increases). ).

DRESS syndrome

Severe life-threatening hypersensitivity reactions, such as drug rash with associated eosinophilia and systemic symptoms, have been reported while taking antiepileptic drugs, including gabapentin. It is necessary to remember this. that early signs of a hypersensitivity reaction, such as fever, lymphadenopathy, can develop even in the absence of skin rash. If such symptoms occur, immediate examination of the patient is necessary. If no other reason is found other than the use of gabapentin, the use of the drug should be discontinued.

Anaphylaxis

Taking gabapentin can lead to the development of anaphylaxis. The following symptoms and signs were noted in cases of anaphylaxis while taking gabapentin: difficulty breathing, swelling of the lips, throat and tongue, and a marked decrease in blood pressure was also noted, requiring urgent medical intervention. Patients should be warned that if signs or symptoms of anaphylaxis develop, they should stop taking the drug and seek medical attention.

Laboratory tests

When gabapentin and other anticonvulsants were co-administered, false-positive results have been reported when measuring urinary protein using Ames N-Multistix SG test strips. To determine protein in urine, it is recommended to use the more specific precipitation method of sulfosalicylic acid.

Effect on the central nervous system

During treatment with gabapentin, cases of dizziness and drowsiness have been observed, which may increase the likelihood of accidental injury (from a fall). Cases of confusion, loss of consciousness and mental impairment have also been reported during the post-marketing period. Therefore, patients should be advised to use caution until they are aware of the possible effects of this drug.

When used simultaneously with opioid analgesics, an increase in the concentration of gabapentin in the blood plasma may be observed. In this regard, the patient needs to be closely monitored for the development of signs of CNS depression, such as drowsiness, sedation, and respiratory depression. Doses of gabapentin or opioid analgesics should be reduced accordingly (see section "Interactions with other drugs").

Combined use with antacids

It is recommended to take gabapentin approximately 2 hours after taking the antacid.

Neurontin, 100 pcs., 600 mg, film-coated tablets

Inside, regardless of meals or with food.

Epilepsy.

Adults and children over 12 years of age: effective dose is 900–3600 mg/day. Therapy can be started with a dose of 300 mg 3 times a day on the first day or the dose can be titrated as described below. Subsequently, the dose can be increased to a maximum of 3600 mg/day (in 3 equal doses). In long-term open clinical studies, the drug was well tolerated in doses up to 4800 mg/day. The maximum interval between doses when taking the drug three times should not exceed 12 hours to avoid the occurrence of seizures.

Children 3–12 years old: effective dose: 25–35 mg/kg/day in equal doses in 3 divided doses (see table). You can start titrating the dose to an effective dose over 3 days: 10 mg/kg/day on the first day, 20 mg/kg/day on the second day and 30 mg/kg/day on the third day (see table). subsequently, the dose can be increased to a maximum of 35 mg/kg/day in equal doses in 3 divided doses. In a long-term clinical study, the drug was well tolerated in doses of up to 40–50 mg/kg/day.

Gabapentin can be used in combination with other antiepileptic drugs without concern for changes in gabapentin plasma concentrations and serum concentrations of other antiepileptic drugs. Gabapentin should be discontinued and/or another anticonvulsant drug added to treatment gradually over a period of at least 1 week.

Neuropathic pain in adults.

Initial dose: 900 mg/day in 3 divided doses; if necessary, depending on the effect, the dose is gradually increased to a maximum of 3600 mg/day. Dose selection treatment should be started as described in the first table.

For patients with impaired renal function or patients receiving hemodialysis treatment, a dose reduction is recommended (see table).

a The daily dose should be administered in 3 divided doses. In patients with normal renal function (Cl creatinine >80 ml/min), the dose ranges from 900 to 3600 mg/day. In patients with impaired renal function (Cl creatinine <79 ml/min), the dose should be reduced. b Prescribe 300 mg every other day.

For patients receiving hemodialysis treatment who have not previously taken gabapentin, it is recommended to prescribe the drug in a loading dose of 300–400 mg, and then use it at 200–300 mg every 4 hours of hemodialysis.

Medical Internet conferences

Cerebrovascular diseases currently remain a leading medical, social and economic problem. According to European researchers, at least 60% of patients after a stroke remain disabled [Kadykov A.S., Shakhparonova N.V., 2006]. The consequences of strokes are extremely varied. Severe manifestations include extrapyramidal disorders (hyperkinesis). We present a clinical observation of the use of the drug pregabalin (Lyrica) for the treatment of hyperkinetic syndrome in a patient who suffered an ischemic stroke.

Patient G., 66 years old, was admitted to the clinic with a diagnosis of consequences of an ischemic stroke in the left middle cerebral artery. Main complaints: weakness in the right extremities, more so in the arm, speech impairment, involuntary movements in the right extremities, due to which he often wakes up, aggravated by voluntary movements, fatigue. In March 2008, against the background of paroxysmal atrial fibrillation, he suffered an ischemic stroke in the LSMA pool. A few months after the stroke, involuntary movements began in the right limbs, more so in the leg, intensifying with voluntary movements. Due to a sharp increase in hyperkinesis in the evening and at night, sleep was disturbed.

In the neurological status: smoothness of the right nasal fold, deviation of the tongue to the right, pseudobulbar dysarthria, right-sided central spastic hemiparesis, more pronounced in the arm (up to 3 points), moderate in the leg, reflexes of oral automatism, right-sided hemihypesthesia of all types of sensitivity, right-sided ataxia in the right limbs , more in hand. Mixed tremor (intentional and postural) in the right extremities. In the right extremities, hyperkinetic syndrome is determined, which has a complex pattern with elements of choreathetosis. According to MRI of the brain, there is a picture of ischemic stroke in the left temporo-occipital region and the left thalamus. Moderately severe external hydrocephalus. To reduce the manifestations of hyperkinetic patient consent syndrome, the drug pregabalin (Lyrica) was added to the basic treatment at a daily dose of 75 mg twice a day. While taking the drug, already during the first week the patient noted a significant decrease in the manifestations of hyperkinesis, which led to a significant improvement in the characteristics of night sleep and the emotional status of the patient. This effect remained at a high level when taking the drug both during the entire hospital stay and over the next six months in an outpatient setting.

Pregabalin is an analogue of GABA, the mechanism of action of the drug is associated with its interaction with an additional subunit (a2-delta-proein) of voltage-dependent calcium channels in the central nervous system. Pregabalin has much in common with gabapentin, the mechanism of action of which also includes a modulating effect on NMDA receptors, a decrease in the synthesis and transport of glutamate, and a decrease in the release of monoamines. A few studies have shown the effect of taking pregabalin in the treatment of essential tremor (Zesiewicz T.A. at al, 2007,2007; Ferrara JM, 2009). In our observation, the drug was used to relieve another form of extrapyramidal hyperkinetic syndrome with a clear positive clinical effect, which significantly improved the patient’s quality of life. Continued study of the drug pregabalin (Lyrica), taking into account various mechanisms of action, will further expand the scope of its use in the treatment of various neurological diseases.