2010/06/16

Gabagamma

Composition, structure and packing Gabagamma 

Hard gelatin capsules, are white.

1 capsule. gabapentin 100 mg.

Excipients: anhydrous lactose, corn starch, talc.

The composition of the shell capsules: gelatin, titanium dioxide (E171).

Hard gelatin capsules, yellow.

1 capsule. gabapentin 300 mg.

Excipients: anhydrous lactose, corn starch, talc.

The composition of the shell capsules: gelatin, titanium dioxide (E171), iron oxide yellow (E172).

Hard gelatin capsules are orange.

1 capsule. gabapentin 400 mg.

Excipients: anhydrous lactose, corn starch, talc.

The composition of the shell capsules: gelatin, titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172).

Clinico-pharmacological group: anticonvulsants.

Pharmacological action

Anticonvulsants.

In in vitro studies have identified new peptide receptors in the brain tissue, through which may be mediated anticonvulsant activity of gabapentin and its derivatives.

At therapeutic concentrations of the drug does not bind to receptors and GABAa GABAb, benzodiazepine, glutamate, glycine, N-methyl-D-Aspartate receptors.

Pharmacokinetics

Absorption

When administered drug is rapidly absorbed. Bioavailability is not proportional to dose: the dose is increased bioavailability is reduced and is at a dose of 300 mg - 60%, at 1600 mg - 30%, respectively. The absolute bioavailability - 60%. Food, including with high-fat diet has no effect on the pharmacokinetics of the drug. Time to reach Cmax - 2-4 pm

The concentration of active substance in the blood plasma is proportional to dose. Tmax was 4.02 mg / ml in the appointment of the drug in a dose of 300 mg every 8 h and 5.50 mg / ml - when receiving a dose of 400 mg.

Distribution Gabagamma 
Vd - 57.7 liters. In patients with epilepsy concentration in the cerebrospinal fluid of approximately 20% of the equilibrium concentrations of the drug in plasma. The drug is associated with poor plasma proteins (less than 5%). The drug penetrates through the BBB, is excreted in breast milk.

Metabolism Gabagamma 

Gabapentin is practically not metabolized, does not induce oxidative enzymes of mixed function involved in the metabolism of the drug.

Withdrawal Gabagamma 

We derive the kidneys. Derivation from plasma has a linear relationship. T1 / 2 - an average of 5-7 hours, not dependent on the dose. The rate constant of elimination, clearance from the plasma and renal clearance of gabapentin is directly proportional to creatinine clearance.

Gabapentin removed from plasma during hemodialysis.

Pharmacokinetics in special clinical situations

Clearance from plasma gabapentin declining in the elderly and patients with impaired renal function. When spacecraft less than 30 ml / min T1 / 2 is 52 hours

Pharmacokinetics is not altered by repeated use.

Statement
epilepsy;
diabetic polyneuropathy;
Postherpetic neuralgia.

Dosage regimen Gabagamma 

The drug is used inside, regardless of the meal.

Patients with epilepsy drug prescribed in doses of 900-3600 mg / day.

Adults and teenagers of the drug beginning with a dose of 300 mg / day.

Increasing the dose can be made for two schemes:

1. Main circuit

The morning dose / daily dose / Evening dose
1 day (300 mg / day.) - - 300 mg.
Day 2 (600 mg / day.) / 300 mg. / - / 300 mg.
Day 3 (900 mg / day.) / 300 mg. / 300 mg. / 300 mg

2. Application of the initial dose of 3 to 300 mg. After that may be made increasing the daily dose to 1.2 g in 3 divided doses, and if necessary may increase the dose of 300 mg steps up to the maximum dose.

The time interval between the evening and the morning followed by doses should not exceed 12 hours in order to avoid new attacks.

Patients with diabetic polyneuropathy and postherpetic neuralgia medication prescribed at a dose of 1.8-2.4 g / maximum daily dose - 3.6 g / day.

Adults of the drug beginning with a dose of 300 mg according to the basic scheme.

After this dose can be increased within 1 week to 1.8 g / day. 3 admission. Within the next week, as needed, the dose may be increased to 2.4 g / day. 3 admission. If necessary, may further increase the dose gradually to 300 mgsut. in 3 divided doses until the maximum dose of 3.6 g / day.

Increasing the dose to achieve the maintenance dose should be done slowly. The time interval between the evening and morning doses should not exceed 12 hours

Patients with impaired renal function is recommended to use lower doses. Because elderly patients with renal function may be compromised, for this group of patients is also needed correction dosing regimen.

Recommended dose, depending on the spacecraft are presented in the table.

CC (ml / min) / total daily dose (mg) 1
> 80 / 900-3600
50-79 / 600-1800
30-49 / 300-900
15-29 / 1502-600
<15 / 1502-300

1 - total daily dose should be divided into 3

2 - 300 mg every 2 days

Patients who are on hemodialysis, use of the drug beginning with a dose of 300-400 mg, and then the drug is used in maintenance dose of 200-300 mg after approximately 4-hour hemodialysis. In the days of free dialysis drug does not accept.

Patients with poor general condition, low body weight or organ transplant patients after increasing doses of the drug should be made gradually with doses of 100 mg.

Side effect

From the side of the central nervous system and peripheral nervous system: drowsiness, dizziness, ataxia, nystagmus (dose-dependent), fatigue, tremor, dysarthria, increased nervous irritability; rare - headache, amnesia, depression, and very rarely - thought disorder, confusion, tics, paresthesia (dose dependent), asthenia, malaise, hyperkinesia, increased, hypo-or arefleksiya, anxiety, hostility, insomnia (for appointment, together with other antiepileptic drugs).

From the senses: visual disturbances (diplopia, amblyopia), ringing in the ears.

Since the cardiovascular system: the symptoms of vasodilation, increased blood pressure (when applied in conjunction with other antiepileptic drugs).

On the part of the respiratory system: rarely - rhinitis, pharyngitis, cough, pneumonia (in the appointment, together with other antiepileptic drugs).

On the part of the digestive system: dyspepsia, flatulence, anorexia, gingivitis (for appointment, together with other antiepileptic drugs) are rarely - nausea, vomiting, abdominal pain, increased appetite, and very rarely - dry mouth or throat, constipation or diarrhea, pancreatitis, increase in liver transaminases.

On the part of the musculoskeletal system: rarely - myalgia, arthralgia, back pain (in the appointment, together with other antiepileptic drugs) are very rarely - increased brittleness of the bones (in the appointment, together with other antiepileptic drugs).

On the part of the genitourinary system: very rarely - urinary incontinence, lower potency, urinary tract infection.

On the part of the hemopoietic system: very rarely - leukopenia.

Dermatological reactions: very rare - rash, itching, fever, erythema multiforme exudative (including Stevens-Johnson syndrome), acne.

From the laboratory parameters: a very rare - fluctuations in the level of glucose in the blood plasma of patients with diabetes mellitus.

Other: purpura, weight gain, very rarely - peripheral edema, discoloration of the enamel of teeth, swelling of the face.

Contraindications
acute pancreatitis;
Children under 3 years;
Hypersensitivity to gabapentin.

Pregnancy and lactation Gabagamma 

Use of the drug during pregnancy is only possible if the intended benefits to the mother outweighs the potential risk to the fetus. In applying the drug during pregnancy may slow fetal growth (in excess of therapeutic dose of 3.6 g in terms of mg/m2).

Gabapentin is excreted in breast milk. Effect on newborn babies has been studied, so the application Gabagammy during lactation (breastfeeding) is possible only when the intended benefits to the mother outweighs the potential risk to the newborn.

Application for violations of renal function

Patients with impaired renal function is recommended to adjust the dosing regimen.

Cautions 

If necessary, discontinuation of the drug or its replacement by an alternative dose should be reduced gradually over a period of at least 1 week.

It should be borne in mind that it is ineffective for the treatment of small epileptic seizures.

Patients should be warned about the fact that the appearance of adult drowsiness, ataxia, dizziness, fatigue, nausea and / or vomiting, weight gain, and the children - somnolence, hyperkinesia and hostility should immediately stop taking the drug and consult your doctor.

Effects on ability to drive vehicles and management mechanisms

During the period of the drug must be careful when driving and busy with other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Overdose Gabagamma 

Symptoms: dizziness, diarrhea, diplopia, speech impairment, drowsiness, lethargy.

Treatment: symptomatic, hemodialysis (chronic renal failure, severe).

Drug Interactions

If necessary, be used together with other antiepileptic drugs (phenytoin, carbamazepine, valproic acid, phenobarbital), with oral contraceptive drugs (containing noretindron and / or ethinylestradiol); drugs that block tubular secretion (reduced excretion of gabapentin by the kidneys).

When applied simultaneously with antacids (containing aluminum ions and magnesium) reduced bioavailability Gabagammy approximately 20%. If you want to use this combination Gabagammu should be taken 2 hours after taking an antacid.

At simultaneous application with myelotoxic drugs increases gematotoksichnoe action (leukopenia).

Terms and Conditions of storage

The drug should be stored out of reach of children at or above 25 ° C.

Shelf life - 2 years.

The drug should not be used after the expiration date