Eplorontin - instructions for use, dose, side effects, contraindications

capsular shell: gelatin - 63.25 mg, purified water 11.02 mg, methyl parahydroxybenzoate 0.61 mg, propyl parahydroxybenzoate 0.15 mg, azorubin dye 0.23 mg, crimson dye [Ponso 4R] - 0.30 mg, titanium dioxide - 0.38 mg, sodium lauryl sulfate - 0.06 mg;

Description:

Hard gelatin capsules, body and lid of dark red color, size 1; the contents of the capsules are white powder.

Pharmacotherapeutic group:Antiepileptic remedy

ATX: & nbsp

N.03.A.X.12 Gabapentin

Pharmacodynamics:

Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs interacting with GABA receptors (valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture inhibitors, GABA agonists and prodrugs of GABA ). It does not possess GABA-ergic properties and does not affect the capture and metabolism of GABA. Preliminary studies have shown that gabapentin binds to α₂-δ-subunit of voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms of action of gabapentin in neuropathic pain are a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, a suppression of the release of neurotransmitters of the monoamine group. Gabapentin in clinically significant concentrations does not bind to receptors of other common drugs or neurotransmitters, including GABA receptors_A, GABA_at, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate. 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 tests in vitro, but only at a concentration of more than 100 μmol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.

Pharmacokinetics:

The bioavailability of gabapentin is not proportional to the dose. So, with an increase in the dose, it decreases. After oral administration, the maximum concentration (C_max) gabapentin in plasma is achieved after 2-3 hours. Absolute bioavailability of gabapentin in capsules is about 60%. Food, including those with a high fat content, does not affect the pharmacokinetics. The elimination of gabapentin from plasma is best described using a linear model. The half-life (T₁_/₂) from the plasma does not depend on the dose and averages 5-7 hours.

Pharmacokinetics does not change with repeated application; equilibrium concentrations 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 volume distribution of 57.7 liters. It is excreted exclusively by the kidneys in unchanged form, it is not metabolized. The drug does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs.

The clearance of gabapentin from plasma decreases in elderly people and in patients with impaired renal function. The rate of elimination constant, clearance from plasma and renal clearance are directly proportional to the creatinine clearance.

Gabapentin is removed from the plasma during hemodialysis.

In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended (see "Method of administration and dose").

Indications:

- Monotherapy or as an additional agent for the treatment of partial seizures with secondary generalization or without it in adults and children from the age of 12;

- Neuropathic pain in adults (18 years and older).

Contraindications:

- Hypersensitivity to any of the components of the drug:

- age to 12 years (due to the impossibility of accurate dosing).

Carefully:

Renal failure (see "Method of administration and dose").

Pregnancy and lactation:

There are no data on the use of the drug in pregnant women, so gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus.

Gabapentin is excreted in breast milk, its influence on the infant is unknown, so during treatment should abandon breastfeeding.

Dosing and Administration:

Inside, swallowing whole, regardless of food intake and plenty of liquids. If it is necessary to reduce the dose, cancel the drug or replace it with an alternative remedy, this should be done gradually for at least one week.

Neuropathic pain in adults

The initial daily dose is 900 mg divided into three doses; if necessary, the dose is gradually increased to a maximum of 3600 mg / day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or within the first 3 days the dose can be increased gradually to 900 mg per day according to the following scheme:

Day 1:	300 mg once a day
Day 2:	300 mg twice a day
Day 3:	300 mg 3 times a day

Partial cramps

Adults and children from 12 years old: Effective dose is from 900 to 2400 mg / day. Therapy can begin with a dose of 300 mg 3 times a day on the first day or increase gradually to 900 mg according to the scheme described above (see the section "Neuropathic pain in adults"). Subsequently, the dose can be increased to a maximum of 3600 mg / day (divided into 3 equal doses). Maximum interval Between doses, with a three-time intake of the drug should not exceed 12 hours in order to avoid the resumption of seizures.

Selection of a dose for renal failure

Patients with renal failure are recommended to reduce the dose of gabapentin according to the table:

Creatinine clearance (ml / min)	Daily dose (mg / day)
>80	900-2400
50-79	600-1200
30-49	300-600
15-29	150*-300
<15	150*

* appoint 300 mg every other day.

Recommendations for patients on hemodialysis

Patients on hemodialysis who had not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it at 200-300 mg every 4 hours of hemodialysis.

Side effects:

The cardiovascular system: symptoms of vasodilation or increased blood pressure, palpitations.

The digestive tract: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental diseases, diarrhea, dyspepsia, increased appetite, dryness in mouth or pharynx, nausea, vomiting, pancreatitis, increased activity of "liver" transaminases, hepatitis, jaundice, pancreatitis.

System of blood, lymphatic system: purpura (most often it is described as bruising that occurs during physical trauma), leukopenia, thrombocytopenia.

Musculoskeletal system: arthralgia, back pain, increased brittle bones, myalgia.

Nervous system: dizziness; headache; hyperkinesis; muscular dyskinesia and dystonia; choreoathetosis; amplification, attenuation or absence of reflexes; dysarthria; ataxia; nystagmus; paresthesia; convulsions; tremor; confusion of consciousness; increased fatigue; asthenia; amnesia; depression; violation of thinking; hostility; emotional lability; insomnia; anxiety; drowsiness; hallucinations.

Respiratory system: pneumonia, bronchitis, dyspnea, respiratory infections, cough, pharyngitis, rhinitis.

Allergic reactions: acne, skin itching, skin rash, peripheral edema, fever, multiforme exudative erythema (including Stevens-Johnson syndrome).

Genitourinary system: urinary tract infection, impotence, urinary incontinence, acute renal failure.

Sense organs: visual impairment, amblyopia, diplopia, tinnitus, otitis media.

Other: fever, viral infection, weight gain, lability of glucose level in blood plasma in diabetic patients, pain of different localization, discoloration of tooth enamel.

Overdose:

Symptoms: dizziness, diplopia, speech impairment, drowsiness, lethargy, diarrhea and increased severity of other side effects.

Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. Patients with severe renal insufficiency can be shown hemodialysis.

Interaction:

Morphine: with the joint administration of gabapentin and morphine, when morphine was taken 2 hours before taking gabapentin, there was an increase in the average area under the pharmacokinetic curve "concentration-time" (AUC) gabapentin by 44% compared with gabapentin alone, 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 remain unchanged.The side effects of morphine when taken together with gabapentin did not differ from those when taking morphine together with placebo.

The interactions between gabapentin and phenobarbital, phenytoin, valproic acid, and carbamazepine not noted. The pharmacokinetics of gabapentin in the equilibrium state is the same in healthy people and patients receiving other anticonvulsants.

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

The simultaneous use of gabapentin with antacids containing aluminum and magnesium, is accompanied by a decrease in bioavailability of gabapentin by about 20%. Gabapentin it is recommended to take about 2 hours after taking an antacid.

Probenecid does not affect renal excretion of gabapentin.

A slight decrease in renal excretion of gabapentin with simultaneous admission cimetidine, probably, has no clinical significance.

Myelotoxic drugs cause increased hematotoxicity (leukopenia).

Special instructions:

Although withdrawal syndrome with the development of seizures in the treatment of gabapentin is not noted, nevertheless, a sharp cessation of PEP therapy in patients with partial seizures can provoke the development of seizures (see "Method of administration and dose").

GABAPENTIN is not considered an effective treatment for absence-epilepsy.

Patients who require co-therapy with morphine may require an increase in the dose of gabapentin. In this case, it is necessary to ensure close monitoring of patients for the development of such a sign of central nervous system (CNS) depression as drowsiness. In this case, the dose of gabapentin or morphine should be adequately reduced (see "Interaction with other drugs").

Laboratory research

When gabapentin was added to other anticonvulsants, false positive results were detected in determining the protein in the urine using test strips Ames N-Multistix SG®. To determine the protein in the urine it is recommended to use a more specific method of precipitation with sulfosalicylic acid.

In the case of adult drowsiness, ataxia, dizziness, increased fatigue, nausea and / or vomiting,increase in body weight, and in children drowsiness, hyperkinesia and hostility should stop treatment and consult with a doctor.

Effect on the ability to drive transp. cf. and fur:

Patients should avoid driving, as well as performing work that requires quickness in performing psychomotor reactions.

Form release / dosage:

Capsules, 300 mg.

Packaging:

10 capsules per blister of aluminum / aluminum.

For 3 or 10 blisters together with instructions for use in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005318/08

Date of registration:07.07.2008

Expiration Date:Unlimited

Date of cancellation:2018-02-01

The owner of the registration certificate:Micro Labs LimitedMicro Labs Limited India

Manufacturer: & nbsp

MICRO LABS, Limited India

Representation: & nbspMICRO LABS LIMITED MICRO LABS LIMITED India

Information update date: & nbsp01.02.2018

Illustrated instructions

Instructions

Eplerontin (Eplyrontin)