🐾 Peksion tablets, 100 mg 100 pcs.

Pharmacotherapeutic group: antiepileptic drugs.

The constituent imepitoin (1,4-chlorophenyl-4-morpholino-imidazol-2-one) belongs to the group of antiepileptic (anticonvulsant) compounds of central action, which penetrates through the blood-brain barrier without involvement in active transport or active excretion, which leads to rapid equilibration of its concentration in plasma and brain cells.

Imepitoin inhibits seizures through potentiation of GABA (GABAa) receptor-mediator effects on neurons. It also has low efficacy in blocking calcium channels, which may contribute to the anticonvulsant properties of the drug.

Imepitoin has a weak anxiolytic (suppressing fear, anxiety) effect.

Decrease or absence of antiepileptic effect has not been observed with prolonged treatment with Peksios for 6 months.

Absorption

Pharmacokinetic studies indicate that imepitoin is well (>92%) absorbed after oral administration, and thus a rapid initial effect is achieved. After oral administration of a 30 mg/kg tablet of imepitoin on an empty stomach, its blood concentration peaks rapidly after about 2 hours (Ttah) to a value of 18 µg/ml (Stah)-Application of imepitoin tablets with food reduces the blood concentration by 30%, but does not result in a significant change in Ttah and Stah. No particular sex differences were found.

Distribution

The linearity appears over the range of therapeutic doses of imepitoin.

Imepitoin has a relatively high volume of distribution (579 to 1548 ml/kg). Binding of imepitoin to plasma proteins in vivo is only 60-70%. Accumulation of imepitoin in plasma does not occur after reaching a stable concentration.

Metabolism

Imepitoin is actively metabolized to elimination. Four major inactive metabolites have been identified in the urine and feces, which are formed by oxidative modification.

Emepitoin is rapidly excreted from the blood (260 to 568 ml/hr/kg) with a half-life of approximately 1.5 to 2 hours. The bulk of imepitoin and its metabolites are excreted through the feces rather than the urine, so one should not expect large deviations in pharmacokinetics and accumulation of the drug in dogs with urinary dysfunction.

Pexion refers to moderately hazardous substances according to the degree of impact on the body (3rd class of hazard according to GOST 12.1.007-76).

Indications

Composition

The active ingredient imipitoin – 100 mg

Auxiliary substances: lactose monohydrate, microcrystalline cellulose, hypromellose, magnesium stearate, sodium starch glycolate.

Directions for use

Pexion is administered to dogs after a physician has confirmed the diagnosis of “idiopathic epilepsy”, orally twice daily at 12-hour intervals, at the same time of day, at an initial single dose of 10 mg imipitoin per 1 kg of body weight of the animal (see table).

The single dose (number of tablets per administration) at the beginning of use of Peksion:

Animal weight (kg)

Number of tablets

Tablet 100 mg

Tablet 400 mg

Special Instructions

There is no information about incompatibility of Peksion with drugs of other pharmacological groups.

Pexion is not intended for use in productive animals.

Contraindications

Contraindications for use is individual hypersensitivity of the animal to the components of the drug (including anamnesis), expressed renal dysfunction, liver, cardiovascular system, gastrointestinal tract. Do not use Peksion in breeding males, animals weighing less than 5 kg.

The drug is not recommended for use in epileptic status (status epilepticus) and cluster epileptic seizures.

Side effects

When using the drug in accordance with these instructions in rare cases the following may occur: polyphagia (at the beginning of treatment), polyuria, lethargy, ataxia, tremor, vomiting and/or diarrhea, somnolence, hypersalivation, ataxia, apathy, third eyelid loss, impaired vision, increased auditory sensitivity.

In dogs with epilepsy, there may be increased aggressiveness immediately after a seizure, as well as behavioral changes that accompany epilepsy.

Pexion use, like other anxiolytic drugs acting on benzodiazepine receptors, may lead to fear, which in turn contributes to increased or decreased aggressiveness in behavior.