GABAPENTIN (oral solution)

Clear, colourless to light yellow solution.

1 ml of the product contains the active substance:

- gabapentin – 50 mg.

Excipients: sodium benzoate, sucralose, disodium edetate, flavour, purified water.

ATCvet code: QN02 – veterinary medicinal products acting on the nervous system. Analgesics. QN02BF01 – Gabapentin.

GABAPENTIN oral solution is an anticonvulsant and analgesic product used for the treatment of pain, seizures and anxiety in dogs and cats.

Gabapentin (1-aminomethylcyclohexaneacetic acid) is a structural analogue of the neurotransmitter γ-aminobutyric acid (GABA); however, its mechanism of action differs substantially from that of classical GABA-ergic medicinal products.

Gabapentin does not alter GABA metabolism and has no affinity for GABA-A or GABA-B receptors. It does not bind to other neurotransmitter receptors in the brain and does not interact with sodium channels.

The principal mechanism of action of gabapentin is related to its selective interaction with the α₂δ (alpha2-delta) subunit of voltage-gated calcium channels in presynaptic neurons of the central nervous system, which produces an anticonvulsant effect in animals and reduces the release of excitatory neurotransmitters (glutamate, substance P, noradrenaline) in various regions of the central nervous system. This, in turn, decreases neuronal hyperactivity and central sensitisation characteristic of neuropathic pain and anxiety states. Extensive screening studies have shown that gabapentin does not bind to any targets other than α2-δ.

Gabapentin has anticonvulsant properties, making it a useful adjunctive therapy for animals with refractory seizures or those whose current treatment regimen is no longer sufficiently effective.

Gabapentin can be used to reduce anxiety in animals in general, and in particular in cases of fear of thunderstorms, explosions or fireworks, as well as in situations of stress associated with transport, veterinary visits or grooming. It reduces the release of excitatory neurotransmitters in the brain, which prevents the escalation of anxiety and provides the animal with a sense of calm.

Gabapentin exerts an analgesic effect both at the level of the spinal cord and in higher brain centres. Its mechanism of action is associated with a reduction in neuronal death and inhibition of the release of monoamine-group neurotransmitters. This makes gabapentin effective in relieving chronic and neuropathic pain. It is most frequently used for chronic pain syndrome caused by degenerative joint pathologies, including arthritis, and for neuralgia. In addition, it demonstrates a synergistic effect when combined with other analgesics – non-steroidal anti-inflammatory drugs (NSAIDs) and opioids – enhancing the effectiveness of pain control associated with surgical procedures.

After oral administration to dogs and cats at a dose of 10–20 mg of gabapentin per 1 kg body weight, maximum plasma concentration is reached after 2–3 hours. The elimination half-life in dogs and cats is 6–8 hours. The absolute bioavailability of gabapentin is approximately 60%. Food intake does not affect the pharmacokinetics of gabapentin. The pharmacokinetics do not change with repeated administration.

Gabapentin is practically not bound to plasma proteins and is excreted by the kidneys unchanged; it is not metabolised in the body of cats, while in dogs it is partially metabolised in the liver. Plasma clearance of gabapentin is reduced in elderly animals and in animals with impaired renal function. The elimination rate constant, plasma clearance and renal clearance are directly proportional to creatinine clearance.

For use in cats and dogs for the prevention and mitigation of stress, management of behavioural disorders, alleviation of acute anxiety (including during veterinary visits, diagnostic procedures, transportation, and grooming), as well as for the management of pain syndrome and behavioural modification.

– for pain syndrome, the dose for dogs and cats is 0,1–0,3 ml of the product (equivalent to 5–15 mg of gabapentin) per 1 kg body weight, 2–3 times daily.

Frequent administration at low doses maintains minimal target plasma concentrations of gabapentin in dogs and cats, since gabapentin is rapidly absorbed and eliminated.

The recommended duration of treatment is up to 14 days; further use in animals should be based on an individual benefit–risk assessment by a veterinarian.

– for the prevention of stress and behavioural correction in animals (transportation, grooming, veterinary visits, diagnostic examinations, loud noises, other phobias), the following single doses are recommended 60–90 minutes before the planned event:

cats – 0,2–0,6 ml of the product (equivalent to 10–30 mg of active substance) per 1 kg body weight;

dogs – 0.4–1.2 ml of the product (equivalent to 20–60 mg of active substance) per 1 kg body weight.

For the prevention of stress in dogs, this product is not the first-choice medicinal product and is less effective than in cats.

Do not administer doses exceeding 100 mg of gabapentin per 1 kg body weight (no more than 2 ml of the product per 1 kg body weight).

The dose may vary depending on the animal's temperament, degree of excitability, age, and body weight. It is recommended to start treatment with an average dose and to select an individual dose for each animal (until a mild sedative effect is achieved), taking into account the animal's response and individual sensitivity.

The duration of action of the product is 8–12 hours. Lethargy and impaired coordination of movement may be observed, which resolve once the effect has worn off.

The product may be used as part of combination therapy with other pathogenetic agents. Disruption of the administration schedule should be avoided, as this may reduce therapeutic efficacy.

After each use, the oral dosing syringe must be rinsed with water and dried.

Do not use in cases of hypersensitivity to the active substance or to any of the excipients.

Do not use in animals with severe renal or hepatic impairment.

Do not use in pregnant or lactating animals.

Do not use in food-producing animals.

When the veterinary medicinal product is used in accordance with the package leaflet, adverse events are not generally observed.

In some animals, particularly cats, increased salivation may occur, which resolves spontaneously without the need for medicinal treatment. In cats, increased appetite may be observed. In rare cases, in animals with hypersensitivity to the components of the product, neurological effects may occur: muscle tremor, seizures, depression, vomiting and gastrointestinal disturbances.

Do not use without a veterinarian's prescription.

Use the product in accordance with the package leaflet.

The recommended doses must be observed.

GABAPENTIN solution should be administered with caution to animals with renal insufficiency, taking into account possible risks and adjusting the dosage or frequency of administration accordingly.

After administration of an antacid containing aluminium and magnesium, the product should be administered 2 hours later.

If an animal has been receiving GABAPENTIN solution for a prolonged period (more than 14 days), the dose must be reduced gradually before complete discontinuation. The recommended discontinuation schedule for long-term use involves a gradual reduction in dosage over 7–14 days (usually by 25–50% every 3–5 days) under veterinary supervision, in order to avoid the risk of "rebound" pain or increased anxiety.

After administration of an antacid containing aluminium and magnesium, the product should be administered 2 hours later.

The product enhances the effect of non-steroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics in chronic and neuropathic pain. Concurrent use with opioids may result in increased plasma concentrations of gabapentin and a risk of CNS depression.

Concomitant use with central nervous system depressants (phenobarbital, antihistamines, tranquillisers) enhances the sedative effect and may cause pronounced drowsiness.

Standard personal hygiene practices must be observed when handling the veterinary medicinal product.

In the event of an overdose, the animal may present with depression, inappetence, drowsiness, lethargy, and gastrointestinal disturbances. In such cases, intestinal adsorbents and symptomatic treatment should be administered. In severely ill animals with severe renal insufficiency, haemodialysis may be indicated.

In the event of overdose, a veterinarian must be consulted immediately; the product packaging or package leaflet should be brought along.

In the event of overdose, treatment is symptomatic.

The recommended doses must be observed.

Polymer or glass bottles of 5, 10, 20, 30, 40, 50, 100 or 200 ml, supplied with a dosage syringe and package leaflet. Secondary packaging – cardboard box.

Store in a dry place, protected from light and out of reach of children and animals, at a temperature between 2 and 25 °C. Do not freeze. After first opening, store the product with the cap tightly closed in a refrigerator at a temperature between 6 and 10 °C.

2 years.

Shelf life after first opening of the bottle is 30 days.

Veterinary medicinal product subject to prescription.