GabaFix 2.5 mg

INDICATIONS

Mirogabalin Besylate tablet is indicated for the treatment of-

Neuropathic Pain
Diabetic peripheral neuropathic pain (DPNP)
Postherpetic neuralgia (PHN)
Peripheral neuropathic pain (PNP)

PHARMACOLOGY

Mirogabalin belongs to the class of gamma amino acids and its derivatives. Mirogabalin selectively binds α2δ subunits of voltage-gated calcium channels (VGCCs). It reduces calcium (Ca2+) influx and neurotransmission which inhibits neurotransmitter release in presynaptic neuron endings. Due to the inhibition of neurotransmitter release, the hyper- excitability of central nervous system (CNS) neurons decreases.Mirogabalin is rapidly absorbed after oral administration; median time to maximum plasma concentration is 0.5-1.5h. Mirogabalin has a low plasma protein binding of approximately 25%. Mirogabalin has a mean apparent volume of distribution of 64-88L after single or multiple doses. The drug is cleared mainly unchanged (61-72%) via renal excretion by filtration and active secretion, however a slight fraction (13-20%) is metabolized by hepatic uridine 5'-diphospho-glucuronosyltransferase isoforms. The mean elimination half-life of mirogabalin observed 2-4.9h. 99% of mirogabalin is excreted through the kidneys, only 1% of the dose is excreted through feces.

DOSAGE & ADMINISTRATION

Adult dose: The initial dose for adults is 5 mg of Mirogabalin twice daily. Then the dose is gradually increased by 5 mg at an interval of at least a week to 15 mg twice daily. The dose may be adjusted appropriately between 10 mg and 15 mg twice daily depending on ages and symptoms.Use in Children and Adolescent: It is not known if Mirogabalin is safe and effective in children and adolescent.Hepatic Impairment: A single 15 mg dose of Mirogabalin does not produce significant adverse reaction, in patients with mild to moderate hepatic impairment. No data available for severe hepatic impairment.Renal Impairment: In mild renal dysfunction, the initial dose starts from 5 mg twice a day, slowly increased by 5 mg at an interval of 1 week to 10 mg. In moderate renal dysfunction, the initial dose starts from 2.5 mg twice a day, slowly increased by 2.5 mg at an interval of 1 week to 7.5 mg twice a day. In severe renal dysfunction, the initial dose starts from 2.5 mg once a day, slowly increased by 2.5 mg at an interval of 1 week to 7.5 mg once a day.

INTERACTION

With Medicine: Co-administration of Mirogabalin with Cimetidine or Probenecid may raise the Mirogabalin plasma concentration. Importantly, if Mirogabalin is taken with Lorazepam, the depressive effects on the CNS may be potentiated. Mirogabalin is OAT1, OAT3, OCT2, MATE1, MATE2-K and UGT substrate. Mirogabalin does not inhibit or induce major human CYP molecular species, and does not inhibit activities of drug transporters (including OAT1, OAT3, organic cation transporter OCT1, OCT2, OATP1B1, OATP1B3, MATE1, MATE2-K, P-gp and BCRP). Co-administrated with OAT1, OAT3, OCT2, MATE1, MATE2-K or UGT inhibitors may increase mirogabalin exposure, so use with caution.With food & others: Administration of Mirogabalin with food has no clinically relevant effect on the total absorption of Mirogabalin. Avoid consuming alcohol while taking Mirogabalin, as Mirogabalin may potentiate the impairment of motor skills and sedating effects of alcohol.

SIDE EFFECTS

The most reported adverse reactions include somnolence, dizziness, edema and weight gain. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.

Light headedness, state close to sleep with impaired consciousness, loss of consciousness (dizziness, somnolence, unconsciousness).
General malaise, loss of appetite, nausea, vomiting, jaundice (liver dysfunction).

PREGNANCY & LACTATION

For pregnant or potentially pregnant women, administer only if the therapeutic benefit outweighs the risks. Presence in placental passage has been reported in animal study. Consider the therapeutic and breastfeeding benefits then consider continuing or discontinuing breastfeeding. It has been reported in animal study that it is transferred into milk.

PRECAUTIONS & WARNINGS

This medicine may cause dizziness, somnolence, or loss of consciousness. Avoid operating dangerous machinery, such as driving a car. Especially for elderly patients, careful attention should be taken. This medicine may cause weight gain. This medicine may cause blurred vision and double vision.If an allergic reaction occurs, stop taking the medicine and consult with doctor. Dose adjustment is needed in patients with renal dysfunction. If taking any other medication, please consult with doctor before administering Mirogabalin. As this medicine may cause dizziness or somnolence, the patient should avoid operating in potentially hazardous activities such as driving a car. Elderly patients should be aware of falling and fracture. The patient should consult with the doctor if the signs of blurred vision or double vision appear while taking this medication.

THERAPEUTIC CLASS

Adjunct anti-epileptic drugs, Primary anti-epileptic drugs

STORAGE CONDITIONS

Store at below 30°C and dry place, away from light and moisture. Keep out of the reach of children.