Pregabalin Capsules

Pregabalin has a high affinity for the α2-δ site (an auxiliary subunit of voltage-gated calcium channels) in the central nervous system. The mechanism of action of pregabalin is still unclear, but results from studies of transgenic mice and structurally related compounds (such as gabapentin) suggest that the analgesic and anticonvulsant effects in animal models may be related to the binding of pregabalin to the α2-δ subunit. In vitro studies have shown that pregabalin may reduce the calcium-dependent release of some neurotransmitters by regulating calcium channel function. Although pregabalin is a structural derivative of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), it does not directly bind to GABAA, GABAB or benzodiazepine receptors, does not increase the GABAA response of cultured neurons in vitro, does not change the GABA concentration in rat brain, and has no acute effect on GABA uptake or degradation. However, studies have found that prolonged exposure of cultured neurons to pregabalin increased the density of GABA transporters and the rate of functional GABA transport. Pregabalin does not block sodium channels, has no activity at opioid receptors, does not alter cyclooxygenase activity, has no activity at dopamine and 5-hydroxytryptamine receptors, and does not inhibit the reuptake of dopamine, 5-hydroxytryptamine, or norepinephrine.

Pregabalin

1. Generalized anxiety disorder. 2. Diabetic peripheral neuropathy. 3. Postherpetic neuralgia. 4. Fibromyalgia syndrome. 5. Adjunctive treatment of epilepsy.

This product can be taken with food or alone. The recommended dose of this product is 75 or 150 mg twice a day; or 50 mg or 100 mg three times a day. The starting dose can be 75 mg twice a day; or 50 mg three times a day. It can be increased to 150 mg twice a day within 1 week based on efficacy and tolerability. Since this product is mainly excreted by the kidneys, patients with impaired renal function should adjust the dose. The above recommended doses are suitable for patients with creatinine clearance ≥ 60 ml/min. Patients who take 300 mg/day of this product and whose pain is not adequately relieved after 2-4 weeks, if they can tolerate this product, can increase to 300 mg twice a day, or 200 mg three times a day (600 mg/day). Since adverse reactions are dose-dependent and adverse reactions can lead to higher discontinuation rates, doses exceeding 300 mg/day should only be used for patients with persistent pain who can tolerate a dose of 300 mg/day. If pregabalin needs to be discontinued, it is recommended to taper off the drug over at least 1 week.

The main symptoms are dizziness, drowsiness, ataxia, confusion, fatigue, abnormal thinking, blurred vision, movement disorder, dry mouth, edema, weight gain and abnormal thinking (mainly difficulty concentrating/attention). See product instructions.

This product is contraindicated for use by those who are allergic to the active ingredients or any excipients contained in it.

Since pregabalin is mainly excreted in the urine as unchanged drug, its metabolism in humans can be ignored (less than 2% of the administered dose of drug metabolites were found in the urine). In vitro studies have shown that pregabalin does not inhibit drug metabolism, nor does it bind to plasma proteins, and pregabalin has almost no pharmacokinetic interactions with other drugs. Similarly, no clinically relevant pharmacokinetic interactions between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol were observed in animal studies. Population pharmacokinetic analysis showed that oral antidiabetic drugs, diuretics, insulin, phenobarbital, tiagabine and topiramate had no significant clinical effect on the clearance of pregabalin. When pregabalin was taken with the oral contraceptives norethindrone and/or ethinyl estradiol, the steady-state pharmacokinetics of both substances were not affected. Pregabalin may enhance the effects of ethanol and lorazepam. In controlled clinical studies, when multiple oral doses of pregabalin were combined with oxycodone, lorazepam, or ethanol, no clinically significant effects on the patient's respiration were observed. Post-marketing reports of respiratory failure and coma have been reported with the combination of pregabalin and centrally acting antidepressants. Pregabalin can enhance cognitive dysfunction and overall motor dysfunction caused by oxycodone. Drug interaction studies have only been conducted in adults, not specifically in elderly volunteers.

Keep sealed.

50 mg