Pregabalin Capsules
Function and Efficacy
Pregabalin has a high affinity for the alpha;2-delta; site (an auxiliary subunit of voltage-gated calcium channels) in the central nervous system. The mechanism of action of pregabalin is not clear, 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 alpha;2-delta; 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 gamma;-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 increases 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.
Ingredients
Pregabalin. Chemical name: (3S)-3-(aminomethyl)-5-methylhexanoic acid Molecular weight: C8H17NO2
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| PregabalinIngredients |
It has a high affinity for the alpha;2-delta; site (an auxiliary subunit of voltage-gated calcium channels) in the central nervous system and may reduce the calcium-dependent release of some neurotransmitters by regulating calcium channel function. Although it does not directly bind to GABAA, GABAB or benzodiazepine receptors, prolonged exposure to pregabalin can increase GABA transporter density and functional GABA transport rate. In addition, pregabalin does not block sodium channels, is inactive at opioid receptors, does not alter cyclooxygenase activity, is inactive at dopamine and serotonin receptors, and does not inhibit the reuptake of dopamine, serotonin or norepinephrine. More |
148553-50-8 | 92 |
Appearance
This product is a hard capsule, and the contents are white to off-white powder.
Indication
1. Generalized anxiety disorder; 2. Diabetic peripheral neuropathy; 3. Post-herpetic neuralgia; 4. Fibromyalgia syndrome; 5. Adjunctive treatment of epilepsy.
Usage and Dosage
Lyrica can be taken with or without food. The recommended dose of Lyrica is 75 or 150 mg twice a day, or 50 mg or 100 mg three times a day. The starting dose may 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 Lyrica is mainly excreted through the kidneys, the dose should be adjusted for patients with impaired renal function. The above recommended doses are for patients with creatinine clearance ≥60 ml/min. For patients who do not experience adequate pain relief after taking Lyrica 300 mg/day for 2-4 weeks, if they can tolerate Lyrica, the dose can be increased to 300 mg twice a day, or 200 mg three times a day (600 mg/day)
Adverse Reactions
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.
Precautions
This product is contraindicated for use by those who are allergic to the active ingredients or any excipients contained in it.
Special Population Medication
Precautions for children: Lyrica is not recommended for children younger than 12 years of age and adolescents (12-17 years) due to insufficient data on safety and efficacy in this population. Precautions for pregnancy and lactation: Insufficient data on the use of pregabalin in pregnant women. Animal studies have shown that Lyrica is reproductively toxic. The possible risks of Lyrica to humans are currently unknown. Lyrica should not be taken during pregnancy unless necessary (the benefits of taking the drug in pregnant women clearly outweigh the potential risks of the drug to the fetus). Women of childbearing age must use effective contraceptive measures. It is not known whether pregabalin is excreted in breast milk; however, Lyrica is excreted in the milk of rats. Therefore, breastfeeding is not recommended during treatment with pregabalin. Precautions for the elderly: Elderly patients (age 65 years and older) may need a dose reduction due to impaired renal function.
Drug Interactions
Since pregabalin is mainly excreted in the urine as unchanged drug, the metabolism of Lyrica 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 and does not bind to plasma proteins, and pregabalin has almost no pharmacokinetic interactions with other drugs. Similarly, no clinically relevant pharmacokinetic interactions were observed between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol in animal studies. Population pharmacokinetic analysis showed that oral antidiabetic drugs, diuretics, insulin, phenobarbital, tiagabine and topiramate had no clinically significant effect on the elimination of pregabalin. Pregabalin interacts with the oral contraceptives norethindrone and
Storage
Keep sealed.
Packaging Specification
150 mg
Validity Period
36 months