Pramipexole Hydrochloride Extended Release Tablets

Pharmacological effects Pramipexole is a non-ergot dopamine agonist. In vitro studies have shown that pramipexole has a high specificity for D2 receptors and has pure intrinsic activity, and has a higher affinity for D3 receptors than D2 and D4 receptors. The relevance of this combined effect of pramipexole and D3 receptors to Parkinson's disease is unclear. The exact mechanism of pramipexole in the treatment of Parkinson's disease is still unclear, and it is currently believed to be related to the capture of dopamine receptors in the striatum. Animal electrophysiological tests have shown that pramipexole can affect the discharge frequency of striatal neurons by capturing dopamine receptors in the striatum and substantia nigra. Toxicological studies Genetic toxicity Pramipexole Bmes test, HGRRTV79 gene mutation test, DHO cell chromosome aberration test, and mouse micronucleus test results were all negative. In reproductive toxicity fertility experiments, rats were given 2.5 mg/kg/day of pramipexole (calculated by mg/m2, equivalent to 5.4 times the maximum recommended human dose (1.5 mg, tid)). It was observed that the estrous cycle was prolonged and the implantation rate decreased, which may be related to the decrease in serum prolactin levels caused by pramipexole (in early pregnancy of rats, prolactin is required for embryo implantation and maintenance, while rabbits and humans do not need it). Pregnant rats were given 1.5 mg/kg/day of pramipexole during the teratogenic sensitive period (calculated by plasma BUD, equivalent to 4.3 times the BUD at the maximum recommended human dose), and the total receptive fetal birth rate increased, which may be related to the decrease in serum prolactin levels caused by pramipexole. Pregnant rabbits were given 10 mg/kg/day of pramipexole during the teratogenic sensitive period (plasma BUD was 71 times the BUD at the maximum recommended human dose), and no abnormalities were observed. Pregnant rats were given 0.5 mg/kg/day of pramipexole (equivalent to the maximum clinically recommended dose for humans calculated on mg/m2) or higher doses during the perinatal period, and the offspring rats did not suffer adverse effects after birth. Carcinogenic mice and rats were given pramipexole 0.3, 2, 10 mg/kg/day (equivalent to 0.3, 2.2 and 11 times the maximum recommended dose for humans calculated on mg/m2) or 0.3, 2, 8 mg/kg/day (equivalent to 0.3, 2.5 and 12.5 times the maximum recommended dose for humans calculated on plasma BUD) by dietary administration, and no increase in tumor incidence was observed.

Pramipexole hydrochloride.

This product is white round tablets.

No data yet

Oral medication, swallow with water, with or without food. Three times a day. Initial treatment: The starting dose is 0.375 mg per day, and then increase the dose every 5-7 days. If the patient can tolerate it, the dose should be increased to achieve the maximum effect. Weekly dose (mg) Total daily dose (mg) 13×0.1250.37523×0.250.7533×0.51.50 If the dose needs to be further increased, it should be increased once a week in weeks, with each daily dose increased by 0.75 mg, and the maximum daily dose is 4.5 mg.

Based on the pooled placebo-controlled trials, which included 1351 patients taking this product and 1131 patients taking placebo, the analysis showed that adverse events occurred frequently in both groups. 88% of patients taking this product and 83.6% of patients taking placebo reported at least one adverse event. The incidence of drowsiness increases when the daily dose of this product is higher than 1.5 mg (see [Dosage and Administration]). The most common adverse reaction when used in combination with levodopa is dyskinesia. Constipation, nausea and dyskinesia often disappear gradually with treatment. Hypotension may occur in the early stages of treatment, especially when the dose of this product is increased too quickly. The following are adverse drug reactions that occurred with this product in placebo-controlled trials (numbers are higher than placebo): Mental disorders: Common (1%-10%): Insomnia, hallucinations, confusion Neurological abnormalities: Common (1%-10%): Dizziness, movement disorders, somnolence (see below) Vascular abnormalities: Uncommon (0.1%-1%): Hypotension Gastrointestinal abnormalities: Common (1%-10%): Nausea, constipation Systemic abnormalities: Common (1%-10%): Peripheral edema This product is associated with somnolence and occasional excessive daytime sleepiness and sudden sleep attacks. This product may be associated with abnormal libido (increase or decrease).

Allergic to pramipexole or any other ingredient in the product.

Precautions for children: Not yet known. Precautions for pregnancy and lactation: The effects of pramipexole on human pregnancy and lactation have not been studied. It is not teratogenic in rats and rabbits, but it is toxic to rat embryos at maternally toxic doses (see Toxicological Studies). This product is contraindicated during pregnancy unless absolutely necessary, for example, when the potential benefit to the fetus outweighs the risk. Because this product inhibits the secretion of human prolactin, it inhibits lactation. Whether this product can be secreted into women's breast milk has not been studied. The intensity of drug-related emissions in rat milk is higher than that in plasma. Due to the lack of human body values, this product should be used as little as possible during lactation. However, if its use is unavoidable, breastfeeding should be discontinued. Precautions for the elderly: Not yet known.

Pramipexole is only minimally bound to plasma proteins (less than 20%) and undergoes little biotransformation in men. Therefore, pramipexole is unlikely to interact with other drugs that affect plasma protein binding and is unlikely to be eliminated by biotransformation. Since anticholinergics are primarily eliminated by biotransformation, although interactions between pramipexole and anticholinergics have not been studied, the likelihood of such interactions is expected to be very limited. Pramipexole did not interact pharmacokinetically with selegiline and levodopa. Cimetidine can reduce the renal clearance of pramipexole by approximately 34%, probably through inhibition of the renal tubular cation secretion transport system. Therefore, drugs that inhibit this active renal elimination pathway or are eliminated by this pathway are more likely to be eliminated by the kidneys.

Store at room temperature, tightly closed.

0.75 mg

36 months