Pramipexole Hydrochloride Extended Release Tablets

Pharmacodynamic properties This product is a dopamine receptor agonist that binds to the dopamine receptor D2 subfamily with high selectivity and specificity, and has a preferential affinity for the D3 receptor therein; and has complete intrinsic activity. This product relieves movement disorders in patients with Parkinson's disease by exciting dopamine receptors in the striatum. Animal experiments have shown that this product inhibits the synthesis, release and renewal of dopamine. This product can protect dopamine neurons from degeneration caused by ischemia or methamphetamine neurotoxicity. In vitro studies have shown that this product can protect neurons from neurotoxicity caused by levodopa. Dose-dependent prolactin reduction was observed in volunteers. In a clinical trial of healthy volunteers, a faster-than-recommended method (from weekly to every three days) was used, and the dose was gradually increased to 4.5 mg/day, which showed an increase in blood pressure and heart rate. No such situation was found in the patient study. Preclinical safety data Repeated dose toxicity studies showed that the functional effects of this product, mainly involving the central nervous system of rats and the reproductive system of female mice, may be caused by the amplified pharmacodynamic effects of this product. Reductions in diastolic and systolic blood pressure and heart rate were observed in minipig studies, and a tendency towards hypotensive effects was observed in monkey studies. Studies in rats and rabbits have shown potential effects on reproductive function. The drug was not teratogenic in rats and rabbits, but was toxic to rat embryos at maternally toxic doses. The effects of the drug on pregnancy and female rat fertility have not been fully elucidated at present due to the drug's effect of reducing prolactin secretion and the specific effects of prolactin on female rat reproductive function. Sexual development (i.e., foreskin separation and vaginal opening) was delayed in rat studies. The effects on humans are unknown. The drug is not genotoxic. In a carcinogenicity study, male rats developed testicular Leydig cell hyperplasia and adenomas, which can be explained by the prolactin inhibition of the drug. However, this finding is not clinically relevant to male humans. The same study also showed that the drug was associated with retinal degeneration in rats at doses of 2 mg/kg and higher, but no similar findings were found in pigmented rats, 2-year-old mice, or other studied populations.

Main ingredients of this product: Pramipexole hydrochloride

This product is white or off-white tablets.

This product is used to treat the signs and symptoms of idiopathic Parkinson's disease in adults. That is, it can be used alone (without levodopa) or in combination with levodopa throughout the course of the disease, including in the later stages of the disease, when the efficacy of levodopa gradually decreases or changes and fluctuates (wearing-off phenomenon or "on-off" fluctuations).

All doses are calculated based on pramipexole hydrochloride monohydrate. Oral administration, once a day. Initial treatment: Starting dose: 0.375 mg daily as the starting dose, and then gradually increase the dose every 5 to 7 days. If the patient does not experience intolerable adverse reactions, the dose should be increased to achieve maximum efficacy. If further dose increases are required, they should be increased weekly, with each daily dose increased by 0.75 mg, and the maximum daily dose is 4.5 mg. It should be noted that the incidence of drowsiness increases when the daily dose is higher than 1.5 mg (see Adverse Reactions). Patients who have taken pramipexole hydrochloride tablets can switch to this product at the current daily treatment dose, with the same dose overnight. After switching to this product, the dose should be adjusted according to the patient's treatment response. (See Clinical Trials). Maintenance treatment: The individual dose should be between 0.375 mg and 4.5 mg per day. In the key study of dose escalation, drug efficacy was observed starting from a daily dose of 1.5 mg. Further dose adjustments should be made based on clinical response and the incidence of adverse reactions. In clinical trials, approximately 5% of patients took doses less than 1.5 mg per day. In patients with advanced Parkinson's disease, daily doses greater than 1.5 mg may be effective, and care should be taken to reduce the dose of levodopa. During the dose-up and maintenance phases of levodopa, it is recommended to reduce the dose of levodopa based on the individual response of the patient. Missed dose: When a dose is missed, levodopa should be taken within 12 hours of the usual medication time. If more than 12 hours have passed, the missed dose can be ignored and the next dose should be taken at the usual medication time the next day. Discontinuation of treatment: Abrupt discontinuation of dopaminergic therapy can lead to neuroleptic malignant syndrome. Therefore, levodopa should be gradually discontinued at a rate of 0.75 mg per day until the daily dose is reduced to 0.75 mg. Thereafter, it should be reduced by 0.375 mg per day. Dosage in patients with impaired renal function: The clearance of levodopa depends on renal function. The following dosage regimen is recommended for initial treatment: Patients with creatinine clearance greater than 50 ml/min do not need to reduce the daily dose or the number of doses. For patients with creatinine clearance between 30 and 50 ml/min, the initial daily dose of this product should be 0.375 mg every other day. After taking this product for one week, the response and tolerability of this product should be carefully evaluated before increasing the daily dose. If further dose increases are required, take this product in weekly increments of 0.375 mg, and the maximum daily dose cannot exceed 2.25 mg. This product is not recommended for patients with creatinine clearance less than 30 ml/min, and there is no supporting data for this patient population. In this case, consider taking pramipexole hydrochloride tablets. If renal function is reduced during the maintenance treatment phase, please follow the above recommendations. Dosage in patients with hepatic impairment: Dose adjustment may not be required for patients with hepatic failure, because approximately 90% of the absorbed active ingredient of the drug is excreted by the kidneys. However, the potential effect of hepatic insufficiency on the pharmacokinetics of this product has not been studied. Dosage: This product should be swallowed with water and should not be chewed, broken or crushed. This product can be taken with or without food. This product should be taken at the same time each day.

Expected adverse reactions The following adverse reactions are expected with this product: abnormal dreams, amnesia, symptoms of impulse control disorders and compulsive behaviors (such as binge eating, compulsive shopping, hypersexuality and pathological gambling), heart failure, confusion, constipation, hallucinations, dizziness, movement disorders, dyspnea, fatigue, hallucinations, headaches, hiccups, cramps, excessive eating, hypotension, antidiuretic hormone secretion disorders, insomnia, sexual desire disorders, nausea, paranoia, peripheral edema, pneumonia, skin itching, rash and other allergies, agitation, drowsiness, sudden sleep attacks, syncope, visual impairment including diplopia, blurred vision and decreased vision, vomiting, weight loss including decreased appetite, weight gain. In placebo-controlled clinical trials, a total of 1,778 patients took this product and 1,297 patients took placebo. The combined analysis results showed that the incidence of adverse reactions in both groups was high. 67% of patients taking this product and 54% of patients taking placebo reported at least one adverse drug reaction. The following table shows the incidence of adverse drug reactions in placebo-controlled clinical trials. The adverse drug reactions reported in the table are events with an incidence of 0.1% or more, events that occur more frequently in patients taking this drug than in the placebo group, or events that are considered clinically relevant. The vast majority of adverse reactions are mild to moderate, usually occur early in treatment, and most tend to disappear with continued treatment. By system organ class, the incidence of adverse reactions uses the following categories: very common (≥1/10); common (≥1/100 to

Allergic to the active ingredients or any excipients of this product.

Precautions for children: Due to the lack of safety and efficacy data, this product is not recommended for use in children and adolescents under 18 years of age. This product has no relevant application in the pediatric population with Parkinson's disease. Precautions for pregnancy and lactation: The effects of this product on human pregnancy and lactation have not been studied. This product is not teratogenic in rats and rabbits, but is embryotoxic in rats at maternally toxic doses. This product is contraindicated during pregnancy unless it is absolutely necessary and can only be used when the potential benefit outweighs the potential risk to the fetus. Since this product inhibits prolactin secretion in humans, it has an inhibitory effect on lactation. It has not been studied whether this product is secreted into female breast milk. The concentration of radioactivity associated with the active substance in rat milk is higher than that in plasma. Due to the lack of human data, this product should not be used during lactation. However, if the use of this product is unavoidable, breastfeeding should be discontinued. The effects of this product on human reproduction have not been studied. As expected, as a dopamine receptor agonist, this product affects the estrous cycle and reduces the fertility of female animals in animal experiments. However, these studies did not show that this product has a direct or indirect damaging effect on male animal fertility. Elderly precautions: The total clearance of this product taken orally is approximately 30% lower in subjects over 65 years of age compared to younger subjects, because its decreased renal clearance is due to the decline in renal function associated with age. This results in an increase in the elimination half-life from approximately 8.5 hours to 12 hours. In placebo-controlled trials, 47% of 259 patients with early Parkinson's disease were 65 years of age or older. Hallucinations are more common in elderly patients after taking this product, with an incidence of 13% in patients over 65 years of age and 2% in patients under 65 years of age.

Plasma protein binding This product is very lowly bound to plasma proteins (

Store at room temperature, tightly closed

0.375mg*7 tablets*1 plate

24 months

Haisco Pharmaceutical(Meishan) Co., Ltd.

• Founded in:

  2019-11-14

• Address:

  No. 53, South Section of Shunjiang Avenue, East District, Economic Development Zone, Meishan City, Sichuan Province

• Tax NO.:

  91511402MA6AXG1C5Y

• Registered Funds:

  290 million yuan

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