What Is Pergolide?

The chemical name of Pergolide is 8 -[(methylthio) methyl] -6-propyl ergot, the molecular formula is C ₁₉ H ₂₆ N ₂ S, the molecular weight is 314.48800, and the density is 1.124 g / cm ³ , Melting point is 207.5ºC, boiling point is 491.3ºC at 760 mmHg. Clinically, it is mainly used in 1. Compound levodopa preparations with Parkinson's disease and Parkinson's syndrome, which have a reduced efficacy or motor dysfunction, such as switching phenomenon; can also be used in early combined treatment;

Chinese name: Pergolet
Foreign name: pergolide

CAS number: 66104-22-1
Molecular formula: C19H26N2S
Molecular weight: 314.48800

Introduction to Pergolide compounds

Basic information

Chinese name

Chinese alias: Pergolide; D-6-n-propyl-8 -methylthiomethylergoline;

English name: pergolide

English alias: Permax (TN); Pergolidum [INN-Latin]; Pergolidum; Pergolida [INN-Spanish]; (6aR, 9R, 10aR) -9- (methylsulfanylmethyl) -7-propyl-6,6a, 8,9, 10,10a-hexahydro-4H-indolo [4,3-fg] quinoline;

CAS number: 66104-22-1

Molecular formula: C ₁₉ H ₂₆ N ₂ S

Molecular weight: 314.48800

Structural formula:

Exact mass: 314.18200

PSA: 44.33000

LogP: 4.20900 ^[1]

Physical properties of Pergolide

Density: 1.124 g / cm ³

Melting point: 207.5ºC ^[1]

Boiling point: 491.3ºC at 760 mmHg

Pergolide molecular structure data

1. Molar refractive index: 97.44

2. Molar volume (cm3 / mol): 279.6

3. Isotonic specific volume (90.2K): 722.4

4. Surface tension (dyne / cm): 44.5

5. Polarizability (10-24cm3): 38.62 ^[2]

Pergolite calculates chemical data

1. Hydrophobic parameter calculation reference value (XlogP): 4.2

2.Number of hydrogen-bonded donors: 1

3.Number of hydrogen bond acceptors: 2

4.Number of rotatable chemical bonds: 4

5.Number of tautomers: none

6. Topological molecular polar surface area 44.3

7.Number of heavy atoms: 22

8.Surface charge: 0

9.Complexity: 388

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 3

12. Uncertain number of atomic stereocenters: 0

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0 ^[2]

15.Number of covalent bond units: 1

Pergolite production method

Compound (I) is reduced by lithium aluminum hydride, and then reacted with methanesulfonyl chloride to obtain D-6-n-propyl-8-methanesulfonyloxymethylergoline (III). 25g of methyl mercaptan was dissolved in 200ml of dimethylacetamide (DMA), cooled to about 0 ° C with an ice bath, and 14.4g of 50% sodium hydride was added in portions to form sodium methylsulfide. Then, a solution of 10.9 g of compound (III) in 60 ml of dimethylacetamide was added at room temperature, and stirred for 1 h under the protection of nitrogen. Dilute with water and extract the aqueous layer with ethyl acetate. The extract was washed with water and saturated sodium chloride, and then dried. The solvent was distilled off, and the residue contained pergolide, and only one spot was detected by TLC; it contained 6.9g of pergolide, and the melting point was 206 to 209 ° C (decomposed). The residue was suspended in 100 ml of boiling methanol, and 1.6 ml of methanesulfonic acid in 10 ml of a methanol solution was added. After the addition was completed, it was left to cool, and pergolite mesylate crystals were precipitated. After cooling, it was filtered to obtain 6.0 g of pergolide mesylate with a melting point of 255 ° C (decomposed). ^[2]

Pergolite uses

Synthetic ergoline drugs are new dopaminergic agonists, with stronger effects and long-lasting effects. As an adjuvant therapy for levodopa and carbidopa, it is used in the treatment of Parkinson's disease. ^[1]

Description of Pergolide Compounds

Pergolide drug name:

[Common name] Pergolide mesylate

[English name] Pergolide Mesylate Tablets

[Chinese Pinyin] Jia Huang Suan Pei Gao Li Te Pian

Pergolite ingredients:

The main ingredient of this product is Pergolide mesylate, whose chemical name is 8 [(methylthio) methyl] -6 propyl ergoline mesylate

Molecular formula: C ₁₉ H ₂₆ N ₂ S · CH ₃ SO ₃ H

Molecular weight: 410.59

Pergolite category:

Chemicals & Biological Products >> Nervous System Drugs >> Anti-Parkinson's Disease and Other Dyskinesia Drugs >> Anti-Parkinson's Disease Drugs

Pergolide indications:

This product is a dopamine receptor agonist, a synergistic drug of a compound levodopa preparation, suitable for:

Compound levodopa preparations in patients with Parkinson's disease and Parkinson's syndrome have reduced efficacy or motor dysfunction, such as switching phenomenon. Can also be used for early combined treatment.
Hyperprolactinemia.

Pergolite specifications:

0.05mg (as C ₁₉ H ₂₆ N ₂ S)

Pergolide adverse reactions:

Nausea, vomiting, dizziness, fatigue, nasal congestion, itching of the skin, constipation and other adverse reactions may occur. If the adverse reactions are severe, the drug should be discontinued.

According to foreign literature reports, some patients have experienced mental symptoms and orthostatic hypotension after oral administration of this product; some patients have sinus tachycardia and atrial premature beats. ^[3]

Pergolite taboos:

People who are allergic to this product or other ergot derivatives.

Notes for Pergaoli :

Taking this product must be under the strict guidance of a doctor, starting from a small dose and gradually increasing to the optimal dose.

Patients with severe heart disease and previous psychiatric history should be cautious when using high doses. ^[3]

Pergolide pharmacology and toxicology:

Pharmacology: Pergolide is a typical central post-synaptic dopamine receptor agonist, which can significantly inhibit the release of prolactin from the anterior pituitary gland, reduce serum prolactin content in normal and reserpine rats; Metabolic transformation, thereby reducing the content of 3,4 dihydroxyphenylacetic acid in the brain, causing contralateral rotation of the nigrostriatal injured rats; increasing the autonomic mobility and climbing behavior of mice, causing stereotypes in rats and guinea pigs Exercise, and counteract spontaneous tremor caused by ventral dorsum of the midbrain of the monkey.
Toxicology: Acutely toxic female mice have an oral LD50 of 81.8 mg / , and male mice have an oral LD50 of 61.7 mg / .
Oral administration of 6-month long-term toxicity test in rats shows that this product can cause a dose-dependent increase in autonomic activity and stress, slow down the rate of weight gain, and significantly increase the weight of ovaries in female rats. Speed and ovarian weight returned to normal. This product has no significant effect on hematology, blood biochemistry, other organs and histopathology of rats. The dogs were orally administered for three months without significant toxicity. Microbial back mutation test, mouse micronucleus test, in vitro cultured human lymphocyte chromosome aberration test, the results show that this product has no mutagenic effect. This product has not caused teratogenic effects in the teratogenic sensitive stage of mice. ^[3]

Pergolide pharmacokinetics:

Wistar rats received a subcutaneous injection of 1 mg / C-labeled megosulfate megosulfate and the plasma concentration peaked quickly and remained above 12 hours. After oral gavage, it is quickly absorbed from the gastrointestinal tract and distributed in all tissues for more than 24 hours. After 72 hours, 53.3% of radioactivity was excreted in feces, 16.6% was excreted in urine, and 67% was detected in cadaver. ^[3]

Pergaert expert reviews

The effect and usage of the drug are basically the same as those of ergometrin, with fewer adverse reactions and high efficacy, and it has a tendency to gradually replace bromocriptine. ^[4]