Pregabalin is a white or almost white crystalline powder chemical. Chemical name (
S ) -3-aminomethyl-5-methylhexanoic acid, molecular formula is C
8 H
17 NO
2 , and molecular weight is 159.22600. Pregabalin is an antiepileptic drug, and it mainly treats postherpetic neuralgia clinically.
Pregabalin is a white or almost white crystalline powder chemical. Chemical name ( S ) -3-aminomethyl-5-methylhexanoic acid, molecular formula is C 8 H 17 NO 2 , and molecular weight is 159.22600. Pregabalin is an antiepileptic drug, and it mainly treats postherpetic neuralgia clinically.
- Name
- Pregabalin
- Name
- Pregabalin
- CAS number
- 148553-50-8
- Molecular formula
- C8H17NO2
- Molecular weight
- 159.22600
Brief Introduction to Pregabalin Compounds
Basic information for Pregabalin
Name: Pregabalin
Chinese alias: (3S) -3-aminomethyl-5-methylhexanoic acid; ( S ) -3-aminomethyl-5-methylhexanoic acid;
Name: pregabalin
English alias: ( S ) -3- (Aminomethyl) -5-methylhexanoic acid CI-1008 PD-144723; Pregabalin; Pregablin; Lyrica; PREDNISOLONESODIUMPHOSPHATE;
CAS number: 148553-50-8
Molecular formula: C 8 H 17 NO 2
Chemical structure:
Molecular weight: 159.22600
Exact mass: 159.12600
PSA: 63.32000
LogP: 1.78240
Pregabalin Regulatory Information
China
Morphine analogs
DEA regulated chemicals
Physical and Chemical Properties of Pregabalin
Appearance and properties: white or almost white crystalline powder
Density: 0.997 g / cm 3
Melting point: 194-196ºC
Boiling point: 274ºC at 760 mmHg
Flash point: 119.5ºC
Refractive index: 1.464
Vapor pressure: 0.00153mmHg at 25 ° C
Pregabalin Safety Information
Symbol: GHS05 GHS08
Signal Word: Danger
Hazard statement: H318; H361
Cautionary statement: P280; P305 + P351 + P338 + P310
Customs code: 2915900090
Pregabalin uses
For the treatment of peripheral neuralgia, or adjuvant treatment of partial seizures .
Overview of Pregabalin Drug Related Basic Information
Pregabalin drug name
Name: Pregabalin
Name: Pregabalin [2-3]
Pregabalin Classification
Neurological Drugs> Antiepileptic Drugs> Others [2-3]
Pregabalin dosage form
25mg; 50mg; 75mg; 100mg; 150mg; 200mg; 300mg .
Pharmacological effects of pregabalin
Pregabalin is a -aminobutyric acid (GABA) analogue. Its structure and effect are similar to those of gabapentin, and it has antiepileptic, analgesic and anxiolytic activities. The mechanism of pregabalin's antiepileptic action is not clear. In laboratory studies, pregabalin has anticonvulsant activity on various epilepsy models; the activity spectrum of animal models is similar to that of gabapentin, but pregabalin is 3 to 10 times more active than gabapentin [2-3] .
Pregabalin pharmacokinetics
After pregabalin is taken orally, it takes effect within 30 minutes for acute toothache and lasts for about 5 hours. It takes effect within 1 week when used for diabetic neuropathy. The peak time is about 1h, and the bioavailability is 90%. Less metabolized in the liver, 92% to 99% are excreted by the kidneys in the original form, 0.1% less than the oral amount is excreted with feces, and the half-life is 5 to 6.5 hours [2-3] .
Pregabalin indication
1. Neuralgia in diabetic peripheral neuropathy and postherpetic neuralgia .
2. Adjuvant treatment of partial seizures (foreign data) .
3. Can also be used for anxiety, social phobia, arthritis .
Pregabalin contraindications
People who are allergic to pregabalin (foreign data) .
Pregabalin notes
1. (1) Patients with congestive heart failure (foreign data). (2) Patients with eye diseases (foreign data) .
2. Patients with diabetes .
3. The impact of drugs on children: The safety and effectiveness of medication have not been determined .
4. The effects of drugs on pregnancy: it is not clear .
5. The effects of drugs on breastfeeding: it is not clear .
6. Check or monitor before, after and during medication: blood biochemical tests are performed regularly .
Pregabalin adverse reactions
1. Peripheral edema and prolonged PR interval can be seen .
2. Central nervous system: dizziness (21% to 32%), lethargy (12% to 22%), ataxia (3% to 15%), headache (7%), weakness (5%), language Disorders (5%), tremors (1% to 8%), forgetfulness (1% to 5%), neurological disorders (3% to 4%), mental disorders (2% to 8%) .
3. Metabolic / endocrine system: can cause weight gain, the incidence is 4% to 12% .
4. Musculoskeletal system: elevated creatine kinase levels (2%), myoclonus (2%), and case reports of rhabdomyolysis .
5. Liver: A large dose (900mg a day) occasionally shows a slight and transient increase in liver enzymes .
6. Gastrointestinal tract: can cause salivary deficiency (4% ~ 8%), constipation (4% ~ 5%), etc. .
7. Blood: Visible thrombocytopenia (3%) .
8. Eyes: blurred vision (4% to 10%), diplopia (2% to 9%), amblyopia, and so on, but the causal relationship with pregabalin has not been determined .
9. Others: (1) Visible infectious diseases (7%). (2) It has been observed that the incidence of tumors in rats has been increased after medication .
Pregabalin dosage
Oral administration:
1. Adjuvant treatment for partial seizures: (1) 75mg once, 50mg twice a day, or 3 times a day According to individual response and tolerance, it can be increased to a maximum of 600 mg a day, divided into 2 to 3 times. (2) Patients with refractory epilepsy who are not effective with other antiepileptic drugs, plus pregabalin 150 to 600 mg a day, divided into 2 to 3 doses .
2. Neuralgia in diabetic peripheral neuropathy: the initial dose is 50mg once a day, three times a day; it can be increased to 100mg once a week, three times a day according to efficacy and tolerance .
3. Postherpetic neuralgia: The initial dose is 75mg once, twice a day or 50mg once a day, three times a day; it can be increased to 300mg a day in one week according to the treatment effect and tolerance. The maintenance amount is 75 to 150 mg once, twice a day or 50 to 100 mg once, and three times a day .
4. Generalized anxiety disorder: 300 to 600 mg per day .
5. Social phobia: 200mg once, 3 times a day.
6. Postoperative toothache: 300mg per injection, which can be repeated once every 6 hours according to the duration of anesthesia. Dose during dialysis: A supplemental dose should be given immediately after hemodialysis .
Pregabalin Drug Interactions
1. The combined use of thiazolidinedione antidiabetic drugs increases the risk of weight gain and peripheral edema, so caution should be used when combined.
2. Pregabalin can enhance the sedative effect of central nervous system inhibitors .
3. Pregabalin can enhance the sedative effect of alcohol .
4. Food can reduce the bioavailability of pregabalin .
