What Is Pregabalin?

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.

Chinese name: Pregabalin
Foreign name: Pregabalin

CAS number: 148553-50-8
Molecular formula: C8H17NO2
Molecular weight: 159.22600

Brief Introduction to Pregabalin Compounds

Basic information for Pregabalin

Chinese name: Pregabalin

Chinese alias: (3S) -3-aminomethyl-5-methylhexanoic acid; ( S ) -3-aminomethyl-5-methylhexanoic acid;

English 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 ^[1]

Pregabalin Regulatory Information

China

Morphine analogs

DEA regulated chemicals ^[1]

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 ^[1]

Pregabalin Safety Information

Symbol: GHS05 GHS08

Signal Word: Danger

Hazard statement: H318; H361

Cautionary statement: P280; P305 + P351 + P338 + P310

Customs code: 2915900090 ^[1]

Pregabalin uses

For the treatment of peripheral neuralgia, or adjuvant treatment of partial seizures ^[1] .

Overview of Pregabalin Drug Related Basic Information

Pregabalin drug name

Chinese name: Pregabalin

English name: Pregabalin ^[2-3]

Pregabalin Classification

Neurological Drugs> Antiepileptic Drugs> Others ^[2-3]

Pregabalin dosage form

25mg; 50mg; 75mg; 100mg; 150mg; 200mg; 300mg ^[2] .

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] .

2. Adjuvant treatment of partial seizures (foreign data) ^[3] .

3. Can also be used for anxiety, social phobia, arthritis ^[2] .

Pregabalin contraindications

People who are allergic to pregabalin (foreign data) ^[2] .

Pregabalin notes

1. (1) Patients with congestive heart failure (foreign data). (2) Patients with eye diseases (foreign data) ^[3] .

2. Patients with diabetes ^[2] .

3. The impact of drugs on children: The safety and effectiveness of medication have not been determined ^[3] .

4. The effects of drugs on pregnancy: it is not clear ^[2] .

5. The effects of drugs on breastfeeding: it is not clear ^[3] .

6. Check or monitor before, after and during medication: blood biochemical tests are performed regularly ^[2] .

Pregabalin adverse reactions

1. Peripheral edema and prolonged PR interval can be seen ^[2] .

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] .

3. Metabolic / endocrine system: can cause weight gain, the incidence is 4% to 12% ^[2] .

4. Musculoskeletal system: elevated creatine kinase levels (2%), myoclonus (2%), and case reports of rhabdomyolysis ^[3] .

5. Liver: A large dose (900mg a day) occasionally shows a slight and transient increase in liver enzymes ^[2] .

6. Gastrointestinal tract: can cause salivary deficiency (4% ~ 8%), constipation (4% ~ 5%), etc. ^[3] .

7. Blood: Visible thrombocytopenia (3%) ^[2] .

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 ^[3] .

9. Others: (1) Visible infectious diseases (7%). (2) It has been observed that the incidence of tumors in rats has been increased after medication ^[2] .

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 ^[3] .

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 ^[2] .

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 ^[3] .

4. Generalized anxiety disorder: 300 to 600 mg per day ^[2] .

5. Social phobia: 200mg once, 3 ^[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 ^[2] .

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 ^[2] .

3. Pregabalin can enhance the sedative effect of alcohol ^[3] .

4. Food can reduce the bioavailability of pregabalin ^[2] .