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Pregabalin

Description Generic formulation Indications Dose titration Plasma levels monitoring Antiepileptic drus and therapeutic drugs for neuropathic pain Cautions Adverse effects Interactions Special populations Behavioural and cognitive effects in patients with epilepsy Psychiatric use
Pregabalin
Pregabalin structure
CAS No.
148553-50-8
Chemical Name:
Pregabalin
Synonyms
Lyrica;Pregablin;PREGABALIN;(R)-Pregabalin;(S)-Pregabalin;xiangxizhiliao;Pregabalin solution;LYRICA (pregabalin);3(S)-(AMINOMETHYL)-5;(S)-(+)-Pregabalin-d4
CBNumber:
CB2251105
Molecular Formula:
C8H17NO2
Formula Weight:
159.23
MOL File:
148553-50-8.mol

Pregabalin Properties

Melting point:
194-196°C
alpha 
D23 +10.52° (c = 1.06 in water)
Flash point:
9℃
storage temp. 
Store at RT
solubility 
deionized water: ≥10mg/mL
form 
white powder
InChIKey
AYXYPKUFHZROOJ-ZETCQYMHSA-N
CAS DataBase Reference
148553-50-8(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn,T,F
Risk Statements  63-48/22-39/23/24/25-23/24/25-11
Safety Statements  22-36/37-45-16-7
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
HS Code  29224999
Hazardous Substances Data 148553-50-8(Hazardous Substances Data)
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H225 Highly Flammable liquid and vapour Flammable liquids Category 2 Danger P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H318 Causes serious eye damage Serious eye damage/eye irritation Category 1 Danger P280, P305+P351+P338, P310
H361 Suspected of damaging fertility or the unborn child Reproductive toxicity Category 2 Warning P201, P202, P281, P308+P313, P405,P501
H370 Causes damage to organs Specific target organ toxicity, single exposure Category 1 Danger P260, P264, P270, P307+P311, P321,P405, P501
Precautionary statements:
P210 Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P311 Call a POISON CENTER or doctor/physician.
P301+P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Pregabalin price More Price(5)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich P-066 Pregabalin solution 1.0mg/mL in methanol, ampule of 1mL, certified reference material 148553-50-8 066-1ml $148 2018-11-20 Buy
Sigma-Aldrich P-120 Pregabalin solution 10.0mg/mL in water, ampule of 1mL, certified reference material 148553-50-8 120-1ml $443 2018-11-20 Buy
Sigma-Aldrich PZ0010 Pregabalin ≥97% (NMR) 148553-50-8 5mg $97.8 2018-11-20 Buy
Sigma-Aldrich Y0001805 Pregabalin EuropePharmacopoeia (EP) Reference Standard 148553-50-8 y0001805 $179 2018-11-23 Buy
Sigma-Aldrich PZ0010 Pregabalin ≥97% (NMR) 148553-50-8 25mg $397 2018-11-20 Buy

Pregabalin Chemical Properties,Uses,Production

Description

Pregabalin is a second- generation antiepileptic drug (AED) known with the proprietary brand name of Lyrica® (Pfizer, Tadworth) in the UK and USA (Pfizer, New York, NY).

Generic formulation

MHRA/ CHM advice to minimize risk when switching patients with epilepsy between different manufacturers’ products (including generic products):

Indications

Epilepsy
Adjunctive therapy of focal seizures with and without secondary generalization.

Recommendations summarized from NICE (2012)
Psychiatry
Generalized anxiety disorder.

Neurology
Peripheral and central neuropathic pain.

Dose titration

If stopping pregabalin, it is recommended to taper over at least 1 week to avoid abrupt withdrawal.

Plasma levels monitoring

Pregabalin pharmacokinetics are linear over the recommended daily dose range; inter- subject pharmacokinetic variability for pregabalin is low (<20%) and multiple dose pharmacokinetics are predictable from single- dose data. Therefore, there is no need for routine monitoring of plasma concentrations of pregabalin.

Antiepileptic drus and therapeutic drugs for neuropathic pain

Pregabalin is a new antiepileptic drug, having a γ-amino butyric acid structure on its molecular structure, which has anticonvulsant effects, and is successfully developed by the company Pfizer for the treatment of peripheral neuropathic pain, or adjuvant treatment of partial seizures.
In December 2008, the US Food and Drug Administration (FDA) approved pregabalin (trade name "Lyrica") for the treatment of diabetic peripheral neuropathic pain (DPN) and postherpetic neuralgia (PHN)which are Both the most common neuropathic pains.
Neuropathic pain is one of the most difficult chronic pain syndromes to treat , dull pain, burning, tingling as the main feature, there are a lot of incentives of neuralgia, diabetes, infections (such as herpes zoster), cancer and AIDS, etc. can cause neurological pain, in Europe about 3% of the population suffer from neuralgia torture.
The above information is edited by the chemicalbook of Tian Ye.

Cautions

  1. Patients with conditions that may precipitate encephalopathy.
  2. Patients with severe congestive heart failure.

Adverse effects

Pregabalin can be associated with adverse effects at the level of the nervous system and other systems.

Interactions

With alcohol/food

Special populations

Hepatic impairment
No dose adjustment is required for patients with hepatic impairment.

Renal impairment
Reduce maintenance dose according to degree of reduction in creatinine clearance.

Pregnancy

Behavioural and cognitive effects in patients with epilepsy

Pregalin is characterized by a good behavioural profile. This AED does not appear to have significant negative effects on mood or behaviour in patients with epilepsy, although depression has been reported in some patients (dose- dependent effects of mild- to- moderate intensity). A potential abuse or misuse of pregabalin has also been reported, with implications in terms of dependence and withdrawal. pregabalin is also associated with limited negative cognitive effects, mainly related to sedation, decreased arousal, decreased attention and concentration (dose- dependent effects of mild- to- moderate intensity).

Psychiatric use

Pregabalin has an approved indication and is widely used for the treatment of generalized anxiety disorder. Several randomized, double- blind, placebocontrolled trials found that pregabalin is an effective treatment for patients with generalized anxiety disorder and social anxiety disorder. Possible implications in the treatment of mood disorders and benzodiazepines dependence are emerging. Moreover, pregabalin may be a therapeutic agent for the treatment of alcohol abuse, in both withdrawal phase and relapse prevention.

Description

As a follow-up to its g-aminobutyric acid (GABA) agonist gabapentin, Pfizer has developed and launched pregabalin for the treatment of epilepsy and neuropathic pain. Although pregabalin is a structural analog of GABA, it does not interact with GABA-A or GABA-B receptors or influence GABA uptake. The exact mechanism of action is unclear, but pregabalin may reduce excitatory neurotransmitter release by binding to the α2-δ protein subunit of voltage-gated calcium channels. The resulting inhibition of excess neuronal activity is believed to be the basis for pregabalin’s efficacy in epilepsy and neuropathic pain alleviation. Since the activity is attributed to the (S′)-enantiomer alone, an efficient asymmetric synthesis is employed for commercial production. The key step is the asymmetric hydrogenation of 3-cyano-5-methyl-3-hexenoic acid using a chiral rhodium catalyst to afford an intermediate that is enriched in the (S′)-enantiomer. The cyano group is ultimately reduced by routine hydrogenation with a nickel catalyst. Further enrichment of the final product is realized by selective recrystallization with (S′)-mandelic acid or simply recrystallizing from water/isopropanol. Compared to gabapentin, pregabalin is 2- to 10-fold more potent in various animal models. For example, in preventing maximal electroshock seizures (MES) in mice, pregabalin has an ED50 of 20 mg/kg p.o. versus 87 mg/kg for gabapentin. A comparable increase in potency is also observed in the rat MES model (ED50=1.8mg=kg p.o. for pregabalin versus 10.3 mg/kg for gabapentin). In addition, pregabalin’s linear pharmacokinetics (Cmax relates to dose) translates to better predictability of pharmacological effects. It has 90% oral bioavailability, with an elimination half-life of approximately 6 h. The primary route of excretion is via the renal system with negligible metabolism. Furthermore, its lack of activity at the cytochrome P450 enzymes was reflected in an absence of pharmacokinetic drug-drug interactions in relevant studies. In a placebocontrolled, fixed dose (up to 600mg/day) trial with pregabalin as an adjunctive therapy for epilepsy, 14 to 51% of patients showed at least a 50% decrease in seizure frequency with a clear dose-response relationship. In a flexible dosing group, (150 mg/day to 600 mg/day), the seizure reduction rate was 35.4%compared to 40.3% for a fixed dose of 600mg/day and 10.6% for placebo. The most common side effects were dizziness (29%) and somnolence (21%). In addition, weight gain (equal to or more than 7% increase from baseline) occurred in 40% of patients in the 12-week study; however, there was no affect on male fertility or efficacy of oral contraceptives in women. Regarding the use of pregabalin in treating painful diabetic peripheral neuropathy, oral administration of 300 and 600 mg/day t.i.d. was superior to placebo (39–48% compared to 15–18% with placebo) in relieving pain and improving pain-related sleep interference. While pregabalin was originally developed as an anticonvulsant for epilepsy, its success in treating neuropathic pain has led to its exploration in treating other CNS disorders, such as, anxiety, social phobia, and fibromyalgia.

Chemical Properties

Off-White Solid

Originator

Warner-Lambert (US)

Uses

S-Enantiomer of Pregabalin. A GABA analogue used as an anticonvulsant. Anxiolytic analgesic used to treat peripheral neuropathic pain and fibromyalgia.

Uses

Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade nam

brand name

Lyrica (CP).

Pregabalin Preparation Products And Raw materials

Raw materials

Preparation Products


Pregabalin Suppliers

Global( 369)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Kono Chem Co., Ltd
+86-132 8924 6953
info@konochemical.com CHINA 2164 58
Hebei Guanlang Biotechnology Co., Ltd.
+86-0311-66562153 whatsapp +8615203118427
+86-0311-66562153 sales@crovellbio.com CHINA 416 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 117 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
alice@hbjkai.com CHINA 277 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Shanghai Time Chemicals CO., Ltd.
+86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com CHINA 1374 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55

View Lastest Price from Pregabalin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-04-18 Pregabalin
148553-50-8
US $1.00 / g 1g 99% 100 Kilogram/Kilograms per Month Cangzhou Wanyou New Material Technology Co.,Ltd
2019-04-02 Pregabalin Manufacturer; In stock GMP Factory
148553-50-8
US $1.00 / KG 1KG High quality manufacturer TOP 3 largest production factory in China Chemwill Asia Co.,Ltd.
2019-04-13 Pregabalin
148553-50-8
US $650.00 / kg 0.01kg 99.9% 6000kg/month Hebei Huanhao Biotechnology Co., Ltd.

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