How is pregabalin synthesized?
Abstract. Pregabalin, a γ-amino acid derivative, can be synthesized by utilizing flow methods. In this synthesis, a three-step sequential-flow system with heterogeneous catalysts was employed to give the precursor of pregabalin in yields of 75–100 %, and a space-time yield of 52.2 g/L d was reached.
What is the chemical formula for pregabalin?
C8H17NO2
Pregabalin/Formula
Is pregabalin optically active?
Optically active (S)-3-(aminomethyl)-5-methyl hexanoic acid (pregabalin, PGB) is a lipophilic γ-aminobutyric acid analogue.
Is pregabalin water soluble?
When misused, pregabalin can be taken orally, intravenously (water soluble), rectally (plugging) or snorted (crushed up).
What is pregabalin and methylcobalamin capsules?
Pregabalin with Methylcobalamin is a medicine that is used for the treatment of Nerve Damage Pain, Seizures, Anxiety Disorder In Adults, Anemia, Nerve Damage, Numbness And Tingling and other conditions. Pregabalin MEthylcobalamin Tablet contains Methylcobalamin, and Pregabalin as active ingredients.
Is pregabalin an amino acid?
A γ-amino acid that is γ-aminobutyric acid (GABA) carrying an isobutyl substitutent at the β-position (the S-enantiomer). Binds with high affinity to the α2-δ site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.
Is pregabalin polar?
Pregabalin is an inhibitor of neuronal activity used for therapy of painful neuropathy and as an anticonvulsant….3.1Computed Properties.
| Property Name | Property Value | Reference |
|---|---|---|
| Topological Polar Surface Area | 63.3 Ų | Computed by Cactvs 3.4.8.18 (PubChem release 2021.05.07) |
Is Lyrica metabolized in the liver?
It is not subject to hepatic metabolism and does not induce or inhibit liver enzymes such as the cytochrome P450 system. Therefore, pregabalin is unlikely to cause, or be subject to, pharmacokinetic drug-drug interactions–an expectation that has been confirmed in clinical pharmacokinetic studies.
Does pregabalin increase GABA?
Specifically, pregabalin administration has been found to slightly increase the extracellular GABA levels in the brain7,108,109,110. Therefore, the weak GABAergic activity of pregabalin may induce GABA-mimetic activity that influences the euphoria and relaxation described by some patients and drug abusers.
Why methylcobalamin is combined with pregabalin?
You have been prescribed Methylcobalamin + Pregabalin for treating and preventing nerve pain. Its side effects are usually mild and temporary.
Can we take methylcobalamin with pregabalin?
As methylcobalamin plays an important role in the regeneration of the myelin sheath, the addition of the same to pregabalin may restore the function of nerves, in addition to relieving the pain.
Is pregabalin a calcium channel blocker?
Pregabalin binds to the alpha2-delta site of voltage-gated calcium channels in the central nervous system (CNS) tissues. This calcium channel modulation may reduce the release of many neurotransmitters. Like gabapentin, the precise mechanism of action of pregabalin is unknown.
How is the skeleton of pregabalin synthesised?
In a reported production process, 4 the basic skeleton is synthesized by Knoevenagel condensation, 1,4-addition of cyanide, hydrolysis, decarboxylation, reduction of the CN group, and finally optical resolution. [ 4] In this process toxic CN sources and a large amount of Raney nickel in the reduction step are required.
What is the trade name for pregabalin 1?
Pregabalin ( 1, trade name: Lyrica) is a γ-amino acid derivative that is widely used as a therapeutic agent for nervous system disorders such as epilepsy, anxiety disorder, and neuropathic pain.
What kind of pain can pregabalin be used for?
Several other schemes of synthesis are patented [113-119]. Pregabalin is used to relieve neuropathic pain, shingles, fibromyalgia, and seizures, and for pain management. Pregabalin (9.1.19) is among the bestsellers drugs for the treatment of epilepsy.
How is the chiral lactone produced in pregabalin?
Borane dimethylsulfide reduction of produced the chiral lactone (9.1.56), which was opened with trimethylsilyl iodide, producing compound (9.1.57) and elaborated to pregabalin via the preparation of azide ( 9.1.58) followed by its hydrolysis to acid ( 9.1.59) and hydrogenation to pregabalin ( 9.1.19 ).