API Pregabalin

Name	Pregabalin
CAS number	148553-50-8
Synonym	(R-)-3-Isobutyl GABA; PD 144723; PD-144723; PD144723; CI 1008; CI-1008; HSDB 7530; Lyrica; Pregabalin
Description	Pregabalin is an anticonvulsant drug used to treat neuropathic pain conditions and fibromyalgia, and for the treatment of partial onset seizures in combination with other anticonvulsants. Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter. It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions. Although as per the FDA Label the mechanism of action has not been definitively characterized, there is evidence that pregabalin exerts its effects by binding to the α2δ subunit of voltage-dependent calcium channels. Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release). It may have dependence liability if misused but the risk appears to be highest in patients with current or past substance use disorders.
Structure
Molecular Formula	C8H17NO2
Molecular Weight	159.229
Appearance	Solid powder
Quality Standard	USP, EP, BP, CP
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition	Dry, dark and at 0 – 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years).
Shelf Life	>2 years if stored properly
Sample package	Aluminium foil bag
Commercial package	Aluminium Tin, Fiber drum
Origin	China

Pregabalin More Info

Pregabalin is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, and generalized anxiety disorder. Its use for epilepsy is as an add-on therapy for partial seizures with or without secondary generalization in adults. Some off-label uses of pregabalin include, restless leg syndrome, migraine, social phobia, panic disorder, mania, bipolar disorder, and alcohol withdrawal. Pregabalin is discontinued.

1. Chemical and Pharmacological Classification

Pregabalin is a gamma - aminobutyric acid (GABA) analogue. Structurally, it's related to the neurotransmitter GABA. However, it doesn't act directly on GABA receptors in the same way as GABA itself. Instead, it binds to the alpha - 2 - delta subunit of voltage - gated calcium channels in the central nervous system. By binding to these channels, it reduces the release of several neurotransmitters, including glutamate, norepinephrine, and substance P. This mechanism of action is crucial for its therapeutic effects in various neurological conditions.

2. Indications

Neuropathic Pain: Pregabalin is highly effective in the treatment of neuropathic pain. It's approved for the management of diabetic peripheral neuropathy pain and post - herpetic neuralgia. For example, in diabetic peripheral neuropathy, nerve damage due to high blood sugar levels can lead to chronic pain in the extremities such as the feet and hands. Pregabalin can help relieve this pain by modulating the abnormal neuronal excitability associated with nerve damage.

Epilepsy: It's also used as an adjunctive therapy in the treatment of partial - onset seizures in adults. In epilepsy cases, it helps to control the excessive and abnormal electrical activity in the brain that leads to seizures.

Generalized Anxiety Disorder: Pregabalin has anxiolytic properties and is sometimes prescribed for the treatment of generalized anxiety disorder. It can reduce the symptoms of excessive worry, restlessness, and tension associated with this mental health condition.

3. Dosage and Administration

The dosage of pregabalin varies depending on the indication and the individual patient's response and tolerance. For neuropathic pain, the initial dose is usually around 150 mg per day, which can be titrated up to a maximum of 600 mg per day in divided doses. In epilepsy, the dosage is also adjusted based on the patient's seizure control and side - effect profile. It's typically taken orally with or without food.

4. Side Effects

Common Side Effects: The most common side effects of pregabalin include dizziness, drowsiness, dry mouth, peripheral edema (swelling of the legs and feet), blurred vision, and weight gain. These side effects usually occur at the beginning of treatment and may subside as the body adjusts to the medication. For example, the dizziness and drowsiness can affect a patient's ability to drive or operate machinery, so patients need to be cautious during the initial phase of treatment.

Less Common but Serious Side Effects: There are also less common but more serious side effects such as angioedema (swelling of the face, lips, tongue, or throat), which can be a life - threatening allergic reaction. In addition, there have been reports of mood changes, including depression and suicidal ideation, although a direct causal link to pregabalin is still being investigated in some cases.

5. Precautions and Contraindications

Pregabalin should be used with caution in patients with a history of drug abuse or dependence, as it has the potential for misuse and addiction. In particular, its effects on the central nervous system can lead to a feeling of euphoria in some individuals, which may increase the risk of abuse.

It's contraindicated in patients with a known hypersensitivity to pregabalin or any of its components. Also, it may interact with other medications such as opioids, benzodiazepines, and certain antidepressants, increasing the risk of side effects such as respiratory depression and sedation. Therefore, it's important for healthcare providers to review a patient's complete medication list before prescribing pregabalin.