How does pregabalin work?

Pregabaline is a famous drug to treat neuropathic pain but how does pregabalin work? And what are the other indications of pregabalin?

Pregabalin approved by the FDA for the treatment of fibromyalgia, neuropathic pain and as add-on therapy for partial-onset seizures in adults with epilepsy

There are other Off-label uses that are not approved by FDA include social anxiety disorder, generalized anxiety disorder, chronic pain conditions, insomnia, and bipolar disorder.

This article will highlight how does pregabalin work? how to take it? adverse event profile, monitoring parameters, contraindication, and toxicity.

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Pregabalin

How does pregabalin work?

Pregabalin resembles the structure of the inhibitory neurotransmitter gamma-aminobutyric acid GABA. It has lipophilic properties to enhance the crossing of it to the blood-brain barrier. However, pregabalin indirectly binds to GABA receptors results in decreasing the influx of calcium into neurons and reduces the release of excitatory neurotransmitters.

This is why pregabalin is used as an anticonvulsant and analgesic.

 

How does pregabalin work

How to take pregabalin?

Pregabalin is available in capsules or oral solution and administered orally. Following oral administration, pregabalin reaches max concentration in the blood within 1.5 hours and achieves a complete action within 24 to 48 hours.

The absorption of pregabalin from the stomach is independent of the dose. Pregabalin can cross the blood-brain barrier. Humans cannot significantly metabolize pregabalin. It eliminates unchanged by renal excretion. In patients with normal renal function, the elimination takes 6.3 hours.

Dosages up to 600 mg/day did not provide additional benefit and were not well-tolerated due to several side effects.

Don’t stop pregabalin suddenly but taper the dose gradually over 1 week to avoid withdrawal symptoms or exacerbation of seizures.

 

How much do you need from pregabalin?

Diabetic Peripheral Neuropathy:

The therapeutic dose is 300 mg/day. The start with 50 mg three times per day. Increase The dose up to 300 mg/day within one week of treatment.

Postherpetic Neuralgia:

The dose is 150 mg to 300 mg per day, and can be taken twice or three times daily. Start with a dose of 75 mg two times per day or 50 mg three times per day.

Increase the dose up to 300 mg per day within one week of treatment. If no optimal pain control within 2 to 4 weeks of treatment with 300 mg per day, increase the dose to 600 mg per day, divided into twice per day or three times per dosing.

Spinal Cord Injury:

The dose ranges from 150 mg to 600 mg per day. start with a dose of 75 mg twice per day. Increase the dose to 150 mg twice per day within one week of treatment.

The dose may be increased up to 300 mg twice per day with suboptimal pain control following 2 to 3 weeks of treatment with 150 mg twice a day. In spinal cord injury, the improvement can be seen within one week after initiating treatment. However, it is recommended to try the medication for 4 to 6 weeks.

 

Adjunctive Therapy with Partial Onset Seizures:

The dose is 150 mg to 600 mg per day, divided into twice per day or three times per dosing. Start the dose with no greater than 150 mg per day and increase to a maximum of 600 mg per day.

Management of Fibromyalgia:

The therapeutic dose is 300 mg to 450 mg per day. Start with a dose of 150 mg/day divided into twice per day dosing. Increase The dose to 300 mg per day within one week of treatment. If no optimal pain control on 300 mg per day may be further increased to 450 mg per day, divided into twice per day dosing.

Dosing Modifications:

Pregabalin is eliminated by the kidney. Dose adjustment is required in impaired renal function. Patients with hepatic impairment do not require dosing modifications.

 

Adverse events

Most of the adverse effects related to pregabalin were mild to moderate intensity.

The severity of adverse events is not dose-dependent and occurred within the first two weeks of initiating treatment.

Somnolence and dizziness are the most common adverse events that have been reported with the use of pregabalin, and they are the most frequent cause of treatment discontinuation, and of course, this is related to how does pregabalin works.

In premarketing controlled trials, The most common adverse reactions reported which occurred in greater than or equal to 5% of patients and twice the rate reported by patients receiving placebo were:  dizziness, somnolence, blurred vision, dry mouth, difficulty with concentration/attention, edema, and weight gain.

Weight gain occurred in up to 14% of patients receiving 600 mg per day and was dose-dependent.

Withdrawal symptoms can occur after rapid discontinuation of pregabalin including hyperhidrosis, insomnia, nausea,  nervousness, irritability, headache, anxiety, and diarrhea.

Contraindications

Pregabalin is contraindicated in case of  hypersensitivity to pregabalin. There are no enough studies on pregnant women. But there are some reported cases that Pregabalin may cause fetal harm, so use caution in case if you are pregnant.

Pregabalin is not recommended in breastfeeding as it can be detected in the milk of lactating women

Monitor patients for symptoms of new or worsening depression, suicidal behavior or ideation, and other changes in behavior or mood, as pregabalin is like the other antiepileptic drugs can increase the risk of suicidal thoughts or behavior.

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