Pregabalin

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Introduction

Pregabalin, sold under the brand name Lyrica belongs to the anticonvulsant group of medications and is used in a wide range of analgesic effects. Pregabalin blocks the VGCC and decreases glutamate and sensory neuropeptides (substance P and CGRP) released at the synapse by reducing Ca2+ influx to carry out its therapeutic effects. In addition to analgesic and anticonvulsant, Pregabalin has prominent anxiolytic and antiallodynic properties.

Uses

Most common Pregabalin uses.

  • In conditions of neuropathic pain.
  • As a concomitant treatment for seizures.
  • In conditions of cancer-associated neuropathic pain.
  • For anxiety conditions like Generalized Anxiety Disorder.
  • As a prophylactic medication for migraines.

Strength and Dosage

The Pregabalin capsule has strengths of 25mg, 50mg, 75mg, 100mg, 150mg, 200mg, 225mg and 300mg. Extended Release Formulations are available in strengths of 82.5mg, 165 mg and 330mg.

  • For diabetic nephropathy conditions, regular-release capsules are started at a strength of 50mg quarterly, while extended-release formulations are begun at a strength of 165 mg quarterly.
  • For Postherpetic Neuralgia conditions, regular-release capsules are started at 150-300mg, while extended-release formulations starting doses are 165mg quarterly.
  • For Fibromyalgia conditions, regular capsules are advised at 75 mg to 150 mg daily. Pregabalin dosage in Extended Release formulations is not recommended in fibromyalgia conditions.

Pregabalin Side effects

  • Mild side effects -: constipation, headache, nausea, somnolence.
  • Moderate side effects -: blurred vision, ataxia, dry mouth, increased weight, joint swelling, nasopharyngitis.
  • Severe side effects -: balance disorder, amnesia, confusion, vertigo, disorientation, disorientation.

If Pregabalin side effects do not reverse or increase in severity, discontinue the medication and get urgent medical attention.

FAQs

What is Pregabalin?

Pregabalin is a derivative of the Gabapentin medication used to treat pain conditions. Along with being effective for a wide variety of pain conditions, it has anxiolytic and myorelaxant properties that make it effective for the management of anxiety and pre-operative stress conditions. Clinical studies have proved that Pregabalin has five times the potency of Gabapentin and 1/85th the potency of morphine. It is three to tenfold more potent than Gabapentin as an antiepileptic and two to more fold more potent for neuropathic pain.

Pregabalin mechanism for Neuropathic pain is in the neuroprotection provided by the medication through various molecular targets and the signalling systems, including Ca2+ channel-mediated neurotransmitter release, activation of excitatory amino acid transporters (EAATs), potassium channels and inhibition of pathways involving inflammatory mediators. Because of its effectiveness in neuropathic pain conditions, it has been declared the first drug to be FDA approved for diabetic neuropathy and post-herpetic neuralgia conditions.

According to the guidelines of the World Federation of Societies of Biological Psychiatry (WFSBP), the first-line treatments for Generalized Anxiety Disorders are Pregabalin, Serotonin selective reuptake inhibitors (SSRIs), Selective serotonin- and norepinephrine reuptake inhibitors (SNRIs). Pregabalin for anxiety reviews by patients and health care experts have proven the drug as a practical option for social anxiety, especially in patients who are intolerant to SSRIs or SNRIs or obtained satisfactory results.

Pregabalin is rapidly absorbed in the fasting state, with peak plasma concentrations occurring within one h. Food reduces the absorption rate of the drug, resulting in lowered and delayed maximum plasma concentration without a clinically significant effect on the overall effectiveness of pain conditions. Following oral administration, Pregabalin reaches peak plasma concentrations within 1.5 hours and achieves a steady state within 24 to 48 hours. Its absorption is independent of the dose. The mean elimination half-life of patients with normal renal function is 6.3 hours.

The time taken by Pregabalin to work depends on the drug’s effectiveness on the system, the condition for which you have advised the medication and other systemic conditions that may affect the drug absorption. Several patients advised by Pregabalin have observed immediate results on using the drug, while in others, the analgesic effects took several weeks to appear. The best time to use it is in the evening to enable the analgesic and sedative effects of the drug.

You can take mild to moderate effect painkillers like Ibuprofen, Paracetamol and Aspirin as they will help with pain relief without compromising on the safety of the user. Strong analgesics like codeine, co-codamol, and dihydrocodeine can make you feel more sleepy if combined with Pregabalin. You can even use Tapentadol and Pregabalin to treat chronic pain conditions like osteoarthritis, keeping in mind to follow safety precautions.

Immediate Release Pregabalin dosage for back pain due to diabetic nephropathy is an initial dose of 50mg every eight hours followed by a maintenance dose of 100 mg every hour. the maintenance dose is increased only if 50 mg is insufficient for pain relief and if suggested by the physician. Care is taken not to exceed 300 mg/day during the entire usage period. Extended-release tablets are advised at an initial dose of 165 mg quarterly and a maintenance dose increased at 330mg quarterly in a day based on the response and tolerability of the patient.

Pregabalin, at fixed doses of 200 mg/day or greater, has proven effective in the acute treatment of DSM-IV-defined Generalized Anxiety Disorder. Studies have shown the early onset of clinical effects and efficacy across psychological anxiety and somatic anxiety symptoms from the dose. A maintenance dosage of 450 mg/day is effective in the prevention of relapse. Adverse effect profiles and studies in healthy volunteers have even suggested that Pregabalin has tolerability advantages over benzodiazepines and venlafaxine as a short-term treatment of anxiety.

There have been increased incidences of Pregabalin-induced side effects in the elderly on initiating the medication for anxiolytic relief. Dizziness, somnolence and impaired motor function are some of the side effects reported of using the drug in people over the age of 60. Pregabalin, in doses of 150-600 mg/day, was a safe and effective treatment of generalized anxiety disorder in patients 65 years and older. For neuropathic pain conditions, the dose is regulated per the physician’s advice for patient safety.


Pregabalin withdrawal symptoms begin within 12 hours to 7 days after quitting the medication and last up to 10 days. Withdrawal symptoms include nausea, dizziness, headaches, insomnia, and anxiety. It takes around two to three weeks for the effects to wear off completely. Tapering the dose will help get rid of the withdrawal effects in a safe manner.

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