Pregabalin

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Pregabalin (Lyrica) mechanism of action is not fully understood, but it is thought to affect the way that calcium enters nerve cells. This reduces the activity of some of the nerve cells in the brain and spinal cord, reducing the release of other neurotransmitters that are involved in pain, epilepsy and anxiety.

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Pregabalin.jpg

[edit] MECHANISM OF ACTION

Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.

Pregabalin is well absorbed after oral administration, is eliminated largely by renal excretion, and has an elimination half-life of about 6 hours.

[edit] INDICATIONS

  • Neuropathic pain (pain due to nerve damage) associated with diabetic peripheral neuropathy (DPN)
  • Postherpetic neuralgia (PHN) in patients who have had herpes zoster (shingles)
  • Adjunctive therapy for adult patients with partial seizures (epileptic fits starting in one specific part of the brain) that cannot be controlled with their current treatment
  • Fibromyalgia
  • Neuropathic pain associated with spinal cord injury (pain experienced by patients who have had a spinal cord injury)
  • Generalised Anxiety Disorder (long-term anxiety or nervousness). (Europe)

[edit] DOSAGE

Pregabalin is given orally with or without food.

When discontinuing Pregabalin, taper gradually over a minimum of 1 week.


Neuropathic Pain Associated with Diabetic Peripheral Neuropathy

Pregabalin treatment can be started at a dose of 150 mg per day given as two or three divided doses. Based on individual patient response and tolerability, the dose may be increased up to 300 mg per day after an interval of 3 to 7 days.


Postherpetic Neuralgia

The recommended dose of Pregabalin is 75 to 150 mg two times a day, or 50 to 100 mg three times a day. Begin dosing at 75 mg two times a day, or 50 mg three times a day (150 mg/day). The dose may be increased to 300 mg/day within 1 week based on efficacy and tolerability.

Patients who do not experience sufficient pain relief following 2 to 4 weeks of treatment with 300 mg/day, and who are able to tolerate Pregabalin, may be treated with up to 300 mg two times a day, or 200 mg three times a day (600 mg/day).


Adjunctive Therapy for Adult Patients with Partial Onset Seizures

Pregabalin treatment can be started with a dose of 150 mg per day given as two or three divided doses. Based on individual patient response and tolerability, the dose may be increased to 300 mg per day after 1 week. The maximum dose of 600 mg per day may be achieved after an additional week.


Management of Fibromyalgia

The recommended dose of Pregabalin for fibromyalgia is 300 to 450 mg/day. Begin dosing at 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability. Patients who do not experience sufficient benefit with 300 mg/day may be further increased to 225 mg two times a day (450 mg/day). Treatment with doses above 450 mg/day is not recommended


Neuropathic Pain Associated with Spinal Cord Injury

The recommended dose range of Pregabalin for the treatment of neuropathic pain associated with spinal cord injury is 150 to 600 mg/day. The recommended starting dose is 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability. Patients who do not experience sufficient pain relief after 2 to 3 weeks of treatment with 150 mg two times a day and who tolerate Pregabalin may be treated with up to 300 mg two times a day.


Generalised Anxiety Disorder

The dose range is 150 to 600 mg per day given as two or three divided doses. The need for treatment should be reassessed regularly.

Pregabalin treatment can be started with a dose of 150 mg per day. Based on individual patient response and tolerability, the dose may be increased to 300 mg per day after 1 week. Following an additional week the dose may be increased to 450 mg per day. The maximum dose of 600 mg per day may be achieved after an additional week.


Patients with renal impairment

Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. As pregabalin clearance is directly proportional to creatinine clearance, dose reduction in patients with compromised renal function must be individualised according to creatinine clearance (CLcr)

[edit] CONTRAINDICATIONS

Known hypersensitivity to pregabalin

[edit] WARNINGS AND PRECAUTIONS

  • Angioedema (e.g. swelling of the throat, head and neck) can occur, and may be associated with life-threatening respiratory compromise requiring emergency treatment. Discontinue Pregabalin immediately in these cases.
  • Hypersensitivity reactions (e.g. hives, dyspnea, and wheezing) can occur. Discontinue Pregabalin immediately in these patients.
  • Increased seizure frequency may occur in patients with seizure disorders if Pregabalin is rapidly discontinued. Withdraw Pregabalin gradually over a minimum of 1 week.
  • Antiepileptic drugs, including Pregabalin , increase the risk of suicidal thoughts or behavior.
  • Pregabalin may cause peripheral edema. Exercise caution when co-administering Pregabalin and thiazolidinedione antidiabetic agents.
  • Pregabalin may cause dizziness and somnolence and impair patients' ability to drive or operate machinery

[edit] INTERACTIONS

Since Pregabalin is predominantly excreted unchanged in the urine, undergoes negligible metabolism in humans (<2% of a dose recovered in urine as metabolites), and does not bind to plasma proteins, its pharmacokinetics are unlikely to be affected by other agents through metabolic interactions or protein binding displacement.

Oxycodone, lorazepam, or ethanol: Although no pharmacokinetic interactions were seen, additive effects on cognitive and gross motor functioning were seen when Pregabalin was co-administered with these drugs. No clinically important effects on respiration were seen.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Use Pregabalin during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: It is not known if pregabalin is excreted in human milk; it is, however, present in the milk of rats. Because many drugs are excreted in human milk, and because of the potential for tumorigenicity shown for pregabalin in animal studies, decide whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Most common adverse reactions (≥ 5% and twice placebo) are dizziness, somnolence, dry mouth, edema, blurred vision, weight gain and thinking abnormal (primarily difficulty with concentration/attention).

[edit] RELATED LINKS

Pharmacology of Antiepileptic Drugs

[edit] BIBLIOGRAPHY

[edit] REFERENCES