Pregabalin; Uses, Dosage, Side Effects, Interactions, Pregnanc

Pregabalin
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Pregabalin is a gamma-aminobutyric acid (GABA) derivative that functions as a calcium channel blocker and is used as an anticonvulsant as well as an anti-anxiety agent. It is also used as an analgesic in the treatment of neuropathic pain and fibromyalgia.
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Pregabalin is a 3-isobutyl derivative of gamma-aminobutyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation.
Pregabalin is an inhibitor of neuronal activity used for therapy of neuropathy and as an anticonvulsant. Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare.

Mechanism of Action of Pregabalin

Pregabalin binds presynaptically to the alpha2-delta subunit of the voltage-gated calcium channels in central nervous system tissues located in the brain and spinal cord. The mechanism of action has not been fully elucidated but studies suggest that pregabalin produces a disruption of calcium channel trafficking or a reduction of calcium currents. The inhibition of subunits of voltage-gated calcium channels reduces calcium release which in order inhibits the release of several neurotransmitters [FDA label] Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.
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Pregabalin is an anticonvulsant that is structurally related to the inhibitory CNS neurotransmitter gamma-aminobutyric acid (GABA). Pregabalin also has demonstrated analgesic activity. Although pregabalin was developed as a structural analog of GABA, the drug does not bind directly to GABA-A, GABA-B, or benzodiazepine receptors; does not augment GABA-A responses in cultured neurons, and does not alter brain concentrations of GABA in rats or affect GABA uptake or degradation. However, in cultured neurons, prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport.
Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissues. In vitro, pregabalin reduces the calcium-dependent release of several neurotransmitters, including glutamate, norepinephrine, and substance P, possibly by modulation of calcium channel function.

Indications of Pregabalin

Therapeutic Uses

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Therapeutic Indications of Pregabalin

  • Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy or spinal cord injury, and postherpetic neuralgia. It is not approved for the management of fibromyalgia or as adjunctive therapy for adult partial onset seizures.
  • Neuropathic pain: Lyrica is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy: Lyrica is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Neuropathic pain, Pregabalin Accord is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy, Pregabalin Accord is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized anxiety disorder; Pregabalin Accord is indicated for the treatment of generalized anxiety disorder (GAD) in adults.
  • Epilepsy; Pregabalin Mylan is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder; Pregabalin Mylan is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults
  • Neuropathic pain; Pregabalin Mylan Pharma is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy -  Pregabalin Mylan Pharma is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder -  Pregabalin Mylan Pharma is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
  • Neuropathic pain Pregabalin Pfizer is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy, Pregabalin Pfizer is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder, Pregabalin Pfizer is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
  • Neuropathic pain Pregabalin Sandoz is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy Pregabalin Sandoz is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder, Pregabalin Sandoz is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
  • Epilepsy, Pregabalin Sandoz GmbH is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized Anxiety Disorder, Pregabalin Sandoz GmbH is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
  • Epilepsy, Pregabalin Zentiva is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized anxiety disorder, Pregabalin Zentiva is indicated for the treatment of generalized anxiety disorder (GAD) in adults.
  • Neuropathic pain, Pregabalin Zentiva k.s. is indicated for the treatment of peripheral and central neuropathic pain in adults.
  • Epilepsy, Pregabalin Zentiva k.s. is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
  • Generalized anxiety disorder, Pregabalin Zentiva k.s. is indicated for the treatment of generalized anxiety disorder (GAD) in adults.

Contra-Indications of Pregabalin

Dosage of Pregabalin

Strengths : 25 mg; 50 mg; 75 mg; 100 mg; 150 mg; 200 mg; 300 mg; 225 mg; 20 mg/mL;

Diabetic Peripheral Neuropathic Pain

Regular-release capsules

  • Initial: 50 mg PO q8hr
  • Maintenance: May increase to 100 mg PO q8hr within 1 week, as needed; not to exceed 300 mg/day
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Extended-release tablets

  • Initial: 165 mg PO qDay
  • Maintenance: May increase to 330 mg PO qDay within 1 week based on response and tolerability; not to exceed 330 mg PO qDay
  • See also Administration

Postherpetic Neuralgia

Regular-release capsules

  • Initial: 150-300 mg/day PO divided q8-12hr
  • Maintenance: May increase to 300 mg/day divided q8-12hr after 1 week, as needed

Extended-release tablets

  • Initial: 165 mg PO qDay
  • Maintenance: May increase to 330 mg PO qDay within 1 week based on response and tolerability; not to exceed 330 mg PO qDay
  • Patients experiencing insufficient pain relief following 2-4 weeks of treatment with 330 mg PO qDay and tolerate the ER tablets, may be treated with up to 660 mg PO qDay

Fibromyalgia

  • Regular-release capsules and oral solution onl
  • Initial: 150 mg/day PO divided q12hr
  • Maintenance: May increase to 300-450 mg/day divided q12hr after 1 week, as needed

Epilepsy

  • Regular-release capsules and the oral solution only
  • Initial: 150 mg/d divided q8-12hr PO
  • Maintenance: May increase to 600 mg/day PO divided q8-12hr, as needed

Neuropathic Pain With Spinal Cord Injury

  • Initial: 150 mg/day PO divided q12hr; may increase within 1 week to 300 mg/day PO divided q12hr
  • If there is insufficient pain relief after 2-3 weeks and 300 mg/day dose is tolerated, may increase the dose again up to 600 mg/day PO divided q12hr

Dosing Modifications

Renal impairment (capsules/oral solution)

  • CrCl 30-60 mL/min
    • Decrease dose by 50% divided bid/tid
  • CrCl 15-30 mL/min
    • If 150 mg/day in normal renal function: Decrease dose to 25-50 mg/day; administer qDay or divided bid
    • If 300 mg/day in normal renal function: Decrease dose to 75 mg/day; administer qDay or divided bid
    • If 450 mg/day in normal renal function: Decrease dose to 100-150 mg/day; administer qDay or divided bid
    • If 600 mg/day in normal renal function: Decrease dose to 150 mg/day; administer qDay or divided bid
  • CrCl <15 mL/min
    • If 150 mg/day in normal renal function: Decrease dose to 25 mg/day; single daily dose
    • If 300 mg/day in normal renal function: Decrease dose to 25-50 mg/day; single daily dose
    • If 450 mg/day in normal renal function: Decrease dose to 50-75 mg/day; a single daily dose of divided bid
    • If 600 mg/day in normal renal function: Decrease dose to 75 mg/day; single daily dose
  • Supplemental dosage following hemodialysis
    • 25 mg qDay regimen: Take 1 supplemental dose of 25 mg or 50 mg
    • 25-50 mg qDay regimen: Take 1 supplemental dose of 50 mg or 75 mg
    • 50-75 mg qDay regimen: Take 1 supplemental dose of 75 mg or 100 mg
    • 75 mg qDay regimen: Take 1 supplemental dose of 100 mg or 150 mg

Renal impairment (ER tablets)

  • CrCl 30-60 mL/min
    • If 165 mg/day in normal renal function: Decrease dose to 82.5 mg/day
    • If 330 mg/day in normal renal function: Decrease dose to 165 mg/day
    • If 495 mg/day in normal renal function: Decrease dose to 247.5 mg/day
    • If 660 mg/day in normal renal function: Decrease dose to 330 mg/day
  • CrCl <30 mL/min or hemodialysis
    • Not recommended
    • Patients should only receive capsules or oral solution

Side Effects of Pregabalin

The most common

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Common

Rare

Drug Interactions of Pregabalin

Pregabalin may interact with the following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Pregabalin

FDA Pregnancy Category C

Pregnancy

Women of childbearing potential/Contraception in males and females. As the potential risk for humans is unknown, effective contraception must be used in women of childbearing potential. There are no adequate data from the use of pregabalin in pregnant women. The potential risk for humans is unknown.

Lactation

Pregabalin is excreted into human milk. The effect of pregabalin on newborns/infants is unknown. A decision must be made whether to discontinue breastfeeding or to discontinue pregabalin therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman. In a clinical trial to assess the effect of pregabalin on sperm motility, healthy male subjects were exposed to pregabalin at a dose of 600 mg/day. After 3 months of treatment, there were no effects on sperm motility.

A fertility study in female rats has shown adverse reproductive effects. Fertility studies in male rats have shown adverse reproductive and developmental effects. The clinical relevance of these findings is unknown.

References

Pregabalin

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