Mechanism of Action of Pregabalin
Indications of Pregabalin
- Treating diabetic peripheral neuropathy
- Treating postherpetic neuralgia
- Treating neuropathic pain associated with spinal cord injury.
- Epilepsy and Treatment of peripheral neuropathic pain
- Treating diabetic peripheral neuropathy
- Treating postherpetic neuralgia
- Treating neuropathic pain associated with spinal cord injury.
- Fibromyalgia
- Pain, Neuropathic
- Postherpetic Neuralgia
- Partial onset seizure Epilepsy,
- Convulsion
- Ankylosing spondylitis
- Pain due to especially musculoskeletal system
- Lumbago
- Pain due to demyelination of nerve
- Paresthesia, itching, numbness or radiating pain.
- Pain due to nerve instrument
- Low back pain
- PLID
- Polyarthralgia
- Muscles stiffness in nerve diseases
- Multiple joint pain
- Muscles stiffness in spinal
- Muscles stiffness in muscle diseases
- Trigeminal neuralgia
- a headache
- a toothache
- muscular aches
- a backache
- minor pain of arthritis temporarily reduces fever
- Polyarthralgia
- Muscles stiffness in nerve diseases
- Frozen shoulder
Therapeutic Uses
- Pregabalin is indicated for the management of post-herpetic neuralgia.
- Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy.
- Pregabalin is indicated as an adjunctive therapy for adult patients with partial onset seizures.
- The U.S. Food and Drug Administration has approved Lyrica (pregabalin), the first drug to treat fibromyalgia, a disorder characterized by pain, fatigue and sleep problems.
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
- Severely Decreased Platelets
- Having Thoughts of Suicide
- Persons to drug class common.
- Avoid abrupt withdrawal
- Renal impairment
- CHF class III, IV NYHA
- Angioedema risk
- Depression
- CNS depressant use
- Alcohol use
- The decrease in the Sharpness of Vision
- Atrioventricular Heart Block
- Chronic Heart Failure
- Suddenly serious symptoms of heart failure
- Rhabdomyolysis
- Drowsiness
- Dizziness
- Fluid Retention in the Legs
- Giant hives
- Moderate to Severe Kidney Impairment
- Muscle Pain or Tenderness with Increase Creatine Kinase
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
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
- Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness the day after taking the medicine.
- Vertigo
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- A headache.
- Skin rashes.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Common
- Constipation
- Frequently passing urine
- Loss of muscle coordination
- sleepiness or unusual drowsiness
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
- a light-headed feeling, like you, might pass out;
Rare
- Convulsions (seizures)
- hallucinations (seeing or hearing things that are not there)
- increase in muscle spasm, cramping, or tightness
- mood or mental changes
- unusual nervousness or restlessness
- Blurred or double vision
- muscle weakness (severe)
- irritability
- lightheadedness
- mood or mental changes
- shortness of breath or unusually slow or troubled breathing
Drug Interactions of Pregabalin
Pregabalin may interact with the following drugs, supplements, & may change the efficacy of drugs
- antacids containing magnesium or aluminum
- cimetidine
- tapentadol
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone
- barbiturates (e.g., butalbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- clonidine
- general anesthetics
- ketorolac
- mirtazapine
- muscle relaxants
- seizure medications (e.g., carbamazepine, phenytoin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- tapentadol
- thiazolidinediones (e.g., pioglitazone, rosiglitazone)
- tramadol
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
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
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