Pregabalin


Generic Medicine Info
Indications and Dosage
Oral
Neuropathic pain associated with diabetic peripheral neuropathy
Adult: As extended-release tab: Initially, 165 mg once daily, then increase to 330 mg once daily within 1 week. Max: 330 mg once daily. Adjust dose according to individual response and tolerability.

Oral
Postherpetic neuralgia
Adult: As extended-release tab: Initially, 165 mg once daily, then increase to 330 mg once daily within 1 week; after 2-4 weeks, may further increase up to a Max of 660 mg once daily. Adjust dose according to individual response and tolerability.

Oral
Neuropathic pain
Adult: For the treatment of peripheral and central pain: As conventional cap or oral solution: Initially, 150 mg daily, may increase to 300 mg daily after an interval of 3-7 days, then up to a Max of 600 mg daily after an additional 7-day interval. Doses are given in 2 or 3 divided doses. Adjust dose according to individual response and tolerability.

Oral
Partial seizures with or without secondary generalisation
Adult: Adjunctive therapy: As conventional cap or oral solution: Initially, 150 mg daily, may increase to 300 mg daily after 1 week, then up to a Max of 600 mg daily after another week. Doses are given in 2 or 3 divided doses. Adjust dose according to individual response and tolerability.

Oral
Fibromyalgia
Adult: As conventional cap or oral solution: Initially, 75 mg bid, may increase to 150 mg bid within 1 week, then to 225 mg bid if necessary. Max: 600 mg daily. Adjust dose according to individual response and tolerability.

Oral
Generalised anxiety disorder
Adult: As conventional cap or oral solution: Initially, 150 mg daily, may increase in increments of 150 mg at weekly intervals. Max: 600 mg daily. Doses are given in 2 or 3 divided doses. Adjust dose according to individual response and tolerability.
Renal Impairment
Neuropathic pain; Partial seizures with or without secondary generalisation; Generalised anxiety disorder; Fibromyalgia:
As conventional cap or oral solution: Patients on haemodialysis: Adjust daily dose according to renal function and a supplemental dose must be given immediately after each 4-hour haemodialysis treatment. Supplementary dose: 25 mg daily as a single dose. Max: 100 mg daily as a single dose.
CrCl (mL/min) Dosage
<15 As conventional cap or oral solution: Initially, 25 mg once daily. Max: 75 mg once daily.
≥15-<30 As conventional cap or oral solution: 25-50 mg daily. Max: 150 mg daily. Doses are given as a single or in 2 divided doses.
≥30-<60 As conventional cap or oral solution: 75 mg daily. Max: 300 mg daily. Doses are given in 2 or 3 divided doses.

Neuropathic pain associated with diabetic peripheral neuropathy; Postherpetic neuralgia:
As extended-release tab: Patients on haemodialysis: Not recommended.
CrCl (mL/min) Dosage
<30 As extended-release tab: Not recommended.
≥30-<60 As extended-release tab: Initially, 82.5 mg once daily, may increase to 165 mg once daily followed by 247.5 mg once daily up to a Max of 330 mg once daily. Dosing adjustment is based on indication (refer to specific product guidelines).
Administration
May be taken with or without food.
extended-release tab: Should be taken with food. Take after an evening meal. Do not split/crush/chew.
Contraindications
Hypersensitivity.
Special Precautions
Patient with diabetes, compromised respiratory function, respiratory or neurological disease, CHF, history of substance abuse, history of angioedema episodes. Patient taking CNS depressants. Avoid abrupt withdrawal (taper gradually over a minimum of 1 week). Renal impairment. Elderly. Pregnancy and lactation; avoid in pregnancy unless clearly necessary.
Adverse Reactions
Significant: Hypersensitivity reactions; dizziness, somnolence, loss of consciousness, confusion, mental impairment; blurred vision, loss of vision, or other changes in visual acuity; renal failure, withdrawal symptoms; convulsions including status epilepticus and grand mal convulsions (during or shortly after discontinuation), CHF (particularly in elderly with compromised CV system), increased risk of suicidal ideation and behaviour; misuse, abuse, and dependence; peripheral oedema, weight gain, increased creatine kinase, decreased platelet count.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, vomiting, abdominal distension, constipation, diarrhoea, dry mouth, flatulence.
General disorders and administration site conditions: Fatigue, oedema, abnormal gait, feeling drunk, fall, feeling abnormal.
Metabolism and nutrition disorders: Increased appetite.
Musculoskeletal and connective tissue disorders: Arthralgia, back pain, cervical spasm, muscle cramp, pain in limb.
Nervous system disorders: Headache, ataxia, abnormal coordination, amnesia, balance disorder, disturbance in attention, dysarthria, hypoaesthesia, lethargy, memory impairment, paraesthesia, sedation, tremor; encephalopathy (particularly in at-risk patients).
Psychiatric disorders: Disorientation, euphoric mood, insomnia, irritability.
Reproductive system and breast disorders: Decreased libido, erectile dysfunction.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis.
Potentially Fatal: Respiratory depression (particularly in patients with underlying respiratory impairment), angioedema with respiratory compromise.
PO: Z (Possible increased risk of major congenital malformation. Avoid unless benefits outweigh risks. If used until delivery, monitor neonate for withdrawal symptoms and toxicity.)
Patient Counseling Information
This drug may cause dizziness, drowsiness, and vision disorders, if affected, do not drive or operate machinery. Women of childbearing potential must use proven birth control methods during therapy.
Monitoring Parameters
Assess measures of drug efficacy (pain intensity or seizure frequency). Evaluate patients for history of substance abuse and potential for drug dependency. Obtain renal function tests (periodically); creatine kinase and platelet count (as clinically indicated). Monitor for signs and symptoms of suicidality (e.g. anxiety, suicidal thoughts, depression, behavioural changes), ocular disturbance, weight gain or oedema; respiratory depression and sedation (in patients with underlying respiratory disease).
Overdosage
Symptoms: Somnolence, reduced consciousness, agitation, confusional state, depression, anxiety, restlessness, seizures, and heart block. Rarely, coma. Management: Supportive and symptomatic treatment. Emesis or gastric lavage may be considered for the elimination of unabsorbed drug. Consider administration of activated charcoal; administration via nasogastric tube in patients who are not fully conscious or have impaired gag reflex may be considered once the airway is protected. Observe usual precautions to maintain the airway. Monitor vital signs and clinical status of the patient. May consider haemodialysis if necessary.
Drug Interactions
Concomitant use with drugs that have the potential to produce constipation (e.g. opioid analgesics) may result in reduced lower gastrointestinal tract function (e.g. constipation, paralytic ileus, intestinal obstruction). May potentiate the effects of lorazepam. May increase the risk of angioedema with ACE inhibitors. Increased risk of weight gain and/or fluid retention with thiazolidinedione antidiabetic agents.
Potentially Fatal: Increased risk of respiratory failure and coma when used concomitantly with opioids and/or other CNS depressants.
Food Interaction
CNS depressant effects of alcohol may be potentiated by pregabalin. Decreased bioavailability if taken without food (extended-release).
Action
Description: Pregabalin is an analogue of the neurotransmitter GABA. The mechanism of action has not been fully elucidated; however, it has been suggested that it binds potently to the α2-δ subunit of voltage-gated Ca channels in the CNS, resulting in modulation of the Ca channels and reduction in the release of several neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, calcitonin gene-related peptide, and substance P. It does not bind to GABA or benzodiazepine receptors. It may affect descending serotonergic and noradrenergic pain transmission pathways from the brainstem to the spinal cord.
Onset: Pain management: Within the 1st week of therapy.
Pharmacokinetics:
Absorption: Rapidly absorbed (fasted state). Decreased bioavailability if taken without food (extended-release). Bioavailability: ≥90%. Time to peak plasma concentration: Immediate-release: Within 1.5 hours (fasted state); approx 3 hours (with food). Extended-release: 8 hours; range: 5-12 hours (with food).
Distribution: Enters breast milk (small amounts). Volume of distribution: Approx 0.5 L/kg.
Metabolism: Undergoes negligible metabolism.
Excretion: Via urine (approx 90% as unchanged drug; minor metabolites). Elimination half-life: 6.3 hours.
Chemical Structure

Chemical Structure Image
Pregabalin

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5486971, Pregabalin. https://pubchem.ncbi.nlm.nih.gov/compound/Pregabalin. Accessed Oct. 26, 2022.

Storage
Store between 15-30°C.
MIMS Class
Anticonvulsants
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
References
Anon. Pregabalin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/10/2022.

Buckingham R (ed). Pregabalin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/09/2022.

Joint Formulary Committee. Pregabalin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/09/2022.

Lyrica 20 mg/mL Oral Solution (Upjohn UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 15/09/2022.

Lyrica 50 mg Hard Capsules (Upjohn UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 15/09/2022.

Lyrica 50 mg, 75 mg, and 150 mg Hard Capsules (Viatris Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 15/09/2022.

Lyrica Capsule; Solution (Parke-Davis Div of Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/02/2022.

Lyrica CR Tablet, Film-coated, Extended-release (U.S. Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/02/2022.

Pharmacy Retailing (NZ) Limited Trading as Healthcare Logistics. Pregabalin Pfizer Capsules data sheet 2 February 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 15/09/2022.

Pregabalin (Lyrica): Findings of Safety Study on Risks During Pregnancy. Medicines & Healthcare products Regulatory Agency. https://www.gov.uk. Accessed 15/09/2022.

Disclaimer: This information is independently developed by MIMS based on Pregabalin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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