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drug profile

Iman Battikha

on 6 November 2012

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Transcript of Lyricamond

Pregabalin Lyricamond AMED Indications Dosing Special Population Adverse Effects FDA EMEA Neuropathic pain associated with
Diabetic Peripheral Neuropathy DPN

Neuropathic pain associated with Spinal Cord Injury SCI

Neuropathic pain associated with Post Herpatic Neuralgia PHN

Fibromyalgia Peripheral & Central
Neuropathic Pain Starting dose: 150 mg/day Divided BID or TID ≤ 1 week if needed 300
mg/day 600
mg/day Divided TID or BID Epilepsy as an adjunctive therapy
Generalized Anxiety Disorder Contraindicated:
Hypersensitivity to Pregabalin or any other component Mechanism of Action Reduce neurotransmission Pregabalin has higher affinity
to αalfa2-delta δsite than Gabapentin 6х Pregabalin Gabapentin Pregabalin has greater analgesic activity than Gabapentin ABSORPTION Pregabalin Gabapentin Bioavailability of all oral dose of Fixed ≥90% Absorption Pregabalin Gabapentin ≥ 90% 900mg 1200mg 2400mg 3600mg 60% 47% 34% 33% BID/TID TID Low dose-dependent
adverse effects Worsen dose-dependent
adverse effects Pregabalin-Possible Drug Interactions Pregabalin is easier to use than Gabapentin Pregabalin TCA
Amitriptyline SSNRIs
Duloxetine Alternation in
Absorption Alternation in
Hepatic metabolism Alternation in
Plasma binding
protein Interactions and metabolism Antacid and drug
affecting gastric acidity Liver enzymes
CYP2C -CYP3A4 Liver enzymes
CYP2D6 96% >90% Pregabalin has low potential for Pharmacokinatics Drug Interaction Anti acid and PPIs TCAs, SSNRIs, Cimetidine, Quinolone
Statins, B.Blockers , Ca channel blockers Phenytoin, Furosemide, Glyburide, Warfarin, Aspirin Distribution Pregabalin has been shown to readily Cross the Blood Brain Barrier
Cross the Placenta Pregabalin gets into targeted sites easily Pregabalin is easier to use than Gabapentin
Pregabalin has low potential for drug interaction
Pregabalin gets into targeted sites easily Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 RCT studies 2010
(n:1513) for DPN for 5-13 weeks Pregabalin is an IMPORTANT treatment option for older patients with pain of neuropathic origin Conclusion:
Pregabalin significantly reduced neuropathic pain in older patients (age ≥65 years)
The relative risks for these AEs is dose-related , but did not appear related to older age
Pregabalin known drug-drug interactions is absent 1- Slow titration
2- Minimal effective dose
3- Dose reduction in renal impariment
4- Drink a lot of water
5- Take it with food Dose related
Mild to moderate
Well tolerated in clinical trials
Minimized by slow dose titration Pregabalin Adverse Effects NOT associated with loss of glycemic control NO clinically significant effect on blood pressure In an overdose up to 15 g of pregabalin, no unexpected adverse effects were reported 150 mg 300 mg 600 mg ≥ 90% ≥ 90% Gabapentin
Duloxetine VS. ONLY ONLY
anticonvulsants 135 mg 270 mg 540 mg 540mg 750mg 800mg 1100mg Elimination Pregabalin has found to be eliminated UNCHANGED through kidneys >90% up to 100%
Excreted in breast milk

Inter-subject variability <2% Gabapentin: Dose-related adverse effects Amitriptyline: Avoided Duloxetine: Caution Dizziness, Solemnness, Mouth dry, Peripheral edema, Weight gain When discontinuing, taper gradually over a minimum of 1 week
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