metformin - manara.edu.symanara.edu.sy/laravel-filemanager/files/2/metformin.pdf · title:...
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Metformin
By pharmacist:
Rasha Barhoum
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Contents
oHistory
oMechanism of action
oMetformin in Guidelines
oDosing
oSide effects
oContraindications
oPharmacokinetics
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Historical Overview• Galega officinalis (Middle ages) reduce DM
• Synthalin A&B less toxic 1920’s
• Advent of insulin 1930’s
• Jean Sterne (Paris) 1956
• UK 1958
• Canada 1972
• US 1995
• FDA approved 1994 !!!
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Mechanism of action
• Insulin sensitizer
• Increases glucose uptake and utilization by target tissues
• Decreases insulin resistance
• Lower risk of hypoglycemia due to its mechanism of action
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Metformin Mechanism of action
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Metformin in Guidelines
• First line agent
• >50 year old molecule
• Current guidelines from the ADA/EASD and the AACE/ACE recommend early initiation of metformin as a first-line drug for monotherapy and combination therapy for patients with T2DM
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Guidelines 2016
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Guidelines 2018
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Guidelines 2019
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Dosing• T2DM
• Initial 500mg po q12 hr or 850mg po qDaywith meals; increase dose in increments of 500 mg/week or 850mg/ 2 weeks
• Maintence dose 1500-2550 mg/day• PCO (off-label)
• 500 mg for 1-2 weeks then 500mg twice a day for 1-2 weeks then 500mg three times a day or 850mg twice a day for 1-2 weeks then 1g twice a day or 850mg three times a day
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Contraindication and cautious use
• Contraindicated:
• Renal / hepatic disease
• Acute MI
• Diabetic ketoacidosis
• Caution:
• 80 years old patient
• History of CHF
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pharmacokinetics
• Bioavailability: 50-60%
• Peak plasma: 2-3 hr
• Metabolism: Not by liver
• Half-life: 4-9 hr
• Excretion: urine (90% by tubular secretion)
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Thanks for listening