losartan simple presentation
DESCRIPTION
This simple slide is about losartan. Those picture in my slide belong to Losartan manufacturerTRANSCRIPT
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LosartanName : Danny Liew Teck Yee
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ObjectiveTo learn what is Losartan
To describe the mechanism of action of Losartan
To state the adverse effects of Losartan
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ContentsIntroductionAppearanceMechanism of actionPharmacokineticIndicationDosage and administrationContraindicationPrecautionPregnancy classAdverse effectsDrug Interaction
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IntroductionLosartan – the first Angiotensin II
receptor developed in 1986
Tradename : Cozaar
Manufacturer: Merck Sharp and Dohme Limited United Kingdom
• http://faculty.babson.edu/gbhardwaj/Losartan%20Case%20History%20-%20EODD.pdf
• http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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Introduction
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AppearancePowder form – A white to off-white powder,
freely soluble in water; slightly soluble in acetonitrile; soluble in isopropyl alcohol
http://www.excitienps.com/losartan-powder-534363.html
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AppearanceFilm-coated tablets form-1. 50 mg – white color with mark 952 in
teardrop shape2. 100mg – white color with mark 960 in
teardrop shape
http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losartan&type=brief
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IntroductionChemical name: 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-methanol mono potassium salt
Empirical formula: C22H23ClN6OStructural formula:
http://structures.wishartlab.com/molecules/DB00678/image.png
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Mechanism of Action
http://www.drugbank.ca/drugs/DB00678
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Mechanism of ActionLosartan competitively inhibit the binding of Angiotensin II to AT1 in many tissues
Result : It decreased vascular resistance and blood pressure.
• http://www.drugbank.ca/drugs/DB00678• www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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PharmacokineticsAbsorption : Bioavailability is 33%
Distribution : Volume of distribution of Losartan is 34 L, 99.7% bound to albumin
Biotransformation : About 14% of orally administered Losartan convert to active metabolite
Elimination : about 4% of the dose is excreted unchanged in the urine and about 6% is excreted in urine as active metabolite.• http://www.drugbank.ca/drugs/DB00678
http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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IndicationHypertension
Hypertensive patients with left ventricular hypertrophy except Black African patient
Nephropathy in Type 2 Diabetic Patients
• Drug fact and comparison 2010, page 782• http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf• British National Formulary 56 September 2008, page 105-106
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Dose and AdministrationHypertension- 50mg once daily, and may
increases to 100mg once dailyHypertensive patients with left ventricular
hypertrophy- 50 mg once per daily, may co-administration with 12.5 mg of hydrochlorothiazide
Neuropathy in Type 2 diabetes mellitus - starting dose is 50mg once per day, and may increases to 100mg once per day based on blood pressure response.
• Drug fact and comparison 2010, page 782• British National Formulary 56 September 2008, page 105-106• http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losartan&type=brief • http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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ContraindicationPatients who hypersensitive to Losartan
Pregnant women
• http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losartan&type=brief
• http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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CautionHepatic impairments - Data showing plasma
concentration of Losartan increased in cirrhotic patients
Renal impairments – Some patients reported reversible renal failure
Lactation – Unknown if it excreted to human milk. A research shown losartan excreted in rat milk.
• http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losartan&type=brief http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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Pregnancy ClassClass D in 2nd and 3rd trimesters
There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk
• Drug fact and comparison 2010, page 782- 783
• http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losartan&type=brief
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Adverse EffectsDizziness
Hypotension
Hyperkalaemia
Angioedema
• http://www.drugs.com/food-interactions/losartan.html• British National Formulary 56 September 2008, page 105-
106
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Drug Interaction
Losartan
Potassium
sparing
diuretics or
potassium
supplements
Hyperkalae
mia• http://www.merck.com/product/usa/
pi_circulars/c/cozaar/cozaar_pi.pdf• http://www.drugs.com/food-
interactions/losartan.html
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Drug Interaction
Losartan
Lithium
Lithium
toxicity
http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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Drug interaction
Losartan
NSAIDS
Decreases of
effect of
Losartan
• http://www.drugs.com/drug-interactions/losartan.htmll
• http://www.merck.com/product/usa/pi_circulars/c/cozaar/cozaar_pi.pdf
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References1. British National Formulary 56 September 2008, page 105-
1062. Drug Facts and Comparisons 2010, page 782-7833. Martindale Edition 36, page 1326-13274. http://www.drugs.com/drug-interactions/losartan.html5. http://www.mims.com/Malaysia/drug/info/Cozaar/?
q=losartan&type=brief6. http://www.drugbank.ca/drugs/DB006787. http://faculty.babson.edu/gbhardwaj/Losartan%20Case
%20History%20-%20EODD.pdf8. http://www.excitienps.com/losartan-powder-534363.html9. http://www.merck.com/product/usa/pi_circulars/c/cozaar/
cozaar_pi.pdf
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