This simple slide is about losartan. Those picture in my slide belong to Losartan manufacturer

1. Name : Danny Liew Teck Yee

2. Objective
 To learn what is Losartan
 To describe the mechanism of action of Losartan
 To state the adverse effects of Losartan

3. Contents
 Introduction
 Appearance
 Mechanism of action
 Pharmacokinetic
 Indication
 Dosage and administration
 Contraindication
 Precaution
 Pregnancy class
 Adverse effects
 Drug Interaction

4. Introduction
 Losartan – the first Angiotensin II receptor
developed in 1986
 Tradename : Cozaar
 Manufacturer: Merck Sharp and Dohme Limited
United Kingdom
•http://faculty.babson.edu/gbhardwaj/Losartan%2
0Case%20History%20-%20EODD.pdf
•http://www.merck.com/product/usa/pi_circulars
/c/cozaar/cozaar_pi.pdf

5. Introduction

6. Appearance
 Powder 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

7. Appearance
 Film-coated tablets form-
1. 50 mg – white color with mark 952 in teardrop shape
2. 100mg – white color with mark 960 in teardrop shape
http://www.mims.com/Malaysia/drug/info/Cozaar
/?q=losartan&type=brief

8. Introduction
 Chemical name: 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-
5-ylphenyl)benzyl]imidazole-5-methanol mono
potassium salt
 Empirical formula: C22H23ClN6O
 Structural formula:
http://structures.wishartlab.com/molecules/DB00678/image.png

9. Mechanism of Action
http://www.drugbank.ca/drugs/DB00678

10. Mechanism of Action
Losartan competitively inhibit the
binding of Angiotensin II to AT1 in
many tissues
This inhibitation prevent
vasoconstritive and asoconstrictive
and aldosterone-secreting effects
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

11. Pharmacokinetics
 Absorption : 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

12. Indication
 Hypertension
 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

13. Dose and Administration
 Hypertension- 50mg once daily, and may increases to
100mg once daily
 Hypertensive 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

14. Contraindication
 Patients who hypersensitive to Losartan
 Pregnant women
•http://www.mims.com/Malaysia/drug/info/Cozaa
r/?q=losartan&type=brief
•http://www.merck.com/product/usa/pi_circulars
/c/cozaar/cozaar_pi.pdf

15. Caution
 Hepatic 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

16. Pregnancy Class
 Class 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/Cozaa
r/?q=losartan&type=brief

17. Adverse Effects
 Dizziness
 Hypotension
 Hyperkalaemia
 Angioedema
•http://www.drugs.com/food-interactions/losartan.html
•British National Formulary 56 September 2008, page 105-106

18. Drug Interaction
Losartan
Potassium
sparing
diuretics or
potassium
supplements
Hyperkalaemia
•http://www.merck.com/product/usa/pi_circulars
/c/cozaar/cozaar_pi.pdf
•http://www.drugs.com/food-
interactions/losartan.html

19. Drug Interaction
Losartan Lithium
Lithium
toxicity
http://www.merck.com/product/usa/pi_circulars/
c/cozaar/cozaar_pi.pdf

20. 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

21. References
1. British National Formulary 56 September 2008, page 105-106
2. Drug Facts and Comparisons 2010, page 782-783
3. Martindale Edition 36, page 1326-1327
4. http://www.drugs.com/drug-interactions/losartan.html
5. http://www.mims.com/Malaysia/drug/info/Cozaar/?q=losarta
n&type=brief
6. http://www.drugbank.ca/drugs/DB00678
7. http://faculty.babson.edu/gbhardwaj/Losartan%20Case%20Hi
story%20-%20EODD.pdf
8. http://www.excitienps.com/losartan-powder-534363.html
9. http://www.merck.com/product/usa/pi_circulars/c/cozaar/co
zaar_pi.pdf