is a chronic disease characterized by rise in blood pressure (systolic
pressure) or arterial pressure.
90-95% of hypertension. Also known as essential/ idiopathic hypertension
defined as hypertension with no known explanation.
due to overconsumption of Na+ or under consumption of K+
to a specific medical/ genetic conditions such as chronic kidney disease,
narrowing of arteries or endocrine disorders.
40% of worlds population ages 25+
cause of death and disabilities.
to Canadian Health Measures Survey 1 in 5 Canadian adults are affected.
rates are rising in Canada, recent reports show 85% of Canadians do not meet
their weekly recommended physical activities.
Funding for Hypertensive drugs have decreased both federally and by
Angiotensin 2receptors were the first target for developing compounds that
could inhibit the renin angiotensin pathway .
are also called as Angiotensin 2 receptor Antagonist and are the analouges of
Angiotensin II receptors.
types: AT1 and AT2
found in heart, brain, liver, kidney and adrenal glands.
function is to regulate blood pressure, fluids and electrolytes.
was a first angiotensin-receptor blocker (ARB) designed to treat hypertension.
It is uricosuric.
to lower blood pressure by competing with angiotensin II for its binding on AT1
by antagonizing the renin-angiotensin-aldosterone system..
was first approved in 1995 by FDA with the brand name of COZAAR.
sharp and Dhome corporation)
is well absorbed and undergoes substantial first-pass metabolism.
bioavailability of losartan is around 33%.
concentration of losartan is achieved in 1 hour and its active compound in
active metabolite, E-3174 is 10-40x more potent than losartan.
is metabolized to E-3174 (5-carboxylic acid derivative) primarily by cytochrome
oral administration 35% recovered in urine ,60% in feces.
IV administration 45% in urine ,50% in feces.
reduce the arterial pressure in normotensive rats.
was infused for 10 days in two groups of rat.
renin activity was supressed in Hna rats compared with
Arterial pressure in Nna rats reduced
Arterial pressure in Hna rats was unaffected.
aim of this study was to establish an optimized fast and safe protocol for the
pharmacological screening of losartan.
were divided into 7 group.
were give same dose of anesthesia.
was infused at different infusion rate.
continuous infusion of losartan at the dose of 1microgm/min for 20 min,
represent rapid and safe pharmacologic screening for losartan.
Other infusion rates did not produce the results that were necessary.
ossification of skull bone, feed intolerance.
arrhythmia in excess doses.
OPEN LABEL. RANDOMIZED ,2 PERIOD
CROSSOVER STUDY TO EVALUATE BIO EQUIVALENCE AFTER ADMINSTRATION OF
LOSARTAN 50mg VS COZAAR 50 mg
Dissolution of drugs in different medium.
water, 0.1 NaCl and phosphate buffer,
INVIVO Study .
Randomized crossover study in 60 adult healthy male.
Similarity in both formulation > 50% in all medium.
losartan was bioequivalent to Cozaar tablet in the term of rate extent of
EFFICACY AND SAFETY OF LOSARTAN IN DOUBLE BLIND CONTROLLED CLINICAL TRIAL
Patient with uncomplicated mild to moderate hypertension.
was given a placebo.
alone or in combination with hydrochlorothiazide was effective
tolerated with incidence similar to that of placebo.
adverse effect was found more was dizziness.
Safety of Amlodipine Plus Losartan Versus Amlodipine and Losartan monotherapy
in Patients With Essential Hypertension.
•440 patient was taken divided into 3 group.
•first group give losartan ,second amlodipine
•third group was given a combination of both.
•Group taking amlodipine proved to be more effected
•combination of both was more effective than
increased dose of either drug.
AN INDIAN POST MARKETING SURVEILLANCE.
and Safety of Losartan-amlodipine combination
by 109 doctors at 708 patients.
receive different doses of combination therapy.
was monitored for 20 days
in SBP WAS 19.90%.
in DBP was 17.70%.
of feet, palpitation. Muscular weakness , headache, insomnia