a brief information a bout losartan for medical students

1. Losartan
NAME : MUHAMMAD SHAHZEB
SUBJECT : CLINICAL PHARMACY
ROLL NO : 29
SEMESTER : 7

2. A) Introduction :
Losartan (Cozaar) belongs to a group of drugs called angiotensin II
receptor antagonists (ARBs). It keeps blood vessels from narrowing, which
lowers blood pressure and improves blood flow.
It is on the World Health Organization's List of Essential Medicines, the most
most effective and safe medicines needed in a health system.

3.  B) i- Chemical name : ( –Butyl–4Chloro–1-[(2–(1htetrazol–5–yl)[11–
biphenyl]- 4yl methyl]–1h–imidazole–5–methanol potassium
 ii- Structure :

4.  iii) Molecular formula : C22H23ClN6O
 iv) Molecular weight : 461.00
 V) Melting Point : 184 °C
 Description : white crystalline Powder

5. 1
losartan Cozaar Tablet 100mg Merch sharp
and Dhome of
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- Encertine Tablet 25 mg English
Pharmacutical
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- Eziday Tablet 100 mg Werrick
Pharmaceutic
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- Corik Tablet 50 mg Razee
therapeutics
PVT LTD.
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- Cardive Tablet 50mg Olive
Laboratories.

10. 2) Indication :
Treatment of hypertension, to lower blood pressure in adults and
children greater than 6 years old. Lowering blood pressure
the risk of fatal and nonfatal cardiovascular events, primarily
and myocardial infarctions
 Reduction of the risk of stroke in patients with hypertension and
left ventricular hypertrophy. There is evidence that this benefit
does not apply to Black patients.
 Treatment of diabetic nephropathy with an elevated serum
creatinine and proteinuria in patients with type 2 diabetes.

11. Side Effects :
GIT: diarrhea, abdominal pain, dyspepsia, nausea.
CVS: chestpain,edema,hypotension
CNS:dizziness,fatigue,headache,insomnia,weaknes

12.  ADVERSE REACTIONS “
Most common adverse reactions (incidence ≥2% and
greater than placebo) are:
i) dizziness
ii) upper respiratory infection
iii) nasal congestion and
iv) back pain

13. 3) DOSAGE FORMS AND STRENGTHS:
Tablets: 25mg; 50mg; and 100mg.
Route of Administration: ORAL

14. 4) Dosage & Administration :
 In Hypertension;
Usual adult dose: 50mg once daily
Usual pediatric starting dose: 0.7 mg per kg once daily (up to 50 mg)
 In Hypertensive Patients with Left Ventricular Hypertrophy;
Usual starting dose: 50mg once daily Add hydrochlorothiazide 12.5mg
to 100 mg losartan
followed by an increase to hydrochlorothiazide 25mg
if further blood pressure response is needed.
 In Nephropathy in Type 2 Diabetic Patients;
Usual dose: 50mg once daily.
Increase dose to 100 mg once daily if further blood pressure
response is needed.

15.  5) Clinical Pharmacology:
A)Pharmacodynamics :
Mechanism of action ;
As we know that losartan potassium is a non-peptide molecule,
angiotensin II receptor (type AT1) antagonist . Losartan and its principal
active metabolite block the vasoconstrictor and aldosterone-secreting effects
effects of angiotensin II by selectively blocking the binding of angiotensin II
to the AT1 receptor found in many tissues, (e.g., vascular smooth muscle,
adrenal gland)

19. b. Pharmacokinetics :
Absorption:
Following oral administration, Losartan is well absorbed and undergoes
substantial first-pass metabolism; the systemic bioavailability of Losartan is
approximately 33%.
Distribution:
The volume of distribution of Losartan and the active metabolite is about 34
liters and 12 liters, respectively.
Biotransformation:
About 14% of an orally administered dose of Losartan is converted to the
active metabolite

20. Metabolism:
Losartan Potassium undergoes substantial first-pass metabolism by cytochrome P450
enzymes. In vitro studies indicate that cytochrome P450 2C9 and 3A4 are involved in
the biotransformation of Losartan to its metabolites.
Excretion:
When Losartan is administered orally, about 4% of the dose is excreted unchanged in
the urine and about 6% is excreted in urine as active metabolite.

21.  DRUG INTERACTIONS :
i) Lithium: Risk of lithium toxicity.
ii) NSAIDs: Increased risk of renal impairment and reduced diuretic,
natriuretic, and antihypertensive effects.
iii) Dual inhibition of the renin-angiotensin system: Increased risk of
renal impairment, hypotension, syncope, and hyperkalemia.

25. Warning :
When pregnancy is detected, discontinue losartan as soon as possible.
Drugs that act directly on the renin-angiotensin system can cause injury and
death to the developing fetus.
Precaution :
Hypotension: Correct volume or salt depletion prior to administration of
losartan k.
Monitor renal function and potassium in susceptible patients.

26.  Reference's :
 https://www.webmd.com
 https://en.wikipedia.org
 https://www.quora.com
 https://www.drugs.com/losartan.html