This document summarizes different classes of diuretic drugs, including their mechanisms of action and examples. It discusses loop diuretics that inhibit sodium reabsorption in the ascending loop of Henle; thiazide diuretics that inhibit sodium transporters in the distal convoluted tubule; carbonic anhydrase inhibitors that suppress carbon dioxide reabsorption in the kidney; potassium-sparing diuretics that decrease sodium transport in the collecting tubule; and osmotic diuretics that increase osmotic pressure in the proximal tubule to prevent water reabsorption. Examples are provided for common drugs in each class, along with their sites and mechanisms of diuretic action.
Measures of Dispersion and Variability: Range, QD, AD and SD
Word copy diuretics
1. Seminar on
DIURETICS
Submittedby
Samarjit Bose
Roll No:17401913041
Reg.No:13174021042
S_ID:B1309
B.Pharm, 3rd Year,6th Semester
Netaji Subhas Chandra Bose Institute of
Pharmacy
Tatla, Roypara, Chakdaha, Dist-Nadia, Pin- 741222
Affiliated to
2. Maulana Abul Kalam Azad University of
Technology
BF-142, Sector 1, Saltlake City, Kolkata-700064,West
Bengal.
ACKNOWLEDGEMENT
This seminar report entitled “DIURETICS” is by far the most significant
scientific accomplishment in my life and I was inspired to work in front
of my supervisor Principal Dr. Arnab Samanta. I take this opportunity to
humble acknowledge the contribution my supervisor, her philosophy to
venture into unknown field sciences opened up new avenues and horizons
before me while pursuing the investigation. Without her constant
encouragement, motivation, fruitful suggestions and inspiration my
review work would not have been materialized.
Next I thank and express my sincere gratitude to the Principal Dr. Arnab
Samanta and I wish to pay my humble respect to all of my teachers who
have nurtured and developed the loyal spirit of education in me for the
facilities has provided.
I am also expressing the thanks to review papers which I consulted during
my review work, I have acknowledged them in reference section of this
report.
Last but not the least; I dedicate the pleasure of presenting this report at
the lotus feet of the Almighty.
Samarjit Bose
(6th Semester, 3rd Year)
3. NETAJI SUBHAS CHANDRA BOSE
INSTITUTE OF PHARMACY
TATLA, ROYPARA, CHAKDAHA, NADIA, PIN 741222.
Estd. 2004
CERTIFICATE
This is to certify that the report entitled, “DIURETICS” submitted
by Mr. SAMARJIT BOSE, 3rdYear, 6thSemester under guidance
of Dr. Arnab Samanta in partial fulfilment for the award of degree
of B.Pharm under MAKAUT.
Dr. Arnab Samanta
Principal of NSCBIP
4.
5. 4
CONTENT PAGE NO
A. Definition………………………………....4
B. Pharmacological classification………….5
C. Loop diuretics…………………………... 7- 9
D. Thiazides……………………………….10-11
E. Carbonic anhydrase inhibitor………...12-13
F. Potassium sparing diuretics……………14-15
1. Aldosterone antagonists
2. Epithelial sodium channel blockers
G. Osmotic diuretics…….………………16-17
H. Reference…………………………………18
6. 5
DEFINITION :-
Diuretics are chemicals that increase the rate of urine formation. By
increasing the urine flow rate, diuretic usage leads to the increased
excretion of electrolytes (especially sodium and chloride ion) and
water from the body.
Diuretics are the drugs which cause a net loss of sodium ion and
water in urine. These drugs increase urine output by the kidney
(promote diuresis). This is accomplishedbyalteringhow the kidney
handles sodium. If the kidney excretes more sodium, then water
excretion will also increase. Most diuretics produce diuresis by
inhibiting the reabsorption of sodium at different segments of the
renal tubular system. Sometimes a combination of two diuretics is
given because this can be significantly more effective than either
compound alone (synergisticeffect).
Example of diuretics are caffeine, yerba mate, nettles, cranberry
juice, alcohol
• Natriuretic: substance that promotes the renal excretion of Na+
9. 8
Loop diuretics (Inhibitors of Na+K+2Cl -cotransport):-
High ceiling diuretics are diuretics that may cause a substantial
diuresis up to 20% of the filtered load of NaCl and water. This is
huge when compared to normal renal sodium reabsorption which
leaves only ~0.4% of filtered sodium in the urine. High ceiling
diuretics often synonymous with Loop diuretics.
Mechanism of action:
Loop diuretics inhibit the body's ability to reabsorb sodium at the
ascending loop in the kidney which leads to a retention of water in
the urine.
No transport systems in descending loop of henle.
Inhibits Na-K-2Cl transporter in thick ascending loopof henle.
Competes with Cl- binding site.
Use : a. edema: cardiacpulmonaryor renal,
b. hypertension
Example of loop diuretics include Furosemide, Bumetanide,
Ethacrynicacid and Torsemide
Use : a. edema: cardiacpulmonaryor renal,
b. hypertension
Example of loop diuretics include Furosemide, Bumetanide,
Ethacrynicacid and Torsemide
10. 9
A .Furosemide-
• The major site of action is the thick AscLH where furosemide
inhibits Na+-K+-2Cl-cotransport. A minor componentofaction on
PT has also been indicated. It is secreted in PT by organic action
transport and reaches Asc LH where it acts from luminal side of
the membrane. . K+ excretion is increased mainly due to high Na+
load reaching DT.
• Furosemide has weak Case inhibitory action,
• increase HCO3 excretion.
B. Bumetanide-
• Bumetanide is similar to furosemide in all respect, but is 40 times
more potent. A secondary action in PT has alsobeen demonstrated.
• It is often used in people in whom high dosage of
furosemide are ineffective.
• It is more lipid –soluble ,oral bioavailabilityis
80%-100%.itis preferred for oral use in severe CHF.
C. Ethacrynicacid-
• It is a loop diuretics used totreathigh blood pressure and swelling
caused by diseases like CHF.
12. 11
Thiazides :-
Thiazide is a type of molecule and a class
of diuretics often used to treat hypertension (high blood
pressure) and edema (such as that caused by heart, liver,
or kidney disease).
The thiazides and thiazide-like diuretics reduce the risk
of death, stroke, heart attack, and heart failure due to
hypertension
Mechanism of action :
active in distal convoluted tubule
inhibit Na+ and Cl- transporter in
distal convoluted tubules
increased Na+ and Cl- excretion
weak inhibitors of carbonic anhydrase,
increased HCO3- excretion
Use : a. hypertension.
b. congestive heart failure.
c. high blood pressure.
Example of thiazides include Chlorthalidone,
Hydroclorothiazide, Metolazone
13. 12
1. Hydrochlorothiazide - Hydrochlorothiazide
belongs to thiazide class of diuretics. It reduces
blood volume by acting on the kidneys to
reduce sodium (Na+) reabsorption in the distal
convoluted tubule.
2. Chlorothalidone - It is a particularly long bacting
compound .use exclusively asm antihypertensive.
3. Metolazone - Inhibit PO4 reabsorption is occur in
PT. Metolazone has been used mainly for edema
(5-10 mg/day, rarely 20 mg).
DRUG DAILY DOSE
(mg)
DURATION OF
ACTION
(hr)
Hydroclorothiazide 12.5-100 6-12
Chlorothalidone 50-100 48
Metolazone 5- 20 12-24
14. 13
4.Carbonic anhydrase inhibitor :-
High concentration of CA occur in ciliary process of
eye. CA enzyme involve in aqueous humor
formation.CA inhibitors reduce intraocular pressure
in glaucoma by decreasing production of aqueous
humor.
Mechanismof action :
Reversibly inhibits carbonic anhydrase in renal
proximal tubule cells.
carbonic anhydrase catalyzes formation of HCO3- and
H+
from H2O and CO2.
Suppress CO2 reabsorption from glomerular filtrate.
Na+ - HCO3
- excretion is increased.
Use : a. used to treat chronic open-angle
glaucoma
b. aqueous humor has high [HCO3-]
c. acute mountain sickness.
Example of carbonic anhydrase inhibitor
include Acetazolamide.
15. 14
1. Acetazolamide –
• Acetazolamide (a seet" a zol' a mide) is inhibitorSE4 of carbonic
anhydrase, an enzyme that converts carbon dioxide and water to
carbonic acid. Inhibition of this enzyme in the kidney causes an
alkalization of the urine and diuresis. In the eye, inhibition of
carbonic anhydrase causes a decrease in intraocular pressure
making these agents valuable in the treatmentof glaucoma.
• Acetazolamide is available in 125 and 250 mg tablets in generic
forms and under the brand name of Diamox.
16. 15
Potassium sparing diuretics :-
Aldosterone antagonists and renal epithelial Na+
channel inhibitors indirectly conserve k+ while inducing
mild natriuresis, and are called potassium sparing
diuretics.
Mechanismof action :
K+ sparing diuretics function in CCD
Do not promote the secretion of potassium into the
urine.
decrease Na+ transport in collecting tubule.
Aldosterone antagonist- These medicines
block the action of a hormone called aldosterone and
this causes the kidney to pass out more fluid and keep
potassium. This is why they are sometimes referred
to as aldosterone antagonists. Example of this
antagonist include Spironolactone.
Inhibitor of renal epithelial Na+ channel-
Triamterene and amiloride are two nonsteroidal
organic base with identical action. their most
important effect is to decrease K+ excretion,
particularly when it is high due to large K+ intake
or use of a diuretic that enhances K+ loss. This is
accompanied by a small increase of Na+ excretion.
17. 16
Use : a. primary hyperaldosteronism
b. cirrhosis
Example of potassium sparing diuretics include
Spironolactone , Triamterene, Amiloride.
18. 17
.
Osmotic diuretics :-
Osmotic diuresis is the increase of urination rate caused
by the presence of certain substances in the small tubes of
the kidneys.[2] The excretion occurs when substances
such as glucose enter the kidney tubules and cannot be
reabsorbed (due to a pathological state or the normal
nature of the substance). The substances cause an
increase in theosmotic pressure within the tubule,
causing retention of water within the lumen, and thus
reduces the reabsorption of water, increasing urine
output (i.e. diuresis).
Mechanismof action :
osmotic diuretics are not reabsorbed.
increases osmotic pressure specifically in the
proximal tubule and loop of Henle.
prevents passive reabsorption of H2O.
increased Na+ excretion.
Use : a. drug of choice: non-toxic, freely filtered,
non-absorbable
b. administered prophylactically for CVS
disease, surgery.
c. for acute renal failure secondary to trauma.
19. 18
Example of osmotic diuretics include Manitol,
Urea, Glycerol
Manitol –
Manitol is a nonelectrolyte of low molecular
weight (182) that is pharmacologically inert ,can be
rise osmolarity of plasma and tubular fluid. It is
minimally metabolized in the body ,freely filtered at
the glomerulus and undergoes limited reabsorbtion.
20. 19
REFERENCE:-
A. KD TRIPATHI MD (Ex-Director-Professor and Head of
Pharmacology Maulana Azad Medical College and associated LN
and GB Pant Hospitals New Delhi), Essentials of Medical
Pharmacology, 5th Edition, 2003: 521-537.
B. http://en.wikipedia.org/wiki/Diuretic.
C.http://www.medpagetoday.com/MeetingCoverage/ HFC/ 32821