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BY:
RAQSHAN JABEEN [14S61T0020]]
PHARM-D III YEAR
AUCOP,
JNTUH
GENERAL
ACKNOWLEDGEMENT
TO THE ALMIGHTY AND ALL
THE READERSā€¦..
THANKFUL TO U ALL FOR
GUIDANCE , SUPPORT AND
ENCOURAGEMENT ā€¦ā€¦
2
ANTI- INFECTIVES
- Anti-infective are drug that can either kill an
infectious agents or inhibit it from spreading.
- Anti-infectives include
ļƒ¼Antibiotics and Antibacterial.
ļƒ¼Antifungal.
ļƒ¼Antiviral.
ļƒ¼Antiprotozoals &
ļƒ¼Anthelmintis. 3
S.NO EXAMPLES
1. Anti-fungal ā€¢ Azole antifungal
ā€¢ Echinocandins
ā€¢ Miscellaneous antifungal
ā€¢ Polyenis
2. Antibiotics and Antibacterial. ā€¢Miscellaneous antibiotics
ā€¢Orazolidinone antibiotics
ā€¢Pencillines.
3. Antiviral. ā€¢Anti viral boosters
ā€¢Anti viral combination
ā€¢Anti viral infections
.4 Antiprotozoals . ā€¢Pentamidine
ā€¢Pyrimethamine
ā€¢Tinidazole
5. Anthelmintis. ā€¢Mebendazole.
ā€¢Ivermectin.
ā€¢Albendazole. 4
URINARY TRACT
INFECTIONā€¦
5
GENERAL INTRODUCTION:
ļ‚§ A urinary tract infection (UTI) is an infection in any
part of urinary system ā€“ kidney, ureters, bladder and
urethra.
ļ‚§ It is define as the presence of at least 1 lakh bacteria
per ml of urine (normal bacterial count=1000 per ml
of urine).
ļ‚§ Most infections involve the lower urinary tract the
bladder and the urethra.
ļ‚§ It is common disorder at all ages in both males and
females. 6
EPIDEMOLOGY:
ļƒ˜UTI is the 2nd most common infections present
in community practices.
ļƒ˜World wide, about 150 million people are
diagnosed with UTI each year .
ļƒ˜Prevalence 35% of healthy women suffer
symptoms of UTI at some time in their life.
7
ETIOLOGY:-
ļƒ¼The causative organism causing UTI are:-
E.Coli , Pseudomonas aeroginosa,
Streptococcus faecalis, Staphylococcus
epidermis and Proteus mirabilis.
ļƒ¼Waiting for long to urinate.
ļƒ¼Sexual transmitted diseases [STD] like
gonorrhea causes urethritis .
ļƒ¼Presence of tumor/ stones/ foreign bodies in
urinary tract.
8
Continuedā€¦.
Following can cause germs to
enter into bladder or kidney
And cause UTI:-
- Having bubble bath
- Wearing tight fitting clothes
Risk factors :-
ļƒ¼Being pregnant .
ļƒ¼Wearing tight fitting clothes.
ļƒ¼Diabetic.
9
SIGNS
AND SYMPTOMS:
ā€¢Abrupt onset of micturation.
ā€¢Pain in urethra during
voiding.
ā€¢Supra pubic pain and
tenderness.
ā€¢Haematuria (blood in urine).
ā€¢Dysuria .
ā€¢Fever, Feeling tired, apathy,
shaky.
ā€¢Pressure in lower belly. 10
Continuedā€¦.
Part of urinary tract
affected
Signs and Symptoms
Kidneys (acute Pyelonephritis) Upper back and side (flank) pain
High fever
Shaking and chills
Nausea
Vomiting.
Bladder (cystitis) Pelvic pressure
Lower abdomen discomfort
Frequent painful urination
Blood in urine.
Urethra (urethritis) Burning with urination
Discharge. 11
PATHOGENESIS
ā€¢ In many cases, bacteria first travel to the
urethra. When bacteria multiply, an infection can
occur. An infection limited to the urethra is called
urethritis.
ā€¢ If bacteria move to the bladder and multiply, a
bladder infection, called cystitis.
ā€¢ If the infection is not treated promptly, bacteria
may then travel further up the ureters to multiply
and infect the kidneys. A kidney infection is
called pyelonephritis. 12
CLASSIFICATION OF UTI
UTI
Acute
Infection
Chronic
Infection
13
Complicated UTI Uncomplicated UTI Primary UTI Recurrent UTI
DRUG THERAPY/ TREATMENT
S.NO AGENTS EXAMPLES
1 Bacteriostatics agents Sulfonamides
Tetracycline
Nitrofurantion
2 Bactericidal agents Cotrimoxazole
Ampicillin
Fluroquinolones
Cephalosporins
Aminoglycosides
3 Urinary Antiseptic Nitrofurantoin
Nalidixic acid
Methanamine Mandelate
14
15
SULPHANAMIDES
ā€¢ The term ā€˜sulfonamideā€™ is employed as generic name for
derivatives of para aminobenzene sulfonamide (sulfanilamide)
ā€¢ 1st effective chemotherapeuutic agent ,for the prevention and
use of bacterial infections in man.
ā€¢ DOMAGK(1932) discovered that prontosil protected mice
against streptococcal infections.
CLASSIFICATION:-
1. Poorly absorbed , locally acting:- sulphasalazine
2. Well absorbed , rapidly excreted:- sulphadiazine
3. Readily absorbed, medium rate of excretion:- sulphafurazole
4. Readily absorbed, slowly excreted:- sulphametopyrazine
16
SULPHAMETHOXAZOLE/
TRIMETROPRIM
PROPERTIES:
o It is a white, odourless , crystalline powder and is bitter in taste .It is
employed principally in lower urinary track & systemic infections
caused by E.COLI.
USES:-
ā€¢ Nocardia (DOC), Mycobacteria, Gram ā€“ve infections, Gram +ve
infections, Fungus ā€“ Pneumocystis carinii, Protozoa ā€“ Toxoplasma
gondii.
ā€¢ Sulfonamides are conjugated in the liver and their metabolites are
excreted in the kidney which can cause crystalluria.
They are high protein bounding drugs. Can cause kernicterus in
neonates.
ā€¢ It is used in treatment of several infections including AIDS. 17
M.O.A
They compete with PABA to
bind to dihydropteroate
synthetase and inhibit
conversion of PABA and
dihydropteroate diphosphate to
dihydrofolic acid, or
dihydrofolate. Inhibiting the
production of dihydrofolate
intermediate interferes with the
normal bacterial synthesis of
folic acid (folate). Since it
inhibits bacterial growth,
sulfamethoxazole is considered
a bacteriostatic antibiotic. 18
Synthesis
19
Continuedā€¦.
DOSAGE:-
o oral:-500mg or 1g tablets.
o suspension (100mg/1ml).
DOSE:-
ļƒ¼ oral 2g , followed by 1g every 8 hrs.
ADVERSE DRUG REACTIONS:-
ļƒ˜ Itching , Rash , Diarrhea, Headache , loss of appetite ,
hepatitis, stevnes. Johson syndrome , bloody urine,
allergic reactions ,decrease blood platelets , hemolytic
anemia , depression, drowsiness. 20
NITROFURANTION
PROPERTIES and USES: -
ā€¢ It is a lemon yellow odourless with a bitter taste powder.
ā€¢ It is very slightly soluble in water.
ā€¢ It is a white anti-bacterial spectrum both gram+ve and
gram-ve bacteria.
ā€¢ It is also active against many strains of Ecoli and
Enterococci.
ā€¢ Mainly used in the treatment of uncomplicated UTI.
ā€¢ Plasma half life is 0.3 ā€“ 1 hour.
21
Continuedā€¦.
MOA: -
The MOA of nitrofuratonin is unique and complex the
drug works by damaging bacteria DNA since it reduced
form is highly reactive. This is made possible by rapid
reduction of nitrofuratonin inside the bacterial cell by
flavoproteins to multiply reactive intermediators that acts
on ribosomal proteins. The broads mechanism of action
for this drug likely is responsible for the low development
of resistance to its effect as a drug effects many different
processes important to bacterial cells.
22
DOSAGE: -
Oral for adults :- 50-100 mg
every 6 hours with meals and at bed time .
23
Continuedā€¦.
Continuedā€¦.
ā€¢ ADVERSE EFFECTS: - Nausea, vomiting,
intestinal fibrosis, may occur in chronic
therapy, jaundice also occur.
ā€¢ Preparations: - Include tablets/ capsules
50&100 mg & a suspension 25mg 15ml .
ā€¢ A microcrystallines preparation
(macrodantin)which may be less nauseating is
available in capsules 25-150mg.
24
25
5 ā€“ETHYL-5,6-DIYDRO-8-ORC- 1,3 DIONOLO(4,5-
g)quinoline-7- carboxylic acid
26
PROPERTIES AND USES:-
It is fourth generation quinolone antibiotic.
Oral availability % = >90
T(1/2)= 6-8 hrs
It is used treat a number of bacterial infections including sinusitis ,
pneumonia , urinary tract infections, pelvic infections.
DOSAGES:-
500mg. OD for 7-14 days.
MOA:-
Inhibiting bacterial DNA gyrase primarily in gram negative bacteria
Inhibiting bacterial topoisomerase IV primarily in gram positive bacteria.
SYNTHESIS:-
ADRā€™S:-
nausea, diarrhea, trouble sleeping
Major:- tendon rupture or inflammation ,
seizures , psychosis , peripherial nerve damage.
27
PROPERTIES AND USES:-
ā€¢ It is one of the most promising newer member of the fluroquinoline family. In this
product, the N-ethyl moiety has been made rigid by incorporation into a heterocyclic
ring. It is useful in the treatment of genito-urinary, respiratory , gastrointestinal, skin
and soft tissue infection and gonorrhea.
MOA:-
ā€¢ It inhibits the enzyme bacterial DNA gyrase and prevents and replication of bacterial
DNA during bacterial growth and reproduction.
DOSAGES:-
ā€¢ 100, 200mg tablets; 200-450 mg daily usually for 5-7 days.
ADRā€™S:-
ā€¢ GTI upset, skin reaction, CNS disturbances.
ā€¢ -Metabolized by N- demethylation, N- oxidation and O- acyl glucomidation.
CONTRA-INDICATED:-
ā€¢ It is contraindicated for children below 16yrs, pregnant and lactating women and
history of epilepsy.
28
Synthesis
29
PROPERTIES :-
ā€¢ It is very effective for the treatment of UTI.
ā€¢ (t1/2=3-4hrs).
USES:-
ā€¢ To Treat endocarditis , gastroenteritis, malignant
otitis enterna, respiratory tract infections etc.
DOSAGES:-
ā€¢ Tab:- 250,500 or 750 mg.
ā€¢ UTI:- 250mg twice daily. 30
31
MOA:-
ā€¢ Itā€™s a broad spectrum antibiotic of the
fluoroquinolone class.
ā€¢ It is active against both gram positive and
negative bacteria. It functions by inhibiting
DNA gyraseand type lltopisomerase,
topisomerase lV , necessary to separate
bacterial DNA thereby inhibiting cell
division. 32
ADRā€™S:-
ā€¢ Diarrhoea
ā€¢ bloody 1 black stools
ā€¢ change in skin colour
ā€¢ chest pain or discomfort
ā€¢ confusion,
ā€¢ coughing / spitting up blood.
ā€¢ Increase heart beat
ā€¢ joint pains. 33
ļ±Tetracycline is a group of
antibiotic that obtained by
fermentation from streptomyces
spp. Or by chemical
transformation of natural
products.
ļ±They are derivatives of an
octahydronaphthacene , a
hydrocarbon system that
comprises four annulated six
member rings.
IUPAC ID: (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-
octahydro
-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-
carboxamide
34
35
PROPERTIES:-
ā€¢ Formula: C22H24N2O8
ā€¢ Molecular weight: 444.44
ā€¢ Melting Point: 170-173Ā°C (with decomposition)
ā€¢ Colour /Crystalline: cr (+3w)
USES:-
ā€¢ First-Line Drug: it is used as first line drug to treat venereal
diseases, cholera, relapsing fever.
ā€¢ Second-Line Drug: Penicillin for leptospirosis.
ā€¢ They are used in urinary tract infections in which causative organism
are sensitive.
ā€¢ As a prophylactic in chronic obstructive lung diseases. 36
37
SYNTHESIS OF
TETRACYCLINE
38
DOSAGES:-
ā€¢ 1g daily in 2-4 divided doses.
Storage:-
ā€¢ In light , light resistant container.
ADRā€™S:-
ā€¢ Hypersensitivity like rashes, urticaria, pruritus, glossitis,
vulva, and dermatitis.
ā€¢ Prolonged usage in diabetes, leucopenia causes super
infections.
ā€¢ Ataxia, Vertigo are produced when minocycline is
discontinued.
39
40
ā€¢ Cephalosporin's are discovered by G.Brotzu
of Sardinia made cultures from sea water at
a sewage, this might contain organisms
antagonistic to intestinal pathogens.
ā€¢ Ccephalosporin's have 7-amin
cephalosporanic acid nuclues. Which closely
resemble to 6-APA nucleus of pencillins.
Structurally they contain beta-lactam and
dihydrothiazine ring .
ā€¢They are water soluble and stable to
changes in PH and Temperature.
41
GUIDANCE PRINCIPLES
FOR THE USE OF CEPHALOSPORINS :
ļ¶ Cephalosporin's are expensive and should not be
used where an equally effective , alternative
antibiotic is available.
ļ¶ None of them is the agent of choice against
anaerobic infections .
ļ¶ None of them is effective against infectious by
enterococci (strep.fecalis)
PROPERTIES:-
ā€¢ White color.
ā€¢ State: crystals.
ā€¢ Solubility: very soluble in water, dilute aqueous
solution, insoluble in organic solvents.
ā€¢ Stability :The alpha -amino group of cephalenin
render its acid stable and the 3- methyl group is
responsible for metabolic stability.
ā€¢ P.Ka : 5.2, 7.3 42
43
44
DOSAGES:-
ļ±ORAL- 200-500 mg every 6 hrs.
ļ±Children's- 18.8-25 mg/kg every 6hrs.
MOA:-
It acts by inhibiting bacterial cell wall synthesis, lack of
bacterial cell wall results in death due to lysis of bacteria.
ADRā€™S:-
Diarrhea, dyspepsia, gastritis, fatigue, headache, abdomen
discomfort, rash, agitation, dizziness and angioedema.
USES:-
Particularly recommended for UTI and sometimes employed
for upper respiratory tract infections.
IUPAC:-
(6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)->2-(methoxyimino)acetyl]amino}-3-
{[(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)thio]methyl}-8-oxo-5-thia-
1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
PROPERTIES AND USES:-
White , crystals, melting point about -155Ā° very soluble in water. It enhibitexcellent
board spectrum antibacterial activity against both gram positive, negative organisms. It
is an antibiotic useful for treatment of an number of bacterial infections such as intra
abdominal infections. It is also use to reduce the risk of post operative infections .
MOA:-
It is an third generation antibiotic from the cephalosporin family. It selectively a an
irreversibly inhibits bacterial cell wall synthesis by binding to transpeptidase, also
called as transamidase which are penicillin binding proteins that catalyse the cross
linking of the peptidoglycan polymers forming the bacterial cell wall . 45
SYNTHESIS
46
DOSAGES:-
ā€¢ Children:50ā€“75mg/kg/DAY in equally divided
doses every 12hrs;max 2g/day.
ā€¢ Adult:1ā€“2g IM or IV once daily or in 2 equally
divided doses; max 4g/day.
ADRā€™S:-
liver enzyme , nausea , vomiting , itchiness,
headache, dizziness .
47
48
HOME REMEDIES FOR UTI :
1. WATER AND JUICES:
- Drink plenty of water
- Have plenty of juices, like CRANBERRY JUICE
CRANBERRY JUICE āž” one of the best remedies to
combat UTI....
2. RAISINS:
- Boil 25 grams of RAISINS in 250 ml of water āž”Boil,
until water reduces to half of its original volume āž”
have this mixture twice a day with sugar
- Considered to be an effective remedy......
49
Continueā€¦
3. BOTTLE GOURD :
- Drink a fresh glass of bottle guard juice,
along with a teaspoon of LIME JUICE.......
4. TENDER COCONUT :
- Have tender coconut
water daily for 15 days...
50
Continueā€¦
5. PARSLEY:
- Possesses natural diuretic properties
- Helps to clean bladder of infectious organisms
- Take half teaspoon of coarsely chopped fresh
parsley āž” boil in 2.5 liters' of water in a covered
pot for 10 mināž” strain it āž” drink this tea over a
period of 3 hours āž” helpful in flushing out
bladder........
51
Continueā€¦
6. CUCUMBER :
- Drink 1 cup of cucumber juice + 1 teaspoon of
HONEY+ 1 teaspoon of FRESH LIME JUICE thrice daily
- This combination acts as a diuretic........
7. RADISH LEAVES :
- Drink 1 cup of RADISH LEAF JUICE in morning for 15
days........
52
Continueā€¦
8. SPINACH :
- Take half cup fresh spinach juice mixed with half
cup of tender coconut water twice a day.......
9 . CARROT :
- Take half glass of carrot juice mixed with an equal
quantity of water (if there is no fever).........
53
Continueā€¦
10. SANDALWOOD OIL:
- Possesses anti-bacterial and diuretic properties.
- Take 5 drops in the beginning
āž”increase to ten drops in a cup of water
with/without 2grams ginger juice...
54
Continueā€¦
11. SANDALWOOD BATH :
- Aromatherapy bath āž”helps ease PELVIC
DISCOMFORT that arises due to bladder infection
- Add 10 drops of SANDALWOOD ESSENTIAL OIL to a
bath of warm water āž” soak for 20 minutes āž” eases
pelvic discomfort...
- Repeat daily until infection subsides...
55
DOā€™s
ā€¢ Fluid Intake(Stay Hydrated).
ā€¢ Apply heat to pelvic area (hot bag/packs).
ā€¢ Use Baking soda.
ā€¢ VITAMIN-C
ā€¢ Proper Hygiene.
ā€¢ Frequently emptying bladder.
ā€¢ Yougurts probiotics.
56
Donā€™ts
ā€¢ smoking .
ā€¢ constipation .
ā€¢ Caffine .
ā€¢ Breavergerā€™s .
ā€¢ Sexual intercourse.
ā€¢ Artificial sweeteners.
57
REFERENCE
BOOKS:-
ā€“ P.PARIMOO- A TEXT BOOK OF MEDICINAL CHEMISTRY
ā€“ RAMARAONADENDLA- 2ND EDITION, MEDICINAL CHEMISTRY
ā€“ Dr. ANEES AHMAD SIDDIQUI -VOL-2- A TEXT BOOK OF MEDICINAL CHEMISTRY
ā€“ S.N PANDEYA ā€“ VOL-2 TEXT BOOK OF MEDICINAL CHEMISTRY
ā€“ S.S.KADAM-VOL-1- PRINCIPLES OF MEDICINAL CHEMISTRY
ā€“ R.S SATOSKAR ā€“ Revised 22nd EDITION -Pharmacology and Pharmacotherapeutics
ā€¢ "Sulfamethoxazole". En.wikipedia.org. N.p., 2016. Web. 20 Nov. 2016
ā€¢ "Cephalexin Uses, Side Effects & Dosage Guide - Drugs.Com". Drugs.com. N.p., 2016. Web. 20
Nov. 2016.
ā€¢ Singh, Jaskeerat. "Antibacterial Drugs". The Medical Post. N.p., 2016. Web. 20 Nov. 2016.
ā€¢ Tetracycline - Biosynthesis". Chm.bris.ac.uk. N.p., 2016. Web. 20 Nov. 2016.
ā€¢ "14 Natural Home Remedies For UTI Pain & Discomfort | Everyday Roots". Everyday Roots. N.p.,
2016. Web. 20 Nov. 2016
ā€¢ "7 Home Remedies For Urinary Tract Infection (UTI) Symptoms". EverydayHealth.com. N.p., 2016.
Web. 24 Nov. 2016.
ā€¢ "LECTURE 10 Classification Of Heterocyclic Compounds On The Basis Of Their Chemical
Structure. Derivatives Of 5-Nitrofuran As Antimicrobial Agents Associate. - Ppt
Download". Slideplayer.com. N.p., 2016. Web. 24 Nov. 2016.
58
ā€¦
59

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Urinary tract infection

  • 2. GENERAL ACKNOWLEDGEMENT TO THE ALMIGHTY AND ALL THE READERSā€¦.. THANKFUL TO U ALL FOR GUIDANCE , SUPPORT AND ENCOURAGEMENT ā€¦ā€¦ 2
  • 3. ANTI- INFECTIVES - Anti-infective are drug that can either kill an infectious agents or inhibit it from spreading. - Anti-infectives include ļƒ¼Antibiotics and Antibacterial. ļƒ¼Antifungal. ļƒ¼Antiviral. ļƒ¼Antiprotozoals & ļƒ¼Anthelmintis. 3
  • 4. S.NO EXAMPLES 1. Anti-fungal ā€¢ Azole antifungal ā€¢ Echinocandins ā€¢ Miscellaneous antifungal ā€¢ Polyenis 2. Antibiotics and Antibacterial. ā€¢Miscellaneous antibiotics ā€¢Orazolidinone antibiotics ā€¢Pencillines. 3. Antiviral. ā€¢Anti viral boosters ā€¢Anti viral combination ā€¢Anti viral infections .4 Antiprotozoals . ā€¢Pentamidine ā€¢Pyrimethamine ā€¢Tinidazole 5. Anthelmintis. ā€¢Mebendazole. ā€¢Ivermectin. ā€¢Albendazole. 4
  • 6. GENERAL INTRODUCTION: ļ‚§ A urinary tract infection (UTI) is an infection in any part of urinary system ā€“ kidney, ureters, bladder and urethra. ļ‚§ It is define as the presence of at least 1 lakh bacteria per ml of urine (normal bacterial count=1000 per ml of urine). ļ‚§ Most infections involve the lower urinary tract the bladder and the urethra. ļ‚§ It is common disorder at all ages in both males and females. 6
  • 7. EPIDEMOLOGY: ļƒ˜UTI is the 2nd most common infections present in community practices. ļƒ˜World wide, about 150 million people are diagnosed with UTI each year . ļƒ˜Prevalence 35% of healthy women suffer symptoms of UTI at some time in their life. 7
  • 8. ETIOLOGY:- ļƒ¼The causative organism causing UTI are:- E.Coli , Pseudomonas aeroginosa, Streptococcus faecalis, Staphylococcus epidermis and Proteus mirabilis. ļƒ¼Waiting for long to urinate. ļƒ¼Sexual transmitted diseases [STD] like gonorrhea causes urethritis . ļƒ¼Presence of tumor/ stones/ foreign bodies in urinary tract. 8
  • 9. Continuedā€¦. Following can cause germs to enter into bladder or kidney And cause UTI:- - Having bubble bath - Wearing tight fitting clothes Risk factors :- ļƒ¼Being pregnant . ļƒ¼Wearing tight fitting clothes. ļƒ¼Diabetic. 9
  • 10. SIGNS AND SYMPTOMS: ā€¢Abrupt onset of micturation. ā€¢Pain in urethra during voiding. ā€¢Supra pubic pain and tenderness. ā€¢Haematuria (blood in urine). ā€¢Dysuria . ā€¢Fever, Feeling tired, apathy, shaky. ā€¢Pressure in lower belly. 10
  • 11. Continuedā€¦. Part of urinary tract affected Signs and Symptoms Kidneys (acute Pyelonephritis) Upper back and side (flank) pain High fever Shaking and chills Nausea Vomiting. Bladder (cystitis) Pelvic pressure Lower abdomen discomfort Frequent painful urination Blood in urine. Urethra (urethritis) Burning with urination Discharge. 11
  • 12. PATHOGENESIS ā€¢ In many cases, bacteria first travel to the urethra. When bacteria multiply, an infection can occur. An infection limited to the urethra is called urethritis. ā€¢ If bacteria move to the bladder and multiply, a bladder infection, called cystitis. ā€¢ If the infection is not treated promptly, bacteria may then travel further up the ureters to multiply and infect the kidneys. A kidney infection is called pyelonephritis. 12
  • 13. CLASSIFICATION OF UTI UTI Acute Infection Chronic Infection 13 Complicated UTI Uncomplicated UTI Primary UTI Recurrent UTI
  • 14. DRUG THERAPY/ TREATMENT S.NO AGENTS EXAMPLES 1 Bacteriostatics agents Sulfonamides Tetracycline Nitrofurantion 2 Bactericidal agents Cotrimoxazole Ampicillin Fluroquinolones Cephalosporins Aminoglycosides 3 Urinary Antiseptic Nitrofurantoin Nalidixic acid Methanamine Mandelate 14
  • 15. 15
  • 16. SULPHANAMIDES ā€¢ The term ā€˜sulfonamideā€™ is employed as generic name for derivatives of para aminobenzene sulfonamide (sulfanilamide) ā€¢ 1st effective chemotherapeuutic agent ,for the prevention and use of bacterial infections in man. ā€¢ DOMAGK(1932) discovered that prontosil protected mice against streptococcal infections. CLASSIFICATION:- 1. Poorly absorbed , locally acting:- sulphasalazine 2. Well absorbed , rapidly excreted:- sulphadiazine 3. Readily absorbed, medium rate of excretion:- sulphafurazole 4. Readily absorbed, slowly excreted:- sulphametopyrazine 16
  • 17. SULPHAMETHOXAZOLE/ TRIMETROPRIM PROPERTIES: o It is a white, odourless , crystalline powder and is bitter in taste .It is employed principally in lower urinary track & systemic infections caused by E.COLI. USES:- ā€¢ Nocardia (DOC), Mycobacteria, Gram ā€“ve infections, Gram +ve infections, Fungus ā€“ Pneumocystis carinii, Protozoa ā€“ Toxoplasma gondii. ā€¢ Sulfonamides are conjugated in the liver and their metabolites are excreted in the kidney which can cause crystalluria. They are high protein bounding drugs. Can cause kernicterus in neonates. ā€¢ It is used in treatment of several infections including AIDS. 17
  • 18. M.O.A They compete with PABA to bind to dihydropteroate synthetase and inhibit conversion of PABA and dihydropteroate diphosphate to dihydrofolic acid, or dihydrofolate. Inhibiting the production of dihydrofolate intermediate interferes with the normal bacterial synthesis of folic acid (folate). Since it inhibits bacterial growth, sulfamethoxazole is considered a bacteriostatic antibiotic. 18
  • 20. Continuedā€¦. DOSAGE:- o oral:-500mg or 1g tablets. o suspension (100mg/1ml). DOSE:- ļƒ¼ oral 2g , followed by 1g every 8 hrs. ADVERSE DRUG REACTIONS:- ļƒ˜ Itching , Rash , Diarrhea, Headache , loss of appetite , hepatitis, stevnes. Johson syndrome , bloody urine, allergic reactions ,decrease blood platelets , hemolytic anemia , depression, drowsiness. 20
  • 21. NITROFURANTION PROPERTIES and USES: - ā€¢ It is a lemon yellow odourless with a bitter taste powder. ā€¢ It is very slightly soluble in water. ā€¢ It is a white anti-bacterial spectrum both gram+ve and gram-ve bacteria. ā€¢ It is also active against many strains of Ecoli and Enterococci. ā€¢ Mainly used in the treatment of uncomplicated UTI. ā€¢ Plasma half life is 0.3 ā€“ 1 hour. 21
  • 22. Continuedā€¦. MOA: - The MOA of nitrofuratonin is unique and complex the drug works by damaging bacteria DNA since it reduced form is highly reactive. This is made possible by rapid reduction of nitrofuratonin inside the bacterial cell by flavoproteins to multiply reactive intermediators that acts on ribosomal proteins. The broads mechanism of action for this drug likely is responsible for the low development of resistance to its effect as a drug effects many different processes important to bacterial cells. 22
  • 23. DOSAGE: - Oral for adults :- 50-100 mg every 6 hours with meals and at bed time . 23 Continuedā€¦.
  • 24. Continuedā€¦. ā€¢ ADVERSE EFFECTS: - Nausea, vomiting, intestinal fibrosis, may occur in chronic therapy, jaundice also occur. ā€¢ Preparations: - Include tablets/ capsules 50&100 mg & a suspension 25mg 15ml . ā€¢ A microcrystallines preparation (macrodantin)which may be less nauseating is available in capsules 25-150mg. 24
  • 25. 25
  • 26. 5 ā€“ETHYL-5,6-DIYDRO-8-ORC- 1,3 DIONOLO(4,5- g)quinoline-7- carboxylic acid 26 PROPERTIES AND USES:- It is fourth generation quinolone antibiotic. Oral availability % = >90 T(1/2)= 6-8 hrs It is used treat a number of bacterial infections including sinusitis , pneumonia , urinary tract infections, pelvic infections. DOSAGES:- 500mg. OD for 7-14 days. MOA:- Inhibiting bacterial DNA gyrase primarily in gram negative bacteria Inhibiting bacterial topoisomerase IV primarily in gram positive bacteria.
  • 27. SYNTHESIS:- ADRā€™S:- nausea, diarrhea, trouble sleeping Major:- tendon rupture or inflammation , seizures , psychosis , peripherial nerve damage. 27
  • 28. PROPERTIES AND USES:- ā€¢ It is one of the most promising newer member of the fluroquinoline family. In this product, the N-ethyl moiety has been made rigid by incorporation into a heterocyclic ring. It is useful in the treatment of genito-urinary, respiratory , gastrointestinal, skin and soft tissue infection and gonorrhea. MOA:- ā€¢ It inhibits the enzyme bacterial DNA gyrase and prevents and replication of bacterial DNA during bacterial growth and reproduction. DOSAGES:- ā€¢ 100, 200mg tablets; 200-450 mg daily usually for 5-7 days. ADRā€™S:- ā€¢ GTI upset, skin reaction, CNS disturbances. ā€¢ -Metabolized by N- demethylation, N- oxidation and O- acyl glucomidation. CONTRA-INDICATED:- ā€¢ It is contraindicated for children below 16yrs, pregnant and lactating women and history of epilepsy. 28
  • 30. PROPERTIES :- ā€¢ It is very effective for the treatment of UTI. ā€¢ (t1/2=3-4hrs). USES:- ā€¢ To Treat endocarditis , gastroenteritis, malignant otitis enterna, respiratory tract infections etc. DOSAGES:- ā€¢ Tab:- 250,500 or 750 mg. ā€¢ UTI:- 250mg twice daily. 30
  • 31. 31
  • 32. MOA:- ā€¢ Itā€™s a broad spectrum antibiotic of the fluoroquinolone class. ā€¢ It is active against both gram positive and negative bacteria. It functions by inhibiting DNA gyraseand type lltopisomerase, topisomerase lV , necessary to separate bacterial DNA thereby inhibiting cell division. 32
  • 33. ADRā€™S:- ā€¢ Diarrhoea ā€¢ bloody 1 black stools ā€¢ change in skin colour ā€¢ chest pain or discomfort ā€¢ confusion, ā€¢ coughing / spitting up blood. ā€¢ Increase heart beat ā€¢ joint pains. 33
  • 34. ļ±Tetracycline is a group of antibiotic that obtained by fermentation from streptomyces spp. Or by chemical transformation of natural products. ļ±They are derivatives of an octahydronaphthacene , a hydrocarbon system that comprises four annulated six member rings. IUPAC ID: (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a- octahydro -3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2- carboxamide 34
  • 35. 35
  • 36. PROPERTIES:- ā€¢ Formula: C22H24N2O8 ā€¢ Molecular weight: 444.44 ā€¢ Melting Point: 170-173Ā°C (with decomposition) ā€¢ Colour /Crystalline: cr (+3w) USES:- ā€¢ First-Line Drug: it is used as first line drug to treat venereal diseases, cholera, relapsing fever. ā€¢ Second-Line Drug: Penicillin for leptospirosis. ā€¢ They are used in urinary tract infections in which causative organism are sensitive. ā€¢ As a prophylactic in chronic obstructive lung diseases. 36
  • 37. 37
  • 39. DOSAGES:- ā€¢ 1g daily in 2-4 divided doses. Storage:- ā€¢ In light , light resistant container. ADRā€™S:- ā€¢ Hypersensitivity like rashes, urticaria, pruritus, glossitis, vulva, and dermatitis. ā€¢ Prolonged usage in diabetes, leucopenia causes super infections. ā€¢ Ataxia, Vertigo are produced when minocycline is discontinued. 39
  • 40. 40 ā€¢ Cephalosporin's are discovered by G.Brotzu of Sardinia made cultures from sea water at a sewage, this might contain organisms antagonistic to intestinal pathogens. ā€¢ Ccephalosporin's have 7-amin cephalosporanic acid nuclues. Which closely resemble to 6-APA nucleus of pencillins. Structurally they contain beta-lactam and dihydrothiazine ring . ā€¢They are water soluble and stable to changes in PH and Temperature.
  • 41. 41 GUIDANCE PRINCIPLES FOR THE USE OF CEPHALOSPORINS : ļ¶ Cephalosporin's are expensive and should not be used where an equally effective , alternative antibiotic is available. ļ¶ None of them is the agent of choice against anaerobic infections . ļ¶ None of them is effective against infectious by enterococci (strep.fecalis)
  • 42. PROPERTIES:- ā€¢ White color. ā€¢ State: crystals. ā€¢ Solubility: very soluble in water, dilute aqueous solution, insoluble in organic solvents. ā€¢ Stability :The alpha -amino group of cephalenin render its acid stable and the 3- methyl group is responsible for metabolic stability. ā€¢ P.Ka : 5.2, 7.3 42
  • 43. 43
  • 44. 44 DOSAGES:- ļ±ORAL- 200-500 mg every 6 hrs. ļ±Children's- 18.8-25 mg/kg every 6hrs. MOA:- It acts by inhibiting bacterial cell wall synthesis, lack of bacterial cell wall results in death due to lysis of bacteria. ADRā€™S:- Diarrhea, dyspepsia, gastritis, fatigue, headache, abdomen discomfort, rash, agitation, dizziness and angioedema. USES:- Particularly recommended for UTI and sometimes employed for upper respiratory tract infections.
  • 45. IUPAC:- (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)->2-(methoxyimino)acetyl]amino}-3- {[(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)thio]methyl}-8-oxo-5-thia- 1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid PROPERTIES AND USES:- White , crystals, melting point about -155Ā° very soluble in water. It enhibitexcellent board spectrum antibacterial activity against both gram positive, negative organisms. It is an antibiotic useful for treatment of an number of bacterial infections such as intra abdominal infections. It is also use to reduce the risk of post operative infections . MOA:- It is an third generation antibiotic from the cephalosporin family. It selectively a an irreversibly inhibits bacterial cell wall synthesis by binding to transpeptidase, also called as transamidase which are penicillin binding proteins that catalyse the cross linking of the peptidoglycan polymers forming the bacterial cell wall . 45
  • 47. DOSAGES:- ā€¢ Children:50ā€“75mg/kg/DAY in equally divided doses every 12hrs;max 2g/day. ā€¢ Adult:1ā€“2g IM or IV once daily or in 2 equally divided doses; max 4g/day. ADRā€™S:- liver enzyme , nausea , vomiting , itchiness, headache, dizziness . 47
  • 48. 48
  • 49. HOME REMEDIES FOR UTI : 1. WATER AND JUICES: - Drink plenty of water - Have plenty of juices, like CRANBERRY JUICE CRANBERRY JUICE āž” one of the best remedies to combat UTI.... 2. RAISINS: - Boil 25 grams of RAISINS in 250 ml of water āž”Boil, until water reduces to half of its original volume āž” have this mixture twice a day with sugar - Considered to be an effective remedy...... 49
  • 50. Continueā€¦ 3. BOTTLE GOURD : - Drink a fresh glass of bottle guard juice, along with a teaspoon of LIME JUICE....... 4. TENDER COCONUT : - Have tender coconut water daily for 15 days... 50
  • 51. Continueā€¦ 5. PARSLEY: - Possesses natural diuretic properties - Helps to clean bladder of infectious organisms - Take half teaspoon of coarsely chopped fresh parsley āž” boil in 2.5 liters' of water in a covered pot for 10 mināž” strain it āž” drink this tea over a period of 3 hours āž” helpful in flushing out bladder........ 51
  • 52. Continueā€¦ 6. CUCUMBER : - Drink 1 cup of cucumber juice + 1 teaspoon of HONEY+ 1 teaspoon of FRESH LIME JUICE thrice daily - This combination acts as a diuretic........ 7. RADISH LEAVES : - Drink 1 cup of RADISH LEAF JUICE in morning for 15 days........ 52
  • 53. Continueā€¦ 8. SPINACH : - Take half cup fresh spinach juice mixed with half cup of tender coconut water twice a day....... 9 . CARROT : - Take half glass of carrot juice mixed with an equal quantity of water (if there is no fever)......... 53
  • 54. Continueā€¦ 10. SANDALWOOD OIL: - Possesses anti-bacterial and diuretic properties. - Take 5 drops in the beginning āž”increase to ten drops in a cup of water with/without 2grams ginger juice... 54
  • 55. Continueā€¦ 11. SANDALWOOD BATH : - Aromatherapy bath āž”helps ease PELVIC DISCOMFORT that arises due to bladder infection - Add 10 drops of SANDALWOOD ESSENTIAL OIL to a bath of warm water āž” soak for 20 minutes āž” eases pelvic discomfort... - Repeat daily until infection subsides... 55
  • 56. DOā€™s ā€¢ Fluid Intake(Stay Hydrated). ā€¢ Apply heat to pelvic area (hot bag/packs). ā€¢ Use Baking soda. ā€¢ VITAMIN-C ā€¢ Proper Hygiene. ā€¢ Frequently emptying bladder. ā€¢ Yougurts probiotics. 56
  • 57. Donā€™ts ā€¢ smoking . ā€¢ constipation . ā€¢ Caffine . ā€¢ Breavergerā€™s . ā€¢ Sexual intercourse. ā€¢ Artificial sweeteners. 57
  • 58. REFERENCE BOOKS:- ā€“ P.PARIMOO- A TEXT BOOK OF MEDICINAL CHEMISTRY ā€“ RAMARAONADENDLA- 2ND EDITION, MEDICINAL CHEMISTRY ā€“ Dr. ANEES AHMAD SIDDIQUI -VOL-2- A TEXT BOOK OF MEDICINAL CHEMISTRY ā€“ S.N PANDEYA ā€“ VOL-2 TEXT BOOK OF MEDICINAL CHEMISTRY ā€“ S.S.KADAM-VOL-1- PRINCIPLES OF MEDICINAL CHEMISTRY ā€“ R.S SATOSKAR ā€“ Revised 22nd EDITION -Pharmacology and Pharmacotherapeutics ā€¢ "Sulfamethoxazole". En.wikipedia.org. N.p., 2016. Web. 20 Nov. 2016 ā€¢ "Cephalexin Uses, Side Effects & Dosage Guide - Drugs.Com". Drugs.com. N.p., 2016. Web. 20 Nov. 2016. ā€¢ Singh, Jaskeerat. "Antibacterial Drugs". The Medical Post. N.p., 2016. Web. 20 Nov. 2016. ā€¢ Tetracycline - Biosynthesis". Chm.bris.ac.uk. N.p., 2016. Web. 20 Nov. 2016. ā€¢ "14 Natural Home Remedies For UTI Pain & Discomfort | Everyday Roots". Everyday Roots. N.p., 2016. Web. 20 Nov. 2016 ā€¢ "7 Home Remedies For Urinary Tract Infection (UTI) Symptoms". EverydayHealth.com. N.p., 2016. Web. 24 Nov. 2016. ā€¢ "LECTURE 10 Classification Of Heterocyclic Compounds On The Basis Of Their Chemical Structure. Derivatives Of 5-Nitrofuran As Antimicrobial Agents Associate. - Ppt Download". Slideplayer.com. N.p., 2016. Web. 24 Nov. 2016. 58