Chemical compounds of drugs and their machanism

against Candida albicans.

Submitted
By: Devendra nikam

T.Y.B.Sc Roll No : 23
A PROJECT REPORT SUBMITTED TO
RAJIV GANDHI INSTITUTE OF I.T & B.T,
BHARATI VIDYAPEETH DEEMED UNIVERSITY,
KATRAJ, PUNE




UNDER THE GUIDANCE OF:
DR. BIPINRAJ N.K.,
ASSISTANT PROFESSOR
MICROBIOLOGY DEPARTMENT,
RAJIV GANDHI INSTITUTE OF I.T & B.T
BHARATI VIDYAPEETH DEEMED UNIVERSITY
PUNE 411043







ACKNOWLEDGEMENT:


We express our sincere gratitude to Dr. G.D Sharma, Principal and Dr. S A Shaikh,
(Vice-Principal M.Sc) , Dr. E.A sing (Vice-Principal B.Sc) of BVDU Rajiv Gandhi
Institute of IT and BT, Pune for giving us permission to carry out our project
successfully.


We sincerely express our deep sense of gratitude and immense respect to our guide
Dr. Bipinraj N. K., for his scholarly guidance, generous encouragement and suggestion
throughout the course of our project work.

We express our sincere thanks to the doctors whom we consulted for giving us their
valuable time and sharing their experience with the patients.

We express our sincere thanks to the chemist we visited for giving us their valuable
time imparting us the necessary information regarding the name of various medicines
and their sales and their nessesary information.

We also express our sincere thanks to the students for co-operating and helping us.
At last we express our special thanks to all our friends for their affectionate co-
operation work without which would have not been possible.

Devendra nikam
T.Y.B.Sc



Sr. No. Content Page
No.
1. Introduction
2. Classification
3. Candida albicans
4. Causes of candidiasis
5. Symptoms of candidiasis
6. Treatment
7.
Table :1 Drugs, chemical
compounds, side effects, and
active mechanism of chemical
compounds.


8. Table :2 chemical compounds and
structure, M.wt, Solubility, Physical
propertyes, Synonyms, General
remarks.

9. Refrances



Introduction
Candidiasis is a fungal infection. Candidiasis also known as candidosis,
moniliasis, and oidiomycosis.(3) This fungal infection caused by any candida
species but mostly by species candida albicans.(1)(2)
Candidiasis may be divided by in to the following types(3). This classification
is done according to site of infection in the body.
Angular cheilitis
Antibiotic candidiasis (iatrogenic candidiasis)
Candidalintertrigo
Candidal paronychia
Candidalvulvovaginitis (vaginal yeast infection)
Candidid
Chronic mucocutaneous candidiasis
Congenital cutaneous candidiasis
Diaper candidiasis
Erosiointerdigitalisblastomycetica
Oral candidiasis (thrush)
Perianal candidiasis
Systemic candidiasis



Generally, candidiasis is often observed in immuno-compromised individuals
such as HIV infected patients(4).
Over growth of several species including candida albicans can causes
superficial infection such as oropharyngeal candidiasis or thrush and
valvovaginal candidiasis also known as vaginal candidiasis.
Many kinds of yeast, viruses, and bacteria present in the human body or
intestinal tract. Most of which are necessary for the manufacture of some
vitamins, the fermentation of undigested food, and the breakdown of mucus.
They stay in their place because of the colon wall and the bodies efficient
immune surveillance system.
Candida albicans
candida albicans is a diploid fungus that grows both as yeast and filamentous
cells and a responsible agent for opportunistic oral and genital infection in
humans(5)(6).
The species candida albicans have ability to change from yeast and become a
fungus.

Causes of candidiasis;
Many factors are responsible for the candidiasis.
These factors include, stress, poor diet a suppressed or compromised immune
system, toxicity and extended use of antibiotics, alcohols, steroids and birth
control pills.
Each of this factors can produce an imbalance of micro-organism in the initial
tract by killing the good bacteria and leaving an overabundance of bad
Candida cells.
Candida cells are proliferates in the gut, penetrates the intestinal wall and is
carried by the circulatory system throught the body. At this point Candida
becomes a systemic.
In systemic infection it infects organ and muscle tissue and compromise the
entire immune system.
Once the immune system is compromised, it may no longer be able to
sufficiently repel invaders; this can result in allergies to chemicals, pollens and
foods.
It also belived that toxins from Candida cells and protein molecules develop an
antigen/antibody reaction which can cause even more allergic reaction.
Immune deficiencies can be either caused by Candida as well as result in
Candida.

The number of factors can increase the chance of yeast growing out of control.
The leading cause is overuse of antibiotics.
Steroids and some treatments like in cancer medication weaken the immune
system and can allow yeast to grow/flourish.
Candida infection can also develop in people with diabetes or who have long-
term irritation resulting from dentures.
Taking birth control pills increases chances of getting vaginal candidiasis. It is
also observed that women are more susceptible to yeast infection then men.
Yeast generally infects intertriginous areas, that is areas where skin contacts
skin.
Overweight people have more folds in their skin. They also sweat more and
Candida albicans is found of moist skin.
Pregnancy causes temporary obesity and may weaken the immune system
increasing the risk of yeast infection.

Hot weather and tight clothing are also risk factor, as they create the ideal
envirment for candida.

Symptoms
Candidiasis is easy to identify.
In candidiasis,
A candida infection of the skin appears as a clearly defined patch red, itchy
skin, often leaking fluid. Scabs and pustules may be seen around the edge of the
rash. It will usually be found in areas such as the groin. The folds of the
buttocks, between the breasts, toes, or fingers, and in the navel.
Genital organs may easily get infected by candida, results itch or burn
especially during urination and sex, generally in case of candida vagineties.
Candidal paranychia is candidiasis of the fingernails, it often observed peoples
whose hands are in water in a lot. Sometimes it present as painful red, swollen
area around the fingernail.
In oral thrush causes curd like white patches inside the mouth, on the tongue
and palate and around the lips, it may also cause cracked, red moist areas of
skin at the corners of the mouth; thrush patches may or may not be painful.


Treatment
The treatments are used to treat candidiasis is based on anatomic location of the
infection.
Various antifungal drugs are available for treating candidiasis, this include,
forcan-150, nuforce-150, azithral, azithromycine, fluca, nystatin, f-conaz,
flucos, etc...
For the infection of the skin, doctors can give an antifungal creams or powder
or prescribed antifungal pills.
For the oral thrush, a suspension of antifungal medication can be swished in the
mouth and swalloed or sometimes the doctor will have dissolved an antifungal
lozenge in the mouth.
Self hygiene is required for avoiding candidial infection.
Infections in HIV positive patients are respond to the treatment are more
slowly. Approximately 60% of patients cured within the six months.

In this article,
We review several drugs available against the candidiasis.
We mainly focus on various types of antifungal drugs for treating candidiasis
and their machanism of action on the fungal cell.(7)
During treatment with these drugs they show some side effects.
In our observation we found that some strains of candida shows resistance
against the antifungal drugs for several generations.(8)
There are many candida species responsible for candidiasis but candida
albicans have high % of infection than any other candida species. (9)
We also done comparative studies between various developed and developing
countries, we observed that % is much higher in developing countries than
developed countries.
Table :1.
No. Name of the
drug/medicine
Active compound Side effects of the Medicine
on to the host
Mechanism of
action

1

Azithromycine

Sub class: Zithromax
&
Azithromycinezmax


Erythromycine

Most common side effects
are: Diarrhea, abdominal
pain, and vomiting, fast
pounding, rash, difficulties
in breathing, swelling of the
face, throats, tongue, lips,
eyes, hands, feets, ankles or
lower legs, hearsenes,

Azithromycine is
prevent bacteria
from growing by
interfering with
their protein
synthesis.
It bind to the 5OS
subunit of the
mouth source ,diarrhea
(wastage of body tools)
after 2 months treat of drug.
unusual bleeding, lack of
energy, loss of
appetitte,pain in upper and
lower stomach, dark colour
of urine, muscle weakness,
etc,,,
bacterial ribosome
and thus inhibit
translocation of
mRNA.
In this mechanism
nucleic acid
synthesis is not
affected

2

Nystatin

Original name:
Fungicidin


Chlorhexidine

Diarrhea, nausea, vomiting
or stomach upset may occur.
Many people use this
medication do not have any
serious side effects.

Symptoms of a serious
allergic reactions may
include: rash, swelling
(especially part of the face,
tongue, throat) trouble in
breathing.


Like amphotericine
B and netamycine,
Nystatin binds to
the ergosterol. a
major component
of the fungal cell
membrane.
When present
insufficient
concentrations, it
forms pores in the
membrane, that
lead to K+ leakage
and death of
fungus, ergosterol
is fairly unique to
fungi so the drug
does not have such
catastrophic effects
on animal or plants.

3

Nuforce-150


Flucronethaolone

Adverse reaction in
digestive system:
Nausea, abdominal pain,
diarrhea, flatulence,
headache, dizziness, allergic

reactions, skin rash,
anaphylactic reactions.
Pregnant women and
children up to age 1 year
increased sensitivity to
fluconazole and triazole
compounds.


Anti-Fungal drug
from the group of
Triazole
compounds, inhibit
the

synthesis of
ergosterol
disrupting the
permeability of the
cell wall caused cell
death.

4

Forcan-150
(Fluconazole)


Flucronethaolone

Upset stomach, loss of
appetite, diarrhea or loose
stool altered tests,
dizziness, fatigue, rashes
itching, vomiting, yellowing

It inhibits the
conversion of
lanosterol to 14
demethyl
lanosterol by
of the skin and eyes dark
urine & pate stools.
inhibiting the
cytochrome P450
enzyme alpha
demethylase and
impair ergosterol
synthesis.

5

Azithral
(Azithromycine)


Azithromycine
(Antibiotic)

Belongs toa group
of antibiotics called
the Macrolides.


Headache, insomnia,
stomach discomfort or
diarrhea, Dizziness, skin
rashes, or irritation, vision
distribution(blurring or
auras)
Nausea or vomiting,
jaundice (yellowing of the
skin and eyes)

The medication
operates by
inhibiting the
bacteria from
reproduction and
preventing the
spared of infection.
Azithromycin
prevents bacteria
from growing by
interfering with
their protein
synthesis. It binds
to the 50S subunit
of the bacterial
ribosome, and thus
inhibits translation
of mRNA

6

Fluka-150

Generic name:
Fluconazole

Fluca-150 is a triazole
antifungal drug.


Fluka
(antifungal
antibiotic)

Nausea, abdominal pain,
loss of appetite, dark urine,
jaundice, shivers, muscle
pain, influenza symptoms,
exfoliation or bleeding,
weakness, seizure(fits)
Fluconazole , a
broad spectrum of
anti-fungal drug
belonging to the
Triazole group of
the anti-fungus that
is potent and
specific inhibitor of
the fungal enzyme
necessary for the
synthesis of
argosterol. An
important
component of
fungal cell
membrane that is
not found in the cell
content to leak-out
which kills the
fungus.
Prevent the
infection from
spreading
symptoms caused
by the infection
,including itching
and inflammation.

7


F-conaz



Narfloxacin 400mg
+ Tinadazole 60mg


Common side effects may
include-
Nausea, drowsiness, skin
rash, diarrhea.
Tinidazole, a 5
nitroimidazole
derivative with
antimicrobial
actions similar to
metronidazole, is
active against both
protozoa
(e.g.Trichomonas
vaginalis,
Entamoeba
histolytica and
Giardia lamblia)
and obligate
anaerobic bacteria.
It damages DNA
strands or inhibit
DNA synthesis in
microorganism

8

Flucos
(Flucos-TZ)


Fluconazole +
Tinadazole

Abdominal pain, nausea,
vomiting, diarrhea, alopecia,
headache, rash, Alteration in
liver enzymes.

It inhibits the
conversion of
lanosterol to 14
demethyl lanosterol
by inhibiting the
cytochrome P450
enzyme alpha
demethylase and
impair ergosterol
synthesis.


9

Zocon


Fluconazole(100mg)

The most common reported
sides effects when taking
Zocon tablets 100mg
including upset of stomach,
stomach cramps, nausea,
and vomiting, diarrhea, skin
rash, headache,
constipation, dizziness,
sensation.

Zocon 100 tablets
contain Fluconazole
100mg, a broad
spectrum of anti-
fungal drug
belonging to the
Triazole group of
the anti-fungus that
is potent and
specific inhibitor of
the fungal enzyme
necessary for the
synthesis of
argosterol. An
important
component of
fungal cell
membrane that is
not found in the cell
content to leak-out
which kills the
fungus.
Prevent the
infection from
spreading
symptoms caused
by the infection
,including itching
and inflammation.


10 Azee. Azithromycin
dehydrate.
mild nausea, vomiting,
diarrhea, constipation,
stomach pain or upset,
dizziness, tired feeling, or
headache, nervous feeling,
sleep problems (insomnia),
vaginal itching or discharge,
mild itching or skin
rash;ringing in ears, problems
with hearing, decreased sense
of taste or smell. Besides the
above side effects serious
allergic reactions, including
angioedema, anaphylaxis, and
dermatologic reactions
including Stevens Johnson
Syndrome and toxic
epidermal necrolysis have
been reported rarely in
patients on azithromycin
therapy
Azithromycin
dehydrate. blocks
transpeptidation by
binding to 50s
ribosomal subunit of
susceptible organisms
and disrupting RNA-
dependent protein
synthesis at the chain
elongation step
11 Azithral 500 Azithromycin
dehydrate.
Nausea, stomach upset, skin
rash, acute toxicity.
Azithromycin
dehydrate blocks
transpeptidation by
binding to 50s
ribosomal subunit of
susceptible organisms
and disrupting RNA-
dependent protein
synthesis at the chain
elongation step
12 Candid. Clotrimazole skin reactions including
blistering of the skin, mouth,
eyes or genitals, skin
discomfort, peeling of the skin
irritation, blister formation
It inhibits the activity
of enzymes within the
cell, and inhibit the
synthesis of
ergosterol this affect
unexpected bruising, seizures,
hair loss
the cell membrane
production, minimal
concentrations of
clotrimazole cause
leakage of
intracellular
phosphorus
compounds cause cell
death.
13 Canesten Clotrimazole allergic reactions to the
capsule or to the cream at the
site of application may occur -
seek immediate medical
advice if you get any of the
following symptoms:
feeling sick or vomiting, taste
changes, stomach discomfort,
diarrhea, wind, headaches,
heart rhythm problems, high
blood cholesterol levels,
blood problems, metabolic
problems, liver problems with
symptoms such as yellowing
of the skin or eyes, dark urine
or pale stools
skin reactions including
blistering of the skin, mouth,
eyes or genitals, skin
discomfort, peeling of the
skin, Irritation, blister
formation, unexpected
bruising, seizures, hair loss,
recurrent infection such as
colds and flu, a rash,
swallowing or breathing
problems, swelling of the lips,
face, throat or tongue,
weakness, feeling dizzy or
faint, nausea, worsening of
pain, burning sensations,
swelling, itching or redness of
the skin

Clotrimazole acts
against fungi by
inhibiting ergosterol
synthesis. Inhibition
of ergosterol
synthesis leads to
structural and
functional impairment
of the cytoplasm
membrane.
14 Cloban G Clotrimazole high blood cholesterol levels,
blood problems, metabolic
problems, liver problems with
symptoms such as yellowing
of the skin or eyes, dark urine
. Clotrimazole acts
against fungi by
inhibiting ergosterol
synthesis. Inhibition
of ergosterol
or pale stools, skin reactions
including blistering of the
skin, mouth, eyes or genitals,
skin discomfort, peeling of the
skin, irritation, blister
formation, unexpected
bruising, seizures hair loss.

synthesis leads to
structural and
functional impairment
of the cytoplasmic
membrane
15 Dk. Gel Miconazole stomach pain or upset,
dizziness, tired feeling, or
headache, nervous feeling,
sleep problems, vaginal
itching or discharge, mild
itching or skin rash, ringing in
your ears, problems with
hearing.

Miconazole works by
inhibiting the
synthesis of
ergosterol, a critical
component of fungal
cell membranes
16 Eumosome Clobetasone
butyrate and
miconazole nitrate
Eumosone cream can cause
thinning of the skin,
particularly on the face and
more easily in children,
changes in skin color or an
increased growth of hair in the
areas where the preparation
has been applied.
Burning, itching, stinging
sensations may occur.
Clobetasone butyrate
is a moderately potent
topical corticosteroid.
When applied to the
skin, clobetasone
butyrate reduces
swelling, itching and
redness by preventing
the release of
chemicals that cause
these symptoms.
(miconazole nitrate,
mechanism is
unknown)
17 Eumosome m Clobetasone
butyrate and
miconazole nitrate
Difficulty in breathing,
swelling face, lips, tongue, or
throat. Sleeping problems
(insomnia), weight gain,
puffiness in face, or muscle
weakness, feeling tired.
Clobetasone butyrate
is a moderately potent
topical corticosteroid.
When applied to the
skin, clobetasone
butyrate reduces
swelling, itching and
redness by preventing
the release of
chemicals that cause
these symptoms.
Clobetasone butyrate
is not a cure for your
condition, but will
help relieve the
symptom
18 Fluconazole. Flucromethaolone Headache, dizziness, diarrhea,
stomach pain, heartburn,
Fluorometholone
suppresses the
change in ability to taste food,
nausea, vomiting, extreme
tiredness, unusual bruising or
bleeding lack of energy loss
of appetite, pain in the upper
right part of the stomach,
yellowing of the skin or eyes,
flu-like symptoms, dark urine,
pale stools, seizures, rash,
blistering or peeling skin,
hives, itching, swelling of the
face, throat, tongue, lips, eyes,
hands, feet, ankles, or lower
legs, difficulty breathing or
swallowing

migration of
polymorphonuclear
leukocytes ( A type
of immune cell that
has granules (small
particles) with
enzymes that are
released during
infections, allergic
reactions, and asthma.
Neutrophils,
eosinophils, and
basophils are
polymorphonuclear
leukocytes. A
polymorphonuclear
leukocyte is a type of
white blood cell. Also
called granular
leukocyte,
granulocyte, and
PMN.)and reversal of
increased capillary
permeability thus
decreasing
inflammation.
19 Fucis-150 Flucromethaolone Headache, dizziness,
diarrhea, stomach pain,
heartburn, change in
ability to taste food,
nausea, vomiting, extreme
tiredness, unusual bruising
or bleeding lack of energy
loss of appetite, pain in
the upper right part of the
stomach, yellowing of the
skin or eyes, flu-like
symptoms, dark urine,
pale stools, seizures, rash,
blistering or peeling skin,
hives, itching, swelling of
the face, throat, tongue,
lips, eyes, hands, feet,
ankles, or lower legs,
difficulty breathing or
swallowing

Fluorometholone
suppresses the
migration of
polymorphonuclear
leukocytes and
reversal of increased
capillary permeability
thus decreasing
inflammation
20 Cloben-G Chlotrimazole Nausea, stomach upset, skin
rash, acute toxicity.
This medication is a
synthetic steroid,
prescribed for skin
disorders. This
medication prevents
the release of
substances that causes
inflammation.
21 Candidum Chlotrimazole Nausea, stomach upset, skin
rash, acute toxicity.
This medication is a
synthetic steroid,
prescribed for skin
disorders. This
medication prevents
the release of
substances that causes
inflammation.
22 Secnidazole. Secnidazole Anorexia, Glossitis , Nausea,
Vomiting, Diarrhea, Fatigue,
Dry mouth,
Abdominal distress,
Headache, Dizziness, Rash,
Urticaria, Leucopenia,



Secnidazole is a nitro
imidazole which has
broad spectrum cidal
activity against
Protozoa and some
anaerobic bacteria. Its
selective toxicity to
anaerobic microbes
involves 1. Drug
enters the cell by
diffusion, 2. Nitro
group of drug is
reduced by redox
proteins present only
in anaerobic
organisms to reactive
nitro radical which
exerts cytotoxic
action by damaging
DNA and other
critical Biomolecules.
3. DNA helix
destabilization &
strand breakage has
been observed.
23 Terbicip-250 Terbinafine All medicines may cause side
effects, but many people have
no, or minor, side effects.
tough; dizziness, headache,
indigestion, nausea, stomach
upset or pain, stuffy nose
tiredness, trouble sleeping,
weakness.
Severe allergic reactions
(rash, hives, itching,
difficulty breathing, tightness
in the chest, swelling of the
mouth, face, lips, or tongue),
Terbinafine acts by
interfering with the
ability of fungi to
make chemicals
called sterols that are
an important part of
the membrane that
surrounds fungal cells
and holds them
together. This
weakens the cell
membrane.
aggressive behavior,
agitation, dark urine; fever,
flu-like symptoms,
hallucinations, irregular
heartbeat, mental or mood
changes, new or worsening
wheezing or other breathing
problems, numbness or
tingling of hands or feet,
seizures, severe or persistent
stomach pain, severe sinus
inflammation, suicidal
thoughts or actions, swelling,
unusual bruising or bleeding,
upper respiratory tract
infection, yellowing of the
skin or eyes.
24 Terbinafine Terbinafine
hydrochloride
burning or irritation Itching
Skin exfoliation Erythematous
rash
Terbinafine
hydrochloride is a
synthetic allylamine
derivative.
Terbinafine
hydrochloride is
hypothesized to act
by inhibiting the
epoxidation of
squalene, thus
blocking the
biosynthesis of
ergosterol, an
essential component
of fungal cell
membranes. The
allylamine
derivatives, like the
benzylamines, act at
an earlier step in the
ergosterol
biosynthesis pathway
than the azole class of
antifungal drugs.
Depending on the
concentration of the
drug and the fungal
species tested in vitro,
terbinafine
hydrochloride may be
fungicidal


Azithromycine: (Erythromycine) :
Azithromycine is prevent bacteria from growing by interfering with their protein
synthesis. It bind to the 5OS subunit of the bacterial ribosome and thus inhibit
translocation of mRNA. In this mechanism nucleic acid synthesis is not affected.
Most common side effects are: Diarrhea, abdominal pain, and vomiting, fast pounding,
rash, difficulties in breathing, swelling of the face, throats, tongue, lips, eyes, hands, feets,
ankles or lower legs, hearsenes, mouth source ,diarrhea (wastage of body tools) after 2
months treat of drug. unusual bleeding, lack of energy, loss of appetitte,pain in upper and
lower stomach, dark colour of urine, muscle weakness, etc.

Nystatin: (Chlorhexidine) :
Like amphotericine B and netamycine, Nystatin binds to the ergosterol. a major component
of the fungal cell membrane. When present insufficient concentrations, it forms pores in
the membrane, that lead to K+ leakage and death of fungus, ergosterol is fairly unique to
fungi so the drug does not have such catastrophic effects on animal or plants.
Most common side effects are: Diarrhea, nausea, vomiting or stomach upset may occur.
Many people use this medication do not have any serious side effects. Symptoms of a
serious allergic reactions may include: rash, swelling (especially part of the face, tongue,
throat) trouble in breathing.



Nuforce-150: (Flucronethaolone) :
Anti-Fungal drug from the group of Triazole compounds, inhibit the synthesis of ergosterol
disrupting the permeability of the cell wall caused cell death.
Most common side effects are: Adverse reaction in digestive system: Nausea, abdominal
pain, diarrhea, flatulence, headache, dizziness, allergic reactions, skin rash, anaphylactic
reactions. Pregnant women and children up to age 1 year increased sensitivity to
fluconazole and triazole compounds.

Forcan-150: (Flucronethaolone) :
It inhibits the conversion of lanosterol to 14 demethyl lanosterol by inhibiting the
cytochrome P450 enzyme alpha demethylase and impair ergosterol synthesis.
Most common side effects are: Upset stomach, loss of appetite, diarrhea or loose stool
altered tests, dizziness, fatigue, rashes itching, vomiting, yellowing of the skin and eyes
dark urine & pate stools.

Azithral: (Azithromycine) :
The medication operates by inhibiting the bacteria from reproduction and preventing the
spared of infection. Azithromycin prevents bacteria from growing by interfering with their
protein synthesis. It binds to the 50S subunit of the bacterial ribosome, and thus inhibits
translation of mRNA.
Most common side effects are: Headache, insomnia, stomach discomfort or diarrhea,
Dizziness, skin rashes, or irritation, vision distribution(blurring or auras) Nausea or
vomiting, jaundice (yellowing of the skin and eyes).


Fluka-150: (Fluka) : Fluconazole , a broad spectrum of anti-fungal drug belonging to the
Triazole group of the anti-fungus that is potent and specific inhibitor of the fungal enzyme
necessary for the synthesis of argosterol. An important component of fungal cell
membrane that is not found in the cell content to leak-out which kills the fungus.
Most common side effects are: Prevent the infection from spreading symptoms caused by
the infection ,including itching and inflammation. Nausea, abdominal pain, loss of appetite,
dark urine, jaundice, shivers, muscle pain, influenza symptoms, exfoliation or bleeding,
weakness, seizure(fits).

F-conaz: (Narfloxacin 400mg + Tinadazole 60mg) :
Tinidazole, a 5 nitroimidazole derivative with antimicrobial actions similar to
metronidazole, is active against both protozoa (e.g.Trichomonas vaginalis, Entamoeba
histolytica and Giardia lamblia) and obligate anaerobic bacteria. It damages DNA strands
or inhibit DNA synthesis in microorganism.

Common side effects may include- Nausea, drowsiness, skin rash, diarrhea.



Flucos: (Fluconazole + Tinadazole) :
It inhibits the conversion of lanosterol to 14 demethyl lanosterol by inhibiting the
cytochrome P450 enzyme alpha demethylase and impair ergosterol synthesis.
Most common side effects are: Abdominal pain, nausea, vomiting, diarrhea, alopecia,
headache, rash, Alteration in liver enzymes.


Zocon: (Fluconazole) : Zocon 100 tablets contain Fluconazole 100mg, a broad spectrum of
anti-fungal drug belonging to the Triazole group of the anti-fungus that is potent and
specific inhibitor of the fungal enzyme necessary for the synthesis of argosterol. An
important component of fungal cell membrane that is not found in the cell content to leak-
out which kills the fungus.
Most common side effects are: Prevent the infection from spreading symptoms caused by
the infection ,including itching and inflammation. The most common reported sides effects
when taking Zocon tablets 100mg including upset of stomach, stomach cramps, nausea,
and vomiting, diarrhea, skin rash, headache, constipation, dizziness, sensation.




Azee: (Azithromycin dehydrate.) : Azithromycin dehydrate. blocks transpeptidation by
binding to 50s ribosomal subunit of susceptible organisms and disrupting RNA-dependent
protein synthesis at the chain elongation step.
Most common side effects are: mild nausea, vomiting, diarrhea, constipation, stomach
pain or upset, dizziness, tired feeling, or headache, nervous feeling, sleep problems
(insomnia), vaginal itching or discharge, mild itching or skin rash;ringing in ears, problems
with hearing, decreased sense of taste or smell. Besides the above side effects serious
allergic reactions, including angioedema, anaphylaxis, and dermatologic reactions
including Stevens Johnson Syndrome and toxic epidermal necrolysis have been reported
rarely in patients on azithromycin therapy

Azithral 500: (Azithromycin dehydrate.) :
Azithromycin dehydrate blocks transpeptidation by binding to 50s ribosomal subunit of
susceptible organisms and disrupting RNA-dependent protein synthesis at the chain
elongation step.
Most common side effects are: Nausea, stomach upset, skin rash, acute toxicity.


Candid: (Clotrimazole):
It inhibits the activity of enzymes within the cell, and inhibit the synthesis of ergosterol
this affect the cell membrane production, minimal concentrations of clotrimazole cause
leakage of intracellular phosphorus compounds cause cell death.
Most common side effects are: skin reactions including blistering of the skin, mouth, eyes
or genitals, skin discomfort, peeling of the skin irritation, blister formation unexpected
bruising, seizures, hair loss

Canesten: (Clotrimazole) : Clotrimazole acts against fungi by inhibiting ergosterol
synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment
of the cytoplasm membrane.
Most common side effects are: allergic reactions to the capsule or to the cream at the site
of application may occur - seek immediate medical advice if you get any of the following
symptoms: feeling sick or vomiting, taste changes, stomach discomfort, diarrhea, wind,
headaches, heart rhythm problems, high blood cholesterol levels, blood problems,
metabolic problems, liver problems with symptoms such as yellowing of the skin or eyes,
dark urine or pale stools.skin reactions including blistering of the skin, mouth, eyes or
genitals, skin discomfort, peeling of the skin, Irritation, blister formation, unexpected
bruising, seizures, hair loss, recurrent infection such as colds and flu, a rash, swallowing or
breathing problems, swelling of the lips, face, throat or tongue, weakness, feeling dizzy or
faint, nausea, worsening of pain, burning sensations, swelling, itching or redness of the
skin.


Cloban G: (Clotrimazole) : Clotrimazole acts against fungi by inhibiting ergosterol
synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment
of the cytoplasmic membrane
Most common side effects are: high blood cholesterol levels, blood problems, metabolic
problems, liver problems with symptoms such as yellowing of the skin or eyes, dark urine
or pale stools, skin reactions including blistering of the skin, mouth, eyes or genitals, skin
discomfort, peeling of the skin, irritation, blister formation, unexpected bruising, seizures
hair loss.


Dk. Gel: (Miconazole) :
Miconazole works by inhibiting the synthesis of ergosterol, a critical component of fungal
cell membranes
Most common side effects are: stomach pain or upset, dizziness, tired feeling, or
headache, nervous feeling, sleep problems, vaginal itching or discharge, mild itching or
skin rash, ringing in your ears, problems with hearing.


Eumosome: (Clobetasone butyrate and miconazole nitrate) :
Clobetasone butyrate is a moderately potent topical corticosteroid. When applied to the
skin, clobetasone butyrate reduces swelling, itching and redness by preventing the release
of chemicals that cause these symptoms. (miconazole nitrate, mechanism is unknown)
Most common side effects are: Eumosone cream can cause thinning of the skin,
particularly on the face and more easily in children, changes in skin color or an increased
growth of hair in the areas where the preparation has been applied.
Burning, itching, stinging sensations may occur.



Eumosome m: (Clobetasone butyrate and miconazole nitrate):
Most common side effects are: Difficulty in breathing, swelling face, lips, tongue, or
throat. Sleeping problems (insomnia), weight gain, puffiness in face, or muscle weakness,
feeling tired.
Clobetasone butyrate is a moderately potent topical corticosteroid. When applied to the
skin, clobetasone butyrate reduces swelling, itching and redness by preventing the release
of chemicals that cause these symptoms. Clobetasone butyrate is not a cure for your
condition, but will help relieve the symptom.

Fluconazole: (Flucromethaolone) :
Fluorometholone suppresses the migration of polymorphonuclear leukocytes ( A type of
immune cell that has granules (small particles) with enzymes that are released during
infections, allergic reactions, and asthma. Neutrophils, eosinophils, and basophils are
polymorphonuclear leukocytes. A polymorphonuclear leukocyte is a type of white blood
cell. Also called granular leukocyte, granulocyte, and PMN.)and reversal of increased
capillary permeability thus decreasing inflammation.
Most common side effects are: Headache, dizziness, diarrhea, stomach pain, heartburn,
change in ability to taste food, nausea, vomiting, extreme tiredness, unusual bruising or
bleeding lack of energy loss of appetite, pain in the upper right part of the stomach,
yellowing of the skin or eyes, flu-like symptoms, dark urine, pale stools, seizures, rash,
blistering or peeling skin, hives, itching, swelling of the face, throat, tongue, lips, eyes,
hands, feet, ankles, or lower legs, difficulty breathing or swallowing.

Fucis-150: (Flucromethaolone) :
Fluorometholone suppresses the migration of polymorphonuclear leukocytes and reversal
of increased capillary permeability thus decreasing inflammation.
Most common side effects are: Headache, dizziness, diarrhea, stomach pain, heartburn,
change in ability to taste food, nausea, vomiting, extreme tiredness, unusual bruising or
bleeding lack of energy loss of appetite, pain in the upper right part of the stomach,
yellowing of the skin or eyes, flu-like symptoms, dark urine, pale stools, seizures, rash,
blistering or peeling skin, hives, itching, swelling of the face, throat, tongue, lips, eyes,
hands, feet, ankles, or lower legs, difficulty breathing or swallowing



Cloben-G: (Chlotrimazole):
This medication is a synthetic steroid, prescribed for skin disorders. This medication
prevents the release of substances that causes inflammation.
Most common side effects are: Nausea, stomach upset, skin rash, acute toxicity.



Candidum: (Chlotrimazole) :
This medication is a synthetic steroid, prescribed for skin disorders. This medication
prevents the release of substances that causes inflammation.
Most common side effects are: Nausea, stomach upset, skin rash, acute toxicity.



Secnidazole: (Secnidazole) :
Secnidazole is a nitro imidazole which has broad spectrum cidal activity against Protozoa
and some anaerobic bacteria. Its selective toxicity to anaerobic microbes involves 1. Drug
enters the cell by diffusion, 2. Nitro group of drug is reduced by redox proteins present
only in anaerobic organisms to reactive nitro radical which exerts cytotoxic action by
damaging DNA and other critical Biomolecules. 3. DNA helix destabilization & strand
breakage has been observed.
Most common side effects are: Anorexia, Glossitis , Nausea, Vomiting, Diarrhea, Fatigue,
Dry mouth,
Abdominal distress, Headache, Dizziness, Rash, Urticaria, Leucopenia,


Terbicip-250: (Terbinafine) : Terbinafine acts by interfering with the ability of fungi to
make chemicals called sterols that are an important part of the membrane that surrounds
fungal cells and holds them together. This weakens the cell membrane.
Most common side effects are : All medicines may cause side effects, but many people
have no, or minor, side effects. tough; dizziness, headache, indigestion, nausea, stomach
upset or pain, stuffy nose tiredness, trouble sleeping, weakness. Severe allergic reactions
(rash, hives, itching, difficulty breathing, tightness in the chest, swelling of the mouth,
face, lips, or tongue), aggressive behavior, agitation, dark urine; fever, flu-like symptoms,
hallucinations, irregular heartbeat, mental or mood changes, new or worsening wheezing
or other breathing problems, numbness or tingling of hands or feet, seizures, severe or
persistent stomach pain, severe sinus inflammation, suicidal thoughts or actions, swelling,
unusual bruising or bleeding, upper respiratory tract infection, yellowing of the skin or
eyes.


Terbinafine: (Terbinafine hydrochloride) :
Terbinafine hydrochloride is a synthetic allylamine derivative. Terbinafine hydrochloride
is hypothesized to act by inhibiting the epoxidation of squalene, thus blocking the
biosynthesis of ergosterol, an essential component of fungal cell membranes. The
allylamine derivatives, like the benzylamines, act at an earlier step in the ergosterol
biosynthesis pathway than the azole class of antifungal drugs. Depending on the
concentration of the drug and the fungal species tested in vitro, terbinafine hydrochloride
may be fungicidal
Most common side effects are : burning or irritation Itching Skin exfoliation
Erythematous rash.


no Name
Synonyms
Formula M.wt
Physical
properties
Solubility General remarks
1. Erythromycine Ery

734.0 (Ery A) Lamda max (pH 6.3)
280nm 50; pk 8.8
v.s. MeOH, EtOH;
s.eth; slowly s. H2O
(2 mg/ml)
Inhibitor of bacterial
protein sysnthesis.
B.subtilis growth
50% inhibit at
0.04g/ml. One of the
macrolide group
which includes
spiramycin and
carbomycine. Soln.,
basic reaction
2. Chlorhexidine Chlorhexidin [Czech],
Chlorhexidinum [INN-
Latin],
Cloresidina [DCIT],
Clorhexidina.


Average:
505.447;

Monoisotopic:
504.203196424
melting point: 134
C..
water solubility: 800
mg/L (at 20 C).
logP :0.08,
pKa :10.8 (at 25 C).


water solubility:
800 mg/L
Chlorhexidine's
antimicrobial effects
are associated with
the attractions
between
chlorhexidine (cation)
and negatively
charged bacterial
cells. After
chlorhexidine is
absorpted onto the
organism's cell wall,
it disrupts the
integrity of the cell
membrane and causes
the leakage of
intracellular
components of the
organisms
3. Flucronethaolone 9-Fluoro-11,17-
dihydroxy-6-methyl-
pregna-1,4-diene-3,
20-dione;(trc Canada.com)

376.46 Melting range:
557.6- 577.4,
Boiling Range
(F) Not available,

Decomposition
Temp (F) Not
available.
(scbt,com)
Solubility: Water,
30 mg/L (25 deg C

4. Azithromycine Azithramycine,
Azithromycin Dihydrate,
Azithromycine ,
Azithromycinum,
Azitromicina.


749 Appearance:
White crystalline
powder.
Solubility in water:
Insoluble.

Melting Point:113.

Vapor pressure: 2E-
30 (25 C),

pKa/pKb: 5.41
(pKa),


Solubility :
practically insoluble
in water, freely
soluble in
ethanol and in
methylene chloride.

Azithromycin binds
to the 50S subunit of
the 70S bacterial
ribosomes, and
therefore inhibits
RNA-dependent
protein synthesis in
bacterial cells
5. Narfloxacin Not Available

Average:
319.3308;

Monoisotopic:
319.133219662
Nelting point:
227 d s
Solubility - In water
at 20
o
C (mg l
-1
)
The bactericidal
action of Norfloxacin
results from
inhibition of the
enzymes
topoisomerase II
(DNA gyrase) and
topoisomerase IV,
which are required
for bacterial DNA
replication,
transcription, repair,
and recombination.
Norfloxacin is a
broad-spectrum
antibiotic that is
active against both
gram-positive and
gram-negative
bacterias. The
fluorine atom at the 6
position increases
potency against gram-
negative organisms,
and the piperazine
moiety at the 7
position is
responsible for anti-
pseudomonal activity
6. Tinadazole Not Available

Average:
247.272;

Monoisotopic:
247.062676609
Melting point:
227-228 ds,
Refractivity:
57.66
polarizability:
23.27



insoluble in water ,
soluble in acetone
and in methylene
chloride, sparingly
soluble in methanol.

Tinidazole is a
prodrug and
antiprotozoal agent.
The nitro group of
tinidazole is reduced
in Trichomonas by a
ferredoxin-mediated
electron transport
system. The free nitro
radical generated as a
result of this
reduction is believed
to be responsible for
the antiprotozoal
activity. It is
suggested that the
toxic free radicals
covalently bind to
DNA, causing DNA
damage and leading
to cell death. The
mechanism by which
tinidazole exhibits
activity against
Giardia and
Entamoeba species is
not known, though it
is probably similar.
7. Fluconazole Elazor, Flusol,
Zoltec, uk49858, diflucan,
Difluean, Fluconal,
FluMycon, Flunazol,
triflucan.

Average:
306.2708;

Monoisotopic:
306.104065446
mp : 138-140C
storage temp. :-20C
solubility :
DMSO: 5 mg/mL
form : solid

solubility : DMSO:
5 mg/mL
Fluconazole interacts
with 14-
demethylase, a
cytochrome P-450
enzyme necessary to
convert lanosterol to
ergosterol. As
ergosterol is an
essential component
of the fungal cell
membrane, inhibition
of its synthesis results
in increased cellular
permeability causing
leakage of cellular
contents. Fluconazole
may also inhibit
endogenous
respiration, interact
with membrane
phospholipids, inhibit
the transformation of
yeasts to mycelial
forms, inhibit purine
uptake, and impair
triglyceride and/or
phospholipid
biosynthesis.
8. Azithromycin dehydrate. CP-62993, XZ-450;
Azitrocin, Ribotrex,
Sumamed, Trozocina,
Zithromaz, Zitromax.

785.02 Mol. Formula:
C38H76N2O14
Appearance:
White Solid
Melting Point:
122-1240C
Chloroform,
Ethanol
Semi-synthetic
macrolide antibiotic;
related to
Erythromycin A.
Antibacteri
References: Langtry,
H.D., et al.: Drugs,
56, 273 (1998),
al////
9. Miconazole
MCZ


Average:
416.129;

Monoisotopic:
413.986023908
melting point
: 159-163 C,
water solubility:
1g/100mL (20 C),
logP:
6.1

Slightly soluble in
water, soluble 1 in
9.5 of ethanol, 1 in
2 of chloroform, 1
in 15 of ether, 1 in 4
of isopropanol, 1 in
5.3 of methanol and
1 in 9 of propylene
glycol. Freely
soluble in acetone
and in
dimethylformamide,
protect from light
[13].

Miconazole interacts
with 14-
demethylase, a
cytochrome P-450
enzyme necessary to
convert lanosterol to
ergosterol. As
ergosterol is an
essential component
of the fungal cell
membrane, inhibition
of its synthesis results
in increased cellular
permeability causing
leakage of cellular
contents. Miconazole
may also inhibit
endogenous
respiration, interact
with membrane
phospholipids, inhibit
the transformation of
yeasts to mycelial
forms, inhibit purine
uptake, and impair
triglyceride and/or
phospholipid
biosynthesis
10. Clobetasone butyrate (16-beta)-);

11,20-trione,21-chloro-9-
fluoro-17-hydroxy-16-
beta-methyl-pregna-4-
diene-3;

21-chloro-9-fluoro-17-
hydroxy-16-beta-
methylpregna-1,4-
diene,3,11,20-trione;

eumovate;molivate;pregna-
1,4-diene-3,11,20-
trione,21-chloro-9-fluoro-
16-methyl-17-(1-
oxobutoxy;

sn203;


21-chloro-9-fluoro-17-
hydroxy-16beta-
methylpregna-1,4-diene-
3,11,20-trione 17-butyrate

478.99 Melting Range (F)
194- 212 Viscosity
Not Applicable
Boiling Range (F)
Not available
water
Clobetasone
butyrate is a
moderately
potent topical
corticosteroid.
When applied to
the skin,
clobetasone
butyrate reduces
swelling, itching
and redness by
preventing the
release of
chemicals that
cause these
symptoms.
11. miconazole nitrate Ecobi, Vodol, Daktar,
Florid, Aflorix, Brentan,
Hi-Pick, Micatin, Miconal,
Micotef.

479.14 Melting Range (F)
338.5- 365 (dec)
Viscosity Not
available
Boiling Range (F)
Not available.
Solubility in water
(g/L) Immiscible
Flash Point (F) Not
applicable


APPEARANCE
White to light beige
crystals or powder,
Water,ethanol,
alcohol,
isopropanol,
chloroform
Active
Pharmaceutical
Ingredients;Organics;
Antifungals for
Research
And Experimental
Use;Biochemistry;AP
I's;
Antifungal;Aromatics
;
Heterocycles;
Intermediates
And fine chemicals;
Pharmaceuticals

almost insoluble in
water. Slightly
soluble in alcohols,
chloroform and
acetone. Solubility
in water 160
mg/litre.
Antifungal agent.
Inhibits
lanosterol
demethylase
and
induces formation of
reactive oxygen
species.
12. Secnidazole alpha,2-Dimethyl-5-nitro-
1H-imidazole-1-ethanol,

185.18
MP:98 ds.
Dencity:1.39 g/cm
3,

Melting
Point:
76 C
Boiling
Point:
396.1 C at
760 mmHg
Flash
Point:
193.4 C
Appearance:
Crystalline solid
Available
Forms:
Powder



Water,ethanol,
alcohol, chloroform
which has
broad
spectrum cidal
activity
against Protozoa
and some
anaerobic
bacteria.
Its
selective
toxicity to
anaerobic
microbes
involves
1. Drug enters
the cell by
diffusion,
2.Nitro group
of drug is
reduced by redox
proteins
present only in
anaerobic
organisms to
reactive
nitro
radical which
exerts
cytotoxic
action by
damaging
DNA and other
critical
Biomolecules.
3. DNA helix
destabilization
& strand breakage
has been
observed.
13. Terbinafine
Terbinafine
HCl,
Terbinafine
Hydrochloride,
Ternbinafine
HCl.

Average:
291.4299;

Monoisotopic:
291.198699805
Terbinafine
hydrochloride is a
white fine crystalline
powder that is freely
soluble in methanol
and
dichloromethane,
soluble in ethanol,
and slightly soluble
in water
Terbinafine
hydrochloride
is a white fine
crystalline
powder
that is
freely
soluble in
methanol
and dichlor
omethane,
soluble in
ethanol,
and slightly
soluble
in waterble.
Terbinafine is
hypothesized to act
by inhibiting squalene
monooxygenase, thus
blocking the
biosynthesis of
ergosterol, an
essential component
of fungal cell
membranes. This
inhibition also results
in an accumulation of
squalene, which is a
substrate catalyzed to
2,3-oxydo squalene
by squalene
monooxygenase. The
resultant high
concentration of
squalene and
decreased amount of
ergosterol are both
thought to contribute
to terbinafine's
antifungal activity.



(Like other
allylamines,
terbinafine inhibits
ergosterol synthesis
by inhibiting squalene
epoxidase, an enzyme
that is part of the
fungal cell membrane
synthesis pathway.
Because terbinafine
prevents conversion
of squalene to
lanosterol, ergosterol
cannot be
synthesized. This is
thought to change cell
membrane
permeability, causing
fungal cell
14. Terbinafine hydrochloride LAMISIL;

(e)-n-(6,6-dimethyl-2-
hepten-4-ynyl)-n-methyl-
1-
naphthalenemethanamine;

6-dimethyl-2-hepten-4-
ynyl)-n-methyl-n-((e)-1-
naphthalenemethanamin;

sf-86-327;

TERBINAFINE;

trans-N-(6,6-Dimethyl-2-
hepten-4-ynyl)-N-methyl-
1-naphthylmethylamine;

1-
Naphthalenemethanamine,

291.44
Physical state
and appearance:
Solid.
Odor:
Not available.
Taste:
Not available.
Molecular Weight:
327.89 g/mole
Color:
Not available.
pH (1%
soln/water):
Not available.
Boiling Point:
Not available.
Melting Point:
Not available.
Terbinafine
hydrochloride
is a white fine
crystalline
powder
that is
freely
soluble in
methanol
and dichlor
omethane,
soluble in
ethanol,
and slightly
soluble
in waterble.
Terbinafine
hydrochloride
is a synthetic
allylamine
derivative.
Terbinafine
hydrochloride is
hypothesized to
act by inhibiting
the epoxidation
of
squalene,
thus blocking
the
biosynthesis of
ergosterol,
N-(2E)-6,6-dimethyl-2-
hepten-4-ynyl-N-methyl-;

N,6,6-Trimethyl-N-
(naphthalen-1-
ylmethyl)hept-2-en-4-yn-
1-amine hydrochloride
Critical
Temperature:
Not available.
Specific Gravity:
Not available.
Vapor Pressure:
Not applicable.
Vapor Density:
Not available.
Volatility:
Not availa
an essential
component of
fungal
cell
membranes.
The allylamine
derivatives,
like the
benzylamines,
act at an earlier
step in the
ergosterol
biosynthesis
pathway
than the azole
class of
antifungal
drugs.
Depending on
the
concentration of
the
drug and the
fungal
species tested
in
vitro,
terbinafine
hydrochloride
may
be fungicidal
15. clotrimazole
Chlotrimazole
And Clotrimazol


Average:
344.837;

Monoisotopic:
344.108026261
melting point:
148 C
Water
solubility:
29.84 mg/mL
logP: 6.1
This product is
soluble
in chloroform
(50 mg/ml),
yielding a clear,
colorless solution.
It has been
reported to be
soluble
in alcohol,
ethyl acetate,
acetone, and
dimethylformamide
.1,2
The solubility
of this product in
DMSO has been
reported to be
25 mM.9
Clotrimazole interacts
with yeast 14-
demethylase, a
cytochrome P-450
enzyme that converts
lanosterol to
ergosterol, an
essential component
of the membrane. In
this way, clotrimazole
inhibits ergosterol
synthesis, resulting in
increased cellular
permeability.
Clotrimazole may
also inhibit
endogenous
respiration, interact
with membrane
phospholipids, inhibit
the transformation of
yeasts to mycelial
forms and the uptake
of purine, impair
triglyceride and/or
phospholipid
biosynthesis, and
inhibit the movement
of calcium and
potassium ions across
the cell membrane by
blocking the ion
transport pathway
known as the Gardos
channel.