Fungal

infections mycoses
are called
• Polyene Sytemic
antifungal
• acts by binding to
ergosterol in fungal
Amphotericin
cell membranes, causing
them to become
B
permeable

molecules with both

hydrophilic and lipophilic
characteristics
(ie, they are
Polyenes
amphipathic)

a sterol specific to
fungal cell membranes,
and cause the
formation of artificial
ergosterol
pores
It has the widest antifungal spectrum of
any agent and remains the drug of
choice,
or codrug of choice, for most systemic
Amphotericin
infections caused by Aspergillus,
Blastomyces, Candida albicans,
Cryptococcus, Histoplasma, and Mucor
B

usually given by slow

intravenous
infusion, but in fungal
meningitis
Amphotericin
intrathecal administration,
though
B
dangerous, has been used

Adverse effects related to

intravenous
infusion commonly include
fever, chills,
Amphotericin
muscle spasms, vomiting, and
a B
shock-like fall in blood pressure

It decreases the
glomerular filtration rate
and causes renal Amphotericin
tubular acidosis with
magnesium and B
potassium wasting
 • pyrimidine
antimetabolite Flucytosine
related to the (5-Fluorocytosine
anticancer drug [5-FC])
5-fluorouracil (5-FU)

• The drug is eliminated

intact in the urine, Flucytosine
and the dose must be (5-Fluorocytosine
reduced in patients [5-FC])
with renal impairment

• When 5-FC is given with

amphotericin B,
or triazoles such as • Nucleic acid
itraconazole,
emergence of resistance is synthesis
inhibitor
decreased and
synergistic antifungal effects
may occur

• its clinical use is limited to the

treatment,
in combination with amphotericin B
The antifungal
or a
triazole, of infections resulting from
spectrum of
Cryptococcus neoformans, possibly
systemic candidal infections and 5-FC is
chromoblastomycosis caused by
molds narrow
 block the
synthesis of
ergosterol
Azoles
They can be
given orally to
treat chronic
mycoses
Azoles
has been supplanted by
more effective,
less toxic triazole
derivatives, such as
fluconazole, itraconazole,
ketoconazole
posaconazole,
and voriconazole

̶has a narrow antifungal

spectrum, not available in
parenteral form,
used for chronic
mucocutaneous
Ketoconazole
candidiasis and
dermatophytes
 ̶ rug of choice in
d
candidiasis and for most
infections caused
by Coccidioides; also drug Fluconazole
of choice for
Cryptococcus neoformans

The broadest-spectrum
triazole, has activity
against most species
of Candida and
Posaconazole
Aspergillus

-Used
intravenously, Echinocandins
others include
anidulafungin and Caspofungin
micafungin

Absorption is increased
by high-fat
foods, distributed to the
stratum corneum,
Griseofulvin
where it binds to keratin
 should not be
used in patients
with Griseofulvin
porphyria

• inhibits a fungal enzyme,

squalene
epoxidase, causes
accumulation of toxic
levels of squalene, which
Terbinafine
can interfere
with ergosterol synthesis

does not inhibit

cytochrome
P450 Azoles
• itraconazole is as Terbinafine
effective in
onychomycoses

polyene antibiotic (toxicity

precludes
systemic use) that disrupts
fungal
membranes by binding to
Nystatin
ergosterol
 • commonly used topically to
suppress
local Candida infections and has
been
used orally to eradicate
gastrointestinal
fungi in patients with impaired
defense
Nystatin
mechanisms

an essential
enzyme in
RBC
Metabolism
G6PD
• Are single-celled animals
• Cause disease in Africa,
South America,
and Asia
• Thrive in areas of poor
Protozoan
sanitation

Several of the
major protozoan
infections
are spread by
vectors
 Most common protozoal
disease
• Second most fatal
infectious
disease in world
• Caused by protozoan
Malaria
Plasmodium

Transmitted by bite
of
female Anopheles
mosquito
Malaria
• prototype
medication for
treating malaria Chloroquine
for over 60 years

• Antiprotozoal, also has

antibiotic activity
against anaerobic
bacteria Metronidazole
• Treats most forms of
amebiasis
parasitic worms that
cause
significant disease in
certain regions of
Helminths
world

• broad-spectrum
• Adverse effects: as
worms die, Mebendazole
abdominal pain,
distension, and diarrhea

Agents for Herpes simplex

Herpesvirus viruses (HSVs)

are a
family of DNA viruses
that cause blisterlike Herpes simplex
lesions on the skin, viruses (HSVs)
genitals, and other
mucosal surfaces
infections of the eye,
mouth,
and lips, although the
incidence
HSV
of genital infections is
increasing type 1
genital HSV
infections type 2
-multiple body •
systems in
immunosuppressed Cytomegalovirus
patients (CMV)

Shingles
(zoster) and Varicella-zoster
chickenpox virus (VZV)
(varicella)
 Infectious
mononucleosis and Epstein-Barr
a form of cancer
known as Burkitt s virus (EBV)
lymphoma

Roseola in children
and hepatitis or Herpesvirus-type
encephalitis in
immunosuppressed 6-
patients

• guanosine analog active

against herpes
simplex virus (HSV-1, HSV-2),
CMV and
varicella-zoster virus at high
doses
Acyclovir
• prevents viral DNA synthesis

commonly used for the

treatment of mucocutaneous
and genital
herpes lesions and for
Oral
prophylaxis in AIDS
and in other
immunocompromised patients acyclovir
 prodrug converted to
acyclovir by hepatic metabolism after oral
administration and reaches plasma levels
3‒5 times greater than those achieved
by acyclovir; has a longer duration of
Valacyclovir
action than acyclovir

Agents for Orthomyxovirus

Influenza genus

• inhibit an early step in

replication of the
influenza A (but not
Amantadine
influenza B) virus
• They prevent uncoating
and
by binding to a
proton channe
Rimantadine
• inhibitors of neuraminidases
produced by
influenza A and B and are
Oseltamivir
currently active
against both H3N2 and H1N1
strains
and
• worldwide resistance remains
rare Zanamivir
a prodrug used
orally,
activated in the Oseltamivir
gut and the liver

Agents for IFN-alpha

(Interferon
Hepatitis alpha)
s a cytokine that acts
through host cell
IFN-alpha
surface receptors
increasing the formation
(Interferon
of antiviral proteins alpha)

prodrug of Adefovir
adefovir Dipivoxil
 suppresses HBV
replication and
improves liver
histology and
Adefovir
fibrosis

antimetabolite
inhibitors of viral primary drugs
reverse transcriptase effective
and inhibitors of viral
aspartate protease against HIV

drug combinations can

slow or reverse the
Highly active
increases in viral RNA antiretroviral
load that normally therapy
accompany progression
of disease (HAART)

resembles
thymidine, one of
the four
Zidovudine
nucleoside building (NRTI)
blocks of DNA
 • is given PO in combination with other
antiretrovirals
• acts by inhibiting reverse transcriptase
• It has the advantage of once-daily
Efavirenz
dosing
and penetration into cerebrospinal fluid
(CSF) (NNRTI)
• liver Efavirenz
enzyme
inducer (NNRTI)
abnormal mass of tissue with
excessive
and uncoordinated growth and
persists in
an extensive manner even after the
cessation of the stimuli which
NEOPLASIA
evoked the
change

• nitrogen mustard, used against

Hodgkin s disease, lymphoma,
multiple
myeloma, breast cancer,
and ovarian cancer.
• acts by attaching to DNA and
Cyclophosphamide
disrupting
replication
• powerful immunosuppressant
will increase the risk
of infections and
further development Cyclophosphamide
of neoplasms

• blocks the synthesis of folic acid

(vitamin
B9), methotrexate inhibits replication,
particularly in rapidly dividing cells
• for choriocarcinoma, osteogenic
sarcoma, leukemias, head and neck
Methotrexate
cancers,breast carcinoma, and lung
carcinoma

a reduced form
of folic acid, is sometimes
administered
Leucovorin
with methotrexate to rescue
normal cells
or to protect against severe
(folinic
bone marrow
damage acid)
• attaches to DNA,
distorting its double
helical structure and
preventing normal
Doxorubicin
DNA and RNA synthesis
specific for the M-phase
of the cell
cycle by inhibiting
microtubule formation in
Vincristine
the mitotic spindle

oral antiestrogen that is a preferred drug

for treating metastatic breast cancer
• It blocks estrogen receptors on breast
cancer cells, but tamoxifen actually
activates estrogen receptors in other
parts
of the body
Tamoxifen
• The only antineoplastic that is approved
for prophylaxis of breast cancer

enhance the ability

of body
Natural
defenses to destroy
certain other
Products
Cytokines or Biologics

• Non-Steroidal
Anti-inflammatory Drugs
• analgesic, antipyretic,
and
anti-inflammatory effects
NSAIDS
 Reye s
a rare,
fatal disorder
characterized by an acute

syndrome
increase in intracranial
pressure and
massive accumulations of
lipids in the liver

a
syndrome that includes
symptoms such as
tinnitus, dizziness,
headache, and
salicylism,
sweating

s inhibit
both cyclooxygenase isoforms

Aspirin
and
thereby decrease prostaglandin
and
thromboxane synthesis
throughout the
body

have less
effect on the
prostaglandins involved in COX-2-selective
homeostatic function, inhibitors
particularly those in
the gastrointestinal tract
 major difference aspirin acetylates
between the and
mechanisms of action thereby irreversibly
of aspirin and other inhibits
NSAIDs cyclooxygenase

The low effective in

reducing
range (<300 platelet
mg/d) aggregation

intermediate have
doses antipyretic and
(300‒2400 analgesic
mg/d) effects

high doses used

(2400‒4000 for an
anti-inflammatory
mg/d) effect
is an older drug used to
relieve mild to
moderate pain, fever,
and inflammation
• inhibition of
Ibuprofen
prostaglandin synthesis

• potent
anti-inflammatory Systemic
action that can
suppress severe Glucocorticoids
cases of inflammation

is a synthetic
glucocorticoid Prednisone

• Its actions are the

result of being
metabolized to an active
form, which is prednisolone
also available as a drug
called
 • is the only
over-the-counter
non-anti-inflammatory Acetaminophen
analgesic
commonly available

• first-generation H1-receptor antagonist

that is a component of some OTC drugs
• primary use is to treat minor symptoms
of allergy and the common cold such as
sneezing, runny nose, and tearing of the
Diphenhydramine
eyes

• is typical of the
intranasal
glucocorticoids
used to treat seasonal
Fluticasone
allergic rhinitis

• effective and common

decongestant
• one of the ingredients
that can be used Pseudoephedrine
to manufacture
methamphetamine
 • drug of
choice for Epinephrine
anaphylaxis