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Basilio Aya Marie.

Classification
Aminoglycosides

Cephalosporins

Generic Names
Amikacin

Cephalexin

Action

Indication

Inhibition of protein
synthesis. Once
inside the bacterial
cell,
aminoglycosides
bind to the 30s
ribosomal sub-unit
and cause a
misreading of the
genetic code. This
subsequently leads
to the interruption of
normal bacterial
protein synthesis.

Aminoglycosides
are used for

They interfere with


bacterial cell wall
synthesis.

Cephalexin is
indicated in the
treatment of the
following infections
when caused by
susceptible strains of
the designated
microorganisms
such as otitis media,
lower respiratory
tract infections,
pharyngitis and
tonsillitis, urinary
tract infections, and
skin structure
infections

Serious gram
negative bacillary
infections
(especially those
due to Pseudomonas
aeruginosa)

Contraindicatio Adverse Effects


n
Aminoglycosides
are contraindicated
in patients who are
allergic to them.

All aminoglycosides
cause

Renal toxicity (often


reversible)

Vestibular and
auditory toxicity
(often irreversible)

Prolongation of effects
of neuromuscular
blockers

Cofactor is
contraindicated in
patients with known
allergy to the
cephalosporin group
of antibiotics.

Diarrhea, increased

transaminase,
eosinophilia,
moniliasis, vaginitis,
rash,
stevens-johnson
syndrome,
sseudomembranous
colitis, nausea,
vomiting, anemia,
neutropenia and
jaundice

Drug
Interaction
The ototoxic effects
of the
aminoglycosides,
including amikacin,
are potentiated by
the coadministration of
ethacrynic acid,
furosemide,
mannitol and
possibly other
diuretics.

Patients receiving
Cefalixon may show
a false-positive
reaction for glucose
in the urine with
tests that use
Benedict's and
Fehling's solutions
and also with
Clinitest tablets.
There have been
reports of increased
anticoagulant effect
when cefaclor and
oral anticoagulants
were administered
concomitantly.

Basilio Aya Marie.

Fluoroquinolones

Norfloxacin

Inhibits bacterial
DNA gyrase, which
in turn inhibits DNA
replication and
transcription, DNA
repair,
recombination and
transposicion,
causing bacterial
cell death.

Norfloxacin is
indicated for the
treatment of adults
with the following
infections caused by
susceptible strains
of the designated
microorganisms
such as urinary tract
infections
Uncomplicated
urinary tract
infections, sexually
transmitted diseases
and prostatitis

All drugs or
conditions that
prolong QT interval.
Norfloxacin is
contraindicated in
persons with a
history of
hypersensitivity,
tendinitis, or tendon
rupture associated
with the use of
norfloxacin or any
member of the
quinolone group of
antimicrobial
agents.

nausea, dizziness,
headache, stomach
cramps, weakness,
abdominal pain,
anorexia, anxiety,
arthralgia, arthritis,
ataxia, back pain,
jaundice, confusion,
constipation,
depression, diarrhea,
diplopia, dyspepsia,
dyspnea, erythema,
exacerbation of
myasthenia gravis,
fever, flatulence, GI
bleeding.

Macrolides

Erythromycin

Inhibition of protein
synthesis.
Macrolides
reversibly bind to
50S subunit of the
ribosomes and
inhibit
transpeptidation and
translocation
processes, resulting
in premature
detachment of
incomplete
polypeptide chains.

Macrolides are active


against

Aerobic and anaerobic


gram-positive cocci

Mycoplasma
pneumoniae

Macrolides are
contraindicated in
patients who have
had an allergic
reaction to them.

Main concerns
include

GI disturbances
(mainly with
erythromycin)

Chlamydia trachomatis

Chlamydophila
pneumoniae

Legionella sp

QT-interval
prolongation by
erythromycin

Inhibition of hepatic
metabolism, leading
to numerous drug
interactions

Norfloxacin, may
enhance the effects
of oral
anticoagulants,
including warfarin
or its derivatives or
similar agents.
When these
products are
administered
concomitantly,
prothrombin time or
other suitable
coagulation tests
should be closely
monitored.

Basilio Aya Marie.

Lincosamides

Monobactam

Clindamycin

Aztreonam
Inhalation
IV and IM

Is a lincosamide

antibiotic that is
primarily
bacteriostatic. It
binds to the 50S
subunit of the
ribosome, thus
inhibiting bacterial
protein synthesis.

Clindamycin is
usually used for
anaerobic
infections; however,
clindamycin
resistance has
emerged among
these organisms in
some regions.
Because these
infections often also
involve aerobic
gram-negative
bacilli, additional
antibiotics are also
used

Inhibits cell wall


Aztreonam
synthesis by binding Inhalation is
to penicillin binding indicated to improve
protein 3; member Gram
respiratory
-ve
of monobactam
symptoms in cystic
interobacteria(gitract
family
fibrosis patients with
), skin,intrapseudomonas
abdominal
gyne
infection
aeruginosa. To
reduce the
development of
bacteria and
maintain the
effectiveness, it
should be used only
to treat patients with
CF.

Clindamycin is
contraindicated in
patients who have
had an allergic
reaction to it, and it
should be used with
caution in those who
have a history of
regional enteritis,
ulcerative colitis, or
antibiotic-associated
colitis.

Abdominal pain,

It is contraindicated
in patients with a
known allergy to
aztreonam.

cough,
MIld: nasal
congestion,
gieffects and
increase
wheezing,
enzymes
pharyngolaryngeal
pain, pyrexia, chest
discomfort,
abdominal pain,
vomiting,
bronchospasm and
rash.

agranulocytosis,
eosinophilia
(transient), diarrhea,
fungal overgrowth,
pseudomembranous
colitis,
hypersensitivity,
stevens-johnson
syndrome, rashes,
urticaria,
hypotension,
nausea, vomiting,
sterile abscess at IM
site,
thrombophlebitis,
granulocytopeni,
neutropenia,
thrombocytopenia,
polyarthritis and
renal dysfunction

Orally or
intravenously
administered
clindamycin has
neuromuscular
blocking properties
that may enhance
the action of other
neuromuscular
blocking agents.
Therefore, it should
be used with caution
in patients receiving
such agents.

________________

Basilio Aya Marie.

Penicillin

Amoxicillin

Amoxicillin is
similar to penicillin
in its bactericidal
action against
susceptible bacteria
during the stage of
active
multiplication. It
acts through the
inhibition of cell
wall biosynthesis
that leads to the
death of the
bacteria.

To reduce the
development of
bacteria and
maintain the
effectiveness, it
should be used only
to treat infections
that are proven or
strongly suspected
to be caused by
susceptible bacteria.
When culture and
susceptibility
information are
available, they
should be
considered in
selecting or
modifying
antibacterial
therapy.

Documented
hypersensitivity to
penicillins,
cephalosporins,
imipenem. Serious
hypersensitivity
reactions is
contraindicated in
patients with a
history of serious
hypersensitivity
reactions,
cholestatic jaundice/
hepatic dysfunction,
renal impairment

anaphylaxis,
anemia, AST/ALT
elevation,
mucocutaneous
candidiasis,
diarrhea, headache,
nausea, vomiting,
rash,
pseudomembranous
colitis, and serum
sickness-like
reactions

Amoxicillin acts as
oral anticoagulants,
allopurinol, oral
contraceptives.

Penicillinaseresistant

Dicloxacillin

Binds to one or
more penicillin
binding proteins,
which in turn inhibit
synthesis of bacterial
cell walls. For
treatment of
infections caused by
penicillinaseproducing
staphylococci.
Resistance to this
drug results from
alterations in
penicillin-binding
proteins.

Dicloxacillin is
indicated in the
treatment of
infections caused by
penicillinaseproducing
staphylococci which
have demonstrated
susceptibility to the
drug. Dicloxacilin
may be used to
initiate therapy in
suspected cases of
resistant
staphylococcal
infections prior to
the availability of
laboratory test
results.

Allergy to
penicillins,
cephalosporins,
imipenem
Initial Tx of severe
infections
Not to be relied on
in N/V, gastric
dilatation,
esophageal
achalasia, intestinal
hypermotility
Concomitant live
bacterial vaccines

abdominal pain,
diarrhea, nausea,
anemia, elevated
LFTs, fever,
hypersensitivity,
nephritis,
pseudomembranous
colitis, seizures with
extremely high
doses &/or renal
failure, rash,
vomiting and
vaginitis

Tetracycline, a
bacteriostatic
antibiotic, may
antagonize the
bactercidal effect of
penicillin and
concurrent use of
these drugs should
be avoided.

Basilio Aya Marie.

Sulfonamides

Captopril
Cortimorazole
sulfadiazine
sulfasaline
sulfilazine

-inhibit folic
acid
synthesis
by the
bacteria =
no mitosis/
multiply

UTI (effective
and
human body do not
inexpensive
create folic acid so the
C-trachomatis> For STD
bacteria synthesis create Norcardia
it to dna and rna of the H- influenzabacteria
meningitis

It is contraindicated chest pain, cough,


Its beneficial effects Captopril is
indicated
for
the
in patients who are
dysgeusia,
in hypertension and
treatment of
hypersensitive to
hypersensitivity
heart failure appear hypertension, > otitisthis
> sulfamethoxazole+trimetoprim
media,bronchitis
product or any
reactions,
to result primarily
heart failure, left
other
hyperkalemia,
from suppression of ventricular
angiotensinconverti Gi
hypotension,
-effects
dysfunction after
ng enzyme inhibitor. renal:crystalluria,he
palpitations, pruritis
the reninDo not corash, tachycardia,
maturia,
protenia
angiotensinaldostero myocardial
cns:
headache,
infection, diabetic
administer in
angioedema,
ne system.
dizziness,vertigo,de
nephropathy and
patients with
neutropenia and
However, there is no head to neck
ppresion.
diabetes
photosensitivity
bone marrow
consistent
angioedema and
allergies
deppression
correlation between intestinal
pregancy>tetragenic
angioedema.
renin levels and
Lactation> kernicterus
response to the drug.

Tetracyclines

Sumycin

Inhibits bacterial
protein synthesis by
binding with 30S
and possibly 50S
ribosomal subunit(s)

To reduce the
This drug is
development of
contraindicated in
bacteria and
persons who have
maintain the
shown hypereffectiveness of it, it sensitivity to any of
should
be used only the tetracyclines.
Doxyxyline> broad spectum > travellers diarrhea
STD>
to treat
prevent
minocycline> severe infection drug
ofor
choice
for mingicoccal carriers
oxytetracycline-> treatment for acute infections
amebiasis=
thatcause
are by ameba
- inhiit CHON synthesis
proven or strongly
allergy ,pregnancy,
suspected to be
lactation= skeletal
caused by
susceptible bacteria. and dental fracture

discoloration of
teeth and enamel
hypoplasia, diarrhea,
nausea,
photosensitivity,
anorexia, abdominal
cramps, bulging
GI effects: fatal
fontanels in infants,
hepatology
diabetes effects
insipidus
skeletal
syndrome,
hypersensitivity
esophagitis,
anaphylaxis
exfoliative
ophalmic fungal and
dermatitis,
mycobacterial or
viral ocular infectionpericarditis,
CAUTION: below 8 pseudotumor
cerebri, pancreatitis,
yrs old
pruritus,
pigmentation of
nails and vomiting

Antimycobacteria
(leprostatic)
> Dapsone (its inhibits folicacid synthesis)> leprosy hansendisease> Adverse rexn Bld dyscrasia
> Clofazimine> binds to bacterial DNA sites
2types of leprosy
-pancibacillary- it is not contagious 6months -> Rifampicin & Dapsine
- multibacillary- contagious 24-30months > Rifampicon, dapsine &clozimine

It interacts as a dual
blockade of reninangiotensin system
(RAS)
+ tolbutamide
tolazamide
glyburide
glypride

therefore
there is an
increase risk
for
hypoglycemia
+cyclosporine
= increase in
nephrotoxitixy

Sumycin interacts
with penicillin, anticoagulants, antacids
and iron containing
products, oral
contraceptives, and
methoxyflurane.

= pen G= decrease effect of pen


+ oral contraceptives= effect of
contraception
+ digoxin = increase digitalis toxity
+ ca,mg,zinc,al,fe,charcoal= decrease
absorption of tetracyline

Basilio Aya Marie.


Rifam+ INH =hepathotoxicity

Antimycobacterial
mycobacteria
- outer layer
contain mycolic
acid that protect
them from
disinfectants.
(ANTI
TUBERCULOSIS)

Bedaquiline

It inhibits
Drug indicated as
nausea, arthralgia,
CYP3A4 Inducers/
mycobacterial
part of combination
headache,
Inhibitors, Other
adenosine 5'therapy in the
transaminases
Antimicrobial
Rifampicin > alters DNA and RNA activity> (adverse effect) orange-red discolorization of body secretions.
triphosphate
(ATP)
treatment
of
adults
increased,
and
blood
Medications, and
INoH- ismazid> affects the mycolic acid coating>(AE)Peripheral neuropathy(advice patient to take vit B6) Pregnant woman-/
synthase,
an
enzyme
with
pulmonary
amylase
increased
Antiretroviral
PZA- purazinamide> dissurpt membranes potencial > hepatotoxity/expect jaundice
essential
the
multi-drug
resistant
Medications
Ethambutol> inhibit
cellularfor
metabolism>
color blidness,optic
neuritis. Pregnant(2.5%)
o=woman-/
generation >otoxicity>
of energy tuberculosis.
Stretomysin-aminogluycoside
Mycobacterium
Type 1 in
2RIPE
4 RI
tuberculosis
2 2RIPE 1 RIPE 5RIE
3 2RIPE 4RI

ANTIVIRALS
Classification

Generic Names

Action

Indication

Contraindicatio Adverse Effects


n

Influenza A and
Respiratory Virus

Rimantadine

Rimantadine
Prevent
shedding
of theits
appears
to exert
vital cordeffect
and
inhibitory
entryinofthe
virus
early
viral
into the cell
replicative
cycle,
possibly inhibiting
the uncoating of the
virus. Genetic
studies suggest that
a virus protein
specified by the
virion M2 gene
plays an important
role in the
susceptibility of
influenza A virus to
inhibition by
Rimantadine.

Influenza A is
Rimantadine
Repiratory
indicated
for the
synthial virus
prophylaxis
and
(RSV)
treatment of illness
caused by various
strains of influenza
A virus in adult.
Rimantadine is
indicated for
prophylaxis against
influenza A virus in
children.

Allergy
Rimantadine
pregnancy
hydrochloride is
lactation
contraindicated
in
renal
and hepatic

Amantadine
Oseltamivir
ribavirin
Rimantadine
Zanamir

patients with known


hypersensitivity to
drugs of the
adamantane class,
including
Rimantadine and
amantadine.

orthostatic
Dizziness
insomia
hypotension, edema,

Drug
Interaction

The
concern about
+ anticholinergics
potential
dizziness,
interference arises
confusion,
principally from the
headache, insomnia, potential for
difficulty in
antiviral drugs to
concentrating,
inhibit replication of
anxiety, restlessness, live vaccine virus.
irritability,
hallucinations,
nausea, vomiting,
xerostomia,
abdominal pain,
anorexia and urinary
retention,

Basilio Aya Marie.

Herpes and Cytom


egalovirus

HIV and AIDS

Ganciclovir
Acyclovir
Cidofovir
Famciclovir
Poscarnet
Gancilovir
Valcyclovir

Crofelemer

Inhibits of viral
DNA polymerases
resulting in chain
termination

Herpes simplex,
Ganciclovir
is
herpes
zoster,
indicated for the
CMVcyclomegalo
viruscanofinfect
treatment
CMV
eyes ,uti, and liver

Allergy
Ganciclovir is
pregnancy
contraindicated in
lactation
patientscns
withd/s
severe

retinitis in
hypersensitivity to
immunocompromise
ganciclovir or
Inhibit viral DNA replication
d patients, including acyclovir.
patients with AIDS.
It is also indicated
for the prevention of
CMV disease.
Crofelemer is an
inhibitor of the
cystic fibrosis
transmembrane
regulator chloride
channel (CFTR), as
evidenced by its
activity on cell
cultures, single cell
patch clamps, single
CFTR channels, and
elaboration of
mouse intestinal
fluid secretion.

For the symptomatic


treatment of noninfectious diarrhea
in adult patients
with HIV/AIDS
who are taking
antiretroviral
therapy.

_____________

neutropenia,
thrombocytopenia,
anemia, confusion,
headache, nausea/
vomiting,
neuropathy,
paresthesia, pruritus,
retinal detachment,
rash, sepsis and
weakness.

+zidovudine,
No formal drug
antirefraviral
interaction studies of
= increase drowsiness

Upper respiratory

Studies have shown


that crofelemer has
the potential to
inhibit cytochrome
P450 isoenzyme 3A
and transporters
MRP2 and
OATP1A2 at
concentrations
expected in the gut.
Due to the minimal
absorption of
crofelemer, it is
unlikely to inhibit
cytochrome P450
isoenzymes 1A2,
2A6, 2B6, 2C9,
2C19, 2D6, 2E1 and
CYP3A4
systemicall

tract infection,
bronchitis, cough,
flatulence, increased
bilirubin, nausea,
back pain,
arthralgia, urinary
tract infection,
nasopharyngitis,
musculoskeletal
pain, hemorrhoids,
giardiasis, anxiety
and bdominal
distension.

ganciclovir
commonly used in
+other
nephrotoxic
transplant
recipients
drugs
have
been in
=
increase
conducted.
neprotoxicity

Basilio Aya Marie.

ANTIFUNGAL
Classification

Generic Names

Action

Systemic

Fluconazole

Topical

Ciclopirox

Indication

Contraindicatio Adverse Effects


n

Drug
Interaction

Fluconazole
For the treatment of
interacts with 14-
fungal infections.
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 is
contraindicated in
patients who have
shown
hypersensitivity to
fluconazole or to
any of its excipients.
Coadministration of
other drugs known
to prolong the QT
interval.

nausea, abdominal
pain, headache,
diarrhea, rash and
vomiting.

Fluconazole is a
potent inhibitor of
cytochrome P450
(CYP) isoenzyme
2C9 and 2C19, and
a moderate inhibitor
of CYP3A4.

Unlike antifungals
such as itraconazole
and terbinafine,
which affect sterol
synthesis, ciclopirox
is thought to act
through the
chelation of
polyvalent metal
cations, such as
Fe3+ and Al3+.

Ciclopirox is
contraindicated in
individuals who
have shown
hypersensitivity to
any of its
components.

Main effects:
erythema, pruritus,
erythema of the
proximal nail fold,
transient burning
sensation of the skin
& pain, dry skin,
acne, rash and
alopecia

Used as a topical
treatment in
immunocompetent
patients with mild to
moderate
onychomycosis of
fingernails and
toenails without
lunula involvement,
due to Trichophyton
rubrum.

_____________

Basilio Aya Marie.

ANTIPROTOZOAL
Classification

Generic Names

Action

Indication

Contraindicatio Adverse Effects


n

Drug
Interaction

Antimalarial

Mefloquine

Mefloquine is an
antimalarial agent
which acts as a
blood schizonticide.
Mefloquine is active
against the
erythrocytic stages
of Plasmodium
species. However,
the drug has no
effect against the
exoerythrocytic
(hepatic) stages of
the parasite.
Mefloquine is
effective against
malaria parasites
resistant to
chloroquine.

For the treatment of


mild to moderate
acute malaria caused
by Mefloquineuinesusceptible strains
of Plasmodium
falciparum (both
chloroquinesusceptible and
resistant strains) or
by Plasmodium
vivax. Also for the
prophylaxis of
Plasmodium
falciparum and
Plasmodium vivax
malaria infections,
including
prophylaxis of
chloroquineresistant strains of
Plasmodium
falciparum.

Mefloquine is
contraindicated in
patients with a
known
hypersensitivity to
mefloquine.
Mefloquine should
not be prescribed for
prophylaxis in
patients with active
depression, a recent
history of
depression,
generalized anxiety
disorder, psychosis,
or schizophrenia or
other major
psychiatric
disorders, or with a
history of
convulsions.

At the doses used


for treatment of
acute malaria
infections, the
symptoms possibly
attributable to drug
administration
cannot be
distinguished from
those symptoms
usually attributable
to the disease itself.

anxiety, difficulty
concentrating,
headache, insomnia,
lightheadedness,
vertigo, vomiting,
diarrhea, stomach
pain, nausea, visual
disturbances and
tinnitus

Basilio Aya Marie.

Other
antiprotozoals

Tinidazole

Antiprotozoal; may
cause cytotoxicity
by damaging DNA
and preventing
further DNA
synthesis

Trichomoniasis,
Giardiasis,
Amebiasis, Bacterial
Vaginosis.
Tinidazole should be
used only to treat or
prevent infections
that are proven or
strongly suspected
to be caused by
susceptible bacteria.

The use of tinidazole


is contraindicated in
patients with a
previous history of
hypersensitivity to
tinidazole or other
nitroimidazole
derivatives, first
trimester of
pregnancy, and
interruption of
breast-feeding is
recommended
during tinidazole
therapy and for 3
days following the
last dose.

SOURCE
http://www.drugbank.ca/drugs/
http://www.drugs.com
http://www.medicinenet.com

anorexia,
constipation,
dizziness, dysgeusia,
dyspepsia, headache,
nausea, vomiting,
weakness/ fatigue/
malaise.

Although not
specifically
identified in studies
with tinidazole, the
following drug
interactions were
reported for
metronidazole, a
chemically-related
nitroimidazole.
Therefore, these
drug interactions
may occur with
tinidazole.

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