ANTICOAGULANT

Generic

Classificatio
n

Cilostazol

Anti-platelet

Dosage with
Indications
Dosage:
Adult: PO 100 mg
twice daily.
Indication:
Management of
peripheral
vascular
disorders

Mechanism of
Action

Adverse Reaction

Brand Names

Cilostazol is a
reversible,
selective inhibitor
of
phosphodiesteras
e-III (PDE-III),
thereby
suppressing cyclic
adenosine
monophosphate
(cAMP)
degradation.
Increase in cAMP
in platelets and
blood vessels
leads to inhibition
of platelet
aggregation and
vasodilation.
Cilostazol also
inhibits adenosine
uptake into cells,
which augments
the cAMPelevating effect of
PDE-III inhibition.

Headache, dizziness,
palpitations,
diarrhoea, abnormal
stools; pain, infection;
peripheral edema,
nausea, vomiting,
other cardiac
arrhythmias, chest
pain, rhinitis,
pharyngitis,
ecchymosis and skin
rash.

Aggravan,
Ciletin,
Clazol, Pencil
50 / Pencil
100, Platecil,
Pletaal,
Trombocil,
Vaxol

GI disturbances,
heartburn, easy
bruising/bleeding,
nausea and vomiting,
ictericia, allergic
reactions

Anthrom,
Asaprim,
Aspen,
Aspilets,
Aspitor,
Asthromed,
Bayer,
Bayprin, COR30, Cortal,
Norplat-s,
Tromcor

Absorption:
Absorbed from
the GI tract after
oral admin.
Aspirin

NSAID

Dosage:
Adult:

PO Prophylaxis
of MI: 75-325
mg/day.
Stent
implantation:
325 mg 2 hr preop, then 160-325
mg/day.
Pain and fever:
325-650 mg 4-6
hrly. Max: 4
g/day.
Pain and
inflammation
associated w/
musculoskeletal
and joint
disorders: Initial:
2.4-3.6 g/day.

It suppresses the
production of
prostaglandins
and
thromboxanes is
due to its
irreversible
inactivation of
the cyclooxygena
se (COX) enzyme.
Cyclooxygenase is
required for
prostaglandin and
thromboxane
synthesis. Aspirin
acts as an
acetylating agent
where an acetyl
group is
covalently
attached to

Maintenance:
3.6-5.4 g/day.
Indication:

Streptokin
ase

a serine residue in
the active site of
the COX enzyme.

It reduces fever
and relieve mild
to moderate pain
from conditions
such as muscle
aches, toothache
s, common cold,
and headaches.
It can be used to
reduce pain and
swelling in
conditions such
as arthritis. It
may also be used
to prevent MI
and stroke.

Anticoagulan Dosage:
t,
Antiplatelet Acute MI: IV
Dissolve
&
1,500,000 iu in
Fibrinolytics
100 mL 0.9%
NaCl or 5%
dextrose inj.
Administer over
30-60 min.
Intracoronary
infusion: Dissolve
250,000-500,000
iu in 100 mL
0.9% NaCl or 5%
dextrose inj.
Administer over
30-60 min.
Acute deep
thrombosis,
acute pulmonary
embolism, acute
arterial
occlusion: Initial
dose: Dissolve
250,000 iu in 100
mL 0.9% NaCl or
5% dextrose inj.
Administer over
30 min.
Maintenance:
Dissolve
1,200,000 iu in
500 mL 0.9%
NaCl or 5%
dextrose inj.
Administer
100,000 iu/hr for
12 hr/day for 3

Streptokinase
forms a complex
with plasminogen
which then
converts
plasminogen to
plasmin. Plasmin
breaks down clots
as well as
fibrinogen and
other plasma
proteins.
Absorption:
Rapidly cleared
from the
circulation after IV
use.
Excretion:
Elimination halflife of
streptokinaseactivator
complex: 23 mins.

Depression of BP,
allergic reactions,
bleeding or
hemorrhage, slight
elevation in body
temp, hypotension,
bradycardia, very
severe low back pain,
Guillain-Barre
syndrome, nausea,
vomiting, dyspnea &
headache.

Britton, STPase,
Streptokin

days.
Conglobation of
arteriovenous
shunt: Dissolve
100,000 iu in 100
mL 0.9% NaCl inj.
Deposit 10,00025,000 iu in the
clotted shunt.
May be repeated
after 30-45 min.
Indication:
Treatment of
thromboembolic
disorders eg MI,
peripheral
arterial
thromboembolis
m & VTE (DVT &
pulmonary
embolism).
For conglobation of
arteriovenous
shunt.
Clopidogr
el

Antiplatelet
agent

Dosage:
Adult:
PO Prophylaxis of
thromboembolic
events 75 mg
once daily.
Acute coronary
syndrome : For
ST-elevation
myocardial
infarction: W/
aspirin: 75 mg
once daily.
Continue
treatment for up
to 28 days. For
unstable angina,
non-ST-elevation
myocardial
infarction: Initial:
300 mg loading
dose, followed by
75 mg once daily
(w/ aspirin 75325 mg once
daily).
Indication:
Alternative
prophylaxis to
aspirin in
patients at risk of
thromboembolic

Clopidogrel
inhibits adenosine
diphosphate
(ADP) from
binding to its
receptor sites on
the platelets and
subsequent
activation of
glycoprotein GP
IIb/IIIa complex
thus preventing
fibrinogen
binding, platelet
adhesion and
aggregation.
Absorption:
Rapidly but
incompletely
absorbed from
the GI tract (oral).
Distribution:
Protein-binding:
Extensive.
Metabolism:
Hepatic:
Extensive;
converted to
inactive
carboxylic acid

Dyspepsia,
abdominal pain,
nausea, vomiting,
flatulence,
constipation,
gastritis, gastric and
duodenal ulcers. GI
upset, diarrhoea,
paraesthesia, vertigo,
headache, dizziness,
pruritus and rashes.
Potentially
Fatal: Bleeding
disorders including GI
and intracranial
haemorrhage. Blood
dyscrasias.

Actaclo,
Antiplar,
Atheros,
Avancur,
Cardogrel,
Clopidowel75, Clopidra,
Clopidrol,
Clopimed,
Clopimet,
Clopivaz,
Clopivin,
Clopix,
Cloplat,
Cloprez,
Clotiz,
Clovas,
Clovax,
Clovix,
Corplet,
Deplatt,
Dogrel,
Dorell,
Hemaflow,
Hivix,
Klopide,
Navorel,
Nogrel,
Noklot,
Norplat,
Norplat-s,
Pharex

disorders eg MI,
peripheral
arterial disease &
stroke.

Fondapari
nux

Anticoagulan Dosage and

t,
Indication:
Antiplatelet
& Fibrinolytic Subcutaneous
(Thrombolyti Deep vein
c)
thrombosis

derivative and
thiol derivative
(active).

Clopidogrel,
Platelex,
Platexan,
Plavihex,
Plavix,
Plogrel,
Ritemed
Clopidogrel,
Timiflo,
Trombix,
Vivelon,
Winthrop
Clopidogrel

Excretion: Via
urine and faeces
(as metabolites
and unchanged
drug).

Fondaparinux, a
synthetic
pentasaccharide,
acts as a selective
inhibitor of
activated factor X.
It works by
Adult: <50 kg: 5
binding
mg once daily, 50selectively to
100 kg: 7.5 mg
ATIII, and
once daily, >100
potentiates the
kg: 10 mg once
neutralisation of
daily. Treatment
Factor Xa. This
duration: 5-9 days,
or at least until oral will interrupt the
blood coagulation
anticoagulation is
cascade and
established.
inhibit both
CrCl
Dosage thrombin
(ml/min)
Recommendation
formation and
thrombus
<20
Contra-indicated.
development. At
the recommended
Subcutaneous
dosage,
fondaparinux
Unstable angina
does not affect
Adult: For patients
fibrinolytic
in which urgent
activity or platelet
percutaneous
function. It cannot
coronary
lyse established
intervention is not
thrombi and does
planned: 2.5 mg
not affect clotting
once daily for up to
function tests
8 days. For acute
(e.g. aPPT, INR).
ST-elevation MI, 1st
dose to be given IV
Absorption:
(directly through an Rapidly and
existing IV line or as completely
infusion in 25 or 50
absorbed after SC
ml of 0.9% saline
inj. SC
over 1-2 minutes),
bioavailability:
subsequent doses
100%.
to be given SC.
Distribution:
Initiate treatment
Protein binding:
as soon as

Bleeding,
thrombocytopenia,
local irritation (e.g.
rash , pruritus, inj site
bleeding), increase in
LFTs, fever, nausea,
vomiting,
constipation.
Potentially
Fatal: Epidural or
spinal haematomas
that may result in
permanent paralysis;
severe haemorrhage.

Arixtra

diagnosis is made
and continued up to
a max of 8 days or
until hospital
discharge,
whichever comes
earlier.

Extensively bound
to antithrombin
III.

Excretion:
Excreted in the
urine as
unchanged drug
CrCl
Dosage (64 -77% of a
dose). Elimination
(ml/min)
Recommendation
half-life: 17-21 hr;
<20
Contra-indicated.
prolonged in
renally impaired,
Subcutaneous
elderly and <50
kg.
Acute ST-elevation
myocardial
infarction
Adult: For patients
in which urgent
percutaneous
coronary
intervention is not
planned: 2.5 mg
once daily for up to
8 days. For acute
ST-elevation MI, 1st
dose to be given IV
(directly through an
existing IV line or as
infusion in 25 or 50
ml of 0.9% saline
over 1-2 minutes),
subsequent doses
to be given SC.
Initiate treatment
as soon as
diagnosis is made
and continued up to
a max of 8 days or
until hospital
discharge,
whichever comes
earlier.
CrCl
Dosage
(ml/min)
Heparin Recommendation
Anticoagulan Dosage and
<20
Contra-indicated.
t,
Indication:
Antiplatelets
Subcutaneous
&
Fibrinolytics Venous
(Thrombolyti
thromboembolis
c)
m
Adult: 15,000 u
injected every 12
hr.
Child: 250 u/kg

Heparin increases
the inhibitory
action of
antithrombin III
(AT III) on clotting
factors XIIa, XIa,
IXa, Xa and
thrombin. This
inhibits the
conversion of
prothrombin to

Slight fever,
headache, chills,
nausea, vomiting,
constipation,
epistaxis, bruising,
slight haematuria,
skin necrosis (SC inj),
osteoporosis,
alopecia.
Hypersensitivity
reactions include

Britton
Heparin Na,
Contractubex
, Hemastat,
Heparin Leo,
Heprin, Lioton
Gel, Meparin
5/ Meparin 25

every 12 hr.
Subcutaneous

Prophylaxis of
postoperative
venous
thromboembolis
m
Adult: 5000 u given
2 hr before surgery
then every 8-12 hr
for 7 days or until
the patient is
ambulant, may
increase to 10,000
u every 12 hr
during the 3rd
trimester of
pregnancy.
Subcutaneous

Prophylaxis of
mural
thrombosis
Adult: 12,500 u
every 12 hr for at
least 10 days.
Intravenous

Unstable angina
Adult: 5000 u
(10,000 u in severe
pulmonary
embolism) IV
loading dose
followed by 10002000 u/hr
continuous infusion.
Alternatively,
intermittent inj of
5000-10,000 u
every 4-6 hr.
Child: Administer a
lower loading dose.
Maintenance: 15-25
u/kg/hr continuous
infusion.
Intravenous

Venous
thromboembolis
m
Adult: 5000 u
(10,000 u in severe
pulmonary
embolism) IV

thrombin and
fibrinogen to
fibrin. It also
inhibits platelet
function. It may
reduce the
activity of ATIII at
very high doses.
Absorption:
Absorbed from
systemic
circulation (IV,
SC).
Distribution:
Reticuloendotheli
al system.
Protein-binding:
Extensive.
Excretion: Via
urine (as
metabolites, or up
to 50% as
unchanged after
admin of large
doses); 1-6 hr
(elimination halflife), prolonged in
renal impairment,
decreased in
pulmonary
embolism,
increased or
decreased in
hepatic
impairment.

urticaria,
conjunctivitis, rhinitis,
asthma, angioedema
and anaphylactic
shock. Priapism.
Potentially
Fatal: Heparininduced
thrombocytopenia
with or without
thrombosis; bleeding.
Incompatibility:
Heparin calcium or
sodium is reported to
be incompatible with
alteplase, reteplase,
amikacin sulfate,
amiodarone
hydrochloride,
ampicillin sodium,
aprotinin,
benzylpenicillin
potassium or sodium,
cefalotin sodium,
ciprofloxacin lactate,
cytarabine,
dacarbazine,
daunorubicin
hydrochloride,
diazepam,
dobutamine
hydrochloride,
doxorubicin
hydrochloride,
droperidol,
erythromycin
lactobionate,
gentamicin sulfate,
haloperidol lactate,
hyaluronidase,
hydrocortisone
sodium succinate,
kanamycin sulfate,
meticillin sodium,
netilmicin sulfate,
some opioid
analgesics,
oxytetracycline
hydrochloride, some
phenothiazines,
polymyxin B sulfate,
streptomycin sulfate,
tetracycline
hydrochloride,
tobramycin sulfate,
vancomycin

loading dose
followed by 10002000 u/hr
continuous infusion.
Alternatively,
intermittent inj of
5000-10,000 u
every 4-6 hr.
Child: Administer a
lower loading dose.
Maintenance: 15-25
u/kg/hr continuous
infusion.
Intravenous

Peripheral arterial
embolism
Adult: 5000 u
(10,000 u in severe
pulmonary
embolism) IV
loading dose
followed by 10002000 u/hr
continuous infusion.
Alternatively,
intermittent inj of
5000-10,000 u
every 4-6 hr.
Child: Administer a
lower loading dose.
Maintenance: 15-25
u/kg/hr continuous
infusion.
Intravenous

Prophylaxis of reocclusion of the

coronary arteries
following
thrombolytic
therapy in
myocardial
infarction
Adult: 5000 u IV
followed by 1000
u/hr IV with
alteplase.

hydrochloride and
vinblastine sulfate.
Heparin sodium has
also been reported to
be incompatible with
cisatracurium
besilate, labetalol
hydrochloride,
levofloxacin,
nicardipine
hydrochloride and
vinorelbine tartrate.

Enoxapari
n

Low
molecular
weight
heparin

Dosage and
Indication:
Subcutaneous

Prophylaxis of
venous
thromboembolis
m during surgical
procedures
Adult: Low to
moderate risk: 20
mg (2000 units)
once daily with the
1st dose 2 hr preoperatively. High
risk: 40 mg (4000
units) once daily
with the 1st dose
12 hr preoperatively.
Alternatively, 30
mg (3000 units) bid
starting within 1224 hr after the
operation. After hip
replacement
surgery, continue
treatment at 40 mg
once daily for a
further 3 wk. For
immobilized
patients, treatment
should continue at
40 mg daily for at
least 6 days or until
patient becomes
fully ambulant, up
to a max of 14
days.
CrCl
Dosage
(ml/mi Recommend
n)
ation
Reduce
dose.
<30
Max: 1
mg/kg/day.
Subcutaneous

Deep vein
thrombosis
Adult: 1 mg (100
units)/kg every 12
hr for 5 days and
until oral
anticoagulation is
established.

Enoxaparin is a
low molecular
weight heparin
with
anticoagulant
properties. It acts
by enhancing the
inhibition rate of
activated clotting
factors including
thrombin and
factor Xa through
its action on
antithrombin III.
Absorption:
Rapidly and
almost completely
absorbed after SC
inj with a
bioavailability of
about 100%.
Metabolism:
Metabolised
hepatically.
Excretion:
Elimination halflife: 4-5 hr.
Excreted in urine
as unchanged
drug and
metabolites.

Bleeding,
Thrombocytopenia,
pain, bruising or
irritation
Symptoms similar to
those of hay fever,
abdominal/chest
pain,
headache,
hyperkalemia
transaminitis

Clexane,
Hepaclex,
Lomoh-40,
Lomoh-60,
Olxarin

CrCl
(ml/min)

Dosage
Recommendation
Reduce dose. Max: 1
<30
mg/kg/day.
Subcutaneous

Prophylaxis of
clotting in the
extracorporeal
circulation during
haemodialysis
Adult: 1 mg/kg (100
units/kg) into the
arterial line of the
circuit at the
beginning of the
dialysis session.
Give a further dose
of 0.5-1 mg/kg (50100 units/kg) if
required. Reduce
dose in patients at
high risk of
haemorrhage.
CrCl
Dosage
(ml/min) Recommendation
Reduce dose. Max:
1 mg/kg/day.
Subcutaneous
<30

Unstable angina
Adult: 1 mg/kg (100
units/kg) every 12
hr for 2-8 days with
low-dose aspirin.

Prasugrel

CrCl
Dosage
(ml/m
Recommendation
in)
Reduce dose. Max: 1
<30
mg/kg/day.
Anticoagulan Dosage:
Prasugrel is a
t,
prodrug, oxidation
Antiplatelet Adult: Single 60 mg by intestinal and
loading dose.
& Fibrinolytic
hepatic
Continue at 10
cytochrome P-450
mg once daily.
(Thrombolyti
enzymes convert
ASA: 75-325 mg
c)
prasugrel into its
daily. Duration:
active metabolite.
12 mth.
Prasugrel has a
Patient
rapid and almost
weighing <60
complete
kg Single 60 mg
absorption after
loading dose.
Continue at 5 mg oral ingestion of a
once daily.
loading dose. Its
Indication:
active form binds

Bleeding, anemia,
hematoma, epistaxis,
GI hemorrhage, rash
ecchymosis,
hematuria, vessel
puncture site
hematoma, puncture
site hemorrhage,
contusion.

Effient

Co-administered w/
acetylsalicylic
acid (ASA) for the
prevention of
atherothrombotic
events in
patients w/ acute
coronary
syndrome (eg
unstable angina,
non-ST segment
elevation MI or
ST segment
elevation MI)
undergoing
primary or
delayed
percutaneous
coronary
intervention.

Triflusal

Anticoagulan Dosage:
t,
Oral
Antiplatelet
& Fibrinolytic Prophylaxis of
(Thrombolyti
thromboembolic
c)
disorders
Adult: Usual dose:
300-900 mg daily.
Indication:
Secondary
prevention after
a 1st coronary or
cerebrovascular
ischemic event of
myocardial
infarction, stable
and unstable
angina,
nonhemorrhagic
stroke or
transient
ischemic attack.

irreversibly to the
adenosine
diphosphate
(ADP) P2Y12
receptor on
platelets for their
lifespan, thereby
inhibiting their
activation and
decreasing
subsequent
platelet
aggregation.
Prasugrel has a
greater
antiplatelet effect
than clopidogrel
because it is
metabolized more
efficiently. Some
of the differences
in metabolism
between
clopidogrel and
prasugrel may be
explained by
genetic
polymorphisms
affecting the
cytochrome P-450
system.

Triflusal, a
derivative of
salicylic acid, is
an inhibitor of
platelet
aggregation. It
inhibits platelet
arachidonic
metabolism and
stimulates
platelet cAMP
production. Unlike
aspirin, it does
not increase
bleeding time. It
may also have
neuroprotective
effects as animal
studies have
shown that it
blocks the
biochemical
pathway that

Nausea, vomiting,
gastric and epigastric
pain, erythema,
conjunctival
haemorrhage,
epistaxis.

Grendis

Reduction of
vein-graft
occlusion after
coronary bypass.

leads to cell
damage during
ischemia in the
nervous system.
Absorption:
Bioavailability: 83100%. Peak
plasma
concentration:
0.88 hr (triflusal);
4.96 hr (HTB).
Distribution:
Protein binding:
extensive.
Metabolism:
Rapidly
metabolised by
liver to active
metabolite, 3Hydroxy-4trifluoromethylbenzoic
acid (HTB).
Excretion: Via
urine as
metabolites.
Terminal half life:
0.53 hr (triflusal);
34.29 hr (HTB)

Dabigatra
n

Anticoagulan Dosage and

t,
Indication:
Antiplatelet
& Fibrinolytic Prevention of
stroke, systemic
(Thrombolyti
embolism &
c)
reduction of
vascular
mortality in
patients w/ atrial
fibrillation: 150
mg bid.
Patients w/
potentially
higher risk of
major
bleeding 110 mg
bid reduced daily
dose.
Elderly 80 yr 110
mg bid.
Adult: Prevention of
VTE in patients
who have
undergone major
orthopedic

Dabigatran and
its acyl
glucuronides are
competitive,
direct thrombin
inhibitors.
Because thrombin
(serine protease)
enables the
conversion of
fibrinogen into
fibrin during the
coagulation
cascade, its
inhibition
prevents the
development of a
thrombus. Both
free and clotbound thrombin,
and thrombininduced platelet
aggregation are
inhibited by the

Bleeding, dyspepsia
(including abdominal
pain upper,
abdominal pain,
abdominal
discomfort, and
epigastric discomfort)
and gastritis-like
symptoms (including
GERD, esophagitis,
erosive gastritis,
gastric hemorrhage,
hemorrhagic gastritis,
hemorrhagic erosive
gastritis, and
gastrointestinal
ulcer).
Hypersensitivity
reactions

Pradaxa

surgery: 2 cap of
110 mg once
daily.
Renal impairment 2
cap of 75 mg
once daily.
Prevention of VTE
following knee
replacement
surgery: Initially
110 mg w/in 1-4
hr of completed
surgery, then 2
cap of 110 mg
daily thereafter
for 10 days.
Prevention of VTE
following hip
replacement
surgery: Initially
110 mg w/in 1-4
hr of completed
surgery, then 2
cap of 110 mg
daily thereafter
for 28-35 days.
For both
surgeries, if
hemostasis is not
secured,
initiation of
treatment should
be delayed. If
treatment is not
started on the
day of surgery,
then treatment
should be
initiated w/ 2 cap
once daily.
Treatment of acute
DVT &/or PE &
prevention of
related
death: 300 mg as
150-mg cap bid
following
treatment w/ a
parenteral
anticoagulant for
at least 5 days.
Therapy should
be continued for
up to 6 mth.
Prevention of
recurrent DVT
&/or PE & related
death: 300 mg as
150-mg cap bid.
Therapy could be
continued life-

active moieties.
Pharmacodynami
cs: At
recommended
therapeutic
doses, dabigatran
etexilate prolongs
the coagulation
markers such as
aPTT, ECT, and TT.
INR is relatively
insensitive to the
exposure to
dabigatran and
cannot be
interpreted the
same way as used
for warfarin
monitoring.

long depending
on the individual
patient risk.
Reduce the risk of
stroke and
systemic
embolism in
patients with
non-valvular
atrial fibrillation.
Rivaroxab
an

Anticoagula Dosage and

nt,
Indication:
Antiplatelet
& Fibrinolytic 10-mg FC tab 10
mg once daily.
(Thrombolyti
Should be taken
c)
6-10 hr after
surgery. Duration
of
treatment: Major
hip surgery- 5
wk. Major knee
surgery-2 wk. 15& 20-mg FC tab
Stroke prevention
in atrial
fibrillation 20 mg
once daily.
DVT & PE
treatment:
Initially 15 mg
bid for the 1st 3
wk, followed by
20 mg once daily
for the continued
treatment &
prevention of
recurrent DVT &
PE. Max: 30 mg
daily during the
1st 3 wk of
treatment & 20
mg daily for the
following
treatment phase.
Prevention of
venous
thromboembolis
m (VTE) in adult
patients
undergoing
elective hip or
knee
replacement
surgery.

Rivaroxaban is a
highly selective
direct factor Xa
(FXa) inhibitor
with oral
bioavailability.
Activation of
factor X to FXa via
the intrinsic and
extrinsic pathway
plays a central
role in the
cascade of blood
coagulation. FXa
directly converts
prothrombin to
thrombin through
the
prothrombinase
complex, and
ultimately, this
reaction leads to
fibrin clot
formation and
activation of
platelets by
thrombin. One
molecule of FXa is
able to generate
>1000 molecules
of thrombin due
to the
amplification
nature of the
coagulation
cascade. In
addition, the
reaction rate of
prothrombinasebound FXa
increases
300,000-fold
compared to that
of free FXa and
causes an
explosive burst of

Anemia, tachycardia;
eye hemorrhage
including conjunctival
hemorrhage; gingival
bleeding, GIT
hemorrhage, GI &
abdominal pains,
dyspepsia, nausea,
constipation,
diarrhea, vomiting;
fever, peripheral
edema, fatigue &
asthenia; post-op
anemia & wound
hemorrhage,
contusion; increased
transaminases; pain
in extremity;
dizziness, headache,
syncope; hematuria
& menorrhagia,
increased blood
creatinine & urea;
epistaxis,
hemoptysis; pruritus,
rash, ecchymosis,
urticaria, cutaneous
& SC hemorrhage;
hypotension,
hematoma.

Xarelto

thrombin
generation.
Selective
inhibitors of FXa
can terminate the
amplified burst of
thrombin
generation.
Consequently,
several specific
and global
clotting tests are
affected by
rivaroxaban. Dose
dependent
inhibition of factor
Xa activity was
observed in
humans.
Warfarin

Anticoagula
nt,
Antiplatelet
& Fibrinolytic

Dosage and
Indication:
Oral

(Thrombolyti Treatment and

prophylaxis of
c)
venous
thromboembolis
m
Adult: Initially, 5 mg
daily. Rapid anticoagulation:
Initially, 10 mg
daily for 2 days.
Adjust subsequent
doses based on
PT/INR. Usual
maintenance dose:
2-10 mg daily.
Elderly: Lower
initial dose.
Renal impairment:
Severe: Avoid.
Hepatic
impairment:
Severe: Avoid.
Intravenous

Treatment and
prophylaxis of
venous
thromboembolis
m
Adult: Given as
slow bolus Inj over

Warfarin inhibits
synthesis of vit Kdependent
coagulation
factors VII, IX, X
and II and
anticoagulant
protein C and its
cofactor protein S.
No effects on
established
thrombus but
further extension
of the clot can be
prevented.
Secondary
embolic
phenomena are
avoided.
Onset: 24 hr
Duration: 2-5
days.
Absorption:
Absorbed readily
from the GI tract
(oral); used as
racemic isomers,
S-isomers more
potent. Peak
plasma
concentration:
within first 4 hr.
Distribution:
Protein binding:
Extensive (99%)

Hypersensitivity,
rash, alopecia,
diarrhoea, drop in
haematocrit, purple
toes syndrome, skin
necrosis, jaundice,
nausea, vomiting,
hepatic dysfunction,
pancreatitis,
increased LFT.
PotentiallyFatal:
Haemorrhage (narrow
therapeutic index).

Coumadin,
Warik, Zyfarin

1-2 min into

peripheral vein.
Initially, 5 mg daily.
Rapid anticoagulation:
Initially, 10 mg
daily for 2 days.
Adjust subsequent
doses based on
PT/INR. Usual
maintenance dose:
2-10 mg daily.
Elderly: Lower
initial dose.
Renal impairment:
Severe: Avoid.
Hepatic
impairment:
Severe: Avoid.

to albumin.
Crosses placenta.
Metabolism:
Hepatic; mainly
by the
cytochrome P450
isoenzyme
CYP2C9, which
shows genetic
polymorphism.
Other enzymes
involved include
CYP2C19,
CYP2C8,
CYP2C18,
CYP1A2, and
CYP3A4. S-isomer
is metabolised
more rapidly than
R-isomer.
Excretion: Via
urine (as
metabolites after
reabsorption from
the bile); 37 hr
(elimination halflife).