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pharmacology > pharmacotherapy with antithrombotic drugs > Flashcards

pharmacotherapy with antithrombotic drugs Flashcards

1
Q

what are the different types of thrombus ? where do they occur? and how do they occur ?

A

there is arterial = coronary , cerebral , mesenteric , renal , lower libs
due to = artherosclerosis (and its risk factors eg hypertnesion, smoking, and high cholestrol!!)
, antipholipid , hyperhomocysteinemia , radiation and chemotherapy

venous in the femoral and popliteal ordeep veins of the pelvis
most common
leads to pulmonary embolism! = venous thromboembolic disease
= prgenancy , fracture , limb immbolisation , hormonal contrcaeptives

and there is thrombus in the heart chambers
sue to MI , arterial fib , endocarditis , cardiomyopathy , prosthetic heart valves
= cause arterial thromboembolism mainly affecting lower extremitis and brain then kidney

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2
Q

what is the risk factor management for DVT ?

A

low risk
minr surgery
major surgery and less than 40
truamatic injury and illnes

moderate risk
major surgery over 40
heart failure , recent MI , malignancy , chronic ulcerative collitis
major trauma and burns

minor surgery , trauma / bursn and prevous DVT and PE

high risk
fracture or othropedic surgery of the hip pelvis and lower limbs

large pelvic or abdominal surgery

paraplegia

amuptation of limb

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3
Q

what are the short and long term goals in thrombosis ?

A

short term
prevent thrombus
recanalisation
prevent embolisation

long term
post thrombotic syndrome prevention
and reoccurance of thrombus

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4
Q

what are the charachteristics of each thrombus ?and the drug of choice accordingly

A

arterial thrombi = white thrombus due to ajorly platlet activation
around the white thrombi there is local stasisi causeing activation of fibrinogen to fibrin = forimg red thrombiaswell
= therefor needs antiplatelet and anticoaguant drugs

venous = red thrombi
= fibrin forms as a long tail and can easly break away causing emboli
anticogulants are the essential

in cardiac
more red thrombi and cougulant activation then platlet activation
needs anticoagulants , however effectiveness increased by antiplatlets

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5
Q

what are the major anti thrombi drugs ?

A

anticogulants

fibrinolytics

antiplatelets

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6
Q

what are the anticogulants ?

A

vit k anatgonist (coumarin) :
warfarin
and acenocoumural

heparin and related drugs :
heparin
LMH = nadroparin etc
synthetic pentasaccharides = fondaparinux

direct thrombin inhibotrs :
dabigatran

inhibotors of 10a
rivaroxaban

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7
Q

what are the reverse drugs for heparin ?

A

protamine sulfate

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8
Q

coumarin anticogulants

route of administration

pharmokinetics

mechanism of action

and lab control

A

route
ORAL

PK
binding to plasma proteins and metabolism in the liver by CP2C9

action:
vit k antagonist = stops 2,5,6,9,10

lab control:
INR and PT

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9
Q

what are the indication of coumarin anticoagulants ?

A

after the intial treatmnet of heparin in DVT and PE = venous thromboembolims = prevention

prevention of thromboemeolsim in the heart (due to whatever reasons)

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10
Q

whata re the side effects of coumarin anticogulants ?

A

bleeding

and skin necrosis

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11
Q

what are the contraindication of coumarin anticoagulants ?

A

patients with increased hemorrhagic risk , pregnancy , breastfeeding

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12
Q

what are the drug to drug intercation of coumarin anticoagulants

A

inhibitors of cyp2c9 increasing its effect of coumarin= amiodarone , antifungal azoles , co-trimoxazole, metronidazole , fluoxentine

inducers of cyp2c9 decreasing effect of coumarin=
phenobarbitural
carbamezapine
rifampicin

affecting pharmodynamic  increasing the effect of coumarin
asa
clopidrogel 
heparin 
3rd gen cephalosproin

body - liver disease , congestive heart failure , hyperthyrodiism

affecting pharmodynamics decreasing the effect of coumarin
estrogen , vit k

body - heriditory resistance hypothyroidism

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13
Q

heparin

route of administration

pharmokinetics

mechanism of action

lab control

A

IV or SC

liver metabolism and renal excretion

binding to antithrombin 3 factors 2a and 10a stopped

lab control= aPTT

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14
Q

indication of heparin ?

A

first line treatmnte for DVT AND PE and its prevention

first line for unstable angina and AMI

during surgery of angiplasty or stenting or ventricular surgery

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15
Q

what are the side effects of heparin ?

A

thrombocytopenia
alopecia
osteoperosisi
and bleeding

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16
Q

contraindication for heparin ?

A

patinets with increased hemorrhagic risk
advanced liver disease
adanced kindey disease
heparin is safe in pregnancy

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17
Q

what is the natagonist of coumarin dervitavies ?

A

phytomenadione

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18
Q

low molecular weight heaprin

route of admin

pk

mechanism of action

A

sc

renal excretion

bnding to antithrombin 3 and majolry stop 10a

19
Q

what is the indication of LMWH?

A

first line of pe and and vt and its prevention

first line for for unstable angina and AMI WITHOUT ST ELEVATION

20
Q

what are teh side effects of LMWH?

A

bleeding is less than heparin
thrombocytopne
osteoperosis

21
Q

contraindications of LMWH?

A

same as heparin

22
Q

can protamine sulfate be used an anatgonist for lmwh?

A

partially not fullly!

23
Q

synthetic pentasaccharide (heparin derivative) fondaparinux

route od admin

pk

mechanism of action

A

sc

enal excretion

binding to antithrombin 3 - activity against mainly 10a

24
Q

what are the indications of fondaparinux ?

A

prevent DVT in orthopedic surgery of hip and knee

prevention of venous thromboemebolism in the old at high risk

acute spontaneous thrombosii of superficial veins of lower limbs with NO DVT

acute coronary syndrome (ami and unstable angina)

25
Q

what are the side effects of fondaparinux ?

A

anemia

and bleeding

26
Q

contraindications of fondaparinux ?

A

pregnancy and breast feeding (no data)

creatinin clearance of less than 10ml/min

bacterial endocarditis

not under 17

heparin induced thrombocytopnea

27
Q

DABIGATRAN

route of admin

pk

mechanism of action

A

oral

renal excretion

direct thrombin inhibitor

28
Q

indication of dabigatran ?

A

prevention of DVT in orthopedic surgery of hip and knee

atrial fib prevention of stroke and systemic embolism

29
Q

what are the side efefcts of dabigatran

A

bleeding but close to lmwh

and anemia

30
Q

contraindication of dabigatran ?

A

increased hemorrhagic risk

preganncya nd breast feeding(lack of info0

creatinin clearance below 30ml/min

liver disease

under 18

31
Q

what are the drug to drug intercation of dabigatran ?

A

inhibitors of efflux transported p-glycoportein = amiodarone , verapamil and clarithromycin
= all reduced effect of these drugs

32
Q

rivaroxaban

route of admin

pk

mechanism of action

A

oral

liver metaboslim and renal excretion

direct inhibotor of factor 10a

33
Q

indication of rivaroxaban ?

A

prevention of dvt in orthopedic surgery

atrial fib prevention of stroke and acute coronary syndrome

34
Q

side effects of rivaroxaban ?

A

increased liver enzymes
anemia
bleeding

35
Q

contraindication of rivaroxaban ?

A

increased hemorrhagic risk

pregnancy and breast feeding

creatinin clearance lower than 15 ml/min

liver diseases associated with coagulopathy

children under 18

36
Q

what are the drug to drug intercation of rivaroxaban ?

A

inhibiting CYP3A4 and P glycoportein efflux transporter
increase effects of azole
hiv portease inhibtrs- ritanovir

37
Q

what are the fibrinolytics ?

A

streptokinase
alteplase
reteplase

38
Q

fibrinolytics

mechanism of action

and indications

A

convert plasminogen to plasmin
directly streptokinase
indirectly ((the plases) - recombinat tissue plasminogen activators

plasm lysisi the clot

indications :
multiple PE 
central DVT 
acute MI WITHIN 6-12 HOURS 
ACUTE THROMBTIC STROKE FIRST 3 HRS
39
Q

whata re the adverse effects of fibrinolyteics and contraindications ?

A

bleeding
streptokinase - allergic reaction

contra 
gastroinetsinal bleeding 
cogulation abnormalities such as liver disease 
pregancy and 1 month after birth 
metastatic cancer 
hemorrhgic stroke patient 
sever hypertension 
hemorrhagic diabetic retinopathy
40
Q

what are the antiplatlet drugs ?

A

inhibitors of TXA2
ASA

adenosine anatgonist
clopidrogel
prasugrel
ticagrelor

phosphodiesterase inhibtors
dipyridamole

glycoportein2b/3a inhibotrs
eptifibatide abciximab

synthetics PgI2
epoprostenol

41
Q

route of adminstration of ASA

mechanism of action

indications

adr

contra

drugs to drug

A

oral

IRREVERSIBILE inhibtor of COX-1

prevention of ischemic heart disease
transient cerebral ischemic attacks and strokes
after angioplasty and stenting
cardiovascular operation = bypass

dyspepsia and gastroinetsinal bleeding

contra
increased hemorhgaic risk suh as severe hypertnsion and previous intrcranila hemorrhage 
ulcer 
active erosive gastrtis 
liver damage
42
Q

ADENOSINE ANTAGONIST ?

rote of admin

mechanism of action

indications

adr

drugs to drug

A

oral

block effect of ADP by P2Y12 recptor block

indic
transient ischemic attack,
stroke ,
coronary angioplasty and stenting in COMBO WITH ASA

adr
bleeding

drug to drg
synergy with ASA
omeprazole - induces cpy2c9 =
decrease the effect of clopidrogel

43
Q

dipyridamole

route of admin

mechanims of action

indic

drug inter

A

oral

inhibition of adenosine uptake and phosphodiesterase= increase intracellular conc of cAMP

indicat
in combo with aspirin for cerebovascular ischemia prevention

drug to drug
synergy with ASA

44
Q

glycoportein2b and 3a receptor antagonists ?

route of admin

indications

adr

contra

drug to drug

A

iv infusion

after coronary angioplasty in addition to the therapy of heprain and asa

bleeding- adr

contra
fibrinolytics

drug to drug
synergy with ASA

pharmacology (7 decks)

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