pharmacotherapy with antithrombotic drugs Flashcards by Janet Jincy

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

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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what is the risk factor management for DVT ?

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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what are the short and long term goals in thrombosis ?

short term
prevent thrombus
recanalisation
prevent embolisation

long term
post thrombotic syndrome prevention
and reoccurance of thrombus

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

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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what are the major anti thrombi drugs ?

anticogulants

fibrinolytics

antiplatelets

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what are the anticogulants ?

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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what are the reverse drugs for heparin ?

protamine sulfate

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coumarin anticogulants

route of administration

pharmokinetics

mechanism of action

and lab control

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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what are the indication of coumarin anticoagulants ?

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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whata re the side effects of coumarin anticogulants ?

bleeding

and skin necrosis

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what are the contraindication of coumarin anticoagulants ?

patients with increased hemorrhagic risk , pregnancy , breastfeeding

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what are the drug to drug intercation of coumarin anticoagulants

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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heparin

route of administration

pharmokinetics

mechanism of action

lab control

IV or SC

liver metabolism and renal excretion

binding to antithrombin 3 factors 2a and 10a stopped

lab control= aPTT

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indication of heparin ?

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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what are the side effects of heparin ?

thrombocytopenia
alopecia
osteoperosisi
and bleeding

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contraindication for heparin ?

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

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what is the natagonist of coumarin dervitavies ?

phytomenadione

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low molecular weight heaprin

route of admin

mechanism of action

renal excretion

bnding to antithrombin 3 and majolry stop 10a

what is the indication of LMWH?

first line of pe and and vt and its prevention

first line for for unstable angina and AMI WITHOUT ST ELEVATION

what are teh side effects of LMWH?

bleeding is less than heparin
thrombocytopne
osteoperosis

contraindications of LMWH?

same as heparin

can protamine sulfate be used an anatgonist for lmwh?

partially not fullly!

synthetic pentasaccharide (heparin derivative) fondaparinux

route od admin

mechanism of action

enal excretion

binding to antithrombin 3 - activity against mainly 10a

what are the indications of fondaparinux ?

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)

what are the side effects of fondaparinux ?

anemia | and bleeding

contraindications of fondaparinux ?

pregnancy and breast feeding (no data) creatinin clearance of less than 10ml/min bacterial endocarditis not under 17 heparin induced thrombocytopnea

DABIGATRAN route of admin pk mechanism of action

oral renal excretion direct thrombin inhibitor

indication of dabigatran ?

prevention of DVT in orthopedic surgery of hip and knee atrial fib prevention of stroke and systemic embolism

what are the side efefcts of dabigatran

bleeding but close to lmwh | and anemia

contraindication of dabigatran ?

increased hemorrhagic risk preganncya nd breast feeding(lack of info0 creatinin clearance below 30ml/min liver disease under 18

what are the drug to drug intercation of dabigatran ?

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

rivaroxaban route of admin pk mechanism of action

oral liver metaboslim and renal excretion direct inhibotor of factor 10a

indication of rivaroxaban ?

prevention of dvt in orthopedic surgery atrial fib prevention of stroke and acute coronary syndrome

side effects of rivaroxaban ?

increased liver enzymes anemia bleeding

contraindication of rivaroxaban ?

increased hemorrhagic risk pregnancy and breast feeding creatinin clearance lower than 15 ml/min liver diseases associated with coagulopathy children under 18

what are the drug to drug intercation of rivaroxaban ?

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

what are the fibrinolytics ?

streptokinase alteplase reteplase

fibrinolytics mechanism of action and indications

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 ```

whata re the adverse effects of fibrinolyteics and contraindications ?

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 ```

what are the antiplatlet drugs ?

inhibitors of TXA2 ASA adenosine anatgonist clopidrogel prasugrel ticagrelor phosphodiesterase inhibtors dipyridamole glycoportein2b/3a inhibotrs eptifibatide abciximab synthetics PgI2 epoprostenol

route of adminstration of ASA mechanism of action indications adr contra drugs to drug

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 ```

ADENOSINE ANTAGONIST ? rote of admin mechanism of action indications adr drugs to drug

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

dipyridamole route of admin mechanims of action indic drug inter

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

glycoportein2b and 3a receptor antagonists ? route of admin indications adr contra drug to drug

iv infusion after coronary angioplasty in addition to the therapy of heprain and asa bleeding- adr contra fibrinolytics drug to drug synergy with ASA