Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
1
ADP receptor blocker
CLOPIDOGREL
TICLOPIDINE
COX
inhibitor
(Aspirin)
Phosphodiesterase
inhibitor-
DIPYRIDAMOLE,
CILOSTAZOL...
Aspirin
N.B.Aspirin inhibitsThromboxane A2 & prostacyclin too, but the former is more
affected because platelets don’t hav...
 Most authorities recommend initial therapy
with a dose of 160 mg (one half-tablet) to 325
mg (one adult tablet)
 Aspiri...
 Prophylaxis against unstable angina
 Post MI
 Post stroke
Adverse effects
GI –ulceration
Prolonged bleeding time  ↑ r...
ABCIXIMAB is composed of 7E3 Fab fragments.
derived from murine (mouse)
 Humanised monoclonal antibody.
 directed agains...
TIROFIBAN -non-peptic
 Synthetic arginine-glycine-aspartic acid (R-G-D)
sequence mimetics
 Hence, it blocks the binding ...
TICLOPIDINE & CLOPIDOGREL
They inhibit irreversibly ADP binding to receptors 
inhibit platelet aggregation
No effect on P...
 Acts by in inhibiting phoshodiesterase enzyme
 Incompletely absorbed from the gastrointestinal
tract with peak plasma c...
 It is an inhibitor of phosphodiesterase III (PDE III)
enzyme
 Vasodilator and inhibitor of platelet aggregation
 Inter...
Prasugrel
Thienopyridine
More rapid onset of action than clopidogrel
Irreversible inhibitor of the P2Y12 receptor
Benefici...
Ticagrelor
Cyclo-pentyl-triazo-pyrimidine (CPTP)
More rapid onset of action than clopidogrel
Reversible inhibitor of the P...
 Myocardial infarction
 Unstable angina
 Coronary bypass implants
 Prosthetic heart valves and arteriovenous shunts
 ...
Streptokinase
Urokinase
Anistreplase
t-PA
Reteplase
tenecteplase
 1ST GEN:
 STREPTOKINASE (SK)
▪ Derived from ß-hemolytic streptococci
▪ Binds & activates plasminogen plasmin “systemi...
 2ND GEN: ALTEPLASE (TPA)
 Cleaves plasminogen plasmin fibrinolysis
 Specific activity in thrombus, less systemic
fib...
 3RD GEN: modifications of TPA
 RETEPLASE
▪ Half-life= 18 min
▪ Double bolus regimen
 TENECTEPLASE (TNK)
▪ Half life= 2...
 The plasma half-life of the third generation drugs is
14-45 minutes, allowing administration as a single or
double intra...
 Coronary Thrombolytics
 Pulmonary embolism
 DVT
 Arterial occlusion e.g. Popliteal artery
 Ischaemic stroke
 Occlud...
 Intracranial hemorrhage or hemorrhagic stroke
 Ischemic Stroke within 3 month
 Known structural cerebrovascular lesion...
Class antiplatele tand fibinolytics
Class antiplatele tand fibinolytics
Class antiplatele tand fibinolytics
Class antiplatele tand fibinolytics
Class antiplatele tand fibinolytics
Class antiplatele tand fibinolytics
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Class antiplatele tand fibinolytics

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  • September 2007
  • September 2007
  • September 2007
  • September 2007
  • September 2007
  • September 2007
  • September 2007
  • Class antiplatele tand fibinolytics

    1. 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. 1
    2. 2. ADP receptor blocker CLOPIDOGREL TICLOPIDINE COX inhibitor (Aspirin) Phosphodiesterase inhibitor- DIPYRIDAMOLE, CILOSTAZOLE Gb IIb/IIIa receptor blockers ABCIXIMAB EPTIFIBATIDE TIROFIBAN TXA2 receptor TERUTROBAN
    3. 3. Aspirin N.B.Aspirin inhibitsThromboxane A2 & prostacyclin too, but the former is more affected because platelets don’t have nuclei can’t synthesize new enzymes for next 7 daysplatelets life span
    4. 4.  Most authorities recommend initial therapy with a dose of 160 mg (one half-tablet) to 325 mg (one adult tablet)  Aspirin should be crushed/chewed (to facilitate faster absorption by breaking the enteric-coated delayed release tablet
    5. 5.  Prophylaxis against unstable angina  Post MI  Post stroke Adverse effects GI –ulceration Prolonged bleeding time  ↑ risk of hemorrhage
    6. 6. ABCIXIMAB is composed of 7E3 Fab fragments. derived from murine (mouse)  Humanised monoclonal antibody.  directed against glycoprotein receptor type GPIIb/IIIa.  Mechanism: The m7E3 Fab binds selectively to the glycoprotein GPIIb/IIIa receptors inhibiting platelet aggregation  Plasma T1/2- 30min  Bolus –followed by slow IV infusion  Major side effect- bleeding
    7. 7. TIROFIBAN -non-peptic  Synthetic arginine-glycine-aspartic acid (R-G-D) sequence mimetics  Hence, it blocks the binding of fibrinogen to glycoprotein GPIIb/IIIa receptors  They are given intravenously for the reduction of thrombotic complications during coronary angioplasty (if they are given orally they are toxic)  Clinical trials showed reductions in the incidence of death and non-fatal MI in response to the use of tirofiban.
    8. 8. TICLOPIDINE & CLOPIDOGREL They inhibit irreversibly ADP binding to receptors  inhibit platelet aggregation No effect on PG synthesis Used in aspirin intolerant patients
    9. 9.  Acts by in inhibiting phoshodiesterase enzyme  Incompletely absorbed from the gastrointestinal tract with peak plasma concentration occuring about 75 minutes after oral administration  More than 90% bound to plasma proteins  A terminal half-life of 10 to 12 hours  Metabolised in the liver  Mainly excreted as glucuronides in the bile; a small amount is excreted in the urine
    10. 10.  It is an inhibitor of phosphodiesterase III (PDE III) enzyme  Vasodilator and inhibitor of platelet aggregation  Intermittent claudication  Indicated for the reduction of events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent MI or established peripheral arterial disease  C/I- CHF patients
    11. 11. Prasugrel Thienopyridine More rapid onset of action than clopidogrel Irreversible inhibitor of the P2Y12 receptor Beneficial in the treatment and prevention of ACS and the prevention of thromboembolic events Adenosine Diphosphate-Receptor Antagonists
    12. 12. Ticagrelor Cyclo-pentyl-triazo-pyrimidine (CPTP) More rapid onset of action than clopidogrel Reversible inhibitor of the P2Y12 receptor
    13. 13.  Myocardial infarction  Unstable angina  Coronary bypass implants  Prosthetic heart valves and arteriovenous shunts  Venous thromboembolism and PVD  Cerebrovascular transient ischemic attacks
    14. 14. Streptokinase Urokinase Anistreplase t-PA Reteplase tenecteplase
    15. 15.  1ST GEN:  STREPTOKINASE (SK) ▪ Derived from ß-hemolytic streptococci ▪ Binds & activates plasminogen plasmin “systemic” fibrinolysis ▪ 1-1.5 million U IV over 60min ▪ Cheap  ANTISTREPLASE (plasminogen-SK) ▪ 30mg IV over 5 min *Allergic reactions (6%) *Avoid re-treatment for 6 months (+Ab)
    16. 16.  2ND GEN: ALTEPLASE (TPA)  Cleaves plasminogen plasmin fibrinolysis  Specific activity in thrombus, less systemic fibrinolysis  Weight-based IV infusion over 60-90min  Half-life<5 min  Heparin commonly administered shortly after
    17. 17.  3RD GEN: modifications of TPA  RETEPLASE ▪ Half-life= 18 min ▪ Double bolus regimen  TENECTEPLASE (TNK) ▪ Half life= 20 min ▪ Single-weight tiered bolus dosing over 5-10s * No absolute mortality benefit in AMI
    18. 18.  The plasma half-life of the third generation drugs is 14-45 minutes, allowing administration as a single or double intravenous bolus.  This is in contrast to second generation t-PA, which with a half-life of 3-4 minutes, must be administered an initial bolus followed by infusion
    19. 19.  Coronary Thrombolytics  Pulmonary embolism  DVT  Arterial occlusion e.g. Popliteal artery  Ischaemic stroke  Occluded AV shunts  Blocked central vacuum catheters
    20. 20.  Intracranial hemorrhage or hemorrhagic stroke  Ischemic Stroke within 3 month  Known structural cerebrovascular lesion (AVMs, aneurysms, tumor)  Closed head injury with in 3 months.  Aortic dissection  Severe uncontrolled hypertension SBP > 180 DBP > 110  Active bleeding or bleeding diathesis  Acute pericarditis

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