pharmcharts by nuhman10

VIEWS: 14 PAGES: 6

									Anticoagulants

Delayed Acting     Adverse         Interactions              Comments
Agents             Effects


Warfarin           Bleeding        Anticoagulant effects     Oral admin. Related to Vit. K. Inhibits
(Coumarins)        Fetal           increased by              formation of clotting factors whose
                   Warfarin        amodiarone,               synthesis utilizes reduced Vit. K.
                   Syndrome        macrolides,               Delay of 2 days to onset of
                                   sulfonamides,             anticoagulant effects. Narrow
                                   quinolones, azole         therapeutic window. Must monitor
                                   antifungals,              PT (INR).
                                   fluoxetine,
                                   gemfibrozil,
                                   sertaraline, gingko,
                                   Vit. E, NSAIDS.
                                   Anticoagulant effects
                                   decreased by
                                   carbamazepine,
                                   rifampin,
                                   cholestryramine, Vit.
                                   K, St. John’s Wort,
                                   ginseng, CoQ.



Anticoagulants and Stroke

Immediate        Adverse Effects        Interactions       Comments

Unfractionated   Bleeding. Must         Increased          5-30 kDa, parenteral delivery. Inhibits
Heparin          monitor aPTT,          bleeding when      thrombin and Xa. High inter-patient
                 Thrombocytopenia       used with other    variability requires monitoring aPTT.
                 (HIT),                 anticoagulants     Used in acute thromboembolic
                 Hyperkalemia in                           disorders and coagulopathies, heart
                 some cases                                surgery, blood transfusion, renal
                                                           dialysis, deep vein thrombosis,
                                                           pulmonary embolism

Low Molec.       Similar to heparin,    Increased          209 kDa purified from heparin. MOA,
Wt. (LMW)        somewhat less          bleeding when      effects, and indications similar to
Heparin                                 used with other    heparin but more selective for Xa
(enoxaparin,                            anticoagulants     inhibition. Parenteral and SQ delivery.
dalteparin,                                                Response more predictable than
tinzaparin)                                                unfractionated heparin
Fondaparinux   Similar to heparin,   Increased         Synthetic pentasaccharide with MOA
               somewhat less         bleeding with     and effects similar to heparin, more
                                     other anticoag.   selective for action on Xa inhibition.
                                                       Also more predicatable response

Hirudin        Bleeding              Increased         Direct thrombin inhibitor that does
Analogs                              bleeding when     not require AT-III for action, more
                                     used with other   predictable effects than heparins.
                                     anticoagulants    Does not cause thrombocytopenia.
                                                       Oral agents under development

Argatroban     Bleeding              Similar to LMW    Thrombin inhibitor. Used in pts with
                                     heparin           HIT or at risk for it. Short half life,
                                                       good in pts with renal dysfunction.
                                                       Use Cautiously in pts with liver
                                                       impairment

Antiplatelet   Adverse Effects       Interactions      Comments
Agents


Aspirin        GI ulceration,        Increased         Irreversible inhibition of COX, Blocks
               hypersensitivity,     bleeding when     synthesis of TxA2, Recovery requires
               Reyes synd. in        used with other   synthesis of new platelets, Prevention
               children              anticoagulants    of arterial thrombosis in pts with
                                                       ischemic heart disease, stroke, TIA.

Dipyramidole                         Increased         Inhibits phosphodiesterase and
                                     bleeding when     raises platelet cAMP to decrease
                                     used with other   aggregation. Usually administered
                                     anticoagulants    with warfarin or aspirin, some
                                                       vasodilatory properties. Used in
                                                       combination with aspirin to prevent
                                                       ischemic stroke and TIA

Aggrenox                             Increased         Combination product of aspirin +
                                     bleeding when     dipyramidole
                                     used with other
                                     anticoagulants

Clopidogrel    GI bleeding,          Increased         Inhibits the action of ADP on platelet
               increased             bleeding when     aggregation by binding to P2Y
               bleeding              used with other   receptor. Increases cAMP.
                                     anticoagulants;   Clopidogrel is a prodrug that is
                                     multiple drug     metabolized to active cmpd with
                                     interactions –    t1/2=8hrs. Used in pts that are
                                     see text          intolerant or unresponsive to aspirin.
                                                       Works for life of platelet. Used in
                                                       ischemia, stroke, TIA, thrombotic
                                                       disorders
Antiplatelet    Adverse Effects     Interactions      Comments
Agents


Abciximab       Bleeding,           Effects persist   Chimeric monoclonal antibody. IV
                thrombocytopenia,   24-48 hrs         only. GPIIb/IIIa inhibitor that blocks
                hypotension,                          integrin receptors on platelets to
                bradycardia                           prevent aggregation. Blocks binding
                                                      of fibrinogen & von Willebrand factor.
                                                      Administered in combination with
                                                      aspirin or heparin. Used for
                                                      prevention of restenois & re-
                                                      infarction. Expensive

Eptifibatide    Bleeding                              IV only. GPIIb/IIIa inhibitor that blocks
Tirofiban                                             integrin receptors on platelets to
                                                      prevent aggregation. Blocks binding
                                                      of fibrinogen. Inhibition is
                                                      comopetitive & reversible. Used for
                                                      prevention of restenois & re-
                                                      infarction, acute coronary
                                                      syndromes. Less expensive than
                                                      abciximab

Fibrinolytic    Adverse Effects     Indications       Comments – All are IV administered.
Agents                                                Note contraindications from slides


Alteplase       Hemorrhage          Use in stroke     Recombinant human t-PA, a serine
Reteplase                           reduces           protease. Lyses fibrin clots through
                                    neurologic        proteolytic activation of plasmin.
Tenecteplase
                                    sequelae          “Fibrin selective” Must use within 3
                                                      hr window post-stroke

Streptokinase   Hemorrhage          Use in stroke     Bacterial product that forms a
                Highly              reduces           complex with plasminogen which
                immunogenic         neurologic        allows conversion to plasmin. Less
                                    sequelae          expensive than others but highly
                                                      immunogenic and cannot be used
                                                      repetitively. Not “Fibrin Selective”.
                                                      Same 3 hr window for use. Less
                                                      expensive than alteplase

Anistreplase    Hemorrhage          Use in stroke     Prodrug. Complex of streptokinase
                Immunogenic         reduces           and plasminogen. Only plasminogen
                                    neurologic        associated with the streptokinase is
                                    sequelae          activated.
Drugs for bleeding

                 Adverse         Interactions       Comments
                 Effects




Phytonadione                     Interferes with    Antagonizes effects of coumarins and used
(Vitamin K)                      oral               to treat bleeding. Response is slow. Use
                                 anticoagulants     fresh frozen plasma if rapid response is
                                                    desired

Protamine        Dyspnea,                           For treatment of heparin-induced bleeding.
Sulfate          flushing,                          Positively charged basic protein that
                 bradycardia,                       inactivates negatively charged heparin
                 hypotension

Aminocaproic     Intravascular                      Synthetic inhibitor of plasminogen activation.
Acid             thrombosis                         Oral admin.



Aprotinin        Renal                              Serine protease inhibitor. Blocks plasmin.
                 dysfunction,                       Inhibits streptokinase. Used for reduction of
                 anaphylaxis                        perioperative blood loss and need for blood
                                                    transfuion in pts undergoing
                                                    cardiopulmonary bypass. Do not use if pt
                                                    had prior use within last 12 months.

Tranexemic       Intravascular                      Synthetic inhibitor of plasminogen activation.
Acic             thrombosis                         Oral admin.




Hemostasis III

Drug             Adverse Effects     Interactions        Indications & Comments


Ferrous          Oxidative stress    Reduces             Iron deficiency anemias. Total dose of
sulphate,        if too much         absorption of       100-200 mg daily. Absorption increased
Ferrous          given, epigastric   tetracyclines,      if given with Vit C. Sustained release
gluconate,       pain, nausea,       fluoroquinones,     preps available to decrease GI
Ferrous          vomiting, black     levothyroxine,      symptoms, but absorption in less with
fumarate         stools, diarrhea    vit E. Large        these preps.
                 or constipation     quantities can
                                     be lethal
Iron Dextran      Fatal                               Dextran conjugated iron. IM or IV only.
                  anaphylactic                        For pts who cannot tolerate or fail on
                  reactions,                          oral iron therapy. Dextran complex
                  injection site                      taken up by reticuloendothelial system,
                  pain &                              degraded to iron and returned to plasma
                  inflammation,
                  brown
                  discolorations

Folic Acid                          May mask B12      Treatment of megaloblastic anemia.
                                    deficiency        Prevention of neural tube defects in
                                                      pregnancy. Rule out B12 deficiency
                                                      before treatment. May be protective for
                                                      coronary artery disease.

Vitamin B12                         Rule out folate   Treatment of megaloblastic anemia.
                                    deficiency        Must give IV or IM if deficiency is due to
                                    before treating   lack of intrinsic factor (pernicious
                                                      anemia). Oral delivery for dietary
                                                      deficiency.

Drug              Adverse Effects   Interactions      Indications & Comments




5-Azacytidine     Risk of cancer                      DNA methylating agent that increases
                                                      HbF. Used in treatment of b thalassemia
                                                      and sickle cell. Does not prevent end
                                                      organ damage.

Hydroxyurea                                           May block expression of HbS and favor
                                                      expression of HbF. Used in treatment of
                                                      sickle cell & thalassemia. Slower
                                                      induction of HbF than azacytidine.
                                                      Effective in 60% of sickle cell pts. Does
                                                      not prevent end organ damage.

Butyrates         Risk of cancer                      Histone deacetylase inhibitors for use in
(arginine                                             treatement of sickle cell disease.
butyrate,                                             Increases HbF and prevents switch from
phenylbutyrate)                                       HbF to HbS in infants & children. Not
                                                      effective in pts with baseline HbF less
                                                      than 1%

Recombinant                                           Growth factor that acts at erythropoietin
Human                                                 receptor to stimulate erythropoiesis. Pts
Erythropoietin                                        should take iron supplements to
(rhEPO, epoetin                                       increase iron stores when taking this
alfa)                                                 drug. Used for treatment of anemias
                                                      resulting from renal failure &
                                                       cancer/cancer chemotherapy




Darbepoetin                                            Same as rhEPO but drug has additional
(NESP)                                                 sialic acid residues to increase half life.


Drug             Adverse Effects      Interactions     Indications & Comments




Filgrastin       Bone pain                             Recombinant human G-CSF, acts like
                                                       the endogenous growth factor to
                                                       increase neutrophil count. For treatment
                                                       of neutropenia. Enhances microbicidal
                                                       actiivity.

Peg-Filgrastin   Same as filgrastin                    Polyethylene glycol conjugate of
                                                       filgrastin. Long lasting, decreases need
                                                       for daily dosing.

Sargramostiim    Fever, arthralgia,                    Recombinant human GM-CSF, acts like
                 edema, pleural &                      endogenous growth factor to increase
                 pericardial                           neutrophil & eosinophil count and
                 effusion                              enhance microbicidal activity.

Thrombopoietin   Thromboembolic       In development   In clinical trials for thrombocytopenia
Analogues        disorders



Interleukin 1    Increased                             Recombinant human interleukin
                 inflammation                          approved for thrombocytopenia

								
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