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Pharm 1 > Hematopoietics, Anticoag, Antiplatelets and Thrombolytic Drugs > Flashcards

Hematopoietics, Anticoag, Antiplatelets and Thrombolytic Drugs Flashcards

1
Q

HEMATOPOIETICS

A

Recombinant growth factors

3 types:

  1. Erythropoietin Stimulating Agent
    - increase RBC production (Epoetin)
  2. Granulocyte Stimulating Agents
    - increase myeloblast cells (G-CSF, GM-CSF)
  3. Platelet Stimulating Agents
    - increases platelet production (thrombocytes)
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2
Q

ESAs

A

Epoetin, Procrit, Darbepoetin given IV or SQ

Uses: Anemia: renal disease

Onset of Action

  • 2 to 6 weeks (take a while to work)
  • 8-26 days to actually increase RBC numbers

Monitoring

  • hemoglobin
  • iron levels
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3
Q

G-CSF

A

Increases WBCS-neutrophils

Filgrastim, Pegfilgrastrim
IV, SQ or patch

Uses:
-treats neutropenia complications in cancer pt.

Pegfilgrastim needs to be given once
Filgrastrim is daily

Monitoring: absolute neutrophil count (ANC)

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4
Q

GM-CSF

A

Increases WBC production (neutrophils, eosinophils, basophils and mast cells) and RBCs

Sargramostin

Uses:

  • acute myelogenous leukemia
  • bone marrow transplant

Monitoring: CBC with differential

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5
Q

TPO Receptors

A

Increase platelet production

Romipolstim(outside of receptor) Eltrombopag (inside of receptor)

MOA:
-binds to and activates human thrombopoetin receptor

OOA:
-increased platelet production in a week

Uses: chronic immune thrombocytopenia

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6
Q

Drugs to combat CLOT FORMATION

A

1: ANTICOAGULANTS
2: ANTI-PLATELETS
3: THROMBOLYTICS

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7
Q

ANTICOAGULANTS

A
  • prevent further propagation of clots
  • disrupt clotting cascade
  • best for treatment of arterial and venous clots
  • inhibit activity of clotting factors
  • inhibit synthesis of clotting factors

HEPARIN, LMWH, FONDAPARINUX, WARFARIN, DIRECT THROMBIN AND DIRECT Xa INHIBITORS

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8
Q

Heparin UNFRACTIONATED MOA

A

MOA: enhance the activity of antithrombin

  • inhibit factor Xa and thrombin equally
  • inhibits the change of fibrinogen to fibrin

A mixture of long polysaccharide chains
Active section is a pentassaccharide sequence found randomly along the chain
Metabolized by the LIVER
Bolus dose

Indications: treatment and prevention of thrombosis

Bodies own way of responding to clot is ENHANCED by heparin

  1. First binds with Antithrombin + causes a conformational change
  2. Then binds to factor 10 (Xa) and thrombin EQUALLY
  3. THIS DISRUPTS FINAL STEP OF FIBRINOGEN TO FIBRIN
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9
Q

UPH Monitoring

A

Monitoring efficacy

  • aPTT (more common) or anti-Xa
  • checked usually every 4-6 hours until stable

APPT and ANTI XA SHOULD BE HIGHER WITH HEPARIN

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10
Q

APTT test

A

Activated partial thromboplastin

  • measures the time it takes for the blood to clot
  • higher aPTT=more anticoagulation effects

We want high aPPT when on heparin
-but not too high or too low

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11
Q

Anti-Xa

A

Measures the amount of Xa not bound by heparin

Higher the level=more anticoagulation effects

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12
Q

UPH Adverse Effects

A

BLEEDING (10%)

  • must monitor for:
  • blood loss
  • decreased BP
  • increased HR
  • black tarry stools
  • red colored urine
  • headache
  • somnolence
  • abdominal pain
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13
Q

UFH Side Effects

A

Spinal epidural hematoma

Heparin-Induced Thrombocytopenia (HIT)
-DECREASE IN PLATELETS
-Type 1: usually 1-2 days after exposure
(transient drop in platelets, will recover)
-Type 2: 4-7 days after exposure WORSE
(>50% drop in platelets over time, worry about thrombosis)
(COULD cause a secondary clot)

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14
Q

HIT

A

Body develops antibodies to heparin-PF4 (platelet factor 4) complex
-results in new thrombosis development

Confirm by ordering HIT antibody test with SRA assay

Treatment

  • discontinue heparin
  • initiate ARGATROBAN (antidote) - different drug that causes clot formation
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15
Q

Reversing bleeding with UFH

A

Antidote: PROTAMINE(+)
-Binds with Heparin(-)—>no longer able to bind to anti-thrombin—>CAUSES CLOTS, prevents heparin from working

  • neutralization occurs immediately and last for 2 hours
  • little roll for protamine if the heparin infusion was discontinued over 4 hours agin
  • give plasma or blood (if Hg<7 or hypotension) in addition to protamine if necessary
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16
Q

PROTAMINE

A

First isolated from fish sperm

Highly positive charged molecule (binds with heparin-negatively charged)

Sequesters heparin so it cannot bind with antithrombin

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17
Q

Low-molecular weight heparins

LMWH

A

Smaller pieces of polysaccharides -cannot hug thrombin

MOA:
-bind to antithrombin and inactivate Factor Xa (only)

Indications: treatment and prevention of thrombosis

Onset: 1-2 hours QUICKER; SQ (Patient can be treated outpatient!

Formulations: Enoxaparin, Tinzaparin, and Dalteparin

Monitoring: anti Xa (level)
-rental cleared (cannot use in patients with acute kidney injury or hemodialysis

PREFERRED OVER UFH to treat and prevent venous thrombosis
-quicker, no hospital stay, can self administer, don’t have to monitor, rare to cause HIT

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18
Q

LMWH Adverse Events

A

Bleeding (less common that UFH)

Spinal /epidural hematoma

Thrombocytopenia (similar to HIT)

  • antibody mediated, less likely with LMWH
  • discontinue medication, treat with Argatroban
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19
Q

LMWH Reversal of Bleeding

A

Antidote: PROTAMINE can be used, not as effective

  • binds 80% of LMWH
  • can give within 12-24 hours after last done of LMWH
  • give plasma or blood (if Hg<7 or hypotension) in addition to PROTAMINE if necessary
  • protamine cannot bind to LMWH, less of a negatively charged tail present for protamine to bind to
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20
Q

Fondaparinux MOA

A

-inhibits Factor Xa by binding to antithrombin

Only contains the essential pentasaccharide

DVT/PE treatment and prevention

Administration: SQ -once a day

Renally eliminated, cannot use in acute kidney injury or hemodialysis

Can be used in patients with a history of HIT

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21
Q

Fondaparinux Adverse Events and Reversal

A

Adverse events:

  • bleeding
  • similar to UFH and LMWH

Antidote: None

  • give plasma or blood (if Hg<7 or hypotensive)
  • cannot give PROTAMINE, drug is too small and will not bind to protamine
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22
Q

Vitamin K Antagonist

A

WARFARIN

Treats and prevents thrombosis

MOA: inhibits clotting factor synthesis that require vitamin K

  • inhibits vitamin K epoxide reductase complex 1 and vitamin k reductase
  • inhibit production of: Prothrombin (Factor II), VII, IX, X, Protein C and S (FACTORS 2, 7, 9, 10 and PROTEIN C and S)
  • conversion of fibrinogen to fibrin will not occur
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23
Q

Warfarin (cont.)

A

Extensively bound to albumin

Metabolized by the liver CYP2C9

OOA: DELAYED! takes approx 2 days to start decreasing clotting factors
-usually takes several days to achieve full therapeutic effect
(Half life of factor II=90hours)
-if drug is stopped, effects linger

  • Must BRIDGE with another anticoagulant to treat the clot in the meantime!
  • bridge while receiving SQ or IV anticoagulants for active clots
24
Q

Warfarin Monitoring and Goals

A

Monitoring:

  • International Normalized Ratio (INR)
  • prothrombin time (PT)

INR measures decrease in clotting factor caused by warfarin

INR=higher=more anticoagulation with warfarin

  • want it around 2-3
  • INR>3-4=HIGH RISK OF BLEEDING
25
Warfarin Adverse Effects and Reversal
BLEEDING Reversal of uncontrolled bleeding: - antidote: Phytonadione (Vitamin K) -takes a while - takes at least 2-6 hours to start reversing effects - total effect within 24 hours - MUST give plasma or prothrombin complex concentrate (PCC) or factor VII (novoseven) in the meantime to treat the bleeding right away-gives you all the factors that warfarin inhibits (2, 7, 9, 10) quicker - can give blood in addition based on HgB
26
Warfarin Interactions | INCREASED
``` Bactrim Amidarone Cimetidine Acetaminophen Metronidazole Anole Antifungals ``` Example: Give warfarin while a patient is on bactrim treating a UTI - bactrim will inhibit metabolization of warfarin - warfarin will accumulate in the blood - INR=too higher, depleted too many clotting factors =HIGH BLEEDING RISK - more warfarin, inhibits anticoagulant factors, not metabolized=toxic effects
27
Warfarin Interactions | DECREASED
Phenobarbital Rifampin Phenytoin Carbamazepine *Anticoagulants and antiplatelets can have an added pharmacodynamic effect to increase rates of bleeding
28
Direct Thromin Inhibitors
MOA: - inhibit thrombin (IIa) to prevent conversion of fibrinogen to fibrin - binds directly to thrombin and inhibit conversion of Oral and IV available - Diabigatran (PO) - Argatroban (IV) - Bivalirudin (IV)
29
Dabigatran (Pradaxa)
Indications: - prophylaxis for non-valvular afib - Treatment of DVT/PE Rapid onset, prodrug converted by blood esterases Renally eliminated and dose adjusted for CKD (Cannot use in hemodialysis patients) Treat life threatening bleed with PRAXBIND (can remove drug with hemodialysis) -sequesters Dabigatran -give plasma or blood in addition if needed
30
Argatroban
Indications: -HIT treatment Metabolized by liver -dose adjustment needed for chronic liver disease Monitoring: aPTT Will artificially increase INR Adverse events: BLEEDING - no antidote - give plasma plus or minus blood if necessary
31
Bivalirudin
For patients going to the cath lab Eliminated by the kidneys -dose adjustment needed for renal dysfunction Monitoring: aPTT Adverse events: BLEEDING - no antidote - give plasma plus or minus blood if needed
32
Direct Xa Inhibitors
Bind directly to Xa and inhibit conversion of fibrinogen to fibrin No monitoring values Rapid onset Oral agents only - Rivaroxaban - Apixaban - Edoxaban - Betrixaban Antidote: Andexxa IF BLEEDING OCCURS HD does not remove drug Can give blood with or without plasma as needed
33
Apixaban (Eliquis)
Indications: - DVT/PE treatment - stroke prophylaxis in non-value afib - post op DVT prophylaxis Dose Adjustments -for afib, if 2 or 3 are met: Age>80, Scr>1.5, or Wt. <60kg Drug Interactions - strong CYP 3A4 - PGP inhibitors or inducers
34
Rivaroxaban (Xarelto)
Indications: - DVT/PE treatment - stoke prophylaxis in non-valve afib - post op DVT prophylaxis Dose Adjustments: -renal insufficiency Drug Interactions: - strong CYP 3A4 - PGP inhibitors or inducers
35
Edoxaban (Savaysa)
Indications: - DVT/PE treatment - stroke prophylaxis in non-valve afib Dose adjustments: -renal insufficiency Drug Interactions: - strong CYP3A4 - PGP inhibitors or inducers
36
Betrixaban (Bevyxxa)
Indications: -prophylaxis for VTE Dose adjustments: -renal insufficiency Drug Interactions: -strong PGP inhibitors
37
ANTIPLATELETS
Used to prevent arterial thrombosis by - cox inhibition - increased plasma adenosine - phosphodiesterase-3 (PDE-3) inhibition - P2Y12 ADP inhibition - glycoproteins IIb/IIIa inhibition *used to treat arterial clots rather than venous clots
38
COX Inhibitors
Cause irreversible inhibition cyclooxygenase 1 and 3 -enzyme responsible for making Throboxane A2 (TXA2) which causes platelets to aggregate Aspirin only medication in this class Effects last for duration of platelet (7-10 days) IRREVERSIBLE: Inhibits enzyme cyclooxygenase for its whole life -Aspirin (a cox inhibitor) binds to cycooxygenase 1 and 2 and prevents formation of thromboxane, platelets won’t clot=PREVENTS CLOTS
39
P2Y12 Inhibitors
Prevent platelet activation by inhibiting ADP binding to P2Y12 receptor Monitoring: platelet assay tests Irreversible and reversible REVERSIBLE: patient cannot stop taking the medication - decreases platelet stickiness and coagulation but has the reverse if the drug is not taken - beneficial for those who need to undergo heart/emergency surgery because the drug will wear off, if the bleeding occurs during surgery normal clotting will occur
40
Clopidogrel (Plavix)
Type of Inhibition: IRREVERSIBLE Prodrugs: Metabolized to active drug by CYP2C19 (genetic variance)
41
Clopidogrel Adverse Effects and Reversal
Bleeding Thrombocytopenia (TTP) No antidote to reverse -give platelets Many drug interactions with CYP2C19 -Genetic factors: poor metabolizes Hold 5 days prior to major surgery/procedure
42
Prasugrel (Effient)
Type of Inhibition: IRREVERSIBLE Prodrug converted by the liver No antidote Hold 5 days prior to surgery Avoid use in patients who are over 75, or have a history of stroke or TIA Dose adjust if patients weighs over 60
43
Prasugrel (Effient) Adverse effects and reversals
Bleeding, angioedma (rare) - avoid using in patients who are over 75 with a history of stroke or TIA - dose adjust if patient weights less than 60kg No antidote -give platelets or blood Hold 5 days prior to surgery
44
Tricagrelor (Brilinta)
Type of Inhibition: REVERSIBLE Significant drug interactions: aspirin, Digoxin, CYP3A4 inhibitors Don’t used if concerned about medication adherence Hold 1 day prior to surgery
45
Tricagrelor (Brilinta) Adverse Effects and Reversal
Adverse effects: - bleeding - dyspnea - ventricular pauses Sig. Drug Interactions: - aspirin dose >100mg/day , make the drug less effective - CYP3A4 inhibitors/inducers - do not exceed over 40mg a day of simvastatin or lovastatin - Digoxin levels may increase (PGP inhibitor) No antidote available -give platelets, wears off fathers Don’t use if concerned about medication adherence Hold 1 day prior to surgery
46
Cangrelor (Kengreal)
Type of inhibition: REVERSIBLE Adverse events: bleeding -treat with platelets or blood Same thing as Ticagrelor but IV form -only in IV formulation
47
GP IIB/IIIA Inhibitors
Block the final receptors where fibrinogen should bind to IV only Cause reversible blockade Available agents: Abciximab, Eptifbatide and Tirofiban Adverse events: bleeding - no antidote available - give platelets or blood
48
Dipyridamole
MOA: Inhibits platelets by increasing plasma levels of adenosine Always given in combo with aspirin (Aggrenox) Adverse effects: bleeding, dyspepsia No antidote available -give platelets or blood
49
Cilostazol (Pletal)
MOA: PDE-3 Inhibitor Full onset of action: 12 weeks -takes a while! Adverse effects: horrible headache Contraindication to use: patients with heart failure Drug interactions: Inhibitors of CYP3A4 No antidote -give platelets of blood Good for people with intermittent clot risks
50
Pentoxyifylline (Trental)
MOA: Increases cAMP in RBCs, leading to increased RBC flexibility and decreased Viscosity-less likely to clot Adverse Events: - nausea, vomiting, leukopenia - no sig. bleeding risk
51
THROMBOLYTICS
Given to remove thrombi that have already formed CLOT BUSTERS - these drugs augment plasminogen conversion to plasmin - plasmin degrades fibrin, breaks up the clot Used emergency Contraindications to using (relative and absolute) 3 formulations: - Alteplase (tPA) - Tenecteplase - Reteplase Example: have an MI, but don’t have access to a catheter lab, you would give a thrombolytic to break up the clot -used in rural areas
52
Alteplase (Activase or tPA)
MOA: binds with plasminogen to form an active complex - complex catalyze the conversion of other plasminogen molecules into plasminogen - digests the fibrin meshwork
53
Alteplase
Drug binds with plasminogen to form an active complex Ischemic stroke, MI, acute massive PE (cant get to cath lab in time) Adverse events: bleeding, angioedema (swelling of lips/tongue Reversal: -no antidote, give plasma or blood
54
Tenecteplase (TNkase)
Only indicated to treat a heart attack (AMI) -rural area, no access to cath lab Single dose Longer half life Adverse events: -bleeding Reversal: -no antidote, give plasma or blood
55
Reteplase (Retavase)
Only indicated to treat AMI Short half life -give 2 intermittent injections Complex dosing schedule, not as favorable as others Adverse events: -bleeding Reversal: -no antidote, give plasma or blood

Pharm 1 (4 decks)

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