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1 STEP Uworld coagulation > Parenteral anticoagulation (I/V) Amboss > Flashcards

Parenteral anticoagulation (I/V) Amboss Flashcards

1
Q

Unfractionated heparin (UFH). What drug?

A

Heparin

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2
Q

What is heparin administration for prophylaxis?

A

subcutaneous

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3
Q

What is heparin administration for therapeutic?

A

continuous intravenous infusion (therapeutic administration requires infusion pump)

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4
Q

Heparin monitoring?

A

aPTT and platelet count

including PLT baseline before treatment is started

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5
Q

Heparin clearance?

A

Clearance: hepatic (preferred agent for patients with renal insufficiency)

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6
Q

Heparin’s antidote?

A

Protamine sulfate

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7
Q

Charge of heparin?

A

negative

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8
Q

protamine sulfate charge?

A

positive

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9
Q

Why protamine sulfate binds heparin?

A

positively-charged protein that can neutralize negatively-charged heparin by forming inactive complexes

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10
Q

What drug is preferred for renal insufficiency?

A

Heparin - because its clearance is hepatic, not renal

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11
Q

What to monitor when use heparin in order to detect HIT?

A

platelets must be continuously monitored during heparin therapy and a baseline should be established before commencing treatment

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12
Q

Low molecular weight heparin (LMWH) drugs?

A

enoxaparin, dalteparin, tinzaparin, nadroparin, certoparin

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13
Q

LMWH. Administration?

A

Subcutaneous

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14
Q

LMWH. Monitoring?

A

Anti-factor Xa activity can be assessed in specific cases; not generally recommended –>
Only necessary in specific cases, e.g., patients with renal failure, underweight/overweight, as there is a risk of accumulation or underdosing. Anti-factor Xa activity needs to be checked 4 hours after administration (follow-up necessary as drug level is only consistent after several administrations)

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15
Q

LMWH. Clearance?

A

renal

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16
Q

Why LMWH not suitable in renal insufficiency?

A

Clearance: renal (contraindicated for patients with renal insufficiency)

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17
Q

LMWH antidote? What scope of reversal?

A

protamine sulfate (partial reversal –> Protamine antagonizes 50% of the effect of LMWH)

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18
Q

Synthetic heparin. What drug?

A

fondaparinux

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19
Q

Fondaparinux. Administration?

A

subcutaneous

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20
Q

Fondaparinux. Monitoring?

A

Same as heparin:
Not generally recommended;
Anti-factor Xa activity can be assessed in specific cases (Such cases include conditions with increased coagulability (e.g., chronic kidney disease, anemia, thrombocytopenia).

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21
Q

Fondaparinux. Antidote?

A

Possibly activated prothrombin complex concentrates (aPCC)

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22
Q

Heparinoid (glycosaminoglycan). What drug?

A

danaparoid

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23
Q

Heparinoid (glycosaminoglycan). All other same with administration and monitoring and antidote as in heparin/fondaparinux.

A

.

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24
Q

Direct thrombin inhibitors. Drugs?

A

I/v argatroban, bivalirudin, desirudin

p/o dabigatranas

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25
Direct thrombin inhibitors. Monitoring?
not recommended
26
Direct thrombin inhibitors. Antidote?
Possibly aPCC and/or antifibrinolytics (e.g., tranexamic acid) - if no reversal agent available Dabigatran: idarucizumab (monoclonal antibody)
27
Heparin mechanism?
Enhances the activity of antithrombin --> and it leads to decreased action of IIa and Xa. (IT'S INDIRECT INHIBITION!!!!! NES DIRECTLY AFFECT ANTITHROMBIN, NOT IIa and Xa).
28
Heparin mechanism. Xa inhibition?
antithrombin III potentiation → inhibition of factor Xa → decreased activation of prothrombin → ↓ thrombin→ ↓ fibrinogen activation → ↓ fibrin
29
Heparin mechanism. IIa inhibition?
Thrombin (factor IIa): UFH binds antithrombin III and thrombin simultaneously at two distinct binding sites → antithrombin III and thrombin held by heparin in close proximity (complex formation) → ↑ thrombin inhibition → ↓ fibrinogen activation → ↓ fibrin
30
Heparin half life?
SHORT - therefore anticoagulant effect quickly ceases once administration is stopped
31
LMWH mechanism?
LMWH: binds to antithrombin III → inhibition of factor Xa → decreased conversion of prothrombin → ↓ thrombin aka PREDOMINANTLY acts on Xa
32
Fondaparinux mechanism?
Only binds to antithrombin III → selective inhibition of factor Xa Aka acts only on Xa.
33
LMWH versus fondaparinux mechanism?
LMWH: PREDOMINANTLY acts on Xa Fondaparinux: ONLY on Xa
34
Heparin versus fondaparinux. Bioavailability?
Fondaparinux has better bioavailability than heparin
35
Heparin versus fondaparinux. Half life?
Fondaparinux has 2-4x longer half time than heparin. Heparin has short half life --> effec ceases quicly once administration is stopped.
36
Direct thrombin inhibitors. Mechanism?
Directly inhibit thrombin (freely circulating and in association with clots) Act independently from antithrombin
37
!!!!!!!The effect of most parenteral anticoagulants (except for direct thrombin inhibitors) depends on native antithrombin. In patients with antithrombin III deficiency (e.g., due to nephrotic syndrome), this effect is reduced.
.
38
If patient has nephrotic syndrome and reduced ATIII, what effect of parenteral anticoagulants?
effect is reduced LMWH, fondaparinux
39
pentasaccharide molecules. what is this anticoagulant?
fondaparinux, ie synthetic heparin
40
Parenteral anticoagulants. What main side effect?
Bleeding, drug interactions
41
Parenteral anticoagulants. | UFH and LMWH. What side effect?
Allergic reactions Heparin-induced thrombocytopenia: risk of type 2 HIT LMWH:UFH ≈ 1:10 Osteoporosis Drug interactions (e.g., ASA, tetracycline)
42
UFH and LMWH. Why is adverse osteoporosis?
Dose-dependent; therefore, switch to oral anticoagulants for long-term therapy. Osteoporosis is most likely related to increased osteoclastic activity, but decreased production of calcitriol is another potential cause
43
Parenteral anticoagulants. What main side effect? | Fondaparinux?
Occasionally low platelet count
44
Parenteral anticoagulants. What main side effect? | Heparinoid (glycosaminoglycan)
Asthma exacerbation (rarely)
45
Parenteral anticoagulants. What main side effect? | Direct thrombin inhibitors
Allergic reactions, fever
46
!!!!!Heparin treatment requires regular monitoring of the platelet count, especially for UFH, even before starting treatment.
.
47
Thrombocitopenia in anticoagulants?
Treatment with heparin, especially UFH, can cause thrombocytopenia. Thrombocytopenia may be immune-mediated heparin-induced thrombocytopenia (formerly known as type 2 HIT) or non-immune heparin associated thrombocytopenia (formerly known as type 1 HIT):
48
Immune HIT. type?
Type 2 HIT
49
Non-Immune HIT. type?
type 1 HIT
50
Indications. | LOW-dose heparin?
DVT prophylaxis for prolonged bedrest, peri- and postoperative state, immobility
51
Indications. | HIGH-dose heparin?
Immediate anticoagulation effect for: 1. Atrial fibrillation 2. DVT, acute arterial thrombosis, PE 3. Acute coronary syndrome, MI 4. Mechanical heart valve replacement 5. VTE prophylaxis for patients with hemodialysis, heart-lung machine, etc.
52
Indications. | Low molecular weight heparin?
Prophylaxis of DVT in orthopedic and abdominal surgery, prolonged immobility Treatment of DVT Acute coronary syndrome
53
Indications. | Direct thrombin inhibitors?
AF, VTE, Type 2 HIT
54
What anticoagulants have highest risk for HIT?
unfractionated heparin
55
Which type of HIT has worse prognosis?
type 2 HIT has a worse prognosis than type 1 HIT
56
What is BAD HIT?
Use direct thrombin inhibitors (Bivalirudin, Argatroban, Dabigatran) to treat the BAD HIT (heparin induced thrombocytopenia)
57
Contraindication for parenteral anticoagulants?
Recent stroke Uncontrolled hypertension Active bleeding HIT (except for direct thrombin inhibitors which can be used for anticoagulation in HIT)
58
HIT. What anticoagulants can be used?
direct thrombin inhibitors
59
Pregnancy and anticoagulations. Mechanism of hypercoagulability?
Physiological hypercoagulability (e.g., due to increased levels of clotting factors) leads to increased risk of thrombosis.
60
What anticoagulants can be used in pregnancy?
UFH and LMWH
61
Which anticoagulant has fewer side effects in comparison to other?
LMWH has fewer side effects.
62
Patients with decreased renal function. Which cannot be used and why?
In severe renal failure: accumulation of LMWH → increased bleeding risk → adjust dose or switch to UFH
63
Heparin Low-dose dosing frequency?
Low dose: subcutaneous administration every 8–12 hrs
64
Heparin High-dose dosing frequency?
High dose: intravenous administration with bolus and continuous application via infusion pump
65
LMWH dosing?
Dosage depends on specific drug used, indication, body weight, and kidney function; adjust to body weight and decreased kidney function.
66
Effect of LMWH lasts for about .........
Effect of LMWH lasts for about 12 hours
67
LMWH. Monitoring of anti-factor Xa is only necessary in patients with decreased kidney function (and significant over- or underweight); anti-factor Xa activity is measured 4 hrs after administration
.
68
Severe bleeding is more common in heparin or LMWH?
Heparin
69
HIT is more common in heparin of LMWH?
Type 2 HIT is about 10-fold more common
70
What to monitor if heparin is used therapeutically?
If used therapeutically, PTT levels have to be monitored frequently (target range: 1.5–2.5-fold prolongation)
71
In what CcCl is contraindicated LMWH?
Contraindicated if renal function is poor (CrCl < 30mL/min)
72
LMWH - No full antagonist available (only partial that binds 50proc)
.
73
When to use heparin?
Emergencies and renal failure
74
Patient has renal failure, what anticoagulant is used?
Heparin - for patients with advanced renal failure (e.g., in patients with severe renal insufficiency (CrCl < 30mL/min) or the elderly) LMWH - contraindicated in <30ml/min
75
LMWH use?
DVT prophylaxis, outpatient care (longer half-life → fewer injections) Generally preferred to UFH (fewer side effects, easier handling) as long as there are no contraindications

1 STEP Uworld coagulation (6 decks)

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