Drugs Flashcards

1
Q

Heparin
Mechanism
Toxicity
Types

A

Mechanism
Binds antithrombin so it can inhibit II and X

Toxicity
Bleeding
Osteoporosis
Heparin Induced TCP (Ab binds heparin/PF4 complex) –> thrombosis.

Reverse with protamine sulfate

Types
Low molecular weight (mostly 10) - subQ and not easily reversible
Unfractionated (mostly 2) - IV and reversible

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2
Q

Argatrobran and Bivalirudin
Mechanism
Uses

A

Mechanism
Blocks Factor II (thrombin)

Uses
Heparin Induced TCP

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3
Q

Warfarin (Coumadin)
Mechanism
Uses
Toxicity

A

Mechanism
Inhibits Vitamin K Epoxide Reductase so Vitamin K cannot be regenerated to y carboxylate 2, 7, 9, 10 C and S. (Metabolized by p450).

Uses
Anticoagulation but not in pregnancy.

Toxicity
Bleeding
Teratogenic
Warfarin Induced Skin Necrosis (Protein C deficiency)
Reverse with fresh frozen plasma and Vitamin K

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4
Q

Apixaban and Rivaroxaban
Mechanism
Uses
Toxicity

A

Mechanism
Inhibit Factor X (like FondaparineuX)

Uses
Anticoagulation and does not require monitoring when taken orally.

Toxicity
Bleeding without a reversal agent.

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5
Q
Thrombolytics
Name 
Mechanism
Use
Toxicity
A

Name
Alteplase, reteplase, teneteplase

Mechanism
TPA which convert plasminogen to plasmin

Use
To lyse clots in PE, MI, Stroke etc.

Toxicity
Bleeding (never in active bleeding, recent surgery or severe hypertension)
Reverse with aminocaproic acid (inhibits fibrinolysis) and administer cryoprecipitate.

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6
Q

Aspirin
Mechanism
Use
Toxicity

A
Mechanism
Blocks COX (covalent acetylation) which prevents TXA2 and PGs from being released by platelets to promote 2nd wave of aggregation.
Use
Antiplatelet
Antipyretic
Antiinflammatory
Analgesic

Toxicity

1) Renal failure and necrosis
2) GI ulceration and bleeding
3) Reye syndrome in kids with viral syndrome
4) Respiratory and metabolic alkalosis

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7
Q
ADP receptor inhibitors
Name
Mechanism
Use
Toxicity
A

Name
Clopidogrel, Prasugrel, Ticagrelor, Ticlopidine

Mechanism
Blocks ADP receptor (PSY12) for platelets, which cross links fibrinogen.

Use
Anti-platelet.
MI , stents, strokes.

Toxicity
Ticlopidine - neutropenia.
TTP/HUS may be seen

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8
Q

Cilostazol and Dipyridamole
Mechanism
Use
Toxicity

A

Mechanism
PDEIII inhibitor. Prevent platelets from making cAMP and aggregating. Vasodilates.

Use
Claudication, TIA, angina, stroke prevention.

Toxicity
Facial flushing, hypotension.

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9
Q
GPIIbIIIa inhibitors
Name
Mechanism
Use
Toxicity
A

Name
Abciximab, eptifibatide, tirofiban

Mechanism
GPIIbIIIa inhibitors, prevent platelet aggregation.

Use
Unstable angina, PCI.

Toxicity
Bleeding, thrombocytopenia.

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10
Q

Cell cycle drugs

A

M - Vina alkaloids and taxols
S - Antimetabolites
S and G2 - Etoposide
G2 - Bleomycin

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11
Q

What drugs inhibit nucleotide synthesis?

A

5-FU and MTX
Inhibit thymidine

6-MCP
Inhibit Purine

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12
Q

What drugs inhibit DNA replication?

A

1) Cross link DNA
Alkylating agents and Cisplatin

2) DNA intercalators
Dactinomycin and doxorubicin

3) Inhibit topoisomerase
Etoposide

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13
Q

What drugs inhibit cell division?

A

1) Inhibit microtubule formation
Vinka alkaloids

2) Inhibit microtubule disassembly
Paclitaxel

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14
Q

Methotrexate
Mechanism
Use
Toxicity

A
Mechanism
Inhibit DHFR (folate analogue) which inhibits dTMP synthesis

Use
Cancer, abortion, RA, psoriasis and IBD

Toxicity - 3Ms

1) Myelosuppression reversible with leucovorin rescue
2) Mucositis
3) Macrovesicular fatty change in liver

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15
Q

5FU
Mechanism
Use
Toxicity

A

Mechanism
Pyrimidine analogue which blocks thymidilate synthase and inhibits dTMP synthesis

Use
Cancer (colon, pancreas, basal cell)

Toxicity
Photosensitive (Fotosensitive FU)
Myelosuppression (can’t use leucovorin)
Overdose reversal: Uridine

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16
Q

Cytarabine (arabinofuranosyl cytidine)
Mechanism
Use
Toxicity

A

Mechanism
Pyrimidine analogue which inhibits DNA polymerase

Use
Leukemia and lymphoma

Toxicity
Pancytopenia (Cytapenia)

17
Q
Azathioprine
6-MP
6-thioguanine
Mechanism
Use 
Toxicity
A

Mechanism
Purine analogues which block de novo purine synthesis (activated by HGPRT)

Use
Azathioprine (organ rejection, RA, SLE)
6-MP and 6-thioguanine (Leukemia, IBD)

Toxicity
Allopurinol increases toxicity (bc xanthine oxidase cannot break down Azathioprine
and 6-MP)
Also bone marrow, liver, GI tract.

18
Q

Dactinomycin (actinomycin D)
Mechanism
Use
Toxicity

A

Mechanism
DNA intercalator

Use
Childhood tumors (children ACT out) Wilm's, Ewing, Rhadbomyosarcoma

Toxicity
Myelosuppression