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rere_girl4ever
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Clopidogrel
MOA: Inhibit platelet aggregation by irreversibly blocking ADP receptors ⇒ prevent expression of glycoproteins IIb/IIIa on platelet surface.
- USE:
- 1. Unstable angina (aspirin + clopidogrel)
- 2. Ischemic stroke
- 3. Acute coronary syndrome
- 4. Coronary stenting
- There is ↓ incidence or recurrence of thrombotic stroke
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Prasugrel
MOA: Inhibit platelet aggregation by irreversibly blocking ADP receptors ⇒ prevent expression of glycoproteins IIb/IIIa on platelet surface.
- USE: Acute coronary syndrome, coronary stenting.
- There is ↓ incidence or recurrence of thrombotic stroke
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Ticagrelor
MOA: REVERSIBLY Inhibit platelet aggregation by irreversibly blocking ADP receptors ⇒ prevent expression of glycoproteins IIb/IIIa on platelet surface.
- USE: Acute coronary syndrome, coronary stenting.
- There is ↓ incidence or recurrence of thrombotic stroke
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Ticlopidine
MOA: Inhibit platelet aggregation by irreversibly blocking ADP receptors ⇒ prevent expression of glycoproteins IIb/IIIa on platelet surface.
- USE: Acute coronary syndrome, coronary stenting.
- There is ↓ incidence or recurrence of thrombotic stroke
- Toxicity: NEUTROPENIA (↓WBCs, fever, mouth ulcers)
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Cilostazol
MOA: Phosphodiesterase III inhibitor; ↑cAMP in platelets, resulting in i nhibition of platelet aggregation; arteriolar vasodilator
1. Intermittent claudication- 2. Coronary vasodilation
- 3. Prevention of stroke or transient ischemic attacks (combined with aspirin)
- 4. Angina prophylaxis
- SIDE EFFECTS: Nausea, headache, facial flushing, hypotension, abdominal pain.
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Dipyridamole
MOA: Phosphodiesterase III inhibitor; ↑cAMP in platelets, resulting in i nhibition of platelet aggregation; arteriolar vasodilator
1. Intermittent claudication- 2. Coronary vasodilation
- 3. Prevention of stroke or transient ischemic attacks (combined with aspirin)
- 4. Angina prophylaxis
- SIDE EFFECTS: Nausea, headache, facial flushing, hypotension, abdominal pain.
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Abciximab
- MOA: Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
- Abciximab is made from monoclonal antibody Fab fragments.
- USE:
- 1. Unstable angina
- 2. Percutaneous transluminal coronary angioplasty
SIDE EFFECTS: Bleeding, thrombocytopenia
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Eptifibatide
MOA: Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
- USE:
- 1. Unstable angina
- 2. Percutaneous transluminal coronary angioplasty
SIDE EFFECTS: Bleeding, thrombocytopenia
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Tirofiban
MOA: Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
- USE:
- 1. Unstable angina
- 2. Percutaneous transluminal coronary angioplasty
SIDE EFFECTS: Bleeding, thrombocytopenia
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Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
- Abciximab
- Eptifibatide
- Tirofiban
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Phosphodiesterase III inhibitor; ↑cAMP in platelets, resulting in inhibition of platelet aggregation; arteriolar vasodilator
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Inhibit platelet aggregation by irreversibly blocking ADP receptors. Prevent expression of glycoproteins IIb/IIIa on platelet surface.
- Clopidogrel
- Prasugrel
- Ticagrelor (reversible)
- Ticlopidine
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Azathioprine
- Purine (thiol) analog → ↓de novo purine synthesis.
- Activated by HGPRT.
Azathioprine is metabolized into 6 -MP.
- USE:
- 1. Preventing organ rejection
- 2. Rheumatoid arthritis
- 3. IBD especially Chrons
- 4. SLE
- 5. Used to wean patients off steroids in chronic disease and to treat steroid-refractory chronic disease.
- SIDE EFFECTS:
- 1. Myelosuppression
- 2. GI
- 3. Liver (abdominal pain, jaundice).
Azathioprine and 6-MP are metabolized by xanthine oxidase; thus both have ↑toxicity with allopurinol or febuxostat.
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6-thioguanine
- Purine (thiol) analog → ↓de novo purine synthesis.
- Activated by HGPRT.
- USE:
- 1. Preventing organ rejection
- 2. Rheumatoid arthritis
- 3. IBD
- 4. SLE
- 5. Used to wean patients off steroids in chronic disease and to treat steroid-refractory chronic disease.
- SIDE EFFECTS:
- 1. Myelosuppression
- 2. GI
- 3. Liver (abdominal pain, jaundice).
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Cladribine (2-CDA)
Purine analog
- MOA:
- 1. Inhibition of DNA polymerase
- 2. DNA strand breaks
- 3. Resistant to degradation by adenosine deaminase
USE: Hairy cell leukemia
- TOXICITY:
- Myelo
- Nephro
- Neuro
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Cytarabine (arabinofuranosyl cytidine)
Pyrimidine analog
MOA: Inhibition of DNA polymerase
USE: Leukemias (AML), lymphomas.
SIDE EFECTS: Leukopenia, thrombocytopenia, megaloblastic anemia.
CYTarabine causes panCYTopenia.
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Arabinofuranosyl cytidine
- CYTARABINE
- Pyrimidine analog
MOA: Inhibition of DNA polymerase
USE: Leukemias ( AML), lymphomas.
SIDE EFECTS: Leukopenia, thrombocytopenia, megaloblastic anemia.
CYTarabine causes panCYTopenia.
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5-fluorouracil (5-FU)
- Pyrimidine analog
- Bioactivated to 5F-dUMP, which covalently complexes folic acid → complex inhibits thymidylate synthase → ↓ dTMP → ↓DNA synthesis.
USE: Colon cancer, pancreatic cancer, basal cell carcinoma (topical).
- SIDE EFFECTS:
- Myelosuppression, which is not reversible with leucovorin (folinic acid).
- Photosensitivity
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