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40 Cards in this Set
- Front
- Back
Adverse Events of IL-11
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- Tachycardia (19-30%)
- Atrial arrhythmias (60-75%) - Peripheral edema (60-75%) - Headache (41%) - Dizziness (38%) - Insomnia (33%) - Fatigue (30%) - Fever (35%) - Rash (25%) - Dyspnea (48%) |
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IL-11
Oprelvekin (Neumega) Activity |
- Promotes megakaryocyte production
- Prevents severe thrombocytopenia * This is not really used because you can just give platelet transfusions |
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Adverse Events of EPO
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- Hypertension (24%)
- Headache (16%) - increase tendency to clot vascular access - Iron deficiency anemia - Seizures - Achiness and cold sensation in long bones - Pyrexia (38% of AZT-treated patients) |
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Activity of EPO
Erythropoietin (Procrit/Epogen) |
Enhances RBC production (inc HCT)
Decreases need for RBC transfusions Patients should have Hgb < 10 g/dL or HCT < 30% Monitor iron stores Requires 2-6 weeks to see response |
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Darbopoietin (AraNesp)
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- Larger molecule with more carbohydrate groups to allow for slower elimination
- Dose: indicated 2.5 mcg/kg SQ weekly or 500 mcg SQ every 3 weeks - Should be used in patients receiving CHEMOTHERAPY with NO INTENT FOR CURE - New FDA guidelines state that all patients should receive medication guide prior to therapy |
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Hematopoietic Growth Factors
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Regulate hematopoiesis
- Proliferation - Differentiation - Maturation Effects of Colony Stimulating Factors on mature cells - Increase chemotaxis - Enhance phagocytosis - Increase cytotoxic killing - Improve responsiveness to antigens - Enhance eosinophil function |
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Activity of G-CSF
Filgrastim (Neupogen) |
- Supports proliferation of neutrophils
- Stimulates neutrophil function - No effect on mature eosinophils and macrophages |
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Filgrastim (Neupogen®)
Adverse Events |
* Bone Pain:
- Occurs in the lumbar, sternal and pelvic areas - Common during initiation of therapy and times of rapid growth - May reflect increased bone marrow activity - Pain responsive to acetaminophen or NSAIDs - Only attributable adverse event of G-CSF |
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Pegylated Filgrastim
(Neulasta) |
- larger chemical structure makes clearance slower and therefore allows administration once after chemotherapy
- Cleared by neutrophils, as the white blood cells recover |
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Activity of GM-CSF
Sargramostim (Leukine®) |
- Stimulates CFU-GM and CFU-GEMM to increase neutrophils, macrophages, monocytes, eosinophils
- No clinically significant activity on other cell lines (RBCs and platelets) |
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Sargramostim (Leukine®)
Adverse Events |
- Constitutional Symptoms
- Fever, headache, myalgias, arthralgias - Fever responds well to antipyretics - May have less fever with SQ administration - Bone pain - Skin reactions - Pleural and pericardial effusions - First-dose effect |
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Potential Mechanisms of CINV
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- Stimulation of chemoreceptor trigger zone (CTZ)
- Peripheral mechanisms - Cortical mechanisms - Vestibular mechanisms - Alterations of taste and smell |
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Central Mechanism
Proposed Pathophysiology of CINV |
- Chemotherapeutic agent activates the CTZ located in the area postrema in the brainstem
- Activated CTZ invokes release of various neurotransmitters, which activates brainstem vomiting center |
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Peripheral mechanism
Proposed Pathophysiology of CINV |
- Chemotherapeutic agent causes GI irritation and damage to GI mucosa, resulting in release of neurotransmitters (serotonin)
- Activated receptors mediated by vagal afferents send signals to brainstem vomiting center |
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Which Neurotransmitters respond will for acute CINV?
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- Serotonin
- Substance P |
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Which Neurotransmitters are good for delayed or rescuing N/V?
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- Dopamine
- Histamine - Acetylcholine |
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Serotonin (5HT3) Receptor Antagonists
Activity |
- Blocks serotonin both centrally and peripherally
- Effective for acute N/V but not any more effective for delayed N/V than other therapies - Most effective when given 30 minutes prior to administration of chemotherapy (PREVENTATIVE) - Increase efficacy when given with corticosteroids (administration with steroids increases efficacy from 60% to 90% |
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What is acute CINV?
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N/V within the 1st 24 hours after chemotherpy
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5HT3 Receptor Antagonists
Adverse Events |
- Headache (too little serotonin)
- Constipation - Diarrhea - EKG changes – concern only with underlying arrhythmias |
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Postfix = -setron
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5HT3 Receptor Antagonists
- - Ondasetron (Zofran) - Granisetron (Kytril) - Granisetron (Sancusco)... patch - Dolasetron (Anzemet) - Palonosetron (aloxi) |
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Neurokinin-1(NK-1) Receptor Antagonists
Activity |
- Inhibits Substance P
- Indicated for the prevention of acute and delayed CINV in combination with serotonin antagonists and corticosteroids |
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Aprepitant (Emend)
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- NK-1 Receptor Antagonists
- this is part of a combination therapy for those at severe risk for acute nausea/vomiting |
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Aprepitant (Emend)
Adverse Events |
- Asthenia/fatigue (18%)
- Nausea (13%) - Hiccups (11%) - Diarrhea (10%) - Somnolence |
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Drug Interactions with Emend
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- Decrease steroids by 50% IV, 25% po
- Use with caution when administering agents that are metabolized by CYP3A4 becuase it could increase the concentrations of other drugs |
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Dopamine Receptor Antagonists
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Phenothiazines
Butyrophenones Substituted benzamide |
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metoclopramide (Reglan®)
drug class |
Substituted benzamide
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droperidol (Inapsine®)
drug class |
Butyrophenones
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prochlorperazine (Compazine®)
promethazine (Phenergan®) drug class |
Phenothiazines
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Phenothiazines
Activity |
Effective for delayed nausea/vomiting
|
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Phenothiazines
Adverse Events |
- akathisia – lorazepam can help
- dystonia – diphenhydramine or benztropine can help - sedation – more common with promethazine |
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Which is more potent: Prochloperazine or Premethazine?
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Prochlorperazine is a more potent antiemetic in cancer patients but has a higher incidence of akathisia and dystonia
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Substituted Benzamides
Action |
Blocks dopamine in the CTZ and peripherally
- increases esophageal sphincter tone - improves gastric emptying - increases transit through small bowel |
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Substituted Benzamides
Adverse Events |
- Extrapyramidal Side Effects (EPS)
- restlessness - sedation - fatigue - nausea and diarrhea (dexamethasone may decrease diarrhea) |
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Benzodiazepines
Action |
- Used for anticipatory nausea
- Not effective for preventing emesis and is usually given with other antiemetics |
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Benzodiazepines
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- retrograde amnesic
- anxiolytic - sedative |
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Anticholinergics
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i.e. Scopolamine
- Beneficial for nausea associated with movement - side effects...no secretions |
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Cannabinoids
Dronabinol (Marinol) |
- Less effective than metoclopramide but more effective than phenothiazines
- Not effective with highly emetogenicity - Beneficial with younger patients - Significantly increases your appetite while decreases N/V |
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Cannabinoids
Dronabinol (Marinol) Adverse Events |
- mood changes
- dysphoria - memory loss - hallucinations - blurred vision - hypotension - tachycardia |
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Corticosteroids
Adverse events |
- mood changes
- anxiety - euphoria - headache - metallic taste - abdominal discomfort |
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Corticosteroids
Dexamethasone |
- Increases appetite, improve mood and sense of well being
- Immunosuppression - May increase the differentiation of WBC and therefore is not given in acute myelogenous leukemia (AML) |