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Fitzpatrick's Dermatology, 9th Edition (Entrance Exam / Board Exam Prep) > 195: Antiangiogenic Agents > Flashcards

195: Antiangiogenic Agents Flashcards

1
Q

What is the mechanism of action of BECAPLERMIN (REGRANEX)?

A

BECAPLERMIN (REGRANEX) is an FDA-approved angiogenesis-stimulating therapy that utilizes endogenous platelet-derived growth factor (PDGF), which is chemotactic for several cell types necessary for wound healing and acts as a mitogen for fibroblasts, aiding in the formation of granulation tissue.

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2
Q

What are the indications for using BEVACIZUMAB (AVASTIN)?

A

BEVACIZUMAB (AVASTIN) is indicated for the first-line treatment of metastatic colorectal carcinoma in combination with intravenous 5-fluorouracil-based chemotherapy, as well as for non-small-cell lung cancer, cervical cancer (including metastatic), glioblastoma, ovarian cancer, and several other cancers.

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3
Q

What are the contraindications for BECAPLERMIN (REGRANEX)?

A

The contraindications for BECAPLERMIN (REGRANEX) include known cancer within the treatment area and a history of hypersensitivity.

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4
Q

What are the risks and precautions associated with BECAPLERMIN (REGRANEX)?

A

Risks and precautions for BECAPLERMIN (REGRANEX) include: Increased rate of mortality due to malignancy in patients treated with 3 or more tubes. Pregnancy category: C. Safety and efficacy have not been evaluated in children younger than 16 years of age.

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5
Q

What complications are associated with BEVACIZUMAB (AVASTIN)?

A

Complications associated with BEVACIZUMAB (AVASTIN) include: GI perforation with associated intraabdominal abscess or fistula formation, serious hemorrhagic events such as hemoptysis, GI bleeding, and pulmonary hemorrhage, arterial thromboembolic events, including cerebral infarction and myocardial infarction, hypertension, and proteinuria.

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6
Q

What precautions should be taken during the application of BECAPLERMIN (REGRANEX)?

A

Precautions include ensuring the wound is adequately vascularized and reaches at least the level of subcutaneous tissue. The gel should not be applied to wounds closed by primary intention. The area should be covered with a saline-moistened dressing for 12 hours after application. Dosing should be recalculated every 1-2 weeks as the wound changes size. Treatment should be reevaluated if there is less than a 30% decrease in size after 10 weeks or if the wound has not completely healed after 20 weeks.

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7
Q

What are the potential risks of BEVACIZUMAB (AVASTIN) therapy in glioblastoma patients?

A

Risks include GI perforation, wound dehiscence, serious hemorrhagic events, arterial thromboembolic events, reversible posterior leukoencephalopathy syndrome, hypertension, proteinuria, and infusion reactions.

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8
Q

What are the potential thromboembolic risks for patients with metastatic colorectal carcinoma treated with BEVACIZUMAB (AVASTIN)?

A

Potential risks include arterial thromboembolic events such as cerebral infarction, transient ischemic attacks, myocardial infarction, and angina.

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9
Q

What is the dosing regimen for BECAPLERMIN (REGRANEX)?

A

The dosing regimen for BECAPLERMIN (REGRANEX) is to apply it once daily, with the amount depending on the size of the lesion. Each square inch of ulcer requires two-thirds of an inch of gel from a 15-g tube or one-and-one-third inches from a 2-g tube, covered with a saline-moistened dressing for approximately 12 hours.

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10
Q

What monitoring therapy is recommended for BECAPLERMIN (REGRANEX)?

A

Monitoring therapy for BECAPLERMIN (REGRANEX) should include evaluating the wound size. If there is less than a 30% decrease in size after 10 weeks or if the wound has not completely healed after 20 weeks, the treatment plan should be reevaluated.

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11
Q

What complications can arise from the use of BECAPLERMIN (REGRANEX)?

A

Complications from BECAPLERMIN (REGRANEX) may include: Rash, hypersensitivity reactions, and ulcer-related complications.

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12
Q

What is the mechanism of action of BEVACIZUMAB (AVASTIN)?

A

BEVACIZUMAB (AVASTIN) is a recombinant, humanized immunoglobulin G1 monoclonal antibody that targets vascular endothelial growth factor (VEGF), inhibiting angiogenesis.

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13
Q

What are the contraindications for BEVACIZUMAB (AVASTIN)?

A

The primary contraindication for BEVACIZUMAB (AVASTIN) is hypersensitivity to the drug.

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14
Q

What are the potential complications associated with BEVACIZUMAB (AVASTIN)?

A

Complications associated with BEVACIZUMAB (AVASTIN) include: GI perforation with associated intraabdominal abscess or fistula formation, wound dehiscence, serious hemorrhagic events including hemoptysis, GI bleeding, CNS hemorrhaging, epistaxis, vaginal bleeding, and pulmonary hemorrhage, arterial thromboembolic events, including cerebral infarction and myocardial infarction, reversible posterior leukoencephalopathy syndrome, hypertension, proteinuria, and infusion reactions.

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15
Q

What is the dosing regimen for BEVACIZUMAB (AVASTIN)?

A

The dosing regimen for BEVACIZUMAB (AVASTIN) is not specified in the provided content, but it is typically administered as an intravenous infusion based on the specific treatment protocol for the cancer being treated.

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16
Q

What monitoring is required for patients receiving BEVACIZUMAB (AVASTIN)?

A

Monitoring for patients receiving BEVACIZUMAB (AVASTIN) should include assessing for signs of hemorrhagic events, thromboembolic events, and hypertension as well as monitoring for any infusion reactions.

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17
Q

What are the indications for using BECAPLERMIN (REGRANEX)?

A

BECAPLERMIN (REGRANEX) is indicated for the treatment of lower extremity, diabetic, neuropathic ulcers that must be adequately vascularized and reach to at least the level of subcutaneous tissue, particularly in the treatment of diabetic foot ulcers.

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18
Q

What are the risks associated with BEVACIZUMAB (AVASTIN)?

A

Risks associated with BEVACIZUMAB (AVASTIN) include serious hemorrhagic events, thromboembolic events, and potential for GI perforation. Close monitoring is required to manage these risks effectively.

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19
Q

How does the mechanism of action of BECAPLERMIN (REGRANEX) contribute to wound healing?

A

The mechanism of action of BECAPLERMIN (REGRANEX) involves promoting angiogenesis and granulation tissue formation through its action as a platelet-derived growth factor (PDGF), which is essential for wound healing processes.

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20
Q

What is the significance of monitoring therapy for BECAPLERMIN (REGRANEX) in clinical practice?

A

Monitoring therapy for BECAPLERMIN (REGRANEX) is significant because it helps to ensure that the treatment is effective, as indicated by a decrease in wound size, and allows for timely adjustments to the treatment plan if healing is not progressing as expected.

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21
Q

What are the implications of hypersensitivity reactions in patients treated with BEVACIZUMAB (AVASTIN)?

A

Hypersensitivity reactions in patients treated with BEVACIZUMAB (AVASTIN) can lead to serious complications, necessitating immediate medical attention and potential discontinuation of the drug, highlighting the importance of monitoring for such reactions during treatment.

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22
Q

What is the role of BEVACIZUMAB (AVASTIN) in cancer treatment?

A

BEVACIZUMAB (AVASTIN) plays a critical role in cancer treatment by inhibiting angiogenesis, thereby limiting the blood supply to tumors and enhancing the effectiveness of chemotherapy in various cancers, including colorectal and lung cancers.

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23
Q

What are the clinical implications of the increased mortality risk associated with BECAPLERMIN (REGRANEX)?

A

The increased mortality risk associated with BECAPLERMIN (REGRANEX) in patients with malignancy underscores the need for careful patient selection and monitoring, particularly in those receiving multiple tubes of the gel, to mitigate potential adverse outcomes.

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24
Q

How does the dosing regimen for BECAPLERMIN (REGRANEX) adapt to changes in wound size?

A

The dosing regimen for BECAPLERMIN (REGRANEX) adapts to changes in wound size by requiring recalculation of the gel dosage every 1 to 2 weeks to ensure accurate dosing as the wound heals and changes in size.

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25
What are the potential side effects of BEVACIZUMAB (AVASTIN) that healthcare providers should monitor?
Healthcare providers should monitor for potential side effects of BEVACIZUMAB (AVASTIN) including hypertension, proteinuria, and serious hemorrhagic events, as these can significantly impact patient safety and treatment outcomes.
26
What is the importance of understanding the contraindications for BECAPLERMIN (REGRANEX) in clinical practice?
Understanding the contraindications for BECAPLERMIN (REGRANEX) is crucial in clinical practice to prevent adverse effects, particularly in patients with known malignancies or hypersensitivity, ensuring safe and effective treatment.
27
What are the implications of the pregnancy category C classification for BECAPLERMIN (REGRANEX)?
The pregnancy category C classification for BECAPLERMIN (REGRANEX) implies that the drug should be used with caution in pregnant women, as its safety has not been established, necessitating a risk-benefit analysis before use.
28
What is the significance of the FDA approval of BEVACIZUMAB (AVASTIN) as the first antiangiogenesis drug?
The FDA approval of BEVACIZUMAB (AVASTIN) as the first antiangiogenesis drug marks a significant advancement in cancer treatment, providing a new therapeutic option that targets tumor blood supply and enhances the efficacy of existing chemotherapy regimens.
29
How does the mechanism of action of BEVACIZUMAB (AVASTIN) differ from that of BECAPLERMIN (REGRANEX)?
The mechanism of action of BEVACIZUMAB (AVASTIN) involves inhibition of vascular endothelial growth factor (VEGF) to prevent angiogenesis, while BECAPLERMIN (REGRANEX) promotes wound healing through stimulation of platelet-derived growth factor (PDGF), highlighting their distinct roles in therapy.
30
What are the clinical considerations for using BECAPLERMIN (REGRANEX) in diabetic foot ulcers?
Clinical considerations for using BECAPLERMIN (REGRANEX) in diabetic foot ulcers include ensuring the ulcer is adequately vascularized, monitoring for hypersensitivity reactions, and evaluating the wound's healing progress to adjust treatment as necessary.
31
What are the potential consequences of not monitoring patients on BEVACIZUMAB (AVASTIN) for thromboembolic events?
Not monitoring patients on BEVACIZUMAB (AVASTIN) for thromboembolic events can lead to serious complications such as cerebral infarction or myocardial infarction, which can be life-threatening and significantly impact patient outcomes.
32
What is the rationale behind the dosing adjustments for BECAPLERMIN (REGRANEX) based on wound size?
The rationale behind dosing adjustments for BECAPLERMIN (REGRANEX) based on wound size is to ensure that the treatment is effective and that the appropriate amount of gel is applied to facilitate optimal healing as the wound changes in size.
33
What are the implications of the hypersensitivity contraindication for BEVACIZUMAB (AVASTIN) in patient management?
The hypersensitivity contraindication for BEVACIZUMAB (AVASTIN) necessitates thorough patient history assessments and monitoring for allergic reactions during treatment, ensuring patient safety and effective management of potential adverse effects.
34
What is the mechanism of action of BORTEZOMIB and its clinical applications?
Bortezomib is a proteasome inhibitor that impairs the ability of the proteasome to degrade ubiquitinated proteins and inhibits angiogenesis mediated by mesenchymal stem cells. It is used for the treatment of recurrent or refractory multiple myeloma and mantle cell lymphoma. Good results can be obtained when combined with bevacizumab to treat temozolomide-resistant malignant gliomas.
35
What are the uses and potential side effects of CETUXIMAB?
CETUXIMAB is a chimeric monoclonal antibody that targets the epithelial growth factor receptor (EGFR). It is used in the treatment of metastatic colorectal carcinoma and squamous cell carcinoma of the head and neck, either alone or in combination with radiation or chemotherapy. Serious infusion reactions, acneiform neutrophilic folliculitis, pruritus, electrolyte disturbances, abdominal pain, and infections associated with neutropenia.
36
What is the role of corticosteroids in angiogenesis?
Corticosteroids have a mixed role in angiogenesis, exhibiting neutral, antiangiogenic, and proangiogenic effects in various cases. Their clinical usefulness as anti-inflammatory and antiangiogenic agents is evident, although the ultimate mechanism and role are still being studied.
37
What are the potential side effects of treatment for carcinoma of the head and neck?
Serious infusion reactions, acneiform neutrophilic folliculitis, pruritus, electrolyte disturbances, abdominal pain, and infections associated with neutropenia.
38
What is the role of corticosteroids in angiogenesis?
Corticosteroids have a mixed role in angiogenesis, exhibiting neutral, antiangiogenic, and proangiogenic effects in various cases.
39
What is the indication for ERLOTINIB?
ERLOTINIB is a small-molecule phosphorylation inhibitor that specifically inhibits the EGFR tyrosine kinase, primarily used for the treatment of non-small-cell lung cancer and pancreatic cancer.
40
What are the side effects of ERLOTINIB?
Hypersensitivity, acneiform rash, gastrointestinal upset, and interactions with CYP450, CYP1A2, and CYP3A4 drug metabolism.
41
What are the clinical applications of EVEROLIMUS?
EVEROLIMUS is an mTOR inhibitor used for the treatment of advanced renal cell carcinoma after failure of sunitinib or sorafenib, and as an agent in drug-eluting stents.
42
What are the side effects of EVEROLIMUS?
Noninfectious pneumonitis, susceptibility to infections, oral ulceration and mucositis, blood dyscrasias, and musculoskeletal pain.
43
What are the potential adverse effects of bortezomib?
Hypotension, peripheral neuropathy, acute respiratory distress syndrome, blood dyscrasias (e.g., neutropenia, thrombocytopenia), fatigue, skin rash, and CYP3A4 drug metabolism interactions.
44
What dermatologic side effects might indicate a positive clinical response to cetuximab?
The appearance of acneiform neutrophilic folliculitis correlates with a positive clinical response.
45
What are the potential pulmonary and oral complications of everolimus?
Potential complications include noninfectious pneumonitis, oral ulceration, and mucositis.
46
What are the potential infusion-related complications of cetuximab?
Potential complications include serious infusion reactions, pruritus, and infections associated with neutropenia.
47
What is the mechanism of action of Bortezomib?
Bortezomib is the first proteasome inhibitor to gain FDA approval. It acts by impairing the ability of the proteasome to degrade a variety of ubiquitinated proteins.
48
What are the potential side effects associated with Cetuximab treatment?
Cetuximab can cause serious infusion reactions, acneiform neutrophilic folliculitis, pruritus, electrolyte disturbances, abdominal pain and upset, and infections associated with neutropenia.
49
How do corticosteroids influence angiogenesis?
Corticosteroids have a mixed role in angiogenesis, exhibiting neutral, antiangiogenic, and proangiogenic effects.
50
What is the role of Erlotinib in cancer treatment?
Erlotinib is a small-molecule phosphorylation inhibitor that specifically inhibits the EGFR tyrosine kinase.
51
What are the clinical applications of Everolimus?
Everolimus is an mTOR inhibitor used in the treatment of advanced renal cell carcinoma after failure of sunitinib or sorafenib, and as an agent in drug-eluting stents.
52
What is the mechanism of action of Imiquimod?
Imiquimod acts by inducing the activation of toll-like receptor 7 in immune cells, which downregulates proangiogenic factors.
53
What are the primary indications for Imiquimod in dermatology?
Imiquimod is indicated for the treatment of clinically typical, nonhyperkeratotic actinic keratosis, superficial basal cell carcinoma, and external genital and perianal condyloma acuminata.
54
What are the common local skin toxicities associated with Imiquimod treatment?
Common local skin toxicities include erythema, flaking/scaling/dryness, scabbing/crusting, induration, edema, erosion/ulceration, vesicles, and weeping or exudates.
55
What precautions should patients take while using Imiquimod?
Patients should avoid or minimize exposure to sunlight and wash the treated area after application.
56
What is the pharmacokinetics of Imiquimod regarding absorption?
Imiquimod is only minimally absorbed transdermally, with less than 0.9% of the topical dose being excreted in the urine or feces.
57
What is the recommended application regimen for actinic keratosis with Imiquimod?
Apply BID 2x/week to the face or scalp, preferably before sleeping, and wash the area after 8 hours.
58
Are erythema and flaking expected side effects of Imiquimod?
Yes, erythema and flaking/scaling/dryness are common local skin toxicities associated with Imiquimod.
59
What is the recommended application regimen for basal cell carcinoma with Imiquimod?
Apply the cream 5x/week plus 1 cm around the lesion, preferably before sleeping.
60
What are the potential systemic side effects of Imiquimod treatment?
Potential systemic side effects may include immunosuppression, upper respiratory tract infection, coughing, sinusitis, musculoskeletal pain, headache, and GI upset.
61
What is the pregnancy classification of Imiquimod?
Imiquimod is classified as Pregnancy class C, indicating that risk cannot be ruled out.
62
What is the recommended treatment duration for external genital and perianal condyloma acuminata with Imiquimod?
For external genital and perianal condyloma acuminata, apply 3x/week until lesions resolve or for a maximum of 16 weeks.
63
What are the primary uses of INTERFERON_2b_INTRON A?
Chronic hepatitis B and C, AIDS-associated Kaposi sarcoma, condylomata acuminata, malignant melanoma, hairy cell leukemia, follicular lymphoma.
64
What are the potential side effects of PANITUMUMAB_VECTIBIX?
Hypersensitivity, severe dermatologic toxicities, photosensitivity, pulmonary fibrosis, electrolyte disturbances, infusion reactions.
65
What is the mechanism of action of PEGAPTANIB_MACUGEN?
PEGAPTANIB is a short peptide strand directed against a specific isomer of secreted VEGF, namely, VEGF165.
66
What are the indications for PROPRANOLOL_HEMANGEOL?
Treatment of hemangioma by blocking both β1- and β2- adrenergic receptors in hemangioma endothelial cells.
67
What are the severe dermatologic toxicities to monitor in a patient treated with panitumumab?
Severe dermatologic toxicities include acneiform dermatitis, pruritus, erythema, rash, skin exfoliation, paronychia, dry skin, and skin fissures.
68
What are the potential ocular risks of pegaptanib treatment?
Potential ocular risks include endophthalmitis, retinal detachment, and traumatic cataract formation.
69
What are the contraindications for using INTERFERON_2b_INTRON A?
Hypersensitivity to IFN, autoimmune hepatitis, renal insufficiency, and combination therapy in pregnancy.
70
What are the potential side effects of INTERFERON_2b_INTRON A?
Flu-like symptoms, depression, sarcoidosis, and spastic diplegia.
71
What is the mechanism of action of PANITUMUMAB_VECTIBIX?
It is an entirely human monoclonal antibody directed against EGFR, used for treating progressing, metastatic colorectal carcinoma.
72
What are the common side effects associated with PANITUMUMAB_VECTIBIX?
Hypersensitivity reactions, severe dermatologic toxicities, photosensitivity, pulmonary fibrosis, electrolyte disturbances, infusion reactions.
73
What is ITUMUMAB VECTIBIX?
It is an entirely human monoclonal antibody directed against EGFR, used for treating progressing, metastatic colorectal carcinoma in combination with or as a single agent following chemotherapy.
74
What are the common side effects associated with PANITUMUMAB VECTIBIX?
- Hypersensitivity reactions - Severe dermatologic toxicities (acneiform dermatitis, pruritus, erythema, rash, skin exfoliation) - Photosensitivity - Pulmonary fibrosis - Electrolyte disturbances - Infusion reactions
75
What is PEGAPTANIB MACUGEN primarily used for?
It is used for the treatment of neovascular, or wet, age-related macular degeneration.
76
What are the potential side effects of PEGAPTANIB MACUGEN?
- Ocular or periocular infection - Endophthalmitis - Retinal detachment - Traumatic cataract formation associated with intravitreal administration - Hypertension - Dizziness, headache, and vertigo
77
What is the role of PROPRANOLOL HEMANGEOL in treating hemangiomas?
It works by blocking both β1- and β2-adrenergic receptors in hemangioma endothelial cells, reducing levels without transactivating VEGF-2 signaling.
78
What are the contraindications for using PROPRANOLOL HEMANGEOL?
- Tremors - Angina - Hypertension - Heart rhythm disorders
79
What are the common side effects of PROPRANOLOL HEMANGEOL?
- Muscle disorder - Bronchitis, emphysema, or other breathing disorders - Low blood glucose or diabetes - Slow heartbeats, low blood pressure - Nausea, vomiting, diarrhea, constipation, or stomach cramps - Decreased sex drive, impotence, or difficulty having an orgasm - Sleep problems (insomnia)
80
What is the mechanism of action of RANIBIZUMAB (LUCENTIS)?
RANIBIZUMAB is an antibody fragment related to bevacizumab that competitively binds to VEGF and inhibits its interactions with VEGFR-1 and VEGFR-2, blocking endothelial proliferation and survival.
81
What are the primary indications for the use of SIROLIMUS (RAPAMUNE)?
SIROLIMUS is indicated for off-label uses in dermatology, including the treatment of psoriasis, Kaposi sarcoma, tuberous sclerosis, and angiofibromatosis, as well as for nephrogenic systemic fibrosis, scleroderma, and dermatomyositis.
82
What are the common side effects associated with SORAFENIB (NEXAVAR)?
Common side effects of SORAFENIB include dermatologic toxicities (rash, hand-foot syndrome, alopecia, pruritus), multiple blood dyscrasias, hypertension, cardiac ischemia, gastrointestinal upset, and nephrotic syndrome.
83
What are the clinical applications of RANIBIZUMAB (LUCENTIS)?
RANIBIZUMAB is used for the treatment of patients with neovascular or wet age-related macular degeneration, diabetic retinopathy, macular edema, and choroidal neovascularization secondary to pathologic myopia.
84
What are the systemic toxicities associated with SIROLIMUS (RAPAMUNE)?
Systemic toxicities of SIROLIMUS include cutaneous toxicities such as angioedema, leukocytoclastic vasculitis, xerosis, and aphthous ulceration, which resolve with discontinuation of therapy, along with increased susceptibility to infections and malignancies.
85
What are the potential dermatologic toxicities and systemic risks of SORAFENIB?
Dermatologic toxicities include rash, hand-foot syndrome, alopecia, and pruritus. Systemic risks include hypertension, cardiac ischemia, GI upset, CYP2B6, CYP2C8, and CYP3A4 drug metabolism interactions, and nephrotic syndrome.
86
What are the potential ocular complications of RANIBIZUMAB?
Potential ocular complications include endophthalmitis, retinal detachment, and an increase in intraocular pressures.
87
What are the contraindications and potential side effects of PROPRANOLOL in infants?
Contraindications include asthma, Raynaud syndrome, pheochromocytoma, and hypoglycemia. Potential side effects include angina, hypertension, heart rhythm disorders, nausea, vomiting, diarrhea, and sleep problems.
88
What are the potential cutaneous toxicities of SIROLIMUS?
Cutaneous toxicities include angioedema, leukocytoclastic vasculitis, xerosis, and aphthous ulceration.
89
What are the potential blood-related complications of SORAFENIB?
Potential complications include multiple blood dyscrasias.
90
What are the potential dermatologic complications of SORAFENIB?
Potential complications include rash, hand-foot syndrome, alopecia, and pruritus.
91
What is the mechanism of action of RANIBIZUMAB and its clinical applications?
RANIBIZUMAB is an antibody fragment related to bevacizumab that competitively binds VEGF and inhibits its interactions with VEGFR-1 and VEGFR-2. It is used in the treatment of neovascular or wet age-related macular degeneration, diabetic retinopathy, macular edema, and choroidal neovascularization secondary to pathologic myopia.
92
What are the off-label uses of SIROLIMUS and its mechanism of action?
SIROLIMUS, isolated from Streptomyces hygroscopicus, acts by inhibiting the interaction of mTOR with its substrates, decreasing levels of hypoxia-inducible factor 1 (HIF-1) and significantly inhibiting VEGF-mediated vascular endothelial cell stimulation, bFGF-induced angiogenesis, and T-cell activation. Off-label uses include treatment for psoriasis, Kaposi sarcoma, tuberous sclerosis, and angiofibromatosis.
93
What are the potential side effects associated with SORAFENIB treatment?
SORAFENIB can cause hypersensitivity reactions and has been associated with dermatologic toxicities (rash, hand-foot syndrome, alopecia, pruritus), multiple blood dyscrasias, hypertension, cardiac ischemia, gastrointestinal upset, perforation, and nephrotic syndrome. It also has drug metabolism interactions with CYP2B6, CYP2C8, and CYP3A4.
94
What are the clinical implications of using RANIBIZUMAB in patients with ocular conditions?
The use of RANIBIZUMAB can lead to ocular or periocular infections, hypersensitivity reactions, endophthalmitis, retinal detachment associated with intravitreal administration, increased intraocular pressures, and arterial thromboembolic events, which are important considerations in clinical practice.
95
How does SIROLIMUS contribute to the treatment of dermatological conditions?
SIROLIMUS is used off-label in dermatology for conditions such as psoriasis and Kaposi sarcoma due to its immunosuppressant and antineoplastic properties, which inhibit mTOR and subsequently reduce angiogenesis and T-cell activation.
96
What are the indications for SORAFENIB in cancer treatment?
SORAFENIB is indicated for the treatment of advanced renal cell carcinoma, unresectable hepatocellular carcinoma, and differentiated thyroid cancer. It is also being studied in clinical trials for metastatic melanoma, both alone and in combination with chemotherapy.
97
What are the systemic toxicities associated with SIROLIMUS?
Systemic toxicities of SIROLIMUS include cutaneous toxicities such as angioedema, leukocytoclastic vasculitis, xerosis, and aphthous ulceration, which typically resolve with discontinuation of therapy. There is also an increased susceptibility to infections and malignancies.
98
What are the contraindications for using RANIBIZUMAB in patients?
Contraindications for RANIBIZUMAB include a history of ocular or periocular infections and hypersensitivity to the drug, as these can lead to serious complications during treatment.
99
What is the role of SORAFENIB in the RAF/MEK/ERK pathway?
SORAFENIB acts as a small-molecule phosphorylation inhibitor of several tyrosine kinase receptors, including PDGF and VEGFRs, thereby contributing to the blockage of the RAF/MEK/ERK pathway, which is crucial in tumor growth and angiogenesis.
100
What are the clinical considerations for patients receiving RANIBIZUMAB therapy?
Clinicians should monitor patients for potential side effects such as ocular infections, retinal detachment, increased intraocular pressure, and thromboembolic events, as well as assess for any hypersensitivity reactions during RANIBIZUMAB therapy.
101
What is the mechanism of action of Sunitinib and its clinical applications?
Sunitinib is a small-molecule phosphorylation inhibitor of several tyrosine kinase receptors, including PDGF, VEGFR-1, VEGFR-2, and VEGFR-3. It is used in the treatment of GI stromal tumors, advanced renal cell carcinoma, and pancreatic neuroendocrine tumors. Clinical trials are ongoing to evaluate its efficacy in metastatic melanoma and it has shown efficacy in treating skin ulcers associated with angioosteohypertrophy syndrome.
102
What are the side effects associated with Temsirolimus?
Temsirolimus can cause several side effects including: - Rash - Mucositis, GI upset, and bowel perforation - Metabolic derangements (hyperglycemia, hyperlipidemia) - Interstitial lung disease - Renal toxicity - Diarrhea and stomatitis - Fatigue Additionally, it has CYP3A4 drug metabolism interactions.
103
What are the indications and precautions for Thalidomide use?
Thalidomide is indicated for the acute treatment and maintenance therapy for the prevention and suppression of cutaneous manifestations of moderate to severe erythema nodosum leprosum. It is also approved for the treatment of newly diagnosed multiple myeloma in combination with dexamethasone. Precautions include: - Pregnancy class: X - Hypersensitivity to the drug or its components - Requires patient monitoring during therapy (S.T.E.P.S.) - Strict guidelines for pregnancy testing for males and females of childbearing potential.
104
What are the potential metabolic and pulmonary complications of Temsirolimus?
Potential complications include metabolic derangements (e.g., hyperglycemia, hyperlipidemia), interstitial lung disease, and renal toxicity.
105
What are the dermatologic and systemic toxicities to monitor with Sunitinib?
Dermatologic toxicities include rash, skin discoloration, hand-foot syndrome, and alopecia. Systemic toxicities include hypertension, adrenal insufficiency, and CYP3A4 drug metabolism interactions.
106
What are the teratogenic risks and precautions for Thalidomide?
Thalidomide is pregnancy category X and highly teratogenic. Strict guidelines for pregnancy testing and contraception must be followed.
107
What are the potential GI complications of Temsirolimus?
Potential GI complications include mucositis, GI upset, and bowel perforation.
108
What are the potential metabolic complications of Temsirolimus?
Potential complications include hyperglycemia and hyperlipidemia.
109
What are the potential neurologic complications of Thalidomide?
Potential complications include peripheral neuropathy and seizures.
110
What are the potential renal complications of Temsirolimus?
Potential complications include renal toxicity.
111
What are the potential dermatologic complications of Thalidomide?
Potential complications include Stevens-Johnson syndrome and toxic epidermal necrolysis.
112
What are the potential pulmonary complications of Temsirolimus?
Potential complications include interstitial lung disease.
113
What are the potential hematologic complications of Thalidomide?
Potential complications include neutropenia.
114
What are the potential fatigue-related complications of Temsirolimus?
Potential complications include fatigue.
115
What are the potential teratogenic risks of Thalidomide?
Thalidomide is highly teratogenic and classified as pregnancy category X.
116
What are the potential GI-related complications of Temsirolimus?
Potential complications include diarrhea and stomatitis.
117
What are the potential cardiovascular complications of Thalidomide?
Potential complications include bradycardia.
118
What are the potential infusion-related complications of Temsirolimus?
Potential complications include infusion reactions.
119
What are the potential systemic complications of Thalidomide?
Potential complications include drowsiness, orthostatic hypotension, rash, fever, and increases in HIV viral loads.
120
What are the potential systemic complications of Temsirolimus?
Potential complications include metabolic derangements, interstitial lung disease, renal toxicity, and fatigue.
121
What are the primary mechanisms of action for Sunitinib in cancer treatment?
Sunitinib is a small-molecule, phosphorylation inhibitor that targets several tyrosine kinase receptors, including PDGF, VEGFR-1, VEGFR-2, and VEGFR-3. It inhibits tumor growth and promotes tumor regression through various downstream mechanisms.
122
What are the clinical applications of Temsirolimus?
Temsirolimus is used in the treatment of advanced renal cell carcinoma and is being evaluated in clinical trials for metastatic melanoma, often in combination with other agents like sorafenib or bevacizumab.
123
What are the common side effects associated with Sunitinib?
Common side effects of Sunitinib include dermatologic toxicities (such as rash and skin discoloration), hypertension, adrenal insufficiency, and potential drug interactions involving CYP3A4.
124
What is the significance of the pregnancy category for Thalidomide?
Thalidomide is classified as pregnancy category X, indicating that it is contraindicated in pregnancy due to its teratogenic effects. Strict guidelines for pregnancy testing are required for patients of childbearing potential.
125
What are the potential adverse effects of Temsirolimus?
Adverse effects of Temsirolimus may include rash, mucositis, gastrointestinal upset, metabolic derangements (such as hyperglycemia and hyperlipidemia), interstitial lung disease, renal toxicity, and fatigue.
126
How does Thalidomide function in the treatment of multiple myeloma?
Thalidomide exhibits antineoplastic, immunomodulatory, and antiangiogenic properties, downregulating factors like VEGF and bFGF. It is approved for the treatment of newly diagnosed multiple myeloma, often in combination with dexamethasone.
127
What monitoring is required for patients taking Thalidomide?
Patients on Thalidomide require monitoring under the S.T.E.P.S. program, which includes guidelines for pregnancy testing and monitoring for hypersensitivity reactions and other serious side effects.
128
What are the implications of hypersensitivity reactions in patients treated with Sunitinib?
Hypersensitivity reactions to Sunitinib can lead to severe adverse effects, necessitating careful monitoring and potential discontinuation of the drug if such reactions occur.
129
What is the role of Temsirolimus in managing advanced renal cell carcinoma?
Temsirolimus is an mTOR inhibitor that downregulates HIF-1 and blocks VEGF-mediated stimulation, making it effective in treating advanced renal cell carcinoma.
130
What are the guidelines for dosing Thalidomide in patients?
Dosing for Thalidomide typically starts at 100 to 300 mg/day, taken with a full glass of water at bedtime or at least one hour after the evening meal.
131
What are the guidelines for dosing Thalidomide in patients?
Dosing for Thalidomide typically starts at 100 to 300 mg/day, taken with a full glass of water at bedtime or at least one hour after the evening meal, with gradual tapering as improvement is noted.
132
What are the off-label uses of Trastuzumab (Herceptin)?
- Kaposi sarcoma - Hemangioendotheliomas - Severe aphthous stomatitis (especially in patients with AIDS) - Psoriasis - A variety of other dermatologic conditions
133
What is the mechanism of action of Trastuzumab (Herceptin) in cancer treatment?
Trastuzumab is a human monoclonal antibody that targets the human estrogen receptor 2 (HER-2). It results in: - Downregulation of angiopoietin-1 - Downregulation of plasminogen-activator inhibitor-1 - Downregulation of VEGF - Downregulation of transforming growth factor - Upregulation of TSP-1, an inhibitor of angiogenesis.
134
What are the known side effects of Trastuzumab (Herceptin)?
- Hypersensitivity - Cardiomyopathy - Pulmonary toxicities - Worsening of chemotherapy-induced neutropenia - Infusion reactions
135
What is the recommended approach for tapering treatment with antiangiogenic agents?
An attempt at tapering should occur every 3 to 6 months.
136
A patient with HER-2 positive breast cancer is being treated with trastuzumab. What are the key risks associated with this therapy?
Key risks include cardiomyopathy, pulmonary toxicities, worsening of chemotherapy-induced neutropenia, and infusion reactions.
137
A patient with HER-2 positive breast cancer is experiencing cardiomyopathy during trastuzumab therapy. What should be the next step?
Cardiomyopathy is a serious risk associated with trastuzumab. Therapy should be reassessed, and cardiology consultation may be required.
138
What are the treatment indications for Trastuzumab?
Trastuzumab is indicated for the treatment of HER-2 overexpression, lymph node-positive breast cancer, and breast cancer that is node-negative.
139
What are the known side effects associated with Trastuzumab?
Known side effects of Trastuzumab include hypersensitivity reactions, cardiomyopathy, pulmonary toxicities, worsening of chemotherapy-induced neutropenia, and infusion reactions.
140
What is the recommended tapering schedule for patients receiving antiangiogenic agents?
The recommended tapering schedule for patients receiving antiangiogenic agents should occur every 3 to 6 months.
141
What should patients do if they experience reproductive toxicity while on antiangiogenic agents?
Patients experiencing reproductive toxicity while on antiangiogenic agents should consult an obstetrician/gynecologist with experience in reproductive toxicity.
142
What is the dosing regimen for Interferon-α2b in patients with malignant melanoma high-dose regimen?
The dosing regimen for Interferon-α2b in patients with malignant melanoma high-dose regimen includes an induction dose of 20 million IU/m² IV infusion over 20 minutes for 5 consecutive days/week for 4 weeks, followed by a maintenance dose of 10 million IU/m² subcutaneously 3 times/week for 48 weeks.
143
What is the initial dose of Thalidomide for Erythema nodosum leprosum?
The initial dose of Thalidomide for Erythema nodosum leprosum is 100-300 mg/day, preferably 1 hour after the evening meal with a full glass of water.
144
What are the maintenance dosing recommendations for patients with chronic graft-versus-host disease receiving Thalidomide?
For patients with chronic graft-versus-host disease receiving Thalidomide, the maintenance dose is 200-400 mg/day, and pediatric doses are 3-5 mg/kg twice daily for 4 days.
145
What are the potential dermatologic uses of Trastuzumab?
Currently, there are no known dermatologic uses or investigations into potential uses for Trastuzumab at this time.

Fitzpatrick's Dermatology, 9th Edition (Entrance Exam / Board Exam Prep) (213 decks)

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