Drugs List Flashcards
<p>What type of drug is Avastin (Bevacizumab)?</p>
<p>Monoclonal antibody.
| Targets VEGF inhibiting angiogenesis. </p>
<p>What is the mechanism of action of avastin/bevacizumab?</p>
<p>Monoclonal antibody for VEGF which binds to VEGF therefore inhibiting angiogenesis.
Used in Colorectal, metastatic breast, renal cell carcinoma, NSCLC and glioblastoma. </p>
<p>What can avastin/bevacizumab be used to treat? [5]</p>
<p>Monoclonal antibody for VEGF which binds to VEGF therefore inhibiting angiogenesis.
Used in:
1. Colorectal,
2. metastatic breast,
3. renal cell carcinoma,
4. NSCLC and
5. glioblastoma. </p>
<p>What are the side effects of avastin/bevacizumab? [8]</p>
<p>1. Bone marrow suppression 2. Bleeding 3. VTE 4. Stroke, TIA, MI, angina, CHF (prev anthracycline treatment). 5. Hypertension 6. Proteinuria 7. Diabetes 8. Anaemia And many more....</p>
<p>What are the resistance mechanisms to avastin/bevacizumab? (2)</p>
<p>1. Neovascularisation via other means.
| 2. Altered behaviour to be able to metastasize without the need to angiogenesis. </p>
<p>What adjunct therapy is there with avastin/bevacizumab? (2)</p>
<p>Colorectal: 5FU or campecitibine.
NSCLC: Pt based chemo.</p>
<p>What are the pharmaceutical care issues with avastin/bevacizumab treatment? [4]</p>
<p>Patient aware of bone marrow suppression.
BP checked.
ECGs frequently.
BG levels. </p>
<p>Avastin (Bevacizumab)
1. What is it?
2. What is its mechanism of action?
3. What cancers is it used to treat? [5]
4. What are its side effects? [8]
5. How do cancers become resistant?
6. What adjunct therapy? [2]
7. Pharmaceutical care issues. [4]</p>
<p>1 +2. Monoclonal antibody for VEGF which binds to VEGF therefore inhibiting angiogenesis.
3. Used in Colorectal, metastatic breast, renal cell carcinoma, NSCLC and glioblastoma.
4.Bone marrow suppression, bleeding, VTE, stroke, TIA, MI, angina, CHF (esp. in those prev. treated with anthracyclines)
Hypertension, proteinuria, asthenia, Abdo pain, Mucosal inflammation, diabetes, anaemia.
5. Re-establishing neovascularisation through other means.
Altering their behaviour to metastasize without the need to angiogenesis.
6. CR – with 5FU or campecitibine
NSCLC – Pt based chemotherapy
7. Make sure patient monitored for bone marrow suppression, that they get BP check, ECGs frequently,and blood glucose levels.
</p>
<p>What is Cetuximab?</p>
<p>Chimeric monoclonal antibody to target the EGFR (no Ras mutations).
It inhibits the rapid proliferaton of cancer cells by blocking signal transduction via the EGFR.
Prevents Ras activation, so no Raf phosphorylation, no MAPK/MEK phosphorylation.
Thus, no MAPK/MEK to act as TF for CREB and c-Myc, Braf, PTEN, PIK3CA, KRAS etc, which normally drive proliferation and growth.
Cetuximab is used to treat squamous cell cancer of the head and neck - trials for NSCLC. </p>
<p>How does Cetuximab work?
| What is its target?</p>
<p>Chimeric monoclonal antibody to target the EGFR (no Ras mutations).
It inhibits the rapid proliferaton of cancer cells by blocking signal transduction via the EGFR.
Prevents Ras activation, so no Raf phosphorylation, no MAPK/MEK phosphorylation.
Thus, no MAPK/MEK to act as TF for CREB and c-Myc, Braf, PTEN, PIK3CA, KRAS etc, which normally drive proliferation and growth.
Cetuximab is used to treat squamous cell cancer of the head and neck - trials for NSCLC. </p>
<p>Why would using Cetuximab in patients with a mutation to Ras be pointless?</p>
<p>Chimeric monoclonal antibody to target the EGFR (no Ras mutations).
It inhibits the rapid proliferaton of cancer cells by blocking signal transduction via the EGFR.
Prevents Ras activation, so no Raf phosphorylation, no MAPK/MEK phosphorylation.
Thus, no MAPK/MEK to act as TF for CREB and c-Myc, Braf, PTEN, PIK3CA, KRAS etc, which normally drive proliferation and growth.
Cetuximab is used to treat squamous cell cancer of the head and neck - trials for NSCLC. </p>
<p>What are the side effects associated with Cetuximab? [7]</p>
<p>1. Skin dryness, fissures and hyperpigmentation.
2. Photosensitivity and radiosensitising effects.
3. Mucositis.
4. Hair and nail growth disruption.
5. LFT disturbances.
6. Headache
7. Electrolyte imbalances: hypo - Ca, Hypo - Mg</p>
<p>What adjunct therapy can be used with Cetuximab?</p>
<p>FOLFOX and FOLFIRI regimes.
FOLinic acid (leucovorin)
Fluorouracil (5FU)
and OXiplatin.
FOLinic acid (leucovorin)
Fluorouracil (5FU)
IRInotecan (camptosar) - topoisomerse inhibitor.
</p>
<p>Cetuzimab. What is it? What does it target? What is the point of targeting this? Who would it be pointless to treat with this? What can it be used to treat? What side effects? What adjunct therapies?</p>
<p>Chimeric monoclonal antibody targeting EGFR (no Ras mutations pls).
Signal transducton via EGFR causes the activation of Ras. Which, in turn, activates Raf via phosphorylation. Activated Raf then phosphorylates MAPK and MEK.
MAPK and MEK then act as transcription factors for a number of genes (CREB, c-myc, BRAF, PTEN, KRAS, PIK3CA), the end result of which is cell growth, proliferation, survival etc.
No point using Cetixumab in people with Ras activating mutations as Cetixumab only works via overexpression of EGFR.
Cetixumab can be used to treat Squamous cell cancer of the head and neck and their are CT into NSCLC.
SE: Skin dryness and fissures, hyperpigmentation, photosensitivity and radiosensitising effects. SJS. Mucositis, disruption of normal hair growth, nail changes, headache, GI, LFT disturbances and fatigue. Hypocalcamia and hypomagnesia
Can be used with:
FOLFOX and FOLFIRI regimes.</p>
<p>What is Capecitibine?
| </p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity. </p>
<p>What does Capecitibine target?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What is the relevance of Capectibine targeting TS?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What is Capectibine used to treat?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What are the side effects of Capectibine use?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What adjunct therapies are usable with Capectibine?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What are the main pharmaceutical care issues with Capecitibine?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>Capecitibine. What is it? What does it target? What does it treat? What side effects? What adjuvant options? What pharmaceutical care issues?</p>
<p>Pro-drug of 5FU.
Targets Thymidylate synthase.
Capecitibine is converted into 5FU in the body, 5FU is an antimetabolite pyrimidine antagonist which blocks TS in the folate cycle.
Capecitibine can be used to treat Duke C colorectal cancer and metastatic breast cancer.
Common side effects of Capecitibine are diarrhoea, abdo pain, stomatitis, PPE (hand-foot syndrome).
Capecitibine is used with anthracycline containing regimens and with iaptatibinib for metastatic BC with HER2 overexpression.
The main pharmaceutical care issues regarding Capectibine use are that folate use concurrently may increase toxicity risks.
Uridine triacetate can be used in the emergency treatment of 5FU toxicity.</p>
<p>What is 5-FU?</p>
<p>An antimetabolite which targets Thymidylate synthase.
It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis.
5-Fu can be used to treat BC, head, neck liver and pancreatic cancer.
5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid.
5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer.
Uridine triacetate for emergency toxicity.
PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected. </p>
<p>5FU mechanism of action.</p>
<p>An antimetabolite which targets Thymidylate synthase.
It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis.
5-Fu can be used to treat BC, head, neck liver and pancreatic cancer.
5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid.
5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer.
Uridine triacetate for emergency toxicity.
PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected. </p>
5FU is used to treat
An antimetabolite which targets Thymidylate synthase. It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis. 5-Fu can be used to treat BC, head, neck liver and pancreatic cancer. 5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid. 5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer. Uridine triacetate for emergency toxicity. PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected.
5FU side effects
An antimetabolite which targets Thymidylate synthase. It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis. 5-Fu can be used to treat BC, head, neck liver and pancreatic cancer. 5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid. 5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer. Uridine triacetate for emergency toxicity. PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected.
5FU adjunct therapy
An antimetabolite which targets Thymidylate synthase. It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis. 5-Fu can be used to treat BC, head, neck liver and pancreatic cancer. 5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid. 5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer. Uridine triacetate for emergency toxicity. PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected.
5FU pharmaceutical care issues
An antimetabolite which targets Thymidylate synthase. It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis. 5-Fu can be used to treat BC, head, neck liver and pancreatic cancer. 5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid. 5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer. Uridine triacetate for emergency toxicity. PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected.
5FU. What is it? How does it work? What does it treat? What off target effects does it have? What adjuvant uses? What are the main PCIs with it?
```An antimetabolite which targets Thymidylate synthase. It is an antimetabolite pyrimidine antagonist. Blocks Ts and interferes with RNA synthesis. 5-Fu can be used to treat BC, head, neck liver and pancreatic cancer. 5-FU s/e: BM suppression, diarrhoea, abdo pain, stomatitis, GI toxicity which is excacerbated if 5FU given with folinic acid. 5-FU is often given with cyclophosphamide and methotrexate or doxorubicin for breast cancer. Uridine triacetate for emergency toxicity. PCIs: monitor WCC, stop 5FU treatment if WCC drops rapidly or neutropenic spsis suspected.
What is oxaplatin?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What does oxaplatin target?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What is the mechanism of action of oxaplatin?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What can oxaplatin be used to treat?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What are the side effects of oxaplatin?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
Oxaplatin is often part of what treatment combination?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What are the main pharmaceutical care issues with oxaplatin treatment?
Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
Oxaplatin. What is it? What does it target? How does it work? What can it treat? What side effects? What combination therapies? What PCIs?
```Platinum based anticancer. Targets DNA. Acts similarly to alkylating agents. Bidentate ligand 1,2-diaminocyclohexane group is displaced to give an aqua complex (H2O+). This water ligand is easily displaced by NH2 groups of guanine. The presence of two carboxy groups allows it to cross link in an intrastrand manner wrt purine bases. (GpG mostly). [GpXpG also, but rapidly repaired by NER]. Oxaplatin is used in the treatment of colorectal cancer and UI for ovarian and lung cancer. Oxaplatin side effects include: N+V, nephrotoxicity and myelosuppression. Toxic effects on kidneys and ears! Oxaplatin is commonly given with 5FU and folinic acid (leuvorocin) in colorectal cancer. FOLFOX. The main pharmaceutical care issues are: possible mutagenic and teratogenic effects + risk of secondary malignancies.
What is Cisplatin?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
How does Cisplatin work?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
What is Cisplatin used to treat?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
What are the side effects of Cisplatin?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
What common therapies include cisplatin?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
What are the pharmaceutical care issues with cisplatin?
Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
Cisplatin. What is it? How does it work? What does it treat? What side effects? What combination therapies? What care issues?
```Platinum based drug which targets DNA. Two Cl on left, two NH3 on the right of the Platinum atom. Works similar to Oxaliplatin, One of the two chloride ligands is displaced by water to give an activated aqua complex due to low levels of chloride in cell. Cisplatin is used to treat testicular, ovarian tumours and squamous cell carcinoma of the head and neck. Side effects of cisplatin: N+V, toxic effects on kidneys, bone marrow and ears. Commonly used: Ciplatin + bleomycin and etoposide or a vinca alkaloid. PCIs: possible mutagenic and teratogenic, increased risk of secondary malignancies.
What is Vismodegib?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
How does Vismodegib work?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
What is the relevance of the MOA of Vismodegib?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
Vismodegib prevents the transcription of what?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
Vismodegib side effects
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
What is Vismodegib used to treat?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
What are the pharmaceutical care issues surrounding Vismodegib use?
Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
Vismodegib. What is it? How does it work? What can it treat? What side effects? What care issues?
```Small molecule inhibitor targeting the HH pathway. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. Relevance: When SHH binds to PTCH1 this removes the inhibition of SMO. SMO can then activate GLI1/2/3 TFs for angiogenic factors (APO1/2) and Cyclin D and B, antiapoptotic genes and decrease Fas (an apoptotic gene). It is used to treat recurrent Basal cell carcinoma. Vismodegib can cause muscle spasms, arthralgias, alopecia, fatigue GI disturbances, reduced appetite and weight loss. It is a known teratogen. PCI: Contraceptive use is encouraged due to teratogenicity.
What is imetelstat?
13-mer oligonucleotide inhibitor of the RNA component of telomerase enzyme. Can be used for metastatic breast cancer, and NSCLC (P2 clinical trials).
What is Pifithrin?
This compound, pifithrin-alpha, protected mice from the lethal genotoxic stress associated with anticancer treatment without promoting the formation of tumors. Thus, inhibitors of p53 may be useful drugs for reducing the side effects of cancer therapy and other types of stress associated with p53 induction.
What is RG7388?
The latest generation MDM2 inhibitor RG7388 has demonstrated selective and potent p53 to MDM2 inhibition with improved bioavailability. The key target of Mdm2 is the p53 tumor suppressor. Mdm2 has been identified as a p53 interacting protein that represses p53 transcriptional activity. Mdm2 is a p53 responsive gene—that is, its transcription can be activated by p53. Thus when p53 is stabilized, the transcription of Mdm2 is also induced, resulting in higher Mdm2 protein levels. Mdm2 is overexpressed in many cancer cells leading to increased repression of p53 and uncontrolled cell growth. Inhibiting MDM2, via molecules such as PG7388, can restore levels of p53 in cancer cells to induce apoptosis.
What is the rationale behind MDM2 inhibitors such as RG7388?
The key target of Mdm2 is the p53 tumor suppressor. Mdm2 has been identified as a p53 interacting protein that represses p53 transcriptional activity. Mdm2 is a p53 responsive gene—that is, its transcription can be activated by p53. Thus when p53 is stabilized, the transcription of Mdm2 is also induced, resulting in higher Mdm2 protein levels. Mdm2 is overexpressed in many cancer cells leading to increased repression of p53 and uncontrolled cell growth. Inhibiting MDM2, via molecules such as PG7388, can restore levels of p53 in cancer cells to induce apoptosis.
What is Pembrolizumab?
Monoclonal antibody against PD1, found on T-cells, and its ligands PD-L1/L2. Pembrolizumab releases the PD1 pathway mediated inhibition of the immune system, including the anti-tumour response. Pembrolizumab can treat PDL1 positive NSCLC or melanoma. Pembrolizumab can cause the following side effects: Fatigue, cough, nausea, rash, decreased appetite, constipation, arthralgia, diarrhoea and immune mediated adverse reactions: pneumonitis, colitis and hepatitis.
How does Pembrolizumab work?
Monoclonal antibody against PD1, found on T-cells, and its ligands PD-L1/L2. Pembrolizumab releases the PD1 pathway mediated inhibition of the immune system, including the anti-tumour response. Pembrolizumab can treat PDL1 positive NSCLC or melanoma. Pembrolizumab can cause the following side effects: Fatigue, cough, nausea, rash, decreased appetite, constipation, arthralgia, diarrhoea and immune mediated adverse reactions: pneumonitis, colitis and hepatitis.
What can Pembrolizumab be used to treat?
Monoclonal antibody against PD1, found on T-cells, and its ligands PD-L1/L2. Pembrolizumab releases the PD1 pathway mediated inhibition of the immune system, including the anti-tumour response. Pembrolizumab can treat PDL1 positive NSCLC or melanoma. Pembrolizumab can cause the following side effects: Fatigue, cough, nausea, rash, decreased appetite, constipation, arthralgia, diarrhoea and immune mediated adverse reactions: pneumonitis, colitis and hepatitis.
What side effects does Pembrolizumab cause?
Monoclonal antibody against PD1, found on T-cells, and its ligands PD-L1/L2. Pembrolizumab releases the PD1 pathway mediated inhibition of the immune system, including the anti-tumour response. Pembrolizumab can treat PDL1 positive NSCLC or melanoma. Pembrolizumab can cause the following side effects: Fatigue, cough, nausea, rash, decreased appetite, constipation, arthralgia, diarrhoea and immune mediated adverse reactions: pneumonitis, colitis and hepatitis.
What is Enzalutamide?
Androgen receptor signalling inhibitor targeting the androgen receptor itself. 3 modes of action: 1. Blocks binding of androgens to androgen receptors. 2. inhibits nuclear translocation of any activated receptors. 3. Prevents associated of the activated receptors with DNA. Treats metastatic prostate cancer. Can cause Headache, hot flushes, memory problems, visual hallucinations and increased risk of seizures.
How does Enzalutamide work? | How many modes of action?
Androgen receptor signalling inhibitor targeting the androgen receptor itself. 3 modes of action: 1. Blocks binding of androgens to androgen receptors. 2. inhibits nuclear translocation of any activated receptors. 3. Prevents associated of the activated receptors with DNA. Treats metastatic prostate cancer. Can cause Headache, hot flushes, memory problems, visual hallucinations and increased risk of seizures
What is enzalutamide used to treat?
Androgen receptor signalling inhibitor targeting the androgen receptor itself. 3 modes of action: 1. Blocks binding of androgens to androgen receptors. 2. inhibits nuclear translocation of any activated receptors. 3. Prevents associated of the activated receptors with DNA. Treats metastatic prostate cancer. Can cause Headache, hot flushes, memory problems, visual hallucinations and increased risk of seizures
What side effects can enzalutamide cause?
Androgen receptor signalling inhibitor targeting the androgen receptor itself. 3 modes of action: 1. Blocks binding of androgens to androgen receptors. 2. inhibits nuclear translocation of any activated receptors. 3. Prevents associated of the activated receptors with DNA. Treats metastatic prostate cancer. Can cause Headache, hot flushes, memory problems, visual hallucinations and increased risk of seizures
Enzalutamide. What is it? How does it work? What does it treat? What side effects?
```Androgen receptor signalling inhibitor targeting the androgen receptor itself. 3 modes of action: 1. Blocks binding of androgens to androgen receptors. 2. inhibits nuclear translocation of any activated receptors. 3. Prevents associated of the activated receptors with DNA. Treats metastatic prostate cancer. Can cause Headache, hot flushes, memory problems, visual hallucinations and increased risk of seizures
What is carboplatin?
Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.
Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.Platinum based chemotherapy drug.
Targets DNA.
The Carboxyl groups are replaced by aqua groups, to form a H2O+ ion. This binds to the NH2 groups on purine bases and can form intrastrand cross linking. Carboplatin is used to treat advanced ovarian cancer and SCLC. Can cause N+V, toxic effects on kidneys (all platinums), bone marrow and ears. Myelosuppression. Carboplatin is less ototoxic than cisplatin but neurological and hearing assessments should still place.
