Chemo Drugs-Final

ONCOLOGY
Cell-Cycle
ANTI CANCER DRUGS
1. Alkylating Agents
2. Antimetabolites
3. Anti tumor antibiotic
4. Natural Products
a. Vinca Alkaloids
b. Taxanes
c. Topoisomerase Inhibitors
5. Miscellaneous Agents
a. Hydroxyurea
b. L Asparginase
c. Biologic Agents
6. Steroid Hormone Agonist and Antagonist and related Drugs
7. Adjunct Agents.
MUSTARD GAS
1. ALKYLATING AGENTS
X
INSERT ALKYL
CROSS X
LINKING OF DNA DAMAGE
IN DNA
DNA
CELL CYCLE
CELL DEATH X
NON SPECIFIC
X AGENTS
X
Chemical Classes Examples
Alkyl Sulfonates Busulfan
Aziridines Thiotepa
Triazines Temozolamide, Dacarbazine
Nitrogen Mustard Meclorethamine, Melphalan,
Chorambucil, Cyclophosphamide,
Ifosfamide
Nitrosoureas Carmustine, Lomustine
Platinum Analogs Cisplatin, Carboplatin, Oxaliplatin,
(Alkylating-like Satraplatin
agents)
Example #1: Busulfan (Alkyl Sulfonates)
• Does not require bioactivation in the liver
• Toxic to bone marrow – Leukemia – CML
• Used before bone marrow transplant
– Myeloablative conditioning
Side effects:
Example #2: Carmustine, Lomustine (Nitrosureas)
• Prodrug – requires activation in the liver
• Lipid soluble – BBB
– Brain tumors
Side Effects:
1. Neurotoxic
– Seizure
– ataxia
Example #3: Cyclophosphamide, Ifosfamide (Nitrogen Mustard)
• Related to PHOSPOGENE – Mustard Gas
• 1st IV chemotherapy
• Prodrugs
CANCERS: Leukemias, Lymphomas and Solid Tumors (ovarian & breast)
Side Effects:
• bladder cancer
• Cystitis
– Increase fluid intake
– Administer Mesna
• Infertility
• teratogenic
• They are Alkylating like agents but don’t have Alkyl grp
• Example #6:
(Platinum Analog)
Carboplatin
Cisplatin
Oxaliplatin
Indications:
1. Solid Tumors (Cisplatin, Carboplatin)
– Testicular
– Bladder
– Ovarian
– Cervical
– Lung
2. Osteosarcoma (Cisplatin, Carboplatin)
3. Advance colon cancer (Oxaliplatin)
Side effects:
2. Nephrotoxic – Hydration & Mannitol
3. Neurotoxic – peripheral neuropathy and CN 8
damage
4. Allergic Reaction
2. ANTI METABOLITES
MIMIC FOLIC MIMIC MIMIC

ACID PYRIMIDINE PURINE
CELL CYCLE
NO DNA
CELL DEATH SPECIFIC
DUPLICATION
X AGENTS
2. ANTI METABOLITES
General Classes Examples
Antifolates Methotrexate
Pyrimidine Analogues 5-Fluoroprimidines: 5FU
(Cytosine/Thymine) Arabinose: Cytarabine,
Gemcitabine
Purine Analogues 6-Thiopurines, 6-Mercapurine,
(Adenine/Guanine) Azathioprine, Cladribine
2. ANTI METABOLITES
Example #1: Azathioprine, Cladribine (Purine Analogues)
Indication:
Azathioprine
• Leukemias – ALL, CML
Cladribine
• Hairy cell and other Leukemias
• Lymphomas
Side Effects:
1. Liver toxicity
– Cholestasis
2. Acute Pancreatitis
2. ANTI METABOLITES
Example #2: 5 Flourouracil Side Effects:
(Pyrimidine Analogues)
Indications:
1. CNS toxicity
• Solid tumors 2. Photosensitivity
– Colorectal 3. Palmar-plantar
– Head and neck
erythrodysesthesia
– Pancratic
– Breast
– Ovarian
– Bladder
– Hepatocellular
– TOPICAL – BASAL CELL
CARCINOMA
• Action of the drug is
enhanced by Leucovorin
(Folinic Acid)
2. ANTI METABOLITES
Example #3: Methotrexate
(Antifolate) Side Effects:
1. Liver toxicity
Indications: – Macrovesicular fatty
• Lymphomas change
– Primary CNS 2. Pulmonary fibrosis
– Non Hodgkins
• Solid Tumors
– Breast
– Head and neck
– bladder
3. ANTI TUMOR ANTIBIOTICS
BLEOMYCI ANTHRACYCLINE
Doxorubicin
N Daunorubicin
CELL CYCLE
DACTINOMYCIN
SPECIFIC
Actinomycin D
G2 Phase
Example #1: Bleomycin Side Effects:
1. Pulmonary Toxicity
– Pneumonitis
Indications: – Pulmonary fibrosis
2. Skin Toxicity
Hodgkin’s Lymphoma – Rashes
Testicular CA – Expoliation
– hyperpigmentation
Squamous cell CA 3. Minimal Myelosuppresion
Example #4: Dactinomycin
Indications:
1. Pediatric Tumors
– Nephroblastoma
– Wilms tumor
2. Rhabdomyosarcoma
3. Ewing Sarcoma
4. NATURAL PRODUCTS
A. Vinca Alkaloids
 Vinblastine (VBL)
 Vincristine (VCR)
B. Taxanes
 Paclitaxel
 Docetaxel
C. Topoisomerase Inhibitors
General Classes Examples
Camptothecins (1) Irinotecan, Topotecan
Epipodophyllotoxins (2) Etoposide, Teniposide

A. VINCA ALKALOIDS
Example #1: Vinblastine,
Side effects:
Vincristine
Indications: 1. Severe Myelosuppression –
1. Solid Tumors Vinblastine
– breast
2. Neurotoxic - Vincristine
2. Pediatric cancers
– Rhabdomyosarcoma, • ANS dysfunction
Wilms tumor – Orthostatic hypotension
3. Leukemias – Urinary retention
4. Lymphoma
– Constipation
• Peripheral neuropathy
B. TAXANES
Example #2: Paclitaxel, Doxitacel
Indications:
1. Solid Tumors
• Breast
• Ovarian
• Lung
• Gastroesophageal
• Prostate
• Bladder
• Head and neck
Side effects:
2. Hypersensitivity
3. Neurotoxicity
C. TOPOISOMERASE INHIBITOR
(CAMPTOTHECINS)
IRINOTECAN TOPOTECAN
PRO DRUG EXCRETED

EXCRETED urine
bile
feces
METASTATIC COLON ADVANCED OVARIAN

CANCER CANCER
SMALL CELL LUNG
CARCINOMA
(EPIPODOPHYLLOTOXINS)
Example : Etoposide and
Teniposide
Indications:
Solid Tumors
• Testicular CA
• Small cell lung CA
Leukemias
Lymphomas
5. MISCELLANEOUS AGENT -
MONOCLONAL ANTIBODIES
Monoclonal – specific B cell line
Antibody – target specific antigen
VEGF OVEREXPRESSION
Monoclonal – specific B cell line

Antibody – target specific antigen
EGFR OR HER 2 OVEREXPRESSION

Cetuzimab Side effects:

(Chimeric) 1. Hypersensitivity
• Targets EGFR reaction
2. GIT problems
Indications:
3. Skin problems
1. Metastatic colorectal – Dryness
CA – Pruritus
2. Head and neck CA – Acneiform skin
rashes
Trastuzumab Side effects:
(Humanized) 1. Cardiotoxicity
• Targets HER2 – Cardiomyopathy
Indications: 2. GIT problems
1. Breast CA
2. Gastric CA
3. Ovarian CA
4. Lung CA
Bevacizumab Side effects:
(Humanized) 1. Inhibition of normal
• Targets VEGF tissues
– Impaired wound healing
Indications:
– Hemorrages
1. Breast CA • Epistaxis
2. Colorectal CA • Hemoptysis
3. Renal cell CA • GI bleeding
• Intracranial bleeding
4. Non Small Cell
• Perforation of GIT
Lung CA
Retuzimab
(Chimeric)
• Targets CD20
Indications:
CD20
1. Non Hodgkin B cell
lymphoma
2. CLL – abnormal
proliferation of B or T cell
Side effects:
3. Hypersensitivity Rxn
4. Suppression of immune
system
– Reactivation of virus
5. MISCELLANEOUS AGENT
A. Hydroxyurea (many cancers)
B. L Asparaginase for ALL (enzyme)
C. Biologic Agents
Cytokines and Cytokine Modifiers
 Thalidomide for MM – immunomodulator, antiangiogenic
 Inteferon alpha for meningioma - biologic response
modifier, cytokine
 Interleukin 2 for renal and other cancers– BRM, cytokine
 BCG (bladder cancer) - BRM
6. STEROID /HORMONE AGONIST AND
ANTAGONIST RELATED DRUGS
A. SERMS (Selective Estrogen Receptor
Modulators) – Tamoxifen
B. Anti Estrogen – Falsodex
C. Gonadonadotropin Releasing Hormone (GnRH)
Analogs – Lupron
D. Aromatase Inhibitor – Anastrozole
E. Androgen Antagonist – Flutamide
7. ADJUNCT AGENTS
A. Leucovorin – chemoprotectant, antidote for MTX
B. Filgrastim – G-CSF, Neupogen - granulocyte
C. Epoeitin Alfa (Epogen) – CSF - RBC
D. Allopurinol (Alloprim) - tumor lysis syndrome
(Antimetabolite)
E. Prednisone – anti inflam, prevent N/V, prevent
allergic rxn, appetite stimulant, adrenal
insufficiency
F. Dipenhydramine, plasil and others.
Common combination chemotherapy regimens[16]
Cancer type Drugs Acronym
Cyclophosphamide, methotrexate, CMF
5-fluorouracil
Breast cancer
Doxorubicin, cyclophosphamide AC
Mustine, vincristine, procarbazine, MOPP
prednisolone
Hodgkin's disease
Doxorubicin, bleomycin, vinblastine, ABVD
dacarbazine
Non-Hodgkin's lym Cyclophosphamide,

prednisolone
doxorubicin, vincristine, CHOP
phoma
Germ cell tumor Bleomycin, etoposide, cisplatin BEP
Epirubicin, cisplatin, 5-fluorouracil ECF
Stomach cancer
Epirubicin, cisplatin, capecitabine ECX
Bladder cancer Methotrexate, vincristine, doxorubicin, MVAC

cisplatin
Lung cancer Cyclophosphamide, doxorubicin, vincristine, CAV
Colorectal cancer 5-fluorouracil, folinic acid, oxaliplatin FOLFOX

ABSOLUTE NEUTROPHIL COUNT
ANC = (% polys + bands) X WBC
Example: polys 77%, bands 3% WBC 4,500
ANC = (0.77 + 0.03) X 4,500
= (0.80) X 4,500
= 0.80 X 4,500
= 3,600
*** hold chemo if ANC is less than 1,500***
DOSAGE CALCULATION
Ex: Give 75mg/m² on day 1 every 21 days
Computation = BSA X dose
Body Surface Area
=
1.71
Computation = BSA X dose

1.71 X 75
128 mg
TOXICITY DRUGS
RENAL Cisplatin – hydration and mannitol
DISTINCTIVE TOXICITIES OF ANTI CANCER
Methotrexate – crystalluria, may give mesna
Nitrosureas
Streptozocin – proximal tubular damage
HEPATIC AGENTS
6MP
Cyclophosphamide
Busulfan, Asparginase, Methotrexate
PULMONARY Bleomycin – pneumonitis, pulmonary fibrosis
Busulfan, Procarbazine
CARDIAC Doxorrubicin – CHF, cardiomyopathy
Daunorubicin - cardiomyopathy
NEUROLOGIC Vincristine
Paclitaxel
Ifosfamide
IMMUNOSUPPRESIVE Cyclophosphamide, Cytarabine, Dactinomycin, Methotrexate
VESICANT Dactinomycin, Daunorubicin, Doxorubicin, Methotrexate, Mitomycin, Vinca
Alkaloids, Nitrosureas
SEVERE MYELOSUPPRESION Camustine, Cytarabine, Daunorubicin, Doxorubicin, Paclitaxel
OTHER IMPT EFFECTS Cyclophosphamide – cystitis, give mesna
TO REMEMBER Procarbazine - leukomogenic
Asparaginase- pancreatitis, hepatotoxic, antigenic
Cisplatin – oto/muta/terato/carcinogenic
Anti Estrogen – hot flashes, N&V, abn menses
LEUKEMIAS
LYMPHOMAS
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Chemo Drugs-Final

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What are the main classes of anti-cancer drugs discussed in the document?

Name two examples of alkylating agents mentioned and briefly describe their uses and side effects.

ONCOLOGY

MIMIC FOLIC MIMIC MIMIC

General Classes Examples

Camptothecins (1) Irinotecan, Topotecan

Epipodophyllotoxins (2) Etoposide, Teniposide

PRO DRUG EXCRETED

METASTATIC COLON ADVANCED OVARIAN

Monoclonal – specific B cell line

EGFR OR HER 2 OVEREXPRESSION

Cetuzimab Side effects:

Non-Hodgkin's lym Cyclophosphamide,

Bladder cancer Methotrexate, vincristine, doxorubicin, MVAC

Colorectal cancer 5-fluorouracil, folinic acid, oxaliplatin FOLFOX

Computation = BSA X dose

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