Antineoplastic

Quinn Karylle Fuentes · 28問 · 2年前

通報

問題一覧

New or unusual growth of tissue (TUMORS)

Neoplasia

Malignant or benign

Tumor

Surgical removal followed by radiation and/or chemotherapy

Treatment of malignate tumor.

Tumor, lymph Node, and Metastasis

Tnm System

are numbered to indicate the size of the tumor and the extent of lymph node involvement. M is followed by either “0” or “1”

T &N

During the entire cycle, movement from one phase to the next is driven by proteins known as cyclins and their associated cyclindependent kinases (CDK)

Cyclins

DNA is thought to lead to cell death

Alkylation

Major targets of drug action are nucleophilic groups present in DNA

Alkylation

Nucleophilic sites on DNA, which are susceptible to electrophilic attack by an alkylating agent

Alkylating agent

The general mechanism for alkylation involves nucleophilic attack by –N=, -NH2, - OH, -O-PO3H of the DNA and RNA. (T/F)

True

Compounds that are chemically similar to sulfur mustard that was developed and used in WW1

Nitrogen mustard

One mustard molecule can alkylate two nucleophiles

Dialkylating agent

This drug is too reactive making it nonselective

MECHLORETHAMINE

The antidote for extravasation is sodium thiosulfate (Na2S2O3)

MECHLORETHAMINE

§ Aryl group decreases reactivity § To be taken orally § Least toxic

Chlorambucil Leukeran®,

The phenylalanine functionality attempts to increase entry into the cancer cell.

Melfalan (Alkeran®,)

What isnthe active part of CYCLOPHOSPHAMIDE

Phospharamide mustard

what isnthe toxic products of CYCLOPHOSPHAMIDE

Acrolein

Coadministration with MESNA is recommended.

CYCLOPHOSPHAMIDE

In case of extravasation, for toxicity, a strong nucleophile is given such as?

Na thiosulfate

concentrates the electrophilic substance in the kidney and conjugates Acrolein

Mesna

As a result of research to investigate compounds with preformed aziridine ring.

THIOTEPA (TIFOSYL, THIOPLEX)

Has a less reactive aziridine ring compared with that formed in mechlorethamine.

THIOTEPA (TIFOSYL, THIOPLEX)

Used for Tx of bladder cancer, ovarian cancer, and breast cancer.

THIOTEPA (TIFOSYL, THIOPLEX)

Alternative to utilizing aziridines as electrophilic species

Busulfan (Myleran ®)

4-5 alkyl substituents are optimal for antineoplastic activity

Busulfan (Myleran ®)

What is the side effects of Busulfan (Myleran ®)

Fatal pulmonary fibrosis, “busulfan lung”

It is used in the patient with chronic myelogenous leukemia (CML

Busulfan (Myleran ®)

Undergo spontaneous non-enzymatic degradation with the formation of the 2- chloroethyl carbonium ion from diazohydroxide formed

Nitrosoureas

Liberates isocyanate that attaches carbamoyl groups to the lysine residues of proteins – inactivates DNA

Nitrosoureas

Carbonium ion: alkylating agent

LOMUSTINE

Alkylation occurs preferentially at the N-7 position of guanine with minor amounts of alkylation at guanine O-6.

Nitrosoureas

Tx for brain tumors, Hodgkin’s and non-Hodgkin’s disease, and multiple myeloma

CARMUSTINE – BCNU (Bis-Chloroethyl nitrosourea)

Tx for primary and metastatic brain cancers and Hodgkin’s lymphoma.

LOMUSTINE – CCNU (Chloroethyl-Cyclohexyl nitrosourea)

was originally developed as a result of efforts to find new inhibitors of monoamine oxidase

PROCARBAZINE (PCZ, PCB, MATULANE)

Available as 50 mg tablets for oral administration in the treatment of Hodgkin’s and non-Hodgkin’s disease, brain cancer, and mycosis fungoides

PROCARBAZINE (PCZ, PCB, MATULANE)

undergoes N-demethylation in the liver through the enzyme CYP450

PROCARBAZINE (PCZ, PCB, MATULANE)

A major pathway for inactivation is through S-Methylation by (TPMTThiopurine-S-methyl transferase) and by oxidation through Xanthine Oxidase (XO).

Mercaptopurine

A derivative of 6-Mercaptopurine is used as an immunosuppressive agent

Azathioprine

D-arabinose from D-ribose

Vidarabine

Chlorine incorporated in the adenine

Cladribine

Presence of 2-Fluoro group on the adenine ring renders fludarabine resistant to breakdown by adenosine deaminase

Fludarabine

Chlorine incorporated in the adenine

Cladribine

Blocks conversation of uridine to thymidine

Pyrimidine analogs

increases acidity and binds more strongly

F atom

is converted into a ‘fraudulent’ nucleotide, fluorodeoxyuridine monophosphate (FDUMP)

Fluorouracil

which is an important enzyme in the synthesis of pyrimidine for DNA replication

thymidylate synthase inhibitor

First for the treatment of colon cancer

5-FU

for the conversion of Uracil to thymine

was discovered in Europe in the 1960s. It gained FDA approval in June 1969.

Cytarabine (Ara-C)

ytosine arabinoside is an antimetabolic agent with the chemical name of

1β-arabinofuranosylcytosine

Its mode of action is due to its rapid conversion into cytosine arabinoside triphosphate, which damages DNA when the cell cycle holds in the S phase.

Cytarabine

In combination with daunorubicin or thioguanine for the treatment of

acute nonlymphocytic leukemia

As with fluorouracil and other analogs of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case, cytidine, during DNA replication.

Gemcitabine (Gemzar)

Inhibition of ribonucleotide reductase

Gemcitabine (Gemzar)

Used for lung cancer

Gemcitabine (Gemzar)

Blocks DNA synthesis through inhibition of the enzyme dihydrofolate reductase

METHOTREXATE

Dihydrofolate reductase inhibitor

METHOTREXATE

Folic acid inhibition kills cells in the S Phase

METHOTREXATE

is given to prevent toxicity in normal cells. Given 6-24 hours after treatment with MTX.

Leucovorin

Anthracyclines

Daunorubicin, Valrubicin, Epirubicin, Idarubicin, Doxorubicin

Actinomycins

Dactinomycin

Glycopeptide antibiotic

Bleomycin

Disrupt DNA function and cell division

Cytotoxic antibiotics

Planar molecule inserts itself between base pair of DNA

Intercalation

Topoisomerase

Intercalation

Isolated from Streptomyces verticillius

Bleomycin

Active in the G2 and M phase of the cell cycle

Bleomycin

Binding to DNA followed by singlestrand or double-strand cleavage

Bleomycin

ROS formation from bleo-iron complex

Bleomycin

The mode of inactivation is through Hydrolysis through bleomycin hydrolase which is found in low concentrations in the skin and lungs. ( T/F)

True

Thus, reddening of the skin, skin darkening (hyperpigmentation), and pulmonary toxicity occur.

Bleomycin

Isolated from Streptomyces spp.

Actinomycin

Intercalates particularly at guaninecytosine bases

Dactinomycin

Streptomyces parvulus, Specific to G1 and S phase

Dactinomycin

Streptomyces peucetius

Anthracyclines

It intercalates into DNA and decreases the synthesis of both DNA and RNA

Anthracyclines

Oxidation of cellular components or anthracyclines results from the intercalation of base pair

Anthracyclines

planar oxidized anthracene nucleus fused to a cyclohexane ring that is subsequently connected to an amino sugar

Anthracyclines

Synthetic, however, is included with the natural products because it shares similarities with anthracyclines

Mitoxantrone (Novantrone®)

- Inhibition of Topoisomerase II - Not a substrate for reductase enzymes Lack of activation (side chain) Reduced cardiotoxicity

Anthracenedione

Binds to microtubule --> suppression of microtubule dynamics --> metaphase arrest

Vinca alkaloids

Depolymerization of microtubules at high concentration

Vinca alkaloids

First isolated from the bark of Western/Pacific yew (Taxus brevifolia)

Taxens

Different binding site compared with vinca alkaloids

Taxanes

The epipodophyllotoxins are semisynthetic derivatives of podophyllotoxin, which is isolated from the mayapple (mandrake) root and functions as an inhibitor of microtubule function

Epipodophyllotoxins

S and G2 phases of the cell cycle

Topoisomerase II

Forms a ternary complex with topoisomerase II and DNA

Etoposide

Leukemia posttreatment

Etoposide

Camptothecins which include irinotecan and topotecan are commonly used type 1 topoisomerase inhibitors, first discovered in the late 1950s. (T/F)

True

these chemotherapy agents are extracted from the bark and wood of the Chinese tree, Camptotheca accuminata. They work by forming a complex with topoisomerase DNA.

Type 1 Topoisomerase inhibitors:

Platinum complexes are inhibitors of DNA polymerase.

Platinum containing

cis isomer

Carboplatin

oxalate containing ligand

Oxaliplatin

six ligands (4 chlorides, 1,2-diamino cyclohexane)

Ormaplatin

much less common with CARBOPLATIN compared with Cisplatin

Nephrotoxicity

used in combination with Bleomycin and Vinblastine for metastatic testicular tumor

Cisplastin

For promyelocytic leukemia Produces DNA fragmentation characteristic of apoptosis

Arsenic trioxide

What is the active form of Arsenic trioxide

dimethyl arsenic acid

100

Complexes with the IRON portion of the subunit

Hydroxyurea

Cell structure.

Cell structure.

28問 • 2年前

Quinn Karylle Fuentes · 29問 · 2年前

Electrolytes and non electrolytes

Electrolytes and non electrolytes

29問 • 2年前

Quinn Karylle Fuentes · 38問 · 2年前

POST LAB (EXP 4)

POST LAB (EXP 4)

38問 • 2年前

Density and specific gravity

Density and specific gravity

Quinn Karylle Fuentes · 18問 · 2年前

FORCES OF ATTRACTION

FORCES OF ATTRACTION

18問 • 2年前

Quinn Karylle Fuentes · 63問 · 2年前

Microbial growth

Microbial growth

63問 • 2年前

Quinn Karylle Fuentes · 61問 · 2年前

Introduction.

Introduction.

61問 • 2年前

Quinn Karylle Fuentes · 97問 · 2年前

Microbial control.

Microbial control.

97問 • 2年前

Quinn Karylle Fuentes · 100問 · 2年前

States of matter

States of matter

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Quinn Karylle Fuentes · 86問 · 2年前

Introduction.

Introduction.

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Quinn Karylle Fuentes · 77問 · 2年前

Drug development.

Drug development.

77問 • 2年前

Quinn Karylle Fuentes · 9問 · 2年前

CGMP

CGMP

9問 • 2年前

Quinn Karylle Fuentes · 24問 · 2年前

Pharmaceutical ingredients.

Pharmaceutical ingredients.

24問 • 2年前

Quinn Karylle Fuentes · 43問 · 2年前

Powdered & granules

Powdered & granules

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Quinn Karylle Fuentes · 24問 · 2年前

Capsule.

Capsule.

24問 • 2年前

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Tablets.

Tablets.

23問 • 2年前

Quinn Karylle Fuentes · 3回閲覧 · 66問 · 2年前

Calculatiom of dose

Calculatiom of dose

3回閲覧 • 66問 • 2年前

Quinn Karylle Fuentes · 29問 · 2年前

Postlab 5&6

Postlab 5&6

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Quinn Karylle Fuentes · 33問 · 2年前

COLLIGATIVE PROPERTIES.

COLLIGATIVE PROPERTIES.

33問 • 2年前

Quinn Karylle Fuentes · 69問 · 2年前

SEMI SOLID

SEMI SOLID

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Quinn Karylle Fuentes · 60問 · 2年前

Basic immunology

Basic immunology

60問 • 2年前

Quinn Karylle Fuentes · 62問 · 2年前

Basic immunology (2)

Basic immunology (2)

62問 • 2年前

Quinn Karylle Fuentes · 44問 · 2年前

Transdermal

Transdermal

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Quinn Karylle Fuentes · 43問 · 2年前

Distribution.

Distribution.

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Quinn Karylle Fuentes · 65問 · 2年前

Infectious disease.

Infectious disease.

65問 • 2年前

Quinn Karylle Fuentes · 79問 · 2年前

Infectious diseases (2)

Infectious diseases (2)

79問 • 2年前

Gram positive ( Bacteriology)

Gram positive ( Bacteriology)

All topic. ( Compressed.)

All topic. ( Compressed.)

Quinn Karylle Fuentes · 30問 · 2年前

All topic ( Compressed)

All topic ( Compressed)

30問 • 2年前

Quinn Karylle Fuentes · 13問 · 2年前

All topics (compressed)

All topics (compressed)

13問 • 2年前

Quinn Karylle Fuentes · 28問 · 2年前

Exercise 6 ; Isotonic solution.

Exercise 6 ; Isotonic solution.

28問 • 2年前

Quinn Karylle Fuentes · 16問 · 2年前

Exercise 5 : Buffers.

Exercise 5 : Buffers.

16問 • 2年前

Quinn Karylle Fuentes · 26問 · 2年前

Exercise 7 : Factors affecting solubility.

Exercise 7 : Factors affecting solubility.

26問 • 2年前

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Experiment 8: Disintegration.

Experiment 8: Disintegration.

23問 • 2年前

Experiment 9 ; Interfacial phenomenon and surface tension.

Experiment 9 ; Interfacial phenomenon and surface tension.

EXP 9 : Aromatic ammonia spirit.

EXP 9 : Aromatic ammonia spirit.

EXP 10-11 : CAMPHOR WATER AND CINNAMON WATER.

EXP 10-11 : CAMPHOR WATER AND CINNAMON WATER.

Quinn Karylle Fuentes · 20問 · 2年前

EXP 12: ACACIA MUCILAGE

EXP 12: ACACIA MUCILAGE

20問 • 2年前

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EXP13&14 : Starch and Barrium sulfate.

EXP13&14 : Starch and Barrium sulfate.

33問 • 2年前

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EXP 15 : Liquid petroleum emulsion 1.0

EXP 15 : Liquid petroleum emulsion 1.0

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EXP 15: Liquid petroleum emulsion 1.1

EXP 15: Liquid petroleum emulsion 1.1

23問 • 2年前

Enterobacteriaceae

Enterobacteriaceae

Quinn Karylle Fuentes · 28問 · 2年前

Enterobacteriaceae.

Enterobacteriaceae.

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Quinn Karylle Fuentes · 31問 · 2年前

LIQUID DOSAGE FORM 1.0

LIQUID DOSAGE FORM 1.0

31問 • 2年前

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Liquid dosage form

Liquid dosage form

12問 • 2年前

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MICROMERITICS 1.0

MICROMERITICS 1.0

44問 • 2年前

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EXP 7 : ENDOGENOUS AND EXOGENOUS MICROORGANISMS

EXP 7 : ENDOGENOUS AND EXOGENOUS MICROORGANISMS

22問 • 2年前

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EXP 8 : KIRBY-BAUER TECHNIQUE

EXP 8 : KIRBY-BAUER TECHNIQUE

40問 • 2年前

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EXP 9: STAPHYLOCOCCI

EXP 9: STAPHYLOCOCCI

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Drug incompatibilities.

Drug incompatibilities.

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Drug compatibilities.

Drug compatibilities.

41問 • 2年前

BACTERIOLOGY 3

BACTERIOLOGY 3

Quinn Karylle Fuentes · 30問 · 2年前

BACTERIOLOGY 3

BACTERIOLOGY 3

30問 • 2年前

SUSPENSION.

SUSPENSION.

Quinn Karylle Fuentes · 40問 · 2年前

Colloidal.

Colloidal.

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BACTERIOLOGY 4 (Rickettsia)

BACTERIOLOGY 4 (Rickettsia)

38問 • 2年前

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BACTERIOLOGY.

BACTERIOLOGY.

44問 • 2年前

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Emulsion.

Emulsion.

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EMULSION

EMULSION

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MEDICAL RELATED PROBLEMS.

MEDICAL RELATED PROBLEMS.

36問 • 2年前

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MEDICATION RELATED PROBLEMS.

MEDICATION RELATED PROBLEMS.

33問 • 2年前

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Mycology.

Mycology.

30問 • 2年前

Mycology 2.0

Mycology 2.0

Quinn Karylle Fuentes · 15問 · 2年前

15問 • 2年前

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ppr

ppr

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MEDICAL DEVICES.

MEDICAL DEVICES.

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Pharmacokinetics. (1.0)

Pharmacokinetics. (1.0)

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Pharmacokinetics (1.1)

Pharmacokinetics (1.1)

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Pharmacokinetics (1.2)

Pharmacokinetics (1.2)

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Introduction.

Introduction.

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Introduction of biochemistry

Introduction of biochemistry

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Intro medicanal chemistry.

Intro medicanal chemistry.

56問 • 2年前

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Carbohydrates

Carbohydrates

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Carbohydrates 1.1

Carbohydrates 1.1

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Detect and quality variation.

Detect and quality variation.

56問 • 2年前

Quinn Karylle Fuentes · 98問 · 2年前

INTRODUCTION

INTRODUCTION

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lab (1-2)

lab (1-2)

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Quinn Karylle Fuentes · 14問 · 2年前

lab 1-2

lab 1-2

14問 • 2年前

Pharmaceutical chemistry.

Pharmaceutical chemistry.

Pharmaceutical chemistry 1.1

Pharmaceutical chemistry 1.1

Quinn Karylle Fuentes · 39問 · 2年前

Unit 3.

Unit 3.

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Histamin and kinins

Histamin and kinins

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PUD.

PUD.

Quinn Karylle Fuentes · 61問 · 2年前

61問 • 2年前

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Lipids.

Lipids.

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lipids.

lipids.

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LAB ✨

LAB ✨

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Drug discovery.

Drug discovery.

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disease of lipids.

disease of lipids.

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Intro (identify structure)

Intro (identify structure)

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Carbohydrates

Carbohydrates

98問 • 2年前

Quinn Karylle Fuentes · 96問 · 2年前

Dynamic.

Dynamic.

96問 • 2年前

Quinn Karylle Fuentes · 32問 · 2年前

Unit 1

Unit 1

32問 • 2年前