Quiz 3 flash cards
What ways can a drug be transported into a cell?
Diffusion
Facillitated diffusion
Active transport
What charactoristics make dissolution the late limiting step of drug metabolism?
Solubility of drug Size of particle Surface area Crystalline and salt drug formation Rate of disintegration
What are the charactoristic of pH-partiition for drug absorption?
Biological membranes act like lipid barriers
Un-ionized forms of drug is better absorbed
Most are absorbed by passive diffusion
rate and amount of drug absorption are related to oil-water partition coefficent
Weak acids and neutral drugs not usually absorbed in the stomach
Basic drugs are normally absorbed in the stomach
What are the hallmarks of cancer?
Sustained proliferative signaling Evading growth suppressors Activating invasion/metasis Enable replicative immortality Induce angiogenesis Resisting cell death
What is the molecular target for Mustard agents?
DNA
What is the MOA of Mustard agents?
Alkylate and crosslink the DNA
What type of cancer are Mustard agents used for?
Multiple
What is the molecular target of Mytomycin C?
DNA
What is the MOA for Mytomycin C?
Alkylate and cross link DNA
What type of cancer does Mytomycin C treat?
Stomach and Intestinal Cancer
What is the molecular target for Platinum Drugs
DNA
What is the MOA of Platinum drugs?
Alkylate and cross link DNA
Can alkylate the protein in the protein-DNA crosslink
What is the molecular target for Anthracyclins?
Topo 2a
What is the MOA for Anthracyclin?
Stabilizes transient cleavage complex with DNA
What cancers are treated with Anthracyclin?
Breast, endometiral, acute leukemia, cervical, stomach, lymphoma
What is the molecular target for Etoposide?
Topo 2A
What is the mechanism of action for Etoposide?
Stabilizes transient cleavage complex with DNA
What cancers are treated with Etoposide?
Lung and Testicular
What are the molecular target of ICRF-193?
Topo 2A and chelate iron preventing ROS production
What is the MOA of ICRF-193?
Stabilized closed clamp complex with DNA
What is the molecular target of Imatinib?
BRC-ABL
What is the MOA of Imatinib?
Competitive BCR-ABL inhibitor- makes ABL inactive
What cancers can be treated by Imatinib?
Mainly leukemia ALL,CEL,CML
What is the molecular target for Dasatinib?
BCR-ABL
What is MOA of Dasatinib?
Binds to active ABL
What cancers can be treated by Dasatinib?
Imatinib resistant Leukemia and Philadelpha chromosome positive
What is the clinical significance of statins?
Lower LDL and sometime increase HDL cholesterol
How do statins work?
They mimic the transition state Mevaidyl-CoA
Which statins are natural products?
Compacitin and Simvastatin
Which statins are SYnthetic products?
Fluvastatin, atorvastatin, rosuvastatin, cerivastatin
What charactorist to all statins have in common?
They have HMG-like functional groups
