Drugs 'n Dat an' dere effects. Innit. Flashcards
Don't get stir crazy.
Describe action of penicillin
Bacterial Cell Wall
Inhibits transpeptidase enzyme that forms cross-links in cell wall. Osmotic pressure causes cell lysis
Describe action of Rifampicin
Bacterial Transcription
Binds to bacterial RNA Polymerase preventing transcription.
Describe action of tertcycline
Bacterial Protein Synthesis
Competes with tRNA at A site of bacterial ribosome.
Describe action of methtrexate
Anti-Folates in Cancer Therapy
Impairs the synthesis of tetrahydrofolate, which is essential for DNA synthesis, from folic acid. Competitively inhibits dihydrofolate reductase (DHFR)
Give ways in which cells can become resistant to antibiotic or drug
High rate of division Decreased influx Increased efflux Increased transcription of target Altered target
Describe high rate of division
High rate of division in both bacteria and cancer cells means that there is a higher rate of mutation.
Positive mutations, such as drug resistance will be positively selected for and breed a population of drug resistant cells.
Describe how decresed influx works?
For drugs, which require to be taken up by their target cells to take effect (Rifampicin, Tetracycline, Methotrexate), influx can be reduced.
Cells achieve this by expressing a reduced amount or altered version that reduces affinity of the carrier protein that allows the drug through the cell membrane.
Describe how increased efflux works
P-Glycoprotein, or Multi-Drug Resistance Protein 1 (MDR1) is a protein similar in structure to CFTR that is responsible for the efflux of toxic products from a cell.
In many cancers, expression of P-Glycoprotein is up-regulated. This allows the cells to increase the efflux of chemotherapy drugs, eg Methotrexate.
Describe how increased transcription of target works
If the drug targets a specific product of transcription, eg a ribosome or enzyme, the cell can acquire resistance by increasing the transcription of the target to overwhelm the drug
Describe how altered target works
Specific target of drug acquires a mutation, lowering the affinity of the drug for it.