Microtubule inhibitors/ plant alkaloids Flashcards
What ae the Microtubule ihibitors/plant alkaloids?
- Docetaxel
- Eribuln
- Etoposide
- Irinotecan
- Paclitaxel
- Vincristine
- Vinorelbine
What is the mechanism of action of docetaxel?
Disrupts microtubular network needed for cell division
Promotes tubulin assembly into stable microtubules and inhibits their disassembly - this means they are stabilised and inhibits mitosis
What is the distribution of Docetaxel?
PPB >95%
How is Docetaxel metabolised?
PY450-3A enxymes
Inactive metbolites only
How is Docetaxel eliminated?
Bile and faeces
What is the half life of docetaxel?
11 hours
What are the indications for docetaxel?
- Breast
- NSCLC
- Ovary
- Prostate
- H&N
What adverse effects are associated with docetaxel?
- Hair loss
- Nail loss
- Rash
- Diarrhoea
- Mucositis
- Nausea and vomiting
- Fatigue
- Fluid retention
- Nueropathy
- Hypersensitivity - give steroids
What drusg does docetaxel interact with?
- CYP3A4 inhibitors and acitvatiors
What is the mechanism of action of Eribulin?
Supresses polymerisation of microtubules and sequesters tubulin intononproductive aggregates
G2/M block
From halichrondin B
How is eribulin distributed?
65% PPB
How is Eribulin metabolised?
isn’t
How is eribulin eliminated?
Faeces
What is the half-life of eribulin?
40 hours
What are the indications for Eribulin?
- Breast
- Liposarcoma
What are the adverse effects of eribulin?
- Hair loss
- Constipation/diarrhoea
- N&V
- LFTs
- Neuropathy
What drugs does eribulin interact with?
- Prolong QT
- Upset electrolytes
What is the mechanism of acion of Etoposide?
- ssDNA breaks
- Ihibits topoisomerase II
S and G2 phase
What is the asorption of Etoposide?
50% oral bioavailability
How is Etoposide distributed?
95% PPB
Extensive distribution in saliva, liver, spleen, kidneys, heart, brain
How is Etoposide metabolised?
p450 - CYP3A4
How is etoposed eliminated?
50% urine
What is the half life of etoposide?
11 hours IV
6.8 hours PO