Microtubule inhibitors Flashcards
What are the classes of drugs in the Microtubule inhibitors category ?
Vinka alkaloids and taxens which inhibit mitosis.
What is the structure and function of the cytoskeleton of the cell ?
It is a network consisting of actin filaments, intermediate filaments, and microtubules. It gives the cells their shape and anchors organells in place and responsible for conformational changes.
What is the structure of microtubules ?
It is a cluster of 13 protofilaments each containing alternating chain of alpha and beta tubulin.
what are the steps of mitosis ?
- Prophase- nuclear membrane disintegration and chromosome condensation occurs.
- Metaphase- Formation of metaphase plate.
- Anaphase- centrosome mediated separation of cistocromatides occurs resulting in the formation of mitotic spindle.
- Telophase- Formation of new nuclear membrane around the each pairs of 46 chromosomes. leading to cytokinesis.
All Microtubule inhibitors are given ______
IV
What are the drugs in the vinka alkaloid class of medications ?
Vincristine and Vinblastine .
What is the MOA of vinka alkaloids ?
They are metaphase specific drugs that bind to beta tubulin and block its polymarization into proto- filaments leading to mitotic arrest at metaphase.
What are the indications for vinka alkaloids ?
They are indicated for the Tx of breast cancer, rhabdomyosarcoma, nephroblastoma and leukaemias.
Vincristine and Vinblastine are both indicated for the treatment of both ——– and ————lymphoma.
Hodgkins and non-hodgkins.
What are the side effects of vinka alkaloids ?
Alopecia, GI symptoms and bone marrow supression. Vincrestine is myelotoxic whereas vinblastine is more neurotoxic.
What are the neurotoxic effects of vinblastine ?
- peripheral neuropathy.
- Dysautonomia
- Urinary retention
- Constipation
What are the drugs belonging to the class of Taxanes?
Pacletaxel and Docetaxel.
What is the MOA of Taxanes ?
They act by directly hyper-stabilising cistochromatids leading to inhibition of the progression of mitosis from metaphase to anaphase.
What is the indication of Taxanes ?
Tx of solid tumours.
What are the side effects of Taxanes ?
- Alopacia
- Myelosuppression
- Neurotoxicity.
- Infusion HSR.