Chemotherapeutic agents
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- Опубликовано: 10 июн 2024
- This is a brief overview of chemotherapeutic agents, their mechanism of action, and some related side effects.
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ADDITIONAL TAGS:
Chemotherapeutic agents
Classes of chemical agents used in the treatment of cancer
Alkylating agents
Antimetabolites
Microtubule targeting agents
Topoisomerase inhibitors
Anthracyclines
Monoclonal antibodies
Other agents
Alkylating agents
Attach alkyl groups to DNA, allows cross linking of base pairs, damaging DNA; cell cycle nonspecific
Typical alkylating agents: cyclophosphamide, ifosfamide, melphalan, busulfan, mechlorethamine, chlorambucil, thiotepa
Side effects: myelosuppression drop in WBC, Hb, crit, nausea/vomiting, secondary malignancies, infertility/impaired fertility, hemorrhagic cystitis hematuria, dysuria from direct irritation of bladder by acrolein metabolite
Atypical alkylating agents
Platinum compounds covalently bind purine DNA bases. Drugs and side effects:
cisplatin causes nephrotoxicity and n/v
carboplatin causes thrombocytopenia
oxaliplatin causes cold sensitivity
all cause peripheral neuropathies, paresthesia
Nitrosoureas: BCNu, CCNu both cause pulmonary toxicity, phlebitis. CNS
Alkylating agents
Antimetabolites
Microtubule targeting agents
Topoisomerase inhibitors
Anthracyclines
Monoclonal antibodies
Other agents
Antimetabolites
Inhibit DNA replication or repair by mimicking normal cell compounds; S phase specific
Folate inhibitor: Methotrexate inhibits DHFR, prevents regeneration of THF
Adjuvant leucovorin to protect healthy cells adjuvant
Side effect is mucositis, myelosuppression
Pyrimidine inhibitors
5-fluorouracil inhibits thymidylate synthetase
Bolus dose causes myelosuppression
Continuous dose causes GI problems mucositis, diarrhea
Synergistic leucovorin potentate mechanism of action synergistic
Capecitabine is essentially an oral prodrug for 5-FU
Side effect: hand-foot syndrome - palms and hands and feet become red, can start blistering
Cytarabine AraC is a DNA chain terminator
Side effects: conjunctivitis and cerebellar neural defects
The 7 in 7+3 chemotherapy
Purine analog is 6-mercaptopurine
Alkylating agents
Antimetabolites
Microtubule targeting agents
Topoisomerase inhibitors
Anthracyclines
Monoclonal antibodies
Other agents
Microtubule targeting agents
These drugs inhibit mitosis, specifically M phase
Vinca alkaloids destroy microtubules, obviously preventing their function
Vincristine, vinblastine, and vinorelbine
Side effects: peripheral neuropathy, myelosuppressive blast others
Fatal if given intrathecally
Taxanes stabilize microtubules, preventing their function
Paclitaxol, docetaxol
Side effects: myelosuppression, peripheral neuropathies
Hypersensitivity
from diluent: Cremophor diluent in paclitaxel Tween80 in docetaxel
Avoid hypersenitivity with abraxane, protein-bound paclitaxol particles
less sensitivity but more neuropathy
Topoisomerase inhibitors
Topoisomerase I inhibitors prevent relaxation of supercoiled DNA
Topotecan, irinotecan
Both have side effect of myelosuppression
Irinotecan causes diarrhea: “I ran to the canâ€
Topoisomerase II inhibitors prevent recoiling of DNA after transcription
Etoposide, teniposide
Both have side effects of myelosuppression, mucositis, secondary malignancies AML
Etoposide also causes hypotension
Anthracyclines
Various mechanisms of action: intercalate DNA, inhibit topo II, generate ROS, perhaps alkylation
-rubicins: doxorubicin, daunorubicin, idarubicin, epirubicin
Side effects: biventricular heart failure, necrotic with extravasation
The 3 in 7+3 chemotherapy
Monoclonal antibodies
Origin determined from suffixes: -omab from mouse; -ximab is chimeric cross between human/mouse; -umab is humanized; -mumab is fully human
mAb
Target
Treats:
Toxicity
Rituximab
CD20
lymphoma
-
Trastuzumab
Her-2
breast cancer
-
Cetuximab
EGFR
solid tumors initially for colorectal cancer
Acneiform rash
Bevacizumab
VEGF
solid tumors initially for colorectal/lung cancers
GI perforation,
Other chemotherapeutic agents
Bleomycin causes lung toxicity
Side effects: pulmonary fibrosis, interstitial pneumonitis, hypersensitivity pneumonitis cough, infiltrates
Hormonal therapies
Antiestrogens block estrogen stimulation of breast cancer
Tamoxifen, fulvestrant, megestrol acetate
Aromatase inhibitors block synthesis of estrogen
Anastrozole, letrozole
Antiandrogens block androgen stimulation of prostate cancer
Other targets for prostate cancer are LHRH agonists prevent testosterone production, GnRH antagonist, CYP17 inhibitor
Excellent
So helpful, as I study for the OCN exam. Glad these videos are available even 7 yrs later. Thank you so much!
Did you take the OCN yet
SO incredibly grateful for this lecture!!!!
Thank you! This helped me a lot, best video on RUclips about Cytostatics in my opinion.
Hey man i just want to thank you for doing these videos, they are great and keep it up! You are awesome!
Oh thank goodness! Finally - something that actually makes sense. Thank you!
as an oncology nurse, truly enlightening, very informative!! Thanx a lot ^^
this was very helpful thank you for this overview!
1:52, hemorrhagic cystitis is not a problem with the kidneys, it's a problem with the bladder. ie it is a "cystitis" not a "nephritis. Happens (as you have mentioned) because of the acrolein metabolite formed from cyclophosphamide metabolism. Acrolein is toxic to the bladder and so causes inflammation and bleeding inside the/of the bladder.
Absolutely right. He goofed that
I too going to say
Kidneys are also affected by cyclophosphamide. That is why sodium-2-mercapto-ethane-sulphonate also known as MESNA is given to protect the kidneys from acrolein. Also, a lot of water is given to dilute the urine and thus lower the probability of contact between the cells and acrolein on its way out of the body.
You're a genius. Helped me a lot thanks
Thank you so much. these are well summarised and easy to remember
i want you
Nice job. Thank you for the information. Video is very helpful.
I love love love this! Thanks a wholllleeee lot ❤
it was really helpful , thank you so much.
Thank you very much for this helpful video....
helpful video.
million thanks.
this has been really helpful, thank you so much akh
thank u so much amazing video and very helpful.
thank you so much for making this video
Great lec, very clear
great work
Thank you so very much!
Great presentation!! Are the slides available somewhere?
great work!
Thank you for the review.
Please where will get videos/slides on sulpfonamides and the rest
Just as a quick correction: 7+3 is Cytarabine IV continuous infusion over 24 hours for Days 1-7, and the anthracycline IV bolus for Days 1-3. It's not a total of 10 days, only a total of 7.
Saline Xiang 6tz l killjoy
thanks bro , in my final exam today I just saw this video and I could get at least 5 marks !
Wow Thank You so much, this is really helpful.
Very helpful! Thank you
A very good summary, need more of ur documents
ruclips.net/video/Y6Dex_8SQZc/видео.html
thank you !
Thank you so much.
Thank you , it helped
Amazing👌
GREAT VIDEO ..ANY CHANCE CAN GET THE SLIDES FOR STUDYING ?
excellent overview!
Lilia C.
This is a pretty helpful summary...thanks!
Mehdi Hedjazi
Mehdi Hedjazi 我
个哦哦都
这
月
Thank you
its really helpful. 😄
Thanks man 🙏
Excellent!
Mayo Mayo
I have polycythaemia vera and klinefeltersyndrome
I love this
What's "crit" in minute 1:40? is this short for platelets?
and what about thalidomide?
I think hematocrit
MahaAlJabri makes sense, thanks!
Thank you...this video is very helpful
Not bad for a start
LIFE SAVERRR!!!
Great overview. The monoclonal antibodies need an update. Humanized Abs are called -zumab ie trastu-zumab (Not -umab) and still have a few percent mouse.
While the fully 100% human Abs are -umabs ipilim-umab and nivol-umab (not mumabs)
Doctors...You guys are awesome, I love you, you're smart as fuck and we wouldn't be here without you. Every single one of you deserves a reward. But, y'all really suck at pronouncing chemicals and functional groups sometimes hahah
Sincerely, A chemist.
I ran to can was epic😂
Cer - A -BELL- AR not cerebral
Cerebellar
What do babies new bod look like when the body cell aae normal? why is Pharam no paying for thsing tretamet tat have been provne to be a quinetitive live supot but detioting bodies imminity can caused the patinet to died fater and not cost efective it is a bdue if not poeply diagnsed patient right I suggets the patient cna tell if they wnat to be the heo to put themsleve as agney pig buyt a bi hsiul be pass for pamacetucla pay or papteint to used trial meidation so malies dont loose tehir jobs and homes
Why are you in such a hurry :P
this is sick and evil im never getting chemo if i get cancer
every body thinks like you but if there is this diagnosis.....every one wants to live....no matter how....
It all depends on how much you are willing to go through in order to extend your life expectancy. If you get a terminal diagnosis, perhaps you would rather have a single year with a relatively high quality of life, but if you are a young person, accepting that your will die within such a short time may be more difficult, and you may be more motivated to go through a tougher treatment, in hopes that you can beat the cancer back into remission. It's all a matter of priorities, also one should never forget, that cancer itself often causes many of the same symptoms that many cancer treatments cause, so in some cases, a milder treatment may allow you to live a much more comfortable life, because the cancer is kept down a bit, although the treatment may not prevent it from spreading further. It's not an always a question of all or nothing, treatment or no treatment - it can be a matter of which treatment, and for how long etc.
Excellent