Cancer

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5-HT3 Antagonist

IND: Naus, Vom. MOA: Act in CTZ and peripheral gut on serotonin receptors. DI: QT prolonging agents, apomorphine, aripiprazole, tramadol, serotonergic drugs (serotonin syndrome). OTH: Aka setrons.
dolasetron: OTH: Taken off market.
granisetron:


ondansetron=Zofran: AVL: Avail IV or PO. IND: Chemo induced N + V. MOA: Blocks 5-HT3 receptor. AE: HA11%, C4%, D, dizziness, flushing/warmth<1%, bradycardia, known QT prolongation. PK: 3A4 substrate. DOS: T 30min before chemo and up to 5d after.
palonosetron:

 

Anti-Androgens

abiraterone=Zytiga: IND: Metastatic prostate cancer. MOA: CYP17 inhibitor (enzyme in adrenal glands, testes, and prostate tumor). ADM: T on empty stomach (food increases F). AE: D, HTN, decreased K, fluid retention, hepatotoxicity, cardiotoxicity, joint swelling, UTI. PRG: CI. PK: t1/2=12h. Prodrug to aberaterone. Met by 3A4 (major). Inhibits PGP, 1A2, and 2D6. DOS: 1g po daily + 5mg prednisone BID. OTH: T w/ prednisone because of excess aldosterone and cortisol.

 

Antiemetics

aprepitant=Emend: AVL: PO. IND: Chemotherapy induced N/V. MOA: NK1 inhibitor. Binds to substance P in the brainstem and GI tract. AE: Fatigue, D, dizziness, dyspepsia, hiccups. DI: Warfarin, COCs. PK: F=60-65%. Moderate 3A4 inhibitor, 2C9 inducer, 3A4 substrate. OTH: Not used alone.


domperidone: AVL: PO, IV, SubQ. DOS: 5-20mg TID – QID before meals.


metoclopramide: AVL: PO, IV, SubQ. DOS: 5-20mg TID–QID before meals.
PHENOTHIAZINES

chlorpromazine: AVL: PO. DOS: PO:10-50mg q4-6h.


prochlorperazine: AVL: Avail PO, IV, IM, PR. IND: Chemo induced N + V. MOA: Blocks DA in chemo receptor trigger zone.
AE: Sedation, anticholinergic effects, hypotension, hypersensitivity rxn. DOS: 5-10mg q6-8h prn. OTH: Also classified as a first gen antipsychotic.


promethazine: AVL: PO, IM, IV, PR. DOS: 12.5-25mg q4-6h prn

 

Aromatase Inhibitors (AIs)

Non-Steroidal

anastrazole: IND: Estrogen positive breast cancer. MOA: Blocks aromatase which converts androgens to estrogens. EVD: Only AI that won’t affect lipids. AE: N, hot flashes, HA, bone loss, increased cholesterol, swelling in hands and feet. PK: t1/2=41h. Inhibits 1A2, 2C9, 3A4.


letrozole: IND: Estrogen positive breast cancer. PK: t1/2= 2-4d. Strong inhibitor of 2A6 and moderate for 2C19.
Steroidal

Exemestane: IND: Estrogen positive breast cancer. AE: Weight gain, acne. PK: t1/2=27h.

 

Corticosteroids

dexamethasone=Decadron: AVL: IV, IM, PO. IND: Chemotherapy induced N + V (increases effect of ondansetron.).
ADM: T w/ food. AE: fluid retension, thrush, bone loss, cataracts, indigestion, muscle weakness, back pain, bruising, increased glucose, weight gain, insomnia. PRG: FDA cat C. PK: Induces and metabolized by 3A4. Duration=3d.

 

Gonadotropin-Releasing Hormone (GnRH) Agonists

Aka LH releasing hormone agonist.

goserelin=Zoladex: AVL: SubQ biodegradable implant. IND: Breast and prostate cancer. MOA: Produces sex hormones in a non-pulsatile manner that disrupts feedback mechanism. AE: N, stop in periods, hot flashes, dizziness, HA, sweating, sexual dyfunction, change in breast size, vaginal dryness, hair loss. Hormone levels will increase in first few weeks causing increased pain, increased difficulty urinating in men. PRG: CI. PK: t1/2=4.2h. DOS: Max=3.6mg q4w x 6 months.

 

Prokinetics

metoclopramide: AVL: PO, IM, SubQ, IV. IND: Chemo induced N + V. MOA: Blocks D2 in the chemo trigger zone. Increases gastric emptying rate. AE: D, sedation, insomnia, EPS in children (CI<1yo). PRG: Used in all stages. LAC: Used (<45mg/d). DOS: Should not exceed 0.5mg/kg/d. Adj dose if CrCl<50.

 

Selective Estrogen Receptor Modulators (SERMs)

tamoxifen=Novaldex: IND: Estrogen receptor positive breast cancer (both pre and post menopause. AE: N, hot flashes, vaginal discharge or dryness, menstrual irregularities, muscle/joint pain, hair thinning, weight loss, possible QT prolongation. CI: Hx of DVT or PE. PRG: CI. LAC: CI. DI: 2D6 inhibition (ex. antidepressants) will stop metabolism to prodrug 4-hydroxytamoxifen. PK: t1/2= 5-7d. F=100%. DOS: 20mg/d x 5 years.

 

Tyrosine Kinase Inhibitors

imatinib: AVL: PO. IND: CML. PK: t1/2=18h. F=98%. Metabolised and inhibits 3A4/5.

 

AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH:
AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH:


AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH:


AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH:


AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH:


AVL: IND: MOA: EVD: ADM: AE: CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: OTH: