COMPLETED - OTC, Asthma/COPD, DM, Chemo

Cell-Cycle Specific Chemotherapy Agents

• Which two major classes of chemotherapy agents are cell-cycle independent?

• Which specific drug class targets the S-phase (DNA synthesis and replication)?

• Which specific drug class targets the G2 phase?

• Which two specific drug classes target the M-phase (mitosis)?

Anzemet

• What is the generic name?

• What is the class?

• Indication

• What toxic effect makes the IV formulation contraindicated?

Dolasetron

• 5-HT3 receptor antagonist

• For chemo induced N/V, only PO

• QTc prolongation (contraindicated for CINV)

Sancuso

• Generic, class

• What is the specific dosage form? Generic also comes in what other formulations

• What is its duration of action? Use how long before chemo

• What is the key environmental counseling point for patients?

Granisetron (5-HT3 receptor antagonist)

• Transdermal patch (granisetron also comes IV, SQ, PO)

• 7 days, 24-48 hrs before chemo

• Avoid sun exposure to the patch site

Zofran, Zuplenz

• What is the generic name?

• What is the pharmacologic class?

• What is the primary clinical indication?

• What is the unique delivery system for Zuplenz?

• What is the absolute maximum single IV dose limit due to

Ondansetron

• 5ht3 receptor antagonist

• Chemotherapy-Induced Nausea and Vomiting (CINV)

• Zuplenz: Oral soluble film (thin strip)

• Also comes oral, ODT, IV

• 16 mg, QT prolongation

Aloxi

• What is the generic name, pharmacologic class, and primary clinical indication?

• Why is this specific agent preferred if a clinician is concerned about cardiac conduction toxicities?

• What unique pharmacokinetic parameter differentiates it from other agents in its class?

Palonosetron; 5HT3 receptor antagonist; Chemotherapy-Induced Nausea and Vomiting (CINV)

• It does not carry the high risk of QTc prolongation seen with other class agents

• A remarkably long half-life (36-48 hrs)

Akynzeo (→ generic)

Netupitant + palonosetron

(NK1 antagonist + 5HT3 antagonist)

Decadron

Medrol

in chemo

Steroids used alone or without 5HT3 antagonist for CINV

Dexamethasone (Decadron)

Methylprednisolone (Medrol)

PO Emend

• What is the generic name, pharmacologic class, and primary clinical indication?

• What is the unique mechanism of action of this class?

• What major CYP enzyme does this drug inhibit, requiring a dose reduction of what other med indicated for CINV?

Aprepitant; Neurokinin-1 (NK1) receptor antagonist; Chemotherapy-Induced Nausea and Vomiting (CINV)

• Blocks substance P from binding to NK1 receptors in the central nervous system

• CYP3A4 inhibitor, dose reduction of co-administered dexamethasone

Emend IV

• What is the generic name, pharmacologic class, and primary clinical indication?

• What is the structural relationship between this drug and aprepitant?

Fosaprepitant; Neurokinin-1 (NK1) receptor antagonist; Chemotherapy-Induced Nausea and Vomiting (CINV)

• It is an IV prodrug of aprepitant

Varubi

• What is the generic name, pharmacologic class, and primary clinical indication?

• Unlike aprepitant, this med does not inhibit CYP3A4, but it is a strong inhibitor of which different CYP enzyme?

• What is the unique

Rolapitant; Neurokinin-1 (NK1) receptor antagonist; Chemotherapy-Induced Nausea and Vomiting (CINV)

• CYP2D6 → caution with Tamoxifen (prodrug requires activation through CYP2D6)

• long t1/2

Marinol, Syndros

• What is the generic name, pharmacologic class, and primary clinical indication (2)?

• What is the federal controlled substance schedule and formulation?

• What are the specific storage requirements

Dronabinol; Cannabinoid; Chemotherapy-Induced Nausea and Vomiting (CINV) (and anorexia/weight loss in AIDS)

• Marinol is Schedule III; Syndros is Schedule II

• Marinol capsules versus Syndros oral solution

• Must be refrigerated

Cesamet

• What is the generic name, pharmacologic class, and primary clinical indication?

• What is the federal controlled substance schedule for this specific agent?

• What is the primary storage requirement for this medication?

Nabilone; Cannabinoid; Chemotherapy-Induced Nausea and Vomiting (CINV)

• Schedule II

• Store at room temperature (does not require refrigeration)

Reglan

• What is the generic name, pharmacologic class, and primary clinical indication?

• What black box warning is associated with chronic or high-dose use of this medication?

• What neurological side effects can occur due to its mechanism

Metoclopramide; Dopamine receptor antagonist; Chemotherapy-Induced Nausea and Vomiting (CINV) (and gastroparesis)

• Tardive dyskinesia (often irreversible involuntary movements)

• Dystonic reactions and parkinsonism; manage with diphenhydramine

Benadryl

Vistaril

in CINV

Ativan in CINV

Zyprexa in CINV

Olanzapine

Atypical antipsychotic used off-label for CINV

Summary of CINV tx medications

PO vs IV timing with chemo

First line

First line: 5-HT3 blockers and/or steroids

Then NK1 receptor blocker

Chemo induced anemia treatment

Epogen, Procrit, Retacrit

Aranesp

• What are the generic names, pharmacologic class, and three primary clinical indications for this class?

• What is the critical prognostic restriction regarding the intent of chemotherapy for using ESAs in cancer patients?

• What cardiovascular and tumor-related toxicities require monitoring, and what five lab values must be checked?

• What are the storage requirements, physical appearance rules, and the room-temperature stability limit for erythropoietin?

Can be used in ESRD with HD, zidovudine or chemo induced anemia

Can only be used if chemo does not have cure

Neumega

Generic, indication

thrombocytopenia: low platelets

Neupogen, Granix, Zarxio

• What is the generic name and primary clinical indication?

• What is the critical regulatory distinction between Zarxio and Granix relative to Neupogen?

• What is the primary, classic adverse effect that patients must be counseled on?

• Storage at room temp for how long

Chemo induced leukopenia/neutropenia (low segments/WBC)

just know formulation

Zarxio is an approved biosimilar to Neupogen; Granix is not a biosimilar (approved via a different biological pathway before the framework existed)

Neulasta

• What is the generic name and primary clinical indication?

• What structural modification differentiates this drug from filgrastim, and what is the resulting dosing frequency per chemotherapy cycle?

• Storage

Chemo induced leukopenia/neutropenia (low segments/WBC)

just know formulation and given once per cycle

Tumor lysis syndrome treatment

Allopurinol

PhosLo

Renvela

Amophjel

Kayexalate

Veltassa

Lokelma

-

Hydration + 4 electrolytes

can also use thiazides and loops to remove K+

-

Watch out for drug interaction with allopurinol → 6 mercaptopurine, azathioprine

Renvela with food

Amphojel avoid with CKD

-

Both cause constipation

-

in severe hyperkalemia, IV calcium (calcium gluconate and calcium chloride) is given immediately for cardioprotection in hyperkalemia, regardless of what the baseline serum calcium level looks like

Compounding chemo agents

• Hood certified every…

• Color sharps container

• What are the explicit gloving requirements relative to the gown cuff when handling these agents?

• What type of outer packaging and what exact cautionary statement must be on the label when dispensing these drugs?

• What specific type of hood/cabinet must be used for compounding chemotherapy, and what is its specific airflow pattern?

• Hood ceritified every 6 months

• Yellow sharps container from chemotherapy

• Eye protection and two pairs of gloves; one pair under the gown cuff and the outer glove pulled over the gown cuff

• Dispensed in a Ziploc-type bag; labeled with "Contains Cytotoxic Agent! After use, dispose of properly."

• Vertical flow hood (Class II BSC); vertical unidirectional airflow with no recirculation within the work area to prevent inhalation exposure

Platinol

• What is the generic name, pharmacologic class, and primary clinical indication?

• What are the signature organ toxicities associated with this agent, and what absolute dosing limit protects against them?

• What two agents are used alongside aggressive IV fluids to protect the kidneys, and what physical inspection step is required for one of them?

• What specific material restriction must be observed when preparing the IV administration set for this drug?

Cisplatin; Alkylating agent (platinum analog)

All platins have peripheral neuropathy

Carboplatin

Class

vs Cisplatin

Alkylating agents

Busulfex

Myleran

-

Generic, Class

Formulation

ADE

Pretreatment for what ADE

DDI for what ADE

Alkylating agent

Cytoxen

Ifex

Generic, class

ADE

Protect what organ with what med

Alkylating agents

BiCNU

Gleostine

• What are the generic names, pharmacologic class, and primary clinical indication for these two agents?

• What unique physical property allows these drugs to cross the blood-brain barrier?

• What 4 organ toxicities are characteristic of this drug class?

• What critical compounding/administration restriction?

Alkylating agents

Also bone marrow suppression

Bendamustine

Class

Diluted in…stable in fridge and room temp for how long

ADE and treatment of ADE

Alkylating agent

Methotrexate

Class

Indications

Side effects

Antidotes (Voraxaze)

Anti-metabolites, chemo agent

METHOTREXATE Side Effects

• M: Mucositis

• H: Hepatotoxicity

• O: phOtosensitivity

• R: Renal → keep urine alkaline (use sodium bicarb) and well hydrated to avoid toxicity

• X: Chest-X ray → pulmonary fibrosis, Pregnancy Category X

5-FU

Adrucil: formulation

Efudex 5%: formulation and indication

-

Generic, class

ADE

Coadminister with what to increase efficacy

Anti-metabolite

Adrucil: IV

Efudex 5%: cream for actinic or solar keratosis, superficial basal cell carcinoma

Xeloda

-

Generic, class

ADE

Formnulation, Regards to food/frequency

BBW

Anti-metabolite

PO twice daily within 30 min after meals

BBW: don’t use with warfarain

Mercaptopurine

-

Class

2 drug interactions

Imuran

Generic, class

Prodrug of..,

DDI

Azathioprine, anti-metabolite

Prodrug of mercaptopurine

DDI w/ xanthine oxidase inhibitors (allopurinol and febuxostat

Cytosar

Generic, class

Formulation

Administration

Cytarabine, antimetabolite

Fludarabine

-

Class

FOrmulation

ADE

Antimetabolite

Bleomycin

-

class

ADE

Max lifetime dose

Anti-tumor antibiotics

Adriamycin

-

Generic, class

ADE → Zenicard, Totect

Max lifetime dose

Anti-tumor antibiotics

dont use in preg

Has the most cardiotoxicity (including Mitoxantrone) of the chemo agents

rub → red urine/tears

Valrubicin

ADE

Indication, Formulation

Anti-tumor antibiotic

Dactinomycin

-

Class

Formulation

ADE

CI

Antitumor antibiotic

Avoid inhalation of vapors → toxic

CI with active chicken pox or herpes zoster

Novantrone

-

Generic, class

ADE

Color of urine/tears

Also indicated for

Max lifetime dose

Antitumor antibiotics

Has the most cardiotoxicity (including Doxa/Daunrubicin) of the chemo agents

Chemo agents have peripheral neuropathy

Vinca, Taxels and platins

Taxotere

Formulation

ADe

Premedicate

Docetaxel, Plant alkaloids

IV

ADE

• Hypersensitivity → premedicate with dexamethasone 8 mg BID for 3-5 days; start 1 day prior to chemo

• Hepatotoxicity

• Visual impairment

• Fluid retention

• Peripheral neuropathy

All taxels are premedicated

Taxol

-

Generic, Class

ADE

Plant alkaloids

PAClitaxel

• P =

  • PVC leeches → use non-PVC

  • Peripheral neuropathy

  • Premedicate (dexamethasone, IV diphenhydramine, IV ranitidine or famotidine)

• A= Alcohol containing → disulfiram like reaction with Flagyl

• Castor oil allergy → dont use

All taxels are premedicated

Etoposide → VP 16-PO

Teniposide

-

Class

Infuse over…

VP-16 storage

Plant alkaloids

Camptosar

(Topotecan)

-

ADE and treatment

Plant alkaloids

I ran to the can → diarrhea

Loperamide usually has Rx max dose of 16 mg/d → but not max dose here bc life threatening diarrhea

VinCristine

VinBlastine

VinOrelbine

-

Med specific ADE

All have…ADE

Formulation

Oncovin (→ generic)

Vincristine

Gleevec

Generic, class

Imatinib, tyrosine kinase inhibitor (all PO)

Tarceva

Generic, class

Other MOA

Erlotinib, tyrosine kinase inhibitor (all PO)

Also targets EGFR

Tykerb

Generic, class

Other MOA

Regards to food

ADE

Lapatinib, tyrosine kinase inhibitor (all PO)

Mixed EGFR and ERBB2 (or HER2) inhibitor

Empty stomach

Can cause hand-foot syndrome, 3A4 substrate, diarrhea

Nilotinib

Generic, class

Tasigna, tyrosine kinase inhibitor (all PO)

Erbitux

Generic, class

ADE

Cetuximab

EGFR inhibitor (all IV)

Can cause skin rash

Avastin

Generic, class

Formulation

ADE

Bevacizumab

VEGF inhibitor

IV with NS

Surgery and wound healing complication

Hydrea, Droxia

Generic

Also indicated for outside of chemo

Recommend what supplement

Thalomid

Generic

ADE

Pomalyst

ADE

Pomalidomide

Misc chemo agent

Pregnancy Category X → strict REMS program due to severe teratogenicity

Alkylating agents

ADE

Causes the most impaired fertility out of chemo agents

Soltamox

• What is the generic name, pharmacologic class

• Unique clinical indication/place in therapy?

• What three severe toxicities/risks are associated with this medication?

• What is the standard treatment duration for this therapy?

• What specific hepatic enzyme pathway activates this drug, and what five medications will decrease its active levels?

Evista

• What is the generic name, pharmacologic class, and key patient population demographic constraint?

• What are its two dual indications regarding breast cancer and bone health?

• What life-threatening cardiovascular toxicity risk does it share with tamoxifen, and what major oncologic risk does it notably not share?

• DC for how long prior to prolonged immobilization and surgery

SERM

Raloxifene (vs Tamoxifen): postmenopausal women, doesnt cause endometrial cancer

-

Prolonged immobilization: DC at least 72 hrs prior and during, restart once fully ambulatory

Surgery: stop 2-4 weeks prior

Aromatase inhibitors

-

Frequency

DDI

ADE

Only for…

QD

Tamoxifen decrease levels

suppress estrogen levels by binding to and blocking the enzyme aromatase → ADE of low estrogen (hot flashes)

for postmenopausal women only

Arimidex (→ generic)

Anastrozole (Aromatase inhibitors)

Femara (→ generic)

Letrozole (Aromatase inhibitors)

Aromasin (→ generic)

Exemastane (Aromatase inhibitor)

Ibrance

-

Generic

Indication

Used in combo with..,.

Palbociclib (Ibrance)

-

ER+, HER2- breast cancer

Used with aromatase inhibitors (Anastrozole, Letrozole, Examestane)

Kisqali

-

Generic, Class

Indication

Used in combo with..,.

Ribociclib (Kisqali)

-

ER+, HER2- breast cancer

Used with aromatase inhibitors (Anastrozole, Letrozole, Examestane)

Afinitor

-

Generic, Class

Indication

Used in combo with..,.

Everolimus (Afinitor)

-

ER+, HER2- breast cancer

Used with aromatase inhibitors (Anastrozole, Letrozole, Examestane)

Faslodex

Generic, Class

Formulation, Dosing

ADE

Herceptin

Formulation, indication

In combo

Used for…weeks

BBW

Trastuzumab

IV infusion indicated for ER-, HER2+ breast cancer

Great in combination with chemo agents (paclitaxel, docetaxel)

Used for 52 weeks

BBW: cardiotox, pulm tox, anaphylaxis

Perjeta

Formulation, indication

In combo

BBW

Pertuzumab

IV infusion indicated for ER-, HER2+ breast cancer

Works best in treatment naive patients with chemo agents (paclitaxel, docetaxel) and trastuzumab

BBW: cardiotox, infusion reactions

Kadcyla

Generic

Formulation

Indication

BBW

Ado-trastuzumab emtansine (monoclonal antibody + chemo agent)

IV

Last line in breast cancer

BBW: cardio and hepato toxicity

Megace

MOA, indication

ADE

Megestrol

Progestin that for breast and endometrial cancer

Can increase appetite → anorexia/cachexia associated with AIDS

Also increase BP, glucose and causes clots

LH-RH agonist/GnRH analog

Names

Indication

Frequency

Initial med pairing and why

ADE

Lueprolide (Lupron)

Goserelin (Zoladex)

Triptorelin

-

Usually for prostate cancer

• Can also be used for endometriosis and pre-menopausal ER+ breast cancer

All given every few months

Will increase hormones first → tumor flare (prevent by pairing with anti androgens) → then decrease via neg feed back

ADE:

• Decrease testosterone → gynecomastia in males

• pulmonary embolism and MI

Lupron (→ generic)

Lueprolide (LH-RH agonist/GnRH analog)

Zoladex (→ generic)

Goserelin (LH-RH agonist/GnRH analog)

Degarelix

Class

Formulation, frequency

LHRH antagonist

SC every 28 days

Casodex

Class

ADE

DDI

Bicalutamide

Anti-androgen → all increase in LFT

Causes diarrhea (but less than flutamide)

Increase warfarin levels

Flutamide

Class

ADE

Anti-androgen → all increase in LFT

Causes the most amount of diarrhea

Causes yellow-green urine

Nilutamide

ADE

Anti-androgen → all increase in LFT

Causes constipation (Bicalutamide, Flutamide cause diarrhea)

Disulfiram reaction

Decrease reaction to darkness → Caution driving

Xtandi

Generic, class

ADE

Enzaulutamide

Last line anti-androgen → all increase in LFT

May cause seizures

Nizoral

Indication

ADE

DDI

Ketoconazole

Reduces levels of testosterone and cortisol → good for prostate cancer and cushings

ADE: gynemcomastia

DDI:

• Needs acidic environment → take with food

• Inhibits CYP3A4

Proscar vs Propecia

Dosing

Class

Indication

Proscar (Finasteride 5 mg) vs Propecia (Finasteride 1 mg for alopecia)

Inhibits 5-alpha-reductase

Prostate cancer prevention

Avodart

Dosing

Class

Indication

Avodart (Dutasteride 0.5 mg)

Inhibits 5-alpha-reductase

Prostate cancer prevention

Provenge

Generic

Formulation

MOA

Spiulencel-T

“vaccine” that exposes patients’s WBC to recombinant immunogen so that the WBC would recognize prostate cancer and stimulate body’s immune response when returned to the patient

Keytruda

Generic, Class

Pembrolizumab

Keytruda, PD-1 inhibitor monoclonal antibody

Immunotherapy

AMES test

Compro

Generic

Class, Indication

Prochlorperazine

Dopamine antagonist for CINV

Amisulpride

Class, Indication

Formulation

Dopamine antagonist for CINV

IV

Pulmonary toxicity/fibrosis chemo meds

Bleomycin, Busulfan, MTX

(amiodarone)

COPD (general)

Chronic, irreversible

Usually from lifestyle (smokers) not from genetic like family history

Not due to inflammation → ICS not used first line (increase risk of pneumonia instead)

SMI

Suffix

Counseling Tips

Dont…

Discard after

“Respimat”

-

P-TOP

Prime. Turn. Open. Press

Dont need to shake or require spacer

-

Discard after 3 months

Anticholinergic oral inhalers

Names and Frequency

CI in…

Dont use in what allergy

Ipratropium - QID

Tiotropium, Umeclidinium - QD

Aclidinium, Glycopyrrolate - BID

Caution: glaucoma, BPH, bladder neck obstruction

-

do NOT give 2 anticholinergics together

Dont use with allergy to atropine

Atorvent HFA

Generic, Class

Formulation

Frequency

Comment

Ipratropium, anticholinerigc

(Atorvent HFA) → MDI

QID

MDI that does NOT need shaking (other one is Ciclesonide (Alvesco))

Combivent Respimat

Generic, class

Formulation → Comment

Not CI…

Discard when

Ipratropium + Albuterol (Combivent Respimat) → anticholinergic + SABA

SMI → shaking NOT needed

NOT contraindicated with soybean or peanut allergy

Discard 3 months after cartridge is inserted

Duoneb

Generic, Formulation

Frequency

Ipratropium + Albuterol (neb) → anticholineric + saba

QID PRN

Spiriva Handihaler

Spiriva Respimat

-

Generic

2 Formulation

Counseling

Tiotropium (anticholinergic)

Handihaler (DPI)

Incruse Ellipta

Generic, Formulation

Frequency

Umeclidinium (anticholinergic)

(Incruse Ellipta) - DPI

QD

Tudorza Pressair

Generic, Formulation

Frequency

Dont…

Discard when… (2)

How to use

Aclidinium (anticholinergic)

(Tudorza Pressair) - DPI

BID

Seebri Neohaler

Generic, Formulation

Frequency

Glycopyrrolate (anticholinergic)

(Seebri Neohaler) - DPI

BID

Lonhala Magnair

Generic, Formulation

Frequency

Glycopyrrolate neb - BID

(anticholinergic)