Antimetabolites: Pyrimidines

SE: DIARRHEA

DOSE LIMITING: myelosuppression=IV bolus

 mucositis=IV infusion

Dihydropyrimidine dehydrogenase deficiency=more likely to experience toxicities

Antimetabolite: Pyrimidine

PO Prodrug of 5-FU

SE: hand-foot syndrome

SC: w/FOOD BID (12h apart=prevent N)

DI: Aluminum/Magnesium containing Antacids, may inhibit 2C9 (decrease metabolicm of phenytoin), Alters coagulation (watch INR with warfarin)

Antimetabolites: Cytidine Analogues

SE: Ocular toxicity (give opthalmic steroid), VESICANT

Dose Adjust: At high doses (>1g/m2/dose) with renal dysfunction 

High dose: cerebellar syndrome (have pt. write name every day if writing gets smaller=cerebellar toxicity)

Antimetabolites: Cytidine Analogues

Related to Cytarabine

SE: Dose Limiting=increase in LFT's (dose reduce when bili is elevated), fever and flu-like syndromes (can give APAP for fever for 7 days but not after=serious prolbem), NOT neurotoxic 

Antimetabolite: Cytidine Analogue

Administration: Continuous infusion, now largely SC. Short stability so fresh bags must e prepared every 2-3 hours.

SE: Injection Site Rxn (b/c SC)

SC: pts. w/ hypoalbuminemia=increase risk of hepatic coma SOME CAUTION

Monitor: Kidney Function 

Antimetabolite: Cytidine Analog

Analog of deoxycytidine 

SE: Thrombocytopenia

SC: AB prophylaxis

Note: Cycle is every 6 weeks b/c of delayed and prolonged melousppression 

Antimetabolite: Purines

Route: IV infusion 

SE: fever (60-70%), CNS toxicity: blindness, coma, and DEATH

SC: AB Prophylaxis

Antimetabolites: Purine

Route: IV infusion 

SC: AB prophylaxis 

Antimetabolite: Purine

Route: ?

NOT a chemo drug: inhibits ADA (stops other drugs from being inactivated) 

SC: AB Prophylaxis, Dose reduce in renal impairment

MP: renal function with each cycle 

Folate Antagonist

 Route: PO

Dose: High with chemotherapy

SE: renal toxicity (alkalinize urine to prevent)

MP: LFTs, pulmonary function tests

DI: Protein bound drugs, Cisplatin (decreases MTX elimination), NSAIDS & ASA (decrease elimination by effects on renal function), BACTRIM

NOT A CHEMO DRUG

Folinic acid

"Rescue Therapy" 

SC: Must be administered 24-48 hours after MTX doses >100mg/m2 to prevent damage to normal tissue (stay in hospital) 

Multitargeted Folate Antagonist

SC: Administer dexamthasone 4mg BID x3 days may prevent/improve rash (begin day prior), Vitamin supplementation with folate and B12 decreases the hematologic SE and mucositis and diarrhea.  Start 1 week before, continue throughout therapy 

Plant Derivatives: Vinca Alkaloids

VinCristine 

SE: Constipation, VESICANT, DO NOT administer intrathecally, neurotoxicity (dose limiting)

MP: Inhibitor of 3A (Grade 4 toxicity with voriconazole/less with fluconazole) 

Plant Derivative: Vinca Alkaloid

VinBlastine

Route: ? 

SE: Bronchospasm, VESICANT

DI: inhibitors of 3A 

Plant Derivative: Vinca Alkaloid

Vinorelbine

Route: ? 

SE: VESICANT 

DI: inhibitor of 3A 

Plant Derivative: Taxanes

Route: ? 

SE: peripheral neuropathy, ALOPECIA (total body hair loss with HD administered q3weeks), myalgias, cardiac toxicity (bradycardia, sometimes heart block and ventricular arrhythmias), VESICANT(?)

SC: non-PVC tubing, bag and use in-line filter

Premedicate (HS before) with diphenhydramine, H2 blocker (cimetidine), & corticosteriod (for allergic reaction) 

DI: 3A4 Substrate 

Plant Derivative: Taxane

Route:

SE: fluid retention

SC: Premedicate (HS before) with diphenhydramine & corticosteriod (for allergic reaction)

DI: 3A4 Substrate 

Plant Derivative 

SC: use DEHP-free tubing/bags, LACTATED RINGERS ONLY

Premedicate: H1, H2 blocker, +/- steroid 

DI: 3A4 Substrate 

Plant Derivative: Podophyllotoxins

Route: PO and IV

DI: Metbolized by 3A4 (?)

Plant Derivative: Camptothecans

Route: ?

"I ran to the can"

SE: DIARRHEA (Grade 4 in 20% of pts)

- EARLY onset (prevent or treat with IV ATROPINE)

- DELAYED onset (treat with LOPERAMIDE 4mg at onset & 2mg q2h until no bowel movement in 12h)

SC: diluent=D5W 

Plant Derivative: Camptothecans

Topoisomerase Inhibitor 

Route: IV

SE: Anemia (50% of pts will require blood transfusions) 

Alkylating Agent

Route: IV & PO

SE: VESICANT (delayed), Hepatotoxicity & pulmonary toxicity (fatal 24-80%) may be dose limiting

Lifetime Dose: 1400mg/m2

SC: Special diluent included (contains EtOH), Non-PVC bags/tubing 

Alkylating Agent

Route:  

SC: take on an EMPTY STOMACH

Alkylating Agents

Route: PO

SE: Rare-cumulative pulmonary fibrosis, Stevens-Johnson Syndrome, peripheral neuropathy, seizures, Drug fever 

Alkylating Agent

Route: PO & IV

SE: hemorrhagic cystitis (cause by metabolite=drink fluids: 3L per day 1-3), secondary neoplasm 

SC: AM (to prevent urination HS) 

Alkylating Agent

SE: hemorrhagic cystitis (Dose limiting), CNS toxicity

SC: give w/MESNA (to inhibit Acrolite) 

Chemopretectant

Route: IV & PO 

Given with Ifosfamide

SC: must continue after ifosfamide b/c MESNA has a shorter t1/2 

Alkylating Agent: Nitrogen Mustard

Route: ?

SE: VESICANT, pain on injection (apply ice)

- monitor to know which SE 

Alkylating Agent: Nitrogen Mustard

Route: IV & PO

Admin: on an empty stomach

SE: mucositis 

Alkylating Agent

KNOW COUNCELING POINTS

Route: PO 

Admin: w/food or after meal

SE: dose limiting N/V, myelosuppression (even 4 weeks later), photosensitivity, alopecia, CNS toxicities (parethesias, lethargy, weakness, hallucinations, ataxia, nystagmus, seizures) 

DI: SSRI, TCA, sympathomimetics, opiates, antihistamines, phenothiazines, antihpertensives, & barbituates

Food Int: alcohol (disulfram-like rxn), tyramine (beer, fermented cheese, smoket meats or salami, some wines, yogurt, bananas), chocolate, & fava beans 

Alkylating Agent

Route: IV infusion

SE: Dose limiting myelosuppression (delayed nadir 2-4 weeks, recovery 1-2 weeks later)

Alkylating Agent

Route: PO

Admin: SAME time daily (decrease N/V at bedtime) or on an empty stomach 

Alkylating Agent

Route: ? 

SE: DL cognitive impairment, ocular toxicities, fever

Heavy Metal Compound

Route: ?

SE: SEVERE N/V, VESICANT

SC: Saline hydration, MIX in SALINE

Other: Radiation Sensitizer 

"Radiation Recall" =  previous skin rxn from radiation will come back when given chemo at the same spot

Heavy Metal Compound

SE: myelosuppression especialy platelets

Dosing: Based on Calvert formula

- Dose = AUC x (GFR +25) 

Heavy Metal Compound

Route: IV infusion 

SE: DL peripheral neuropathy exacerbated by the cold (slow infusion if pharyngolaryngeal dysesthesia [throat freezes] occurs)

Dose: reduce in neurotoxicity & neutropenia 

SC: D5W=diluent

-NEVER dilute w/ NS (oxaliplatin degrates in chlorid-containing solutions)

- do not administer w/ other agents in NS

Anthracene Derivative

Route: IV

"Red Death" 

SE: VESICANT, Irreversibel cardiac damage 

SC: red urine (councel)

Lifetime Dose: 500-550mg/m2 

Anthracene Derivative

SC: VESICANT, red urine

Lifetime Dose: 500mg/m2

Anthracene Derivative

DI: Heparin causes precipitation (flush lines w/ heparin free solution), 5-FU (chemically incompatible)

Lifetime Dose: 900mg/m2

SC: VESICANT 

Anthracene Derivative

Route:

SC: Blue/Green Color (tints urine, sclera, skin) VESICANT

Dose: 140-160mg/m2 Lifetime Dose increases CV toxicity 

Anti-tumor Antibiotics

Route:

SE: IRREVERSIBLE pulmonary toxicity, hypersensitivity rxn (test dose=controverisal), drug-induced fever

Lifetime Dose: 400 Units 

MP: Pulmonary Function Tests 

Anti-tumor Antibiotics

Route:

SE: VESICANT

Not used very often 

SE: Hypersensivity rxn (TEST DOSE), prolonged pt/ptt, decrease in fibinogen, depression of clotting factors

MP: coagulation parameters (increased bleeding risk w/warfarin)

Route: PO

CU: Blast Crisis

Admin: PO can be dissolved (some excipients won't dissolve=white powder, which can be discarded) 

Tamoxifen

Toremifene 

Estrogen Antagonist

SE: DVT, thrombophlebitis, elevated LFT, hot flashes, Nausea, endometrial hyperplasia, HA, dizziness, vaginal bleeding 

Anastrozole

Letrozole

Exemestane

Selective Aromatase Inhibitors

SC: POSTMENOPAUSAL women

SE: less DVT 

Flutamide

Bicalutamide

Nilutamide

Dihydrotestosterone Inhibitors

WOMEN SHOULD NOT HANDLE 

GhRh agonists

Castration levels of testosterone & postmenopausal levels of estrogen

CU: prostate, breast (premenopausal)

 Progestin w/anti-estrogenic properties

Used for weight gain

SE: high doses=cushings syndrome & adrenalcortical suppression 

CU: breast, endometrial 

SE: DL wt. gain secondary to fluid retention and peripheral neuropathy, QTc prolongation,

Retinoid acid syndrome (30-50%)

- pulmonary infliltrates, respiratory distress, HTN (treated w/steroids) 

Retinoids

SE: HA, Retinoic Acid Syndrome (may lead to multi-organ failure=DEATH)

Targeted Therapy: Proteosome Inh

SE: DL peripheral neuropathy 

Targeted Therapy: Antiangiogenesis Agent

Route: PO

SE: TERATOGEN, Peripheral neuropathy (25%), DVT 

Targeted Therapy: Tyrosine Kinase Inh

Route: PO

DI: 3A4 substrate (ANY 'nib)

Admin: w/meal & H20

SE: mild to moderate N/V, periorbital and lower limb edema (50%), increase in LFT

Targeted Therapy: Tyrosine Kinase Inh

MOA: Dual BCR/ABL and Src

CI: imatinib resistance 

DI: 3A4 substrate 

Targeted Therapy: EGFR Inh

Route: PO

Admin: empty stomach (1h prior, 2h following meal) QD 

SC: AVOID SUN 

DI: 3A4 substrate

Targeted Therapy: Tyrosine Kinase Inh

Route: PO

Admin: NO regard to meals 

SC: AVOID SUN 

SE: decrease in LVEF 

MP: baseline Ejection Fraction

DI: 3A4 substrate

Targeted Therapy: Multitargeted Inh

Route: PO

Admin: w/OUT food BID 

SC: AVOID SUN

DI: 3A4, UGT1A9 (increases irinotecan's active component)

Targeted Therapy: Tyrosine Kinase Inh

Route: PO

Admin: w/OUT food QD

SE: plantar plamar erythrodysesthesia

SC: AVOID SUN 

DI: 3A4 substrate

Biological Therapy

Vaccine! 

Route: intravesically  

SC: pt must have competent immune system 

Biological Therapy

Toxicities: Flu-like syndrome (fever, chills, malaise, myalgias, HA), DL fatigue, psychiatric 

Biological Therapy

SE: hypotension, fluid retention, renal dysfunction, Capillary leak syndrome, bacterial infections (staph infections)

MP: steroids reduce SE but also reduce effects 

Humanized Monoclonal Antibody

Route: IV 

Storage: Fridge

Admin: use w/in 8h of diluting, protect from light

Premedicate: PO antihistamines (diphenhydramine 50mg) & APAP 650mg (prevent infusion related SE) 30 min prior to infusion

Prophylaxis: pneumocysitis carinii & HSV infection

- at initiation & continued 2 months later or if CD4 Count is 200cell/L whichever is later 

DO NOT ADMIN. IF: Active systemic infection, underlying immunodeficiency 

Primate Monoclonal Antibody

SC: +HER1 (EGFR1) expression

SE: PHOTOSENSIVITY, acneform follicular rash (88% w/in 2-3 weeks)

Human Monoclonal Antibody

SE: PHOTOSENSIVITY 

Primate Monoclonal Antibody

Route: 

Premedicate: APAP & diphenhydramine

Mouse Monoclonal Antibody

Black Box Warning: hypersensitivity rxn (anaphylaxis), prolonged and sever neutropenia  thrombocytopenia

Mouse Monoclonal Antibody

Route: ?

2 Components

Precaution: Radiation (can't be anywhere near kids/pregnant women)

SC: Premedicate w/ APAP & Diphenhydramine (Similar to Rituximab)

Humanized Monoclonal Antibody

Herceptin 

MOA: HER2 Receptor

SE: cardiovascular toxicity (especially w/doxorubin)

DI: doxorubicin 

Humanized Monoclonal Antibody

Avastin

VEGF (V=vascular)

SE: HTN, Gi perferations, proteinurea

SC: Dilute NS (NOT D5W), wait 28 days after surgery due to bleeding risk

Humanized Monoclonal Antibody

Admin: TURN OFF LIGHTS when mixing, give immediately after mixing

SE: neutropenia, thrombocytopenia, fever, diarrhea, stomatitis

SC: premedicate w/ Diphenhydramine & APAP 650mg 1h prior, then q4 x2 doses