Pharmacology to KNOW (Week 5 for Week 6)

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Antifungal, Antimalarial/Protozoal/Hemlmintic, Dermatologic, Antiinflammatory/Antigout, Immunosuppressants, Immunizing Drugs, Cancer/Oncologic


Anti-metabolite drug

Imitates dihydrofolate (DHF or FH2)

Used in standard breast cancer chemotherapy cocktail, CMF

Blocks dihydrofolate reductase (enzyme in thymidine synthesis, resulting in inhibition of deoxyribonucleotide synthesis)

Will also (minor effect) block purine synthesis


Anti-metabolite drug

Imitates tetrahydrofolate (THF of FH4); blocks dihydrofolate reductase

Antidote to methotrexate toxicity, but at excess it facilitates 5-FU's action; used with 5-FU and irinotecan in colon cancer (FOLFIRI)


Imitates cytidine in pyrimadine synthesis

Blocks thymidylate synthetase, resulting in inhibition of deoxyribonucleotide synthesis


Used in standard breast cancer chemotherapy cocktail, CMF

Alkylating, DNA cross-linking agent

Prodrug, can be given orally, activated by CYP450

Results in thrombocytopenia and leukopenia, so is also used for leukemia.


Alkylating, DNA cross-linking agent

Mechlorethamine (aka nitrogen mustard, mustargen)

Alkylating, DNA cross-linking agent

Results in thrombocytopenia and leukopenia, so is also used for leukemia

M in MOPP (O=oncovorin, P=procarbazin, P=prednisone) for Hodgkin's

Nitrosourea (NU)

Alkylating, DNA cross-linking agent


DNA cross-linking agent

Has platinum in structure

Different body distribution from cyclophosphamide (ovarian, lung cancers)

Additional side effect = renal insufficiency

Carboplatin and derivatives

DNA cross-linking agent

Has platinum in structure

Different body distribution from cyclophosphamide (ovarian, lung cancers)

Additional side effect = renal insufficiency

Vincristine (aka oncovorin)

From rosy periwinkle (Vinca rosea)

Inhibits mitotic spindles by inhibiting microtubule formation

Additional dose-dependent side effect = peripheral neuropathy

Used in Hodgkin's (MOPP)


From rosy periwinkle (Vinca rosea)

Inhibits mitotic spindles by inhibiting microtubule formation

Additional dose-dependent side effect = peripheral neuropathy


From pacific yew tree (Taxus brevifolia)

Inhibits mitotic spindles by inhibiting microtubule breakdown into tubulin monomers

Additional dose-dependent side effect = peripheral neuropathy


Anti VEGF (soluble vascular endothelial growth factor)

Turned out to be a disappointment because did not decrease recurrence of tumors

Used in macular degeneration

Adverse side effect: HTN


Anti EGFR (aka HER1)

Used for colorectal cancer in addition to FOLFIRI

Only use on tumors with wild-type KRAS (doesn't work if constitutively active, so patient gets side effects without treatment)

Side effects: skin reactions, infusion related reactions, rash, dermatitis acneiform, diarrhea


Anti EGFR (aka HER1)

Used for colorectal cancer

Not used very often (IgG2, thus less complement binding and less ADCC)


Anti HER2 (aka erbB2)

Used in breast cancer

Cardiac side effects


Anti CD20 (expressed on B cells)

Used for B cell lymphomas in addition to CHOP (cyclophosphamide, hydroxydaunorubicin, oncovorin, prednisone)


EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity


EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity


HER-2 kinase small molecule inhibitor

Imatinib (Gleevec)

abl small molecule inhibitor (also kit and PDGF-R)

Used in CML

Resistance is quick because leukemic cells replicate very quickly


Mainly VEGF-R small molecule inhibitor (also kit and PDGF-R)

Low specificity (affects many kinases)


Mainly VEGF-R small molecule inhibitor (also kit and PDGF-R)

Low specificity (affects many kinases)


Reversible inhibitor of proteasome

Causes tumor cells to undergo apoptosis

Used in multiple myeloma

Expected high toxicity in patients (because proteosome is ubiquitous), but turned out OK (mild effects: GI, sensorineural, neutropenia)

General side effects

Bone Marrow: leukopenia, lymphocytopenia, thrombocytopenia, some anemia,
immunosuppression, and potentially leukemia

GI Tract: ulceration, mucositis, diarrhea, vomiting

Hair Follicles: alopecia

Gonads: premature menopause, reduced spermatogenesis

Wound healing is impaired

Fetal teratogenesis

Injection site reactions and tissue damage


Muscle Relaxant



Muscle Relaxant



Muscle Relaxant



Muscle Relaxant






























(cox-2) NSAID



Gouty Agent



Gouty Agent


What are the primary indications for immunosuppresants

1. Prevention of organ rejection in transplant clients
2. Treatment of autoimmune disorders (eg rheumatoid arthritis, SLE, MS)

What are the primary concerns with immunosuppressants

1. increased risk of infection
2. increased risk of neoplasms

What effect can immunosuppressants have on vaccines

reduce their effectiveness

What are the special considerations for administration of immunosuppressants

1. Don't take on an empty stomach to avoid GI upset
2. Don't mix oral solutions in a styrofoam cup because meds can adhere to sides

What special instructions should be given to female patients receiving immunosuppressants

Use contraceptive during treatment and for up to 12 weeks after therapy ends

Name 5 immunosuppressants

1. cyclosporine
2. azathioprine (Imuran)
3. mycophenolate mofetil (Cell Cept)
4. glatiramer acetate (Copaxone)
5. muromonab-Cd3 (Orthoclone OKT3)

What is an allogenic transplant

A transplant between genetically nonidentical individuals of the same species

What is the drug of coice for preventing organ rejection following allogenic transplantation


What drug is often given in conjuction with cyclsporines and why

glucocorticoids because they are also immunosuppressants so you are doubling up

What is a very common concern with cyclosporines? How can you monitor for it? What can you do if it happens?

1. nephrotoxicity
2. Monitor BUN & creatnine levels
3. it is usually reversible following dosage reduction

How is cyclosporine administered

oral or IV

Why should a patient starting cycloesporine have a baseline oral assessment performed

it can cause gingival hyperplasia

What effect can grapefruit juice have on cyclosporine

It can inhibit metabolism of cyclosporine and which will raise the serum levels and increase the risk of toxicity

2 types of vaccine

killed organism or live, but attenuated

both of these are needed if bitten by animal w. rabies

vaccination and immunization

vaccination is

administer both vaccine/toxoid to elicit antibody response

immunization is

provision of both active/ passive immunity

contraindications of live virus vaccine

immunosupressed and pregnant women

you can not get what from a shot?


ADRs from immunizations are

local reactions, mild fever

only potentially serious ADR of immunization is

acute encephalopathy

MMR( measles, mumps, rubella): is a

live viral vaccine of all 3

MMR is 97% effective and it's ADRs are

local soreness, redness, swelling/ rash, fever

DTaP(diptheria and tetanus) you give an

acellular vaccine (avoid whopping cough)

DTaP is 80-90% effective and it's ADRs are

local reactions, mild fever, and very rare (encephalopathy)

IPV(inactive poliovirus vaccine) 97% and ADRs are

devoid of serious ADRs

HIB(hemophilus influenza) prevents

meningitis, arthritis, pneumonia

HIB is 98% effective and ADRs

well tolerated, local reactions/fever

Varicella is also known as

chicken pox

Varicella is a live attenuated varicella virus that is 97% and ADRs are

local reaction, fever, rash

Hep B surface antigen 85% and ADRs

local reaction, fever

Hep B used in preggers what's neg vs pos?

if mother Hep B neg- newborn gets vaccine if mother Hep B pos- newborn gets vaccine and HBIG

Hep A is the inactive hep A virus 94-100% effective risk dependant on

risk factors, immunization so effective- worth getting, AZ is high risk

Hep A ADRs

mild local reaction, HA, anorexia, malaise

Pneumococcal conjugate vaccine causes

pediatric disease

Pneumococcal is 89% effective and ADRs

easily tolerated- mild local, fever

Meningococcal conjugate vaccine has an old product and a new product

menomune(not T cell dependant) and menactra(T cell dependant good memory)

Influenza inactive or live attentuated and it is


Rotavirus vaccine most common cause of


Rotavirus vaccine had an early application that was discontinued because it caused

intussuception: intestine folds up inside itself

Rotavirus has 5 common

serotypes and produce IgA (mucosal surface)

Rotavirus has a new product that is a live vaccine called


Human papillomavirus vacine prevents

genital warts and cervical cancer

Human papillomavirus vacine include two drugs that both have virus-like particles but not live

gardasil and ceravix (not tested on preggers)


The uncontrolled growth and spread of abnormal human cells


Rescue therapy; Some protocols use massive amounts of chemotherapy to kill off cancer cells. This treatment is given over a short period followed by an antidote drug immediately thereafter to spare the normal cells.


Mimics a necessary nutrient or blocks a reaction, which synthesizes a necessary nutrient; ex. Fluorouracil (5-FU, Efudex) - gloves should be worn b/c an irratant to skin; Cytarabine (Ara-C, Cytosar); Thioguanine (6-TG, 6-Thioguanine

Alkylating Agents

used to treat leukemia, testicular and ovarian cancers, and bladder cancers; Bind to DNA (the genetic material of the cell) and prevent its relocation
Utilized to a greater extent in cancer cells; ex. Chlorambucil (Leukeran)
Cisplatin (Platinol)
Mechlorethamine (Nitrogen Mustard)


To treat hormone dependent cancers such as breast cancer; blocks effect of estrogen in target tissues such as breast; Side Effects - hot flashes; ex. Leuprolide Acetate (Lupron); Medroxyprogesterone Acetate (Depo-Provera); Testolactone (Teslac)

Vinca Alkaloids

Vinblastine (Velban); Vincristine (Oncovin); Vinorelbine (Navelbine); Arrests mitotic division at the metaphase of cell division; side effects: bone marrow suppression, hari loss, vomiting

Asparaginase (Elspar)

Blocks asparagine dependent protein synthesis in tumor cells; side effects: vomiting, depression, bleeding, hypersensitivity, bone marrow sensitivity


Inhibits nucleic acid synthesis; ex. Bleomycin (Blenoxane)
Doxorubicin (Adriamycin); Mitomycin (Mutamycin); side effects: Bleomycin - pulmonary fibrosis, fever, chills, nausea/vomiting; Doxorubicin - myelosuppression, cardiotoxicity, nausea/vomiting ; Mitomycin - bone marrow toxicity, nausea/vomiting


inhibits heme polymerase activity leading to toxic bulidup of heme; kills malaria trophozoites in the RBCs only


kills liver schizonts of P. vivax and P. ovale


inhibits heme polymerase activity leading to toxic buildup of heme; kills trophozoites in RBCs and gametocytes


kills erythrocyte form of malaria only


inhibits ribosome


inhibits synthesis of Tetrahydrofolate which is needed for pyrimidine synthesis

True/False: All of the antimalarials can be given in oral form


What side effect is common to antimalarials?

Gi upset

Which antimalarials are safe for all trimesters of pregnancy?

Chloroquine, pyrimethamine/sulfadoxine, quinine, quinidine


amphotericin B ( Fungizone)


fluconazole (Diflucan)


nystatin (Mycostatin)


allopurinol (Zyloprim)


colchicine generic only


probenecid (Benemid)

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