Pharmacology to KNOW (Week 5 for Week 6)

108 terms by maria080605 

Create a new folder

Advertisement Upgrade to remove ads

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

Methotrexate

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

Leucovorin

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)

Gemcitabine

Imitates cytidine in pyrimadine synthesis

Blocks thymidylate synthetase, resulting in inhibition of deoxyribonucleotide synthesis

Cyclophosphamide

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.

Busulfan

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

Cisplatin

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)

Vinblastine

From rosy periwinkle (Vinca rosea)

Inhibits mitotic spindles by inhibiting microtubule formation

Additional dose-dependent side effect = peripheral neuropathy

Paclitaxel

From pacific yew tree (Taxus brevifolia)

Inhibits mitotic spindles by inhibiting microtubule breakdown into tubulin monomers

Additional dose-dependent side effect = peripheral neuropathy

Bevacizumab

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

Cetuximab

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

Panitumumab

Anti EGFR (aka HER1)

Used for colorectal cancer

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

Trastuzumab

Anti HER2 (aka erbB2)

Used in breast cancer

Cardiac side effects

Rituximab

Anti CD20 (expressed on B cells)

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

Gefitinib

EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity

Erlotinib

EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity

Lapatinib

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

Sorafenib

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

Low specificity (affects many kinases)

Sunitinib

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

Low specificity (affects many kinases)

Bortezomib

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

carisoprodol

Muscle Relaxant

Soma

cyclobenzaprine

Muscle Relaxant

Flexeril

methocarbamol

Muscle Relaxant

Robaxin

dantrolene

Muscle Relaxant

Dantrium

adalimumab

NSAID

Humira

indomethacin

NSAID

Indocin

diclofenac-misoprostol

NSAID

Arthrotec

ibuprofen

NSAID

Motrin

Ketorolac

NSAID

Toradol

etodolac

NSAID

Lodine

meloxicam

NSAID

Mobic

Naproxen

NSAID

Naprosyn

piroxicam

NSAID

Feldene

celecoxib

(cox-2) NSAID

Celebrex

Colchicine

Gouty Agent

Colchicine

allopurinol

Gouty Agent

Zyloprim

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

cyclosporine

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?

influenza!!

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

seasonal

Rotavirus vaccine most common cause of

diarrhea

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

Rotarix

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)

Cancer

The uncontrolled growth and spread of abnormal human cells

Leucovorin

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.

Antimetabolites

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)

Hormones

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

Antibiotics

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

Chloroquine

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

Primaquine

kills liver schizonts of P. vivax and P. ovale

Quinine

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

Mefloquine

kills erythrocyte form of malaria only

Doxycycline

inhibits ribosome

pyrimethamine/sulfadoxine

inhibits synthesis of Tetrahydrofolate which is needed for pyrimidine synthesis

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

True

What side effect is common to antimalarials?

Gi upset

Which antimalarials are safe for all trimesters of pregnancy?

Chloroquine, pyrimethamine/sulfadoxine, quinine, quinidine

antifungal

amphotericin B ( Fungizone)

antifungal

fluconazole (Diflucan)

antifungal

nystatin (Mycostatin)

antigout

allopurinol (Zyloprim)

antigout

colchicine generic only

antigout

probenecid (Benemid)

Please allow access to your computer’s microphone to use Voice Recording.

Having trouble? Click here for help.

We can’t access your microphone!

Click the icon above to update your browser permissions above and try again

Example:

Reload the page to try again!

Reload

Press Cmd-0 to reset your zoom

Press Ctrl-0 to reset your zoom

It looks like your browser might be zoomed in or out. Your browser needs to be zoomed to a normal size to record audio.

Please upgrade Flash or install Chrome
to use Voice Recording.

For more help, see our troubleshooting page.

Your microphone is muted

For help fixing this issue, see this FAQ.

Star this term

You can study starred terms together

NEW! Voice Recording

Create Set