Term
|
Definition
Inhibits DNA synthesis by competing with dGTP (causes non-functional DNA complex to be formed to halt DNA production)
Activated by viral thymidine kinase
Guanosine analog
Resistance developed due to decrease in viral thymidine kinase
Oral, topical
3-4x/day
Excreted by kidney
Used against Herpes and Shingles
Herpes encephalitis
Prophylaxis in organ transplant
Nephrotoxicity in high doses
Safe in pregnancy |
|
|
Term
|
Definition
Similar to acycolivr longer half life
A little more toxic |
|
|
Term
|
Definition
Inhibits viral fusion to cell membrane
OTC for cold sores, herpes simplex
Minor side effects |
|
|
Term
| Ganciclovir, Valgancyclovir |
|
Definition
Inhibits CMV DNA replication
Activated by viral kinases in cells infected with CMV or herpes
Less selective than acyclovir, more toxic
IV or oral
Tx or prophylaxis of CMV/herpes in transplant pts
CMV retinitis
Causes neutropenia, thrombocytopenia |
|
|
Term
|
Definition
Used for resistent CMV, herpes
Renal toxicity |
|
|
Term
|
Definition
Inhibits DNA and RNA polymerase, RT
IV
Renal toxicity |
|
|
Term
|
Definition
Antisense compound to viral mRNA
Intraocular compound for CMV retinitis |
|
|
Term
|
Definition
INhibit neuraminidase, blocks release of virus from the cell
ACtive against influenza A and B
Oral or nasal
GI side effects or breathing problems |
|
|
Term
|
Definition
Inhibits viral RNA synthesis
Inhibits viral RNA polymerase and synthesis of GTP
Used for RSV and hepatitis C
CI PREGNANCY
Aerosol
Causes anemia |
|
|
Term
|
Definition
|
|
Term
|
Definition
RT inhibitor used for HIV
Also for HBV polymerase inhibition
DOC chronic hep B |
|
|
Term
|
Definition
Used for Hep C
Causes flu-like sxs
Depression, anemia |
|
|
Term
|
Definition
Protease inhibitors against Hep C
Poor oral absorption
STRONG inhibitor of CYP3A4
Anemia, leukopenia, rash |
|
|
Term
|
Definition
Thymidine analogue
Used for HIV
Incorporated into DNA, inhibits RT
Used for prophylaxis, slows progressiong
Widely used, combined ith lamivudine
Gets into CNS
All RT inhibitors are in the form of triphosphates to incorporate into DNA
Maintains CD4 count
Treats AIDS dementia, psoriasis and T cell leukemia
Resistance develops quickly with monotherapy
Can cause neutrophenia and anemia, CAUTION when bone marrow compromised
STOP if lactic acidosis or hepatotoxicty develops (all nucleoside RT inhibitors)
Probenecid decreases elimination |
|
|
Term
|
Definition
Inhibits HIV RT and HBV polymerase
Combined with Zidovudine: first choice
Very effective, low toxicity
Monotherapy for HBV
Very well tolerated |
|
|
Term
|
Definition
New drugs to treat HIV
E alos used for HBV
Biggest side effect is flatulence |
|
|
Term
|
Definition
Protease inhibitor
Mutations common, so not used alone
Poor bioavailability, improved with inhibitors of CYP3A4 like grapefruit juice
Side effects are altered body fat distribution, buffalo hump and thin face
Leads to cholesterol increase; atherosclerosis, strokes
DM, depression
DOC, well-tolerated
Once-a-day dosing
Less effect on lipoproteins; may increase bilirubin |
|
|
Term
|
Definition
Protease inhibitor
Well tolerated
Second drug of choice
Causes HA and nightmares |
|
|
Term
|
Definition
Protease inhibitor inhibits CYP3A4
Combined with other protease inhibitors to increase bioavailability
Many drug interactions
Contains alcohol |
|
|
Term
|
Definition
Protease inhibitor
Poor oral bioavailability, increased with grapefruit juice
Inducers of CYP3A4 decrease effectiveness
GI side effects common |
|
|
Term
|
Definition
Protease inhibitor
Cross resistance with ritonavir
Can cause kidney stones and increase bilirubin |
|
|
Term
|
Definition
Protease inhibitor
Many drug interactions |
|
|
Term
| Amprenavir, Fosamprenavir |
|
Definition
Protease inhibitors
Well absorbed
Contains propylene glycol--avoid metronidazole
Inhibits CYP3A4,
Casuses Stevens Johnson |
|
|
Term
|
Definition
Protease inhibitors
Second line |
|
|
Term
|
Definition
| Non-peptide protease inhibitor |
|
|
Term
|
Definition
Binds to HIV viral envelope glycoprotein
NO cross resistance with other drugs
Used in advanced disease when other drugs fail
Pneumonia, injection reactions common
Binds to gp41 |
|
|
Term
|
Definition
Used only if there is a CCR5 receptor on T cells, CCR5 virus
Few side effects
Rash most common
Resistance may develop |
|
|
Term
|
Definition
Integrase inhibitor in HIV
Prevents viral replication
Used when other drugs stop working
N/V, HA |
|
|
Term
| Didanosine, Zalcitabine, Stavudine, Abacavir |
|
Definition
Nuceloside RT inhibitors
Cause peripheral neuropathy
Not used as frequently
A causes hypersensitivity
D causes pancreatitis, acts in mitochondria, NOT widely used |
|
|
Term
| Efavirenz, Nevirapine, Delaviridine, Ertavirine |
|
Definition
Non nucleotide RT inhibitors
Bind direclty to inhibit RT
Metabolized by CYP3A4
Ef is highly teratogenic
N causes hepatitis, Stevens Johnson
Used ONLY with nucleoside analogues |
|
|
Term
|
Definition
Alkylating agent, mustardogen
Most effective in G1 and M phase
Vesicant, hyperuricemia |
|
|
Term
|
Definition
Pro-drug
Alkylating agent
Activated by CYP 450
One toxic metabolic product is acrolein, which causes hemorrhagic cystitis
NOT a vesicant
Broad spectrum
Causes SIADH
Treatment for toxicity is MESNA |
|
|
Term
|
Definition
| Alkylating agent that is oral |
|
|
Term
|
Definition
Alkylating agent
USED FOR BLADDER CANCER
Has three rings |
|
|
Term
|
Definition
Alkylating agent
Used for CML
Causes hyperuricemia, give allopurinol |
|
|
Term
|
Definition
Nitrosourea
Used for BRAIN TUMORS
Terrible myleosuppression |
|
|
Term
|
Definition
Nitrosourea
Brain tumors
Terrible myelosuppression |
|
|
Term
|
Definition
Nitrosourea
Selective for pancreas |
|
|
Term
|
Definition
Inhibits human DHF
No thymidylate
Blocks DNA, RNA, protein synthesis
Leucovorin bypasses blockade
Resistance can develop with decreased uptake or increased amount of enzyme
Causes kidney toxicity, precipitates in renal tubules
Hepatotoxicity
Myleosuppression
Pemetexed very similar, direclty inhibits thymidylate synthase (leucovorin won't help OD); cause hand-foot and mouth disease |
|
|
Term
|
Definition
Converted by HGPRT to nucleotide
Resistance in decreased HGPRT
Inhibit synthesis of DNA, RNA purines
Myelosuppressive
Metabolized by XO
Causes bone marrow depression and jaundice
Azathioprine pro-drug used as immunosuppressive |
|
|
Term
|
Definition
Inhibits thymidylate synthase, blocks DNA synthesis
Cell-cycle specific at G1 and S phases
Response increased by leucovorin
Broad spectrum |
|
|
Term
|
Definition
Competes with dCTP
Chain termination in DNA syntehsis
Works in S phase
Causes leukopenia, thrombocytopenia, anemia |
|
|
Term
|
Definition
|
|
Term
| Doxorubicin, Daunorubicin |
|
Definition
Intercalate into DNA
Generate free radicals, effect increased by iron
Cardiotoxic especially c herceptin
Chelator reduces toxicity
Red urine
Causes radiation recall
Widely used |
|
|
Term
|
Definition
Directly damages DNA
Cell cycle specific at G2 and M
Little myelosuppression
Pulmonary fibrosis
For your balls (testicular cancer) |
|
|
Term
|
Definition
Binds to DNA between C and G, strand breaks, stops RNA synthesis
Causes myelosuppression, N/V, alopecia
Severe vesicant
Causes radiation recall |
|
|
Term
|
Definition
Plant alkaloids
Bind to tubulin in M phase
From periwinkles
Neurotoxicity and myelosuppression |
|
|
Term
|
Definition
Binds tubulin, arrests mitosis, disrupts axonal transport
Very active and quite toxic
Causes myelosuppression, peripheral neuropathy |
|
|
Term
|
Definition
Topoisomerase inhibitor II
DNA strand breaks
Myelosuppression |
|
|
Term
|
Definition
Topoisomerase inhibitor I
Cell cycle arrest, DNA damage
Myelosuppression |
|
|
Term
|
Definition
Leukemia cells require asp
Hydrolyzes asp
Causes hypersensivity reactions |
|
|
Term
|
Definition
Inhibitor of Bcr-abl fusion protein
Used for CML
Can be immunosuppresive |
|
|
Term
|
Definition
EGF receptor blocker
Blocks cell growth and survival |
|
|
Term
|
Definition
Blocks ATP binding to HER1/EGFR tyrosine kinase
Diarrhea, rash, anorexia, fever common |
|
|
Term
|
Definition
VEGF inhibitor
Decreases blood supply to slow tumor growth
Improve delivery of cytotoxic drugs
Can cause bleeding and thromboembolism in systemic use |
|
|
Term
|
Definition
Blocks estrogen receptor in breast
Can cause hot flashes, uterine hyperplasia |
|
|
Term
|
Definition
Antibody to HER2 receptor
Can cause cardiac toxicity |
|
|
Term
|
Definition
| Anti-androgen for prostate cancer |
|
|
Term
|
Definition
Alkylate DNA
Cause miscoding, breakage, crosslinking
Not cell cycle phase specific
Most effective on rapidly proliferating cells like tumor cells (also GI, hair, BM)
Vesicants, burn tissues at injection site
Effects CTZ and local to cause N/V
Immunosuppression |
|
|
Term
|
Definition
|
|
Term
|
Definition
Crosslinks DNA in two places
Sensitizes cells to radiation
Broad spectrum
Causes nephrotoxicity and ototoxicity
Used for TESTICULAR CANCER |
|
|
Term
|
Definition
Acts on cyclophilin to inhibit caclcineurin to inhibit production of IL-2 and thereby inhibit T cell activaiton
Suppresses immune response for transplant rejection prophyalxis
NO bone marrow suppression
Metabolized CYP3A4, watch out for ALL drug interactions
NO grapefruit juice
Narrow therapeutic range
Avoid phenobarb, phenytoin, rifampin, erythromycin, ketoconazole, verapamil
Used for maintenance following organ transplant and for autoimmune diseases
RENAL toxicity
Can cause HTN, gingival hyperplasia, hyperglycemia |
|
|
Term
|
Definition
Acts on FK506 to inhibit caclcineurin to inhibit production of IL-2 and thereby inhibit T cell activaiton
Decreases IL-2 and IL-4
Used to prevent rejection in transplantation
Can cause nephrotoxicity, HTN, hyperglycemia (have to put on insulin)
Neurotoxicity, insomnia
Oral absorption affected by food
Narrow therapeutic range
Metabolized with CYP3A4 |
|
|
Term
|
Definition
Calcienurin inhibitor
Cream used for atopic dermatitis
Better than steroids for skin |
|
|
Term
|
Definition
Inhibits mammalian target of Rapamycin
Blcks T cell proliferation in response to IL-2
Inhibits B cell prolif
Causes bone marrow suppression
Used to replace cyclosporine |
|
|
Term
|
Definition
Prodrug
Inhibits monophosphate dehydrogenase
T and B cells require this enzyme for purine synthesis
Specific for T and B cells
Prevents rejection after transplants
Causes rash, leukopenia
NOt recommended in pregnancy
Don't give with antacids |
|
|
Term
|
Definition
Inhibits de novo purine synthesis
Cell prolif, especially lymphocytes, in response to antigen stimulation inhibited
Prevents rejection in transplants
Treats GN and lupus
Teratogenic
Causes bone marrow suppression, increased risk of infections
Metabolized by xanthine oxidase |
|
|
Term
|
Definition
Inhibits pyrimidine synthesis
Decreases TNFa
Used in RA
Causes diarrhea, liver toxicity, teratogenic |
|
|
Term
|
Definition
Alkylating agent that cross-links DNA
Direct effect on T and B cells
Can destroy T cells
Blocks response to new antigens
Can inhibit established immune response
Used for organ transplant rescue and bone marrow transplants
Treats MS, RA, lupus
Causes hemorrhagic cystitis, prevent wiht hydration and MESNA
Causes bone marrow suppression, alopecai |
|
|
Term
|
Definition
Inhibits human DHF
Used for Organ transplants, RA, psoriasis, severe asthma, antineoplastic
Causes bone marrow suppression, alopecia, hepatotoxicity |
|
|
Term
|
Definition
Decreases TNFa, IL-6
Antiproliferative/antitumor
Teratogenic
Prevents GVHD
Used in MM, leprosy, some cancers
Causes sedation, neutropenia |
|
|
Term
|
Definition
Antibody to CD3 on T cells
T cells removed for circulation
Used for steroid-resistant rejection, kideny rejection
Depelets T cells in donor bone marrow
Severe reactions |
|
|
Term
|
Definition
Bind to IL-2 receptor on activated T cells, inhibits further IL-2 activation
Prophylaxis decreases renal rejection
Don't cause general immunosuppression because only work on activated T cells |
|
|
Term
|
Definition
Prevents T cell activation but doesn't destroy them
Used for psoriasis |
|
|
Term
|
Definition
Blcoks T cell activation at CD2
Used for psoriasis |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Neutralizes TNFa used for FA |
|
|
Term
|
Definition
Proliferation and differentiation of Th and CTLs
Prolif of B cells and macrophages
Used for RCC and MM
Very toxic, causes pulmonary edema, severe hypotension, hematological |
|
|
Term
|
Definition
Recombinant IL-11
Prevents chemo-inducd thrombocytopenia
Reduces need for platelet transfusions
Given subQ
Causes fluid retention, edema |
|
|
Term
|
Definition
Recombinant C-CSF (colony stimulating factor) used for tx of neutropenia in stem cell stransplants, chemo, HIV treatment
SubQ
Bone pain common |
|
|
Term
|
Definition
Recombinant EPO
Used to decrease anemia in chemo
SubQ
Increased risk of blood clots, stroke, HTN |
|
|
Term
|
Definition
Recombinant human cytokine
Used for hepatitis, cancers
Increased response to viruses
Causes depression, flu sxs, bone marrow suppression, alopecia |
|
|
Term
|
Definition
Recombinant human cytokine
Suppress class II MHC, decreased antigen in NS
USed for MS
Causes depression, flu sxs, bone marrow suppression, alopecia |
|
|
Term
|
Definition
Activates phagocytes and macrophages
Activates PMN, NK cells
Potentiates TNFa, increase Th1
Decreased infections in chronic granulomatous disease, treats pulmonary/hepatic fibrosis
Causes depression, flu sxs, bone marrow suppression, alopecia |
|
|
Term
|
Definition
Decoy for myelin basic protein, few side effects
USed for MS |
|
|
Term
|
Definition
Antibodies to T cells
Used in acute rejection episodes, to prevent rejection
Foreign proteins, so severe reactions happen |
|
|
Term
|
Definition
Antibodies to Rh antigen
Binds to antigen and prvents mother from mounting immune response |
|
|
Term
|
Definition
Polyene antifungal
Inhibits sterol synthesis in cell wall, causes depolarization of membrane, formation of pores permeable to proteins and cell death
Broad spectrum to even some protozoa
DOC for most systemic fungal infections
IV
Renal impairment doesn't affect filtration
Toxicities due to infusion are chills, fever, V
Toxicities due to long term use are azotemia (nephrotoxic)
Fungicidal |
|
|
Term
|
Definition
Antagonizes fungal DNA and RNA
Coverted into 5-fluorouracil that inhibits fungal DNA and RNA synthesis
Synergistic with amphotericin B
DOC for Cryptococcus
Oral
Can be used for Candida, Aspergillus, Sporothrix
Causes depression of bone marrow, elevation of liver enzymes |
|
|
Term
|
Definition
Inhibit synthesis of ergosterol, leads to accumulation of toxic intermediate sterols
Borad spectrum antifungal
Oral
Extensive metabolism hepatic prior to elimination
Can cause GI upsets, pruritis
Inhibits CYP3A4, causes gynecomastia
Inhibits testicular and adrenal steroidogenesis |
|
|
Term
|
Definition
Inhibits synthesis of ergosterol
Oral and IV for cryptococcus, Candida
Inhibits fungal CYP450
Penetrates CSF, used for fungal meningitis
Better penetration, less toxic than ketoconazole
Fewer drug interactions |
|
|
Term
|
Definition
Inhibits synthesis of ergosterol
DOC Aspergillus
Visual impairment and drug interactions becuase it inhibits CYP450
IV and oral |
|
|
Term
|
Definition
Inhibits synthesis of ergosterol
Oral
Approved for Blasto, histo, onychomcosis, Candida
Hepatically metabolized to 30 metabolites
High plasma protein bound |
|
|
Term
|
Definition
Inhibits synthesis of glucan cell wall component
Fungicidal
IV
Used for tx of invasive Aspergillus in refractory pts
Causes increased liver enzymes, histamine release |
|
|
Term
|
Definition
Inhibits synthesis of glucan cell wall component
Fungicidal
Used for esophageal candidiasis
IV |
|
|
Term
|
Definition
Inhibits synthesis of glucan cell wall component
Fungicidal
IV
Used for esophageal candida |
|
|
Term
|
Definition
Binds to microtubules of certain fungi, destroys mitotic spindle
Fungistatic
Systemic tx of dermatophytes
Binds to keratin, prevents infection in new skin
Oral
CI in acute intermittent porphyria, hepatocellular failure, pregnancy
Cuases disulfiram-like effects, hematologic disturbances, skin rashes, hepatotoxicity
Reduces activity of warfarin
Barbs decrease its absorption |
|
|
Term
|
Definition
INterferes with sterol biosynthesis, inhibits squalene monooxygenase, buildup of toxic squalene
Oral or topical
Best for onychomycosis
Fungicidal against dermatophyes
Less active against Candida
Well absorbed from GI
NO dosage adjustements in pts with hepatic or renal impairment |
|
|
Term
|
Definition
POlyene antibiotic that alters permeability and casues leakage of small molecules from fungal cell
Oral and topical
Used for Candida
Swished in mouth for oral candida |
|
|
Term
|
Definition
Cream or vaginal tablets
Used for Tinea pedis, vulvovaginal candida |
|
|
Term
|
Definition
Used to treat dermatophytes, yeasts, and Malasezia furfur
Used for vagina and oral candidiasis, tinea |
|
|
Term
|
Definition
Use for tinea versicolor
Not effective in onychomycosis
Topical and powder |
|
|
Term
|
Definition
DOC for malaria
Prophylaxis for sensitive organisms
Resistant form are a serious problem
Transport pump removes drug from parasite
Blood Schizonticide
Oral or IV
Well absorbed from GI
Accumulates in melanin-rich tissues
Metabolised by liver CYP
One week duration of action
Toxicity is hemolysis in G6PD deficiency, retinal and corneal toxicity, ototoxicity
CNS dizziness
Skin rashes, pruritis
CI in pts with psoriasis
Associated with long QT |
|
|
Term
|
Definition
First line for chloroquine-resistant malaria
DOC for prophylaxis of chloroquine resistant malaria
Blood Schizonticide
Oral
Slow elimination
Can cause seizures and aggravate latent psychoses; don't use in pts with hx of epilepsy or mental illness
CArdiac toxicity |
|
|
Term
| Quinine and Qunidine Gluconate |
|
Definition
Blood Schizonticide
Found in cinchona bark
Gametocidal in vivax and ovale
DOC for complicated chloroquine resistant malaria
Oral or IV
Analgesic and antipyretic
Causes cinchonism--tinnitus, HA, dizziness, flushing, visual disturbances
Antiarrhythmic Class 1A
Hemolysis in G6PD deficiency
May increase uterine contractions
CI in pts with myasthenia gravis |
|
|
Term
|
Definition
Tetracycline antibiotic
Tx of complicated chloroquine resistant malaria |
|
|
Term
| Pyrimethamine, Proguanil, Pyrimetamine and Sulfadoxine, Trimethoprim |
|
Definition
Folate metabolism inhibitors used for malaria
Inhibit DHF
Used for presumptive tx and acute attacks |
|
|
Term
|
Definition
Interferes with mitochondrial ETC and ATP synthesis
Synergisitic combination effective in regions where chloroquine and mefloquine resistance is high
Oral
ACtive against tissue and erythrocytic malaria
Few side effects
Caution in pregnant women |
|
|
Term
|
Definition
Chinese herbal anti-malarial
Most rapid action against falciparum
Oral
Combined with other drugs discouraged |
|
|
Term
|
Definition
Alternative for MDR falciparum and vivax
Oral, absorption increased with fatty foods
ACtive against erthrocytic forms
QT elongation, teratogenic
Used when nothing else works |
|
|
Term
|
Definition
Tissue schizonticide in malaria
ONly active against tissue forms and gametocytes
Will not suppress disease once developed Oral
Used for terminal prophylaxis, antirelapse therapy
Usually mild, but CI in SLE, RA
Causes fetal hemolytic anemia in pregnancy |
|
|
Term
|
Definition
DOC for E. histolytica, G. lamblia, T. vaginalis
For amebiasis, give with luminal ambicide
Also used for anaerobic bacteria, nonspecific bacterial vaginosis or Gardnerella
Topical for rosacea
Inhibits DHF reductase
Disulfiram-like effects |
|
|
Term
|
Definition
MOA similar to metronidazole
Used for E. histolytica, Giardia, T. vaginalis |
|
|
Term
|
Definition
Effective against luminal trophozoites and cysts of E. histolytica
Useful for asymptomatic amebiasis
Oral
Toxicities are skin reactions, thyroid enlargement
Optic neuritis |
|
|
Term
|
Definition
Effective against luminal torphozoites but NOT tissue trophozoites
Combined with metro for amebiasis
Mild side effects |
|
|
Term
|
Definition
Aminoglycoside
Oral
Effective against luminal trophozoites
Used for asymptomatic amebiasis, giardiasis, T. vaginlais
Side effect upset stomach |
|
|
Term
| Emetine and Dehydroemetine |
|
Definition
Alternative to metronidazole for severe intestinal or systemic E. histolytica infections
Injection
Risk of serious cardiotoxicity, GI effects, teratogenicity |
|
|
Term
| Pyrimethamine plus Sulfadiazine |
|
Definition
DOC for toxoplasmosis
Administer with folinic acid |
|
|
Term
|
Definition
DOC for pneumocystosis
Useful against toxoplasmosis
Prophylaxis for jiroveci in AIDS pts
Inhibits folate metabolism
Causes transaminase elevation, rash, pruritis |
|
|
Term
|
Definition
Effective against Pneumocystis
IM or nebulization
Used to treat active infection
Can cause hypotension, arrhythmias, hypoglycemia
For those who don't tolerate TMP-SMX |
|
|
Term
|
Definition
DOC for roundworms, whipworms, hookworm, pinworm
With steroids for trichinosis
Oral
Broad spectrum, effective against some nematodes
Useful agaisnt mixed infection
Inhibits microtubule polymerization by binding to B-tubulin, higher affinity in parasite
Cuases block of uptake of glucose and toher nuterients, gradual immobilization and death of helminth
Oral
May be embryotoxic or teratogenic
Can be used topically for cutaneous larva migrans |
|
|
Term
|
Definition
Oral
Braod spectrum against neamtodes
Alternative to mebendazole
Cholinesterase inhibitor; produces depolarizing neuromuscular blockade in worm; worm NMJ more sensitive than humans |
|
|
Term
|
Definition
Oral
Effective against many nematodes
DOC for filaria infestation
Also used for threadworm, roundworm, cutaneous larva migrans
Paralyzes parasite, intensifies GABA trasmission signals |
|
|
Term
|
Definition
Oral
DOC for schistosomes
Effective against many cestodes and trematodes
Paralysis of worms muscles
Well-absorbed, used in systemic infections
Few side effects, nausea due to release of death worm proteins |
|
|
Term
|
Definition
Oral
Uncopules oxidative phosphorylation
ACtive against flukes, including liver and lung fluke
DOC only for sheep liver flukes
Can cause rash, nausea due to dead worm parts |
|
|
