| Drug Name |
Category |
Comments |
| Foscarnet |
Anti-Microbial; Anti-Viral |
Indicated for treatment of (1) CMV Retinitis
(administer with Ganciclovir), and (2) Serious HSV or VZV infections
that are resistant to treatment by Acyclovir. Serious Adverse Effect: It
chelates Ca+2 which can lead to life-threatening
hypocalcemia. |
| 3- Deoxy thmidin- 2-ene (d4T)
(Stavudine) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
|
| Dideoxy cytosine (ddC) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Dideox yinosine (ddI) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Lamivudine (3TC) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog |
|
| Azidothymidine (AZT)
(Zidovudine) |
Anti-Microbial; Anti-Viral
Anti-AIDS; Nucleoside Analog
Immunosuppressant |
Half-life of 1-3 hrs. Gets into CNS (60%). Mech: It is
phosphorylates to the triphosphate form, which is the active form. Then,
(1) It competitively inhibits HIV Reverse Transcriptase,
and (2) It is a chain-terminator of HIV viral DNA
synthesis. Resistance is common, due mutations in viral Reverse
Transcriptase.
Adverse Effects: May be severe. Bone marrow depression.
Headaches, agitation, insomnia. |
| Indinavir |
Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
|
| Ritonavir |
Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
|
| Saquinavir |
Anti-Microbial; Anti-Viral
Anti-AIDS; Protease Inhibitor |
Well tolerated, but low oral bioavilability (5%). |
| Interferon -alpha (IFN-alpha) |
Anti-Microbial; Anti-Viral
Endogenous Factor |
Enhances host-cell resistance to viral infections, and
possibly some tumors. Adverse effects: fever, malaise, headaches,
anemia, GI distress. |
| Acyclovir |
Anti-Microbial; Anti-Viral
Nucleoside Analog |
Indicated for HSV-1, HSV-2, VZV. Used topically for skin
lesions, or IV for encephalitis or neonatal disease. It is activated by
HSV viral Thymidine Kinase ------> (1) it binds and
inhibits viral DNA polymerase, and (2) it is
incorporated into viral DNA, where it acts as a chain-terminator.
Resistance in HSV is due to mutations in Thymidine Kinase or the DNA
Polymerase.. |
| Ganciclovir |
Anti-Microbial; Anti-Viral
Nucleoside Analog |
Indicated for CMV. Deoxyguanosine
analog, it reversibly inhibits viral DNA polymerase.
Works similar to Acyclovir.
Adverse Effects are bad: Neutropenia (common),
anemia, eosinophila. Also CNS changes (headache, behavioral changes,
seizure, coma), fever, rash, phlebitis, nausea. |
| Ribavirin |
Anti-Microbial; Anti-Viral
Nucleoside Analog |
Aerosol spray. Nucleoside analog blocks the formation of
GTP. Indicated for severe Respiratory Syncitial Virus (RSV)
infections in infants. No serious adverse effects. |
| Vidarabine (Ara-A) |
Anti-Microbial; Anti-Viral
Nucleoside Analog |
Topical or IV. It inhibits DNA synthesis by affecting
DNA polymerase. Indicated for HSV, Varicella-Zoster.
Adverse effects are minimal: nausea, vomiting, possible neurotoxicity. |
| Amantidine |
Anti-Microbial; Anti-Viral
Uptake Inhibitor |
It inhibits viral absorption and uptake. Indicated for
Influenza A, Rubella. Used prophylactically after
Influenza-A exposure.Adverse Effects: Insomnia, restlessness,
nervousness, depression. |
| Rinantidine |
Anti-Microbial; Anti-Viral
Uptake Inhibitor |
Longer half-life than Amantadine, biliary excretion.
Perhaps fewer CNS effects. |
| Taxol |
Chemotherapy
Alkaloid; Paclitaxel |
IV only; biliary excretion. Extensively metabolized by
the liver. It stabilizes the mitotic spindle during
metaphase, causing metaphase arrest.
Indications: head and neck carcinomas, ovarian carcinomas, breast
cancers, lung cancers. Adverse Effects: bone marrow suppression,
peripheral neuropathy. |
| Etoposide (VP-16) |
Chemotherapy
Alkaloid; Podophyllotoxin |
IV only; urinary excretion. It inhibits
topoisomerase II ------> cause DNA strand breaks, increase DNA
degradation.
Indications: small-cell lung cancer, lymphomas and leukemias,
testicular carcinoma. |
| Teniposide (VM-26) |
Chemotherapy
Alkaloid; Podophyllotoxin |
|
| Vinblastine |
Chemotherapy
Alkaloid; Vinca Alkaloid |
IV only; biliary excretion. Binds to microtubules
------> inhibits the mitotic spindle, causing metaphase arrest.
More likely to show bone marrow toxicity than Vincristine.
Indications: Testicular carcinoma, breast cancers, lymphomas. |
| Vincristine |
Chemotherapy
Alkaloid; Vinca Alkaloid |
IV only; biliary excretion. Binds to microtubules
------> inhibits the mitotic spindle, causing metaphase arrest.
Less likely to suppress bone marrow than Vinblastine, but do see
peripheral neuropathy which is dose-limiting.
Indications: Part of the MOPP group of drugs, to fight
Hodgkin's Disease. Also acute leukemias, Non-Hodgkin's
Lymphomas. |
| Glutatione S-Transferases (GST's) |
Chemotherapy; Adjunct |
Experimental. In rats and monkeys, when injected
directly into lymphocytes (inject in vitro and then reimplant
in the animal), it prevents lymphocyte death, helping
to alleviate bone-marrow suppression before it occurs. Hasn't been tried
in humans yet. |
| Granulocyte Colony Stimulating Factor
(G-CSF) |
Chemotherapy; Adjunct |
It is thought to mobilize peripheral
hematopoeitic stem cells. It can be given to combat the bone-marrow
suppression side-effects of chemotherapy drugs. |
| Ondansetron |
Chemotherapy; Adjunct |
Serotonin antagonist can be given to alleviate nausea
associated with chemotherapy. Phenothiazines and other
drugs can also be used. |
| Verapamil |
Chemotherapy; Adjunct |
Ca+2-channel blocker can competitively
inhibit phosphoglycoprotein pumps in tumor cells, thus
hopefully helping to combat this form of resistance. Clinical trials are
under way. |
| Busulfan |
Chemotherapy; Alkylating Agent
Alkylsulfonate |
Alkylsulfonate, pro-drug, oral. Indicated for
Chronic Myelogenous Leukemia.
Adverse Effects: Adrenal Insufficiency, increased skin pigmentation.
Pulmonary fibrosis. |
| Thiotepa |
Chemotherapy; Alkylating Agent
Aziridine |
Aziridine, pro-drug. IV. |
| Triethylene malamine |
Chemotherapy; Alkylating Agent
Aziridine |
Aziridine, pro-drug. IV. |
| Procarbazine |
Chemotherapy; Alkylating Agent
Hydrazine |
Hydrazine. Part of the MOPP group of drugs, to fight
Hodgkin's Disease. Adverse Effects: Has especially high
incidence of secondary malignancies, particularly
leukemias. |
| Chlorambucil |
Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, Oral. Indicated for lymphomas,
CLL. |
| Mechlore thamine |
Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, IV. Directly toxic. It has the
shortest half-life (a few minutes) and is the least stable of all
alkylating agents. Is often infused directly into artery supplying the
tumor, due to its short half-life. Part of the MOPP group of drugs, to
fight Hodgkin's Disease. |
| Melphalan |
Chemotherapy; Alkylating Agent
Nitrogen Mustard |
Nitrogen Mustard, Oral. Indicated for Multiple
Myeloma. |
| Cyclopho sphamide |
Chemotherapy; Alkylating Agent
Nitrogen Mustard
Immunosuppressant |
Pro-drug, oral. It is converted to its active
form by Cytochrome-P450 enzyme.
Broad-spectrum agent Useful at fighting solid tumors,
leukemias, ovarian carcinoma.
Immunosuppresant: Bone marrow transplants (but it does not
prevent GVHD), autoimmune disorders (PRCA, Wegener's Granulomatosis).
Adverse Effect: Hemorrhagic cystitis, higher incidence
of alopecia than other drugs. |
| Carmustine (BCNU) |
Chemotherapy; Alkylating Agent
Nitrosurea |
Nitrosurea, pro-drug. IV. Gets into CNS, thus
useful for treating brain cancers. |
| Lomustine (CCNU) |
Chemotherapy; Alkylating Agent
Nitrosurea |
Nitrosurea, pro-drug. IV. Gets into CNS, thus
useful for treating brain cancers. |
| Streptozotocin |
Chemotherapy; Alkylating Agent
Nitrosurea |
Indicated for malignant pancreatic insulinoma. |
| Carboplatin |
Chemotherapy; Alkylating Agent
Platinum Complex |
Platinum complex, similar to Cis-Platin. |
| Cis-Platin |
Chemotherapy; Alkylating Agent
Platinum Complex |
Forms Platinum complex, a unique
platinum-bond with DNA causes both damage and cross-linkage of DNA
strands. Broad-spectrum agent. Useful at fighting solid tumors:
breast, ovarian, testicular, lung, bladder cancers.
Adverse Effect: Relatively non-toxic to bone marrow, but does have
nephrotoxicity which is dose-limiting. |
| Bleomycin |
Chemotherapy; Antibiotic |
Only IV. Bleomycin hydrolase
inactivates the drug in the liver and kidney, but the enzyme is not
found in skin and lungs.
It is the only cell-cycle specific (CCS) agent among
the antibiotics. It intercalates between DNA base pairs, and it also
chelates iron, generating oxygen radicals
which further damage the DNA.
Indicated for testicular carcinoma. Adverse Effects: Irreversible
pulmonary fibrosis. |
| Dactinomycin |
Chemotherapy; Antibiotic |
Only IV. It tightly intercalates DNA between G-C base
pairs, blocking transcription. DNA replication is only
slightly affected. |
| Mithramycin |
Chemotherapy; Antibiotic |
|
| Mitomycin C |
Chemotherapy; Antibiotic |
Only IV. It is metabolized to 6-Mercaptopurine,
active metabolite, which then cross-links with DNA.
Indications: Solid tumors of cervix, stomach, pancreas, lung,
bladder, colon. May be instilled directly into bladder to treat
bladder carcinoma. Adverse Effects: pronounced and long-lived
bone-marrow suppression. |
| Plicamycin |
Chemotherapy; Antibiotic |
Only IV. It binds to DNA as a ternary complex with Mg+2,
blocking transcription.
Indications: used primarily to combat paraneoplastic
hypercalcemia. It has an inhibitory effect on osteoclasts,
slowing down bone resorption. |
| Daunorubicin |
Chemotherapy; Antibiotic
Anthracycline |
Only IV. Undergoes extensive metabolism in the liver.
They are intercalating agents, blocking both
replication and transcription by non-covalent interactions. Adverse
Effect = Cumulative cardiotoxicity, which can be
potentially fatal.
Indications: Narrower in spectrum, used only against Acute
Leukemias. |
| Doxorubicin |
Chemotherapy; Antibiotic
Anthracycline |
Only IV. Undergoes extensive metabolism in the liver.
They are intercalating agents, blocking both
replication and transcription by non-covalent interactions. Cumulative
cardiotoxicity, which can be potentially fatal.
Indications: Broad-spectrum agent, used in combo
chemotherapy to treat many tumors. |
| Mitoxantrone |
Chemotherapy; Antibiotic
Anthracycline; Synthetic |
The only synthetic anti-cancer antibiotic, with
properties similar to the other Anthracyclines. They are
intercalating agents, blocking both replication and
transcription by non-covalent interactions. Cumulative
cardiotoxicity, which can be potentially fatal.
Indications: Used for Acute Myelogenous Leukemia (AML),
non-Hodgkin's Lymphomas, breast cancer. |
| 5-Fluorouracil (5-FU) |
Chemotherapy; Antimetabolite |
Pyrimidine antagonist. Must be given IV. Active
metabolite is 5-FdUMP, which inhibits
thymydilate synthetase ------> cell death due to lack of
thymine. Resistance: decreased bioactivation of 5-FU, mutations in
thymydilate synthetase, increased levels of thymidilate synthetase.
Indications: GI tumors, head and neck carcinomas. |
| 6-Mercaptopurine (6-MP) |
Chemotherapy; Antimetabolite |
Purine antagonist. Effective orally. It is converted to
its active nucleotide form by HGPRT. Resistance primarily due to lower
amounts of HGPRT; increased levels of alkaline phosphphydrolase can also
inactivate the active metabolites.
Drug is eliminated by xanthine oxidase, so Allopurinol
raises its blood levels and potentiates its effects. |
| 6-Thioguanine (6-TG) |
Chemotherapy; Antimetabolite |
Purine antagonist. Effective orally. It is converted to
its active nucleotide form by HGPRT. Resistance primarily due to lower
amounts of HGPRT; increased levels of alkaline phosphphydrolase can also
inactivate the active metabolites. |
| Azacitidine |
Chemotherapy; Antimetabolite |
|
| Cytarabine (Cytosine Arabinoside, AraC) |
Chemotherapy; Antimetabolite |
Pyrimidine antagonist. Must be given IV. Active
metabolite is AraCTP, which inhibits DNA
polymerase during the S-Phase. Resistance: decreased uptake of
AraC by tumor cells, decreased conversion of AraC to AraCTP, increased
breakdown of AraCTP. Indicated for acute leukemias (ALL)
and lymphomas.
Adverse Effects: Ocular toxicity, neurotoxicity. |
| Floxuridine |
Chemotherapy; Antimetabolite |
Pyrimidine antagonist. |
| Fludarabine |
Chemotherapy; Antimetabolite |
Pyrimidine antagonist. |
| Gemcitabine |
Chemotherapy; Antimetabolite |
Pyrimidine antagonist, similar to Cytarabine. |
| Aminoglu tethamide |
Chemotherapy; Hormonal Agent |
Aromatase Inhibitor decrease the
conversion of androstenedione to estrone. Interrupts estrogen synthesis
and is thus useful in metastatic breast cancer. |
| Diethyl stilbestrol (DES) |
Chemotherapy; Hormonal Agent |
Can induce remission of prostatic carcinoma. |
| Estrogens |
Chemotherapy; Hormonal Agent |
Can induce remission of prostatic carcinoma. |
| Flutamide |
Chemotherapy; Hormonal Agent |
Anti-androgen used in the treatment of
prostate cancer. |
| Leoprulide Acetate |
Chemotherapy; Hormonal Agent |
Synthetic analog of GnRH ------> blocks FSH and LH in
pituitary ------> decreased androgen synthesis and an inhibitory effect
on prostatic carcinoma. |
| Progestins |
Chemotherapy; Hormonal Agent |
Can induce remission of metastatic endometrial
cancer. Has shown some success with breast cancer. |
| Tamoxifen |
Chemotherapy; Hormonal Agent |
Estrogen receptor antagonist is
effective against susceptible breast cancers. The tumor
must have an estrogen-receptor to be susceptible. |
