| Drug Name |
Category |
Comments |
| Streptozotocin |
Chemo therapy; Alkylating Agent
Nitrosurea |
Indicated for malignant pancreatic insulinoma. |
| Carboplatin |
Chemo therapy; Alkylating Agent
Platinum Complex |
Platinum complex, similar to Cis-Platin. |
| Cis-Platin |
Chemo therapy; 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 |
Chemo therapy; 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 |
Chemo therapy; Antibiotic |
Only IV. It tightly intercalates DNA between G-C base pairs,
blocking transcription. DNA replication is only slightly
affected. |
| Mithramycin |
Chemo therapy; Antibiotic |
|
| Mitomycin C |
Chemo therapy; 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 |
Chemo therapy; 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 |
Chemo therapy; 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 |
Chemo therapy; 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
chemo therapy to treat many tumors. |
| Mitoxantrone |
Chemo therapy; 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) |
Chemo therapy; Antime tabolite |
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-Mercap topurine (6-MP) |
Chemo therapy; Antime tabolite |
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) |
Chemo therapy; Antime tabolite |
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 |
Chemo therapy; Antime tabolite |
|
| Cytarabine (Cytosine Arabinoside, AraC) |
Chemo therapy; Antime tabolite |
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 |
Chemo therapy; Antime tabolite |
Pyrimidine antagonist. |
| Fludarabine |
Chemo therapy; Antime tabolite |
Pyrimidine antagonist. |
| Gemcitabine |
Chemo therapy; Antime tabolite |
Pyrimidine antagonist, similar to Cytarabine. |
| Aminoglu tethamide |
Chemo therapy; Hormonal Agent |
Aromatase Inhibitor decrease the conversion of
androstenedione to estrone. Interrupts estrogen synthesis and is thus
useful in metastatic breast cancer. |
| Diethylstilbestrol (DES) |
Chemo therapy; Hormonal Agent |
Can induce remission of prostatic carcinoma. |
| Estrogens |
Chemo therapy; Hormonal Agent |
Can induce remission of prostatic carcinoma. |
| Flutamide |
Chemo therapy; Hormonal Agent |
Anti-androgen used in the treatment of
prostate cancer. |
| Leoprulide Acetate |
Chemo therapy; Hormonal Agent |
Synthetic analog of GnRH ------> blocks FSH and LH in pituitary
------> decreased androgen synthesis and an inhibitory effect on
prostatic carcinoma. |
| Progestins |
Chemo therapy; Hormonal Agent |
Can induce remission of metastatic endometrial cancer.
Has shown some success with breast cancer. |
| Tamoxifen |
Chemo therapy; Hormonal Agent |
Estrogen receptor antagonist is effective against
susceptible breast cancers. The tumor must have an
estrogen-receptor to be susceptible. |
| Corticosteroids
(Prednisone, etc.) |
Chemo therapy; Hormonal Agent
Anti- Inflammatory; Anti-RA
Immuno suppressant |
Actions: (1) They inhibit Phospolipase-A2,
(2) They inhibit the induction of COX-2
Chemo therapy: They suppress proliferation of lymphocytic cells, thus
they are useful at combating lymphomas. Part of the MOPP group of drugs,
to fight Hodgkin's Disease.
RA: It is a potent anti-inflammatory, but it does nothing to prevent
destruction of bone and cartilege.
Immuno suppressant: Organ transplantation, auto-immune diseases,
asthma. |
| Amsacrine (AMSA) |
Chemo therapy; Miscellaneous |
|
| Hydroxyurea |
Chemo therapy; Miscellaneous |
|
| L-Asparaginase |
Chemo therapy; Miscellaneous |
For Leukemia. Leukemic cells are deficient in asparagine
synthetase and thus cannot replenish asparagine when it is
broken down by this drug. That makes them selectively susceptible to the
drug. Adverse Effects: Allergy, hepatitis, mental depression,
pancreatitis. |
| Erythropoeiten |
Hemopoeitic; Anemia |
Useful for treating the hypoproliferative anemia caused by
end-stage renal disease. Produced by recombinant DNA
techniques. |
| Ferrous Fumarate |
Hemopoeitic; Anemia
Iron- Deficiency Anemia |
Like Ferrous Sulfate |
| Ferrous Sulfate |
Hemopoeitic; Anemia
Iron- Deficiency Anemia |
Take them on an empty stomach. Enteric-coated iron preparations are
not used, because we want to absorb the iron in the stomach and proximal
duodenum. 200-400 mg of iron daily are required to
treat iron deficiency.
Adverse Effects: Black stools, constipation, nausea, epigastric
discomfort, abdominal cramps, diarrhea. |
| Ferrous Gluconate |
Hemopoeitic; Anemia
Iron- Deficiency Anemia |
Like Ferrous Sulfate |
| Iron Dextran |
Hemopoeitic; Anemia
Iron- Deficiency Anemia |
Parenteral iron administration, IM or IV. IM can be painful.
Indications: Parenteral iron is given for severe iron
deficiency, after a bowel resection or after Inflammatory Bowel
Disease involving the proximal jejunum.
Adverse Effects: Headache, light-headedness. Nausea, vomiting, back
pain, fever, arthralgia, urticaria, anaphylaxis (rare), flushing. |
| Folic Acid |
Hemopoeitic; Anemia
Megaloblastic Anemia |
Folic acid will cure dietary folate deficiency. It will not
cure folate deficiency due to anti-folate drugs (such as Trimethoprim).
For that you use folinic acid.
No adverse effects. |
| Hydroxy cobalamin
(Vitamin B12) |
Hemopoeitic; Anemia
Megaloblastic Anemia |
IM. Highly bound to plasma proteins and remains in circulation
longer than cyanocobalamin. Therapy continues for life. |
| Cyanocobalamin
(Vitamin B12) |
Hemopoeitic; Anemia
Megaloblastic Anemia
Toxicity |
IM. The drug of choice in patients who are hypersensitive to the
Hydroxy cobalamin -Transcobalamin-II Complex. Therapy continues for life.
Cyanide Toxicity: Co2 EDTA +
Hydroxy cobalamin takes up free cyanide, neutralizing it and forming
cyanocobalamin (Vit B12). |
| Dextran |
Hemopoeitic; Clotting
Anti-Coagulant |
Used to prevent post-operative thrombosis. Long
chain sugars physically interfere with platelet function and fibrin
polymerization. |
| Heparin |
Hemopoeitic; Clotting
Anti-Coagulant |
IV or SQ anti-coagulant. It potentiates Antithrombin-III
and is monitored using the PTT. It has a fast onset of
action and short duration of action. |
| Warfarin
(Coumadin) |
Hemopoeitic; Clotting
Anti-Coagulant |
Oral anti-coagulant. It is an analog of Vitamin-K
and inhibits Vit-K-dependent factors. It is monitored using the
PT. It has a slow onset of action and longer duration of
action. It is eliminated by P450 metabolism and has lots of drug
interactions. |
| Dipyridamole |
Hemopoeitic; Clotting
Platelet Inhibitor |
Inhibits phosphodiesterase ------> potentiate
prostacyclin, which is a cAMP dependent factor.
In combination with warfarin, it is effective in preventing arterial
embolization in patients with prosthetic heart valves. |
| Ticlopidine |
Hemopoeitic; Clotting
Platelet Inhibitor |
Inhibits ADP-Induced platelet aggregation. Effective in preventing
the recurrence of arterial thrombosis in patients with a history of MI,
Transient Ischemic Attacks (TIA's), stroke, unstable angina pectoris.
Adverse Effects: GI Disturbances in 20% of patients, Hemorrhage in 5%
of patients, Leukopenia in 1% of patients. |
| Timolol |
Hemopoeitic; Clotting
Platelet Inhibitor
beta-Blocker |
Has been approved for the prophylaxis and prevention of first MI. It
is not known whether the beneficial effects are due to inhibited
platelets, beta-blocking activity, or combination of both. |
| Desmopressin Acetate |
Hemopoeitic; Clotting
Prothrom bogenic |
Useful as an adjunct in treatment of mild Hemophilia A.
It potentiates the activity of Factor VIII. |
| Factor VIII |
Hemopoeitic; Clotting
Prothrom bogenic |
Given to treat primary Hemophilia A (Factor VIII
Deficiency). Administration of the blood-derived factor carries a risk
of getting viral infections such as Hepatitis-C. |
| Aminocaproic Acid |
Hemopoeitic; Clotting
Prothrom bogenic
Toxicity |
They inhibit the conversion of plasminogen to plasmin. Used as
adjunctive therapy in treating hemophilias.
Indicated for tPA, streptokinase toxicity. |
| Factor IX |
Hemopoeitic; Clotting
Prothrom bogenic
Toxicity |
Given for treatment of warfarin overdose, whenever
immediate coagulation needs to take effect.
Given to treat primary Hemophilia B (Factor IX
Deficiency). Administration of the blood-derived factor carries a risk
of getting viral infections such as Hepatitis-C. |
| Phytonadione
(Vitamin-K) |
Hemopoeitic; Clotting
Prothrom bogenic
Toxicity |
Given for treatment of warfarin overdose, or
whenever the effects of warfarin need to be reversed, such as in
preparation for surgery. The effect is delayed by about 24 hours, the
time required to synthesize new clotting factors.
Given prophylactically before gallbladder surgery. |
| Tranexamic Acid |
Hemopoeitic; Clotting
Prothrom bogenic
Toxicity |
Analog of aminocaproic acid. They inhibit the conversion of
plasminogen to plasmin. Used as adjunctive therapy in treating
hemophilias.
Indicated for tPA, streptokinase toxicity. |
| Anistreplase |
Hemopoeitic; Clotting
Thrombolytic Agent |
The acylated form of the Streptokinase-Plasminogen Activated Complex
(APSAC); no risk of systemic fibrinolysis. Longer
lasting than the others. Infused IV for 3-5 minutes. |
| Streptokinase |
Hemopoeitic; Clotting
Thrombolytic Agent |
From Streptococcus. Can cause systemic fibrinolysis and DIC.
May see allergies, in patients who have anti-streptococcal antibodies.
Given as IV loading dose, then 24-48 hours of infusion. |
| Tissue Plasminogen Activator (tPA) |
Hemopoeitic; Clotting
Thrombolytic Agent |
Active only at the site of the clot; no risk of systemic
fibrinolysis. Given as IV loading dose, then 2 hours of infusion.
Particularly efficacious for post-MI treatment, and
that is the only indication currently approved.
Adverse Effect: Higher risk for hemorrhagic stroke
than with the other drugs. |
| Urokinase |
Hemopoeitic; Clotting
Thrombolytic Agent |
Isolated from human kidney. Can cause systemic fibrinolysis and DIC.
Given as IV loading dose, then 12 hours of infusion. |
| Adjuvants
Bacille Calmette-Guerin (BCG) |
Immuno modulating Agent |
Attenuated M. Bovis strain can be employed as
immunostimulant in cancer therapy. It activates macrophages,
making them more apt at killing tumor cells. |
| Inosiplex |
Immuno modulating Agent |
Enhanced T-Cell and monocyte activities. Potentially useful in AIDS. |
| Thymosin |
Immuno modulating Agent |
10 kDa protein. Thymic hormone that induces and stimulates the
maturation of lymphoid stem-cells and pre-T-Cells into T-Cells.
Indications: DiGeorge Syndrome, other conditions of
T-Cell Deficiency. |
| Levamisole |
Immuno modulating Agent
Anti- Inflammatory; Anti-RA |
It is an immunostimulatory drug that has
paradoxical effect in treating RA. Treament has not yet been approved by
FDA. Latency period of 3 - 4 months. May also be useful for Hodgkin's
Disease. |
| Tacrolimus (FK-506) |
Immuno suppressant
Anti-Bacterial; Macrolide |
Macrolide antibiotic of fungal origin, similar in use to
Cyclosporin. Used in situations where Cyclosporin is ineffective, toxic,
or cannot otherwise be used. |
| Anti-Lymphocyte Globulin |
Immuno suppressant
Antibody |
It activates complement-mediated destruction of lymphocytes ------>
decreased cellular immunity. There is little effect on
humoral immunity. Indications: Organ transplantations, GVHD.
Adverse Effects: Pain, erythema, possibly lymphoma at site of
injection. Anaphylactic shock, serum sickness. |
| Anti-T-Cell Antibody OKT3 |
Immuno suppressant
Antibody |
Mouse monoclonal antibody against the CD3 T-Cell Receptor.It
inhibits the interaction between antigen-presenting cells and T-Cells.
Indications: Kidney transplantation. |
| Anti-Thymocyte Globulin |
Immuno suppressant
Antibody |
Indications: Idiopathic aplastic anemia, or to
counter the auto-immune effects of gamma-Interferon, secondary to
hemopoeitic suppression. |
| Rh0(D) Globulin
(Rhogam) |
Immuno suppressant
Antibody |
For the primary prevention of Erythroblastosis Fetalis
(hemolytic anemia of newborn). It is given to Rh- mothers, 72
hours after first childbirth of an Rh+ fetus, to
prevent formation of anti-Rh antibodies in the mother. |
| Methotrexate |
Immuno suppressant
Chemo therapy; Antime tabolite
Anti-RA |
Inhibits dihydrofolate reductase. Well absorbed orally, or
intrathecal. Polyglutamic-acid conjugates of methotrexate are retained
intracellularly, where they have activity.
Indications: GVHD, Acute Lymphocytic
Lymphoma, Choriocarcinoma, RA, psoriasis.
Adverse Effects: Oral, gastric ulcerations, and
liver cirrhosis with long-term use. High dose
methotrexate may be followed by high-dose folinic acid
in order to "rescue" the anti-folate effects of the
drug. |
| Cyclosporin A |
Immuno suppressant
Chemo therapy; Miscellaneous |
From the fungus, Tolypocladium Inflatum. Binds to
cyclophillins ------> inhibit IL-2 production
in T-Cells ------> inhibit T-Cell differentiation and activation.
Extensive Cyt-P450 metabolism.
Indications: Suppress organ rejection after transplantation, IDDM.
Adverse Effects: Viral infections, lymphoma. Nephrotoxicity, but it
can be prevented with mannitol. |
| Azathioprine |
Immuno suppressant
Chemo therapy; Miscellaneous
Anti-RA |
Pro-drug, it is converted by glutathione S-transferase to
6-Mercaptopurine, active form of drug. It is toxic to
proliferating T-Cells and B-Cells, after antigen exposure. Allopurinol,
renal disease raise its blood levels.
Indications: kidney transplants, autoimmune diseases
(glomerulonephritis, hemolytic anemia).
Adverse Effects: Nausea, vomiting, diarrhea. Bone marrow suppression.
Fever, skin rashes. Liver dysfunction and jaundice, ocassionally.
Azothioprine or Methotrexate can be used to treat severe RA. |
| 2-PAM
(Pralidoxime) |
Toxicity |
Organophosphate poisoning: Only effective within
the first few minutes of exposure. It is a strong nucleophile that can
bind with the organophosphate, releasing it from cholinesterase, before
the bond has aged. |
| 4- methyl pyrazole |
Toxicity |
A specific inhibitor of alcohol dehydrogenase that
may be used instead of ethanol, for methanol and
ethylene glycol poisoning.
|
| Atropine |
Toxicity |
Treatment of choice after the bond has aged and become irreversible,
in organophosphate poisoning. First-line treatment for
carbamate poisoning. |
| Defero xamine (Desferal) |
Toxicity |
IM or IV to chelate iron in blood, for iron toxicity. |
| Digoxin- specific antibody fragments. |
Toxicity |
Indicated for Digitalis toxicity. |
| Ethanol |
Toxicity |
It is given to displace the substrates and prevent their metabolism,
in methanol and ethylene glycol poisoning.
Prevent methanol from going to formic acid, and prevent
ethylene glycol from going to oxalic acid. |
| Factor IX |
Toxicity |
Used for immediate coagulation, in the event of warfarin
toxicity. |
| Fluazenil |
Toxicity |
Indicated for Benzodia zepine toxicity. |
| Methylene Blue |
Toxicity |
Indicated for treatment of methemoglobinemia, such
as that due to nitrite poisoning. Methylene Blue speeds
the conversion of methemoglobin back to hemoglobin. |
| N- Acetyl cysteine |
Toxicity |
Indicated for Acetominophen toxicity. It provides
reduced sulfhydryl groups and restores glutathione to its reduced form. |
| Nalorphine |
Toxicity |
Indicated for opioid overdose, alternative to
naloxone. |
| Naloxone |
Toxicity |
Opioid antagonist, indicated for acute opioid toxicity. |
| Nitrite |
Toxicity |
It causes methemoglobinemia which can then bind up
all of the extra cyanide, driving it away from the cytochrome oxidase.
For cyanide poisoning. |
| Phytonadione (Vitamin-K) |
Toxicity |
Given to reverse the effects of warfarin toxicity,
but it takes 24 hours to take effect. |
| Protamine Sulfate |
Toxicity |
Given IV for treatment of heparin overdose. It is a
basic peptide that binds to heparin. Must dose it carefully, as
protamine sulfate is itself an anti-coagulant! |
| Prussian Blue |
Toxicity |
Thallium poisoning: It interrupts the enterohepatic
circulation of Thallium, enhancing its excretion. |
| Pyridoxine (Vit B6) |
Toxicity |
Can reverse convulsions and peripheral neuritis associated with
Isoniazid toxicity. |
| Thiosulfate |
Toxicity |
Given to promote the formation of thiocyanate and its subsequent
excretion, in cyanide poisoning. |
| Dimercaprol
(British Anti-Lewisite, BAL) |
Toxicity
Metal Chelator |
Administered in oil by deep IM injection. Fast-acting and short
half-life. Enters tissues more readily than does EDTA.
Forms stable complexes with mercury, arsenic, gold.
It can free the sulfahydral compounds bound by the metals, but it is
better at primary prevention. Adverse Effects: It can cause transient
hypertension.
Used in combination with CaNa2 EDTA for lead poisoning,
particularly when there are signs of Lead Encephalopathy. |
| Edetate Calcium Disodium
(CaNa2 EDTA) |
Toxicity
Metal Chelator |
Poor oral absorption. Usually administered IV or IM. Half-life 20 -
60 minutes. Urinary excretion. Water soluble; does not easily enter
tissues or get into cells.
Indications: Primarily used for lead poisoning. Not
effective against mercury, arsenic, most other metals. |
| Succimer |
Toxicity
Metal Chelator |
New drug that can be given PO. Both urinary and
biliary excretion, with enterohepatic circulation.
Chemically similar to Dimercaprol.
Indications: Severe Lead Poisoning: Used to treat
children with lead poisoning above 45 �g / dL. It does not metabolize
essential minerals like zinc, copper, iron, making it more attractive.
Has been shown in labs to chelate arsenic, cadmium, mercury. |
