Chemotherapy Drugs (A - Doc)

The following list of chemotherapeutic agents is not all inclusive, but many commonly used medications are described.

BCNU (Carmustine): administration is via the intravenous route over 15-45 minutes. Shorter infusions are associated with severe burning along the vein and generalized flushing. Side effects include bone marrow suppression, which is often delayed. Other effects include pain at the intravenous site; marked facial flushing and nausea and vomiting. Rare side effects include liver and kidney toxicity, which is generally reversible. With long term therapy pulmonary scarring may occur (leading to shortness of breath) with a high mortality (death) rate.

Bleomycin (Blenoxane): administration may be either by the intramuscular, intravenous, intraarterial, subcutaneous or intracavitary route. Side-effects include severe febrile reactions (high fevers); skin reactions (increased coloration- hyperpigmentation) as well as skin inflammation and swelling and thickening of the nail beds. Hair loss, itchiness and headache are also potential side effects. Cumulative doses greater than 400U are associated with increased risk of pulmonary toxicity.

Busulfan (Myleran): administration is via the oral route (pills). Side effects include decreased white counts at low doses and suppression of all cell lines (pancytopenia) at high doses. Interstitial lung fibrosis (lung scarring with decreased function leading to shortness of breath) can occur and may rarely be fatal. Hormonally, gynecomastia (growth of breast tissue) may occur as well as testicular atrophy, erectile dysfunction (impotence) and loss of menses (amenorrhea). Decreased adrenal gland function may occur. Additionally, hyperpigmentation of the skin may be seen.

Carboplatinum (Paraplatin): administration is via the intravenous route over 15 minutes or longer. The dose limiting toxic effect is bone marrow suppression, particularly lowering of the platelet counts (thrombocytopenia) leading to increased risk of bleeding. Nausea and vomiting, nephrotoxicity (manifested by kidney damage, neurotoxicity (manifested by tingling and numbness of the hands and feet) and ototoxicity (manifested by decreased hearing ability) are significantly less than with Cis-platin. Other rare side effects (occurring less than 3% of the time) include hair loss, skin rash, mouth sores and a flu-like syndrome.

CCNU (Lomustine): administered orally. The drug should be taken on an empty stomach. The dose limiting toxicity is bone marrow suppression leading to increased risk of infection, bleeding and anemia. Other effects include diarrhea, loss of appetite and rarely confusion, lethargy and ambulation problems (ataxia). Hair loss and temporary liver dysfunction may occur.

Chlorambucil (Leukeran): administration is orally (with pills). Bone marrow suppression leading to decreased white cells, red cells and platelets is the dose limiting toxicity. At high doses central nervous system effects are noted (seizure, coma). Gastrointestinal distress can occur although not often. With long term use pulmonary scarring can occur. Lastly, spermatogenesis (production of sperm) is depressed during therapy with this drug.

2-Cholrodeoxyadenosine (2-CDA; Cladribine, Leustatin): administered intravenously as a continuous infusion over 5-7 days. The major side effect is decreased neutrophil counts (a type of white blood cell) and a more prolonged suppression of the helper and suppressor lymphocyte counts. This may lead acutely to increased risk of bacterial infections and a delayed, increased risk of developing opportunistic infections secondary to drug induced immunosuppression. About 50% of patients taking this drug also develop a rash.

Cis-platinum (Platinol): administered intravenously. The patient should be well hydrated prior to administration of the drug. It has been shown that administration in the face of poor hydration increases the likelihood of developing side effects. In patients with kidney dysfunction, impaired hearing, preexisting peripheral nerve damage (neuropathy) or past history of allergies to platinum this medication should be given (if at all) with extreme caution. Side effects include nausea and vomiting, anaphylactic reactions (consisting of fast heart rate, wheezing, lowered blood pressure and facial edema), kidney damage (nephrotoxicity), decreased hearing (ototoxicity), nerve damage (neurotoxicity; peripheral neuropathy) manifested by tingling and numbness of the hands and/or feet, bone marrow suppression with increased risk of bleeding and infection, electrolyte (sodium, potassium and magnesium) disturbances and possible heart toxicity (manifested by EKG changes) may be seen. It is important to discuss these issues with your physican so htat you may inform him/her of any symptoms, which may be attributable to the use of this drug.

Cytarabine (Ara-C): can be administered by either the subcutaneous, intramuscular or intravenous routes. Dose limiting effects are generally secondary to bone marrow suppression. However, high cumulative doses can lead to permanent central nervous system damage (noted by the development of cerebellar dysfunction). The cerebellar dysfunction consists of slurring of speech, walking problems, as well as eye motion problems and other neurological problems. Cerebellar dysfunction tends to occur more often in patients older than 50 years of age. Other potential side effects are skin rash, nausea and vomiting, diarrhea, loss of appetite, mild to moderate mouth sores, transient liver dysfunction and the development of a flu-like syndrome with fevers, body aches and rashes. Rarely, fluid in the lungs (pulmonary edema) not related to heart malfunction can occur.

Cyclophosphamide (Neosar; CTX): may be administered orally or intravenously. Side effects include bone marrow suppression, hemorrhagic cystitis (severe inflammation of the bladder with blood in the urine), hair loss, electrolyte imbalances (especially sodium), gastrointestinal toxicity as manifested by nausea and vomiting and possible liver dysfunction. A rare lung toxicity manifested by lung inflammation and similar to "Busulfan lung" has been seen. Sexually, testicular atrophy, loss of periods (menses) and ovarian failure can occur.

Daunorubicin (Cerubidine): should be administered as a short intravenous "push" infusion over 1-5 minutes. The drug can cause severe deep tissue damage if extravasted (injected in the soft tissues instead of a vein); a constantly attended slow intravenous injection (2-3 minutes) is generally recommended. Side effects include bone marrow suppression. Gastrointestinal effects include stomatitis (sores at the corners of the mouth); nausea and vomiting and rarely diarrhea. The use of this medication can cause hair loss (involving all body hair areas); a generalized rash; discoloration of the nail beds. Additionally, this drug can reactivate skin damage from prior radiotherapy (called radiation recall effect). Daunorubicin usually does not impart specific side effects in the kidney or liver; however, it can impart a red color to the urine (not a toxicity) and in patients with liver dysfunction the dose of the drug should be modified.

Extravasation leads to painful soft tissue ulcers, which heal poorly, if at all. Surgical excision of necrotic areas is recommended to prevent progressive ulceration into adjacent tissues. There are no good antidotes for this complication.

The major risk factor in the use of this drug is the development of cardiotoxicity. It manifests as congestive heart failure with symptoms of fatigue, decreased exercise tolerance secondary to shortness of breath. This complication is total dose dependent (that is at low doses the risk is low but above a certain threshold the risk rapidly raises). The package insert calls for halting therapy after a total cumulative dose of 550 mg/m2 has been attained (this correlates with a 1-2% incidence of congestive heart failure). In patients with prior radiotherapy involving the heart area and in patients with preexisting heart disease or prior therapy with Daunorubicin or similar drugs total doses should be lowered as they are at increased risk of cardiotoxic effects.

Docetaxel (Taxotere): administered via intravenous infusion. The dose limiting side effect is neutropenia (low white count) and less often decreased platelets (thrombocytopenia). Hypersensitivity reactions have also been noted; additionally, drug-associated edema has been seen. The edema includes fluid around the lungs (pleural effusions) and edema of the legs.

Publication Review By: Stanley J. Swierzewski, III, M.D.

Published: 15 Aug 1999

Last Modified: 13 Oct 2011