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Flashcards in Drug Table - Complete Deck (328)
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1

Alkylating Agents Mechanism

Produce strong electrophiles throughcarbonium or ethyleneimonium ionintermediates, which covalently bond viaalkylation of nucleophilic moieties in DNA(mostly N7 position of guanine); Cell CycleNon-Specific (CCNS)

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Alkylating Agents Important Side Effects

Bone marrow, mucosal toxicity,nausea and vomiting, toxic effectson reproductive systems,increased leukemia risk

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Alkylating Agents Miscellaneous

Resistance may occur due to:decreased permeability or uptake;increased rates of catabolism;enhanced DNA repair; increasedglutathione production (inactivatesvia conjugation)

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List 11 Alkylating Agents

Mechlorethamine (Mustargen)Cyclophosphamide (Cytoxan)Ifosfamide (Ifex)Carmustine (Gliadel)Lomustine (Ceenu)Dacarbazine (DTIC)Procarbazine (Matulane)Temozolomide (Temodar)Cisplatin (Platinol)Carboplatin (Paraplatin)Oxaliplatin (Eloxatin)

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Mechlorethamine class

(Mustargen)Nitrogen mustard

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Mechlorethamine mechanism

Alkylating agent; spontaneous conversion to active metabolites in body fluids orenzymatically converted in liver

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Mechlorethamine Therapeutics

Hodgkin's disease, topically for treatment of cutaneous T-cell lymphoma

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Mechlorethamine "Other" side effects

Severe nausea and vomiting,myelosuppression (leucopenia,thrombocytopenia)

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Mechlorethamine Misc

Don't use much anymore due to sterility

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Cyclophosphamide(Cytoxan)Class

Nitrogen mustard

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Cyclophosphamide(Cytoxan)Mechanism

Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard

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Cyclophosphamide(Cytoxan)Therapeutics

Most widely used alkylating agent (broad clinical spectrum); singly or incombination for ALL, CLL, non-Hodgkin's lymphoma, and breast, lung, and ovarian cancer

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Cyclophosphamide(Cytoxan)Important Side Effects

Hemorrhagic cystitis (bladderirritation) due to acrolein (toxicdrug metabolite); adequatehydration and administration ofMESNA (2-mercaptoethanesulfonate) minimizes problem

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Cyclophosphamide(Cytoxan)"Other" Side Effects

Nausea, vomiting,myelosuppression

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Cyclophosphamide(Cytoxan)Miscellaneous

Relatively long plasma half-life (7-15 hrs); taken orally

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Difference between Ifosfamide and Cyclophosphamide

TherapeuticsIfos is used for Sarcoma and testicular cancerCyclophosphamide is the most widely used

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Carmustine (Gliadel)Lomustine (Ceenu)Class

Nitrosoureas

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Carmustine (Gliadel)Lomustine (Ceenu)Mechanism

Alkylating agent

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Carmustine (Gliadel)Lomustine (Ceenu)Therapeutics

Brain tumors (cross blood-brain barrier)

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Carmustine (Gliadel)Lomustine (Ceenu)Imp Side Effects

Renal toxicity, pulmonary fibrosis

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Carmustine (Gliadel)Lomustine (Ceenu)Other side effects

Profound myelosuppression,severe nausea and vomiting

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Dacarbazine (DTIC)class

Triazenes

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Dacarbazine (DTIC)Mechanism

Alkylating agent; prodrug activated by livercytochromes

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Dacarbazine (DTIC)Therapeutics

Part of ABVD for Hodgkin's disease; also, malignant melanoma

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Dacarbazine (DTIC)"Other" Side Effects

Nausea and vomiting,myelosuppression (neutropenia, thrombocytopenia), flu-likesymptoms (fever, fatigue)

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Dacarbazine (DTIC)Miscellaneous

IV administration

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Procarbazine(Matulane)class

Triazenes

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Procarbazine(Matulane)Mechanism

Alkylating agent; forms free radicals

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Procarbazine(Matulane)Therapeutics

Hodgkin's lymphoma

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Procarbazine(Matulane)Important side effects

May cause leukemia