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90 Cards in this Set
- Front
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Time it takes for drug to fall to half its value; this is constant in first order kinetics (majority of drugs)
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Half life (T1/2)
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Relates to amount of drug in the body to the plasma concentration
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Volume of distribution (Vd)
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Plasma concentration of a drug at a given time
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Cp
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The ratio of the rate of elimination of a drug to its plasma concentration
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Clearance (Cl)
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Elimination of a drug that occurs before it reaches systemic circulation
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First pass effect
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Fraction of administered dose of a drug that reaches systemic circulation
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bioavailability
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When rate of drug input equals the rate of drug elimination
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Steady state
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This step of metabolism makes a drug more hydrophilic and hence augments elimination
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Phase 1
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Different steps of Phase I
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hydrolysis, oxidation, reduction
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Inducers of Cytochrome P450
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rifampin, barbiturates, phenytoin, carbamazepine
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Inhibitors of CYP450
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grapefruit juice, ketaconazole, cimetidine, erythromycin
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Products of Phase II conjugation
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glucoronate, acetic acid, glutathione sulfate
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Type of kinetics when a constant percentage of substrate is metabolized per unit
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First order kinetics
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Drug elimination with a constant amount metabolized regardless of drug concentration
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Zero order kinetics
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Target plasma concentration times (volume of distribution divided by bioavailability)
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Loading dose (Cp * (Vd/F)
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Concentration in plasma times (clearance divided by bioavailability)
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Maintenance dose (Cp * (Cl/F)
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Strength of interaction between a drug and its receptor
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Affinity
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Selectivity of a drug for its receptor
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Specificity
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Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
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Potency
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Maximum response achievable from a drug
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Efficacy
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Ability of drug to produce 100% of the maximum response regardless of the potency
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Full agonist
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Ability to produce less than 100% of the response
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Partial agonist
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Ability to bind reversibly to the same site as the drug and without activating the effector system
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Competitive antagonist
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Class of drugs with ability to decrease the maximal response to an agonist
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Noncompetitive antagonist
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A hormone whose mechanism of action utilizes intracellular receptors
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Thyroid hormones
steroid hormones |
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A hormone whose MOA utilizes transmembrane receptors
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Insulin
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Class of drugs whose MOA utilizes ligand gated ion channels
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Benzodiazepines
calcium channel blockers |
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Median effective dose required for an effect in 50% of population
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ED50
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Median toxic dose required for a toxic effect in 50% of the population
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TD50
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Dose which is lethal to 50% of the population
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LD50
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Window between therapeutic effect and toxic effect
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Therapeutic index
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Term for high margin of safety
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High therapeutic index
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Term for narrow margin of safety
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Low therapeutic index
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Antidote used for lead poisoning
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Dimercaprol
EDTA |
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Antidote used for cyanide poisoning
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Nitrites
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Antidote used for anticholinergic poisoning
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Physostigmine
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Antidote used for organophosphate/anticholinesterase poisoning
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Atropine
pralidoxime (2-PAM) |
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Antidote used for iron salt toxicity
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Deferoxamine
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine (Mucomyst)
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Antidote for arsenic, mercury, lead and gold poisoning
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Dimercaprol
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, arsenic
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Penicillamine
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Antidote used for heparin overdose
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Protamine
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Antidote used for warfarin toxicity
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Vitamin K
Fresh Frozen Plasma |
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid
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Antidote used for methanol and ethylene glycol
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Ethanol
Fomepizol |
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Antidote used for opiod toxicity
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Naloxone (IV)
Naltrexone (oral) |
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Antidote used for benzodiazepine toxicity
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Flumanezil
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Antidote used for tricyclic antidepressants (TCA)
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sodium bicarbonate
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Antidote used for carbon monoxide poisoning
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100% Oxygen (O2)
Hyperbaric O2 |
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Antidote used for digitalis toxicity
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Digibind (also need to d/c digoxin, normalize potassium, and lidocaine is patient is arrhythmic).
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Antidote for beta agonist toxicity (eg. metaproterenol)
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Esmolol
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Antidote for methotrexate toxicity
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Leucovorin
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Antidote for beta blockers and hypoglycemia
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Glucagon
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Antidote useful for some drug induced Torsade de pointes
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Magnesium sulfate
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Antidote for hyperkalemia
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Sodium polystyrene sulfonate (kayexalate)
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Constant proporation of cell population killed rather than a constant number
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log-kill hypothesis
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Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
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Pulse therapy
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Toxic effect of anticancer drug can be lessened by rescue agents
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rescue therapy
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Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
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Allopurinol
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Pyrimidine analog that causes "thymine-less death" given with leucovorin rescue
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5-flouracil (5-FU)
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Drug used in cancer therapy causes Cushing-like symptoms
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Prednisone
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Side effect of mitomycin
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SEVERE myelosuppresion
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MOA of cisplatin
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Alkylating agent
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Common toxicities of cisplatin
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Nephrotoxicity
Ototoxicity |
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Analog of hypoxanthine, needs HGPRTase for activation
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6-mercaptopurine (6-MP)
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interaction with drug requires dose reduction of 6-MP
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Allopurinol
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May protect against doxorubicin toxicity by scavenging free radicals
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Dexrazoxane
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Blows DNA (breaks DNA strands) limiting SE is pulmonary fibrosis
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Bleomycin
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Bleomycin + vinblastine + etoposide + cisplatin produce almost a 100% response when all agents are used for this neoplasm
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Testicular cancer
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ABVD regimen for HD, but appers less likely to cause sterility and secondary malignancies than MOPP
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Adriamycin (Doxorubicin)
Bleomycin Vinblastine Dacarbazine |
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Regimen used for non-Hodgkin's lymphoma
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CDVP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
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Regimen used for breast cancer
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CMF (cyclophosphamide, methotrexate, and flourouracil)
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Alkylating agent, vesicant that causes tissue damage with extravasation
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Meclorethamine
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Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
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Cyclophosphamide
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Prevention of cyclophosphamide induced hemorragic cystitis
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Hydration
mercaptoethanesulfonate (MESNA) |
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Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
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Vincristine
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Interact with microtubules (but unlike vinca whch prevent disassembly tubules), it stabilizes tubulin and cells remain frozen in metaphase
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Paclitaxol (taxol)
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Toxicities include nephrotoxicity and ototoxicity, leading to severe interaction with aminoglycosides
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Cisplatin
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Agent similar to cisplatin, less nephrotoxic, but greater myelosuppresion
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Carboplatin
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Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
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L-asparaginase
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Used for hairy cell leukemia; it stimulates NK cells
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interferon alpha
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Anti-androgen used for prostate cancer
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Flutamide (eulexin)
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Anti-estrogen used for esterogen receptor + breast cancer
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Tamoxifen
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Aromatase inhibitor used in breast cancer
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Letrozole
Anastrozole |
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Newer estrogen receptor antagonist used in advanced breast cancer
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Toremifene (Fareston)
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Some cell cycle specific anti-cancer drugs
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Bleomycin
Vinca alkaloids Antimetabolites: 5-FU, 6-MP, methotrexate, etoposide |
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Soem cell cycle non-specific drugs
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Alkylating agents: meclorethamine, cyclophosphamide
Antibiotics: doxorubicin, daunorubicin Cisplatin Nitrosourea |
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Anti-emetics used in assocation with anti-cancer drugs that are 5-HT3 (serotoning receptor subtype) antagonists
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Odansetron
Granisetron |
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Nitrosoureas with high lipophilicity, used for brain tumors
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Carmustine (BCNU)
Lomustine (CCNU) |
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Produces disulfarim-like reaction with ethanol
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Procarbazine
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