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129 Cards in this Set

  • Front
  • Back
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue
5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
Side effect of Mitomycin
SEVERE myelosuppression
MOA of cisplatin
Alkylating agent
Common toxicities of cisplatin
Nephro and ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6-MP
Allopurinol
May protect against doxorubicin toxicity by scavenging free radicals
Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
Bleomycin
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular cancer
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphoma
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
Prevention of cyclophosphamide induced hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA)
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Vincristine
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxel (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Carboplatin
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
Used for hairy cell leukemia; it stimulates NK cells
Interferon alpha
Anti-androgen used for prostate cancer
Flutamide (Eulexin)
Anti-estrogen used for estrogen receptor + breast cancer
Tamoxifen
Aromatase inhibitor used in breast cancer
Letrozole, anastrozole
Newer estrogen receptor antagonist used in advanced breast cancer
Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonists
Odansetron, granisetron
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU) and lomustine (CCNU)
Produces disulfiram-like reaction with ethanol
Procarbazine
Common side effect of hypnotic agents
Sedation
Occurs when sedative hypnotics are used chronically or at high doses
Tolerance
The most common type of drug interaction of sedative hypnotics with other depressant medications
Additive CNS depression
Benzodiazepines used to promote sleep
Temazpam, trizolam, flurazepam
Benzodiazepine used for anxiety
Alprazolam
Non-benzodiazepine used as an anxiolytic
Buspirone
Non-benzodiazepine used for sleep
Zolpidem
Major effect of benzodiazepines on sleep at high doses
REM is decreased
Neurologic SE of benzodiazepines
Anterograde amnesia
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
Main route of metabolism for benzodiazepines
Hepatic
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
MOA of benzodiazepines
increase the FREQUENCY of GABA-mediated chloride ion channel opening
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Diazepam
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
Clonazepam
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
Benzodiazepine that is used for anesthesia
Midazolam
DOC for status epilepticus
Diazepam
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
sedative/hypnotic agents having active metabolites, long half lives, and a high incidence of adverse effects
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
Barbiturates may precipitate this hematologic condition
Acute intermittent porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Liver enzyme INDUCTION
Barbiturates MOA
Increase the DURATION of GABA-mediated chloride ion channels
Barbiturate used for the induction of anesthesia
Thiopental
Site of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
Agent that is a partial agonist for the 5-HT1A receptor
Buspirone
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Buspirone
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Ethanol
Agent with zero-order kinetics
Ethanol
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
System that increases in activity with chronic ethanol exposure and may contribute to tolerance
MEOS
Enzyme that metabolizes acetaldehyde to acetate
Aldehyde dehydrogenase
Agents that inhibit alcohol dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Disulfiram
The most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
Agent that is teratogen and causes a fetal syndrome
Ethanol
Agent that is the antidote for methanol overdose
Ethanol, fomepizole
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Fomepizole
MOA of general anesthetics
Most are thought to act at GABA-A receptor - chloride channel
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC)
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Halothane and methoxyflurane
Most inhaled anesthetics SE
Decrease arterial blood pressure
Inhaled anesthetics are myocardial depressants
Enflurane and halothane
Inhaled anesthetic causes peripheral vasodilation
Isoflurane
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Halothane
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Nitrous oxide
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Methoxyflurane
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous oxide
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
Desflurane
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene
IV barbiturate used as a pre-op anesthetic
Thiopental
Benzodiazepine used adjunctively in anesthesia
Midazolam
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
Flumazenil
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
Ketamine
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
Fentanyl
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
Neuroleptanesthesia
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Propofol
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
Nondepolarizing type antagonists
Agent with long duration of action and is most likely to cause histamine release
Tubocurarine
Non-depolarizing skeletal muscle antagonist that has short duration
Mivacurium
Skeletal muscle agent that can block muscarinic receptors
Pancuronium
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
Atracurium
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
Succinylcholine
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Cholinesterase inhibitors
Drugs decrease intestinal absorption of cholesterol
Bile acid-binding resins
Cholestyramine and colestipol are
Bile acid-binding resins
Major nutritional side effect of bile acid-binding resins
Impair absorption of fat soluble vitamin absorption (A,D,E,K)
MOA of lovastatin (STATIN)
inhibits HMG COA reductase
HMG CoA reductase inhibitors are contraindicated in
Pregnancy
MOA of drug or foods (grapefruit juice) that increase statin effect
Inhibit Cytochrome P450 3A4
SE of HMG COA reductase inhibitors
Rhabdomyolysis and Hepatotoxicity
Monitoring parameter to obtain before initiation of STATINS
LFT's
Decreases liver triglycerol synthesis
Niacin
SE of niacin
Cutaneous flush
Cutaneous flush can be reduced by pretreatment with
Aspirin
Fibrates (gemfibrozil) increase activity of
lipoprotein lipase
Most common SE of fibrates
Nausea
Fibrates are contraindicated in
Pregnancy
Concurrent use of fibrates and statins increases risk of
Rhabdomyolysis
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
ezetimibe (Zetia)