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129 Cards in this Set
- Front
- Back
Constant proportion 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 myelosuppression
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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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Nephro and 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 this 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 used for HD, but appears 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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CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
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Regimen used for breast cancer
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CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
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Alkylating agent, vesicant that causes tissue damage with extravasation
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Mechlorethamine
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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 hemorrhagic cystitis
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Hydration and 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 which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
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Paclitaxel (taxol)
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Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
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Cisplatin
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Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
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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 estrogen 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 (eg., 5-FU, 6-MP, methotrexate, etoposide)
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Some cell cycle non-specific drugs
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Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
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Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin 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) and lomustine (CCNU)
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Produces disulfiram-like reaction with ethanol
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Procarbazine
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Common side effect of hypnotic agents
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Sedation
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Occurs when sedative hypnotics are used chronically or at high doses
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Tolerance
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The most common type of drug interaction of sedative hypnotics with other depressant medications
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Additive CNS depression
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Benzodiazepines used to promote sleep
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Temazpam, trizolam, flurazepam
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Benzodiazepine used for anxiety
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Alprazolam
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Non-benzodiazepine used as an anxiolytic
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Buspirone
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Non-benzodiazepine used for sleep
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Zolpidem
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Major effect of benzodiazepines on sleep at high doses
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REM is decreased
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Neurologic SE of benzodiazepines
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Anterograde amnesia
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Reason benzos are used cautiously in pregnancy
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Ability to cross the placenta
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Main route of metabolism for benzodiazepines
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Hepatic
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Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
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Lorazepam, oxazepam, and temazepam
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MOA of benzodiazepines
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increase the FREQUENCY of GABA-mediated chloride ion channel opening
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Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
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Flumazenil
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Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
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Diazepam
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Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
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Clonazepam
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Benzodiazepines that are the most effective in the treatment of panic disorder
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Alprazolam and Clonazepam
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Benzodiazepine that is used for anesthesia
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Midazolam
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DOC for status epilepticus
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Diazepam
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Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
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Chlordiazepoxide and Diazepam
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sedative/hypnotic agents having active metabolites, long half lives, and a high incidence of adverse effects
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Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
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Barbiturates may precipitate this hematologic condition
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Acute intermittent porphyria
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Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
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Liver enzyme INDUCTION
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Barbiturates MOA
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Increase the DURATION of GABA-mediated chloride ion channels
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Barbiturate used for the induction of anesthesia
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Thiopental
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Site of action for zaleplon and zolpidem
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Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
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Good hypnotic activity with less CNS SE than most benzodiazepines
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Zolpidem, zaleplon
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Agent that is a partial agonist for the 5-HT1A receptor
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Buspirone
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Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
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Buspirone
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Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
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Ethanol
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Agent with zero-order kinetics
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Ethanol
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Rate limiting step of alcohol metabolism
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Aldehyde dehydrogenase
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System that increases in activity with chronic ethanol exposure and may contribute to tolerance
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MEOS
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Enzyme that metabolizes acetaldehyde to acetate
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Aldehyde dehydrogenase
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Agents that inhibit alcohol dehydrogenase
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Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
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Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
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Disulfiram
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The most common neurologic abnormality in chronic alcoholics
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Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
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Agent that is teratogen and causes a fetal syndrome
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Ethanol
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Agent that is the antidote for methanol overdose
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Ethanol, fomepizole
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Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
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Fomepizole
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MOA of general anesthetics
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Most are thought to act at GABA-A receptor - chloride channel
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Inhaled anesthetic with a low blood/gas partition coefficient
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Nitrous oxide
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Inversely related to potency of anesthetics
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Minimum alveolar anesthetic concentration (MAC)
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Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
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Halothane and methoxyflurane
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Most inhaled anesthetics SE
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Decrease arterial blood pressure
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Inhaled anesthetics are myocardial depressants
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Enflurane and halothane
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Inhaled anesthetic causes peripheral vasodilation
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Isoflurane
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Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
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Halothane
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Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
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Nitrous oxide
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Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
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Methoxyflurane
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Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
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Nitrous oxide
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Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
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Desflurane
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DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
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Dantrolene
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IV barbiturate used as a pre-op anesthetic
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Thiopental
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Benzodiazepine used adjunctively in anesthesia
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Midazolam
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Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
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Flumazenil
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This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
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Ketamine
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Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
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Fentanyl
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State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
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Neuroleptanesthesia
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Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
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Propofol
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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
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Neuromuscular blocking drugs
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These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
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Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
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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)
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Nondepolarizing type antagonists
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Agent with long duration of action and is most likely to cause histamine release
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Tubocurarine
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Non-depolarizing skeletal muscle antagonist that has short duration
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Mivacurium
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Skeletal muscle agent that can block muscarinic receptors
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Pancuronium
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Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
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Atracurium
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One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
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Succinylcholine
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During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
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Cholinesterase inhibitors
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Drugs decrease intestinal absorption of cholesterol
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Bile acid-binding resins
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Cholestyramine and colestipol are
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Bile acid-binding resins
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Major nutritional side effect of bile acid-binding resins
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Impair absorption of fat soluble vitamin absorption (A,D,E,K)
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MOA of lovastatin (STATIN)
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inhibits HMG COA reductase
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HMG CoA reductase inhibitors are contraindicated in
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Pregnancy
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MOA of drug or foods (grapefruit juice) that increase statin effect
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Inhibit Cytochrome P450 3A4
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SE of HMG COA reductase inhibitors
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Rhabdomyolysis and Hepatotoxicity
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Monitoring parameter to obtain before initiation of STATINS
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LFT's
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Decreases liver triglycerol synthesis
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Niacin
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SE of niacin
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Cutaneous flush
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Cutaneous flush can be reduced by pretreatment with
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Aspirin
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Fibrates (gemfibrozil) increase activity of
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lipoprotein lipase
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Most common SE of fibrates
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Nausea
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Fibrates are contraindicated in
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Pregnancy
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Concurrent use of fibrates and statins increases risk of
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Rhabdomyolysis
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New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
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ezetimibe (Zetia)
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