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M2 Fall > Pharmocology Unit 2 > Flashcards

Pharmocology Unit 2 Flashcards

1
Q

mechloroethylamine

A 
anti-tumor alkylating agent; bischloroethyl amine
DNA alkylating/damaging agent
highly reactive, metabolized quickly
can cause necrosis at infusion site (IV)
adverse: secondary cancers
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2
Q

cyclophosphamide

A

anti-tumor alkylating agent; bischloroethyl amine
less reactive; requires activation in liver or tumor tissue
adverse: hemorrhagic cystitis, SIADH-like syndrome, secondary cancers

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3
Q

nitrosoureas

A

Class of alkylating agents
crosses BBB; useful in brain tumors
little cross-resistance with other alkylating agents
risk of secondary cancers

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4
Q

procarbazine

A

alkylating agent; metabolized to alkylating and radical (reactive) metabolites
Used in Hodgkin’s disease MOPP regimen
leukemogenic (5-10%risk with MOPP use)

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5
Q

methotrexate

A

anti-tumor antimetabolite; folic acid analog; DHFR inhibitor; blocks DNA, RNA synthesis (S specific)
accumulates as ployglutamate derivative
adverse: renal and hepatic dysfunction

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6
Q

leucovorin

A

famyl H4-folate; rescue from methotrexate; bypasses DHFR in thymidine synthesis

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7
Q

6-mercaptopurine

A

purine antagonist; inhibit de novo purine synthesis (S specific)
fraudulent base incorporation; ctiviated by HGPRT
downregulation of HGPRT in resistance
inactvated by xanthine oxidase (administartion with allopurinol (XO inhibitor) increases concentration and effective cytotoxicity)

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8
Q

mechanisms of methotrexate resistance

A

amplifaction of DHFR
DHFR gene mutation
decreased drug uptake
increased drug efflux

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9
Q

6 thioguanine

A

purine antagonist; inhibit de novo purine synthesis (S specific)
fraudulent base incorporation; ctiviated by HGPRT
downregulation of HGPRT in resistance

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10
Q

5-FU (fluorouracil)

A

pyrimidine antagonist; metabolite inhibits thymidylate synthetase (thymidine synthesis)
fraudulent base incorportaion (S specific)
adverse: severe diarrhea

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11
Q

capecitabine

A

oral prodrug of fluorouracil; preferentially activated in tumor tissue;
used in colon cancer and refractory brease cancer

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12
Q

cytarabine (cytosine arabinoside)

A

converted to araCTP and inhibits DNA synthesis; fradulent incorporation;
activation requires deoxycytidine kinase;
mutational loss of deoxycytidine kinase -> tumor resistance
adverse: cerebellar dysfunction, fever

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13
Q

daunorubcin

A

anti-tumor antibiotic; anthracycline
broad spectrum use; DNA intercalation (mutagenic, carcinogenic)
topoisomerase II inhibitor
irreversible cardiac toxicity at high dose

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14
Q

doxorubicin

A

anti-tumor antibiotic; anthracycline
broad spectrum use; DNA intercalation (mutagenic, carcinogenic)
topoisomerase II inhibitor, DNA scission
irreversible cardiac toxicity at high dose

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15
Q

bleomycin

A 
anti-tumor antibiotic;
DNA scission; free radical production
broad spectrum use
Used in Hodgkin's lymphoma ABVD regimen
adverse: pulmonary fibrosis, anaphylaxis, fever
no significant myelosuppression
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16
Q

vinblastine

A

mitotic spindle poison (M specific); vinca alkaloid
mitotic arrest (inhibit microtubule polymerization)
effective in Hodgkin and other lymphome ABVD
side effects: nausea, vomiting, dose-limiting myelosuppression
resistance from tubulin mutations

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17
Q

ABVD

A

doxorubicin (adriamycin), bleomycin, vinblastine, dacarbazine

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18
Q

vincristine

A

mitotic spindle poison (M specific); vinca alkaloid
mitotic arrest binds tubulin; Used in Hodgkin’s MOPP regimen, acute childhoos leukemia
adverse: milder side effects than vinbastine (no myelosuppression); significant neurotoxocity/ peripheral neuropathy/ SIADH
resistance from tubulin mutations

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19
Q

paclitaxel

A

mtotic spindle poison; plant alkaloid; enhances tubulin polymerization (blocks disassembly)
Used in ovarian and advanced breast cancers
adverse: neuropathy

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20
Q

topotecan

A

camptothecin topoisomerase inhibitor; binds cleavage complex of topo I and DNA -> blocks religation -> double strand breaks (S specific)
Uses: ovarian, lung cancer
Adverse: dose-limiting myelosuppression

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21
Q

irinotecan

A

camptothecin topoisomerase inhibitor; binds cleavage complex of topo I and DNA -> blocks religation -> double strand breaks (S specific)
Uses: colorectal cancer
Adverse: severe diarrhea, irinotecan and metabolite induce muscarinic agonist effects (prevented with atropine premedication)

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22
Q

etoposide

A

topo II inhibitor; form complex with topo II and DNA, interfere with religation of ds break; DNA strand scission

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23
Q

cisplatin

A

platinum coordination complex; DNA cross-linking; may inhibit DNA biosynthesis; used in various regimens
Uses: ovarian and testicular cancer
Adverse: nephrotoxicity (alleviate c hydration), acoustic nerve dysfunction (tinnitus)

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24
Q

tamoxifen

A

estrogen receptor competitive partial agonist (SERM);
Used: estrogen dependent breast cancer/ prophylaxis, reduced risk of fx in postm women
Adverse:low toxicity, manageable side effects; risk of thrombosis/ endometrial cancer

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25
Q

raloxifene

A

SERM; used for estrogen dependant breast cancer; reduced risk of thrombosis and endometrial cancer; prevention of breast cancer in patients with osteoporosis

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26
Q

letrozole

A

aromatase inhibitor; blocks estrogen production in postm women; not used in pre-m woem; more effective than tamoxifen in ER+ breast cancer and tamoxifen-resistant tumors
adverse: joint pain, loss of bone density

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27
Q

anastrozole

A

aromatase inhibitor; blocks estrogen production in postm women; not used in pre-m woem; more effective than tamoxifen in ER+ breast cancer and tamoxifen-resistant tumors
adverse: joint pain, loss of bone density

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28
Q

exemstane

A

aromatase inhibitor; blocks estrogen production in postm women; not used in pre-m woem; more effective than tamoxifen in ER+ breast cancer and tamoxifen-resistant tumors; reduces risk of breast cancer in high risk post-m women
adverse: joint pain, loss of bone density

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29
Q

leuprolide

A

anti-androgen therapy; synthetic analog of GnRH
pulsatile: elevates andro/estro in men and women
continuous (depot): lowers andro/estro in men/women
Uses: androgen ablation, as effective as estrogen therpay or orchietctomy in prostate cancer

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30
Q

flutamide

A

anti-androgen; androgen receptor antogonist; ineffective alone against prostate cancer (rapid receptor mutation); Used in conjunction with leuprolide to block initial rise in androgen levels and “flare” of prostate cancer

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31
Q

prednision

A

induces apoptosis in leukemia cells; used in multidruf therapies for leukemia, lymphoma, and myeloma;induces remission in childhood leukemias; palliative agent (decrease nausea, inflammation)

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32
Q

erlotinib

A

small molecule EGFR inhibitor; non-small cell lung cancer; head and neck cancers (clinical trials)

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33
Q

cetuximab

A

chimeric ant-EGFR antibody; colon and head and neck cancers

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34
Q

EGF-receptor tyrosine kinase

A

oncogene; overexpressed/mutationally active in l;ung, brain, colon, head and neck cancers

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35
Q

lapatinib

A

small molecule EGFR and HER2 kinase inhibitor in breast cancer (clinical trials)

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36
Q

trastuzumab

A

humanized anti-HER2 antibody for HER2+ breast cancer; refractory metastatic breast cancer

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37
Q

imatinib

A

small molecule bcr/abl tyrosine kinase inhibitor; used for chronic myelogenous leukemia (bcr/abl mutation)

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38
Q

brentuximab

A

chimeric IgG anti-CD30 surface antigen antibody; conjugated to vedotin (mitotic spindle poison); used for Hodgkin’s lymphoma and anaplastic large cell lymphoma; IgG-vedotin is internalized and toxin is exposed to specific CD30+ tumor cell “magic bullet”

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39
Q

ifosfamide

A

bifunctional alkylator

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40
Q

chlorambucil

A

bifunctional alkylator

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41
Q

carmustine

A

alkylator

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42
Q

lomustine

A

alkylator

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43
Q

busulfan

A

alkylator

adverse: pulmonary fibrosis

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44
Q

dacarbazine

A

alkylator

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45
Q

carboplatin

A

platinum coordination complex; DNA cross-linking; may inhibit DNA biosynthesis; used in various regimens
Uses: ovarian and testicular cancer
Adverse: nephrotoxicity (alleviate c hydration), acoustic nerve dysfunction (tinnitus);

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46
Q

hydromorphone

A

mu opioid analgesic; IV, PO; more lipid soluble than morphine, faster onset; 5X potency; hydromorphone-6-glucuronide less active than morphine-6-glucuronide, hydromorphone-3-glucuronide inactive)

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47
Q

hydrocodone

A

mu opioid analgesic; combined with acetaminophen (vicodin, lortab); metabolized to hydromorphone (CYP2D4); #1 Rx in US today

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48
Q

oxycodone

A

mu opioid analgesic; solo or combined with acetaminophen (percocet); sustained release form. greater bioavailabilty than morphine; metabolized to oxymorphone CYP2D4

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49
Q

oxymorphone

A

mu opioid analgesic; PO; available in extended release; not popular with FDA

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50
Q

codeine

A

weak analgesic; pro-drug converted to morphine (CYP2D4); pharmacogenetic variability clinically significant (inactive prodrug vs active metabolite); anti-tussive effect

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51
Q

heroin

A

mu opioid analgesic; pro-drug converted to manoacetyl morphine; fast onset, lipis soluble, quick access to brain (deactylated); increased euphoria

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52
Q

methadone

A

mu opioid analgesic; PO; lutralong acting (half-life 15 to 60 hrs); maintenance of opioid drug addiction and pain management; slow onset, long acting, no euphoria, no withdrawal

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53
Q

meperidine

A

mu opioid analgesic; IV, poor oral absorption; less potent than morphine 1/10X; converted to nor-meperidine by liver -> CNS stimulation, convulsions; renal failure prolongs half-life; use has decreased; involved with old MAOIs in serotonin syndrome

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54
Q

fentanyl

A

mu opioid analgesic; patch for chronic pain, oral (lollipop, sublingual); IV, epidural, intrathecal (subarachnoid); used in anesthetics

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55
Q

tramadol

A

mu partial agonist and monoamine reuptake inhibitor; weak analgesic + nonopioid analgesic effects; metabolized by CYP2D4, CYP3A4 high pharmacogenetic variability; mild to moderate acute and chronic pain

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56
Q

tapentadol

A

mu partial agonist and monoamine reuptake inhibitor; weak analgesic + nonopioid analgesic effects; less pharmacogenetic variability than tramadol, metabolized by UDP glucuronosyltransferase 1; mild to moderate acute and chronic pain

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57
Q

pentazocine

A

kappa agonist/mu partial agonist

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58
Q

butorphanol

A

kappa agonist/mu partial agonist

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59
Q

nalbuphine

A

kappa agonist/mu partial agonist; can reverse respiratory depression, mild analgesia reversal, leads to dysphoria, potential inductino of withdrawal; billed as non-addictive, not true

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60
Q

buprenorphine

A

kappa agonist/mu partial agonist; high affinity for mu receptor; dificult to provide analgesia; utility for drug abuse and addiction; 7-day patch; con produce withdrawal

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61
Q

diphenoxylate

A

opioid agnoist; oral, poor Gi absoption; antidiarrheal

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62
Q

loperamide

A

opioid agnoist; oral, poor Gi absoption; antidiarrheal

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63
Q

naloxone

A

opioid antagonist; parenteral; prevent/antagonize effects of analgesics

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64
Q

naltrexone

A

opioid antagonist; oral; prevent/antagonize effects of analgesics

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65
Q

alvimopan

A

opioid antagonist; oral, poorly absorbed by GI; prevents opioid Gi effects without effecting analgesia

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66
Q

methylnaltrexone

A

opioid antagonist; quaternary ammonium derivative; IV; peripherally restricted opioid antagonist for constipation

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67
Q

morphine-naloxone

A

abuse resistant opioid; extended release morphine with sequestered naloxone

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68
Q

isoflurane

A

volatile general anesthetic; 1MAC=1.15% (potency); 1.4 blood:gas partition (solubility); irritation to airway, undergoes metabolism of 0.2%, myocardial depression is minimal; malignant hyperthermia

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69
Q

desflurane

A

volatile general anesthetic; 1MAC=7.25% (potency); 0.42 blood:gas partition; irritation to airway; undergoes metabolism os 0.2%; myocardial depression minimal; prompt onset/offset; $$$; malignant hyperthermia

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70
Q

sevoflurane

A

volatile general anesthetic; 1MAC=2.05% (potency); 0.68 blood:gas partition; no irritation to airway; undergoes metabolism of 2%-5% (significant bu tnot harmful); myocardial depression minimal; prompt onset/offset; malignant hyperthermia

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71
Q

Nitrous Oxide

A

volatile general anesthetic; 1MAC=105-110% (potency); 0.46 blood:gas partition; adjunct to potent volatile anesthetics; reduces MAC requirements; very soluble; little side effects; malignant hyperthermia

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72
Q

dantrolene

A

treatment for malignant hyperthermia induced by volatile anesthetics; blocks Ca2+ release from sarcolplasmic reticulum in skeletal muscle

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73
Q

propofol

A

anesthetic induction agent; also used for maintainence; cardiovascular and respiratory depression; cannot be antagonized; least “hangover” effect

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74
Q

etomidate

A

IV induction agent; produces respiratory depression; no cardiovascular depression; cannot be antagonized

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75
Q

ketamine

A

phencyclidine derivative; NMDA receptor anatgonist (glutamate); dissociative anesthetic; used for sedation, amnesia, analgesia; no respiratory or cardiovascular depression; cannot be antagonized; emergence delirium

76
Q

methohexital

A

oxybarbiturate

77
Q

thiopental

A

thiobarbiturate

78
Q

alfentanil

A

like fentanyl

79
Q

fentanyl (IV)

A

high lipid solubility; high potency; fast onset; short duration of action; very addicting; used as premedication; reduces MAC of volatile anesthetics; respiratory depression; no effect on BP; antagonist naloxone

80
Q

remifentanil

A

like fentanyl; metabolized by plasma esterase

81
Q

sufentanil

A

like fentanyl

82
Q

flumazenil

A

antagoinst for benzodiazepines

83
Q

midazolam

A

benzodiazepine; premedication; high lipid soluble; sedation and amnesia; IV benzodiazepine produces respiratory depression; antagonized by flumazenil; other benzodiazepines include diazepam and lorazepam

84
Q

barbiturates (anesthesia)

A

IV induction; highly lipid soluble; produces rapid, profound unconsciousness; marked respiratory depression; prompt recovery from redistribution form brain; no drugs available for reversal; decreased sympathetic outflow from brain; not currently used due to cost and “hangover” effect

85
Q

amitriptyline

A

tricyclic antidepressant

86
Q

nortryptiline

A

tricyclic antidepressant

87
Q

imipramine

A

tricyclic antidepressant

88
Q

amoxapine

A

tricyclic antidepressant

89
Q

tricyclic antidepressants

A

nonspecific blockers of monoamine reuptake; treat severe depression; also block muscarinic, adrenergic, and histamine receptors; oral, small intestine absorption; effect requires >2 wks; high lipis soluble; long half-life (40 hrs); high plasma protein binding (95%); hepatic metabolism, renal elimination

90
Q

tricyclic antidepressant side effects

A

antimuscarinic effects; cardiovascular overstimulation, slow AV conductance; ortho hyoptension; sedation; weight gain, sexual dysfunction; seizures; delirium, aggravation or psychosis, mania (bipolar)

91
Q

fluoxetine

A

SSRI

92
Q

citalopram

A

SSRI

93
Q

escitalopram

A

SSRI

94
Q

sertraline

A

SSRI

95
Q

SSRI

A

seretonin selective reuptake inhibitor; neurogenesis; oral, small intestine absorption; effet requres >2 wks; high lipid soluble; long half-life (3days); high plasma protein binding (95%); block several P450 enzyme; renal elimination;

96
Q

SSRI side effects

A

safer than TCAs: early onset nausea, anxiety, sleep disturbance/insomnia; laste onset: anorexia, sexual dysfunction, mania (bipolar)

97
Q

SSRI drug interactions

A

Blocks CYPs: TCAs, neuroleptic drugs, antiarrhythmic drugs, some beta-adrenergic antagonists

98
Q

vanlafaxine

A

SNRI; 27% bound to plasma proteins; metabolized by CEP2D6

99
Q

Duloxetine

A

SNRI; 97% bound to plasma proteins; metabolized by CYP1A2 and CYP 2D6; hepatotoxic (contraindicated in liver disease)

100
Q

SNRI

A

serotonin/norepi reuptake inhibitors; unrelated to TCAs; treat patients refractory to SSRIs; oral; half-life (12 hrs)

101
Q

SNRI side effects

A

less off-target effects than TCAs; nausea, anxiety, sleep disturbance/insomnia; sexual dysfunction; high doses incrase BP and HR

102
Q

Bupropion

A

atypical antidepressant; inhibits dopamine reuptake; useful in rapid-cycling bipolar disorder

103
Q

nefazodone

A

atypical antidepressant; inhibits reuptake of serotonin and blocks 5-HT2 receptors

104
Q

mirtazapine

A

atypical antidepressant; increases NE and serotonin release by blocking alpha-2 receptors

105
Q

attypical antidepressants use and side effects

A

used in combination with TCAs to lower side effeects; side effects include headache, nausea, tinnitus, insomnia, and nervousness

106
Q

phenelzine

A

MAO A- & B-type; oral

107
Q

tranylcypromine

A

MAO A- & B-type; oral

108
Q

selegiline

A

MAO B-type (MAO A-type at high concentrations); transdermal patch

109
Q

MAOIs

A

third-line drugs for those that dont respond to SSRIs or TCAs; irreversible and long-lasting inhibitors of MAO; increase presynaptic concentrations of monoamines; effects require >2 wks; eliminated by kidneys; effects persist long after drug use stops; severe and unpredicatble side effects

110
Q

MAO-A

A

deaminates dopamine, Norepi, and 5-HT

111
Q

MAO-B

A

deaminates dopamine

112
Q

MAO inhibitors side effects

A

CNS: hallucinations, agitation, hyperreflexia, convulsions; CV: ortho hypo, HTN, tachycardia; GI: constipation; combination with SSRI leads to serotonin syndrome; tyramine consumption leads to HTN, arrhythmia, stroke, headache, nausea

113
Q

Lithium Salts

A

drug of choice for bipolar maintainence; effect requires >3 wks; very toxic (low therapeutic index); blocks hydrolysis of inositol phosphate, blocks SK-3beta kinase, inhibits 5-HT1 receptors, enhances glutamate reuptake

114
Q

Li Salts pharmacokinetics

A

oral as carbonate or citrate salt; rapid absorption by GI tract; soluble ion, peak concentrations in 3 hrs; half-life (24 hrs); eliminated by kidney (reduced kidney fxn increases toxicity

115
Q

Li salts side effects

A

low therpeautic index; substitutes Na+; CV: arrhythmias; CNS: tremor, confusion, convulsions, coma; thyroid: dcrs fxn; renal: poly dipsia, polyuria, diabetes insipidous; teratogenic

116
Q

benzodiazepine

A

fist choice antianxiety; treat insomnia, anxiety, dystonia/spasticity; anticonvulsant (not first line)l; NOT general anesthetic, NOT analgesic; bind GABA receptor - facilitate GABA transmission; increases # of open channels and duration of open; metabolized by CYP3A4 and CYP2C19 -> urine elimination

117
Q

flumazenil

A

blocks effects of agnoinst and inverse aganist at GABA receptors. No biological function by itself; does not effect GABA function; short acting 5 min - 2hrs per IV reduced respiratory depression

118
Q

diazepam

A

BZ; peak 1-2 hrs; long half-life; used for anxiety, withdrawal, muscle relaxant; antiepileptic- emergency status epilepticus, myoclonic, absence; metabolized -fast> desmethyldiazepam -slow> oxazepam -> inactive

119
Q

chlordiazepam

A

..

120
Q

alprazolam

A

benzodiazepine; peak 1-2 hrs; short half-life; insomnia, anxiety; maetabolized -fast> alpha-OH metabolite -fast>inactive

121
Q

oxazepam

A

..

122
Q

lorazepam

A

BZ,; peak 1-6 hrs; intermediate half-life; insomnia, anxiety, muscle relaxnt; antiepileptic-emergency status epilepticus, myoclonic, absence; metabolized -inter>inactive

123
Q

midazolam

A

beznodiazepine; peak .2-1 hr; ultra-short half-life; pre-anestheic medication; metabolized -quick> apla-OH metabolite -fast> inactive

124
Q

benzodiazepine drug interactions

A

minimal induction of CYPs; severe CNS depression and death with other CNS depressants (EtOH)

125
Q

zolpidem

Zaleplon

A

non-BZ; act on BZ-site of GABA receptor; increases frequency of channel opening; peak PO 1-2 hrs; half-life 1.5-3 hrs; metabolized by CYP3A4 and aldehyde oxidase; induce sleep, hypnotic dose w/o respiratory or CV depression; IV or CV disease -> CV and respiratoy depression

126
Q

Barbiturates

A

advantages: effective and inexpensive; extesnively studies
disadvantages: dose-dependant respiratory depression, CV depression at hypnotic doses; induce CYPs; bind GABA receptor -> increase duration of channel open; metabolized by dealkylation, glucuronidation, excretion

127
Q

phenobarbital

A

barb; long (oral) onset; long half-life; antianxiety; anticonvulsant for simple partial, recurrent tonic-clonic, and febrile seizure; teratogenic

128
Q

pentobarbital

A

barb; short (IV) to inter onset; inter half-life; preop sedation

129
Q

amobarbital

A

barb; ultra-short(IV) onset; short half-life; preop sedation

130
Q

thiopental

A

barb; ultra-short (IV) onset; ultra-short half-life; anesthetic induction (balanced anesthesia)

131
Q

barbiturate dise effects/drug interactions

A

side effects: drowsiness, confusion, diminished motor and impaired judgment;CI: Pain-increase sensitivity to pain; respiratory insufficiency-depression
drug interactions: enhances CNS depressive effects of antipsychotics, antihistamines, EtOH; CYP induction (beta-blockers, Ca channel clockers, steroids, estrogens, phenothiazine, valproic acid, theophylline)
toxicity: toaxic at 10X hypnotic dose, respiratory depression CV collapse (fatal);

132
Q

propranolol

A

beta-adrenergic blocker, antianxiety; blocks autonomic effects of anxiety (palpitations, sweating, shaking)

133
Q

buspirone

A

partial agonist for 5-HT1A receptor; metabolized by CYP3A4; aanxiolytic effects wo CNS depression; onset of effect 1-3 wks

134
Q

carbamazepine

A

antiepileptic; inhibit voltage-gated Na channel reset - prolong refractory period, decrease firing; 1st choice partia simple, partial complex, and tonic-clonic, trigeminal neuralgia, bipolar disorder; hepatotoxic, teratogenic

135
Q

ethosuxidine

A

antiepileptic; inhibit Tvoltage-gated Ca channels -> inhibit rhythmic activity; absence seizures

136
Q

gabapentin

A

antiepileptic; GABA analog, enhances inhibitory GABAergic neutransission; blocks Ca channels; simple or copmplex partial, tonic-clonic; no plasma proteins; short half-life; no drug interactions

137
Q

lamotrigine

A

antiepileptic; inhibit voltage-gated Na channel reset - prolong refractory period, decrease firing; simple or complex parital, tonic-clonic

138
Q

phenytoin

A

antiepileptic; inhibit voltage-gated Na channel reset decrease firing; initial therpay for epilepsy in adults, parital simple, partial comples, tonic-clonic; emergency IV treatment for status epilepticus, arrhythmias; NOT for absence seizures; gingival hyperplasia, megaloblastic anemia, teratogenic

139
Q

valproic acid

A

antiepileptic; inhibit voltage-gated Na channel reset - prolong refractory period, decrease firing; inhibit T voltage-gated Ca channels -> inhibit rhythmic activity; enhances inhibitory GABAergic neurotransmission; myoclonic seizures, second line for tonic-clonic and absence; hepatotoxic, thrombocytopenia, teratogenic

140
Q

pregabalin

A

antiepileptic; blcoks Ca channels and release of glutamate; simple and complex partial; thrombocytopenia

141
Q

topiramate

A

antiepileptic; blocks Na channels, increases activity of postsynaptic GABA receptors; simple and partal seizures, tonic-clonis

142
Q

levetiracetam

A

antiepileptic; modifies glutamate and GABA release; adjuvant treatment for simple and complex parital, tonic clonis

143
Q

clonazepam

A

BZ; antiepileptic; enhanced GABAergic transmission; myoclonic and absence seizures

144
Q

chlorpromazine

A

antipsychotic; selective DA receptor antagoinst; low potency; antimuscarinic, antiadrenergic, anithistamine (H1); side efffects: anti-muscarinic, anti-adrenergic, antihistamine

145
Q

fluphenazine

A

antipsychotic; selective DA receptor antagoinst; high potency; available in slow release (IM)

146
Q

thiothixene

A

antipsychotic; selective DA receptor antagoinst; medium potency

147
Q

haloperidol

A

antipsychotic; selective DA receptor antagoinst; high potency; available slow release (IM)

148
Q

aripiprazole

A

antipsychotic; partial agonist of DA receptor, serotonin receptor antagonist; discontinuation must be done gradually to avoid withdrawal
sideeffects: anticholinergic, antiadrenergic, antihistamine

149
Q

clozapine

A

antipsychotic; selective DA/serotonin receptor antagonist; sideeffects: all receptors

150
Q

olanzapine

A

antipsychotic; selective DA/serotonin receptor antagonist; only one to outperform typicals; severe metabolic side effects: all receptors

151
Q

paliperidone

A

antipsychotic; selective DA/serotonin receptor antagonist; major active metabolite of risperidone; antimuscarinic

152
Q

quetiapine

A

antipsychotic; selective DA/serotonin receptor antagonist; sideeffects: all receptors

153
Q

risperidone

A

antipsychotic; selective DA/serotonin receptor antagonist; available slow release (IM); antimuscarinic

154
Q

prochlorperazine

A

antiemetic; low potency antipsychotic; H1 receptor blocker

155
Q

promethazine

A

antiemetic; low potency antipsychotic; H1 receptor blocker

156
Q

typical antipsychotics

A

symptomatic relief for 70% of patients; potency = D2 selectivity; 4-8 wks delay onset of action; metabolized by CYPs (2D6, 3A4); some tolerance, no physical dependence; increase prolactin release -> infertility, impotence

157
Q

neuroleptic malignant syndrome

A

antipsychotic side effect; instability and colapse of autonomic regulation; seen also in parkinson patients that stop dopamanergic therapy

158
Q

atypical antipsychotics

A

symptom relief for 70%; equal efficacy to typical

159
Q

levodopa

A

enhance DA synthesis; oral ; rapid absorbed from small intestine

160
Q

carbidopa

A

blocks LDOPA metabolism in periphery. increases LDOPA in brain; used with LDOPA

161
Q

entacapone

A

COMT inhibitor; decrease LDOPA metabolism in periphery; used with LDOPA+carbidopa

162
Q

selegiline

A

MAO-B inhibitor used PO; used with LDOPA; increases DA at synapse; decreases H202 production in brain; metabolized to methamphetamine and amphetamine

163
Q

rasagiline

A

MAO-B inhibitor used PO with LDOPA; like selegiline but not metabolized to amphetamine-like substance

164
Q

bromocriptine

A

D2 agonist and D1 partial agonist; parkinsons

165
Q

ropinirole

A

D2 and D3 agonist; parkinsons

166
Q

pramipexole

A

D2 and D3 agonist; parkinsons

167
Q

apomorphine

A

DA receptor agonist; used SubQ for “off” period acute treatment;

168
Q

benztropine

A

muscarinic antagonist for Parkinsons therpay; alleviate tremor and rigidity; not bradykinesia; typical antimuscarinic side effects

169
Q

trihexyphenidyl

A

muscarinic antagonist for Parkinsons therpay; alleviate tremor and rigidity; not bradykinesia; typical antimuscarinic side effects

170
Q

amantadine

A

increase DA release, block muscarinic, NMDA receptors; used for brdaykinesia and rigidity in parkinsons, not tremor; side effects: hallucinations, confusion, nausea, dizziness, rash on LE, do not take with CHF or glaucoma

171
Q

Donepezil

A

AChE for alzheimers therapy; half-life 70 hrs metabolized by CYPs (3A4, 2D6)

172
Q

galantamine

A

AChE for alzheimers therapy; half-life 7 hrs metabolized by CYPs (3A4, 2D6)

173
Q

rivastigmine

A

AChE for alzheimers therapy; half-life 1.5 hrs; metabolized by plasma ChE

174
Q

tacrine

A

AChE for alzheimers therapy; half-life 3 hrs; limited by hepatotoxicity; metabolized by CYPs (3A4, 2D6)

175
Q

memantine

A

NMDA receptor antagonist for alzheimers; low affinity (derived from amantadine); protects from excitotoxicity (Ca overload); additive effect with donepezil; side effects: dizziness headache, confusion, constipation

176
Q

acetazolamide

A

carbonic anhydrase inhibitor diuretic; inhibit HCO3 reuptake, reduce H excretion; K wasting; counters diuretic induced alkalosis, non renal effects (glaucoma); adverse: allergic rxn (sulfa), acidosis, incr ammonia -> hepatic encephalopathy, bone marrow supression (sulfa)

177
Q

glycerin

A

osmotic diuretic; increases volume and concentration of all ions; K wasting; used in acute renal failure, glaucoma; Adverse: pulm edema, hyponatremia, dehydration; not used in anuria, may cause hyprglycemia

178
Q

mannitol

A

osmotic diuretic; same as glycerin; used preop and postop to reduce intracranial swelling; may cause intracranial bleeding

179
Q

bumetanide

A

loop diuretic; 0.8 hr half-life, 62R/38M; high ceiling

180
Q

ethacrynic acid

A

loop diuretic; 1 hr half-life; 67R/33M; ototoxicity

181
Q

furosemide

A

loop diuretic; weak carbonic anhydrase; increases venous capacitance (used in HF, pulm edema); high ceiling diuretic, 1.5 hr half-life, 65R/35M(in kidney); sulfa sensitivity

182
Q

torsemide

A

loop diuretic; 3.5 hr 20R/80M

183
Q

chlorothiazide

A

thiazide diuretic; 1.5 hr half-life; HTN

184
Q

hydrochlorothiazide

A

thiazide diuretic; 2.5 hr half-life; acute diuresis with edema, HTN

185
Q

metolazone

A

thiazide-lide diuretic; 20 hr half-life; HTN

M2 Fall (5 decks)

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