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
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
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
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)
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
6
Q
leucovorin
A
famyl H4-folate; rescue from methotrexate; bypasses DHFR in thymidine synthesis
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)
8
Q
mechanisms of methotrexate resistance
A
amplifaction of DHFR
DHFR gene mutation
decreased drug uptake
increased drug efflux
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
10
Q
5-FU (fluorouracil)
A
pyrimidine antagonist; metabolite inhibits thymidylate synthetase (thymidine synthesis)
fraudulent base incorportaion (S specific)
adverse: severe diarrhea
11
Q
capecitabine
A
oral prodrug of fluorouracil; preferentially activated in tumor tissue;
used in colon cancer and refractory brease cancer
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
13
Q
daunorubcin
A
anti-tumor antibiotic; anthracycline
broad spectrum use; DNA intercalation (mutagenic, carcinogenic)
topoisomerase II inhibitor
irreversible cardiac toxicity at high dose
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
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
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
17
Q
ABVD
A
doxorubicin (adriamycin), bleomycin, vinblastine, dacarbazine
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
19
Q
paclitaxel
A
mtotic spindle poison; plant alkaloid; enhances tubulin polymerization (blocks disassembly)
Used in ovarian and advanced breast cancers
adverse: neuropathy
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
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)
22
Q
etoposide
A
topo II inhibitor; form complex with topo II and DNA, interfere with religation of ds break; DNA strand scission
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)
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
25
raloxifene
SERM; used for estrogen dependant breast cancer; reduced risk of thrombosis and endometrial cancer; prevention of breast cancer in patients with osteoporosis
26
letrozole
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
27
anastrozole
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
28
exemstane
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
29
leuprolide
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
30
flutamide
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
31
prednision
induces apoptosis in leukemia cells; used in multidruf therapies for leukemia, lymphoma, and myeloma;induces remission in childhood leukemias; palliative agent (decrease nausea, inflammation)
32
erlotinib
small molecule EGFR inhibitor; non-small cell lung cancer; head and neck cancers (clinical trials)
33
cetuximab
chimeric ant-EGFR antibody; colon and head and neck cancers
34
EGF-receptor tyrosine kinase
oncogene; overexpressed/mutationally active in l;ung, brain, colon, head and neck cancers
35
lapatinib
small molecule EGFR and HER2 kinase inhibitor in breast cancer (clinical trials)
36
trastuzumab
humanized anti-HER2 antibody for HER2+ breast cancer; refractory metastatic breast cancer
37
imatinib
small molecule bcr/abl tyrosine kinase inhibitor; used for chronic myelogenous leukemia (bcr/abl mutation)
38
brentuximab
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"
39
ifosfamide
bifunctional alkylator
40
chlorambucil
bifunctional alkylator
41
carmustine
alkylator
42
lomustine
alkylator
43
busulfan
alkylator
| adverse: pulmonary fibrosis
44
dacarbazine
alkylator
45
carboplatin
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);
46
hydromorphone
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)
47
hydrocodone
mu opioid analgesic; combined with acetaminophen (vicodin, lortab); metabolized to hydromorphone (CYP2D4); #1 Rx in US today
48
oxycodone
mu opioid analgesic; solo or combined with acetaminophen (percocet); sustained release form. greater bioavailabilty than morphine; metabolized to oxymorphone CYP2D4
49
oxymorphone
mu opioid analgesic; PO; available in extended release; not popular with FDA
50
codeine
weak analgesic; pro-drug converted to morphine (CYP2D4); pharmacogenetic variability clinically significant (inactive prodrug vs active metabolite); anti-tussive effect
51
heroin
mu opioid analgesic; pro-drug converted to manoacetyl morphine; fast onset, lipis soluble, quick access to brain (deactylated); increased euphoria
52
methadone
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
53
meperidine
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
54
fentanyl
mu opioid analgesic; patch for chronic pain, oral (lollipop, sublingual); IV, epidural, intrathecal (subarachnoid); used in anesthetics
55
tramadol
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
56
tapentadol
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
57
pentazocine
kappa agonist/mu partial agonist
58
butorphanol
kappa agonist/mu partial agonist
59
nalbuphine
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
60
buprenorphine
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
61
diphenoxylate
opioid agnoist; oral, poor Gi absoption; antidiarrheal
62
loperamide
opioid agnoist; oral, poor Gi absoption; antidiarrheal
63
naloxone
opioid antagonist; parenteral; prevent/antagonize effects of analgesics
64
naltrexone
opioid antagonist; oral; prevent/antagonize effects of analgesics
65
alvimopan
opioid antagonist; oral, poorly absorbed by GI; prevents opioid Gi effects without effecting analgesia
66
methylnaltrexone
opioid antagonist; quaternary ammonium derivative; IV; peripherally restricted opioid antagonist for constipation
67
morphine-naloxone
abuse resistant opioid; extended release morphine with sequestered naloxone
68
isoflurane
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
69
desflurane
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
70
sevoflurane
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
71
Nitrous Oxide
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
72
dantrolene
treatment for malignant hyperthermia induced by volatile anesthetics; blocks Ca2+ release from sarcolplasmic reticulum in skeletal muscle
73
propofol
anesthetic induction agent; also used for maintainence; cardiovascular and respiratory depression; cannot be antagonized; least "hangover" effect
74
etomidate
IV induction agent; produces respiratory depression; no cardiovascular depression; cannot be antagonized
75
ketamine
phencyclidine derivative; NMDA receptor anatgonist (glutamate); dissociative anesthetic; used for sedation, amnesia, analgesia; no respiratory or cardiovascular depression; cannot be antagonized; emergence delirium
76
methohexital
oxybarbiturate
77
thiopental
thiobarbiturate
78
alfentanil
like fentanyl
79
fentanyl (IV)
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
remifentanil
like fentanyl; metabolized by plasma esterase
81
sufentanil
like fentanyl
82
flumazenil
antagoinst for benzodiazepines
83
midazolam
benzodiazepine; premedication; high lipid soluble; sedation and amnesia; IV benzodiazepine produces respiratory depression; antagonized by flumazenil; other benzodiazepines include diazepam and lorazepam
84
barbiturates (anesthesia)
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
amitriptyline
tricyclic antidepressant
86
nortryptiline
tricyclic antidepressant
87
imipramine
tricyclic antidepressant
88
amoxapine
tricyclic antidepressant
89
tricyclic antidepressants
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
tricyclic antidepressant side effects
antimuscarinic effects; cardiovascular overstimulation, slow AV conductance; ortho hyoptension; sedation; weight gain, sexual dysfunction; seizures; delirium, aggravation or psychosis, mania (bipolar)
91
fluoxetine
SSRI
92
citalopram
SSRI
93
escitalopram
SSRI
94
sertraline
SSRI
95
SSRI
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
SSRI side effects
safer than TCAs: early onset nausea, anxiety, sleep disturbance/insomnia; laste onset: anorexia, sexual dysfunction, mania (bipolar)
97
SSRI drug interactions
Blocks CYPs: TCAs, neuroleptic drugs, antiarrhythmic drugs, some beta-adrenergic antagonists
98
vanlafaxine
SNRI; 27% bound to plasma proteins; metabolized by CEP2D6
99
Duloxetine
SNRI; 97% bound to plasma proteins; metabolized by CYP1A2 and CYP 2D6; hepatotoxic (contraindicated in liver disease)
100
SNRI
serotonin/norepi reuptake inhibitors; unrelated to TCAs; treat patients refractory to SSRIs; oral; half-life (12 hrs)
101
SNRI side effects
less off-target effects than TCAs; nausea, anxiety, sleep disturbance/insomnia; sexual dysfunction; high doses incrase BP and HR
102
Bupropion
atypical antidepressant; inhibits dopamine reuptake; useful in rapid-cycling bipolar disorder
103
nefazodone
atypical antidepressant; inhibits reuptake of serotonin and blocks 5-HT2 receptors
104
mirtazapine
atypical antidepressant; increases NE and serotonin release by blocking alpha-2 receptors
105
attypical antidepressants use and side effects
used in combination with TCAs to lower side effeects; side effects include headache, nausea, tinnitus, insomnia, and nervousness
106
phenelzine
MAO A- & B-type; oral
107
tranylcypromine
MAO A- & B-type; oral
108
selegiline
MAO B-type (MAO A-type at high concentrations); transdermal patch
109
MAOIs
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
MAO-A
deaminates dopamine, Norepi, and 5-HT
111
MAO-B
deaminates dopamine
112
MAO inhibitors side effects
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
Lithium Salts
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
Li Salts pharmacokinetics
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
Li salts side effects
low therpeautic index; substitutes Na+; CV: arrhythmias; CNS: tremor, confusion, convulsions, coma; thyroid: dcrs fxn; renal: poly dipsia, polyuria, diabetes insipidous; teratogenic
116
benzodiazepine
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
flumazenil
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
diazepam
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
chlordiazepam
..
120
alprazolam
benzodiazepine; peak 1-2 hrs; short half-life; insomnia, anxiety; maetabolized -fast> alpha-OH metabolite -fast>inactive
121
oxazepam
..
122
lorazepam
BZ,; peak 1-6 hrs; intermediate half-life; insomnia, anxiety, muscle relaxnt; antiepileptic-emergency status epilepticus, myoclonic, absence; metabolized -inter>inactive
123
midazolam
beznodiazepine; peak .2-1 hr; ultra-short half-life; pre-anestheic medication; metabolized -quick> apla-OH metabolite -fast> inactive
124
benzodiazepine drug interactions
minimal induction of CYPs; severe CNS depression and death with other CNS depressants (EtOH)
125
zolpidem
| Zaleplon
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
Barbiturates
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
phenobarbital
barb; long (oral) onset; long half-life; antianxiety; anticonvulsant for simple partial, recurrent tonic-clonic, and febrile seizure; teratogenic
128
pentobarbital
barb; short (IV) to inter onset; inter half-life; preop sedation
129
amobarbital
barb; ultra-short(IV) onset; short half-life; preop sedation
130
thiopental
barb; ultra-short (IV) onset; ultra-short half-life; anesthetic induction (balanced anesthesia)
131
barbiturate dise effects/drug interactions
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
propranolol
beta-adrenergic blocker, antianxiety; blocks autonomic effects of anxiety (palpitations, sweating, shaking)
133
buspirone
partial agonist for 5-HT1A receptor; metabolized by CYP3A4; aanxiolytic effects wo CNS depression; onset of effect 1-3 wks
134
carbamazepine
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
ethosuxidine
antiepileptic; inhibit Tvoltage-gated Ca channels -> inhibit rhythmic activity; absence seizures
136
gabapentin
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
lamotrigine
antiepileptic; inhibit voltage-gated Na channel reset - prolong refractory period, decrease firing; simple or complex parital, tonic-clonic
138
phenytoin
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
valproic acid
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
pregabalin
antiepileptic; blcoks Ca channels and release of glutamate; simple and complex partial; thrombocytopenia
141
topiramate
antiepileptic; blocks Na channels, increases activity of postsynaptic GABA receptors; simple and partal seizures, tonic-clonis
142
levetiracetam
antiepileptic; modifies glutamate and GABA release; adjuvant treatment for simple and complex parital, tonic clonis
143
clonazepam
BZ; antiepileptic; enhanced GABAergic transmission; myoclonic and absence seizures
144
chlorpromazine
antipsychotic; selective DA receptor antagoinst; low potency; antimuscarinic, antiadrenergic, anithistamine (H1); side efffects: anti-muscarinic, anti-adrenergic, antihistamine
145
fluphenazine
antipsychotic; selective DA receptor antagoinst; high potency; available in slow release (IM)
146
thiothixene
antipsychotic; selective DA receptor antagoinst; medium potency
147
haloperidol
antipsychotic; selective DA receptor antagoinst; high potency; available slow release (IM)
148
aripiprazole
antipsychotic; partial agonist of DA receptor, serotonin receptor antagonist; discontinuation must be done gradually to avoid withdrawal
sideeffects: anticholinergic, antiadrenergic, antihistamine
149
clozapine
antipsychotic; selective DA/serotonin receptor antagonist; sideeffects: all receptors
150
olanzapine
antipsychotic; selective DA/serotonin receptor antagonist; only one to outperform typicals; severe metabolic side effects: all receptors
151
paliperidone
antipsychotic; selective DA/serotonin receptor antagonist; major active metabolite of risperidone; antimuscarinic
152
quetiapine
antipsychotic; selective DA/serotonin receptor antagonist; sideeffects: all receptors
153
risperidone
antipsychotic; selective DA/serotonin receptor antagonist; available slow release (IM); antimuscarinic
154
prochlorperazine
antiemetic; low potency antipsychotic; H1 receptor blocker
155
promethazine
antiemetic; low potency antipsychotic; H1 receptor blocker
156
typical antipsychotics
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
neuroleptic malignant syndrome
antipsychotic side effect; instability and colapse of autonomic regulation; seen also in parkinson patients that stop dopamanergic therapy
158
atypical antipsychotics
symptom relief for 70%; equal efficacy to typical
159
levodopa
enhance DA synthesis; oral ; rapid absorbed from small intestine
160
carbidopa
blocks LDOPA metabolism in periphery. increases LDOPA in brain; used with LDOPA
161
entacapone
COMT inhibitor; decrease LDOPA metabolism in periphery; used with LDOPA+carbidopa
162
selegiline
MAO-B inhibitor used PO; used with LDOPA; increases DA at synapse; decreases H202 production in brain; metabolized to methamphetamine and amphetamine
163
rasagiline
MAO-B inhibitor used PO with LDOPA; like selegiline but not metabolized to amphetamine-like substance
164
bromocriptine
D2 agonist and D1 partial agonist; parkinsons
165
ropinirole
D2 and D3 agonist; parkinsons
166
pramipexole
D2 and D3 agonist; parkinsons
167
apomorphine
DA receptor agonist; used SubQ for "off" period acute treatment;
168
benztropine
muscarinic antagonist for Parkinsons therpay; alleviate tremor and rigidity; not bradykinesia; typical antimuscarinic side effects
169
trihexyphenidyl
muscarinic antagonist for Parkinsons therpay; alleviate tremor and rigidity; not bradykinesia; typical antimuscarinic side effects
170
amantadine
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
Donepezil
AChE for alzheimers therapy; half-life 70 hrs metabolized by CYPs (3A4, 2D6)
172
galantamine
AChE for alzheimers therapy; half-life 7 hrs metabolized by CYPs (3A4, 2D6)
173
rivastigmine
AChE for alzheimers therapy; half-life 1.5 hrs; metabolized by plasma ChE
174
tacrine
AChE for alzheimers therapy; half-life 3 hrs; limited by hepatotoxicity; metabolized by CYPs (3A4, 2D6)
175
memantine
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
acetazolamide
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
glycerin
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
mannitol
osmotic diuretic; same as glycerin; used preop and postop to reduce intracranial swelling; may cause intracranial bleeding
179
bumetanide
loop diuretic; 0.8 hr half-life, 62R/38M; high ceiling
180
ethacrynic acid
loop diuretic; 1 hr half-life; 67R/33M; ototoxicity
181
furosemide
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
torsemide
loop diuretic; 3.5 hr 20R/80M
183
chlorothiazide
thiazide diuretic; 1.5 hr half-life; HTN
184
hydrochlorothiazide
thiazide diuretic; 2.5 hr half-life; acute diuresis with edema, HTN
185
metolazone
thiazide-lide diuretic; 20 hr half-life; HTN
