Med Chem, Mental Illnesses

Front 1

where does the da hypothersis for schizo come from

Back 1

cuz drugs that decrease da neurotransmission

Front 2

neuroleptics suppress behavior and movement by blocking --- type da receptors

Back 2

D2

Front 3

d1 is g---

Back 3

s

Front 4

d2 is g---

Back 4

i

Front 5

which d type increases Ac and camp

Back 5

d1

Front 6

where does the da hypothersis for schizo come from

Back 6

cuz drugs that decrease da neurotransmission

Front 7

neuroleptics suppress behavior and movement by blocking --- type da receptors

Back 7

D2

Front 8

d1 is g---

Back 8

s

Front 9

d2 is g---

Back 9

i

Front 10

which d type increases Ac and camp

Back 10

d1

Front 11

which d type decreases AC and camp

Back 11

D2 type

Front 12

neuroleptics block postsynatptic d2 type da and are ---- --- drugs

Back 12

typical antipsychotics

Front 13

atypical antipsy better at controlling --, but ineffective at controlling very severe --- ----

Back 13

negative symptoms

impulsive behavior

Front 14

which meds will tx positive best

Back 14

neuroleptics

typical tx

Front 15

which meds are less expensive

Back 15

atypical

Front 16

what else will the typicals antagonize

Back 16

ach

histamine

adrenergic

sertonin

Front 17

typical neurolepitics

Back 17

phenothiazines

thioxantheses

haldolperidol

Front 18

why does promethazine bind to d2 receptor

Back 18

cuz side chain all over the place, so doesn't bind well

Front 19

what makes chlropromazine antipsychotic

Back 19

Cl

Front 20

why is promthazine have antinausea effects

Back 20

due to h1 and mucarinic blockade

Front 21

which isomer active at D2 isomer

Back 21

cis

also causes movement se

Front 22

why is fluphenazine given as in depot

Back 22

greasier to prolong diffusion from muscle

given to noncompliance pts

Front 23

d2 side effects

Back 23

acute dystonias

parkinsonian

akathisia

hyperprolactemia

gynecomastia

tardive dyskinesia

Front 24

autonomic se

sedation caused by

Back 24

m1

ach

histamine h1

Front 25

autonomic se

hypotension caused by

Back 25

alpha 1

alpha 2

Front 26

autonomic se

sex dysfunction caused by

Back 26

alpha 1

Front 27

autonomic se

tachycardia

Back 27

ach

m2

Front 28

autonomic se

mydriasis caused by

Back 28

ach

m3

Front 29

autonomic se

constipation caused by

Back 29

ach

m3

Front 30

autonomic se

difficulty urinating caused by

Back 30

ach

m3

Front 31

derm se of typical antipsychotics

Back 31

photosensitivity

urticaria

Front 32

what can cause the weigth gain in typical psychotics

Back 32

weight gain. .. .due h1 or 5ht blockade

(mainly in atypical)

Front 33

how many metabolites for antipsychotics

Back 33

100's

in bl stream for 24 hrs so consider dosing and se

Front 34

what on haldol will help it last longer

Back 34

OR

Front 35

haldol has affinity to

Back 35

D2

5HT

M1-M5

H1

alpha 1

alpha 2

Front 36

drugs made from meperidine to decrease addiction

Back 36

propiophenone

buryrophenone

Front 37

other buryrophenone

Back 37

droperidol

pimozide

Front 38

droperiol is --- acting, sedating

used in ---- for antiemetic effect

adminstered w/ ----

Back 38

short

anesthesia

fentalyl

Front 39

pimozide used for

Back 39

tourette's syndrome

Front 40

haldol is lipo/hydrophilic

Back 40

lipophilic

Front 41

how is haldol excreted

Back 41

it hydrolated (OH added) to make more polar

Front 42

what's the possible cause to tardive dyskinesia

Back 42

n methytransferase . . . put methyl group there

Front 43

metabolic pathways for haldol

Back 43

p450 n-dealkylation

Front 44

haldol neurotoxicity:

--- yields metabolite similar to mptp (hptp)

Back 44

dehydration

Front 45

further metabolism of haldol to mptp by mao leads to

Back 45

mpp+ like compoound . . hpp+

Front 46

t/f

hpp+ causes reversible neuronal damage

Back 46

f

irreversible

Front 47

hpp+ goes into the ------- inhibits respiration and then inhibits ---

Back 47

mitochondria

atp

Front 48

hpp+ goes into the -- neuron and kills

Back 48

Da

toxic

Front 49

benzamide derivative that's still used

Back 49

metoclopramide

Front 50

why isn't metoclopramide used as an antipsychotic

Back 50

hydrophilic. . . doesn't cross the bbb

Front 51

metoclopramide decreases ---- from enteric

Back 51

Ach

decreaes gi motility

increases gastric empyting

Front 52

metoclopromide used to tx

Back 52

gerd

decreases gi motility

increases gastric emptying

Front 53

metoclopramide also has anti ---- acitvity

Back 53

m1-m5

decreased gastric acid

Front 54

atypicals

benzazepines

Back 54

clozapine

olanazapine

quetiapine

loxapine

amoxapine

Front 55

severe se of clozapine

Back 55

1-2% agranulycytosis

Front 56

why's there less eps w/ atypicals

Back 56

D4>>>>D2

increased 5HT

Front 57

amoxapine is an antidepressant that blocks ths uptake of ---

Back 57

NE

Front 58

5HT2 antag in cortex has --- activity

Back 58

antipsychotic

Front 59

nt involved in anxiety

Back 59

5HT

NE

GABA

Front 60

which receptor has the closet link to anxiety

Back 60

GABA

Front 61

ion w/ gaba

Back 61

Cl

Front 62

Cl going thru GABA A receptor ---- the cell which leads to no neuron firing so gaba is inhbitory

Back 62

hyperpolarizes

Front 63

less neruon firing will lead to

Back 63

anxiolytic

sedation

anti-convulsant

Front 64

example of BZR agonsit

Back 64

diazepam

Front 65

this will decrease gaba binding produces action opposite of gaba. . .cl channel stays closed

Back 65

BZR inverse agonist

anxiogenesis

pro-convulsant

not used!

Front 66

bzr antagonist will have no --- activity, but block binding of agonist or ---- ---

Back 66

intrinsic

inverse agonist

Front 67

ex of bzr antagonist

Back 67

flumazenil

Front 68

ex of bzr inverse agonist

Back 68

DMCM

other carbolines endogenous anxiogenic substances

Front 69

gaba has -- polypeptides subunits

Back 69

5

Front 70

the 5 polypeptide subunits are composed of - membrane spanning --- -----

Back 70

4

alpha helices

Front 71

subunits of gaba can be combined in ----proportions, thus, many possible receptor subtypes may exist

Back 71

varied

so also many se

Front 72

adding OH to the 3 position of the bzr will. ..

Back 72

make it more polar and excreted faster

good for insomnia . . . will wake up in AM refreshed and not groggy

Front 73

what position will increase potency

Back 73

1,2

due to electron richness

Front 74

librium has -- metabolites

Back 74

5

so watch out for tx and side effects after several days after d/cing

Front 75

t1/2 of librium

Back 75

48 hrs

Front 76

what metabolites do librium and diazepam share

Back 76

desoxydemoxepam

oxazepam

Front 77

t/f

inactive metabolites of librium can be given as a drug

Back 77

f

only the active metabolites

Front 78

nonbzr's that bind to gaba site

Back 78

imidazopyridines

eszopiclone

pyrazolopyrimidines

Front 79

imidazopyridines have receptors containing --- subunit

Back 79

alpha 1

Front 80

what isomer of eszopiclone is marketed in the us

Back 80

S

Front 81

eszopiclone given for ------

radid/slow onset of action

---duration

Back 81

insomnia

rapid

moderate

Front 82

zalepon is given to tx --- ---

Back 82

sleep latency

Front 83

zalepon doesn't appear to tx --- ---

Back 83

sleep latency

Front 84

zalepon is absorbed ----

reaches peak plasma conc in about -- hr

t1/2 life also of about -- hr

Back 84

rapidly

1

1

Front 85

cyp -- and ---- eszopiclone to metabolites that's primarily excreted via the ---

Back 85

oxidation

demethylation

urine

Front 86

zalepon is oxidized by --- --- and cyp and is eliminated in the urine

Back 86

aldehyde dehydrogenase

Front 87

gaba b has is a ----, it has -- subunits

Back 87

dimer

2

Front 88

t/f

gaba b receptors are w/in the membrane

Back 88

f

outside

Front 89

only drug that's used on gaba b

Back 89

baclofen

Front 90

what's gaba b used for

Back 90

muscle relaxant

analgesic

spinal truama

muscle spasticity

Front 91

t/f

baclofen only works in the periphery

Back 91

f

periphery and cns