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Midterm Exam Solution - Pharmacology and Medicinal Chemistry I | PHAR 752, Exams of Health sciences

Material Type: Exam; Class: PHARMACOLOGY AND MEDICINAL CHEMISTRY I; Subject: Pharmacy; University: Oregon State University; Term: Unknown 2004;

Typology: Exams

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Autonomic Nervous System Nam (Lt, First)
Social Seurty #
Th tet consists of 43 questions wort 8 tota of 100 points (Quesons #1-36 ar 2 pts each; #37-
43 ar vaable). There ar a tota of 11 pages. Check that your te is complete Record your
for questions #1-36 on a sctron sheet and tum in H ths printed exa and the
b\J 4-' D
1. jl Which strctu modfication to the n neprin lea . agonist selectivity?
A. Addtion of an cr-methyl grup
B. Addition of an N-isopropyl grup
C. A meta argement of hydrxyls on the armatic ring
Replacement of the catehol with a
!-!
S' dimethoxy substituted armatic ring.
E. Removal of the jJhydrxyl grup
2. B- -Phenoxybenzamne has a long durtion of action beaus:
j: ("
lv (:1" .' J"
A. It is only slowly metabolized by Cyp 3A4.
($
It is activate to form an aZridini ion which irrversibly alatthe repto taet.
C. It has a long arl alkyl chain that provides for gratr affinity at the taet
D. The high lipophilcity of the drg results in better tissue absorption and then slow
relea frm the site of action.
E. It is formulate in an extende relea formulation.
3. .
& -
Which of e following dtgs is prg!
A. -Methyldopa--1
B. . Bitolterol - +-
C. Midodne+
D. Latanoprost
- ..
Ritodne
4. The adjacent strctu reprnts a prog that has a longer durtion of action than the
parnt compound How would the active drg be classified for its action at adrnergic
reptors?
GI Adrnergic agonist with activity at both a- and p-reeptors
B. Genera p-agonist
C. Genera a-agonist - H
D. li-selective adrnergic antagonist
E. P2-selective adrnergic agonist
. -
CHs
Ae\Jt.:: D \
0 .
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Autonomic Nervous System

Nam (Lt, First)

Social Seurty #

Th tet consists of 43 questions^ wort 8 tota^ of^100 points^ (Quesons #1-^36 ar^2 pts each; #37-

(^43) ar vaable). There ar a tota of 11 pages. Check that your te is complete^ Record your

for questions #1-36 on a sctron sheet and tum in H ths printed exa and the

b\J 4-' D

  1. (^) jl Which^ strctu^ modfication to the n^ neprin^ lea^. agonist selectivity?

A. Addtion of an cr-methyl grup

B. Addition of an N-isopropyl (^) grup

C. A meta^ argement of^ hydrxyls^ on^ the armatic ring

Replacement of the catehol with a^ S'^ dimethoxy substituted^ armatic ring.

E. Removal of the (^) jJhydrxyl grup

  1. B- -Phenoxybenzamne has a long durtion of^ action^ beaus:^

lv (:1"^

.' J"

A. It is only slowly metabolized by Cyp 3A4.

It is activate to form an aZridini ion which irrversibly^ alat the^ repto taet.

C. It has a long^ arl alkyl chain that provides for^ gratr affinity at the^ taet

D. The high lipophilcity of the drg results in better tissue absorption and then slow

relea frm the site of action.

E. It is formulate in an extende relea^ formulation.

3.. Which of e following dtgs is (^) prg!

A. -Methyldopa--

B.. Bitolterol - +-

C. Midodne+

D. Latanoprost

Ritodne

  1. The adjacent strctu reprnts a prog that has a longer durtion^ of action^ than^ the

parnt compound How would the active drg be classified for its action at adrnergic

reptors?

GI

Adrnergic agonist with activity at both a- and p-reeptors

B. Genera p-agonist

C. Genera a-agonist

  • H

D. (^) li-selective adrnergic antagonist

E. P2-selective adrnergic agonist

CHs

Ae\Jt.::

D \

:Plar"152,'EXam 112Wo

Autonomic Nervous System

Name (Lt, First)

Socal Securty #

Which of the following statements about ephedrine is

A. It has goo ora (^) activity because it cannot be metablized by COMT and MAO

w.

B. Ephedne is a preur for the ilicit synthesis of methamphetane

(S

Ephedrne and epinephrne have similar centrl actions due to similar

NHC

abilty to crss the BBB.

D. The IS,2R enantiomer has mainly indit activity-l '

E. The IR,2S enantiome has diret activity at both and preptors.+- lR

The adjacent strcture repreents a drg that is used asa raemic mixtur. What would

the expeted action of the drg on the adrenergic syste

A. Exclusively (^) agonist action

B. Exclusively (^) fJ agonist action

ODiret agonist action in addition to^

indiret action

D. Diret (^) fJ agonist action in addtion to indiret action

:E. Genera and (^) fJ agonist action as well as indiret action

Tolcapone is a COMT tor us^ in the^ trtment of Parkinson s diseas.

would be expete to inc th hal life for which of the following drgS?

c.vJl"' -e. Q. \

. A. Terutaine-tVo

B. Tizaidine-t.o

Isoroterenol-

D. Phenylephrine..O

E. Dorzolamde-

  1. Which statement^ regarng^ dobutane is false?^ f\P^

()f V+

A. The apparnt PI-selectivity of dobutane arse frm a "canceling" of a^ agonist,

antagonist, and (^) fJ agC?njst effects.

B. The enantio IS an a, agonist.

C. The enantiomer is an (X) antagonist.

D. Both enantiomers have genera Ii agonist action.

The dobutaine isomers have different^ metalic^ fates - the S enantiomer is^1

metalize by COMT,^ while the^ enantiomer is^ metalize^ by^ MAO.

1Q; ,

C,..

' f#

g:tY'

. t'

r; :

..'

Autonomic Nervous System

Nam (^) (Lt, First)

Social Securty #

.. -

Which of the following is not an essential strctur featur for cysteinylleukotre

(CysLT.) antagonists?:

A. A centr lipophilc and flat unt, which is believed to mimic the trene system of the

natu agonist L1D

B. One or two acidic^ grups, as potential mimics ofthe peptide unit and/or the Cl-

caxylic acid ofL1D

Spaers to connect and prerganze the other strctur elements.

lE A

positively charged

amonium grup which acts in adtion to the negatively charged

acidic (^) grup to localize action of the drg to the lungs.

f. A lipophilc anchor

which fits into the lipophilc poket of the

CysLT, reptor.

13. J2 -Bas on the acompanying strctu. doxazin is

A. Genera (^) fJ antagonist

B. General (^) fJ antagonist with a antagonist action.

C. Genera antaonist

Selective a antagonist

E. Genera and (^) fJ antagonist.

:'lOSir\ an:)""i

14. -6 -Which statement regarng aprlonidine is false?

A. Apraclonidine has a higher (^) pI( than cIonidine, which leads to a (^) grter proporton

ionize moleules at physiologic pH. reucing systemic effects when^ adnistere in

the eye.

B. Oxidaon of apralonidine prouces an intermate that can alkylate^ prteins in the

eye..

C. Apralonidine differ strctuly^ frm^ c10nidine^ by^ having^ a^ pa amino^ grup. t-

D. Apralonidine is a selective agonist t-

/E Apralonidine has a long duron of^ action in the eye^ beaus it is^ activate^ to an

intermedate aziridinium ion which can alkylate the^ reptor.

'!'1 h:*'-.'"

  • Phaf752. ifl/n

Autonomic Nervous System

, Nam (^) (Lt, First)

Social Security #

  1. Which of the following has strctu featus consistent with a general^ agnist (actions at

both a and reptors)?

H -

H COH ' I - H

CD

Nt) , l. HO

iJ

1J(

HO W

  1. Impulse regulation of tyrosine hydrxylas^ depends^ upon activaton of which kinas?

A. (^) Ii-adrnergic reptor kinas

B. protein^ kinas A

C. (^) prtein kinas C

D. ' protein kinas G

Ca++/Calmodulin-dependent protein kinas

  1. -.Conversion of dopamine to norepinephrine involves

c.o-

p-ot+

A. the addition of a methyl group to the amine

B. the conversion of the catehol ring 3-hydrxy to a^ 3-methoxy

the addtion of a hy.drxyl grup to the fl canr

D. the oxidation of the amine to a carxyl grup

E. the removal of the^ carxyl grup^ convertng the amno acid to an^ amine

  • A. tachycardia

B. bradycara

hyptension

D. anidrsis

E. bronchoconstrction

The most n.rominent e of reserpine in a normal resting patient wil be

tocS VlSi c.^

\lr

,ra

(\B- -

'r+ 'V\

rt.

e -

Phar'752 1"' ;t. if-

Autonomic Nerous System

Name (Lt, First)

Social Securty #

' - q jC7,

  1. Rapid IV infusion of Dopamine (InotrpineO) wil mos^ diretly stimulate th^ hea^ by

A. activating D 1 dopamine reeptors to^ decas bloo^ prssure and stimulate a

compensatory bareflex

B. acvating a2 adrnergic repto to decree blood (^) prssur and stimulate a

compensatory barreflex.

/C activating f:H adergc repto to incre hea rate

activating D 1 dopamne reptors to incre hear

E. incrasing NE synthesis in sympatetic nerve tennnals

    • Caffeine. through its effects on cyclic AM levels. could possibly mediate all of the

followingactions

1"

A. incred hea rate t-

B. increasd prouction of aqueous humor+^ IL (-ltt o.cf (C

C. bronchodlation

vasoconstrction of th major ares -r

l' C It r-

E. myometal relaxation\

26. - The possible side effects associate with albuterol therapy^ includ

A. excess histaine relea (^) NO '

,.a

'S-r

! .. t

. A

P
B. utene hypctivity AI

J,.

.)W,--

C. setion NU l' f \t"

dereas (^) periphera reistace

E. hypglycemia

27. -iL - Tachy ara could be^ revers^ with all of the following agents^ EXCE

A. esmolol

+-4 et-K

(i

albuterol \ c;^

-CWsntY l' t^

(

Q,\7'

C. mitodne-d -f.^

  • J

D. clonidine- (^) '1-o.

E. propraolol +-

    • One condition where^ trtment with^ propraolol has NO^ thrapeutic indication

A. famlial palsy-

B. carac disease-t

C. migrne+

D. hypyridism

benign protatic hyprplasia

Name (Lt, First)

Social Securty #

-_..

29.. The best agent to us in^ the tratment of^ anaphylactic shock is

A. norepinephrine

($

epinephrine

C. isoproterenol

D. dopaine

E. albuterol

br-

p-bl ker ar contrndicated with all of the following condition EXCE

A. diabetes

B. history of depression

C. asthm.a

glaucoma

E. (^) potasium-sparng diurtics - CLj

The difference between meterol and Pin^ 1 is that" o^ of them

A. is a paral f3reptoragonist N-t

P'( ". 4\

;5+

B. is a paal f3reeptor antaonist h'fJ

C. has sOme effcacy to lower periphera^ reistace

is somewhat 132 reptor^ selective

E. has some effcacy to caus bronchodlation

Matchig: Use the following choices to match activation^ of^ the^ corrct^ reeptor^ subtype^ with^ the

actions liste in questions #32-^36

A. aI-adrnergc

B. a2-adrnergic

C. 13 i-adrnergic

D. 2.-adrnergc

E. none of the above

inhibition of the bareflex (^) d-,-

constrction of bladdr sphi cter

stimulation of epinephrine seretion

incras renin seretion

inhibition of mast cell degranulation

.:fi am (^) *grll/21/

Autonomic erous System

Nam (L Fint)

Socal Securty #

38. (6 pts)

A)Name a non-selective a-antagonist

hJ\O

. P

B)Di ss in detaH the arac effects of an non-selective a-antaonist. Mae sur^ to list the

actiVIty of the agent at all of th repto^ subtys^ involved, thir locations,^ and the effect(s)

that thy meat.

-\o.fN tL+"^ t\

, ft.

R,-;)(CI,;-e- 4W^

tIo.)rr (^) 1c ,1.11I't

pt("'

('tSl -kCt

J. d\o.

b\IWJ

!.S"'rv H-^ 0/:; nUf^

J 1+ ""ell

?'aCt. \.i+;^ (t-ltQ.SR

(WJ,

lV\ \ , 1 t1 +k^ bU^ R.f^. "1e.^ loa4..k

:kf

i' '1 (^) tft d. ' bt c Ck^

+ka- '

0( (^) tYJ.

Q.-/

" tf (^) St

V\ (^) BP o.+

wHt

\o'fOfttkx -H(). rt^

btpr

bloe

  1. Esmolol and unoprostone isopropyl shar a^ common mechanism of initial^ metalism.^ Explain

hoWdD.

:;t:(

Si

\JV\

'o(

\c: Q\k.

:k 4k

tD(Y\

lUcl ('!-kc^

C;i

Qt., J ).\

-h

to'

AJ. f;SWtc l.

\1.t'\ .. h.

J~(Ol

"'I (^) i+

Autonomic Nervous System Socal Securty #

  • ,
  1. (4 pts)

A) Name one of the thre inhaled cortcosteroids that is used in the trtmnt of asthma.

Dif(OP;Ot

B) Explain why the systemic side effects for the swallowed (^) porton of the drg named^ in^ pa A

ar gratly reduced compard to an orly administe steid (include speific informaton

about th chosn drg in the answer).

1thlY\ d.Uj i^

i+

\\X(

.L Ii- Vt'd.t-'(?\ -ky-

n'\ t)b^ c.n 21 fJopiOV

4 f(a:cl ,s. i;

,c.

C(. bJ4,^ 4(''' i..

  1. Labetalol acts at both and (^) fJ adnergc reeptors.-Sxpain labetaol'^ s actions based on the -l (^) "&

contrbutions of isomer. (4 pts)

,liJQ.J.

o.f-TaQ 'l

oovi

;1 o.cfvi:,

,o t4. c:d

,c. lh ft^ l.

\I; (wJ ('

U- 4.cI ckto.

  • 6(lS-\

c.

., hl

cmis

  1. Salmeterol is used in the tratment^ of^ asthma.^ Explain^ why salmeterol has high affnity for its

reptor taget and a long duration of action. (3 pts)

\h ")^ r^

r'J.'

-\

!i",o

ch1t"

So.\ V'+ao^

-. I--h Iay

JvfQ. tn

o.Ct.

cl\I

-#tL

\J-l(

CP:

(lV\d.

V\ 0U-^

-k

\V\

ra

\ ,- , '" ', '( -- -. "

yY

+-

l \J

c: \ )\1\

LCU

f

Pa

11 of 11

-wO)

bi eleJ(t-c\ %um