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42 Questions for Exam 1 - Medicinal Chemistry and Pharmacology | PHAR 752, Exams of Health sciences

Oregon State University (OSU)Health sciences

Material Type: Exam; Class: PHARMACOLOGY AND MEDICINAL CHEMISTRY I; Subject: Pharmacy; University: Oregon State University; Term: Fall 2005;

Typology: Exams

Pre 2010

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Phar 752 Name (Last, First) ___________________
Exam #1, 13 October 2005 Student ID #___________________
Page 1
This test consists of 45 questions worth a total of 150 points (Questions #1-36 are 3 pts
each; #37-45 are variable). There are a total of 16 pages. Check that your test is complete.
Record your answers for questions #1-36 on a scantron sheet and turn in BOTH the
printed exam and the scantron sheet.
Use the following choices for answering questions 1 through 5. You may use any answer more
than once:
A. M1
B. M2
C. NN
D. NM
E. None of the above
1. ____ Activation of which cholinergic receptor subtype will increase blood pressure in a
whole animal or person? (3 pts)
2. ____ Activation of which cholinergic receptor subtype mediates skeletal muscle
contraction? (3 pts)
3. ____ Activation of which cholinergic subtype mediates smooth muscle contraction? (3
pts)
4. ____ Activation of which cholinergic receptor subtype mediates the cardiac response of
the baroreflex to increased blood pressure? (3 pts)
5. ____ Activation of which cholinergic receptor subtype mediates activation of protein
kinase A (PKA) in smooth muscle? (3 pts)
6. ____ The sympathetic and parasympathetic nervous systems function in an oppositional
manner in all of the following EXCEPT (3 pts)
A. control of heart rate
B. control of bronchiol smooth muscle tone
C. control of vascular smooth muscle tone
D. control of peptic acid secretion
E. control of urinary output
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Download 42 Questions for Exam 1 - Medicinal Chemistry and Pharmacology | PHAR 752 and more Exams Health sciences in PDF only on Docsity!

Exam #1, 13 October 2005 Student ID #___________________ Page 1 This test consists of 45 questions worth a total of 150 points (Questions #1-36 are 3 pts each; #37-45 are variable). There are a total of 16 pages. Check that your test is complete. Record your answers for questions #1-36 on a scantron sheet and turn in BOTH the printed exam and the scantron sheet. Use the following choices for answering questions 1 through 5. You may use any answer more than once: A. M 1 B. M 2 C. NN D. NM E. None of the above

  1. ____ Activation of which cholinergic receptor subtype will increase blood pressure in a whole animal or person? (3 pts)
  2. ____ Activation of which cholinergic receptor subtype mediates skeletal muscle contraction? (3 pts)
  3. ____ Activation of which cholinergic subtype mediates smooth muscle contraction? ( pts)
  4. ____ Activation of which cholinergic receptor subtype mediates the cardiac response of the baroreflex to increased blood pressure? (3 pts)
  5. ____ Activation of which cholinergic receptor subtype mediates activation of protein kinase A (PKA) in smooth muscle? (3 pts)
  6. ____ The sympathetic and parasympathetic nervous systems function in an oppositional manner in all of the following EXCEPT (3 pts) A. control of heart rate B. control of bronchiol smooth muscle tone C. control of vascular smooth muscle tone D. control of peptic acid secretion E. control of urinary output

Exam #1, 13 October 2005 Student ID #___________________ Page 2

  1. ____ One problematic side effect of trospium can be (3 pts) A. dizziness and motion sickness B. hallucinations C. postural hypotension D. incontinence E. dry mouth
  2. ____ The primary benefit of the use of echothiophate or isofluorophate compared to other therapeutic agents in its drug class is (3 pts) A. duration of action B. absorption from the GI C. decreased nicotinic effects D. decreased effects on secretions E. efficacy to induce mydriasis
  3. ____ Activation of acetylcholine-gated ion channels on post-ganglionic neurons will cause (3 pts) A. depolarization B. hyperpolarization C. an action potential D. special summation E. inhibition of neurotransmitter release
  4. ____ The safest drug for patients with insufficient cardiac reserve would most likely be (3 pts) A. muscarine B. pilocarpine C. nicotine D. bethanechol E. civemiline

Exam #1, 13 October 2005 Student ID #___________________ Page 4

  1. ____ Botulin toxin is used to treat hyperhydrosis by (3 pts) A. poisoning and shrinking sweat glands B. blocking nicotinic receptors C. permanently activating Gi subunits coupled to muscarinic receptors D. blocking neuronal conductance E. blocking acetylcholine release
  2. ____ Dantrolene is used to treat (3 pts) A. Malathion poisoning B. Myasthenia gravis C. Mushroom poisoning D. Malignant hyperthermia E. Muscarinic amnesia
  3. ____ Parasympathetic relaxation of the bladder sphincter occurs through (3 pts) A. activation of M2 receptors on bladder sphincter smooth muscle B. activation of M2 receptors on sympathetic presynaptic neurons C. inhibition of M1 receptor on bladder sphincter smooth muscle D. inhibition of M2 receptors on bladder sphincter smooth muscle E. inhibition of M1 receptors on sympathetic presynaptic neurons
  4. ____ Once an action potential is initiated, neuronal conductance can be blocked by (3 pts) A. toxics that block Ca++^ channels B. toxins that block vesicle fusion with plasma membrane C. toxins that block acetylcholinesterase D. toxins that inhibit Na+^ channels E. all of the above
  5. ____ The GTPase activity of a heterotrimeric Gsubunit is required for (3 pts) A. Initial activation B. Effector stimulation C. Association with G protein coupled receptors D. Reassociation with G subunits E. Receptor desensitization

Exam #1, 13 October 2005 Student ID #___________________ Page 5

  1. ____ Tubocurare causes paralysis by (3 pts) A. blocking the acetylcholine binding site B. phase I blockade C. phase II blockade D. phase I followed by phase II blockade E. spinal blockade
  2. ____ The most dangerous complication with succinylcholine use is (3 pts) A. abnormally extended duration of action in renal insufficiency B. abnormally extended duration of action in liver dysfunction C. chelation of calcium in muscle tissue D. excessive release of calcium in muscle tissue E. toxic combinations with antibiotics
  3. ____ Paradoxially, nausea is listed as a side effect of scopolamine because A. it activates the chemoreceptor trigger zone B. it delays stomach emptying C. it increases peptic acid secretion D. it relaxes the pyloric sphincter at the top of the stomach E. nausea is a side effect for everything
  4. ____ Bethanechol should be used post-surgery if a patient (3 pts) A. Does not show evidence of dementia B. Is not on antibiotics C. Did not receive inhalational anesthetics D. Was not intubated E. Has no evidence of bowel obstruction

Exam #1, 13 October 2005 Student ID #___________________ Page 7

  1. ____ Which of the following is not consistent with the SAR for muscarinic antagonists? (3 pts) R 2 R 1 R 3 X-(CH 2 )n-N A. The R3 substituent in more potent antimuscarinics is a hydroxyl or a hydroxymethyl group. B. The N group is a tertiary amine or quaternary ammonium salt, with the alkyl substituents usually methyl, ethyl, or isopropyl. C. The distance between the X group and the amine nitrogen can vary from 2 to 4 carbons. D. The X substituent in the most potent anticholinergics is an ester. E. The size of the R1 and R2 groups should be no larger than a methyl group.
  2. ____ What is the approximate half-life (t1/2) for hydrolysis of the modified serine intermediate of acetylcholinesterase shown below? (3 pts) A. 200 sec (microseconds) B. 15-30 sec C. 45 min D. 8 hours E. 24 hours
  3. ____ Muscarine and pilocarpine are natural products that have similar pharmacological actions, but only one is useful as a drug to treat glaucoma. What key structural difference supports the use of pilocarpine rather than muscarine? (3 pts) A. Muscarine lacks the ester group that is crucial for optimal activity. B. Pilocarpine is a tertiary amine that is readily absorbed in the eye, while muscarine is a quaternary ammonium compound with poor absorption. C. Pilocarpine has several chiral centers that lead to greater selectivity to receptors in the eye. D. Muscarine is much more highly lipophilic than pilocarpine, which results in broad systemic distribution of the compound, leading to undesired side effects. E. The lactone ring system in pilocarpine is resistant to hydrolysis, resulting in much longer duration of action than would be seen with muscarine. N H O O Ser-AChE

Exam #1, 13 October 2005 Student ID #___________________ Page 8

  1. ____ Some antipsychotic drugs are known to have peripheral anticholinergic effects. Based on structural features, which of the following antipsychotics would be most likely to display these antimuscarinic side effects? (3 pts)

A B

D E

C

N S Cl N CH 3 CH 3 Cl N N N (^) S H N O O N N H H^ O 3 CH 2 C H 3 C O N OH Cl F O N N Cl Cl H O N

  1. ____ Which non-depolarizing neuromuscular blocking agent is efficiently inactivated by plasma cholinesterase (pseudocholinesterase) cleavage? (3 pts) A. Pipecuronium B. Tubocurarine C. Mivacurium D. Rocuronium E. Succinylcholine
  2. ____ Ketoconazole, a Cyp3A4 inhibitor, would be expected to increase the half-life of drugs metabolized by Cyp3A4, potentially requiring a reduction in dose to reduce unwanted effects. Which muscarinic receptor antagonist used to treat overactive bladder would be least likely to have a drug interaction if co-administered with ketoconazole? (3 pts) A. Tolterodine B. Oxybutynin C. Trospium D. Solifenacin E. None of the above

Exam #1, 13 October 2005 Student ID #___________________ Page 10

  1. ____ All of the following muscarinic antagonists except one have been used to treat extrapyramidal symptoms associated with Parkinson’s disease. Which structure represents an antagonist that would NOT be effective? (3 pts) N+ O H H 3 C N OH CH 3 N OH

A^ B

C

D

E

N HO (^) O N H 3 C H 3 C

  1. ____ Which of the following structures represents an acetylcholinesterase inhibitor that acts by covalently modifying the AChE? (3 pts) N H 3 CO H 3 CO O H O N H CH 3 H 3 CO H^ OH NH H 3 C H 2 N (^) O CH 3 N+ O O (H 3 C) 2 N CH 3 N+ H 3 C CH 3 CH 3 OH A B C D^ E

Exam #1, 13 October 2005 Student ID #___________________ Page 11

  1. ____ Which of the following muscarinic agonists does not undergo hydrolysis and would be expected to have the longest elimination half-life? (3 pts) H 3 C O N+ CH 3 O CH 3 CH 3 CH 3 H 2 N O N+ CH 3 O CH 3 CH 3 O N+ CH 3 CH 3 CH 3 H 2 N O CH 3 N O CH 3 S

A

B

C

D E

O N N O H 3 CH 2 C CH 3 H

Exam #1, 13 October 2005 Student ID #___________________ Page 13

  1. (3 pts) Draw the structure of the plant natural product that selectively acts at nicotinic cholinergic receptors (correct stereochemistry, if present, is required).
  2. (4 pts) On the structure of acetylcholine below, add two different structural changes, one that will: A) Increase selectivity for muscarinic over nicotinic receptors. And a second that will: B) Significantly increase the duration of action of acetylcholine. (Clearly indicate which change correlates to part A and which correlates to part B.)

CH 3

N+

H 3 C O

O

CH 3

CH 3

Exam #1, 13 October 2005 Student ID #___________________ Page 14

  1. (4 pts) The following structure represents a drug that is currently in Phase III clinical trials. This molecule is a prodrug, which is modified in the body to produce the active agent. Draw the structure of the active species and indicate what type of pharmacological action the active species will have (agonist/antagonist; include specific receptor/enzyme selectivity). N O HO O
  2. (2 pts) Explain why ipratropium is a better choice than atropine as an inhaled muscarinic antagonist to treat chronic obstructive pulmonary disorder (COPD). Base your answer on structural difference(s) between the two drugs.

Exam #1, 13 October 2005 Student ID #___________________ Page 16

  1. (4 pts) The structure of an acetylcholinesterase reactivator is shown below. Circle the portion of the molecule that acts as a strong nucleophile to regenerate the active AChE. Draw the structure of the modified reactivator that would result from regeneration of AChE from the phosphorylated enzyme depicted below. N+ N OH CH 3 H O O P O CH 3 Ser AChE
  2. (2 pts) Although ambenonium is a non-covalent modifier (non-covalent inhibitor) of AChE, it still has a very long duration of action. Explain this phenomenon based on the structure of ambenonium?