Sunday 18 December 2011

PHARMACOLOGY OBJECTIVES FROM YAKUBU H.YAKUBU

  1. Mechanism(s) of drug permeation:
    1.   lipid diffusion
    2.   aqueous diffusion
    3.   use of carrier molecules
    4.   endocytosis and exocytosis
    5.   all of the above
  2. Bond type that is seen in some drug-receptor interactions and tends to very strong, often nearly irreversible:
    1.   hydrophobic
    2.   electrostatic
    3.   covalent
    4.   A & C
    5.   B & C
  3. Drug delivery method LEAST suitable for long term (days to weeks) slow release.
    1.   pellet implant under the skin (subcutaneous)
    2.   time release capsule
    3.   i.m. injection of a drug-oil suspension
    4.   transdermal patch
    5.   none of the above
  4. Most drug have molecular weights between:
    1.   10 - 100
    2.   100 and 1000
    3.   7 - about 60000
    4.   above 60000
    5.   none of the above
  5. Most important factor influencing drug absorption rate following intramuscular injection:
    1.   needle diameter
    2.   rate of administration
    3.   injection site blood flow
    4.   injection volume
  6. Most common mechanism of drug permeation:
    1.   endocytosis
    2.   carrier-mediated transport
    3.   active-transport
    4.   passive diffusion
    5.   none of the above
  7. Weak organic acid, pKa 6.5. Percent ionization at pH 7.5
    1.   1%
    2.   10%
    3.   50%
    4.   90%
    5.   99%
  8. General term having to do with actions of the body on the drug:
    1.   pharmacodynamics
    2.   pharmacogenetics
    3.   pharmacokinetics
    4.   absorption
    5.   none of the above
  9. Drug-transport system described as "energy requiring":
    1.   glomerular filtration
    2.   facilitated diffusion
    3.   active transport
    4.   B & C
    5.   A, B & C
  10. Drug with this ionization property most likely to diffuse from intestine (pH 8.4) to blood (pH 7.4)
    1.   weak acid (pKa 7.4)
    2.   weak base (pKa 8.4)
    3.   weak acid (pKa 8.4)
    4.   weak base (pKa 6.4)
    5.   weak acid (pKa 6.4)
  11. Term having to do with drug actions on the body:
    1.   pharmacokinetics
    2.   pharmacodynamics
    3.   pharmacogenetics
    4.   placebo
    5.   all of the above
  12. Dramatic decrease in systemic availability of a drug following oral administration is most likely due to:
    1.   extreme drug instability at stomach pH
    2.   hepatic "first-pass" effect
    3.   drug metabolized by gut flora
    4.   tablet does not dissolve
    5.   patient non-complance
  13. Pharmacological antagonists:
    1.   cause receptor down regulation
    2.   prevent binding of other molecules to the receptor by their binding to the receptor
    3.   atropine (blocks ACh action on the heart
    4.   A & B
    5.   B & C
  14. Increasing ionization at pH ABOVE pKa:
    1.   weak acid
    2.   weak base
  15. Example(s) of covalent drug-receptor interactions:
    1.   activated phenoxybenzamine-receptor
    2.   anti-cancer DNA alkylating drugs, like cyclophosphamide (Cytoxan)
    3.   norepinephrine
    4.   A & B
    5.   A, B & C
  16. Faster drug absorption:
    1.   lung
    2.   stomach

    1. Stereoselectivity and metabolism:
      1.   enzymes typically exhibit stereoselectivity -- a preference for one or the other enantiomeric form
      2.   duration of action of one enantiomer may be different from the other
      3.   both
      4.   neither
    2. Percentage of all drugs that exist as enantiomeric pairs:
      1.   less than 1%
      2.   5%-15%
      3.   30%
      4.   > 50%
      5.   > 90%
    3. The binding of the activated form of phenoxybenzamine (alpha-receptor antagonist) with the alpha receptor is an example of this type of chemical force/bond:
      1.   electrostatic
      2.   covalent
      3.   hydrophobic interactions
    4. Characteristic(s) of enantiomers:
      1.   chemically identical
      2.   mirror images of each other
      3.   both
      4.   neither
    5. Saturable transport system(s):
      1.   facilitated diffusion
      2.   passive diffusion
      3.   active transport
      4.   A & B
      5.   A & C
    6. Characteristics those aqueous diffusion:
      1.   occurs within large intracellular and extracellular components
      2.   occurs across epithelial membrane tight junctions
      3.   occurs across endothelial blood vessel lining -- often through pores
      4.   A & C
      5.   A, B & C
    7. Examples of enantiomeric differences important in anesthesia:
      1.   cardiotoxicity is probably associated with both enantiomers of bupivacaine
      2.   Ropivacaine is less cardiotoxic compared to bupivacaine because it is metabolized faster
      3.   cisatracurium is an atracurium isomer that doesn't cause histamine release
      4.   both l- and d- morphine occur in nature
    8. Factors that influence the rate of passive movement to molecules down the concentration gradient (Fick's Law)
      1.   concentration difference across the barrier
      2.   area across which diffusion occurs
      3.   drug mobility in the diffusion panel
      4.   thickness -- length of the diffusion pass
      5.   all the above
    9. Description of enantiomers:
      1.   may be readily superimposed
      2.   enantiomers, when presence in equal proportions, are referred to as racemates
      3.   may be characterized by absolute configuration or by direction in which enantiomers rotate polarized light
      4.   A & C
      5.   B & C
    10. Major types of chemical forces/bonds:
      1.   hydrophobic interactions
      2.   electrostatic
      3.   covalent
      4.   A & C
      5.   A,B, & C

      1. Sympathetic nervous system anatomy and properties:
        1.   gangionic neurotransmitter: acetylcholine
        2.   generalized response upond sympathetic stimulation
        3.   thoraco-lumbar origin for preganglionic cell bodies
        4.   all of the above
      2. Comparing autonomic and somatic nerves:
        1.   somatic nerves, like autonomic nerves contain ganglia.
        2.   Most of the fibers in the vagus nerve ar sensory
        3.   denervated smooth muscle show spontaneous activity
        4.   motor nerves are typically unmyelinated.
      3. Major anatomical site for integration of autonomic information:
        1.   cerebellum
        2.   sensory cortex
        3.   hypothalamus
        4.   spinal cord--dorsal horn
      4. Division of the autonomic nervous system associated with diffuse autonomic responses.
        1.   sympathetic
        2.   parasympathetic
        3.   both
        4.   neither
      5. Activation of the sympathetic nervous system will caus which change in the skeletal muscle versus cutaneous vascular beds.
        1.   vasoconstriction, vasoconstriction
        2.   vasodilatation, vasodilatation
        3.   vasodilatation, vasoconstriction
        4.   vasoconstriction, vasodilation
      6. Adrenergic receptor type(s) mediating pupillary dilation
        1.   beta-2
        2.   alpha-1
        3.   muscarinic
        4.   serotonergic
      7. Cholinergic receptor type that mediates vasodilation following low-dose i.v. acetylcholine administration:
        1.   nicotinic
        2.   muscarinic
        3.   nitric oxide receptor
        4.   substance P receptor
      8. "True" acetylcholinesterase is found in:
        1.   glia
        2.   liver
        3.   erythrocytes
        4.   plasma
      9. Catalyzes rate-limiting step in catecholamine biosynthesis:
        1.   DOPA decarboxylase
        2.   phenylethanolamine N-methyl transferase
        3.   tyrosine hydroxylase
        4.   dopamine-beta-hydroxylase
      10. Inhibited by drugs such as phenelzine or tranylcypromine;
        1.   COMT (catechol-O-methyl transferase)
        2.   MAO (monoamine oxidase)
        3.   choline acetyltransferase
        4.   reuptake-I inhibitor
      11. Concentation increased by epinephrine:
        1.   blood free fatty acids
        2.   blood glucose
        3.   skeletal muscle glycogen
        4.   A & B
      12. Due to receptor specificity, catecholamine LEAST likely to produce bronchiolar smooth muscle relaxation:
        1.   epinephrine
        2.   terbutaline (Brethine)
        3.   phenylephrine
        4.   phentolamine (Regitine)
      13. Alpha adrenergic receptor blocker
        1.   phentolamine (Regitine)
        2.   phenoxybenzamine (Dibenzyline)
        3.   terbutaline (Brethine)
        4.   A & B
      14. Covalent inhibitor of acetylcholinesterse:
        1.   edrophonium (Tensilon)
        2.   diisopropylphosphate (DFP)
        3.   atropine
        4.   muscarine
      15. Alpha-adenergic receptor agonist:
        1.   terbutaline (Brethine)
        2.   atropine
        3.   methoxamine (Vasoxyl)
        4.   isoproterenol (Isuprel)
      16. Parasympathetic direct cardiac effects:
        1.   decrease heart rate; increase contractility
        2.   increase heart rate; decrease contractility
        3.   decrease heart rate; decrease contractility
        4.   increase AV nodal conduction velocity
      17. Choline ester substrate for acetylcholinesterase:
        1.   carbachol
        2.   methacholine (Provocholine)
        3.   both
        4.   neither
      18. Alkaloid agonist acting at muscarinic, cholinergic receptors:
        1.   DFP
        2.   pilocarpine (Pilocar)
        3.   physostigmine (Antilirium)
        4.   ipratropium (Atrovent)
      19. Effective in treating both organophosphate and muscarine intoxication:
        1.   nicotine
        2.   echothiophate (Phospholine)
        3.   atropine
        4.   pilocarpine (Pilocar)
      20. Cholinergic activity on stomach acid secretion
        1.   increased
        2.   decreased
        3.   no changed
        4.   one of the others is right

        1. Most likely to reduce blood pressure by directly decreasing heart rate:
          1.   phentolamine (Regitine)
          2.   propranolol (Inderal)
          3.   nitroprusside sodium (Nipride)
          4.   phenylephrine (Neo-Synephrine)
        2. From the point of view of Starling's law which antihypertensive would be most likely to reduce contractility.
          1.   methoxamine (Vasoxyl)
          2.   nitroprusside sodium (Nipride)
          3.   propranolol (Inderal)
          4.   metoprolol (Lopressor)
        3. Negative inotropism
          1.   isoproterenol (Isuprel)
          2.   epinephrine
          3.   diltiazem (Cardiazem)
          4.   norepinephrine
        4. Increases pulmonary congestion in congestive heart failure (CHF)
          1.   dopamine (Intropin)
          2.   metoprolol (Lopressor)
          3.   nitroprusside sodium (Nipride)
          4.   digoxin (Lanoxin, Lanoxicaps)
        5. Major neurotransmitter released at end organ effectors of the thoracolumbar division of the autonomic nervous system:
          1.   dopamine (Intropin)
          2.   epinephrine
          3.   norepinephrine
          4.   acetylcholine
        6. Neurotransmitter of preganglionic fibers:
          1.   norepinephrine
          2.   substance P
          3.   epinephrine
          4.   acetylcholine
        7. "Fight or flight" activation of the ANS:
          1.   pupillary constriction
          2.   blood flow shifted from cutaneous beds to skeletal muscle
          3.   blood glucose falls
          4.   bronchiolar constriction
        8. Methoxamine (Vasoxyl)-induced bradycardia would be prevented by:
          1.   phentolamine (Regitine)
          2.   mecamylamine (Inversine)
          3.   atropine
          4.   all of the above
        9. Dopamine beta hydroxylase catalyzes:
          1.   tyrosine to DOPA
          2.   DOPA to dopamine
          3.   dopamine to norepinephrine
          4.   norepinephrine to epinephrine
        10. Primary mechaism for termination of norepinephrine and epinephrine action:
          1.   metabolic transformation catalyzed by MAO
          2.   metabolic transformation catalyzed by COMT
          3.   diffusion away from the synaptic cleft and uptake at extraneuronal sites
          4.   reuptake into nerve terminals
        11. Most potent at beta adrenergic receptors
          1.   epinephrine
          2.   isoproterenol (Isuprel)
          3.   norepinephrine
          4.   dopamine
        12. Interferes with norepinephrine release:
          1.   alpha-methyltyrosine by preventing synthesis of a protein that promotes fusion of the vesicle and the presynaptic membrane
          2.   bretylium (Bretylol) following a transient stimulation of release by displacement
          3.   reserpine
        13. alpha-2 receptor agonist; peripheral sympathomimetic
          1.   yohimbine (Yocon)
          2.   dobutamine (Dobutrex)
          3.   clonidine (Catapres)
          4.   phenylephrine
        14. Primary antihypertensive effect due to nitric oxide mediation of smooth muscle relaxation.
          1.   atropine
          2.   nitroprusside sodium (Nipride)
          3.   mecamylamine (Inversine)
          4.   captopril (Capoten)
        15. Inhibits neurotransmitter enzymic degradation:
          1.   tubocurarine
          2.   phenoxybenzamine (Dibenzyline)
          3.   physostigmine (Antilirium)
          4.   bretylium (Bretylol)
        16. Cardiac effects not like to be directly affected by the presence of an anticholinesterase:
          1.   acetylcholine
          2.   methacholine (Provocholine)
          3.   vagal stimulation
          4.   carbamylcholine (carbachol)
        17. Pilocarpine (Pilocar):
          1.   dry mouth
          2.   pupillary dilation
          3.   increased gastrointestinal tone
          4.   bronchiolar relaxation
  17. Elaboration of vesicular content (neurotransmitter) into the synaptic cleft is an example of:
    1.   carrier transport
    2.   passive diffusion
    3.   endocytosis
    4.   exocytosis
    5.   lipid diffusion
  18. Most acidic
    1.   urine
    2.   breast milk
    3.   jejunum,ileum contents
    4.   stomach contents
    5.   vaginal secretions
  19. Lipid solubility and drugs:
    1.   more of the weak acid drug will be in the lipid-soluble form at alkaline pH.
    2.   more of the weak acid drug will be in the lipid soluble form at acid pH.
    3.   more of the weak base drug will be in the lipid soluble form at alkaline pH
    4.   A & C
    5.   B & C
  20. Definition: Therapeutic Index
    1.   ED50/LD50
    2.   potency/selectivity
    3.   EC50/LD50
    4.   TD50/ED50
    5.   ED50
  21. Ion-trapping in the kidney:
    1.   Weak acids are usually excreted slower in alkaline urine
    2.   Weak bases are usually excreted faster in acidic urine
    3.   both
    4.   neither
  22. Weak base:
    1.   neutral molecule that dissociates into an anion and a proton
    2.   neutral molecule that forms a cation upon combining with a proton
    3.   charged molecule that remains charged independent upon pH
    4.   neutral molecule that remains uncharged independent of pH
    5.   none of the above
  23. Driving force for passive flux of molecules down a concentration gradient:
    1.   area/thickness
    2.   difference in concentration
    3.   permeability coefficient
    4.   area x permeability coefficient/thickness
    5.   thickness
  24. Most common drug permeation mechanism:
    1.   passive diffusion in aqueous or lipid medium
    2.   active transport
  25. Most likely to be transportred into cells by endocytosis:
    1.   propranolol
    2.   iron-complex with its binding protein
    3.   erythromycin-macrolide antibiotic
    4.   phenylalanine
    5.   peptide
  26. Permanently charged amine:
    1.   primary amine
    2.   secondary amine
    3.   tertiary amine
    4.   quaternary amine


    1. Cytochrome-P450 INDEPENDENT oxidation
      1.   amine oxidase
      2.   epoxidation
      3.   N-oxidation
      4.   S-oxidation
      5.   deamination
    2. Most drugs are oxidized in the:
      1.   smooth endoplasmic reticulum
      2.   rough endoplasmic reticulum
      3.   smooth and rough about equally
      4.   nucleus
      5.   none of the above
    3. Drug mixed-function oxidase (p450) mainly localized:
      1.   mitochondrial fraction
      2.   cell membranes
      3.   golgi bodies
      4.   microsomal fraction
      5.   nucleolus
    4. Primary site for drug metabolism:
      1.   stomach
      2.   small intestine
      3.   kidney
      4.   muscle
      5.   liver
    5. Drug biotransformation:
      1.   mainly, but not exclusively in the liver
      2.   products are usually less biologically active
      3.   biotransformation products can be toxic
      4.   A & B
      5.   A, B & C

      1. Weak base:
        1. phenobarbital (Luminal)
        2. acetaminophen (Tylenol, Panadol)
        3. morphine
        4. aspirin
        5. pentobarbital (Nembutal)
      2. Ion trapping:
        1. the fetal pH is higher than maternal pH
        2. in fetal distress alkalosis contributes to local anesthetic accumulation
        3. local anesthetics may tend to accumulate in the fetus
        4. A & C
        5. B & C
      3. Drug transport:
        1. Very hydrophilic drugs may not be well absorbed
        2. Excessively lipid-soluble (hydrophobic) drugs may not be soluble enough to cross a water layer near the cell membrane
        3. both
        4. neither
      4. Lipid diffusion:
        1. uncharged form: lipid-soluble
        2. charged form: lipid-soluble
        3. charged form: lipid insoluble
        4. charged and uncharged forms equally lipid-soluble
      5. Weak base at alkaline pH:
        1. relatively lipid-soluble
        2. probably uncharged
        3. both
        4. neither
      6. Disadvantages of the oral route of drug administration
        1. emesis
        2. gastric acidity may destroy the drug
        3. inconsistent absorption due to food or other effects
        4. usually expensive
      7. Percentage of oral digoxin (Lanoxin, Lanoxicaps) dose likely to reach systemic circulation:
        1. 100%
        2. 90%
        3. 70%
        4. 30%
        5. 10%
      8. Quaternary amine
        1. permanently charged
        2. charge dependent on pH relative to pKa
        3. uncharged
      9. First pass effect:
        1. requires passage of the drugs through the portal venous system
        2. lidocaine (Xylocaine)
        3. may result in minimal drug delivery to the systemic circulation
        4. A & C
        5. A, B & C
      10. A weak acid at acid pH:
        1. likely to be lipid-soluble
        2. probably will be uncharged
        3. both
        4. neither
      11. Primary factor in determining the rate of an orally ingested drug onset: rate and absorption extent by the gastrointestinal tract
        1. true
        2. false
      12. Aqueous diffusion:
        1. within large aqueous components
        2. across endothelial blood vessel lining
        3. across epithelial membrane tight junctions
      13. Transdermal delivery
        1. clonidine (Catapres)
        2. fentanyl (Sublimaze)
        3. scopolamine
        4. nitroglycerin
        5. none of the above
      14. Site(s) of drug metabolism following oral ingestion:
        1. blood
        2. intestinal wall
        3. liver
        4. A & C
        5. A, B & C
      15. Parenteral administration:
        1. less likely to be certain of active drug absorption
        2. acceptable route of administration for the unconscious patient
        3. rated systemic absorption will depend on drugs solubility in interstitial fluid
        4. aqueous channels (vascular endothelium) promote high diffusion rates of drugs, independent of their lipid solubility
      16. Rectal administration:
        1. Absorption of drug into superior hemorrhoidal veins results in the absence of the first-pass effect
        2. Low rectal administration may allow drugs to enter the systemic circulation without passing to the liver
        3. both
        4. neither
      17. Transport system requiring energy, e.g. ATP hydrolysis
        1. facilitated diffusion
        2. active transport
        3. both
        4. neither
      18. Weak acid:
        1. morphine
        2. chlordiazepoxide (Librium)
        3. phenobarbital (Luminal)
        4. cocaine
        5. ephedrine
      19. Release of neurotransmitter by synaptic terminal:
        1. endocytosis
        2. exocytosis
        3. both
        4. neither
      20. Important factor(s) in determining flux (molecular transport per unit time)
        1. concentration gradient
        2. area across which diffusion occurs
        3. lengthly of diffusion path
        4. A & C
        5. B & C
      21. Renal pharmacology/pharmacokinetics:
        1. Most drugs are not filtered by the glomerulus
        2. lipid-soluble drugs are typically reabsorbed by passive diffusion after glomerular filtration
        3. weak acids tend to be excreted faster in alkaline pH
        4. weak bases tend to be excreted faster in alkaline pH
      22. Optimal factors contributing to reliable transdermal drug absorption:
        1. drug promotes histamine release
        2. molecular weight < 1000
        3. daily drug requirement < 10 mg
        4. pH range < 4
      23. The lower the pH relative to the pKa the greater fraction of protonated drug is found
        1. true
        2. false
      24. More likely to require transport system to cross biological membranes:
        1. glucose
        2. ethanol
        3. both equally likely
        4. both equally unlikely to require transport systems
      25. Magnitude of first-pass hepatic effect
        1. depends on hepatic blood flow (Q)
        2. depends on clearance
        3. both
        4. neither
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