Pharm- Drug Receptors Agonists and Antagonists.txt

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Pharm- Drug Receptors Agonists and Antagonists.txt
2015-04-14 16:49:38
vetmed pharm

vetmed, pharm
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  1. Drugs act through their _________ for certain forms of living matter; they alter the function of...
    chemical affinity; ALL cells that contain the right receptor.
  2. The action of drugs is __________ and not __________; the __________ of living matter may be changes, but the _________________ is unchangeable.
    quantitative; qualitative; activity; form which the activity assumes (can only change in degree but not type)
  3. Drugs cannot produce an action that is _______________, but they can only __________ that action by __________ or __________ it.
    qualitatively different than the cell is already capable; modify; stimulating; inhibiting
  4. Many drug act by combining with _______________ which normally respond to _________ and ___________; other drugs act by interfering with ____________ and _______________.
    physiologic receptors; endogenous hormones; neurotransmitter chemicals; natural enzymatic processes; cellular transport systems/ionic channels
  5. Cholinergic nicotinic receptors utilize _____________.
    structure action relationships
  6. Nicotinic receptors at all _____________ relay messages from the ___________ to _________ of both _______________(2). Nicotinic receptors are also located at __________.
    autonomic ganglia; CNS innervated organs; parasympathetic and sympathetic divisions; muscle motor end plates
  7. Mucarinic cholinergic receptors provide transmission at _________________, such as ______________.
    parasympathetic neuroeffector junctions; SA node of the heart
  8. Of the drug-receptor binding forces, ______________ act at the greatest distance and are the strongest.
    electrostatic forces
  9. What are the 4 drug-receptor binding forces?
    electrostatic, ion-dipole, hydrogen bonds, van der waals
  10. The hypothetical nicotinic ganglionic receptor employs a congeneric series of compounds differing in the...
    methyl carbons separating cationic groups and in the receptor blocking capabilities of different compounds.
  11. Neuromuscular blocking drugs will bind to the ____________ and prevent __________ from occupying the active site and producing ____________.
    nicotinic receptor; acetylcholine; depolarization
  12. Succinylcholine has a carbonyl O which can initiate _____________ and ___________.
    Na channel opening; depolarization
  13. The initial depolarization caused by succinylcholine is _______________ which often precedes the ____________ and ____________; in contrast, tubocurarine causes induction that is ____________ because it _____________.
    twitching; actual blockade; relaxation; smooth without twitching; lacks that appropriate carbonyls
  14. Blockade by tubocurarine is ______________.
    strictly competitive
  15. The acetylcholine molecule is ____(2)____ and capable of _________ and _________to assume ____(2)____.
    linear and flexible; rotating and folding; a cis or partial ring shape or a trans or extended shape
  16. The cis and trans forms of acetylcholine are not isomers because of __________________ but when you have an _____________, is possible to have optical isomers.
    unrestricted rotation; asymmetric carbon
  17. The two natural hormones oxytocin and vasopressin (ADH) differ only in the.....
    amino acid found at the 3 and 8 position.
  18. With a competitive cholinergic blocking drug (such as _________), ______ doses of ________ are needed to produce the same maximal response without the blocker.
    atropine; higher; Ach;
  19. With a non-competitive cholinergic blocker, the maximal response is...
    reduced, regardless of the amount of Ach added.
  20. Type of dose where increasing the dose results in a corresponding increase in response in an organ or system.
    graded-dose response
  21. The occupancy theory of drug-receptor interactions proposed that the effect of drug produced was proportional to the ___________________, so that when the response was 50% maximal, ...
    number of receptors occupied; half the total receptors were occupied by drug molecules.
  22. The maximal drug effect when all receptors are occupied.
    ceiling effect
  23. The maximal drug effect when all receptors are occupied is analogous to the ______________.
    maximal velocity of the reaction, Vmax
  24. The concentration at which the drug effect is half maximal is a measure of the __________ for the _________ and is analogous to the ________.
    affinity of the drug; receptor; Km
  25. For a receptor associated with an ion channel, when a full agonist occupies the receptor, the channel ____________.
    opens fully
  26. Affinity = __________, intrinsic activity= _________.
    potency; efficacy
  27. ___________ is a competitive antagonist of Morphine.
  28. By definition, partial agonist= ____________.
    competitive antagonist
  29. Agonists and analogs of the natural product morphine vary primarily in the _____________ and therefore _________ based on affinity at the receptor.
    effective dose; potency
  30. Compounds that act as antagonists of morphine act at the ________ and effectively ___________ the effects oft he agonists.
    opiate receptor; block or reverse
  31. Differences in affinity of agonists and antagonists of morphine can be expressed as ________ and intrinsic activity as ______.
    1/KD; K3
  32. Non-receptor acting drugs usually act through _____________.
    physical-chemical actions
  33. Isoflurane is a _________ that is _____________ mediated; it interrupts __________ by combining with ___________.
    complete anesthetic; non-receptor; impulse conduction; myelin
  34. 2 examples of processes utilized by non-receptor mediated drug effects.
    osmotic pull (diuretics, cathartics, plasma volume expanders) and chelation (Na EDTA)