Speth Final (Opioids, Ligand & Voltage Gated Channels) Flashcards
(133 cards)
1
Q
What classification of drugs are alkaloids found in the opium poppy?
A
opiates
(e.g. codeine and morphine)
2
Q
What is the major cause of death of opioid use?
A
respiratory depression
3
Q
List 4 clinical problems associated with opioid use:
A
- constipation
- endocrine disturbances
- tolerance to analgesic effect
- interactions with other CNS-depressant drugs
4
Q
In proopiomelanocortin (POMC), what amino acid is a critical part of the peptide that stimulates opioid receptors?
A
methionine (Met)
5
Q
What two amino acids are found in the first 5 sequences of endogenous ligands?
A
Met or Leu
6
Q
Which endogenous ligand is the “exception to the rule” and only has a 4 amino acid sequence instead of 5?
A
endomorphins
7
Q
The overall effect of u-opioid receptor actions at these effectors is to inhibit neuronal activity. What g-coupled protein receptor is it acting on? (the “u” is pronounced “mu”).
A
Gsub-i (aka Gai)
8
Q
List 3 generic and proprietary names of opioid agonists:
A
- Fentanyl (Duragesic = skin, Sublimate = pill form)
- Hydrocodone (Hycodan = potent analgesic)
- Oxycodone (oxycontin, Roxicodone)
9
Q
Name a prototypical opioid partial agonist that is often used to help patients in withdraw.
A
Buprenorphine (Buprenex, Subutex)
10
Q
Name two opioid antagonist. Which one is most popular?
A
- Naloxone (Narcan) = most popular
- Naltrexone (Revia, Depade)
11
Q
Give an example of each opioid classification by origin: natural, semisynthetic, synthetic.
A
- natural = morphine
- semisynthetic = heroin
- synthetic = fentanyl
12
Q
Which opioid receptor has “good and bad effects” in terms of response?
A
mu (u) receptor
13
Q
List the three opioid receptors:
A
- mu (u)
- delta
- kappa
14
Q
List 4 pharmacological actions of opioids that are considered “good”:
A
- analgesia
- cough suppression
- sedation
- constipation
- miosis
15
Q
List 4 pharmacological actions of opioids that are considered “bad”:
A
- respiratory depression
- euphoria
- tolerance
- physical dependence
- increased body temp
- convulsions
16
Q
The first cultivation of opium was from which plant?
A
Hul Gil “the joy plant”
17
Q
Morphine was derived from which Greek god?
A
Morpheus (God of Dreams)
18
Q
What did the patent medicines in the 1900s like snake oil contain?
A
opium, morphine, cocaine, alcohol
19
Q
What Pharma company aggressively marketed opioids by fear-mongering the public with “it’s important to control pain to speed recovery”?
A
Purdue Pharma
20
Q
Why does hardly anyone die from a drug overdose in Portugal?
A
they decided to treat possession and use of small quantities as a public health issue, not a criminal one
21
Q
What is another name for drug dealer?
A
a criminal
22
Q
Between 1998 and 2008, how much did the production of oxycodone increase?
A
nearly 6-fold
23
Q
What two drugs are considered the “most common killers”?
A
fentanyl and methamphetamine
24
Q
What is the HB21 bill?
A
a prescriber or dispenser must consult the PDMP database to review a patient’s controlled substance dispensing history before prescribing or dispensing a controlled substance for a patient who is 16 years or older.
25
What complaint is the most common reason for seeking health care?
acute and chronic pain-related complaints
26
The HB21 bill also provides that a prescription for a schedule II opioid for treatment of acute pain may not exceed a ___ day supply.
3-day supply
27
Paracetamol and Ibuprofen are combined into a tablet called "combogesic". What is the rule for oral administration of this tablet?
for short term use ONLY (not more than 3 days)
28
Name two types of ion channels:
- ligand gated
- voltage gated
29
What is the main neurotransmitter excitatory ligand-gated channels act on?
glutamate
30
What is the main neurotransmitter inhibitory ligand-gated channels act on?
GABA
31
What are inhibitory interneurons and what do they do?
short axons that inhibit neurotransmission balance
32
Activation of the GABA receptor ________ neurons by increasing Cl- permeability.
hyperpolarizes
33
If a patient is suffering from seizure, which neurotransmitter do you want to increase?
GABA
34
T/F all GABA receptors are ion channels
FALSE
35
How many GABA binding sites are there per receptor?
two
36
Name two depressants that act on GABA receptors:
benzodiazepines and barbiturates
37
Z drugs bind to ______ sites on the GABA A receptor to potentiate GABA mediated channel opening.
allosteric
38
What blocks the GABA-gated chloride channel?
Picrotoxin
39
Benzodiazepine (BZD) effects on anxiety are blocked by ______ antagonists.
GABA
40
List 3 Benzodiazepine (BZD) actions on the body:
- muscle relaxation
- sedation
- anticonvulsant action
41
What is the difference between Benzodiazepines (BZD) and Phenobarbital?
BZD doesn't do anything without GABA, phenobarbital can activate channels without GABA
42
Name two GABA receptor blockers:
Picrotoxin and Bicuculline
43
Z drugs are selective to which GABA receptor subunit?
GABA a1 subunit
44
High levels of GABA subunit a5 receptor is found where in the brain?
hippocampus
45
What drug is a selective competitive antagonist of Benzodiazepine (BZD) binding site?
Flumazenil (Romazicon)
(reverses sedative effects of BZDs in overdoses)
46
Name one GABA A receptor agonist and one antagonist.
agonist = Muscimol
antagonist = Bicuculline
47
Which Benzodiazepine (BZD) was a prototype for all BZD?
Diazepam (Valium)
48
In the Rolling Stones song "Mother's Little Helper" there's a little yellow pill. What drug is this song about?
Valium
49
Give two examples of "Z drugs".
- Ambien
- Sonesta
50
Z drugs are more selective than ______ and bind to the BZD binding site of the _____ receptor.
benzodiazepines; GABA
51
Z drugs are more selective than BZD because they bind only to the _____1 _____2 subunit interface associated with sedation and ______.
alpha1; gamma2; amnesia
52
T/F Z drugs can be used for short-term and chronic use.
TRUE AND FALSE
should be used for only short-term but many people use them chronically
53
Z drugs are primarily for the treatment of what?
insomnia
54
Which Z drug has a very short duration of action and is for initiating sleep?
Zaleplon (Sonata)
55
Which Z drug has a shorter duration in men more than women?
Zolpidem (Ambien)
56
Some sleeping pills have strange effects like sleep walking. What is another name for sleep walking?
somnambulism
57
The Beers Criteria Medication List is a list of drugs not recommended for who?
older people
58
What drug at high concentrations can be a full agonist of the GABA A receptor?
barbiturates
59
What drug was administered by IV to induce anesthesia and used to kill people for executions?
Thiopental
60
What was "Mother's Little Helper?"
Valium (Diazepam)
61
What receptor reacts with MDMA?
glycine receptor
62
What was the first performance enhancing drug?
Strychnine (nut vomica)
63
What are two major groups of ionotropic glutamate receptors?
NDMA and AMPA
64
_____ receptor activation enhances inhibitory GABA transmission.
NMDA
65
Which receptors need to open first before NMDA is open?
AMPA
66
Name two NMDA antagonists:
- ketamine
- phencyclidine (PCP)
67
Name one NMDA agonist
glutamate
68
What are the two glutamate receptor subtypes and which one is a GPCR?
- ionotropic
- metabotropic (GPCR)
69
What are the functional classes of the inotropic glutamate receptor?
AMPA, Kainate, NMDA
70
What are the functional classes of the metabotropic glutamate receptor?
class I, class II, class III
71
What two ion channels do AMPA receptors work on?
Na+ and K+
72
AMPA receptors act on Na+ and K+ ion channels, which mediate the majority of _____ ______ neurotransmission.
fast excitatory
(AMPA receptors has fast kinetics)
73
What subunit makes most AMPA receptors calcium impermeable?
the GluR2 subunit
(has arginine instead of glutamine)
**I think this will def be a question**
74
Do NMDA receptors or AMPA receptors have slower kinetics?
AMPA
75
What receptors require glycine or D-serine as a co-agonist?
NMDA
76
Depolarization by AMPA receptors is stimulated by what?
glutamate
77
What drug is a great antidepressant because it acts instantly but unfortunately causes hallucinations?
ketamine
78
In seizure disorders, excessive stimulation by glutamate will cause neuronal cell death by elevating _____ levels in the cell.
calcium
79
What drug can sustain cognitive gentian for a short time in Alzheimers patients and is a unique antagonist at NMDA receptors?
Memantine (Namenda)
(weak agonist, doesn't completely block NMDA)
80
What amino acid will you find in excess in Alzheimers disease?
glutamate
81
The NMDA receptor has involvement in _____ and _____ and long-term potentiation.
learning; memory
82
In the long-term potentiation (LTP) of Namenda, LTP requires what?
activation of synapses and depolarization of postsynaptic membrane
83
In the long-term potentiation (LTP) of Namenda, LTP involves what?
Hint: 4 things
- release of glutamate
- activation of NMDA receptors in depolarized membrane
- entry of calcium ions
- new AMPA receptors in the postsynaptic membrane
84
PCP and Ketamine block what channel?
NMDA
85
Which serotonin receptor is a nonselective ion channel and is not a GPCR?
5HT3
86
Name the 3 primary voltage-gated ion channels and the 1 secondary voltage-gated ion channel:
- calcium
- sodium
- potassium
- chloride (secondary)
87
Which voltage-gated ion channel is responsible for neurotransmission, secretion, cardiac pacemaker activity and contraction of muscle cells?
calcium
88
Which voltage-gated ion channel is responsible for neurotransmission and conduction of nerve impulses?
sodium
89
Which voltage-gated ion channel is reestablished the membrane potential?
potassium
90
Which voltage-gated ion channel is responsible for the regulation of pH, volume homeostasis, organic solute transport, cell migration, cell proliferation and differentiation?
chloride
91
Where is potassium stored?
in the cytoplasm
92
the Cav1 subfamily mediates what type of calcium currents?
L-type
93
The Cav2 subfamily mediates what type of calcium currents?
P/Q-type, N-type, R-type
94
What type of calcium currents are mainly on the heart?
L-type
95
Most drugs work on what type of calcium currents?
L-type
96
A strong change in membrane potential can shorten the _______ period.
refractory
97
_______ refractory period is the time after opening of channel when it is unable to open again.
absolute
98
_______ refractory period is the time after opening of a channel when only a strong depolarization can reactivate it.
relative
99
What mV does it take for an action potential to get activated?
-55 mV
100
What is a neurotoxin with potential analgesic activity?
Tetrodoxin (TTX)
101
What does TTX do that makes it so toxic?
inhibits nerve action potentials and blocks nerve transmission
102
Pyrethroids are synthetic chemicals that act like ______.
pyrethrin
103
What is a natural extract from the chrysanthemum flower that is a "secondary metabolite" that has no other function other than to protect the plant from insects?
pyrethrin
104
Permethrin can be used on food, crops, livestock, and pets but NOT _____.
cats
105
Some permethrin products can be used to treat ______ and ______ on people.
scabies; head lice
106
Local anesthetics bind to the inside of ______ channels.
sodium
107
Local anesthetics bind with higher affinity to "activated" and "inactivated" states of channel use ________ inhibition.
dependent
108
Which local anesthetics are esters?
- cocaine
- procaine (novocaine)
- benzocaine
- tetracaine
109
Which local anesthetics are amides?
- lidocaine
- bupivacaine
- mepivacaine
- ropivacaine
110
Which local anesthetics (amides or esters) tend to be short acting because they are quickly metabolized by plasma cholinesterase?
esters
111
Which local anesthetics (amides or esters) tend to be more resistant to metabolic inactivation which occurs in the liver via P450s?
amides
112
What will limit the systemic distribution of a local anesthetic?
potent vasoconstrictor
(epi or phenylephrine)
113
High concentrations of local anesthetics can cause what?
Hint: 4 things
- weakness
- methemoglobinemia
- convulsions
- dysrhythmias
114
Gabapentin is a synthetic analogue of the neurotransmitter ______-________ acid.
gamma-aminobutyric acid
115
gamma-aminobutyric acid can have anticonvulsant activity but can also be used for the treatment of _________ pain and _______ _____ syndrome.
neuropathic pain; restless legs syndrome
116
Pregabalin selectively binds to alpha2delta subunits of presynaptic voltage-dependent ______ channels.
calcium
117
The drug action of B-adrenergic receptor blockade treats what abnormal cardiac condition?
atrial fibrillation or flutter
118
_______ is a short-term inhibitory neurotransmitter that treats paroxysmal supra ventricular tachycardia.
adenosine
119
Name a Class II B-adrenergic receptor blocker.
propranolol
120
Does the drug Diltiazem have an increased or decreased effect on action potential duration?
decreased
121
Does lidocaine have an increased or decreased effect on action potential duration?
decreased
122
Lidocaine rapidly blocks both activated and inactivated ______ channels, though there is some preference for the inactivated state.
sodium
123
In partially depolarized cells, lidocaine significantly _______ membrane responsiveness.
depresses
124
Lidocaine also elevates the ________ _______ threshold.
ventricular fibrillation
125
What is a derivative of lidocaine that is orally active?
Mexiletine
126
Mexiletine ______ the maximal rate of depolarization of the cardiac action potential and exerts a negligible effect on depolarization.
slows
127
T/F lidocaine is not orally active:
TRUE
128
Drugs that act upon calcium channels are almost exclusively _______ of calcium channel function aka calcium channel blockers.
antagonists
129
What are the 3 calcium channel blocker drug classes?
- dihydropyridines
- phenylalkylamines
- benzothiazepines
130
What calcium channel blocker drug class preferentially block vascular smooth muscle calcium channels and doesn't have cardiac effects at therapeutic doses?
dihydropyridines
131
What calcium channel blocker drug class acts on the heart as well as vascular smooth muscle?
phenylalkylamines
132
What calcium channel blocker drug class acts on heart as well as vascular smooth muscle?
benzothiazepines
133
The molecular structure of CL- channel types varies from ___ to ___ transmembrane segments.
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