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Pharmacodynamics > Speth Final (Opioids, Ligand & Voltage Gated Channels) > Flashcards

Speth Final (Opioids, Ligand & Voltage Gated Channels) Flashcards

1
Q

What classification of drugs are alkaloids found in the opium poppy?

A

opiates

(e.g. codeine and morphine)

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2
Q

What is the major cause of death of opioid use?

A

respiratory depression

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3
Q

List 4 clinical problems associated with opioid use:

A
  • constipation
  • endocrine disturbances
  • tolerance to analgesic effect
  • interactions with other CNS-depressant drugs
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4
Q

In proopiomelanocortin (POMC), what amino acid is a critical part of the peptide that stimulates opioid receptors?

A

methionine (Met)

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5
Q

What two amino acids are found in the first 5 sequences of endogenous ligands?

A

Met or Leu

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6
Q

Which endogenous ligand is the “exception to the rule” and only has a 4 amino acid sequence instead of 5?

A

endomorphins

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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)

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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)
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9
Q

Name a prototypical opioid partial agonist that is often used to help patients in withdraw.

A

Buprenorphine (Buprenex, Subutex)

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10
Q

Name two opioid antagonist. Which one is most popular?

A
  • Naloxone (Narcan) = most popular
  • Naltrexone (Revia, Depade)
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11
Q

Give an example of each opioid classification by origin: natural, semisynthetic, synthetic.

A
  • natural = morphine
  • semisynthetic = heroin
  • synthetic = fentanyl
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12
Q

Which opioid receptor has “good and bad effects” in terms of response?

A

mu (u) receptor

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13
Q

List the three opioid receptors:

A
  • mu (u)
  • delta
  • kappa
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14
Q

List 4 pharmacological actions of opioids that are considered “good”:

A
  • analgesia
  • cough suppression
  • sedation
  • constipation
  • miosis
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15
Q

List 4 pharmacological actions of opioids that are considered “bad”:

A
  • respiratory depression
  • euphoria
  • tolerance
  • physical dependence
  • increased body temp
  • convulsions
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16
Q

The first cultivation of opium was from which plant?

A

Hul Gil “the joy plant”

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17
Q

Morphine was derived from which Greek god?

A

Morpheus (God of Dreams)

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18
Q

What did the patent medicines in the 1900s like snake oil contain?

A

opium, morphine, cocaine, alcohol

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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

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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

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21
Q

What is another name for drug dealer?

A

a criminal

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22
Q

Between 1998 and 2008, how much did the production of oxycodone increase?

A

nearly 6-fold

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23
Q

What two drugs are considered the “most common killers”?

A

fentanyl and methamphetamine

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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.

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25
Q

What complaint is the most common reason for seeking health care?

A

acute and chronic pain-related complaints

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26
Q

The HB21 bill also provides that a prescription for a schedule II opioid for treatment of acute pain may not exceed a ___ day supply.

A

3-day supply

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27
Q

Paracetamol and Ibuprofen are combined into a tablet called “combogesic”. What is the rule for oral administration of this tablet?

A

for short term use ONLY (not more than 3 days)

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28
Q

Name two types of ion channels:

A
  • ligand gated
  • voltage gated
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29
Q

What is the main neurotransmitter excitatory ligand-gated channels act on?

A

glutamate

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30
Q

What is the main neurotransmitter inhibitory ligand-gated channels act on?

A

GABA

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31
Q

What are inhibitory interneurons and what do they do?

A

short axons that inhibit neurotransmission balance

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32
Q

Activation of the GABA receptor ________ neurons by increasing Cl- permeability.

A

hyperpolarizes

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33
Q

If a patient is suffering from seizure, which neurotransmitter do you want to increase?

A

GABA

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34
Q

T/F all GABA receptors are ion channels

A

FALSE

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35
Q

How many GABA binding sites are there per receptor?

A

two

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36
Q

Name two depressants that act on GABA receptors:

A

benzodiazepines and barbiturates

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37
Q

Z drugs bind to ______ sites on the GABA A receptor to potentiate GABA mediated channel opening.

A

allosteric

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38
Q

What blocks the GABA-gated chloride channel?

A

Picrotoxin

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39
Q

Benzodiazepine (BZD) effects on anxiety are blocked by ______ antagonists.

A

GABA

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40
Q

List 3 Benzodiazepine (BZD) actions on the body:

A
  • muscle relaxation
  • sedation
  • anticonvulsant action
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41
Q

What is the difference between Benzodiazepines (BZD) and Phenobarbital?

A

BZD doesn’t do anything without GABA, phenobarbital can activate channels without GABA

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42
Q

Name two GABA receptor blockers:

A

Picrotoxin and Bicuculline

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43
Q

Z drugs are selective to which GABA receptor subunit?

A

GABA a1 subunit

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44
Q

High levels of GABA subunit a5 receptor is found where in the brain?

A

hippocampus

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45
Q

What drug is a selective competitive antagonist of Benzodiazepine (BZD) binding site?

A

Flumazenil (Romazicon)

(reverses sedative effects of BZDs in overdoses)

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46
Q

Name one GABA A receptor agonist and one antagonist.

A

agonist = Muscimol
antagonist = Bicuculline

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47
Q

Which Benzodiazepine (BZD) was a prototype for all BZD?

A

Diazepam (Valium)

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48
Q

In the Rolling Stones song “Mother’s Little Helper” there’s a little yellow pill. What drug is this song about?

A

Valium

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49
Q

Give two examples of “Z drugs”.

A
  • Ambien
  • Sonesta
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50
Q

Z drugs are more selective than ______ and bind to the BZD binding site of the _____ receptor.

A

benzodiazepines; GABA

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51
Q

Z drugs are more selective than BZD because they bind only to the _____1 _____2 subunit interface associated with sedation and ______.

A

alpha1; gamma2; amnesia

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52
Q

T/F Z drugs can be used for short-term and chronic use.

A

TRUE AND FALSE

should be used for only short-term but many people use them chronically

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53
Q

Z drugs are primarily for the treatment of what?

A

insomnia

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54
Q

Which Z drug has a very short duration of action and is for initiating sleep?

A

Zaleplon (Sonata)

55
Q

Which Z drug has a shorter duration in men more than women?

A

Zolpidem (Ambien)

56
Q

Some sleeping pills have strange effects like sleep walking. What is another name for sleep walking?

A

somnambulism

57
Q

The Beers Criteria Medication List is a list of drugs not recommended for who?

A

older people

58
Q

What drug at high concentrations can be a full agonist of the GABA A receptor?

A

barbiturates

59
Q

What drug was administered by IV to induce anesthesia and used to kill people for executions?

A

Thiopental

60
Q

What was “Mother’s Little Helper?”

A

Valium (Diazepam)

61
Q

What receptor reacts with MDMA?

A

glycine receptor

62
Q

What was the first performance enhancing drug?

A

Strychnine (nut vomica)

63
Q

What are two major groups of ionotropic glutamate receptors?

A

NDMA and AMPA

64
Q

_____ receptor activation enhances inhibitory GABA transmission.

A

NMDA

65
Q

Which receptors need to open first before NMDA is open?

A

AMPA

66
Q

Name two NMDA antagonists:

A
  • ketamine
  • phencyclidine (PCP)
67
Q

Name one NMDA agonist

A

glutamate

68
Q

What are the two glutamate receptor subtypes and which one is a GPCR?

A
  • ionotropic
  • metabotropic (GPCR)
69
Q

What are the functional classes of the inotropic glutamate receptor?

A

AMPA, Kainate, NMDA

70
Q

What are the functional classes of the metabotropic glutamate receptor?

A

class I, class II, class III

71
Q

What two ion channels do AMPA receptors work on?

A

Na+ and K+

72
Q

AMPA receptors act on Na+ and K+ ion channels, which mediate the majority of _____ ______ neurotransmission.

A

fast excitatory

(AMPA receptors has fast kinetics)

73
Q

What subunit makes most AMPA receptors calcium impermeable?

A

the GluR2 subunit

(has arginine instead of glutamine)

I think this will def be a question

74
Q

Do NMDA receptors or AMPA receptors have slower kinetics?

A

AMPA

75
Q

What receptors require glycine or D-serine as a co-agonist?

A

NMDA

76
Q

Depolarization by AMPA receptors is stimulated by what?

A

glutamate

77
Q

What drug is a great antidepressant because it acts instantly but unfortunately causes hallucinations?

A

ketamine

78
Q

In seizure disorders, excessive stimulation by glutamate will cause neuronal cell death by elevating _____ levels in the cell.

A

calcium

79
Q

What drug can sustain cognitive gentian for a short time in Alzheimers patients and is a unique antagonist at NMDA receptors?

A

Memantine (Namenda)

(weak agonist, doesn’t completely block NMDA)

80
Q

What amino acid will you find in excess in Alzheimers disease?

A

glutamate

81
Q

The NMDA receptor has involvement in _____ and _____ and long-term potentiation.

A

learning; memory

82
Q

In the long-term potentiation (LTP) of Namenda, LTP requires what?

A

activation of synapses and depolarization of postsynaptic membrane

83
Q

In the long-term potentiation (LTP) of Namenda, LTP involves what?
Hint: 4 things

A
  • release of glutamate
  • activation of NMDA receptors in depolarized membrane
  • entry of calcium ions
  • new AMPA receptors in the postsynaptic membrane
84
Q

PCP and Ketamine block what channel?

A

NMDA

85
Q

Which serotonin receptor is a nonselective ion channel and is not a GPCR?

A

5HT3

86
Q

Name the 3 primary voltage-gated ion channels and the 1 secondary voltage-gated ion channel:

A
  • calcium
  • sodium
  • potassium
  • chloride (secondary)
87
Q

Which voltage-gated ion channel is responsible for neurotransmission, secretion, cardiac pacemaker activity and contraction of muscle cells?

A

calcium

88
Q

Which voltage-gated ion channel is responsible for neurotransmission and conduction of nerve impulses?

A

sodium

89
Q

Which voltage-gated ion channel is reestablished the membrane potential?

A

potassium

90
Q

Which voltage-gated ion channel is responsible for the regulation of pH, volume homeostasis, organic solute transport, cell migration, cell proliferation and differentiation?

A

chloride

91
Q

Where is potassium stored?

A

in the cytoplasm

92
Q

the Cav1 subfamily mediates what type of calcium currents?

A

L-type

93
Q

The Cav2 subfamily mediates what type of calcium currents?

A

P/Q-type, N-type, R-type

94
Q

What type of calcium currents are mainly on the heart?

A

L-type

95
Q

Most drugs work on what type of calcium currents?

A

L-type

96
Q

A strong change in membrane potential can shorten the _______ period.

A

refractory

97
Q

_______ refractory period is the time after opening of channel when it is unable to open again.

A

absolute

98
Q

_______ refractory period is the time after opening of a channel when only a strong depolarization can reactivate it.

A

relative

99
Q

What mV does it take for an action potential to get activated?

A

-55 mV

100
Q

What is a neurotoxin with potential analgesic activity?

A

Tetrodoxin (TTX)

101
Q

What does TTX do that makes it so toxic?

A

inhibits nerve action potentials and blocks nerve transmission

102
Q

Pyrethroids are synthetic chemicals that act like ______.

A

pyrethrin

103
Q

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?

A

pyrethrin

104
Q

Permethrin can be used on food, crops, livestock, and pets but NOT _____.

A

cats

105
Q

Some permethrin products can be used to treat ______ and ______ on people.

A

scabies; head lice

106
Q

Local anesthetics bind to the inside of ______ channels.

A

sodium

107
Q

Local anesthetics bind with higher affinity to “activated” and “inactivated” states of channel use ________ inhibition.

A

dependent

108
Q

Which local anesthetics are esters?

A
  • cocaine
  • procaine (novocaine)
  • benzocaine
  • tetracaine
109
Q

Which local anesthetics are amides?

A
  • lidocaine
  • bupivacaine
  • mepivacaine
  • ropivacaine
110
Q

Which local anesthetics (amides or esters) tend to be short acting because they are quickly metabolized by plasma cholinesterase?

A

esters

111
Q

Which local anesthetics (amides or esters) tend to be more resistant to metabolic inactivation which occurs in the liver via P450s?

A

amides

112
Q

What will limit the systemic distribution of a local anesthetic?

A

potent vasoconstrictor
(epi or phenylephrine)

113
Q

High concentrations of local anesthetics can cause what?
Hint: 4 things

A
  • weakness
  • methemoglobinemia
  • convulsions
  • dysrhythmias
114
Q

Gabapentin is a synthetic analogue of the neurotransmitter ______-________ acid.

A

gamma-aminobutyric acid

115
Q

gamma-aminobutyric acid can have anticonvulsant activity but can also be used for the treatment of _________ pain and _______ _____ syndrome.

A

neuropathic pain; restless legs syndrome

116
Q

Pregabalin selectively binds to alpha2delta subunits of presynaptic voltage-dependent ______ channels.

A

calcium

117
Q

The drug action of B-adrenergic receptor blockade treats what abnormal cardiac condition?

A

atrial fibrillation or flutter

118
Q

_______ is a short-term inhibitory neurotransmitter that treats paroxysmal supra ventricular tachycardia.

A

adenosine

119
Q

Name a Class II B-adrenergic receptor blocker.

A

propranolol

120
Q

Does the drug Diltiazem have an increased or decreased effect on action potential duration?

A

decreased

121
Q

Does lidocaine have an increased or decreased effect on action potential duration?

A

decreased

122
Q

Lidocaine rapidly blocks both activated and inactivated ______ channels, though there is some preference for the inactivated state.

A

sodium

123
Q

In partially depolarized cells, lidocaine significantly _______ membrane responsiveness.

A

depresses

124
Q

Lidocaine also elevates the ________ _______ threshold.

A

ventricular fibrillation

125
Q

What is a derivative of lidocaine that is orally active?

A

Mexiletine

126
Q

Mexiletine ______ the maximal rate of depolarization of the cardiac action potential and exerts a negligible effect on depolarization.

A

slows

127
Q

T/F lidocaine is not orally active:

A

TRUE

128
Q

Drugs that act upon calcium channels are almost exclusively _______ of calcium channel function aka calcium channel blockers.

A

antagonists

129
Q

What are the 3 calcium channel blocker drug classes?

A
  • dihydropyridines
  • phenylalkylamines
  • benzothiazepines
130
Q

What calcium channel blocker drug class preferentially block vascular smooth muscle calcium channels and doesn’t have cardiac effects at therapeutic doses?

A

dihydropyridines

131
Q

What calcium channel blocker drug class acts on the heart as well as vascular smooth muscle?

A

phenylalkylamines

132
Q

What calcium channel blocker drug class acts on heart as well as vascular smooth muscle?

A

benzothiazepines

133
Q

The molecular structure of CL- channel types varies from ___ to ___ transmembrane segments.

A

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Pharmacodynamics (4 decks)

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