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Pharmacology and Medical Chemistry I > Exam 3 - Lecture 30, Opioids > Flashcards

Exam 3 - Lecture 30, Opioids Flashcards

1
Q

Opiate

A

defines drugs derived from opium, including semi-synthetic derivatives of morphine

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2
Q

Opioid

A

term for all agents, natural and synthetic, with morphine or opium-like actions

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3
Q

Endogenous opioid peptides are

A

the group of endogenous peptides with opioid actions; natural ligands for opioid receptors

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4
Q

Narcotic

A

Legal designation for opioid drugs and other drug of abuse that produce stupor and insensibility

medically defined as drugs with sedative/hypnotic and analgesic properties

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5
Q

How do opioid drugs produce their effects?

A

Stereospecificity - Levo isomers are active form

Saturability - finite number of sites; receptor occupancy determines magnitude of agonist effect

Competitive inhibition of binding by antagonists inhibits opioid effects

Affinity of receptor for opioid drugs correlates with their analogies potencies clinically

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6
Q

Four opioid classes

A

Enkephalins
Endorphins
Endomorphins
Nociception/ Orphanin FQ

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7
Q

Enkephalins derived from

A

proenkephalin

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8
Q

Forms of Enkephalin

A

Methionine - enkephalin (H-tyr-gly-gly-phe-met-OH)

Leucine - enkephalin (H-tyr-gly-gly-phe-leu-OH)

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9
Q

Endorphins

A

larger polypeptides than enkephalins but contain in their sequence met-enkephalin

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10
Q

Prodynorphin yields

A

dynorphin A, B, and a-neoendorphin

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11
Q

Pro-opiomelanocortin yields

A

B- endorphin

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12
Q

Endomorphins derived from

A

unknown source currently

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13
Q

Form of Endomorphins

A

Endomorphin 1 = Tyr-Pro-Trp-Phe-NH2

Endomorphin 2 = Tyr-Pro-Phe-Phe-NH2

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14
Q

Nociceptin/Orphanin FQ

A

17 amino acid peptide derived from pronociceptin

Considered the natural ligand for the ORL1 (OP4) opioid receptor

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15
Q

Opioid analgesia mediated in (Descending inhibitory pathway)

A

Mediated in dorsal columns of spinal cord, periaqueductal gray, raphe nucleus (5HT containing neurons)

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16
Q

Opioids produce analgesia by

A

Inhibiting release of substance P (Pain transmitter) from primary afferent pain fibers in spinal cord (Spinal level)

Altering subjective response to pain sensation, probably mediated at higher (supra spinal) centers in brain

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17
Q

Opioids effect on GI and motility

A

Mediated by stimulation of opioid receptors in nerve plexes and glands of stomach and intestine

Can be used as an anti-diarrheal

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18
Q

Four opioid receptor subtypes

A

Mu
Kappa
Delta
ORL1

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19
Q

Mu receptors and binding affinity

A

Morphine, prototype agonist

Endorphins>enkephalins>dynorphins

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20
Q

Kappa receptors and binding affinity

A

Ketocyclazocine, prototype agonist

Dynorphins>endorphins and enkephalins

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21
Q

Delta receptors and binding affinity

A

D-ala, D-leu enkephalin, prototype agonist

Enkephalins > endorphins> and dynorphins

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22
Q

ORL1 (opioid-receptor-like receptor)

A

Named after discovery of nociceptin/orpganin FQ, the endogenous ligand for this receptor

23
Q

Neurons Expressing D2 show

A

enkephalins

24
Q

Neurons Expressing D1 show

A

Dynorphins

25
Mu receptor physiological effect
analgesia, euphoria, respiratory depression, dependence, decrease GI motility
26
Kappa receptor physiological effect
Analgesia, dysphoria, diuresis
27
Delta receptor physiological effect
analgesia, decreased GI motility, immunity
28
ORL1 receptor physiological effect
Complex effects on pain, drug reward, feeding, learning and memory
29
Classical opioid receptors
Mu, Kappa, Delta Found in brain, spinal cord and peripheral tissues
30
Opioid receptor structure + biology
7 Transmembrane receptors G protein coupled Activate Gi/Go to inhibit Adenylate cyclase, activate inward rectifying K+ channels, and or inhibit Ca++ current
31
CNS effects: analgesia
Analgesia without loss of consciousness Distinction between pain sensation and pain as suffering (emotional) Opioids both elevate pain threshold and increase the capacity to tolerate pain (ie subjective, emotional response to pain)
32
CNS effects: Drowsiness and euphoria
Feeling of warmth over entire body, facial itching, especially of nose (cause of abuse). Some individuals find these effects unpleasant Muscle tone reduced, ability to concentrate and awareness reduced, apathy and lethargy prominent, "mental clouding"
33
CNS effect: Suppression of cough
Known as "anti-tussive" effect due to a direct action on medullary cough center
34
CNS effect: CNS excitation
only at extremely high doses or moderate doses in susceptible individuals Convulsions may occur, mechanism unkown
35
CNS effect: Emetic effects
Nausea and vomiting are frequent side-effects of opioid drugs Due to stimulation of CTZ in medulla Apomorphine, DA agonist, potent emetic agent
36
CNS effect: effect on pupil diameter (Miosis)
Pin point pupils consistent features of opioid drug use No tolerance develops to the pupillary constriction caused by opioid drugs Due to action on oculomotor nucleus in brain
37
CNS effect: effect on respiration (depression)
Direct depression of brainstem respiratory center - Reduced rate, minute volume, tidal exchange Blunting of normal reflex response to CO2 Deaths from opioid OD almost always due to respiratory arrest
38
Morphine effects on GI
Delay gastric emptying Decrease propulsive movement of small and large intestine, increase in resting ton and periodic intestinal spasms Failure to perceive sensory stimuli which normally activate defecation reglex No tolerance develops to the constipating effects of opioid drugs
39
Morphine: Cardiovascular effects
Little effect on heart rate, rhythm or blood pressure in supine patient (laying on back) Postural hypotension due to opioid induced vasodilation prominent in upright position
40
Morphine vasodilation due to
release of histamine Suppression of adrenergic vasoconstrictor tone Suppression of reflex vasoconstriction due to increased CO2 levels
41
Morphine effects on smooth muscle
Urinary bladder reduce capacity, urinary urgency with difficulty in peeing Uterine contractions no significantly affected, but duration of labor my be prolonged Bronchial muscle maybe constricted causing narrowing of the airway
42
ADME opioids
Well absorbed from GI tract, nasal mucosa, subcutaneous and intramuscular site Effects of a a given dose are greater after parenteral admin than oral admin due to "first pass" effect Distribution influenced by plasma protein binding (1/3) of total and accumulation of drug in kidney, lung, liver, Skm Metabolism of morphine primarily by hepatic conjugation with glucuronic acid; conjugated drug excreted primarily in pee and 7-10% poop
43
Drugs that potentiate opioid effects
Phenothiazine antipsych Tricyclic antidepressants Monoamine oxidase inhibitors
44
Opioid and amphetamine
Amphetamine potentiates euphorigenic effects, "speed-balling"
45
Opioid tolerance develops to
Analgesic action Euphoric effect Respiratory depressant effects No tolerance develops to mitosis and constipating effects
46
Tolerance opioids
Decreased response to drug after its chronic use Higher doses needed to achieve original response, cell mechanism unknown
47
Cross-tolerance
Tolerance of one drugs invokes tolerance to drugs with similar mechanisms of action
48
Dependence
Change resulting from chronic drug exposure such that drug is required for normative response Only seen in absence of drug (withdrawal) or can be shown with antagonist Cell mechanism unknown, can be suppressed by re-admin of drug or another drug with similar mechanism of action
49
High Chances of Tolerance Opioids
``` Analgesia Euphoria Mental clouding Sedation Respiratory depression Cough suppression Nausea and vomiting ```
50
Minimal to no chances of Tolerance opioids
Miosis Constipation Convulsions
51
Physical Dependence
develops after repeated use revealed as a withdrawal syndrome when drug is discontinued Admin of any opioid agonist can abruptly abolish withdrawal symptoms
52
Opioid Addiction
Distinct from tolerance and physical dependence Many addictions start with prescription use of opioids for pain
53
Criteria for Opioid addiction
``` tolerance Withdrawal symptoms when stopped use of large amounts over time unsuccessful attempt to stop alot of time spent getting drug continued use despite negative effects ```
54
Opioid locations in Afferent pain transmission
VPL, Amygdala, Parabrachial nucleus, Dosal Horn

Pharmacology and Medical Chemistry I (30 decks)

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