Opioid Sheet To My Own Flash Cards
Two Natural opioids …
Morphine
Codeine
“Five “Semisynthetic opioids
Buprenorphine
Hydromorphone
Hydrocodone
Oxycodone
Oxymorphone
Five Synthetic opioids
1 Fentanyl
2 Meperidine
3 Methadone
4 Tapentodol
5 Tramodol
Strong opioid receptor agonist
“6”
Morphine
Fentanyl
Alfentanil
Remifentanil
Pethidine = meberidine
Methadone
Moderate opioid receptor agonist
Codeine
Partial agonist “opioid receptor “& Mixed
agonist/Antagonist
“3”
Pentazocine
Buprenorphine
Nalbuphine
Pure”opioid receptor” antagonists
Naloxone
Naltrexone
Me : Semisynthetic partial agonist & Mixed
agonist/Antagonist
Buprenorphine
The major effects of the opioids are
mediated by three main receptor families,
commonly designated as
u (mu, MOR),
K (kappa, KOR), and
8 (delta, DOR).
All three opioid receptors are members of the …$ receptor family and inhibit…..1 They are also associated with ion channels, *increasing …..2 efflux (hyperpolarization) or * reducing…..3 influx, thus impeding neuronal firing and transmitter release in the spinal dorsal horn.
$ G protein coupled receptor
1 inhibit adenyl cyclase.
2 postsynaptic K+
3 presynaptic Ca2+
Most of the clinically useful opioid
analgesics, however, have preferential or
strong selectivity for ……. receptors.
mu opioid receptors
What is the source of morphine?
a) Synthetic production
b) Opium poppy (Papaver somniferum)
c) Cannabis plant
d) Willow bark
b) Opium poppy (Papaver somniferum)
Which Greek god does the name “Morphine” represent?
a) Zeus
b) Hades
c) Morpheus
d) Apollo
C
What is the mechanism of action of morphine?
a) Inhibition of acetylcholinesterase
b) Activation of adenylyl cyclase
c) Inhibition of opioid receptors
d) Inhibition of adenylyl cyclase and modulation of ion conductance
d) Inhibition of adenylyl cyclase and modulation of ion conductance
the prototypical strong
Mu receptor agonist.
Morphine
The receptor on which morphine acts is called……1.
………..2 are the endogenous peptide ligands found in the brain
the brain for opioid receptors.
1 opioid receptor
2 Endorphins
In activation of opioid receptors with morphine
The activated……1 subunit of the G protein directly inhibits the adenyl cyclase enzyme, and the GBy subunits are thought to mediate the changes at the …….2
1 “G alpha i“
2 Ca2+ and K+ channels.
The mechanism of action of morphine after the activation of opioid receptors and inhibition of adenyl cyclase is An increase in K+ conductance, and a decrease in Ca2+ conductance.
These actions cause both:
…..1 of neurotransmitter release from the central terminations of
small diameter primary afferent fibers and
……2 of membrane depolarization of dorsal horn nociceptive
neurons.
1 presynaptic inhibition
2 postsynaptic inhibition
What effect does the activation of opioid receptors by morphine have on neurotransmitter release?
a) Increase in neurotransmitter release
b) No effect on neurotransmitter release
c) Inhibition of neurotransmitter release
d) Potentiation of neurotransmitter release
c) Inhibition of neurotransmitter release
Which subunit of the G protein is thought to directly inhibit adenylyl cyclase enzyme?
a) Gαi
b) Gαs
c) Gβγ
d) Gαq
a) Gαi
What is the consequence of activation of opioid receptors in the dorsal horn nociceptive neurons?
a) Hyperpolarization
b) inhibition of membrane Depolarization
c) Inhibition of neurotransmitter release
d) Activation of adenylyl cyclase
b) inhibition of membrane Depolarization
G.R
subcutaneous and IV injections of morphine produce the most reliable response than oral preparation ?
b.c of significant first-pass metabolism of morphine occurs in the liver,
G.R
Morphine should not be used for analgesia during labor.
b.c During delivery (may cause neonatal asphyxia & prolong labor),
+
Morphine rapidly enters all body tissues, including the fetuses of pregnant
women. Infants born to addicted mothers show physical dependence on opioids
and exhibit withdrawal symptoms if opioids are not administered
G.R
Only a small percentage of morphine crosses the blood-brain barrier ?
because morphine is the least lipophilic of the common opioids. By contrast, the more lipid-soluble opioids, such as fentanyl and methadone, readily
penetrate the CNS.
Morphine is conjugated with glucuronic acid in the liver to two active
metabolites
…..1 is a very potent analgesic and morphine glucuronide metabolites undergo
enterohepatic circulation.,
…..2does not have analgesic activity, but is believed
to cause neuroexcitatory effects
- M6G (morphine-6-glucuronide)
- M3G (morphine-3-glucuronide)
The duration of action of morphine is ……… h when administered systemically.
4 to 5 hours
Which route of administration produces the most reliable response in terms of morphine absorption?
a. Oral
b. Subcutaneous
c. Intravenous
d. b & c
d. b & c
absorption of morphine after oral administration is slow and erratic
……..oral preparations provide more consistent
plasma levels.
Extended-release
Why is morphine not recommended for analgesia during labor?
a. It rapidly enters all body tissues, including the fetus.
b. It causes physical dependence on opioids in newborns.
c. It exhibits withdrawal symptoms if opioids are not administered.
d. a & b
d. a & b
Which of the following opioids readily penetrates the central nervous system (CNS) due to its high lipid solubility?
a. Morphine
b. Fentanyl
c. Methadone
d. b&c
d. b&c
What is the primary fate of morphine in the body after metabolism?
a. Renal excretion of unchanged morphine
b. Conversion to inactive metabolites
c. Conjugation with glucuronic acid in the liver to two active metabolites
c. Conjugation with glucuronic acid in the liver to two active metabolites
Which metabolite of morphine is responsible for causing neuroexcitatory effects?
a. Morphine-6-glucuronide (M6G)
b. Morphine-3-glucuronide (M3G)
c. Unconjugated morphine
d. Morphine-6-phosphate (M6P)
b. Morphine-3-glucuronide (M3G)
What is the approximate duration of action of morphine when administered systemically?
a. 1 to 2 hours
b. 2 to 3 hours
c. 4 to 5 hours
d. 6 to 7 hours
c. 4 to 5 hours
What is the Pharmacologic Effects of morphine on the CENTRAL NERVOUS SYSTEM?
“6”
a. Analgesia:
b. Sedation and euphoria:
c. Depression of cough reflex;
d. Emesis:
e. Respiration depression
f. Miosis
Which receptor activation is associated with euphoria?
a) Mu receptor
b) Kappa receptor
c) delta receptor
a) Mu receptor
Which of the following effects may occur at doses lower than those required for maximum analgesia of morphine ?
a) Sedation
b) Euphoria
c) Dysphoria and Hallucinations
d) b&c
d) b&c
The sedation “also one of the effects of morphine “
is additive with other CNS depressants, but there is little amnesia.
Which receptor activation by morphine is associated with dysphoria and hallucinations?
a) delta receptor
b) Kappa receptor
c) Mu receptor
d) G receptor
b) Kappa receptor
Which opioid directly stimulates the chemoreceptor trigger zone, causing vomiting?
a) Codeine
b) Fentanyl
c) Morphine
d) Oxycodone
c) Morphine
Which opioid is known for its antitussive properties?
a) Heroin
b) both morphine and codeine
c) Morphine
d) Tramadol
b) both morphine and codeine
G.R
morphine should be used
with caution in patients with asthma.
Because it can cause bronchoconstriction,
G.R
Morphine is usually contraindicated in individuals with head trauma or
severe brain injury.
*Because of respiratory depression and carbon dioxide
retention, cerebral vessels dilate and increase cerebrospinal
fluid pressure (increased intracranial Pressure).