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179 Cards in this Set

  • Front
  • Back
Where does opium come from?
it is an extract of the juice on the poppy Papaver somniferum.
What two things does opium resin contain?
two groups of alkaloids: phenanthrenes and isoquinolones.
What do phenanthrenes contain percentagewise?
morphine 10%, codeine .5%, thebaine .2%.
What do Isoquinolones contained percentagewise?
noscapine 6%, papaverine 1%.
Where did opium get its name?
from the ancient Greeks - opion, or poppy juice.
What did the aging creeks use opium for who?
medical purposes.
What is laudenum?
a liquid version of opium. It is dissolved in wine.
When and where was tincture of opium invented?
Britain, 1680. It was referred to as tincture of laudenum.
What was the view on opium, and 17th-century Europe?
" gods own medicine." God created disease, so now he has given us the cure.
What was the Greeks interpretation of opium?
"morphose" God of sleep.
When was the hypodermic needle invented?
1853.
When did opium addiction start?
in 1853, when people started injecting morphine.
When was heroine synthesized?
in the 1890s.
When were opiate receptors and endogenous peptides discovered?
in the 1970s.

Also, There are receptors for other drugs that we have not discovered yet (example: cocaine.).
What is the definition of a opiate?
a drug delivered from opium poppy.
What is the definition of an opioid?
includes opiates,opiopeptines, synthetic opiates, semisynthetic opiates.
What are the endogenous opioid peptide called?
opiopeptine. It is produced in the body naturally.
What are the fourth endogenous opioids we need to remember?
dynorphines

enkephalines

endorphins

endomorphins

D, then 3 E's
Describe enkephalines?
they consist of pentapeptides (five and amino acids.).
Describe dynorphines?
they are a 17 amino acid peptide.
What 2 types of dynorphines are there?
dynorphine A and dynorphine B.
Describe endorphin:
they are 31 amino acid peptides.
Describe endomorphines:
they are 4 amino acid peptides
how big are endogenous opioids?
they are small. They are low molecular weight substances. They cross the blood brain barrier.
Which is more potent, pharmacological opioids or endogenous opioids?
the endogenous opioids that the brain produces are far more potent.
What was anesthesia like in the 1920s?
a large concentration was given. There were lots of complications.
What was anesthesia like after the revolution in anesthesia?
the concentration of general anesthesia was decreased. Multiple drugs were used in combination.
what six types of drugs are included in the anesthesia balance?
opioids, barbiturates, benzodiazepines, neuromuscular relaxants, nitrous oxide, oxygen.
What part of the brain regulates the autonomic nervous system?
the hypothalamus.
In what 5 parts of the brain are opioid receptors found?
limbic system, medial and lateral thalmus, hypothalamus, medulla oblongata, spinal cord.
What part of the brain deals with emotion?
limbic system.
What part of the brain is the relay station?
thalamus.
What part of the brain is the headquarters of the autonomic nervous system?
hypothalamus.
What part of the brain controls respiration, digestion, and respiratory depression with morphine overdose?
medulla oblongata.
How many opioid receptor subtypes are there?
four
what form of signal transduction to all 4 opioid receptors use?
G. protein.
How is phospholipase C activated in opioid receptors?
through inhibition of adenyline cyclase
what happens to cAMP in opioid receptors?
it's gets inhibited in some.
What happens with channels in opioid receptors?
potassium channel gets opened. Membrane is hyper polarized. Calcium channel gets closed. neurotransmitter release is inhibited
overall, what do opioid receptors do to synaptic activity?
they inhibit it. This is the major affect.
What is the main effect on the cell membrane by opioid receptors?
inhibition.
Why does our body have opioid receptors?
because we have and endogenous opioids.
Which opioid receptor is responsible for the majority of analgesic effects of opioids?
Mu.
Which opioid receptor is responsible for supraspinal analgesia?
Mu.
Which opioid receptor is responsible for spinal analgesia?
kappa
which opioid receptor is responsible for hallucinations?
Sigma.
Which opioid receptor is important in the periphery?
delta
which opioid receptor is responsible for respiratory depression?
Mu.
Which opioid receptor is responsible for euphoria (sense of well-being)?
Mu.
Which opioid receptor is responsible for physical dependence?
Mu.
Which opioid receptor is responsible for analgesia?
Mu.
Which opioid receptor is responsible for physical dependence?
Mu.
Which opioid receptor is responsible for miosis?
kappa.
Which opioid receptor is responsible for sedation?
kappa.
What are the symbols for each opioid receptor, Mu, kappa, Sigma, Delta?
see picture one
which drug is the gold standard for analgesia?
morphine. It is a natural substance.
What is the major general effect of opioid receptors?
inhibitory effect.
List the morphine like agonists:
morphine sulfate, hydromorphone, oxymorphone, heroine.
List the 4 codeine like agonists:
codeine, tramadol, hydrocodone, oxycodone
lists the synthetic opioid agonists:
meperidine, Fentanyl, methadone, levorphanol.
List the 3 opioid agonists/antagonists:
pentazocine, butorphanol, nalbuphine.
Lists the opioid antagonists:
Narcan, naltrexone.
What is the chemical name for morphine?
7,8 didehydro-4,5-epoxy-17-methylmorphine-3,6-diol
what is the chemical formula for morphine?
C17 H19 NO3
what is the molecular weight of morphine?
285. It is low molecular weight.
What are the 8 central nervous system effects of morphine?
dose-related analgesia, sedation and euphoria, stimulation of chemoreceptor trigger zone (CTZ), nausea and vomiting, people constriction (miosis), small permeability of blood brain barrier, alteration of hypothalamic set point (mild hypothermia), convulsions with high doses.
is stimulation of the chemoreceptor trigger zone a G.I. effect of morphine?
no. It is a central nervous system affect.
In regard to respiratory/digestive effects, what's general effect does morphine usually have?
usually simply depression.
What are some respiratory/digestive effects of morphine?
respiratory depression (medulla), chest wall rigidity, bronchoconstriction, reduced peristalsis and stomach motility, decreased biliary/pancreatic secretion, constriction of sphincter of oddi
what's type of morphine effect is bronchoconstriction?
autonomic effect.
What's type of morphine effect is reduced peristalsis and stomach motility?
autonomic effect.
What are some urogenital effects of morphine?
urinary bladder contraction (causing urgency), relaxation of uterine tone (prolonging labor), crossing placental barrier.
What part of the brain controls uterine tone?
the hypothalamus. It controls uterine contraction
what's does morphine due to the skin?
allergic skin rashes and dilation of cutaneous vessels.
How is morphine absorbed from a G.I. system?
very well.
Describe percentage of protein binding with morphine:
30% protein bound. 70% free. Pretty low protein binding.
Where is morphine metabolized?
in the liver. It undergoes significant first pass metabolism.
What substance is morphine metabolized to in the body?
morphine 6-glucuronide, which is more potent as an analgesic.
How is morphine excreted from the body?
in the urine
What 4 major effects will a person feel when taking morphine?
euphoria (sense of well-being),

reduced anxiety,

mental clouding,

orgasm-like rush
in a patient with chronic pain, what will they feel with morphine?
analgesia with very little euphoria.
What will a patient with sharp pain feel with morphine?
decrease in sensation, with very little euphoria.
Generally, do pain patients experience euphoria on morphine?
no.
What are 5. clinical uses for morphine?
analgesia,

pulmonary edema,

severe diarrhea,

cough suppression,

As part of the anesthesia balance
at what speed does tolerance developed with morphine use?
very fast. There is quick down-regulation of receptors
how soon after last dose does withdrawal from morphine start?
eight to 12 hours.
How long does morphine withdrawal continued for?
10 days.
What are symptoms of morphine withdrawal?

4 groups: resp, GI, CNS, CV
resp: lacrimation, violent coughing and sneezing,

GI: anorexia, N/V/D,

CNS: insomnia, mydriasis cold turkey, muscle cramps/spasms, depression

CV: tachycardia/hypertension,
How, chemically, is codeine obtained?
it is obtained from opium/methylation of morphine. It is a 3-methyl ether of morphine, obtained from opium.
what is the analgesic potency of codeine compared to morphine?
potency 1/12 of morphine.
What does codine equal in aspirin?
30 mg of codeine equals 600 mg of aspirin
codeine versus morphine, what's does codeine offer less of?
less sedation, less respiratory depression, fewer G.I. side effects (constipation), less addiction
what is codeine used for?
as an oral analgesic for mild pain
what is the potency of hydrocodone/oxycodone compared to morphine?
almost the same
Is heroin man-made or synthetic?
it is semisynthetic.
Why was the heroin invented?
to wean people off of morphine after the needle was invented.
What alteration is made to the molecule of morphine to get heroin?
morphine is diacelted.
What is heroin converted to in the body?
morphine.
What is the onset/duration of heroin compared to morphine?
rapid onset, short duration.
What's does a 3 mg of heroin equal in morphine?
10 mg morphine.
How does heroine travel in the blood brain barrier compared to morphine?
its crosses blood brain barrier more rapidly than morphine. This accounts for the stronger rush, effect.
What was the use for heroine in the United Kingdom?
as a cough suppressant.
What is heroine used for clinically in the United States today?
there is no clinical use for heroine in the United States today.
How many times more potent is hydromorphone than morphine?
10 times.
How does hydromorphone depress respiration compared to morphine?
it is a stronger respiratory depressant
which causes more nausea: hydromorphone or morphine?
morphine has more nausea.
Which has more constipation: hydromorphone or morphine?
morphine has more constipation
list the three synthetic opioids, we need to know:
methadone, Demerol, fentanyl
what is the chemical formula for methadone?
C21H27NO
important: what is the molecular weight of methadone?
309. It is a low molecular weight substance.
Where and when was methadone synthesized?
Germany in 1937. This was due to embargoes that prevented Germany from obtaining opioids
when was methadone introduced to the United States?
1947.
Pharmacologically, how does methadone compare to morphine?
it is pharmacologically similar to morphine.
What is another name for methadone?
dolophine.
What routes can methadone be given?
oral, IM, SC.
Which is more effective orally: morphine or methadone?
methadone.
What is a concern when taking methadone for a long time?
gradual accumulation in the tissues with the danger of cumulative toxicity.
How is methadone affected with the liver metabolism?
there is extensive by a transformation in the liver.
Can a person develop tolerance to methadone?
yes.
Can a person develop physical dependence with methadone?
yes.
How are the physical abstinence symptoms of methadone compared to morphine?
physical abstinence syndrome is less pronounced than for morphine. Used to treat morphine withdrawal.
What is a common methadone regiment used for morphine addicts?
methadone and morphine given together. There is no euphoria with this combination.
What is the chemical formula for meperidine?
C15H21NO2
what is the molecular weight of meperidine?
247.
What is the analgesic potency of meperidine compared to morphine?
meperidine is 1/8 the analgesic potency of morphine.
What effect does meperidine have on respiratory drive?
it causes respiratory depression.
Does meperidine cross the placental barrier?
yes.
Does meperidine cause euphoria and addiction?
yes.
What effect does meperidine have on the airways?
smooth muscle spasm and bronchospasm. This is an autonomic effect.
What is the autonomic side effect of meperidine?
atropine like activity. Dry mouth, blurring of vision. All anticholinergics effects
what local side effects does meperidine have?
irritation with subcutaneous or intramuscular injection.
How does tolerance with meperidine develop, compared to morphine?
slowly.
Would you give meperidine or morphine during labor?
meperidine, because it has a shorter duration of action
what will happen if you give meperidine with an MAO inhibitor?
hyperthermia, convulsions.
Where does metabolism of meperidine take place?
in the liver.
What is meperidine metabolized to in the liver?
normeperidine
what effects can the metabolite normeperidine have on a person?
hallucinogenic/convulsant defects
what can large doses of meperidine do to the central nervous system?
cause CNS excitation.
What are some other names for fentanyl?
Duragesic, sublimaze,actiq.
What is the analgesic potency of the fentanyl, compared to morphine?
fentanyl is 80 times more potent than morphine.
What effect does fentanyl have on respiratory drive?
significant respiratory depression.
What effect does fentanyl have on blood pressure?
there is better hemodynamic stability. This is because there is less histamine Effect.
What are the two principal uses for fentanyl?
anesthesia and postoperative analgesia.
Describe the onset and duration of action of fentanyl?
rapid onset, short duration of action.
What muscular symptom can you see with fentanyl? When would you see this?
muscular rigidity. You would see this in high doses.
What is naloxone a derivative of?
it is an oxymorphone derivative.
What is naloxone's claim to fame?
it was the first pure opioid antagonist.
What does naloxone block opioid receptors from?
endogenous opioids and morphine like agents.
Which opioid receptors does naloxone block?
Mu, Kappa, Sigma.
What will happen if you give naloxone to somebody who has not taken in opioid?
nothing.
What effect does naloxone have on respiratory depression and cardiac symptoms associated with opioids?
it reverses respiratory depression, and cardiovascular effects.
Is there tolerance with naloxone?
no.
What is the withdrawal concern with naloxone?
naloxone can elicit withdrawal syndrome.
Given intravenously, how long does it take for naloxone to have its effect?
almost immediately.
How long does naloxone effect last for?
two to four hours. Must know that this is shorter than that of morphine like agents. Naloxone is rapidly metabolized.
How is naltrexone given?
orally.
What is another name for naltrexone?
Revia.
What is the potency of naltrexone compared to naloxone?
2/1 of naloxone.
What is the duration of action of naltrexone compared to naloxone?
3/1 of naloxone.
Name four side effects of naltrexone:
anxiety, cramps, nausea, joint pain.
Where is naltrexone metabolized?
in the liver.
In what patients is naltrexone contraindicated?
acute hepatitis or hepatic failure.
Name the drug that is enkephalinase inhibitor:
thiorphan
how does thiorphan work?
it inhibits degradation of endogenous opioids.
What effect does thoirphan have in the body?
analgesia and morphine like effects.
Does thiorphan cause dependence?
no.
Name the drug that is a neuropeptide:
somatostatin.
What effect does somatostatin promote?
analgesia.
How do adenosine, and adenosine kinase inhibitors work as pain medicines?
they increase in inhibitory effects of adenosine upon nervous system.
When was the currently accepted formula for morphine invented?
1925.
When was morphine first synthesized?
1952.
What is morphine hydrochloride?
hot aqueous morphine suspension combined with HCl.
What is morphine sulfate?
hot aqueous morphine suspension combined with sulfuric acid.
How do we get hydromorphone?
morphine hydrogenated/dehydrogenated, low pH, plus platinum/Palladium.
How do we get codine?
methylation of the phenolic hydroxyl group of morphine.
What is the codeine phosphate made up of?
codeine plus phosphoric acid
What happens with codeine phosphate in alcohol?
precipitation.
What is codeine sulfate made up of?
coding plus with sulfuric acid.
What is hydrocodone compared to codine?
it is a catalytic rearrangement of codine