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Oxycodone was first synthesized in Germany in 1916, derived from thebaine.
Answer: True
Explanation: The synthesis of oxycodone from thebaine occurred in Germany in 1916.
The first documented medical use of oxycodone occurred in Germany in 1917.
Answer: True
Explanation: Following its synthesis in 1916, oxycodone saw its first documented medical application in Germany in 1917.
Skophedal, containing oxycodone, was used by the Wehrmacht and was noted for causing less sedation than other opiates at similar doses.
Answer: True
Explanation: Skophedal, a formulation containing oxycodone, was utilized by the Wehrmacht and was recognized for its potent analgesic effects with reportedly less sedation compared to other opiates at equivalent doses.
Oxycodone was first synthesized in which country?
Answer: Germany
Explanation: The initial synthesis of oxycodone took place in Germany.
The drug Skophedal, mentioned in the source, contained oxycodone and was used by which group?
Answer: The Wehrmacht (German Army) as a battlefield analgesic
Explanation: Skophedal, a formulation containing oxycodone, was employed by the Wehrmacht as a battlefield analgesic.
What does the 'Miracle Drug of the 1930s' designation for oxycodone in Europe signify?
Answer: It was perceived as highly effective and well-received during that decade.
Explanation: The designation 'Miracle Drug of the 1930s' in Europe reflects the perception of oxycodone as highly effective and widely accepted during that period.
Oxycodone functions by blocking the mu-opioid receptor (MOR) to prevent pain signals.
Answer: False
Explanation: Oxycodone acts as an agonist, activating the mu-opioid receptor (MOR), rather than blocking it.
Oxycodone and codeine share the exact same chemical structure.
Answer: False
Explanation: Oxycodone and codeine possess distinct chemical structures; oxycodone has specific modifications, such as a hydroxyl group at carbon-14, differentiating it from codeine.
The IUPAC name for oxycodone is a relatively simple chemical descriptor.
Answer: False
Explanation: The IUPAC name for oxycodone, (5R,9R,13S,14S)-4,5α-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one, is a complex and precise chemical descriptor.
What is the primary mechanism of action for oxycodone?
Answer: Activating the mu-opioid receptor (MOR).
Explanation: Oxycodone's primary mechanism of action involves the activation of the mu-opioid receptor (MOR).
Which structural modification distinguishes oxycodone from codeine, as per the source?
Answer: Oxycodone has a hydroxyl group at carbon-14.
Explanation: A key structural distinction is the presence of a hydroxyl group at carbon-14 in oxycodone, which is absent in codeine.
The primary enzyme responsible for the O-demethylation of oxycodone is CYP3A4.
Answer: False
Explanation: The O-demethylation of oxycodone to oxymorphone is primarily mediated by the CYP2D6 enzyme, not CYP3A4.
Noroxycodone and oxymorphone are identified as the main metabolites of oxycodone, both possessing pharmacological activity.
Answer: True
Explanation: Noroxycodone and oxymorphone are indeed the principal metabolites of oxycodone, and both exhibit pharmacological activity.
When taken orally, oxycodone is less potent than morphine.
Answer: False
Explanation: Orally administered oxycodone is approximately 1.5 times more potent than oral morphine, not less potent.
The bioavailability of oral oxycodone typically ranges between 60% and 87%.
Answer: True
Explanation: The oral bioavailability of oxycodone generally falls within the range of 60% to 87%.
Oxycodone and its metabolites cannot be detected in biological fluids like blood or urine.
Answer: False
Explanation: Oxycodone and its metabolites are detectable in biological fluids such as blood and urine, which is utilized in drug monitoring and forensic analysis.
Oxymorphone, an active metabolite of oxycodone, has a lower affinity for the mu-opioid receptor compared to oxycodone.
Answer: False
Explanation: Oxymorphone, an active metabolite of oxycodone, possesses a higher affinity for the mu-opioid receptor than oxycodone itself.
The elimination half-life of immediate-release oxycodone is typically around 4.5 hours.
Answer: False
Explanation: The elimination half-life of immediate-release oxycodone is generally shorter, around 2-3 hours, whereas the controlled-release formulation has a half-life closer to 4.5 hours.
Intranasal oxycodone administration shows significantly lower bioavailability than oral administration.
Answer: False
Explanation: Intranasal administration of oxycodone exhibits a bioavailability of approximately 77%, which is comparable to, not significantly lower than, oral administration.
How does the oral analgesic potency of oxycodone compare to oral morphine?
Answer: Oxycodone is approximately 1.5 times more potent than morphine.
Explanation: When administered orally, oxycodone exhibits approximately 1.5 times the analgesic potency of morphine.
Which liver enzymes are primarily responsible for the metabolism of oxycodone?
Answer: CYP3A4 and CYP2D6
Explanation: Oxycodone metabolism is primarily carried out by the hepatic enzymes CYP3A4 and CYP2D6.
According to the source, what are the two main active metabolites of oxycodone?
Answer: Noroxycodone and Oxymorphone
Explanation: The principal active metabolites of oxycodone are noroxycodone and oxymorphone.
What is the typical bioavailability range for orally administered oxycodone?
Answer: 60% - 87%
Explanation: The bioavailability of oxycodone following oral administration typically ranges between 60% and 87%.
How does the potency of intravenous oxycodone compare to intravenous morphine?
Answer: They are considered equianalgesic (1:1 ratio).
Explanation: Intravenously administered oxycodone and morphine are considered equianalgesic, meaning they possess similar potency at a 1:1 ratio.
What is the approximate bioavailability of intranasally administered oxycodone?
Answer: Approximately 77%
Explanation: Intranasal administration of oxycodone yields an approximate bioavailability of 77%.
Oxycodone is primarily indicated for the treatment of mild pain and inflammation.
Answer: False
Explanation: The primary indication for oxycodone is for moderate to severe pain, not mild pain or inflammation.
OxyContin is a brand name for an immediate-release formulation of oxycodone.
Answer: False
Explanation: OxyContin is specifically an extended-release formulation of oxycodone, designed for prolonged pain management.
Oxycodone is sometimes combined with naloxone to improve its pain-relieving properties.
Answer: False
Explanation: When combined with oxycodone, naloxone is typically included to deter abuse and counteract constipation, not to enhance pain relief.
Immediate-release oxycodone formulations are designed to provide pain relief for 10-12 hours.
Answer: False
Explanation: Immediate-release oxycodone formulations are designed for shorter durations, typically providing relief for 3-6 hours, not 10-12 hours.
According to the source, oxycodone use in early pregnancy is considered definitively unsafe.
Answer: False
Explanation: The source indicates that oxycodone use in early pregnancy appears relatively safe, though consultation with a healthcare provider is always advised.
What is the primary medical purpose of oxycodone as stated in the source?
Answer: To manage moderate to severe acute or chronic pain when other treatments are insufficient.
Explanation: The source material explicitly states that oxycodone is primarily indicated for the management of moderate to severe acute or chronic pain when alternative treatment modalities are inadequate.
Which of the following is identified as an extended-release formulation of oxycodone?
Answer: OxyContin
Explanation: OxyContin is identified as an extended-release formulation of oxycodone, designed for prolonged pain management.
What is the typical duration of pain relief provided by immediate-release oxycodone?
Answer: 3 to 6 hours
Explanation: Immediate-release oxycodone formulations typically provide pain relief for a duration of 3 to 6 hours.
When oxycodone is combined with naloxone in certain formulations, what is the purpose of the naloxone?
Answer: To deter abuse and counteract constipation.
Explanation: In combination formulations, naloxone serves to deter abuse and mitigate opioid-induced constipation.
The 'Contradicts other' notice in the pharmacology section indicates a potential issue with:
Answer: Discrepancies in equianalgesic data between articles.
Explanation: The 'Contradicts other' notation highlights potential discrepancies in equianalgesic data presented across different sections or related articles.
In which region is oxycodone mentioned as being administered via injection?
Answer: United Kingdom
Explanation: The source mentions that oxycodone can be administered via injection in the United Kingdom.
Oxycodone possesses a low potential for addiction and abuse, rendering it a relatively safe medication.
Answer: False
Explanation: Oxycodone has a high potential for addiction and abuse, classifying it as a controlled substance with significant risks.
Common side effects associated with oxycodone use include euphoria, nausea, and drowsiness.
Answer: True
Explanation: Euphoria, nausea, and drowsiness are indeed among the frequently observed side effects of oxycodone administration.
Abruptly discontinuing oxycodone after developing physical dependence poses a high risk of severe withdrawal symptoms.
Answer: True
Explanation: Sudden cessation of oxycodone in physically dependent individuals can precipitate severe and distressing withdrawal symptoms.
Chronic oxycodone use can lead to hypogonadism, characterized by reduced sex hormone levels.
Answer: True
Explanation: Chronic administration of oxycodone is associated with hypogonadism, a condition marked by diminished levels of sex hormones.
Symptoms of an oxycodone overdose include rapid breathing and increased heart rate.
Answer: False
Explanation: Symptoms of an oxycodone overdose typically involve slowed or shallow breathing and a decreased heart rate, not rapid breathing and increased heart rate.
The primary danger of chronic constipation from oxycodone is mild discomfort.
Answer: False
Explanation: The primary danger associated with chronic constipation induced by oxycodone is not mild discomfort but the potential for severe complications, including bowel perforations.
Which of the following is listed as a common side effect of oxycodone?
Answer: Itching
Explanation: Itching (pruritus) is frequently listed as a common side effect associated with oxycodone use.
What is a significant risk if a patient physically dependent on oxycodone stops taking it abruptly?
Answer: Severe withdrawal symptoms.
Explanation: Abrupt cessation of oxycodone in physically dependent individuals carries a significant risk of precipitating severe withdrawal symptoms.
Chronic use of oxycodone can potentially lead to which hormonal imbalance?
Answer: Hypogonadism
Explanation: Chronic oxycodone use is associated with the potential development of hypogonadism, characterized by reduced sex hormone levels.
Which of the following is NOT a symptom of oxycodone overdose according to the source?
Answer: Rapid, deep breathing
Explanation: Rapid, deep breathing is not characteristic of an oxycodone overdose; symptoms typically include shallow breathing, slowed heart rate, and constricted pupils.
Which of the following is categorized as a less common but potentially serious side effect of oxycodone?
Answer: Delirium
Explanation: Delirium is considered a less common but potentially serious adverse effect associated with oxycodone use.
What is the primary danger associated with chronic constipation induced by oxycodone?
Answer: It can cause severe complications like bowel perforations.
Explanation: Chronic constipation resulting from oxycodone use poses a significant danger, with the potential for severe complications such as bowel perforations.
How does oxycodone's activation of the mu-opioid receptor (MOR) contribute to addiction?
Answer: By activating MOR in the mesolimbic reward pathway.
Explanation: Activation of the mu-opioid receptor (MOR) within the mesolimbic reward pathway by oxycodone is implicated in its contribution to addiction.
The development of tolerance to oxycodone's effects is described as a complex process involving:
Answer: Receptor-level, cellular-level, and system-level neural adaptations.
Explanation: Tolerance to oxycodone develops through a complex interplay of adaptations at receptor, cellular, and system-level neural networks.
In the United States, oxycodone is classified as a Schedule II controlled substance.
Answer: True
Explanation: Oxycodone is indeed classified as a Schedule II controlled substance within the United States regulatory framework.
Purdue Pharma's development of OxyContin significantly contributed to the opioid epidemic.
Answer: True
Explanation: The marketing and widespread use of OxyContin by Purdue Pharma are widely recognized as major contributors to the opioid epidemic in the United States.
The 1961 Single Convention on Narcotic Drugs classified oxycodone under Schedule I, imposing strict international controls.
Answer: True
Explanation: The 1961 Single Convention on Narcotic Drugs classified oxycodone under Schedule I, establishing stringent international controls on its use.
Purdue Pharma's reformulation of OxyContin aimed to make the pills more resistant to crushing and dissolving to reduce abuse.
Answer: True
Explanation: Purdue Pharma reformulated OxyContin with the objective of increasing resistance to crushing and dissolution, thereby aiming to mitigate abuse potential.
The FDA's 2013 labeling update for long-acting opioids removed the indication for moderate pain.
Answer: True
Explanation: The FDA's 2013 labeling update for long-acting opioids did indeed remove the indication for moderate pain, restricting its use to severe pain.
What is the legal classification of oxycodone in the United States?
Answer: Schedule II
Explanation: In the United States, oxycodone is classified as a Schedule II controlled substance.
Purdue Pharma is primarily associated with the development and marketing of which oxycodone formulation?
Answer: OxyContin
Explanation: Purdue Pharma is principally recognized for the development and marketing of OxyContin, an extended-release formulation of oxycodone.
The 1961 Single Convention on Narcotic Drugs classified oxycodone under which schedule?
Answer: Schedule I
Explanation: The 1961 Single Convention on Narcotic Drugs placed oxycodone under Schedule I, signifying strict international controls.
According to the source, since 2012, which drugs have become more prominent causes of drug-related deaths in the US compared to oxycodone?
Answer: Heroin and Fentanyl
Explanation: Since 2012, heroin and fentanyl have emerged as more prominent causes of drug-related deaths in the US relative to oxycodone.
What was the main goal of the FDA's 2013 labeling update for long-acting opioids?
Answer: To restrict use to severe, long-term pain management.
Explanation: The primary objective of the FDA's 2013 labeling update for long-acting opioids was to restrict their indication to severe, long-term pain management.
What does the source indicate about the non-medical use of oxycodone among injecting drug users in Australia by 2015?
Answer: A significant majority (91%) reported using it, with notable recent injection.
Explanation: By 2015, the source indicates that a substantial majority (91%) of injecting drug users in Australia reported oxycodone use, with a notable prevalence of recent injection.