Opioids Flashcards
Seizures may occur with overdoses of which of the following opioids: A Meperidine B Methadone C Tramadol D Oxycodone E Both Meperidine and Tramadol
Normeperidine, a metabolite of meperidine, and Tramadol both may cause seizures in overdose or withdrawal. They are both contraindicated with MAOs and may lead to serotonin syndrome. (WF): syndrome.
Which of the following opioids does NOT have an active metabolite: A Buprenorphine B Methadone C Morphine D Heroin E Oxycodone
Buprenorphine has norbuprenorphine, morphine has M3G and M6G, Heroin has 6MAM, Oxycodone has small amounts of oxymorphone. Methadone has no active metabolites
A patient on 120mg of methadone complains of lightheadedness and a syncopal episode. His EKG reveals a QTc of 550msec. All the following are FALSE except: A Buprenorphine prolongs the QTc interval at usual clinical doses B QTc intervals above 500msec predispose to Torsades de Pointe C Potassium levels should be checked because Hyperkalemia prolongs the QTc interval. D Medications which induce CYP3A4 and 2D6 will increase the QTC interval in a methadone maintained patient. E Routine EKG screening of all methadone maintained patients has been shown to decrease morbidity and mortality.
QTc intervals above 500msec predispose to Torsades de Pointe. Buprenorphine does not significantly increase the QTc interval. Hypokalemia prolongs the QTc interval. Inducers of the 3A4 and 2D6 will decrease methadone levels, and thereby decrease not increase the QTC interval. Routine EKG screening of all methadone maintained patients has not been validated. It is a topic of controversy, but evidence of decrease morbidity and mortality is not available.
Which of the following statement concerning heroin is true? A In 1924, the US Congress banned heroin’s sale, importation or manufacture. (Correct Answer) B When injected, heroin (diacetylmorphine) rapidly passes directly through the blood brain barrier then directly binds to the mu opioid receptors resulting in the drug’s euphoric effects. (Your Answer) C Metabolites of heroin include 6-monoacetylmorphine (6-MAM), morphine, morphine-3-glucuronide and codeine. D “Golden Crescent” is a term related to heroin-induced euphoria. E Symptoms of heroin withdrawal may include sweating, malaise, anxiety, depression and priapism and usually begin 36 to 54 hours after discontinuing the drug.
In 1924, the US Congress banned heroin’s sale, importation and manufacture. In 1925, the Health Committee of the League of Nations banned diacetylmorphine, although it took more than three years for this to be implemented. Heroin is a prodrug; therefore, after crossing the blood-brain barrier, it is then deacetylated variously into the inactive 3-monoacetylmorphine then rapidly into the active 6-monoacetylmorphine (6-MAM) and then into morphine which bind to the mu opioid receptors resulting in the drug’s euphoric effects. Codeine is not a metabolite of heroin. Golden Crescent is a term related to heroin trafficking. Heroin’s metabolites are full agonists to the opiate receptors and are short-acting. Withdrawal syndromes may begin 6 to 24 hours after discontinuing the drug.
A 44-year-old man who has a past medical history of alcohol abuse develops chronic abdominal pain and starts taking his wife’s Percocet. He reads about “Kratom” on the internet and subsequently buys the “full spectrum tincture” of Kratom from the vendor and begins taking it as a substitution for the Percocet. He eventually increases the dose of Kratom to 6 “dropper squeezer” every 4 hours on a continuous basis and is unable to stop. He presents to your office with typical opiate-type withdrawal symptoms and the additional history that he has gained 60 pound s over the past year, has become lethargic, and he is edematous. The most likely explanation for this man’s clinical presentation is: A Congestive heart failure. B Chronic liver disease. C Primary hypothyroidism. D Chronic renal insufficiency. E Severe anemia.
Kratom is known as mitragyna speciosa korth and is a tropical tree indigenous to Thailand and other areas of South East Asia. Mitragynine, the major alkaloid identified from Kratom has been reported as a partial opioid agonist producing effects similar to morphine. Some indole alkaloids such as reserpine may primarily affect thyroid gland and cause primary hypothyroidism and Kratom is an indole alkaloid in high doses.
How many different types of opiate receptors have been identified in the human nervous system? A 2 B 3 C 4 D 5 E 6
Most of the clinically active opioids are active at the mu receptor. The other 3 receptors are kappa, delta, and ORLF, mediating both the analgesic and rewarding effects of opioid compounds as well as their effects on many systems in the body such as the hypothalamic-pituitary-adrenal (HPA) axis, immune, gastrointestinal (GI) and pulmonary function.
Which of the following statements about naltrexone is true? A It is only available in parenteral form. B It has low receptor affinity. C It is poorly absorbed from the gut. D It has a short duration of action. E It prevents opiate agonists from binding to the receptor.
Naltrexone is a relatively pure antagonist in that it produces little or no agonist activity at usual doses and prevents opiate agonists from binding to the receptor and producing opiate effects. Naltrexone has high receptor affinity, and thus it can block virtually all the effects of the usual doses of opioids and opiates such as heroin
Methadone was developed in 1937 by scientists working for: A Adolph Hitler. B Marie Nyswander. C I.G. Farbenkonzern. D Professor Vincent Dole. E Eli Lilly and Company.
Methadone was developed when scientists at the Farbwerke Hoechst in 1937 under the direction of I.G. Farbenkonzern were looking for a synthetic opioid that could be created with readily available precursors to solve Germany’s opium shortage problem. Methadone was first manufactured in the USA by Eli Lilly and Company who first obtained FDA approval on August 14, 1947. Marie Nyswander and Professor Vincent Dole studied methadone substitution therapy successfully in the 1960’s and Adolph Hitler had no documented role in the development of methadone
A legislative act provided that physicians could prescribe narcotics to their patients “in the course of professional practice only.” A 1906 Pure Food and Drug Act. B 1914 Harrison Narcotic Tax Act. C 1961 Convention on Narcotics. D 1970 Controlled Substance Act. E 2000 Drug Addiction
The Harrison Narcotic Tax Act provided that physicians could prescribe narcotics to their patients in the course of their usual practice, but they could not use narcotics to treat opiate addiction because addiction was not recognized as a disease in 1914. The Pure Food and Drug Act did not address opiates specifically. The 1961 Convention on Narcotics addressed marijuana. The 2000 Drug Addiction Treatment Act provided that qualified physicians could utilize Schedule III, IV, and V drugs to treat opiate addiction and changed buprenorphine to Schedule III.
A 45-year-old female methadone clinic patient with a history of prior seizures, recent tuberculosis exposure and mild edema is brought in by her family in a lethargic state for evaluation. The patient had been stable on 80 mg per day of methadone for four months. The patient’s sister reports that she visited their family doctor recently and something was prescribed. Which of the following medications prescribed by the patient’s family doctor could be responsible for the patient’s lethargy? A Dilantin B Spironolactone C Ciprofloxacin D Acamprosate E Rifampin
Ciprofloxacin is a cytochrome P450 inhibitor. Administration will increase methadone levels. Dilantin, spironolactone and rifampin are cytochrome P450 inducers, and methadone levels will decrease. Thus, opiate withdrawal symptoms would be more likely. Acamprosate would likely have no effect on methadone metabolism.
What is the average dose necessary to achieve an optimal treatment outcome for a patient in a methadone maintenance program? A 30 mg/day. B 40 mg/day. C 50 mg/day. D 80 mg/day. E 140 mg/day.
Multiple studies have confirmed that methadone doses in the range of 60-120 mg/day lead to superior outcomes as compared to doses below this range. No evidence suggests that doses above 120 mg/day are consistently more beneficial with regard to outcome measures.
All of the following are true regarding opioid agonist maintenance therapy except A The effectiveness of methadone and other opioid agonist treatments for reducing morbidity, mortality, and social dysfunction has been validated by several meta-analytic studies. B Only about one-fifth of heroin-dependent individuals are enrolled in agonist maintenance treatment. C When methadone maintenance treatment has been made easily available at a low cost, and publicized, 90% or more heroin addicts have sought treatment. D Daily dosing of methadone above 100 mg per day should be avoided because it is dangerous and rarely helpful. E Patients who are provided minimal drug counseling have been shown to be at substantially increased risk of continued illicit drug use, despite adequate methadone dosing.
Although effective doses of methadone generally are between 60 and 100 mg daily, full attenuation of heroin effects may only be seen at higher doses, and should be optimized based on individual patient response
Methadone may be used effectively to assist in withdrawing a patient from opioids that are more addicting. However, this is only advised for certain opioids. Addiction to which of the following is not appropriately managed by using methadone substitution and eventual taper? A Pentazocine B Morphine C Hydromorphone D Oxycodone E Heroin
In general, a more addictive drug should not be used to detoxify a patient from a less addictive one. Although methadone can be used to withdraw patients from narcotics such as heroin, morphine, hydromorphone, oxycodone, or meperidine, it should be avoided for drugs such as propoxyphene or pentazocine, for which the withdrawal should be handled by gradually decreasing the dosage of the agent itself or by an agent such as clonidine.
There are a number of potential medication interactions with methadone. Which of the following medications may reduce plasma methadone levels? A Risperidone B Fluoxetine C Sertraline D Cimetidine E Fluvoxamine
Risperidone may reduce plasma methadone levels, while fluoxetine, sertraline, cimetidine, and fluvoxamine may increase them.
Nalmefene differs from naloxone primarily in which of the following ways? A Nalmefene is available in parenteral form. B Nalmefene is a pure agonist. C Nalmefene is available in an oral form. D Nalmefene has a much longer duration of action. E Nalmefene activates opiate receptors.
Nalmefene has a much longer duration of action than naloxone. Both nalmefene and naloxone are available in parenteral and oral form. They are antagonists and occupy opiate receptors but do not activate them.
