Opioid Analgesics Flashcards

Question

Meperidine | route, potency, smooth muscle, use, newborns, duration

Answer 1

synthetic drug route of administration - oral and parenteral 1/10 the potency of morphine weaker effects on smooth muscle than morphine - less constipation and urine retention, although the evidence to support this is weak. has been used for moderate to severe pain has been commonly used in obstetrics - may cause less respiratory depression in the newborn than morphine relatively short acting 1-3 hours; not appropriate for chronic pain because of the buildup of an active metabolite (normeperidine) that can cause seizures. falling into disfavor in many circles.

Answer 2

more potent and more euphoric than morphine; duration of action about 4-6 hours. available for medical use in some countries, but not in the US abuse commonly taken by injection, snorting or smoking

Answer 3

less euphoric and longer duration of action (12- 24 hours) than heroin or morphine (4-6 hours) used as an analgesic and in treating opioid addiction (stigma in use for this) dosing can be tricky and needs to be done carefully, with close monitoring of the patient. - When used acutely as an analgesic, duration of action = 4-6 hours. When used chronically (as in methadone maintenance for the treatment of opioid dependence, or for the management of chronic pain), it has a duration of action of 12-24 hours.

Answer 4

very potent mu agonist (about 100 x more potent than morphine) - given parenterally to supplement surgical anesthesia. A transdermal preparation (Duragesic) is available for the management of chronic pain. Lozenge/lollipop preparations are also available for the treatment of severe “breakthrough” pain in chronic pain patients. -controversy regarding this due to fear of kids finding

Answer 5

Contain a lot of acetaminophen, and can lead to liver toxicity / damage

Answer 6

– agonist effects are dominant - acts as an agonist at κ (kappa) receptors, but only as a partial agonist at µ (mu) receptors; it acts as a µ antagonist at high doses. – less effective than morphine for severe pain – sedation and respiratory depression are less than with morphine – CNS stimulation and hallucinations are more common than with morphine – with chronic use, the potential for physical dependence is less than morphine, but still significant - can precipitate withdrawal syndrome in opioid addicts

Answer 7

– acts as a partial agonist at µ-receptors and possibly κ-receptors. – analgesic effects may be slightly less than that of morphine, its abuse potential is much lower. **– Buprenorphine is the primary agent used for the so-called “office based” treatment of opioid addiction.** – reduces drug craving in heroin addicts and is being used in the treatment of heroin addiction. --Suboxone is a new combination product containing buprenorphine plus nalaxone designed for sublingual use. When taken as directed, the naloxone does not reach a therapeutic blood level and the buprenorphine can produce its effects. However, if the user tries to inject the drug to achieve a high, the naloxone will block the effects of the buprenorphine. – Although it is usually given by injection, it is also effective when administered sublingually, intranasally, or transdermally.

Answer 8

newer drug for use in mild-moderate pain. It supposedly is a weak mu agonist and inhibits the synaptic reuptake of norepinephrine and serotonin, much like the tricyclic antidepressants. It produces good analgesia, with only mild side effects. In general, the side effects resemble those of other opioids (dizziness, sedation, nausea, constipation). The manufacturer has claimed that the drug has a very low abuse and addiction potential. However, there are a significant number of reports indicating that the drug has opioid-like abuse potential.

Answer 9

Tramadol may induce psychic and physical dependence of the morphine-type (µ-opioid) Dependence and abuse, including drug-seeking behavior - not limited to prior hx - higher risk with prior hx Tramadol is associated with craving and tolerance development. Withdrawal symptoms may occur if tramadol is discontinued abruptly. - anxiety, sweating, insomnia, rigors, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection and rarely hallucinations - relieved by reinstitution of opioid therapy and gradual dose reduction

Answer 10

Newer drug that is similar to tramadol, except that it has stronger agonist activity at mu receptors. -It also inhibits reuptake of NE and 5-HT. More effective for pain than tramadol, but also greater abuse potential. Classified as Shedule II drug. Tramadol is Schedule IV. May have some special benefits for“neuropathic pain”.

Answer 11

drug of choice for opioid poisoning, can reverse the respiratory depressant effects of opioids – not effective orally, because of first pass metabolism, usually given parenterally in Ed or intranasaly by first responders. – sometimes included in combination with oral narcotic analgesics (eg. Talwin NX) to prevent abuse (i.e. injection of the drug) – relatively short duration of action (i.e. only about 1-2 hours)…….agonists have longer actions -- patients must stay in hospital for this reason as opioid effects will return when naloxone wears off – can precipitate withdrawal in addicts, which is not pleasant for patient or care givers!!!

Answer 12

orally effective, long acting antagonist (24 hours) used in "immunizing" addicts (ie. preventing the high produced by opioid agonists) risk of hepatotoxicity is a serious drawback its effectiveness in the long-term treatment of opioid dependence is not clear patient compliance is a major problem Keep in mid that an opioid addict must first be detoxified (ie. brought through withdrawal) before naltrexone therapy can be initiated. It has been shown to decrease the craving for alcohol in alcoholics. It is now approved for use in the treatment of alcoholism

Answer 13

Quaternary analog of naloxone approved for the treatment/prevention of opioid-induced constipation. Must be given parenterally, usually SC Only appropriate for serious constipation resulting from use higher doses of opioids for more severe pain. Alvimopan (Enterig) is a similar agent but can be given orally.

Answer 14

New drug approved for opioid-induced constipation. It consists of a naloxone molecule conjugated to short chain polyethylene glycol-like molecule. Taken orally, it has few systemic effects. May be more useful than similar agents for use in out patients

Answer 15

– tolerance - develops to some effects more than others. For example, there can be a high degree of tolerance to the analgesic, euphoric and sedative effects of opioids whereas there is usually little tolerance to opioid-induced miosis or constipation. – withdrawal syndrome

Answer 16

– craving for drug – anxiety, insomnia – dilation of pupils – severe GI hypermotility – hypertension and tachycardia – "goose flesh" – yawning and sweating

Answer 17

– short acting drug (e.g. heroin) - intense symptoms, short duration (2-3 days) – long acting drug (e.g. methadone) - moderate symptoms, long duration (4-7 days) – Note: The acute withdrawal phase is often followed by prolonged syndrome consisting of mild anxiety irritability, sleep disturbances and autonomic excitability that may last for several weeks - months.

Answer 18

– "cold turkey" – weaning patient off the drug – methadone – substitution - wean patient off drug – maintenance - maintain patient on drug – buprenorphine is also being used – naltrexone (Trexan) - long acting opioid antagonist – clonidine (Catapress) - will suppress some withdrawal symptoms; lofexidine (Lucemyra) is a newer alpha 2 agonist for opioid detox.

Answer 19

Healthcare provider must maintain control Define outcomes and develop a therapeutic plan to achieve Monitor patient to insure compliance with the plan and efficacy Periodic drug holidays to monitor level of pain and look for signs of dependence Patient contracts Drug screening

Opioid Analgesics Flashcards

(43 cards)