Drugs

Does naloxone reverse buprenorphine? Buprenorphine has a much higher binding affinity for the mu-opioid receptor compared with naloxone. Buprenorphine has a longer elimination half-life than naloxone. The half-life of buprenorphine is between 24 and 42 hours, depending on the patient. Comparatively, the half-life of naloxone is only 2 to 12 hours. Therefore, buprenorphine binds to […]

Is tapentadol a glorified tramadol? Tapentadol is a mu-opioid agonist and also blocks reuptake of norepinephrine, the latter of which is particularly useful for the treatment of neuropathic pain. Additionally, tramadol blocks reuptake of serotonin; hence it is a serotonin norepinephrine reuptake inhibitor (SNRI) of sorts. Tramadol is metabolized by CYP 2D6 via O-demethylation to

Are any opioids contraindicated in opioid naive patents? Fentanyl is absolutely contraindicated in opioid naïve patients in the outpatient setting. It can be used in a controlled environment for patients that present for ambulatory procedures, where intravenous (IV) access and intubation is available. Fentanyl is 100 times more potent than morphine and even the lowest

Are opioids useful in the treatment of neuropathic pain ? There are four unique opioids that are presumed to have enhanced efficacy for neuropathic pain syndromes. They include methadone, levorphanol, tramadol, and tapentadol. Each medication exhibits opioid agonist activity; however, each also inhibits the reuptake of norepinephrine in a similar fashion to certain antidepressants that

Are there any extended release opioids that can be crushed without causing harm? Until recently, there were no extended release opioid products that were safe to crush. In fact, there is a black box warning to caution against crushing or splitting all ER or long acting (LA) dosage units, with the exception of one product

How does medicinal chemistry or structure activity relationship impact opioid tolerability? Medicinal chemistry can absolutely be used to a clinician’s advantage when predicting how a patient may respond to a specific opioid. There are five chemical classes of opioids: phenanthrenes, benzomorphans, phenylpiperidines, diphenylheptanes, and phenypropylamines. Semisynthetic dehydroxylated phenanthrenes such as hydrocodone, hydormorphone, levorphanol, oxycodone, buprenorphine,

Are extended release opioids always more dangerous than immediate release opioids? No. In fact, if used properly, extended release opioids may be a safer option of treatment over immediate release opioids but only if taken as intended. Use of certain extended release (ER) opioid preparations may actually result in less total daily opioid dose than use of