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Opioid Analgesics

TermDefinition
Morphine Extensive first pass metabolism. 6-glucuronide (metabolite) is more active than morphine and has >half life.
Fentanyl lollipo for pediatricts. IV for acute pain, anesthesia. P450 metabolites INACTIVE.
Sufentanyl Synthetic opiod. Potent fentanyl analogue. 7.5x potency of fentanyl. High affinity for mu opiod receptor. Low affinity for others. RAPID ELIMINATION. Used for painful procedures.
Carfentanil high affinity for mu and high selectivity. One of most potentn known. Strongest commercially available 10000x morphine, 100x fentanyl. NOT FOR HUMANS. Used as an analgesic, anaesthetic etc… for large animals.
Meperidine (Demerol) 1/10th as potent as morphine, equal affect in equianalgesic dosages. Can lead to accumulation of toxic metabolite normeperidine, = cns hyperexcitability, anxiety, tremors.
Morphine 2 Provides analgesia. Diacetic acid ester (diacetylmorphine) is heroin. Morphine used for severe pain with trauma, and myocardial infarction and cancer.
Oxycodone Semi-synthetic. Moderate to severe pain. Roxicodone (acute), Oxycontin (sustained release for chronic pain). Acts at mu and kappa recptors. Percocet = formulated with acetaminophen.
Codeine (3-methylmorphine) naturally occurring. Used for its analgesic, antitussive, antidiarrheal, antihypertensive etc.. etc.. Can suppress premature labor contractions and myocardial infarctions.
Codeine (3-methylmorphine) 2 **CYP2D6 converts codeine into morphine. Which undergoes glucuronidation. Can lead to problems if you have multiple fucnctioning alleles of this enzyme.
Hydrocodone semisynthetic opiod derived from codeine. Used orally as a narcotic analgesic and antitussive. Often with acetaminophen or ibuprofen. 4hr half life. CYP2D6 converts it into hydromorphone, a more potent opiod.
Naloxone mu opioid receptor competitive antagonist. EXTREMELY high affinity for mu in CNS. Rapid blockade often produces RAPID ONSET OF WITHDRAWAL SYMPTOMS.
Petazocine used in combination with Naloxone. Is a kappa receptor agonist, -prevents abuse of drug.
Naltrexone like naloxone but higher bioavailbility, for long-term treatment of addiction.
Buprenorphine PARTIAL AGONIST. Has less abuse liability. Withdrawal in patients who have repeated doses of morphines. Does not produce psychotomimetic effects. Resp depressant reversed by naloxone.
Methadone Mu agnoist used for analgesia and for detoxification or maiteneance in opiod addiction. Methadone absitence has same effects as morphine but slower and less severe over a longer period of time.
NOTE: Naloxone and Naltrexone can be used to counter the effects of opiod overdose. (ex heroin or morphine). Naloxone is specifically used to counteract life threatening depression of CNS and resp system. Binds to mu receptor but does NOT alter its conformation (no activation).
NOTE: opiod receptors on mast cells stimulate histamine release = rash.
Created by: vbukorovic
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