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Summarized By: Shahdad Azmoon, MD Date of Publication: March 30th, 2005
Opium is the crude substance derived from the opium poppy used as early as 4000 BC opioid = morphine-like Opiate = subclass of opioids extracted from opium (eg. Morphine, codeine) Endorphin = another subclass of opioids, endogenous (enkephalins, dynorphins, beta-endorphins) Analgesic, CNS depressant effects, euphorics Heroin is a derivative of morphine and is the most commonly abused opioid. Heroin abuse is on the rise in the United States. Health care professionals with access to opioids may personally abuse them, especially meperidine and injectable fentanyl. Heroin-related visits to an emergency department has increased Health care costs of opioid dependence have been estimated to be $1.2 billion yearly Opium extracted from poppies is more commonly abused outside the United States Opioid dependence or addiction is defined as continued use of opioids despite significant opioid-induced problems (cognitive, behavioral, physiological) Repeated use results in tolerance requiring escalating doses to achieve the same effect complicated by withdrawal 1998 National Household Survey 2.4 million people in US used heroin at some time 130,000 reported use in the last month 81,000 new heroin users in 1997 and 87 percent were under age 26 Heroin has a half-life of 30 minutes and has a duration of action of 4-5 hours Heroin is more lipid soluble than other opioids, allowing it to rapidly cross the blood-brain barrier (within 15 to 20 seconds) and to reach high brain levels. Routes of administration: intranasal ("snorting" or "sniffing") subcutaneous ("skin-popping") IV ("shooting up" or "mainlining"); most overdoses, infections Tolerance and physical dependence occur after one to two weeks of daily use Tolerance to meiosis, constipation, and respiratory depression more slowly
Consequences of abuse Heroin addiction is associated with increased mortality Study showed mortality rate of 115 untreated heroin addicts 63 times higher than nonaddicted same age same sex distribution mortality also higher than maintenance program group
street drugs diluted ("cut") by dealers with other white powders
Acute Opioid Intoxication Most deaths due to acute heroin intoxication late 20s to early 30s who have used heroin for 5 to 10 years, and dependent 17% deaths among novice users (high does w/ little tolerance) eg. Oxycontin 80mg tablet crushed, snorted or dissolved in water for IV by people who have no tolerance can be fatal combination drugs may cause seizures ("T's and blues") alcohol combo significantly increases risk of acute opioid intoxication Acute opioid intoxication is characterized by: abnormal mental status (drowsiness, slurred speech, impaired cognition) decreased respiration pinpoint (miotic) pupils Common reasons for increased morbidity and mortality after acute intoxication include anaphylaxis, pulmonary edema, respiratory acidosis, aspiration pneumonitis.
Opioid Withdrawal Abrupt withdrawal usually causes physical effects no worse than a bad flu pupillary dilatation water eyes (lacrimation), runny nose (rhinorrhea), piloerection, yawning, sneezing, anorexia, nausea, vomiting, diarrhea, muscle twitching, anxiety Time of withdrawal symptoms depends on drug half-life Abrupt discontinuation not justifiable secondary to drug user’s extreme anxiety Temporary substitution with a long-acting opioid reduces withdrawal severity Virtually any opioid can be administered to relieve acute withdrawal symptoms daily intake should be reduced by ~ 10% per day methadone can be given once a day; patients do not experience "rush" Some treatment centers subscribe to blind treatments Methadone dose is blinded by giving elixir mixed with juice patient receives same volume of liquid each day progressively juice is increased as the methadone dose is reduced often drug users have coexisting medical problems and require analgesics. Attempts should be made to control the pain via non-narcotic analgesics Pentazocine (Talwin), nalbuphine (Nubain) and butorphanol (Stadol) should not be administered to any patient taking pure agonists (eg methadone) because drugs have antagonist properties and may cause immediate withdrawal
Rapid and ultrarapid opioid detoxification detoxification quickly and on to maintenance program Rapid detoxification has been studied using a variety of protocols, usually including opioid antagonists such as nalxone, naltrexene plus clonidine with or without adjunctive medications such as benzodiazepines, antiemetics, and nonsteroidal antiinflammatory drugs. UROD = ultrashort opioid detoxification patient undergoes opioid antagonist-induced withdrawal under general anesthesia Patients are anesthetized, then intubated and mechanically ventilated. They are given a large bolus of naloxone to precipitate acute opioid withdrawal while unconscious and a diuretic to enhance excretion of the opioid. Patients may experience mild withdrawal symptoms for about six days after awakening from anesthesia, compared with similar withdrawal symptoms on a 20 day methadone taper. Patients must be in good health to tolerate such stress. UROD is most useful in patients who do not qualify for or desire opioid maintenance therapy, patients who have failed other attempts of detoxification, and patients who desire quick detoxification because of family or other reasons. Additional substance abuse counseling may increase chances of recovery from addiction and is found to be helpful.
Maintenance drugs Methadone (pure agonist) buprenorphine (agonist/antagonist) clonidine (alpha-2 adrenergic receptor agonist decreases withdrawal symptoms in patients taking low doses of opioids) One study showed increased death risk in recovering addicts who complete detoxification and use and overdose within the following year. This is thought to be because of loss of tolerance and dose misjudgment. Studies reveal that during maintenance therapy one-third of patients do well, one-third have fluctuating improvement, and one-third show no significant improvement. Maintenance can be years long depending on pt Alternative to methadone for opioid dependence is levo-alpha-acetylmethadole (LAAM, trade name Orlaam); it is like methadone but longer acting (one dose effective for several days). It may cause QT prolongation (should not be used with any drug that can prolong QT). LAAM has been withdrawn from the European market. In Switzerland use of injectable heroin versus oral therapy for addicts who failed other maintenance solutions has revealed decreased risk of hepatitis B and C infection and other positive health outcomes. A separate study also showed methadone and heroin (either injectable or inhalable) combination was more effective than methadone alone in reducing physical, mental, and social problems of heroin addicts. References: "UpToDate"
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Remember: 1) Please follow up with your physician on a routine basis as needed. 2) Please follow directions when taking medications. 3) Please do not hesitate to see a physician when concerns arise regarding your health. 4) Your health should be your most important investment, take good care of it! Sincerely, Dr. Azmoon
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