An antagonist is a substance that counteracts the action of something else. A drug that is an antagonist has an affinity for a cell receptor, and by binding to it, prevents the cell from responding. Thus, a narcotic antago-nist reverses the actions of a narcotic. Specific antagonists have been developed to reverse the respiratory depression associated with the opiates. The two narcotic antagonists in use today are naloxone (Narcan) and naltrexone Naloxone is capable of restoring respiratory function within 1 to 2 minutes after administration.
Naltrexone is used primarily for the treatment of narcotic dependence to block the effects of the opiates, especially the euphoric effects experienced in opiate dependence.
NALOXONE
ACTIONS
Administration of naloxone prevents or reverses the effects of the opiates. The exact mechanism of action is
not fully understood, but it is believed that naloxone reverses opioid effects by competing for opiate receptor site If the individual has taken or180 received an opiate, the effects of the opiate are reversed.If the individual has not taken or received an opiate,naloxone has no drug activity.
USES
This drug is used for complete or partial reversal of narcotic depression, including respiratory depression Narcotic depression may be due to intentional or acci dental overdose (self-administration by an individual)
accidental overdose by medical personnel, and drug idiosyncrasy. Naloxone also may be used for diagnosis of a suspected acute opioid overdosage.
ADVERSE REACTIONS
Although not a true adverse reaction, abrupt reversal of narcotic depression may result in nausea, vomiting, sweat-ing, tachycardia, increased blood pressure, and tremors.
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
Naloxone is contraindicated in those with a hypersensi-tivity to the narcotic antagonists. Naloxone is used cautiously in those with a narcotic addiction. Naloxone is used cautiously in patients with cardiovascular dis-
ease; those who are pregnant (Pregnancy Category B);
and in infants of opioid-dependent mothers. These drugs may produce withdrawal symptoms in those physically dependent on the narcotics. The patient must not have taken any opiate for the last 7 to
10 days. Naloxone may prevent the action of opioid antidiarrheals, antitussives, and analgesics. This drug is used cautiously during lactation.
NALTREXONE
ACTIONS
Naltrexone completely blocks the effects of IV opiates,as well as drugs with agonist-antagonist actions
(butorphanol, nalbuphine, and pentazocine). The mechanism of action appears to be the same as that for
naloxone.
USES
Naltrexone is used to treat persons dependent on opioids. Patients receiving naltrexone have been detoxified and are enrolled in a program for treatment of narcotic addiction. Naltrexone, along with other methods of
treatment (counseling, psychotherapy), is used to maintain an opioid-free state. Patients taking naltrexone on a scheduled basis will not experience any narcotic effects if they use an opioid.
ADVERSE REACTIONS
Administration of naltrexone may result in anxiety, dif-ficulty sleeping, abdominal cramps, nasal congestion,joint and muscle pain, nausea, vomiting, dizziness, irritability, depression, fatigue, and drowsiness.
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
Naltrexone is contraindicated in those with a hyper- sensitivity to the narcotic antagonists. Naltrexone is contraindicated during pregnancy (Category C).
Naltrexone is used cautiously in those with a narcotic addiction; in patients with cardiovascular disease, acute hepatitis, liver failure, or depression; and in patients who are suicidal. Naltrexone is used cau-tiously during lactation.Naltrexone may produce withdrawal symptoms in those physically dependent on narcotics. The patient must not have taken any opiate for the last 7 to 10 days.Concurrent use of naltrexone with thioridazine may cause increased drowsiness and lethargy. Naltrexone may prevent the action of opioid antidiarrheals, antitussives, and analgesics .
Naltrexone is used primarily for the treatment of narcotic dependence to block the effects of the opiates, especially the euphoric effects experienced in opiate dependence.
NALOXONE
ACTIONS
Administration of naloxone prevents or reverses the effects of the opiates. The exact mechanism of action is
not fully understood, but it is believed that naloxone reverses opioid effects by competing for opiate receptor site If the individual has taken or180 received an opiate, the effects of the opiate are reversed.If the individual has not taken or received an opiate,naloxone has no drug activity.
USES
This drug is used for complete or partial reversal of narcotic depression, including respiratory depression Narcotic depression may be due to intentional or acci dental overdose (self-administration by an individual)
accidental overdose by medical personnel, and drug idiosyncrasy. Naloxone also may be used for diagnosis of a suspected acute opioid overdosage.
ADVERSE REACTIONS
Although not a true adverse reaction, abrupt reversal of narcotic depression may result in nausea, vomiting, sweat-ing, tachycardia, increased blood pressure, and tremors.
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
Naloxone is contraindicated in those with a hypersensi-tivity to the narcotic antagonists. Naloxone is used cautiously in those with a narcotic addiction. Naloxone is used cautiously in patients with cardiovascular dis-
ease; those who are pregnant (Pregnancy Category B);
and in infants of opioid-dependent mothers. These drugs may produce withdrawal symptoms in those physically dependent on the narcotics. The patient must not have taken any opiate for the last 7 to
10 days. Naloxone may prevent the action of opioid antidiarrheals, antitussives, and analgesics. This drug is used cautiously during lactation.
NALTREXONE
ACTIONS
Naltrexone completely blocks the effects of IV opiates,as well as drugs with agonist-antagonist actions
(butorphanol, nalbuphine, and pentazocine). The mechanism of action appears to be the same as that for
naloxone.
USES
Naltrexone is used to treat persons dependent on opioids. Patients receiving naltrexone have been detoxified and are enrolled in a program for treatment of narcotic addiction. Naltrexone, along with other methods of
treatment (counseling, psychotherapy), is used to maintain an opioid-free state. Patients taking naltrexone on a scheduled basis will not experience any narcotic effects if they use an opioid.
ADVERSE REACTIONS
Administration of naltrexone may result in anxiety, dif-ficulty sleeping, abdominal cramps, nasal congestion,joint and muscle pain, nausea, vomiting, dizziness, irritability, depression, fatigue, and drowsiness.
CONTRAINDICATIONS, PRECAUTIONS,
AND INTERACTIONS
Naltrexone is contraindicated in those with a hyper- sensitivity to the narcotic antagonists. Naltrexone is contraindicated during pregnancy (Category C).
Naltrexone is used cautiously in those with a narcotic addiction; in patients with cardiovascular disease, acute hepatitis, liver failure, or depression; and in patients who are suicidal. Naltrexone is used cau-tiously during lactation.Naltrexone may produce withdrawal symptoms in those physically dependent on narcotics. The patient must not have taken any opiate for the last 7 to 10 days.Concurrent use of naltrexone with thioridazine may cause increased drowsiness and lethargy. Naltrexone may prevent the action of opioid antidiarrheals, antitussives, and analgesics .
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Unknown - Thursday, 22 April 2010
