Notes
Narcotics and antimigraine agents provide treatment for acute or chronic severe pain. These agents exert their effect on the brain and spinal cord to alter the way impulses from peripheral nerves are processed. As a result, pain perception and tolerance are altered.
Table of Common Drugs and Generic Names
Here is a table of commonly encountered narcotics, narcotic antagonists, and antimigraine agents, their generic names, and brand names:
Classifications | Generic Name | Brand Name |
---|---|---|
Narcotics | ||
Narcotic Agonists | codeine | |
fentanyl | Actiq, Duragesic | |
hydrocodone | Hycodan | |
levorphanol | Levo-Dromoran | |
meperidine | Demerol | |
methadone | Dolophine | |
morphine | Roxanol, Astramorph | |
opium | Paregoric | |
oxycodone | OxyContin, Oxecta | |
oxymorphone | Numorphan | |
tramadol | Ultram | |
Narcotic Agonists-Antagonists | buprenorphine | Buprenex |
butorphanol | Stadol | |
nalbuphine | Nubain | |
pentazocine | Talwin | |
Narcotic Antagonists | naloxone | Narcan |
naltrexone | Re Via | |
Antimigraine Agents | ||
Ergot derivatives | dihydroergotamine | Migranal |
ergotamine | Ergomar | |
Triptans | almotriptan | Axert |
eletriptan | Relpax | |
frovatriptan | Frova | |
naratriptan | Amerge | |
rizatriptan | Maxalt | |
sumatriptan | Imitrex | |
zolmitriptan | Zomig |
Condition Spotlight: Pain
Pain is mostly a subjective experience of unpleasant sensation and emotional experience. People respond to pain differently because of cultural differences, learned experiences, and environmental stimuli.
A-delta and C-fibers are two sensory nerves that respond to stimulation by generating nerve impulses that produce pain sensations.
Acute vs. Chronic Pain
Pain can be acute or chronic:
- Acute Pain – is caused by tissue injury. It is the type of pain which makes the person aware of the injury and leads him to seek for care and education about the injury and how to take care for it.
- Chronic Pain – is a constant or intermittent pain that keeps occurring long past the time the area would be expected to heal. This is the type that can interfere with activities of daily living.
Pain Classification According to Source
- Pain is also classified according to source:
- Nociceptive Pain – caused by direct pain receptor stimulus
- Neuropathic Pain – caused by nerve injury
- Psychogenic Pain – associated with emotional, psychological, or behavioral stimuli
Narcotic Drugs
Narcotic drugs are drugs that react with different type of opioid receptors, receptor sites that respond to naturally occurring peptides, enkephalins, and endorphins. These are found in the CNS, peripheral nerves, and GI tract cells. In the spinal cord, they integrate and relate pain information. Pain relief and side effects depend on the type of receptor site. The different types of opioid receptors are the following:
- Mu-receptors – primarily pain-blocking receptors; also account for respiratory depression, euphoria, and development of physical dependence.
- Beta-receptors – modulate pain transmission by reacting with enkephalins in the periphery
- Kappa-receptors – associated with some analgesia, pupillary constriction, sedation, and dysphoria
- Sigma-receptors – pupillary dilation, hallucinations, psychoses with narcotic use
Narcotic drugs are divided into three classes:
- Narcotic Agonists – react with opioid receptors in the CNS; cause analgesia, sedation, or euphoria. They are classified as controlled substances because they have potential for physical dependence.
- Narcotic Agonists-Antagonists – stimulate certain opioid receptors but block other such receptors. They exert similar analgesic effect with that of morphine but they have less potential for abuse. However, they are associated with more psychotic like reactions.
- Narcotic Antagonists – bind strongly to opioid receptors without causing receptor activation. They block opioid receptor effects as well as effects of too much opioids in the system.
Narcotic Agonists
Therapeutic Action
The desired and beneficial action of narcotic agonist is:
- Narcotic agonists act as agonist to specific opioid receptors in the CNS to produce analgesia, euphoria, and sedation.
Indications
Narcotic agonists are indicated for the following medical conditions:
- Relief of moderate to severe acute pain or chronic pain; preoperative medication; component of combination therapy for severe chronic pain; intraspinal to reduce intractable pain.
Here are some important aspects to remember for indication of narcotic agonists in different age groups:
Children
- Safety and effectiveness has not been established in children.
- Narcotic agonists that have established pediatric dosage guidelines are codeine, fentanyl (except transdermal), hydrocodone, meperidine, and morphine only.
- Naloxone is the antidote for narcotic overdose and reversal of narcotic effects.
Adults
- They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
- They should be educated about the importance of asking for pain medication before the pain becomes acute.
- Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus and the baby.
- Narcotics used in labor include morphine, meperidine, and oxymorphone.
- All narcotic agonists are pregnancy category B except oxycodone (category C) so it might be the drug of choice if one is needed during pregnancy.
Older adults
- They are more susceptible to drug adverse effects because of existing medical conditions.
- Safety measures should be established (side rails, call light, assistance to ambulate).
Pharmacokinetics
Here are the characteristic interactions of narcotic agonists and the body in terms of absorption, distribution, metabolism, and excretion:
Route | Onset | Peak | Duration |
Oral | Varies | 60 min | 5-7 h |
PR | Rapid | 20-60 min | 5-7 h |
Subcutaneous | Rapid | 50-90 min | 5-7 h |
IM | Rapid | 30-60 min | 5-6 h |
IV | Intermediate | 20 min | 5-6 h |
T1/2: 1.5-2 h Metabolism: liver Excretion: liver (bile), kidney (urine) |
Contraindications and Cautions
The following are contraindications and cautions for the use of narcotic agonists:
- Allergy to narcotic agonists. Prevent hypersensitivity reaction
- Diarrhea caused by toxic poisons. Drug depresses GI activity and this could lead to increased absorption and toxicity
- Respiratory dysfunction. Exacerbated by respiratory depression caused by drugs
- Recent GI/GU surgery, acute abdomen, ulcerative colitis. Can be worsen by the GI depressive effects of the narcotics
- Head injuries, alcoholism, delirium tremens, cerebral vascular disease. Can be exacerbated by the CNS effects of the drug
- Liver, renal dysfunction. Can interfere with metabolism and excretion of the drug
- Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
Adverse Effects
Use of narcotic agonists may result to these adverse effects:
- CNS: light-headedness, dizziness, psychoses, anxiety, fear, hallucinations, pupilconstriction, impaired mental processes
- GI: nausea, vomiting, constipation, biliary spasm
- GU: ureteral spasm, urinary retention, hesitancy, loss of libido
- Others: sweating, physical and psychological dependence
- Narcotic-induced respiratory center depression: respiratory depression with apnea, cardiac arrest, shock
Interactions
The following are drug-drug interactions involved in the use of narcotic agonists:
- Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression, hypotension, and sedation or coma
- SSRI, MAOI, TCA, St. Johns Wort: increased risk of potentially life-threatening serotonin syndrome if taken with tapentadol, the newest narcotic agonists that blocks norepinephrine reuptake in the CNS
- Methylnaltrexone bromide (Relistor) is the treatment for opioid-induced constipation in palliative care patients who are no longer responding to traditional laxatives.
Narcotic Agonists-Antagonists
Therapeutic Action
The desired and beneficial action of narcotic agonist-antagonist is:
- Narcotic agonists-antagonists act on certain opioid receptorsbut block other such receptors. They have less potential for abuse compared to narcotic agonists but are able to exert similar analgesic effect as morphine.
Indications
Narcotic agonists-antagonists are indicated for the following medical conditions:
- Relief of moderate to severe pain; preanesthetic medication and a supplement to surgical anesthesia
- May be desirable for relieving chronic pain in patients who are susceptible to narcotic dependence.
Here are some important aspects to remember for indication of narcotic agonist-antagonists in different age groups:
Children
- Safety and effectiveness has not been established in children.
- Narcotic agonist-antagonist of choice for children older than age 13 is buprenorphine.
- Naloxone is the antidote for narcotic overdose and reversal of narcotic effects.
Adults
- They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
- They should be educated about the importance of asking for pain medication before the pain becomes acute.
- Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus and the baby.
Older adults
They are more susceptible to drug adverse effects because of existing medical conditions. Safety measures should be established (side rails, call light, assistance to ambulate).
Pharmacokinetics
Here are the characteristic interactions of narcotic agonists-antagonists and the body in terms of absorption, distribution, metabolism, and excretion:
Route | Onset | Peak | Duration |
PO, IM, subcutaneous | 15-30 min | 1-3 h | 3 h |
IV | 2-3 min | 15 min | 3 h |
T1/2: 2-3 h Metabolism: liver Excretion: liver (bile), kidney (urine) |
Contraindications and Cautions
The following are contraindications and cautions for the use of narcotic agonists-antagonists:
- Allergy to narcotic agonists-antagonists. Prevent hypersensitivity reaction
- Physical dependence on narcotics. Withdrawal symptom may be precipitated
- COPD, other respiratory dysfunction. Can be exacerbated by respiratory depression
- MI, CAD, hypertension. Can be exacerbated by cardiac stimulatory effects
- Renal, hepatic dysfunction. Interfere with drug metabolism and excretion
- Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
- Nalbuphine is specifically contraindicated to patients who are also allergic to sulfites to prevent cross-hypersensitivity reactions.
Adverse Effects
Use of narcotic agonists-antagonists may result to these adverse effects:
- CNS: light-headedness, dizziness, psychoses, anxiety, fear, hallucinations, pupil constriction, impaired mental processes
- GI: nausea, vomiting, constipation, biliary spasm
- GU: ureteral spasm, urinary retention, hesitancy, loss of libido
- Others: sweating, physical and psychological dependence
- Narcotic-induced respiratory center depression: respiratory depression with apnea, suppression of cough reflex
Interactions
The following are drug-drug interactions involved in the use of narcotic agonist-antagonists:
- Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression, hypotension, and sedation or coma
- Tripelennamine: increased hallucinogenic and euphoric effect with pentazocine (“Ts and Blues”)
- Methylnaltrexone bromide (Relistor) is the treatment for opioid-induced constipation in palliative care patients who are no longer responding to traditional laxatives.
Nursing Considerations
Here are important nursing considerations when administering these drugs:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking, and examination:
- Assess for mentioned cautions and contraindications (e.g. drug allergy, respiratory dysfunction, myocardial infarction and CAD, hepatorenal dysfunction, etc.) to prevent untoward complications.
- Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
- Perform thorough physical (CNS, vital signs, bowel sounds, urine output) to establish baseline status before beginning therapy, determine drug effectiveness and evaluate for any potential adverse effects.
- Monitor laboratory results (liver function, kidney function) to determine need for possible dose adjustment and identify toxic drug effects.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of these drugs for therapy:
- Impaired gas exchange related to respiratory depression
- Disturbed sensory perception related to CNS effects
- Constipation related to GI effects
- Risk for injury related to CNS effects
Implementation with Rationale
These are vital nursing interventions done in patients who are taking narcotic agonists and narcotic agonists-antagonists:
- Perform baseline and periodic pain assessments with patient to monitor drug effectiveness and provide appropriate changes in pain management protocol as needed.
- Have a narcotic antagonist and equipment for assisted ventilation readily available when administering this drug IV to provide patient support in case of severe reaction.
- Monitor timing of analgesic doses. Prompt administration may provide a more acceptable level of analgesia and lead to a quicker resolution of the pain.
- Provide non-pharmacological pain measures like breathing exercises, back rubs, and stress reduction to increase drug effectiveness and reduce pain.
- Provide comfort measures (e.g. small, frequent meals for GI upset) to help patient tolerate drug effects.
- Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
- Educate client on drug therapy to promote understanding and compliance.
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
- Monitor patient response to therapy (relief of pain, sedation).
- Monitor for adverse effects (e.g. GI depression, respiratory depression, arrhythmias, etc).
- Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
- Monitor patient compliance to drug therapy.
Narcotic Antagonists
Therapeutic Action
The desired and beneficial action of narcotic antagonists is as follows:
- Narcotic antagonists are drugs that bind strongly to opioid receptors but do not activate them. They block the opioid receptors and reverse the effects of opioids like respiratory depression and sedation.
Indications
Narcotic antagonists are indicated for the following medical conditions:
- Indicated for complete or partial reversal of narcotic depression; diagnosis of suspected opioid overdose.
Here are some important aspects to remember for indication of narcotic antagonists in different age groups:
Children
- Safety and effectiveness has not been established in children.
- Naloxone is the antidote for narcotic overdose and reversal of narcotic effects.
Adults
- They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
- They should be educated about the importance of asking for pain medication before the pain becomes acute.
- Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus and the baby.
Older adults
- They are more susceptible to drug adverse effects because of existing medical conditions.
- Safety measures should be established (side rails, call light, assistance to ambulate).
Pharmacokinetics
Here are the characteristic interactions of narcotic antagonists and the body in terms of absorption, distribution, metabolism, and excretion:
Route | Onset | Peak | Duration |
IV | 2 min | Unknown | 4-6 h |
IM, Subcutaneous | 3-5 min | Unknown | 4-6 h |
T1/2: 30-81 minutes Metabolism: liver Excretion: kidney (urine) |
Contraindications and Cautions
The following are contraindications and cautions for the use of narcotic antagonists:
- Allergy to narcotic antagonists. Prevent hypersensitivity reaction
- Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
- Narcotic addiction. Precipitation of a withdrawal symptom
- CV disease. Exacerbated by the reversal of the depressive effects of narcotics
Adverse Effects
Use of narcotic antagonists may result to these adverse effects:
- CNS: excitement, reversal of analgesia
- CV: tachycardia, blood pressure changes, dysrhythmias, pulmonary edema
- Acute narcotic abstinence syndrome: nausea, vomiting, sweating, tachycardia, hypertension, tremulousness, feelings of anxiety. A naloxone challenge should be administered before giving naltrexone to help to avoid acute reactions.
Interactions
There is no significant drug-drug interactions involved with narcotic antagonists.
Nursing Considerations
Here are important nursing considerations when administering this drug:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking, and examination:
- Assess for mentioned cautions and contraindications (e.g. drug allergy, history of narcotic addiction, myocardial infarction, etc.) to prevent untoward complications.
- Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
- Perform thorough physical (neurological status, respiratory rate and rhythm, vital signs) to establish baseline status before beginning therapy, determine drug effectiveness and evaluate for any potential adverse effects.
- Obtain an electrocardiogram as appropriate to evaluate for cardiac effects.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
- Decreased cardiac output related to CV effects
- Acute pain related to withdrawal and CV effects
- Risk for injury related to CNS effects
Implementation with Rationale
These are vital nursing interventions done in patients who are taking narcotic antagonists:
- Maintain open airway and provide artificial ventilation and cardiac massage as needed to support the patient.
- Administer vasopressors as ordered and as needed to manage narcotic overdose.
- Administer naloxone challenge before giving naltrexone because of the serious risk of acute withdrawal.
- Provide comfort measures to help patient cope with withdrawal syndrome.
- Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
- Ensure that patients receiving naltrexone have been narcotic-free for 7-10 days to prevent severe withdrawal syndrome.
- Educate client on drug therapy to promote understanding and compliance.
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
- Monitor patient response to therapy (reversal of opioid effects, treatment of alcohol dependence).
- Monitor for adverse effects (e.g. CV changes, arrhythmias, hypertension, etc).
- Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
- Monitor patient compliance to drug therapy.
Antimigraine Agent: Ergot Derivatives
Therapeutic Action
The desired and beneficial actions of ergot derivatives are as follows:
- Antimigraine agents are drugs used to treat migraine headaches, a type of headache that is pounding and is associated with nausea, vomiting, and light sensitivity.
- There are two antimigraine agents available now: ergot derivatives and triptans.
- Ergot derivatives decrease the pulsation of cranial arteries and cause constriction of cranial blood vessels by blocking alpha-adrenergic and serotonin-receptor sites. As a result, the hyperperfusion of the basilar artery vascular bed is reduced.
Indications
Ergot derivatives are indicated for the following medical conditions:
- Ergot derivatives are indicated for the prevention or abortion of migraine or vascular headaches. Ergotamine was the drug of choice for migraines before triptans were developed.
- Triptans are indicated for the treatment of acute migraine and are not used for prevention of migraines.
Here are some important aspects to remember for indication of ergot derivatives in different age groups:
Children
- Both classes are not recommended for children.
- Ergot derivatives have a lot of adverse effects and there is no sufficient clinical experience to prove that triptans can be recommended for children’s use.
Adults
- Careful assessment of headache should be done before antimigraine agents can be indicated.
- Both classes are contraindicated to pregnancy and lactation.
Older adults
- They are more likely to have their chronic conditions be exacerbated by antimigraine agents so utilization with extreme caution is exercised.
- The dose should be the least amount possible and safety precautions are extremely important.
Pharmacokinetics
Here are the characteristic interactions of ergot derivates and the body in terms of absorption, distribution, metabolism, and excretion:
Route | Onset | Peak | Duration |
Sublingual | Rapid | 0.5-3 h | N/A |
T1/2: 2.7 h, then 21 h Metabolism: liver Excretion: intestines (feces) |
Contraindications and Cautions
The following are contraindications and cautions for the use of ergot derivatives:
- Allergy to ergot derivatives. Prevent hypersensitivity reaction
- CAD, hypertension, peripheral vascular diseae. Can be exacerbated by CV effects of the drug
- Impaired liver function. Alter the metabolism and excretion of drugs
- Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
- Pruritus. Caution is exercised because it can be worsened by drug-induced vascular constriction
- Malnutrition. Caution is applied because drugs can stimulate CTZ and can cause severe GI reactions
- Ergotism in infants: vomiting, diarrhea, seizures
Adverse Effects
Use of ergot derivatives may result to these adverse effects:
- CNS: numbness, tingling of extremities, muscle pain
- CV: pulselessness, weakness, chest pain, arrhythmia, localized edema and itching, MI
- Direct stimulation of CTZ: GI upset, nausea, vomiting, diarrhea
- Ergotism: nausea, vomiting, severe thirst, hypoperfusion, chest pain, blood pressurechanges, confusion, drug dependency, drug withdrawal syndrome
Interactions
The following are drug-drug interactions involved in the use of ergot derivatives:
- Beta-blockers: increased risk for peripheral ischemia and gangrene
Antimigraine Agent: Triptans
Therapeutic Action
The desired and beneficial action of triptans is:
- Antimigraine agents are drugs used to treat migraine headaches, a type of headache that is pounding and is associated with nausea, vomiting, and light sensitivity.
- There are two antimigraine agents available now: ergot derivatives and triptans.
- Triptans is a relatively new antimigraine agent that causes cranial vascular constriction and relief of migraine headache pain. They do this by binding to serotonin receptors.
Indications
Triptans are indicated for the following medical conditions:
- Triptans are indicated for the treatment of acute migraine and are not used for prevention of migraines.
Here are some important aspects to remember for indication of triptans in different age groups:
Children
- Both classes are not recommended for children.
- Ergot derivatives have a lot of adverse effects and there is no sufficient clinical experience to prove that triptans can be recommended for children’s use.
Adults
- Careful assessment of headache should be done before antimigraine agents can be indicated.
- Both classes are contraindicated to pregnancy and lactation.
Older adults
- They are more likely to have their chronic conditions be exacerbated by antimigraine agents so utilization with extreme caution is exercised.
- The dose should be the least amount possible and safety precautions are extremely important.
Pharmacokinetics
Here are the characteristic interactions of triptans and the body in terms of absorption, distribution, metabolism, and excretion:
Route | Onset | Peak | Duration |
Nasal spray | Varies | 5-20 min | Unknown |
Oral | 1-1.5 h | 2-4 h | Up to 24 h |
Subcutaneous | Rapid | 1-5 h | Up to 24 h |
T1/2: 115 min Metabolism: liver Excretion: kidney (urine) |
Contraindications and Cautions
The following are contraindications and cautions for the use of triptans:
- Allergy to triptans. Prevent hypersensitivity reaction
- Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
- Active CAD. Can be exacerbated by vessel-constricting effects of the drug
- Renal, hepatic dysfunction. Can alter drug metabolism and excretion
Adverse Effects
Use of triptans may result to these adverse effects:
- CNS: numbness, tingling, burning sensation, feelings of coldness or strangeness, dizziness, weakness, myalgia, vertigo
- CV: blood pressure alterations, tightness or pressure in the chest
- GI: dysphagia, abdominal discomfort
Interactions
The following are drug-drug interactions involved in the use of triptans:
- Ergot-containing drugs: risk of prolonged vasoactive reactions
- MAOI: increased risk of vasoconstriction if used within 2 weeks of MAOI discontinuation
Nursing Considerations
Here are important nursing considerations when administering this drug:
Nursing Assessment
These are the important things the nurse should include in conducting assessment, history taking, and examination:
- Assess aforementioned cautions and contraindications (e.g. drug allergy, history of myocardial infarction and CAD, hepatorenal dysfunction, etc.) to prevent untoward complications.
- Perform thorough physical (neurological status, vital signs, etc) to establish baseline status before beginning therapy, determine drug effectiveness and evaluate for any potential adverse effects.
- Monitor laboratory test results (liver, kidney function tests) to determine need for dose adjustment and identify possible toxic effects.
Nursing Diagnoses
Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:
- Decreased cardiac output related to CV effects
- Acute pain related to withdrawal and CV effects
- Risk for injury related to CNS effects
Implementation with Rationale
These are vital nursing interventions done in patients who are taking narcotic antagonists:
- Administer drug to relieve acute migraines (at first sign of headache) and not to prevent migraine because these are not indicated for prevention.
- Monitor for complaints of extremity numbness and tingling to identify effects on vascular constriction.
- Provide comfort measures to help patient cope with withdrawal syndrome.
- Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
- Educate client on drug therapy to promote understanding and compliance.
Evaluation
Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:
- Monitor patient response to therapy (relief of acute migraine headache).
- Monitor for adverse effects (e.g. CV changes, arrhythmias, hypertension, etc).
- Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
- Monitor patient compliance to drug therapy.
Practice Exam
[mtouchquiz 766 title=off]