Term
Morphine
(Opioid Agonist: Prototype) |
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Definition
| CU: Acute/chronic Pain, Post-op Pain, Anes. Supp., Labor Pain, Dyspnea d/t acute LV dysfunction or Pulmonary Edema, MI analgesia-decrease HR&vasodialation, anxiolytic. MOA: Activates teh MU Receptors, Dorsal Horn of the Spinal cord, Activates the descending inhibitory system. PK: PO, PR, SC, IM, IV, Epidural/Intrathecal, onset:<5 min, t1/2: 1.5-4.5 hr, duration: up to 7h, 36% Protein binding. MET: liver (conjugation w/ glucuronic acid) to 6-glucuronide, 3-glucuronide. EX:urine & feces. AE: Respiratory Depression: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest. CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures. GI: nausea, vomiting, constipation, CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, VTach, MI, angina pectoris, syncope. Anticholinergic Effects: dry mouth, palpitation, tachycardia, urinary retention. Other Adverse Effects: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
MS Contin
(Opioid Agonist) |
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Definition
CU: Acute & chronic pain, post-op pain, anesthesia supplement, labor, Dyspnea d/t acute LV failure & pulmonary edema, pain management in CA pts. MOA: Principal opium alkaloid; narcotic agonist. PK: Half-life: 1.5-4.5 hr. Onset: PO: 15-30min. Duration: up to 7 hr
Vd: 1-4.7 L/kg (IV). MET: liver (conjugation w/ glucuronic acid) to Metabolites: 6-glucuronide; 3,6-diglucuronide; 3-glucuronide. EX: urine & feces. AE:Respiratory Depression: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest. CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures. GI: nausea, vomiting, constipation
CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, VTach, MI, angina pectoris, syncope. Anticholinergic Effects: dry mouth, palpitation, tachycardia, urinary retention. Other Adverse Effects: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
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Definition
CU:Pain, cough, Off-label: diarrhea. MOA:Narcotic agonist analgesic with antitussive activity, mu receptor agonist. PK:t 1/2: 3-4 hr PO: 30-60 min IM: 10-30 min Duration: 4-6 hr Protein Bound: 25% MET: Inactive but metabolized to morphine by CYP2D6 (missing in 5-10% of population) Demethylated/conjugated in liver (undergoes O-demethylation, N-demethylation, & partial conjugation with glucuronic acid) EX: urine, feces
Note: Utilized in combination w/ other analgesia, eg: ASA and Acetaminophen |
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Term
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Definition
| CU: Opioid intoxication, as an antagonist to reverse fentanyl-induced anesthesia, refractory shock, opioid overdose dx, Off-label: alcoholic coma, Alzheimer's dz, schizophrenia, opioid addiction. MOA: Competitive opioid antagonist; synthetic congener of oxymorphone. PK: Onset: IV: 1-2 min; IM/SC: 2-5 min, t1/2: 60-90 min (adults); 3 hr (neonates), Duration: depends on admin route, generally 1-4 hr. AE: Withdrawal reaction precipitated Note: Not effective PO |
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Term
Hydromorphone
(Opioid Agonist) |
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Definition
CU:Pain/severe pain, Antitussive. MOA:Narcotic agonist analgesic. PK: t1/2: 2-4 hr, Onset: PO: 30 min, IM: 15 min
IV: 10–15 min, PR: 15–30 min; Duration: 4-5 hr (IV: 2-3 hr).
MET: liver CYP2D6 to active metabolite only (conjugation with glucuronic acid). EX: urine (primarily). AE:Respiratory Depression: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest, CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures, GI: nausea, vomiting, constipation, CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, ventricular tachycardia, MI, angina pectoris, syncope, Anticholinergic: dry mouth, palpitation, tachycardia, urinary retention Other: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
Oxycodone
(Opioid Agonist)
(derivatives of codeine and morphine)
10x potency of codeine
Controlled release form: OxyContin
May be used in combination with non-opioid analgesia |
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Definition
CU:Moderate-severe pain, Off-label: postherpetic neuralgia. MOA:Narcotic agonist analgesic. PK:t1/2: 3-4.5 hr, Onset: PO: 10-15 min, Duration: 3-6 hr
MET: hepatic P450 enzyme CYP2D6, active prodrug and metabolites: noroxycodone, oxymorphone (and their glucuronide conjugates) EX: urine (primarily) AE:Respiratory Depression: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest. CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures. GI: nausea, vomiting, constipation; CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, VTach, MI, angina pectoris, syncope. Anticholinergic Effects: dry mouth, palpitation, tachycardia, urinary retention. Other Adverse Effects: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
Meperdine
(Synthetic Opioid)
1/8 potency of Morphine |
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Definition
CU: Moderate-severe pain; pre-op analgesia. MOA: Narcotic agonist analgesic PK:Half-life: 3-5 hr
Onset: rapid Duration: 2-4 hr (SC/IM), Protein Bound: 60-80%, MET: liver (hydrolysis to meperidinic acid followed by partial conjugation with glucuronic acid; N-demethylation to normeperidine), EX: urine (primarily). AE:RESP: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest, CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures, GI: nausea, vomiting, constipation
CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, VTach, MI, angina, syncope, Anticholinergic: dry mouth, palpitation, tachycardia, urinary retention, Other: sweating, flushing, warmness of the face/neck/upper. Note: Toxic Metabolite build up may induce Seizures. |
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Term
Fentanyl
(Synthetic Opioid)
80-100x potency of morphine |
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Definition
| CU:Pain (breakthrough cancer pain, surgery), IV Anesthesia. MOA: Narcotic agonist analgesic (little hypnotic activity). PK: t1/2: 7.1 hr, Onset: immediate (IV); 7-15 min (IM), Duration: up to 72 hr, Time: 30-60 min (IV doses up to 100 mcg); 1-2 hr (IM), Protein Bound: 80-85%, MET: hepatic P450 enzyme CYP3A4, EX: urine, feces. AE: RESP: respiratory/ circulatory depression, respiratory arrest, shock, cardiac arrest, CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures, GI: nausea, vomiting, constipation, CV: bradycardia, QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, VTach, MI, angina pectoris, syncope, GU&Endocrine: urinary retention, oliguria, Anticholinergic: dry mouth, palpitation, tachycardia, Other: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
Fentanyl Derivatives
(Synthetic Opioids)
Alfentanil
Sufentanil
Remifentanil |
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Definition
Alfentanil-Intraoperative anesthesia(IV): loading and maintenance dose
Sufentanil: Intraoperative anesthesia (IV)
Remifentanil: Intraoperative anesthesia; loading and maintenance dose. Post operative analgesia, sedation (IV) |
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Term
Methadone
(Narcotic agonist analgesic)
4x potency of Morphine (PO only) |
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Definition
| CU: Pain; detoxification of narcotic addiction. MOA:Narcotic agonist analgesic. PK: t1/2: 13-47 hr, Onset: rapid, Duration: 4-6 hr; 22-48 hr (repeated administration); 36-48 hr (overdosage)*increases w/ repeated uses, Protein Bound: high, MET: liver (N-demethylation), EX: urine & feces. AE: Respiratory Depression: respiratory/circulatory depression, respiratory arrest, shock, cardiac arrest, CNS: dizziness, visual disturbances, mental clouding/depression, sedation, coma, euphoria, dysphoria, weakness, faintness, agitation, restlessness, nervousness, seizures, GI: nausea, vomiting, constipation, CV: QT-interval prolongation, severe cardiac arrhythmias, cardiac arrest, ST segment elevation, ventricular tachycardia, myocardial infarction, angina pectoris, syncope, GU&Endocrine: urinary retention, oliguria, Cholinergic: bradycardia, anticholinergic effects (dry mouth, palpitation, tachycardia), Other: sweating, flushing, warmness of the face/neck/upper thorax, pruritus, urticaria |
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Term
| L-alpha-acetyl-methadol (LAAM) |
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Definition
| CU: Treatment of opioid withdrawals. Suppresses opiate withdrawals for 4-5 days.PK: Extremely long plasma half-life (>72h) |
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Term
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Definition
| CU: Alcoholism , opioid craving (following successful detox, Treatment of dependence. MOA: Opioid antagonist; congener of oxymorphone. PK: Absorption: 96% from GI tract, only 5-40% reaches systemic circulation d/t first-pass metabolism, t1/2: naltrexone (9.7-10.31 hr); 6-beta-naltrexol (11.4-16.8 hr); Onset: 15-30 min, Duration: 24 hr, Protein Bound: 21-28%, Vd: 1350 L, MET: liver, EX: urine (principally), NOTE: Available in oral form only. |
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Term
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Definition
CU: Opioid induced respiratory depression, opioid overdose, Off label: alcoholism. MOA: Opioid receptor antagonist. PK:Half-Life: 6-16 hr, Duration: 4-6h (8)
MET: liver (glucuronide conjugation), EX: urine, feces. AE: CV: tachycardia, hypertension, hypotension, vasodilation, bradycardia, arrhythmia, GI: N&V, diarrhea, dry mouth, CNS: dizziness, somnolence, depression, agitation, nervousness, tremor, confusion, withdrawal syndrome, myoclonus, Other Effects: fever, headache, chills, postoperative pain, pharyngitis, pruritus, urinary retention. |
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Term
| Nalorphine and Cyclazocine |
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Definition
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Term
Pentazocine
(Narcotic agonist-antagonist) |
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Definition
| CU: General/local anesthesia adjunct, pain, pain/labor. MOA:Narcotic agonist-antagonist analgesic. PK: Half-life: 2-3 hr, Onset: IM 15-20 min; IV 2-3 min, Duration: IM 2 hr; IV 1 hr, Protein Bound: 60%, MET: liver, (oxidation of terminal methyl groups-dimethyl alkyl side chain); glucuronide conjugation to alcoholic/carboxylic acid metabolites, EX: urine (mainly); feces. AE: CNS: dizziness, lightheadedness, euphoria, sedation, nervousness, apprehension, depression, floating feeling, headache, weakness or faintness, disturbed dreams, insomnia, syncope, GI: nausea, vomiting, constipation, abdominal distress, cramps, anorexia, diarrhea, CV: tachycardia, circulatory depression, shock, increased blood pressure, DERM:, diaphoresis, flushed skin (including plethora), rash, pruritus, urticaria, edema of the face, LOCAL: stinging, soft tissue induration, nodules, cutaneous depression, ulceration, severe sclerosis of the skin, HEME: depression of leukocytes (especially granulocytes), moderate transient eosinophilia, OCULAR: blurred vision, focusing difficulty, nystagmus, diplopia, miosis |
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Term
Butorphanol
(Mixed agonist-antagonist) |
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Definition
| CU: Pre-op/post-op analgesia; anesthesia supplement; labor pain, MOA:Narcotic agonist-antagonist analgesic. PK: t1/2: 4.6 hr, Onset: <1 min, Duration: 2-4 hr, Protein Bound: 80%, MET: liver (hydroxylation) Metabolites: hydroxybutorphanol; N-dealkylation & conjugation of butorphanol & its metabolites), EX: urine & feces. AE: Sedation; dizziness; nausea and/or vomiting (13%); clamminess, sweatiness, headache, vertigo, floating feeling, asthenia, anxiety, euphoria, nervousness, paresthesia, lethargy, confusion, lightheadedness; unusual dreams, agitation, hallucinations, seizures, hostility, transient difficulty in speaking &/or executing purposeful movements, delusion ; insomnia; taste perversion, anorexia, constipation, tinnitus; otic pain, tremor ; abdominal cramps, constipation; vasodilation, palpitation ; chest pain, tachycardia, bradycardia, increased/decreased BP ; respiratory depression, apnea |
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Term
Nalbuphine
(Narcotic agonist-antagonist) |
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Definition
CU: General/local anesthesia adjunct, pain, pain/labor. MOA: Narcotic agonist-antagonist analgesic. PK: t1/2: 5 hr, Onset: IM 15 min; IV 2-3 min, Duration: 3-6 hr
Protein Bound: not significant, MET: hepatic, EX: urine, feces. AE: CNS: sedation (36%), headache, dizziness, vertigo, miosis, GI: nausea, vomiting, dry mouth
CV: hypertension, hypotension, bradycardia, pulmonary edema, tachycardia (<1%), DERM&ALLERGIC RXN: itching, burning, urticaria (<1%), RESP: respiratory depression, dyspnea, asthma (<1%) |
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Term
Buprenorphine
(Semisynthetic narcotic agonist-antagonist analgesic) |
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Definition
CU: moderate-severe pain, Tx of opioid dependence. MOA: Semisynthetic narcotic agonist-antagonist analgesic. PK:Half-life: 2.2 hr, Onset: rapid, Duration: 4-10 hr, Protein Bound: 96%
MET: liver (N-dealkylation) to norbuprenorphine (N-dealkylbuprenorphine), EX: urine & feces. AE: CNS: sedation; dizziness, vertigo; headache; confusion, euphoria, weakness, fatigue, nervousness, mental depression, slurred speech, paresthesia, dreaming, psychosis, malaise, hallucinations, depersonalization, coma , GI: nausea; vomiting; dry mouth, constipation, dyspepsia, abdominal cramps, flatulence, CV: hypotension; hypertension, tachycardia, bradycardia, ECG abnormalities, RESP: respiratory depression; hypoventilation; dyspnea, cyanosis, apnea, OCULAR: Miosis; blurred vision, diplopia, amblyopia, mydriasis, conjunctivitis, DERM: pruritus, reactions at the injection site, rash, urticaria |
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