PAIN DRUGS HANDBOOK TABLE
OF CONTENTS
About the
Author
About
the Handbook
Acknowledgments
Forward
to 2rd Edition
Forward
to 1st Edition
DRUGS (Alphabetical Order)
TOPICAL AGENTS
Amitriptyline
Baclofen
Clonidine
Cyclobenzaprine
2-deoxy-d-glucose
Dexamethasone
Dextromethorphan
Diclofenac
Doxepin
DMSO
Gabapentin
Ketamine
Ketoprofen
NEUROLYTIC AGENT
Phenol
APPENDICES
Appendix 1: World Health Organization
Three-step Ladder
Appendix 2: Drug Tables
Appendix 3: Infusion Tables
Appendix 4: Relative Potencies of
Opioids Effects
Appendix 5: Relative Potencies of Steroids
Appendix 6: Intravenous PCA
Standard Orders
Appendix 7: Patient Controlled Analgesia Flow Sheet
Appendix 8: Relative Potencies of Opioids
Appendix 9: Epidural Analgesia Monitoring Orders
Appendix 10: Pain Rating Scales
Appendix 11: Multiplication Factors for Converting the
Daily Dose of a Prior Opioid to the Daily Dose of Oxycontin
Appendix 12: CPR Algorithms
Appendix 13: Pediatric CPR Algorithms
Appendix 14: Trade Name Table
BIBLIOGRAPHY
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Sota
Omoigui's
Pain Drug Handbook
2nd Edition:
Oxycodone
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SECTION
ONE:
Class,
Uses, Dosing,
Elimination
SECTION TWO:
Preparation, Pharmacology, Pharmacokinetics
SECTION THREE:
Interactions, Toxicity
Guidelines/Precautions
Principal Adverse Reactions
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Class
(NARCOTIC AGONIST)
Uses
treatment of acute, chronic and cancer pain, treatment of severe refractory headache and migraine
Dosing
Analgesia: PO immediate-release 5-10 mg every 4-6 hours
PO sustained release (OxyContin): 10-160 mg every 12 hours.
Titrate dose to maintain adequate analgesia with acceptable side effects. Opioid tolerant patients with severe pain may require up to 240 mg every 12 hours. Combinations with adjuvant drugs e.g. NSAIDs, antidepressant agents and use of non-drug therapies enhance analgesia and reduce opioid requirements.
Max Daily Dose of Non Opioid Ingredient in Fixed-Combination Preparations (e.g. Percocet): Acetaminophen - 4 Grams, Aspirin - 6 Grams
Administer sustained release preparation regularly (i.e. around-the-clock). Administer immediate-release preparation prn for breakthrough pain. Due to impaired elimination, dose should be modified depending on clinical response in patients with renal or hepatic dysfunction.
Elimination
hepatic, renal
Preparation
Oxycodone HCL (Roxicodone)
Tablets: 5 mg, 15mg, 30mg
Oral Solution: 5 mg/5ml
Oxycodone HCL (OxyFast Oral Concentrate, Roxicodone Intensol)
Concentrated Oral Solution: 20 mg/ml
Oxycodone HCL (OxyIR)
Capsules immediate release: 5 mg
Oxycodone HCL (Oxycontin)
Tablets sustained release: 10 mg, 20 mg, 40 mg, 80 mg*, 160 mg*
*Oxycontin 80 mg and 160 mg tablets are for use only in opioid tolerant patients requiring daily oxycodone equivalent dosages of 160 mg and 320 mg respectively. One OxyContin 160 mg tablet is comparable to two 80 mg tablets when taken on an empty stomach. With a high fat meal, however, there is a 25% greater peak plasma concentration following one 160mg tablet. Dietary caution should be taken when patients are initially titrated to 160 mg tablets.
Oxycodone HCL and Acetaminophen (Tylox, Roxilox)
Capsules: Oxycodone 5 mg and Acetaminophen 500 mg
Oxycodone HCL and Acetaminophen (Percocet, Oxycet, Roxicet)
Tablets: Oxycodone 5 mg and Acetaminophen 325 mg
Tablets: Oxycodone 5 mg and Acetaminophen 500 mg
Oxycodone HCL and Acetaminophen (Roxicet)
Solution: Oxycodone 5 mg/5 ml and Acetaminophen 325 mg/5 ml
Oxycodone HCL, Oxycodone Terephthalate and Aspirin (Percodan-Demi)
Tablets: Oxycodone HCL 2.25 mg, Oxycodone Terephthalate
0.19 mg and Aspirin 325 mg
Oxycodone HCL, Oxycodone Terephthalate and Aspirin (Percodan, Roxiprin)
Tablets: Oxycodone HCL 4.5 mg, Oxycodone Terephthalate
0.38 mg and Aspirin 325 mg
Pharmacology
A synthetic phenanthrene derivative opiate agonist. Oxycodone differs from hydrocodone by the attachment of a hydroxyl group on the phenanthrene nucleus. Oxycodone exerts its primary effects on the central nervous system and organs containing smooth muscle. Excitatory synaptic pain transmission is decreased by opioid-receptor mediated inhibition of neurotransmitter release e.g. bradykinin at site of tissue injury, substance P in the dorsal horn and dopamine in the basal ganglia. In addition, oxycodone (and other opioids) may alter cognitive and emotional processing of painful input by acting on limbic and cortical opioid receptors. Oxycodone is a potent analgesic and has no ceiling effect for analgesia. Drowsiness, euphoria, depression of the cough reflex and dose dependent respiratory depression may occur. Clinically important respiratory depression is rarely seen in patients with severe pain due to malignant disease even with large doses, because pain and emotional stress are powerful antagonists to narcotic induced respiratory depression. Constipating effects of oxycodone result from induction of non-propulsive contractions through the GI tract. Emetic effects are due to opioid-induced stimulation of the chemo-receptor trigger zone in the floor of the fourth ventricle. Adverse effects are generally milder than those of morphine.10 mg of orally administered oxycodone is equivalent in analgesic efficacy to 20 mg of oral morphine sulfate, 70 mg of oral codeine, 5 mg of intramuscular oxycodone, and 3.3 mg of intramuscular morphine sulfate. Antitussive effects may occur with doses lower than those usually required for analgesia. The drug has no antipyretic effects. Physical dependence and tolerance may develop with repeated administration. Abuse liability is similar to that of codeine. Oxycodone will only partially suppress the withdrawal syndrome in patients physically dependent on other narcotics. Oxycodone crosses the placenta and low levels may be detected in breast milk. However no adverse effects have been noted in nursing infants.
Pharmacokinetics
ONSET OF ACTION: PO 10-15 mins
PEAK EFFECT: PO 30-60 mins
DURATION OF ACTION: PO 3-6 hours PO Slow Release: 12 hours
Interactions
potentiates CNS and circulatory depressant effects of other narcotic analgesics, volatile anesthetics, phenothiazines, sedative-hypnotics, alcohol, tricyclic antidepressants; analgesia enhanced and prolonged by narcotic and non narcotic analgesics (e.g. aspirin, acetaminophen), alpha-2 agonists (e.g. clonidine); increases serum levels and toxic effects of carbamazepine, hepatic metabolism increased and efficacy of oxycodone decreased in cigarette smokers, hypoprothrombinemic effects of warfarin increased by oxycodone-acetaminophen combination.
Toxicity
Toxic Range:
0.6-10 mcg/ml
Manifestations:
Somnolence
Coma
Respiratory Arrest
Apnea
Cardiac Arrhythmias
Combined respiratory and metabolic acidosis
Circulatory Collapse
Cardiac Arrest
Death
Antidote:
Naloxone 0.4-2 mg IV/IM/SC. Repeat dose every 2 to 3 minutes to a maximum of 10-20 mg.
Management:
Discontinue or reduce medication
Support ventilation and circulation (Patent Airway, Oxygen, IV Fluids and Vasopressors)
Administer antidote
Monitor blood gases, pH and electrolytes
Correct acidosis and electrolyte disturbance (lactic acidosis may require IV sodium bicarbonate 1-2 mEq/kg)
Symptomatic treatment
Airway protected - ipecac syrup induced emesis (30 mls or 0.5 mls/kg ipecac syrup followed by 200 mls or 4 mls/kg of water or clear fluid) or gastric lavage (with drug ingestion) followed by administration of activated charcoal (PO 50-100 grams or 1-2 gram/kg)
Guidelines
(1) Reduce dosage in elderly patients and with concomitant use of narcotics and sedative hypnotics.
(2) The drug formulation may contain sodium metabisulfite, which may cause allergic reactions or anaphylaxis in susceptible individuals
(3) Prescribe or supply an antiemetic e.g. metoclopramide for use in the event of nausea and/or vomiting.
(4) Constipation may be more difficult to control than pain. Prevent and/or treat by daily administration of stool softeners or laxatives e.g. Colace (docusate sodium) 100-300 mg/day. Do not administer bulk forming agents that contain methylcellulose, psyllium or polycarbophil. Temporary arrest in the passage through the gastrointestinal tract may lead to fecal impaction or bowel obstruction.
(5) Tolerance is manifested by decreased duration of effect and increasing need for the drug. In these cases, add adjuvant drugs (e.g. NSAIDs, antidepressant agents) or switch to alternative opioids (starting at one-half the equi-analgesic dose) or supplement with non-drug therapies (e.g. TENS).
(6) Abrupt discontinuation of opioids in patients with physical dependence may manifest with withdrawal symptoms. To avoid withdrawal, doses should be reduced slowly (e.g. dose reduction of 75% every 2 days). Withdrawal should be treated symptomatically.
(7) Addiction occurs rarely (frequency of less than 1:3000) and should not be considered in deciding the proper dose and schedule of oxycodone.
(8) Drug combinations with adjuvant drugs enhance analgesia (see front section)
(9) Adjuvant drug therapies also include regional blockade, trigger point injections (with local anesthetics and steroids) and intravenous regional anesthesia.
(10) Adjuvant non-drug therapies include transcutaneous electrical nerve stimulation (TENS) and modalities such as ice or heat application, ultrasound and soft tissue mobilization.
(11) Patients should be warned that oxycodone may impair their ability to perform hazardous tasks requiring mental alertness or physical coordination (e.g. driving a motor vehicle, operating heavy machinery).
(12) OxyContin sustained-release 80 mg tablets are for use only in opioid tolerant patients requiring daily oxycodone equivalent dosages of 160 mg or more Patients should be instructed against use by individuals other than the patient for whom it was prescribed, as such inappropriate use may have severe medical consequences.
(13) Oxycodone is subject to control under the Federal Controlled Substances Act of 1970 as a schedule II (C-II) drug.
Adverse
CVS: hypotension, circulatory depression, bradycardia, syncope
PULM: respiratory depression
CNS: sedation, somnolence, euphoria, dysphoria, disorientation
GU: urinary retention
GI: nausea, vomiting, abdominal pain, biliary tract spasm, constipation, anorexia, hepatic dysfunction
EYE: miosis
ALLERGIC: rash, pruritus, urticaria
Reactions
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