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Chapter 4: Drugs for Pain, Fever, and Inflammation Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Conditions Commonly Treated by Pain, Fever, and Inflammation Drugs • Mild-to-moderate pain caused by injury or surgery • Fever, headaches, & painful menstruation • Rheumatoid arthritis • Osteoarthritis • Chronic pain associated with cancer, AIDS, multiple sclerosis, or sickle cell disease Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs • Analgesics: drugs that control pain without causing patient to lose consciousness – Nonopioid: not derived from opium plant; do not cause physical dependence in patients – Opioid: synthetic or derived from opium plan; may cause physical dependence • Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) – Reduce redness, swelling, pain, & heat of inflammation Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Nonopioid analgesics & NSAIDs – Stop body from producing prostaglandin, which has 2 effects: • Analgesic effect: reduce pain response • Anti-inflammatory effect: reduce inflammation – Are antipyretics, meaning they can reduce body temperature to control fever – Four main groups: • Salicylates • Nonsalicylate analgesics • NSAIDs • Urinary tract analgesic phenazopyridine hydrochloride Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Salicylates – Among most commonly used medications for controlling pain, fever, & inflammation – Mainly used for following: • Relieving mild-to-moderate pain • Reducing fever • Reducing inflammation from rheumatic fever, rheumatoid arthritis, & osteoarthritis – Relieve headache & muscles at same time – Not effective for relieving pain of organs or smooth muscles or controlling severe pain from trauma Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Salicylates • Adverse Reactions – Acetylsalicylic acid – Gastric distress – Choline magnesium trisalicylate – Nausea – Vomiting – Bleeding tendencies – Choline salicylate – Diflunisal & salsalate Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Acetaminophen – Belongs to a group of drugs called para-aminophenol (APAP) derivatives – An OTC drug with analgesic & antipyretic properties – Affects central nervous system – Relieves fever by acting on hypothalamus – Does not have an anti-inflammatory effect – Does not affect way blood platelets work to form clots – Used to treat fever, headache, muscle ache, & general pain Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Nonsteroidal Anti-Inflammatory Drugs – Typically used to combat inflammation – Have analgesic & antipyretic effects – May affect blood platelets, but effects are temporary – Are absorbed through GI tract – Two types • Nonselective: block both COX-1 & COX-2 enzymes • Selective: block only COX-2 enzymes – May cause higher risk for heart attack, stroke, or kidney problems Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Nonselective Nonsteroidal Anti-Inflammatory Drugs – Nabumetone – Naproxen – Diclofenac – – Etodolac, fenoprofen, & flurbiprofen Oxaprozin, piroxicam, & sulindac – Misoprostol – Ibuprofen – Indomethacin – Ketoprofen, ketorolac, & meloxicam Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Adverse Reactions to Nonselective Nonsteroidal Anti-Inflammatory Drugs – Constipation – Diarrhea – Dizziness – Drowsiness – GI upset or pain – GI bleeding – Ulcers – Headache – Nausea – Rash – Visual disturbances – Vomiting Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Selective Nonsteroidal Anti-Inflammatory Drugs – Reduce possibility of some adverse GI effects, such as ulcers, compared with nonselective NSAIDs – Celecoxib (Celebrex) is only COX-2 inhibitor currently available – Used to relieve pain & inflammation associated with following: • Osteoarthritis • Rheumatoid arthritis • Ankylosing spondylitis Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Selective Nonsteroidal Anti-Inflammatory Drugs – Celecoxib (Celebrex) • Adverse Reactions – Dyspepsia – Nausea – Vomiting – GI ulcers – Hypertension – Fluid retention – Peripheral edema – Dizziness – Headache Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Nonopioid Analgesics, Antipyretics, and NSAIDs (cont’d) • Phenazopyridine Hydrochloride – A dye used in commercial coloring that helps relieve symptoms associated with urinary tract infections, including: • Pain • Burning • Urgency • Frequency – Adverse reactions • Yellow tinge to patient’s skin & whites of eyes • Acute renal or hepatic failure Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs • Opioid Agonists – Controlled substances used to relieve or decrease pain without causing patient to lose consciousness – Sometimes called narcotic agonists • Opioid Antagonists – Drugs that work against opioid agonists to block their effects and reverse adverse reactions, such as respiratory & CNS depression • Mixed Opioid Agonist-Antagonists – Act like agonists & antagonists by relieving pain & reducing risk of adverse reactions Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Opioid Agonists – Mainly used to manage moderate-to-severe acute & chronic pain – Bind with opiate receptors in central, peripheral nervous systems – Mimic effects of endorphins, body’s natural opiates – Binding process has following effects: • Antidiarrheal action • Contraction of bladder & ureters • Constriction of bronchial muscles • Dilation of blood vessels • Slowing of intestinal peristalsis & suppression of cough center Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Opioid Agonists – Oxymorphone – Codeine – Propoxyphene – Fentanyl citrate – Remifentanil – Hydrocodone – Sufentanil – Hydromorphone – Levorphanol – Constipation – Meperidine – Flushing – Methadone – Orthostatic hypotension – Morphine – Pupil constriction – Oxycodone • Adverse Reactions Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Mixed Opioid Agonist-Antagonists – Relieve pain while reducing toxic effects & dependency – Affect CNS – Act in 2 ways at same time: • At some receptor sites, they bind with receptor & produce pain relief effect similar to other opioids • At other sites, they block agonist action, reducing adverse effects – Used for pain relief during childbirth & after surgery – Sometimes prescribed instead of opioid agonists because of lower risk of drug dependence Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Mixed Opioid AgonistAntagonists • Adverse Reactions – Euphoria – Buprenorphine – Lightheadedness – Butorphanol & nalbuphine – Nausea – Pentazocine – Vomiting – Sedation Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Opioid Antagonists – Counteract effects of opioids – Have strong attraction for opiate receptors – Don’t stimulate receptors, but fill up receptor sites so that opioids can’t bind with them (competitive inhibition) – 2 most common opioid antagonists: • Naloxone • Naltrexone Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Opioid Agonist and Antagonist Drugs (cont’d) • Adverse Reactions – Naloxone • Nausea • Vomiting • Hypertension • Tachycardia – Naltrexone • Anxiety, depression, disorientation, dizziness, headache, mood changes, or nervousness • Anorexia, diarrhea, constipation, nausea, thirst, GI pain, cramps, vomiting • Urinary frequency • Edema, hypertension, palpitations, phlebitis, shortness of breath • Liver toxicity Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs • Block perception of pain or cause a loss of feeling • Allow individual to undergo surgery or other medical procedures without distress & pain • Three classes – General anesthetics • Inhalation • Intravenous – Local anesthetics – Topical anesthetics Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Inhalation Anesthetics – Used for surgery – Allow precise & quick control of depth of anesthesia – Most are liquid & volatile – Move from lungs to blood; are eliminated by lungs or liver – Work by depressing CNS – Effects • Loss of consciousness • Loss of responsiveness to sensory stimulation • Muscle relaxation Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Inhalation Anesthetics • Adverse Reactions – Desflurane – Ataxia – Enflurane, isoflurane, & sevoflurane – Confusion – Depressed breathing & circulation – Hypothermia – Nausea – Sedation – Vomiting – Nitrous oxide Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Intravenous Anesthetics – Typically used when patient needs general anesthesia for a short period, such as outpatient surgery – Used to help induce general anesthesia more rapidly or supplement inhalation anesthetics – Different types of drugs are used as intravenous anesthetics: • Barbiturates • Benzodiazepines • Dissociatives • Hypnotics • Opiates Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Intravenous Anesthetics (& associated adverse reactions) – Methohexital & Sufentanil – Thiopental: respiratory depression; hiccups, coughing, muscle twitching; depressed cardiac function & peripheral dilation – Midazolam: CNS & respiratory depression, hypotension, dizziness – Ketamine: irrational behavior, excitement, disorientation, delirium, hallucinations, increased heart rate, hypertension – Etomidate: hiccups, coughing, muscle twitching – Propofol: respiratory depression – Fentanyl: CNS & respiratory depression, hypoventilation, cardiac arrhythmias, muscle rigidity Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Local Anesthetics – Administered to prevent or relieve pain in a specific area of body – Often used as an alternative to general anesthesia for elderly or debilitated patients – Two main groups: “amide” drugs & “ester” drugs – Uses • To prevent & relieve pain from procedures, disease, injury • To treat severe pain that topical anesthetics or analgesics can’t relieve • As an alternative to general anesthetics in surgery for older patients & patients with respiratory disorders Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Local Anesthetics – – Amide drugs • Adverse Reactions – Shivering • Bupivacaine – Positional headache • Lidocaine – Pain • Mepivacaine – Bradycardia • Prilocaine – Hypotension • Ropivacaine – Anxiety – Restlessness – Palpitations – Tachycardia Ester drugs Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Topical Anesthetics – Are applied directly to unbroken skin or mucous membranes to prevent or relieve minor pain – Most produce little systemic absorption – Many work by blocking nerve signals – Aren’t well absorbed into systemic circulation Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins Anesthetic Drugs (cont’d) • Topical Anesthetics • Adverse Reactions – Lidocaine – A rash – Tetracaine – Itching – Benzocaine – Hives – Cocaine – Swelling of mouth & throat – Dyclonine & dibucaine – Breathing difficulty – Pramoxine – Aromatic compounds – Cooling effect Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins