ANALGESICS I.

Pain  occurs when there is tissue damage release of kinins & prostaglandins stimulate sensory nerves (A-delta & C fibers) pain is perceived  Gate-Control Theory

II.

Non -Narcotic Analgesics A. Nonsteroidal Antiinflammatory Drugs (NSAIDs) • ibuprofen (Advil, Alaxan, Dolan, Muskelax, Midol) • mefenamic acid (Dolfenal, Gardan, Ponstan) • Naproxen (Flanax) • Ketorolac (Toradol) • ketoprofen (Orudis) • diclofenac (Cataflam, Neopyrazone ) • indomethacin • piroxicam • Meloxicam (Mobic) Indic:   analgesic (arthritis, mild-moderate pain, dysmenorrhea) antipyretic

MOA: block prostaglandin (PG) synthesis Side Effects: 1. gastric irritation & bleeding -MC 2. blood dyscrasias 3. dizziness 4. hypotension 5. pruritus 6. Na & water retention 7. tinnitus B. Salicylates • aspirin (ASA, Aspilet) Indic:   analgesic antipyretic

 anticoagulant (reduce risk of TIA, stroke, or MI) MOA: block PG synthesis Side Effects: 1. gastric irritation 2. 8th CN damage 3. salicylism a. tinnitus, dizziness b. difficulty hearing c. N, V & diarrhea d. confusion 4. salicylate toxicity C. Cyclooxygenase (COX)- 2 inhibitors • celecoxib ( Celebrex ) • valdecoxib ( Bextra ) Indic:  analgesic MOA: block cyclooxygenase-2 ---> reduce inflammation & pain Side Effect: less GI & CNS effects D. Acetaminophen • acetaminophen (Tylenol) Indic:   analgesic, antiypyretic

MOA: blocks PG synthesis Side Effects: 1. V,A, N 2. rash 3. hepatotoxicity 4. acetaminophen toxicity III. Narcotic (Opioid) Analgesics • morphine • meperidine (Demerol) • nalbuphine (Nubain) • codeine • oxycodone

Indic:

• methadone • Butorphanol (Stadol)     DOC for severe pain cough suppressant slows motility of GIT induction of anesthesia

MOA: bind with opioid receptors -->regulate transmission of pain impulses, promote feelings of well-being & euphoria Side Effects: 1. constipation 2. hypotension 3. urinary retention 4. miosis 5. respiratory depression 6. euphoria & sedation 7. drug tolerance & drug dependence 8. increase ICP  Opioid Antagonist • naloxone (Narcan) • Naltrexone Indic:   reversal of opioid effects in narcotic overdose Dx of narcotic overdose

MOA: reverses opioid effects ( resp. depression, sedation & hypotension) Side Effects: 1. Acute narcotic abstinence syndrome  NV, sweating, tachycardia, hypotension 2. BP changes 3. pulmonary edema

ANTIMIGRAINE DRUGS I. Headaches a. Migraine headache i. Common migraine ii. Classic migraine b. Cluster headache c. Tension headache II. Ergot Derivatives  ergotamine Indic: prevent or abort migraine attacks in adults MOA: not understood, constricts cranial blood vessels Side Effects: 1. peripheral vasoconstriction (sometimes severe) a. numbness, tingling in toes & fingers b. muscle pain c. pulselessness or weakness of legs 2. CV changes 3. ergotism a. NV, b. diarrhea c. excessive thirst d. hypoperfusion e. chest pain f. confusion III. Triptans  sumatriptan Indic: tx of acute migraine tx of cluster headache (Sub-Q route) MOA: binds with serotonin receptors --> constricts cranial bld vessels Side Effects: same as ergots but less systemic effects IV. others: Propranolol – beta blocker Side Effect : bradycardia, bronchospasm

CNS STIMULANTS I. Amphetamines • amphetamine sulfate • dextroamphetamine (Dexedrine) • methylphenidate HCl (Ritalin) Indic:  Tx of narcolepsy  Tx of attention deficit hyperactivity disorder MOA: stimulate cerebral cortex II. Anorexiants (Antiobesity ) • phentermine HCL (Ionamin , Duromine) • benzphetamine HCl Indic: simple obesity MOA: act on cerebral cortex & hypothalamus --> suppress appetite III. other CNS stimulants: • aminophylline • theophylline • caffeine Indic: tx of asthma MOA: act on brainstem & medulla --> stimulate respiration Side Effects of CNS stimulants: 1. irritability 2. restlessness & tremors 3. insomnia 4. heart palpitations & tachycardia 5. HPN 6. dry mouth 7. anorexia & weight loss 8. diarrhea or constipation 9. impotence 10. dependence & tolerance

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