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