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Analgesics
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  • 1. ANALGESIC S NARCOTIC & OPIOID narke----any substance that relieved pain, dulled the senses, or induced sleep. Opiate receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. narcotic=substance that binds to opiate receptors or illicit substance pain will give release of opiates (endorphins and enkephalins, dynorphin) Act like inhibitory transmitters… yields less pain.
  • 2. ANALGESICS opium poppy used by Egyptians,Greeks, Romans. morphine=purified constituent of opium---Morpheus---Greek god of dreams….euphoria MOA----these drugs interact with specific receptor sites and have effect on CNS, acting on receptors located on neuronal cell membranes. The presynaptic action of opioids to inhibit neurotransmitter release is considered to be their major effect in the nervous system. also acts on gut wall and joints. Even in therapeutic doses, narcotic analgesics can cause respiratory depression, nausea, and drowsiness. Long term administration produces tolerance, psychic, and physical dependence called addiction. These drugs are commonly prescribed to manage pain, but can also be prescribed to treat diarrhea (Lomotil) or severe cough (codeine).
  • 3. ANALGESICS Narcotic agents may be classified into four categories: 1--Morphine and codeine-- natural alkaloids of opium. 2---Synthetic derivatives of morphine such as heroin. 3--- Synthetic agents which resemble the morphine structure. 4---Narcotic antagonists which are used as antidotes for overdoses of narcotic analgesics.
  • 4. ANALGESIC S opioids --- bind to presynaptic nerve terminal calcium channels. this shortens action potential and yields inhibitied neurotransmitter release. opioids---bind to postsynaptic receptors in ascending pain pathway yields reduced action potential opioids---cause increased transmission of the descending inhibition of spinal nociceptive conduction. Schedule II/III controlled drugs. adverse reaction----respiratory depression, constipation, confusion, naseau, euphoria consider----addiction and tolerance. federal and state laws for processing, dispensing, maintaining records.
  • 5. ANALGESICS examples-acet w codeine----tylenol w codeine codeine---Codeine fentanyl-----Duragesic patch hydrocodone----Hycodan acet w hydrocodone----Lortab hydromorphone----Dilaudid meperidine---Demerol methadone----Dolophine morphine----MS Contin oxycodone----Oxycontin acet w oxycodone----Percocet pentazocine---Talwin acet w propoxyphene----Darvocet
  • 6. NSAIDs NON-NARCOTIC ANALGESIC Nonsteroidal Antiinflammatory Drugs: prostaglandins have 20 carbon chain that includes 5 carbon ring. Make a prostaglandin-------cell injury releases arachidonic acid. cyclooxygenase will convert AA into PG. This irritates nerve endings, yields pain and inflammation. COX 1and COX2 hit different sites on AA. COX1 makes PG for kidney function,stomach protection mucous, blood clotting. COX2 makes PG for pain,heat, swelling. Most NSAID attack COX1 and COX2.
  • 7. NON-NARCOTIC ANALGESIC NSAID indications------fever, pain, antiinflammatory reactions----gastric upset, diarrhrea, kidney failure, hypertension NSAID examples--ibuprofen----Motrin,Advil ketorolac---Toradol naproxen---Naprosyn celecoxib--Celebrex meloxicam---Mobic nabumetone---Relafen
  • 8. COX2 inhibitor NON-NARCOTIC ANALGESIC indications----rheumatoid arthritis, osteoarthritis, menstration cramps, acute pain reactions------GI issues, fluid retention exampleonly celecoxib/Celebrex vioxx and bextra removed from production--MI,strokes Aspirinmoa---redcued fever by increased skin blood flow and inhibit prostaglandin indications-pain, inflammation, fever
  • 9. NON-NARCOTIC ANALGESIC aspirin reactions--stomach ulcer, anemia, tinnitus, confusion, prolonged labor consider----not given to children exposed to chickenpox.(reyes syndrome) avoid with warfarin Acetominophen--moa-----exact mechanism unknown indications----fever, pain, inflammation reaction----avoid with warfarin, liver damage
  • 10. NON-NARCOTIC ANALGESIC aspirin reactions--stomach ulcer, anemia, tinnitus, confusion, prolonged labor consider----not given to children exposed to chickenpox.(reyes syndrome) avoid with warfarin Acetominophen--moa-----exact mechanism unknown indications----fever, pain, inflammation reaction----avoid with warfarin, liver damage