pharm opiod and algesics

fetanyl, codeine, oxycodone, propoxyphene

any drug natural or synthetic that has actions similar to those of morphine.

enkephalins, endorphins, dynorphins bodies natural peptides. they have opioid like properties they are found in the CNS and peripheral tissues.

Mu, Kappa, delta

Mu. opiod analgesics act primarily by activating mu recepotrs, weak activation of kappa and do not interact with delta receptors.

• analgesia
• respiratory depression,
• euphoria
• sedation
• (also activation is related to physical dependence.)

• analgesia
• sedation

a drug that produces low to moderate receptor activation when administered alone. but will block the action of a full agonist if given together.

• •Transduction—cell damage stimulates pain
• receptors (nocioceptors) to activate nerve messages

• •Transduction—cell damage stimulates pain receptors (nocioceptors) to activate nerve messages
• •Transmission—peripheral nerves carry in messages to the CNS
• •Perception— CNS recognizes & interpretes pain sensations
• •Modulation- CNS releases neurotransmitters in response to pain to prevent further tissue damage

• (named after morpheus greed god of dreams)
• a prototype of strong opioid analgesics. produces analgesia
• sedation
• euphoria
• respiratory depression
• cough supression
• supression of bowel motility

• causes drowsiness
• mental clouding
• anxiety reduction
• sense of well -being
• respiratory depression
• constipation
• urinary retention
• orthostatic hypotension
• emesis
• cough supression
• biliary colic

contant, dull sharp, acts at mu receptors

• respiratory depression- serious resp rate should be obtained prior to administration. if rate less than 12/min hold
• -avoid drugs that speeds this process
• constipation-can be given with stimulant laxative to elleviate constipation
• orthostatic hypotension- from morphine induced release of histamine causes vasodialtion
• urinary retention- increases bladder sphincter tone. suppresses awareness of bladder-intervention palpate bladder every 4-6hours. notify prescriber
• cough suppression-
• biliary colic
• emesis- nausea and vomiting
• Miosis

nausea and vomiting

take less at more frequent intervals

pupillary constriction

All Oral, Iv, IM

cross blood brain barier, morphine is inactivated by the hepatic system, but morphine is not lipid soluble. oral doses must be larger because of the first past effect

an abstinence syndrome will occur if drug use is abruptly stopped

• can cause further respiratory issue- use with caution in patients with asthma, emphysema, kyphoscoliosis, extreme obesity, chronic pulmonale
• can cause respiratoryy depression in neonate- resp depression can be reversed with naloxone.
• head injury- use with caution

• coma
• respiratory depression resp as low as 2-4b/min
• pinpoint pupils - pupils may dilate as hypoxia sets in rpolonged hypoxia results in shock

give opiod antagonist (naloxone ( narcan), or nalmefene (revex) longer acting than naloxone), and ventillary support

• resp rate- resp below 12 hold drug
• bp - if below pretreatment value
• pulse - if below pretreatment value

Sublimaze- high potency 100 times that of morphine metabolized by cyp3a4 isozyme of cp450

• rapid action, short duration
• lipid soluble crosses blood brain barier

• like morphine, acts on mu and delta receptors.
• effective orally, long duration action. treats pain and treat opioid addicts.
• effects QT interval- may cause fatal dysrhythmias
• use with caution in patients with patients taking other QT polonging meds (amiodarone, quinidine, erythromycin, tricyclics

• take as directed
• avoid cns depressants benzos, alcohol and other opioids drugs that inhibit CYP3A4 (clarithomycin, fluvoxamine, fluconazole, and nelfinavir

2.5 to 20mg q 3 to 4 hours as needed

strong opioid agonist similar to morphine, used in europe US prohibits use

strong opiod agonist for moderate to severe pain

aspirin, ibuprofen

gastric ulceration, acute renal failure, and bleeding

• ihibits cyclooxygenase
• celebrex
• ibuprofen

the nonacetylated salicylates ie magnesium salicylate. COX -2 inhibitors such as celecocib (celebrex)

Does not inhibit COX in periphery, lacks anti inflammatory actions, does not inhibit platelet aggregation and does not promote gastric ulceration, safe for patients with thrombocytopenia

Causes ulceration, bleeding

• alcohol and wafaran (anticoagulant)
• with alcohol causes liver damage
• wafarin increases risk of bleeding inhibits wafarin metabolism and causes it to acumulate to dangerous levels

pure opioid agonists

methadone (dolopine, methadose), Levorphanol (Levo-dromoran)

protective sensory warning system

Peripheral tissue

provide an early warning system about impending or actual tissue injury which threathens physiological intergrity of the individual

• NSAIDS - tradition and COX 2 inhibitors
• Opiod- agonist and agonist /antagonists, adjuvant drugs, opioid antagonists

• They decrease production of inflammatory and chemicals (prostaglandins, prostacyclin, thromboxane A) by inhibiting Cyclooxygenase production.
• they reduce inflammation and nocioreceptor stimulation that cause pain

• COX-1
• COX - 2

• Cox -1
• Gastric protection- prostaglnadins-keep stomach from being irritated
• reduce gastric acid
• increase bicarbonate and mucus production
• promotes mucosal blood flow
• promotes platelet aggregation- thromboxane A
• Vasodilation with improved renal blood flow- prostacyclin
• uterine contraction drugin labor- prostaglandins

• tissue inflammation- prostaglandins
• fever - central effect of prostaglandins/prostacyclin
• CNS sensitization to pain
• Tissue/blood flow changes promoting colorectal cancer development

• good for fever not much antiinflammatory, higher safety index than NSAID, safer for stomach, but not liver
• acts primarily in brain. limited peripheral activity

• means you take drug once it hits the ceilling taking more will not increase effectiveness.
• thus increasing dose will increase toxicity without improving analgesia.

• increse b/p by decreasing renal blood flow and produce gastric irritation through decreased GI mucus protection.
• inhibit platelets contributing to bleeding risk.

If NASAID is affecting bp don't take. Aspiring keeps platelet from aggregating

• GI effects
• bleeding
• renal impairment
• salicylism- toxicity metabolic acidosis
• hypersensitivity reactions- hive
• bronchoconstriction
• rhinorrhea
• nasal polyps

• give with adequate flui/food to prevent gastric irritationk, monitor signs of gastri irritation/bleeding
• monitor bp for hypertension

• inhibit prostaglandins, thromboxane A and prostacyclin production in both CNS and peripheral tissue
• Reduces inflamation
• produces peripheral and central analgesia
• antipyretic effect in hypothalamus

• anti-inflammatory and analgesic for arthritis, headache, musculoskeletal pain; dysmysmenorrhea
• used in MI and stroke
• Treatment of fever in adults
• pushes body to metabolic acidosis

irreversibly inhibits platelet aggregation; widely used in antiplatelet agents in losw doses to prevent MI and Stroke (325mg)

• abrsorbed in small intestin
• rectal route is less reliable and is rapidly converted to sallicylicacid; active metabolite in the liver
• highly albumin bound; crosses blood brain barrier and placenta

po or RP(rectal syppository)

• anticoagulants- wafarin and heparin effects potential with increased risk of bleeding.
• alcohol and glucocorticoids - increases risk of gastric ulceration and GI bleeding
• ACE inhibitors and angiotensin receptor blockers concurrent reduction in renal blood flow can lead to renal failure

• children with influenza/viral illness- risk for reye's syndrome (hematic encephalopathy
• pregnancy cat D;increased risk of bleeding and anemia; fetal grwth retardationd
• severe renal disease
• allergy- may worse asthma or contribute to nasal polyps in sensitive individuals.

• Metabolic acidosis
• hyperventilation, tinnitus
• nausea/vomitting
• abdominal pain
• sweating
• renal impairment

• it intefers with energy use for cellular ATP formation leadin to : hyperthermia
• increased production of lactic and pyruvic acid
• increased co2 production and respiratory acidosis

• respiratory support
• colling to treat hyperthermia
• Iv hydration/sodium bicarb
• hemodialys

• Propionic Acid Derivative NSAID
• Least likely to cause GI irretation/bleeding

• analgesi,
• antipyretic
• antiinflammatory effects

• fever in adults and children
• moderate to mild arthritis

PO, oral suspension or pediatric drop

2400mg/day

GI and renal toxicity with long term use or overdose

can interfere with anti platelet activity of aspirin and increase CV risk

a propionic acid derivative ; that is higlhy cox 1 selective enzyme; some anti platelet effecs

it has a long half life

• fever, arthritis
• moderate pain
• headaches,
• dysmenorrhea

gi bleeding and renal failure

it can be conbined with proton pump inhibitor (lansaprazole) to reduce bleeding

parenteral NSAID - potent analgesia with limited anti inflammatory effect

for actue/postoperative pain expecially orthopedic or gynecological procedures.

• IV push should be diluted with normal saline and given slowly to reduce vein irritation.
• Deep IM in large muscle to reduce tissue irritation. Ztrack

not longer than 5 days

with opioid agonist for better postoperative pain control.

• Centrally acting- inhibition of prostaglandin production primarily in CNS
• less peripheral antiinflammatory effects than other NSAID
• NO GI irritation
• No iffect on renal blood flow or platelets

• pain or fever, less effect on inflammatory or dysmenorrhea,
• can be used in pediatric and pregnancy; safe for those who have aspirin allergy

readily absorbed orally ; metabolized by the liver and excreted renally.

few reduce doses with liver disease

• alcohol no more than 3 drinks
• anticoagulants- warfarin- bleeding risks

nausea/vomitting, abd pain, liver failure from toxic metabolite- metabolites injure liver tissue

• acetylcystein (mucomyst) po or IV to break down the toxic metabolite; start within 10 hrs of OD
• Serever overdose require liver transplant
• chronic overdose - bone marrow suppression

• nocioceptive pain in soft tissue
• not shapr neuropathic pain - since calcium channels in nerves are not effectively blocked by opioid binding

give higher dose opiod with adjuvant drugs

opiod agonist

bindst and activates endogenous opiate receptors, primarily mu receptors in CNS and peripheral tissue

• for mederate to severe pain
• relieves anxiety
• antitussive
• dilates pulmonary vasculatrue and relieves left ventricular heart failure. dyspnea and pulmonary edema in congestive hear failure and Mi
• antidurrheal

PO, MI, IV, SC, Ipidural and intrathecal routes

• small amount morphine is water soluble.
• much of oral dose is loss in first pass. thus oral doses are larger

prolongs action

more neurotoxic effects including myoclonus (muscle jerks and confusion

• respiratory disease
• use of depressants
• head injury
• pregnancy and childbirth
• hypotension
• all blood trhough GI goes through liver

never crush because it causes overdose

• sedation/rep depression
• hypotension- histamine effects- itching, flushing, temporary flair reaction with undiluted IV admin
• vomitting/nausea
• urinary retention
• pruritis/itching
• constipation
• pinpoint pupils
• with morphine you have more histamine release

when pure opiod agonist given for 2-3 weeks causes an increase in opioid receptor sites in the CNS

• rhinorrea, goosebups
• tremmors,
• gi upset
• diarrhea
• irritability
• anxiety

a state of ongoing drug craving with excalating use unrelated to pain control;

potent semi synthetic opioid agonist use as pare nteral alternative to morphine for moderate to severe acute pain

• useful if tolerance is build to morphine or morphine is not tolerated
• has less itching then morphiene

similar to morphine

• very poten synthetic opioid receptor agonists acts mostly on mu receptors in the brain.
• has rapid onset; short duration activity
• lipid soluble so it crosses membranes

muscle rigidity occurs, laryng ospams if given with enzyme inhibitors they can increase drug concentrations

oralet lollipop for anesthesia induction and breakthrough cancer pain.

• higly lipid soluble
• dose in micrograms

• cannot be cut
• hyperthermia may increase rate of absorption
• avoid heat on patch
• decreased perfusion may impair absorption

• handle with gloves
• apply to intact skin of upper trunk
• rotate sites; date/time when applied
• dispose of as biohazard

• acts on mu and delta receptors in CNS
• used primarily for treating opioid addiction adn chronic pain management. low cosst
• less euphoria /dysphoria than morphine
• long half life

late resp. depression and cardiac arrhythmias (prolonged QT interval) can occure

opioid agonis used for moderate pain or non productive cough

metabolized in liver; genetic variation on metabolism

lower doses

• nausea /vomitting most frequent problem
• it is effective in cough syrup

• semi-synthetic opiod for moderate pian - analgesia equivalent to codeine
• often combined with acetaminophen (percocet ) or apirin (percodan)

PO imediate release, long acting controlled relase

risk for acetaminophen/asmpirin toxicity in pts using high dose

• most prescribed
• semi synthetic opioid used for moderate pain and cough ; efficacy as that of codeine

combined with acetaminophen orally. does not need new written prescription each time dispensed.

avoid driving, hydration, constipation, execessive NASAI.

• agonist/antagonist drug acts by activating kappa receptors in spinal cord and blocks mu recpeotr in the brain
• less risk of resp depression since less activity on mu recpeotrs in brain

dysporia, nightmares, and anxiety from excessive kappa stimulation

opioid agonist and opioid agonist/antagonist should not be given together because the antagonist will block effectiveness of opioid agonist (agonist/antagonist- buprenorphine)

opiod antagonist- blocks opiod receptors in opiod overdose.

respiratory depression, sedation Miosis (constricted pupils)

IV. adminiter dilute in saline for IV give slowly assess for response.

because naloxone will leave system before opoid and send pt back to rep depression

• anticonvulsant
• antidep
• local anesthesia

• respiratory depression
• Nausea/vomittin
• orthostasi
• urinary retention
• itchin (pruritis)
• constipation

• assess pain
• monitor resp/bp/pulse/sao2 prior to giving opioid
• stop med if reps<12/min, encourage deep breathing get o2 order if needed
• re assess client 30 minute after iv med or 1 hour po
• use safety with ambulation
• i and o breath sounds
• abdomen for distention or nausea

if resp <10 or physical stimulation insuficient.

• due to receptor stimulation and GI motility
• nausea and vomiting is most common with codeine
• can premedicate with anti emetics initially

• hypotension associated wth vasodilation and histamine release
• more severe with fluid deficit --IV and oral hydration help to minimize assess b/p before ambulation chage position slowly
• monitor i and o.

• due to increased tone of urinary sphincter and decreased awareness of bladder distention
• is most sever with epidural/spinal admin
• monitor i and o
• catherter if neededo
• often temporary
• tr

• antihistamine or a very dilute naloxone infusion may be used cool compresses/lotion;
• swithc opiod
• itching less frequent with hydromorphone (dilaudid)

• opioids directly decrease GI peristalsis for as long as client are taking them.
• give stool softener (docusate) and stimulant laxative (senna) often combined for treatment
• lactulose may be added
• fiber, fluids and activity helpful

recurrent rather than acute pain.

• used for acute postoperative trauma
• morphine, fentanyl, hydromorphone are used
• programable
• patient activated for breakthrough dosing
• use effectively age 8 and older

• review physican order
• establish iv access
• obtain/;rogram pump
• give loading dose and client teaching
• assess resp
• maintain Iv infusion to deliver drug doses
• assess client ability to use effectively
• document pain
• cosign waste drug and when D/C'd

• used for lower extremeties surgery, childbrith refracory or other therapy
• catherter place in epidural spac outside dural covering of spine
• small doses of opiod and or local anesthetis diffuse across dura and bind to opiate receptors in spinal nerve

• less CNS and respiratroy depressant effects than IV route since lower boses
• small risk for bleeding if client anticoagulate with epidural placemtn

• monitor respiratory rate, depth and level of sedation hourly
• vital sign q 4 hours
• assess pain
• assess dressing for drainage q shift
• asses catherter for dislodgement q shift
• assess sensation/stength of lower extremites if local anesthetic used in infusion.