Opioid Treatment

HIGH dose

Analgesia

Morphine

r

strong opioid agonistIVundergoes significant first pass metabolism when taken orally

AE:

CNS

respiratory depression

drowsiness

N/V

tolerance & dependence

pneumonia

miosis

r

= constrictionexception: Meperidine

CV

postural hypotension

GI/Kidney/Gallblader

r

increased tone

constipation

painful urine retention

painful biliary spasm

other

prolonged labor

pruritis

drug interactions

w/ SSRI, MAOI, or TCA (incr. serotonin)

r

cause "serotonin syndrome"

drugs that add to sedation or cause respiratory depression

preanesthetic

Fentanyl

r

strong opioid agonistrapid onset, short durationIV100x more potent than morphineused during labor, as preanesthetic, and for pre-, intra-, post-op, & breakthru paincan use for "balanced anesthesia" (ie to supplement the analgesia and sedative-hypnotic effects of NO and halothane)Fentanyl + droperidol = Innovar (induces neuroleptanalgesia, permitting wakeful state when cooperation is needed during surgery)can be given in transdermal patch or lollipop for breakthru pain

AE:

severe musc. rigidity

r

on rapid IV administration

minimal cardiac depression

minimal respiratory depression

minimal constipation

Codeine

r

weak opioid agonistalso Oxycodone, Hydrocodone, Dihydrocodeinegets its analgesic activity from conversion to morphine (10% is converted)good oral bioavailability (unlike morphine)less respiratory depression than morphinehydrocodone + acetaminophen = Vicodin/Lortaboxycodone + acetaminophen = Percocetoxycodone + aspirin = Percodan

AE:

tolerance & dependence

r

less than morphine

constipation

Meperidine

r

strong opioid agonistno effect on cough reflexlargely replaced by other opioids

AE:

Overdose: CNS excitation, seizures

r

due to formation of N-demethylated metabolite (normeperidine) -- no analgesic activity

constipation

r

less than with morphine

vomiting

r

less than with morphine

midriasis

r

d/t weak anticholinergic activitynote: this is OPPOSITE from what you would expect with an opioid!

drug interactions

w/ MAOI

r

"serotonin syndrome"severe restlessnessexcitementfeverseizuresdelirium

neuropathic pain

Tramadol

Tramadol
r

for neuropathic painenhances 5-HT and NE neurotransmission by blocking reuptake (makes you happier)actions partially reversed by naloxoneNO effect on respiration

AE:

increased risk of seizures

r

CONTRAINDICATED IN PATIENTS WITH EPILEPSY OR PATIENTS TAKING MAOI'S (lower seizure threshold)

moderate pain

Pentazocine

Pentazocine
r

for moderate pain (has analgesic ceiling)resistant to naloxone reversal

AE:

may increase BP

r

CONTRAINDICATED FOR MI's

dysphoria

anxiety

hallucinations

Buphrenorphine

Buphrenorphine

r

for moderate pain (has analgesic ceiling)resistant to naloxone reversal

AE:

dysphoria

anxiety

hallucinations

Anesthesia

r

very high dose

Morphine

r

less constipating effect than codeineno analgesic activityno dependence riskAE:dizzinessnauseadrowsiness

Fentanyl

LOW dose

Cough Suppression

Codeine

AE:

tolerance & dependence

constipation

overdose: seizures

Dextromethorphan

r

less constipating than codeineno analgesic activityno dependence risk

AE:

nausea

dizziness

drowsiness

Diarrhea Suppression

Diphenoxylate (+ atropine)

r

weak opioid agonistminimal dependence riskcombined with atropine to decrease misuse by IV route

Loperamide

r

weak opioid agonistminimal dependence riskpoorly absorbeddoesn't cross BBB

Codeine

Morphine

Dyspnea

r

for dyspnea associated with acute pulmonary edema secondary to acute left ventricular failure

Morphine

r

morphine's ability to relieve SOB is due to:1) decreased peripheral RESISTANCE2) slowing of RESPIRATION3) relief from ANXIETY

Overdose tx

r

both are pure competitive opioid antagonists --> can preciptate opioid withdrawal

(IV)

Naloxone

r

to reverse opiod overdose and toxicityshort duration of action (so you need to maintain vigilance around the patient - they might go back into opioid-induced respiratory depression)only partially reverses tramadoldoesn't reverse pentazocine or buphrenorphine at all

(oral)

Naltrexone

r

to dx opioid dependencecan also reduce craving for alcoholNaltrexone + Clonidine or Buprenorphine = rapid opioid detox

Phycial Dependence tx

Methodone

r

strong opioid agonistorallong duration, so less severe withdrawal syndromealso has good analgesia for cancer and neuropathic paincross tolerance decreases heroin's reinforcing propertiesno euphoria

Buprenorphine

r

in addition to analgesia, also tx opioid addictionsafer and as effective as methodonealso used to tx depresion and in smoking cessation programs

Not approved for clinical use!

Heroin

r

strong opioid agonistmore lipid soluble and faster acting than morphineeuphoria