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75 Cards in this Set
- Front
- Back
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3 precursors of endogenous
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proenkephalin, pro-opiomela
nocortin---endorphins, prodynorphin---dynorphins |
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receptors?
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mu (morphine)
kappa (in spinal cord predominately) (dynorphin) delta (enkephalin) |
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prototype of opioid?
source and structure? |
morphine
From opium poppy (papaver somniferum) |
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All produce what?
Most can do what? |
Tolerance and cross tolerance!
most can support the dependence of another |
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big adverse effect?
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Constipation
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What happens when stopped suddenly?
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withradwal syndrome
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what is the opioid antagonist?
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naloxone
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Effect on specific body systems?
mental? |
a) euphoria
b) mental clouding |
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GI?
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Nausea and vomiting
(stimulate CTZ) This can be blocked by naloxone |
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Lungs?
mech? |
Respiratory depression
Morph causes release of histamine and morph decreases the brain resonse to c02 |
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what to cough?
What to pupil |
antitussive
myosis |
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what to bladder
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urinary retention
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inhib gonadotropin release
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decrease lh and fsh release
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cardiovascular
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postural hypotension
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what to cough?
What to pupil |
antitussive
myosis |
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morphine IV or oral
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mostly IV but some oral
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what to bladder
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urinary retention
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does morphine get into brain well?
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NO!
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inhib gonadotropin release
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decrease lh and fsh release
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Which really get into brain?
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Heroine fentanyl codeine
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cardiovascular
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postural hypotension
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metab
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glucuronide conjugation
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morphine IV or oral
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mostly IV but some oral
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Excretion
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urine
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does morphine get into brain well?
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NO!
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Tolerance because?
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internalization of receptor; no metabolic tolerance
opioid withdrawal not life threat |
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Which really get into brain?
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Heroine fentanyl codeine
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metab
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glucuronide conjugation
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Excretion
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urine
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Tolerance because?
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internalization of receptor; no metabolic tolerance
opioid withdrawal not life threat |
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withdrawal syn
drug to help? |
first symp 8-12 hours, peak 36-72 hours
diarrhea, vomit, chills fever lacrimation, rhinorrhea, tremor, kicking of legs Clonidine |
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Comparison of opioid
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yes
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Natural
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morph, codeine
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partial synthetic
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heroine, naloxone
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synthet
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levophanol, meperidine, methadone
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Activity
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yes
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agonist
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morphine
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antagonist
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naloxone
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agonist/antagonist
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will be described later
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codeine
uses |
orally active has only 1/10th analgesic property of morphine;
antitussin and analgesic |
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Heroine (diacetylmorphine)
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Oral absorpt is variable. Crosses bbb well
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Oxycodone (oxycontin)
hydromorphone (dilaudid) |
same effects as morph but have higher oral activity.
Also, hydromorphone is 10x more potent |
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Apomorphine
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has little analgesic activity but has dopamine agonist activity so used to induce vomiting by direct action on CTZ
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Dextromehtorphan
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very little analgesic or addictive activity; used as antitussant
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synthetic drugs
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yes
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meperidine (demerol)
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shorter duration of action than morphine and is used for shorter analgesia. orally active, 1/10th potent of morphine
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fentanyl
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oral active but used iv in anesthesia; short duration, lipid soluble, redistribution is major means of termination of action; 80x more potent than morphine
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fentanyl uses?
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anesthetic induction
sole anesthetic for cardio surg neuroleptic state, combined with drperidol |
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alfentanil and sufentanil
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similar to fentanyl
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methadone
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same action and potency; but long half life, orally active
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LAAM
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long acting congener of methadone that is used for maint treatment of heroin addiction
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so put methadone and laam together in head
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yes
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propoxyphene
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very similar to codeine so remember them together
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loperamide (imodium) and diphenoxylate
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only for treatment of diarrhea
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opioid overdose
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coma
depressed respiration miosis |
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tx
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restore respiration,
administer naloxone (but naloxone duration is only few hours so can wear off before cure) |
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interactions
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sed/hypnotics, ehtanol, mao inhib, tricyc antidepress, tranquilizers
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opioid antagonists and agonist antagonists
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yes
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pure antagonist
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naloxone: works on all receptors
short duration of action drug of choice for opium overdose |
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another pure antagonist
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naltrexone,
24 hour duration orally active |
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agonist/antagonist
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yes
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Pentazocine
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used as an analgesic for mild to moderate pain
weak mu antag, so blocks morph analges and induces withdrawal in physically dependent... |
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does pentazocine block morphine respiratory depression?
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NO!
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pentazocine agonist where?
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agonist at kappa receptors and sigma recept
1. spinal analgesia that is as effective as morph, 2. resp dep less severe 3. dysphoria and hallucinations with repeated high doses |
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withdrawal sympt?
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milder than morphine withdrawal
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can you block the kappa effects?
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yes with naloxone
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Nalbuphine and butorphanol
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analgesic for moderate to severe
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antagonist?
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mu antagonist
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agonist
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kappa
produces effective analgesia low incidence of psychotomimetic effect because don't bind SIGMA milder withdrawal Can be blocked by naloxone |
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Buprenorphine
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analgesic for mod to severe pain
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agonist
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partial mu (effects are slow in onset and long lasting)
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what are these effects?
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analgesic
respiratory depression; only minor problem with this drug euphoria miosis mild morphine type abstinence syndrome |
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antagonist?
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induces an morph abstinence syndrome
also, kappa antagonist |
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antag'd by
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naloxone
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another something useful
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can replace methadone
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