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35 Cards in this Set

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List two types of analgesics
(1) narcotic analgesics -- opiods - have CNS effect

(2) non-narcotic analgesics -- NSAIDs - Do Not have CNS effect
Describe two components of pain
(1) physcial: perception, discrimination of pain

(2) psychological: reaction to pain
How do opioids change the threshold of pain?
Opiods raise the threshold for pain perception and alter the affective response. Opioids relieve both aspects of pain.
List 4 sites of opiod action
(1) thalamus
(2) limbic system
(3) brain stem
(4) spinal cord
Describe opiod action at the spinal cord.
Epidural opiod analgesia is segmental, rapid in onset, long lasting, produces few side effects, and no physical dependence.
The 3 opioid receptors plus the other one.
Mu, Kappa, Delta
Sigma - kind of is.
Compare and contrast naloxone and naltrexone.
Both are pure, competitive opiod antagonists.

Naloxone has a shorter duration of action (1-4h) compared to naltrexone (24h). Given for opioid overdose

Naloxone is the drug of choice in treating opiod OD.
Naltrexone is given to drug users so if they take street drugs they won't have euphoria.

Uses of pure antagonists: treatment of opioid overdose, diagnose addiction (pt will have withdrawal symptoms), treatment of compulsive use
Morphine
Prototype of opioids
Uses:Analgesic, treatment of cough (antitussant - suppress the cough reflex) and Antidiarrheal (causes constipation!)
-Usually given by IV
Besides the 3 therapeutic uses of morphine, list its other effects on the body. (Essentially its side effects
(1) mood changes - Euphoria, Mental Clouding (drowsy, lethargic, can't think)
(2) nausea & vomiting - opiods stimulate the chemoreceptor trigger zone (CTZ)
(3) respiratory depression - morphine causes decreased response of the brain stem respiratory neurons to CO2 --> decreased breathing. Also caused bronchoconstriction.
(4) miosis - constriction of pupil
(5) urinary retention - increased ADH release --> water retention
(6) dec LSH, FH release - so decreased estrogen in females and testosterone in males
(7) postural/orthostatic hypotension - due to a/v dilation due to histamine release and depressed vasomotor and adrenergic tone
8) GI effects - constipation!!
9) antitussant - inhibits cough reflex
Describe pharmacokinetics of morphine.

-absorption
-solubility
-metabolism
-excretion
Morphine

--variable oral absorption so administered parenterally
--low solubility so little enters brain

--glucuronide conjugation is major metabolic pathway

--excreted as glucuronide conjugate in urine
TRUE or FALSE

All tolerance to opiods is considered a metabolic tolerance.
FALSE

All tolerance to opiods is pharmacodynamic, meaning that there is decreased opiod receptors from down-regulation.
Describe the onset and symptoms of opiod withdrawal.

Is it life threatening?
What drug can be used to decrease these symptoms?
Morphine withdrawl symptoms appear 10hr after last dose and will peak between 36-72hr.
Symptoms include vomiting, diarrhea, chills, fever, tremor, and kicking of legs, increased tears (watery eyes)

It is not life threatening.
Clonidine (alpha2 agonist) can decrease symptoms.
Opioids
Uses: Analgesia - most can relieve all types of pain and are reserved for moderate to severe pain, Antitussive (low doses), Antidiarrheal
Sources:
-naturally occuring-from opium poppy (morphine, codeine)
-Partial synthetic (heroin, naloxone)
-Synthetic (levorphanol,merperidine, methadone)
Codeine
Naturally occuring opioid
-orally active but only 1/10th as analgesic as morphine.
-Used as antitussant and as analgesic in combination with aspirin or acetminophen
Heroin (diacetylmorphine)
Opioid
-Parenteral absorption. (IV -drug users)
-crosses BBB due to high lipid-solubility
-Not used clinically in US
Oxycodone
Opioid
-same effects and potency as morphine.
-But higher oral activity (can take as pills)
Hydromorphone (Dilaudid)
Opioid
-same effects as morphine but higher oral acitivity and 10X more potent.
Apomorphine
Opioid
-has little analgesic activity
-Causes respiratory depression
-Used to induce vomiting -direct action on CTZ.
-used in pts that took toxins, poisons, etc
Dextromethorphan
Opioid
-very little analgesic or addiction activity.
-Used as antitussant
-less drowsiness or GI effects than codeine
Meperidine
Synthetic Opioid
-Shorter duration of action than morphine
-used for shorter analgesia
-Orally active
-1/10th potentcy of morphine
-Used for women in labor
Fentanyl
Synthetic Opioid
-orally active but IV in anesthesia
-80 times potency of morphine
-Short duration of action (very lipid soluble so redistribution is major means of termination of action)
-Uses: Anesthetic induction, sole anesthetic for cardiac surgeries, Neuroleptic state.
-Neuroleptic state - when combined with droperidol = Innovar --> relaxation of the muscle. Used for outpatient surgeries
-Alfentanil and Sufentanil are similar in action and potency to Fentanyl
Methadone
Synthetic Opioid
-orally active
-same actions/potency of morphine
-Long duration of action with half-life of 15 hours
-Uses: Chronic pain, methadone maintenance
LAAM (L-alpha-acetyl-methadol)
Synthetic Opioid
-long-acting twin of methadone.
-Used for maintenance treatment of heroin addiction.
-Orally active
Propoxyphene
Synthetic Opioid
-1/10th potency of morphine.
-used as antitussant or analgesic in combination with aspirin or acetaminophen (like Codeine)
-Orally active
Diphenoxylate (Lomotil)
Synthetic Opioid
-Only Oral
-Treats diarrhea
-Has abuse potential so it is combined with atropine in preparation of Lomotil.
Loperamide (Imodium)
Synthetic Opioid
-OTC drug for diarrhea
-As effective as Diphenoxylate in controlling chronic diarrhea but has less abuse potential.
-Poorly absorbed after oral administration and acts on intestinal musculature to inhibit motility.
Opioid Overdose
Classic triad of symptoms: Coma, Depressed respiration, pinpoint pupils!!!!!
Overdose Treatment:
-Restore respiration (O2 but not pure O2 - need some CO2)
-Administer Naloxone
-Watch pt because naloxone half life is much shorter than opioids
List the specific natural or partial-synthetic opiod that fits the following..

--higher oral activity vs. morphine but same effects & potency

--higher oral activity & effects as morphine but higher potency

--higher oral activity vs. morphine but has 1/10 the potency
(1) higher oral activity + same effects + same potency = oxycodone

(2) higher oral activity + same effects + higher potency = hydromorphone

(3) higher oral activity + 1/10 potency = codeine
List the specific synthetic opiod that fits the following...

--used for shorter analgesia & has 1/10 potency of morphine

--same potency as morphine but has long half-life of 15h

--sole anesthetic for cardiac surgeries

--treats heroin addiction
(1) short analgesia + 1/10 potency = meperidine

(2) same potency + halflife of 15hr = methadone

(3) cardiac surgery anesthetic = fentanyl

(4) treats heroin addiction = LAAM
This synthetic opiod is used as an IV anesthetic and has 80x the potency of morphine.
Fentanyl
Name the specific drug that fits the following description..

(1) combined with droperidol to produce neuroleptic state
(2) anti-diarrheal opiod that is combined with atropine
(3) drug of choice for opiod overdose
(4) sigma agonism produces dysphoria
(5) primarily an anti-tussant
(6) 10x more potent than morphine
(7) decreases opiod withdrawal symptoms

(8) analgesic for moderate - severe pain w/ kappa antagonism
Name the specific drug that fits the following description..

(1) combined with droperidol to produce neuroleptic state = fentanyl

(2) anti-diarrheal opiod that is combined with atropine = diphenoxylate

(3) drug of choice for opiod overdose = naloxone

(4) sigma agonism produces dysphoria = pentazocine

(5) primarily an anti-tussant = dextromethorphan

(6) 10x more potent than morphine = hydromorphone

(7) decreases opiod withdrawal symptoms = clonidine

(8) analgesic for moderate - severe pain w/ kappa antagonism = buprenorphine
Opioid Drug Interactions
-Additive or synergistic effects to produce CNS and/or respiratory depression - can occur with: sedative-hypnotics, ethanol, monoamine oxidase inhibitors, tricyclic antidepressants and major tranquilizers
Pentazocine
Opioid agonist-antagonist
-Used as analgesic for mild to moderate pain
-Weak mu antagonist - blocks morphine analgesia, induces opioid withdrawal in physically dependent. Doesn't block morphine respiratory distress.

-Agonist at kappa and sigma receptors: effective analgesia w/ limited respiratory depression, mild abstinence syndrome, Psychotomimetic effects (dysphoria, hallucinations)
-All the kappa agonist effects are blocked by naloxone
Nalbuphine and Butorphanol
Opioid agonist-antagonist
-analgesic for moderate to severe pain
-Mu antagonists - blocks morphine analgesia, induces opioid withdrawal in physically dependent. Doesn't block morphine respiratory distress.

-Kappa agonist: effective analgesia with limited respiratory depression, low incidence of psychomimetic effects, mild abstinence syndrome
-antagonized by naloxone
Buprenorphine
Opioid Agonist-Antagonist
-Analgesic for moderate to severe pain
-partial agonist at mu receptors- effects it induces are slow in onset and long lasting : analgesic, respiratory depression, euphoria, miosis, mild abstinence syndrome

-Kappa antagonist
-Antagonized by Naloxone
-Potential replacement for methadone as maintenance in opioid drug abusers.