- Methadone (Dolophine) - Meperidine (Demerol) - Propoxyphene (Darvon) - fentanyl (innovar)

Opioid antagonist other name is narcan - reverses effects of opioid agonists - precipitates withdrawal in users

opioids Flashcards by Harris Jordan

opium derivatives

morphine 10%

Codeine <1%

Thebaine

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Harrison Narcotic Tax Act of 1914

US law that regulated and taxed the production, importation, and distribution of opiates. eventually was extended into modern drug laws.

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US Drug Schedule I

No Medical use

LSD, MDMA, heroin

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US Drug Schedule II

High abuse potential

amphetamine, morphine

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US Drug Schedule III

Moderate abuse potential

ketamine, codeine

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US Drug Schedule IV

Mild Abuse Potential

benzodiazepines

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US Drug Schedule V

Low abuse potential

buprenorpine

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semisynthetic Opioids

heroin (diacetylmorphine)

- hydromorphone (Dilaudid)

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synthetic Opioids

Methadone (Dolophine)
Meperidine (Demerol)
Propoxyphene (Darvon)
fentanyl (innovar)

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Endogenous opioids

enkephalins
endorphins
dynorphins

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criteria for opioid agonist classification

Exerts effects similar to morphine

Acts at opioid receptors

Effects blocked by antagonist, Naloxone

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Naloxene

Opioid antagonist
other name is narcan

reverses effects of opioid agonists
precipitates withdrawal in users

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Naltrexone (Trexan)

long acting form of opioid antagonist

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opioid administration

weak base

oral
parenteral
inhalation
intranasal

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opioid administration

onset and duration of action

depends on preperation
route of administration
metabolism

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opioid receptors

metabotropic, inhibitory

inhibits formation of cyclic amp

post synaptic inhibition - k+ Efflux

Presynaptic inhibition - transmitter release

Autoreceptor activation - less transmitter release`

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presynaptic inhibition

kappa receptors
-
Ca++ channels close
-
Reduced transmitter release

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Autoreceptor activation

Autoreceptors
-
Ca++ channels close
-
Reduced Transmitter release

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endogenous opioids

endomorphin - Mu receptor

Enkephalin - Proenkephalin precursor - Mu, Delta receptor

Dynorphin - Prodynorphin precursor, Kappa receptor

Endorphin - POMC precursor - Mu, Delta receptor

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opioid Acute effects

cortex

sedation
drowsiness
relaxation

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opioid Acute effects

(Mesolimbic DA pathway_

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Euphoria

opioid Acute effects

Meulla

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Pupillary constriction
Nausea, Vomiting
Cough Suppression
Respiratory Suppression

opioid Acute effects

Hypothalamus

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Hypothermia

Reduced Sexual Drive

opioid Acute effects

many areas

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analgesia

opioid Acute effects | intestine

Constipation

sites of opiod induced analgesia

``` Spinal -sensation Brain stem -Sensation Limbic, Thalamic and Cortical -Perception ```

``` opioid overdose (central nervous system) ```

sleepiness | loss of consciousness

``` opioid overdose (Pupils) ```

Widening

``` opioid overdose (Skin) ```

Coldness Clamminess Blueness

``` opioid overdose (Muscular) ```

Seizures

``` opioid overdose (Breathing) ```

Slowed Shallow Stopped occurs in medulla (pontine respiratory centers)

opioid thereapeutic use

``` analgesia anesthesia substance abuse treatment cough suppression Reduce intestinal ```

Opioid Tolerance | cellular

Pharmacodynamic Decrease in opioid receptors increase in adenylyl cyclase

opioid tolerance | situational

contextual context in which drug is taken induces tolerance

opioid physical dependence

withdrawal syndrome opposite of acute effects not life threatening 1 - 2 weeks in duration

opioid psychological dependence

powerful reinforcer intense craving, 'rush' increases release of dopamine in accumbens

opioid acute and withdrawal effects

withdrawal effects are literally the exact opposite of acute effects

Opioid pleasurability

they inhibit GABA neurons in the VTA which Disinhibit the dopamine system

Drug therapies for opioid dependence

methadone buprenorphine naltrexone Clonidine Mixed Preperations

Drug therapies for opioid dependence | methadone

full agonist administered daily, typical opioid effects but milder, reduces effects of heroin and morphine

Drug therapies for opioid dependence | Buprenorphine

Partial agonist at mu receptors, typical opioid effects but milder, reduced risk of overdose, reduced intensity of withdrawal

Drug therapies for opioid dependence | naltrexone

opioid antagonist blocks effects of opioids,precpitates withdrawal in users, blocks life threatening effects

Drug therapies for opioid dependence | Clonidine

Noradrenergic alpha autoreceptor agonist, suppresses physical withdrawal symptoms during week of withdrawal

Drug therapies for opioid dependence | mixed preperations

various combinations of medications are under study

dealin drugs

people love dealin drugs, even when their not on heroine any more

opioid overdose signs

Deep slow snoring or gurgling Heavy nod, not responsive to stimulation - apply sternal rub (rub breastbone hard with knuckles) slowed breathing cyanotic - bluish lips and nail beds -pinpoint pupils

risks of opioid overdose

loss of tolerance Mixing drugs using alone variation in strength of 'street' drugs Serious illnesses

risks of opioid overdose | loss of tolerance

increased risk after period of abstinence

risks of opioid overdose | mixing drugs

mixing opioids with other drugs, especially depressants such as benzodiazepine or alcohol

risks of opioid overdose | using alone

when using drugs alone there is no one present to see signs of overdose

risks of opioid overdose | variation in strength of 'street' drugs

street drugs may vary in strength and effect based on purity of the drug and the amount of other ingredients used to cut the drug

risks of opioid overdose | serious illnesses

AIDS, liver disease, diabetes and heart disease

opioids Flashcards

(52 cards)