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Flashcards in Opiates Deck (47):
1

Narcotic

Older term initially used to describe a drug that caused "narcosis" or sleep, but then became a loosely applied universal term for many illegal drugs, primarily for legislative purposes. Not a pharmacologically accurate term

2

Opiate

Any drug that is derived from the opium poppy, including natural and synesthetics

3

Opioid

General term for any drug(or endogenous peptide) that acts on the opiate receptor

4

Opium

Coagulated juice of the poppy pod that contains various opiates

5

Endorphine

Endogenous opiate like peptide that modifies the actions of other transmitters

6

Opiate Receptor Subtypes

mu
kappa
delta
nociception

7

Mu

Analgesia, physical dependence, respiratory depression, miosis, euphoria, reduced GI motility

8

Kappa

Analgesia, sedation, physical dependence

9

Delta

analgesia, anti depressant, physical dependence

10

Nociception

Anxiety, depression, appetite, develop tolerance to mu agonists

11

Endogenous Opiates

Enkephalins were first discovered, very potent (delta)
Beta endorphin (mu) and dynorphin (kappa)
Rapidly inactivated
Located in hypothalmus, forebrain, limbic medial thalamus, locus coeruleus to mediate pain perception and mood and released from pituitary during stress

12

Medical Use for Opiates

Pain
Cough
Diarrhea

13

Pain

Most common human experiences in which people seek medical treatment
Chronic pain is defined as that which lasts at least 3 months
It is difficult to measure because subjective

14

Types of Pain

Nociceptive- Physiological process of transmitting pain producing stimuli that emerge from tissue damage

Neuropathic- caused by lesion of the nervous system as a result of trauma, injury, or infection

15

Opiate Induced Analgesia

Blocks both perception and emotional components of pain
Does not impair conciousness
Reduces dull chronic pain

16

Patient Controlled Analgesia

- Patients control their pain by activating a pump on demand
Receives immediate dose, does not need to wait for nursing staff and physicians to administer the dose
Typically patient lets staff know, it takes 30-60 minutes
Faster alleviation of pain = less medication used

17

Euphoria

Intense sense of well-being and contentment, with a complete lack of concern for anything
Ecstatic- with sexual connotations
Primary reason for abuse

18

Physiological Effects

Histamine release- itching, red eye, sweating, fall in BP
Reduces gastric motility- constipation
Respiratory Depression- cause of death in overdose
Pupillary Constriction

19

Side Effects/Toxicity

Respiratory Depression
Opiates inhibit brainstem ability to detect buildup in CO2
Most important cause of death during overdose

20

Physiological Tolerance

Develops to everything, except for pupils and GI tract
Accounts for the increase in dose
Rate of development not the same- slow for respiratory rate
Lethal effects require 4-8 times the dose
Cross tolerance to all opiates

21

Physical Dependence

Withdrawal or abstinence signs
craving, anxiety
yawn, sweating, pupil dilation
tremors, flashes, insomnia

22

Heroin

Conversion of morphine to heroin is preferred by drug traffickers because
- 10 times more potent
Less space to hide
more lipid soluble
enters the brain more quickly
rapidly converted to morphine in bloodstream

23

Oxycodone

Developed in 1996 as timed release formulation
Abusers avoid the delay by crushing the tablets and snort or mix with water and inject in IV
Immediately delivers entire dose, sometimes combined with ecstasy
FDA released black box warning, prescription instructions
Reformulation- pills cannot be crushed, turned into a gel when mixed with water
- Decreased abuse by a little, more people turned to heroin

24

Public Heath

53 million Americans used prescription drugs for non-medical reasons
70% obtain from relatives and friends
DISPOSE OF ALL PRESCRIPTION DRUGS WHEN FINISHED

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Signs of Opiate Overdose

Loss of Conciousness
Unresponsive
Unable to talk
Breathing very slow, erratic

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Fetanyl

Synthetic opioid with potency 80-100 times that of morphine
Highly lipid soluble, immediate rise in plasma levels followed by an immediate fall
Rapid offset of action is due to redistribution

27

Fetanyl Abuse

Use needle to remove fetanyl gel from transdermal patch
Drug/gel is put in a syringe, and injected
High doses absorbed in short period
Results in thrombophelebitis, deep venous and abscesses
Revised formulation eliminates gel, reduced incidence of abuse
Mylan Fentanyl Transdermal System- Comes in a variety of doses to make it easier for patients

28

Opiates Toxicity

Generally non-toxic, as tolerance develops
Overdoses from combination or pure batch
Coma, respiratory depression, pinpoint pupils
ER treatment with naloxone
Related to IV use
AIDS
unsterile technique
Adulterants
Infections, abscesses in skin poppers

29

Methadone Maintenance

Developed in 1964
Dose was higher than used on street
Prevents withdrawal, but produces significant amount of cross tolerance, so prevents heroin or other opiates from binding to receptors, preventing acute effects-- leads to extinction
Converts to less risky route- oral vs IV
Use of pure medication with known potency
Slower onset of action avoids the rush
Improved general heath status
Reduced use of healthcare services
Stabilization may take days or weeks
Patients must be educated to expect this delay
Withdrawal and craving suppressed slowly
Cross tolerance at 5-20 mg
After a few weeks- pool of methadone is established
Patient can miss a daily dose and not feel withdrawal
Does not assist analgesia, no need for additional analgesics for pain medication

30

Positive Results of Methadone Maintenance

Death rate is 10 times lower than in untreated individuals
Needle sharing is 14% vs 47 %
Slower progression to AIDS in HIV infected individuals
Decreased incidence of ER visits
Fewer upper respiratory infections
Improved immune function
Improved nutritional status
Reduced incidence of criminal convictions
Reduced incidence of selling drugs
Long-acting (24-36 hours)

31

Methadone Side effects

Constipation
Sweating
Nonmalignant edema
Loss of libido
Relatively safe, true methadone related deaths in maintenance are rare

32

Methadone Efficacy

1/3 get better, 1/3 vacillate, 1/3 get worse
Methadone does not treat antisocial behavior
Methadone decreases needle sharing, decreases HIV/AIDS

33

Methadone controversy

Switch to use methadone as primary medication for treating chronic pain
Developed after OxyContin crisis
But methadone pharmacokinetics are more complicated so OD is more common

34

Buprenorphine

Partial agonist at mu receptor
Similar effects to morphine at receptor but at a lower dose range
.3 mg buprenorphine = 10 mg morphine

35

Subutex

Sublingual buprenorphine formulation that does not contain naloxone
Management of pain in low risk patients

36

Buprenorphine Maintenance

Slow release off receptor will delay appearance of withdrawal, even after abrupt termination

37

Suboxone

Sublingual formulation that contains naloxone HCl
Naloxone not absorbed orally or sublingually, so has no effect on buprenorphine
If preparation is injected, naloxone blocks buprenorphine access to opiate receptor

38

Buprenorpine Delivery of Therapy

Office-based prescribing of buprenorphine, allows private physicians to manage
Physician training is available from a variety of source
Strategy opens opiate dependence treatment options to many more individuals

39

Naltrexone

Orally absorbed
Use only after detoxification- with patients who are highly motivated
Prevents heroin or morphine from getting into receptor
Injectable formulation vivitrol has been approved for use as a treatment

40

Naloxone

Opiate receptor antagonist
Not orally absorbed- IV
Sometimes used to asses dependence
Not useful in maintenance-- too short acting
Reverses opiate overdose in emergency
Must put on slow drip after bolus

41

Naloxone Controversy

Giving naloxone injectors to the public
Given to ambulance drivers, police officers, first responders

42

Treatment Plan Heroine Users

use short acting opiates to engage
Gradually shift to longer acting drugs
Increase drug-taking interval
Survey urine for illicit opiates
Switch to antagonists after they have been detoxified

ALTERNATE
Some period may need maintenance for an extended period of time
Very low dose methadone may be all that is needed

43

Heroin Use

Troops had very little dependence once they returned to the US

44

Speedball

IV combination of heroine and cocaine
sometimes norted
often co-administered, but can also give one after the other in a short time period
Heroine allows a parachute from the intense high of cocaine

45

Cheese Heroine

Black tar mexican heroin mixed with crushed OTC that contain antihistamine diphenhydramine
Sedative effects of the heroin and sleep aids make it very dangerous
Targeted to middle school children

46

Krokodil

Desomorphine- 8-10 X more potent
Homemade from codeine, iodine, red phosphorous, gasoline, lighter fluid, and industrial clearners
Sensationalized as flesh eating heroin- causes skin necrosis and gangrene
Popular in Russia and Ukraine

47

Kratom

Made from the leaves of Mitragyna speciosa, southeast asian tree related to coffee, and has been consumed in Asia for Millenia, typically as tea or powder
Herb contains alkaloids that activate opioid receptors in the brain and reduce pain
Although most opioids have sedative qualities, low to moderate doses of kratom serve as a mild stimulant
Led advocated to claim kratom can be used as a maintenance drug to help recovering opiate dependents
DEA planning to place it on schedule 1
Mitragynine and 7hydroxymitragynine active ingredients in kratom, bind to opiate receptors in the brain