Opiates Flashcards

1
Q

Narcotic

A

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

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2
Q

Opiate

A

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

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3
Q

Opioid

A

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

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4
Q

Opium

A

Coagulated juice of the poppy pod that contains various opiates

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5
Q

Endorphine

A

Endogenous opiate like peptide that modifies the actions of other transmitters

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6
Q

Opiate Receptor Subtypes

A

mu
kappa
delta
nociception

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7
Q

Mu

A

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

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8
Q

Kappa

A

Analgesia, sedation, physical dependence

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9
Q

Delta

A

analgesia, anti depressant, physical dependence

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10
Q

Nociception

A

Anxiety, depression, appetite, develop tolerance to mu agonists

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11
Q

Endogenous Opiates

A

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

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12
Q

Medical Use for Opiates

A

Pain
Cough
Diarrhea

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13
Q

Pain

A

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

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14
Q

Types of Pain

A

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

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15
Q

Opiate Induced Analgesia

A

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

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16
Q

Patient Controlled Analgesia

A
  • 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
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17
Q

Euphoria

A

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

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18
Q

Physiological Effects

A

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

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19
Q

Side Effects/Toxicity

A

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

20
Q

Physiological Tolerance

A

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
Q

Physical Dependence

A

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

22
Q

Heroin

A

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
Q

Oxycodone

A

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
Q

Public Heath

A

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

25
Signs of Opiate Overdose
Loss of Conciousness Unresponsive Unable to talk Breathing very slow, erratic
26
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