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Midterm

PHA 3112 Study Guide - Midterm Guide: Opioid Overdose, Opioid Antagonist, Cocaine Dependence


Department
Pharmacology
Course Code
PHA 3112
Professor
Pierre Fortier
Study Guide
Midterm

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1
Lecture 5 Opioid Analgesics & Drug Abuse
CHAPTER 28: OPIOID ANALGESICANTAGONISTS
CHAPTER 28: OPIOID ANALGESICANTAGONISTS: OTHER CENTRALLY ACTING ANALGESICS
o ANALGESICS: drugs that relieve pain without causing a loss of consciousness.
o OPIOD ANALGESIC MOST EFFECTIVE PAIN RELIEVES.
o OPIOD: any drug, natural or synthetic that has actions similar to those of morphine.
o OPIATE: more specific compounds that have opium present (ie. Morphine, codeine)
o NARCOTIC: analgesic, CNS depressant, any drug capable of causing physical dependence
ENDOGENOUS OPIOID PEPTIDES:
o ENKEPHALINS, ENDORPHINS, DYNORPHINS opiod-like properties & serve as neurotransmitters,
neurohormones, & neuromodulators.
o OPIOD RECEPTORS: MU, KAPPA, DELTA.
o OPIOID ANALGESICS ACT ON MU & KAPPA RECEPTORS.
o ENDOGENOUS OPIOID PEPTIDES ACT ON ALL 3 TYPES (MU, KAPPA, DELTA) RECEPTORS.
CLASSIFICATION OF DRUGS THAT AT @ OPIOD RECEPTORS:
1. PURE OPIOD AGNOIST: PRODUCE ANALGESIA, EUPHORIA, SEDATION, RESPIRATORY DEPRESSION,
PHYSICAL DEPENDENCE, CONSTIPATION. Drugs: morphine, codeine, meperidine
- Act on MU & KAPPA receptors as AGONIST PROMOTION OF PAIN REFLIEF
2. AGONIST-ANTAGONIST OPIOD/PARTIAL AGONIST: PRODUCE ANALGESIA ALONE. CAN ANTAGONIZE
ANALGESIA CAUSED BY PURE AGONIST. LOW POTENTIAL OF ABUSE, less respiratory depression, less
powerful analgesic effects.
Drugs: pentazocine (Mu: Antagonist & Kappa: Agonist), nalbuphine (Mu: Antagonist & Kappa: Agonist),
butorphanol (Mu: Antagonist & Kappa: Agonist), buprenorphine (Mu: partial agonist, Kappa:
antagonist).
3. PURE OPIOD ANTAGONIST: don’t PRODUCE ANALGESIA/EFFECTS CAUSED BY OPIOID AGONIST.
- Use for treatment: REVERSAL OF RESPIRATORY & CNS DEPRESSION CAUSED BY OVERDOSE W/OPIOD
AGONIST)
- Drugs: Nalozone, naltrexone, nalmefene. All 3 act as Antagnoists for MU & KAPPA RECEPTORS.
STRONG OPIOID:
MORPHINE:
- Source; Extraction from opium from poppy plant.
- Pharmacologic actions: pure opioid agonist.
- Effects: PRODUCE ANALGESIA, EUPHORIA, SEDATION, RESPIRATORY DEPRESSION, PHYSICAL
DEPENDENCE, CONSTIPATION
- Therapeutic use: Relief for pain: moderate to severe pain: postoperative cancer, labor & delivery.
- Relieves pain without affecting other senses & without causing a loss of sonciousness.
- Dosage depeds o the pt’s pai leel.
- Adverse effects:
1) respiratory depression (most serious), 2) constipation, 3) orthostatic hypotension, 4) urinary
retention, 5) cough suppression, 6) emesis (nausea & vomiting), 7) elevation of intracranial pressure
(ICP), 8) euphoria (exaggerated sense of well-being), 9) dysphoria (sense of anxiety & unease), 10)
sedation, 11) miosis (papillary constriction), 12) neurotoxicity.
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2
Lecture 5 Opioid Analgesics & Drug Abuse
CHAPTER 28: OPIOID ANALGESICANTAGONISTS
- Tolerance can occur with prolong uses. Pt; develop CROSS-TOLERANCE amount other opiod agonist.
- Pharmacokinetics: oral doses must be large to achieve same analgesic effect. Preference IV
- Precautions: avoid use in pregnancy, labour & delivery, head injury and decrease respiratory reserve.
- Drug interactions: DON’T COMBINE WITH MEPERIDINE WITH MONOAMINE OXIDASE (MAO) INHIBITOR
cause EXCITATION, delirium, hyperpyrexia, convulsions and severe respiratory depression and death.
Toxicity: Opioid overdose: TRIAD of symptoms: coma, respiratory depression, pinpoint pupil, and
death.
- Treatment: Naloxone (Narcan).
- WD Symptoms: yawning, rhinorrhea, sweating, followed by anorexia, irritability, tremor & gooseflesh.
- Peak symptoms: violent sneezing, weakness, nausea, vomiting, diarrhea, abdominal cramps, bone &
muscle pain, muscle spasms and kicking movements.
- Morphine withdrawal lasts 7-10 days; not dangerous
- Physical dependence rarely an issue when used acutely to treat pain.
- Infant w/ opioid exposure in utero born drug dependant; taper down by administering dilute paregoric
- WD signs: excessive crying, sneezing, tremor, hyperreflexia, fever, & diarrhea.
MODERATE TO STRONG OPIOIDS: produce less analgesia & respiratory depression than morphine,
and lower potential for abuse.
1. CODEINE: Oral administration; produce significant pain relief & greater w/ combo of nonopioid analgesic
- Liver converts this into morphine, active form of codeine.
2. OXYCODONE [Percocet, oxycontin]: similar analgesic actions to codeine.
3. HYDROCODONE [VICODIN, VICOPROFIN, LORTAB]: similar analgesic actions to codeine. Normal dose:
5mg. Avalialbe with aspirin, acetaminophen, or ibuprofen.
4. PROPOXYPHENE [DARVON]: analgesic effect equal to asprin. Low potential for abuse & physical
dependence. Large dose cause toxic psychosis.
AGONIST-ANTAGONIST OPIOIDS:
1. PENTAZOCINE [TALWIN]: used for mild to moderate pain, less effective than mirphien against
severe pain. Produces analgesia, sedation, low respiratory depression, produces little to no
euphoria. Adverse effects: anxiety, strange thoughts, nightmares, hallucinations. Phsyical
dependence can develop.
2. Nalbubphine/butorphanol: SAME AS ABOVE
3. BUPRENORPHINE: Agonist @ Mu RECEPTORS, & ANTAGONIST @ KAPPA RECEPTORS greater
abuse potential. Treatment use: MANAGING OPIATE AGONIST WITHDRAWAL
OPIOID ANTAGONIST: drugs that BLOCK THE EFFECTS OF OPIOD AGONISTS.
Treatment use: opiod overdose, relief of opioid induced constipation, reversal of postoperative opioid
effects, & opiod addiction management.
1. NALOXONE: administered only if the pt. has opid in their blood, it will reverse all the OPID ACTIONS
REVERSE ANALGESIA, SEDATION, EUPHORIA, & RESPIRATORY DEPRESSION.
2. METHYLNALTREXONE & ALVIMOPAN: Both selective MU opiod antagonist.
- Treatment use: OPIOID INDUCED CONSTIPATION in pt with late-stage disease to relieve pain.
3. NALTREXONE: pure opioid antagonist for OPIOID AND ALCOHOL ABUSE.
4. NALMEFENE [REVEX]: long-acting analog of naltrexone.
- Treatment use: reversing opiod effects from after surgery & treating opioid overdose.
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3
Lecture 5 Opioid Analgesics & Drug Abuse
CHAPTER 28: OPIOID ANALGESICANTAGONISTS
NINOPIOID CENTRALLY ACTING ANALGESICS: relieve pain by affecting unrelated opioid receptors.
1. Tramadol: STRONG ANALGESIC WITH MINIMAL POTENTIAL FOR DEPENDENCE, ABUSE OR
RESPIRATORY DEPRESSION. Works through A WEAK AGONIST ACTIVTY @ MU OPIOD RECEPTORS
BLOCK UPTAKE OF NOREPINEPHRINE & SEROTONIN
2. CLONIDINE: 1) Relieve severe pain, 2- treat hypertension. DOES NOT INTERACT W/OPIOD
RECEPTORS. Adverse effect: severe hypotension, slow heart rate (bradycardia).
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