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134 Cards in this Set
- Front
- Back
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Receptor type
- Supraspinal analgesia - Euphoria |
Mu-1
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Receptor type
- Spinal analgesia - Respiratory depression - Constipation |
Mu-2
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Receptor type
- Spinal analgesia - Diuresis - Dysphoria |
Kappa
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Receptor type
- Supraspinal and spinal analgesia |
Delta
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Receptor type that has had an increased use b/c causes less respiratory depression than the other types
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Kappa
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Receptor type
- Dysphoria - Hallucinations - Cardiac Stimulation |
Sigma
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Morphine action at receptors
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- Mu, Kappa and delta agonist
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Buprenorphine action at receptors
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Mu partial agonist only
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Butorphanol, Pentazocine and Nalbuphine action at receptors
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- Mu antagonist
- Kappa agonist |
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Naloxene action at receptors
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Mu, Kappa and Delta antagonist
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Naltrexone action at receptors
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Mu, Kappa and Delta anatagonists
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Endogenous Opioids -->Electrical stimulation of specific CNS areas (ex: _____________ )can produce strong analgesia
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Periaqueductal gray area
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________ opioids effects very similar to narcotic drugs
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Endogenous
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Precursor for beta endorphin
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Propiomelanocortin
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Beta endorphin is a ____ AA peptide
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31
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Propiomelanocortin = makes (3)
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- beta endorphin
- ACTH - Melanocyte stimulating hormone (MSH) |
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Beta endorphins found primarily in _________
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Pituitary gland
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Beta endorphins bind primarily to (2)
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- Mu
- Delta |
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Enkephalins precursor
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Proenkephalin
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2 type of enkephalins (each are 5 peptides long)
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- Met-enkephalin
- Leu-enkephalin |
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Met enkephalin = AA # 61-65 of ________
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Beta endorphin
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Located especially in:
- Brainstem - Dorsal horn - spinal cord - Basal ganglia - Limbic system |
Enkephalins
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Probable mechanism of enkephalins
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- Bind to opioid R--> dec release of substance P --> dec pain transmission
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Enkephalins bind equally to (2)
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- Delta
- Mu1 |
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Dynorphin precursor
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Prodynorphin
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Dynorphins bind primarily to
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kappa
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Endorphins and enkephalins not of clinical value b/c (2)
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- Not absorbed PO
- Rapid biotransformation |
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Narcotic definition
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- Ring structure + carbon chain + oxygen + nitrogen
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CNS actions of Narcotics (5)
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- Analgesia
- Sedation - Emesis - Depression of cough reflex - Respiratory Depression |
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Supraspinal Narcotic Analgesia MOA
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- Act at opioid receptors in periaqueductal gray and other areas --> stimulate descending inhibition --> dec transmission of pain from spinal cord to higher sites
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Spinal Narcotic Analgesia MOA
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Stimulate enkephalin R's --> decs Ca2+ availability --> dec substance P --> dec pain
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When stimulated, Mu/Delta cause:
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Dec adenylate cyclase activity --> dec cAMP --> inc K+ efflux --> hyperpolarization --> dec Ca2+ influx --> dec substance P
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When stimulated, Kappa causes:
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Dec Ca2+ influx --> dec substance P
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Narcotic cause this CNS effect but barbiturates are better at it
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Sedation
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This CNS ADR of narcotics increases when pt is ambulatory
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N/V
(b/c inc sensitivty to motion) |
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Narcotic CNS effect --> depression of _________
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Cough reflex
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Narcotic CNS effect that can be cause of death
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Respiratory depression
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Narcotic CNS effect that is usually not an effect at therapeutic dose unless pt has previous problem
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Respiratory depression
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Narcotic ADR = hypotension --> the direct cause = ___________
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Depression of vasomotor center
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Narcotic ADR = hypotension --> the indirect cause = _________
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Histamine release --> peripheral vasodilation
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Narcotic GI ADRs (2)
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- Decreased peristalsis
- Delayed gastric emptying (Constipation) |
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Narcotic eye ADRs
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Miosis
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Narcotic ADR - increases smooth muscle tone in(3)
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1. GI
2. Biliary Tract --> can't give morphine for gall bladder attack 3. Urinary |
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Pts receiving narcotics for 1 month+ may have decreases in (3)
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- Cortisol
- Sex Hormone - DHEA |
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Opioid cause relief of ___________ pain
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Moderate to severe
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Chronic use of opioids does not cause addiction, it causes _____________
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Psychological dependence
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Degree of physical dependence on opioids depends on _____ and ______ of use
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Amount and duration
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Most effective dose of opioids for chronic pain =
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Fixed schedule (ex: every 6 hrs around the clock)
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______ improves when a patient receives regular analgesia (3)
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- Quality of sleep
- Mood --> better interactions with caregivers - Appetite |
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In addiction, pain control may improve so that _____ narcotic is required --> so decs
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Less narcotic --> decs ADRs
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More restrictive narcotic regulations has less to
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Opiophobia and less use of narcotics
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Causes of Opiophobia (3)
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- Fear of Addiction
- Causes dec in cognition --> people don't want this before they die - Some think that their decreased pain and suffering leads to decreased spiritual growth |
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Goldstein study found:
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- Opioids given pre-op reduced pain, N/V and use (blood levels) of opioids post-op
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Narcotics can be used for __________ chronic cough
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non-productive
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Narcotics can be used for relief of severe _______
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Diarrhea (b/c ADR = constipation)
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Narcotics can cause immediate and short term relief of dyspnea associated with (2)
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- Pulmonary edema
- LVF (by dec'ing L ventricular workload) |
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Narcotics can improve respiration on pts with ventilators by __________
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Decrease tendency to 'fight' assisted breathing
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Narcotic ADRs that people develop tolerance to (5)
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- H/A
- N/V - Dizziness - Sedation - Respiratory depression |
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Ways to prevent Constipation ADR (4)
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- Inc fluids
- Inc fiber - Ambulation when possible - May req daily laxatives |
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Narcotic ADR that is observed in newborn after dose to mom
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Respiratory depression
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Genitourinary ADRs of Narcotics (3)
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- Urinary retention
- Dysuria - Dec sexual desire |
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OD of Narcotic signs(6)
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- Miosis
- Hypotension + Bradycardia - Hypothermia - Oligouria - Pulmonary edema - Respiratory depression --> come |
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Contraindications for Narcotic Use
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- Convulsive states
- Inc ICP (b/c dec resp --> inc CO2 --> cerebral vasodilation --> inc ICP - Undx acute abdominal conditions |
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Narcotics cause further _______ when combo with alcohol, barbiturates, etc
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CNS depression
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Withdraw rxns within 12 hrs after last dose (6)
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- Lacrimation
- Sweating - Rhinorrhea - Yawning - Chills - Piloerection |
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Withdraw rxns within 36 hrs of last dose (6)
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- Abdominal cramping
- Muscle aching - N/V - Diarrhea - Hyperthermia - Hyperventilation |
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Most withdraw rxns end within ____
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3-5 days
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When pts on narcotics, muscle relaxation and respiratory depression inc with ______
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Muscle relaxants
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Most widely used narcotic
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Morphine
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Morphine given ___ for cancer pts
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orally
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Morphine used for ___ for limited periods of pain
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Patient Controlled Anesthesia
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2 morphine metabolites
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- Morphine-6-glucuronide (M-6-G)
- M-3-G |
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- High affinity for Mu
- Analgesic - More powerful than morphine - Highly polar - Stays prolonged in CSF |
M-6-G
(morpine 6 glucoronide) |
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If switch pt from 1 opioid to another (3)
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- Calculate dose based on acute potency difference
- Reduce dose - Adjust dose up if necessary |
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_______ between 2 drugs is incomplete --> so can't just switch easily from 1 drug to another
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Cross tolerance
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____ reported with higher doses of morphine --> may be due to M-3-G
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Seizures
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____ release occurs after morphine epidural and intrathecal
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Histamine
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________ if effective at decreasing morphine histamine release but may also decrease analgesia effects
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Naloxone
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_______ effective at decreasing morphine histamine release and does NOT dec analgesia
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Propofol
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Can not give ________ forms of morphine with alcohol, because it dissolves it immediately and makes it an instant dose
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Sustained release forms (of morphine and related opioids)
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100x more potent than morphine
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Fentanyl
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- Greater lipid solubility than morphine (can't do PO)
- Shorter acting than morphine |
Fentanyl
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Major ADR = pruritis at injection site
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Fentanyl
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Contraindication for = acute pain b/c patches take a while to work ---> so pt may put on multiple and die
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Fentanyl
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Different forms of Fentanyl (5)
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- Transdermal
- Oral Lozenge - Lozenge of a stick (lollipop) - Buccal tablet - Buccal film |
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Contraindications =
- acute pain - post-op pain - mild or intermittent pain - doses > 25 mg |
Fentanyl
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- Less potent than morphine
- Can only use for acute tx |
Meperidine
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Meperidine can not use chronically, b/c will get accumulation of _______ which has a longer t1/2 (15-30 hrs)
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Normeperidine
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- Not reversed with naloxone
- Toxicity more frequent in those with renal failure |
Meperidine
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ADRs = CNS stimulant
- Tremor - Muscle twitch - Seizures |
Meperidine
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- Strongly binds Mu
- Hard to reverse with naloxone - Anatagonist at Kappa |
Buprenorphine
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- Dose related respiration depression
- Only used to tx narcotic addiction (esp when given with naloxone) |
Buprenorphine
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Physicians who prescribe must:
- Meet reqts - Notify secretary of health and human services |
Buprenorphine
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- Good PO absorption
- Limited biotransformation - Very LONG lasting |
Methadone
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Methadone danger of use
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Duration of respi depression > analgesia
(pt may take more to help pain but may further inc resp depression) |
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2 uses of methadone
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- Tx of cancer pts
- Tx of narcotic addiction |
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When used to tx cancer pt chronically, pt also needs short-acting opioid for "rescue" pain
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Methadone
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Tx of narcotic addiction --> goal is to get patient to be on this chronically = more stable
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Methadone
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Methadone advantages in tx'ing narcotic pts (2)
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- Can be given PO
- Long t 1/2 so less frequent doses needed |
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Mechanism of Methadone used as tx of addiction --> makes pt stable by producing ______-
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Tolerance
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Best candidates for tx of addiction with this drug:
- 18+ yrs - 2+ yrs of addiction - Failed other modalities - Volunteer |
Methadone
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- Not used much anymore
- Longer acting derivative of Methadone |
Levomethadyl
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FDA approved ONLY for tx of narcotic addiction (need approved tx program to give)
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Levomethadyl
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Centrally acting analgesic
- synthetic codeine with less R affinity |
Tramadol
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Tramadol MOA (2)
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- Mu R agonist
- Block of 5HT uptake (like antidep's) |
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- Centrally acting analgesic
- Less chance for abuse and resp depression than others - Partial reversal by Naloxone |
Tramadol
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Narcotic agonists-antagonist activate __ R's
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Kappa
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Narcotic agonists-antagonists have antagonist activity at __ R's --> can cause withdraw rxns in pts on opiods that inc this R activity
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Mu
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Narcotic agonist-antagonists have less _______ than pure narcotics
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Respiratory Depression
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- Developed as 'non-addictive' opioid but dependence can develop
- ADR = psychological: hallucinations, nightmares (more likely in hepatic and renal probs bc less metabolism) |
Pentazocine
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- PO only
- Pentazocine + naloxone |
Talwin Nx
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ADRs = nightmares and hallucinations --> more likley in people with renal and hepatic probs bc inc don't metabolize
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Pentazocine
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- Combo drug --> decreased abuse
- Naloxone in it does not cause decreased analgesia - Significant antagonist effects may cause withdraw sx's |
Talwin Nx
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Agonist-Antagonist
- 5x more potent than morphine - Nasal spray or parenteral |
Butorphanol
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Narcotic agonist-antagonists MOA (2)
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Kappa agonist
Mu antagonist |
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Agonist-antagonist
- Like Butorphanol, has no increase in respiratory depression with inc dose |
Nalbuphine
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Agonist-antagonist
- Only one that has increased respiratory depression with increased dose (so acute use only) |
Dezocine
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Narcotic antagonists (3)
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- Naloxone
- Nalmefene - Naltrexone |
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Narcotic antagonist
- Derivative of oxymorphone - Short acting |
Naloxone
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Naloxone MOA
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- Blocks opioid Rs with HIGH affinity (so rapid reversal)
(Does not activate R's) |
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Used to determine if there is presence of narcotics in pts prior to initiation of Naltrexone therapy
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Narcan Challenge test
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Test that puts person in immediate withdraw to determine if he or she is a chronic opioid user (addict)
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Narcan Challegne Test
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Before putting pt on ______, have to do narcan challenge test to see if person goes into withdraw (proves person is addict)
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Methadone
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Narcan =
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Naloxone
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Too rapid reversal of OD with Naloxone can cause (3)
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CNS excitation:
- N/V - Inc BP |
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Antagonist
- Derivative of Naltrexone - Used only IV - Longer t 1/2 |
Nalmefene
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Like naloxone, is a derivative of oxymorphone, but is longer acting
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Naltrexone
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To initiate therapy of this, need 2 reqts:
- Pt must be opioid free for 7-10 days - Negative narcan challenge test (no withdraw rxn) |
Naltrexone
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ADRs =
- Hepatotoxic - Confusion - Hallucination |
Naltrexone
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Contraindications for Naltrexone
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- Pts taking opioids
- In withdraw - + urine opioid test - Liver probs |
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Naltrexone can also be used to tx _________ b/c decs induced euphoria
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Alcoholism
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Alcohol induced euphoria can be treated with Naltrexone and is explained by:
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Inc BF to R prefrontal cortex
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ADRs for treating alcoholism with Naltrexone = same as when treating narcotic addiction + ___________
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Increased N/V
(may explain anorexia and wt loss) |
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Naltrexone decs alcohol use - 4 ways of proof =
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- Dec # drinks/day
- Improved compliance - Dec relapses - Better coping with relapses |
