PHARMACOLOGY
Pharmacology Final Exam
Module 10
Opioid Tolerance: Develops for euphoria, respiratory depression, nausea. Does NOT develop for constipation or miosis.
Opioid Physical Dependence: Substantial for opioids. Abstinence syndrome extremely unpleasant but rarely dangerous. Protracted withdrawal
may persist for months and characterized by insomnia, irritability and fatigue.
OUD Maintenance Therapy Opioid Overdose Reversal
Drug Class Pure Opioid Agonist Partial Mu Agonist, Kappa Pure Opioid Antagonist Pure Opioid Antagonist
Antagonist
Prototype Methadone Buprenorphine Naltrexone Naloxone
MOA Replaces/substitutes the misused Replaces/substitutes the misused Discourages opioid use by Reverses respiratory and CNS
opioid opioid blocking euphoria/effects depression
Therapeutic OUD withdrawal/detox, OUD OUD withdrawal/detox, OUD AUD, OUD (after detox) Reversal agent for overdose,
Uses maintenance/suppressive therapy, maintenance/suppressive post-op effects, neonate resp.
pain management therapy, pain management depression
AEs Standard opioid AEs; QT prolongation; HA; GI upset; anxiety; sleep GI; HA, sedation, anxiety; Reversal of pain control,
respiratory depression; hepatic injury disturbances; LE edema; sweating injection-site rxns; liver withdrawal if physically
toxicity dependent on opioids
Nursing CII Controlled Substance CIII Controlled Substance MUST be opioid-free (- urine) Titrate carefully to prevent
Implications Baseline ECG, routine thereafter for Administer tablets and film Manufacturer provided withdrawal/loss of pain
cardiac hx; report sx of liver injury; sublingually needles in gluteal muscle control
monitor VS and dose sufficiency to Greater risk of death if relapse Greater risk of death if Monitor for 4+hrs after
suppress withdrawal after discontinuation relapse after discontinuation overdose
Greater risk of death if relapse after effectiveness with counseling effectiveness with counseling Teach proper admin
discontinuation technique based on product
effectiveness with counseling prescribed
Other PK: LONG half-life and duration of IV: PMH/FH of QT prolongation. IV: contraindicated in acute PK: SHORT half-life, onset 2-
action, cross tolerance to other opioids PREFERRED in pregnancy alone. hepatitis/liver failure; NOT 5mins, duration; hours,
IV: PMH/FH of QT prolongation. May DDIs: Strong inducer/inhibitors used in pregnancy STRONG mu binding, NOT PO
be used in pregnancy of CYP3A4, CNS depressants DF: Monthly IM injection. (1st pass)
DDIs: CNS depressants, QT-prolonging Safety: Ceiling effect: lower Preferred in OUD DF: SubQ/IM/IV, IN
drugs, CYP3A4 inhibitors abuse/respiratory depression ( DDIs: Opioids (no others) DDIs: opioids
Safety: Accumulation/respiratory with concomitant CNS
depression with repeat dosing, only depressants) Pain management may be
prescribed for OUD through opioid tx difficult given drug properties
program (exception for 72hrs of IP Can precipitate withdrawal Can precipitate withdrawal
use)
Opioid Overdose Risk Factors*
, AUD: Chronic, relapsing disorder characterized by: impaired control over drinking, preoccupation with consumption, use of alcohol despite
awareness of adverse consequences, distortions in thinking, esp. aeb denial of problem.
Influenced by genetics, psychosocial, and environmental factors. May lead to psychological issues, malnutrition, poor work performance,
family/social deterioration, and health consequences.
Alcohol Withdrawal Syndrome: Begins 4-12hrs after last drink. May continue for 5-7 days. [N/V, tremors, restlessness, insomnia, depression,
irritability, HR/BP/temp/RR, diaphoresis, seizures, illusions]
Alcohol Withdrawal Delirium: 2-3 days after abrupt withdrawal. < MEDICAL EMERGENCY
Withdrawal Maintenance
Drug Class Benzodiazepines Aversion Therapy Pure Opioid Antagonist
Prototype Disulfiram Naltrexone Acamprosate
MOA Disrupts alcohol metabolism, Cravings/blocks Reduces unpleasant feelings
irreversible inhibition of aldehyde reinforcing (pleasurable) associated with abstinence
dehydrogenase effects
Therapeutic Uses AUD SEE PREVIOUS CHART. AUD
AEs W/ Alcohol: Acetaldehyde Syndrome Diarrhea; suicide-related events
{Mild: N/V, flushing, palpitations, HA, Tablets administered (rare)
sweating, thirst, hypotension. Severe: daily (option for AUD)
resp. dep., CV collapse, dysrhythmias,
seizures, death}
W/out Alcohol: rash; drowsiness; liver
dysfunction (rare); peripheral/optic
neuritis (rare)
Nursing Admin no sooner than 12 hours after Give with meals tid; Start after
Implications last drink detox is over (~5 days after
High quality patient education (effects cessation); evaluate renal
persist 2 weeks after d/c, medical function; effectiveness with
alert bracelet) counseling
Other IV: heart disease, hepatic DF: tablets tid
dysfunction, psychiatric disorders IV: ESRD or CrCl < 30mL/min;
DDIs: alcohol, metronidazole, avoid in pregnancy
warfarin
Safety: avoid alcohol containing Mouthwash,
products cough syrup,
cologne, etc.
, Sedation Drugs
Drug Class Benzodiazepines
Prototype Diazepam Propofol
MOA Interact with GABA receptors enhancing inhibitory effects Promotes release of GABA, major inhibitory NT in the brain
of GABA in the brain
Therapeutic Uses IV sedation; produces unconsciousness and amnesia when Induction and maintenance of general anesthesia, sedation
used in large doses, IV induction
AEs Severe resp. dep.; hypotension Resp. dep., apnea; hypotension; risk for bacterial infection; IV site
pain (use large vein, lidocaine); Propofol infusion syndrome ( dose)
Nursing Implications Admin: emulsion in phospholipid carrier. Dedicated IV catheter for
continuous infusion. Change bottle tubing after 12hrs of hanging
Other DDIs: IV formulation incompatible with many drugs
Safety: Abuse potential *Narrow Therapeutic Index*
Hypnotics
Drug Class Benzodiazepines BZDRAs Melatonin Receptor Agonists Sedating Antidepressants Antihistamines
Prototype Triazolam Zolpidem Ramelteon Trazodone Diphenhydramine
MOA Interact with GABA receptors, Agonist @ BZD Activates melatonin receptors sleep latency and prolongs (Benadryl)
enhancing inhibitory effects of receptor site on sleep duration
GABA in brain GABA receptor
Therapeutic DOC for short-term insomnia Insomnia only First line for insomnia Insomnia (esp. in conjunction w/ FDA approved for
Uses tx; anxiety; seizure disorders CNS stimulating antidepressants) insomnia
AEs Tolerance, rebound insomnia; Daytime Somnolence, dizziness, Daytime sedation, Daytime sedation,
anterograde amnesia; drowsiness, fatigue, prolactin levels, anticholinergic effects, weight anticholinergic
teratogenic; CNS depression dizziness, sleep severe allergic rxn (small risk) gain, postural hypotension, effects
Overdose tx: Flumazenil driving dizziness
Nursing CIV Controlled Substance
Implications Withdrawal d/t abrupt d/c
from long-term high-dose use
(anxiety, insomnia, CNS
excitability > seizures) > wean
dose gradually
Other DDIs: resp. dep. When used DDIs: resp. dep. Wider therapeutic index, few OTC
with other CNS depressants With other CNS DDIs, low abuse potential
PK: Short half life dep. IV: avoid in hepatic
impairment/pregnancy
All BZD have essentially BZD Withdrawal
equivalent actions. Use depends Sx: anxiety, insomnia, tachycardia, diaphoresis, tremor, agitation, vomiting, seizures
on time course of action. Paradoxical agitation/rage can occur (unusual rxn)
Pharmacology Final Exam
Module 10
Opioid Tolerance: Develops for euphoria, respiratory depression, nausea. Does NOT develop for constipation or miosis.
Opioid Physical Dependence: Substantial for opioids. Abstinence syndrome extremely unpleasant but rarely dangerous. Protracted withdrawal
may persist for months and characterized by insomnia, irritability and fatigue.
OUD Maintenance Therapy Opioid Overdose Reversal
Drug Class Pure Opioid Agonist Partial Mu Agonist, Kappa Pure Opioid Antagonist Pure Opioid Antagonist
Antagonist
Prototype Methadone Buprenorphine Naltrexone Naloxone
MOA Replaces/substitutes the misused Replaces/substitutes the misused Discourages opioid use by Reverses respiratory and CNS
opioid opioid blocking euphoria/effects depression
Therapeutic OUD withdrawal/detox, OUD OUD withdrawal/detox, OUD AUD, OUD (after detox) Reversal agent for overdose,
Uses maintenance/suppressive therapy, maintenance/suppressive post-op effects, neonate resp.
pain management therapy, pain management depression
AEs Standard opioid AEs; QT prolongation; HA; GI upset; anxiety; sleep GI; HA, sedation, anxiety; Reversal of pain control,
respiratory depression; hepatic injury disturbances; LE edema; sweating injection-site rxns; liver withdrawal if physically
toxicity dependent on opioids
Nursing CII Controlled Substance CIII Controlled Substance MUST be opioid-free (- urine) Titrate carefully to prevent
Implications Baseline ECG, routine thereafter for Administer tablets and film Manufacturer provided withdrawal/loss of pain
cardiac hx; report sx of liver injury; sublingually needles in gluteal muscle control
monitor VS and dose sufficiency to Greater risk of death if relapse Greater risk of death if Monitor for 4+hrs after
suppress withdrawal after discontinuation relapse after discontinuation overdose
Greater risk of death if relapse after effectiveness with counseling effectiveness with counseling Teach proper admin
discontinuation technique based on product
effectiveness with counseling prescribed
Other PK: LONG half-life and duration of IV: PMH/FH of QT prolongation. IV: contraindicated in acute PK: SHORT half-life, onset 2-
action, cross tolerance to other opioids PREFERRED in pregnancy alone. hepatitis/liver failure; NOT 5mins, duration; hours,
IV: PMH/FH of QT prolongation. May DDIs: Strong inducer/inhibitors used in pregnancy STRONG mu binding, NOT PO
be used in pregnancy of CYP3A4, CNS depressants DF: Monthly IM injection. (1st pass)
DDIs: CNS depressants, QT-prolonging Safety: Ceiling effect: lower Preferred in OUD DF: SubQ/IM/IV, IN
drugs, CYP3A4 inhibitors abuse/respiratory depression ( DDIs: Opioids (no others) DDIs: opioids
Safety: Accumulation/respiratory with concomitant CNS
depression with repeat dosing, only depressants) Pain management may be
prescribed for OUD through opioid tx difficult given drug properties
program (exception for 72hrs of IP Can precipitate withdrawal Can precipitate withdrawal
use)
Opioid Overdose Risk Factors*
, AUD: Chronic, relapsing disorder characterized by: impaired control over drinking, preoccupation with consumption, use of alcohol despite
awareness of adverse consequences, distortions in thinking, esp. aeb denial of problem.
Influenced by genetics, psychosocial, and environmental factors. May lead to psychological issues, malnutrition, poor work performance,
family/social deterioration, and health consequences.
Alcohol Withdrawal Syndrome: Begins 4-12hrs after last drink. May continue for 5-7 days. [N/V, tremors, restlessness, insomnia, depression,
irritability, HR/BP/temp/RR, diaphoresis, seizures, illusions]
Alcohol Withdrawal Delirium: 2-3 days after abrupt withdrawal. < MEDICAL EMERGENCY
Withdrawal Maintenance
Drug Class Benzodiazepines Aversion Therapy Pure Opioid Antagonist
Prototype Disulfiram Naltrexone Acamprosate
MOA Disrupts alcohol metabolism, Cravings/blocks Reduces unpleasant feelings
irreversible inhibition of aldehyde reinforcing (pleasurable) associated with abstinence
dehydrogenase effects
Therapeutic Uses AUD SEE PREVIOUS CHART. AUD
AEs W/ Alcohol: Acetaldehyde Syndrome Diarrhea; suicide-related events
{Mild: N/V, flushing, palpitations, HA, Tablets administered (rare)
sweating, thirst, hypotension. Severe: daily (option for AUD)
resp. dep., CV collapse, dysrhythmias,
seizures, death}
W/out Alcohol: rash; drowsiness; liver
dysfunction (rare); peripheral/optic
neuritis (rare)
Nursing Admin no sooner than 12 hours after Give with meals tid; Start after
Implications last drink detox is over (~5 days after
High quality patient education (effects cessation); evaluate renal
persist 2 weeks after d/c, medical function; effectiveness with
alert bracelet) counseling
Other IV: heart disease, hepatic DF: tablets tid
dysfunction, psychiatric disorders IV: ESRD or CrCl < 30mL/min;
DDIs: alcohol, metronidazole, avoid in pregnancy
warfarin
Safety: avoid alcohol containing Mouthwash,
products cough syrup,
cologne, etc.
, Sedation Drugs
Drug Class Benzodiazepines
Prototype Diazepam Propofol
MOA Interact with GABA receptors enhancing inhibitory effects Promotes release of GABA, major inhibitory NT in the brain
of GABA in the brain
Therapeutic Uses IV sedation; produces unconsciousness and amnesia when Induction and maintenance of general anesthesia, sedation
used in large doses, IV induction
AEs Severe resp. dep.; hypotension Resp. dep., apnea; hypotension; risk for bacterial infection; IV site
pain (use large vein, lidocaine); Propofol infusion syndrome ( dose)
Nursing Implications Admin: emulsion in phospholipid carrier. Dedicated IV catheter for
continuous infusion. Change bottle tubing after 12hrs of hanging
Other DDIs: IV formulation incompatible with many drugs
Safety: Abuse potential *Narrow Therapeutic Index*
Hypnotics
Drug Class Benzodiazepines BZDRAs Melatonin Receptor Agonists Sedating Antidepressants Antihistamines
Prototype Triazolam Zolpidem Ramelteon Trazodone Diphenhydramine
MOA Interact with GABA receptors, Agonist @ BZD Activates melatonin receptors sleep latency and prolongs (Benadryl)
enhancing inhibitory effects of receptor site on sleep duration
GABA in brain GABA receptor
Therapeutic DOC for short-term insomnia Insomnia only First line for insomnia Insomnia (esp. in conjunction w/ FDA approved for
Uses tx; anxiety; seizure disorders CNS stimulating antidepressants) insomnia
AEs Tolerance, rebound insomnia; Daytime Somnolence, dizziness, Daytime sedation, Daytime sedation,
anterograde amnesia; drowsiness, fatigue, prolactin levels, anticholinergic effects, weight anticholinergic
teratogenic; CNS depression dizziness, sleep severe allergic rxn (small risk) gain, postural hypotension, effects
Overdose tx: Flumazenil driving dizziness
Nursing CIV Controlled Substance
Implications Withdrawal d/t abrupt d/c
from long-term high-dose use
(anxiety, insomnia, CNS
excitability > seizures) > wean
dose gradually
Other DDIs: resp. dep. When used DDIs: resp. dep. Wider therapeutic index, few OTC
with other CNS depressants With other CNS DDIs, low abuse potential
PK: Short half life dep. IV: avoid in hepatic
impairment/pregnancy
All BZD have essentially BZD Withdrawal
equivalent actions. Use depends Sx: anxiety, insomnia, tachycardia, diaphoresis, tremor, agitation, vomiting, seizures
on time course of action. Paradoxical agitation/rage can occur (unusual rxn)
