substance-related disorders PART 2 opiates and depressants - dr krysiak

what kind of opiates have the greatest abuse potential?

a. full agonist

b. antagonist

c. partial agonist

a.

list the opiate antagonists (bind to receptors but do not activate —> no effect)

naloxone

naltrexone

what is buprenorphine?

a. full agonist

b. antagonist

c. partial agonist

c.

what does SAMHSA recommend to assess addictive potential (opiates)?

current opioid misuse measure (COMM)

screener and opioid assessment for patients with pain (SOAPP)

what are the most important factors to consider in terms of addictive potential (opiates)?

• prior history of substance abuse

• family history of substance abuse

• major psychiatric pathology

what screener for opiate addiction is based on potential for abuse PRIOR to starting therapy?

a. SOAPP

b. COMM

a.

what screener for opiate addiction is useful for patients ALREADY on chronic opiates?
a. SOAPP

b. COMM

b.

what is important to remember with COMM screening?

NOT A LIE DETECTOR

may have false positives and negatives

who is PDMP used by?

who is required to report?

• prescribers

• pharmacies — required reporting

• law enforcement

• monitoring/safety programs

how does acute opiate intoxication present?

• decr. level of consciousness

• may be combative

• decr. respiratory drive

• slurred speech

• miosis

• motor retardation

list signs of acute opiate intoxication

• bradycardia

• hypotension

• hypothermia

• sedation

• miosis (pinpoint pupils)

• hypokinesis (slowed movement)

• slurred speech

• head nodding

list nonpharm tx of opiate intoxication

• place in a safe and monitored environment

• decr. external stimulation and provide orientation and reality testing

• monitor for signs and symptoms of respiratory depression

• intubation may be required

what is the pharmacologic tx of opiate intoxication?

a. clonidine

b. benzodiazepines

c. naloxone

d. lofexidine

c.

what formulations of naloxone are given for take-home use? (SATA)

a. IV

b. IM

c. IN

b. c.

how often can we repeat the dose of naloxone?

what is the max dose?

repeat every 2-3 minutes until full reversal achieved

up to a total dose of 10 mg

when does the onset of opioid withdrawal typically occur?

list signs and symptoms of opioid withdrawal

think of it as the opposite of opiate intoxication

• tachycardia

• hypertension

• hyperthermia

• insomnia

• mydriasis (enlarged pupils)

• hyperreflexia

• diaphoresis

• piloerection

• incr. respiratory rate

• lacrimation

• yawning

• rhinorrhea

• muscle spasms

• abdominal cramps, N/V/D

• bone and muscle pain

• anxiety

how do we evaluate opiate withdrawal?

clinical opiate withdrawal scale (COWS)

list sx management options for opiate withdrawal

• clonidine

• lofexidine (lucemyra)

• benzos

• anti-emetics

• muscle relaxants

  • as needed

what does clonidine decrease when used for opioid withdrawal?

what do we need to monitor?

decreases noradrenergic hyperactivity

-reduces nausea, vomiting, diarrhea, cramps, sweating

monitor BP and sedation

-hold dose BP <90/60

idk if we need to know

what dose of clonidine is initiated for opioid withdrawal?

0.1 mg PO TID

which of these meds to treat opioid withdrawal are alpha 2-adrenergic agonists? (SATA)

a. clonidine

b. lofexidine (lucemyra)

c. benzos

d. anti-emetics

e. muscle relaxants

a. b.

how long do we continue lofexidine for opioid withdrawal?

adverse effects?

what do we need to monitor?

continue for up to 14 days

adverse effects: hypotension, bradycardia, syncope, QT prolongation

monitor ECG in high-risk populations

monitor for electrolyte abnormalities

which of these requires hepatic dosing and is metabolized by CYP2D6?

a. clonidine

b. lofexidine

b.

list nonpharm tx for opioid use disorder therapy

• support groups and counseling

• combined with medications for best outcomes

list medications for opioid use disorder (MOUD)

• agonist therapy

  • methadone

  • buprenorphine

  • heroin

• antagonist therapy

  • naltrexone

methadone is primarily metabolized through ______ to inactive metabolite

CYP3A4

ex: antiretroviral drugs, rifampin

CYP3A4 inducers ______ levels of methadone

a. decrease

b. increase

a.

ex: azole fungals, macrolides (erythromycin)

CYP3A4 inhibitors ______ levels of methadone

a. decrease

b. increase

b.

when do we need and EKG if a patient is being put on methadone?

at what QTc level do we decrease dose or remove other causes?

EKG at baseline, 30 days, and then annually

QTc > 500 remove other causes or decrease dose

how do we dose methadone initially for OUD?

• 20 mg PO daily

• wait 2-4 hours

  • no withdrawal sx: continue as daily dose

  • withdrawal sx: give additional 5-10 mg dose

• first total daily dose is limited to 40 mg

which of these treatments for OUD is a partial mu agonist and weak kappa antagonist?

a. methadone

b. buprenorphine

c. heroin

d. naltrexone

b.

which buprenorphine product comes as tablets and films?

a. buprenorphine (Subutex)

b. buprenorphine/naloxone (Suboxone)

b.

buprenorphine is metabolized by ______

CYP3A4

why did we combine bupernorphine with naloxone?

it prevents abuse basically somehow idk

it’s not absorbed when it’s taken as intended (SL)

do we need to wait after stopping opioids before starting buprenorphine?

YES — wait > 12 hours after last use

*usually wait till onset of withdrawal symptoms

how are patients usually monitored when on buprenorphine?

in office at 2-hour intervals until withdrawal symptoms are eliminated

which buprenorphine product would be equivalent to subutex 4 mg tablet?

a. subutex 4 mg film

b. suboxone 4/1 mg tablet

b.

different dosage forms are not equivalent

what OUD treatment requires a REMS program?

buprenorphine implant (Probuphine)

what patients are eligible for the buprenorphine implant (probuphine)?

• sustained stability on transmucosal (SL) buprenorphine

• on dose of ≤ 8 mg of SL tablet for ≥ 3 months

T/F many patients require life-long OUD therapy

TRUE

can anyone prescribe buprenorphine?

NO — must have special training and waiver

DEA number begins with “X”

do we need to wait for patients to be opioid free before starting naltrexone?

YES — wait 7-10 days

idk if we need to know

what oral dose of naltrexone may increase risk of liver damage?

> 50 mg

when does naltrexone require a REMS program?

injection

is naltrexone a controlled substance?

NO

how do we manage pain with opiate dependence?

use non-opioids and non-pharm options 1st for pain

single provider for any opiate use

how do we manage pain with opiate dependence if patients are not on methadone?

START METHADONE

how do we manage pain with opiate dependence if patients are on naltrexone?

• won’t respond to opiate agonists

• withhold naltrexone for 3-7 days after opiate

• withhold naltrexone for 72 hours prior to opiate need

how do we manage pain with opiate dependence if patients are on buprenorphine?

• consider high doses and/or more potent agonists (fentanyl)

• consider adjunct options (BZD, ketamine)

• if full agonist is needed: d/c buprenorphine

how should we treat pregnant patients with opiate abuse?

med therapy with an opioid agonist

what medications can we use in pregnancy with opiate abuse? (SATA)

a. methadone

b. buprenorphine

c. naltrexone

a. b.

T/F benzodiazepines do not typically cause life-threatening respiratory depression as a single agent

TRUE

list signs/symptoms of benzodiazepine intoxication

• memory impairment

• drowsiness

• visual disturbances

• confusion

• GI distress

• slurred speech

• poor coordination

• swaying

• bloodshot eyes

how do we treat benzodiazepine intoxication?

flumazenil (romazicon)

list signs/symptoms of benzodiazepine withdrawal

• agitation and restlessness

• dizziness

• flu-like sx

• impaired memory and concentration

• n/v

• visual disturbances

• convulsions

• hallucinations

how do we treat benzodiazepine withdrawal?

benzo as replacement therapy and to prevent seizures

taper benzo over a long duration

what is the most commonly abused OTC medication?

dextromethorphan

what is known as “robodosing” or “robotripping”?

consuming large quantities of dextromethorphan to become intoxicated

may cause profound hallucinogenic effect

how do you treat dextromethorphan intoxication?

naloxone

but mixed efficacy