Week 10: Tolerance and Dependence Pharmacology

Disulfiram (Antabuse) - MOA

Causes accumulation of acetaldehyde to produce an unpleasant reaction when alcohol is consumed.

Disulfiram (Antabuse) - Therapeutic Uses

To maintain sobriety for patients with chronic alcoholism.

Disulfiram (Antabuse) - Administration

Orally (PO). Do not take if alcohol has been consumed. Can be sedating.

Disulfiram (Antabuse) - Adverse Effects

Black Box Warning: Do not give if patient consumed alcohol in last 12 hours. With alcohol: Headache, confusion, seizures, chest pain, flushing, palpitations, hypotension, sweating, blurred vision, N/V, dysrhythmias, heart failure, cardiovascular collapse, MI, death. Can also cause hepatic failure.

Disulfiram (Antabuse) - Nursing Considerations

Ensure patient is fully aware they cannot consume any alcohol. Monitor for signs of the disulfiram-alcohol reaction and for hepatotoxicity.

Benzodiazepines (e.g., Chlordiazepoxide, Lorazepam, Diazepam) - MOA

Enhance the effects of GABA (an inhibitory neurotransmitter) to slow down neuronal activity.

Benzodiazepines - Therapeutic Uses

Treatment of withdrawal from alcohol and CNS depressants; anxiety disorders.

Benzodiazepines - Administration

PO, IM, IV. Should be administered as soon as it is identified the patient needs it.

Benzodiazepines - Adverse Effects

Black Box Warning: Combination use with opioids can cause slowed/difficult breathing and death. CNS depression, lethargy, sedation, dizziness.

Benzodiazepines - Nursing Considerations

Monitor vital signs. Taper dose gradually based on patient's response (e.g., using CIWA/CIWA-Ar scale).

Naltrexone - MOA

Blocks opioids from binding to opioid receptor sites.

Naltrexone - Therapeutic Uses

Maintain an opioid-free state in opioid use disorder; decrease cravings in alcohol use disorders.

Naltrexone - Administration

PO, IM depot injection.

Naltrexone - Adverse Effects

Black Box Warning: Risk of hepatocellular injury. May precipitate withdrawal. GI upset.

Naltrexone - Nursing Considerations

NOT for emergency use (do not confuse with naloxone). Patient must be opioid-free for at least 7 days before starting therapy.

Buprenorphine - MOA

A partial opioid agonist. It has agonist effects at some receptor sites and antagonist effects at others.

Buprenorphine - Therapeutic Uses

Treatment of moderate to severe pain; opioid dependence.

Buprenorphine - Administration

PO, buccal film, sublingual (SL) tablets, subcutaneous depot injection, IV, IM.

Buprenorphine - Adverse Effects

Black Box Warning: Risk of addiction, abuse, misuse, and life-threatening respiratory depression. N/V, drowsiness, dizziness, orthostatic hypotension, urinary retention.

Buprenorphine - Nursing Considerations

May precipitate withdrawal if taken with full opioid agonists. Avoid combining with other CNS depressants.

Buprenorphine/Naloxone (Suboxone) - Administration

Available as a sublingual film/tablet and buccal film.

Flumazenil (Romazicon) - MOA

Competes with benzodiazepines for receptor sites, acting as a GABA receptor antagonist.

Flumazenil (Romazicon) - Therapeutic Uses

Reversal of benzodiazepine-induced sedation, coma, and respiratory depression (overdose).

Flumazenil (Romazicon) - Administration

IV, often requiring repeated doses.

Flumazenil (Romazicon) - Adverse Effects

Black Box Warning: Risk of seizures. Overdose symptoms may recur. May precipitate withdrawal.

Flumazenil (Romazicon) - Nursing Considerations

Monitor for return of sedation/respiratory depression and for seizure activity. Use with caution in patients with a history of seizures.