Drug Name Indication (Bold is FDA approved) Neurotransmitter(s) Affected Target Symptoms Half-life (T1/2), Metabolism (CYP 450 enzyme) Notable Side
... [Show More] Effects (link to NT or affected brain circuit) Initial Dosing Considerations Specific lifespan considerations (age, pregnancy, breastfeeding)
Buprenorphine
(Subutex) Indication:
◗ Maintenance treatment of opioid dependence (sublingual)
◗ Maintenance treatment of
opioid dependence in patients who have achieved and sustained prolonged clinical stability on low-to-moderate doses (no more than 8 mg) of a transmucosal buprenorphine- containing product (implant)
◗ Moderate to severe opioid
use disorder in patients who have initiated treatment with a transmucosal buprenorphine-containing product, followed by dose adjustment for a minimum of 7 days (injection)
Affected Neurotransmitters:
◗ Partial agonist at mu opiate receptors
◗ Antagonist at the kappa
opioid receptor
◗ Agonist at delta opioid receptors
◗ Partial agonist at nociceptin Half-life:
Sublingual buprenorphine: 24–42 hours
Naloxone:
2–12 hours Implant: Tmax is 12
hours; time to steady state is 4 weeks
Metabolism: CYP450 3A4 Notable Side Effects:
◗ Headache, constipation, nausea
◗ Oral hypoesthesia,
glossodynia
◗ Orthostatic hypotension
◗ Implant specific:
insertion site pain, pruritis, erythema
Side Effect Pathways:
✓ Binding at mu opioid receptors Initial Dosing Considerations:
◗ Patients must be in a mild withdrawal state prior to starting buprenorphine
◗ Day 1 – 8 mg
◗ Day 2 – 12 or 16 mg
◗ Days 3-7 – Increase in
increments of 4 mg to max dose of 32 MG
◗ Observe patient for at least 2
hours with initial dose, then have 1–2 visits in first week
◗ Achieve the lowest dose that
eliminates withdrawal symptoms and illicit opioid use
◗ During stabilization patients
should be seen once per week
◗ During maintenance patients should be seen biweekly or monthly
Specific lifespan considerations Age:
◆ Elderly - Use with caution
◆ Children and adolescents -
Safety and efficacy have not been established
Pregnancy:
◆ Controlled studies have not
been conducted in pregnant women
◆ Buprenorphine may be
opioid peptide receptors
Target Symptoms:
◗ Opioid dependence preferable to methadone in pregnant women
◆ Neonatal withdrawal has been
reported following use of buprenorphine during pregnancy
◆ Not generally recommended
for use during pregnancy, especially
during first trimester
◆ Effective June 30, 2015, the US FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001
Breastfeeding:
◆ Some drug is found in mother’s breast milk
◆ Recommended either to
discontinue drug or bottle feed
Buprenorphine/Naloxone (Suboxone, Zubsolv, Bunavail) Indication:
◗ Maintenance treatment of opioid dependence
◗ Induction of treatment for
opioid dependence (Bunavail only) Half-life: Buprenorphine: 24–42 hours Naloxone:
2–12 hours
Metabolism: CYP 450 3A4 Notable Side Effects:
◗ Headache, constipation, nausea
◗ Oral hypoesthesia,
glossodynia
◗ Orthostatic hypotension
◗ Implant specific: insertion site pain, Initial Dosing Considerations:
◗ Patients must be in a mild withdrawal state prior to starting buprenorphine
◗ Day 1 - 8 mg/2 mg
◗ Day 2 – 12 mg/3 mg or 16
Affected Neurotransmitters:
◗ Partial agonist at mu opiate receptors – Buprenorphine
◗ Antagonist at the mu opioid receptor - Naloxone
◗ Antagonist at the kappa opioid receptor
◗ Agonist at delta opioid receptors
◗ Partial agonist at nociceptin opioid peptide receptors
Target Symptoms:
◗ Opioid dependence pruritis, erythema
Side Effect Pathways:
✓ Binding at mu opioid receptors mg/4 mg
◗ Days 3-7 - Increase in increments of 4 mg/1 mg to max dose of 32 MG/8 mg
◗ Observe patient for at least 2
hours with initial dose, then have 1–2 visits in first week
◗ Achieve the lowest dose that
eliminates withdrawal symptoms and illicit opioid use
◗ Stabilization (up to 2 months)
and maintenance dose is generally 8 mg/2 mg up to 24 mg/6 mg
◗ During stabilization patients
should be seen once per week
◗ During maintenance patients should be seen biweekly or monthly
Specific lifespan considerations Age:
◆ Elderly - Use with caution
◆ Children and adolescents - Safety and efficacy have not been established
Pregnancy:
◆ Controlled studies have not been conducted in pregnant women
◆ Buprenorphine may be
preferable to methadone in pregnant women
◆ Neonatal withdrawal has been
reported following use of
buprenorphine during pregnancy
◆ Extremely limited data on
sublingual naloxone exposure in pregnancy
◆ Not generally recommended
for use during pregnancy, especially during first trimester
◆ Effective June 30, 2015, the US
FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001
Breastfeeding:
◆ Some drug is found in mother’s breast milk
◆ Recommended either to
discontinue drug or bottle feed
Methadone
(Dolophine, Methadose) Indication:
◗ Moderate-to-severe pain not responsive to nonnarcotic analgesics
◗ Maintenance treatment of
opioid addiction (heroin or other morphine-like drugs), Half-life:
15 to 55 hours
Metabolism: CYP 450 3A4, 2B6, 2C19, 2C9,
and 2D6 Notable Side Effects:
◗ Dizziness
◗ Tiredness
◗ Sweating
◗ Legs swelling
◗ Rash or hives
◗ Chest pain Initial Dosing Considerations:
◗ Methadone is administered daily under close supervision
◗ When used for detoxification:
Patient may receive methadone when there are significant symptoms of withdrawal, in [Show Less]