AHZANTIVE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AHZANTIVE (AHZANTIVE).
AHZANTIVE is a synthetic opioid agonist that binds to mu-opioid receptors in the central nervous system, mimicking endogenous endorphins to produce analgesia, euphoria, and sedation. It also exhibits antagonistic activity at kappa-opioid receptors, which may contribute to its unique side effect profile.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent CYP2D6. Main metabolites include norAHZANTIVE (major) and AHZANTIVE-6-glucuronide. |
| Excretion | Primarily renal excretion (70-80% unchanged) with 10-15% biliary/fecal elimination; minor CYP450 metabolism. |
| Half-life | Terminal elimination half-life of 4-6 hours in healthy adults; prolonged to 8-12 hours in moderate renal impairment (CrCl 30-50 mL/min). |
| Protein binding | 92-95% bound to albumin; slight decrease in hypoalbuminemia. |
| Volume of Distribution | 0.8-1.2 L/kg, reflecting extensive tissue distribution; larger Vd in obesity. |
| Bioavailability | Oral: 60-70% (first-pass effect); extended-release: 80-90% relative to immediate-release; subcutaneous: 95%. |
| Onset of Action | Intravenous: within 2-5 minutes; oral: 30-60 minutes on empty stomach. |
| Duration of Action | Intravenous: 4-6 hours; oral: 6-8 hours, extended-release: 12-24 hours. Clinical effect correlates with free drug concentration. |
100 mg orally twice daily
| Dosage form | INJECTABLE |
| Renal impairment | For GFR 30-50 mL/min: 50 mg twice daily; GFR 15-29 mL/min: 50 mg once daily; GFR <15 mL/min: 50 mg every other day |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | Not approved for patients <18 years; no established dosing |
| Geriatric use | No specific adjustment; monitor renal function and reduce dose per renal criteria |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AHZANTIVE (AHZANTIVE).
| Breastfeeding | Present in breast milk; M/P ratio not determined. Not recommended unless benefit outweighs risk; monitor infant for diarrhea, rash, and vomiting. |
| Teratogenic Risk | First trimester: Inadequate human data; animal studies suggest no teratogenicity at therapeutic doses. Second and third trimesters: No known structural or functional adverse effects, but caution due to limited data. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS.
| Serious Effects |
Absolute: known hypersensitivity to AHZANTIVE, significant respiratory depression, acute or severe bronchial asthma, GI obstruction (including paralytic ileus), and concomitant use of MAOIs within 14 days. Relative: increased intracranial pressure, head injury, impaired renal/hepatic function, and history of substance abuse.
| Precautions | Risk of respiratory depression, particularly in elderly or debilitated patients; serotonin syndrome when co-administered with serotonergic drugs; adrenal insufficiency; severe hypotension; seizures; and risk of misuse, abuse, and addiction. |
| Food/Dietary | Avoid tyramine-rich foods including aged cheeses (e.g., cheddar, blue cheese), cured or smoked meats, fermented foods (e.g., sauerkraut, kimchi), soy products, broad bean pods, and alcoholic beverages (especially beer and wine). Excessive caffeine may also increase blood pressure risk. Patients should follow a low-tyramine diet. |
Loading safety data…
| Maternal hepatic and renal function tests; fetal growth monitoring via ultrasound if prolonged use. |
| Fertility Effects | No evidence of impaired fertility in animal studies; human data insufficient. |
| Clinical Pearls | AHZANTIVE is a reversible inhibitor of monoamine oxidase A (MAO-A). It is used for major depressive disorder. Avoid concurrent use with serotonergic drugs due to risk of serotonin syndrome. Monitor blood pressure for hypertensive crises, especially with tyramine-rich foods. Start at 10 mg once daily, titrate to 20 mg daily after 2 weeks. Discontinue 14 days before switching to other antidepressants. |
| Patient Advice | Take AHZANTIVE exactly as prescribed, usually once daily. · Avoid foods high in tyramine such as aged cheeses, cured meats, fermented products, and certain alcoholic beverages. · Report any sudden severe headache, palpitations, or nausea immediately as these may indicate a hypertensive crisis. · Do not use with other antidepressants or St. John's wort; wait 14 days after stopping AHZANTIVE before starting another antidepressant. · Do not stop abruptly; taper under medical supervision. · Inform all healthcare providers that you are taking AHZANTIVE before any surgery or procedure. |