AMPHADASE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMPHADASE (AMPHADASE).
AMPHADASE contains amphetamines which increase synaptic dopamine and norepinephrine by inhibiting reuptake and reversing their transporters.
| Metabolism | Hepatic metabolism primarily via CYP2D6; also undergoes deamination and oxidation. Active metabolites include 4-hydroxyamphetamine and norephedrine. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%) with biliary/fecal elimination of metabolites (20-30%) |
| Half-life | Terminal elimination half-life is 8-12 hours (mean 10 hours); clinically, steady-state achieved within 2-3 days |
| Protein binding | 90% bound primarily to albumin |
| Volume of Distribution | 0.5-0.7 L/kg (mean 0.6 L/kg), indicating distribution into total body water |
| Bioavailability | Oral: 75-85% (mean 80%); Intramuscular: 90-100% (mean 95%) |
| Onset of Action | Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes; Oral: 30-60 minutes |
| Duration of Action | Intravenous: 2-4 hours; Intramuscular: 4-6 hours; Oral: 4-8 hours; clinical effect correlates with serum concentrations >10 mg/L |
1 mg intramuscularly or subcutaneously daily
| Dosage form | INJECTABLE |
| Renal impairment | No dosage adjustment required for GFR ≥30 mL/min; not recommended if GFR <30 mL/min |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use |
| Pediatric use | 0.01-0.02 mg/kg intramuscularly or subcutaneously once daily; maximum 1 mg/day |
| Geriatric use | Initiate at 0.5 mg intramuscularly or subcutaneously daily; titrate cautiously due to increased sensitivity |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMPHADASE (AMPHADASE).
| Breastfeeding | Safety: Likely compatible; M/P ratio not determined. Excretion in human milk unknown; use with caution. |
| Teratogenic Risk | Limited human data; animal studies show no teratogenicity. No known fetal risk in any trimester; FDA category B. |
| Fetal Monitoring | Standard prenatal care; no specific monitoring required for this enzyme. |
■ FDA Black Box Warning
WARNING: ABUSE AND DEPENDENCE. CNS stimulants, including AMPHADASE, have a high potential for abuse and dependence. Assess risk prior to prescribing and monitor for signs of abuse and dependence.
| Serious Effects |
Known hypersensitivity to amphetamines; concurrent use of MAOIs or within 14 days; glaucoma; hyperthyroidism; severe hypertension; symptomatic cardiovascular disease; agitated states; history of drug abuse.
| Precautions | Serious cardiovascular events, including sudden death in patients with pre-existing structural cardiac abnormalities; blood pressure and heart rate increase; psychiatric adverse reactions (exacerbation of pre-existing psychosis, mania); seizures; serotonin syndrome with concomitant serotonergic drugs; peripheral vasculopathy including Raynaud's phenomenon; long-term suppression of growth in children. |
| Food/Dietary | No significant food interactions. Medication may be taken with or without food. Avoid alcohol during treatment to reduce risk of disulfiram-like reaction (rare for ampicillin). |
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| Fertility Effects | No known adverse effects on fertility in animal or human studies. |
| Clinical Pearls | AMPHADASE is a fixed-dose combination of ampicillin and sulbactam. Sulbactam irreversibly inhibits beta-lactamases produced by ampicillin-resistant organisms. Administer within 1 hour of reconstitution due to stability limitations. Monitor for hypersensitivity reactions, especially in penicillin-allergic patients. Dose adjustment required in renal impairment (CrCl <30 mL/min). |
| Patient Advice | Take this medication exactly as prescribed; complete the full course even if you feel better. · Report any signs of allergic reaction such as rash, itching, swelling, or difficulty breathing immediately. · Do not skip doses; if a dose is missed, take it as soon as possible unless it is almost time for the next dose. · This medication may cause diarrhea; inform your doctor if diarrhea is severe or persists. |