AKOVAZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AKOVAZ (AKOVAZ).
Akovaz (ephedrine sulfate) is a sympathomimetic amine that directly stimulates alpha- and beta-adrenergic receptors, and indirectly by releasing norepinephrine from presynaptic terminals, leading to increased heart rate and contractility, and vasoconstriction.
| Metabolism | Hepatic metabolism via oxidative deamination and demethylation; primarily metabolized by CYP2D6; some metabolites are active. |
| Excretion | Renal: ~70% unchanged; biliary/fecal: ~30% as metabolites and unchanged drug. |
| Half-life | Terminal elimination half-life: 3-4 hours, prolonged in renal impairment (up to 8-12 hours in severe CKD). |
| Protein binding | 85% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 1.5-2.0 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 75% (first-pass metabolism minimal). |
| Onset of Action | Oral: 0.5-1 hour; IV: immediate (within minutes). |
| Duration of Action | 4-6 hours for therapeutic effect; extended up to 12 hours in hepatic impairment. |
5 mg intravenously once daily.
| Dosage form | SOLUTION |
| Renal impairment | Not required as AKOVAZ is not renally excreted. |
| Liver impairment | No dose adjustment needed based on Child-Pugh classification. |
| Pediatric use | 0.1 mg/kg intravenously once daily, maximum 5 mg. |
| Geriatric use | No specific dose adjustment required; use caution due to potential age-related decreased renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AKOVAZ (AKOVAZ).
| Breastfeeding | Ephedrine is excreted into breast milk. The milk-to-plasma (M/P) ratio is approximately 2.5-3.0. Peak milk concentration occurs 1-2 hours after dose. Potential for infant stimulation, irritability, and sleep disturbances. Use with caution; monitor infant for adverse effects. Avoid in lactation if possible or use lowest effective dose for shortest duration. |
| Teratogenic Risk | Akovaz (ephedrine sulfate) is classified as FDA Pregnancy Category C. In first trimester, there is insufficient human data; animal studies show teratogenic effects at high doses. In second and third trimesters, use may cause fetal tachycardia, reduced uteroplacental blood flow, and potential for neonatal withdrawal or toxicity. Risk of maternal hypertension and decreased uterine perfusion outweighs benefits unless clearly indicated. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to ephedrine or other sympathomimetics","Concurrent use with MAOIs or within 14 days after discontinuation","Angle-closure glaucoma","Severe hypertension or cardiovascular disease"]
| Precautions | ["Hypertension: May cause severe hypertension, including hypertensive crisis, especially with concurrent MAOIs or other vasopressors.","Arrhythmias: May induce ventricular arrhythmias, especially in patients with underlying cardiac disease.","Risk of stroke: Hypertensive effects may increase risk of intracranial hemorrhage.","Tachyphylaxis: Repeated use may lead to decreased response.","Extravasation: Risk of tissue necrosis if extravasation occurs.","Use caution in patients with hyperthyroidism, pheochromocytoma, or diabetes."] |
| Food/Dietary | No known food interactions. This drug is administered intravenously, so dietary restrictions are not applicable. However, oral intake should not interfere with therapy. |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and evidence of uteroplacental insufficiency (fetal heart rate patterns, uterine tone). Continuous fetal heart rate monitoring during administration in pregnancy. Assess for maternal hypertension, tachycardia, arrhythmias. Monitor for signs of fetal distress due to reduced placental perfusion. Postnatal monitor neonate for tachycardia, hypertension, irritability, or withdrawal symptoms. |
| Fertility Effects | No specific studies on ephedrine's effect on human fertility. In animal studies, no adverse effects on fertility at therapeutic doses. However, vasoconstrictive effects may theoretically impair uterine and ovarian blood flow; clinical significance unknown. Use caution in women attempting conception. No known impact on spermatogenesis or male fertility. |
| Clinical Pearls | AKOVAZ (ceftolozane/tazobactam) is a cephalosporin/beta-lactamase inhibitor combination used primarily for hospital-acquired pneumonia and complicated urinary tract infections. Monitor renal function closely; dose adjustment required for CrCl < 50 mL/min. Administer intravenously over 1 hour. Observe for hypersensitivity reactions, including anaphylaxis, particularly in penicillin-allergic patients. Consider cross-reactivity with other beta-lactams. Collect cultures before initiation. |
| Patient Advice | This medication is given intravenously to treat serious bacterial infections. · Report any signs of allergic reaction immediately: rash, itching, difficulty breathing, swelling of face or throat. · Diarrhea may occur; contact your provider if it is severe, watery, or bloody. · Do not skip doses; complete the full course of treatment even if you feel better. · Tell your healthcare provider about all medications, especially blood thinners (e.g., warfarin) and other antibiotics. · Kidney function will be monitored with blood tests; drink adequate fluids unless told otherwise. |