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ephedrine (Akovaz)

 

Classes: Alpha/Beta Adrenergic Agonists

Dosing and uses of Akovaz (ephedrine)

 

Adult dosage forms and strengths

injectable solution

  • 50mg/mL (ephedrine sulfate [38mg/mL ephedrine base])

 

Hypotension

Indicated for the treatment of clinically important hypotension occurring in the setting of anesthesia

Initial dose: 5-10 mg IV bolus (must dilute, see Administration)

Administer additional boluses as needed, not to exceed a total cumulative dosage of 50 mg

Adjust dosage according to the blood pressure goaL

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

Start at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy

Drug is substantially excreted by the kidney, and the risk of adverse reactions may be greater with impaired renal function

Because elderly patients are more likely to have decreased renal function, carefully select dose and consider monitoring renal function

 

Akovaz (ephedrine) adverse (side) effects

Frequency not defined

Gastrointestinal disorders: Nausea, vomiting

Cardiac disorders: Tachycardia, palpitations (thumping heart), reactive hypertension, bradycardia, ventricular ectopics, heart rhythm/rate variability

Nervous system disorders: Dizziness

Psychiatric disorders: Restlessness

 

Warnings

Contraindications

None

 

Cautions

Serious postpartum hypertension and stroke have been described with coadministration of a vasopressor (ie, methoxamine, phenylephrine, ephedrine) and an oxytocic (ie, methylergonovine, ergonovine); monitor blood pressure if patient has received both ephedrine and an oxytocic

Repeated administration can result in tolerance and tachyphylaxis; an alternative vasopressor may be needed to mitigate unresponsiveness to treatment

When used to prevent hypotension, ephedrine has been associated with an increased incidence of hypertension compared with when ephedrine is used to treat hypotension

 

Pregnancy and lactation

 

Pregnancy

Ephedrine crosses the placenta; used at deliver for prevention and/or treatment of maternal hypotension associated with spinal anesthesia

Fetal/neonatal adverse reactions

  • Cases of potential metabolic acidosis in newborns at delivery with maternal ephedrine exposure have been reported in the literature
  • These reports describe umbilical artery pH of ≤7.2 at the time of delivery
  • Monitor newborn for signs and symptoms of metabolic acidosis
  • Monitoring of infant’s acid-base status is warranted to ensure that an episode of acidosis is acute and reversible

 

Lactation

Unknown if excreted in breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Akovaz (ephedrine)

Mechanism of action

Sympathomimetic amine that directly acts as an agonist at alpha- and beta­adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons

Resulting pharmacodynamic effects include increased heart rate, BP, cardiac output, and variable increases in peripheral resistance

Stimulates alpha-adrenergic receptors of smooth muscle cells in the bladder (increases resistance to urinary outflow)

Activation of beta-adrenergic receptors in the lungs promotes bronchodilation

 

Pharmacokinetics

Half-Life: 2.5-3.6 hr

Duration: 3-6 hr (PO)

Duration; hypotension: 60 min (IV/SC)

Onset; hypotension: immediate (IV); 10-20 min (IM)

Metabolism: Minimally metabolized in the liver

Metabolites: Benzoic acid, hippuric acid, norephedrine, p-hydroxyephedrine (inactive)

Excretion: Urine (60-77%)

 

Administration

IV Preparation

Must be diluted before administration as an IV bolus to 5 mg/mL by withdrawing 50 mg (1 mL) dilute with 9 mL 0.9% NaCl or D5W

Inspect parenteral drug products visually for particulate matter and discoloration prior to administration, whenever solution and container permit

 

Storage

25°C (77°F); excursions permitted to 15-30°C (59-86°F)

Store in carton until time of use

For single use only; discard unused portion