Ephedrine (Akovaz) Injection - Uses, Dose, Side effects, MOA, Brands

Ephedrine (Akovaz) is a stimulant drug that is used in the treatment of peri-operative hypotension (anesthesia-induced hypotension). It is also used as off-label medicine for the treatment of postoperative nausea and vomiting.

Ephedrine Uses:

  • Anesthesia-induced hypotension:

    • It is indicated in the treatment of anesthesia-induced hypotension.

Note:

  • The ephedrine for treatment of different conditions like acute bronchospasm, Stokes-Adams syndrome (e.g. presyncope/syncope) with complete heart block, narcolepsy, depression, or myasthenia gravis is not being used nowadays.
  • More effective agents available for these conditions.
  • Off Label Use of Ephedrine in Adults:

    • prevention of postoperative nausea and vomiting

Ephedrine (Akovaz) dose in Adults

Ephedrine (Akovaz) dose in the treatment of anesthesia-induced hypotension:

  • IV: 5 - 25 mg/dose IV push slowly; can be repeated accordingly to maintain blood pressure
  • Maximum total dose: 50 mg

Dose in the prevention of postoperative nausea and vomiting (off-label):

  • IM: 0.5 mg per kg at the end of surgery.

Ephedrine Dose in Children:

Dose in the treatment of anesthesia-induced hypotension:

Note: Use the smallest effective dose:

  • Infants, Children, and Adolescents ≤15 years: Limited data available:

    • Slow IV push: 0.1 to 0.3 mg/kg/dose, can be repeated accordingly to maintain blood pressure;
    • maximum dose: 25 mg per dose;
    • Maximum total dose: 50 mg
  • Adolescents >15 years:

    • IV: 5 to 25 mg/dose slow IV push repeat according to the requirement to maintain blood pressure;
    • Maximum total dose: 50 mg

Pregnancy Risk Factor C

  • There are currently no studies on animal reproduction.
  • It can also cross the placental boundary.
  • It is used to treat and prevent hypotension caused by spinal anesthesia during delivery in women who are having a cesarean section.
  • Combining oxytocin with severe postpartum hypertension can lead to stroke and even serious postpartum hypertension.
  • After the mother's use, neonates have been diagnosed with metabolic acidosis.

Use during breastfeeding:

  • Breast milk contains the drug.
  • According to the manufacturer the decision to use breastfeeding mothers should be made after considering the risks and benefits to the mother.

Dose in Kidney disease:

No dose adjustments listed in the manufacturer's labeling. Caution is advised

Dose in Liver disease:

No dose adjustments listed in the manufacturer's labeling.

Side effects of Ephedrine (Akovaz):

  • Cardiovascular:

    • Angina Pectoris
    • Bradycardia
    • Cardiac Arrhythmia
    • Hypertension
    • Palpitations
    • Pulse Irregularity
    • Tachycardia
    • Ventricular Ectopy
    • Visceral Vasoconstriction (Renal)
  • Central Nervous System:

    • Anxiety
    • Confusion
    • Delirium
    • Dizziness
    • Hallucination
    • Headache
    • Insomnia
    • Intracranial Hemorrhage
    • Nervousness
    • Precordial Pain
    • Restlessness
    • Tension
    • Vertigo
  • Dermatologic:

    • Diaphoresis
    • Pallor
  • Gastrointestinal:

    • Anorexia
    • Nausea
    • Vomiting
  • Genitourinary:

    • Dysuria
    • Oliguria
    • Urinary Retention (Males With Prostatism)
  • Neuromuscular & Skeletal:

    • Tremor
    • Vesicle Sphincter Spasm
    • Weakness
  • Respiratory:

    • Dyspnea
  • Miscellaneous:

    • Tachyphylaxis

Contraindications to Ephedrine (Akovaz):

  • Hypersensitivity to any component ephedrine, or other sympathomimetics
  • Angle-closure glaucoma
  • Myocardial sensitizing agents such as halothane, cyclopropane or halothane can be co-administered. cyclopropane, halothane

Warnings and precautions

  • Cardiovascular effects

    • High blood pressure can cause intracranial hemorhage.
    • It can cause potentially fatal arrhythmias in patients with heart disease or those who are taking myocardium sensitizing medications.
  • Urine output

    • Due to constriction in the renal blood vessels, there may be a decrease in urine output.
  • Cardiovascular disease

    • Ephedrine should not be used in situations where vasopressor medications are contraindicated. Angina pectoris and coronary artery disease are all possible side effects.
    • If necessary, use caution.
  • Diabetes:

    • Avoid Ephedrine in situations where vasopressor drugs are contraindicated.
  • Prostatic hyperplasia/urinary restriction:

    • Caution is advised in cases of prostatic hyperplasia or urinary stricture
  • Renal impairment

    • Increased elimination half-life could occur. Use caution if you have renal impairment
    • You should monitor for signs of renal impairment.
  • Thyroid dysfunction:

    • Avoid Ephedrine in situations where vasopressors drugs might be contraindicated.
    • Use caution when treating thyroid dysfunction.
  • Vasomotor symptoms:

    • Use caution if you have unstable vasomotor symptoms

Ephedrine (systemic): Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Alkalinizing Agents DirectActing may increase serum concentrations of Alpha-/Beta Agonists.
Alpha1-Blockers May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. In the same way, Alpha-/Beta Agonists could antagonize Alpha1Blocker vasodilation.
AtoMOXetine Might increase the hypertensive effects of Sympathomimetics. AtoMOXetine could increase the tachycardic effects of Sympathomimetics.
Atropine (Systemic) May increase the therapeutic effects of EPHEDrine Systemic.
Cannabinoid-Containing Products Sympathomimetics may increase the tachycardic effects of Sympathomimetics. Cannabidiol is an exception.
Inhibitors of carbonic anhydrase Increases the serum concentration of Alpha/Beta-Agonists through indirect-acting.
Cardiac Glycosides EPHEDrine (Systemic), may increase the arrhythmogenic effects of Cardiac Glycosides.
Chloroprocaine May enhance the hypertensive effect of Alpha-/Beta-Agonists.
CloNIDine May increase the therapeutic effects of EPHEDrine Systemic.
CloZAPine May diminish the therapeutic effect of Alpha-/Beta-Agonists.
Doxofylline Doxofylline may be more toxic or harmful if taken with Sympathomimetics.
Droxidopa EPHEDrine (Systemic), may increase the hypertensive effects of Droxidopa.
FentaNYL FentaNYL serum concentrations may be decreased by Alpha-/Beta Agonists (Indirect Acting). Particularly, the serum concentrations of fentanyl nasal spray may decrease and the onset may be delayed.
Guanethidine May increase the arrhythmogenic effects of Sympathomimetics. The hypertensive effects of Sympathomimetics may be enhanced by Guanethidine.
Oxytocin May increase the hypertensive effects of EPHEDrine Systemic.
Propofol May increase the therapeutic effects of EPHEDrine Systemic.
QuiNIDine EPHEDrine Systemic may have a reduced therapeutic effect. QuiNIDine may have a decreased therapeutic effect from EPHEDrine Systemic.
Rocuronium EPHEDrine (Systemic), may increase the therapeutic effects of Rocuronium.
Solriamfetol Sympathomimetics could increase the hypertensive effects of Solriamfetol.
Spironolactone May diminish the vasoconstricting effect of Alpha-/Beta-Agonists.
Sympathomimetics May increase the toxic/adverse effects of other Sympathomimetics.
Tedizolid Might increase the hypertensive effects of Sympathomimetics. Tedizolid could increase the tachycardic effects of Sympathomimetics.
Urinary acidifying agents Direct-Acting may cause a decrease in serum Alpha-/Beta Agonists.

Risk Factor D (Alternative therapy)

BenzylpenicilloylPolylysine Alpha-/Beta-Agonists may diminish the diagnostic effect of BenzylpenicilloylPolylysine. Management: A histamine skin test may be used as a positive control in order to determine if a patient is able to mount a wheal or flare response.
Topical Cocaine Sympathomimetics may increase hypertensive effects. Management: If possible, consider other options to this combination. Concurrent use of this combination can cause significant elevations in blood pressure and heart rate. You should also be aware of any signs of myocardial injury.
Hyaluronidase May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Avoid the use of hyaluronidase to enhance dispersion or absorption of alpha-/beta-agonists. Clinically, it may be indicated to use hyaluronidase in patients who are receiving alpha/beta-agonists for other purposes.
Linezolid Sympathomimetics may increase hypertensive effects. Patients receiving linezolid should be reduced in initial doses and closely monitored for an increased pressor response. There are no recommendations for dose adjustments.
Serotonin/Norepinephrine Reuptake Inhibitors May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists.
Tricyclic Antidepressants DirectActing may increase the vasopressor effects of Alpha/Beta-Agonists. Patients on tricyclic antidepressants should avoid direct-acting alpha/beta-agonists. Monitor for increased pressure effects when combined and reduce the initial doses of alpha/beta-agonists.

Risk Factor X (Avoid Combination)

Ergot Derivatives May enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. There are exceptions: Ergoloid Mesylates and Nicergoline.
Inhalational Anesthesia EPHEDrine (Systemic), may increase the arrhythmogenic effects of Inhalational Anesthetics.
Iobenguane Radiopharmaceutical Products Iobenguane Radiopharmaceutical Products may be affected by indirect-acting Alpha-/Beta-Agonists. Management: Stop using any drugs that could inhibit or interfere catecholamine transport for at least five biological half-lives prior to iobenguane. These drugs should not be administered until 7 days following each iobenguane dosage.
Monoamine Oxidase Inhibitors May increase the hypertensive effects of Alpha/Beta Agonists (Indirect Acting). Although linezolid should interact through this mechanism, management guidelines differ from those for other monoamine-oxidase inhibitors. For more information, refer to linezolid's specific monographs. Exceptions: Linezolid; Tedizolid.

Monitoring parameters:

  • Blood pressure,
  • pulse
  • respiratory symptoms
  • Monitor patients with renal impairment for adverse reactions.

How to administer Ephedrine (Akovaz)?

Administer slow IV push as a diluted solution. For post-operative nausea and vomiting (off-label use), Use IM route

Mechanism of action of Ephedrine (Akovaz):

It releases tissue stores of norepinephrine and produces alpha- or beta-adrenergic stimulation. It is longer-acting and less potent as compared to epinephrine.

At the beginning:IM:

  • In between 10 and 20 minutes.

Duration:

  • Pressor/cardiac effects: SubQ: 1 hour

Absorption: IV:

  • Rapid, complete

Metabolism:

  • It is minimally metabolized in the liver; metabolites include p-hydroxyephedrine, p-hydroxynorephedrine, norephedrine

Half-life elimination:

  • Dependent upon urinary pH;
    • Urine pH 5: about 3 hours;
    • Urine pH 6.3: about 6 hours

Excretion:

  • Urine (primarily in unchanged form; depends upon urinary pH with the greatest excretion in acid pH)

International Brand Names of Ephedrine:

  • Akovaz
  • Efedrin
  • Efedrin NAF
  • Efedrina
  • Efipres
  • Ephedrine Hydrochloride
  • Ephedrine Sulfate Inj
  • Epherit
  • Forasm
  • Kemiphedrine
  • Muchan
  • Sulfato de Efedrina
  • Sulfato de Efedrina Klinos
  • Sulfidrin
  • Sympathodrine
  • Tabellae Ephedrini
  • Unifedrine
  • Vasodrin
  • Vitadrine

Ephedrine Brands Names in Pakistan:

Ephedrine Tablets 30 mg in Pakistan

Aksidrin Akson Pharmaceuticals (Pvt) Ltd.
E-Drine Tg Pharma
E-Drine Tg Pharma
Efdrin Regent Laboratories Ltd.
Efdrin Regent Laboratories Ltd.
Efed Wilshire Laboratories (Pvt) Ltd.
Efedra Genome Pharmaceuticals (Pvt) Ltd
Ephedra Polyfine Chempharma (Pvt) Ltd.
Ephedrine Shifa Laboratories.(Pvt) Ltd.
Ephedrine Karachi Chemical Industries
Ephedrine Krka-Pak Pharmaceutical & Chemical Works
Ephedrine Jawa Pharmaceuticals(Pvt) Ltd.
Ephedrine Hcl Unexo Labs (Pvt) Ltd.
Epherin Semos Pharmaceuticals (Pvt) Ltd.
F-Drins Farm Aid Group Pak Ltd.
Globodrin Global Pharmaceuticals
Metone Danas Pharmaceuticals (Pvt) Ltd
Pliphid Pliva Pakistan (Pvt) Limited

Comments

NO Comments Found