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

Ephedrine is a medication and stimulant compound derived from plants in the Ephedra genus. It has been used for various medical purposes, including as a decongestant, bronchodilator (to treat asthma), and to aid weight loss. It is a sympathomimetic amine, meaning it mimics the effects of the sympathetic nervous system, which controls functions such as heart rate, blood pressure, and metabolism.

Due to its stimulant properties, ephedrine has also been used as a performance-enhancing drug and as an ingredient in some dietary supplements marketed for weight loss and athletic performance. However, its use in these contexts has been controversial due to concerns about its safety and potential for abuse.

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 recommended for the management of hypotension brought on by anesthesia.

Note:

  • Ephedrine is no longer utilized to treat a variety of ailments, such as acute bronchospasm, Stokes-Adams syndrome (such as presyncope/syncope) with full heart block, narcolepsy, depression, or myasthenia gravis.
  • For some disorders, there are more potent treatments available.
  • 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: 

  • The dose is usually between 5 to 25 milligrams at a time, given slowly.
  • If needed, they can give it again to keep the blood pressure stable.
  • But they shouldn't give more than a total of 50 milligrams.

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

  • After surgery, if someone might feel nauseous or vomit, doctors might use ephedrine in a way that's not officially approved (called off-label).
  • They might inject it into a muscle at a dose of 0.5 milligrams per kilogram of the person's weight at the end of the surgery.

Ephedrine Dose in Children:

Dose in the treatment of anesthesia-induced hypotension:

Use the lowest effective dosage possible:

  • When children and adolescents under 15 years old have low blood pressure because of anesthesia, doctors might give them ephedrine through a vein.
  • The dose depends on their weight and ranges from 0.1 to 0.3 milligrams per kilogram of body weight for each dose, given slowly.
  • They can repeat this dose if needed to keep the blood pressure stable, but they shouldn't give more than 25 milligrams in one dose or a total of 50 milligrams overall.
  • For adolescents over 15 years old, the dose is similar to adults: between 5 to 25 milligrams per dose, repeated as necessary, but not exceeding a total of 50 milligrams.

Pregnancy Risk Factor C

  • Ephedrine is considered a Pregnancy Risk Factor C, meaning there haven't been specific studies on its effects during pregnancy in animals or humans.
  • However, it does cross the placenta, potentially affecting the unborn baby.
  • Doctors sometimes use ephedrine during cesarean sections to prevent or treat low blood pressure in the mother due to spinal anesthesia.
  • However, there are risks, including postpartum high blood pressure and the possibility of stroke if ephedrine is given with oxytocic medications.
  • Newborns might also experience metabolic acidosis if their mothers were given ephedrine, so careful monitoring is necessary in such cases.

Use during breastfeeding:

  • Ephedrine is known to be excreted in breast milk.
  • The decision to breastfeed while undergoing therapy with ephedrine should be carefully considered, weighing the potential risk of exposing the infant to the medication against the benefits of treatment for the mother.
  • It's essential for mothers and their healthcare providers to have an open discussion about this matter to make an informed decision that prioritizes the well-being of both the mother and the baby.

Dose in Kidney disease:

  • The manufacturer's labeling does not specify any dosage adjustments for ephedrine in individuals with renal impairment.
  • However, caution should be exercised when using ephedrine in such cases.

Dose in Liver disease:

  • The manufacturer's labeling for ephedrine does not include specific dosage adjustments for individuals with hepatic impairment.

Side effects of Ephedrine (Akovaz):

  • Cardiovascular:
    • Ventricular Ectopy
    • Visceral Vasoconstriction (Renal)
    • Angina Pectoris
    • Hypertension
    • Palpitations
    • Bradycardia
    • Cardiac Arrhythmia
    • Pulse Irregularity
    • Tachycardia
  • Dermatologic:
    • Diaphoresis
    • Pallor
  • Central Nervous System:
    • Dizziness
    • Hallucination
    • Headache
    • Insomnia
    • Anxiety
    • Confusion
    • Delirium
    • Intracranial Hemorrhage
    • Restlessness
    • Tension
    • Vertigo
    • Nervousness
    • Precordial Pain
  • Gastrointestinal:
    • Anorexia
    • Nausea
    • Vomiting
  • Neuromuscular & Skeletal:
    • Tremor
    • Vesicle Sphincter Spasm
    • Weakness
  • Genitourinary:
    • Dysuria
    • Oliguria
    • Urinary Retention (Males With Prostatism)
  • Respiratory:
    • Dyspnea
  • Miscellaneous:
    • Tachyphylaxis

Contraindications to Ephedrine (Akovaz):

  • If someone is allergic to ephedrine, other similar drugs, or any part of the medicine, they shouldn't use it.
  • Also, if they have a type of glaucoma called angle-closure glaucoma, or if they're taking certain types of anesthesia like cyclopropane or halothane that make the heart more sensitive, they shouldn't take ephedrine either.

Warnings and precautions

Cardiovascular effects

  • Ephedrine can have serious effects on the heart and blood vessels.
  • It might raise blood pressure high enough to cause bleeding in the brain.
  • It could also trigger chest pain in people with heart problems like coronary artery disease, and in some cases, it might even cause dangerous heart rhythms, especially in people with heart disease or who are taking certain medications that make the heart more sensitive.

Urine output

  • Ephedrine can cause the blood vessels in the kidneys to narrow, which might reduce the amount of urine produced.

Cardiovascular disease

  • If someone has cardiovascular disease like high blood pressure, angina (chest pain), coronary artery disease, or heart rhythm problems, doctors need to be careful about giving them ephedrine.
  • In these cases, using ephedrine might not be a good idea because it can make the heart work harder, potentially worsening the condition.
  • However, if it's necessary, it should be used cautiously, with close monitoring.

Diabetes:

  • For individuals with diabetes, caution should be exercised when considering the use of ephedrine, as it may not be suitable in cases where medications that raise blood pressure are not recommended.
  • Using ephedrine in individuals with diabetes should be approached with care and close monitoring, as it may affect blood sugar levels and worsen the condition if not managed properly.

Prostatic hyperplasia/urinary restriction:

  • If someone has an enlarged prostate (prostatic hyperplasia) or a urinary stricture, they should be cautious when using ephedrine.
  • These conditions can affect urination, and ephedrine might make it harder to pass urine.
  • So, it's important for such individuals to use ephedrine carefully and under medical supervision.

Renal impairment

  • If someone has kidney problems (renal impairment), using ephedrine should be done cautiously.
  • Their body might take longer to get rid of ephedrine, which could affect how it works and increase the risk of side effects.
  • So, it's essential to keep a close eye on these individuals for any negative reactions while using ephedrine.

Thyroid dysfunction:

  • For individuals with thyroid dysfunction, such as thyrotoxicosis (overactive thyroid), caution is advised when considering the use of ephedrine.
  • It's generally not recommended to use ephedrine in situations where medications that raise blood pressure are not suitable.
  • However, if it's deemed necessary, it should be used cautiously in individuals with thyroid dysfunction, with close monitoring for any adverse effects.

Vasomotor symptoms:

  • If someone has unstable vasomotor symptoms (like hot flashes or sudden changes in blood pressure), they should be cautious when using ephedrine.
  • These symptoms might be worsened by ephedrine, so it's important to use it carefully and under medical supervision in such individuals.

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

by indirectly acting raise the serum level of Alpha/Beta-Agonists.

Cardiac Glycosides

Cardiac Glycosides' arrhythmogenic effects may be enhanced by EPHEDrine (Systemic).

Chloroprocaine

Alpha-/Beta-Agonists' hypertensive effects could be amplified.

CloNIDine

EPHEDrine Systemic's therapeutic benefits could be enhanced.

CloZAPine

may reduce the alpha/beta agonists' therapeutic efficacy.

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 intensify EPHEDrine Systemic's hypertensive effects.

Propofol

EPHEDrine Systemic's therapeutic benefits could be enhanced.

QuiNIDine

EPHEDrine Systemic's therapeutic impact might be diminished.QuiNIDine's therapeutic benefit may be inferior to that of EPHEDrine Systemic.

Rocuronium

EPHEDrine (Systemic) may enhance Rocuronium's therapeutic benefits.

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

Alpha-/Beta-Agonists' ability to constrict blood vessels may be increased. Avoid using hyaluronidase to improve alpha- or beta-agonist dispersion or absorption. Patients who are getting alpha/beta-agonists for other reasons may benefit clinically from the usage of hyaluronidase.

Linezolid

Sympathomimetics may increase hypertensive effects. Patients receiving linezolid should be reduced in initial doses and closely monitored for 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

Alpha/Beta Agonists' hypertensive effects could be amplified (Indirect Acting).Although this is the expected mechanism of action for linezolid, the treatment recommendations are different from those for other monoamine-oxidase inhibitors.Consult the detailed monographs for linezolid for further details.Exceptions: Tedizolid; linezolid.

Monitoring parameters:

Blood Pressure:

  • Keep an eye on blood pressure levels regularly.

Pulse Rate:

  • Monitor pulse rate to ensure it stays within normal limits.

Respiratory Symptoms:

  • Watch out for any breathing difficulties or changes in breathing patterns.

Adverse Reactions:

  • Pay close attention to any adverse reactions or side effects, especially in individuals with kidney problems.

How to administer Ephedrine (Akovaz)?

For Intravenous Use:

  • Dilution: Prepare a diluted solution of ephedrine.
  • Method: Administer the diluted solution slowly through a vein (IV push).

For Prevention of Postoperative Nausea and Vomiting (Off-label Use):

  • Method: Administer intramuscularly (IM).
  • References: Based on studies by Hagemann in 2000 and SAMBA by Gan in 2007.

Mechanism of action of Ephedrine (Akovaz):

  • Ephedrine works by releasing norepinephrine stored in tissues, which then stimulates both alpha- and beta-adrenergic receptors.
  • It's not as strong as epinephrine and stays active in the body for a longer time.

Onset and Duration

  • IM Onset: Starts working within 10 to 20 minutes after injection into the muscle.
  • Duration of Pressor/Cardiac Effects (Subcutaneous): Lasts about 1 hour.

Absorption and Metabolism

  • IV Absorption: Quickly and completely absorbed into the bloodstream.
  • Metabolism: Ephedrine is minimally metabolized by the liver. Metabolites include p-hydroxyephedrine, p-hydroxynorephedrine, and norephedrine.

Elimination and Excretion

  • Half-life: The time it takes for half of the drug to leave the body varies depending on urinary pH. For example, with a urine pH of 5, it's around 3 hours, and with a urine pH of 6.3, it's about 6 hours.
  • Excretion: Primarily excreted through urine, mostly unchanged. The rate of excretion depends on urinary pH, with the highest excretion in acidic urine.

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

Ephedrine is a medication and stimulant compound derived from plants in the Ephedra genus. It has been used for various medical purposes, including as a decongestant, bronchodilator (to treat asthma), and to aid weight loss. It is a sympathomimetic amine, meaning it mimics the effects of the sympathetic nervous system, which controls functions such as heart rate, blood pressure, and metabolism.

Due to its stimulant properties, ephedrine has also been used as a performance-enhancing drug and as an ingredient in some dietary supplements marketed for weight loss and athletic performance. However, its use in these contexts has been controversial due to concerns about its safety and potential for abuse.

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 recommended for the management of hypotension brought on by anesthesia.

Note:

  • Ephedrine is no longer utilized to treat a variety of ailments, such as acute bronchospasm, Stokes-Adams syndrome (such as presyncope/syncope) with full heart block, narcolepsy, depression, or myasthenia gravis.
  • For some disorders, there are more potent treatments available.
  • 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: 

  • The dose is usually between 5 to 25 milligrams at a time, given slowly.
  • If needed, they can give it again to keep the blood pressure stable.
  • But they shouldn't give more than a total of 50 milligrams.

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

  • After surgery, if someone might feel nauseous or vomit, doctors might use ephedrine in a way that's not officially approved (called off-label).
  • They might inject it into a muscle at a dose of 0.5 milligrams per kilogram of the person's weight at the end of the surgery.

Ephedrine Dose in Children:

Dose in the treatment of anesthesia-induced hypotension:

Use the lowest effective dosage possible:

  • When children and adolescents under 15 years old have low blood pressure because of anesthesia, doctors might give them ephedrine through a vein.
  • The dose depends on their weight and ranges from 0.1 to 0.3 milligrams per kilogram of body weight for each dose, given slowly.
  • They can repeat this dose if needed to keep the blood pressure stable, but they shouldn't give more than 25 milligrams in one dose or a total of 50 milligrams overall.
  • For adolescents over 15 years old, the dose is similar to adults: between 5 to 25 milligrams per dose, repeated as necessary, but not exceeding a total of 50 milligrams.

Pregnancy Risk Factor C

  • Ephedrine is considered a Pregnancy Risk Factor C, meaning there haven't been specific studies on its effects during pregnancy in animals or humans.
  • However, it does cross the placenta, potentially affecting the unborn baby.
  • Doctors sometimes use ephedrine during cesarean sections to prevent or treat low blood pressure in the mother due to spinal anesthesia.
  • However, there are risks, including postpartum high blood pressure and the possibility of stroke if ephedrine is given with oxytocic medications.
  • Newborns might also experience metabolic acidosis if their mothers were given ephedrine, so careful monitoring is necessary in such cases.

Use during breastfeeding:

  • Ephedrine is known to be excreted in breast milk.
  • The decision to breastfeed while undergoing therapy with ephedrine should be carefully considered, weighing the potential risk of exposing the infant to the medication against the benefits of treatment for the mother.
  • It's essential for mothers and their healthcare providers to have an open discussion about this matter to make an informed decision that prioritizes the well-being of both the mother and the baby.

Dose in Kidney disease:

  • The manufacturer's labeling does not specify any dosage adjustments for ephedrine in individuals with renal impairment.
  • However, caution should be exercised when using ephedrine in such cases.

Dose in Liver disease:

  • The manufacturer's labeling for ephedrine does not include specific dosage adjustments for individuals with hepatic impairment.

Side effects of Ephedrine (Akovaz):

  • Cardiovascular:
    • Ventricular Ectopy
    • Visceral Vasoconstriction (Renal)
    • Angina Pectoris
    • Hypertension
    • Palpitations
    • Bradycardia
    • Cardiac Arrhythmia
    • Pulse Irregularity
    • Tachycardia
  • Dermatologic:
    • Diaphoresis
    • Pallor
  • Central Nervous System:
    • Dizziness
    • Hallucination
    • Headache
    • Insomnia
    • Anxiety
    • Confusion
    • Delirium
    • Intracranial Hemorrhage
    • Restlessness
    • Tension
    • Vertigo
    • Nervousness
    • Precordial Pain
  • Gastrointestinal:
    • Anorexia
    • Nausea
    • Vomiting
  • Neuromuscular & Skeletal:
    • Tremor
    • Vesicle Sphincter Spasm
    • Weakness
  • Genitourinary:
    • Dysuria
    • Oliguria
    • Urinary Retention (Males With Prostatism)
  • Respiratory:
    • Dyspnea
  • Miscellaneous:
    • Tachyphylaxis

Contraindications to Ephedrine (Akovaz):

  • If someone is allergic to ephedrine, other similar drugs, or any part of the medicine, they shouldn't use it.
  • Also, if they have a type of glaucoma called angle-closure glaucoma, or if they're taking certain types of anesthesia like cyclopropane or halothane that make the heart more sensitive, they shouldn't take ephedrine either.

Warnings and precautions

Cardiovascular effects

  • Ephedrine can have serious effects on the heart and blood vessels.
  • It might raise blood pressure high enough to cause bleeding in the brain.
  • It could also trigger chest pain in people with heart problems like coronary artery disease, and in some cases, it might even cause dangerous heart rhythms, especially in people with heart disease or who are taking certain medications that make the heart more sensitive.

Urine output

  • Ephedrine can cause the blood vessels in the kidneys to narrow, which might reduce the amount of urine produced.

Cardiovascular disease

  • If someone has cardiovascular disease like high blood pressure, angina (chest pain), coronary artery disease, or heart rhythm problems, doctors need to be careful about giving them ephedrine.
  • In these cases, using ephedrine might not be a good idea because it can make the heart work harder, potentially worsening the condition.
  • However, if it's necessary, it should be used cautiously, with close monitoring.

Diabetes:

  • For individuals with diabetes, caution should be exercised when considering the use of ephedrine, as it may not be suitable in cases where medications that raise blood pressure are not recommended.
  • Using ephedrine in individuals with diabetes should be approached with care and close monitoring, as it may affect blood sugar levels and worsen the condition if not managed properly.

Prostatic hyperplasia/urinary restriction:

  • If someone has an enlarged prostate (prostatic hyperplasia) or a urinary stricture, they should be cautious when using ephedrine.
  • These conditions can affect urination, and ephedrine might make it harder to pass urine.
  • So, it's important for such individuals to use ephedrine carefully and under medical supervision.

Renal impairment

  • If someone has kidney problems (renal impairment), using ephedrine should be done cautiously.
  • Their body might take longer to get rid of ephedrine, which could affect how it works and increase the risk of side effects.
  • So, it's essential to keep a close eye on these individuals for any negative reactions while using ephedrine.

Thyroid dysfunction:

  • For individuals with thyroid dysfunction, such as thyrotoxicosis (overactive thyroid), caution is advised when considering the use of ephedrine.
  • It's generally not recommended to use ephedrine in situations where medications that raise blood pressure are not suitable.
  • However, if it's deemed necessary, it should be used cautiously in individuals with thyroid dysfunction, with close monitoring for any adverse effects.

Vasomotor symptoms:

  • If someone has unstable vasomotor symptoms (like hot flashes or sudden changes in blood pressure), they should be cautious when using ephedrine.
  • These symptoms might be worsened by ephedrine, so it's important to use it carefully and under medical supervision in such individuals.

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

by indirectly acting raise the serum level of Alpha/Beta-Agonists.

Cardiac Glycosides

Cardiac Glycosides' arrhythmogenic effects may be enhanced by EPHEDrine (Systemic).

Chloroprocaine

Alpha-/Beta-Agonists' hypertensive effects could be amplified.

CloNIDine

EPHEDrine Systemic's therapeutic benefits could be enhanced.

CloZAPine

may reduce the alpha/beta agonists' therapeutic efficacy.

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 intensify EPHEDrine Systemic's hypertensive effects.

Propofol

EPHEDrine Systemic's therapeutic benefits could be enhanced.

QuiNIDine

EPHEDrine Systemic's therapeutic impact might be diminished.QuiNIDine's therapeutic benefit may be inferior to that of EPHEDrine Systemic.

Rocuronium

EPHEDrine (Systemic) may enhance Rocuronium's therapeutic benefits.

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

Alpha-/Beta-Agonists' ability to constrict blood vessels may be increased. Avoid using hyaluronidase to improve alpha- or beta-agonist dispersion or absorption. Patients who are getting alpha/beta-agonists for other reasons may benefit clinically from the usage of hyaluronidase.

Linezolid

Sympathomimetics may increase hypertensive effects. Patients receiving linezolid should be reduced in initial doses and closely monitored for 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

Alpha/Beta Agonists' hypertensive effects could be amplified (Indirect Acting).Although this is the expected mechanism of action for linezolid, the treatment recommendations are different from those for other monoamine-oxidase inhibitors.Consult the detailed monographs for linezolid for further details.Exceptions: Tedizolid; linezolid.

Monitoring parameters:

Blood Pressure:

  • Keep an eye on blood pressure levels regularly.

Pulse Rate:

  • Monitor pulse rate to ensure it stays within normal limits.

Respiratory Symptoms:

  • Watch out for any breathing difficulties or changes in breathing patterns.

Adverse Reactions:

  • Pay close attention to any adverse reactions or side effects, especially in individuals with kidney problems.

How to administer Ephedrine (Akovaz)?

For Intravenous Use:

  • Dilution: Prepare a diluted solution of ephedrine.
  • Method: Administer the diluted solution slowly through a vein (IV push).

For Prevention of Postoperative Nausea and Vomiting (Off-label Use):

  • Method: Administer intramuscularly (IM).
  • References: Based on studies by Hagemann in 2000 and SAMBA by Gan in 2007.

Mechanism of action of Ephedrine (Akovaz):

  • Ephedrine works by releasing norepinephrine stored in tissues, which then stimulates both alpha- and beta-adrenergic receptors.
  • It's not as strong as epinephrine and stays active in the body for a longer time.

Onset and Duration

  • IM Onset: Starts working within 10 to 20 minutes after injection into the muscle.
  • Duration of Pressor/Cardiac Effects (Subcutaneous): Lasts about 1 hour.

Absorption and Metabolism

  • IV Absorption: Quickly and completely absorbed into the bloodstream.
  • Metabolism: Ephedrine is minimally metabolized by the liver. Metabolites include p-hydroxyephedrine, p-hydroxynorephedrine, and norephedrine.

Elimination and Excretion

  • Half-life: The time it takes for half of the drug to leave the body varies depending on urinary pH. For example, with a urine pH of 5, it's around 3 hours, and with a urine pH of 6.3, it's about 6 hours.
  • Excretion: Primarily excreted through urine, mostly unchanged. The rate of excretion depends on urinary pH, with the highest excretion in acidic urine.

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