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Ephedrine

Ephedrine is a medication and stimulant.

 

 

Ephedrine works by increasing the activity of the α and β adrenergic receptors.

 

 

Ephedrine is a sympathomimetic amine and substituted amphetamine, and a structural methamphetamine analogue. 

 

 

Ephedrine was obtained from the plant Ephedra. but most drug produced today is made synthetically.

 

 

It is used to prevent low blood pressure during spinal anesthesia.

 

 

Used for asthma, narcolepsy, and obesity but is not the preferred treatment.

 

 

It has questionable benefit in nasal congestion.

 

 

It can be taken by mouth or by injection into a muscle, vein, or subcutaneous.

 

 

Onset of action: intravenous seconds, intramuscular 20 minutes, orally up to 1 hour.

 

 

When taken by mouth it can last up to four hours.

 

 

Trade names: Akovaz, Corphedra, Emerphed

 

 

Pregnancy category AU: A

 

 

Bioavailability 85%

 

 

Metabolism minimally by  liver

 

 

Elimination half-life 3 h to 6 h

 

 

Duration of action

 

IV/IM (60 min), by mouth (2 h to 4 h)

 

 

Excretion 22% to 99% via urine

 

 

Common side effects:  trouble sleeping, anxiety, headache, hallucinations, hypertension, tachycardia, loss of appetite, and inability to urinate.

 

 

Serious side effects:  stroke and heart attack.

 

 

Likely  safe in pregnancy.

 

 

Ephedrine and pseudoephedrine increase blood pressure and act as bronchodilators.

 

 

It may decrease motion sickness, but is mainly used to decrease the sedating effects of other medications used for motion sickness.

 

 

Ephedrine a long-lasting responsiveness in congenital myasthenic syndrome in early childhood.

 

 

Ephedrine promotes modest short-term weight loss, specifically fat loss.

 

 

Ephedrine decreases gastric emptying. 

 

 

Methylxanthines such as caffeine and theophylline have a synergistic effect with ephedrine with respect to weight loss. 

 

 

Ephedrine has a similar chemical structure to amphetamine and is a methamphetamine analogue.

 

 

It can be used to create methamphetamine using chemical reduction: making ephedrine a highly sought-after chemical precursor in the illicit manufacture of methamphetamine.

 

 

Ephedrine may be quantified in blood, and urine to monitor possible abuse, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation. 

 

 

Blood ephedrine concentrations are typically in the 20-200 µg/l range in persons taking the drug therapeutically, 300-3000 µg/l in abusers or poisoned patients and 3–20 mg/l in cases of acute fatal overdosage. 

 

 

The World Anti-Doping Agency (WADA) limit for ephedrine in an athlete’s urine is 10 µg/ml.

 

 

In conjunction with certain antidepressants, namely norepinephrine-dopamine reuptake inhibitors (NDRIs), ephedrine levels are increased and are associated with risk of symptoms due to excessive serum levels of norepinephrine.

 

 

Bupropion should not be used with ephedrine, as it may increase the likelihood of side effects.

 

 

Ephedrine use should be with caution in patients with: inadequate fluid replacement, impaired adrenal function, hypoxia, hypercapnia, acidosis, hypertension, hyperthyroidism, prostatic hypertrophy, diabetes mellitus, cardiovascular disease, during delivery if maternal blood pressure is >130/80 mmHg, and during lactation.

 

 

Ephedrine contraindications include: 

 

 

closed-angle glaucoma, 

 

 

pheochromocytoma, 

 

 

idiopathic hypertrophic subaortic stenosis

 

 

concomitant or recent monoamine oxidase inhibitor (MAOI) therapy, 

 

 

general anaesthesia with halogenated hydrocarbons, particularly halothane.

 

 

Tachyarrhythmias or ventricular fibrillation,

 

 

Pregnancy

 

 

Ephedrine is a potentially dangerous natural compound.

 

 

Adverse drug reactions are more common with systemic administration.

 

compared to topical administration, such as nasal instillation.

 

 

Adverse drug reactions : 

 

 

Cardiovascular: tachycardia, cardiac arrhythmias, angina pectoris, vasoconstriction with hypertension

 

 

Dermatological: flushing, sweating, acne 

 

 

Gastrointestinal: nausea

 

 

Genitourinary: decreased urination due to vasoconstriction of renal arteries.

 

 

Constriction the internal urethral sphincter, mimicking the effects of sympathetic nervous system stimulation.

 

 

Nervous system: restlessness, confusion, insomnia, mild euphoria, mania/hallucinations, delusions, paranoia, hostility, panic, agitation

 

 

Respiratory: dyspnea, pulmonary edema

 

 

Dizziness, headache, tremor, hyperglycemic reactions, dry mouth

 

 

Its molecular structure is similar to phenylpropanolamine, methamphetamine, and epinephrine.

 

 

Ephedrine works by increasing the activity of norepinephrine (noradrenaline) on adrenergic receptors.

 

 

It is a substituted amphetamine and a structural methamphetamine analogue. 

 

 

Ephedrine, a sympathomimetic amine, that acts on part of the sympathetic nervous system (SNS). 

 

 

It indirectly  stimulates the adrenergic receptor system by increasing the activity of norepinephrine at the postsynaptic α and β receptors.

 

 

L-ephedrine, and its stereoisomer norpseudoephedrine has indirect sympathomimetic effects and due to its ability to cross the blood-brain barrier is a CNS stimulant similar to amphetamines, but less pronounced, as it releases noradrenaline and dopamine in the substantia nigra.

 

 

 

 

 

 

 

 

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