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Ephedrine

Ephedrine has mixed actions

Source

Natural ephedra plant. It can also be synthesized synthetically.

Mechanism of Action

Stimulates both alpha and beta receptors, but less stronger than adrenaline.

It acts in a mixed manner, stimulating either directly or indirectly by stimulating release of noradrenaline.

It also shows tachyphylaxis.

Pharmacokinetics

Non catecholamine given orally. It is non polar and crosses blood brain barrier. It is excreted unchanged in the urine.

Pharmacological Actions

CVS
  1. Increases heart contraction
  2. Increases heart rate (less than adrenaline)
  3. Increases systolic as well as diastolic blood pressure
  4. Increases cardiac output
Respiratory System
  1. Causes bronchodilatation due to beta 2 effect.
  2. Causes decongestion because of vasoconstriction of respiratory mucosa (alpha 1 effect)
CNS

As it is a non catecholamine, it crosses the blood brain barrier and stimulates CNS directly. It produces alertness, euphoria, insomnia, this action is milder than amphetamines.

Therapeutic Uses

Ephedrine has fallen out of favour these days. It was used in

  1. Bronchial asthma
  2. Nasal decongestion (pseudo ephedrine used even now)
  3. Can be used even now for Spinal Anesthesia. When lignocaine etc. are injected in between the L2 and L3 segment in the spinal canal for producing paralysis below the umbilicus, sometimes the local anesthetic spreads leading to progressive paralyzation of sympathetic trunk. As a result severe hypotension might develop. This can be countered by ephedrine, which has a longer duration of action

Side Effects

CNS

Insomnia, restlessness, irritability, anxiety

CVS

Tachycardia, palpitations, hypertension, precipitation of angina pectoris

Urinary Bladder

Because of alpha effect, contractions of smooth muscles of prostate and trigone might occur in older males, resulting in urinary retention.

Continue Reading

Sympathomimetics -Introduction

Adrenaline

Noradrenaline

Isoprenaline

Dopamine

Dobutamine

Amphetamines

Phenyl Ephrine

Salbutamol/Terbutaline

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