Pharmacodynamics and pharmacokinetics
The main ingredient – ephedrine hydrochloride. What is it and how does it work? The active ingredient stimulates the beta adrenergic receptors and alpha. Under the action of the drug is released norepinephrine in the synaptic cleft lumen. The drug acts on a varicose thickening adrenergic, efferent fibers. Ephedrine is able to provide a weakly expressed stimulating effect on the adrenergic receptors.
The drug causes a psychostimulant, bronchodilatory and vasoconstrictor effects on the body. The drug improves atrioventricular conduction, increases the heart rate, the IOC, the force of heart contractions, increases the level of systemic blood pressure and peripheral vascular resistance, inhibits intestinal peristalsis, increases the level of sugar in the blood, increases the tone of the skeletal muscles.
Active substance dilates the pupil, without affecting the intraocular pressure and accommodation of . According to the effects of psychostimulant medication close to fenaminu. The drug is able to inhibit the activity of catecholamine-0-methyl transferase, monoamine oxidase. The medicament stimulates alpha-adrenergic receptors in the blood vessels of the skin, narrowing the dilated blood vessels, which leads to lower their increased permeability. This mechanism explains the decrease in the severity of edema in hives.
When taken into ephedrine therapeutic effect develops over 15-60 minutes and lasts for about 5 hours. In intramuscular effect is registered in 10-20 minutes and lasts about an hour.
The pressor effects of the drug with repeated administration of 10-30 minutes decreasing rapidly, develop tachyphylaxis caused by a decrease in norepinephrine reserves varicose bulges.
Ephedrine is prescribed for hay fever, catarrhal rhinitis, sinusitis, vasomotor rhinitis, with arterial hypotension (spinal anesthesia, surgery, shock, collapse, an overdose of antihypertensive medications, blockers, drugs ganglioblokiruyuschimi, bacteremia, blood loss, trauma).
The drug is prescribed for depression, narcolepsy, asthma, sleeping pills poisoning, serum sickness, urticaria, bleeding from the pulp of the tooth and gums, for poisoning drugs, diagnostic purposes in ophthalmic practice (mydriasis).
Ephedrine is not indicated for insomnia, intolerance of the main component, pheochromocytoma, GOKMP, tachycardia, uncontrolled hypertension during at fibriddyatsii ventricles.
When hypoxia, hypercapnia, metabolic acidosis, hypovolemia, pulmonary hypertension, closed-form of glaucoma, atrial fibrillation, Buerger’s disease, atherosclerosis, arterial embolism, occlusive vascular lesions in the patient’s history, with myocardial infarction, Raynaud’s disease, diabetic endarteritis, frostbite, thyrotoxicosis, diabetes diabetes, benign prostatic hyperplasia, ventricular arrhythmia, tachyarrhythmia, angina pectoris, hypertension, coronary heart disease and other diseases of the cardiovascular system Ephedrine is prescribed with caution.
Nervous system: restlessness, nervousness, fatigue, sleep disturbances, headache, tremor, limb, muscle spasms, convulsions, dizziness, mental changes and mood, hallucinations, increased drowsiness, numbness of hands and feet .
Cardiovascular system: discomfort and chest pain, ventricular arrhythmia, drop in blood pressure, palpitations, tachycardia or bradycardia, angina, flushing of the skin, unusual bleeding.
Digestive tract: heartburn, appetite disorders, irritation, and dryness of the throat and mouth, vomiting, nausea.
Urinary: painful and difficult urination.
The injection site may burning pain. It is also noted peripheral vasoconstriction, pale skin, sweating,SHORTNESS of breath, blurred vision, allergic reactions, dilated pupils, pyrexia, chills, shortness of breath.
Instructions for use Ephedrine (Method and Dosage)
The drug is taken orally, intravenously, subcutaneously, intramuscularly.
In allergic diseases, bronchial asthma drug for 10-15 days is taken orally 2-3 times a day by 25-50 mg, or a cycle of three days, a three-day intervals.
As CNS stimulatory and bronchodilatory drug prescribed to children means subcutaneously, intravenously at 3 mg / kg (doses 4-6).
Before spinal anesthesia when bacteremia is administered subcutaneously and intramuscularly at 20-50 mg 2-3 times a day.
Higher dosages for subcutaneous administration, oral administration: daily – 150 mg, single – 50 mg.
If hypotension Ephedrine administered slowly intravenously, subcutaneously 20-50 mg saline. Re-introduction is carried out under the control of blood pressure.
When used vasomotor rhinitis 2-3% solution, in ophthalmic practice designate 1.5% solution.
As children vasoconstrictor is administered intravenously or subcutaneously to 750 mg / kg of a patient under the control of the reaction.
Manifested rashes on the skin, excessive sweating, vomiting, decreased appetite, excessive increase in the level of blood pressure, urinary retention, insomnia, agitation, severe weakness.
It recommended the introduction of alpha-blockers short-acting.
Ephedrine is able to attenuate the effect of sleeping pills, narcotic analgesics. Medicines, which was made alkaline urine (citrate, antacids, sodium bicarbonate, carbonic anhydrase inhibitors) increase the half-life of ephedrine, increasing the risk ofINTOXICATION
Co-administration with quinidine, cardiac glycosides, dopamine, tricyclic antidepressants, drugs for inhalation anesthesia (methoxyflurane, isoflurane, halothane, enflurane, chloroform, trichlorethylene ) increases the likelihood of severe ventricular arrhythmias.
The combination with antihypertensive drugs, Rauwolfia alkaloids, diuretics, sympatholytic causes a decrease in the hypotensive effects. Increased severity of side effects of the cardiovascular system is registered, while the use of sympathomimetic drugs. With simultaneous use of adrenergic bronchodilator medication indicated additional, excessive stimulation of the central nervous system, which is manifested by insomnia, increased irritability, excitability, seizures, arrhythmias.
Monoamine oxidase inhibitors, reserpine, selegiline, procarbazine, furazolidone in combination with ephedrine causes a pronounced rise in blood pressure, arrhythmia, headaches, vomiting, hypertensive crises. Appointment of non-selective beta-blockers, nitrates, lead to a decrease in the effectiveness of ephedrine. Phenoxybenzamine enhances the severity of tachycardia, the hypotensive effect.
Ergotamine, ergometrine, oxytocin, metilergometrin increase the risk of gangrene, ischemia, increase the vasoconstrictor effect of hypertension may intracranial hemorrhage. Methylphenidate, trimetafan, mecamylamine, mazindol, methyldopa, doxapram, guanethidine, guanadrel increase the severity of the pressor effect. The use of levodopa can cause arrhythmia, reduce the dosage required sympathomimetic.
Ephedrine methylphenidate amplifies stimulus, mazindol on the central nervous system. Admission ritodrine is mutual reinforcement effects, including side.
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