Ephedrine

General characteristics. Structure:

Active ingredient: 50 mg of ephedrine of a hydrochloride in 1 ml of solution.

Excipients: water for injections.

Pharmacological properties:

Pharmacodynamics. The sympathomimetic, stimulates alpha and beta adrenoceptors. Affecting varicose thickenings of efferent adrenergic fibers, promotes allocation of Norepinephrinum in a synaptic gap. Besides, exerts the weak stimulating impact directly on adrenoceptors. Causes vasopressor, bronkhodilatiruyushchy and psychogogic action. Increases the general peripheric vascular resistance and system arterial pressure, increases the minute volume of blood, number of cordial reductions and force of cordial reductions, improves atrioventricular conductivity; raises a tone of skeletal muscles, concentration of glucose in blood; brakes an intestines peristaltics, expands a pupil (without influencing accommodation and intraocular pressure). Stimulates the central nervous system, on psychogogic action it is close to Phenaminum. Brakes activity of monoamine oxidase and катехоламино.................... Exerts the stimulating impact on alpha adrenoceptors of blood vessels in skin, causing narrowing of expanded vessels, reducing, thus their hyperpermeability leading to reduction of hypostasis at a small tortoiseshell.

The beginning of therapeutic effect at intramuscular introduction of 25-50 mg - in 10-20 min., action duration - 0,5-1 h. At repeated introduction with a small interval (10-30 min.) pressor effect of ephedrine quickly decreases (there is a tachyphylaxis connected with the progressing reduction of stocks of Norepinephrinum in varicose thickenings).

Pharmacokinetics. Absorption after intramuscular or hypodermic introduction - bystry.

In small amounts it is metabolized in a liver. An elimination half-life at urine pH 5 - 3 h, at pH 6,3 urine - 6 h.

It is removed by kidneys, it is preferential in not changed look. The amount of the removed drug depends on pH of urine and increases at shift of pH of urine in the acid party.

Indications to use:

Arterial hypotension (collapse, shock, operative measures, spinal anesthesia, injury, blood loss, bacteremia, overdose ganglioblokiruyushchy, adrenoblockers and other hypotensive medicines); the uncontrollable sympathetic block at various options of the central segmented blockade.

Route of administration and doses:

Subcutaneously, intravenously and intramusculary. The way of introduction depends on indications. At an acute lowering of arterial pressure slow intravenous administration is shown; at infectious diseases, before spinal anesthesia - hypodermic or intramuscular introduction.

Intravenously ephedrine is applied struyno or kapelno. At a single-step injection enter slowly struyno 0,02-0,05 (0,4-1 ml of solution with concentration of 50 mg/ml).

At drop introduction ephedrine is applied in isotonic solution of sodium chloride in the general dose of 0,06-0,08; amount of isotonic solution from 100 to 800 ml.

At hypodermic introduction apply 0,02-0,05 (0,4-1 ml) solution with concentration of 50 mg/ml 1-2 times a day.

For the prevention of a lowering of arterial pressure at spinal anesthesia enter under skin 1 ml of solution with concentration of 50 mg/ml in 10-30 min. prior to the beginning of anesthesia.

The highest doses of ephedrine for adults at hypodermic introduction: one-time - 0,05 g, daily - 0,1 g.

Features of use:

At infusion it is necessary to use the device with measuring adaptation for the purpose of regulation of speed of infusion. Infusions should be carried out in large (better in central) a vein. During treatment measurement of arterial pressure, volume of urine, minute volume of blood, the electrocardiogram, the central venous pressure, pulmonary pressure and pressure of jamming in pulmonary capillaries is recommended.

In order to avoid development of disturbances of a night dream it is not necessary to appoint ephedrine and medicines supporting him at the end of the day and before going to bed.

It is recommended to be careful in order to avoid hit of drug in okolososudisty fabrics that can cause their necrosis (in case of formation of extravasate, it is necessary to make immediately infiltration of 10-15 ml of 0,9% of NaCl containing 5-10 ml of phentolamine). Overdoses at a myocardial infarction can strengthen ischemia by increase in need of a myocardium for oxygen.

Prior to treatment whenever possible there has to be a skorrigirovana a hypovolemia. Treatment by ephedrine does not replace hemotransfusion, plasmas, blood-substituting liquids and/or saline solutions.

Ephedrine is inexpedient to be applied is long (the narrowing of peripheral vessels leading to possible development of a necrosis or gangrene).

At appointment for correction of arterial hypotension or addition in solution of mestnoanesteziruyushchy drug during childbirth/delivery, and also joint appointment with some medicines stimulating patrimonial activity (for example, vasopressin, ergotamine, эргоновин, метилэргоновин), can cause persistent arterial hypertension (up to a rupture of vessels of a brain); during spinal anesthesia, it can increase heart rate at a fruit.

If arterial pressure at mother exceeds 130/80 mm Hg, ephedrine is not recommended to be used.

In connection with the stimulating influence on the central nervous system can be a subject of abuse of addicts.

At the termination of treatment of a dose it is necessary to reduce gradually as sudden cancellation of therapy can lead to heavy hypotension. If solution opaque, it cannot be entered. An unused part should be destroyed.

Monoamine oxidase inhibitors, increasing pressor effect of sympathomimetics, can cause developing of headaches, arrhythmias, vomitings, hypertensive crisis therefore at inclusion by patients of monoamine oxidase inhibitors in the previous 2-3 weeks of a dose of sympathomimetics have to be reduced (to 1/10 parts from a usual dose).

Side effects:

From a nervous system and sense bodys: more often - a headache, a sleep disorder; less often - weakness, nervousness, motive concern, dizziness; frequency is unknown - spasms, muscular spasms, a tremor, numbness of hands or legs, drowsiness; at use in high doses - hallucinations, change of mood or mentality.

From cardiovascular system: less often - stenocardia, bradycardia or tachycardia, heartbeat, increase or a lowering of arterial pressure, at high doses - ventricular arrhythmias; seldom - a sensation of discomfort or thorax pain; frequency is unknown - unusual hemorrhages, a dermahemia of the person.

From the alimentary system: more often - nausea, vomiting; less often - dryness or irritation of an oral cavity or throat, appetite loss; frequency is unknown - heartburn.

From an urinary system: less often - complicated and an urodynia.

Local reactions: pain or burning in the place of an intramuscular injection.

Others: less often - the increased sweating, pallor of integuments; narrowing of peripheral vessels, allergic reactions, an asthma or the complicated breath, a fever, a hyperthermia, expansion of pupils, an illegibility of visual perception.

If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Weakens effects of narcotic analgetics and somnolent medicines.

The medicines alkalinizing urine (including the antacids containing Sa2 + and Mg2+, karboangidraza inhibitors, citrates, Natrii hydrocarbonas), increase an elimination half-life of ephedrine and risk of developing of intoxication.

At use along with cardiac glycosides, quinidine, tricyclic antidepressants, a dopamine, means for an inhalation anesthesia (chloroform, энфлуран, a halothane, изофлуран, метоксифлуран, trichloroethylene) the risk of development of heavy ventricular arrhythmias increases; with other sympathomimetic means - strengthening of expressiveness of side effects from cardiovascular system; with anti-hypertensive means (including with sympatholytics, diuretics, Rauwolfia alkaloids) - decrease in hypotensive effect.

Simultaneous use with adrenergic bronchodilatory means can lead to additional excess stimulation of the central nervous system that can cause a hyperexcitability, irritability, sleeplessness, spasms, arrhythmias.

Cocaine strengthens the stimulating influence on the central nervous system and cardiovascular system.

Co-administration with Reserpinum and monoamine oxidase inhibitors (including furasolidone, Procarbazinum, селегилин) can cause a headache, heart arrhythmias, vomiting, the sudden and expressed increase in arterial pressure, hyperpyrexial crisis; with non-selective beta adrenoblockers and nitrates - weakening of therapeutic action (blockade of beta adrenoceptors can lead to a prevalence of alpha and adrenergic activity with risk of development of arterial hypertension and sharply expressed bradycardia with possible development of a heart block; blockade of beta adrenoceptors also interferes with beta2-adrenergic bronchodilatory action); with phenoxybenzamine - strengthening of hypotensive effect and tachycardia; with Phenytoinum - a sudden lowering of arterial pressure and bradycardia (depends on a dose and rate of administering); with drugs of hormones of a thyroid gland - mutual strengthening of action.

Increases metabolic clearance of glucocorticosteroids, adrenocorticotropic hormones at prolonged use (correction of their doses can be required); neurologic effects of Diatrizoatums, yotalamovy and yoksaglovy acids. Ergometrine, ergotamine, methylergometrine, oxytocin increase vasopressor effect and risk of developing of ischemia and gangrene, and also heavy arterial hypertension, up to intracraneal hemorrhage. Doksapram, sympatholytics (guanadret, гуанетидин), Mazindolum, мекамиламин, Methyldopum, триметафан, methylphenidate strengthen pressor effect.

The levodopa increases risk of developing of arrhythmias (demands a sympathomimetic dose decline).

Strengthens the stimulating influence (mutually) on the central nervous system of Mazindolum, methylphenidate.

Ritodrinum strengthens (mutually) effects (including collateral).

Strengthens the stimulating influence on the central nervous system and risk of emergence of the toxic phenomena of xanthines (including Aminophyllinum, caffeine, Diphyllinum, an okstrifillin, theophylline).

Contraindications:

Hypersensitivity, sleeplessness, hypertrophic subaortic stenosis, pheochromocytoma, fibrillation of ventricles, uncontrollable arterial hypertension and tachycardia.

If at you one of the listed diseases, before administration of drug surely consult with the doctor.

With care. A metabolic acidosis, a hypercapnia, a hypoxia, a ciliary arrhythmia, closed-angle glaucoma, pulmonary hypertensia, a hypovolemia, a myocardial infarction, occlusal diseases of vessels (including in the anamnesis): arterial embolism, atherosclerosis, Thrombangiitis obliterans, freezing injury, diabetic endarteritis, Raynaud's disease; diseases of cardiovascular system (including stenocardia, a tachyarrhythmia, ventricular arrhythmia, coronary insufficiency, arterial hypertension), a diabetes mellitus, a thyrotoxicosis, a benign hyperplasia of a prostate, simultaneous use of means for an inhalation anesthesia.

If at you one of the listed diseases, before administration of drug surely consult with the doctor.

Overdose:

Symptoms: the expressed weakness, excitement, sleeplessness, an ischuria, excessive increase in arterial pressure, a loss of appetite, vomiting, the increased sweating, rash.

Treatment: at overshot hypertensive effect to reduce rate of administering or temporary to stop introduction if it is inefficient - alpha adrenoblockers of short action.

Storage conditions:

In the place protected from light at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 5 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections. Packaging: 50 mg/ml in ampoules on 1 ml. 5 ampoules in a blister strip packaging. 1 or 2 blister strip packagings with the application instruction in a pack from a cardboard. 20, 50 or 100 blister strip packagings with 20, 50 or 100 application instructions in a box from a cardboard or in a box from corrugated fibreboard (for a hospital).