Handbook covers dosage, side effects, interactions, uses. This alkaloid is identical with ephedrine and isomeric with pseudoephedrine. The elimination of ephedrine and its metabolites is enhanced by an acidic urinary ph. We examined the sympathomimetic effects of lephedrine, currently used as a. It is often used to prevent low blood pressure during. Pharmacological effects of ephedrine alkaloids on human. In addition to their direct pharmacological effects, many of these co.
Pdf pharmacological effects of ephedrine alkaloids on. Presentation by marc bouchard history also known as mahuang ephedra has been used as medicine for over 60,000 years used in chinese medicine for more than 5,000 years originally prescribed to treat asthma, congestion and allergies ephedra equisetina ephedrine is a naturally occurring central nervous system stimulant obtained from the plant ephedra equisetina. Ephedrine mechanism, indication, contraindications. The elimination halflife of ephedrine is reported to be about 3 hours and 6 hours at a urinary ph of 5 or 6. However, it appears that the following information is consistent across different publication regardless which analytical methods used. The success of ephedrine in the treatment of asthma and allied conditions has created a demand for the drug which encourages the search for a more easily available source or, failing this, a cheaper but effective substitute.
Ephedrine 3739 191193 epidural infusion 5 epinephrine 3337 415 epoetin alfa 160161 eprosartan 146147 eptifibatide 165169 erectile dysfunction therapy drugs 231232 ergoloid mesylates 4043. In several meetings with the applicant prior to submission of the nda, the division communicated multiple issues to the applicant. Of note, when discussing drug class, pharmacology, efficacy, safety, etcetera most references including published articles, drug databases and the reference product pi accessed by the evaluator discussed these issues in terms of the dose of ephedrine the free. Ephedrine is a synthetic noncatecholamine agonist at.
All of its effects are comparable to those of sympathetic stimulation. The purest form of ephedrine is used for therapeutic purpose, primarily as a bronchodilator and decongestant. Ephedra species of plants have both beneficial and adverse effects primarily associated with the presence of ephedrine alkaloids. If the pharmacy thats willing to deliver medicines to your home doesnt have ephedrine in stock, you can ask for one of the branded alternatives for ephedrine. Which of the following drugs used for the treatment of angina by inhalation has a very rapid onset and a brief duration of effect. Akovaz ephedrine sulfate dose, indications, adverse. Given its rather nonspecific activation of the sns, the pharmacological actions of ephedrine are rather predictable and include vasoconstriction, cardiac activation, and bronchodilation. When the constrictor action of tyramine and of ephedrine is examined on the hind limbs of the dog perfused with defibrinated blood by way of the abdominal aorta, the action is very feeble. Pdf katzung basic and clinical pharmacology 14th edition. This pharmacology i and pharmacology ii pdf notes will help all the b pharmacy and d pharmacy students very much to make a good score in their university and any other competitive exams.
The pharmacokinetics of ephedrine after oral dosage in. This greater response to the compound tablet did not achieve statistical significance but the probability of an additional effect from theophylline was supported by patient l. Following ingestion of an oral dose, clinical effects are seen within 60 min and persist from 2 to 6 h. Patients were assigned in a doubleblind randomized fashion to receive a standardized general anesthetic followed by an intramuscular dose of either ephedrine 0. None of the drugs given alone was associated with significant adverse effects but both ephedrine.
A blinded anesthesiologist asked the patient to evaluate the pain score verbal rating scale. Death follows gradual depression without convulsions. Ephedrine, alone or in combination, was relatively ineffectual in these patients. Ephedra is a medicinal preparation from the plant ephedra sinica. Inhaled epinephrine and oral theophyllineephedrine in the. Ephedrine is safe when used under the supervision of a doctor and with proper monitoring of the patient. Ephedrine hydrochloride has a melting point of 187. The effects of lowdose ephedrine on intubating conditions.
All the notes available on this website are free to download and easy use to understand. Research article preliminary phytochemical screening. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. In rats with a unilateral lesion in the substantia nigra made by stereotaxic injection of 6. Ephedrine is a sympathomimetic agent that has widespread use as an adrenergic stimulant. Each group consisted of 1643 healthy volunteer medical students. It has a role as an alphaadrenergic agonist, a cardiotonic drug, a mydriatic agent, a protective agent, a vasoconstrictor agent, a sympathomimetic agent and a nasal decongestant. If however, adrenaline is added to the circulating blood the constrictor action of tyramine and ephedrine is greatly increased. Ephedrine is a direct and indirect sympathomimetic amine. Clinical use of ephedrine has fallen out of favor given its wideranging effects and its use has been replaced by more specific adrenergic agonists. It is generally accepted that the primary pharmacological activities and adverse effects of ephedra herb are caused by ephedrine. Its pharmacological applications are related to its sympathomimetic properties, which in turn occur due to its stimulating action on.
Pdf pharmacological effects of ephedrine researchgate. May 15, 20 the purest form of ephedrine is used for therapeutic purpose, primarily as a bronchodilator and decongestant. Interaction of ephedrine and theophylline weinberger 1975. Ephedrine hydrochloride injection is indicated in the treatment of hypotension secondary to spinal anaesthesia. Katzung basic and clinical pharmacology 14th edition c2018 txtbk. Ephedrine drugs pharmacology free 30day trial scribd. It can be taken by mouth or by injection into a muscle, vein, or just under the skin. A193650 these actions combined lead to larger quantities of norepinephrine present in the synapse, for. Fev 1 responses were significantly greater p ephedrine compared with metaproterenol beginning at 2 hours. Ephedrine sulphate in comparatively large doses is toxic to animals.
There were no original nonclinical pharmacology or toxicology studies submitted in support of this nda application. Ephedrine hydrochloride myx injection name of the medicine. Mehendale, in encyclopedia of toxicology third edition, 2014 animal. Comparison of the acute physical and mental effects of. Ephedrine has been used clinically as a vasopressor for decades. Pharmacology pdf notes for pharmacy students download 2020. The effect of various environmental factors on cocaine and. The addition of pituitary posterior lobe extract to the blood in the.
The data showed that ephedrine alkaloids did not activate alpha1 and alpha2ars and that they antagonized the agonistmediated effects of phenylephrine and medetomidine on alpha1 and alpha. L ephedrine is a natural plant alkaloid isolated originally from the dried young. Dec 09, 2020 pdf ephedrine is a sympathomimetic agent that has widespread use as an adrenergic stimulant. Limited permission is granted free of charge to print or photocopy all pages of this publication. Aim the combination of ephedrine and caffeine has been used in herbal products for weight loss and athletic performance. Ephedrine was first described in western literature in 1888, as a naturally occurring component of the ephedra plant, along with pseudoephedrine. Ephedrine became a highly popular and effective treatment for asthma, particularly because, unlike adrenaline until then the. Ephedrine is metabolized in the liver by oxidative deamination, demethylation, aromatic hydroxylation, and conjugation. Ephedrine is a sympathomimetic which stimulates both alpha and beta adrenergic receptors, and also releases noradrenaline from its storage site. Ephedrine mechanism, indication, contraindications, dosing.
Several additional species belonging to the genus ephedra have traditionally been used for a variety of medicinal purposes, and are a possible candidate for the soma plant of indoiranian religion. Patients in shock may require intravenous administration to. Ephedrine is a generic medicine name and there are several brands available for it. The physiological effects of ephedrine are very similar to those of epinephrine but are much more prolonged. Ephedrine has several benefits that stems from using this drug such as, treating obesity and asthma, however, there are also a string of negative effects including, overdose and death, if not used. There are very few animal studies conducted investigating the toxic effects of ephedra. Ephedrine sulfate injection is administered by the intramuscular, subcutaneous or intravenous route. Ephedrine free download as powerpoint presentation. Onset with intravenous use is fast, while injection into. Ephedrine and its metabolites are excreted primarily in the urine, mostly as unchanged drug. In order to ensure that usersafety is not compromised and you enjoy faster downloads, we have used trusted 3rdparty repository links that are not hosted on our website. In the present study, ephedrine alkaloids were evaluated for their binding affinities on human alpha1a, alpha1b, alpha1d, alpha. Ephedrine is a substituted amphetamine and a structural methamphetamine analogue. Both drugs produce an aggregation effect and forced exercise increases the toxicity of each drug as much as does grouping.
In all parameters tested the effects of ephedrine and cocaine resemble qualitatively those of amphetamine, but are less potent. Enhanced stimulant and metabolic effects of combined. It has been used in traditional chinese medicine for more than 2,000 years. Ephedrine reduces the pain from propofol injection. Ephedrine hydrochloride myx injection contains no preservative and is for single use in one patient on one occasion only. Asthma research council clinical pharmacology unit, department of medicine, cardiothoracic institute, brompton, london, sw36hp i ephedrine plasma levels have been measured in ten asthmatic patientsgiven a single dose of ephedrine hydrochloride 22 mg alone and in combination with theophylline and a barbiturate. Pseudoephedrine is a phenethylamine and a diastereomer of ephedrine with sympathomimetic property. Pharmacological effects of ephedrine alkaloids on human alpha. Ephedrine shares many pharmacological actions with epinephrine, although ephedrine is much less active.
The free base forms derivatives such as hydrobromides, hydrochlorides, phosphates, oxalates, and sulphates. Ephedra and ephedrine complementary and alternative. Publications studying pharmacokinetics of oral administration of ephedrine support that ephedrine is metabolized into norephedrine. Ephedrine s chemical structure contains two chiral centers, resulting in two stereoisomers of ephedrine 1r,2s and 1s,2r and two enantiomers 1r,2r and 1s,2s, known as pseudoephedrine. The acute toxicity of ephedrine journal of pharmacology. Studies using ephedrine in animals suggest that if it is given in excessive amounts, it produces symptoms of sympathetic stimulation, manifested by anxiety and restlessness. Ephedrine may deplete norepinephrine stores in sympathetic nerve endings.
At a concentration of 10 3 m, drug effect was reversible after rinsing with a drug free the mepc disappeared. These considerations, as we have stated elsewhere,1 led us into an. All of these agents increased blood pressure and respiratory rate, produced similar types of subiective changes, and increased the excretion of epinephrine. Lowdose ephedrine plus priming with lowdose cisatracurium before an intubating dose, significantly improved clinical intubating conditions at 60 seconds. Physiologic, subjective, and behavioral effects of. At 10 3 m ephedrine, the mepp and by 67%, respectively but the decay phase of the became undetectable after 45 min of incubation. Pdf the early importance of ephedrine was its role as the first oral bronchodilator available for the treatment of asthma. Ephedrine, synephrine, and caffeine are all well absorbed from the gastrointestinal tract. Pharmacological effects of the four ephedrine isomers were investigated. It differs from methamphetamine only by the presence of a hydroxyl group oh. Identification name ephedrine accession number db064 description. The sympathomimetic actions of lephedrine and dpseudoephed. Phenylephrine is a member of the class of the class of phenylethanolamines that is 1r2methylamino1phenylethan1ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.
Native americans and mormon pioneers drank a tea brewed. Pdf ephedrine is a sympathomimetic agent that has widespread use as an adrenergic stimulant. Central nervous system effects are similar to those of amphetamine drugs but less pronounced. The synthesis and pharmacology of ephedrine analogues. A pharmacological study of the ephedrine isomers pdf. Nausea, retching, or vomiting, as well as the degree of sedation and discharge times, were assessed in the recovery. The mass of ephedrine per 30mg of the ephedrine salt is 24. Efficacy of ephedrine in the prevention of postoperative nau. Ephedrine is a chemical contained in the ephedra herb.
Akovaz injection, 50 mgml, equivalent to 38 mg ephedrine base is injected intravenously as a. Ephedrine plus caffeine increased systolic blood pressure peak difference, 11. Physical and mental effects of a single oral dose of ephedrine ephedrine hcl 30 or 40 mg, fenfluramine fenfluramine hcl 15 or 20 mg, phentermine 7. Firstly, as ephedrine possesses two chiral centers and exists as four stereoisomers, the. Ephedrine c10h15no cid 9294 structure, chemical names, physical and. Ephedrine became a highly popular and effective treatment for asthma, particularly because, unlike adrenaline until then the standard therapy, it can be given by mouth. Efficacy of ephedrine in the prevention of postoperative. Of note, when discussing drug class, pharmacology, efficacy, safety, etcetera most references including published articles, drug databases and the reference product pi accessed by the evaluator discussed these issues in terms of the dose of. Akovaz ephedrine sulfate dose, indications, adverse effects.
Ephedrine is related to phenylpropanolamine, a decongestant removed from the market place due to concerns that its use increased the risk of. A pharmacological study of the ephedrine isomers journal of. Mehendale, in encyclopedia of toxicology third edition, 2014 acute and shortterm toxicity or exposure animal. Ephedrine is a longstudied stimulant available both as a prescription and overthecounter medication, as well as an ingredient in widely marketed herbal preparations, and is also used as a precursor for the illicit synthesis of methamphetamine. Ephedrine increases the level of norepinephrine whereas propanolol is a. Its peripheral actions, which it owes in part to the release of norepinephrine, simulate responses that are obtained when adrenergic nerves are stimulated. Identify and discuss the pharmacology of methamphetamine. Pseudoephedrine displaces norepinephrine from storage vesicles in presynaptic neurones, thereby releasing norepinephrine into the neuronal synapses where it stimulates primarily alphaadrenergic receptors. Few reports have appeared that examine the direct actions of ephedrine alkaloids on human subtypes of adrenergic receptors ars. It is often used to prevent low blood pressure during spinal anesthesia. This can be considered as an interesting biotransformation process for evaluation, as it includes both toxic substrate and endproduct inhibition. Ephedrine has medical uses, mostly in operating rooms and intensive care units.
Ephedrine as a treatment for asthma reached its zenith in the late 1950s, since when there has been a gradual and inevitable decline. Ephedrine hydrochloride should be administered in the lowest effective dose. Some of the brands for ephedrine might be better known than ephedrine itself. The pharmacological properties of the four stereoisomers may be quite diffe. To determine whether lowdose ephedrine plus priming with lowdose cisatracurium improves intubating conditions. Pediatric dosage calculations the first section of this topic is. Ephedrine stimulates both alpha and beta receptors and its peripheral actions are due partly to norepinephrine release and partly to direct effect on receptors. Mechanistic pharmacokinetic modelling of ephedrine, norephedrine. In general, the toxicity of either drug is increased by a rise in ambient temperature. Ephedrine s basic pharmacological action is that of a sympathomimetic. Download pharmacology books pdf free all medical stuff. The acute and chronic bronchodilator effects of ephedrine.
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