Buy Ephedrine Online

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What is Ephedrine?

Ephedrine is a phenethylamine present in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. Also It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It his in use for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It is becoming less extensively in use with the advent of more selective agonists.

Ephedrine is an alpha-Adrenergic Agonist, and beta-Adrenergic Agonist, and Norepinephrine Releasing Agent. The mechanism of action of ephedrine is as an Adrenergic alpha-Agonist, and Adrenergic beta-Agonist. The physiologic effect of ephedrine is by means of Increased Norepinephrine Activity.    An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. Also It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. Also It has become less extensively used with the advent of more selective agonists.

Ephedrine is an alkaloid that is an hydroxylate form of phenethylamine and sympathomimetic amine, with potential bronchodilatory and anti-hypotensive activities. Also Following administration, ephedrine activates post-synaptic noradrenergic receptors. Activation of alpha-adrenergic receptors in the vasculature induces vasoconstriction, and activation of beta-adrenergic receptors in the lungs leads to bronchodilation.

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Drug Indication

Ephedrine

Use of the bronchodilator and stimulant ephedrine [(1R,2S)-2-(methylamino-1-phenylpropan-1-ol] by athletes at the Olympic Games is not permissible. Its 1S,2S isomer is the common nasal decongestant pseudoephedrine, so the sniffling at award ceremonies might not just be emotional. Ephedrine commonly in use as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia.

Therapeutic Uses

Adrenergic alpha-Agonists, adrenergic beta-Agonists, adrenergic Agents; appetite Depressants; Bronchodilator Agents; Central Nervous System Stimulants; Sympathomimetics; Vasoconstrictor Agents

Ephedrine hydrochloride injection is on the WHO Model list of essentials for use in spinal anesthesia during delivery, to prevent hypotension. Also Its use requires specialist diagnostic or monitoring facilities, and/or specialist medical care, and/or specialist training. /Ephedrine hydrochloride/

Uses: Diseases of the respiratory tract with mild bronchospasms in adults and children over the age of six. /Ephedrae herba, ephedra, ma-huang/

Blumenthal M, ed.; Ephedra. In the Complete German Commission E Monographs. Therapeutic Guide to Herbal Medicines. p. 125-6. The American Botanical Council, Austin, TX (1998)

Indications and Usage: Approved by /German/ Commission E: Cough/bronchitis. Uses: Ma-huang in use for diseases of the respiratory tract with mild bronchospasms in adults and children over the age of six. Various indications include asthma, cardiovascular stimulation and as a CNS stimulant. Chinese Medicine: Also The drug is in use for over 4000 years for severe febrile illnesses, bronchial asthma, joint symptoms, inability to perspire, coughing with dyspnea, edema and pains in the bones. /Ma-huang (Ephedra sinica)/

Ephedra preparations to be in support by clinical data: treatment of nasal congestion due to hay fever, allergic rhinitis, acute coryza (rhinitis), common cold, sinusitis, and as a bronchodilator in treatment of bronchial asthma /Herba ephedrae/

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Pharmacology

Ephedrine is similar in structure to the derivatives amphetamine and methamphetamine. Chemically, it is an alkaloid from various plants in the genus Ephedra (family Ephedraceae). Also It works mainly by increasing the activity of noradrenaline on adrenergic receptors. Moreover the video below.

Metabolism/Metabolites

Ephedrine is a sympathomimetic amine – that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system. Also Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine.

Also the ephedrine, mixture with noradrenaline, transportation through the noradrenaline reuptake complex and packages (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell.  However, only a relatively small amount of MEPH (15.5%)  comes out unchanged in urine.
Abstract: PubMeds

Mechanism of Action

Ephedrine is a sympathomimetic amine – that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system. Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine.

The ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell. Ephedrine’s action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent, serotonin by the same mechanism is presumed to have a major role in its mechanism of action.

Methods of Manufacturing

Fermentation of benzaldehyde & molasses with yeast to give levo-1-phenyl-2-keto-1-propanol which is condensed with methylamine & reduced with activated aluminum in moist ether to yield the free base; the salts are produced by addition of hydrochloric or sulfuric acid

Microbial fermentation medium + benzaldehyde + methylamine (microbial conversion/reductive amination)

Also Ephedrine is a naturally occurring alkaloid drugs are derivatives of Ephedra equistina and Ephedra vulgaris.

Furthermore (-)-Ephedrine from the Ma Huang drug (Ephedra “vulgaris”, E. sinica Stapf, E. equisetina Bunge) and other types of Ephedra. The powder drug is alkalize and extracts from benzene are done. Also The solution obtain is with dilute acid, and the ephedrine crystallized after concentration of the aqueous phase.

Adverse effects

Adverse drug reactions (ADRs) are more common with systemic administration (e.g. injection or oral administration) compared to topical administration (e.g. nasal instillations). ADRs associated with ephedrine therapy include.

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

Dermatological: flushing, sweating, acne vulgaris

Gastrointestinal: nause Also

Nervous system: restlessness, confusion, insomnia, mild euphoria, mania/hallucinations (rare except in previously existing psychiatric conditions), delusions, formication (may be possible, but lacks documented evidence) paranoia, hostility, panic, agitation

Respiratory: dyspnea, pulmonary edema

Miscellaneous: dizziness, headache, tremor, hyperglycemic reactions, dry mouth

 

Also The neurotoxicity of l-ephedrine is in dispute

 

 

Reference

  1. http://whqlibdoc.who.int/hq/2005/a87017_eng.pdf
  2. https://en.wikipedia.org/wiki/Ephedrine
  3. https://pubchem.ncbi.nlm.nih.gov/compound/Ephedrine
  4. https://www.drugbank.ca/drugs/DB01364

 

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