Epherdrine

[bulkyboy]

Can anyone give me any info on epherdrine?

[PEWN]

Chemistry
Ephedrine exhibits optical isomerism and has two chiral centres. By convention the enantiomers with opposite stereochemistry around the chiral centres are designated ephedrine, while pseudoephedrine has same stereochemistry around the chiral carbons. That is, (1R,2R)- and (1S,2S)-enantiomers are designated pseudoephedrine; while (1R,2S)- and (1S,2R)-enantiomers are designated ephedrine.

The isomer which is marketed is (-)-(1R,2S)-ephedrine.[2]

As with other phenylethylamines, it is also somewhat chemically similar to methamphetamine, although the amphetamines are more potent and have additional biological effects.

Ephedrine may also be referred to as: (αR)-α-[(1S)-1-(methylamino)ethyl]benzenemethanol, α-[1-(methylamino)ethyl]benzyl alcohol, or L-erythro-2-(methylamino)-1-phenylpropan-1-ol. Ephedrine hydrochloride has a melting point of 187-188°C.[3]


[edit] Mode of action
Ephedrine is a sympathomimetic amine - that is, its principal mechanism of action relies on its indirect action on the adrenergic receptor system, which is part of the sympathetic nervous system or SNS. Whilst it may have weak agonist activity at α- and β-adrenergic receptors, the principal mechanism is to displace norepinephrine from storage vesicles in presynaptic neurons. The displaced norepinephrine is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors.

Ephedrine's mechanism of action on neurotransmission in the brain is wide. Its action as an agonist at most major norepinephrine receptors and its ability to induce moderate stimulation of the release of both dopamine and to a lesser extent, serotonin, is presumed to have a major role in its mechanism of action.

Because of ephedrine's ability to potentiate dopamine neurotransmission it is thought to have addictive properties by some researchers.

While ephedrine's role in the serotonin system is less understood there is preliminary documentation of clinically significant agonism at excitory serotonin receptors, perhaps as a downstream response to the large release of norepinephrine in the nucleus accumbens (commonly referred to as the "pleasure center" of the brain). In mice, stereotypical behaviour was both easily induced by administration of ephedrine and it's primary alkaloids and reversed when serotonin antagonists were administered.


[edit] Clinical use

Ephedrine Sulphate (1932) Ephedrine Compound (1932) and Swan-Myers Ephedrine Inhalant No. 66 (ca. 1940)
[edit] Indications
Ephedrine was once widely used as a topical decongestant and as a bronchodilator in the treatment for asthma. It continues to be used for these indications, although its popularity is waning due to the availability of more effective agents for these indications which exhibit fewer adverse effects.[4] The role in nasal congestion has largely been replaced by more potent α-adrenergic receptor agonists (e.g. oxymetazoline). Similarly the role of ephedrine in asthma has been almost entirely replaced by β2-adrenergic receptor agonists (e.g. salbutamol). Ephedrine continues to be used intravenously in the reversal of hypotension from spinal/epidural anaesthesia.[4] It is also used in other hypotensive states, including overdose with ganglionic blocking agents, antiadrenergic agents, or other medications that lower blood pressure.[5] It can be used in narcolepsy and nocturnal enuresis.

In traditional Chinese medicine, ephedrine has been used in the treatment of asthma and bronchitis for centuries.[6]

An ECA stack is a component found in thermogenic weight loss pills, composed of ephedrine, caffeine and aspirin (many supplement manufacturers include salicin instead of aspirin) working to speed up the metabolism and thus cause food energy to burn faster. The ECA stack is a popular supplement taken by body builders before workouts due to the increased amount of energy and alertness.

For many years, the US Coast Guard recommended ephedrine together with an equal 25 mg dose of promethazine to its sailors to combat seasickness. Promethazine manages nausea and ephedrine fights the ensuing drowsiness. Commonly referred to as the Coast Guard cocktail, ephedrine may still be available for prescription for this purpose.


[edit] 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:[4]

Cardiovascular: tachycardia, cardiac arrhythmias, Angina pectoris, vasoconstriction with hypertension
Dermatological: flushing, sweating, acne vulgaris
Gastrointestinal: nausea, appetite loss
Genitourinary: increased urine output due to increased blood flow (difficulty urinating is not uncommon, as alpha-agonists such as ephedrine constrict the internal urethral sphincter, mimicking the effects of sympathetic nervous system stimulation)
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
The approved maximum daily dosage of ephedrine for use as a bronchodilator is 150mg, as specified on the packaging of the bronchodilator and expectorant combination, Bronkaid, made by Bayer pharmaceuticals.

Overdose can lead to death, although the approved dose is not likely to cause severe reactions when used as directed.

Ephedrine can also lead to damage of the brain receptors over a period of high usage; this is because of its constant action on the neurochemicals. It also leads to high increase in blood pressure which over time can lead to damage in the blood vessels.


[edit] Contraindications
Ephedrine should not be used in conjunction with certain antidepressants, namely SNRIs (Selective norepinephrine re-uptake inhibitors), as this increases the risk of the above symptoms due to excessive serum levels of norepinephrine.

Wellbutrin is an example of an antidepressant with an amphetamine-like structure similar to ephedrine. It has a similar action but also releases serotonin from presynaptic clefts. It should not be used with ephedrine as it may increase the likelihood of the above side effects.

Ephedrine should be used with caution in patients with inadequate fluid replacement, impaired adrenal function, hypoxia, hypercapnia, acidosis, hypertension, hyperthyroidism, prostatic hypertrophy, diabetes mellitus, cardiovascular disease, during delivery if maternal BP > 130/80 mmHg, and lactation.[7]

Contraindications for the use of ephedrine include: closed angle glaucoma, phaeochromocytoma, asymmetric septal hypertrophy (idiopathic hypertrophic subaortic stenosis), concomitant or recent (previous 14 days) monoamine oxidase inhibitor (MAOI) therapy, general anaesthesia with halogenated hydrocarbons (particularly cyclopropane or halothane), tachyarrhythmias or ventricular fibrillation, hypersensitivity to ephedrine or other stimulants. Ephedrine should NOT be used at any time during pregnancy unless specifically indicated by a qualified physician and ONLY when other options are unavailable.[7]

[Amorphic]

A simple search would have also found this info as well, good job to pewn for finding it for you.

[fatrock]

good info Bro way to answer a very vague question

[magic32]

Good post Pewn.

[SilverToungedDevil]

you remember when ephedra was legal.... what was the dose on things like ripped fuel.. was it a 200mg caffeine 200mg ephedra ?? i can't remember. that shiiit was the shiiiiiit

[bulkyboy]

cheers for that,i just wanted a bit more info and to c what you guys thought of it. i already knew the basics of it. ive got some now so will be testing them out.

[Kelleh]

200mg of epedra ..........I know when I took ECA stack the epdedrine pills were only 8mg lol

[juststartin]

you remember when ephedra was legal.... what was the dose on things like ripped fuel.. was it a 200mg caffeine 200mg ephedra ?? i can't remember. that shiiit was the shiiiiiit

it was 20mg of ephedra

[Kelleh]

hahaha that makes a little more sense.

[SilverToungedDevil]

it was 20mg of ephedra

right on... i used to take that stuff like it was going out of style back in the day, works wonders

[Dizz28]

you remember when ephedra was legal.... what was the dose on things like ripped fuel.. was it a 200mg caffeine 200mg ephedra ?? i can't remember. that shiiit was the shiiiiiit

It was legalized again for only a few months earlier this year. I remember walking into a gas station and seeing it in those blister packs of 6 - 50mg ephedrine/200mg guifenisen (sp). I think they were called "2way" or something. Anyway, i ended up buying about 20 packs over the next week and then it was gone off the shelves again....annoying

[magic32]

you remember when ephedra was legal.... what was the dose on things like ripped fuel.. was it a 200mg caffeine 200mg ephedra ?? i can't remember. that shiiit was the shiiiiiit

By far my favorite supplement ever!

So permit me to inject some light into this cloudy often confusing era of supplemental history while simultaneously explaining some of the wildly varying figures seen within this thread, most of which are the result of conversion ratios:

The basic elements in early more popular ECA stacks (Ripped & Diet Fuel, Hydroxycut, Xenadrine, Metabolift, etc.), although the blends vary, was an approximate ratio of a 3-2-1 (E-C-A) profile.

Below I've listed the ratio along with the actual elements.

• 300mgs MaHaung; 334mgs in most blends (standardized at between 6-8% Ephedra alkaloids) which is equivalent to 20mgs (some used 25mgs) of Ephedra.
• 910mgs Guarana Extract (standardized for 22% caffeine) or approx. 200mgs of caffeine sometimes 171mgs.
  (Should be used in a 10:1 ratio of caffeine:Ephedra; 200 mgs of caffeine to 20 mgs of EPH)
• 100mgs White Willow Bark which is 100mgs of Aspirin (but often slightly lower).

Those were the days, but they can and still are being lived by many...myself included!

Side note: Two other basic ingredients were 100mgs of L-Carnitine, and 200mcgs of Chromium Picolinate.