Ephedrine Caffeine

The main classes of over-the-counter stimulants contain caffeine, ephedrine/pseudoephedrine, or herbal varieties of stimulants. Each of these will be discussed in this chapter. 

For most substances, just their presence in a urine sample means a positive result. Other substances must be present in an amount higher than a certain threshold. According to Dr. Ayotte, a male athlete would have to consume "10 very strong French coffees within 15 min" to go over the 12 mg/L limit for caffeine. Ephedrines and pseudoephedrines, two decongestants that are found in cough remedies and that act as stimulants, have a cut-off level. This allows athletes to take them up to one or two days before a competition. 

Look-alikes contain caffeine, ephedrine, or phenylpropanolamine, either singly or in combination. Ephedrine is a natural stimulant with a chemical structure resembling adrenaline that produces more anxiety and less euphoria than amphetamines. It... 

Povidone K 25 added, jig Lactose Glucose Tartaric acid Acetyl- salicylic acid Thiamine hydro- chloride Brom- isoval Caffeine Ephedrine hydro- chloride Lidocaine Meproba- mate Pheno- barbital Salicyl- amide... 

A, S,codeine, papaverine,quinine, caffeine, ephedrine Various drugs Retention behaviour basic drugs in ion-pair HPLC pBondapak C18 pBondapak Phenyl pBondapak CN pBondagel Chromegabond C8 Chromegabond CgH 300x4 0.005M heptanesulfonic acid in H,0-MeOH-AcOH(50 49 1) (pH <-0) 50... 

Interactions with caffeine and aspirin can increase the effects of ephedrine. Norepinephrine works in part by increasing the levels of cyclic aminomethyl propanol (AMP) in cells. Caffeine inhibits the enzyme that breaks down cyclic AMP. Together, ephedrine makes more cyclic AMP, and caffeine prevents it from breaking down. Aspirin inhibits the receptors that turn off release of norepinephrine. 

Ephedrine by itself has been shown to be ineffective as a weight-loss treatment. Ephedrine combined with either caffeine or aspirin is effective. The effect appears to stem from a combination of appetite reduction and avoidance of the metabolic rate decrease usually associated with a reduced-calorie diet. 

Many diet pills that work by increasing the number of calories burned have been developed. Most of these contain one or more of the three ingredients caffeine, phenylpropanolamine (PPA), and ephedrine. In the United States, PPA and ephedrine have been withdrawn from the market because they produce serious side effects, including heart attack and stroke. Caffeine, which is still found in many diet pills, will be further discussed in Chapter 6. 

Many pharmacologically active organic chemicals fonnd in natnre are alkaloids. In general, these componnds contain one or more nitrogen atoms, which in turn impart some basicity to the molecnle. Well-known alkaloid examples are caffeine, cocaine, codeine, ephedrine, morphine, nicotine, qninine, and scopolamine. Heroin is derived from morphine by a chemical modification that increases lipophilicity, making the heroin molecnle inherently more pharmacologically potent than morphine. The exhibition of its basic properties by an alkaloid (Aik) involves (by definition) the acceptance of a proton H+ according to ... 

These alkaloids can also be derived from non-aminoacid precursors. The N atom is inserted into the molecule at a relatively late stage, for example, in the case of steroidal or terpenoid skeletons. Certainly, the N atom can also be donated by an amino acid source across a transamination reaction, if there is a suitable aldehyde or ketone. Pseudoalkaloids can be acetate and phenylalanine-derived or terpenoid, as well as steroidal alkaloids. Examples of pseudoalkaloids include such compounds as coniine, capsaicin, ephedrine, solanidine, caffeine, theobromine and pinidine (Figure 6). More examples appear in Table 1. 

Doxapram Nikethamide Pentylenetetrazol Strychnine Picrotoxin Bicuculline Amphetamine Methamphetamine Methylphenidate Pemoline Ephedrine Phentermine Fenfluramine Phenylpropanolamine Caffeine Theophylline Theobromine... 

Ephedra (ma huang) is a popular botanical incorporated into a variety of formulations for weight loss, energy or performance enhancement, and symptomatic control of asthma. A pharmacodynamic interaction leading to a fatality has been reported with concurrent use of caffeine and ephedra (62), possibly as a result of additive adrenergic agonist effect of the ephedrine alkaloids and caffeine on the cardiovascular system and the CNS (63). Ephedra was recently withdrawn from the market (64). 

Stimulant drugs commonly abused in the USA include methamphetamine ("crank," "crystal"), methylenedioxymethamphetamine (MDMA, "ecstasy"), and cocaine ("crack") as well as pharmaceuticals such as pseudoephedrine (Sudafed) and ephedrine (as such and in the herbal agent Ma-huang) (see Chapter 32). Caffeine is often added to dietary supplements sold as "metabolic enhancers" or "fat-burners" and is also sometimes combined with pseudoephedrine in underground pills sold as amphetamine substitutes. 

CNS, smooth muscle T diuresis X- pit aggregation Available forms Daily t doses w/ max 3 g PO daily Contra Avoid in PRG lactation, CAD, hyperthyroidism, anxiety disorders d/t high, caffeine content Notes/SE Insomnia, tach, anxiety, N/V, HA, HTN, Sz Interactions T Effects OF anticoagulants, anti-pits, BBs, bron-choclilators T risk of hypertensive crisis W/ MAOIs T effects W/ cimetidine, ciprofloxacin, ephedrine, hormonal contraceptives, dieophylline, cola, coffee X-effects OF adenosine, antihypertensives, benzodiazepines, Fe, X- effects W/ smoking EMS Tinctures contain EtOH may exacerbate GI disorders HTN T effects of anticoagulants and BBs... 

Norephedrine and ephedrine mimic and stimulate the release of the adrenal hormones norepinephrine and epinephrine. Norephinephrine raises heart rate and epinephrine stimulates carbohydrate metabolism resulting in an increased metabolic rate, fatty acids release from lipocytes (fat cells), and a protein sparing effect. Caffeine simply prolongs the effect. 

Headaches, high blood pressure, and elevated body temperature were among noted side effects. Many reported side effects after 8-12 days. The body quickly adapts to clenbuterol so "on/off periods were a must for successful results. By alternating between E/C (Ephedrine and caffeine) stacks and Clenbuterol, the effective period was extended and results increased. Rotations weekly such as clenbuterol, week 1, ephedrine/ caffeine week 2, seem to have brought superior results. 

Clenbuterol 80-120 MCG daily, 2 days on alternated with 50 MG of Ephedrine /350 MG of Caffeine. 

Some body builders tout the combination of caffeine with the herbal stimulant ephedra as harmless, and suggest the combination helps turn fat into muscle. A study published in 2001 does support the claim that caffeine and ephedrine can boost results in laboratory attempts to mimic the tasks of competing athletes. However, ephedra, the herbal drug containing the chemical ephedrine, has been linked to several deaths. 

Bell, Douglas. Effect of Caffeine and Ephedrine Ingestion on Anaerobic Exercise and Performance. Medicine and Science in Sports and Exercise 33 (August 2001) 1399-1403. 

Because of high demand, ecstasy pills are frequently mixed with fillers and other active substances, most commonly amphetamines (speed), caffeine, and ephedrine (a natural amphetamine-like substance). Some pills have been found to contain DXM (dextromethorphan), a dissociative psychedelic found in some cough medicine, and PMA (paramethoxyamphetamine), a highly toxic hallucinogenic stimulant. 

In the United States, ephedrine alkaloids are derived from the Ephedra sinica, or ma huang plant. Most ephedra supplements contain a standard extract of 6-8% ephedrine alkaloids. Other herbs and ingredients, including caffeine, may also be added to ephedra supplements. 

In general, plants do very well in their environments, notwithstanding the omnipresence of a multitude of potential insect herbivores and a number of vertebrate herbivores as well. Some plant species are very insecticidal, as a consequence of their producing a variety of alkaloids including nicotine, piperine, lupine alkaloids, steroidal alkaloids, ephedrine, berberine, strychnine, gramine, and caffeine.37 These biologically active alkaloids also function as deterrents. In terms of families, caffeine is the the most widely distributed alkaloid, a fact that may be... 

Several SM have been used by mankind for thousands of years22,27 as dyes (e.g., indigo, shikonine), flavors (e.g., vanillin, capsaicin, mustard oils), fragrances (e.g., rose oil, lavender oil and other essential oils), stimulants (e.g., caffeine, nicotine, ephedrine), hallucinogens (e.g., morphine, cocaine, mescaline, hyoscyamine, scopolamine, tetrahydrocannabinol), insecticides (e.g., nicotine, piperine, pyrethrin), vertebrate and human poisons (e.g., coniine, strychnine, aconitine) and even therapeutic agents (e.g., atropine, quinine, cardenolides, codeine, etc.). 

The liquid form of ketamine is sometimes baked to yield a solid form that is often sold on the street as a fine white powder. This powdered form can be snorted, smoked, or packed into gel caps and taken orally. These ketamine pills are usually very diluted and cut with a stimulant such as caffeine or ephedrine (a natural amphetamine-like chemical). 

---