| Cocaine | |
|---|---|
| [[File:|250px]] | |
| Formula | C₁₇H₂₁NO₄ |
| Type | Tropane alkaloid; local anesthetic; CNS stimulant (dopamine/norepinephrine reuptake inhibitor) |
| Administration | Insufflation (nasal), smoked (crack), IV injection, oral (coca leaf chewing), topical (medical) |
| Solubility | Hydrochloride salt: freely soluble in water; freebase (crack): insoluble in water, soluble in lipids |
| Legal status | Schedule II (US) — medical use permitted; illegal for recreational use in most countries |
| Synonyms | Benzoylmethylecgonine, coke, crack (freebase form), coca, blow, white girl, goey |
| Bioavailability | Oral: ~33%; Insufflated: ~60-80%; Smoked: ~70%; IV: 100% |
| Recommended dose | |
| Upper limit | |
| LD50 | |
| Ray's verdict | Blames malnutrition for coke babies |
Cocaine is a tropane alkaloid derived from the coca plant (Erythroxylum coca), native to the Andes mountains of South America. The coca leaf has been used medicinally in South America for improved fertility, prolongation of virility into old age, prevention of altitude sickness, and various other purposes.
Weston Price described how the natives of the Andes used coca leaves: they could increase the quantity of the drug used to a point at which they are quite unconscious of pain and able to endure injuries without suffering and operations without discomfort.
In the 19th century in the U.S., cocaine was officially recognized as a therapy for asthma. The popular perception in America was that morphine was "unamerican" because it made you lazy and tired while cocaine was positively American because it increased alertness and efficiency which were much prized qualities in the time of industrialization.
Julius Axelrod's research demonstrated: Cats pretreated with cocaine showed a dramatic decrease in tissue H³-noradrenaline... cocaine markedly reduces the uptake of noradrenaline in tissues, presumably the sympathetic neurone. The inhibition of uptake by cocaine thus raised the extraneural concentration of noradrenaline... By blocking uptake into the nerves, cocaine caused an elevated concentration of noradrenaline to reach the receptor.
Additionally, cocaine increases progesterone production and probably has antihistamine action. Cocaine increases the production of the pituitary gonadotrophin, LH (luteinizing hormone), which increases ovarian progesterone production. In men, LH increases testosterone production.
Research citation: "Cocaine (0.8 mg/kg) stimulated a significant increase in luteinizing hormone (LH) within 10 to 20 min (P < .01) and LH reached peak levels (59-60% above base line) within 30 min after cocaine administration... Male testosterone increased by 50% above average base-line levels 50 min after the LH peak."[1]
The Andean people who use coca regularly appear to suffer no harmful effects. Coca chewing prevents the hypoglycemia that can be produced by extremely high altitude. It is common to keep a wad of the leaf in the mouth all day. The dental health of coca-chewers is so good that a Bolivian company has marketed a toothpaste containing coca leaf.
Novocaine (procaine) was introduced as a substitute for cocaine, but it has been found to have protective effects on the organism, as an adaptogen. Lidocaine and other local anesthetics have many important protective effects.
The "local anesthetics," which generally have a broad range of effects, are an important class of adaptogens. Procaine has been found to normalize almost every system studied. Doses far too small to have an anesthetic effect have clear biological effects.
Cocaine suppresses appetite. When pregnant animals are fed the same limited amount of food consumed by cocaine-treated animals, their undernourished offspring show most of the same effects seen in the litters that were exposed to cocaine.
As a stimulant, cocaine increases the metabolic rate, which in turn can lead to the wastage of protein, to provide energy. Conventional first aid for a cocaine overdose includes providing glucose and thiamine, to provide energy.
Some researchers have concluded that cocaine might not be a behavioral teratogen.[2] Others have described it as "not a potent neuroteratogen."[3]
Research citation: "Despite treatment during the major periods of organogenesis and brain development, few congenital abnormalities were observed... Despite suppression of maternal weight gain, there was preservation of fetal weights at cocaine doses up to and including 80 mg/kg/day, suggesting some protection of fetal growth."[4]
Despite extensive adverse publicity, tobacco use continues in approximately 25% of all pregnancies in the United States, overshadowing illicit drugs of abuse, including cocaine... In light of the fact that nearly all crack cocaine users smoke cigarettes, the identification of specific developmental effects of cocaine may prove difficult to detect.[5]
| Route | Lethal Threshold |
|---|---|
| IV | As little as 20 mg reported fatal
|
| Oral | Average lethal dose ~`500 mg` |
| Rat teratogenic threshold | 50 mg/kg IP (no effect at 40 mg/kg); 80 mg/kg lethal to dam
|
Ray Peat noted: "In animal studies, doses equivalent to thousands of milligrams per day in humans are injected into rats before harmful effects are seen in the fetuses... the only doses that caused measurable fetal harm in rats were doses that, on a weight basis, almost certainly would have caused nearly instantaneous death in humans."
Traditional: Coca leaf (Erythroxylum coca) — chewed or brewed as tea in Andean cultures
Medical derivatives:
Ray Peat mentioned that Mexican Coca-Cola still contains coca leaf extractives (with cocaine removed): "I think the coca leaf extractives are really biologically active, doing something very different from the caffeine content... when they compared Pepsi to Coke... Coke was very high in potassium, and the plant extractives are the only logical source for potassium."
Legal status: Schedule II (US) — medical use permitted under strict controls; illegal for recreational use globally.