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Cocaine Cocaine - Mixed Information (LD50, Fatal Human Doses, Roads of adminstraion, adulterants)

Ignio

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Everything from http://www.inchem.org/documents/pims/pharm/pim139e.htm#SectionTitle:7.2 Toxicity

Cocaine hydrochloride
Taste and smell:
Hygroscopic odourless bitter tasting crystals.
Solubility in water:
200 grams per 100 mLs
Solubility in alcohol: 25 grams per 100 mLs In ether: insoluble Melting point: 197°C 1% solution is of neutral pH (Pharmacopée française, 1982; Clarke, 1986; Dorvault, 1987) Cocaine freebase: Slightly volatile, anhydrous, bitter tasting crystals Solubility in water: 0.17 grams per 100 mL In alcohol: 15.4 grams per 100 mL In ether: 28.6 grams per 100 mL Melting point 98°C Boiling point 187 to 188°C pH: alkaline (Budavari, 1989) Street cocaine used by addicts can be mixed with a number of diluents ("cut"), and these include amphetamines, anti-histamines, benzocaine, inositol, lactose, lidocaine, mannitol, opioids, phencyclidine, procaine, sugars, tetracaine, and sometimes arsenic, caffeine, quinidine, and even flour or talc.


Cocaine hydrochloride Solubility in water: 200 grams per 100 mLs
In other words, 2 gram pure cocaine should disolve completely in 1 ml of water

Cocaine may disturb glucose control because of its propensity to cause hyperglycemia. Drugs that affect catecholamine metabolism (eg, guanethidine, dopamine, alpha-methyldopa, tricyclic antidepressants, monoamine oxidase inhibitors) enhance the sympathomimetic effects of cocaine. In overdose but not in therapeutic doses, the propensity of cocaine to produce cardiovascular depression and dysrhythmias incr the risk to those patients with underlying cardiovascular disease.
Ellenhorn, M.J. and D.G. Barceloux. Medical Toxicology - Diagnosis and Treatment of Human Poisoning. New York, NY: Elsevier Science Publishing Co., Inc. 1988., p. 650

Repeated topical application of cocaine can result in psychic dependence and tolerance; the drug is often abused by parenteral or intranasal administration or by inhalation (smoking) because of its CNS stimulating effects. Prolonged intranasal use of cocaine can cause ischemic mucosal damage or perforation of the septum.
American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 2893

A survey of cocaine users revealed that 61% were intranasal users, 21% smoked the freebase form, and 18% were IV users.
[Gossel, T.A., J.D. Bricker. Principles of Clinical Toxicology. 3rd ed. New York, NY: Raven Press, Ltd., 1994., p. 351] **PEER REVIEWED**

Fatal Human Dose
Lethal doses are estimated at 0.5 to 1.3 grams per day by mouth; 0.05 to 5 grams per day by the nasal route, 0.02 grams of cocaine by the parenteral route.
International Programme on Chemical Safety; Poisons Information Monograph: Cocaine (PIM 139) (1999) Available from, as of November 14, 2011: http://www.inchem.org/pages/pims.html

Lethal doses are estimated at 0.5 to 1.3 grams per day by mouth; 0.05 to 5 grams per day by the nasal route, 0.02 grams of cocaine by the parenteral route (Baschard & Richard, 1984; Haddad & Winchester, 1990; Burnat & Le Brumant-Payen, 1992). Cocaine addicts can tolerate doses up to 5 grams per day. Toxic effects can be manifest with plasma concentrations equal to or above 0.50 mg per litre; deaths have been reported with concentrations of 1 mg per litre (Clarke, 1986).
http://www.inchem.org/documents/pims/pharm/pim139e.htm

Non-human LD50 values
LD50 Rat iv 17,500 ug/kg (Own comment: If converted to a human with a body weight of 80 kg: LD50 1,4 g of pure cocaine)
Lewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 978

LD50 Mouse oral 99 mg/kg (Own comment:If converted to a human with a body weight of 80 kg: LD50 7,920 g of pure cocaine) This one I stronly doubt the correctness of.
Lewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 978

LD50 Mouse iv 30 mg/kg (Own comment: If converted to a human with a body weight of 80 kg: LD50 2,4 g of pure cocaine)
Lewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 978

LD50 Dog iv 13 mg/kg (Own comment: If converted to a human with a body weight of 80 kg: LD50 1,040 g of pure cocaine)
Lewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 978

LD50 Rabbit iv 17 mg/kg (Own comment: If converted to a human with a body weight of 80 kg: LD50 1,360 g of pure cocaine)
Lewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 978

AVERAGE IV LD50 of a 80 kg person: 1,55 g pure cocaine
(if we assume that the values from animals tests can be converted to humans). I assume this is a rather than estimate. A saver bet would be around or below 1 gram of 99% pure cocaine

Absorption by route of exposure

Cocaine is absorbed by all routes of administration, but the proportion absorbed depends on the route (Haddad & Winchester, 1990). After oral administration, cocaine appears in blood after about 30 minutes, reaching a maximum concentration in 50 to 90 minutes (Clarke, 1986). In acid medium, cocaine is ionised, and fails to cross into cells. By the nasal route, clinical effects are evident 3 minutes after administration, and last for 30 to 60 minutes, the peak plasma concentration being around 15 minutes. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed (Ellenhorn & Barceloux, 1988; Stinus, 1992). By inhalation, the absorption can vary from 20 to 60%, the variability being related to secondary vasoconstriction.

Freebase cocaine does not undergo first-pass hepatic metabolism, and plasma concentrations rise immediately to 1 to 2 mg per litre. The effects on the brain occur very rapidly, after about 8 to 12 seconds, are very violent ("flash"), a nd last only 5 to 10 minutes (Burnat & Le Brumant-Payen, 1992; Stinus, 1992). By the intravenous route blood concentrations rise to a peak within a few minutes (Clarke, 1986).

By the nasal route, clinical effects are evident 3 minutes after administration, and last for 30 to 60 minutes, the peak plasma concentration being around 15 minutes. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed. By inhalation, the absorption can vary from 20 to 60%, the variability being related to secondary vasoconstriction. Freebase does not undergo first-pass hepatic metabolism, and plasma concentrations rise immediately. The effects on the brain occur very rapidly, after about 8 to 12 seconds, are very violent flash, and last only 5 to 10 minutes. By the intravenous route blood concentrations rise to a peak within a few minutes. Distribution by route of exposure: Cocaine is distributed within all body tissues, and crosses the blood brain barrier. Metabolism: Cocaine metabolism takes place mainly in the liver, within 2 hours of administration. The rate of metabolism varies according to plasma concentration. The principle metabolites are therefore benzoylecgonine, ecgonine methyl ester, and ecgonine itself, which are inactive; and norcocaine which is active, and may be relevant after acute intoxication. In the presence of alcohol, a further active metabolite, cocaethylene is formed, and is more toxic then cocaine itself.
https://toxnet.nlm.nih.gov/cgi-bin/sis/search2/r?dbs+hsdb:mad:term+@rn+@rel+50-36-2

Harm Reduction: Effective Anticonvulsant drugs
A number of anticonvulsant drugs were studied for their efficacy in preventing seizures and death from intoxication with cocaine. Rats were first pretreated with the test drug then subjected to large doses of intraperitoneally administered cocaine. In this model, control animals developed seizures in approximately 6 min, followed by death in approximately 10 min. Statistically significant protection against seizures and death was afforded by pretreatment with diazepam, phenobarbital and the blocker of the uptake of gamma-aminobutyric acid (GABA), SKF 100330A. Only partial protection was afforded by the N-methyl-d-aspartate(NMDA) antagonist MK 801, the benzodiazepine antagonist, flumazenil and the novel aminobenzamide, LY 201116. Valproic acid and phenytoin demonstrated limited efficacy against cocaine-induced seizures, without consistently reducing death. Carbamazepine and ethosuximide did not significantly reduce seizures or death. In this model of acute cocaine toxicity, the anticonvulsants diazepam, phenobarbital and the blocker of the uptake of GABA, SKF 100330A were the most effective in protecting rats from cocaine-induced seizures and death. These data offer insight into future approaches for the treatment of patients with the acute toxic effects of cocaine.
Abstract: PubMed
Derlet RW, Albertson TE; Neuropharmacology 29 (3): 255-9 (1990)


Harm Reduction: Interactions: Cholinesterase inhibition, MAO inhibitors, Anabolic Steroids and more
Inhibition of cholinesterase activity by these agents /cholinesterase inhibitors, such as antimyasthenics, cyclophosphamide, demecarium, echothiophate, neurotoxic insecticides possibly including large quantities of topical malathion, isoflurophate, thiotepa/ reduces or slows cocaine metabolism, thereby increasing and/or prolonging its effects and increasing the risk of toxicity; cholinesterase inhibition caused by echothiophate, demecarium, or isoflurophate may persist for weeks or months after the medication has been discontinued. /Cocaine hydrochloride/
USP. Convention. USPDI - Drug Information for the Health Care Professional. 19th ed. Volume I.Micromedex, Inc. Englewood, CO., 1999. Content Prepared by the U.S. Pharmacopieal Convention, Inc., p. 925

Monoamine oxidase (MAO) inhibitors /including furazolidone, procarbazine, and selegiline/ may prolong and intensify the cardiac stimulant and vasopressor effects of cocaine because of release of catecholamines that accumulate in intraneuronal storage sites during MAO inhibitor therapy, resulting in headache, cardiac arrhythmias, vomiting, or sudden and severe hypertensive and/or hyperpyretic crises; cocaine should not be administered during, or with 14 days following, administration of an MAO inhibitor. Phenelzine also inhibits cholinesterase activity and may reduce or slow cocaine metabolism, thereby increasing and/or prolonging its effects and increasing the risk of toxicity. /Cocaine hydrochloride/
USP. Convention. USPDI - Drug Information for the Health Care Professional. 19th ed. Volume I.Micromedex, Inc. Englewood, CO., 1999. Content Prepared by the U.S. Pharmacopieal Convention, Inc., p. 925

Cocaine and androgenic-anabolic steroids (AAS) abuse have become a serious public health problem. Despite reports of an increase in the incidence of simultaneous illicit use of these substances, potential toxic interactions between cocaine and AAS on the cardiovascular system are unknown. In the present study, we investigated the effect of single or combined administration of testosterone and cocaine for one or 10 consecutive days on basal cardiovascular parameters, baroreflex activity and hemodynamic responses to vasoactive agents in unanesthetized rats.Ten-day combined administration of testosterone and cocaineincreased arterial pressure baseline. Changes on arterial pressure were associated with altered baroreflex activity, and impairment of both hypotensive response to intravenous sodium nitroprusside (SNP) and pressor effect of intravenous phenylephrine. Chronic single administration of either testosterone or cocainedid not affect arterial pressure baseline. However, testosterone-treated animals presented rest bradycardia, cardiac hypertrophy, alterations in baroreflex activity, and enhanced response to SNP. Repeated administration of cocaine affected baroreflex activity and impaired vascular responsiveness to both SNP and phenylephrine. One-day single or combined administration of the drugs did not affect any parameter investigated.In conclusion, present results suggest a potential interaction between toxic effects of cocaineand testosterone on cardiovascular activity. Changes on arterial pressure baseline following combined administration of these two drugs may result from alterations in baroreflex activity and impairment of vascular responsiveness to vasoactive agents.
Abstract: PubMed
Engi SA et al; J Cardiovasc Pharmacol. 59 (3): 231-40 (2012)

Harm Reduction: Interactions: Cocaine and Hash
Combinations of cocaine and marijuana increase (up to 50 beats/min) the heart rate above levels seen with either drug alone.
Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 363

Purity and Methods of Purification that can be used for Harm Reduction
The average purity of cocaine in Europe at consumer level is high. It varied in 2009 from 18 % (Denmark) to 51.3. % (Belgium). Data available for 2004-09 show an overall decrease in the purity of cocaine in most reporting countries. The purity of crack is generally higher, but depends not only on the purity of the cocaine used in its manufacture, but also on the method of production. Common adulterants are phenacetin, lignocaine, benzocaine, procaine, caffeine, paracetamol and sugars. Some of these may be removed in the production of crack. Occasionally, unusual additives have been reported, such as atropine, diltiazem and other pharmaceutical substances. The free base constitutes 89 % of the hydrochloride salt.
[European Monitoring Centre for Drugs and Drug Addiction (EMCDDA); Drug Profiles: Cocaine and Crack (September 2011). Available from, as of November 14, 2011: http://www.emcdda.europa.eu/publications/drug-profiles/cocaine] **PEER REVIEWED**

Substances such as mannitol, lactose, glucose, and cornstarch may be added to increase bulk. Amphetamines and caffeine as well as lidocaine (Xylocaine) or procaine (Novocaine) may be added to mimic the stimulating and numbing effects buyers expect to receive with cocaine. Substances such as strychnine, PCP, and other toxic agents also may be mixed in, often with malicious intent.
Young, L.Y., M.A. Koda-Kimble (eds.). Applied Therapeutics. The Clinical Use of Drugs. 6th ed. Vancouver, WA., Applied Therapeutics, Inc. 1995., p. 84-8

Sources for the purification methods that I use to make cocaine of 99% purity (if the batch of cocaine you started out with did not contain levamisole (Here in Denmark, as a rule of thumb) most of the Bolivian and Peruvian cocaine do NOT contain levamisole while the Columbian cocaine does contain levamisole) if the cocaine contains levamisole I can achieve a purity of about 90-95% (there is an UNIMAGINABLE difference between 95% purity and 99% purity. For me those 4 percent feels like the difference between 25% purity and 75% purity in other words a 200% increase

Phenyltetrahydroimidazothiazole (i.e., levamisole, dexamisole, or tetramisole) has been increasingly utilized as a cutting agent by South American illicit cocaine laboratories for the past eight years, and is now the most predominant adulterant in cocaine produced in Colombia (Mallette, Casale and Jones, 2013)

Do not - I repeat: DO NOT - attempt to clean your morphine without having read extensively about the process as well as the chemicals you need to use in the purification process. One of the chemicals is acidic and can scare your air ways and longs, which is my you need a medical grade gasmask as well as a room with a system that sucks out air or else do it in a very large place and keep your distance after having used the chemical. Some of the chemicals can give you severe chemical burns as well on your skin, so avoid getting any on you and make sure to use containers that can actually contain the acid in order to avoid to acid burning through your container and whetever is underneath. It is my experience as well as you should not attempt to purify cocaine that you have not had tested at a medical grade lab thus being sure how pure it is and what is it laced with. The 2 dollar home made tests are not realiably enough. Mix in the wrong chemical with the wrong adulterant and you may have disaster on your hand. I set the limit at 20 grams because even if you have 10 grams that is 90% pure there will be some waste product stuck to the items you use in the purification process. The higher the dose of cocaine your purify the lower percantage of cocaine will go to waste. Seek advice and read extensively as I said before prior to attempting the process.

Description of common adulterants used to cut cocaine
(ATTENTION - The source is non-scientific, be critical to what you read)
(Everything from: http://www.rehabcocaine.com/blog/5-of-the-most-dangerous-impurities-added-to-cocaine/)
Benzocaine – This drug is known as a local anesthetic, typically found in topical, over-the-counter products such as creams and suntan lotions. While Benzocaine is commonly found in oral care products, regular ingestion can bring about very serious results, including a potentially life-threatening condition calledmethemoglobinemia, wherein the user will have dangerously abnormal levels of the hemoglobin called methemoglobin in the bloodstream. Further danger is present because while the more common onset of this condition occurs over time through the use of Benzocaine, there are also cases when the condition can present even with just a one-time exposure, such as in adulterated cocaine use.

Boric Acid – One of the reasons why boric acid is sometimes added to cocaine supplies is that it heightens the anesthetic effects, while also having the physical appearance of cocaine crystals. However, boric acid is also one of the most dangerous adulterants to encounter with cocaine use, particularly because it is considered a dangerous poison. Imagine having to ingest boric acid, when it is used in products such as glass fiber manufacturing, rodent and ant pesticides, photography chemicals, and a fireproofing agent for timber.

Lignocaine/Lidocaine – Lignocaine, also known as Lidocaine, can be used to lace cocaine due to its similar physical properties and anesthetic effects. The danger in its usage lies in the seriousness of allergic reactions, and may include tremors or seizures, uneven heartbeat, confusion, drowsiness and blurred vision. The non-recreational use of Lidocaine has to be cleared with a doctor, which is why cocaine use involving this substance makes the abuser even more susceptible to serious side effects.

Mannitol – Mannitol is commonly seen as an additive in heroin. It is also considered a successful adulterant for cocaine because of its anti-caking properties, used to keep the drug in its powdered state. The ingestion of Mannitol also comes with precautions, especially in cocaine use, as those who have allergic reactions to the substance, a history of heart failure or heart disease, or other problems involving the kidney, brain, or lungs, are already forewarned against the use of Mannitol.

Phenacetin – Among the many negative effects that come with the use of Phenacetin are dizziness, loss of consciousness, heart failure, severe swelling of the tongue, low blood pressure, and even death. Reports have also shown that Phenacetin has suspected cancer-causing properties, leading to a ban of the substance in the UK.

"Fun" (and not so fun) findings about cocaine
Cocaine has been reported to produce a prolonged and intense orgasm if taken prior to intercourse, and its use is associated with compulsive and promiscuous sexual activity. Long-term cocaine use, however, usually results in reduced sexual drive; complaints of sexual problems are common among cocaine users presenting for treatment.
Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 11th ed. New York, NY: McGraw-Hill, 2006., p. 621


Prevalence of substances traced in 104 samples sold as cocaine.
Substance
Prevalence (%)
4-Methylethcathinone1
Amphetamine1
Benzocaine2
Benzoylecgonine51
cis-Cinnamoylcocaine15
Caffeine35
Hydroxyzine1
Cocaine93
Mephedrone1
Levamisole
63
3,4-Methylenedioxy-N-methylamphetamine (MDMA)2
3′,4′-Methylenedioxy-α-pyrrolidinobutyrophenone (MDPBP)1
Lidocaine18
Methylenedioxypyrovalerone (MDV)2
Paracetamol7
Phenacetin43
Tetracaine1
Procaine4
trans-Cinnamoylcocaine13
Unknown substance
14
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4077236/

Notice the high percentage of cocaine cut with Levamisole. Avoud columbian cocaine if you wish to avoid Levamisole. As of yet Peruvian and Bolivian cocaine have a much lower risk of containing Levamisole. And whether you wish to purify your cocaine or just snort it or shoot it Levamisole should be avoided if possible.
The side effects of Levamisole are bad. The lesser side effects are things like vomiting and abdominal pain. The more seriouse are increased risk of serious infections and agranulocytosis (depletion of the white blood cells). Levamisole have also been seen to cause necrosis syndrome (rotting your skin from the inside).
 
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