Background Information

METHAQUALONE

General

The synthesis of methaqualone was first reported 1951. The drug was introduced pharmaceutically as non barbiturate, nonaddictive "sleeping pills" in 1965. It has been listed in the US Federal Register of March 1966 as an approved sedative-hypnotic with trade name Quaalude. The abuse potential of methaqualone quickly became apparent resulting in it being listed in the 1971 United Nations (UN) Convention on Psychotropic Substances, and its subsequent banning in most member countries. Methaqualone is currently listed in the UN Convention on Psychotropic Substances of 1988.

The production, trafficking, and abuse of methaqualone are of particular forensic importance to South Africa as it remains the synthetic drug of choice amongst South African drug abusers. This is illustrated by the fact that methaqualone-seizures amounts to more than 60% of all street-drug seizures submitted to the South African Police Service National Forensic Science Laboratories (SAPS FSL).During 2002 a total of 6064 methaqualone-related cases was submitted to the SAPS FSL, with the cumulative number of dosage units exceeding three million.

Methaqualone was introduced pharmaceutically in South Africa under the trade name "Mandrax", a formulation containing methaqualone (250 mg) and diphenhydramine hydrochloride (25 mg). Following the identification of its abuse potential, methaqualone and its isomers were effectively removed from the legal market in 1971. Methaqualone is currently regarded as an Undesirable Dependence-Producing Substance and is therefore listed in Part III of Schedule 2 of the South African Drugs and Drug Trafficking Act, Act 140 of 1992.

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Methaqualone seized in South Africa originates from illicit manufacturing sources in the Middle-East, South and Central Asia, as well as South and Southern Africa. The product is marketed in South Africa as illicit tablet formulations usually in combination with the antihistaminic drug diphenhydramine, and less frequently with the benzodiazepine tranquilliser diazepam. The formulation of methaqualone with diphenhydramine is thought to be historic in nature with illicit producers simply mimicking the original licit "Mandrax" formulation, or by design due to the fact that diphenhydramine inhibits the metabolism of methaqualone.

Methaqualone is highly addictive and abuse gives rise to a barbiturate-type dependence. The most prevalent abuse pattern observed in South Africa is in conjunction with Cannabis. This involves mixing methaqualone with Cannabis and then smoking it as a so-called "witpyp", i.e. white pipe.

The most frequent reported synthetic route for methaqualone involves the condensation of a primary aromatic amine, or salts thereof, with acylanthranilic acid, or acylanthranil. These compounds are either used as precursors, or prepared as intermediates, or in situ from anthranilic acid.
The second most reported route involves the reaction of isatoic anhydride with a primary aromatic amine and an acylating agent in either a one, or a two-step reaction. A third type of synthesis involves the cyclization of o-acylamino (N-substituted) benzamides. Some other more exotic synthetic approaches have been reported in literature, and many more should be possible.

Pharmacological Effects

Sought-after effects

• Relief of tension, mental stress, anxiety
• Relief of side-effects of over-stimulation or withdrawal of other drugs

Short-term and Long-term Effects

Similar to other CNS depressants and include reduction of mental activity, cardiac and respiratory depression as well as the development of tolerance, psychological and physical dependence

Note: Of specific concern regarding illicitly manufactured methaqualone is the fact that laboratory analysis has revealed that the majority of the dosage units on the South African market contains significant amounts of the precursor chemical o-toluidine. o-Toluidine is reasonably anticipated to be a human carcinogen: Ninth Report on Carcinogens (PB2000-107509, 2000) p III-207.

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Reference

Van Zyl, E.F. The synthesis and analysis of methaqualone and some positional and structural isomers thereof. M.Sc (Chemistry) Thesis 2001.

Terminology and Information on Drugs, Revised Edition, United Nations Office for Drug Control and Crime Prevention, New York, 1999.

Merck Index, 13th Edition, Merck & Co., Inc., Whitehouse Station NJ, 2001.

AMPHETAMINE-TYPE STIMULANTS (ATS)

This group of drugs can be divided into two subgroups namely the predominantly CNS-stimulants and the Hallucinogenic-ATS. During 2002 the SAPS Forensic Science Laboratory received more than 1600 ATS-related cases that amounted to more than 500 000 dosage units submitted. Several illicit ATS production facilities were also raided during 2002, with a specific increase in the illicit manufacturing of methcathinone being observed. All ATS listed below are controlled in South Africa and are listed as Undesirable Dependence Producing Substances in Part III of Schedule 2 of the Drugs and Drug Trafficking Act, Act 140/92

CNS-stimulants

The primary examples in this group include -

• amphetamine (Street names include Bennies, Dexies, Benzedrine)
• methamphetamine (Street names include Ice, Meth, Crystal)
• methcathinone (Usual street name is "CAT")

Pharmacological Effects of CNS-stimulating ATS

Sought-after effects

• Feelings physical and mental well being, exhilaration, euphoria
• Increased alertness and energy
• Postponement of hunger and fatigue
• Improved performance at manual and intellectual tasks

Short-term effects

• Loss of appetite
• Faster breathing, increased heart rate and blood pressure
• Dilation of pupils
• Bizarre, erratic, sometimes violent behaviour
• With larger doses: hallucinations, talkativeness, sense of power/superiority, restlessness, hyperexcitability, irritability which can lead to panic and paranoid psychosis
• Excessive doses may lead to convulsions, seizures, and death from respiratory failure, stroke, cerebral haemorrhage or heart failure

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Long-term effects

• Destruction of tissues in nose if sniffed
• Respiratory problems if smoked
• Infectious diseases, abscesses if injected
• Malnutrition, weight loss
• Disorientation, apathy, confusion, exhaustion due to lack of sleep
• Tolerance
• Psychological dependance
• Possible paranoid psychosis
• Excessive sleeping and depression after stopping

Hallucinogenic-ATS

Primary examples in this group include -

• 3,4-Methylenedioxymethamphetamine [MDMA] (Street names include Ecstasy, XTC, E, Adam as well as various of the names as catalogued in the 2003 Logo Index.)
• 3,4-Methylenedioxyamphetamine [MDA] (Street names include Ecstasy, XTC, E, as well as various of the names as catalogued in the 2003 Logo Index.)
• 3,4-Methylenedioxyethylamphetamine [MDEA] (Street names include Ecstasy, XTC, E, Adam as well as various of the names as catalogued in the 2003 Logo Index.)

Pharmacological Effects of Hallucinogenic-ATS

Sought-after effects

• Feelings of emotional closeness to other (empathy), facilitation of communication and increased sociability (used at so-called "rave" parties)
• Increased physical and emotional energy

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Short-term effects

• Fatigue and perhaps depression after the drug is stopped
• Restlessness, anxiety and pronounced visual and auditory hallucinations at larger doses
• Nausea and vomiting
• A rise in blood pressure and heart rate, death from heatstroke

Long-term effects

• Potential neurotoxicity and brain damage as well as liver damage

Note: The use of the precursor chemical safrole as a precursor in the manufacturing of hallucinogenic-ATS is of particular concern as this substance is reasonably anticipated to be a human carcinogen: Ninth Report on Carcinogens (PB2000-107509, 2000) p III-196.

Reference

Terminology and Information on Drugs, Revised Edition, United Nations Office for Drug Control and Crime Prevention, New York, 1999.

Merck Index, 13th Edition, Merck & Co., Inc., Whitehouse Station NJ, 2001.

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D-LYSERGIC ACID DIETHYLAMIDE (LSD)

LSD is a semi-synthetic drug derived from lysergic acid, an alkaloid found in Claviceps purpurea, a fungus which grows on rye and other grains. Also known as Lysergide or LSD-25, it is a colourless, tasteless, odourless, crystalline substance which is soluble in water or alcohol. Common illicit forms include -

• Impregnated on paper (blotter papers)
• Mini tablets (“microdots”) and capsules
• Gelatine sheets

LSD is also known under the street name “Acid”. LSD is listed in Part III of Schedule 2 of The South African Drugs and Drug Trafficking Act, Act 140/92 as an Undesirable Dependence Producing Substance even though from a pharmacological point-of-view it is not considered dependence producing.

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