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These drugs are known in the UK as controlled drug, because this is the term by which the act itself refers to them. In more general terms, however, many of these drugs are also controlled by the Medicines Act 1968, there are many other drugs which are controlled by the Medicines Act but not by the Misuse of Drugs Act, and some other drugs (alcohol, for example) are controlled by other laws.
The Misuse of Drugs Act sets out three separate categories, Class A, Class B, and Class C. Class A drugs represent those deemed most dangerous and so carry the harshest punishments. Class C represents those thought to have the least capacity for harm, and so the Act demands more lenient punishment. In reality the potential harm has little bearing on the class,[1] which has led to dissatisfaction with drug laws.[2]
Being found in possession of a drug on this list is dealt with less seriously than would be if it were deemed that there is intent to supply (even without payment) the drug to others. Possession with intent to supply carries a maximum penalty of life imprisonment.
With regard to lawful possession and supply, a different set of categories apply which are set out in the Misuse of Drugs Regulations 2001 (as amended). This sets out five schedules each with their own restrictions. Schedule 1 contains substances considered by the government to have no medicinal value, such as hallucinogens, and their use is limited primarily to research, whereas schedules 2–5 contain the other regulated drugs. This means that although drugs may fall into the category of Class A/B/C, they may also fall into one of the schedules for legitimate medicinal use. For example, morphine is a Class A drug under the Misuse of Drugs Act 1971, but when lawfully supplied falls under the category of a Schedule 2 controlled drug.
Substances may be removed and added to different parts of the schedule by statutory instrument, provided a report of the Advisory Council on the Misuse of Drugs has been commissioned and has reached a conclusion, although the Secretary of State is not bound by the council's findings. This list has in practice been modified a great number of times, sometimes removing substances, but more commonly adding some; for example, many benzodiazepines became Class C drugs in 1985, and many cathinones became Class B drugs in 2010.
Strongest known opioid; 10,000 times more potent than morphine, 100 times more potent than fentanyl. Used as a tranquilliser for large game (elephants etc.).
Commonly used in the production of Pethidine, although it has little opioid activity in its own right
N.B. Sub-paragraphs (b) and (c) were added in 1977, sub-paragraphs (d) and (e) were added in 1986. Sub-paragraph (ba) was subsequently added in 2001.[10]
(b) any compound (not being a compound for the time being specified in sub-paragraph (a) above) structurally derived from tryptamine or from a ring-hydroxy tryptamine by modification in any of the following ways, that is to say—[11]
(i) by substitution at the nitrogen atom of the sidechain to any extent with alkyl or alkenyl substituents, or by inclusion of the nitrogen atom of the side chain (and no other atoms of the side chain) in a cyclic structure;
(ii) by substitution at the carbon atom adjacent to the nitrogen atom of the side chain with alkyl or alkenyl substituents;
(iii) by substitution in the 6-membered ring to any extent with alkyl, alkoxy, haloalkyl, thioalkyl, alkylenedioxy, or halide substituents;
(iv) by substitution at the 2-position of the tryptamine ring system with an alkyl substituent;
(d) any compound (not being a compound for the time being specified in sub-paragraph (a) above) structurally derived from fentanyl by modification in any of the following ways, that is to say,
(i) by replacement of the phenyl portion of the phenethyl group by any heteromonocycle whether or not further substituted in the heterocycle;
(ii) by substitution in the phenethyl group with alkyl, alkenyl, alkoxy, hydroxy, halogeno, haloalkyl, amino or nitro groups;
(iii) by substitution in the piperidine ring with alkyl or alkenyl groups;
(iv) by substitution in the aniline ring with alkyl, alkoxy, alkylenedioxy, halogeno or haloalkyl groups;
(v) by substitution at the 4-position of the piperidine ring with any alkoxycarbonyl or alkoxyalkyl or acyloxy group;
(vi) by replacement of the N-propionyl group by another acyl group;
(e) any compound (not being a compound for the time being specified in sub-paragraph (a) above) structurally derived from pethidine by modification in any of the following ways, that is to say,
(i) by replacement of the 1-methyl group by an acyl, alkyl whether or not unsaturated, benzyl or phenethyl group, whether or not further substituted;
(ii) by substitution in the piperidine ring with alkyl or alkenyl groups or with a propano bridge, whether or not further substituted;
(iii) by substitution in the 4-phenyl ring with alkyl, alkoxy, aryloxy, halogeno or haloalkyl groups;
(iv) by replacement of the 4-ethoxycarbonyl by any other alkoxycarbonyl or any alkoxyalkyl or acyloxy group;
(v) by formation of an N-oxide or of a quaternary base.
(f) any compound (not being benzyl(α-methyl-3,4-methylenedioxyphenethyl)amine) structurally derived from mescaline, 4-bromo-2,5-dimethoxy-α-methylphenethylamine, 2,5-dimethoxy-α,4-dimethylphenethylamine, N-hydroxytenamphetamine (N-hydroxy-MDA), or a compound specified in sub-paragraph (ba) or (c) above, by substitution at the nitrogen atom of the amino group with a benzyl substituent, whether or not substituted in the phenyl ring of the benzyl group to any extent.”.
3. Any ester or ether of a substance for the time being specified in paragraph 1 or 2 above [not being a substance for the time being specified in Part II of this Schedule].
4. Any salt of a substance for the time being specified in any of paragraphs 1 to 3 above.
5. Any preparation or other product containing a substance or product for the time being specified in any of paragraphs 1 to 4 above.
6. Any preparation designed for administration by injection which includes a substance or product for the time being specified in any of paragraphs 1 to 3 of Part II of this Schedule.
legal without prescription in quantities of up to 12.8mg per dosage unit or 15mg/5ml in oral solution and only in combination with other drug. UK Codeine law
downgraded from class A to class C in 2004[14] and upgraded to class B in 2009[15] (Legalised for medicinal use in July 2018, and law excludes cannabidiol entirely)
Used by Doctors on Air Ambulance duties to provide pain relief for serious or life-threatening injuries in extreme circumstances, when casualty sedation is required prior to a potential RSI.
(aa)[20] Any compound (not being bupropion, cathinone, diethylpropion, pyrovalerone or a compound for the time being specified in sub–paragraph (a) above) structurally derived from 2–amino–1–phenyl–1–propanone by modification in any of the following ways, that is to say,
(i) by substitution in the phenyl ring to any extent with alkyl, alkoxy, alkylenedioxy, haloalkyl or halide substituents, whether or not further substituted in the phenyl ring by one or more other univalent substituents;
(ii) by substitution at the 3–position with an alkyl substituent;
(iii) by substitution at the nitrogen atom with alkyl or dialkyl groups, or by inclusion of the nitrogen atom in a cyclic structure
(ab)[21] Any compound structurally derived from 2–aminopropan–1–one by substitution at the 1-position with any monocyclic, or fused‑polycyclic ring system (not being a phenyl ring or alkylenedioxyphenyl ring system), whether or not the compound is further modified in any of the following ways, that is to say,
(i) by substitution in the ring system to any extent with alkyl, alkoxy, haloalkyl or halide substituents, whether or not further substituted in the ring system by one or more other univalent substituents;
(ii) by substitution at the 3–position with an alkyl substituent;
(iii) by substitution at the 2‑amino nitrogen atom with alkyl or dialkyl groups, or by inclusion of the 2‑amino nitrogen atom in a cyclic structure
Any compound structurally derived from 3–(1–naphthoyl)indole or 1H–indol–3–yl–(1–naphthyl)methane by substitution at the nitrogen atom of the indole ring by alkyl, alkenyl, cycloalkylmethyl, cycloalkylethyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indole ring to any extent and whether or not substituted in the naphthyl ring to any extent.
Any compound structurally derived from 3–(1–naphthoyl)pyrrole by substitution at the nitrogen atom of the pyrrole ring by alkyl, alkenyl, cycloalkylmethyl, cycloalkylethyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the pyrrole ring to any extent and whether or not substituted in the naphthyl ring to any extent.
Any compound structurally derived from 1–(1–naphthylmethyl)indene by substitution at the 3–position of the indene ring by alkyl, alkenyl, cycloalkylmethyl, cycloalkylethyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indene ring to any extent and whether or not substituted in the naphthyl ring to any extent.
Any compound structurally derived from 3–phenylacetylindole by substitution at the nitrogen atom of the indole ring with alkyl, alkenyl, cycloalkylmethyl, cycloalkylethyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indole ring to any extent and whether or not substituted in the phenyl ring to any extent.
Any compound structurally derived from 2–(3–hydroxycyclohexyl)phenol by substitution at the 5–position of the phenolic ring by alkyl, alkenyl, cycloalkylmethyl, cycloalkylethyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the cyclohexyl ring to any extent.";
Any compound structurally derived from 3-benzoylindole by substitution at the nitrogen atom of the indole ring by alkyl, haloalkyl, alkenyl, cyanoalkyl, hydroxyalkyl, cycloalkylmethyl, cycloalkylethyl, (N-methylpiperidin-2-yl)methyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indole ring to any extent and whether or not substituted in the phenyl ring to any extent.
Any compound structurally derived from 3-(1-adamantoyl)indole or 3-(2-adamantoyl)indole by substitution at the nitrogen atom of the indole ring by alkyl, haloalkyl, alkenyl, cyanoalkyl, hydroxyalkyl, cycloalkylmethyl, cycloalkylethyl, (N-methylpiperidin-2-yl)methyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indole ring to any extent and whether or not substituted in the adamantyl ring to any extent.
Any compound structurally derived from 3-(2,2,3,3-tetramethylcyclopropylcarbonyl)indole by substitution at the nitrogen atom of the indole ring by alkyl, haloalkyl, alkenyl, cyanoalkyl, hydroxyalkyl, cycloalkylmethyl, cycloalkylethyl, (N-methylpiperidin-2-yl)methyl or 2–(4–morpholinyl)ethyl, whether or not further substituted in the indole ring to any extent.
(ca)[23] any compound (not being clonitazene, etonitazene, acemetacin, atorvastatin, bazedoxifene, indometacin, losartan, olmesartan, proglumetacin, telmisartan, viminol, zafirlukast or a compound for the time being specified in sub-paragraph (c) above) structurally related to 1-pentyl-3-(1-naphthoyl)indole (JWH-018), in that the four sub-structures, that is to say the indole ring, the pentyl substituent, the methanone linking group and the naphthyl ring, are linked together in a similar manner, whether or not any of the sub-structures have been modified, and whether or not substituted in any of the linked sub-structures with one or more univalent substituents and, where any of the sub-structures have been modified, the modifications of the sub-structures are limited to any of the following, that is to say—
(i) replacement of the indole ring with indane, indene, indazole, pyrrole, pyrazole, imidazole, benzimidazole, pyrrolo[2,3-b]pyridine, pyrrolo[3,2-c]pyridine or pyrazolo[3,4‑b]pyridine;
(ii) replacement of the pentyl substituent with alkyl, alkenyl, benzyl, cycloalkylmethyl, cycloalkylethyl, (N-methylpiperidin-2-yl)methyl, 2-(4-morpholinyl)ethyl or (tetrahydropyran-4-yl)methyl;
(iii) replacement of the methanone linking group with an ethanone, carboxamide, carboxylate, methylene bridge or methine group;
(iv) replacement of the 1-naphthyl ring with 2-naphthyl, phenyl, benzyl, adamantyl, cycloalkyl, cycloalkylmethyl, cycloalkylethyl, bicyclo[2.2.1]heptanyl, 1,2,3,4-tetrahydronaphthyl, quinolinyl, isoquinolinyl, 1-amino-1-oxopropan-2-yl, 1‑hydroxy-1-oxopropan-2-yl, piperidinyl, morpholinyl, pyrrolidinyl, tetrahydropyranyl or piperazinyl.
(d)[22] 1-Phenylcyclohexylamine or any compound (not being ketamine, tiletamine or a compound for the time being specified in paragraph 1(a) of Part 1 of this Schedule) structurally derived from 1-phenylcyclohexylamine or 2-amino-2-phenylcyclohexanone by modification in any of the following ways, that is to say,
(i) by substitution at the nitrogen atom to any extent by alkyl, alkenyl or hydroxyalkyl groups, or replacement of the amino group with a 1-piperidyl, 1-pyrrolidyl or 1-azepyl group, whether or not the nitrogen containing ring is further substituted by one or more alkyl groups;
(ii) by substitution in the phenyl ring to any extent by amino, alkyl, hydroxy, alkoxy or halide substituents, whether or not further substituted in the phenyl ring to any extent;
(iii) by substitution in the cyclohexyl or cyclohexanone ring by one or more alkyl substituents;
(iv) by replacement of the phenyl ring with a thienyl ring.
(e) Any compound (not being a compound for the time being specified in paragraph 1(ba) of Part 1 of this Schedule) structurally derived from 1-benzofuran, 2,3-dihydro-1-benzofuran, 1H-indole, indoline, 1H-indene, or indane by substitution in the 6-membered ring with a 2-ethylamino substituent whether or not further substituted in the ring system to any extent with alkyl, alkoxy, halide or haloalkyl substituents and whether or not substituted in the ethylamino side-chain with one or more alkyl substituents.
2. Any stereoisomeric form of a substance for the time being specified in paragraph 1 of this Part of this Schedule.
3. Any salt of a substance for the time being specified in paragraph 1 or 2 of this Part of this Schedule.
4. Any preparation or other product containing a substance or product for the time being specified in any of paragraphs 1 to 3 of this Part of this Schedule, not being a preparation falling within paragraph 6 of Part I of this Schedule.
Class C drugs
1. Class C drugs, supposedly the least harmful drugs, include the following substances:—[3][non-primary source needed]
(c) any compound (not being Trilostane or a compound for the time being specified in sub-paragraph (b) above) structurally derived from 17-hydroxyandrostan-3-one or from 17-hydroxyestran-3-one by modification in any of the following ways, that is to say, (i) by further substitution at position 17 by a methyl or ethyl group; (ii) by substitution to any extent at one or more of positions 1, 2, 4, 6, 7, 9, 11 or 16, but at no other position; (iii) by unsaturation in the carbocyclic ring system to any extent, provided that there are no more than two ethylenic bonds in any one carbocyclic ring; (iv) by fusion of ring A with a heterocyclic system;
(d) any substance which is an ester or ether (or, where more than one hydroxyl function is available, both an ester and an ether) of a substance specified in sub-paragraph (b) or described in sub-paragraph (c) above;
(f) 1–benzylpiperazine or any compound (not being 1–(3–chlorophenyl)piperazine or 1–(3–chlorophenyl)–4–(3–chloropropyl)piperazine) structurally derived from 1–benzylpiperazine or 1–phenylpiperazine by modification in any of the following ways
(i) by substitution at the second nitrogen atom of the piperazine ring with alkyl, benzyl, haloalkyl or phenyl groups;
(ii) by substitution in the aromatic ring to any extent with alkyl, alkoxy, alkylenedioxy, halide or haloalkyl groups;
2. Any stereoisomeric form of a substance for the time being specified in paragraph 1 of this Part of this Schedule [not being phenylpropanolamine.]
3. Any salt of a substance for the time being specified in paragraph 1 or 2 of this Part of this Schedule.
4. Any preparation or other product containing a substance for the time being specified in any of paragraphs 1 to 3 of this Part of this Schedule.
Derivatives and analogues
The act contains several references to "derivatives" of compounds but the extent of this term is not fully clarified. Where unspecified it is thought to indicate derivatives which can be made from the specified compound in a single synthetic step, although such a definition would indicate that alkyllysergamide analogues would be uncontrolled. Where the derivatives are specified to be "structural derivatives" there is precedent that the statute applies whenever the structure could be converted to the specified derivatives in any number of synthetic steps.[29]
Aromatic compounds or arenes usually refers to organic compounds "with a chemistry typified by benzene" and "cyclically conjugated." The word "aromatic" originates from the past grouping of molecules based on odor, before their general chemical properties were understood. The current definition of aromatic compounds does not have any relation to their odor. Aromatic compounds are now defined as cyclic compounds satisfying Hückel's Rule. Aromatic compounds have the following general properties:
In chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia, wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group. Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine.
In organic chemistry, an alkyl group is an alkane missing one hydrogen. The term alkyl is intentionally unspecific to include many possible substitutions. An acyclic alkyl has the general formula of −CnH2n+1. A cycloalkyl group is derived from a cycloalkane by removal of a hydrogen atom from a ring and has the general formula −CnH2n−1. Typically an alkyl is a part of a larger molecule. In structural formulae, the symbol R is used to designate a generic (unspecified) alkyl group. The smallest alkyl group is methyl, with the formula −CH3.
In organic chemistry, an aryl is any functional group or substituent derived from an aromatic ring, usually an aromatic hydrocarbon, such as phenyl and naphthyl. "Aryl" is used for the sake of abbreviation or generalization, and "Ar" is used as a placeholder for the aryl group in chemical structure diagrams, analogous to “R” used for any organic substituent. “Ar” is not to be confused with the elemental symbol for argon.
In organic chemistry, a substituent is one or a group of atoms that replaces atoms, thereby becoming a moiety in the resultant (new) molecule.
A sigmatropic reaction in organic chemistry is a pericyclic reaction wherein the net result is one σ-bond is changed to another σ-bond in an uncatalyzed intramolecular reaction. The name sigmatropic is the result of a compounding of the long-established sigma designation from single carbon–carbon bonds and the Greek word tropos, meaning turn. In this type of rearrangement reaction, a substituent moves from one part of a π-bonded system to another part in an intramolecular reaction with simultaneous rearrangement of the π system. True sigmatropic reactions are usually uncatalyzed, although Lewis acid catalysis is possible. Sigmatropic reactions often have transition-metal catalysts that form intermediates in analogous reactions. The most well-known of the sigmatropic rearrangements are the [3,3] Cope rearrangement, Claisen rearrangement, Carroll rearrangement, and the Fischer indole synthesis.
The Misuse of Drugs Act 1977, the Misuse of Drugs Act 1984, Misuse of Drugs Act 2015 and the Criminal Justice Act 2010 are the acts of the Oireachtas regulating drugs in Ireland. The acts define the penalties for unlawful production, possession and supply of drugs.
The Controlled Drugs and Substances Act is Canada's federal drug control statute. Passed in 1996 under Prime Minister Jean Chrétien's government, it repeals the Narcotic Control Act and Parts III and IV of the Food and Drugs Act, and establishes eight Schedules of controlled substances and two Classes of precursors. It provides that "The Governor in Council may, by order, amend any of Schedules I to VIII by adding to them or deleting from them any item or portion of an item, where the Governor in Council deems the amendment to be necessary in the public interest."
A PDE3 inhibitor is a drug which inhibits the action of the phosphodiesterase enzyme PDE3. They are used for the therapy of acute heart failure and cardiogenic shock.
Substituted amphetamines are a class of compounds based upon the amphetamine structure; it includes all derivative compounds which are formed by replacing, or substituting, one or more hydrogen atoms in the amphetamine core structure with substituents. The compounds in this class span a variety of pharmacological subclasses, including stimulants, empathogens, and hallucinogens, among others. Examples of substituted amphetamines are amphetamine (itself), methamphetamine, ephedrine, cathinone, phentermine, mephentermine, tranylcypromine, bupropion, methoxyphenamine, selegiline, amfepramone (diethylpropion), pyrovalerone, MDMA (ecstasy), and DOM (STP).
Substituted cathinones, which include some stimulants and entactogens, are derivatives of cathinone. They feature a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon, along with additional substitutions. Cathinone occurs naturally in the plant khat whose leaves are chewed as a recreational drug.
Cannabicyclohexanol is a cannabinoid receptor agonist drug, developed by Pfizer in 1979. On 19 January 2009, the University of Freiburg in Germany announced that an analog of CP 47,497 was the main active ingredient in the herbal incense product Spice, specifically the 1,1-dimethyloctyl homologue of CP 47,497, which is now known as cannabicyclohexanol. The 1,1-dimethyloctyl homologue of CP 47,497 is in fact several times more potent than the parent compound, which is somewhat unexpected as the 1,1-dimethylheptyl is the most potent substituent in classical cannabinoid compounds such as HU-210.
JWH-164 is a synthetic cannabinoid receptor agonist from the naphthoylindole family. It has approximately equal affinity for the CB1 and CB2 receptors, with a Ki of 6.6 nM at CB1 and 6.9 nM at CB2. JWH-164 is a positional isomer of the related compound JWH-081, but with a methoxy group at the 7-position of the naphthyl ring, rather than the 4-position as in JWH-081. Its potency is intermediate between that of JWH-081 and its ring unsubstituted derivative JWH-018, demonstrating that substitution of the naphthyl 7-position can also result in increased cannabinoid receptor binding affinity.
JWH-098 is a synthetic cannabinoid receptor agonist from the naphthoylindole family. It is the indole 2-methyl derivative of a closely related compound JWH-081, but has markedly different affinity for the CB1 and CB2 receptors. While JWH-081 is around tenfold selective for CB1 over CB2, in JWH-098 this is reversed, and it is around four times weaker than JWH-081 at CB1 while being six times more potent at CB2, giving it a slight selectivity for CB2 overall. This makes JWH-098 a good example of how methylation of the indole 2-position in the naphthoylindole series tends to increase CB2 affinity, but often at the expense of CB1 binding.
HU-243 (AM-4056) is a synthetic cannabinoid drug that is a single enantiomer of the hydrogenated derivative of the commonly used reference agonist HU-210. It is a methylene homologue of canbisol. It is a potent agonist at both the CB1 and CB2 receptors, with a binding affinity of 0.041 nM at the CB1 receptor, making it marginally more potent than HU-210, which had an affinity of 0.061 nM in the same assay.
A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a Ki of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group of A-834,735 and related compounds imparts significant selectivity for CB2, with most compounds from this group found to be highly selective CB2 agonists with little affinity for CB1. However, low nanomolar CB1 binding affinity is retained with certain heterocyclic 1-position substituents such as (N-methylpiperidin-2-yl)methyl (cf. AM-1220, AM-1248), or the (tetrahydropyran-4-yl)methyl substituent of A-834,735, resulting in compounds that still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
To combat the illicit synthetic cannabinoid industry many jurisdictions have created a system to control these cannabinoids through their general structure as opposed to their specific identity. In this way new analogs are already controlled before they are even created. A large number of cannabinoids have been grouped into classes based on similarities in their chemical structure, and these classes have been widely adopted across a variety of jurisdictions.
Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research.
References
This article incorporates text published under the British OpenGovernmentLicencev3.0: To maintain the accuracy of the article, some of the text is copied directly from the legislation.
↑ Nutt, David (1 April 2010). "Trashing evidence-based drugs policy". The Guardian. Retrieved 8 February 2012. We will give the public the kind of high-quality evidence on drug harms our current crop of politicians apparently do not feel they need before making far reaching decisions around drugs classification.
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