Names

Class/Schedule

Description/Primary Uses

ALFENTANIL

CD: POM
Classs A, Sch.2

Mainly used in surgery

Rapifen

Notes: Powerful analogue of fentanyl; strong respiratory suppression.
Not known as a street drug.

Names

Class/Schedule

Description/Primary Uses

BUPRENORPHINE

CD: POM
Class C, Sch.3

Moderate to severe pain

Treatment for heroin dependency

Temgesic, Subutex
temmies, subbies, bupe

 Notes:

Buprenorphine is a partial opiate agonist; it is a potent pain-killer. It binds powerfully to specific opiate receptors, but only partially activates these receptors hence the “partial agonist” name. This characteristic means that doses of buprenorphine can be given to fill opiate receptors, blocking other opiates (such as heroin) from working at them but with less risk of an opiate overdose.

The net result for the user is that, if buprenorphine is taken correctly at a sufficiently high dose, other opiates used “on top” won’t work, and so such use on top should be reduced. In practice, “use on top” may take the form of drinking or use of benzos, neither of which is blocked by burprenorphine.

Buprenorphine will compete with other opiates, such as heroin and methadone, and if these compounds are present at receptor sites, buprenorphine is likely to displace them. This can mean that a user with heroin in their system may experience withdrawal effects when they take buprenorphine as the full agonist (heroin, methadone) is displaced by the partial agonist.

However, if someone who has no opiates in their system takes buprenorphine, they can and do get a significant level of opiate reward – less intense than heroin, but sufficient to warrant buprenorphine having a street value as a drug of misuse.

Buprenorphine causes less respiratory suppression than heroin or methadone and so the risk of overdose is lower. However people can and do overdose on buprenorphine. Naloxone is not wholly effective at reversing buprenorphine overdoses. Overdose is more likely where burprenorphine has been snorted or injected.

Buprenorphine is still an opiate with attendant issues of addiction and withdrawal. It is also constipating. Some users find that it provides a better level of clarity of thought than methadone; while some people find this aspect beneficial, others don’t like the new clear-headedness that buprenorphine provides.

Buprenorphine is generally prescribed and dispensed for sublingual administration. It is powerfully broken down by the liver so swallowing buprenorphine is highly ineffective. However, even when taken sublingually, it is likely that bioavailability is only around 33%.

This level of availability goes up if the drug is crushed and snorted, and goes up higher still if injected. This has seen a huge increase in the administration of buprenorphine by these routes.

Buprenorphine tablets, under the brand-name Temgesic were widely used as an illicit drug, especially in Scotland. They were typically crushed and injected. At this time it was primarily marketed as a low dose tablet for pain relief.

However, it was when it was reformulated and rebranded as Subutex that interest in the drug really took off. It has been used extensively in France since 1996, and became a lynchpin of the US prescribing system, being the only opiate-substitute that can be dispensed away from specialist clinics.

Buprenorphine started to gain acceptance in the UK as a treatment from around 1999, and has become an increasingly popular alternative to methadone.

In some parts of the UK, cost of branded Subutex has meant it was less widely available than its cheaper rival, Methadone. However, with the patent for Subutex now over, there is scope for cheaper generics to hit the market.

In an effort to discourage diversion and non-intended use, Schering Plough is marketing “Suboxone,” its new, licensed product. See separate entry on Suboxone.

Names

Class/Schedule

Description/Primary Uses

CO-CODAMOL

OTC – low dose
POM – higher dose

Mixture of codeine phosphate and paracetamol.
Treatment of mild to moderate pain

Paracodol, Solpadol

Notes:

Available in a variety of strengths, ranging from 8:500 (8mg codeine to 500mg paracetamol) through to 30:500. Small quantities of 8:500mg formulations are available as an OTC but high strength formulations require a prescription.

Tolerance and dependency on codeine can develop with constant use, and there is a risk that people will escalate their dose. Codeine can also cause severe constipation.

The key risk of abuse of co-codamol is liver damage stemming from the high intake of paracetamol, and so people taking excessive quantities of co-codamol expose themselves to risk of liver damage.

Some preparations contain methionine which may prevent paracetamol-induced liver toxcicity.

Names

Class/Schedule

Description/Primary Uses

CO-DYDRAMOL

OTC  - low dose

POM – higher dose

Mixture of dihydrocodeine and paracetamol

Mild to moderate pain

Paramol

Comments: A compound analagesic combining the opiate pain killer dihydrocodeine tartrate with the analgesic paracetamol. Available in a range of strengths; the weakest is mixed at a strength of 7.46mg dihydrocodeine to 500mg paracetamol. In this form it is available as an OTC medicine sold as Paramol. Stronger versions, mixed at 10, 20 and 30mg dihydrocodeine to 500mg paracetamol are POMs.

As with cocodamol, excessive doses of co-dydramol bring with it significant risk of liver damage through paracetamol toxcicity.

Names

Class/Schedule

Description/Primary Uses

CO-PHENOTROPE

OTC – low dose
POM – higher dose

Diarrhoea treatment:

Mixture of diphenoxylate hydrochloride and atropine

Lomototil; Dymotil

Notes: The opiate part, which is structurally similar to pethidine and slows down gut movement. It has the potential for dependency and misuse. To reduce these risks, it is sold in combination with atropine which in higher doses can cause severe negative side-effects such as irregular heart beat, double vision, nausea and agitation.

Names

Class/Schedule

Description/Primary Uses

CO-PROXAMOL

POM

Mixture of detropropoxyphene hydrochloride and paracetamol
Mild to moderate pain

Distalgesics

Notes: The opioid analagesic dextropropoxyphene is a relatively weak painkiller but can be dangerous in overdose, and can cause mood-swings and arrythmias, and is especially dangerous in combination with alcohol.

Due to  these risks, and  its relatively low therapeutic index some argue that it is no more effective than the paracetamol with which it is combined its legal status in the Uk was reviewed in 2004. It was decided to stage a staggered withdrawal of the drug with a view to it being removed from the market. At the time of writing it is still available but on a limited basis, typically on a ‘named patient basis.’.

Names

Class/Schedule

Description/Primary Uses

CODEINE PHOSPHATE

CD; 

Class A; Sch 2 in injectable form

Class B: Sch 5 in non injectable form

Pain relief – used alone or in compounds with other analgesics
Cough relief

Found in: Feminax, Solpadeine, Panadol Ultra as a compound analgesic

Notes: effective in the treatment of mild to moderate pain relief but causes significant constipation. Has the potential to cause dependency and is subject to non-medical use.

Names

Class/Schedule

Description/Primary Uses

DEXTROMORPHAN HYDROBROMIDE

OTCs

Used in many cough-relief preparations.

In: Actifed, benylin:

Notes: Dextromethorphan is used in many cough medicines for its anti-tussive effects. It is derived from an opioid leverpharnol, but doesn’t exhibit opiate type effects such as euphoria or sedation. Indeed it may inhibit the action of other opiates.

However, in high doses, Dextromethorphan can cause dissassociative hallucinations and when misused in this way has similar effects to Ketamine.

Misuse in this way has been uncommon in the UK, but has been a significant cause of concern in the USA, where access to compounds containing dextromorphan has been restricted to reduce abuse.

Names

Class/Schedule

Description/Primary Uses

DIAMORPHINE HYDROCHLORIDE

CD: Class A, Sch.2

Pharmaceutically pure heroin hydrochloride:

Severe pain relief; treatment of dependency

Diagesil, Diaphine

Notes: Pharmaceutical grade heroin, produced from morphine through reaction with acetic anhydride.
In the sixties this drug was prescribed quite widely to opiate dependent people, but following review of drug laws and prescribing practice, prescribing for addiction is now much less common.
Contrary to media confusion on the subject, it has always been lawful to “prescribe heroin on the NHS.” It is most commonly used for severe pain relief in hospital settings. However, GPs can undertake additional training and seek a Home Office licence to prescribe diamorphine for the treatment of addiction.

It is prescribed in injectable form, either pre-dissolved (‘wet amps’) or for dissolving in sterile water (‘dry amps.’) Currently, prescribing takes place across the UK to a number of individuals. A small number of clinical trials have been established to assess how effective this model of treatment is and early reports (November 1997) are encouraging.

However, due to its relatively short period of effect, risks of diversion, and the need to continue injecting, it remains the least widely used opiate substitute treatment.

Names

Class/Schedule

Description/Primary Uses

DEXTROMORAMIDE

CD: Class A , Sch.2
(discontinued in UK 2003)

For severe and intractable pain-relief:

Palfium Peach Palfs

Notes: Dextromoramide is a powerful pain killer with a high potential for overdose and misuse. It is the subject of control internationally. It is no longer prescribed in the UK though this was because of difficulty sourcing the precursors and the drug reliably rather than due to misuse.

Historically, 5mg and 10mg Palfium (Peach Palfs) were a highly-sought opiate, often injected.

Names

Class/Schedule

Description/Primary Uses

DEXTROPROPOXYPHENE HYDROCHLORIDE

POM

Mild to moderate pain relief

Constituent of: co-proxamol, costalgesic, distalgesic, dolxene

Notes: The opioid analagesic dextropropoxyphene is a relatively weak painkiller but can be dangerous in overdose, and can cause mood-swings and arrythmias, and is especially dangerous in combination with alcohol. See entry on Co-proxamol

Names

Class/Schedule

Description/Primary Uses

DIHYDROCODEINE TARTRATE

CD: Class B, Sch.2/5
Depends on formulation

Class A in injectable form

Moderate to severe pain relief

DF118, DFs
DHC Continue

Notes:  Dihydrocodeine is a relatively popular opiate in the UK; it is not as potent as morphine or heroin, but can provide good pain relief. It has often been considered a reasonably good “standby” for opiate users self-medicating through withdrawal or as a street drug if stronger opiates weren’t available.
It is available as an OTC as co-drydamol. Stronger preparations are a Schedule 2 drug, and in injectable form it is a Class A, Schedule 2 drug.
Internationally, especially on mainland Europe, tablets containing dihydrocodeine are available as a wax-bound sustained-release tablet. These are currently not common in the UK. Attempts to inject such wax-based tablets are likely to result in severe injecting complications.

Names

Class/Schedule

Description/Primary Uses

DIPIPANONE

CD: Class A, Sch.2

Moderate to severe pain relief

Diconal – dipipanone and Cyclizine
Dikes, Pinks, Strawberry Milkshake

Notes: Structurally similar to methadone, dipinanone is a powerful opiate. It tends to cause a high level of nausea so it was combined in tablet form with the anti-emetic (anti-nausea) drug cyclizine. The snag was that the two drugs, crushed and injected, provided a powerful and intense rush, leading to the drug being highly popular on the illicit market.

To add to the problems, diconal was formulated with tiny silicon particles that would block veins leading to tissue loss, and amputations. A significant number of older injectors lost digits or limbs through the injection of diconal.

Although still licensed in the UK, diconal rarely appears as a street drug now.

Names

Class/Schedule

Description/Primary Uses

FENTANYL

CD: Class A, Sch.2

Severe pain;

Breakthrough-pain in opiate dependent patients;

anaesthesia

Durogesic

Notes: Fentanyl is a powerful opiate analgesic, some 80 times more potent that morphine. It’s main use is on hospital settings for severe and chronic pain. It is also used in anaesthesia.
There are a number of analogues of Fentanyl, including:
Alfentanil (short acting 5-10 mins), Sufentanil (10x potency of Fentanyl), Remifentanil (shortest acting) and Carfentanil (10,000x potency of methadone: can quite literally put down an elephant and indeed is used to do so).
Fentanyl crops up as a significant street drug in the States, where it is diverted from medical supplies or , less commonly manufactured in underground labs.
Fentanyl comes in Transdermal patches, and also in lollipops or lozenges for oral consumption. It may be extracted from patches and injected, or sold in powder form for snorting or injection.
Reports suggest that Fentanyl offers a less euphoric high but is a more potent respiratory suppressant and so is a key risk in overdose. It is comparatively short acting, leading to more frequent use. Tolerance to heroin does not equate to tolerance to fentanyl and this, combined with the increased potency of fentanyl, means that even opiate-dependent users are at risk of fentanyl overdoses.
At present, use in the UK is not widespread, and the extraction of fentanyl from patches can be a  messy and wasteful process. However, there is every chance that misuse of Fentanyl will increase in the UK, and bring with it an increase in overdoses.

Names