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Codeine

2015-08-05T01:54:48Z

Laika: Edited Harm Reduction section, added "interactions" subsection, added minor details

[[File:Codeine_structure.jpg|right]]
Codeine is an opiate used for its analgesic, antitussive, antidiarrheal, antihypertensive, anxiolytic,antidepressant, sedative and hypnotic properties. It is also used to suppress premature labor contractions, myocardial infarction, and has many other potential and indicated uses. It is often sold as a salt in the form of either codeine sulfate or codeine phosphate in the United States and Canada; codeine hydrochloride is more common worldwide and the citrate, hydroiodide, hydrobromide, tartrate, and other salts are also seen. It occurs naturally in the opium poppy and as such has a long history of human use.

== History ==

In 1832, codeine was isolated from opium, which has a codeine content of 2 to 30/0 (see Papaver somniferum). Codeine is also biosynthesized in the roots of Papaver somniferum 1. cv. Marianne (Tam et al. 1980). It is possible that trace amounts of codeine can also be found in other Papaver species (Papaver bracteatum, Papaver decaisnei; cf. Papaver spp.) (Theuns et al. 1986). Codeine is also an endogenous neurotransmitter in humans (cf. morphine). A dosage of 20 to 50 mg produces "general mental stimulation, warmth in the head, and an increase in the pulse rate, as also appear after the consumption of alcohol" (Rompp 1950*). Codeine does not appear to be metabolized in the body and is excreted unchanged. Because codeine suppresses the urge to cough, its most important pharmaceutical use is in cough syrups.

The dosage when codeine is used as a cough suppressant is 50 mg three times a day. A dosage of 100 to 200 mg results in sleep and sedation.
Higher dosages elicit effects comparable to those of morphine. The medical literature contains repeated mentions of "codeine addiction." Codeine "addicts" are said to ingest up to 2 g of codeine daily (Rompp 1950, 115*). Today, codeine is gaining increasing medicinal importance as a substitution therapy for heroin addicts (Gerlach and Schneider 1994). The pharmaceutical industry synthesizes codeine primarily from thebaine, the main active constituent in Papaver bracteatum Lindl. (cf. Papaver spp.) (Morton 1977, 125*; Theuns et al. 1986). Codeine has acquired a certain significance in the music scene (jazz, rock, psychedelia), primarily as a substitute for heroin or morphine. Buffy Saint-Marie sang about the anguish of her codeine dependence in the song "Cod'ine" (LP It's My Way! Vanguard Records 1964). Quicksilver Messenger Service later covered the song and made it famous. In the 1990s, the wave band Codeine had several albums out through Sub Pop. Cough syrups496 with a high codeine content were often consumed as inebriants at concerts, festivals, et cetera (usually in combination with alcohol and cannabis) (Bangs 1978, 158).

Since the 1990's codeine has gained popularity in the rap music scene where a mixture containing codeine promethazine cough syrup is consumed under the name [https://en.wikipedia.org/wiki/Purple_drank purple drank] and several artists have released songs about it. ([http://link.springer.com/article/10.1007%2Fs12103-013-9213-7 Hart, Agnich, Stogner, Miller 2013])

== Dosage ==

{| class="wikitable"
|+ Oral
|-
| Light || 50-100mg
|-
| Common || 100-150mg
|-
| Strong || 150-200mg
|-
| Ceiling || 400-600mg
|}

== Duration ==

{| class="wikitable"
|+ Oral
|-
| Onset || 30-45 minutes
|-
| Duration || 3-6 hours
|}

== Effects ==

=== Positive ===

* Euphoria

* Pain relief

* Elevated mood

* Overall feeling of contentedness

=== Neutral ===

* Itching

=== Negative ===

* Nausea

* Constipation

* CNS depression

* Drowsiness

* Hot/cold flashes

* Dizziness

* Vomiting

* Urinary retention (difficulty urinating)

== Harm Reduction ==

* People seeking Codeine experiences from medications that contain Acetaminophen (Paracetamol) may be putting themselves at risk for Acetaminophen-related complications such as liver damage. Generally do not consume more than 4g Acetaminophen per day. It is a good idea to conduct a [https://wiki.tripsit.me/wiki/Cold_Water_Extraction cold water extraction] with codeine that contains acetaminophen, which removes most of the acetaminophen. It is an easy and quick procedure. See our wiki for a quick tutorial.

* Avoid driving and operating heavy machinery

* Recommended time (pauses) between using the substance

* Addictive

=== Interactions ===

* Do not mix with alcohol, benzodiazepines, opioids, or other CNS depressants

* Avoid combining with stimulants

== Chemistry and Pharmacology ==

The conversion of codeine to morphine occurs in the liver and is catalysed by the cytochrome P450 enzyme CYP2D6. CYP3A4 produces norcodeine and UGT2B7 conjugates codeine, norcodeine, and morphine to the corresponding 3- and 6- glucuronides.

Some medications are CYP2D6 inhibitors and reduce or even completely block the conversion of codeine to morphine. The most well-known of these are two of the selective serotonin reuptake inhibitors, paroxetine(Paxil) and fluoxetine (Prozac) as well as the antihistamine diphenhydramine (Benadryl) and the antidepressant, bupropion (Wellbutrin, also known as Zyban). Other drugs, such as rifampicin and dexamethasone, induce CYP450 isozymes and thus increase the conversion rate.

The active metabolites of codeine, notably morphine, exert their effects by binding to and activating the μ-opioid receptor.

== Legal Status ==

Codeine is available as a pure substance and as codeine hydrochloride, codeine phosphate, and codeine phosphate hemihydrate. Codeine is on Schedule III in the United States. Preparations containing codeine (tinctures, cough syrups, et cetera) require a special prescription (i.e., with no refills allowed and/or on special prescription forms). But in other countries, including France, Spain, Nepal, and India, a prescription is still unnecessary and the medicine can be obtained over the counter from any pharmacy.

== Links ==

[http://en.wikipedia.org/wiki/Codeine Wikipedia]

[http://www.erowid.org/pharms/codeine/codeine.shtml Erowid]

[[Category:Drugs]]

[[Category:Opioid]]

[[Category:Depressant]]

Opioids

2015-05-13T19:57:07Z

Laika: /* History */

[[File:Papaver_somniferum.jpg|250px|right|Close-up color photo of a Papaver somniferum pod]]

Opiates and opioids are classes of depressant analgesics derived from or chemically similar to substances found in Papaver somniferum, the opium poppy. They include both naturally occurring and synthetic substances. The term opiate is often used interchangeably for opioid. Opiate is limited to the natural alkaloids found in the resin of the poppy. Opioid refers to both opiates and synthetic substances as well as opioid peptides. The analgesic effect of opioids are due to decreased perception of pain, decreased reaction to pain as well as increased pain tolerance. They can also be used as for their antitussive properties.

= Common opioids =

*[[Heroin]]

*[[Codeine]]

*[[Tramadol]]

*[[Hydrocodone]]

*[[Oxycodone]]

*[[Hydromorphone]]

*[[Oxymorphone]]

= History =

Opioids are among the world's oldest known drugs; the therapeutic use of the opium poppy predates recorded history. Excavations of the remains of neolithic settlements in Switzerland (the Cortaillod culture, 3200-2600 B.C.), have shown that Papaver was already being cultivated then; perhaps for the food value in the seeds (45% oil), which we know as poppy seeds. The slightly narcotic property of this plant was undoubtedly already known then.

[[Opium]] contains a considerable number of different substances, and in the nineteenth century these were isolated. In 1806 Friedrich Serturner was the first to extract one of these substances in its pure form. He called morphine after Morpheus, the Greek god of sleep. Codeine (Robiquet, 1832) and papaverine (Merck, 1848) followed. These pure substances supplanted the use of raw opium for medical purposes. Like opium they were frequently used as painkillers and as anti-diarrheal. The invention of the hypodermic needle in the mid-nineteenth century lead to widespread use of morphine intravenously as a painkiller and recreational drug.

= Effects =

All opiate drugs have similar effects. At low doses they relieve pain and anxiety, and if the dose is increased, they produce a sedative effect.The analgesic (painkiller) effects of opioids are due to decreased perception of pain, decreased reaction to pain as well as increased pain tolerance. Opioids can cause cough suppression, which can be both an indication for opioid administration or an unintended side effect.

Opiates influence the pupils: they contract (miosis). This is an extremely reliable signal of opiate use. Besides this, when suffocation occurs (as a result of respiratory inhibition) in the case of an overdose, the pupils dilate (mydriasis).

The most striking quality of painkilling effect of opiates is that it has virtually no effect whatever on the other sensory perceptions, consciousness or the motor functions. All other substances with a painkilling effect, such as laughing gas, alcohol, ether and barbiturates also have, in an effective dose, a definate effect on consciousness, motor coordination, the intellect and emotional control. The drowsiness which can be caused by opiates is experienced only at high dosage.

Opiates are affecting respiratory center. Both frequency and the depth of breathing is reduced. In the case of overdose, respiration can come to a complete halt resulting in death.

Dependence is characterised by unpleasant withdrawal symptoms that occur if opioid use is abruptly discontinued. The withdrawal symptoms for opiates include severe dysphoria, craving for another opiate dose, irritability, sweating, nausea, rhinorrea, tremor, vomiting and myalgia.

== Positive ==

*Euphoria

*Analgesic effect

*Pain relief

== Neutral ==

*Itching

== Negative ==

*Opioid-induced hyperalgesia (More sensitive to pain after stopping the use)

*Nausea

*Vomiting

*Constipation

*Respiratory depression

= Addiction =

Opiates also give us the classical model of addiction. Used regularly, they produce tolerance - a need to continue increasing the dose in order to get the same effect, and stopping after repeated use produces withdrawal symptoms that can reinforce the addiction - physical discomfort and a mental craving for the drug, driving the user to continue taking the drug despite negative consequences of behavior.

= Chemistry and Pharmacology =

An opioid is any psychoactive chemical that resembles an opiate in its pharmacological effects. They work by binding to the opioid receptors (Delta, Kappa, Mu) Which are found in the Central/Peripheral nervous system and in the GI tract.

= Harm Reduction =

Avoid driving on higher doses.

Opioid analgesics do not cause any specific organ toxicity, unlike many other drugs, such as aspirin and acetaminophen. They are not associated with upper gastrointestinal bleeding and renal toxicity, however people seeking codeine experiences from medications that contain acetaminophen (paracetamol) may be putting themselves at risk for acetaminophen-related complications such as liver damage. In the case of Acetaminophen and aspirin containing medications, [[Cold Water Extraction]] is useful to reduce the amount of non opioid analgesics ingested

If possible, having Naloxone available (especially when dealing with high doses) is a good idea. Naloxone is a pure opioid antagonist, which means it reverses the effects of opiate drugs and can reverse overdose symptoms.

Some users have noted that following the "3 day rule" prevents chemical dependency with some opioids, meaning that using no more than 3 days in a row. (this has no medical basis however, and should be taken as only a guideline at best)

When preparing IV solutions for injection of street drugs, a wheel filter (micron filter) is essential for reducing particulate matter in the solution, as well as using sterile needles, and clean distilled water. Never re-use injection equipment

== Interactions ==

Don't mix any of the class with any other CNS [[Depressants]] as it increases the risk of an overdose, and respiratory depression.

[[Tramadol]] and [[Meperidine]] are affecting serotonin levels in the brain, and might cause Serotonin Syndrome with some combinations. Check [[Drug Combinations]] for more information.

==Research Chemicals==

Respiratory depression is one of the very common side effects with this class, and puts users at a high risk of overdose. With research chemicals, this is a particular issue since there are some substances being openly sold for which a single microgram can be the difference between life and death. With the emerging research chemical market for opioids, most have been explored in-vivo (outside of a human) and also in-vitro (in human) - though there are some exceptions (e.g. W-18/Acryl-Fentanyl).

It's suggested to start at the lowest possible dose; in the case of W-18, animal testing has shown it to be around 10,000x the potency of Morphine. So the logical way to start is either to volumetrically dose, or use a precise scale with a +/- microgram amount. Titrating up to an active dose on this class might be the most difficult, due to the massively steep dosage curves.

See the [[Research Chemicals]] page for more information.

= Links =

[https://en.wikipedia.org/wiki/Opiod Wikipedia]

[https://www.erowid.org/chemicals/opiates/ Erowid]

[http://www.drugtext.org/sub/opiat1.html drugtext]

[[Category:Drug class]]