There’s a lot of buzz in Nigeria on codeine and tramadol no thanks to Olamide’s hit song #ScienceStudent
Codeine is an opiate used to treat pain, as a cough medicine, and for diarrhea. It is typically used to treat mild to moderate degrees of pain. Greater benefit may occur when combined with paracetamol (acetaminophen) or a nonsteroidal anti-inflammatory drug (NSAID) such as aspirin or ibuprofen. Evidence does not support its use for acute cough suppression in children or adults. In Europe it is not recommended as a cough medicine in those under twelve years of age. It is generally taken by mouth. It typically starts working after half an hour with maximum effect at two hours. The total duration of its effects last for about four to six hours.
Common side effects include vomiting, constipation, itchiness, lightheadedness, and drowsiness. Serious side effects may include breathing difficulties and addiction. It is unclear if its use in pregnancy is safe. Care should be used during breastfeeding as it may result in opiate toxicity in the baby. Its use as of 2016 is not recommended in children. Codeine works following being broken down by the liver into morphine. How quickly this occurs depends on a person’s genetics.
Codeine was discovered in 1832 by Pierre Jean Robiquet. In 2013 about 361,000 kilograms of codeine were produced while 249,000 kilograms were used. This makes it the most commonly taken opiate. It is on the World Health Organization’s List of Essential Medicines, the most effective and safe medicines needed in a health system. The wholesale cost in the developing world is between 0.04 and 0.29 USD per dose as of 2014. In the United States it costs about one dollar a dose. Codeine occurs naturally and makes up about 2% of opium.
Withdrawal and dependence
As with other opiate-based pain killers, chronic use of codeine can cause physical dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops the medication. Withdrawal symptoms include: drug craving, runny nose, yawning, sweating, insomnia, weakness, stomach cramps, nausea, vomiting, diarrhea, muscle spasms, chills, irritability, and pain. To minimize withdrawal symptoms, long-term users should gradually reduce their codeine medication under the supervision of a healthcare professional.
There is also no evidence that CYP2D6 inhibition is useful in treating codeine dependence, though the metabolism of codeine to morphine (and hence further metabolism to glucuronide morphine conjugates) does have an effect on the abuse potential of codeine. However, CYP2D6 has been implicated in the toxicity and death of neonates when codeine is administered to lactating mothers, particularly those with increased 2D6 activity (“ultra-rapid” metabolizers).
Codeine can be used as a recreational drug. A heroin (diamorphine) or other opiate/opioid addict may use codeine to ward off the effects of withdrawal during periods of time where their preferred drug is unavailable or unaffordable.
Codeine is also available in conjunction with the anti-nausea medication promethazine in the form of a syrup. Brand named as Phenergan with Codeine or in generic form as promethazine with codeine. In the 1990s it started to be used as a recreational drug and was called ‘syrup’, ‘lean’, or ‘purple drank’. Rapper Pimp C, from the group UGK, died from an overdose of this combination. Codeine is used in illegal drug laboratories to make morphine.
Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually occurs within an hour. It is often combined with paracetamol (acetaminophen) as this is known to improve the efficacy of tramadol in relieving pain.
Common side effects include: constipation, itchiness and nausea. Serious side effects may include seizures, increased risk of serotonin syndrome, decreased alertness, and drug addiction. A change in dosage may be recommended in those with kidney or liver problems. It is not recommended in those who are at risk of suicide. While not recommended in women who are breastfeeding, those who take a single dose should not generally stop breastfeeding.
It works by binding to the μ-opioid receptor and as a serotonin–norepinephrine reuptake inhibitor (SNRI). Tramadol is in the benzenoid class. In the body it is converted to desmetramadol, which is a more potent opioid.
Tramadol is used primarily to treat mild–severe pain, both acute and chronic. Its analgesic effects take about one hour to come into effect and 2 h to 4 h to peak after oral administration with an immediate-release formulation. On a dose-by-dose basis tramadol has about one tenth the potency of morphine and is approximately equally potent when compared with pethidine and codeine.
For pain moderate in severity its effectiveness is equivalent to that of morphine; for severe pain it is less effective than morphine. These painkilling effects last for approximately 6 h.
Available dosage forms include liquids, syrups, drops, elixirs, effervescent tablets and powders for mixing with water, capsules, tablets including extended release formulations, suppositories, compounding powder, and injections.
Dependence and withdrawal
Long-term use of high doses of tramadol will cause physical dependence and withdrawal syndrome. These include both symptoms typical of opioid withdrawal and those associated with SSRI withdrawal; symptoms include numbness, tingling, paresthesia, and tinnitus. Psychiatric symptoms may include hallucinations, paranoia, extreme anxiety, panic attacks, and confusion. In most cases, tramadol withdrawal will set in 12–20 hours after the last dose, but this can vary. Tramadol withdrawal typically lasts longer than that of other opioids. Seven days or more of acute withdrawal symptoms can occur as opposed to typically three or four days for other codeine analogues.
However, according to a 2014 report by the World Health Organizations Expert Committee on Drug Dependence ‘”….in many cases of tramadol dependence, a history of substance abuse is present….but….the evidence for physical dependence was considered minimal. Consequently, Tramadol is generally considered as a drug with low potential for dependence.
Because of the possibility of convulsions at high doses for some users, recreational use can be very dangerous. Tramadol can cause a higher incidence of nausea, dizziness, loss of appetite compared with opioids, which could deter recreational use. Compared to hydrocodone, fewer persons choose to use tramadol recreationally.