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Ramsey Jaswal

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(L-Codeine, 3-Methylmorphine, Morphine monomethylether, N-Methyl Norcodeine,
Codicept/Coducept)

Codeine, a
prodrug
derived from Opium is an
agonist
of opioid receptor types. Its main action of
pain relief
is accomplished through its ability to decrease the signalling between neurons; Codeine acts upon opioid receptors within much of the
central nervous system
and
gastrointestinal tract
. Taken
orally
, Codeine is often coupled with other analgesics. It is metabolized to prodrug form within the liver, through the actions of two major enzymes,
CYP 2D6
and
CYP 3A4
. Codeine is often abused for its analgesic tendencies, and its use is implicated in the deaths of numerous well known individuals. Alternative treatments to codeine include the use of other drugs, such as acetaminophen.
INTRODUCTION
Codeine, a
prodrug
derived from
Opium
is an
agonist
of
opioid receptor types
. Its main action of
pain relief
is accomplished through its ability to decrease the signalling between neurons; Codeine acts upon opioid receptors within much of the
central nervous system
and
gastrointestinal tract
. Taken
orally
, Codeine is often coupled with other analgesics. It is metabolized to prodrug form within the liver, through the actions of two major enzymes,
CYP 2D6
and
CYP 3A4
. Codeine is often abused for its analgesic tendencies, and its use is implicated in the deaths of numerous well known individuals. Alternative treatments to codeine include the use of other drugs, such as acetaminophen.
ABSTRACT
Codeine is a compound derived from
opium
and was first isolated in 1834 by Pierre Robiquet in France. Although it is primarily used as a
pain reliever
, many other symptoms can be treated with it including
anxiety, hypertension, diarrhea, coughing, myocardial infarctions and premature labor contractions
. Codeine acts as an
agonist
on the
µ-opioid receptor
and is known to create a dependency in individuals using it chronically and can cause withdrawal symptoms if its administration is suddenly stopped. Pharmaceutically, codeine is primarily produced using a semi-synthetic process, although it can be derived naturally as well. It is found marketed by itself or in combination with paracetamol (in the form of Tylenol 3 or 4), aspirin, or ibuprofen where
drug synergy
is expressed. Additionally codeine can also be found in mixtures with other analgesics or muscle relaxants.
INTRODUCTION


Although codeine has some
analgesic properties
it is primarily considered a
prodrug
of much more potent opiates including morphine and norcodeine. Taken
orally
codeine has a
bioavailability of 30-40%
and a
half life of 2.5-3.5 hours
. Codeine is quickly metabolized to opiate derivatives, mainly
codeine-6-gluconuride
by
CYP2D6
and
CYP3A4
followed by
gluconuride transferase
. 90% of metabolites are excreted through
urine
, with the remaining 10% excreted through
biliary action.
The expression levels and isoforms of CYP2D6 and CYP3A4 are
highly variable
among individuals leading to different kinetic profiles. Some individuals are termed poor metabolizers and have almost no ability to convert codeine to more active metabolites. Stronger opiates often have to be administered to these types of patients as very little analgesic effects are seen with codeine. On the other extreme ultra metabolizers may convert up to 75% of codeine into morphine following repeated dosing. Due to morphine’s longer half-life repeated doses of codeine can cause overdose leading to respiratory failure and death in ultra metabolizers.
PHARMACOKINETICS
Codeine is considered a
prodrug
, its effects are primarily derived from its active metabolites,
morphine
and
Codeine-6-gluconuride
. These metabolites are
partial agonists
of
Mu
and
Kappa

opioid receptors
throughout the body. Opioid receptors are
G-protein coupled receptors
signaling through
Gi/o proteins
. Binding of these receptors by codeine metabolites leads to activation of
MAP kinase, decreasing cAMP
in the cell. Downstream effectors cause
excitability of K+ channels
and
inhibition of voltage gated Ca+2 channels in neuronal cells
. The resultant hyper-polarization reduces neuronal excitability
inhibiting secretion of nociceptive neurotransmitters
such as GABA, substance P and dopamine. Decreased signaling between neurons leads to analgesia and sedation.

The distribution of opioid receptor subtypes is heterogeneous throughout the
central nervous system
and
gastrointestinal tract.
Activation of
Mu1
and
Mu2
subtypes in the
dorsal horn of the spinal cord and insular cortex leads to supraspinal analgesia, respiratory depression and constipation
. The Kappa opioid receptor is present in the
amygdala
and
hypothalamus
and is responsible for
sedation
and
physical dependency
.
Major
- To relieve
mild to moderate pain
- To relieve mild
postoperative pain
(dental surgeries and other surgeries)
Minor
- To manage
chronic cough
- To treat
diarrhea
- To manage
acute bronchitis
- To manage
neuropathic pain
- To manage
headaches
in adults

Codeine Contraindications (Do not use if:)
o Severe
liver disease
o History of
hepatic encephalopathy
o
Paralytic Ileus
o
Hypersensitivity
CLINICAL INDICATIONS


Codeine is available over the counter (OTC) in Canada in
tablet
form usually in combination with other drugs such as
caffeine
and
acetaminophen
(Tylenol codeine series for example). IV administration is not recommended due to possible reactions leading to anaphylaxis, thus IM and SC routes are preferred if Oral administration is not an option. Doses are prescribed for short term relief of mild to moderate pain and also relief of cough and diarrhea.
Doses are adjusted according to the severity of pain and response.
DOSAGE
ALTERNATIVE TREATMENTS
Alternative Treatments
- ibuprofen
- hydrocodone
- oxycodone
- vicodin
- paracetamol
- acetaminophen
- NSAIDs

Cardiovascular
- hypotension (rare, usually with high doses)

Respiratory
- Respiratory depression

Gastrointestinal
- nausea, vomiting, constipation, ileus

Renal
- acute renal failure

Nervous system
- mental depression, delirium, seizures, dizziness, psychotic symptoms

Withdrawal
- agitation, restlessness, anxiety, insomnia, tremor, abdominal cramps, blurred vision, vomiting, and sweating
SIDE EFFECTS
Codeine is often abused as a recreational drug in the form of “Purple Drank”, which is mixture of prescription-strength codeine (in cough syrup), Sprite, and Jolly Rancher
s. Rapper PIMP C (above) died from an overdose.
FUN FACTS


Baldi, F et al. Focus on Acute Diarrhoeal Disease. World Journal of Gastroenterology. (2009).

Bosilkovska, M et al. Analgesics in Patients With Hepatic Impairment. Drugs. (2012).
Derry, S; Moore, RA; McQuay, HJ. Single Dose Oral Codeine, asa Single Agent, For Acute Postoperative Pain in Adults. Cochrane Database of Systemic Reviews. (2010).

Browining, Juliet et al. Management of chronic cough in patients receiving palliative care: Review of evidence and recommendations by a task group of the Association for Palliative Medicine of Great Britain and Ireland. Palliative Medicine. (2011).

Drugs (2009). Codeine. Retrieved from http://www.drugs.com/codeine.html

DrugBank. Codeine. Retrieved from http://www.drugbank.ca/drugs/DB00318)

Katzung, B. G. (1998). Opioid analgesics & Antagonists. Basic & clinical pharmacology (7th ed., pp. 496-515). Stamford, Conn.: Appleton & Lange.

Leinwand, D. (2006, Oct 19). DEA warns of soft drink cough-syrup mix. USA Today. Retrieved from http://www.nytimes.com/2004/04/18/arts/music-the-woozy-syrupy-sound-of-codeine-rap.html

Medline Plus. Pain Relievers. Retrieved from http://www.nlm.nih.gov/medlineplus/painrelievers.html

Sanneh, K. (2004, April 18). Music; The Woozy, Syrupy Sound of Codeine Rap. The New York Times. Retrieved from http://www.nytimes.com/2004/04/18/arts/music-the-woozy-syrupy-sound-of-codeine-rap.htm
l
REFERENCES
CODEINE
Group 7
Nijiati Abulizi, Jeremy De Wet, Ayden Gouveia,
Ramsey Jaswal, Brittany Jeffries, Trung Phan,
Ravpal Randhawa,Chrystal Scholl
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