Abstract
OxyContin is a opioid pain reliever similar to morphine. An opioid is sometimes called a narcotic.
[2]
Manufacturers
MALLINCKRODT PHARMA
MEDISCA INC
SPECTRUM PHARMA
FAGRON PHARMA
PROFESSIONAL CO
FREEDOM PHARMA
ELGE INC
B&B PHARM
HAWKINS CHEMICALS
BLENHEIM PHARMA
QUALITY CARE
4UORTHO LLC
PHYSICIANS TC
ETHEX CORP
MALLINCKRODT PHARMA
PALMETTO STATE
APOTEX CORP
CORE PHARMA
RANBAXY PHARMA
STAT RX USA
[1]
Brand Names
Dazidox
Oxyfast
OxyIR
Percolone
Roxicodone
Roxicodone Intensol
M-Oxy
ETH-Oxydose
Endocodone
[2]
History
Freund and Speyer of the University of Frankfurt in Germany first synthesized oxycodone from thebaine in 1916, a few years after the German pharmaceutical company Bayer had stopped the mass production of heroin due to hazardous use, harmful use, and dependence.
The first clinical use of the drug was documented in 1917, the year after it was first developed. It was first introduced to the US market in May 1939. In early 1928, Merck introduced a combination product containing scopolamine, oxycodone, and ephedrine under the German initials for the ingredients SEE, which was later renamed Scophedal (SCOpolamine ePHEDrine & eukodAL)—this combination is essentially an oxycodone analogue of the morphine-based Twilight Sleep with ephedrine added to reduce circulatory and respiratory effects.
[3]
Uses
Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes.
[4]
Pharmacology
Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
[4]
Schedule
It is a potent schedule II opioid analgesic drug with an abuse liability similar to morphine and other schedule II opioids
[5]
Dosage:
Opioid-naïve patients: 5-15 mg PO q4-6hr
Usual: 10-30 mg PO q4-6hr
Controlled release (continuous relief for extended period sought): 10 mg PO q12hr
Immediate-release preparation with "abuse aversion" technology (if crushed, crumbles into chunks instead of powder and foams if mixed with liquid).
Must be swallowed whole; do not chew, crush, or dissolve NOT for use via NG, gastric, or other feeding tubes.
[6]
Drug Interactions
Contraindicated interactions with:
alvimopan
Serious interactions with:
buprenorphine
butorphanol
cimetidine
dezocine
fluoxetine
furazolidone
isocarboxazid
ivacaftor
linezolid
lumefantrine
moclobemide
nalbuphine
naltrexone
pargyline
paroxetine
pentazocine
phenelzine
procarbazine
quinidine
rasagiline
selegiline
selegiline transdermal
sodium oxybate
tramadol
tranylcypromine
Significant interactions with:
albuterol
alfentanil
alprazolam
benperidol
benzphetamine
brompheniramine
butalbital
butorphanol
caffeine
carbinoxamine
carisoprodol
celecoxib
dezocine
diamorphine
diazepam
dopamine
dopexamine
dosulepin
doxepin
enflurane
ephedrine
maprotiline
maraviroc
marijuana
mazindolmorphine
motherwort
moxonidineyohimbine
ziconotide
ziprasidone
zotepine
[7]
Adverse Effects
Nausea
Vomiting
Constipation
Sweating, flushing, warmness of the face/neck/upper thorax
Pruritus, urticaria
Bradycardia
Dizziness
Visual disturbances
Mentalclouding/depression
Sedation
Coma
Euphoria/Dysphoria
Weakness
Faintness
Agitation
Restlessness
Nervousness
Seizures
[8]
Contraindications
Absolute:
Acute abdominal condition, bleeding gastrointestinal ulcers, peptic ulcer, diarrhea associated with toxins, pseudomembranous colitis
Hemolytic anemia from PK and G6PD deficiency, hemophilia, hemorrhagic diathesis, thrombocytopenia
Pregnancy/lactation
Nasal polyps associated with asthma, respiratory depression
Relative:
Asthma, respiratory impairment
Erosive gastritis, inflammatory bowel disease
[9]
Cautions
Anemia, cardiac arrhythmias, drug abuse/dependence, emotional lability, gallbladder dz, gout, head injury, hepatic dz/impairment, hypoprothrombinemia, hypothyroidism, incr ICP, prostatic hypertrophy, renal impairment, seizures w/ epilepsy, thyrotoxicosis, urethral stricture, urinary tract surgery, vitamin K deficiency, anoxia, CNS depression, hypercapmia, respiratory depression/dz, untreated myxedema, Addison's dz
Controlled-release (OxyContin) reformulated April 2010 to prevent medication from being cut, broken, crushed, or dissolved to release more medication; inability to tamper CR product decreases ability to snort/abuse
If crushed, controlled-release caps (OxyContin) can deliver large opiate dose with potential for abuse or overdose
Caution with OxyContin in patients who have difficulty swallowing or have underlying GI disorders that may predispose them to obstruction.
[9]
Pricing
The pricing varies depending on what form one would like to buy, and the brand.
The 10mg tablet is priced in between $0.78 to $11.11. The prices for 15mg tablet vary from
$0.92 to $8.62. The 20mg tablet may be priced in the range of $1.42 to $16.36. The 30mg tablet is priced $0.92 to $8.60. The 40mg tablet is priced in between $7.42 to $19.09
[1]
References:
[1] http://reference.medscape.com/drug/roxicodone-oxycontin-oxycodone-343321#90
[2] http://www.drugs.com/oxycontin.html
[3] http://www.ncbi.nlm.nih.gov/pubmed/8844441
[4] http://www.drugbank.ca/drugs/DB00497
[5] http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000589/
[6] http://reference.medscape.com/drug/roxicodone-oxycontin-oxycodone-343321#13
[7] http://reference.medscape.com/drug/roxicodone-oxycontin-oxycodone-343321#3
[8] http://reference.medscape.com/drug/roxicodone-oxycontin-oxycodone-343321#4
[9] http://reference.medscape.com/drug/roxicodone-oxycontin-oxycodone-343321#5
