Hydrocodone or
dihydrocodeinone is a semi-synthetic
opioid derived from either of two naturally occurring
opiates:
codeine and
thebaine It is an orally active
narcotic analgesic and
antitussive. It is available in tablet, capsule, and syrup form.
Hydrocodone is often compounded with other generally less effective non-opioid compounds such as
paracetamol (also known as acetaminophen) or
ibuprofen, both often added to discourage recreational use
(as paracetamol can cause potentially fatal liver toxicity at high
doses), and to provide a possible synergy of analgesic effects between
hydrocodone and the non-opioid compounds present. The particular niche
in which hydrocodone is most commonly used is as an intermediate
centrally acting analgesic. Abrupt discontinuation of hydrocodone (
Vicodin, Vicodin ES, and Norco) may result in withdrawal symptoms.
Because of concerns about liver damage from protracted use of
paracetamol at high doses, four pharmaceutical companies (Purdue
Frederick, Cephalon, Zogenix, and Egalet) are developing
extended-release capsules and other forms of hydrocodone by itself.
Hydrocodone was first synthesized in Germany in 1920 by
Carl Mannich and Helene Löwenheim.
It was approved by the
Food and Drug Administration on 23 March 1943 for sale in the United States and approved by
Health Canada for sale in Canada under the brand name Hycodan.
Hydrocodone and compounds containing it are marketed, in varying
forms, under a number of trademarks, including Anexsia, Biocodone,
Damason-P, Dicodid, Duodin, Hycet, Hycodan (or, generically, Hydromet),
Hycomine, Hydrococet, Hydrokon, Hydrovo, Kolikodol, Lorcet, Lortab,
Mercodinone,
Norco, Norgan, Novahistex, Orthoxycol, Panacet, Symtan, Synkonin,
Vicodin, Xodol and Zydone. Hycodan was the original trade name.
The trade name Dicodid was chosen because hydrocodone is the codeine analogue of
hydromorphone
(Dilaudid) and the naming scheme extended to related drugs like
Dihydrin (dihydrocodeine) and Dinarkon (oxycodone). The trade name
Vicodin refers to hydrocodone being six times stronger than codeine by
mouth, as in the Roman numeral VI.
[citation needed]
Likewise, the tradename Hycodan points to its relationship with
oxycodone (Percodan) hy- for hydogen, per- for oxygen (as in potassium
permaganate) -- this can also be seen with other trade names for other
drugs like Permonid (desomorphine) and Hydal (hydromorphone).
Fentanyl (also known as
fentanil, brand names Sublimaze,
Actiq,
Durogesic, Duragesic, Fentora, Matrifen, Haldid, Onsolis,
Instanyl,
Abstral,
Lazanda
and others) is a potent, synthetic
narcotic analgesic with a rapid onset and short duration of action.
It is a strong agonist at the
μ-opioid receptors. Historically it has been used to treat
breakthrough pain and is commonly used in pre-procedures as a pain reliever as well as an
anesthetic in combination with a
benzodiazepine.
Fentanyl is approximately 100 times more potent than
morphine,
with 100 micrograms of fentanyl approximately equivalent to 10 mg of morphine and 75 mg of
pethidine (meperidine) in analgesic activity.
It has an
LD50 of 3.1 milligrams per kilogram in rats, and an LD
50 of 0.03 milligrams per kilogram in monkeys.
Fentanyl was first synthesized by
Paul Janssen in 1960
following the medical inception of
pethidine
several years earlier. Janssen developed fentanyl by assaying analogues
of the structurally-related drug pethidine for opioid activity.
The widespread use of fentanyl triggered the production of fentanyl
citrate (the salt formed by combining fentanyl and citric acid in a 1:1
stoichiometry),
which entered the clinical practice as a general anaesthetic under the
trade name Sublimaze in the 1960s. Following this, many other fentanyl
analogues were developed and introduced into the medical practice,
including
sufentanil,
alfentanil,
remifentanil, and
lofentanil.
In the mid-1990s, fentanyl was first introduced for widespread palliative use with the clinical introduction of the
Duragesic
patch, followed in the next decade by the introduction of the first
quick-acting prescription formations of fentanyl for personal use, the
Actiq lollipop and
Fentora buccal tablets. Through the delivery method of
transdermal patches, as of 2012 fentanyl was the most widely used synthetic opioid in clinical practice,
with several new delivery methods currently in development, including a sublingual spray for cancer patients.
In military applications, fentanyl and, possibly, derivatives can be used to very rapidly incapacitate and to kill.
Fentanyl and derivatives have been used as recreational drugs; as such they have caused fatalities.
Codeine or
3-methylmorphine (a natural isomer of methylated morphine, the other being the semi-synthetic
6-methylmorphine) is an
opiate used for its
analgesic,
antitussive, and
antidiarrheal properties. Codeine is the second-most predominant
alkaloid in
opium, at up to three percent; it is much more prevalent in the Iranian poppy (
Papaver bractreatum),
and codeine is extracted from this species in some places although the
below-mentioned morphine methylation process is still much more common.
It is considered the prototype of the weak to midrange
opioids (
tramadol, dextropropoxyphene, dihydrocodeine,
hydrocodone).
Codeine is used to treat mild to moderate
pain and to relieve
cough.
Codeine is also used to treat
diarrhea and diarrhea predominant
irritable bowel syndrome, although
loperamide (which is available
OTC for milder diarrhea),
diphenoxylate,
paregoric or even
laudanum (also known as
Tincture of Opium) are more frequently used to treat severe diarrhea.
Zydone
Zydone
® is the combination of two drugs, Hydrocodone Bitartrate and
acetaminophen. Hydrocodone Bitartrate belongs to a class of drugs called
opioid analgesics.
Zydone ® is indicated for the relief of
moderate to moderately severe pain. Dosage may need to be adjusted while
taking Zydone. Never attempt to adjust this on your own, always consult
with your physician first. Hydrocodone may be habit forming, so take
this medication exactly as directed. Never take Zydone ® more frequently
or in higher doses until consulting with your healthcare professional.
Zydone Uses
Zydone
is the brand name for tablets made up of hydrocodone and acetaminophen.
There are three strengths of the drug, all which have 400 mg of
acetaminophen. The hydrocodone strengths are 5 mg, 7.5 mg and 10 mg.
Hydrocodone is an opiate analgesic and cough suppressant. Acetaminophen
(Tylenol) is a milder pain reliever and non-narcotic. Zydone is
indicated for pain that is moderate to moderately severe.
The
combination of the two main ingredients is marketed under various names,
including Vicodin, Norco, Lortab and Lorcet. Hydrocodone attaches to
the opioid receptors in the brain and spinal cord to block pain.
Acetaminophen decreases the formation of prostaglandins and increases
pain-relieving power. Hydrocodone can be habit-forming if not used as
prescribed. It is derived from the opium plant and classified as a
Schedule II controlled substance in the U.S., meaning it has the
potential to be abused and cause dependence.
Zydone Warningsz
Zydone
is intended to be taken whole. Crushing, chewing or snorting opiate
drugs can lead to severe side effects or overdose. As with other
opiates, warnings from manufacturers say Zydone should not be taken more
often or in larger doses than what is prescribed. Anyone who has more
than three alcoholic drinks per day or cirrhosis of the liver should
talk to a doctor before taking any medication with acetaminophen. An
overdose of acetaminophen can cause serious liver damage. The maximum
recommended amount of acetaminophen for an adult is 1,000 mg per dose
and 4,000 mg in a day. Doctors recommend knowing the amount of
acetaminophen in each medication you take. Zydone can impair motor
skills, affecting reaction time, and can cause changes in mood and
thought processes. Warnings on the prescription say care should be taken
when driving or performing other tasks that require alertness.
Possible Side Effects Of Zydone
Constipation,
upset stomach, nausea, dizziness and dry mouth are considered among the
most commonly reported side effects. Less common, but more serious,
side effects include allergic reaction, clammy skin, seizures, extreme
weakness, unconsciousness, jaundice, bleeding, bruising, decreased
appetite, hot flashes, rash, itching, swelling, hearing loss, decreased
sex drive and muscle twitches. Because of the hydrocodone, Zydone can
also depress the central nervous system. Other side effects, which may
attract some recreational users, include extreme relaxation, euphoria
and drowsiness.
Tolerance, Dependency, Withdrawal And Detox
When
taken as directed, Zydone can be a useful tool in pain relief.
Prolonged use of opiates can lead to tolerance and dependence. Tolerance
occurs when the drug builds up in the system, requiring people to take
more to achieve the same pain-relieving effects. A tell-tale sign of
dependence is a strong craving for the drug. Once addicted, withdrawal
symptoms can set in. They include muscle and bone pain, insomnia,
restlessness, diarrhea, vomiting, other flu-like symptoms and
involuntary leg movements. Overdosing on Zydone or other opiates can be
fatal. Kicking a Zydone addiction can be difficult. Many users delay
treatment because of a fear of withdrawal. Numerous treatment options
are available for opiate dependence. They include hospital-based
detoxification, rehabilitation, faith or therapy-based programs and
rapid drug detox.
Tramadol hydrochloride (trademarked as Conzip, Ryzolt, Ultracet,
Ultram in the USA, Ralivia and Zytram XL in Canada) is a centrally-acting synthetic
analgesic
used to treat moderate to moderately-severe pain. The drug has a wide
range of applications, including treatment of rheumatoid arthritis,
restless legs syndrome and
fibromyalgia. It was launched and marketed as
Tramal by the German
pharmaceutical company Grünenthal GmbH in 1977.
[1][2]
Tramadol is a very weak
μ-opioid receptor agonist, induces
serotonin release, and inhibits the
reuptake of
norepinephrine.
[3][4] Tramadol is converted to
O-desmethyltramadol,
a significantly more potent μ-opioid agonist. The opioid agonistic
effect of tramadol and its major metabolite(s) is almost exclusively
mediated by such μ-opioid receptors. This further distinguishes tramadol
from opioids in general (including
morphine),
which do not possess tramadol's degree of receptor subtype selectivity
and which are much stronger opiate-receptor agonists. Similarly, the
habituating properties of tramadol (such as they are) are arguably
mainly due to μ-opioid agonism with contributions from serotonergic and
noradrenergic effects.