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Medical Areas: Neurology | Family Medicine
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Ultracet (acetaminophen and tramadol HCl)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Company: Ortho-McNeil Pharmaceutical
Approval Status: Approved August 2001
Treatment Area: Acute pain
Ultracet has been approved by the FDA for the short-term (five
days or less) management of acute pain. This medication is a
centrally acting analgesic that controls pain through different
mechanisms of action than non-steroidal anti-inflammatory drugs
(NSAIDs), the most commonly used pain medications. As a result,
Ultracet is not associated with the side effects that can result
from NSAID use, such as gastrointestinal ulcers or bleeding.
Ultracet combines Ultram (tramadol HCl), a leading prescription
pain reliever, with the common non-prescription pain treatment,
acetaminophen. Clinical trials have shown that the combination is
more effective than either drug alone, providing longer duration
than acetaminophen and a faster onset of action than tramadol.
Ultracet has been evaluated for efficacy and safety in pivotal
single-dose trials in subjects with acute pain. In these trials,
subjects with pain following oral surgical procedures who received
two tablets of Ultracet experienced greater relief than
placebo-treated subjects. Additionally, subjects treated with
Ultracet experienced greater relief than subjects on either of the
individual components given at the same dose. The onset of pain
relief after Ultracet (occurring in less than one hour) was faster
than with tramadol alone, whereas the duration of pain relief after
Ultracet was longer than with acetaminophen alone. Analgesia was
found to be generally comparable to ibuprofen.
Side effects reported with Ultracet include constipation,
somnolence (sleepiness) and increased sweating.
Ultracet should not be used concomitantly with alcohol. Since
tramadol can reinitiate physical dependence, Ultracet is not
recommended for subjects disposed to drug or alcohol abuse.
Seizures have been reported in subjects receiving tramadol
treatment. Data indicates that the risk of seizures is increased
with doses of tramadol above the recommended range. Tramadol use
has been shown to increase seizure risk in subjects taking the
- Selective serotonin reuptake inhibitors
- Tricyclic antidepressants
Additionally, tramadol may enhance the risk of seizures in
subjects taking the following:
- MAO inhibitors
- Other drugs that reduce the seizure threshold
As with any medication, please consult a physician to discuss
possible adverse effects or contraindications.
Mechanism of Action
Tramadol is a centrally acting synthetic opioid analgesic.
Although its mode of action is not completely understood, from
animal tests, at least two complementary mechanisms appear
applicable: binding of parent and M1 metabolite to mu-opioid
receptors and weak inhibition of reuptake of norepinephrine and
Opioid activity is due to both low affinity binding of the
parent compound and higher affinity binding of the O-demethylated
metabolite M1 to mu-opioid receptors. In animal models, M1 is up to
six times more potent than tramadol in producing analgesia and 200
times more potent in mu-opioid binding. Tramadol-induced analgesia
is only partially antagonized by the opiate antagonist naloxone in
several animal tests. The relative contribution of both tramadol
and M1 to human analgesia is dependent upon the plasma
concentrations of each compound.
Tramadol has been shown to inhibit reuptake of norepinephrine
and serotonin in vitro, as have some other opioid analgesics. These
mechanisms may contribute independently to the overall analgesic
profile of tramadol.
Acetaminophen is a non-opiate, non-salicylate analgesic. (from
Ultracet Prescribing Information)