TRAMADOL HYDROCHLORIDE tablet, film coated TRAMADOL HYDROCHLORIDE ER- tramadol hydrochloride tablet, extended release

Land: USA

Språk: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv ingrediens:

TRAMADOL HYDROCHLORIDE (UNII: 9N7R477WCK) (TRAMADOL - UNII:39J1LGJ30J)

Tilgjengelig fra:

DirectRX

INN (International Name):

TRAMADOL HYDROCHLORIDE

Sammensetning:

TRAMADOL HYDROCHLORIDE 100 mg

Administreringsrute:

ORAL

Resept typen:

PRESCRIPTION DRUG

Indikasjoner:

Tramadol hydrochloride extended-release tablets are indicated for the management of moderate to moderately severe chronic pain in adults who require around-the-clock treatment of their pain for an extended period of time. Tramadol hydrochloride extended-release tablets should not be administered to patients who have previously demonstrated hypersensitivity to tramadol, any other component of this product or opioids. Tramadol hydrochloride extended-release tablets are contraindicated in any situation where opioids are contraindicated, including acute intoxication with any of the following: alcohol, hypnotics, narcotics, centrally acting analgesics, opioids or psychotropic drugs. Tramadol hydrochloride extended-release tablets may worsen central nervous system and respiratory depression in these patients. - Tramadol hydrochloride extended-release tablet is a mu-agonist opioid. Tramadol, like other opioids used in analgesia, can be abused and is subject to criminal diversion. Drug addiction is characterized by

Autorisasjon status:

Abbreviated New Drug Application

Preparatomtale

TRAMADOL HYDROCHLORIDE- TRAMADOL HYDROCHLORIDE TABLET, FILM COATED
TRAMADOL HYDROCHLORIDE ER- TRAMADOL HYDROCHLORIDE TABLET, EXTENDED
RELEASE
DIRECTRX
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TRAMADOL HYDROCHLORIDE
DESCRIPTION SECTION
Tramadol hydrochloride is a centrally acting synthetic analgesic in an
extended-release
formulation. The chemical name is (±)cis-2-[(dimethylamino)
methyl]-1-(3-
methoxyphenyl) cyclohexanol hydrochloride. Its structural formula is:
Figure 1
tramadol-structure
The molecular weight of tramadol hydrochloride is 299.84. It is a
white, crystalline
powder that is freely soluble in water and methanol, very slightly
soluble in acetone and
has a pKa of 9.41. The n-octanol/water log partition coefficient
(logP) is 1.35 at pH 7.
Tramadol hydrochloride extended-release tablets contain 100 mg, 200 mg
or 300 mg of
tramadol hydrochloride, USP in an extended-release formulation. The
tablets are white in
color and contain the inactive ingredients pregelatinized maize
starch, hypromellose,
mannitol, magnesium stearate, cellulose acetate and polyethylene
glycol.
Imprinting ink contains, shellac glaze, iron oxide black, N-butyl
alcohol, ammonium
hydroxide and propylene glycol.
CLINICAL PHARMACOLOGY SECTION
12.1 Mechanism of Action
Tramadol hydrochloride extended-release tablets contain tramadol, an
opioid agonist
and an inhibitor of reuptake of norepinephrine and serotonin. Although
the mode of
action of tramadol is not completely understood, the analgesic effect
of tramadol is
believed to be due to both binding to μ-opioid receptors and weak
inhibition of reuptake
of norepinephrine and serotonin.
Opioid activity of tramadol is due to both low affinity binding of the
parent compound
and higher affinity binding of the O-desmethyl metabolite M1 to
μ-opioid receptors. In
animal models, M1 is up to 6 times more potent than tramadol in
producing analgesia
and 200 times more potent in μ-opioid binding. Tramadol-induced
analgesia is only
partially antagonized by the opioid antagonist naloxone in several
animal tests. The
relative cont