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(Nabilone) Capsules CII
Cesamet (nabilone) is a new therapeutic option for treating patients with chemotherapy-induced nausea and vomiting
(CINV) who have failed to respond adequately to conventional antiemetic treatments. Cesamet provides healthcare
professionals and patients a needed alternative to address this important challenge. Nausea and vomiting are still among
the most-feared side effects of cancer treatment, CINV continues to remain a challenge in a significant number of
patients, despite the availability of newer, more potent antiemetic agents.
Cesamet is a synthetic cannabinoid that is thought to trigger its effects by activating the endocannabinoid receptors,
CB1 and CB2, which are present in the human body. These receptors are involved in regulating nausea and vomiting.
Cesamet targets a different emetic pathway than conventional therapies, it can complement the other antiemetic therapies
to provide more chances for complete relief. Cesamet has a long duration of action, which allows for less frequent
dosing, typically twice-daily.
Recent evidence suggests that Cesamet acts as an neuromodulator via agonist action on cannabinoid CB1
receptors,
which are ubiquitous in the central nervous system, and serve to modulate neuronal signaling.
Cesamet also acts as a
CB2 agonist, primarily on immune cells in the periphery. Activation of CB1 receptors in the brainstem
emetic
circuitry is a powerful inhibitor of nausea and vomiting. Neuromodulation by exogenous cannabinoids (e.g., Cesamet) is
thought to mimic or enhance the natural functions of the innate or endogenous cannabinoids, which act in
reverse from
classical neurotransmitters and serve as retrograde synaptic messengers.
Valeant has filed an Investigational New Drug (IND) application with the U.S. Food and Drug Administration (FDA) for
Cesamet (CII) (nabilone) oral capsules for the treatment of cancer chemotherapy-induced neuropathic pain (CINP). (Read more about the Cesamet Pain IND).
Chemotherapy-induced neuropathic pain can be caused by certain chemotherapy drugs, including taxanes, vinca-alkaloids
and platinum-derived treatments. The onset of chemotherapy-induced neuropathic pain is generally early in treatment,
between the first and third cycle, with the peak in severity occurring approximately three months into therapy.
Incidence and severity depend on a variety of factors including type of chemotherapy and dose. For example, neuropathy
occurs in approximately 45 percent to 50 percent of ovarian cancer patients receiving cisplatin alone, but this
increases to a frequency of 90 percent to 100 percent when cisplatin is administered along with paclitaxel.
The endocannabinoid system is a key mediator of nausea and vomiting
- Several neurotransmitter systems, including the endocannabinoid system, are involved in the complex process of
nausea and vomiting
- The endocannabinoid system includes cannabinoid-1 (CB1) and cannabinoid-2 (CB2) receptors, which modulate a
broad range of effects within the body
- CB1 receptors, which modulate neuronal signaling, are found throughout the central and peripheral nervous
systems
- Activation of CB1 receptors in the brainstem emetic circuitry is a powerful inhibitor of nausea and vomiting
- The antiemetic effect of Cesamet may also be due to activation of CB1 receptors in the stomach and
gastrointestinal tract
Cesamet, a synthetic cannabinoid similar to the active ingredient found in naturally occurring Cannabis sativa L.
[Marijuana; delta-9-tetrahydrocannabinol (_9-THC)], is contraindicated in any patient who has a history of
hypersensitivity to any cannabinoid. Patients receiving treatment with Cesamet should be specifically warned not to
drive, operate machinery, or engage in any hazardous activity while receiving Cesamet. During controlled clinical trials
of Cesamet, virtually all patients experienced at least one adverse reaction. The most commonly encountered events were
drowsiness, vertigo, dry mouth, euphoria (feeling "high"), ataxia, headache, and concentration difficulties. Cesamet
should not be taken with alcohol, sedatives, hypnotics, or other psychoactive substances because these substances can
potentiate the central nervous system (CNS) effects of nabilone. Since Cesamet can elevate supine and standing heart
rates and cause postural hypotension, it should be used with caution in the elderly, and in patients with hypertension
or heart disease. Cesamet should also be used with caution in patients with current or previous psychiatric disorders
(including manic depressive illness, depression, and schizophrenia), as the symptoms of these disease states may be
unmasked by the use of cannabinoids. Cesamet should be used with caution in individuals receiving concomitant therapy
with sedatives, hypnotics, or other psychoactive drugs because of the potential for additive or synergistic CNS effects.
Cesamet should be used with caution in patients with a history of substance abuse, including alcohol abuse or dependence
and marijuana use, since Cesamet contains a similar active compound to marijuana. Cesamet should be used with caution in
pregnant patients, nursing mothers, or pediatric patients because it has not been studied in these patient populations.
Please see full Prescribing Information at www.cesamet.com. |
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