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nabiximols (Sativex, Cannador)
Schedule 1 drug*. Approved for use in Canada
Indications:
- neuropathic pain from multiple sclerosis
- cannabis dependence?* [2]
* in combination with motivational enhancement therapy & cognitive behavioral therapy
Contraindications:
1) absolute
a) hypersensitivity to cannabinoids, ethanol, propylene glycol, or peppermint oil
b) patients who are nursing or pregnant
2) relative
a) significant hepatic or renal dysfunction
b) history of a psychotic disorder (e.g., schizophrenia)
- discontinue use with psychotic episode while on Sativex
c) under 18 years of age
d) women of child-bearing age not on a reliable form of contraceptive
e) men expecting to start a family
f) patients with severe cardiovascular disease
- ischemic heart disease,
- arrhythmias
- poorly controlled hypertension
- heart failure
Dosage:
1) 100 uL peppermint-flavoured buccal spray (under the tongue or inside the cheek) delivers
a) 2.7 mg of tetrahydrocannabinol
b) 2.5 mg of cannabidiol
2) 1 spray every 4 hours; max 4 sprays on day 1
3) gradually adjust as needed
4) median daily dose of 5 sprays/day in clinical trials
5) limited experience > 12 sprays/day, but higher doses tolerated
5.5 mL vial.
stored in the refrigerator (2-8 C)
once opened, may be stored at room temperature (15-25 C)
discard after 28 days
Adverse effects:
1) generally mild to moderate#
2) gastrointestional
- nausea, vomiting, diarrhea, sensation of heaviness dysgeusia, thirst, increased appetite,
3) neuromuscular
- fatigue, weakness, lethary, falls, vertigo
4) CNS
- feeling drunk, disturbance in attention, somnolence, dizziness, disorientation, dissociation, euphoria
- subjects not able to subjectively distinguish nabiximols from placebo [2]
5) respiratory tract
- cough, pharyngitis
6) cardiovascular
- tachycardia, transient changes in blood pressure
7) local application site reaction*
- dry mouth, oral pain, stinging
* avoid spraying onto sore or inflamed mucous membranes
# dose-related with increasing incidence at higher doses symptoms generally resolve with reducing the dose
Drug interactions:
1) see dronabinol & cannabidiol
2) avoid concurrent administration of hypnotics
Pharmacokinetics:
- fast onset of action like smoked marijauna without smoke
Mechanism of action:
- contains delta-9 tetrahydrocannabinol & cannabidiol
* Importation into US is illegal.
General
pharmacologic combination
Database Correlations
PUBCHEM cid=44148067
References
- Prescriber's Letter 12(6):32 2005
New Drug: Sativex (Delta-9-tetrahydrocannabinol and Cannabidiol)
Detail-Document#: 210605
(subscription needed) http://www.prescribersletter.com
- Trigo JM, Soliman A, Quilty LC et al.
Nabiximols combined with motivational enhancement/cognitive
behavioral therapy for the treatment of cannabis dependence:
A pilot randomized clinical trial.
PLoS One 2018 Jan 31; 13:e0190768.
PMID: 29385147 Free PMC Article
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0190768
Components
cannabidiol (Epidiolex, Zygel, ZYN002, CBD)
tetrahydrocannabinol; delta-9-tetrahydrocannabinol; THC