nabiximols (Sativex, Cannador)

Introduction

Schedule 1 drug*. Approved for use in Canada

Indications

• neuropathic pain from multiple sclerosis
• cannabis dependence?*

* in combination with motivational enhancement therapy & cognitive behavioral therapy

Contraindications

• absolute
  • hypersensitivity to cannabinoids, ethanol, propylene glycol, or peppermint oil
  • patients who are nursing or pregnant
• relative
  • significant hepatic or renal dysfunction
  • history of a psychotic disorder (e.g., schizophrenia)
    • discontinue use with psychotic episode while on Sativex
  • under 18 years of age
  • women of child-bearing age not on a reliable form of contraceptive
  • men expecting to start a family
  • patients with severe cardiovascular disease
    • ischemic heart disease,
    • arrhythmias
    • poorly controlled hypertension
    • heart failure

Dosage

• 100 uL peppermint-flavoured buccal spray (under the tongue or inside the cheek) delivers
  • 2.7 mg of tetrahydrocannabinol
  • 2.5 mg of cannabidiol
• 1 spray every 4 hours; max 4 sprays on day 1
• gradually adjust as needed
• median daily dose of 5 sprays/day in clinical trials
• 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

Pharmacokinetics

• fast onset of action like smoked marijauna without smoke

Adverse effects

• generally mild to moderate#
• gastrointestional
  • nausea, vomiting, diarrhea, sensation of heaviness dysgeusia, thirst, increased appetite,
• neuromuscular
  • fatigue, weakness, lethary, falls, vertigo
• CNS
  • feeling drunk, disturbance in attention, somnolence, dizziness, disorientation, dissociation, euphoria
  • subjects not able to subjectively distinguish nabiximols from placebo
• respiratory tract
  • cough, pharyngitis
• cardiovascular
  • tachycardia, transient changes in blood pressure
• 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

• see dronabinol & cannabidiol
• avoid concurrent administration of hypnotics

Mechanism of action

• contains delta-9 tetrahydrocannabinol & cannabidiol

* Importation into US is illegal.

More general terms

• pharmacologic combination

Components

• tetrahydrocannabinol; delta-9-tetrahydrocannabinol; THC
• cannabidiol (Epidiolex, Zygel, ZYN002, CBD)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=44148067