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Published online by Cambridge University Press: 06 October 2020
THERAPEUTICS
Brands
• Sativex
Generic?
• No
Class
• Cannabinoid
Commonly Prescribed for
(FDA approved in bold)
• Spasticity and spastic pain in multiple sclerosis (MS)
• Neuropathic pain
• Advanced cancer pain
• Pain in fibromyalgia, rheumatoid arthritis
How the Drug Works
• It is composed of 1:1 mixture of 2 cannabinoids: cannabidiol (CBD) and 9-δ- tetrahydrocannabinol (THC)
• THC, a partial agonist of both cannabinoid receptors (CB1, CB2) in brain and spinal cord, reduces spasticity but causes sedation and psychotropic side effects. Its action also involves analgesia, muscle relaxation, antiinflammation, neuroprotection, and anxiolysis
• CBD reduces sedation and psychotropic side effects
How Long Until It Works
• Minutes to hours
If It Works
• Takes weeks to months for full effect. Usually within 4 weeks
If It Doesn't Work
• Treat underlying conditions. Consider addition of other agents
Best Augmenting Combos for Partial Response or Treatment-Resistance
• For spasticity, may consider use of other centrally acting muscle relaxant or botulinum toxin
• For neuropathic pain, many consider use of TCAs, SNRIs, AEDs, and opioids
Tests
• None
ADVERSE EFFECTS (AEs)
How the Drug Causes AEs
• Related to CB1 and CB2 agonist effect in peripheral tissues, such as sympathetic ganglia, adrenal gland, heart, lung, reproductive tissues, urinary bladder, GI tract, immune cells
Notable AEs
• Sedation, dizziness, dry mouth, nausea, headache. Administration site irritation
Life-Threatening or Dangerous AEs
• Cardiac arrhythmia, myocardial infarction
• Operational hazard (driving, heavy machinery)
• Psychosis and dependence
Weight Gain
• Not unusual
Sedation
• Common
What to Do About AEs
• Lower the dose and titrate more slowly
Best Augmenting Agents to Reduce AEs
• Most AEs cannot be reduced by an augmenting agent
DOSING AND USE
Usual Dosage Range
• 5–12 sprays per day
Dosage Forms
• Buccal spray: THC 27 mg/mL and CBD 25 mg/mL
How to Dose
• First day: 1 spray every 4 hours, maximum 4 sprays
• Titrate: spread out the doses throughout the day. Watch for adverse reactions. Titrate to a tolerated dosage with acceptable pain relief
• Maximum: 12 sprays per day
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