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