Drug reference

dronabinol

Cannabinoid receptor agonist · Antiemetic, Appetite Stimulant

Cannabinoid receptor agonistAntiemetic, Appetite StimulantATC A04AD10

CDSCO approvedATC A04AD10

EXCRETION

—

not curated

INTERACTIONS

8 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 8 →

BuprenorphineSevereDatabaseDDInter
BupropionSevereDatabaseDDInter
DextropropoxypheneSevereDatabaseDDInter
IohexolSevereDatabaseDDInter

Mechanism

Dronabinol is a low-efficacy agonist of CB1 and CB2 cannabinoid receptors.

Indications

treatment of nausea and vomiting associated with cancer chemotherapy after traditional pharmacological regimens are unsuccessfulanorexia associated with weight loss in patients with AIDSAntiemetic (chemotherapy-induced nausea and vomiting)Prevention of chemotherapy-induced nausea and vomiting (when other antiemetics are ineffective)Appetite stimulation in patients with AIDS and anorexiaCancer chemotherapy induced vomitingalternative antiemetic for moderately emetogenic chemotherapy (in patients who cannot tolerate other antiemetics or are unresponsive)appetite stimulant (in cachectic/AIDS patients)

Dosing

Adult: For nausea and vomiting associated with cancer chemotherapy: begun at 5 mg/m2 given 1 to 3 h before chemotherapy and then every 2 to 4 h after chemotherapy up to four to six doses per day. The first dose should be given at least 30 min prior to eating. Later doses can be given without regard to fed status; however, dosing relative to meals should be kept constant to facilitate titration.…
Pediatric: Dronabinol is not approved for pediatric use.
Renal adjustment: Care should be used in prescribing dronabinol to individuals who may be at greater risk for any of these adverse effects.

Pharmacokinetics

Onset

Within an hour

Peak effect

1 to 3 h after oral administration (capsule form); ~15 min after inhalation

Bioavailability

10% to 20% (oral); 60% to 70% (inhaled)

Protein binding

Highly bound (>95%) to plasma proteins

Metabolism

Phase 1 metabolism appears to be chiefly by CYP2C9 and CYP3A4, with the former having a greater contribution. Undergoes successively oxidation at C11, leading to 11-hydroxy-tetrahydrocannabinol (11-OH-THC), followed by 11-nor-carboxy-THC. 11-OH-THC retains high activity at CB1 cannabinoid receptors, and its levels may be greater than THC after oral consumption.

Excretion

primarily via the bile, with lesser amounts in the urine. THC metabolism is prolonged, with metabolites being detected in the feces and urine more than 5 weeks after a single dose.

Side effects

Common

dizzinessfatiguecognitive impairmenttachycardiahypo- or hypertensionabdominal painincreased nausea and vomiting (suggestive of cannabinoid hyperemesis syndrome)EuphoriaSomnolenceDetachmentAnxietyNervousnessPanicPalpitationsVasodilationHypotensionConjunctival injection (bloodshot eyes)Hallucinogenic effectsPsychomotor effectsdisorienting effectscentral sympathomimetic effects

Serious

exacerbation of mania
depression
schizophrenia
Paranoid reactions
Abnormalities of thinking
Abstinence syndrome (irritability, insomnia, restlessness) after abrupt withdrawal
addiction potential (may experience a ‘high’)