Dronabinol (dronabinol)

Antiemetic Oral Capsule

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Dronabinol, a synthetic cannabinoid, is an antiemetic and appetite stimulant.

Dronabinol, a synthetic cannabinoid, is an antiemetic and appetite stimulant. The active ingredient in dronabinol capsules and oral solution is synthetic delta-9-tetrahydrocannabinol (delta-9-THC); delta-9-THC also is a naturally occurring component of Cannabis sativa (marijuana).

Like other cannabinoids, dronabinol has complex effects on the CNS, including central sympathomimetic activity. Cannabinoid receptors have been discovered in neural tissues, and these receptors may play a role in mediating the effects of dronabinol. Dronabinol and nabilone, another synthetic cannabinoid, can produce alterations in mental state (e.g., dysphoria, euphoria, anxiety, or panic reactions in some individuals) and psychotomimetic reactions.

Dronabinol-induced sympathomimetic activity may result in tachycardia and/or conjunctival injection. Effects of dronabinol on blood pressure are inconsistent; orthostatic hypotension and/or syncope upon abrupt standing occasionally occurs. Dronabinol exerts reversible effects on appetite, mood, cognition, memory, and perception; these effects appear to be dose-related and exhibit considerable interpatient variability.

Tachyphylaxis and tolerance develop to some of the pharmacologic effects (e.g., cardiovascular and subjective adverse CNS effects) of dronabinol and other cannabinoids with chronic administration, suggesting an indirect effect on sympathetic neurons. However, tachyphylaxis and tolerance do not appear to develop to the appetite stimulant effect of dronabinol.

Dronabinol (delta-9-THC) is almost entirely absorbed (90-95%) after administration of a single oral dose. Due to the combined effects of first-pass hepatic metabolism and high lipid solubility, only 10-20% of the administered dose reaches the systemic circulation. Peak plasma concentrations of dronabinol and its major active metabolite (11-hydroxy-delta-9-THC) occur approximately 0.5-4 hours following oral administration of dronabinol as oral solution or capsules.

The onset of action following administration of dronabinol capsules is approximately 0.5-1 hours, and peak effect is at 2-4 hours. The duration of psychoactive effects is 4-6 hours; however, the appetite stimulant effect of dronabinol may continue for 24 hours or longer. In a pharmacokinetic study in healthy individuals, bioequivalence was demonstrated between a single 4.25-mg oral dose of dronabinol oral solution and a single 5-mg oral dose of dronabinol capsules given under fasting conditions.

In this study, drug absorption was more rapid following administration of the oral solution than capsules; plasma dronabinol concentrations were detected within 15 minutes in all individuals following administration of dronabinol oral solution compared with 17% of individuals following administration of dronabinol capsules.

Administration of dronabinol (as capsules or oral solution) with food delays time to peak plasma concentration and increases systemic exposure compared with administration in the fasted state. Administration of dronabinol capsules with a high-fat, high-calorie meal delayed time to peak plasma concentrations by 4 hours and increased total exposure 2.9-fold; peak plasma concentration was unchanged. Administration of dronabinol oral solution with a high-fat, high-calorie meal delayed time to peak plasma concentration by approximately 5 hours, decreased peak plasma concentration by approximately 20%, and increased total exposure approximately 2.5-fold.

Dronabinol and its metabolites are approximately 97% bound to plasma proteins. Dronabinol undergoes extensive first-pass hepatic metabolism, principally by hydroxylation, producing both active and inactive metabolites. Dronabinol is metabolized principally by cytochrome P-450 (CYP) isoenzymes 2C9 and 3A4.

Formation of the major active metabolite of dronabinol, 11-hydroxy-delta-9-THC, appears to be mediated primarily by CYP2C9. Dronabinol exposure has been reported to be 2-3 times higher in individuals with diminished CYP2C9 function (i.e., poor CYP2C9 metabolizers). Dronabinol and 11-hydroxy-delta-9-THC are present in plasma in approximately equal concentrations.

Following oral administration, dronabinol and its metabolites are eliminated principally in feces (approximately 50%) and to a lesser extent in urine (approximately 10-15%) within 72 hours; less than 5% of an oral dose is recovered unchanged in feces. The principal excretory pathway appears to be the biliary system. The elimination of dronabinol follows a two-compartment model with an initial elimination half-life of about 4 hours and a terminal elimination half-life of 25-36 hours.

Because of redistribution, dronabinol and its metabolites may be excreted at low concentrations for extended periods of time; dronabinol metabolites have been detected in urine and feces for more than 5 weeks following single-dose administration of the drug. Steady-state cannabinoid concentrations appear to be achieved within about 2 weeks following chronic oral administration of the drug.

USES: Dronabinol is used to treat nausea and vomiting caused by cancer chemotherapy. It is usually used when other drugs to control nausea and vomiting have not been successful. Dronabinol is also used to treat loss of appetite and weight loss in patients with HIV infection.

Dronabinol (also called THC) is a man-made form of the active natural substance in marijuana (cannabis).

Generic name: dronabinol
Pronunciation: (dro-NAB-in-all)
Drug class: Antiemetic
Therapeutic class: Gastrointestinal Therapy Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Dronabinol:

  • Anorexia From Hiv
  • Cancer Chemotherapy-Induced Nausea And Vomiting

Also known as: Anorexia Associated With Hiv Infection, Anorexia With Human Immunodeficiency Virus Infection, Chemotherapy-Induced Nausea And Vomiting.

Dosing

The manufacturer of dronabinol oral solution states that a 4.2-mg dose of the oral solution appears to provide comparable systemic exposure to dronabinol as a 5-mg dose of the dronabinol oral capsule, under fasted conditions.

Drug interactions

No formal drug interaction studies have been performed with dronabinol to date. The enzyme inhibition and induction potential of dronabinol and its active metabolite have not been fully elucidated. Dronabinol is metabolized principally by cytochrome P-450 (CYP) isoenzymes 2C9 and 3A4.

Contraindications

*History of hypersensitivity to dronabinol or any ingredient in the formulation. Hypersensitivity reactions reported with dronabinol include lip swelling, hives, disseminated rash, oral lesions, skin burning, flushing, and throat tightness.

*History of hypersensitivity to sesame oil (for dronabinol capsules (e.g., Marinol(R)) as it contains sesame oil).

*History of hypersensitivity to alcohol, or in patients who are receiving or have recently received (i.e., within 14 days) preparations containing disulfiram or metronidazole (for dronabinol oral solution (Syndros(R)) as it contains 50% dehydrated alcohol and 5.5% propylene glycol).

Adverse reactions

The most common adverse reactions (>=3%) are abdominal pain, dizziness, euphoria, nausea, paranoid reaction, somnolence, abnormal thinking, and vomiting.

Precautions

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ICD codes

CodeTypeDescription
Anorexia from HIV
R63.0ICD10CMAnorexia
Cancer chemotherapy-induced nausea and vomiting
R11.2ICD10CMNausea with vomiting, unspecified
Z51.11ICD10CMEncounter for antineoplastic chemotherapy

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data