MARINOL®(dronabinol) Capsules


Introduction

Marinol is the brand name for dronabinol, synthetic delta-9-tetrahydrocannabinol (delta-9-THC).1
Delta-9-THC is a naturally occuring cannabinoid primarily produced by marijuana plants. Marinol is primarily used as an appetite stimulant to treat patients suffering from AIDS-related anorexia, and also as an antiemetic to treat nausea and vomiting associated with cancer chemotherapy.

DESCRIPTION:
Dronabinol, the active ingredient in MARINOL® Capsules, is synthetic delta-9-tetrahydrocannabinol (delta-9-THC). Delta- 9-tetrahydrocannabinol is also a naturally occurring component of Cannabis sativa L. (Marijuana).

Dronabinol is a light yellow resinous oil that is sticky at room temperature and hardens upon refrigeration. Dronabinol is insoluble in water and is formulated in sesame oil. It has a pKa of 10.6 and an octanol-water partition coefficient: 6,000:1 at pH 7.

Capsules for oral administration: MARINOL® Capsules is supplied as round, soft gelatin capsules containing either 2.5 mg, 5 mg, or 10 mg dronabinol. Each MARINOL® Capsule is formulated with the following inactive ingredients: FD&C Blue No. 1 (5 mg), FD&C Red No. 40 (5 mg), FD&C Yellow No. 6 (5 mg and 10 mg), gelatin, glycerin, methylparaben, propylparaben, sesame oil, and titanium dioxide.

- Marinol Prescribing Information1

My only encounter with Marinol was through a friend of mine in high school. I had known that Marinol was supposed to get you high, but I was still doubtful as to its recreational value. It was hard to believe that with the government's nefarious record if spreading propaganda and outright lies about marijuana that it would approve the commercial sale of basically a cannabis extract to the terminally ill, and one that would get them high as well. I mean, if getting high was harmful for a healthy individual, how could it be good for someone debilitated by AIDS or cancer?

Still, I decided to take 15mg(3 5mg pills) before a concert and expected to recieve very little effect from it. However, the dronabinol kicked in in about half an hour after I took the pills, and I was suprisingly intoxicated. I found myself completely baked without having smoked any weed, which was a very strange sensation as I'd always associated the cannabis high with the act of smoking.

In my opinion, there's very little difference between the high from smoking weed and from taking marinol, the main difference being that marinol takes much longer to take effect. And when you take price into consideration, Marinol is hardly worth what it costs for the consumer. Marinol is sold for about $9/5mg pill. I paid $5 per 5mg pills from my friend, and even then I could have gotten much more bang for the buck had I bought actual pot. For this reason, I believe it would be extremely hard for Unimed Pharmaceuticals to market their product if marijuana was actually legal to grow and consume. In fact, a good amount of patients who switch from medical marijuana to marinol complain about marinol being much less effective, especially for the cost of the prescriptions.

Clearly it does not cost $9 to synthesize 5mg of dronabinol, and it would make much more sense economically for patients to just grow their own pot for their own consumption. So maybe this is just another case of business corporations exploiting consumers with the help of the law.


Clinical Pharmacology

Although Cannabis contains many active cannabinoids (including delta-9-tetrahydrocannabinol, cannabinol, cannabidiol, cannabinolidic acid, cannabigerol, and cannabichromene), delta-9-THC is commonly accredited for most of the psychoactive effects of Cannabis.
Marinol's effects are described in its clinical documentation as:

A cannabinoid dose-related “high” (easy laughing, elation and heightened awareness) -1
In other words, Marinol gets you stoned.

I've heard of a lot of people claiming that the high they get from Marinol is completely different from that of smoking weed and although I cannot corroborate this with my own experiences, as I felt very much the same way on Marinol as I did on pot, it is very possible that for some people there are significant differences in the high they experience. This is due to the fact that there are many other active ingredients in Cannabis other than tetrahydrocannabinol. The presence of different levels of different cannabinoids in each strain of Cannabis contributes to each strain producing a slightly different high unique to itself. The absence of these other cannabinoids in Marinol is likely to be much more apparent in individuals that are perhaps more sensitive to the effects of these cannabinoids.


Effects

Marinol is orally active and has complex effects on the central nervous system (CNS). Specifically, Marinol demonstrates reversible effects on the following CNS functions1:

Patients using Marinol also demonstrate trends towards:
  • improved body weight
  • improved mood
  • decreases in nausea
These effects have been observed to be dose-related, increasing in frequency with higher dosages, and subject to great interpatient variability.1

As it would be expected, Marinol's effects are nearly identical to that of consuming Marijuana. What is peculiar, is that all of the pharmacological characteristics that give cannabis its recreational value are categorized by studies as "side-effects," or signs of overdose. I guess this categorization reinforces the criminality and social disapprobation of recreational drug use.

I believe that if clinical studies were conducted objectively, without pressure from a society which already made its judgements on cannabis prematurely, then physiological effects such as "heightened sensory awareness," euphoria, and positive mood changes would probably be touted benefits proclaimed as theraputic qualities rather than as signs of overdose or as negative side-effects.


Pharmacodynamics

Dronabinol works within the endocannabinoid system by binding to cannabinoid receptors, primarily, the CB1- and CB2-receptors. Little is known about the function of CB2-receptors, but CB1-receptors have been found in high concentrations in the following regions of the brain, thus influencing the specific mental processes handled by these regions:

This activation of cannabinoids receptors produces the following clinical effects5:
  1. Appetite Stimulation
    • Cannabinoids active receptor to maintain food intake
    • Hormone leptin regulates appetite and endocannabinoids
  2. Nausea/Vomiting Reduction

Chronology of action1:

  • onset action - 0.5 to 1 hours
  • peak duration - 2 to 4 hours
  • duration of psychoactive effects - 4 to 6 hours
  • duration of appetite stimulation - 24 hours+
Chronic use leads to the development of Tachyphylaxis and tolerance to some of the pharmacologic effects of dronabinol and other cannabinoids. Clinical studies have also shown that patients develope tolerance to cardiovascular and subjective adverse CNS effects of dronabinol within 12 days of treatment initiation. Tachyphylaxis and tolerance do not, however, appear to develop to the appetite stimulation effect of dronabinol.1

Dronabinol and its principal active metabolite, 11-OH-delta-9-THC, are present in approximately equal concentrations in plasma. Concentrations of both reach a peak level at approximately 2 to 4 hours after oral administration and decline over several days.
The two part elimination phase of dronabinol can be broken down as follows1:
  1. initial (alpha) half-life - 4 hours
  2. terminal (beta) half-life - 25 to 36 hours
Following single dose administration, low levels of dronabinol metabolites have been detected for more than 5 weeks in the urine and feces.1


Dosage

The recommended starting dose for anorexia associated with weight loss due to AIDS is 2.5 mg BID (twice-a-day) before lunch and supper. In the treatment of nausea and vomiting associated with cancer chemotherapy, the recommended starting dose is 5 mg/m2 administered one to three hours prior to chemotherapy, then every two to four hours after chemotherapy, for a total of four to six doses/day.4

Recreational dosages are naturally much higher than the recommended dosage. In my experience 15mg is a sufficient amount for someone who has low THC tolerance. However, for most pot smokers who have developed a high tolerance to THC, 25mg is probably the optimal starting dosage. And be patient, since Marinol is orally administered, it will take up to an hour to take effect depending on your body, and how much food you have in your stomach. Don't get impatient after waiting only 45 minutes to redose yourself only to find out 15 minutes later that your original dose was already more than you can handle.


Side Effects/Adverse Effects

Some personal commentary:
In what kind of fascist society is feeling good considered an adverse effect? Oh yea, ours. And "exaggerated happiness?"--the word "exaggerated" suggests that something is increased to an abnormal degree, or is represented as greater than the actual case. So who determines the normative level of happiness that one should experience? Is there such a thing as being TOO happy? And if there were such a thing, is it really an issue we ought to be concerned with in a world which seems to be overwhelmingly plagued by unhappiness?

Additionally, thinking "abnormally" is also listed here as an adverse effect implying that unconventional thought is undesirable. And once again, who determines what is normal thinking? Maybe charging patients with terminal illnesses extortionate prices for a synthetic version of something that occurs naturally in marijuana plants, which are cheap and easy to grow, is abnormal thinking. Some might even say this goes beyond abnormal, and extends into immoral and opportunistic. I guess this is just another "side effect" of capitalism.

Overdose
Signs and symptoms following MILD MARINOL® (Dronabinol) Capsules intoxication include1: Signs and symptoms following MODERATE intoxication1: Signs and symptoms following SEVERE intoxication1: As with the use of any psychedelic, using Marinol also comes with the acute psychological risk of paranoia, and panic/anxiety attacks. However, if you are a habitual pot smoker and have been acustomed to functioning under the influence of marijuana, you will have no problem functioning on Marinol. And as noted above, these side effects are reversible and usually subside once the high wears off in 4-5 hours. Chronic use may cause marginal memory impairment for up to a month after discontinued use.

In any case, it is not recommended that you drive or operate heavy machinery while under the influence of Marinol. In order to make any progress towards societal acceptance of recreational drug use, recreational drug users need to make an active effort towards being informed about the drugs they partake in, and always exercise moderation and safe judgement in their use of recreational drugs.


Legal Status

Dronabinol is a schedule III substance and is classified as a hallucinogen. Oddly enough marijuana, a naturally occuring form of delta-9-THC with arguably superior clinical effects and is prefered by most patients, is a schedule I substance that the U.S. government does not recognize as having any accepted use in medical treatment.

So what are the differences between Marinol and Marijuana that might account for this scheduling difference? Consider these points:

  • The effects produced by the mixture of different cannabinoids produced by Marijuana plants is prefered by most patients to the effects of the isolated delta-9-THC in Marinol.
  • Marijuana is cheap and easy to grow and harvest
  • Marinol is much more expensive to produce
  • Marijuana is widely available from many different sources and can be grown by anyone
  • Marinol is a patented drug which is only produced by Solvay Pharmaceuticals
And although Solvay Pharmaceuticals has isolated the naturally occuring THC from the rest of the other active cannabinoids in Marijuana, the effects of the illicit plant drug, and the effects of its pharmaceutical counter-part are nearly identical. So what is the point of paying all that extra cost for the isolated, and arguably inferior, synthetic? My opinion--none.

It's also interesting to note that government studies on Marijuana describe very different effects produced by the very same tetrahydrocannabinol that dronabinol is in fact an exact copy of(the only difference being that one is produced naturually by a plant, and the other is synthesized by a pharmaceutical company in factories). Marinol clearly demonstrates one of the great disparities in the U.S. government's drug policies.

Sources:

  1. Unimed Pharmaceuticals, inc. 2003. MARINOL® 3 (Dronabinol) Capsules. 5000412 4E. Revision 5/2003. <http://www.marinol.com/pdfs/MARINOLPI.pdf> (18 Sept. 2004).
  2. Erowid. 15 Jan. 2002. Cannabis Basics. <http://www.erowid.org/plants/cannabis/cannabis_basics.shtml> (18 Sept. 2004).
  3. Erowid. 5 Aug. 2004. Cannabis Legal Status. <http://www.erowid.org/plants/cannabis/cannabis_law.shtml> (18 Sept. 2004).
  4. Unimed Pharmaceuticals, inc. MARINOL® (dronabinol) Capsules CIII Brand Fact Sheet. <http://www.marinol.com/pdfs/FactSheet.pdf> (18 Sept. 2004).
  5. Unimed Pharmaceuticals, inc. Cannabinoid Science: The Neurobiology of MARINOL® (dronabinol) CIII Capsules. <http://www.marinol.com/ppt/MOA.pdf> (18 Sept. 2004).

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