Clinical trials on Sativex: Sativex MS, Sativex Cancer And Possible Sativex benefits for Other Conditions
Sativex Contraindications
Sativex Side Effects. Warnings & Precautions. Does Sativex Get You High?
Sativex Dosage
How To Get a Sativex Prescription
Sativex. I like to see herbal- based prescription drugs like this on the market. They are proving the power of herbs with modern, well design scientific studies. Yes, there are quite a few studies on Sativex and a lot more research in progress.
I also like this format, as a prescription medicine, and being recommended in a specific dosage. This is how everyone should treat marijuana- as a medicine. You should avoid recreational marijuana, or overusing it in any way. If you live in one of those 25+ countries where Sativex already got the regulatory approval for MS-related spasticity and cancer-related pain I am sure you want to know more about it. It is currently under FDA evaluation, as well. If Sativex is not available where you live, but you have access to medical marijuana, you can still look at this drug’s profile- simply because you could get its equivalent from a cannabis clinic.
Something I noticed…. Even if this drug is available (in a country like Canada, for example), it won’t be easy to get it prescribed, because many doctors/specialists are still hesitant to explore this option. I will give you some tips at the end of the article. For now, let’s look at the health benefits of Sativex.
2.Sativex: How It Works (Mechanisms Of Action)
Sativex’ key ingredients are THC and CBD (1:1 ratio), but also contains other minor cannabinoids and non-cannabinoid compounds. It comes in a spray formula, so the active ingredients are absorbed in the mouth. Non -medicinal ingredients include alcohol (ethanol anhydrous), propylene glycol and peppermint oil.
A quick note here: a very smart choice to use this drug in spray form. The mucosa of the mouth has a rich blood supply, allowing this drug to be well absorbed in the body. In addition, this route allows for more precision in self-titration. It’s a win-win.
Why does it work? Well, the reason why medical marijuana has so many effects on humans is very simple: we have a built-in system called the endocannabinoid system (ECS) that the plant cannabinoids can interact with. I wrote in details about the endocannabinoid system here and in more details here
CB1 receptors are found in the brain/spinal cord in some peripheral tissues including nerves, adrenals, heart, lung, reproductive tissues, urinary bladder, gastrointestinal and immune cells. CB1 receptors are more abundant in the brain areas related to motor function, cognition, and memory. Regarding pain modulation: CB1 receptors are found on pain pathways in the brain and spinal cord, and peripheral nervous system. CB2 receptors are found mainly on peripheral and central immune cells, being involved in immune system modulation. THC activates (is an agonist of) CB1 and CB2 receptors. CBD mainly works on another receptor called TRPV-1 (vanilloid) receptor. Technical: CBD is an agonist of TRPV-1 receptor with inhibitory action on adenosine uptake.
3.The effects of THC and CBD (based on animal studies):
THC effects: analgesic (pain killer), muscle relaxant, anti emetic (anti-vomiting), appetite stimulant and of course, has those well known psychoactive effects.
CBD effects: analgesic, anticoagulant (anti-seizure) muscle relaxant, anti-anxiety, neuroprotective, anti-oxidant and anti psychotic activity. CBD helps counteract the psychoactive effects of THC. Technical: THC is metabolized to 11-OH-THC, a psycho-active metabolite. The main primary metabolite of CBD is 7-OH-CBD.
4.Clinical trials on Sativex
As of May 2019, there are over 40 clinical trials on Sativex published on Pub med, and other studies in progress. The key areas of research are related to its benefits for MS and cancer
Sativex for the treatment of MS-related spasticity
An extensive review (2017) of the last decade of clinical studies on Sativex for MS concluded that “ Sativex was proven effective in treating spasticity and also in improving the patient’s quality of life”. In addition, this review found Sativex to be well tolerated and have a good safety profile.
Sativex was found to reduce spasticity by 20% in one large placebo-controlled randomized study. The participants of this study had to be either on a standard anti-spasticity drug or had been tried but failed to benefit from standard anti-spasticity medication. Another randomized study showed a pain (neuropathic pain) reduction of at least 50% in 48% of the participants treated with SATIVEX®, compared with 12% of the placebo group. (Sativex Monograph)
Sativex seems to be safe and well tolerated long term, too. One study evaluates its effects over a 3-4 years period. This drug was well tolerated, the most common side effects include dizziness and fatigue, especially at the beginning of treatment. Another fact observed by scientists is that if improvements are not seen in the first four weeks, you are unlikely to respond better in the future, and therefore treatment should be stopped.
Sativex may help manage other symptoms related to MS. For example, one study found Sativex to be effective in improving overactive bladder symptoms in MS.
There is a case report of improved trigeminal neuralgia with Sativex use, too.
Sativex for treating cancer-related pain.
Sativex can be used as an add on therapy in individuals with advanced cancer who do not get enough pain relief from the highest tolerated dose of strong opioid drugs. One randomized study found an improvement of more than 30% in pain score was in 43% of patients on SATIVEX® (vs 21% in the placebo group).
We will see more studies on Sativex because cannabis has quite a few potential benefits for people with cancer: besides pain relief, cannabis may help nausea associated with chemotherapy, stimulate the appetite and improve sleep. In addition, lab/animal studies suggest that cannabis has anti-cancer effects (inhibiting the tumor growth, cutting off the blood supply of the tumor, and even suppressing stem cancer cells, and prevent cancer metastasis)
Sativex may also work with anti-cancer drug temozolomide to manage glioma (a form of brain cancer)
Other possible benefits of Sativex
Sativex may help manage withdrawal symptoms in chronic cannabis smokers who quit (symptoms like irritability, insomnia, decreased appetite, depressed mood, anxiety, and restlessness)
One case study showed significant improvement in motor and vocal tics associated with the Tourette syndrome.
5.Sativex Contraindications
SATIVEX® is contraindicated in those:
with known or suspected allergy to a cannabinoid or to the other ingredients found in this drug (propylene glycol, ethanol or peppermint oil)
Those with serious cardiovascular disease (ie ischemic heart disease, arrhythmia, poorly controlled hypertension or severe heart failure)
Those with a history of schizophrenia or any other psychotic disorder
children under 18
women of child-bearing potential who do not use a reliable contraceptive or men intending to start a family
pregnant or nursing women
Cautions in those with a history of epilepsy/ recurrent seizures
Sativex Side Effects. Warnings & Precautions
THC can cause dependence and has the potential for being abused. Possible side effects include changes of mood, decrease in cognitive performances and memory, decrease in the ability to control drives and impulses, and alteration of the perception of reality (especially time sense). Other possible side effects: fainting, dizziness (the most frequent side effect documented, and is dose related) Sativex should be discontinued in certain cases (ie if confusion, disorientation, psychotic reaction, suicidal ideation develop). Other possible adverse reactions may involve cardio-vascular system: tachycardia, and transient changes in blood pressure (including postural hypo tension).
Does Sativex get you high ? The chances to get high are low, because the THC: CBD ratio is about 1:1 (marijuana strains that get you high have much higher doses of THC). However, do not drive after using Sativex. Sativex may impair the mental and/or physical abilities needed for driving a car/ operating machinery, you do need to keep this in mind. Check out page 16 of Sativex monograph how Sativex compared with placebo to affect the nervous system and/or cause psychiatric disturbances. For example “feeling abnormal” occurred in 2.4% in Sativex group vs 0.4 % in the placebo group, amnesia in 1.1% in Sativex group vs 0.3% placebo group.
In addition, Sativex has additive/synergistic effects with other CNS depressants (ie opioids, GABA inhibitors, sedative/hypnotics, and alcohol)
Possible drug-drug interactions: THC and CBD are metabolized by the Cytochrome P450 enzyme system. Sativex may interact with amitriptyline, fentanyl, and the related opioids ketoconazole rifampicin
No interactions had been documented with foods or herbs
Sativex Dosage
Sativex dosage will vary from one person to another. You will have to work with your doctor to determine the right dosage for you. On the first day, the dose will be one spray in the morning and one in the afternoon or evening. The following days the dose will increase by one spray each day as needed and tolerated.
The median number of daily spray in routine clinical practice is 4, and in clinical studies, for MS the median number of daily sprays was 8. The maximum dose is 12 sprays per day if needed. You should leave at least 15 minutes between 2 successive sprays.
No issues around missed doses, as Sativex is a self-titration regime to be used “as needed”.
Signs of overdose: in clinical studies, some individuals developed symptoms after using 18 sprays in 20 minutes — these side effects were similar with intoxication with cannabis/THC: depression, anxiety, paranoia, delusions, hallucinations, and/or psychosis. These symptoms resolved within 24 hours. The estimated lethal human dose of intravenous THC is 30 mg/kg (2100 mg for a 70 kg person).
How To Get a Sativex Prescription
If you have MS or cancer, want to learn more, and possibly use Sativex, you will need to follow a few steps.
You need a referral from a family doctor to see a specialist (neurologist) from a MS (or cancer clinic). Make sure you print this document (Sativex monograph) to have your doctor review it and discuss the benefits/safety of this drug for you.
Have another copy of the monograph for Sativex handy for your trip to the specialist. Since not all specialists are open to prescribing (or even research) Sativex, you will need to play a bit the detective role- check patients online forums, as people from the clinic (ie nurses or secretaries can be very helpful) to recommend you a specialist who does see benefits from using Sativex.
You should also consider the price. Sativex is more expensive than medical marijuana. If you choose to use medical marijuana instead, make sure you have again the Sativex documents with you. You can ask the cannabis specialist to match the key ingredients’ ratio with the ration found in Sativex (THC: CBD- about 1:1).
