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Levonantradol

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Last Updated: 13 November 2020

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General | Latest Info

Levonantradol

Chemical and physical data
(verify)
3D model ( JSmol )Interactive image
FormulaC 27 H 35 N O 4
Molar mass437.580 gmol 1
Clinical data
ATC codenone
Identifiers
CAS Number71048-87-8 Y
ChemSpider4514867 Y
CompTox Dashboard ( EPA )DTXSID80221271
PubChem CID5361881
UNII03S640ADSK

Double-blind administration of single intramuscular dose of 1. 5 2. 0 2. 5, or 3. 0 mg Levonantradol or placebo to 56 patients with moderate to severe postoperative or trauma pain show significant analgesic effects of each dose of Levonantradol as compared to placebo. However, no significant dose response was observe. Compared to 2 / 16 patients on placebo, 23 / 40 patients on Levonantradol report one or more side effect. Drowsiness was most frequent. Dry mouth, dizziness, weird dreams, mild hallucinations, nervousness, apprehension and confusion occur less frequently. Changes in resting heart rate and blood pressure were minor and general acceptability was good.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Treatment

Levonantradol, new antiemetic compound pharmacologically related to cannabinoids, was given to 17 patients who had experienced severe and protracted nausea and vomiting during previous courses of cancer chemotherapy, and to six patients receiving first course of strongly emetic cytostatic treatment. Eight patients were partially protected from acute gastrointestinal disturbances. Of 23 patients, 21 exhibited some toxicity, with six patients exhibiting major affective side-effects and 13 patients complaining of pain at the injection site. Levonantradol is an active antiemetic compound. Due to the rate of side-effects observed in our study, however, we would not recommend use of this agent as an antiemetic drug. T1-Levonantradol, new antiemetic with high rate of side-effects for prevention of nausea and vomiting in patients receiving cancer chemotherapy n2-Levonantradol, new antiemetic compound pharmacologically related to cannabinoids, was given to 17 patients who had experienced severe and protracted nausea and vomiting during previous courses of cancer chemotherapy, and to six patients receiving first course of strongly emetic cytostatic treatment. Eight patients were partially protected from acute gastrointestinal disturbances. Of 23 patients, 21 exhibited some toxicity, with six patients exhibiting major affective side-effects and 13 patients complaining of pain at the injection site. Levonantradol is an active antiemetic compound. Due to the rate of side-effects observed in our study, however, we would not recommend use of this agent as an antiemetic drug. AB-Levonantradol, new antiemetic compound pharmacologically related to cannabinoids, was given to 17 patients who had experienced severe and protracted nausea and vomiting during previous courses of cancer chemotherapy, and to six patients receiving first course of strongly emetic cytostatic treatment. Eight patients were partially protected from acute gastrointestinal disturbances. Of 23 patients, 21 exhibited some toxicity, with six patients exhibiting major affective side-effects and 13 patients complaining of pain at the injection site. Levonantradol is an active antiemetic compound. Due to the rate of side-effects observed in our study, however, we would not recommend use of this agent as an antiemetic drug.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Primate models of Parkinson disease

In cynomolgus monkeys, cannabinoid agonist levonantradol decreases general and locomotor activity and increases bradykinesia, while tetrahydrocannabinol increases bradykinesia only. Rimonabant, however, had no significant effects compared with vehicle. Moreover, authors find that rimonabant fail to alleviate motor deficits in the early and advanced stage of MPTP-induced parkinsonism. In MPTP-marmoset model, 9-THC improved locomotor activity and hand-eye coordination performance. In l-DOPA-prim MPTP-treat rhesus monkeys with moderate and severe parkinsonism, selective CB1 antagonism increased duration responses to l-DOPA by 30 %. In same model, systemic administration of rimonabant displayed antiparkinsonian actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

2.1.2 Effects of Medicinal Cannabinoids

Table 5: Published Positive, Randomized, Double-Blind, Placebo-Controlled, Clinical Trials on Smoked/Vapourized Cannabis and Associated Therapeutic Benefits

Primary medical conditions and associated secondary end-points (if any) for which benefits were observedPercent and dose of 9 -THC (if known)Trial duration; and number of patients/participantsReference
HIV/AIDS-associated weight lossOne cannabis cigarette (~800 mg) containing 1.8% or 3.9% THC by weight, smoked once daily (i.e. one dose per day) (~14 - 31 mg 9 -THC /day)8 sessions total (3 sessions per week); 30 participantsReference 224
HIV/AIDS-associated weight loss; disease-associated mood and insomniaOne cannabis cigarette (~800 mg) containing 2.0% or 3.9% THC by weight, smoked four times per day (i.e. four doses per day) (~64 - 125 mg of 9 -THC /day)4 days total; 10 participantsReference 223
Multiple sclerosis-associated pain and spasticityOne cannabis cigarette (~800 mg) containing 4% THC by weight, smoked once per day (i.e. one dose per day) (~32 mg 9 -THC /day)3 days total; 30 patientsReference 278
Central and peripheral chronic neuropathic pain (various etiologies)One cannabis cigarette (~800 mg) containing either 3.5% or 7% THC by weight, smoked in bouts over a 3 h period (i.e. one dose per day) (daily dose of THC unavailable)1 day total; 38 patientsReference 222
Chronic neuropathic pain from HIV-associated sensory neuropathyOne cannabis cigarette (~900 mg) containing 3.56% THC by weight, smoked three times daily (i.e. three doses per day) (~96 mg 9 -THC /day)5 days total; 25 patientsReference 195
HIV-associated chronic neuropathic pain refractory to other medicationsOne cannabis cigarette (~800 mg) containing between 1 and 8% THC by weight, smoked four times daily (i.e. four doses per day) (daily dose of THC unavailable)5 days total; 28 patientsReference 281
Chronic post-traumatic or post-surgical neuropathic pain refractory to other medications and associated insomniaOne 25 mg dose of cannabis containing 9.4% THC by weight, smoked three times daily (i.e. three doses per day) (~7 mg 9 -THC /day)5 days total; 21 patientsReference 59
Chronic pain of various etiologies (musculoskeletal, post-traumatic, arthritic, peripheral neuropathy, cancer, fibromyalgia, migraine, multiple sclerosis, sickle cell disease, thoracic outlet syndrome)One 900 mg dose of vapourized cannabis containing 3.56% THC by weight administered three times per day (one dose the first day, three doses per day for next three days, one dose the last day) (~96 mg 9 -THC /day)5 days total; 21 patientsReference 280
Neuropathic pain of various etiologies (spinal cord injury, complex regional pain syndrome (CRPS) type I, causalgia-CRPS type II, diabetic neuropathy, multiple sclerosis, post-herpetic neuralgia, idiopathic peripheral neuropathy, brachial plexopathy, lumbosacral radiculopathy, and post-stroke neuropathy)Inhalation of vapourized cannabis (800 mg) containing either a low (1.29% or 10.3 mg 9 -THC) or a medium-dose of 9 -THC (3.53% 9 -THC or 28.2 mg 9 -THC)3 sessions total; 39 patientsReference 598
Crohn's diseaseOne cannabis cigarette (500 mg) containing 23% THC by weight, smoked twice daily (i.e. two doses per day) (23 mg 9 -THC /day)8 weeks; 21 patientsReference 603
Neuropathic pain of various etiologiesInhalation of a single vapourized dose of 15 mg dried containing 20% 9 -THC by weight (~3 mg 9 -THC)One session only; 10 patientsReference 58
Diabetic peripheral neuropathy (i.e. diabetes mellitus type I and II)Inhalation of single vapourized doses of dried cannabis (400 mg/dose) containing either low (1% 9 -THC or 4 mg 9 -THC), medium (4% 9 -THC or 16 mg 9 -THC) or high (7% 9 -THC or 28 mg 9 -THC) doses of 9 -THC (four single dosing sessions; each separated by two weeks)4 sessions total; 16 patientsReference 599
Neuropathic pain from spinal cord injury or diseaseInhalation of between 8 and 12 puffs from 400 mg of dried cannabis (2.9% and 6.7% THC)3 sessions total; 42 patientsReference 276

Treatment with synthetic cannabinoids has also been linked to transient psychotic symptoms Dronabinol, nabilone and Levonantradol have been used to manage pain syndromes, chemotherapy-induce nausea and spasticity from multiple sclerosis. Patients being treated with these synthetic cannabinoids have reported experiencing transient psychotic symptoms, such as loss of control, think disturbances, feelings of unreality, apprehension, fear and paranoia, anxiety and panic, dissociation, depersonalization, dysphoria, difficulty concentrating, hallucinations, perceptual alterations, amnesia and anxiety. Severity of these symptoms appear to be dose-dependent and dependent on affinity of compound for CB-1R receptor. In fact, Levonantradol, which has 30 times higher affinity for CB-1R receptor than 9-THC and was being developed as analgesic agent, had to be abandoned from further drug development because of high incidence of intolerable behavioral side effects. In two systematic reviews of randomized clinical trials that examined the efficacy of synthetic cannabinoids for chemotherapy-induced nausea and vomiting, use of these synthetic cannabinoids led to hallucinations in 6 % of patients, paranoia in 5 % of patients, and was responsible for nearly 30 % of dropouts, primarily because of intolerable behavioral effects. Importantly, in these trials, hallucinations and paranoia were seen exclusively with cannabinoids, and not with other antiemetic agents. These effects appear to increase both with increasing potency, dose and with repeat dosing.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

1 Introduction

Table 5: Published Positive, Randomized, Double-Blind, Placebo-Controlled, Clinical Trials on Smoked/Vapourized Cannabis and Associated Therapeutic Benefits

Primary medical conditions and associated secondary end-points (if any) for which benefits were observedPercent and dose of 9 -THC (if known)Trial duration; and number of patients/participantsReference
HIV/AIDS-associated weight lossOne cannabis cigarette (~800 mg) containing 1.8% or 3.9% THC by weight, smoked once daily (i.e. one dose per day) (~14 - 31 mg 9 -THC /day)8 sessions total (3 sessions per week); 30 participantsReference 224
HIV/AIDS-associated weight loss; disease-associated mood and insomniaOne cannabis cigarette (~800 mg) containing 2.0% or 3.9% THC by weight, smoked four times per day (i.e. four doses per day) (~64 - 125 mg of 9 -THC /day)4 days total; 10 participantsReference 223
Multiple sclerosis-associated pain and spasticityOne cannabis cigarette (~800 mg) containing 4% THC by weight, smoked once per day (i.e. one dose per day) (~32 mg 9 -THC /day)3 days total; 30 patientsReference 278
Central and peripheral chronic neuropathic pain (various etiologies)One cannabis cigarette (~800 mg) containing either 3.5% or 7% THC by weight, smoked in bouts over a 3 h period (i.e. one dose per day) (daily dose of THC unavailable)1 day total; 38 patientsReference 222
Chronic neuropathic pain from HIV-associated sensory neuropathyOne cannabis cigarette (~900 mg) containing 3.56% THC by weight, smoked three times daily (i.e. three doses per day) (~96 mg 9 -THC /day)5 days total; 25 patientsReference 195
HIV-associated chronic neuropathic pain refractory to other medicationsOne cannabis cigarette (~800 mg) containing between 1 and 8% THC by weight, smoked four times daily (i.e. four doses per day) (daily dose of THC unavailable)5 days total; 28 patientsReference 281
Chronic post-traumatic or post-surgical neuropathic pain refractory to other medications and associated insomniaOne 25 mg dose of cannabis containing 9.4% THC by weight, smoked three times daily (i.e. three doses per day) (~7 mg 9 -THC /day)5 days total; 21 patientsReference 59
Chronic pain of various etiologies (musculoskeletal, post-traumatic, arthritic, peripheral neuropathy, cancer, fibromyalgia, migraine, multiple sclerosis, sickle cell disease, thoracic outlet syndrome)One 900 mg dose of vapourized cannabis containing 3.56% THC by weight administered three times per day (one dose the first day, three doses per day for next three days, one dose the last day) (~96 mg 9 -THC /day)5 days total; 21 patientsReference 280
Neuropathic pain of various etiologies (spinal cord injury, complex regional pain syndrome (CRPS) type I, causalgia-CRPS type II, diabetic neuropathy, multiple sclerosis, post-herpetic neuralgia, idiopathic peripheral neuropathy, brachial plexopathy, lumbosacral radiculopathy, and post-stroke neuropathy)Inhalation of vapourized cannabis (800 mg) containing either a low (1.29% or 10.3 mg 9 -THC) or a medium-dose of 9 -THC (3.53% 9 -THC or 28.2 mg 9 -THC)3 sessions total; 39 patientsReference 598
Crohn's diseaseOne cannabis cigarette (500 mg) containing 23% THC by weight, smoked twice daily (i.e. two doses per day) (23 mg 9 -THC /day)8 weeks; 21 patientsReference 603
Neuropathic pain of various etiologiesInhalation of a single vapourized dose of 15 mg dried containing 20% 9 -THC by weight (~3 mg 9 -THC)One session only; 10 patientsReference 58
Diabetic peripheral neuropathy (i.e. diabetes mellitus type I and II)Inhalation of single vapourized doses of dried cannabis (400 mg/dose) containing either low (1% 9 -THC or 4 mg 9 -THC), medium (4% 9 -THC or 16 mg 9 -THC) or high (7% 9 -THC or 28 mg 9 -THC) doses of 9 -THC (four single dosing sessions; each separated by two weeks)4 sessions total; 16 patientsReference 599
Neuropathic pain from spinal cord injury or diseaseInhalation of between 8 and 12 puffs from 400 mg of dried cannabis (2.9% and 6.7% THC)3 sessions total; 42 patientsReference 276

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Sources

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

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