Scientific Name(s): Lobelia inflata L.
Common Name(s): Herba Lobellae Chinensis, Asthma weed, Bladderpod, Chinese Lobelia , Eyebright, Gagroot, Indian tobacco, Indian weed, Pukeweed, Vomitwort
L. inflata and its major alkaloid, lobeline, have been used in smoking cessation programs and have been proposed for treatment of other drug dependencies; however, clinical evidence is limited.
There is no recent clinical evidence to support the use of lobelia. The sale of OTC lobeline products for smoking cessation was prohibited by the US Food and Drug Administration (FDA) in 1993.
Traditional use of the leaf (eg, as an expectorant) suggests 100 mg of dry herb up to 3 times a day. However, there are no clinical trials to support this use. Doses of 0.6 to 1 g leaf are considered toxic, while 4 g of leaf is considered to be fatal.
Contraindications have not been defined; however, the sale of lobelia OTC products for smoking cessation is prohibited by the FDA due to a lack of efficacy and safety evidence.
Avoid use. Documented adverse effects, including loss of uterine tone and lack of safety evidence.
None well documented.
Lobelia and lobeline are capable of inducing nausea, vomiting, tremors, and dizziness at high doses. Lobelia alkaloids are cardioactive, and cardiotoxicities, including hypotension, tachycardia, and convulsion, have been reported. Contact dermatitis has also been reported.
Toxic dosages of the plant have been described: 1 g of leaf is toxic, while 4 g of leaf is considered to be a fatal dose. The alkaloid lobeline was not genotoxic or mutagenic in 1 study, and liver and kidney biochemistry in mice appeared unaffected.
L. inflata is a branching, perennial herb that is completely self-fertilizing and reproduces only once in its lifetime.1 It grows from 0.3 to 0.9 m tall and produces small, violet-pinkish flowers in the alternate leaf axils. The base of the flower expands to form the seed capsule, which is the source of the name "inflata." It is native to the eastern half of United States and parts of Canada.2, 3 The genus Lobelia has more than 400 recognized species, some of which contain alkaloids similar to those of L. inflata, including Livistona chinensis, a plant important in traditional Chinese medicine.3
The plant was named in honor of Matthias de Lobel, a 16th century Flemish physician and botanist, and is native to North America. American Indians smoked the leaves like tobacco and used them medicinally for respiratory ailments. Lobelia was introduced into New England medical practice in the 18th century to produce emesis. It was also used in treating colic, rheumatism, fever, and asthma. By the 19th century, lobelia was considered an important medicinal plant used in many conditions (eg, abscess, insomnia, tetanus, shock); however, fatalities were recorded due to dosing inconsistencies.4, 5 In 1993, the sale of lobelia OTC products for smoking cessation was prohibited by the FDA.3, 6, 7
The piperidine alkaloid lobeline was isolated as the main active component of Lobelia in 1921,8 and its absolute stereochemistry was determined in 1965.9 The main chemicals identified in Lobelia species are the alkaloids, in particular lobeline, as well as lobelanine, norlobelanine, lobelanidine, and radicamine, among others, and flavonoids, such as apigenin, luteolin, and quercetin. Other compounds include terpenes, alkynes, coumarins, and mineral elements.10, 11, 12 Lobeline concentration is highest in the seeds of the plant.13 Antiviral activity observed in L. chinensis has been attributed to lobechine and scoparone.14
Uses and Pharmacology
Lobeline has a high affinity for nicotinic acetylcholine receptors, and exhibits both agonist and antagonistic actions.13, 15, 16, 17 However, because a large diversity of nicotinic receptor subtypes have been identified, lobeline's actions are now thought to be only partly caused by agonism at nicotinic receptors, with some subtypes insensitive to lobeline.18, 19, 20 Similarly to nicotine, stimulation of respiration and bronchoconstriction have been observed with lobeline21; however, lobeline exhibits a slow off rate from receptors17 and probably acts via a different mechanism than does nicotine.13, 22 The effects of lobeline on N-methyl-D-aspartate,23 and [3H]5-HT,24 and norepinephrine25 release have been described. A review of potential mechanisms of action has been published.13
Experimental work has provided evidence that lobeline may be useful in the treatment of amphetamine abuse, based on the blockade of amphetamine-induced dopamine release in rat striatum, and the observed high affinity of lobeline for opioid receptors.13, 26 Lobeline attenuated the self-administration of amphetamine, methamphetamine, and heroin by rats.26, 27, 28, 29 In several rodent models, lobeline had a selective effect on amphetamine-induced behavior and neurochemistry.30 Limitations of lobeline may include the observation of self-administration in drug-naive mice,31 although disputed,13 and the fact that cross-tolerance to nicotine has been observed.15
There are no clinical data regarding the use of lobeline or lobelia extracts in management of psychostimulant abuse. The addiction liability of lobeline in humans has not been established.
Experiments in rodents and in vitro studies have produced equivocal results, possibly reflecting a diversity of experimental procedures, as well as actions of lobeline on receptor sites.13, 32, 33, 34
Lobeline was a component of OTC products for smoking cessation for many years. Results from clinical studies of the efficacy of lobeline have been mixed,35, 36, 37 and a meta-review found that none of the available studies were adequately controlled or of sufficient duration to prove its efficacy.38, 39 The FDA required the removal of lobeline products for smoking cessation from the market because of lack of demonstrated efficacy as part of its OTC review process in 1993.6
CNS, other effects
Experiments have shown lobeline to exert analgesic,40, 41 enhanced memory and learning,42, 43 antidepressant,44 and anxiolytic effects.5, 13, 45, 46 Lobeline has also been shown to reduce seizures in mice, possibly by increasing the levels of gamma-aminobutyric acid in the brain.47
A small study (N = 42) evaluated the effect of lobeline in attention deficit hyperactivity disorder (ADHD) compared with placebo and methylphenidate. No discernable difference could be found; however, the small study size could be responsible for the lack of effect.46 There are no clinical data on the use of lobeline in epilepsy.
Orally administered lobeline inhibited herpes simplex virus (HSV) 1 replication in mice (decreased HSV titre)48 and in vitro.14
Lobeline and extracts of L. chinensis have been studied in vitro and in rodents for anticancer activity. In mice, an extract of L. chinensis inhibited growth of liver and gastric cancers12 and reduced the number of precancerous colon lesions.49 In human cancer cell lines, lobeline showed potential in reversing P-glycoprotein transporter–dependent multidrug resistance.50
Lobeline was traditionally used for the management of respiratory conditions, such as pneumonia, asthma, and bronchitis, because it induces coughing and consequent expectorant action.5 With the development of more effective agents, use of lobelia became obsolete. However, a group of researchers reported on the effect of lobeline on juxtapulmonary receptors using intravenous (IV) bolus administrations.51
There is no recent clinical evidence to support the use of lobelia. The sale of OTC lobeline products for smoking cessation was prohibited by the US FDA in 1993.6
A study among patients with ADHD used daily doses of lobeline (salt form undefined) 7.5, 15, and 30 mg for 7 days.46 IV lobeline as a bolus has been used in limited clinical studies at doses of up to 100 mcg/kg (a mean dose of 45 mcg/kg [+/-23 mcg] produced a distinct dry cough).51
Traditional use of the leaf (eg, as an expectorant) suggests 100 mg of dry herb up to a maximum of 3 times a day.7 Doses of 0.6 to 1 g of leaf are considered toxic, while 4 g of leaf is considered to be fatal.7
Pregnancy / Lactation
Avoid use. Documented adverse effects, including loss of uterine tone,52 and lack of safety evidence.7
None well documented.
Lobelia and lobeline are capable of inducing nausea, vomiting, tremors, and dizziness at high doses (lobeline sulfate 8 mg).7 Respiratory effects have also been described; at high doses, lobeline can induce sensations of choking or breathlessness.51, 53 The lobelia alkaloids are cardioactive, and cardiotoxicities, including hypotension, tachycardia, and convulsion, have been reported.54, 55 Death from overdose has been recorded in historical literature; however, reports in the medical literature are lacking.3, 7 In 1993, sale of lobelia OTC products for smoking cessation was prohibited by the FDA due to a lack of efficacy and safety evidence.3, 6, 7, 38 Contact dermatitis has been reported.56
Toxic doses of the plant have been described (1 g of leaf as toxic, while 4 g of leaf is considered to be fatal).7 The alkaloid lobeline was not genotoxic or mutagenic in 1 study,57, 58 and liver and kidney biochemistry in mice appeared unaffected.57, 58
1. Hughes PW, Simons AM. Secondary reproduction in the herbaceous monocarp Lobelia inflata
: time-constrained primary reproduction does not result in increased deferral of reproductive effort. BMC Ecol
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2. Lobelia inflata
L. USDA, NRCS. 2015. The PLANTS Database (http://plants.usda.gov
, 1 April 2015). National Plant Data Team, Greensboro, NC 27401-4901 USA. Accessed April 1, 2015
3. Khan IA, Abourashed EA. Leung's Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics
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4. Bolyard JL. Medicinal Plants and Home Remedies of Appalachia
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5. Felpin FX, Lebreton J. History, chemistry and biology of alkaloids from Lobelia inflata
6. Food and Drug Administration, HHS. Drug products containing active ingredients offered over the counter (OTC) for use as a smoking deterrent. 2014 Apr 1;21(5):21CFR310.544
7. Duke J, Bogenschutz-Godwin M, duCellier J, Duke P. Handbook of Medicinal Herbs
. 2nd ed. Boca Raton, FL: CRC Press; 2003.
8. Wieland H. Alkaloids of the lobelia plant (preliminary communication). Chem Ber
9. Schöpf C, et al. Absolute configuration of (-)-lobeline and of its reduction products. Ann Chem
10. Duke J. Dr. Duke's phytochemical and ethnobotanical databases. http://www.ars-grin.gov/duke/
. Accessed April 1, 2014.
11. Yang S, Shen T, Zhao L, et al. Chemical constituents of Lobelia chinensis
12. Chen MW, Chen WR, Zhang JM, Long XY, Wang YT. Lobelia chinensis
: chemical constituents and anticancer activity perspective. Chin J Nat Med
13. Dwoskin LP, Crooks PA. A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse. Biochem Pharmacol
14. Kuo PC, Hwang TL, Lin YT, Kuo YC, Leu YL. Chemical constituents from Lobelia chinensis
and their anti-virus and anti-inflammatory bioactivities. Arch Pharm Res
15. Flammia D, Dukat M, Damaj MI, Martin B, Glennon RA. Lobeline: structure-affinity investigation of nicotinic acetylcholinergic receptor binding. J Med Chem
16. Damaj MI, Patrick GS, Creasy KR, Martin BR. Pharmacology of lobeline, a nicotinic receptor ligand. J Pharmacol Exp Ther
17. Kaniakova M, Skrenkova K, Adamek S, Vyskocil F, Krusek J. Different effects of lobeline on neuronal and muscle nicotinic receptors. Eur J Pharmacol
18. Decker MW, Brioni JD, Bannon AW, Arneric SP. Diversity of neuronal nicotinic acetylcholine receptors: lessons from behavior and implications for CNS therapies. Life Sci
19. Parker MJ, Beck A, Luetje CW. Neuronal nicotinic receptor beta2 and beta4 subunits confer large differences in agonist binding affinity. Mol Pharmacol
20. Briggs CA, McKenna DG. Activation and inhibition of the human alpha7 nicotinic acetylcholine receptor by agonists. Neuropharmacology
21. Klide AM, Aviado DM. Carotid receptors and bronchomotor responses. Effects of cigarette smoke, lobeline, and cyanide. Arch Environ Health
22. Teng L, Crooks PA, Sonsalla PK, Dwoskin LP. Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake. J Pharmacol Exp Ther
23. Rao TS, Correa LD, Lloyd GK. Effects of lobeline and dimethylphenylpiperazinium iodide (DMPP) on N-methyl-D-aspartate (NMDA)-evoked acetylcholine release in vitro: evidence for a lack of involvement of classical neuronal nicotinic acetylcholine receptors. Neuropharmacology
24. Lendvai B, Sershen H, Lajtha A, Santha E, Baranyi M, Vizi ES. Differential mechanism involved in the effect of nicotinic agonists DMPP and lobeline to release [3H]5-HT from rat hippocampal slices. Neuropharmacology
25. Sántha E, Sperlágh B, Zelles T, et al. Multiple cellular mechanisms mediate the effect of lobeline on the release of norepinephrine. J Pharmacol Exp Ther
26. Hart N, Rocha A, Miller DK, Nation JR. Dose-dependent attenuation of heroin self-administration with lobeline. J Psychopharmacol
27. Harrod SB, Dwoskin LP, Crooks PA, Klebaur JE, Bardo MT. Lobeline attenuates d-methamphetamine self-administration in rats. J Pharmacol Exp Ther
28. Nickell JR, Siripurapu KB, Vartak A, Crooks PA, Dwoskin LP. The vesicular monoamine transporter-2: An important pharmacological target for the discovery of novel therapeutics to treat methamphetamine abuse. Adv Pharmacol
29. Neugebauer NM, Harrod SB, Stairs DJ, Crooks PA, Dwoskin LP, Bardo MT. Lobelane decreases methamphetamine self-administration in rats. Eur J Pharmacol
30. Miller DK, Crooks PA, Teng L, et al. Lobeline inhibits the neurochemical and behavioral effects of amphetamine. J Pharmacol Exp Ther
31. Rasmussen T, Swedberg MD. Reinforcing effects of nicotinic compounds: intravenous self-administration in drug-naive mice. Pharmacol Biochem Behav
32. Benwell ME, Balfour DJ. The influence of lobeline on nucleus accumbens dopamine and locomotor responses to nicotine in nicotine-pretreated rats. Br J Pharmacol
33. Lecca D, Shim I, Costa E, Javaid JI. Striatal application of nicotine, but not of lobeline, attenuates dopamine release in freely moving rats. Neuropharmacology
34. Tani Y, Saito K, Imoto M, Ohno T. Pharmacological characterization of nicotinic receptor-mediated acetylcholine release in rat brain—an in vivo microdialysis study. Eur J Pharmacol
35. Grabowski J, Hall SM. Tobacco use, treatment strategies, and pharmacological adjuncts: an overview. NIDA Res Monogr
36. Schuster CR, Lucchesi BR, Emley GS. The effects of d-amphetamine, meprobamate, and lobeline on the cigarette smoking behavior of normal human subjects. NIDA Res Monogr
37. Plakun Al, Ambrus J, Bross I, Graham S, Levin ML, Ross CA. Clinical factors in smoking withdrawal: preliminary report. Am J Public Health Nations Health
38. Stead LF, Hughes JR. Lobeline for smoking cessation. Cochrane Database Syst Rev
39. Glover ED, Rath JM, Sharma E, et al. A multicenter phase 3 trial of lobeline sulfate for smoking cessation. Am J Health Behav
40. Khan IM, Stanislaus S, Zhang L, Taylor P, Yaksh TL. A-85380 and epibatidine each interact with disparate spinal nicotinic receptor subtypes to achieve analgesia and nociception. J Pharmacol Exp Ther
41. Damaj MI, Fei-Yin M, Dukat M, Glassco W, Glennon RA, Martin BR. Antinociceptive responses to nicotinic acetylcholine receptor ligands after systemic and intrathecal administration in mice. J Pharmacol Exp Ther
42. Vicens P, Bernal MC, Carrasco MC, Redolat R. Effects of lobeline on spatial learning in C57BL mice. Neurosci Res Commun
43. Levin ED. Nicotinic agonist and antagonist effects on memory. Drug Dev Res
44. Roni MA, Rahman S. The effects of lobeline on nicotine withdrawal-induced depression-like behavior in mice. Psychopharmacology (Berl)
45. Roni MA, Rahman S. The effects of lobeline on depression-like behavior and hippocampal cell proliferation following chronic stress in mice. Neurosci Lett
46. Martin CA, Nuzzo PA, Ranseen JD, et al. Lobeline effects on cognitive performance in adult ADHD. J Atten Disord
47. Tamboli AM, Rub RA, Ghosh P, Bodhankar SL. Antiepileptic activity of lobeline isolated from the leaf of Lobelia nicotianaefolia
and its effect on brain GABA level in mice. Asian Pac J Trop Biomed
48. Kuo YC, Lee YC, Leu YL, Tsai WJ, Chang SC. Efficacy of orally administered Lobelia chinensis
extracts on herpes simplex virus type 1 infection in BALB/c mice. Antiviral Res
49. Han SR, Lv XY, Wang YM, et al. A study on the effect of aqueous extract of Lobelia chinensis
on colon precancerous lesions in rats. Afr J Tradit Complement Altern Med
50. Ma Y, Wink M. Lobeline, a piperidine alkaloid from lobelia can reverse P-gp dependent multidrug resistance in tumor cells. Phytomedicine
51. Anand A, Roy A, Bhargava B, Raj H, Barde PB, Vijayan VK. Early symptom-relief after valvulotomy in mitral stenosis indicates role of lobeline-sensitive intrapulmonary receptors. Respir Physiol Neurobiol
52. Ernst E. Herbal medicinal products during pregnancy: are they safe? BJOG
53. Butler JE, Anand A, Crawford MR, et al. Changes in respiratory sensations induced by lobeline after human bilateral lung transplantation. J Physiol
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55. Dangerous supplements: What you don't know about these 12 ingredients could hurt you. Consum Rep
56. Idriss MH, Lovell C, Woldeyes M. Occupational irritant contact dermatitis caused by Lobelia richardii
in an Ethiopian flower farm. Contact Dermatitis
57. da Costa E Silva LD, Rodrigues LC, Dos Santos VR, et al. Evaluation of mutagenic and genotoxic activities of lobeline and its modulation on genomic instability induced by ethanol. Life Sci
58. Verde Rodrigues LC, Decker N, Picada JN, Pereira P. Neurotoxicological profile assessment of lobeline after acute treatment in mice. Basic Clin Pharmacol Toxicol
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