LOBELIA (Lobelia inflata L. +(Campanulaceae))

HERBAL

MEDICINE

PLANT

LOBELIA

(loe-beel’yuh)

Lobelia inflata L. +(Campanulaceae)

by

RETTODWIKART THENU

LOBELIA

(loe-beel’yuh)

Lobelia inflata L. + (Campanulaceae)

SUMMARY AND PHARMACEUTICAL COMMENT

The principal constituent of lobelia is lobeline, an alkaloid with similar pharmacological properties to those of nicotine. Lobelia has previously been used in herbal preparations for the treatment of asthma and bronchitis, and in anti-smoking preparations aimed to lessen nicotine withdrawal symptoms. However, in view of its potent alkaloid constituents, excessive use of lobelia and use during pregnancy and lactation should be avoided.

OTHER COMMON NAMES

Asthma weed, bladderpod, cardinal fl ower, emetic herb, gagroot, great lobelia, Indian pink, Indian tobacco, pukeweed, rapuntium inflatum, vomitroot, vomitwort

PHARMACOPOEIAL AND OTHER MONOGRAPHS

BHC 1992(G6)

BHP 1996(G9)

Martindale 35th edition(G85)

LEGAL CATEGORY (LICENSED PRODUCTS)

GSL(G37)

CONSTITUENTS

The following is compiled from several sources, including General Reference G6.

Alkaloids Piperidine-type. 0.48%. Lobeline (major); others include lobelanine, lobelanidine, norlobelanine, lelobanidine, norlelobanidine, norlobelanidine and lobinine.

Other constituents Bitter glycoside (lobelacrin), chelidonic acid, fats, gum, resin and volatile oil.

USES

Lobelia traditionally has been used to treat asthma, bronchitis, cough, and pneumonia, usually as an expectorant.

INVESTIGATIONAL USES

Researchers are studying lobelia for its cardiac effects and its antispasmodic effects in the gastrointestinal system. Its use as a smoking deterrent and treatment for psychostimulant abuse is also under investigation.

FOOD USE

Lobelia is not generally used as a food.

HERBAL USE

Lobelia is stated to possess respiratory stimulant, antasthmatic, antispasmodic, expectorant, and emetic properties. Traditionally, it has been used for bronchitic asthma, chronic bronchitis, and specifically for spasmodic asthma with secondary bronchitis. It has also been used topically for myositis and rheumatic nodules.(G6, G7, G8, G64)

ACTIONS

Lobelia is often used in combination with Capsicum frutescens (capsicum) and Symphlocarpus factida (skunk cabbage). Studies have focused on its use as a smoking deterrent and its emetic, cardiac, and expectorant properties.

Smoking Deterrent

Three of the chemical components of lobelia, lobeline, lobelanine, and lobelanidine, have properties similar to those of nicotine but generally are considered less potent. However, toxicity is higher with lobelia than with other traditional smoking deterrents currently on the market, such as nicotine transdermal systems (e.g., Nicoderm and Habitrol). The chemical components of lobelia inhibit smoking by fi rst stimulating nicotine receptors and then inhibiting them.

Emetic Action

The emetic action of lobelia results from stimulation of the chemoreceptor trigger zone. This action is similar to that of other emetics that are available. Lobelia also activates the vagal and afferent neural pathways responsible for vomiting.

Cardiovascular Action

Lobelia’s cardiac action results from both positive inotropic and chronotropic effects. Blood pressure and the neurotransmitters epinephrine and norepinephrine are increased in a manner similar to that seen with nicotine usage.

Expectorant Action

Lobelia is considered to be a very effective expectorant and has been used to treat respiratory conditions for many years. It causes bronchodilation.

Other Actions

Lobelia infl ata was found to functionally antagonize the neurochemical and behavioral effects of the psychostimulants amphetamine and methamphetamine (Dwoskin et al, 2002; Neugebauer et al, 2007).

ACTIVITIES

Analeptic (1; PH2); Antiasthmatic (1; CAN; CRC); Anticholinesterase (1; JAD); Antispasmodic (1; APA; CRC; HHB; PED); Antiviral (f; APA); CNS Stimulant (1; CAN); Convulsant (f; CRC); Diaphoretic (f; CRC; PNC); Diuretic (1; FNF; MAD; PED); Emetic (1; APA; CAN; WAM); Euphoric (f; CRC); Expectorant (1; APA; CAN; HHB; WAM); Laxative (f; PED); Myorelaxant (1; APA; FEL); Nervine (f; CRC; PED); Respirastimulant (1; CAN; PHR; PH2); Sedative (1; CRC; PED; WAM); Sialagogue (f; CRC; FEL); Stimulant (f; CRC); Tranquilizer (1; CRC).

Figure 1. Lobelia (Lobelia inflata).

INDICATIONS

Abscess (f; DEM); Acne (f; JLH); Addiction (1; CRC; PHR); Alcoholism (f; CRC; DEM); Alopecia (f; CRC); Alzheimer’s (1; JAD); Amenorrhea (f; CRC); Angina (f; CRC; FEL); Apoplexy (f; FEL); Asphyxia, neonatal (f; MAD); Asthma (1; APA; CAN; CRC; PHR; PH2); Atony (f; FEL); Bite (f; DEM); Boil (f; PNC); Bronchiectasis (f; MAD); Bronchosis (1; APA; CAN; CRC; HHB); Bruise (f; APA); Bug Bite (f; APA; PED); Cancer (f; CRC; JLH); Cancer, breast (f; CRC; JLH); Cardiopathy (f; APA; FEL); Catarrh (f; CEB; MAD); Chancre (f; DEM); Childbirth (f; CRC); Chorea (f; CRC; FEL); Cold (f; APA); Colic (f; DEM); Constipation (f; PED); Convulsion (f; CRC); Cough (1; CRC; FAD; WAM); Cramp (1; APA; CRC; FEL; HHB; MAD; PED); Croup (f; CRC); Deafness (f; CRC); Debility (f; CRC); Dermatosis (f; HHB); Diarrhea (f; CRC); Diphtheria (f; CRC); Divination (f; DEM); Dysentery (f; CRC); Dysmenorrhea (f; CRC; MAD); Dyspepsia (f; CRC; FEL; MAD); Dyspnea (f; MAD); Dysuria (f; CRC); Earache (f; CRC); Eczema (f; FEL); Emphysema (f; CRC); Encephalosis (f; MAD); Epilepsy (f; CRC; DEM; MAD); Erysipelas (f; CRC; FEL); Esophagosis (f; MAD); Faintness (f; CRC); Felon (f; JLH); Fever (f; CRC; FAD; PNC); Flu (f; APA); Gallstone  (f;CRC); Gastrosis (f; CRC; MAD); Hangover (f; CRC); Hay Fever (f; CRC; HHB); Headache (f; CRC; MAD); Heart (f; CRC); Hemorrhoid (f; CRC); Hepatosis (f; CRC; MAD); Hernia (f; CEB; CRC); Hydrophobia (f; CRC); Hyperemesis (f; MAD); Hypertony (f; MAD); Hysteria (f; CRC); Infection (f; MAD); Inflammation (f; FEL); Insomnia (1; CRC; PED; WAM); Jaundice (f; CEB; MAD); Laryngosis (1; FEL; PED); Measles (f; CEB); Meningosis (f; CRC); Morning Sickness (f; CRC); Morphinism (f; CRC); Mucososis (1; WAM); Myososis (f; PED); Narcosis (f; CRC); Nausea (f; CRC); Nephrosis (f; CRC); Nervousness (1; CRC; MAD; PED; WAM); Neuralgia (f; CRC; FEL; MAD); Neurasthenia (f; MAD); Nicotinism (1; CAN; CRC; PHR); Ophthalmia (f; CRC); Pain (1; CRC; DEM); Palpitation (f; CRC); Periostosis (f; CRC); Peritonosis (f; CRC); Pertussis (1; APA; CRC; HHB; PED); Phrenosis (f; CRC); Phthisis (f; DEM); Pleurisy (f; CRC); Pneumonia (f; CRC; FEL; MAD); Poison Ivy (f; APA; CRC; PED); Psoriasis (f; CRC); Pulmonosis (f; MAD); Respirosis (1; CRC; WAM); Rheumatism (f; FEL; PED); Ringworm (f; APA); Seborrhea (f; CRC); Shock (f; HHB); Shoulder (f; CRC); Smoking (1; PH2; PNC); Sore (f; DEM; PNC); Sore Throat (1; FAD; FEL); Spasm (f; CRC; FEL); Sprain (f; APA); Sting (f; DEM; FEL); Stomatosis (f; HHB); Tetanus (f; CEB; CRC; FEL); Tonsilosis (f; CRC); Tuberculosis (f; CEB); Typhoid (f; DEM); Urethrosis (f; CRC); Vaginosis (f; CRC); VD (f; DEM); Vertigo (f; MAD); Virus (f; APA); Wart (f; HHB; JLH); Water Retention (1; FNF; MAD; PED); Wen (f; CRC). Not covered by Commission E (KOM).

PRODUCT AVAILABILITY

Capsules, fl uid extract, lozenges, tablets, tincture; available in combination with cayenne pepper (Capsicum frutescens) and lungwort (Pulmonaria offi cinalis)

Plant Part Used: Dried leaves

DOSAGES

Smoking Deterrent

·         Adult PO tablets: the usual dosage is 2 mg taken with 4 oz water after meals for 6 wk

Other

·         Adult PO dried herb: 0.2-0.6 g tid

·         Adult PO fl uid extract: 8-10 drops tid (Pizzorno, Murray, 2006)

·         Adult PO tincture: 15-30 drops tid

Expectorant

·         Adult PO: 100 mg leaf or 0.6-2 ml tincture (Jellin et al, 2008)

DOSAGES

Dosages for oral administration (adults) for traditional uses recommended in older and contemporary standard herbal and/or pharmaceutical reference texts are given below.

·         Dried herb 0.2–0.6 g as an infusion or decoction three times daily.(G6, G7)

·         Liquid extract 0.2–0.6 mL (1 : 1 in 50% alcohol) three times daily.(G6, G7)

·         Simple Tincture of Lobelia (BPC 1949) 0.6–2.0 mL.

·         Tincture Lobelia Acid 1–4mL (1 : 10 in dilute acetic acid) three times daily.(G6, G7)

DOSAGES

100 mg leaf as expectorant (AHP); 2–6 tsp fresh leaf (PED); 1–3 g dry leaf (PED); 2 g dry leaf:10 ml alcohol/10 ml water (PED); 0.2–0.6 g herb, or in tea, 3 ×/day (CAN); 50–600 mg herb/day (HHB); maximum dose 100 mg dry herb up to 3 ×/day (MAD); 4–10 drops herb 3 ×/day with water or juice (NH); 0.2–0.6 ml liquid herb extract (1:1 in 50% ethanol) 3 ×/day (CAN); 0.6–2.0 ml herb tincture (BPC) (CAN); 1–4 ml lobelia tincture (1:10 in dilute acetic acid) (CAN); 10–20 drops (0.5–1 g) leaf tincture, up to several ×/day (MAD).

Figure 2. Lobelia – dried drug substance (herb).

PHARMACOLOGICAL ACTIONS

The pharmacological activity of lobelia can be attributed to the alkaloid constituents, principally lobeline. Lobeline has peripheral and central effects similar to those of nicotine, but is less potent. Hence, lobeline initially causes CNS stimulation followed by respiratory depression. Lobeline is also reported to possess expectorant properties.

Clinical studies

There is a lack of clinical research assessing the effects of lobelia and rigorous randomised controlled clinical trials are required.

SIDE-EFFECTS, TOXICITY

Side-effects of lobeline and lobelia are similar to those of nicotine and include nausea and vomiting, diarrhoea, coughing, tremors and dizziness. Symptoms of overdosage are reported to include profuse diaphoresis, tachycardia, convulsions, hypothermia, hypotension and coma, and may be fatal.(G45)

CNS: Tremors, dizziness, headache, anxiety, insomnia, seizures

CV: Palpitations, hypotension or hypertension

GI: Nausea, vomiting, anorexia, pain in abdomen, heartburn

INTEG: Hypersensitivity reactions

RESP: Cough, respiratory depression or stimulation

Toxicity: Seizures, nausea, vomiting, increased salivation, diarrhea, mental confusion, weakness, change in vision and hearing, respiratory depression, arrhythmias, tremors, hypothermia, coma, death

CONTRA-INDICATIONS, WARNINGS

The pharmacological actions of lobeline are similar to those of nicotine. Drug interactions None documented. However, the potential for preparations of lobelia to interact with other medicines administered concurrently, particularly those with similar or opposing effects, should be considered. The pharmacological activity of lobeline is similar to that of nicotine.

Pregnancy and lactation Lobelia should not be used during pregnancy or lactation.

Class 2b herb.

Until more research is available, lobelia should not be used during pregnancy and breastfeeding. It should not be given to children in large doses as an emetic. Lobelia should not be used by geriatric clients, or by persons with hepatic/renal disorders, pneumonia, nicotine sensitivity, or hypersensitivity to it. It should not be used by people who have cardiovascular disorders such as congestive heart failure, cardiac decompensation, sinus arrhythmias, valvular dysfunction, bundle branch block, or hypertension. Toxicity can result from the use of lobelia.

CONTRAINDICATIONS, INTERACTIONS, AND SIDE EFFECTS

Class 2b, 2d. May cause nausea and vomiting. Cardioactive (AHP; WAM). APA gives it their negative 5 rating, “definite health hazard to using this substance internally, even in recommended amounts.” I’d consider the risks of smoking versus the risk of lobeline and might opt for the lobeline, perhaps first trying transdermal lobelia plants taped to my arm. I’m not even keen on transdermal nicotine, but I find it perhaps healthier than smoking, and it doesn’t affect my neighbors with second-hand smoke. The alkaloid lobeline can cause cough, diarrhea, dizziness, nausea, tremors, and vomiting (CAN). Overdose may cause coma, convulsions, diaphoresis, hypotension, hypothermia, tachycardia, and even fatality. Because of lobeline and its toxicity, its use in pregnancy and lactation is to be avoided (CAN; WAM). 0.6–1 g leaf is toxic, 4 g fatal (PHR; PH2).“Health hazards not known with proper therapeutic dosages” (PH2) (but PH2 designates no specific quantified dosage! JAD).

Interactions

Drug     Nicotine: Lobelia increases the effects of nicotine-containing products; do not use concurrently.

Herb     Mayapple: Lobelia may decrease the laxative effect of mayapple.

CLIENT CONSIDERATIONS

Assess

·         Assess the reason the client is using lobelia.

·         Assess for hypersensitivity reactions. If present, discontinue the use of lobelia and administer an antihistamine or other appropriate therapy.

·         Assess for symptoms of toxicity: seizures, nausea, vomiting, increased salivation, diarrhea, mental confusion, weakness, change in vision and hearing, respiratory depression, arrhythmias, tremors, hypothermia, and coma.

·         Assess for the use of nicotine-containing products and mayapple (see Interactions).

Administer

·         Instruct the client to store lobelia products in a cool, dry place, away from heat and moisture.

·         Instruct the client to use lobelia for no more than 6 weeks for smoking cessation.

·         Administer atropine 2 mg subcut for acute toxicity.

Teach Client/Family

·         Caution the client not to give lobelia to children in large doses as an emetic, and not to use in those who are pregnant or breastfeeding until more research is available.

·         Warn the client to stop smoking before using lobelia as a smoking deterrent. Nicotine toxicity can occur.

PREPARATIONS

Proprietary multi-ingredient preparations

UK: Catarrh Tablets.

REFERENCE

Barnes, J., Anderson, LA, dan Phillipson, JD 2007. Obat Herbal Edisi Ketiga. Pers Farmasi. Auckland dan London.

Duke, JA dengan Mary Jo Bogenschutz-Godwin, Judi duCellier, Peggy-Ann K. Duke. 2002. Buku Pegangan Obat Herbal 2nd Ed. CRC Press LLC. AMERIKA SERIKAT.

Linda S-Roth. 2010. Mosby's Handbook Of Herbal & Suplemen Alami, Edisi Keempat. Mosby Elsevier. AMERIKA SERIKAT.