Review on Methylxanthine, Theobromine and Theophylline

 

Mr. Ritik S. Jain, Miss. Shital I. Rathod, Mr. Paresh A. Patil, Mr. Dipesh R. Karnavat

Department of Organic Chemistry, Ahinsa Institute of Pharmacy Dondaicha Dist. Dhule.

*Corresponding Author E-mail: ritikbadera390@gmail.com

 

ABSTRACT:

Theobromine, formely known as xantheose is a bitter alkaloid of the cacao plant, with the chemical formula C7H8N4O2. It is found in chocolate, as well as in a number of other foods, including the leaves of tea plant, and the kola nut. Theophylline also known as 1,3-dimethylxanthine, is a methylxanthines drug used in therapy for respiratory diseases such as chronic obstructive pulmonary diseases (COPD) and asthma under a variety of brand name. Methylxanthine is also derivative of xanthenes. These all three are mostly present in tea, and these chemical have some effective property related with respiratory tract disorder.

 

KEYWORDS: Methylxanthine, Theobromine, theophylline, xanthose, immuno-modulatory action.

 

 

 

 

INTRODUCTION:

Theobromine, diuretics drugs and major alkaloidal constituent of cocoa. Theobromine is a xanthine alkaloid[7].

 

Therapeutics Uses of Theobromine:

1.       Theobromine is associated with increases in energy and urine production and the potential to shield heart health and airways.[1]

2.       In a study of 21 young adults with asthma, theobromine capsule increases bronchial diameter, which increased airflow to the lungs.[1}

3.       It can reduce the levels of inflammatory cytokines such as IFN-y and TNF-a.[1]

4.       Human molars (teeth) were more protected when treated with theobromine solution.[1]

5.       In people with gout, crystals of uric acid salts build up in the join which can trigger severe pain and inflammation. In test tubes, theobromine prevented uric acid crystallization.[1]

6.        Theobromine may cause blood pressure to decrease by widening the blood vessels and stimulating urination.[1]

7.       Theobromine extracted from cacao inhibits the buildup of uric acid crystals, which may form kidney stones. Since theobromine is a diuretics, it may also increasing urine flow.[1]

8.       About 30mg theobromine supplements contributed to staying asleep for a long period.[1]

9.       Theobromine may raise HDL (High-Cholesterol Level) is referred to as “good cholesterol”.[4]

10.    In one study involving 24 healthy female subjects, participants reported strong feeing of calmness after ingesting 700mg of theobromine.[4]

 

General Introduction of Methylxanthines:

Methylxanthines are naturally occurring alkaloids in several foods and beverages all over the world as well as in some veterinary and human medications [8]. Methylxanthines are alkaloids that can be found in high concentration in tea, coffee and chocolate.[9]In comparison with theobromine caffeine has less effect on cardiac stimulation and coronary artery dilation[13].

 

Therapeutics Uses of Methylxanthines:

1.       Methylxanthines, acting on adenosine receptors in the central nervous system, enhance arousal mood and concentration levels.[2]

2.       The main pharmacological effects of methylxanthines include central nervous system stimulation, diuresis, cardiovascular and metabolic effects, bronchial relaxation and increased secretion of gastric acids.[2]

3.       Methylxanthines relax airways and vascular smooth muscle and as mentioned earlier, a relationship can be observed between PDE inhibition by methylxanthine and relaxation of airways smooth muscles.[3]

4.       Methylxanthines have vasodilatory, Anti-inflammatory and immunomodulatory actions[11].

5.       The potential effects of methylxanthine are numerous, controversial and of uncertain importance[11].

6.       Methylxanthines increases chemo-receptor sensitivity as well as respiratory drive and can also improve diaphragmatic contractility[12].

7.       Skeletal muscles are stimulated more by caffeine than by other methylxanthines[12].

 

General Introduction of Theophylline:

Theophylline is a naturally occurring occuring alkaloid closely related to caffeine. The pharmacologic actions of theophylline include stimulation of respiration, augmentation of cardiac inotropy and chronotropy, relaxation of smooth muscle including that in te bronchi and the blood vessels and other than cerebral vessels and diuresis.[6]

 

Therapeutics Uses of Theophylline:

1.       Theophylline is widely prescribed drugs for the treatment of asthma and chronic obstructive pulmonary diseases (COPD).[5]

2.       It was also used as diuretics.[5]

3.       Theophylline increases the activity and number of suppressor T-cells and reduces the activity of many inflammatory cells implicated in asthma[10].

4.       For IV administration aminophylline (Containing 85% anhydrous theophylline by weight) is used because of its greater aqueous solubility[10].

5.       Theophylline increases the forces and rate contraction of cardiac muscle through it’s effect on CAMP, but also causes arterial vasodilation by inhibiting the breakdown of CGMP[11].

6.       Theophylline is a potent antagonist at adenosine A1, A2 and A3 receptors and may reduce broncho-constriction by this mechanism[11].

7.       The action of theophylline on HDAC may potentiate the anti-inflammatory effects of costicosteroids[11].

 

REFERENCE:

1.        Review article on “Theobromine Benefits, side effects and dosage by Jonathan Ritter, PuyaYazdi and AlekshaRistic publish by “Selfhacked”, Publish on 3-Jan-2020.

2.        Article on “Health Benefits of Methylxanthines in cacao and chocolate by Rofaelfranco, AihnhoaOnotibia-Astibia and Eva Martinez-Pinilla.

3.        Article on Effect of Theophylline and Non-selective xanthine derivatives on PDE Isoenzymes and cellular function by Gordon Dent, Klaus F. Rabe.

4.        Article on Theobromine: Benefits and Side-effects of Cocoa’s Interesting Phytochemical by Michael Joseph on August 13, 2018.

5.        Article on Theophylline by Peter.J. Barnes published by American Journal of Respiratory and Critical Care Medicine, Volume 188, Issue 8.

6.        Article on “Dosage of theophylline in bronchial asthma” by Kenneth.M. Piafsky and Richard. I. Ogilvie published by “The New England Journal of Medicine”

7.        Article on “Theobromine “Written by “The Editor of Encyclopaedia Britannica” and published by “Britannica”.

8.        Article on Pharmaceuticals by Konnie. H. Plumlee, , In Clinical Veterinary Toxicology, -2004.

9.        Article on “Nootropics, functional foods and dietary patterns for prevention of Cognitive decline”, by Francesco Bonetti, Giovannizuliani, “Nutrition and functional foods for healthy Aging-2017.

10.     Article on “Airway pharmacology” by David.R. Ball, Barry.E. Mcguire, in Benum and Hegberg’s Airway Management- 2013.

11.     Article on “Asthma and chronic obstructive pulmonary diseases” by Derek.G. Waller and Anthony.P. Sampson, published by “Medical Pharmacology and Therapeutics, Fifth edition-2018.

12.     Article on “Apnea of prematurity, sudden Infant Death Syndrome and apparent life – Threatening Events, by Christian.F. Poets, published by Pediatric Respiratory Medicine, second edition-2008.

13.     Article on “Methylxanthines” by Linda.K. Dolder, Small Animal Toxicology, Third edition-2013.

 

 

 

Received on 01.07.2020       Modified on 24.07.2020

Accepted on 02.08.2020      ©Asian Pharma Press All Right Reserved

Asian J. Pharm. Ana. 2020; 10(3): 173-174.

DOI: 10.5958/2231-5675.2020.00031.9