Caffeine-Pharmacology and other info by DrugsInfo

It's is all you need to know about caffeine. All the information available in this ppt, made by authenticated sources. That is following evidence-based medicine process.

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1. All you need to know about the Caffeine Information through Evidence-Based Medicine Prepared By: Akash Agnihotri

2. All you need to know about the Caffeine Part-5 Nutritional facts for some brands that contains caffeine Part-4 Pregnancy Considerations Mechanism of action Pharmacokinetics Facts Part-3 Health Effects continue Labeled uses Off-label uses Adverse Reactions Contraindications Part-2 Pharmacological Effects Health Effects Part-1 General Info Effects Consumption and Content Metabolism Physiology

3. Caffeine: General Info Caffeinated coffee and tea are the most consumed, socially accepted stimulants in the world. Approximately 90 percent of all adults in the world consume caffeine daily. In their natural forms, coffee and tea contain several chemical components that may confer both beneficial and adverse health effects, including caffeine and antioxidants ( eg , polyphenols, catechins, and flavonoids).

4. Caffeine: Effects Caffeine has multiple systemic effects on the neuropsychiatric, cardiovascular, endocrine, and gastrointestinal systems. The impact on health may be modified by genetic factors, age, sex, medications, and other environmental exposures.

5. Caffeine: Consumption & Content For most adults, consumption of up to 400 mg of caffeine a day appears to be safe (as per FDA) Table: Caffeine Content of Commercially Available Energy Drinks in the Indian Market Table: Nidhi Bedi et al., Indian Pediatr 2014;51: 529-533 https://www.indianpediatrics.net/july2014/july-529-533.htm

6. Caffeine: Content in soft drinks Source: https://www.uptodate.com/contents/benefits-and-risks-of-caffeine-and-caffeinated-beverages?search=caffeine%20in%20bevarages&source=search_result&selectedTitle=1~150&usage_type=default&display_rank=1

7. Caffeine: Content in Chocolates Source: https://www.uptodate.com/contents/benefits-and-risks-of-caffeine-and-caffeinated-beverages?search=caffeine%20in%20bevarages&source=search_result&selectedTitle=1~150&usage_type=default&display_rank=1

8. Caffeine: In children and adolescents Wikoff D, Welsh BT, Henderson R, et al. Systematic review of the potential adverse effects of caffeine consumption in healthy adults, pregnant women, adolescents, and children.  Food Chem Toxicol . 2017;109(Pt 1):585-648. doi:10.1016/j.fct.2017.04.002 Limited data are available about safe levels of caffeine consumption in children and adolescents. A systematic review found that intake of 2.5 mg caffeine/kg of body weight per day is not associated with adverse effects

9. Caffeine: Metabolism Caffeine is rapidly absorbed in the gastrointestinal tract and undergoes demethylation in the liver via the enzyme cytochrome P450 1A2 (CYP1A2) Defects in the CYP1A2 enzyme are associated with impaired caffeine metabolism and prolonged caffeine half-life

10. Caffeine: Physiology Caffeine is a potent antagonist of central and peripheral nervous system adenosine receptors, thereby stimulating the release of excitatory neurotransmitters The behavioral effects of caffeine are attributed to its effects on adenosine receptors

11. All you need to know about the Caffeine Information through Evidence-Based Medicine Part-2 Pharmacological Effects Health Effects

12. Caffeine: Pharmacological effects Chlorogenic acid, found in both coffee and black tea, raises homocysteine concentrations in plasma In addition, polyphenols in coffee such as caffeic acid and chlorogenic acid inhibit DNA methylation in a dose-dependent manner, which prevents downregulation of tumor suppressor proteins and DNA repair enzymes involved in carcinogenesis

13. Caffeine: Pharmacological effects Diterpenoids in unfiltered coffee may raise plasma low-density lipoprotein (LDL) cholesterol and lower high-density lipoprotein (HDL) cholesterol Induction of detoxifying enzymes ( eg , glutathione S-transferase) that protect against oxidative insults has been identified in vitro studies with rat liver cells exposed to coffee

14. Caffeine: Pharmacological effects Unidentified compounds in coffee, other than caffeine, activate the sympathetic system and may increase blood pressure. This effect is brief and occurs primarily in non-habitual coffee drinkers. Several other antioxidants in coffee, cocoa, and teas may contribute to beneficial effects. Antioxidants do pass through coffee filters.

15. Caffeine: Health effects 1. Cognitive/neuropsychiatric I n rested individuals, caffeine in low and moderate doses, approximately 30 to 300 mg , improves vigilance and reaction time In sleep-deprived individuals, caffeine's positive effects generalize to a wide variety of functions, including learning and decision-making and real-world activities such as automobile and aircraft operation Individuals who are habitual consumers of coffee and tea perform better on various tests of cognitive performance, such as reaction time and visuospatial reasoning

16. Caffeine: Health effects 2. Alertness Caffeine consumption leads to increased alertness, mental energy , and ability to concentrate, particularly when subjects are fatigued or working at night This is probably the fundamental reason why so many humans regularly consume caffeine.

17. Caffeine: Health effects 3. Headache Caffeine has significant pharmacologic properties that can alleviate or generate headache symptoms . Caffeine has long been used for its analgesic properties in the treatment of headache and is frequently used alone or in combination with other medications . Randomized trials have found that combination medications that include caffeine ( aspirin ,  acetaminophen , and caffeine) are more effective for tension and migraine headaches than acetaminophen or low-dose  ibuprofen  alone. Goldstein J, Silberstein SD, Saper JR, Ryan RE Jr, Lipton RB. Acetaminophen, aspirin, and caffeine in combination versus ibuprofen for acute migraine: results from a multicenter, double-blind, randomized, parallel-group, single-dose, placebo-controlled study.  Headache . 2006;46(3):444-453. doi:10.1111/j.1526-4610.2006.00376.x Diener HC, Gold M, Hagen M. Use of a fixed combination of acetylsalicylic acid, acetaminophen and caffeine compared with acetaminophen alone in episodic tension-type headache: meta-analysis of four randomized, double-blind, placebo-controlled, crossover studies. J Headache Pain. 2014;15(1):76. Published 2014 Nov 19. doi:10.1186/1129-2377-15-76

18. Caffeine: Health effects 3. Headache Habitual caffeine consumption is associated with chronic migraine and analgesic rebound headache. In a case-control study, patients with daily caffeine consumption were more likely to have chronic migraines (odds ratio [OR] 2.9, 95% CI 1.5-5.3) and analgesic rebound headaches (OR 2.2, 95% CI 1.2-3.9) than patients who did not regularly consume caffeine. Headaches are the most common symptom of caffeine withdrawal.

19. All you need to know about the Caffeine Information through Evidence-Based Medicine Part-3 Health Effects continue Labeled uses Off-label uses Adverse Reactions Contraindications

20. Caffeine: Health effects 4. Parkinson disease A meta-analysis found evidence of a dose-response relationship between coffee or tea intake and decreased risk for Parkinson disease. The mechanism of how caffeine might protect against Parkinson disease is not known . Hernán MA, Takkouche B, Caamaño-Isorna F, Gestal -Otero JJ. A meta-analysis of coffee drinking, cigarette smoking, and the risk of Parkinson's disease.  Ann Neurol . 2002;52(3):276-284. doi:10.1002/ana.10277

21. Caffeine: Health effects 5. Alzheimer disease There are very few studies examining the relationship between coffee and Alzheimer disease. In a pooled analysis of two cohort and two case control studies on coffee and Alzheimer disease, coffee consumption was associated with a small protective effect against Alzheimer disease (relative risk [RR] 0.70, 95% CI 0.55-0.90)  Barranco Quintana JL, Allam MF, Serrano Del Castillo A, Fernández- Crehuet Navajas R. Alzheimer's disease and coffee: a quantitative review.  Neurol Res . 2007;29(1):91-95. doi:10.1179/174313206X152546

22. Caffeine: Health effects 6. Cardiovascular Low to moderate coffee consumption (up to three cups per day) may protect against myocardial infarction. Heavy coffee intake may trigger coronary and arrhythmic events in susceptible individuals, although coffee intake is not considered a long-term risk factor for myocardial disease.

23. Caffeine: Label Uses Caffeine citrate:   Treatment of apnea of prematurity. Caffeine [OTC labeling]:   Helps restore mental alertness or wakefulness when experiencing drowsiness or fatigue.

24. Caffeine: Off-Label Uses Augmentation of seizure induction during electroconvulsive therapy (caffeine and sodium benzoate) Postdural puncture headache (caffeine and sodium benzoate) Reversal of dipyridamole- or regadenoson -induced adverse reactions ( eg , angina, hypotension) during nuclear cardiac stress testing (alternative agent)

25. Caffeine: Adverse Reactions The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified (1% to 10%): Dermatologic: Skin rash (9%) E pidermal thinning (2%) X eroderma (2%) Endocrine & metabolic: Acidosis (2%) Gastrointestinal: Gastritis (2%), gastrointestinal hemorrhage (2%)

26. Caffeine: Contraindications Hypersensitivity to caffeine or any component of the formulation; sodium benzoate is not for use in neonates. OTC labeling :  When used for self-medication, do not use in children <12 years of age or as a substitute for sleep.

27. All you need to know about the Caffeine Information through Evidence-Based Medicine Part-4 Pregnancy Considerations Mechanism of action Pharmacokinetics Facts

28. Caffeine: Pregnancy Considerations Caffeine crosses the placenta Serum concentrations in the fetus are similar to those in the mother Breastfeeding considerations Caffeine and its metabolites are present in breast milk 

29. Caffeine: Mechanism of action Increases levels of 3'5' cyclic AMP by inhibiting phosphodiesterase CNS stimulant which increases medullary respiratory center sensitivity to carbon dioxide, stimulates central inspiratory drive, and improves skeletal muscle contraction (diaphragmatic contractility) P revention of apnea may occur by competitive inhibition of adenosine

30. Caffeine: Pharmacokinetics Distribution : V d : Neonates: 0.8 to 0.9 L/kg. Adults: 0.6 L/kg. Protein binding : 36%. Metabolism : Hepatic, via demethylation by CYP1A2 Half-life elimination : Neonates : 72 to 96 hours. Infants ≥9 months, Children, Adolescents Adults : 5 hours.

31. Caffeine: Pharmacokinetics Time to peak, serum : Preterm neonates: Oral: 30 minutes to 2 hours. Caffeine is absorbed into the blood and tissues within about 45 minutes of being consumed Excretion: Neonates: Urine (86% unchanged). Infants ≥9 months, Children, Adolescents, and Adults: Urine (1% unchanged).

32. Caffeine: Facts Death from too much caffeine is rare, but possible In rare instances, when caffeine is consumed at high enough doses (typically in excess of 5 grams in adults — the amount in about 30 to 50 cups of coffee ), it can kill.

33. Caffeine: Facts Caffeine withdrawal is a real condition In the latest version of the psychology handbook "Diagnostic and Statistical Manual of Mental Disorders" (DSM-5), caffeine withdrawal is listed as a mental health condition . The text describes the effects seen in some people who abruptly stop or dramatically cut back on their daily use of caffeine

34. Caffeine: Facts Caffeine resembles a brain chemical Caffeine has a similar molecular structure to adenosine , a neurotransmitter (a substance that transmits nerve impulses in the brain). Because of its chemical resemblance to adenosine, caffeine can bind to adenosine receptors in brain cells. I t blocks the sleep-inducing actions of adenosine and speeds up nerve cell activity. This causes a person to  feel temporarily more awake  and energetic.

35. Caffeine: Facts Caffeine can be found in unusual places These days, consumers might notice caffeine in some unexpected places. People can purchase caffeine-infused bottled water, jelly beans, breath mints, peanut butter and chewing gum. E ven caffeinated bath soaps that supposedly help wake people up in the morning, also added to shampoos In addition, caffeine is in some weight-loss products and dietary supplements . It may be listed on the label as guarana, kola nut, yerba mate, green tea extract or green coffee bean extract, according to the National Institutes of Health.

36. Caffeine: Facts Coffee beans come from a red fruit Coffee comes from shrubs, known as coffee cherries, that produce a red berry when ripe. The actual  coffee beans , which are green, are found inside the coffee cherries. 

37. All you need to know about the Caffeine Information through Evidence-Based Medicine Part-5 Nutritional facts for some brands that contains caffeine

38. Caffeine: Nutrition Facts: Some Brands Caffeine- 50mg/sachet

39. Caffeine: Nutrition Facts: Some Brands Caffeine- 72mg/bottle (250ml)

40. Caffeine: Nutrition Facts: Some Brands Caffeine- 75mg/Can (250ml)

41. Caffeine: Nutrition Facts: Some Brands Caffeine- 61.5mg/Bottle (250ml) Pepsi (354ml can)- 38mg caffeine Coca-Cola (354ml can)- 34mg caffeine

42. Thanks for Reading Part-5 Nutritional facts for some brands that contains caffeine Part-4 Pregnancy Considerations Mechanism of action Pharmacokinetics Facts Part-3 Health Effects continue Labeled uses Off-label uses Adverse Reactions Contraindications Part-2 Pharmacological Effects Health Effects Part-1 General Info Effects Consumption and Content Metabolism Physiology Information through Evidence-Based Medicine Comment your drug which you want info in next post

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