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Community pharmacy Topic: 2 part(1) Vitamins supplements 1 Vitamins • They are complex organic compounds required by the body in very small amounts. They are concerned with vital metabolic function in the body, and hence essential for maintenance of health. • Since vitamins can not be manufactured in body, they have to be supplied through the diet. 2 • Vitamins are classified into two major groups: 1. Fat soluble vitamins: A, D,E,K 2. Water soluble vitamins: B complex and C (ascorbic acid)… 3 Ref: 4Food and Vitamins and Supplements! Oh My! Demystifying nutrition: the value of food, vitamins and supplements, Harvard Medical School, 2013 IU mg 5 mcg • Dietary supplement containing multiple vitamins for children and adults Recommended doses classification 1. Recommended Dietary Allowance (RDA): • average daily level of intake sufficient to meet the nutrient requirements of nearly all (97%–98%) healthy individuals. 2. Adequate Intake (AI): • established when evidence is insufficient to develop an RDA and is set at a level assumed to ensure nutritional adequacy. 7 3. Estimated Average Requirement (EAR): • average daily level of intake estimated to meet the requirements of 50% of healthy individuals. It is usually used to assess the adequacy of nutrient intakes in population groups but not individuals. 4. Tolerable Upper Intake Level (UL): • maximum daily intake unlikely to cause adverse health effects. 8 • International unit (IU) • Standard measure of the biological activity (biological effect) of manufactured medicinal drugs and vitamins. • For every substance to which this unit is assigned, there is an internationally accepted biological effect expected with a dose of 1 IU. • - Ex: 1 IU = 0.3 microgram (0.0003 milligram) of vitamin-A 50 micrograms (0.050 milligram) of vitamin-C 25 nanograms (0.000025 milligram) of vitamin-D. Vitamin A • VITAMIN A: Retinol, retinal, and retinoic acid — two forms of vitamin A in the body are: - preformed vitamin A (retinol and its esterified form, retinyl ester) - Alpha,Beta carotene can easily be converted to vitamin A as needed. 10 In pregnancy Teratogenic in excessive amounts Avoid multivitamins containing vitamin A like fish liver oils • Benefits: 1. Vision: - Essential component of rhodopsin ( protein that absorbs light in the retinal receptors) - It supports the normal differentiation and functioning of the conjunctival membranes and cornea - Foods rich in the carotenoids may protect against cataracts 2. Skin: Keeps tissues and skin healthy. 3. Bone: Plays an important role in bone 11growth. 4. Cancer: Diets rich in the carotenoids alpha carotene and lycopene seem to lower lung cancer risk. 5. Antioxidants : Carotenoids. 6. Body system: • supports cell growth and differentiation, • playing a critical role in the normal formation • Maintenance of the heart, lungs, kidneys • involved in immune function, reproduction 12 Recommended amount (daily RDA or daily AI) • Because the body converts all dietary sources of vitamin A into retinol, 1 mcg of physiologically available retinol is equivalent to the following amounts from dietary sources: - 12 mcg of beta-carotene - 24 mcg of alpha-carotene. • Vitamin A is listed on food and supplement labels in international units 13 (IUs). • Converting from RAE to IU depend on vit A type • From dietary supplements, the body converts 2 mcg of beta-carotene to 1 mcg of retinol. • 1 IU retinol = 0.3 mcg RAE • Ex: the RDA of 900 mcg RAE for adolescent and adult men is equivalent to 3,000 IU if the food or supplement source is preformed vitamin A (retinol) • Multivitamin supplements typically contain 2,500–10,000 IU vitamin A, often in the form of both retinol and beta-carotene 14 Table 1: Recommended Dietary Allowances (RDAs) for Vitamin A Age Male Female 14–18 years 900 mcg RAE 700 mcg RAE 19–50 years 900 mcg RAE 700 mcg RAE 51+ years 900 mcg RAE 700 mcg RAE •Deficiency signs :Loss of night vision (night blindness)….xerophthalmia •Risk groups: Premature Infants Infants and Young Children in Developing Countries Pregnant and Lactating Women in Developing Countries People with Cystic Fibrosis 16 • Health Risks from Excessive Vitamin A • Chronic intake of excessive amount: increased intracranial pressure, dizziness, nausea, headaches, skin irritation, pain in joints bones, liver damage, and even coma • Congenital birth defects: Total intakes of preformed vitamin A that exceed the UL and some synthetic retinoids used as topical therapies (such as isotretinoin) • Risk of lung cancer and cardiovascular disease in smokers 17 THIAMIN (vitamin B1) • Benefits: Helps to convert food into energy. Needed for healthy skin, hair, muscles, and brain and helps the nervous system, heart, digestive system and nerve tissues damaged by alcoholism. Table 1: Recommended Dietary Allowances (RDAs) for Thiamin Age Male Female Pregnancy Lactation 14–18 years 1.2 mg 1.0 mg 1.4 mg 1.4 mg 19-50 years 1.2 mg 1.1 mg 1.4 mg 1.4 mg 51+ years 1.2 mg 1.1 mg 18 • Heating foods containing thiamin can reduce their thiamin content. For example, bread has 20%–30% less thiamin than its raw ingredients, and pasteurization reduces thiamin content in milk by up to 20% • Thiamin is available in many dietary supplements. Multivitamin supplements with thiamin typically provide about 1.5 mg thiamin (100% of the DV) and sometimes more • The most commonly used forms of thiamin in supplements are thiamin mononitrate and thiamin hydrochloride 19 • Deficiency signs: - Early stage: can cause weight loss and anorexia, confusion, short-term memory loss, muscle weakness; and cardiovascular symptoms. - Beriberi: rare condition which is characterized mainly by peripheral neuropathy, some have impaired sensory, motor, and reflex functions. In rare cases, beriberi causes congestive heart failure that leads to edema in the lower limbs and, occasionally, death 20 • Wernicke-Korsakoff syndrome : 8–10 times more in alcoholic • Groups at Risk of Thiamin Inadequacy: • • • • • People with alcohol dependence Older adults People with HIV/AIDS People with diabetes People who have undergone bariatric surgery 21 RIBOFLAVIN(vitamin B2) • Helps to convert food into energy. Needed for healthy skin, hair, blood, brain, proper metabolism of fat, protein and carbohydrates, the eyes and sensitive oral areas. • M: 1.3 mg, W: 1.1 mg • Deficiency signs: Itching of the lips, eyes, throat, nose and mouth. Can also show up as cracking in the lip corners. 22 • Safety: This vitamin is water soluble and excess amounts are excreted in the urine. No known toxicity • During lactation there is increased requirements for some vitamins and minerals (folate, vitamin B2, B6, B12, C) • Avoid use of megadose regimens. 23 NIACIN (vitamin B3, nicotinic acid) • Helps convert food into energy. Essential for healthy skin, blood cells, brain, and nervous system • M: 16 mg, W: 14 mg • Niacin occurs naturally in food and can also be made by your body from the amino acid tryptophan, with the help of B6. 24 PANTO-THENIC-ACID (vitamin B5) • Helps to convert food into energy. Helps to make lipids (fats), neurotransmitters, steroid hormones, and hemoglobin • M: 5 mg, W: 5 mg • Deficiency: causes burning in feet and other neurologic symptoms. • Wide variety of nutritious foods, including chicken, whole grains, broccoli, mushrooms, avocados, tomato products 25 VITAMINB6(pyridoxine, pyridoxamine) • Help in lowering homocysteine levels and may reduce the risk of heart disease. • Helps to convert tryptophan to niacin and serotonin (a neurotransmitter that plays key roles in sleep, appetite, and moods). • Helps to make red blood cells, enzyme reactions and protein metabolism • 31–50: M: 1.3 mg, W: 1.3 mg • 51+: M: 1.7 mg, W: 1.5 mg 26 • Prevents issues with nerves, skin problems, increases proper absorption of carbohydrates and protein • Deficiency signs: • Isolated vitamin B6 deficiency is uncommon; inadequate vitamin B6 status is usually associated with low concentrations of other B-complex vitamins, such as B12 and folic acid….Inflammation of the skin • Vitamin B6 deficiency is associated with microcytic anemia 27 • Dietary supplements: • Vitamin B6 is available in multivitamins, in supplements containing other B complex vitamins, and as a stand-alone supplement . The most common form in supplements is pyridoxine (in the form of pyridoxine hydrochloride 28 Groups at Risk of Vitamin B6 Inadequacy • Individuals with Impaired Renal Function • Individuals with Autoimmune Disorders(RA inflammation) • People with Alcohol Dependence • Safety: chronic use may cause issues with the nervous system (administration of 1–6 g oral pyridoxine per day for 12–40 months can cause severe and progressive sensory 29 neuropathy characterized by ataxia (loss of control of bodily movements) Vitamin B12(cobalamin) • Vitamin B12 is required for proper red blood cell formation, neurological function, and DNA synthesis. • M: 2.4 mcg, W: 2.4 mcg • Meat, fish, milk, cheese, eggs, fortified cereals and liver, fortified soymilk 30 • Dietary supplements: • In dietary supplements, vitamin B12 is usually present as cyanocobalamin, body readily converts to the active forms methylcobalamin and 5-deoxyadenosylcobalamin • Prescription medications: - The form of cyanocobalamin and occasionally hydroxocobalamin - can be administered parenterally, usually by intramuscular injection - vitamin B12 deficiency caused by pernicious anemia 31 Table 1: Recommended Dietary Allowances (RDAs) for Vitamin B12 Age Male Female 4–8 years 1.2 mcg 1.2 mcg 9–13 years 1.8 mcg 1.8 mcg 14+ years 2.4 mcg 2.4 mcg Pregnancy Lactation 2.6 mcg 2.8 mcg • Vitamin B12 deficiency: malabsorption, pernicious anaemia – lack of gastric intrinsic factor. • Deficiency Signs: Anemia, fatigue, memory issues, numbness and tingling. 32 Groups at Risk of Vitamin B12 Deficiency • Older adults • Individuals with pernicious anemia • Individuals with gastrointestinal disorders • Individuals who have had gastrointestinal surgery • Vegetarians • Pregnant and lactating women who follow strict vegetarian diets and their 33 infants • Dementia and cognitive function: • A deficiency in vitamin B12 causes an accumulation of homocysteine in the blood and might decrease levels of substances needed to metabolize neurotransmitters • A positive associations between elevated homocysteine levels and the incidence of both Alzheimer's disease and dementia. • Low vitamin B12 status has also been positively associated with cognitive decline. 34 • Energy and endurance Due to its role in energy metabolism, vitamin B12 is frequently promoted as an energy enhancer and an athletic performance and endurance. As The anemia caused by vitamin B12 deficiency associated with symptoms of fatigue and weakness. • However, vitamin B12 supplementation appears to have no beneficial effect on performance in the absence of a nutritional deficit 35 • Metformin Metformin, a hypoglycemic agent used to treat diabetes, might reduce the absorption of vitamin B12, possibly through alterations in intestinal mobility, increased bacterial overgrowth, or alterations in the calcium-dependent uptake by ileal cells of the vitamin B12-intrinsic factor complex 36 • Some people, particularly older adults, are deficient in vitamin B12 because they have trouble absorbing this vitamin from food. • Safety: This vitamin is water soluble and not known to be toxic. • Damaged By: Alcohol, estrogen, sunlight and water. 37 BIOTIN (Vitamin H) • Helps to convert food into energy and synthesize glucose. Helps to make and break down some fatty acids. Needed for healthy bones and hair • Strong's the hair and nails, keeping blood sugar levels stable and helping metabolism react to changes in the body. • M: 30 mcg, W: 30 mcg 38 • body needs very little biotin. Some is made by bacteria in the GI tract. However, it’s not clear how much of this the body absorbs. • It’s a Key role in metabolizing fats, carbohydrates, and proteins • Deficiency: Not common; symptoms include baldness, a rash around the mouth and nose, dry and flaky skin, Fatigue, loss of hair, muscle weakness and pain, poor appetite, & depression and nausea. 39 • Biotin can used in high doses. For example, in the treatment of seborrheic dermatitis in infants, no adverse effects are reported. 40 Vitamin C (ascorbic acid) • Foods rich in vitamin C may lower the risk for some cancers, including those of the mouth, esophagus, stomach, and breast. • Long-term use of supplemental vitamin C may protect against cataracts. • Helps to make collagen (a connective tissue that knits together wounds and supports blood vessel walls) • Vitamin C supplementation (citrus fruit) improves absorption of iron. 41 • Helps to make the neurotransmitters serotonin and norepinephrine Acts as an antioxidant, neutralizing unstable molecules that can damage cells. • Wound healing, protection from viral and bacterial infections, immune system support, prevention of scurvy, cell lifespan and lowering cholesterol. • Total body content of vitamin C ranges from 300 mg (at near scurvy) to about 2 g 42 Table 1: Recommended Dietary Allowances (RDAs) for Vitamin C Age Male Female Pregnancy Lactation 9–13 years 45 mg 45 mg 14–18 years 75 mg 65 mg 80 mg 115 mg 19+ years 90 mg 75 mg 85 mg 120 mg Smokers Individuals who smoke require 35 mg/day more vitamin C than nonsmokers. Safety: Over 2000 mg daily can cause nausea and diarrhea. There is a chance that 1000 to 5000 mg daily can have damaging effects on DNA 43 • For cold and influenza: Vitamin C is an antioxidant that neutralises the oxidising compounds released by neutrophils during a viral infection. Doses of 1–4 g/ day decrease duration and severity of cold symptoms by 10– 30%. • At high doses it interferes with diabetes urine tests and increases risk of production of urinary oxalate leading to renal stones. 44 • Deficiency: Acute vitamin C deficiency leads to scurvy. Poor wound healing, fatigue and gum bleeding • Damage by: Heat, smoking, boiling foods, and light. • Risk groups: Smokers and passive, Infants fed evaporated or boiled milk, Individuals with limited food variety or with malabsorption and certain chronic diseases 45 VITAMIN D(calciferol) • Vitamin D promotes calcium absorption in the gut and maintains adequate serum calcium and phosphate concentrations to enable normal mineralization of bone and to prevent hypocalcemic tetany Serum [25(OH)D] Concentrations and Health* nmol/L** Health status <30 Associated with vitamin D deficiency, leading to rickets in infants and children and osteomalacia in adults 30–50 ≥50 Generally considered adequate for bone and overall health in healthy individuals >125 Emerging evidence links potential adverse effects to such high levels, particularly >150 nmol/L (>60 ng/mL) 46 47 • Safety: Vitamin D is stored in the body’s fat cells and can accumulate. Too much vitamin D can cause toxicity, but the overdose amounts are different for everyone. For example, children should not take more than 400 iu daily. • cod liver oil, 1 tablespoon (1,360 IU) • salmon, cooked, 3 ounces (447 IU) • vitamin D-fortified orange juice, 1 cup (137 IU) 48 • • • • • Calcitriol (hydroxylated derivative of vitamin D) Stimulates active transport of calcium Acts on bone mineralisation Side-effect: occurrence of hypercalcaemia • Monitor plasma calcium concentration and creatinine levels. 49 Recommended Dietary Allowances (RDAs) for Vitamin D Age Male 14–18 years 600 IU (15 mcg) 19–50 years 600 IU (15 mcg) 51–70 years 600 IU (15 mcg) >70 years 800 IU (20 mcg) Female Pregnancy 600 IU (15 mcg) 600 IU (15 mcg) 600 IU (15 mcg) 800 IU (20 mcg) 600 IU (15 mcg) 600 IU (15 mcg) Lactation 600 IU (15 mcg) 600 IU (15 mcg) In supplements and fortified foods, vitamin D is available in two forms, D2 (ergocalciferol) and D3(cholecalciferol) 50 Groups at Risk of Vitamin D Inadequacy • • • • • Breastfed infants Older adults People with limited sun exposure People with dark skin People with inflammatory bowel disease and other conditions causing fat malabsorption • People who are obese or who have undergone gastric bypass surgery 51 VITAMIN E (alpha-tocopherol) • Acts as an antioxidant, neutralizing unstable molecules that can damage cells. Protects vitamin A and certain lipids from damage. Diets rich in vitamin E may help prevent Alzheimer’s disease. Supplements may protect against prostate cancer • M: 15 mg, W: 15 mg (15 mg equals about 22IU from natural sources of vitamin E 52 and 33 IU from synthetic vitamin E) • Deficiency: Fertility issues and muscle weakness. • Safety: Amounts in excess of 400 iu daily can increase the risk of death from long term illness and heart failure. Known drug interaction with Coumadin to increase the risk of bleeding issues 53 VITAMIN K(phylloquinone) • Activates proteins and calcium essential to blood clotting, May help prevent hip fractures • M: 120 mcg, W: 90 mcg • Intestinal bacteria make a form of vitamin K that accounts for half of requirements • Assists with blood clotting after injury, wound healing, protects bones from osteoporosis and may protect against 54 cancer. • Deficiency: Bleeding gums, easy bruising, anemia, nose bleeds and increase menstrual bleeding in females. • It is only considered clinically relevant when prothrombin time increases significantly. • Significant vitamin K deficiency in adults limited to a malabsorption disorders or those taking drugs that interfere with vitamin K metabolism 55 • Groups at Risk of Vitamin K Inadequacy • Newborns not treated with vitamin K at birth • People with malabsorption disorders • Osteoporosis: • Vitamin K is a cofactor …. gammacarboxylation of many proteins (osteocalcin ) ….. undercarboxylated osteocalcin are associated with lower bone mineral density FOLIC ACID • The total body content of folate is estimated to be 10 to 30 mg; about half of this amount is stored in the liver • Vital for new cell creation • Helps prevent brain and spine birth defects when taken early in pregnancy; should be taken regularly by all women of child-bearing age since women may not know they are pregnant in the first weeks of pregnancy. 57 • Can lower levels of homocysteine and may reduce heart disease risk • May reduce risk for colon cancer. Table 1: Recommended Folate Age Male 9–13 years 300 mcg DFE 14–18 years 400 mcg DFE 19+ years 400 mcg DFE Dietary Allowances (RDAs) for Female Pregnant Lactating 400 mcg DFE 600 mcg DFE 500 mcg DFE 400 mcg DFE 600 mcg DFE 500 mcg DFE 300 mcg DFE 1 mcg DFE = 1 mcg food folate, dietary folate equivalents (DFEs) • Many people don’t get enough of this nutrient. Occasionally, folic acid masks a B12deficiency, which can lead to severe neurological complications. That’s not a reason to avoid folic acid; just be sure to get enough B12. • association with poor diet, alcoholism, and, sometimes, malabsorptive disorders 59 • When taken within the first three months of pregnancy can assist with cleft lip, cleft palate and spinal bifida prevention, helps to build healthy red blood cells. • Women who are planning to become pregnant or who are in the first 3 months of pregnancy need to take 400 mcg daily. All others should take 200 mcg daily. 60 • Deficiency signs: Anemia, red tongue and fatigue from anemia. • Folate deficiency can also produce soreness and shallow ulcerations in the tongue and oral mucosa; changes in skin, hair, or fingernail pigmentation. • Risk groups: People with alcohol dependence, Women of childbearing age , Pregnant women, People with 61 malabsorptive disorders References 1. A Textbook of community pharmacy: new age international publishers, rakesh saini, 2012. 2. Lecture Notes in Pharmacy Practice, Lilian M Azzopardi, 2010. 3. Food and Vitamins and Supplements! Oh My! Demystifying nutrition: the value of food, vitamins and supplements, Harvard Medical School, 2013 4. Listing of vitamins, Harvard medical school, 2009. 5. National institute of health, office of dietary supplements, fact sheet ,USA