Estrogens Natural Estrogens: Natural Estrogens: Female Sex Hormones (Estrogens and Progestins) Sex Hormones

Structure Activity Relation Ships  Aromatic ring with C-3-OH is essential for activity.  Steroidal structures is not essential for activity.  Alkylation of the aromatic ring decrease the activity.  Unsaturation of ring B decreases the activity.  17α- and 16 position when modified enhance the activity.

Physiological Effects Development of the female sexual organs. Development of the female sexual organs. Development of the female secondary sex characters. Development of the female secondary sex characters. Control of the menstrual cycle. Control of the menstrual cycle.Uses Birth control pills. Birth control pills. Failure of ovarian development. Failure of ovarian development. Menstrual disturbances. Menstrual disturbances. Postmenopausal osteoporosis. Postmenopausal osteoporosis. Prostate cancer. Prostate cancer. Side Effects Nausea, vomiting and diarrhea. Nausea, vomiting and diarrhea. Sodium and water retention. Sodium and water retention. Inhibition of ovulation in large doses. Inhibition of ovulation in large doses.

Steroidal Estrogenic Drugs Estradiol: Most active natural estrogen. Most active natural estrogen. Very short duration of action. Very short duration of action. Mainly used for local effect on the uterus. Mainly used for local effect on the uterus. Ethinyl estradiol: more potent than estradiol orally more potent than estradiol orally.

Nonsteroidal Estrogens Diethylstilbestrol: The trans form is the active one. The trans form is the active one.Advantages: As active as Estradiol. As active as Estradiol. Longer duration of action. Longer duration of action. Orally active Orally active Cheap. Cheap.Disadvantages: Increase the risk of uterine cancer. Increase the risk of uterine cancer.Uses: Treatment of prostate cancer. Treatment of prostate cancer.

Progestins Progesterone in the major natural progestin. Progesterone in the major natural progestin. Secretion: By the ovary mainly the corpus luteum during the second half of the menstrual cycle. Physiological Effects: Development of the endometrium. Development of the endometrium. Development of the mammary gland during pregnancy. Development of the mammary gland during pregnancy.

Structure Activity Relation-ships: Steroidal nucleus essential for activity. Steroidal nucleus essential for activity. Removal of the 19 CH 3 increase activity. Removal of the 19 CH 3 increase activity. Unsaturation of ring B or C increase the activity. Unsaturation of ring B or C increase the activity. Have some androgenic activity. Have some androgenic activity. Removal of the keto function remove androgenic activity. Removal of the keto function remove androgenic activity.

Progestrogenic Drugs Lynestrenol: Semisynthetic progestin with pure progestrogenic activity. Semisynthetic progestin with pure progestrogenic activity.

Uses: Contraceptive pills. Contraceptive pills. Uterine bleeding. Uterine bleeding. Prevention of abortion. Prevention of abortion. Amenorrhea, dysmenorrhea, endometriosis. Amenorrhea, dysmenorrhea, endometriosis. Renal and breast carcinoma. Renal and breast carcinoma. Side Effects: Nausea, vomiting, irregular bleeding, edema, weight gain. Nausea, vomiting, irregular bleeding, edema, weight gain.

Female Oral Contraceptive Sequential Preparations: Estrogens for 16 days then Estrogen and Progesterone for 5- 6 days. Estrogens for 16 days then Estrogen and Progesterone for 5- 6 days % successful % successful. Combination Preparation: Estrogens and Progesterone from the beginning to the end in small doses. Estrogens and Progesterone from the beginning to the end in small doses % successful % successful.Mechanism: The above two types inhibit both FSH and LH so prevent ovulation. The above two types inhibit both FSH and LH so prevent ovulation.

Female Oral Contraceptive (Cont.) Minipills: Small doses of Progesterone from the beginning to the end. Small doses of Progesterone from the beginning to the end % successful % successful.Mechanism: Alter the structure of the Endometrium. Alter the structure of the Endometrium. Increase consistency of the cervical mucus. Increase consistency of the cervical mucus.

Male Sex Hormones (Androgens) Natural Androgens: Natural Androgens:

Physiological Effects Development of the male sexual organs and male secondary sex characters. Development of the male sexual organs and male secondary sex characters. Anabolic effect. Anabolic effect.Uses Replacement therapy in cases of hypogonadism. Replacement therapy in cases of hypogonadism. Anabolic effect. Anabolic effect. Side Effects Side Effects Sodium and water retention leads to edema. Sodium and water retention leads to edema. Masculinization of women. Masculinization of women. Hepatic dysfunction. Hepatic dysfunction.

Structure Activity Relation-ships: Steroidal nucleus essential for activity. Steroidal nucleus essential for activity. The C-3 and C-17 oxygenation increase the activity. The C-3 and C-17 oxygenation increase the activity. Oxidation of C-17 to carbonyl eliminates activity. Oxidation of C-17 to carbonyl eliminates activity. C-17 esters prolonged the activity. C-17 esters prolonged the activity. Trans A/B ring junction is essential for activity. Trans A/B ring junction is essential for activity. 17  -substitutions render compounds orally active. 17  -substitutions render compounds orally active.

Androgenic Drugs 17  -methyltestosterone: Orally active. Orally active. Prolonged action. Prolonged action. Androgenic and anabolic effects. Androgenic and anabolic effects. Synthetic Anabolic Steroids: Norethandrolone Orally active. Orally active. Anabolic effects. Anabolic effects. C-10 CH 3 group removed to C-10 CH 3 group removed to eliminate androgenic effect. eliminate androgenic effect.

Adrenal cortex secretes: - Mineralocorticoids (mainly aldosterone) - Glucocorticoids (mainly cortisol) Adrenal medulla secretes: - Epinephrine and lesser amounts of norepinephrine. Adrenal Gland

Secretion: Adrenal cortex of the adrenal gland. Adrenal cortex of the adrenal gland.Regulation: Stimulation: ACTH. Stimulation: ACTH. Inhibition: Feed back Mechanism. Inhibition: Feed back Mechanism. Steroidal Hormones (Adrenocorticosteroids, Adrenocorticoids, Corticosteroids, Corticoids)

Classification of corticosteroids

Physiological Functions and Pharmacological Effects of corticosteroids :  Carbohydrates and Proteins Metabolism: Stimulate glucose formation in the brain. Stimulate glucose formation in the brain. Decrease peripheral utilization of glucose. Decrease peripheral utilization of glucose. Promote storage of glucose in the liver. Promote storage of glucose in the liver. Promote gluconeogenesis. Promote gluconeogenesis.  Lipids Metabolism: Redistribution of body fat (Buffalo hump, Moon face). Redistribution of body fat (Buffalo hump, Moon face). Enhance lipolyses of Triglycerides. Enhance lipolyses of Triglycerides.  Electrolyte and Water balance: Enhance reabsorption of sodium and water into plasma. Enhance reabsorption of sodium and water into plasma. Increase urinary excretion of potassium. Increase urinary excretion of potassium.

 Blood Picture: Increase hemoglobin and Red blood cells. Increase hemoglobin and Red blood cells. Decrease white blood cells. Decrease white blood cells.  Anti-inflammatory effects: Suppress inflammations regardless to their cause. Suppress inflammations regardless to their cause.  Immunosuppressive Effects: Decrease immunity as a result of decrease the WBC’s. Decrease immunity as a result of decrease the WBC’s.

Disease States (abnormalities of adrenal cortex function): Addison’s disease: Rare syndrome 1/100,000 due to Hypoadrenalism. Rare syndrome 1/100,000 due to Hypoadrenalism.Causes: Atrophy of adrenal gland. Atrophy of adrenal gland. Tuberculoses (result of infectious disease ). Tuberculoses (result of infectious disease ). Low level of ACTH. Low level of ACTH.Symptoms: Weakness, fatigue, depression and irritability. Weakness, fatigue, depression and irritability. Anemia and low blood pressure. Anemia and low blood pressure. Loss of sodium and dehydration. Loss of sodium and dehydration. Low blood sugar. Low blood sugar. Excess pigmentation on skin. Excess pigmentation on skin. Nausea and vomiting. Nausea and vomiting.

Cushing’s disease: Rare syndrome 2- 5/Million due to Hyperadrenalism. Rare syndrome 2- 5/Million due to Hyperadrenalism.Causes: Tumor of the Adrenal Cortex. Tumor of the Adrenal Cortex. Tumor of the Pituitary gland. Tumor of the Pituitary gland.Symptoms: Alteration of fat distribution. Alteration of fat distribution. Hypertension. Hypertension. Osteoporosis. Osteoporosis. Growth retardation. Growth retardation. Decrease Immunity. Decrease Immunity.

Conn’s syndrom: Conn’s syndrom:Causes: Conn's syndrome is a disease of the adrenal glands involving excess production of aldosterone (hyperaldosteronism). Conn's syndrome is a disease of the adrenal glands involving excess production of aldosterone (hyperaldosteronism).Symptoms: Hypertension. Hypertension. Alkalosis. Alkalosis. Polyuria. Polyuria. Edema. Edema.

Adrenocorticoid Drugs Systemic Corticosteroids : * They can be administered by IV, IM, oral, topical or by inhalation. * They can be short, intermediate or long-acting. Cortisone and Cortisone acetate: Can be given orally or by IM injection. Can be given orally or by IM injection. Acetate has longer duration of action. Acetate has longer duration of action. Drug of choice in replacement therapy. Drug of choice in replacement therapy. Cortisone acetate

Fludrocortisone: Fludrocortisone:  9  -fluorocortisone.  10 times more active than cortisone as antiinflammatory.  times more active as mineralocorticoids. Prednisone and Prednisolone: Prednisone and Prednisolone:  They are Δ 1 corticoids.  3, 4 times more active than cortisone and hydrocortisone.

Dexamethasone: Dexamethasone: 9  -fluoro, 16  -methylprednisolone. 9  -fluoro, 16  -methylprednisolone times more active than prednisolone times more active than prednisolone. Betamethasone: Betamethasone: 9  -fluoro, 16  -methylprednisolone. 9  -fluoro, 16  -methylprednisolone. Slightly more active than Dexamethasone. Slightly more active than Dexamethasone.

Clinical uses Hypoadrenalism. Hypoadrenalism. Rumatic diseases. Rumatic diseases. Renal diseases. Renal diseases. Collagen diseases. Collagen diseases. Ocular diseases. Ocular diseases. Skin diseases. Skin diseases. GIT inflammation. GIT inflammation. Liver diseases. Liver diseases.

Side effects Due to Prolonged use: Fluid and electrolyte disturbances, edema and hypertension. Fluid and electrolyte disturbances, edema and hypertension. Hyperglycemia and glucosuria. Hyperglycemia and glucosuria. Peptic ulcer. Peptic ulcer. Increase susceptibility to infections. Increase susceptibility to infections. Growth arrest Growth arrest Osteoporoses Osteoporoses Withdrawal Symptoms: Rapid withdrawal after prolonged use leads to sever hypoadrenalism. Rapid withdrawal after prolonged use leads to sever hypoadrenalism.

The posterior lobe is the source of 2 hormones:  Vasopressin (ADH)  Oxytocin (OT) Hormones of posterior lobe of Pituitary gland Antidiuretic Hormone (ADH) Function: - ADH is to conserve body water by reducing the loss of water in urine. - ADH binds to receptors on cells in the collecting ducts of the kidney and promotes reabsorption of water back into the circulation.

Diabetis insipidus DI (Hyposecretion of ADH) Sign & symptoms: polyuria (10-12 L/ day) Treatment: Synthetic vasopressin injection (Pitressin) This condition can arise from either of two situations: Hypothalamic diabetes insipidus: ■ Results from a deficiency in secretion of ADH from the posterior pituitary. ■ Causes of this disease include head trauma and infections or tumors involving the hypothalamus. Nephrogenic diabetes insipidus: ■ occurs when the kidney is unable to respond to ADH. ■ Most commonly, this results from some type of renal disease.

Function in female: Oxytocin -Stimulation of milk ejection - Stimulation of uterine smooth muscle contraction.

A food supplement, also known as dietary supplement or nutritional supplement, is a preparation intended to provide nutrients that are missing or are not consumed in sufficient quantity in a person's diet.  Marketed as pills, tablets, capsules, liquids in measured doses. Definition

Essential organic nutrients: that promote energy for living Essential organic nutrients: that promote energy for living organisms requiring them are: organisms requiring them are: - Amino acids (the precursors of protein) - Amino acids (the precursors of protein) - Fatty acids - Fatty acids - Carbohydrates. - Carbohydrates. - Purine and pyrimidine and their derivatives (precursors - Purine and pyrimidine and their derivatives (precursors of nucleic acids). of nucleic acids). - Vitamins. - Vitamins. Essential inorganic nutrients that promote the growth and Essential inorganic nutrients that promote the growth and maintenance of living organisms such as: maintenance of living organisms such as: boron, calcium, iodine, iron, magnesium, boron, calcium, iodine, iron, magnesium, potassium, selenium and zinc potassium, selenium and zinc

 All nutrients required for human life work interdependently in order to metabolize and facilitate optimal functioning. in order to metabolize and facilitate optimal functioning. E.g.: intake of calcium requires a complementary amount of magnesium so the calcium will be absorbed properly. E.g.: intake of calcium requires a complementary amount of magnesium so the calcium will be absorbed properly. An excess of calcium may be responsible for a magnesium deficiency. An excess of calcium may be responsible for a magnesium deficiency.

When You May Need a Dietary Supplement You eat a very low-calorie diet You eat an all-plant diet (vegan) You are in a certain stage of the life cycle (e.g., a pregnant, breastfeeding) Your doctor may prescribe a supplement for you if: You have a disease, infection, or injury or recently had surgery You have a nutritional deficiency You are taking medications that interfere with your body’s use of specific nutrients  Dietary supplement would include: ■ Vitamins (e.g.: Vitamin B6, Niacin,Vitamin C) ■ Minerals (e.g.: Calcium and Iron) ■ Amino acid (e.g.: Tyrosine, Creatine, L-tryptophan, Phenylalanine) ■ Herbals

 Pregnant women.  Infants.  Children.  Adolescents.  Elderly.  Individuals with inherited disorders of amino acid metabolism.  Individuals with certain diseases. L-tryptophan and phenylalanine in dietary supplement caused potential risks for: E.g.: L-tryptophan and phenylalanine in dietary supplement caused potential risks for:  Food and Drug Administration (FDA) advises caution with amino acid supplements.

 Eosinophilia-myelgia syndrome (EMS) was associated with the ingestion of L-tryptophan in a dietary supplement.  EMS is a systemic connective tissue disease characterized by: - Severe muscle pain - Increase in white blood cells - Certain skin and neuromuscular manifestations.  People with phenylketonuria (PKU), a rare genetic condition, when ingest too much phenylalanine, serious problems could occur, especially brain and mental problems in children.

Some of the fastest growing herbal categories include the following:  Herbals that increase circulation (Ginko biloba)  Herbals used for calmative effect (Kava kava, Valerian, Chamomile)  Herbals to lessen a cold flu symptoms and boost immunity (Echinacea, Goldenseal)  Herbs for mild depression (St. John's Wort ).  Herbs for inflammation (Curcuma domestica).  Herbs for lowering cholesterol (Allium sativum).  Herbs to treat hypertension (Valariana officinalis, Panax ginseng) Herbs  Combining herbals with medicines can result in an adverse reaction where "double-dosing" can occur or a worsening of symptoms in those with a chronic medical condition.

Be careful when using Herbal Supplements:  Herbals can interact with drugs used for anesthesia (all herbals be discontinued 2-3 weeks prior to a scheduled surgery).  Stop all herbals if pregnant or breast-feeding.  Many herbals can interact with the anticoagulant: - Avoid taking supplements of garlic, ginko biloba, ginger, - Avoid taking supplements of garlic, ginko biloba, ginger, while taking the blood thinner Coumadin ® as these while taking the blood thinner Coumadin ® as these herbs can further prolong clotting times. herbs can further prolong clotting times.  Don't give herbal remedies to children without first checking with the child's pediatrician.  Many drugs interact with St. John's Wort, prompting the FDA to issue a health advisory: St. John's Wort can cause some drugs to be eliminated from the body too quickly, making them less effective such as oral contraceptives, anti-cancer agents, heart medications and drugs that fight HIV. St. John's Wort can cause some drugs to be eliminated from the body too quickly, making them less effective such as oral contraceptives, anti-cancer agents, heart medications and drugs that fight HIV.  Don't take herbal products containing ephedra. Many deaths have been associated with its use.

Possible Side Effects of Supplement Use Dehydration Dehydration Nervousness and Dizziness Nervousness and Dizziness Changes in Blood Pressure and Heart Rate Changes in Blood Pressure and Heart Rate Heart Attack Heart Attack Seizures Psychosis Death Interaction with medications

Supplements to Avoid Steroids and Steroid-Enhancers Linked to liver toxicity and increased risk of heart attack. Kava Kava Linked to liver damage Banned in European countries and Canada St Johns Wort Interferes with a huge number of medications

Dietary Supplements D/S Distinguished from Drugs: Distinguished from Drugs: Drug must undergo FDA approval after clinical studies to determine effectiveness and safety D/S = no pre-market testing Drug must undergo FDA approval after clinical studies to determine effectiveness and safety D/S = no pre-market testing DSHEA (Dietary Supplement Health Education Act)  DSHEA defines a dietary supplement as any product that contains a vitamin, mineral, herb, or amino acid and that is intended as a supplement to the normal diet. DSHEA authorized to provide accurate information to consumers and the label must include: DSHEA authorized to provide accurate information to consumers and the label must include: Name of each ingredient Name of each ingredient Quantity of each ingredient Quantity of each ingredient Total weight of all ingredient if a blend Total weight of all ingredient if a blend Identity of part of plant derived from Identity of part of plant derived from Term “Dietary Supplement” Term “Dietary Supplement” Statements may be included on the label that give the manufacturers description of the role of the D/S Statements may be included on the label that give the manufacturers description of the role of the D/S Not authorized by FDA Not authorized by FDA

Food coloring is any substance that is added to food or drink to change its color. Purpose of food coloring Offsetting color loss due to light, air, extremes of temp., moisture, and storage conditions. - Enhancing naturally occurring colors. - Decorative purposes. Natural food dyes Caramel coloring (E150), made from caramelized sugar, used in cola products and also in cosmetics. Annatto (E160b), a reddish-orange dye made from the seed of the Achiote. Turmeric (curcuminoids, E100) Saffron (carotenoids, E160a) Paprika (E160c)

A great deal of research finds definite connections between behavioral problems and hyperactivity in children. Other effects on health from food dyes are allergies, headache, asthma, fatigue, nausea, concentration problems, agitation and nervousness. Side effects of coloring agents