Unit XI Drugs used for hormonal disorders & Supplementation, Contraception and Medical Termination of Pregnancy QUESTION 1: Classify Insulins. Write the mechanism of action of Insulin. Insulin is a polypeptide hormone synthesized and secreted from the β-cells of Langerhans of pancreas and regulates the metabolism of carbohydrates, proteins and lipids in the body. CLASSIFICATION OF INSULIN PREPARATIONS: Based on the duration of action Insulin preparations can be classified as follows I. RAPID ACTING INSULIN: Insulin lispro, Insulin Aspart, Insulin Glulisine II. SHORT ACTING INSULIN: Regular insulin III. MEDIUM ACTING INSULIN: Intermediate acting Insulin zinc suspension (Lente) Neutral protamine hagedorn IV. LONG ACTING INSULIN: Protamine zinc insulin Insulin glargine Mechanism of action: Insulin reduces blood glucose concentration by stimulating its utilization by peripheral cells, stimulating glycogenesis and also by inhibiting gluconeogenesis and glycogenolysis. It acts as follows Increases utilization of glucose: Insulin stimulates transportation of glucose into the tissues such as adipose tissue, skeletal muscle and liver and increases the utilization of glucose and reduces blood glucose level. Stimulates glycogenesis: Insulin stimulates conversion of Glucose to Glycogen which is deposited in liver and adipose tissue and lowers blood glucose. Dr. Ramesh C, Professor & HOD, EWCP Inhibits glycogenolysis: Insulin inhibits the breakdown of glycogen to glucose in liver and adipose tissue and reduces blood glucose. Inhibits gluconeogenesis: Insulin inhibits the synthesis of glucose from noncarbohydrate substances and hence reduces concentration of glucose in glucose. Synthesis of proteins: Insulin promotes the synthesis of proteins from amino acid and involved in anabolic process. Synthesis of Triglycerides: Insulin stimulates the synthesis of triglycerides from serum free fatty acids and deposit in adipose tissue. Therapeutic uses Insulin dependent diabetes mellitus (IDDM/Type I) Diabetic ketoacidosis Adverse effects Hypoglycemia Weight gain Lactic acidosis QUESTION 2: Classify oral hypoglycemic agents. Write the actions and side effects of Metformin. The drugs which are used in the treatment of non-insulin dependent diabetes mellitus (Type-2/NIDDM) are known as oral hypoglycemic agents. I. INSULIN RELEASING AGENTS: a. Sulfonylureas: Glipizide, Glimepiride, Glibenclamide b. Phenyl alanine analogues: Nateglinide II. INSULIN SENSITIZERS: a. Biguanides: Metformin b. Thiazolidinediones: Pioglitazone, Rosiglitazone III. Α-GLUCOSIDASE INHIBITORS: Acarbose, Voglibose Dr. Ramesh C, Professor & HOD, EWCP METFORMIN The metformin known as insulin sensitizers and stimulates the action of insulin and reduces blood glucose level as follows. Increases utilization of glucose: Insulin stimulates transportation of glucose into the tissues such as adipose tissue, skeletal muscle and liver and increases the utilization of glucose and reduces blood glucose level. Stimulates glycogenesis: Insulin stimulates conversion of Glucose to Glycogen which is deposited in liver and adipose tissue and lowers blood glucose. Inhibits glycogenolysis: Insulin inhibits the breakdown of glycogen to glucose in liver and adipose tissue and reduces blood glucose. Inhibits gluconeogenesis: Insulin inhibits the synthesis of glucose from noncarbohydrate substances and hence reduces concentration of glucose in glucose. Synthesis of proteins: Insulin promotes the synthesis of proteins from amino acid and involved in anabolic process. Synthesis of Triglycerides: Insulin stimulates the synthesis of triglycerides from serum free fatty acids and deposit in adipose tissue. Therapeutic uses Non-Insulin dependent diabetes mellitus (NIDDM/Type II) Diabetic ketoacidosis Adverse effects Abdominal pain, Anorexia, Metallic taste Diarrhea Tiredness Hypoglycemia Dr. Ramesh C, Professor & HOD, EWCP Weight gain Lactic acidosis QUESTION 3. Name any thyroid supplement and thyroid suppressants. Write the side effects of anti-thyroid drugs. Thyroid supplement: These are also known as thyroids and are used for the treatment of hypothyroidism (Decreased activity of thyroid gland). Examples: Thyroxine (T4), Tri-ido-tyronine (T3), Thyroid suppressants: These are also known as anti-thyroid agents which are used to treat hyperthyroidism (Increased activity of thyroid gland). Examples: Propyl-thiouracil, Carbimazole, Methimazole. Adverse effects of Anti-thyroids: GIT Intolerance: Nausea, Vomiting, Abdominal pain. Hair loss Loss of taste Liver damage Hypothyroidism and goiter ( on overdose) QUESTION 4: Name any TWO steroidal preparations. Write the side effects of steroidal administration. Steroidal drugs are substances secreted from adrenal cortex and produce various biological actions in the body. Types of steroids are Gluco-corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone Dr. Ramesh C, Professor & HOD, EWCP Mineralo-corticosteroids: Aldosterone Sex-corticosteroids: Estrogen, Progesterone and testosterone. Side effects of steroids Suppression of immunity Sodium and water retention Hypertension and Edema Hyperglycemia Muscle weakness Peptic ulcer Osteoporosis Glaucoma Growth retardation QUESTION 5: What are pharmacological effects and side effects of anabolic steroids. The anabolic steroids are class of testosterone hormones which stimulates the synthesis of proteins and increases anabolism and hence used to gain weight. Examples: Nandrolone, Oxymetholone Pharmacological actions of anabolic steroids Stimulates the synthesis of proteins and increases muscle growth Development of male sexual organs Stimulates the synthesis of sperm. Synthesis of RBC. Therapeutic uses of anabolic steroids Catabolic state Osteoporosis Suboptimal growth in boys Dr. Ramesh C, Professor & HOD, EWCP To enhance physical ability in athletes Hemolytic anemia Side effects of anabolic steroids Complete amenorrhoea Acne, hirsutism, Decreased breast size, Deepening of voice, Edema Weight gain. Loss of libido in men, Hot flashes in women and night sweats, Muscle cramps, GIT upset, QUESTION 6: Name two uterine stimulants. Write their uses and side effects. Uterine stimulants are the drugs/agents which are used to produce the contraction of uterine smooth muscle. These are also known as oxytocic agents. Examples: Posterior pituitary hormones: Oxytocin Ergot alkaloids: Ergotamine, Ergometrine, Prostaglandins: PGF2α Therapeutic uses of uterine stimulants Induction of labour To induce abortion Uterine inertia Postpartum hemorrhage Breast engorgement Dr. Ramesh C, Professor & HOD, EWCP Side effects of uterine stimulants Uterine cramps and severe pain Complete dilation of the birth canal Fetal tissue injury Uterine tissue damage Anti-diuretic action QUESTION 7: Write uses and side effects of uterine relaxants. Uterine relaxants are the drugs/agents which cause relaxation of uterine smooth muscle. These are also known as Tocolytic agents. Examples: Ritodrine, Isoxsuprine, Magnesium sulfate, Nifedipine Therapeutic uses of uterine relaxants To prevent threatened abortion To avoid premature labour To prolong the labour Acute fetal distress To treat uterine cramps Side effects of uterine relaxants CVS Complications: Hypotension, Tachycardia, Cardiac arrhythmia, pulmonary edema Metabolic Complications: Hyperglycaemia,, hyperinsulinaemia, hypokalaemia. CNS complications: Anxiety, Restlessness, Headache May cause maternal morbidity Dr. Ramesh C, Professor & HOD, EWCP QUESTION 8: What are types of oral contraceptive preparations. Explain the actions of Progesterone. The oral contraceptives are the preparations consisting of progesterone and/or estrogen which are used to prevent pregnancy. Types of oral contraceptives I. II. Combined pill: Consists of both progesterone and estrogen. Progesterone only pill: Consists of only progesterone and also known as mini pill. III. Post coital pill: There are three preparations available as follows Levonorgestrel 0.5 mg + ethinylestradiol 0.1mg Levonorgestrel alone 0.75 mg Mifepristone 600 mg single dose Actions of progesterone Uterus: Regulates secretory changes in the uterus and maintain pregnancy. Vagina: Progesterone induces pregnancy like changes in the vaginal mucosa Breast: Progesterone causes proliferation of acini in the mammary glands CNS: Produces sedation Body temperature: Progesterone slightly increases body temperature. Respiration: Progesterone stimulates respiration in higher doses. Regulation of ovulation, Regulation of menstrual cycle Implantation of ovum in uterus Development of pregnancy Therapeutic use of progesterone As contraceptive Hormone replacement therapy Dysfunctional uterine bleeding Dr. Ramesh C, Professor & HOD, EWCP Endometriosis Premenstrual syndrome/tension Threatened/habitual abortion Endometrial carcinoma Side effects of progesterone Breast engorgement, Headache, Rise in body temperature, Edema, Esophageal reflux, Acne Mood swings Irregular bleeding or amenorrhoea Hyperglycemia Congenital abnormalities QUESTION 9: What are the regulators of Calcium in the body? Name any two calcium preparations with side effects. These are the drugs which increases or decreases the calcium level in the bod are known as calcium regulators. They are as follows. a) Drugs increase calcium in the body: Calcitriol (Vitamin D), Calcitonin b) Drugs decrease calcium in the body: Parathorome List of calcium salts Calcium gluconate Calcium chloride Calcium carbonate Dr. Ramesh C, Professor & HOD, EWCP Side effects of calcium salts Anorexia. Constipation. Flatulence. Dizziness. Flushing. Abnormal heartbeats Nausea. Vomiting. Dr. Ramesh C, Professor & HOD, EWCP