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Hormonal drugs for basic science level. ptx

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Hem Gautam
Hem Gautam

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Hormonal drugs DR. HEM
Thyroid inhibitors The thyroid gland secretes 3 hormones thyroxine(T4), triiodothyronine(T3), and calcitonin. These are drugs used to lower the functional capacity of the hyperactive thyroid gland. Classification of thyroid inhibitors- 1. Inhibit hormone synthesis- propylthiouracil, methimazole, carbimazole. 2. Inhibit iodide trapping (ionic inhibitors)- thiocyanates, perchlorates, nitrates 3. Inhibit hormone release iodine, iodides of Na and K, organic iodide. 4. Destroy thyroid tissue- radioactive iodine.
Antithyroid drugs Antithyroid are thyroid inhibitors, which inhibit thyroid hormones synthesis. MOA-- These drugs bind to thyroid peroxidase and prevent oxidation of iodide/ iodo-tyrosyn residues, thereby; 1. Inhibit iodination of tyrosine residues in thyroglobulin. 2. Inhibit coupling of iodotyrosine residues to form T3 and T4. 3. Propylthiouracil also inhibits peripheral conversion of T4 to T3 whereas methimazole and carbimazole do not have this action.
A/E- Hypothyroidism and goiter can occur due to overtreatment, but is reversible on stopping of drug. GI intolerance, skin rashes, joint pain. Loss of graying of hair, loss of taste, fever, liver damage. Agranulocytosis a rare adverse effect. Doses- Propylthiouracil 50-150mg TDS followed by 25-50mg BD to TDS, for maintenance. Methimazole- 5-10mg TDS initially, maintenance dose 5-15mg daily. Carbimazole- 5-15mg TDS initially, maintenance dose 2.5- 10mg daily . Uses- Thyrotoxicosis in both Graves disease and toxic nodular goiter as a definitive therapy. Preoperatively during surgery in thyrotoxic patients. Mostly young patients are rendered euthyroid with carbimazole before performing subtotal thyroidectomy. Along with radioactive iodine usually preferred in older patients. During pregnancy antithyroid drugs- are safe, low doses of propylthiouracil are preffered. However there is risks of foetal hypothyroidism and goiter.
Iodine and iodides Though iodine is a constituent of thyroid hormones, it is the fastest acting thyroid inhibitor. MOA : Excess iodide inhibits its own transport in thyroid cells and interfere with iodination reduced T3/T4 synthesis (Wolff-Chaikoff effect). Doses- lugols solution, colloid iodine 10%: 5-10drops/ day. Sodium /potassium Iodide- 100mg- 300mg /day therapeutic, 5-10mg/day for endemic goiter.
Uses- Preoperative preparation for thyroidectomy : generally given for 10 days just before surgery. Thyroid storm- Lugols iodine( 6-10drops) or iodine containing radiocontrast media orally to stop any further release of T3/T4 from the thyroid and to decrease T4 to T3 conversion. Prophylaxis of endemic goiter as iodized salt. Antiseptic as tincture iodine. A/E- 1. Acute reaction- in sensitive individuals only, swelling of lips, eyelids, angioedema of larynx, fever, joint pain, petechial haemorrhages, thrombocytopenia, lymphadenopathy. 2. Chronic reaction- salivation, lacrimation, rhinorrhoea, swelling of eyelids, headache, rashes, burning sensation in mouth, GI symptoms, acne. 3. In pregnancy or lactating mothers, may cause foetal /infantile goitre and hypothyroidism.
Radioactive iodine Radioactive iodine emits xrays as well as beta particles. Beta rays are utilised for their destructive effect on thyroid cells. MOA: Radioactive iodine is concentrated by thyroid, incorporated in colloid- emits radiation from within the follicles. The beta particles penetrate only 0.5-2mm of tissues. The thyroid follicular cells are affected from within, undergo necrosis followed by fibrosis when a sufficiently large dose has been administered, without a damage to neighbouring tissues. Uses- 1. Diagnostic- 25 to 100micro curie is given. 2. Therapeutic- hyperthyroidism due to Graves disease or toxic nodular goiter. Dose is 3 to 6 micro curie.
Advantages- OPD basis treatment and inexpensive. No surgical risk of injury to parathyroids/ recurrent laryngeal nerve. Once hyperthyroidism is controlled, cure is permanent. Disadvantages Hypothyroidism Long latent period of response. Contraindicated during pregnancy- foetal thyroid destroyed resulting in cretinism, other abnormalities if given during first trimester. Not suitable for young patients, likely to develop hypothyroidism later and would require life- long T4 treatment
Beta adrenergic blockers Beta blocker like Propanolol are used in thyrotoxicosis to decrease sympathetic overactivity like palpitation,tremor,nervousnessand sweating. MOA: Block beta adrenergic receptor thus decreases sympathetic overactivity. Uses- Used in hyperthyroidism while awaiting response to carbimazole or radioactive iodine. Along with iodide for preoperative preparation before subtotal thyroidectomy. Thyroid storm (thyrotoxic crisis) . DOSE: 10 mg, 20mg, 40mg OD A/E- Bradycardia Hypotension Depression Fatigue Insomnia Pruritis Nausea, vomiting.
Oxytocin Uterine stimulants that increase uterine motility, especially at term. Hormone secreted by Posterior pituitary gland along with vasopressin(ADH). Both are synthesized within nerve cells bodies(supraoptic and paraventricular nuclei) of hypothalamus. Released by stimuli as such; coitus, parturition, suckling. MOA- activates oxytocin receptors that increases intracellular calcium levels in uterine myofibrils, which results in uterine contractions; - increases local prostaglandins production, which further stimulates uterine contractions. Uses and Dosage- Induction of labour- slow iv infusion- 5IU diluted in 500ml of NS. Uterine inertia when uterine contractions are feeble and labour is not progressing satisfactorily, oxytocin is infused iv to augment contractions. Postpartum haemorrhage, caesarean section. Breast engorgement. A/E- uterine rupture, injury to birth canal, foetal asphyxia, death. Water intoxication( because of ADH like action of large doses given along with iv fluids, especially in toxaemia of pregnancy and renal insufficiency)
Ergometrine , Methylergometrine MOA: Ergot alkaloids which act In uterus- to increase force, frequency and duration of uterine contractions. At low doses, contractions are phasic with normal relaxation in between but only moderate increase in dose raises the basal tone, contracture occurs with high doses. Gravid uterus is more sensitive esp at term and in early puerperium. DOSE;0.25mg IM/iv up to max 1.25mg Uses- To control and prevent Postpartum haemorrhage. After caesarean section/instrumental delivery to prevent uterine atony. To ensue normal involution. A/E- Nausea, vomiting, rise in BP Should be avoided in patients with vascular disease, hypertension, toxaemia Presence of sepsis- may cause gangrene Liver and kidney disease.
Diabetes mellitus
Conventional insulin Conventional preparation of insulin are produced from beef and pork pancreas. Types of insulin preparations- 1. Rapid acting insulin lispro, insulin aspart, insulin glulisine 2. Short acting- regular insulin 3. Intermediate acting- insulin zinc suspension or lente, neutral protamine hagedorn, isophane insulin. 4. Long acting- protamine zinc insulin, insulin glargine. MOA insulin acts on specific insulin receptors on cell membranes more on liver and fat cells, receptors containing alpha and beta subunits. Alpha subunits carry insulin binding sites, while beta subunits have tyrosine protein kinase activity. Insulin stimulates glucose transport across cell membrane by ATP dependent glucose transporter. Doses- 5. Regular insulin- 40U/ml, 100U/ml, for sc or iv inj. 6. Isophane insulin 40U/ml for sc inj.
Uses- 1. Diabetes mellitus 2. Diabetic ketoacidosis 3. Hyperosmolar nonketotic hyperglycemic coma. Reactions to insulin 4. Hypoglycemia- most frequently and serious. 5. Local reactions- swelling, erythema, stinging, lipodystrophy at injection sites. 6. Allergy- infrequent, urticaria, angioedema, anaphylaxis. 7. Edema- due to Na+ retention.
Oral hypoglycaemic drugs These drugs lower blood glucose levels and effective orally. Classification- 1) Sulfonylureas- tolbutamide, chlorpropamide, glipizide, glimepiride, glibenclamide, gliclazide 2) Biguanides- metformin 3) Meglitinides- repaglinide, nateglinide 4) Thiazolidinediones- rosiglitazone, pioglitazone 5) Alpha glucosidase inhibitors- acarbose, miglitol.
Metformin A biguanide, MOA not understood clearly. MOA- Supress hepatic gluconeogenesis and glucose output from liver;the major action. Enhance insulin-mediated glucose disposal in muscle and fats. Retard intestinal absorption of glucose, other hexoses, aminoacids and vit.B12. Interfere with mitochondrial respiratory chain-promote peripheral glucose utilisation by enhancing anaerobic glycolysis. A/E- Abdominal pain, anorexia, nausea, metallic taste, mild diarrhoea Tiredness Lactic acidosis- rare, alcohol ingestion can precipitate severe lactic acidosis Vitamin B12 deficiency- due to interference with its absorption can occur with higher doses.
Sulfonylureas MOA- provoke release of insulin from pancreas, act on sulfonylurea receptors on pancreatic Beta cell membrane-cause depolarisation by reducing conductance of ATP sensitive K+ channels. This enhances Ca2+ influxdegranulation, increasing rate of insulin secretion. A/E- Hypoglycemia-commonest problem, may be severe, rarely fatal. Nausea, vomiting, flatulence,diarrhoea or constipation Headache, paresthesias Weight gain Rashes, photosensitivity, purpura Transient leukopenia Rarely agranulocytosis
Corticosteroids Has antiinflammatory and immunosupressant actions Systemic corticosteroids- 1. Short acting- hydrocortisone 2. Intermediate acting- prednisolone, methylprednisolone, triamcinolone 3. Long acting- dexamethasone, betamethasone. Uses- 4. Replacement therapy Acute adrenal insufficiency Chronic adrenal insufficiency(Addisons disease) Congenital adrenal hyperplasia (Adrenogenital syndrome)
2. Pharmacotherapy in- Arthritis -Rheumatoid arthritis, Osteoarthritis, Rheumatic fever, Gout Collagen diseases Severe allergic reactions Autoimmune diseases Bronchial asthma Eye diseases Skin diseases- eczema, pemphigus etc Intestinal diseases- ulcerative colitis, crohns diseases Cerebral odema Organ transplantation and skin allograft, malignancies Thyroid storm
A/E- 1. Cushings habitus- rounded face, narrow mouth, supraclavicular hump, obesity of trunk with thin limbs 2. Fragile skin, purple striae, easy bruising,hirsutism 3. Hyperglycemia, glycosuria 4. Muscle weakness, proximal more, myopathy 5. Susceptibility to infections- e.g. candidiasis 6. Delayed healing of wounds and surgical incisions 7. Peptic ulceration risk increased 8. Osteoporosis 9. Posterior subcapsular cataract 10. Glaucoma in prolonged topical therapy 11. Growth retardation in childrens as large doses may inhibit GH secretion. 12. Psychiatric disturbances- euphoria, nervousness, psychosis 13. Supression of hypothalamo-pituitary adrenal axis- malaise, fever, anorexia, nausea, postural hypotension, pain in muscles
Contraindications- I. Peptic ulcer, diabetes mellitus, hypertension II. Viral and fungal infections, tuberculosis and other infections, herpes simplex keratitis III. Osteoporosis IV. Psychosis, epilepsy V. CHF, renal failure
III. Female Sex Hormones and Hormonal Contraception Oestrogens These drugs can be classified into three groups. 1. Natural estradiol, esterone, estriol 2. Semisynthetic Ethnylestradiol 3. Synthetic: Diethylstibosterol
ORAL CONTRACEPTIVEs These are drugs taken orally to prevent conception. They are available in the following forms: 1. Combined regimen type 2. sequential regimen type 3. triphasic pill regimen Combined regimen: involves the administration of pills containing combination of Estrogen and Progestogen. They are administered starting 5th day of menustral cycle for 21 days.
Formulation: a) low estrogen, low progesterone(0.03mg ethinylestradiol+0.15 mg norgestril b) Low esterogen, high progestogen (0.03 mg ethinylestradiol + 1.5 mg norethindrone) c) High estrogen, high progestrone(0.05 mg ethinylestradiol + 0.5 mg norgestril) Mechanism: includes inhibition of release of FSH and LH, increase viscosity of cervical mucus endometrial changes, interfere with contraction of cervix, uterus and fallopian tube
Side effects of oral contraceptive: Thromboembolic complication, Weight gain & fluid retention, Menstrual disorder, Breast tenderness & fullness, Skin changes, Nausea & vomiting, Depressed mood, Reduced lactation Beneficial effects of estrogen /progesterone oral contraceptive 1) Reduced risk of endometrial Carcinoma, ovarian cyst 2) regular Menses, No excessive blood loss 3) Less premenustrual tension and dysmennorrhea 4) Relief of endometriosis Contraindication: In patients withcardiovascular diseases (hypertension, coronary heart disease) Thromboemolic disease, breast Cancer, diabetes mellitus, liver disease, women > 35 years

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Hormonal drugs for basic science level. ptx

  • 2. Thyroid inhibitors The thyroid gland secretes 3 hormones thyroxine(T4), triiodothyronine(T3), and calcitonin. These are drugs used to lower the functional capacity of the hyperactive thyroid gland. Classification of thyroid inhibitors- 1. Inhibit hormone synthesis- propylthiouracil, methimazole, carbimazole. 2. Inhibit iodide trapping (ionic inhibitors)- thiocyanates, perchlorates, nitrates 3. Inhibit hormone release iodine, iodides of Na and K, organic iodide. 4. Destroy thyroid tissue- radioactive iodine.
  • 3. Antithyroid drugs Antithyroid are thyroid inhibitors, which inhibit thyroid hormones synthesis. MOA-- These drugs bind to thyroid peroxidase and prevent oxidation of iodide/ iodo-tyrosyn residues, thereby; 1. Inhibit iodination of tyrosine residues in thyroglobulin. 2. Inhibit coupling of iodotyrosine residues to form T3 and T4. 3. Propylthiouracil also inhibits peripheral conversion of T4 to T3 whereas methimazole and carbimazole do not have this action.
  • 4. A/E- Hypothyroidism and goiter can occur due to overtreatment, but is reversible on stopping of drug. GI intolerance, skin rashes, joint pain. Loss of graying of hair, loss of taste, fever, liver damage. Agranulocytosis a rare adverse effect. Doses- Propylthiouracil 50-150mg TDS followed by 25-50mg BD to TDS, for maintenance. Methimazole- 5-10mg TDS initially, maintenance dose 5-15mg daily. Carbimazole- 5-15mg TDS initially, maintenance dose 2.5- 10mg daily . Uses- Thyrotoxicosis in both Graves disease and toxic nodular goiter as a definitive therapy. Preoperatively during surgery in thyrotoxic patients. Mostly young patients are rendered euthyroid with carbimazole before performing subtotal thyroidectomy. Along with radioactive iodine usually preferred in older patients. During pregnancy antithyroid drugs- are safe, low doses of propylthiouracil are preffered. However there is risks of foetal hypothyroidism and goiter.
  • 5. Iodine and iodides Though iodine is a constituent of thyroid hormones, it is the fastest acting thyroid inhibitor. MOA : Excess iodide inhibits its own transport in thyroid cells and interfere with iodination reduced T3/T4 synthesis (Wolff-Chaikoff effect). Doses- lugols solution, colloid iodine 10%: 5-10drops/ day. Sodium /potassium Iodide- 100mg- 300mg /day therapeutic, 5-10mg/day for endemic goiter.
  • 6. Uses- Preoperative preparation for thyroidectomy : generally given for 10 days just before surgery. Thyroid storm- Lugols iodine( 6-10drops) or iodine containing radiocontrast media orally to stop any further release of T3/T4 from the thyroid and to decrease T4 to T3 conversion. Prophylaxis of endemic goiter as iodized salt. Antiseptic as tincture iodine. A/E- 1. Acute reaction- in sensitive individuals only, swelling of lips, eyelids, angioedema of larynx, fever, joint pain, petechial haemorrhages, thrombocytopenia, lymphadenopathy. 2. Chronic reaction- salivation, lacrimation, rhinorrhoea, swelling of eyelids, headache, rashes, burning sensation in mouth, GI symptoms, acne. 3. In pregnancy or lactating mothers, may cause foetal /infantile goitre and hypothyroidism.
  • 7. Radioactive iodine Radioactive iodine emits xrays as well as beta particles. Beta rays are utilised for their destructive effect on thyroid cells. MOA: Radioactive iodine is concentrated by thyroid, incorporated in colloid- emits radiation from within the follicles. The beta particles penetrate only 0.5-2mm of tissues. The thyroid follicular cells are affected from within, undergo necrosis followed by fibrosis when a sufficiently large dose has been administered, without a damage to neighbouring tissues. Uses- 1. Diagnostic- 25 to 100micro curie is given. 2. Therapeutic- hyperthyroidism due to Graves disease or toxic nodular goiter. Dose is 3 to 6 micro curie.
  • 8. Advantages- OPD basis treatment and inexpensive. No surgical risk of injury to parathyroids/ recurrent laryngeal nerve. Once hyperthyroidism is controlled, cure is permanent. Disadvantages Hypothyroidism Long latent period of response. Contraindicated during pregnancy- foetal thyroid destroyed resulting in cretinism, other abnormalities if given during first trimester. Not suitable for young patients, likely to develop hypothyroidism later and would require life- long T4 treatment
  • 9. Beta adrenergic blockers Beta blocker like Propanolol are used in thyrotoxicosis to decrease sympathetic overactivity like palpitation,tremor,nervousnessand sweating. MOA: Block beta adrenergic receptor thus decreases sympathetic overactivity. Uses- Used in hyperthyroidism while awaiting response to carbimazole or radioactive iodine. Along with iodide for preoperative preparation before subtotal thyroidectomy. Thyroid storm (thyrotoxic crisis) . DOSE: 10 mg, 20mg, 40mg OD A/E- Bradycardia Hypotension Depression Fatigue Insomnia Pruritis Nausea, vomiting.
  • 10. Oxytocin Uterine stimulants that increase uterine motility, especially at term. Hormone secreted by Posterior pituitary gland along with vasopressin(ADH). Both are synthesized within nerve cells bodies(supraoptic and paraventricular nuclei) of hypothalamus. Released by stimuli as such; coitus, parturition, suckling. MOA- activates oxytocin receptors that increases intracellular calcium levels in uterine myofibrils, which results in uterine contractions; - increases local prostaglandins production, which further stimulates uterine contractions. Uses and Dosage- Induction of labour- slow iv infusion- 5IU diluted in 500ml of NS. Uterine inertia when uterine contractions are feeble and labour is not progressing satisfactorily, oxytocin is infused iv to augment contractions. Postpartum haemorrhage, caesarean section. Breast engorgement. A/E- uterine rupture, injury to birth canal, foetal asphyxia, death. Water intoxication( because of ADH like action of large doses given along with iv fluids, especially in toxaemia of pregnancy and renal insufficiency)
  • 11. Ergometrine , Methylergometrine MOA: Ergot alkaloids which act In uterus- to increase force, frequency and duration of uterine contractions. At low doses, contractions are phasic with normal relaxation in between but only moderate increase in dose raises the basal tone, contracture occurs with high doses. Gravid uterus is more sensitive esp at term and in early puerperium. DOSE;0.25mg IM/iv up to max 1.25mg Uses- To control and prevent Postpartum haemorrhage. After caesarean section/instrumental delivery to prevent uterine atony. To ensue normal involution. A/E- Nausea, vomiting, rise in BP Should be avoided in patients with vascular disease, hypertension, toxaemia Presence of sepsis- may cause gangrene Liver and kidney disease.
  • 13. Conventional insulin Conventional preparation of insulin are produced from beef and pork pancreas. Types of insulin preparations- 1. Rapid acting insulin lispro, insulin aspart, insulin glulisine 2. Short acting- regular insulin 3. Intermediate acting- insulin zinc suspension or lente, neutral protamine hagedorn, isophane insulin. 4. Long acting- protamine zinc insulin, insulin glargine. MOA insulin acts on specific insulin receptors on cell membranes more on liver and fat cells, receptors containing alpha and beta subunits. Alpha subunits carry insulin binding sites, while beta subunits have tyrosine protein kinase activity. Insulin stimulates glucose transport across cell membrane by ATP dependent glucose transporter. Doses- 5. Regular insulin- 40U/ml, 100U/ml, for sc or iv inj. 6. Isophane insulin 40U/ml for sc inj.
  • 14. Uses- 1. Diabetes mellitus 2. Diabetic ketoacidosis 3. Hyperosmolar nonketotic hyperglycemic coma. Reactions to insulin 4. Hypoglycemia- most frequently and serious. 5. Local reactions- swelling, erythema, stinging, lipodystrophy at injection sites. 6. Allergy- infrequent, urticaria, angioedema, anaphylaxis. 7. Edema- due to Na+ retention.
  • 15. Oral hypoglycaemic drugs These drugs lower blood glucose levels and effective orally. Classification- 1) Sulfonylureas- tolbutamide, chlorpropamide, glipizide, glimepiride, glibenclamide, gliclazide 2) Biguanides- metformin 3) Meglitinides- repaglinide, nateglinide 4) Thiazolidinediones- rosiglitazone, pioglitazone 5) Alpha glucosidase inhibitors- acarbose, miglitol.
  • 16. Metformin A biguanide, MOA not understood clearly. MOA- Supress hepatic gluconeogenesis and glucose output from liver;the major action. Enhance insulin-mediated glucose disposal in muscle and fats. Retard intestinal absorption of glucose, other hexoses, aminoacids and vit.B12. Interfere with mitochondrial respiratory chain-promote peripheral glucose utilisation by enhancing anaerobic glycolysis. A/E- Abdominal pain, anorexia, nausea, metallic taste, mild diarrhoea Tiredness Lactic acidosis- rare, alcohol ingestion can precipitate severe lactic acidosis Vitamin B12 deficiency- due to interference with its absorption can occur with higher doses.
  • 17. Sulfonylureas MOA- provoke release of insulin from pancreas, act on sulfonylurea receptors on pancreatic Beta cell membrane-cause depolarisation by reducing conductance of ATP sensitive K+ channels. This enhances Ca2+ influxdegranulation, increasing rate of insulin secretion. A/E- Hypoglycemia-commonest problem, may be severe, rarely fatal. Nausea, vomiting, flatulence,diarrhoea or constipation Headache, paresthesias Weight gain Rashes, photosensitivity, purpura Transient leukopenia Rarely agranulocytosis
  • 18. Corticosteroids Has antiinflammatory and immunosupressant actions Systemic corticosteroids- 1. Short acting- hydrocortisone 2. Intermediate acting- prednisolone, methylprednisolone, triamcinolone 3. Long acting- dexamethasone, betamethasone. Uses- 4. Replacement therapy Acute adrenal insufficiency Chronic adrenal insufficiency(Addisons disease) Congenital adrenal hyperplasia (Adrenogenital syndrome)
  • 19. 2. Pharmacotherapy in- Arthritis -Rheumatoid arthritis, Osteoarthritis, Rheumatic fever, Gout Collagen diseases Severe allergic reactions Autoimmune diseases Bronchial asthma Eye diseases Skin diseases- eczema, pemphigus etc Intestinal diseases- ulcerative colitis, crohns diseases Cerebral odema Organ transplantation and skin allograft, malignancies Thyroid storm
  • 20. A/E- 1. Cushings habitus- rounded face, narrow mouth, supraclavicular hump, obesity of trunk with thin limbs 2. Fragile skin, purple striae, easy bruising,hirsutism 3. Hyperglycemia, glycosuria 4. Muscle weakness, proximal more, myopathy 5. Susceptibility to infections- e.g. candidiasis 6. Delayed healing of wounds and surgical incisions 7. Peptic ulceration risk increased 8. Osteoporosis 9. Posterior subcapsular cataract 10. Glaucoma in prolonged topical therapy 11. Growth retardation in childrens as large doses may inhibit GH secretion. 12. Psychiatric disturbances- euphoria, nervousness, psychosis 13. Supression of hypothalamo-pituitary adrenal axis- malaise, fever, anorexia, nausea, postural hypotension, pain in muscles
  • 21. Contraindications- I. Peptic ulcer, diabetes mellitus, hypertension II. Viral and fungal infections, tuberculosis and other infections, herpes simplex keratitis III. Osteoporosis IV. Psychosis, epilepsy V. CHF, renal failure
  • 22. III. Female Sex Hormones and Hormonal Contraception Oestrogens These drugs can be classified into three groups. 1. Natural estradiol, esterone, estriol 2. Semisynthetic Ethnylestradiol 3. Synthetic: Diethylstibosterol
  • 23. ORAL CONTRACEPTIVEs These are drugs taken orally to prevent conception. They are available in the following forms: 1. Combined regimen type 2. sequential regimen type 3. triphasic pill regimen Combined regimen: involves the administration of pills containing combination of Estrogen and Progestogen. They are administered starting 5th day of menustral cycle for 21 days.
  • 24. Formulation: a) low estrogen, low progesterone(0.03mg ethinylestradiol+0.15 mg norgestril b) Low esterogen, high progestogen (0.03 mg ethinylestradiol + 1.5 mg norethindrone) c) High estrogen, high progestrone(0.05 mg ethinylestradiol + 0.5 mg norgestril) Mechanism: includes inhibition of release of FSH and LH, increase viscosity of cervical mucus endometrial changes, interfere with contraction of cervix, uterus and fallopian tube
  • 25. Side effects of oral contraceptive: Thromboembolic complication, Weight gain & fluid retention, Menstrual disorder, Breast tenderness & fullness, Skin changes, Nausea & vomiting, Depressed mood, Reduced lactation Beneficial effects of estrogen /progesterone oral contraceptive 1) Reduced risk of endometrial Carcinoma, ovarian cyst 2) regular Menses, No excessive blood loss 3) Less premenustrual tension and dysmennorrhea 4) Relief of endometriosis Contraindication: In patients withcardiovascular diseases (hypertension, coronary heart disease) Thromboemolic disease, breast Cancer, diabetes mellitus, liver disease, women > 35 years