androgens and antiandrogens.pptx by rammohan

99% of calcium of our body is in bone & teeth.
Metabolism regulated by
Parathormone (PTH)
Vit-D
Calcitonin
Ca++ metabolism also connected to phosphorous + Magnesium metabolism
Physiological role of calcium
Controls excitability of nerves & muscles.
Maintains integrity and regulates permeability of cell membrane.
Essential for muscle contraction (skeletal, cardiac)
Formation of milk, bone & teeth.
Necessary for blood coagulation.
Necessary for release of some neurotransmitters from storage vesicles of the never terminal.
Acts as a second messenger.
Absorption & Excretion
Absorption by facilitated diffusion & carrier mediated active transport in duodenum.
Phosphates, oxalates & tetracycline’s complexes calcium in gut & inhibits its absorption.
Vit-D & Parathyriod Ca2+ reabsorption.
Calcitonin Ca2+ reabsorption in kidney.
Dietary supplement
Children 1-10yrs 0.8-1.2 grms
Young adults 11-24 yrs
Pregnant & lactating women 1.2-1.5 gms
Men 25-65 yrs
Women 25-50 yrs
Women 51-65 yrs if taking HRT 1 gms
Women 51-67 yrs not taking HRT
Everyone ≥65 yrs 1.5 gms
Intake of calcium
A bout 1000 mg Ca is ingested per day.
About 200 mg of this is absorbed into the body.
Absorption occurs in the small intestine and requires Vit D
Milk & dairy products- egg yolk, fish, beans
Cow milk 100mg/kg
Human milk 30mg/ml
Drugs stimulate bone formation
Calcium preparations
Calcium phosphate/
carbonate/lactate/
lactobionate/gluconate/glucobionate
hydroxyapatite
Vitamin D preparations
Ergocalciferol (Vit.D2)
Cholecalciferol (Vit.D3)
Calcitriol (1,2,5,(OH)2 D3)
Alfacalcidol
Doxercalciferol
Paracalcitol
Parathormone preparations
Teriparatide
Teriparatide
Drugs increasing calcium levels are useful in:
Hypocalcaemia
Hypoparathyroidism
Rickets
Osteomalacia
Osteoporosis
Drugs inhibits bone resorption
Miscellaneous Bisphosphonates
Calcitonin Etidronate
Cinacalcet Alendronate
Denosumab Pamidronate
SERM
Gallium nitrate
They are also use in hypercalcemia
Paget's disease of bone
Strontium ranelate- process both (stimulate bone formation + inhibit bone resorption)
Miscellaneous Bisphosphonates
Calcitonin Etidronate
Cinacalcet Alendronate
Denosumab Pamidronate
SERM
Gallium nitrate
They are also use in hypercalcemia
Paget's disease of bone
Strontium ranelate- process both (stimulate bone formation + inhibit bone resorption)
Preparation of calcium
Oral preparation
Calcium-gluconate
Calcium citrate
Calcium lactate
Calcium carbonate
Parenteral preparations
Intravenous-calcium gluconate
Intravenous-calcium chloride
Calcium chloride (27% calcium)
Highly water soluble but irritant to gastric mucosa so no use.
Calcium gluconate (9% calcium)
Nonirritati

1. T estosterone - IM. Daily to twice a wkly Test.propionate Test.enanthate Test.phenylpropionate , isocaproate & decanoate T est.undecanoate – hypogonadism & ostpsis Mesterolone methytestosterone synthetic analogs fluoxymesterolone Preparations and doses

2. ADVERSE EEFECTS: Masculinization & acne Hepatotoxicity Testicular atrophy precocious puberty gynecomastia in males supression of spermatogensis

3. Therapeutic Uses : 1. Testicular failure: R X : PRIMARY FAILURE parental or transdermal patches of testosterone / dihydrotestosterone in 4-6M SECONDARY FAILURE: Loss of libido loss of muscle mass and energy 3. impotence and anaemias - corrected by over months with androgen treatment.

4. 2. Hypopituitarism : hypogonadism – androgen are given at the time of puberty to other harmonal replacement. 3.AIDS related disease : Testosterone therapy need AIDS pts. 4.Hereiditary angioneurotic edema : genetic disorder methytestosterone , stanozolol and danazol incse synthesis of estarase inhibitors.

5. 5.Ageing : Here safety therapy is need in old ages small amount of androgen is added to post menopausal harmone replacement. 6.Idiopathic male infertility: High intratesticular level of testosterone is essential – spermatogenesis androgens – adverse effect spermatogeneis by supress Gn secretion. Mesterolone can cause less inhibition of Gn

6. Anabolic steroids

7. PREPARATIONS : Methadienone N androlone N androlone decanoate Oxymetholone Stanozolol

8. Catabolic states senile osteoporois Growth stimulation in children renal failure and anaemia abuse in atheletes Therapeutic uses

9. Contraindications pregnancy Carcinoma of prostate / breast in males infants n childrens renal /cardiac/liver diseases

10. DANAZOL KETOCONAZOLE CIMITIDINE AND SPIRANOLACTONE Drugs mainly used for to alter the adrogen action Impeded Androgen

11. Danazol : ethisterone derivative weak andogenic , anabolic and progeststional binds AR mRNA production supression of Gn secrtion Inh . Of testicular/ ovarian functions. directly inhibiting steroidogenic enzyme women –endometrial atrophy & amenorrhea

12. endometriosis: improvement in 75% cases dismenorrhoea is prompt estrogen – progrs combination better progestin can give alone – NR Cases infreuntly used Therapeutic uses

13. 2.Menorrhagia: menstrual blood loss. amenorrhoea – 200mg/day 2 nd line drug to an oral progestin 3. Fibrocystic breast diseases : 3-6m therapy reduce pain , nodularity and engorgement in 75% cases. 4.Hereditary angioneurotic edema : in this condition danazol can give prophylatic effect.

14. ADR: Amenorrhoea – high doses loss of libido hot flushes - women Weight gain decreased breast size Deepening of voice muscle cramps and git upset.

15. Antiandrogens

16. Cyproterone acetate: weak AR antgonists – progesterone inhibits LH release bi its proges . activity lowering of serum testosterone suppliment high doses – boys used in precocious puberty in boys acne and hirutisim in women effficacy in metastatic prostate carcinoma Clinical drugs

17. Flutamide : non steroidal AR antagonist blocks androgen sex organs & on pituatary plasma testosterone levels incerase in males limits utility of monotherapy in prostate can. now used only in supress LH and testosterone it has been tired in female hirutisim ADR: libido , gynecomastia ,libido & potency liver damage – restricted

18. Finasteride : its 5 α reductase inhibitor testeosterone to DHT prostate gland and hair follicles predominant in male GUT USED in decrease prostate size BPH – max 6month to get symptomatic relief sudden withdrawl to regrowth the prostate effective in baldness, hair follicle

19. Sidenafil : 1 st agent to be effective orally for treatment of ED(Erectile dysfunction) inhibits phosphodiesterase causes relaxation of smmoth muscle side effects: Headache ,dizziness and nasal stiffness. Drugs used in male sexual impotence