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HYPOTHALAMIC & PITUITARY HORMONES Anterior Pituitary Hormones 1.GH 2.PRL 3.FSH & LH 4.ACTH 5.TSH 6.

MSH
::::::::GROWTH HORMONE : ••Regulation : Hypothalamus -> Antr Pituitary -> Target gland -> Hormone -> -ve feedback
effect •• Disorder : Hypersecrn -> Children -> Gigantism & Adult -> Acromegaly-> treat by Irradiation/Surgery/Drugs &
Dwarfism -> rGH •• Funcn : growth pro + Anabolic in muscle + +ve nitrogen balance + Fat utilization ••Uses : Treat GH
defn + AIDS- related wasting ••• Drug : MECASERMIN : Bachha k dim jodi GH diute respond kora ni + parenterally +
hypog/lipod SOMATOSTATIN : Pan/CNS/hypot + inhibit gluca/insu/gas + Constrict B.V. of hepa,splan, ren + Shirt half-life
1-3min + Synthetic analogue OCREOTIDE : Pot / long / inhi GH /sc. & i.v. -> used for Acromegaly + Tumor + Diarrhoea
asso with diabetes + bleeding from esophageal varices ; LANREOTIDE : Long duration ; Drugs for acromegaly ->
1.Somatostatin Analogues : Ocreotide -> Surgery hole nidibi + Jodi kam nkre then PEGVISOMANT dibi -> GH recpr
antago 2.Dopamine recpr antago -> Bromocriptine -> GH borhai dye normal manuhor tat ; komai diye acromegaly thokar
taat.... ::::::::PROLACTIN(PRL) : Reguln : Hypothalamus -> PR & RIH to antr pituitary -> Prolactin -> stimulate Breast
development & Milk Production -> Suckling -> Stimulate Hypothalamus • Disorders -> Hyperprolactinemia -> due to
dopamine antagonists -> so postoperatively give dopamine agonists -> i.e, BROMOCRIPTINE Semisynthetic ergot
derivative -> potent dopamine agonist @D2 -> produce various motor / behavioural / endocrine effects ; Action : Reduce
PRL / relieve Parkin / NauVomit & Hypot-> due to aplha-ad blockade ; Kinet : Oral + extensive 1st pass ; Uses :
Hyperprolac / acromegaly / parkin / restless leg syndrome ; Adv Effcts : Nau Vomit Postu Hypot Hallucin :::::::::::::
FSH[Urofollitropin + Follitropin alpha] : Female -> dev of follicles + regulate spermatogenesis & LH[Lutropin] : Female ->
Ovulation + produce testosterone :::::: GONADORELIN { Short duration + i.v or s.c + test function of pituitary gonadal axis
} {GnRH Analogues : Nafa/Bus/Gos/Tripto - relin -> •Pulsatile admin -> inc. FSH & LH -> Ovulation • Continuous therapy :
inc. gonadotropin then downregulation of GnRH recpr -> dec.FSH & LH -> Suppress ovulation & spermatogenesis ; Uses :
Prostatic Carcinoma + Precocius Puberty + Breast Cancer ; Adv effects -> hot flush / libido loss / vaginal dryness } {
GnRH antago : CETRO/GANI/ABA/DEGA - relix -> block GnRH recpr -> Inhibit FSH & LH -> dec. testosterone + suppress
LH surge } (Advtg over Agonists are -> quick onset of action + lower risk of ovarian hyperstimulation syndrome )

THYROID { Hyper / Hypo : BMR / HR : Inc./ Dec } (Synth : Iodide trap -> Oxidn -> Coupling -> Release -> Conversn of T4
tobT3 ) (Diff : DIT+MIT -> Rapid -> Short & DIT+DIT -> Slow -> Long ) (MoA : Cell t T4 to T3 -> bind nuclear recpr ->
activate genes -> Synth of proteins ) (Prep : Levothyroxine + Liothyronine + Combiation of T4 & T3 in 4:1 ) (Use : Creti /
myxo Coma / Nodule / Carci ) }

ANTITHYROID DRUGS { (

SEX HORMONES { ANDROgens ( Classfn : 1.Natural -> Testosterone 2.Synthetic -> Methyltestosterone/Fluoxymesterone
: oral-slow-longer & Esters of cy/propionate ) ::::: TESTOSTERONE (Action: Secondary sexual characters + mature
reproductive orgns + mass & strength of muscle + erythropoiesis) (Kinet : oral , Extensive metabo in liver) (Advrse :
hirsutism/irreg/breast atrophy/acne /deepen voice /impaired growth / edema/Cholestatic Jaundice) (Use :
hypogonad/pit , inc muscle mass, osteoporosis) (Contra : Preg/Prostate Carci/Renal & Cardiac disease) (Anabolic
Steroids : Anabolic to androgenic activity with testosterone is 1 :::::: Ox/N- androlone decanoate ; Stanzolol ;
Ethylestrenol -> Uses : Improve appetite / Recovery from prolonged illness/Senile osteoporosis -> Advrse : Inc. muscle
strength & athletic performance -> Dope test :::::::: DANAZOL -> weak androgenic/Suppress FSH & LH - use in
endometriosis - Hirsutism, cramps - Contra in preg }
ANTIANDROGENS { (Fin/duta- steride inhibit 5-alpha reductase) (Flutamide , Cyproterone , Spironolactone : Competitive
antago/treat -> Pros Carci + hirsu + acne / Advrse -> Impot,flush,gynaecom, hepatic damage, dec. splenomegaly) }

OESTROGENS { (Types - Natural : Estrone /Estriol Synthetic : steroidal r Mestranol & Non steroidal r dienestrol) (MoA :
Estro bind ER in nucleus -> regulate protein synthesis -> effects) (ER : types alpha & beta located in
ter,vagi,ova,breast,hypot,b.v & pros,ova) (Kinet : High 1st pass) (Use : Contracep/HRT/Vaginitis/Dysmenorrhoea/Delay
puberty/pros carci) (Adv : NauVomitTenderness) }
ANTIOESTROGEN { (CLOMIPHENE CITRATE : Block estrogen recpr -> abolish -ve feedback effect of estrogen ->
stimulate gonadot secn FSH & LH -> ovulation) (Oral - long plasma half-life) (Use : ART/INFERTILITY/GIFT) (Advrse : Nau
Vomit Headache Hairloss) ::::::: FULVESTRANT (Breast Carci) }
OESTROGEN RECEPR MODULATORS { TAMOXIFEN : (Action : reduce breast tumor/prolifern endomet / peripheral sites -
> flush/ Bone -> antiresorp/ Plasma lipid -> reduce cholesterol) (Oral/ Enterohepatic cycling) (Use : Breast Carcinoma)
(Advrse : NauVomit) }
{RALOXIFEN : (Action : Breast , Endomet - no prolifern, bone -> antiresorp , plasma lipid -> reduce cholesterol , blood ->
inc. the risk of thrombosis) (Kinet : Poor bioval/ exten 1st pass metabolism) (Use : Osteoporosis) (Advrse : Cramps /
thromboembol) }
{ ORMELOXIFEN : Uterine bleeding -> Headache Nausea }
AROMATASE INHIBITORS { (Exmestane -> irreversible inhibition) (Letrozole -> reversible inhibn) inhibition of aromatase
which conv. testosterone to estradiol) (dec. oestrogen levels) (no endometrial hyperplasia, venous thromboembolism)
(should not be administerd to premenopausal women) }

PROGESTIN { (MoA : same) (Prep : Natural are Progesterone + Synthetic -> Progesterone deriv : Megestrol Acetate & 19-
Nor testosterone derivatives : Nor/Levono/Deso- gestrel) (Kinet : Not oral -> extensive 1st pass metabolism) (Use :
Contraception + Dysfunctional uterine bleeding + HRT + endometriosis & carcinoma + postpone periods) (Advrse : acne
- fluid retention - weight gain - depression - irregular periods - hirsutism - inc. Bglucose) }

ANTIPROGESTIN { (MIFEPRISTONE : competitive antago of progesterone + luteolytic property + oral /long plasma half-
life/enterohepatic cycling) (Use : Termination of preg : single oral 600mg followed 48 hrs by PGE1 1mg vaginal
pessary/Contraception/Labour induc/Cervical rip/hypercortisolism) (Advrse : NauVomitDia)

HORMONAL CONTRACEP { ADVRSE : NauVomitWeigainBp inc. VTE Gallstones } {Rifampin + Phenytoin +


Carbamazepine cause failure of contraception & Tetra reduce absopn of contracep } { (Oral : 1.Combined : Nelova
Yasmin Ovral Novelon Mala D -> (ethinyl estradiol + n/l/d - gestrel) (a.n/l/d - gestrel inhibit Endomet proli i.e,
SYNERGISTIC) (b.desogestrel inc. HDL -> counteracts atherogenesis) (c.Mono/Bi/Tri - phasic : (O+P) (O + proges inc.
gradually) (inc. oestrogen midcycle + progesterone inc. gradually) (d.20 to 30 mcg + 0.1 to 1mg ::: less than 30 mcg are
low dose pills) (e.Act synergistically / tubal & uterine contractions/less suitable for implantn/prevent sperm penetration)
(f.Schedule : bleeding huar pisot 1 tab orally daily for 21 consecutive days then gap of 7 days) (g.Contra : hyperten -
Cardiac disease - porphyria - liver disease - Obesity - DM - migraine) ::::::: 2.Minipill (Micronor & Norgest : Cervix
alter/implan interfer/inhi ovuln /cause irregularities /Ectopic preg) (Schedule : 1 tab oral daily without a break b/w 1 to
28th day) :::::: 3.Emergency : Levonogestrel : 0.75mg x 2 -> one immediately & another 12 hrs later ; alternatives are ->
Mifepristone =600mg & Ulipristal=30mg )
PARENTERAL : { Injectable -> NET-EN -> 200mg i.m. once in 2 months -> Advtg : Compliance better+Safe in lactation +
risk of endomet cancer & Disadvtg : Irreg/Mood Change/Osteoporosis } ::::: {Norplant -> 6rods of 216mg levonogestrel ->
for osteoporosis } {Implanon -> Single rod of 68mg desogestrel -> for 3 yrs }
DEVICES : {Levonogestrel -> •Tshaped device • last for 5 yrs } {Progestasert : •Efficacy low •replaced yearly}
NONSTEROIDAL { Centchchroman(Ormeloxifene) : Orally twice weekly for 12 weeks , weekly therafter ; fertility returns
within 6 months of stoppage drug ; no teratogenic/carcinogenic ; long plasma half-life }

CORTICOSTEROIDS { MoA (bind recpr -> form complex -> enter Nucleus -> bind DNA -> protein synthesis -> response ;
Classfn (GC : Short -> Hydrocortisone ; Intermed -> Prednisolone/sone & Triamcinolone ; Long -> Betamethasone) (MC :
DOCA) ; Actions (Diabetes bemari k nidibi, glycogen to liver -> dec. glucose utiliztn) (besi use korile fat distribute hbo)
(GC conv. proteins to aa -> muscle wasting + lympholysis + thinning of skin + osteop + gro retard + No wound healing)
(Ca absorb nhoi excrete hoi -> blood t komai dye) (Stimulate osteoclasts -> khandi nohua kori fracture kore) :::::
CVS(retain sodi/water; hyperten, CHF) :::::: Muscle (weakness, fatigue, steroid myopathy) ::::::::CNS(Maintain Bp/g; Na K)
:::::::: GIT (aggravate p.ulcer /dec. immunity against pylori) ::::::BLOOD (dec lympho/eosino/baso/mast) ::::::: AntiInfla :::::
Immunosup :::::::Use (R/O arth+ RF +Gout + Allergy + Asthma + Collagen disease) ::::: (Contra in high bp/Epilepsy/herpes
keratitis/renal failure) :::::: (Adv : Hypergly/Cushing syn/pulcer/Ed/hyperten/mus weak / osteop/ gro retar
/glaucoma/cataract/Immunosupp/HPA supp) :::: { HPA SUPP -> }

INSULIN { Reguln (Chem : proteins -> aa ; Carb -> glucose ; Fats -> f.acid cause beta cell to secrete insulin) (Neural ->
Parasym / Sym) (Hormonal : Hypo /hypergly) :::::: Mecha (Insulin binds Alpha -> beta with tyrosine kinase activity ->
phosphorylation of tyrosine residues -> Phos Dephos rx -> Glucose entry) ::::::: Kinet( not effective orally) ::::: Prep ( Rapid
/ Short/ Intermed/Long acting -> Lispro/Regular/Isophane/Glargine) ::::::::: Therapy ( Concn : 100 or 40 U/ml) (Regimen -
> 70:30 NPH regular /long acting -> before breakfast & dinner) (Mixed : 1.Intermed + reg/rapid ;;; NPH + regular ;;;; NPH +
Lispro ;;;;; Protamine + Lispro = NPL & Protamine + aspart = NPA ) (Indications : Syri/needle /Pen devices /Pump) (Site :
Abdomen / buttock/ antr thigh or dorsal arm) (Complications : Hypog / allergy/lipodystrophy/Edema) (Interacn :
Salicylates hypoglycemia) (Resistance : Stress surgery -> so inc. the dose) (DKA : Insu / N-S/KCl /Na2CO3
/PO43-/Antibo) (HNDC : hypergly/ osmol/ dehy -> more & faster fluid replacement) (Action : Ali abs + glycogenol +
gluconeog -> Pro syn + lipogen + peri uti )

ORAL ANTIDIABETIC AGENTS { (1.Sulphonylureas : Tolbutamide/glibenclamide 2.Biguanide : Metformin 3.Meglitinide


analogue : Repaglinide 4.D-PA derivative : Nateglinide 5.Thiazolidinediones : Pioglitazone 6.alpha-glucosidase inhibr -
Acarbose 7.DPP-4 inhibr : Saxagliptin 8.SGLT2 inhibr : Canagliflozin }
:::::: SULPHONYLUREAS { (MoA : 1.Bind recpr on beta cells -> block K channel -> influc Ca -> release insulin 2.inc. insulin
recpr 3.reduce glucagon) (Kinet : Oral , low volm of distribution) (Adv : Hypog/ GI dis/Wei gain/ Aller/Terratogen/ Alco
Intol) (Interacn : War/Sali- hypog + Propanolol - delay hypog recovery + Rifampicin - Accelerate metabolism) } :::::::::: {
BIGUANIDES (MoA : Ali Absorpn + Glycogenol + Gluconeog -> Pro syn + Lipo gen + Peri Uti) (Kinet : Oral) (Advs : Lactic
Acidosis/b12 def) (Use : type 2 DM) }

CALCIUM { (Funcn : nerve excita/membr per/coglun /mus con/bone & teeth form/neurotrans release/second
messenger) (Prep : Calcium Carbonate) (Uses : Correct Calcium def/Tetany/Antcid/Urticaria & dermatoses) }
PARAT HORMONE { (Action : dec calcium stimulate pth release -> bone gut & renal reabsorption -> inc. plasma Calcium)
(Hypoparat : Treat -> ••• Acute = 10% calcium gluconate 10-20 ml -> i.v. & Oral Ca Salts ••• Chronic = D2 & Oral ca salts)
HYPERPARAT (Treat : Surgical & Cinacalcet ; CINACALCET : bind recpr on parat gland -> dec. PTH -> dec. Ca + Oral +
Hypercalcemia + Advrse : Hypocalcemia)
CALCITONIN { (Action : Opp. to parat) (Prep : Porcine / Salmon / Human calcitonin) ( Uses : hypercalcemic states +
paget disease + postmenopausal osteoporosis) ( Advrse : NauVomitFlushPain) }
VITAMIN D { Pathways : 7-dehydrocholesterol to cholecalciferol to 25-hydroxycholecalciferol to 1,25-
Dihydroxycholecalciferol in skin , liver , kidney) (Actions : gut bone renal reabsorpn -> inc. plasma Calcium -> Bone
mineralization) (Prep : Ergo & Chole - calciferol + Calcitriol ) (Uses : Nutrional / renal rickets + Vit D dep & res. rickets +
hypoparat + D analogue Calcipotriol topically for psoriasis) }
BIPHOSPHONATE { (ZOLEDRONate : deposit at sites of osteoclastic activity -> taken up by osteoclasts -> interfer with
mevalonate pathway of cholesterol synth) (Kinet : Highly polar /Once a year admin) ( Uses : Paget disease +
Postmenopausal & Corticosteroid induced Osteoporosis + Hypercalcemia of malignancy & hyperparat + relieve pain of
lytic bone lesions) (Advrse : NauVomit Dia + take with plenty of water -> upright for atleast 30 mins to prev esophagitis) }
Drug for Hypercalcemia { DENOSUMAB : Monoclonal antibo -> For osteoporosis -> s.c. once in 6 months }

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