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HORMON DAN ANTAGONIS HORMON

A. Hormon Adenohipofisa dan Hypothalamic Releasing Factors

Hormon somatotropika. Growth hormone (GH): somatropin,

somatrem, sermorelin acetate. Obat pada kelebihan GH: 1. Somatostatin analog: octreotide,

lanreotide, vapreotide. 2. Dopamin reseptor agonis: cabergolin. 3. Growth Hormone antagonist:

pegvisomant.

b. Prolactin (Prl) Pemicu prolactin : TRH, dopamine. Obat pada kelebihan prolactin Dopamine receptor agonist: bromocriptine, pergolide, cabergoline, quinagolide,

c. Placental lactogen (PL)

Hormon Glikoprotein:a. Gonadotropic Hormone

Regulator gonadotropin: Gonadotropin Releasing Hormon (GnRH): factrel, lutrepulse, gonadorelin acatate; GnRH analog: leuprolide, buserelin, nafarelin, deslorelin, histrelin, goserelin, cetrorelix, ganirelix.

1. Luteinizing hormone (LH) 2. Folicle stimulating hormone (FSH):

urofollitropin, follitropin alfa, follitropin beta, metrodin.

3. Chorionic gonadotropin (CG) : chorionic gonadotropin (pregnyl), menotropin

b. Thyroid stimulating hormone (TSH)

POMC‑Derived Hormonesa. Alfa melanocyte stimulating

hormone (alfa MSH)b. Beta melanocyte stimulating

hormone (beta MSH)c. Beta‑lipotropin (beta LPH)d. Gamma‑lipotropin (gamma‑LPH)

B. Tiroid dan Obat Antitiroid, Paratiroid dan Obat Yang Berpengaruh Pada Metabolisme Kalsium

Thyroid dan antithyroid• Regulator fungsi thyroid:

Thyrotropin releasing hormone (TRH), Thyroid stimulating hormon (TSH). TRH inhibitors: somatostatin, dopamine, glucocorticoid.

• Hormon tiroid : thyronine, thyroxine, 3,5,3 triiodothyronine, 3,3,5‑ triiodothyronine, diiodothyrosine, iodothyrosine. Sintetik hormon: levothyroxine‑Na,

liothyronine‑Na, liotrix.

• Tiroid inhibitor dan obat antitiroid lainnya:

1. Antitiroid: propylthiouracil (PTU), methimazole, carbimazole.

2. Ionic inhibitors: thiocyanate, perchlorate.

• Yodida. : Lugol's solution, isotop iodium: Na jodida

131.

Hormon paratiroid, kalsium, fosfat, vitamin D, kalsitonin dan lain‑lain obat yang mepengaruhi kalsifikasi.

• Regulator fungsiparathyroid: ion Ca• Hormon Parathyroid (PTH) • Kalsium: Parenteral/IV: CaCl,

Ca‑gluceptate, Ca‑gluconate; Oral: Ca-gluconate, Ca-lactate, Ca-carbonate, Ca-phosphate, Ca‑acetate.

• Fosfat: Na‑fosfat.• Vitamin D: ergocalciferol (vitamin

D2),cholecalciferol. (vitamin D3), calcifediol,calcitriol, analog vitamin DDHT(dihydrotachysterol), analog calcitriol: calcipotriol, paricalcitol (reduktor PTH produksi), 22‑oxacalcitriol (supresor PTH)

• Kalsitonin (CT, hypocalcemic hormone):Salmon‑CT untuk Paget diseases

• Mineralisasi inhibitor: Biphosphonate• etidronate, clodronate, tiludronate,

alendronate, ibandronate, pamibronate, risedronate.

• Fluoride

• Terapi osteoporesis: Ca; vitaminD/analog; SERM: raloxifene; calcitonin (CT); bisphosphonates: alendronate, palmidronate, risedronate, ibandronate; HCT; fluoride, androgen, PTH.

C. Hormon kelamin dan antagonisnya

• Estrogen dan antiestrogen : 1. a. Estrogen: estradiol, estradiol

valerate, estradiol cypionate, ethinyl estradiol, mestranol, quinestrol, estrone, estrone sulfate, equilin,

b, Senyawa nonsteroid dengan aktivitas estrogenik: diethylstilbesterol,

p,p'‑DDT, bisphenol‑A, genistein. 2. Selective estrogen receptor

modulators (SERMS) : tamoxifen, raloxifene, toremifene.

3. Antiestrogen: clomiphene, ICI 182,780 (faslodex)

4. Estrogen syntesis inhibitors: fortnestane, exemestane, anastrozole, letrozole, vorozole

• Progestin dan antiprogestin : 1.a. Progestin: progesterone,

senyawa pregnane (17 alfa acetoxy progesterone), senyawa estranes (19 nortestosterone), senyawa gonane (norgestrel).

b. Steroid : medroxyprogesterone acetate (MPA), megestrol acetate., norethindrone acetate.

2. Antiprogestin: mifepristone, onapriston, (kombinasi antiprogestin‑prostaglandin: sulprostone, gemeprost, misoprostol)

• Kontrasepsi : a. Kombinasi oral (progestin

estrogen): monofasik, bifasik, trifasik.

b. Progestin only : oral, parenteral: DMPA, implants: norethinrone

• Hormon androgen dan antiandrogen :1. Androgen: testosterone (histerone);

testosterone esters: testosterone enanthate, testosterone cypionate, testosterone undecanoate; 17alfa‑alkylated androgens: methyltestosterone, oxandrolone, stanozolol, fluoxymesterone, danazol.

2. Selective androgen receptor modulators: senyawa quinolinones.

3. Antiandrogen : a. inhibitor sintesa testosterone: ketoconazole; b. inhibitor androgen action: androgen receptor antagonists: flutamide, bicalutamide, spironolactone, cyproterone acetate; c. 5‑alfa reductase inhibitors : finasteride.

D. Hormon adrenokortikotropik dan adrenokortikosteroid

• Regulator corticotropin : Corticotropin Releasing Hormon (CRH) di hipothalamus, AVP sebagai sekretagoga, negative feed back oleh glucocorticoid. CRH preparat:corticorelin

• Hormon adrenokortikotropik ACTH (corticotropin), cosyntropin (sintetik peptida)

• Steroid adrenokotikal : a. Glukokortikoid: hidrokortison

(cortisol)b. Mineralokortikoid aldosteron. (lihat diuretika)

• Analog sintetik steroid adrenokortikal: aclomethasone, amcinonide, beclomethasone, betamethasone, budesonide, clobetasol, clocortolone, hydrocortisone (cortisol), cortisone acetate, desonide, desoximethasone, dexamethasone, diflorasone, fludrocortisone, flunisolide, fluocinolone, fluocinonide, fluorometholone, flurandrenolide, halcinonide, medrysone, methyl prednisolone, momethasone, prednisolone, prednison, triamcinolone.

• Inhibitor biosintesa dan aksi dari steroid adrenokortikal:

a. Inhibitor biosintesa kortikosteroid: mitotane, metyrapone, aminoglutethimide, ketoconazole, trilostane.

b. Antiglucocorticoid: mifepristone.

E. Insulin dan obat hipoglisemik oral

• Insulin : a. Rapid: regular soluble crystaline,

human insulin Lispro, HI-aspart. b. Intermediate: NPH (isophane),

Lente.c. Slow: Ultralente, protamine zinc,

Glargine HI.

• Obat hipoglikernik Oral 1. Sulfonyl urea:

a. Generasi I: tolbutamide, chlorpropamide, tolazamide, acetohexamide. b. Generasi II: glyburide (glibenclamide), glipizide, gliclazide, glimipiride.

2.Biguanide: metformin.

3. Repaglinide4. Nateglinide. 5. Thiazolidinedione: rosiglitazone,

pioglitazone. 6. Alfa‑glucosidase inhibitors:

acarbose, miglitol.

• Glukagon, somatostatin dan diazoksid: obat untuk hipoglikemi.

F. Vasopresin (ADH), oksitosin

Vasopresin (ADH)• Vasopresin peptida alami :

Mamalia: arginin vasopresin (AVP), lypressin, phenypressin; Non marnalia: vasotocin; Invertabrata: arginin conopressin, lysine conopressin, locust subesophageal ganglia peptides.

• Vasopresin peptida sintetik : 1. V‑ I selective agonist : [Phe2,Ile3,

Orn8] AVP (selective V‑1a), Deamino[D‑3‑(3'‑pyridil) Ala2] AVP (selective V‑1b);

2. V‑2 selective agonists: Desmopressin deamino[Val4,D‑Arg8]AVP.

• Vasopresin peptide antagonists: 1. V‑1 selective antagonist:

d(CH2)5[Tyr(Me)2]AVP (V‑1a selective), dP[Tyr(Me)2] AVP (V‑1b selective;

2. V‑2 selective antagonist: des Gly‑NH2 9 d(CH2)5[ D‑Ile2,Ile4]AVP; d(CH2)5[D Ile2, Ile4, Ala NH2 9]AVP.

• Vasopresin non peptide antagonist:

1. V‑la selective: OPC‑21268, SR 49059,

2. V‑2 selective: SR 121463A, VPA‑985;

3. V‑1a/ V‑2 selective antagonist: OPC‑31260, YM 087

• Antidiuretik peptida yang tersedia: vasopresin, lypressine, desmopressin acetate.

Oksitosin :• Oxytocin, pitocin, syntocinon.• Oxytocin‑receptor antagonist:

atosiban.