HORMON DAN

ANTAGONIS HORMON
 HORMON

Berasal dari bahasa Yunani

όρμή: horman, artinya yang
menggerakkan, membangkitkan
 HORMON

 Zat aktif yg dihasilkan oleh kelenjar endokrin

 Kelenjar endokrin merpkn kelenjar yg tdk memilki
ductus, sekresi hormon langsung ke sirkulasi darah, kmd
menuju sel target.
 Jaringan yg dipengaruhi (SEL TARGET) umumnya
terletak jauh dari tempat hormon tersebut dihasilkan.
 Terbuat dari asam amino dan kolesterol
ANTAGONIS HORMON
 ZAT KIMIA YG MENGHAMBAT SINTESIS, SEKRESI MAUPUN
KERJA HORMON PD RESEPTORNYA
Contoh :
- HORMON ANTITIROID : Menghambat sintesis hormon
tiroid ... pada hipertiroidisme.
- KLOMIFEN menghambat kerja estrogen dg meniadakan
mekanisme umpan balik oleh estrogen shg sekresi
gonadotropin dr kelenjar hipofisis ttp tinggi.
 SISTEM
ENDOKRIN
 SISTEM
-ENDOKRIN
Dikendalikan oleh hipotalamus dan
kelenjar hipofisis.

- Bersama dg sistem saraf

mengkordinasikan dan mengatur sistem
tubuh.

- Mempertahankan homeostasis dengan

melepaskan zat kimia yang disebut
HORMON.
 ENDOKRIN VS SARAF

- Sistem saraf berkomunikasi secara lokal

melalui impuls listrik dan neurotransmitter
yang disalurkan melalui saraf ke saraf yag
lain atau ke organ target tertentu.
- Impuls saraf umumnya bekerja dlm milidetik
SISTEM SARAF
 ENDOKRIN VS SARAF
- Sistem endokrin melepaskan hormon ke
dalam sistem sirkukasi darah.
- Hormon kemudian dibawa melalui sistem
sirkulasi darah menuju sel target ke seluruh
tubuh.
- Hormon memiliki rentang waktu respon yg
luas (bekerja dlam hitungan detik, hari atau
bahkan lebih lama)
 Endokrin vs Saraf
o Terdapat hubungan yg dekat antara
sistem endokrin dan sistem saraf.
 SISTEM
ENDOKRIN
Proses-proses yang dikontrol oleh sistem
endokrin :
1. Pertumbuhan dan perkembangan
2. Reproduksi
3. Pertahanan tubuh
4. Keseimbangan air, elektrolit dan
nutrisi
5. Pengaturan metabolisme selular dan
keseimbangan energi
Obat2 endokrin
HORMON
Sumber :
- Alamiah (dari binatang)
- senyawa semi sintetik atau sintetik.
- Indikasi:
a. Replacement therapy
b. Pengobatan gangguan tertentu
c. Untuk diagnostik
Obat-obat Endokrin
I. Hormon Hipotalamus dan pituitari
II. Hormon Steroid
A. Hormon gonad
1. Estrogens
2. Progestins
3. Androgens
B. Hormon adrenal kortex
1. Adrenokortikosteroid
2. Adrenal Androgen
III. Hormon tiroid dan obat-obat untuk gangguan tiroid
IV. Obat antidiabet
Hypothalamic & Pituitary
Hormones
Hypotalamus
- Organ endokrin utama
- mensekresi releasing/inhibiting
hormones
KELENJAR PITUITARI
- Berat 600 mg, berada pada sella turcica
di bawah lapisan dura mater di otak
- Terdiri dr 2 lobi
a. Lobus anterior
b. Lobus posterior lobe
 Hormon2 HIPOTALAMUS & PituitarI
Hypothalamic Hor mone Pituitary Target Or gan Target Organ
Horm one Hor m one
1. Growth Hor m one – Growth Hor mone (GH) Liver Somatomedi ns
Releasing Hor m one aka: Somatotropin
(G HRH)
aka: Sermorelin
2. Growth H or m on e – Inhibits Growth Hor mone
Inhibiting Hor m one (GHIH)
aka: Somatostatin
3. Corticotropin – Releasing Adrenocorticotropic Adrenal Cortex Glucocorticoids
Horm on e (CRH) Hor mone ( ACTH) Mineralocorticoids
aka: Corticotropin Adrenal Androgens
4. Thyrotropin – Releasing Thyroid – Stimulating Thyroid Gland T 3 (Triiodothyronine)
Horm on e (T RH) Hor mone (TSH) T 4 (Thyroxine)
aka: Thyrotropin
5. Gonadotropin – Releasing
Horm on e (GnRH) or Gonadotropins Ovaries (Females) Estrogen (by FSH)
Luteinizing H or m on e – a. Follicle Testes (Males) Progesterone (by L H
Releasing Hor m one Stimulating in females)
(L HRH) H or mon e (FSH) Testosterone (by L H
b. Luteinizing Hor m on e in males)
(LH)
6. Prolactin – Releasing Prolactin Breasts
Horm on e (PRH)

7. Prolactin – Inhibiting Inhibits Prolactin

Horm on e (PIH)

8. Oxytocin Stored in the Posterior

Pituitary Gland
9. Vasopressin Stored in the Posterior
Pituitary Gland
Growth Hormone
 GROWTH HORMONE (GH)
- Somatotropin, Asellacrin
- Senyawa polypeptide yg besar, terdiri : kurang
lebih 191 asam amino (BM: 21,500)
- Dilepaskan oleh pituitari anterior sbg respon
thd GHRH (growth hormone releasing
hormone /Sermorelin) yg dihasilkan
hipotalamus.
- Secara sintetik diproduksi melalui recombinant
DNA technology
Growth Hormone (GH)
- Hormon dari binatang tdk efektif pd manusia.
- Menginduksi pelepasan somatomedin di liver.
- Meningkatkam proliferasi sel dan
pertumbuhan tulang pd epifisis terbuka.
- mendorong synthesis cartilage/tulang rawan.
Growth Hormone (GH)
Indikasi:
- Perawatan panjang pada kasus
defisiensi hormone pertumbuha pd
anak (Dwarfism)
- Anak pendek yg tdk kekurangan GH (dpt
tumbuh sampai 2 cm per tahun)
Dwarfism
SOMATREM
- Obat yg secara terapeutik setara dengan
growth hormone
- Mengandung extra terminal gugus
methionyl.
Growth Hormone Inhibiting
Hormone
Growth Hormone Inhibiting
Hormone (GHIH)
Hormon penghambat hormon pertumbuhan

- Somatostatin
- Menghambat Growth Hormone
- Indikasi:
Pituitary Gigantism (pre-pubertal)
Acromegaly (post-pubertal)
Pituitary Gigantism
Acromegaly
macrognathia (rahang besar)
wide-spaced teeth
macroglossia
thickened lips
broad nose
enlarged joints
cardiomegaly
organomegaly
Octreotide
- analog octapeptide sintetik dari
somatostatin
- 45x lebih potent dari GHIH
Adrenocorticotropic Hormone
Adrenocorticotropic Hormone (ACTH)

- Corticotropin, Acthar
- Rantai tunggal polypeptide yg mengandung 39
asam amino
- precursor: pro-opiomelanocortin
- Dilepaskan oleh pituitary anterior sbg
respons terhadap CRH (cronotropic
releasing hormone) yg diproduksi oleh
hypothalamus
Adrenocorticotropic Hormone (ACTH)

- Menstimulasi adrenal cortex untuk memproduksi

adrenocorticosteroid & androgen
- Digunakan terutama untuk diagnosis dan membedakan
primer dan & sekunder insuffisiensi adrenal.
- Primer : Addison’s Disease disebabkan adrenal atrophy
- Sekunder: disebabkan kurangnya sekresi ACTH oleh
kelenjar pituitari
ADDISON’S DISEASE
• hyposecretion of adrenocorticosteroids

• gejala:
– anorexia
– dehydration
– weakness and lethargy
– hyperpigmentation (bronze-colored skin)
CUSHING’S SYNDROME
• hypersecretion of adrenocorticosteroids

• characterized by:
– moon face
– buffalo hump
– pendulous abdomen
– hypertension
Cushing's Syndrome
Cosyntropin
- Human ACTH sintetik
- Lebih disukai dari pada animal ACTH dpt
menyebabkan reaksi alergi
Thyrotropin Stimulating
Hormone
THYROTROPIN STIMULATING HORMONE
(TSH)

- : Thyrotropin
- dilepaskan oleh pituitary anterior sbg
respons terhadap TRH (Co: Protirelin)
yg dihasilkan hipotalamus
- Merangsang thyroid untuk memproduksi T3
and T4
- T3: triiodothyronine (most active)
- T4: thyroxine (diubah menjadi T3 dlm tubuh
Thyrotropin Stimulating Hormone (TSH)

- Hormon tiroid T3 and T4 sangat

esensial untuk pertumbuhan normal
dan maturasi tubuh
- Kondisi:
hypothyroidism
hyperthyroidism
HYPOTHYROIDISM
- Ketidakmampuan kelenjar thyroid untuk
mensupply hormon tiroid yg cukup di
dlm tubuh

- Manifestasi:
Cretinism (infant-state)
Myxedema (adult-state)
CRETINISM
- Hypothyroidism saat bayi
- Ditandai dengan hambatan
perkembangan fisik dan mental
Myxedema
- Hypothyroidism pada saat dewasa
- Ditandai dengan:
• bradycardia
• Kelemahan dan kelesuan
• Kulit dan rambut kering
• kedinginan
• gondok
Hyperthyroidism
- Kelebihan hormon tiroid dalam tubuh
- thyrotoxicosis
- Bentuknya berupa:
Graves’ Disease – umum
Plummer’s Disease – jarang
- dengan abnormalitas jantung
Graves' Disease
Gonadotropins
GONADOTROPIN
- Meliputi :
Follicle-Stimulating Hormone (FSH)
Luteinizing Hormone (LH)
- Dilepaskan oleh kelenjar pituitary anterior sbg
respons terhadap GnRH / LHRH
- Stimulasi kelenjar gonad (ovarium & testes)
untuk memproduksi sex hormone
- Wanita : FSH  estrogen
LH  progesterone
- Pria : LH  testosterone
Gonadotropins
NOTE:
Pituitary gonadotropin (FSH, LH) tidak
tersedia untuk penggunaan terapi, tetapi
terdapan non-pituitary gonadotropins yang
memiliki aktivitas FSH-like atau LH-like
dan salah satu yg digunakan dlm terapi.
Non-Pituitary Gonadotropins

1. Menotropin
2. Urofollitropin
3. Human Chorionic Gonadotropin
Non-Pituitary Gonadotropins
- Indikasi:
wanita: untuk induksi ovulasi &
kehamilan
pria: untuk menginduksi spermatogenesis

- Adverse effects:
Pembesaran ovarium
multiple births
gynecomastia pada pria
Menotropin
- Contoh:
Human Menopausal Gonadotropin
(hMG)
Pergonal®
- Diperoleh dari urine Wanita post-
menopause
- Sebagian dipecah menjadi FSH and LH di
dalam tubuh.
Urofollitropin
- Metrodin®
- Diperoleh dari urine Wanita post-
menopause
- Memiliki aktivitas FSH-like yg
tinggi
Human Chorionic Gonadotropin
- Contoh obat: hCG, Follutein®
- placental hormone
- Memiliki efek LH agonis
- Diperoleh dari urine Wanita hamil
Hormone Kelenjar Pituitari
Posterior
Hormon Kelenjar Pituitari
Posterior
1. Oxytocin
2. Vasopressin
Oxytocin
- stimulasi kontraksi uterus dan berperan penting
dlm induksi persalinan
- Juga mendorong keluarnya ASI
- Indikasi:
Induksi kontraksi saat persalinan
Untuk mengontrol postpartum bleeding
- Kontraindikasi:
Presentasi janin yg tdk normal
Gawat janin
premature births
Oxytocin
Vasopressin
- Antidiuretic Hormone (ADH)
- Mempunyai efek antidiuretik dan
activitas vasopressor
- Bekerja di ginjal, menyebabkan
reabsorpsi air pada tubula pengumpul
-Indikasi:
Diabetes Insipidus
Postoperative Abdominal Distention
Diabetes Insipidus (DI)
- Gangguan yg disebabkan defisiensi atau
kurangnya respons Antidiuretic Hormone
(ADH)
- 2 Tipe:
a. Central DI - defisiensi ADH
b. Nephrogenic DI - cukup ADH
Tetapi tubuh tdk respon
terhadap hormon
Desmopressin

- Modified analog of vasopressin

- Lebih sering digunakan untuk DI dan
nocturnal enuresis karena lebih besara
efek free of pressor dan bekerja lebih
Panjang.
Hormone Steroid
 Hormon Steroid

- Mengandung inti steroid, CPPP

cyclopentanoperhydrophenanthrene
Hormon Steroid

• Carbon 3 & Carbon 17

• -OH (sterol)

• =O (sterone)
Gonadal / Sex Hormones
Hormon Steroid
A. Gonadal / Sex Hormones
1. Estrogens
2. Progestins
3. Androgens
B. Hormon Cortex Adrenal
1. Adrenocoticosteroid
a. Glucocorticoids
b. Mineralocortic
oids
2. Adrenal Androgen
Gonadal / Sex Hormones
Estrogen
Estrogens
- Inti dasar : estrane

Estradiol
Estrogen
- Efek:
1. Maturasi dan perkembangan normal
wanita
2. Menghambat resorpsi tulang
3. Meningkatkan HDL, menurunkan
LDL
4. Menurunkan adhesifitas platelet
Estrogens
- Indikasi:
kontrasepsi
postmenopausal hormone therapy
primary hypogonadism osteoporosis
Steroidal Estrogen Alamiah
Estradiol – estrogen paling poten
yg dihasilkan pd wanita
Estrone, Estriol – mempunyai efek 1/10
potensi estradiol
* Premarin – sediaan conjugated estrogens
(sulfate esters of estrone & equilin)
- Diperoleh dari urine kuda hamil
Premarin
Synthetic Steroidal Estrogens
Ethinyl estradiol
Mestranol
Quinestrol
Synthetic Nonsteroidal
Estrogens
Diethylstilbestrol – dpt menyebabkan
adenocarcinoma dg pada servik dan
vagina pd anak perempuan yg
menggunakan obat pd awal kehamilan
Estrogen Antagonis/
Antiestrogen
Clomiphene – obat penyubur,
menginduksi ovulasi melalui
negative feedback mechanism.

Tamoxifen & Toremifene - palliative

treatment of advanced breast cancer in
postmenopausal women
Estrogen Related Drugs
Aromatase Inhibitors
Selective Estrogen Receptor Modulators
Aromatase Inhibitor
- non-steroid aromatase inhibitor yg poten
dan selektif, suatu enzim yg
bertanggung jawab mengkonversi
androgen menjadi estrogen.
- Digunakan pada pengobatan advanced
breast cancer
- Anastrozole, Letrozole
SERMs
- Selective Estrogen Receptor Modulators
- Mengurangi resorpsi tulang dan
menurunkan turnover tulang
- Digunakan untu pencegahan
osteoporosis
- Raloxifene
Progestin
Progestin
- Inti dasar : pregnane
Progestin
- Efek:
1. Perubahan endometrium
2. Perkembangan alveolobular
secretory apparatus pada payudara
3. Hepatic glycogenesis &
ketogenesis
4. Meningkatkan aktivitas lipoprotein
lipase dan deposisi lemak
Progestin
- Indikasi:
kontrasepsi
Untuk menstrual disorders
-dysfunctional uterine bleeding
-dysmenorrhea
endometriosis
 Natural Progestin
Progesterone
- progestin endogen yg diproduksi sbg
respon sthd luteinizing hormone (LH)
- Juga disintesis dlm adrenal cortex
- Pada Wanita, menyebabkan peningkatan
sekret endometrium yg membantau
implantasi pada proses pembentukan embryo
baru.
Synthetic Progestins
- Lebih stabil thd first-pass metabolism, bisa
digunakan scr oral dg dosis lebih rendah
- medroxyprogesterone
hydroxyprogesterone
megestrol norethindrone
norgestrel
Progestin Antagonist /
Antiprogestin

Mifepristone
Contoh : RU 486
- Progestin antagonist dg partial
agonist activity
- Dapat menyebabkan abortus bayi
Oral & Implantable
Contraceptives
Major Classes
1. Combination Pills
2. Progestin Only Contraceptives
3. Postcoital Contraceptives
Combination Pills
- contain both estrogen and progestin
- provided as 21 day or 28 day-packs
- most common type of oral contraceptives
- estrogen: suppresses ovulation ethinyl
estradiol - most common mestranol
Combination Pills
- progestin: prevents implantation in the
endometrium and makes the cervical mucus
impenetrable to the sperm
norethynodrel
norethindrone
norgestrel
Progestin Only Contraceptives
- kurang efektif dibandingkan combination
pills
- dosage forms/ delivery systems:
a. “mini-pill” - low dose progestins
350 g norethindrone or
75 g norgestrel
b. progestin implants - subdermal implant of
216 mg of norgestrel (Norplant®)
effective for 5 years
Progestin Only Contraceptives
c. intramuscular - given every 3 months
150 mg of medroxyprogesterone
acetate (Depo-Provera®)
Progestin Only Contraceptives

d. intrauterine device (IUD) - for yearly

insertion; Progestasert®
Postcoital Contraceptives
- called, “morning-after pills”
- high dose estrogen administered within 72
hours after coitus and continued 2x for 5
days
- ethinyl estradiol
diethylstilbestrol
conjugated estrogens
estrone
Androgen
Androgen
- Inti dasar : androstane

Testosterone
Androgen

- group hormon steroid yg mempunyai

efek anabolic dan/atau efek maskuliin
pad Wanita maupun pria
 Androgen Endogen
Testosterone
- androgen endogen yg utama
- Disintesis oleh Leydig cells di testes pria
dan dlm jumlah kecil pd sel ovarium
wanita, dan di kelenjar adrenal
- Diproduksi sbg response thd LH
Synthetic Androgen
Methyltestosterone
Danazol Stanozolol
Nandrolone
 Penggunaan terapi
1. Androgenic Effects
- in hypogonadism in males
2. Anabolic Effects
- pd senile osteoporosis, luka bakar yg
luas, recovery cepat setelah pembedahan
atau penyakit kronis yang melemahkan
3. Endometriosis (Danazol)
Unapproved Use

 Digunakan untuk meningkatkan massa tubuh , kekuatan otot

dan agresivitas atlit dan body builders (Nandrolone &
Stanozolol)
Antiandrogen
- Menghambat kerja androgens melalui
gengguan terhadap sintesis atau melaui
blocking thd reseptor
a. Finasteride – digunakan pada terapi
Benign Prostatic Hypertrophy (BPH)
Antiandrogen
b Flutamide - for prostatic carcinoma

c. Cyproterone acetate - for hirsutism in

females
Hormones of the Adrenal
Cortex
Hormones of the Adrenal Cortex

1. Adrenocorticosteroids
a. Mineralocorticoids
b. Glucocorticoids
2. Adrenal Androgens
Adrenal Cortex
3 Zone:
1. Zona glomerulosa
- memproduksi mineralocorticoid
2. Zona fasciculata
- Memproduksi glucocorticoid
3. Zona reticularis
- memproduksi adrenal androgen
Adrenal Cortex

Zona glomerulosa

Zona fasciculata

Zona reticularis

Kidney
Mineralocorticoid
- Mempunyai efek retensi natrium dan
sekresi kalium.
- Mengatur keseimbangan cairan dan
elektrolit.
- Endogen : aldosterone
desoxycorticosterone
- Sintetik : fludrocortisone
Glucocorticoid
- Endogen : Cortisol
Cortisone
Corticosterone
Hydrocortisone
- Berperan pada metabolisme karbohydrat,
lemak dan protein
- Meningkatkan respon pada otot polos vascular dan
bronchus terhadap katekolamin
Glucocorticoid
Sedian obat:
Prednisone Betamethasone
Methylprednisolone Dexamethasone
Triamcinolone
- Memiliki efek anti-inflammasi, dan anti-
alergi, imunosupressan
- Menghambat pertumbuhan dan pembagian
sel
- Memiliki efek katabolik terhadap protein
dan tulang.
Glucocorticoid
Penggunaan terapi :
anti alergi
Peradangan pada sendi dan tulang
Penyakit kulit
Organ transplant immunosuppression
Pulmonary Diseases: Bronchial Asthma
COPD
Glucocorticoid
Adverse effects: Cushing’s
syndrome Adrenal
suppression osteoporosis
PUD (peptic ulcer disease)
impaired wound healing
increased susceptibility to infection
hyperglycemia/DM
cataract
Addison’s Disease
• hyposecretion of adrenocorticosteroids

• Gejala :
– anorexia
– dehydration
– weakness and lethargy
– hyperpigmentation (bronze-colored skin)
Cushing’s Syndrome
• hypersecretion of adrenocorticosteroids

• Gejala :
– moon face
– buffalo hump
– pendulous abdomen
– hypertension
Cushing's Syndrome
HORMON TIROID DAN
OBAT2 UNTUK GANGGUAN
TIROID
Kelenjar tiroid
Synthesis Hormone Thyroid
1. Iodide uptake
2. Peroxidation of iodide to iodine
3. Organification of iodine
4. Coupling reaction: DIT + DIT  T4
MIT + DIT  T3
5. Proteolysis
6. Peripheral conversion of T4 to T3
Thyroid Hormones
- Hormon tiroid T3 dan T4 penting
dalam pertumbuhan normal dan
maturasi tubuh.
T4
- thyroxine
- Diubah menjadi T3 melalui proses
enzyme deiodinase
- 99.98% protein terikat thyroxine-
binding globulin
- 0.02% dalam bentuk bebas
- half-life: 7 days
 T3
- triiodothyronine
- Bentuk aktif
- 3-4x lebih poten daripada T4
- Bertanggung jawab pd Sebagian besar efek
hormone tiroid
- Memiliki afinitas ikatan yg besar dg reseptor
- 99.8 % terikat protein
- 0.2% is in free form
- half-life: 1.5 days
Hypothyroidism
- Ketidakmampuan kelenjar tiroid untuk
supply hormon tiroid dlm jumlah yg
mencukupi kebutuhan tubuh
- manifestations:

Cretinism (infant-state)
Myxedema (adult-state)
Cretinism
- infant-state hypothyroidism
- characterized by physical and mental
retardation
Myxedema
- adult-state hypothyroidism
- Gejala :
• bradycardia
• weakness and lethargy
• dry skin and hair
• coldness
• goiter
Sediaan hormone tiroid
Preparation T4:T3 ratio
Thyroid, USP
Beef 4:1
Pork 2-3:1
Thyroglobulin 2:1
Levothyroxine Pure T4
Levothyronine Pure T3
Liotrix 4:1
Hyperthyroidism
- overabundance of thyroid hormone in
the body
- thyrotoxicosis
- Forms:
Graves’ Disease - most common
Plummer’s Disease - less common
- with cardiac abnormalities
Graves' Disease
Antithyroid Drugs
1. Thioamides
2. Inorganic Anions/Anionic Inhibitors
3. Iodides
4. Radiocontrast dyes
5. Beta-blocker
6. Dexamethasone
7. Radioactive Iodine
Thioamides
- MoA: inhibit iodine organification and
coupling
- examples:
Propylthiouracil (PTU)
Methimazole
Carbimazole
- ES :
pruritic maculopapular rash
agranulocytosis
Inorganic Anions
- Anionic Inhibitors
- MoA: mengganggu penyerapan iodium
menyebabkan keluarnya yodium intra tiroid
- examples:
Potassium perchlorate
Potassium thiocyanate
- ES:
aplastic anemia, nephrotic
syndrome
Iodides
- MoA: inhibit pembentukan dan pelepasan
hormone.
- Menurunkan ukuran dan vaskularisasi gondok
- examples:
KISS - Potassium iodide saturated solution
Lugol’s solution - strong iodine
solution
Beta-blocker
- MOA: menguarngi gejala sebg
manifestasi hipotiroid pada saraf
sympathetic, dpt juga menghambat
peripheral conversion dari T4
menjadi T3
- Propranolol
Dexamethasone
- MOA: inhibits peripheral conversion of
T4 to T3
Radioactive iodine

- 131I
- MOA: destruction of thyroid cells by
emission of high-energy beta radiation
- can offer cure
- Contraindicated to pregnant women or
women who will become pregnant
Anti-diabetic Agents
Pancreas
- is a mixed gland
- Exocrine portion
-releases pancrealipase &
chymotrypsin
- Endocrine portion
-1million islets of
Langerhan
-have at least 4 hormone-producing
cells
Endocrine Pancreas
Cell Type % islet Hormone
A (alpha) 20 glucagon
proglucagon
B (beta) 75 insulin
pro-insulin
D (delta) 3-5 somatostatin
F (PP cell) <2 pancreatic
polypeptide (PP)
Diabetes Mellitus (DM)
- diabetes = Greek “siphon”
mel = honey
- “something sweet is passing through or
siphoning from the body”
- Suatu gangguan metabolic dimana kadar
glucose dalam darah terlalu tinggi dan
mulai terbuang ke dlm urine karena
tubulus ginjal tdk mampu resbsorbsi dg
cukup cepat.
Types of DM
Type 1
Type 2
Gestational DM
Secondary DM
Type 1
- insulin-dependent DM (IDDM)
- juvenile-onset DM
- ketosis-prone diabetes
- most common in children
- insulin secretion is destroyed
- dependent upon exogenous insulin to
sustain life
Type 2
- non-insulin-dependent DM (NIDDM)
- adult-onset DM
- not insulin dependent
- endogenous insulin levels may appear
normal or increased but beta-cell
dysfunction is manifested by a relative
insulin insufficiency
Gestational DM
- defined as any degree of glucose
intolerance that has its onset during
pregnancy
Secondary DM

 broad term used to classify patients who have

unusual causes of DM due to certain diseases of
the pancreas, endocrinopathies or drugs
3 gejala DM
1.Polyuria - excessive urination to flush
out the glucose and ketones

2.Polydipsia - excessive thirst resulting

from water loss

3.Polyphagia - excessive hunger due to

inability to use sugars and the loss of fats
and proteins from the body
Insulin
- is the storage and anabolic hormone of the body
- produced by the Beta-cells of the
pancreas
- Hormon utama yg dibutuhkan untuk proses
metabolin normal
- previously extracted from beef/pork
pancreas
- now is produced via recombinant DNA
Insulin - Effects
1.It facilitates transport of glucose across
cell membrane
2.In the liver, it promotes glycogenesis
and gluconeogenesis
3.In the muscles, it increases amino acid
transport, protein synthesis and
glycogenesis
4.In adipose tissues, it increases
triglyceride storage
Insulin - Indications
• Diabetes Mellitus Type 1
• Diabetes Mellitus Type 2 that cannot be
controlled by diet, exercise and oral
hypoglycemic agents (OHAs)
• Ketoacidosis
• Diabetic coma
Insulin Preparations
Pharmakokinetic Species Type Activity in hours
Type Peak Duration
Ultra rapid-acting Human
Insulin Lispro (Modified) 0.25 – 0.50 3–4

Rapid acting
Insulin injection, USP Human, Pork 0.50 – 3 5–7
(Regular, Crystalline)
Intermediate acting
NPH Insulin Human, Pork 8 – 12 18 – 24
(Isophane)
Lente Insulin Human, Pork 8 – 12 18 – 24
(Insulin zinc susp)
Long acting
Ultralente Insulin Human 8 – 16 18 – 28
(Insulin zinc susp
extended)
Ultra long acting
Insulin glargine Human No peak > 24
(Modified)
Oral Hypoglycemic Drugs
• Insulin secretagogues
• Biguanides
• Alpha-glucosidase inhibitors
• Thiazolidinedione derivatives
Insulin Secretagogues
• Sulfonylureas
• Meglitinides
Sulfonylureas
MOA:
- stimulate pancreatic release of insulin
- inhibit pancreatic release of glucagons
- increase insulin receptor binding
- decrease hepatic extraction of insulin
Sulfonylureas
IstGeneration
 Chlorpropamide Acetohexamid
Tolbutamide e Tolazamide

2nd Generation
 Glibenclamide
Glipizide
Gliclazide
Glimepiride
Sulfonylureas
Side-effects:
hypoglycemia
blood dyscrasias
disulfiram-like reactions with 1st Gen
and glipizide
weight gain
Meglitinide
- MOA: increase pancreatic insulin
secretion
- short duration of action: 1 to 3
hours
- examples: Repaglinide
Nateglinide
- S/E:
hypoglycemia
weight gain
Biguanide
- unknown MOA
- reduce blood glucose level even in the
absence of beta cell function
- proven as a useful initial therapy among DM
Type 2 patients, especially among obese
patients
- not associated with hypoglycemia
- ex. Metformin (most proven)
Phenformin ( no longer available)
- S/E: lactic acidosis, megaloblastic
anemia
Alpha-glucosidase inhibitors
- MOA: competitive inhibition of intestinal alpha-
glucosidase enzyme, preventing digestion of
dextrins and disaccharides into absorbable
monosaccharides

- examples: Acarbose
Voglibose
Miglitol
- S/E: flatulence, potential hepatotoxicity of
acarbose
Thiazolidinedione derivatives
- MOA: insulin sensitizers - increase
skeletal muscle sensitivity to insulin;
they also decrease hepatic
gluconeogenesis
- examples: Rosiglitazone
Pioglitazone
- S/E: Hepatic failure (reason for the
withdrawal of Troglitazone), edema and
mild anemia
Let’s see how much
you can recall… :)
Question 1:
Which of the following is generally true of
hormones?
A. Exocrine glands produce them.
B.They travel throughout the body in the
blood.
C.They affect only non-hormone
producing organs.
D.All steroid hormones produce very
similar physiologic effects in the body.
B
Question 2:
All of the following substances are
endogenous tropic hormones secreted by
the pituitary gland EXCEPT:
A. Somatotropin
B. hCG
C. FSH
D. TSH
E. Corticotropin

B
Question 3:
Which of the following is secreted by the
posterior pituitary gland?
A. Luteinizing Hormone
B. ACTH
C. Oxytocin
D. Thyrotropin
E. Growth Hormone

C
Question 4:
ACTH or Adrenocorticotropic Hormone is
released by the anterior pituitary gland in
response to which hypothalamic
hormone?
A. GnRH
B. TRH
C. GHIH
D. CRH
E. PRH
D
Question 5:
All of the following are steroidal hormones
except:
A. testosterone
B. levothyroxine
C. cortisone
D. dexamethasone
E. estradiol

B
Question 6:
Which of the following insulins can be
administered IV?
A. Lente insulin
B. Isophane insulin
C. Protamine Zinc Insulin
D. Ultralente insulin
E. Regular insulin

E
Question 7:
It is a fertility drug. It induces ovulation by
negative feedback mechanism.
A. Tamoxifen
B. Ethinyl estradiol
C. Clomiphene
D. Finasteride
E. Prednisone

C
Question 8:
Which of the following is not properly
paired with its indication?
A. testosterone - hypergonadism
B. finasteride - BPH
C. cyproterone - hirsutism
D. PTU - hyperthyroidism
E. Tamoxifen - estrogen-dependent
breast cancer
A
Question 9:
Which of the following drugs can be used
for rheumatoid disorders?
A. diethylstilbestrol
B. triiodothyronine
C. methimazole
D. betamethasone
E. metformin

D
Question 10:
Which of the following is a sulfonylurea?
A. metformin
B. repaglinide
C. acarbose
D. rosiglitazone
E. glibenclamide

E
“Success is to be measured not so much by the
position that one has reached in life, but by the
obstacles which he has overcome.”

- Booker T. Washington
Thank You for Listening!