Obat Antianemia

7/25/2019 Obat Antianemia

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OBAT ANTIANEMIA

EVI SOVIA


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Anemia: penurunan konsentrasi seldarah merah atau hemoglobin

Kriteria anemia: Wanita: b ! "# g$dl atau hematokrit !

%&'

(aki)laki:b ! "* g$dl atau hematokrit !*+'


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Anemia

#ndmost presenting mani,estation o,disease- .ith pain being the /rst0

It is de/ned as: lo. hemoglobin- lo. 1B23ount and lo. 1B2 mass0

4suall5 presents .ith pallor- ,atigabilit5-.eakness and pale 3on6un3ti7ae

In order to properl5 treat the anemia- 5oumust determine the 3ause0


4/49

2auses o, Anemia

"0 8iminished produ3tion and orrepla3ement o, red blood 3ells0

#0 E93essi7e breakdo.n and loss o,red blood 3ells0

emodilution .hile not a 3ause o,anemia- it does 3ause an anemia)like

ee3t0


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"0 8iminished ;rodu3tion$1epla3emento, 1B2 de/3ien35 o, ?e 1B2 de/3ien35 o,Er5thropoietin

2aused b5 3ompromised renal ,un3tion0

Ma3ro35ti3 Anemia) de/3ien35 o, ,oli3 a3idand B"#

8iminished 3ell di7ision and release o, larger 3ellsin 3ir3ulation0


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#0 Breakdo.n o, 1B2


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Obat)obat Antianemia

;iridoksin 4ntuk terapi anemia sideroblastik

idroksiurea 4ntuk terapi si3kle 3ell disease

8e,eroksamin 4ntuk mengkhelat besi pada iron

loading anemia

;rednison 4ntuk anemia hemolitik


8/49

Siklosporin dan antitimosit globulin 4ntuk anemia aplastik

Siklo,os,amid dosis tinggi dan iradiasi

seluruh tubuh 4ntuk anemia aplastik- sindroma

mielodisplastik- talasemia dan anemiasel sabit

Besi 4ntuk anemia hipokrom mikrositer 5ang

berhubungan dengan de/siensi besi


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Vitamin B"# dan ,olat 4ntuk anemia megaloblastik

Eritropoietin 4ntuk anemia pada pen5akit gin6al

stadium akhir dan anemia 5angberhubungan dengan kanker tertentu


10/49

Besi ?e

8iberikan se3ara peroral atauparenteral pada kasus 5ang berat

;emberian preparat besi Cmeningkatkan ke3epatan produksisel darah merah sesuai dengan

6umlah besi 5ang tersedia dalam sel

eritroid sumsum tulang


11/49

Iron 253le

D ) "+'o, ingested

iron is absorbed

On3e ingested thea3idin the stoma3h:

"0 Aids inioniation o, iron #0 Splits 3helated

,ood iron,rom3helator

%0 Maintains iron

in soluble ,orm *0 Allo.s iron to

remain in theabsorbable ,orm?e%F


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Me3hanism o, Iron Absorption


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Therapeuti3 uses o, Iron

Iron 8e/3ientAnemia

;regnan35

;remature Babies

Blood loss

ook.ornin,estation

MalabsorptionS5ndrome

@I Bleeding due to: 4l3ers Aspirin

E93ess 3onsumptiono, 3oee


14/49

Iron ;reparations

Oral Iron

?errous Sul,ate?eosol > %++ mg tid Side Ee3ts are e9tremel5 mild:

Nausea- upper abdominal pain- 3onstipation ordiarrhea0

2heapest,orm o, Iron and one o, the most.idel5 used

;arenteral Iron 8e9tranIm,eron > IM or IV

Indi3ated ,or patients .ho 3annot tolerate orabsorboral ironor .here oral iron isinsuG3ient to treat the 3ondition ie0Malabsorption s5ndrome- prolonged sali35late

therap5- dial5sis patients


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;emberian at besi C produksi seldarah merah H

1OA: p0o atau parenteral

Absorpsi meningkat bila diberikanbersama as3orbate mereduksi besidari bentuk ,erri men6adi ,erro

8istribusi: plasma trans,erin proteinglikoprotein


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O7erdosis ?e C muntah- gastritishemoragik- hipotensi- letargi

Terapi C gastrik la7age dengansodium bi3arbonat dan pemberiande,eroksamin


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To9i3it5 o, Iron O7erdose

D+++ deaths$5earin the 4S- usuall5 in3hildren

#+' o, 3hildren presenting .ith ironto9i3it5 .ill die

" to # grams are suG3ient to 3ause death

At high doses- Iron is absorbed throughpassi7e diusion .ith no regulation


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Iron > 2lini3al Ee3ts

Earl5 3hanges Vomiting- diarrhea Blood Volume 1 T;1ree9

A3idosis ,rom Iron o9idation- Krebs 353le and

anaerobi3 metabolism 3itri3 a3id and la3ti3

a3id

Intermediate 3hanges Impro7ement short li7ed pro,ound sho3k

and 2V 2ollapse epati3 ?ailure- 6aundi3e-pulmonar5 edema and death

(ate Stage Intestinal s3arring- ,att5 a3id degeneration o,

li7er- 3irrhosis and death0


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Treatment o, Iron O7erdose

To9i3 le7els A(8 > #++)%++mgkg- plasma iron J %++ug$dl

AB2


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Vitamin B"# ada dalam # bentukkoenim: M2B metil B"# dandeoksiadenosilkobalamin

deoksiadenosil B"#

M2B


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Vitamin B"# Absorpsi: memerlukan ,aktor intrinsik

glikoprotein 5ang dihasilkan oleh sel

parietal Anemia pernisiosa C ,ungsi sel parietal

)

8istribusi: terikat dengan plasma

globulin kemudian ditranspor ke6aringan terutama hati dan disimpansebagai koenim

Siklus enterohepatik C

mempertahankan konsentrasi 7it B"#


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Vitamin B"#

Sour3e: In ,ood- espe3iall5 in li7er andkidne5s0 @I Mi3roorganism s5nthesis- VitaminSupplements 25ano3obalamin

Ne3essar5 ,or normal 8NA s5nthesis

Absorption o, B"#

"0 Intrinsi3 ?a3tor lo. dose: a protein made b5stoma3h parietal 3ells that binds to B"# and deli7ers it,rom the ileum 7ia a 3al3ium mediated e7ent0

#0 Mass A3tion igh dose: "+++mg$da5- absorbed7ia passi7e diusion


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B"#8e/3ien35

A B"#de/3ien35.ill 3ause peripheral

neuropath5 and a ma3ro35ti3 anemia- aperni3ious anemia0

?oli3 A3idadministration 3an 3orre3t thema3ro35ti3 anemia but .ill ,ail to 3orre3tthe peripheral neuropath50

To treat the neuropath5- Vit B"#must be

utilied0


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Therapeuti3 4ses o, B"# 8ail5 1eLuirements ) +0)"0+ mh$da5 T

"$#

"5ear

;erni3ious Anemia

Impaired @I absorption o, B"#

@astre3tom5

2orrosi7e In6ur5o, @I mu3osa

?ish tape .orm: .orm siphons o B"#

;la3ebo abuse .ith B"#- espe3iall5 in elderl5

patients0


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Asam ,olat 8alam makanan: pol5glutamat

8ihidrolisis oleh karboksipeptidase-

direduksi men6adi dihidro,olat reduktasedidalam intestin

8imetilasi men6adi MT? methen5l

tetrah5dro,olate kemudian ditransportke 6aringan

Siklus enterohepatik


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?oli3 A3id

Sour3e in ,ood > 5east- egg 5olk- li7er and lea,57egetables

?oli3 A3id ?0A0 is absorbed in the smallintestines0

?0A0 is 3on7erted to tetrah5dro,olate b5dih5dro,olate redu3tase0

?oli3 A3id de/3ien35 ?0A0 8e/3ien35 is also 3alledWill


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Therapeuti3 4ses o, ?oli3 A3id

"0 Megaloblasti3 Anemiadue toinadeLuate dietar5 intake o, ,oli3 a3id

2an be due to 3hroni3 al3oholism- pregnan35-in,an35- impaired utiliation: uremia- 3an3er orhepati3 disease0

#0 To alle7iate anemiathat is asso3iated.ith dih5dro,olate redu3tase inhibitors0

i0e0 Methotre9ate2an3er 3hemotherap5-;5rimethamineAntimalarial

Administration o, 3itro7orum ,a3tormeth5lated

,oli3 a3id alle7iates the anemia0

Therapeuti3 4ses o, ?oli3 A3id


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Therapeuti3 4ses o, ?oli3 A3id3ont

%0 Ingestion o, drugs that inter,ere .ithintestinalabsorptionand storage o, ,oli3 a3id0

Me3hanism) inhibition o, the 3on6ugases that breako ,oli3 a3id ,rom its ,ood 3helators0

E90 > phen5toin- progestin$estrogens oral3ontra3epti7es

*0 Malabsorption > Sprue- 2elia3 disease-

partial gastre3tom50

D0 1heumatoid arthritis> in3reased ,oli3 a3iddemand or utiliation0


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;iridoksin Vitamin B

8igunakan untuk anemiasideroblastik ditandai dengan inti seldarah merah 5ang mengandung

partikel besi C de/siensi sintesis bdan akumulasi besi dalammitokondria sel prekursor eritroid

5ang disebut 3in3in sideroblast Sel terdiri dari S8M normal dan sel

hipokrom dan mikrositer


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;iridoksin C memperbaiki de/siensisintesis asam 5ang diperlukan untuksintesis hemoglobin

;iridoksin terdapat dalam makanan

8iabsorpsi dengan baik padapemberian peroral


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Eritropoietin

Beberapa ,aktor humoral dan selulerberperan dalam eritropoiesis- 5angpaling berperan adalah eritropoietin

Eritropoietin C merangsangproli,erasi- di,erensiasi- dan maturasistem sel men6adi sel hematopoietik

P+' erotropoietin disintesis dalamkortek gin6al dan sisan5a diekstrarenal terutama sel hati


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ipoksia C sekresi eritropoietin H

Anemia- hipobaria- iskemia C 1B? QC produksi eritropoietin H

8iberikan IV atau S2

T"$# R 6am Konsentrasi pun3ak di3apai dalam )

"# 6am setelah pemberian S2

8istribusi ke seluruh tubuh Metabolisme di hepar

Sites o, a3tion ,or E;O


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Sites o, a3tion ,or E;O

Bi l i l A ti , Oth


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Biologi3al A3tions o, Otherematopoieti3 @ro.th ?a3tors

"0 @ranulo35te$Ma3rophage 2olon5 Stimulating?a3tor @M)2S?) Sargramostim A3ts s5nergisti3all5 .ith I()% to stimulate the

,ormation and proli,eration o, 3olon5 ,orming 3ells:2?4)@EMM- B?4)E- 2?4)Meg- 2?4)@M- 2?4)M- 2?4)E

In3reases 35toto9i3 phago35ti3 a3ti7it5o, maturegranulo35tes

#0 Interleukin % I()% A3ts s5nergisti3all5 .ith @M)2S?to stimulate the

,ormation o, granulo35tes- ma3rophages- eosinophilsand megakar5o35tes0 A3ts s5nergisti3all5 .ith E;Oto stimulate ,ormation

o, B?4)E3olonies Indu3es 2?4)S and leukemi3 blast 3ells into 3ell 353le


38/49

More ematopoieti3 @ro.th?a3tors

%0 2olon5 stimulating ?a3tor)" 2S?)" or M)2S?

A3ts s5nergisti3all5 .ith @M)2S? and I()% to

stimulate mono35te$ma3rophage 3olon5,ormation and ,un3tion

*0 @ranulo35te 2olon5 Stimulating ?a3tor

@)2S? ) flgrastim A3ts s5nergisti3all5.ithI()%- @M)2S? and 2S?)"tostimulate ,ormation o, megakar5o35tes- granulo35te)ma3rophage and high proli,erati7e potential ;;3olonies

Indu3es release o, granulo35tes ,rom marro.


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More ematopoieti3 @ro.th?a3tors

D0 Thrombopoietin TS? In3reases the sie and number o, megakar5o35tes0

I()"" also use,ul in stimulating produ3tion

In3reases the 3on3entration o, earl5 megakar5o35tes3ellsSA2EF3ells in bone marro.0

;rodu3es an in3rease in megakar5o35tesendomitosis0

In3reases platelet sie and number in plasma0


40/49

idroksiurea

8igunakan untuk terapi anemia selsabit- dimana ter6adi peningkatansintesis ,etal b

Mekanisme ker6a belum 6elas- tetapimempengaruhi ribonukleotidadi,os,at reduktase C tahap

biosintesis 8NA C menghan3urkanpembentukan radikal bebas tirosildalam pusat katalitik enim


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Absorpsi peroral baik

Konsentrasi pun3ak di3apai dalam #6am

ESO: menekan hematopoietik-neutropenia


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8e,eroksamin

8e,eroksamin e,ekti, mengikat besiC digunakan untuk anemia dengankelebihan besi

A/nitas tinggi terhadap ion besi danmengikat besi dari hemosiderin dan,eritin- 6uga dari trans,erin

8e,eroksamin tidak mengikat besipada b


43/49

Absorpsi peroral buruk

T"$# "D menit

8iberikan melalui S2 pump

ESO: reaksi alergi- neurotoksik padapenggunaan 6angka pan6ang


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Imunosupresan

Siklosporin dan antitimosit globulindigunakan untuk anemia aplastik


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Antitimosit globulin

8iberikan se3ara IV setelahdilarutkan dalam salin normal dandiberikan melalui in,us pada kateter

intra7ena sentral ESO: ana/laksis- serum si3kness

k ki ik


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?armakokinetik

Drug

s

RO

A

Notes

Recombinant

humanerythrop

oietin

IV,SC

SCmaybe as

effective asIV,!"# $

hr

Iron Ora%,I&,I

Absorpsi p'oferrou

? k ki ik


47/49

?armakokinetik

Dru

gs

RO

A

Notes

Asamfo%at

Ora%,I&,

IV

Absorpsi p'ogoo(,

enterohepaticcyc%in

g

Vitamin*!#

Ora%,SC,I&

Ora%routeineffective in

? k ki ik


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?armakokinetik

Dru

gs

R

OA

Notes

-i(rosi

urea

Ora%

Absorpsi p'o

goo(

+re(nison

Ora%orIV

Absorpsi p'ogoo(

Si%

osp

Or

a%

Ora%

(ose is

? k ki tik


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?armakokinetik

Drugs RO

A

Notes

Deferosamin

SCorIV

Absorpsip'opoor,mustbegivenbycontin

Obat Antianemia

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