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Bi 6: THUC TC DNG TRN H ADRENERGIC
MC TIU HC TP: Sau khi hoc xong bi ny, sinh vien c kha nang:
1. Irinh by duoc chu trinh chuyen hoa cua catecholamin tai ngon day than kinh giao
cam
2. Phan biet duoc tac dung cua adrenalin, noradrenalin v DA
3. Phan biet duoc tac dung cua thuoc cung
1
v

: /soproterenol, dobutamin v
salbutamol
4. Phan tich duoc co che tac dung cua cac thuoc huy giao cam
5. Irinh by duoc tac dung v ap dung dieu tri cua thuoc huy giao cam
6. Phan biet duoc co che tac dung v ap dung dieu tri cua thuoc huy
1
He adrenergic l he hau hach giao cam, giai phng chat trung gian ha hoc goi chung l
catecholamin v deu mang nhan catechol (vng benzen c hai nhm -OH o vi tr ortho v mot goc
amin o chuoi ben. Cc catecholamin gom c adrenalin (duoc san xuat chu yeu o tuy thuon g than)
noradrenalin (o dau tan cng cc soi giao cam) v dopamin (o mot so vng tren than kinh trung
uong).
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Hnh 6.1. Sinh tong hop catecholamin
1. CHUYN HA CA CATECHOLAMIN
Catecholamin duoc sinh tong hop t tyrosin dui tc dung cua mot so enzym trong te bo ua
crom o tuy thuong than, cc noron hau hach giao cam v mot so noron cua than kinh trung uong
theo so do tren (hnh 6.2)
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Hnh 6.2. Chuyen van cua catecholamin tai tan cng day giao cam
Iyrosin duoc van chuyen vo dau tan cng day giao cam nh c hat van chuyen phu thuoc Aa
+
(A). Iyrosin duoc chuyen hoa thnh dopamin (DA) roi duoc chat van chuyen (B) dua vo cac tui
du tr (cac hat). Chat van chuyen ny cng van chuyen ca noradrenalin (AA) v vi amin khac.
Irong tui du tr, DA duoc chuyen hoa thn h AA. Dien the hoat dong lm mo kenh calci, Ca
2+
vo te bo, giai phong AA t tui du tr.
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Sau khi duoc tong hop, mot phan catecholamin s ket hop vi ATP hoac vi mot dang protein ha
tan l chromogranin de tro thnh dang khong c hoat tnh, khong bi cc e nzym ph huy, luu lai
trong cc 'kho du tr l nhng hat dac biet nam o bo tuong (khoang 60%), cn mot phan khc
(khoang 40%) van o dang tu do trong bo tuong, de di dong, nam o ngoi hat. Gia hai dang ny
luon c su thang bang dong, khi dang tu do giam di th lai duoc bo sung ngay t cc kho du tr.
Luong noradrenalin trong bo tuong dieu chinh hoat tnh cua tyrosin hydroxylase theo co che
dieu ha nguoc chieu: khi noradrenalin tang th hoat tnh cua enzym giam, v nguoc lai. Mat
khc, cc chat cung receptor
2
lm giam giai phng noradrenalin ra khe xinap v do d tr
luong cua noradrenalin trong bo tuong s tang len.
Theo gia thiet cua Burn v Rand (1959 - 1962) dui anh huong cua xung tc than kinh, ngon day
giao cam lc dau tiet ra acetylcholin, l m thay doi tnh tham cua mng te bo, do d Ca
++
t
ngoi te bo tham nhap duoc vo trong te bo, dng vai tr nhu mot enzym lm v lien ket ATP -
catecholamin, giai phng catecholamin ra dang tu do.
Sau khi duoc giai phng, mot phan noradrenalin s tc don g len cc receptor (sau v truc xinap),
mot phan chuyen vo mu tuan hon de tc dung o xa hon roi bi ging ha, cn phan ln (tren
80%) s duoc thu hoi lai, phan nho khc bi mat hoat tnh ngay trong bo tuong.
Hnh 6.3. So phan cua noradrenalin khi duoc giai phng
1. Iac dung tren receptor sau (1a) v truoc (1b) xinap
2. Ihu hoi
3. \o tuan hon v bi chuyen hoa boi COMI
4. Chuyen hoa trong bo tuong boi MAO
Catecholamin bi mat hoat tnh boi qu trnh oxy ha khu amin do hai enzym MAO (mono - amin
- oxydase) v COMT (catechol - oxy- transferase) de cuoi cng thnh acid 3 - methoxy- 4
hydroxy mandelic (hay vanyl mandelic acid - VMA) thai tr qua nuc tieu.
MAO c nhieu trong ti the (mitochondria), v vay n dng vai tr ging ha catecholamin o trong
te bo hon l o tuan hon. Phong toa MAO th lm tang
catecholamin trong mo nhung khong anh huong den tc dung cua catecholamin ngoai lai.
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COMT l enzym ging ha catecholamin o ngoi te bo, c o mng xinap v o nhieu noi nhung
dam do cao hon ca l o gan v than. Phong toa COMT th ko di duoc thi gian tc dung cua
catecholamin ngoai lai.
Receptor: Adrenalin v noradrenalin sau khi duoc giai phng ra s tc dung len cc receptor cua
he adrenergic. Ahlquist (1948) chia cc receptor d thnh hai loai v do chng c tc dung
khc nhau tren cc co quan (bang sau).
Ta thay rang tc dung cung c tnh chat kch thch, lm co that cc co tron, chi c co tron
thnh ruot l gin. Nguoc lai, tc dung cung c tnh chat c che, lm gin co, tr co tim lai
lm dap nhanh v dap manh.
Land, Arnold v Mc Aulijj (1966) cn chia cc receptor thnh hai nhm
1
(tc dung tren tim
v chuyen ha m) v nhm
2
(lm gin mach, gin kh dao v chuyen ha dung).
2
truc
xinap kch thch lm tang giai phng NA, c vai tr dieu ha nguoc vi
2
.
Theo de xuat cua Langer (1974), cc receptor duoc chia thnh hai loai: loai
1
l receptor sau
xinap, lm co mach tang huyet p, loai
2
l receptor truc xinap, c tc dung dieu ha, khi kch
thch s lm giam giai phng norad renalin ra khe xinap, dong thi lm giam tiet renin, gay ha
huyet p. Cc receptor
2
c nhieu o he giao cam trung uong. Hien cng thay c receptor
2
o
sau xinap cua mach mu v te bo co tron (lm co), mo m v cc te bo bieu mo xuat tiet (ruot,
than, tuyen noi tiet)
Dopamin chu yeu tc dung o than kinh trung uong, o than v cc tang, tren cc receptor dac hieu
doi vi n goi l cc receptor dopaminergic (receptor delta - )
Bang 6.1: Cc receptor adrenergic
Recepto
r
Chat chu
van
Chatdoi
khng
Mo p ng Co che phan tu

1
Adr NA
>>Iso
Phenylephrin
Prazosin - Co tron
thnh mach
- Co tron
sinh duc
tiet nieu
- Gan
- Co tron
ruot
- Tim
Co that
Co that
Huy glycogen
Tan tao dung
Uu cuc ha v
gin
Tang co bp, loan
nhip
Kch thch
phospholipase C
de tao IP
3
v
DAG: tang Ca
++
cytosol
- Hoat ha kenh
K
+
phu thuoc vo
Ca
++
- c che dng K
+

2
AdrNA >>
Iso
Clonidin
Yohimbi
n
- Te bo
cua tuy
- Tieu cau
- Tan cng
soi TK
- Co tron
thnh mach
Giam tiet insulin
Ngung ket
Giam tiet NA
Co
- c che
adenylcyclase
(Gi) - Hoat ha
kenh K
+
c che kenh Ca
++
-Tang luong Ca,
tang Ca
++
trong
cytosol

1
Iso>Adr =NA
Dobutamin
Metoprol
ol
- Tim Tang tan so, bien
do v toc do dan
Hoat ha
adenylcyclase v
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- Te bo
gan cau
than
truyen A-V
Tang tiet renin
kenh Ca

2
Iso>Adr >>
NA
Terbutalin
ICI
118551
- Co tron
(mach kh
quan,
ruot...)
- Co van
- Gan
- Gin
- Huy glycogen
gan K
+
- Huy glycogen
- Tan tao dung
Hoat ha
adenylcyclase

3
Iso=NA>Adr
BRL 37344
ICI
118551
CGP
20712A
Huy lipid Hoat ha
adenylcyclase
Iso
*
: Isoproterenol Adr: adrenalin NA: noradrenalin
Chi chu cua bang 3:
- Moi receptor deu kich thich adenylcyclase thong qua protein C
S
v lm tng AMPv, ngoi ra
cn lm kenh calci cam ung voi dien the cua co van v co tim.
- Receptor
2
, trai lai, uc che adenylcyclase thong qua protein C
i
, dong thi hoat hoa kenh kali,
uc che kenh calci.
- Receptor
1
kich thich lm tng calci noi bo thong qua 2 chat trung gian Diacylglycerol
(DAC) v /nositol triphosphat (/P
3
).
2. THUC CUONG H ADRENERGIC
L nhng thuoc c tc dung giong adrenalin v noradrenalin , kch thch hau hach giao cam nen
cn goi l thuoc cung giao cam. Theo co che tc dung c the chia cc thuoc ny lm hai loai:
- Loai tc dung truc tiep tren cc receptor adrenergic sau xinap nhu adrenalin, noradrenalin,
isoproterenol, phenylephrin
- Loai tc dung gin tiep do kch thch cc receptor truc xinap, lm giai phng catecholamin noi
sinh nhu tyramin (khong dng trong dieu tri), ephedrin, amphetamin v phenyl - ethyl- amin. Khi
dng reserpin lm can du tr catecholamin th tc dung cua cc thuoc d s giam di. Trong nhm
ny, mot so thuoc c tc dung kch thch than kinh trung uong theo co che chua hon ton biet r
(nhu ephedrin, amphetamin), reserpin khong anh huong den tc dung ny: hoa c c che mono-
amin- oxydase (MAOI), lm vng ben catecholamin.
2.1.Thuoc cung receptor alpha v beta
2.1.1.Adrenalin
oc, bang A
L hormon cua tuy thuong than, lay o dong vat hoac tong hop. Chat tu nhien l dong phan ta
tuyen c tc dung manh nhat.
2.1.1.1.Iac dung
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Adrenalin tc dung ca tren v receptor.
- Iren tim mach:
Adrenalin lm tim dap nhanh, manh (tc dung ) nen lm tang huyet p toi da, tang p luc dot
ngot o cung dong mach chu v xoang dong mach canh, t d pht sinh cc phan xa giam p qua
day than kinh Cyon v Hering lm cung trung tam day X, v vay lm tim dap cham dan v huyet
p giam. Tren dong vat th nghiem, neu cat day X hoac tiem atropin (hoac methylatropin) truc
de cat phan xa ny th adrenalin chi lm tim dap nhanh manh v hu yet p tang rat r.
Mat khc, adrenalin gay co mach o mot so vng (mach da, mach tang - receptor ) nhung lai gay
gin mach o mot so vng khc (mach co van, mach phoi - receptor ...) do d huyet p toi thieu
khong thay doi hoac c khi giam nhe, huyet p tru ng bnh khong tang hoac chi tang nhe trong
thi gian ngan. V l d adrenalin khong duoc dng lm thuoc tang huyet p.
Tc dung lm gin v tang luu luong mach vnh cua adrenalin cng khong duoc dng trong dieu
tri co that mach vnh v tc dung ny lai km theo lm tang cong nang v chuyen ha cua co tim.
Dui tc dung cua adrenalin, mach mu o mot so vng co lai s day mu ra nhng khu vuc t chiu
anh huong hon, gay gin mach thu dong o nhng noi d (nhu mach no, mach phoi) do d de gay
cc bien chng dt mach no, hoac ph phoi cap.
- Iren phe quan:
t tc dung tren ngui bnh thung. Tren ngui bi co that phe quan do hen th adrenalin lm gin
rat manh, km theo l co mach niem mac phe quan, lm giam ph cho nen anh huong rat tot ti
tnh trang benh. Song adrenalin bi mat tc dung rat nhanh vi nhng lan dng sau, v vay khong
nen dng de cat con hen.
- Iren chuyen hoa:
Adrenalin lm tang huy glycogen gan, lm tang glucose mu, lm tang acid bo tu do trong mu,
tang chuyen ha co ban, tang su dung oxy cu a mo.
Cc co che tc dung cua adrenalin hay catecholamin ni chung l lm tang tong hop adenosin 3' -
5'- monophosphat (AMP- vng) t ATP do hoat ha adenylcyclase (xem so do)
So do tc dong cua catecholamin len chuyen ha dung v mo
Catecholamin Cafein
Diazoxid
(-)
Adenylcyclase Phosphodiesterase
ATP 3', 5'- AMP AMP
(AMP vng)
Triglycerid Triglycerid
lipase
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Glycogen (-)
Glycogen
Phospho- Glucose- 1- phosphat synthetase Diglycerid Acid bo
rylase
Glucose- 6- phosphat Monoglycerid Acid bo
Glucose mu Nang luong
Acid lactic Glycerol Acid bo
2.1.1.2. p dung dieu tri:
- Chong chay mu ben ngoi (dap tai cho dung dich adrenalin hydroclorid 1% de lm co mach).
- Tang thi gian gay te cua thuoc te v adrenalin lm co mach tai cho nen lm cham hap thu thuoc
te.
- Khi tim bi ngng dot ngot, tiem adrenalin truc tiep vo tim hoac truyen mu c adrenalin vo
dong mach de hoi tinh.
- Soc ngat: dng adrenalin de tang huyet p tam thi bang cch tiem tinh mach theo phuong php
trng bom tiem.
Lieu trung bnh: tiem dui da 0,1- 0,5 mL dung dich 0,1% adrenalin hydroclorid.
Lieu toi da: moi lan 1 mL: 24 gi : 5 mL
ng 1 mL = 0,001g adrenalin hydroclorid
2.1.2. Noradrenalin (arterenol)
oc, bang A
L chat dan truyen than kinh cua cc soi hau hach giao cam. Tc dung man h tren cc receptor ,
rat yeu tren , cho nen:
- Rat t anh huong den nhip tim, v vay khong gay phan xa cung day phe vi.
- Lm co mach manh nen lm tang huyet p toi thieu v huyet p trung bnh (manh hon adrenalin
1,5 lan)
- Tc dung tren phe quan rat yeu, v co tron phe quan c nhieu receptor
2
.
- Tc dung tren dinh dung v chuyen ho deu km adrenalin. Tren nhieu co quan, tc dung cua
NA tren receptor km hon adrenalin mot cht. Nhung do ty le cung do tc dung gia v
khc nhau nen tc dung chung khc nhau r ret.
Tren than kinh trung uong, noradrenalin c nhieu o vng dui doi. Vai tr sinh l chua hon ton
biet r. Cc chat lm giam du tr catecholamin o no nhu reserpin, methyldopa deu
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gay tc dung an than. Tri lai, nhng thuoc c che MAO, lm tang catecholamin th deu c tc
dung kch than.
ieu ha than nhiet phu thuoc vo su can bang gia NA, serotonin v acetylcholin o phan truc
cua vng dui doi.
C the cn tham gia vo co che giam dau: thuoc lm giam luong catechola min tiem vo no that
c che duoc tc dung giam dau cua morphin.
Chi dinh: nang huyet p trong mot so tnh trang soc: soc nhiem doc, nhiem khuan, soc do di
ng...
Chi truyen nho giot tinh mach t 1 - 4 mg pha long trong 250- 500 mL dung dich glucose dang
truong. Khong duoc tiem bap hoac dui da v lm co mach ko di, de gay hoai tu tai noi tiem.
ng 1 mL = 0,001g
2.1.3. Dopamin
Dopamin l chat tien than cua noradrenalin v l chat trung gian ha hoc cua he dopaminergic.
C rat t o ngon day giao cam. Trong no, tap trung o cc nhan xm trung uong v b den van.
Tren he tim mach, tc dung phu thuoc vo lieu:
- Lieu thap 1- 2 g/ kg/ pht duoc goi l "lieu than", tc dung chu yeu tren receptor dopaminergic
D
1
, lm gin mach than, mach tang v mach vnh. Chi d inh tot trong soc do suy tim hoac do giam
the tch mu (can phuc hoi the tch mu km theo).
- Tai than, "lieu than" cua dopamin lm tang nuc tieu, tang thai Na
+
, K
+
, Cl
-
, Ca
++
, tang san xuat
prostaglandin E
2
nen lm gin mach than gip than chiu dung duo c thieu oxy.
- Lieu trung bnh > 2- 10 g/ kg/ pht, tc dung tren receptor
1
, lm tang bien do v tan so tim.
Sc can ngoai bien ni chung khong thay doi.
- Lieu cao tren 10g/ kg/ pht tc dung tren receptor
1
, gay co mach tang huyet p.
Trong lam sng, tuy thuoc vo tng loai soc m chon lieu.
Dopamin khong qua duoc hng ro mu no
Chi dinh: cc loai soc, km theo vo nieu
ng 200 mg trong 5 mL. Truyen cham tinh mach 2 - 5 g/ kg/ pht. Tang giam so giot theo hieu
qua mong muon.
Chong chi dinh: cc benh mach vnh
2.2. Thuoc cung receptor
2.2.1. Metaraminol (Aramin)
Tc dung uu tien tren receptor
1
. Lm co mach manh v lau hon adrenalin, c the cn do kch
thch giai phng noradrenalin, khong gay gin mach th pht. Lm tang luc co bp cua co tim, t
lm thay doi nhip tim. Khong kch thch than kinh trung uong, khong anh huong den chuyen ha.
V mat goc phenol tren vng benzen nen vng ben hon adrenalin.
Dng nang huyet p trong cc trung hop ha huyet p dot ngot (chan thuong, nhiem khuan, soc).
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Tiem tinh mach 0,5- 5,0 mg trong trung hop cap cu. Truyen cham tinh mach dung dich 10 mg
trong 1 mL. C the tiem dui da hoac tiem bap. ng 1 mL= 0,01g metaraminol bitartrat.
2.2.2. Phenylephrin (neosynephrin)
Tc dung uu tien tren receptor
1
. Tc dung co mach tang huyet p ko di, nhung khong manh
bang NA. Khong anh huong den nhip tim, khong kch thch than kinh trung uong, khong lm
tang glucose huyet.
Chi dinh: nhu noradrenalin
Tiem bap 5- 10 mg
Truyen cham vo tinh mach 10- 15 mg trong 1000 mL dung dich glucose dang truong
Cn dng de chong xung huyet v gin dong tu trong mot so che pham chuyen khoa.
2.2.3. Clonidin (Catapressan)
Clonidin (dicloro- 2, 6 phenyl- amino- imidazolin) c tc dung cung receptor
2
truc xinap o
trung uong v thuoc qua duoc hng ro mu- no. Tc dung cung
2
sau xinap ngoai bien chi
thong qua nen gay tang huyet p ngan. Sau d, do tc dung cung
2
trung uong chiem uu the,
clonidin lm giam giai phng NA t cc noron giao cam o hnh no, gay giam nhip tim, giam
truong luc giao cam, giam luu luong mu o no, tang, than v mach vnh, dua den ha huyet p.
Clonidin lm can bi tiet nuc bot, dich vi, mo hoi, lm giam hoat tnh cua renin huyet tuong,
giam loi nieu. ong thi c tc dung an than, giam dau v gay met moi. Mot so t c gia cho rang
clonidin gan vo receptor imidazolin o than kinh trung uong, l loai receptor mi dang duoc
nghien cu.
Tc dung khong mong muon: ngu g, kho mieng
Chi dinh: tang huyet p the va v nang (xin xem bi "Thuoc cha tang huyet p")
Chong chi dinh: trang thi tram cam.
Khong dng cng vi guanetidin hoac thuoc liet hach v c the gay con tang huyet p.
Lieu luong: vien 0,15 mg. Uong lieu tang dan ti 6 vien mot ngy, tc dung xuat hien cham.
Dng cng vi thuoc loi nieu, tc dung ha huyet p s t ang.
2.3. Thuoc cung receptor
C 4 tc dung duoc l chnh
- Tc dung gin phe quan, dng cha hen: loai cung
2
.
- Tc dung gin mach: loai cung
2
- Tc dung kch thch
1
lm tang tan so, tang luc co bp cua co tim, tang toc do dan truyen trong
co tim, tang tui mu cho co tim.
- Tren tu cung c chua, thuoc cung
2
lm giam co bp duoc dng chong doa xay thai.
2.3.1. Isoproterenol (Isoprenalin, Isuprel, Aleudrin, Novodrin, Isopropyl noradrenalin)
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Tc dung uu tien tren receptor (
1
v
2
). Lm tang nhip tim, tang sc co bp cua co tim v
cung luong tim, gay gin mach, ha huyet p, lm gin kh quan nhanh v manh (gap 10 lan
adrenalin), dong thi lm giam tiet dich niem mac nen cat con hen rat tot.
Dng trong cc trung hop nhip tim cham thung xuyen , nghn nhi that hon ton, loan nhip do
nhoi mu co tim: truyen tinh mach 0,5mg trong 250 - 500 ml dung dich glucose 5%. Tc dung
tang dung huyet km adrenalin v cn truc tiep kch thch te bo tuy tiet insulin.
Trong hen phe quan v trn kh phe mac man tnh, dat dui lui vien 10 mg, 2 - 3 lan/ ngy.
Khong uong v bi chuyen ha nhanh.
ng Novodrin 1 mL= 0,5 mg isoprenalin clohydrat
Vien 10- 20 mg isoprenalin sulfat
Phun dich 1 phan nghn
2.3.2. Dobutamin (Dobutrex)
Cong thc gan giong dopamin: tc dung u u tien tren
1
receptor. Tc dung phc tap do
dobutamin raxemic c 2 dong phan: dong phan ( -) dobutamin c tc dung cung
1
manh, gay
tang huyet p: trong khi dong phan (+) dobutamin lai c tc dung doi lap huy
1
. Ca hai dong
phan deu c tc dung cung , nhung dong phan (+) 10 lan manh hon dong phan ( -). Tc dung
cua dobutamin raxemic l tong hop cua ca hai dong phan.
Tren tim, do dobutamin lm tang co bp manh v t lm tang nhip , v vay khong lm tang nhu
cau su dung oxy cua co tim. Tc dung km isopr oterenol. t tc dung tren mach nhung lm gin
mach vnh. Tc dung loi nieu chu yeu l do tang luu luong tim.
Chi dinh: suy tim cap sau mo tim, nhoi mu co tim
V thi gian bn thai chi khoang 2 pht nen chi dng bang dung truyen cham tinh mach.
Che pham: Dobutamin hydroclorid (Dobutrex) lo 20 mL cha 250 mg dobutamin. Khi dng, ha
long trong 50 mL dung dich dextrose 5%, truyen tinh mach vi lieu 2,5 - 10 g/ kg/ pht. Neu
nhip tim tang nhanh, giam toc do truyen.
2.3.3. Thuoc cung uu tien (chon loc) rece ptor
2
L thuoc thung duoc dng de dieu tri cat con hen. Tuy nhien, lieu cao cng van kch thch ca
1
,
lm tang nhip tim. V vay hung nghien cu ti van l tm cch thay doi cau trc de c cc thuoc
tc dung ngy cng chon loc tren
1
hon v c sinh kha dung cao hon. ong thi dng thuoc dui
dang kh dung de trnh hap thu nhieu thuoc vo dung ton than, de gay tc dung phu (tim dap
nhanh, run tay)
Cc thuoc cung
2
dng dui dang kh dung, ngoi tc dung lm gin phe quan cn c the c
che giai phng leucotrien v histamin khoi dung bo o phoi (xem them bi "Thuoc dieu chinh
roi loan ho hap")
Chong chi dinh: benh mach vnh, loan nhip tim, cao huyet p nang, di tho dung, cung gip.
Dng ko di lien tuc, tc dung c the giam dan do so luong recept or
2
o mng te bo sau xinap
giam ("down regulation")
2.3.3.1. Ierbutalin
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Do c vng resorcinol trong cau trc nen khong bi COMT metyl ha. Sau kh dung, tc dung ko
di duoc 3- 6 gi.
2.3.3.2. Albuterol (Salbutamol - \entolin)
Tnh chat duoc l v chi di nh dieu tri nhu terbutalin. Dng dung uong hoac kh dung. Sau kh
dung, tc dung toi da vo pht th 15 v duy tr duoc 3 - 4 gi.
- Vien giai phng cham (Volmax): 4- 8 mg 2 lan/ ngy
- Kh dung dinh lieu (Ventolin): 100 g/ nht bp 2 nht/ lan 3- 4lan/ ngy cch nhau 4
tieng.
2.3.2.3. Ritodrin
Dng lm gin tu cung, chong de non (xem bi " Thuoc tc dung tren tu cung"). Hap thu nhanh
qua dung uong nhung sinh kha dung chi duoc 30%. Thai tr qua nuc tieu 90% dui dang lien
hop. Tiem tinh mach, 50% thai tr dui dang nguyen chat.
2.4. Thuoc cung giao cam gin tiep
2.4.1. Ephedrin (ephedrinum)
oc, bang B
Ephedrin l alcaloid cua cay ma hong (Ephedra equisetina v Ephedra vulgaris). Hien nay d
tong hop duoc. Trong y hoc, dng loai ta tuyen v raxemic.
L thuoc va c tc dung gin tiep lm giai phng catecholamin ra khoi noi du tr, va c tc
dung truc tiep tren receptor.
Tren tim mach, so vi noradrenalin, tc dung cham v yeu hon 100 lan, nhung ko di hon ti 10
lan. Lm tang huyet p do co mach v kch th ch truc tiep tren tim. Dng nhieu lan lien nhau, tc
dung tang p s giam dan (hien tuong quen thuoc nhanh: tAChyphylaxis)
Thung dng chong ha huyet p v de kch thch ho hap trong khi gay te tuy song, trong nhiem
doc ruou, morphin, barbiturat.
Kch thch trung tam ho hap o hnh no v lm gin phe quan nen dng de cat con hen, tc dung
tot tren tre em.
Tren than kinh trung uong, vi lieu cao, kch thch lm mat ngu, bon chon, run, tang ho hap.
Ephedrin de dng hap thu theo moi dung. Vng ben vi MAO. C huyen ha o gan, khoang 40%
thai tr nguyen chat qua nuc tieu.
Dng dui the muoi clohydrat hoac sulfat de ha tan.
Uong 10- 60 mg / ngy. Lieu toi da 24h l 150 mg
Tiem dui da, bap thit hoac tinh mach 10 - 20 mg/ ngy
Nho niem mac (mat, mi) dung dich 0, 5- 3%
ng 1 mL= 0,01g ephedrin clohydrat
Vien 0,01g ephedrin clohydrat
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Pseudoephedrin l dong phan lap the cua ephedrin, t gay tim nhanh, tang huyet p v kch thch
than kinh trung uong hon ephedrin. Thung duoc dng trong cc che pham nho mi chong xun g
huyet niem mac.
2.4.2. Amphetamin
L thuoc tong hop phenylisopropanolamin. Tc dung duoc l theo kieu ephedrin, gin tiep lm
giai phng noradrenalin (v c the cn ca dopamin v serotonin) ra khoi noi du tr. Khc
ephedrin l tham vo than kinh trung uong nhan h, tc dung kch thch manh tam trang v su
nhanh nhen do tc dong len vo no v he lien vng hoat ha (v vay, duoc xep vo loai doping,
cam dng trong thi dau the thao). Cn c tc dung gay chn an, dng de chong bo ph.
Mot so dan xuat cua amphetamin ( methamphetamin, dimethoxyamphetamin...) kch thch than
trung uong rat manh, gay loan than, deu xep vo chat ma tu.
2.4.3. Phenylpropanolamin
t tc dung trung uong hon. ngoai bien, tc dung co mach thung duoc dng de chong ngat
mi, l thuoc phoi hop trong vien thuoc chong cam cm (Atussin, Decolgen). Tuy nhien, gan day
thay nhieu tc dung phu tren tim mach nen c xu hung khong dng na.
3. THUC HU H ADRENERGIC
L nhng thuoc lm mat tc dung cua adrenalin v noradrenalin. Cc thuoc ny thung duoc
dng dieu tri chng tang huyet p, benh Raynaud, loan nhip tim, hoi chng cung tuyen gip
(tim nhip nhanh, loi mat, gin dong tu, tang ho hap: chnh l nhng dau hieu cung giao cam).
Cc thuoc duoc chia thnh hai nhm:
- Ihuoc huy giao cam (sympatholytic): l nhng thuoc phong toa noron adrenergic truc xinap,
lm giam giai phng catecholamin, khong c tc dung tren receptor sau xinap, khi cat cc day
hau hach giao cam th thuoc mat tc dung. Do thieu chat dan truyen than kinh noi sinh, tnh cam
thu cua cc receptor sau xinap vi catecholamin ngoai lai s tang len.
- Ihuoc huy adrenalin (adrenolytic) l nhng thuoc phong toa ngay chnh cc receptor adrenergic
sau xinap, cho nen khi cat dt cc soi hau hach giao cam, tc dung cua thuoc khong thay doi.
Catecholamin ca noi sinh ngoai lai deu bi mat tc dung.
1.1. Thuoc huy giao cam
Cc thuoc c the c tc dung o nhng khau sau:
1.1.1. c che tong hop catecholamin
Thuoc hay duoc dng l methyl dopa (Aldomet) phong toa dopa decarboxylase, lm dopa
khong chuyen thnh dopamin v 5 - hydroxytryptophan khong chuyen thnh 5 -
hydroxytryptamin (5 HT- serotonin). Do d so luong catecholamin v serotonin o ca ngoai bien
v than kinh trung uong deu giam. Mat khc cn ngan can kha nang gan catecholamin vo cc
hat luu tr.
Ngoi ra, trong co the methyldopa cn c the chuyen thnh methyl noradrenalin, tc dung
nhu mot chat trung gian ha hoc gia chiem cho cua noradrenalin (xem bi "Thuoc cha tang
huyet p")
Tc dung phu: mo mng, c che tam than, chng mat, nhc dau, kho mieng, ph.
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Khong dng khi c roi loan tuan hon no v mach vnh, cc trang thi tram cam, roi loan gan,
than.
Lieu luong: uong vien 250 mg. C the dng ti 8 vien/ ngy.
Che pham: Dopegyt vien 0,25 g methyl dopa.
Carbidopa v bemerazid, c che dopa decarboxylase o ngo ai bien. uoc dng phoi hop vi l -
dopa de dieu tri benh Parkinson.
1.1.2. Lm giam du tru catecholamin trong cc hat
* Reserpin:
Lm giai phng t t catecholamin t cc hat luu tr ra ngoi bo tuong de MAO ph huy, do d
luong catecholamin giam o ca tren than kinh trung uong (gay an than), ca o ngoai bien (lm ha
huyet p). Reserpin cn can tro qu trnh gan catecholamin (ca noi sinh lan ngoai sinh) vo cc
hat luu tr.
* Cuanetidin (Ismelin)
Chiem cho noradrenalin trong cc hat luu tr v tro thnh chat trung gian ha hoc gia. Khc
reserpin l lc dau guanetidin gay tang nhe huyet p do lm giai phng nhanh noradrenalin ra
dang tu do, mat khc guanetidin khong tham duoc vo than kinh trung uong nen khong c tc
dung an than.
Tc dung toi da xuat hien sau 2- 3 ngy v mat di 6- 10 ngy sau khi ngng thuoc.
Khong dng cho ngui benh c lot da dy, suy mach vnh, suy than. Khong dng cng vi
clonidin.
Lieu luong: lc dau uong 10 mg/ ngy, sau d tang dan ti 50 - 75mg/ ngy
Che pham: vien 10 v 20 mg
1.1.3. Ngan can giai phng catecholamin
Bretylium (Darentin)
Co che chua that r. c che giai phng catecholamin, nhung khong anh huong den tc dung cua
adrenalin v noradrenalin ngoai lai. C the l bretylium d lm cho mng cc hat luu tr giam
tnh tham vi ion Ca
++
m lm cho catecholamin khong duoc giai phng ra.
C tc dung gay te tai cho.
V c nhieu tc dung phu (nhu xung huyet niem mac mi, kh tho, ia long, ha huyet p, nhuoc
co) cho nen cn t duoc su dung o lam sng.
1.1.4. Thay the catecholamin bang cc chat trung gian ho hoc gia
Mot so chat khong c tc dung duoc l, nhung chiem cho cua catecholamin v cng duoc giai
phng ra dui xc tc kch thch day giao cam nhu mot chat trung gian ha hoc, duoc goi l chat
trung gian ha hoc gia:
- methyldopa tao thnh methyl noradrenalin
- Thuoc c che MAO: tyramin chuyen thnh octopamin
- Guanetidin
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1.2. Thuoc huy adrenalin
Cc thuoc phong toa tc dung tren receptor tuong doi dac hieu hon thuoc kch thch, nghia l
nhieu thuoc kch thch c tc dung ca tren hai loai receptor v , cn thuoc phong toa thung
chi tc dung tren mot loai receptor m thoi. Do d thuoc loai ny duoc chia thnh hai nhm:
thuoc huy v thuoc huy adrenergic.
1.2.1. Thuoc huy - adrenergic
V phong toa cc receptor nen lm giam tc dung tang huyet p cua nor adrenalin, lm dao
nguoc tc dung tang p cua adrenalin. Khong c che tc dung gin mach v tang nhip tim cua cc
thuoc cung giao cam v deu l tc dung tren cc receptor . Hien tuong dao nguoc tc dung tang
p cua adrenalin duoc giai thch l cc mao ma ch c ca hai loai receptor v , adrenalin tc
dung tren ca hai loai receptor d, nhung bnh thung, tc dung chiem uu the nen adrenalin lm
tang huyet p. Khi dng thuoc phong toa , adrenalin chi cn gay duoc tc dung kch thch tren
cc receptor nen lm gin mach, ha huyet p.
Nhm thuoc ny duoc chi dinh trong cc con tang huyet p, chan don u tuy thuong than, dieu tri
benh Raynaud. Hien dang nghien cu thuoc huy
1A
de dieu tri ph dai lnh tnh tuyen tien liet.
Nhuoc diem chung l de gay ha huy et p khi dng, nhip tim nhanh, xung huyet niem mac mi,
co dong tu, buon non, non v tieu chay do tang nhu dong da dy - ruot.
Cc thuoc chi khc nhau ve cung do tieu chay v thi gian tc dung.
1.2.1.1. Ahom haloalkylamin:
C phenoxybenzamin (dibenzylin) v diben amin.
Ve ha hoc, c cong thc gan giong nhu m tac nito (nitrogen mustard). Khi vo co the, amin
bac 3 duoc chuyen thnh etylen amoni, chat ny gan chat vo cc receptor theo lien ket cong
ha tri (chu yeu l receptor
1
), gay c che rat manh v ko d i (ti 24 gi cho mot lan dng
thuoc) theo kieu c che mot chieu.
Lieu luong: phenoxybenzamin, vien nang 10 mg, uong 2 - 10 vien/ ngy
1.2.1.2. Dan xuat imida:olin
C tolazolin (Priscol, Divascon) v phentolamin (Regitin)
c che tranh chap vi noradrenalin o recepto r
1
v
2
nen tc dung yeu v ngan hon
phenoxybenzamin nhieu.
Lieu luong: Priscol uong hoac tiem bap 25 - 50 mg/ ngy. Regitin uong 20- 40 mg/ ngy
Cn dng de chan don u tuy thuong than: nghiem php duoc coi l duong tnh neu ngui benh
nghi ngoi, hon ton yen tinh, tiem bap hoac tiem tinh mach 5 mg phentolamin, sau vi pht lm
huyet p toi da v toi thieu ha khoang 4 - 5 cmHg, duy tr duoc 7 pht roi tro lai huyet p ban dau
trong 10- 15 pht.
3.2.1.3. Pra:osin (Minipress): chat dien hinh phong toa
1
. Dng dieu tri tang huyet p, uong 1 -
20 mg mot ngy. (xin xem bi "Thuoc cha tang huyet p")
3.2.1.4. Alcaloid nhan indol:
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Cc alcaloid cua nam cua g (ergot de seigle: Secale cornutum: Claviceps purpurea), duoc chia
thnh hai nhm: loai huy giao cam v lm co bp tu cung (gom ergotamin, ergotoxin) v loai lm
co bp tu cung don thuan (ergometrin).
Vi lieu thap, ergotamin c tc dung cung giao cam nhe v ngan can thu hoi noradrenalin o
ngon day giao cam. Lieu cao, tri lai c tc dung phong toa recepto r . Ngoi ra cn c tc dung
truc tiep lm co co tron, nen c the lm co mach tang huyet p, hoac hoai tu dau chi v vch mi
trong trung hop nhiem doc man tnh do an la mach am moc, lm co that ruot, phe quan v tu
cung.
Chi dinh: cat con migren, roi l oan thi ky mn kinh, chay mu tu cung sau so rau
Dan xuat hydro ha cua cc ergot (nhu dihydroergotamin, hydroergotoxin) c tc dung phong toa
tang len trong khi tc dung co co tron giam xuong. Ngoi tc dung phong toa receptor , tc
dung ha huyet p cua ergotamin cn duoc giai thch l lm giam truong luc trung tam van mach
v kch thch trung tam ph giao cam. Do d duoc dng lm thuoc gin mach, ha huyet p: uong
4- 6 mg/ ngy, hoac tiem dui da 0,1- 0,5 mg/ ngy.
Chong chi dinh: c thai, roi loan ma ch vnh
- Yohimbin: l alcaloid cua Corynantheyo himbe c nhieu o Chau Phi. Cau trc ha hoc gan
giong reserpin, tranh chap vi NA tai receptor
2
. De vo than kinh trung uong. Tc dung yeu v
ngan, nen t duoc dng trong dieu tri.
Trong lam sng cn dng lm thuoc cung duong, v ngoi tc dung gin mach cn kch thch
phan xa tuy.
Lieu luong: Yohimbin clorhydrat 5 - 15 mg/ ngy
1.2.2. Thuoc huy adrenergic
Cn goi l thuoc "phong toa " (" blocking agent") c tc dung c che tranh chap vi
isoproterenol o cc receptor. Chat dau tien duoc tm ra l dicloisoproterenol (Powell v Slater,
1958). uoc dng nhieu trong lam sng.
1.2.2.1. Iac dung duoc ly: co 4 tac dung duoc ly chinh voi muc do khac nhau gia cac thuoc:
* Kha nang huy giao cam : l tnh chat chung duy nhat cua tat ca cc thuoc huy :
- Tren tim: lm giam nhip tim (20- 30%), giam luc co bp cua co tim, giam luu luong tim, giam
cong nang v giam su dung oxy cua co tim, giam toc do dan truyen cua to chc nt. Chu yeu l
do huy
1
.
- Tren kh quan: lm co, de gay hen. Chu yeu l do huy
2
, gay tc dung khong mong muon.
- Tren than: lm giam tiet renin, ha huyet p tren ngui c HA cao
- Tren chuyen ha: c che huy glycogen v huy lipid
+Tc dung lm on dinh mng: giong quinidin, lm giam tnh tham cua mng te bo v i su trao
doi ion nen c tc dung chong loan nhip tim.
+ C hoat tnh noi tai kch thch receptor : mot so thuoc phong toa khi gan vo cc receptor d
lai c tc dung kch thch mot phan. Hieu qua thuc te t quan trong, nhung c the han che tc
dung lm giam nhip tim, giam co bp co tim, giam co kh quan cua chnh n.
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+ Tnh chon loc: nhieu thuoc phong toa doi lap vi tat ca cc tc dung cung giao cam cua
(
1
: tim v
2
: mach, kh quan). Nhung mot so thuoc lai chi phong toa duoc mot trong hai loai
receptor (
1
hoac
2
), v the phan biet thnh cc loai phong toa chon loc tren giao cam :
- Loai tc dung chon loc tren
1
hay loai chon loc tren tim ("cardioselectifs"), nhu practolol,
acebutalol, atenolol. Thung dng metoprolol (Lopressor) v atenolol (T enormin)
Loi ch cua loai thuoc ny l:
- Do rat km tc dung tren
2
cua kh quan nen han che duoc tai bien co that kh quan.
- Km tc dung tren
2
cua thnh mach s c loi cho dieu tri cao huyet p (giam co mach ngoai
bien)
- Do rat km tc dung tren
2
cua thnh mach vnh nen khong boc lo tc dung cung -
adrenergic (tc dung co mach vnh cua CA tuan hon trong mu). Bnh thung, do c tc dung
th tc dung cua bi lu m. Khi bi phong toa th tc dung cua s duoc boc lo ra.
- Do khong anh huong den cc receptor trong huy glycogen nen khong lm nang them tnh trang
ha dung huyet.
- Loai c tc dung chon loc tren
2
, dng dau l Butoxamin, t c nghia trong lam sng.
1.2.2.2. Chi dinh chinh
- Con dau that nguc, chu yeu do lm giam su dung oxy cua co tim . Trong nhoi mu co tim, tiem
tinh mach ngay t gi dau s lm giam lan rong o nhoi mu v cai thien duoc tien luong benh.
- Loan nhip tim: nhip nhanh xoang, nhip nhanh tren that, tim cung gip, cuong dong nhi do
nhiem doc digital.
- Tang huyet p: do lm giam luu luong tim, giam sc can ngoai bien, giam tiet renin v giam
giai phng noradrenalin (xin xem them bi "Thuoc cha tang huyet p")
- Mot so chi dinh khc: cung gip, migren, glocom gc mo (do lm giam san xuat thuy dich),
run tay khong r nguyen nhan.
1.2.2.3. Chong chi dinh:
- Suy tim l chong chi dinh chnh v n c che co che b tr cua tim.
- Bloc nhi- that v thuoc c tc dung lm giam dan truyen noi tai trong co tim.
- Hen phe quan. Loai c tc dung chon loc tren receptor
1
dng cho ngui hen t nguy hiem hon,
nhung vi lieu cao, trong dieu tri tang huyet p th cng bi mat tnh chon loc.
- Khong dng cng vi insulin v cc sulfamid ha dung huyet v c the gay ha dung huyet dot
ngot.
- C thai: khong chong chi dinh tuyet doi, nhung d gap tre mi de bi cham nhip tim, ha dung
huyet, suy ho hap, thai cham pht trien.
1.2.2.4. Cac tac dung khong mong muon
uoc chia lm hai loai:
* Loai tai bien l hau qua cua su phong toa receptor
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- Tim: suy tim do lm yeu co bp cua co tim, cham nhip tim, nhi that phan ly .
- Mach: hoi chng Raynaud, tm lanh dau chi, di khap khieng, (thung gap vi propranolol, do
bi phong toa th s cung). Cc thuoc chon loc tren
1
v c hoat tnh kch thch noi tai th t tai
bien ny hon
- Phoi: cc thuoc c tc dung huy
2
>
1
s gay co kh quan, kh tho. Khong dng cho ngui
hen.
- Than kinh trung uong: met moi, mat ngu, hay ngu me, ao anh, tram cam, thung gap hon vi
cc thuoc de tan trong m v de tham vo te bo than kinh (propranolol, metoprolol), loai t tan
trong m (atenolol, nadolol) t tai bien hon.
- Chuyen ho: lm ha dung huyet (can than trong vi ngui bi di tho dung), tang triglycerid
trong mu.
* Loai tai bien khong lien quan den tc dung phong toa
- Hoi chng mat- da- tai: xuat hien rieng hoac phoi hop vi cc ton thuong cua mat (viem gic
mac, viem cung mac), da (san nga lng bn tay, bn chan, day da), tai (diec v viem tai nang).
gap vi practolol, dieu tri trong 1 - 2 nam
- Viem phc mac xo cng: dau cng bung phc mac c nhng mng dy do to chc xo . Sau khi
ngng thuoc hoac dieu tri bang corticoid s khoi. Gap sau khi dieu tri ko di tren 30 thng.
- Tren thuc nghiem, d gap ung thu tuyen c, ung thu v, lymphosarcom. Do d can theo di tren
ngui khi dng lieu cao ko di.
1.2.2.5. Iuong tac thuoc
- Cc thuoc gay cam ng cc enzym chuyen ha o gan nhu phenytoin, rifampin, phenobarbital,
ht thuoc l, s lm tang chuyen ha, giam tc dung cua thuoc huy .
- Cc muoi nhom, cholestyramin lm giam hap thu
- Cc thuoc huy c tc dung hiep dong vi thuoc chen kenh calci, cc thuoc ha huyet p
- Indomethacin v cc thuoc chong viem phi steroid lm giam tc dung ha huyet p cua cc thuoc
huy .
1.2.2.6. Phan loai
Khong c tc dung "chon loc
tren tim"
C tc dung "chon loc tren tim"
n dinh mng
Khong on
dinh mng
n dinh mng
Khong on dinh
mng
Khong cung
noi tai
Propranolol Sotalol
Timolol
Esmolol
Atenolol
Co cung noi
tai
Alprenolol
Oxprenolol
Pindolol Acebutolol
Metoprolol
Practolol
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Su phan loai ny gip cho chon thuoc trong dieu tri. Th du benh nhan c r oi loan co that phe
quan th nen dng loai c tc dung "chon loc tren tim": benh nhan c nhip tim cham th dng loai
"c cung noi tai "
1.2.2.7. Mot so thuoc chinh
* Propranolol (Inderal, Avlocardyl)
L isopropyl aminonaphtyl oxypropranolol. C tc dung phong t oa nhu nhau tren ca
1
v
2
,
khong c hoat tnh noi tai kch thch.
Iac dung:
- Tren tim:lm giam tan so, giam luc co bp, giam luu luong tim ti 30%. c che tim l do tc
dung rieng cua propranolol ngan can calci nhap vo te bo co tim, giam nong do cal ci trong ti
lui noi bo.
- Tren mach vnh: lm giam luu luong 10 - 30% do c che gin mach. Lm giam tieu thu oxy cua
co tim.
- Tren huyet p: lm ha huyet p r sau 48 gi dng thuoc. Huyet p toi thieu giam nhieu.
- Ngoi ra cn c tc dung chong loan n hip tim, gay te (do tc dung on dinh mng) v an than
Chi dinh:
- Tang huyet p, loan nhip tim, nhip nhanh xoang, cuong dong nhi, nhip nhanh tren that, benh
cung gip, suy mach vnh. Uong lieu hng ngy 120- 160 mg
Vien 40 v 160 mg
- Dng trong cap cu loan nhip tim do nhiem doc digital hay do thong tim, do dat ong noi kh
quan.
Tiem tinh mach 5- 10 mg. ng 5 mg
Chong chi dinh: ngoi chong chi dinh chung, propranolol khong duoc dng cho ngui c thai
hoac lot da dy dang tien trien.
Thuoc duoc de dng hap thu qua dung tieu ha do tan nhieu trong m. Gan vo protein huyet
tuong ti 90- 95%, dam do toi da trong mu dat duoc sau khi uong t 1 - 2 gi. Chuyen ha thnh
hydroxy- 4- propranolol v acid naphtoxyl acetic rat nhanh tai gan nen chi khoang 25% lieu uong
vo duoc vng tuan hon, t/2: 3- 5 gi.
Vien 40 mg. Uong trung bnh 2- 4 vien / ngy, chia lm nhieu lan
ng 1 mL= 1 mg. Dng cap cu, tiem tinh mach rat cham, t 1 - 5 mg/ ngy
* Pindolol (Visken):
C tc dung cung noi tai v khong anh huong den van chuyen cua ion Ca
++
nen lm tang luc
co bp v tan so cua tim. Thung dng trong cc trung hop c loan nhip cham vi lieu uong 5 -
30 mg/ ngy. Tan va trong m, sinh kha dung 75% v t/2 = 3 - 4 gi.
* Oxprenolol (Trasicor):
DUOC L HOC 2007 - AI HOC Y HA NOI
(SCH DNG CHO SINH VIN H BC SI A KHOA)
Dng dieu tri cao huyet p, con dau that nguc, loan nhip tim. Uong 160 - 240 mg/ ngy.
* Atenolol (Tenormin): Tc dung chon loc tren
1
- rat tan trong nuc nen t tham vo than kinh
trung uong, sinh kha dung 50%, t/2 = 5 - 8 gi. Uong 50- 100 mg/ ngy.
* Metoprolol (Lopressor). C tc dung chon loc tren tim (
1
) nen d gay con hen phe quan (
2
).
Uong 50- 150 mg/ ngy. Hap thu nhanh qua dung uong, sinh kha dung 40% v t/2 = 3 - 4 gi.
CU HI T LUNG GI
1. Irinh by sinh chuyen hoa cua catecholamin tai ngon day giao cam.
2. Irinh by su phan loai cac receptor cua he giao cam: vi tri, dap ung v chat chu van.
3. Phan tich, so sanh tac dung v ap dung dieu tri cua adrenalin, noradrenalin v
dopamin.
4. Phan biet tac dung cua thuoc cung
1
v
2
giao cam.
5. Irinh by co che tac dung, tac dung v ap dung lam sng cua isoproterenol,
dobutamin v albuterol (Salbutamol, \entolin).
6. Phan tich co che cua cac thuoc huy giao cam.
7. Irinh by dc diem tac dung v ap dung dieu tri cua thuoc huy giao cam, neu 2
thuoc thi du.
8. Irinh by tac dung duoc ly v ap dung lam sng cua thuoc huy .
Irinh by cac tac dung khong mong muon cua thuoc huy .