Gthiu

1) Dc lc hc:
- Tng ca thuc ln c th
- C ch tc ng
- T/d ph - tng bt li
- Li ch lm sng - ng dng lm sng
2) Dc ng hc
- Tc ng ca c th /v thuc
- Hp thu, phn b, chuyn ha, thi tr
3) Thuc: l cht ngoi sinh, ko fi l t/n, tg n c/n ca CT qua nh` c ch # nhau
- Tng tc VL
- Thay i hot tnh enzyme
- Gn trn pt ch (90%)
- c ch chc nng t bo
S PHN CA THUC TRONG C TH
DC NG HC (ADME): Hthu, pb, ch ha, thi tr
1) Hp thu:
a) S hp thu thuc:
- Mng TB: lp PL kp, dch lng, linh g, thm nc, pt nh
MTB mi ni u ging nhau tr Mng no & Nhau thai
- Hthu: thuc t d dy vo mu
- V/c th ng:
Ph thuc t/c mng & thuc, khuynh hng n, ko cn NL
(1)Khuch tn trog mt nc: pt nh
M k, bo tng, ni m
Khuch tn trog l
Mao mch no, tinh hon: ko c dng l
Tun theo lut Fick.
(2)Khuch tn qua lp lipid:
Tnh tan trong lipid
Mc ion ha (acid yu, base yu)
H s fn chia lipid nc
pH mtrng
tun theo nh lut Henderson Hasselbalch:
Log dng proton ha/ dng ko proton ha = pKa pH
Thuc dng ko phn ly a s hthu tt hn (acid yu, base yu ty thuc mt)
Thuc ion qu ko hthu c
Thuc dng ion ha hn ch s hthu ca thuc
S thm qua mng f thuc vo t l ion ha, cng cao cng kh hthu.
(3)Khuch tn qua khong gia cc TB
M di da, c
Cu trc t cht
Cho php thm vo mch mu
Mmch/ TKTW, m biu m: lkt TB rt cht gy hn ch s v/c gia cc TB

- V/c ch ng:
Cn cht v/c, cc bm, cn NL, ngc khuynh hg n, bo ha & cnh tranh
o Transporter: ch 1 ion/pt theo 1 hng
o Symporter: nh` ion/pt theo 1 hng
o Antiporter: trao i cc ion hoc pt
o Pump: cn NL, ch yu v/c tri cc ion
Bm Na+: ngoi > trong;
Bm K+: ngoi < trong
Na+ cn cht v/c, cn ATP a Na+ ra, mag K+ ngoi vo ngc gradient n
- Cc loi v/c khc:
Nhp bo (endocytosis): vit.B12
Thc bo (phagocytosis): thuc dng rn ( thuc khg ung th)
m bo (pinocytosis): vit. A,D (dng lng)
Xut bo (exocytosis): acetylcholine
b) Cc yu t nh hng n s hthu thuc
- Tnh htan: dd nc > du, dch trep, rn
- N: dng ktn qua lipid : n cao tng hthu
- pH: nh hg n mc ion ha. pH ti t l dg ko ply & ko ply ti
hthu
- Tun hon: hthng mao mch(nh` hthu tt), co(hthu km) gin mch, lu
lng mu( m gan nhiu hn m m txc thuc nh` hn)
- B mt: Shthu tng hthu tng
c) Cc ng hthu thuc
(1)Hthu gin tip:
- Qua da :
Yu t nh hng: tnh tan trog lipid, Stx, hydrat ha lp sng, loi t dc
(gip thuc ktn tt trog TB, nh hng rt nh` n s hthu), dy lp
sng, ch xt, xoa bp da, tui tc
u im: SD c tgian di ngy, gfng t t thuc, n thuc n nh, tin li
Nhc: Kh hthu, d ng ti ch, td b bi f thuc nh` yu t: la tui (da
mi ng dy mg khc nhau, tr em d b hthu vo mu), vtr sd (da trn cth
c ~ ch mng nh bn, khe, k), m.
- Qua nim mc ming:
Nim mc li, sn ming, mt trog 2 m
Khng b chuyn ha ln u gan, tgian khi ft nhanh
Thuc dg di li fi: d tan, mi d chu, d thm qua MTB, hm lng
nh v n.mc di li mng d hthu nhg dch rt t, ko tiu ha dc nh`
Li thm vo mmu vo TM cnh tim : nhanh (liu dng < liu ug)
- Qua nim mc d dy
Hn ch: lp c dy, mao mch t ptrin, pH khc nghit, Shthu nh
Acid yu d hthu (do kt hp vs proton H+ trog d dy dg ko ply)
Kim yu km hthu.
D dy gip ptn thuc 1 fn, nghin to thnh hn dch. pH << f hy thuc
- Qua nim mc rut non:
Hthng mao mch ptrin

Shthu rng (khong 200m2)

Tgian lu lu (2-12 ting)
Nhu mao
Hthng nim mc ptrin
pH t hi acid n hi kim (thuc c th c tnh acid, base nn thuc no
cg hthu tt c)
Nhc im: chuyn ha ln u gan.
Qua nim mc trc trng
Trnh 1 phn chuyn ha ln u gan
Trnh tng ca dch tiu ha
Liu dng nh hn liu ung
Tin li: thuc c mi v kh chu, khi nn ma, hn m
Tc dng ti ch: tr, vim trc trg
Nhc im: tnh n nh km (tdg f thuc vtr t thuc), gy kch ng
ti ch
Nm nghing bn tri nhu ng ko y thuc ra
Qua ng h hp
Dng hi, d bay hi, kh dung
Shthu ca fi ln (khag 140m2)
Liu dng gn = liu tim di da.
Phi: kh sd v ph nag c knh rt nh rt kh v/c, hthu ko ti c m
ch, fi d b kthch (ho), thuc ht vo cha chc n fi m dnh ming.
u im: cho t/d ti ch, ko gy t.d ton thn
(2)
Hthu trc tip:
c im: ktn th g do chnh lch n, cc l mao mch tng i ln
pt ln c th i qua.
u im:liu dng < liu ung, hthu nhanh,sd khi thuc c mi v kh chu,
thuc ko tan trog lipid, hy hoi/PO(g` ug), nn ma, hn m, liu lng d
ksot, ko b chuyn ha ln u qua gan.
Nhc im: bt tin (cn v trng, k thut chuyn mn), km an ton, t
tin, gy au, tim qu liu fi lc mu hoc lc tiu.
Tim di da (SC):
Hthng mao mch di da t hn c hthu chm, n nh, t/d ko di.
Vin cy di da Insulin SC
Ngn dy TK cm gic nhiu hn c au, hoi t, trc da
Tim bp (IM):
Hp thu nhanh, t au hn SC
Tim truyn tnh mch (IV)
Vtim ln, hthu trn vn
Tng tc thi
Liu dng cxc, ksot c
Ko dng IV khi b kch ng, dd du, cht ko tan, c trn tim
Ko dng dd du v du gp nc nh ha tc nghn mch mu

- Tim ng mch: khi b ung th.

Ung th ly dinh dng t mu tg sinh mmu nui khi u tim M
nui khi u tc M mt g` th of khi u
Nhi mu no: tim thuc lm tan mu lu thg mu no
- ng thm qua thanh mc:
B m lt rt mng d hthu thuc
Tim mng fi, phc m, hot dch (KSinh, corticosteroid)
ng phc m gn bng ng tnh mch
- ng ty sng:
a thuc vo HTKTW
Vim mng no, ung th no
- Tc ng ti ch: t hthu vo mu hn ch dc t/d f, ch u nh vo
Nim mc: mi hu, m o, niu o; mt
Thuc ung: nhc im: tc hthu chm, VK g` rut, enzyme, hthu ko hton, thuc
kh ung, d gy nn
Thc qun ko hthu nhg d b nghn hoc dnh thuc
d) Sinh kh dng: (Bioavailability):
KN: knng c th sd v mt sinh hc p ng c th.
(Lng thuc hiu qu i vo vtr tg, dng chuyn ha ssg ti vtr tg)
- Tc + mc hthu ca thuc
- Hin din ti vtr tc ng
F = Liu thuc c hthu / liu thuc sd = AUCPO / AUCIV
AUC: ditch di ng cong tng lng thuc hthu ca c th
AUCIV = 100%
ng sd thuc c SKD ti nhiu nht l ng ung v ng ht
2) Phn b:
Sau hthu: thuc pb mu, m k, dch ni bo
- Phn b ban u:
L thuc vo cung lng tim, lu lng mu
Lu lng mu cao: no, phi, gan, thn
Lu lng mu thp hn: m m, da
B gii hn bi cc ro cn (Hng ro mu no)
- Phn b li (Ti pb): lquan tgian tc ng ca thuc
Sau khi pb cc m c lu lg mu cao ti pb cc m c i lc >
Thuc c th lu tr trog m m n c i lc cao
N thuc trog mu gim thuc t m fng thch li vo mu ko di
tg of thuc
Thuc pb nh` trog m: tgian tg ko di, tgian o thi chm li.
- Lin kt vi Protein huyt tng (Albumin, -glycoprotein acid, -globulin,
lipoprotein):
Gn ko chuyn bit
Phc hp thuc Protein: thun nghch, ko hot tnh, (ko chuyn ha, ko
o thi)lm chm chuyn ha, thi tr thuc.
Dng t do: c hot tnh (tg dc l), c htng cnh tranh,

Tr em: thuc t gn vs Pr huyt tng

Thuc gn vs Pr cao: liu cao ban u
Pr huyt tng gim: thn trng c tnh
90% dng lkt, 10% dng t do dn dn thi tr khi c th
- Kt hp vs m:
ch tc ng: thuc m/TKTW, digoxin/c tim
Ko fi l ch tc ng: tetracylin/rang
ngha: tg th tch pb, tg knag tng tc, tg tch ly thuc trog m,
ko di tgian tc ng
Thuc dng t do mi di chuyn c vo trog cc khoang ca c th. Thuc
dng lkt ko di chuyn c.
Thuc trong cc m gan, thn ko c i lc nn ko i vo m i ra.
- Th tch pb (Vd):
Thng s dc ng ca gon pb
Ko fi l 1 th tch tht s
Thg s: lquan gia n thuc/huyt tng vs tg lng thuc trog c th:
Vd = tg lg thuc trog cth (liu sd) / n thuc tr.thi n nh trog htg
Thuc A: Chtng=10mg/l, liu = 1000mg Vd = 100 l
Mc gn trn m >< mc gn trn Pr huyt tng
Vd cao gn vs m cao
Vd gn = Vmu gn vs Pr huyt tng
- Phn phi thuc vo no:
Thuc phn cc kh qua HRMN
Mng b vim thuc d thm qua
Bo thai, tr s sinh HRMN cha hon chnh thuc vo gy c cho
no di chng
Thuc ko thm qua HRMN tim ty sng
- Phn phi thuc/nhau thai:
Mch mu fi thai + mmu m HR nhau thai
90% thuc qua nhau thai ko c chuyn ha gy c tnh trn thai nhi
3) Chuyn ha (Bi sinh hc ca thuc trog c th):
Chuyn ha chuyn thnh cht d tan d d o thi
- Chuyn ha: chm dt, ti hot tnh ca thuc.
Thuc pcc (tan trog nc) thng ko chuyn ha ko THT, o thi nguyn
vn qua thn
Thuc ko pcc chuyn ha thnh thuc t pcc sau ti hthu thnh thuc pcc
ri o thi ra ngoi.
- Thng thng, chuyn ha:
Ti cht tan trog lipid cht tan trog nc bi tit
Thuc c hot tnh dc lc gim hoc mt hot tnh dc lc
Chuyn ha tg hot tnh, c tnh
Tin dc (Prodrug) thucc hot tnh

- Lm mt hot tnh (kh c tnh ) : phenol phenyl hydrogen sulfat tan trog
nc d thi ra ngoi
- Thay i hot tnh:
Diazepam thuc ng tg di ~24h Tenazepamm ~ 12h Oxizepam ~ 6h
L-dopa (prodrug) Dopamin c hot tnh tr bnh Parkinson R-(-)-Ibuprofen
ko hot tnh S-(+)-ibuprofen c hot tnh
Paracetamol c tdng h st, gim au. Liu cao: gy c, mt H trn phenol
chuyn thnh kinol gn t do vs Pr TB gan gy hy hoi TB gan vim gan
- Pha 1:thay i cu trc ha hc = cc phh.
- Pha 2: lin hp, lkt vs cht c sn trog c th
- Bi sinh hc ca thuc trc khi hthu: pH acid ca dch v c th lm mt hot
tnh ca thuc : insulin ch dng g` tim di da
- Bi sinh hc ca thuc trog mu: cc enzyme trog mu c th lm mt hot
tnh ca thuc: Esmolol thy fn nhm ester bi esterase/hcu h HA rt
nhanh do tg ln 1 RCT tim ko dg tr h/p lu di..
- Bi sinh hc ca thuc trog m: gan, g` tiu ha, thn, fi, da
Trong microsome cha tt c cc E chuyn ha thuc
Cc microsome enzyme ngoi gan (OXH, glucuronic ha)
Microsome enzyme gan (OXH, glucuronic ha)
Cc enzyme ko thuc microsome gan (acetyl ha, sulfat ha, GSH,
alcohol/aldehyde, dehydrogenase, thy fn, OXH-K)
Phn loi:
Microsomal enzyme:
Monooxygenase (mixed function oxidase)
C trn LNC trn
Gan thn fi rut
Chuyn ha fn ln thuc
P OXH, K, thy fn, lin hp
CYP (Cytochrom P450 CYP) : enzyme chuyn ha thuc chnh
FMO (Flavin-containing monooxygenase)
EH (Epoxide hydrolase)
UGT (UDP-Glucuronosyltransferase)
C th cm ng nhg microsome gan
Cm ng l khi dg 1 thuc bt k vo c th kthch TB gan tg s
hin din of CYP tg s lng CYP thuc ch?ha nhanh n thuc
trog mu gim tgian tdng gim
Non microsomal enzyme:
Ko c hiu
C trong bo tng, ty th
TB gan, cc m, huyt tng
Xc tc cc p OXH, kh, thy fn, lin hp
Ko b cm ng nhng a hnh
Protein oxidase, esterase, amidase, conjugase

Tr s sinh ko c hoc c rt t cc enzyme ny c tnh

Cc siro c cn, codein
L thuc di truyn (m d ng th con cng d ng)
Chuyn ha ln u:
Htng ch? ha thuc (ung) lm gim n thuc trc khi i vo vg tun hon
Thuc g` tiu ha (chuyn ha NM tiu ha) tnh mch ca (chuyn
ha gan) h tun hon chung
Gan: vtr chuyn ha chnh, y cc h enzyme
Nim mc tiu ha: CYP, sulfat ha, esterase, lipase.
VK rut: kh cc hp cht azo, nitro
100% thuc qua nim mc rut cn 30%, theo TM ca vo gan cn 15%
vo vng tun hon chung ca cth
H thng Cytochrom P450 (enzyme c mu)
LNC trn
Dg kh lkt vs CO
Hthu cc i 450nm
Hemoprotein (heme-thiolate)
Chuyn in t qua Fe2+& Fe3+
H cc hemoprotein : xc nh > 1000 loi, khong 50 loi c hot tnh ng`
ng chuyn ha chung:
Pha 1:
P thy fn: ester & cc amid, epoxide & cc aren oxid bi epoxide hydrase
OXH: nhn thm, olefin, C of benzyl & allyl, - C ca C=O & C=N, C ca
aliphatic alicylic, C ca h nt khc loi, alcohol & aldehyde
Kh: aldehyde, ceton, nitro, azo
Pha 2:
Lin hp vi: a.glucuronic, sulfat, glycin & a.a khc, glutathione or
a.mercapturic, acetyl ha, metyl ha
Phn t lng (MW):
MW < 300 thn nc tiu
MW >300 ti mt mt
Cc yu t nh hng n hot tnh & s biu hin cc enzyme ch? ha thuc:
Dinh dng: 1A2; 3A4,5
Ht thuc: 1A2
Ru: 2E1
Thuc tr: 2C; 2D6; 3A3; 3A4,5
Mtrng: 1A2; 2E1; 3A3; 3A4,5
Di truyn: 2C9,19; 2D6
S c ch cc enzyme chuyn ha thuc (inhibitor):
Nh` cht (thuc) c ch enzyme microsom gan
Tng tc dng, tng c tnh
Prodrug: gim t/d, gim c tnh

- S cm ng cc enzyme chuyn ha thuc (inducer):

Tng tng hp enzyme
Gim tc dng, gim c tnh
Prodrug: tng tc dng, tg c tnh
4) Thi tr:
Cc ng o thi chnh ca thuc:
- Nc tiu, nc bt, dch v, mt, dch rut, hi th, sa, m hi
- Thn, tiu ha, h hp, dch tit
- Cht tan trog nc qua g` tiu, cht ko tan theo phn, cht d bay hi &kh
qua fi.
- Tinh du bi tit qua g` h hp
a) o thi qua thn:
- Phn ln thuc htan o thi qua thn
- ~ 80% lng thuc b o thi trog 24h u
- Ph thuc 3 c ch:
Lc qua cu thn: thuc Pr huyt tg, f thuc tc lc, ch dg t do mi
c lc. khi lng mu n cu thn gim thuc b gim hot tnhnn bnh
nhn suy thn fi gim liu sd
Bi tit ch ng qua biu m ng thn: OAT, OCT
Ti hp thu th g biu m ng thn: ktn th g, pH nc tiu, pKa of thuc
b) o thi qua g` tiu ha:
- o thi trog mt qua fn ra ngoi
- Ko tan, ko hthu o thi qua fn
- Bi tit nc bt, mt, dch tiu ha o thi qua tiu ha
- THT tr li gan qua TM ca chu k gan - rut (thuc lu tr trog mu lu)
c) o thi qua h hp: D bay hi
d) o thi qua con g` khc: da, lg, tc, m hi, nc mt, nc mi
Cc thng s dc ng ca qt o thi
- thanh thi (Clearance CL)
Thut ng m t hiu qu loi tr thuc khi c th
Ko fi ch s cho bit lng thuc c loi tr
Vmu (l thuyt) thanh thi thuc theo v tgian
Thg thg`: tng quan bc 1 (tuyn tnh)
CL = tc thanh thi/ n trog huyt tng (Cp) = Liu/AUC
CL = CLthn + CLgan + CLm khc
Khong tr liu, tgian tg, n n nh C ss: t hthu = t thanh thi
- ng hc bc 1:
L 1 t l hng nh o thi theo n v tgian
N thuc gim dn theo hng s m, theo g` cong tgian
Ko f thuc n thuc ban u
Tng liu, tg s ln sd c lng c n thuc trog huyt tng
- ng hc bc 0:
L lng thuc hng nh c o thi trong 1 v tgian

 N thuc gim dn theo hm bc 1 (tuyn tnh)

Tng liu, tng s ln sd kh c lng c n thuc/ huyt tng
- Thi gian bn thi T1/2: tgian m n thuc/huyt tng gim xung 1 na
- Tnh ton liu lng:
IV: Tc truyn = thanh thi x n tr liu / sinh kh dng
Liu duy tr (PO): = kcch liu x tc truyn/sinh kh dng
Liu np = th tch pb x n tr liu
C CH TC NG CA THUC
1) ch tc ng ca thuc
- Receptor:
Cht ch vn: tr.tip ti c/n TB hot ha, c ch enzyme, ng m knh
ion, iu bin knh ion, sao chp DNA
Cht i khng: ko c tg, ngn chn tg ca cht ch vn
- Knh ion:
Cht chn knh ion: ko cho ion vo TB
Cht iu bin: lm tng, gim t l m knh ion
- Enzyme
- Cht vn chuyn
Metyldopan ung vo chuyn thnh metyldopamin gn vo RCT lm cn tr mch
mu gim huyt p
2) RECEPTOR:
Cc pt Pr
Gn c hiu vs 1 s cht (ni, ngoi sinh ligand) tr` tn hiu p ng
a) Tng tc thuc RCT:
Pt hiu ng (Effector): thuc receptor p ng
- i lc ca thuc vs RCT
- Loi, s lng
- Cu trc ko gian
- Lc ni pt
- LK Van der Waal: lk yu, o nghch c.
LK hydro: lk TBnh, o nghch c
LK CHT: lk mnh, ko o nghch
LK ng t
- Hiu qu ca p ng: f thuc t l thuc gn vs Pr
(1) p ng ti a (full agonist): cht ch vn, g vn ton fn
Gn v hot ha RCT
Cho p ng ti a
Hot tnh ni ti (bn th) = 1
(2) Khng p ng (Antagonist): cht i khng
Gn vs RCT nhg ko hot ha RCT
Ngn chn p ng
Hot tnh ni ti (bn th) = 0
(3)p ng 1 fn (Partial Agonist): cht ch vn, ng vn 1 fn
Gn v hot ha RCT

 Khng cho p ng ti a
Hot tnh ni ti (bn th) 0 < < 1
i khng khi c s hin din ca cht ch vn ton fn
(4)p ng nghch (Inverse Agonist): cht ch vn o nghch
Gn vs RCT & c ch RCT
Cho p ng di ngng bth
(5) Constitutive RCT: RCT cu trc
c hot ha khi ko c mt ca ligand (phi t, thuc) ngn chn
p ng : inverse agonist > antagonist
RCT of benzodiazepine, cannabinoid, serotonin
(6)Spare RCT: RCT d tr
Ko gn vs ligand nhg vn cho tg ti a
T l gn thp
Cc thuc kthch co c
Cht i khng
- Cht i khng dc l: 2 thuc gn cg RCT vs cht ch vn ko hot ha
- i khng cnh tranh: gn thun nghch vs RCT, khi fc hot tnh khi tg liu
- i khng ko thun nghch: gn cht vo RCT ( rt kh ply), tg liu ko khi
fc hot tnh
- i khg sinh l: gn trn 2 RCT hton khc
- i khng ha hc: cht i khg gn tr.tip vs cht b i khg ngn cht
ny tin n mc tiu tg
b) C ch tc ng mc pt:
(1)Receptor gn vs knh ion:
- p ng TB: mili giy; Nicotin RCT
- Pr xuyn mng cho fp 1 s ion c hiu i qua
- Knh ion c 3 tr.thi:
Ngh: ag ng, c th m khi c hot ha
ang hot g: ag m
Bt hot: g nhg ko m c d hot ha
(2)RCT gn vs G Protein: l 1 RCT chnh
- 3 tiu v: , , (c nh` dg khc nhau)
- Gn vs GDP (Guanosin diphosphat) khi ko hot ha
- Khi c hot ha GDP GTP
- Effector: adenylyl cyclase (AC), guanylyl cyclase (GC), phospholipase C
(PLC), knh ion
Adrenalin gn tr.tip ln 1 RCT co mch
G* PLC tg Ca2+
GS AC tg AMPvng
Gi AC gim AMPvng
(3)RCT gn vs enzyme
(4)RCT ni bo
c) iu ha cc receptor:

Kthch ltc mt nhy cm

c ch ltc tng p ng (p hi ng rebound)
Tnh chn lc ca thuc trn receptor:
Ko c thuc tc ng chuyn bit (specific)
Ch c thuc tc ng chn lc (selective)
Dng thuc liu thp nht, fi hp khc c ch, tng tinh chn lc
e) Cc c ch khc:
- Thuc li tiu loi thm thu (manitol, ur)
- Thuc khg acid ca d dy
- Cc thuc gy acid ha, kim ha nc tiu
CC YU T NH HNG N TC NG CA THUC
1) TNG TC THUC
KN: Sd g thi (>= 2 thuc) lm ti tc dg hoc c tnh KQ c li hoc c hi
L htng xy ra khi t/d ca 1 thuc b bi do s hin din ca 1 thuc khc, t/n,
thc ung, dc liu, bnh l no
Phn loi:
- Theo i tng: thuc thuc, thuc t/n, thuc bnh l
- Theo dc l
a) Tng tc dc ng: xy ra lm ti c tnh dc ng ca thuc
- Tng tc trog qt hp thu: tetracylin to fc vs Ca2+ nn n ksinh ko b sug Ca dc
- Tng tc trog qt pb: tng gim s lng ion trog mu
- Tng tc trog qt chuyn ha: triazolam tr gic ng u gic to fc vs
Ketoconazol tr nm xt nh enzyme CYP 3A4 cht ch? ha t c n ch nh
- Tng tc trog qt bi tit: penicillin to fc vs probenecid ng thn lm tng n
penicillin mu tr nhim khun
b) Tng tc dc lc:xy ra khi t/d of 1 thuc b ti do s hin din of 1 thuc
khc, cht khc ti vtr tg ca n
- i khng: thuc A lm gim hoc mt hiu lc thuc B
- Hip lc:
Thuc A lm tng hiu lc /v thuc B v: t t/g, c tg, tgian tg
Hip lc b sung : c = a + b
Hip lc bi tng: c > a + b
c) ngha:
- nh gi tg trn lm sng:
Ksot c tnh: thuc c khag tr liu hp, chg ch nh, gii c
Liu lng: liu, tn sut, tgian
Mc tng tc
Tn sut xy ra tng tc
- Chin lc tr liu hp l:
Gim s thuc k toa, nm r tt c cc thuc BN sd, sd cch xa, khi u = liu <
2) DUNG NP L THUC D NG THUC:
a) Dung np thuc:
Kh nng c th thch nghi vs thuc:
- p ng yu hn bth
- c tnh xy ra liu cao hn bth
d)
-

Dung np bm sinh: chng, gtnh

Dung np thu nhn: xy ra khi dng lu di, lp li
Min dch nhanh: dung np thuc ch trog tgian ngn
Lm dng thuc (abuse): dng thuc ngoi mc ch tr
Dng sai thuc (missuse): sai v liu lg v ch nh
b) L thuc thuc
L 1 tr.thi do lm dng thuc vi cc t/cht :
- Sd liu cao hn bth nh` ln
- Dung np thuc r
- Hi chng cai thuc
L thuc tm l: tm l & hnh vi tm kim thuc 1 cch bt buc
L thuc th cht: cc triu chng do thiu thuc
L thuc cho: (2 nhm thuc # nhau) l thuc nhm ny l thuc nhm kia
Quen thuc (habituation): mc nh ca l thuc thuc
Nghin (addiction): mc nng ca l thuc thuc
3) TUI TC TH TRNG MI TRNG:
a) Yu t thuc c im ng bnh:
Tui tc
- Tr em: chuyn ha cha hon chnh, gn vo Pr huyt tg km, HRMN cha
ptr y , hthng o thi thuc qua thn cha hon chnh
- Ng cao tui: rt nhy cm vs thuc, chuyn ha & o thi thuc km
Trng lng:
- Liu dng:
Liu tr em = Sb mt c th tr em(m2)/1,73(m2) x liu ng ln
= liu ng ln x th trng tr em/60
= tui/(tui + 12) x liu ng ln
(/v tr em >2t)
= tui (thng) / 150 x liu ng ln
(/v tr em <=2t)
Phi tnh: morphin / mnh hn n
Chng tc: da trng > da mu (m rg con ngi ca atropine
Cch dng thuc: dung np thuc
Trng thi c th: mn cm bm sinh, thu nhn
Ch n ung
Tr.thi bnh l
Thi k kinh nguyt, mang thai
b) Yu t ko thuc ng bnh:
To mt, as tia cc tm, s ng, t/d thi theo ma & chu k ngy m
C LNG C TNH THUC:
Thuc nh hng ln tim tun 3 8
Tun 3: h ban tim
Tun 3 5: h hm ch nu m b cm
Ung t tun 12: ko b nh hng.
Phn loi thuc trn thai k:
- Loi A: th lm sng c i chng thuc ko c nguy c vs bo thai trog sut thai k
(acid folic, vit B6) sd dc cho pn c thai
- Loi B: th trn sc vt ko c nguy c & cha th pn c thai or sc vt c nguy c
nhg cha c = chng tin cy chg t c nguy c /v thai ph (prednisolone, insulin)

- Loi C: th trn sc vt c nguy c & cha c = chg trn pn c thai or cha th c

trn sc vt v cha c = chg trn ng` (fluconazole, ciprofloxacin)
- Loi D: c = chg nguy c vs thai nhg vi THp li ch tr > nguy c (phenytoin)
- Loi X: th trn sc vt or ng` or trn knghim dg thuc lu di c nguy c vs thai
& nguy c cao hn li ch tr ph n mang thai (isotretinoin)
THUC TC NG TRN H THN KINH THC VT
H GC pb ht tt c cc CQ, xft t si tin hch
H GC xft t fa trn ct sng
1) H Adrenergic (GC):
- - adrenergic:
1 : c trn mch mu, gan, ty tng, tuyn ngoi tit, c tia mng mt
2 : TKTW, mch mu, si tin xynap
- - adrenergic:
1 : c tim
2 : c trn f qun, t cung,bng quang, mmu c vn
3 : m m
2) H Cholinergic (GC)
- Muscarin:
M1: c trn, tuyn, hch TKTV
M2: c tim
M3 : c trn, tuyn
- Nicotin:
NM: bn vng c xng
NN: hch TKTV, m TKTW, tuyn thng thn
THUC CNG GIAO CM
1) Phn loi:
- Tng tr.tip: tng ln rct andrenergic, i lc khc nhau trn cc rct
- Tng gtip: tng s lng Catecholamin ni sinh (dopamine, adrenalin,
noradrenalin) ri gn ln rct
- Kthch :
1 G* PLC tng Ca2+ TB
2 Gi AC Gim AMPvng TB
Gs AC tng AMPv TB
2) Sinh tng hp thoi ha:
Tyrosin dopa dopamine noradrenalin adrenalin
- TKTW ch tit dopamine
- Tyrosin, dopa, dopamine HTKTW dopamine
- Tyrosin dopa dopamine noradrenalin: HTK ngoi bin
- Adrenalin : TKTV
- dopamine noradrenalin adrenalin: Catecholamin kthch GC
- phn ty ca tuyn thng thntit ra Catecholamin
- phn v ca tuyn thng thn tit ra corticoid

3) Cng giao cm trc tip

a) Receptor &:
ADRENALIN (EPINEPHRIN) :
- ng hthu:
PO: ko hiu lc
SC: t/d chm (co mch) tim vs thuc t ko di tgian gy t
IM: t/d nhanh t dng v ko ksot c n
IV: dng khi cp cu: ngng tim, try tim, sc phn v
Xng ht: t trn nim mc
- Tc dng dc l: u th trn tim, mch, c trn khc
Tim: rct 1: tng sc co bp c tim, tg nhp tim, tg dn tr` tim p
nhanh, mnh tng nhu cu sd oxy
Mch huyt p:
Liu thp: rct 2 : gin mch, h HA
Liu TB: tng HA va fi (tim p nhanh, tg sc co bp c tim)
Liu cao: tng huyt p rt mnh chm nhp tim (1 u th - tim)
C trn: rct 2
Gin c trn (ph qun, tiu ha)
Co c vng (bng quang)
Ngn co c t cung cui thai k
Chuyn ha: tng n glu huyt (kthch 2, 2 ly gii glycogen gan),
tg n acid bo t do
TKTW: kthch TKTW yu liu tr (bn chn, run ry, au u)
- S dng tr liu:
Chng co tht f qun
Nng huyt p, sc phn v
Ko di t.d thuc t
Cm mu ti ch do lm co mch
Phc hi tim cho bnh nhn ngng tim t ngt
- Tc dng ph -c tnh:
Lo u, hi hp, bn chn, au u, kh th, nh trng ngc
Xut huyt no, lon nhp tim (him gp) khi qua liu tg ln 1, 1
tng HA, v mch mu (thn trg vs bnh nhn cao HA)
- Chng ch nh
Cng gip, bnh tim (nhi mu c tim, au tht ngc), thn kinh
S dng vs cht chn ko chuyn bit gy i khng hton
NORADRENALIN:
- Ng.gc: tn cng dy hu hch GC, ty thng thn, m TK
- Ko dc sd trog cp cu, ch dng ng tim IV. Ko tim bp, di da trn
thuc ni tim hoi t.
- Tc dng dc l:
Tim: ging adrenalin trn 1

 Mch: hiu lc trn 2 kthch tim co mch ton thn tng HA (nhp
tim chm)
C trn: tdng yu, gy co tht t cung trog thai k
- Tc dng ph -c tnh:
Tng t adrenalin nhg nh v him xy ra hn
Liu c tg HA nng, lon nhp tim
Chng ch nh PH N MANG THAI
- Sd tr liu:
Sc do chn thng, phu thut
Ko dng trog nhi mu c tim
DOPAMIN: (D1, D2,.RECEPTOR nm trong no)
- Tc dng dc l:
Liu thp: gin mch (D1 ngoi bin) thn: tng sc lc, lu lng mu
qua thn ci thin tc lc cu thn
Liu TB: kthch co bp c tim (1), HA tm thu tg, HA tm trg t b a?h?
Liu cao: gy co mch (1)
D2 c ch catecholamine
- S dng tr liu:
Sc do tim (lu lg tim gim, HA gim px co mch, tng nhp tim) hay
do nhim trng
Sc bnh nhn b tiu niu, ri lon chc nng thn, try tim
Ch dng g` IV
- c tnh:
Do qu liu: nn ma, au tht ngc, au u, lon nhp tim, tng HA
- Chng ch nh: fi hp vs IMAO (Mono amin oxidase inhibitor)
b) Receptor :
- 1 : Trc tip (Methoxamin, Phenylephrin), Trc tip & gtip (Mephentermin,
Metaraminol)
- 2 : Lit GC TW (Clonidin, Methyldopa, Guanabenz, Guanfacin)
Cht tc ng u th trn receptor 1:
- Hot ha rct 1 trn c trn mch mu co mch, tng HA
- Sd tr liu gii hn trog THp h huyt p hay sc
- Dng ti ch: co mch ti ch nhanh & ko di, gim sg, gim xung huyt
- t/d ph: kthch TKTW, tng HA qu , lon nhp (mephentermin, metaraminol)
Kch thch chuyn bit rct 1:
- Phenylephrine: dd thg` sd trog tc cc g` tim h HA do gy t ty sng,
chn thg ty sng, gin g t, chg xug huyt mng nhy mi
- Naphazolin, Tetrahydrozolin, Xylometazolin: dd nh mi lm co mch mu,
gim triu chng ngt mi, gim xung huyt
c) Receptor :
ISOPRENALIN:
- Kthch ko chn lc rct :

- 1 : kthch c tim co bp
- 2: kthch c trn ph qun gin f qun
- Tc dng dc l:
Tim mch:
1 : tng sc co bp, tg nhp tim tg lu lng tim tg HA tm thu,
gim HA tm trg & TBnh
2: gin mch gim sc cn ngoi bin
C trn:
Gin c trn h hp (kthch tim, lm ngng tim ko dng tr hen )
Gin c trn tiu ha
Kthch 2 dng bo c ch tit Histamin, Leucotrien
Liu cao gy dung np
Chuyn ha: t gy tg glu mu, kthch thy fn lipid
- Tdng ph -c tnh: t xy ra hn adrenalin, liu cao gy lon nhp
- Sd tr liu: kthch tim (tim chm, ngng tim), Hen suyn (t sd)
DOBUTAMIN:
- u th trn 1 ca tim
- Tng co bp c tim
- t lm tng nhp tim
- Gn c trn rct D1 gin ng mch thn ci thin c tc lc cu thn
- Tim truyn TM: t/d nhanh
- S dng tr liu:Suy tim sau m, suy tim xung huyt, nhi mu c tim cp
Cc thuc kthch chuyn bit trn rct 2
- c sd trog tr hen suyn
- C ch: tg chn lc trn 2
G-Pr loi Gs gn vs AC tng AMPv
c ch pthch cht TGHH t TB mast : Histamin(gy p d ng), Leucotrien (gy
co tht ph qun mnh)
- C th dng g` PO (do bn vs MAO & COMP)
- C th dng qua g` h hp t t/d ph ton thn
- COPD: hi chng phi tc nghn mn tnh
- Metaproterenol (Orciprenalin), Terbutalin, Albuterol (Salbutamol),
Pirbuterol, Bitolterol: thuc c thi gian khi pht cc nhanh (sau 3-4 gin f
qun), dng ct cn hen, ch nh co tht ph qun cp & mn
- Bambutero, Salmetetol (ksot cn hen v m), Formoterol, Ritodrin (chg
co tht t cung, nga sinh non): thuc c tgian khi pht chm & ko di.
- Tc dng ph: hin tng dung np : liu cao, g` tim chch
4) Cng GC gin tip:
AMPHETAMIN (ma ty )
- Kthch TKTW mnh
- C ch: fng thch NE khe xynap kthch ltc ko cm thy mt
EPHEDRIN:
- Alkaloid / cy Ma hong
- C ch tc ng: gin tip & trc tip tng catecholamine C

PSEUDOEPHEDRIN (tin cht ma ty): c tnh thp hn

Kthch TK TW
Kthch TK GC: tng HA & nhp tim, gy gin ph qun (2)
Gy quen thuc nhanh
PHENYLPROPANOLAMIN (PPA): ko sd
Fi hp vs cc thuc tr cm cm, vim mi
SD lu di gy nguy c cao v tim mch, t qu

THUC LIT GIAO CM

1) Phn loi:
- Tng tr.tip: c ch ln rct ca h adrenergic
- T.ng gin tip: lm gim lng catecholamineni sinh tn cng TK GC =
cc c ch khc nhau
2) Cht c ch - adrenergic:
- Tc ng dc l
Cht c ch 1 adrenergic: gim n catecholamin
Gy gin mch, h HA tim p nhanh (t/c b tr) a HA v bth
Px tim nhanh
C thm hiu lc c ch 2 px tim nhanh cg r
Cht c ch 2 adrenergic
Tng HA, tim nhanh tng n catecholamine
C thm hiu lc c ch 1 tng tng HA c th ko xy ra
a) Cc cht c ch ko chn lc (chn 1 & 2)
Phenoxybenzamin, Phentolamin, Tolazolin tng s lng TB tg n
catecholamine tng HA t ngt
- Sd tr liu: u ty thng thn
b) PRAZOSIN: thuc dng gin mch d lu thg mu
- i khng chn lc trn 1 h HA
- Thng k gy tim nhanh
- SD tr liu: tng HA, suy tim mu, hin tng Raynaud (tm ti u chi), ph
i tuyn tin lit lnh tnh
- Kthch 1 co kh tiu
- Ko c sd u tin tr tng HA
c) ALKALOID : ca nm ca g Ergoalkaloid
- Thuc i khng trn rct serotonin
- Tng trn rct adrenergic, dopamine, serotonin
Ergotamin:
Ch vn tng fn trn adrenergic
t/d trc tip lm co c trn
tr au na u
Dihydroergotamin:
Ch vn trn adrenergic
i khng trn rct serotoninergic

 tr ct cn & fng nga cn au na u

Methysergid:
Khng serotonin mnh
Dng tt hn ergotamine & dihydroergotami (DHE) do t c tnh hn
Dng fng nga cn au na u
Bromocriptin :
Kthch rct Dopaminergic
Dng trong chng chy sa do tit Prolactin (to v nam), bnh Parkinson
Ergonovin:
Kthch co tht c trn gim chy mu sau sinh (hu sn)
- c tnh: bun nn, nn ma, au c, co mch, Raynaud hoi t, co mch
vnh tim au tht ngc, lon nhp tim
3) Cht c ch - adrenergic:
a) Phn loi:
- c ch ko chn lc: trn 1&2
- c ch chn lc: ch trn 1
b) Tc ng dc l:
- Tim mch huyt p:
Tim: gim s co bp, gim nhp tim & dn truyn c tim gim lu lng
tim & gim nhu cu oxy c tim
Mch: gin mch
Huyt p: lm h huyt p BN cao HA cn ng` bth ko gy h HA
- H hp: c ch 2 co tht ph qun BN hen suyn
- S bin dng: i khng vs cc tng ca adrenalin
BN i tho g`: tng tc g insulin & cc thuc h g` huyt ng PO
BN cao huyt p, hen suyn: chn thuc chn 1
c) S dng tr liu:
- au tht ngc (Mmu tim b hp mu ko cug cp cho tim)
- Lon nhp tim ( chn 1 c ch dn tr` tg nhp tim n nh)
- Cao HA
- Tng nhn p (Timolol
- au na u
- Cng gip
d) Tc dng ph - ctnh :
- Thn kinh: xo trn gic ng, suy nhc
- Tim mch: chm nhp tim
- Co tht ph qun BN hen suyn
- Che y triu chng h ng huyt
- Khng c ngng thuc t ngt gy p hi ng HA tng t ngt
e) Chng ch nh
- Hen suyn
- Nhp tim chm (<45 ln/p)
- Nghn nh tht mc nng tim co bp ko ng b

- Suy tim xung huyt mu trn tim

- Phi hp vs floctafenin (thuc gim au), thuc gim dn tr`, gim sc co bp,
gim tnh t ng ca tim
- Hin tng Raynaud
4) Lit GC gin tip:
- Lm gim lng catecholamine ni sinh tn cng TKGC
- B mt tdng khi ct dy TK hu hch GC
- Reserpin, Guanethidin, Clonidin, Methyldopa cht TGian gi to
- Thuc kthch 2 : iu khin ngc gn vo NE gim fng thch NE lit
GC gin tip ko gn c trn rct
RESERPIN: t sd
- Liu thp: h HA
- Liu cao: suy nhc, an thn
- Tdng ph: mt knng tp trug, tiu chy, lot d dy, ung th v
GUANETHIDIN
CLONIDIN:
- Kthch 2ti no gim trng lc giao cm ti trug khu ha tim mch
- Sd tr liu: cao HA, tr h tr cai nghin cc cht loi morphin (do c ch dn
tr` TK lquan), gim au BN ung th ko p ng vs morphin
- Tc dng ph:
Kh ming, an thn, nhp tim chm
C th gy triu chng thiu thuc
METHYLDOPA:
Phi hp vs thuc li tiu hiu qu h HA tt cho ph n mang thai
THUC CNG I GIAO CM
1) Phn loi:
- Cng i giao cm trc tip: tc ng trn rct ca acetylcholine
- Cng i giao cm gin tip: tng n ACh, ko gn vs rct c ch men
acetylcholinesterase (AChE)
Khng cholinesterase c phc hi
Khng cholinesterase ko phc hi
2) C ch
Choline + Acetyl CoA Acetylcholine transferase Ach fn hy bi AChE
Choline + acid acetic
ACh gn trn Ach rct: M & N
3) Cng i giao cm tr.tip:
ACETYLCHOLINE:
a) C ch:
M ch kthch:
- M1, M3: G* + PLC tng Ca2+ ni bo p ng TB
- M2: Gi + AC gim AMPv gim hot p ng TB tim p chm li
- NN & NM gn trn knh ion hot ha knh ion Na+ vo trog lm ti HT
kthch c hng tng Ca2+ ni bo co c

b) Cht i khng in hnh:

- M rct: Atropin
- N rct: N1 hexamethonium, N2 decamethonium
c) Tc ng loi Muscarin
- Tim mch (M2): gin mch, h HA gim nhp tim, sc co bp, dn truyn
- C trn (M3): co tht (ph qun, d dy, rut)
- C vng: gin c (bang quang,)
- Mt: thu hp con ngi iu tit nhn gn. M rng ng Schlemm (knh
thot nc mt trong hc mt) g` thot nc mt rg ra tr Glaucom
Glaucom: bnh tng nhn p
- Tuyn (M1): tng tit (nc bt, m hi, dch tiu ha, h hp)
Cc tc dng trn b hy bi atropin
d) Tc ng loi Nicotin
- Hch GC & ty thng thn (NN): co mch, tg nhp tim, h HA
- C vn (NM): liu thp gy co tht, liu cao gy lit c (chut rt)
e) S dng tr liu:
- t dng trn lm sng
- Ch dng gin mch trong bnh Raynaud
Cc cht tng t ACh: cc ester ca choline
- Methacholin: nhy cm vs AChE, tg muscarin trn tim mch tr glaucom
(+neostigmine)
- Carbachol: ko b phn hy bi AChE, tg nicotinicch nh chnh tr glaucom
- Bethanechol: ko b phn hy bi AChE, tg muscarin trn c trn tiu ha
ch nh: lit rut (mt K+ trog tiu chy, sau fu thut rut ko hg),d dy
ALKALOID: ch gn ln rct M
- Muscarin:
Alkaloid trong nm c : Amanita muscaria
Hiu lc mnh hn ACh, ko b fn hy bi AChE
c tnh cao ko dng trog tr liu
Gii c = atropine
- Pilocarpin: chit t alkaloid
Ko b phn hy bi AChE
Amin bc 3, bn hn so vi ACh
Tng ch yu trn Muscarinic, 1 fn rt t Nicotinic
Kthch TKTW
Ch nh chnh: co ng tnh mt: tr glaucom
Khng atropine (gin ng t)
Tng tit cc tuyn ngoi tit ung: tr kh ming
- Arecholin:
Alkaloid trong ht cau : Areca catechu
Tng mnh hn ACh
c tnh cao, dng trog th y: tr giun
4) Cng i giao cm gin tip:

a) Khng Cholinesterase c phc hi: gn vo ri nh ra, hi phc khi ht thuc :

tr li AChE gim n ACh
- Amin bc 3 (Physostigmin):
tr Glaucom, nhc c
Gii c atropine, cht chng trm cm 3 vng
tr Alzheimer (bnh mt tr nh ng` cao tui: vg no b tn thng lm
gim n ACh) : thuc tr Physostigmin, Tacrin, Donepezil,
Rivastigmin, Galantamin.
- Amin bc 4:
Neostigmin, Pyridostigmin, Edrophonium: lit rut, b tiu sau m,
nhc c, gFlaucom, ng c atropine
Ambenonium (tr nhc c), Demecarium (tr glaucom): tng ko di
b) Khng cholinesterase ko phc hi:
- Cc phosphor hu c gn bn vng vs cholinesterase tch t ACh
- Thn du d thm qua MTB TK, TKTW ch dng cc cht cho tng ti ch
- Hu ht l cht c ko sd tr liu: DFP (cht c ctranh), Echothiopat iodur (co
g t ko di nh` tun), Paraoxon, Malathion, TEPP (dit cn trg), Tabun,
Sarin, Soman (cht c ctranh)
- Triu chng: nn ma, kh th, chy nc bt (M1), thu nh con ngi, tiu
chy, co git, tim chm (M2), suy nhc.
- iu tr: cht lm ti sinh AChE
Pralidoxim: IV chm
Trimedoxim: IM hay SC
Obidoxim: mnh hn Pralidoxim
C 3 cht trn u fi kt hp vs ATROPIN
THUC LIT I GIAO CM
(ngn chn s tg ca ACh n rct, gn ln & c ch rct)
- Hp cht thin nhin: Atropin, Scopolamin
- Hp cht bn tng hp & tng hp: N-butyl sopolamin
1) ATROPIN SCOPOLAMIN:
i khng cnh tranh vs rct Cholinergic ti hu hch GC
- Ch tg ln receptor M gn vo M ngn ko cho ACh gn vo lit GC
- Gm cc rct ti c trn, tuyn ngoi tit, tim & mt
nhy cm tng theo th t: ph qun, tuyn nc bt & m hi, mt, tim,
ng tiu ha
- Khng tc ng trn rct nicotinic
a) Tc ng dc l:
- TKTW:
Liu thp (0,5mg): suy nhc, bun ng, th (Scopolamin)
Liu c (10mg): kthch, o gic, m sng
- Mt: ko di 7 12 ngy nguy him: glaucom
- Trn tim:
Atropin (0,4 0,6 mg), Scopolamin (0,1 0,2 mg): Tim chm (M1)
Liu cao: tim nhanh (M2)

- Trn mch:
Dng ring l: t/d ko r
Liu iu tr: i khng vs tc ng gy gin mch
Liu c: bng
- Trn ng tiu ha:
Gim nhu ng d dy rut
Lm gim s tit dch v
- H hp: c ch s tit dch h2, lm kh mng nhy dng lm thuc tin m
Khi gy m dch hh tit nhiu trn vo g` hh gy nght th
- Cc c trn khc:
Gim co tht bng quang, ti mt, ng dn mt
c ch bi tit m hi da kh, tng thn nhit
Thuc gim au do co tht c trn - ATROPIN
b) Tc ng theo liu:
- 0,5 mg: gim nh nhp tim, hi kh ming, gim tit m hi
- 1 mg: kh ming r, kht, nhp tim nhanh, gin nh ng t
- 2 mg: nhp tim , trg ngc, kh ming, gin g t r, kh iu tit nhn gn
- 5 mg: cc t/c trn r hn: kh ft m v nut; mt mi, ng ny, au u, da kh
nng, kh tiu, gim nhu ng rut
- 10 mg: mch nhanh, yu, ko nhn r, da kh, nng, : tht iu, kthch, o
gic m sng
c) Dc ng hc:
- Hthu d dng qua PO, tim di da
- Kh thm qua da
- Chuyn ha 1 fn qua gan, fn cn li c o thi qua nc tiu
- T1/2 = 4h
d) S dng tr liu:
- Nhn khoa: gin ng t soi y mt
- Tim mch: block nh tht, tim chm do f v
- Phu thut: tin m (chng ngng tim trog khi gy m)
- iu tr ng c: thuc dit su ry, phosphor hu c
- Chng nn: Scopolamin ming dn say tu xe
Thuc
Nhm thuc
Say tu xe
Dimenhydrinat
Khng Histamin H1
Diphenhydramin
Scopolamin
Khng choline (thuc lit GC)
Thai k
Dimenhydrinat
Khng Histamin
Diphenhydramin
Metoclopramid
Khng dopamine
Domperiden
Do thuc tr
Ondansetron
Khng serotonin
Granisetron
ung th
e) Tc dng ph - c tnh:
- Kh ming

- Ri lon th gic
- Kh tiu, to bn
- Tim nhanh, nh trng ngc
- Kthch TK
- Ng c/tr em, ng gitr vs thuc khng cholinesterase
2) DN CHT AMIN BC 4:
Tng chn lc hn atropine/nhn khoa, c trn, h hp, tiu ha, tit niu &
bnh Parkinson
a) Hormotropin, Metybromid:
c ch hch mnh trn rct N l ch yu, 1 fn M tr au do co tht h THa
b) Methanthelin, Propanthelin:
- c ch hch mnh
- t tc dng ph do h M
c) N-butyl scopolamine:
- Chg co tht c trn mnh hn atropine
- t t/d ph ton thn, ko nh hng TKTW
d) Ipratropium:
- Khng tc ng trn HTKTW
- Tng khng ACh mnh hn atropine gin ph qun, ko lm kh n.mc hh
- Km hthu ti ch, tiu ha
- Tr liu: COPD & hen suyn
ng xng ht: t tc dng ph ton thn
Tim chch: tc ng trn h M& N u mnh
3) DN CHT AMIN BC 3:
- Homatropin.HCl, HBr; Cyclopentolat.HCl; Tropicamid nhn khoa
- Benztropin, TrihexyphenidylParkinson, RL ngoi thp. Phi hp vs levodopa
- Dicyclomin, Oxyphencyclimin, Oxybutynin, Flavoxat chg co tht c trn.
Lit GC yu gin c trn
4) CHT C CH CHUYN BIT Receptor M1
Pirenzepin/Telenzepin
- c ch tit acid dch v dng trong lot d dy t trng hin nay ko sd
- T.d f loi atropine rt thp
- Ko t.d trn TKTW
THUC CHNG CO THT C TRN
Hng c
1) Phn loi:
- Thuc chng co tht c trn hng thn kinh (Neurotrope)
Rct TK c
Cht TGHH TK
Thay i in th mng
- Thuc chng co tht c trn hng c trn (Musculotrope):
Thay i lng Ca2+ t bo
2) PAPAVERIN:
- Alkaloid nhn isoquinolein: Papaver somniferum (nha cy thuc phin)

- Chng co tht c trn do: BaCl2, ACh, Histamin

- C ch tc ng: c ch phosphodiesterase tng AMPv gim lng Ca2+
ni bo gin c
- Sd tr liu:
Co tht c trn ng tiu ha, tit niu, ng mt
C trn mch mu (au tht ngc, nhi mu c tim, co tht ph qun)
Si thn, si mt
- Tc dng ph - c tnh:
Tim chm, h HA th ng
Lon nhp tin
RL tiu ha, au u
c vs gan
- Thuc tng hp (tng tng t):
Drotaverin, Fenoverin, Alverin Dipropylin, Aminopromazin
THUC LM MM C XNG. THUC LIT HCH: ch yu trn rct N
c ch co tht c xng do tng ln rct NM bn vn ng
- Tc ng ln bn vng ngn kh cc of c
Cc cht loi curare: Toxiferin, D tubocurarin, Alcuronium, Pancuronium.
- Tc ng ln bn vg ko di s kh cc of c
Succinylcholin (suxamethonium), Decamethonium
Phng thch ACh lm mm c
- Tc ng dc l
TKTW: ko c tg
Hch TKTV:
Loi curare: c ch 1 fn liu tr
Loi kh cc: c ch km
Bn vgc xng: gin c lit c, c t.c tim tin
Phng thch Histamin
- SD tr liu:
H tr gy m, phu thut chnh hnh, t ni kh qun, thg kh c hc, ni
soi thanh qun, kh qun, gp d vt
Tubocurarin cn chn on bnh nhc c, fg co tht c trog pp sc in
- c tnh:
Kh th ko di, try tim mch, suy h hp
Thuc gin c theo c ch TK c
Thuc
Sd tr liu
Tc dng ph
Mephenesin
Co tht c gy au do
Bun ng, nn, d ng da
Thiocolchicosid thoi ha ct sng, RL t D ng da, RL tiu hom au
e
bg, au d dy
th vng
Tolperison
Cc bnh l chn thng Nhc c, nhc u, h HA<
TK, fc hi c/n
bun nn, au bg, p qu mn
Eperison
RL chc nng gan, thn, cthc

mu, pht ban, triu chng tm

thn kinh, RLTH
THUC LIT HCH
i khng vi AChti rct NN: (c ch rct N)
- Amin bc 4: Hexamethonium, Pentholinium
- Amin bc 3:Pempidin, Trimethaphan
- Amin bc 2:Mecamylamin
C quan
H u th
Tc dng lit hch
Tiu M
GC
Gin mch, h HA
TM
GC
Gin mch, tr tr tun hon
Tim
GC
Nhp tim nhanh
Mng mt
GC
Gin con ngi
C mi
GC
Gim knng iu tit
H tiu ha
GC
Gim trng lc, nhu ng
Bng quang
GC
Gim tiu tin
Tuyn nc bt, nc mt
GC
Gim tit
a) Tc dng dc l:
- Tim mch: tim nhanh, h HA t th
- Lu lng mu: gim ni tng & tng vng chi
b) Dc ng hc:
- Amin bc 4: kh hthu, c th gy c (try tim)
- Amin bc 3: d hthu (hthu thuc dg ko ply), nhg c th gy lit rut
c) S dng tr liu: Ksot HA
d) c tnh:
- Nh: RL th gic, kh mig, kh tiu, mt ngon, nn ma
- Nng: h HA, lit rut, lit g t, RL TKTW

THUC M
1) nh ngha: l thuc c t/dng
c ch tt c cc m c tnh kthch (TKTW, c tim, c trn, c vn), lm mt
thc, mt px, mt mi cgic (au, ng, lnh), gin c, phc hi hton liu tr
lieu, t gay xo trn tun hon, h hp (thuc m an ton ko c t/c ny)
2) Cc gon gy m:
G 1 (khi m): (thuc m mt thc). Mt cgic au. c ch ton b v no
ni xft cc dy TK
G 2 (kthch ch yu trn TKTW): (mt thc kthch, m sng). H hp, nhp
tim ko n nh, vg mt ksot, nn ma, gin ng t. Cc dy TK b chi fi bi
hthng li (ksot mi px co git, tg tit sd atropine c ch). G ny qua
nhanh nn ko fu thut s gy nguy him
G 3 (phu thut): (c ch TKTW, ngoi tr hnh ty). Ht kthch, mt px, g t
bth, h hp ha, mt px mi mt, gin c. c ch no c ch hthg li
G 4 (lit hnh ty): (c ch hnh ty, r no). Ngng h hp, suy tun hon t
vog
3) Cc nh hng chnh ca thuc m:
Tai bin v h hp: tng tit dch h hp gy ngt th, ngt do ngg h hp
Tai bin v tim mch: ngt do ngng tim, sc do thuc m, fu thut
Tai bin sau khi gy m: vim fi,f qun,suy tim do gy m ko di,suy gan, thn
SD atropine hn ch cc tai bin.
4) Cc nh hng hu phu: (tai bin)
Tng HA (do c ch tim mch), nhanh nhp tim: khi fc h GC
Thiu mu c tim bnh nhn b bnh mch vnh (do lc fu thut tim ko hg
nh bth suy tim)
Tr.thi kthch (5-30%): nhanh nhp tim, bn chn, khc, rn r
Run (Meperidine hay clonidine CGC 2 hu qu gy lit GC do au)
Gim c/n fi
Ksot cn au: opiod c ch hh
Ketorolac (IV), NSAID (IV) (BN fu thut xg sd thuc gim au c t/d c ch hh)
5) Tiu chun ca 1 thuc m tt:
Khi pht nhanh, m du
Gin c thch hp ko nh hng bi hh, tun hon
Ko c, t gy TDP
K/c an ton rng d chnh liu
Phn loi:
Thuc m ng tnh mch
Thuc m ng h hp
Barbiturat: Thiopental, Methohexital,
Loi halogen ha: Halothan, Isofuran,
Thiamylal
Enfluran, Desfluran, Sevofluran, Cloroform
Thuc khc: Ketamin, Propofol, Ketomidat Thuc khc: Cyclopropan, Ether m,
Nitrous oxid, Xenon
6) C ch:
Vtr tc ng: ngn chn dn tr` v no, r no, ct sg, TK cgic ngoi bin

C ch TB: lm ti tnh thm MTB vs Na+(ngn ko cho Na vo trog mng) ngn

chn s kh cc
C ch phn t: tng tnh nhy cm of GABA ln GABAA receptor tg dn tr` c
ch & gim hng TK m knh ClA- Thuc m ng tim:
Hcht thm, d vg, TLPT thp, k nc
Tnh ko a nc pb cao trog m cha nh` lipid (vo no nhanh) + mc
ti mu > (no, ct sg)
N trog mu ngoi bin gim nhanh (khi ft nhanh) Ti pb t TKTW
mu c, tg, m m
Thiopental c sd lu i, an ton; Propofol hi fc rt nhanh; Etomidat dg cho BN
c nguy c h HA, thiu mu c tim (ko nh hng n cug lg tim); Ketamin thch
hp nht cho BN hen (gn trn f qun gy gin f qun), tr em cc ch nh fu
thun ngn, qtrnh gy au

a) Cc barbiturat: Sodium Thiopental (Bdc Pentothal), Thiamylal, Methohexital

- u im: khi m & hi fc nhanh, em du, t gy nn ma
-Nhc im: Ho, co tht f qun, thanh qun, gy fg thch Histamin sd
atropine or scopolamine trc gy m, c ch hh, h HA (gim t.tch TH, nhim
trg`), gim au km, gin c km
Gy kt tun cc thuc gin c, thuc tin m.
THIOPENTAL(Bdc Pentothal):
- Liu: ng ln 3 5 mg/kg, tr < 2t: 5 8 mg/kg, ph n c thai, gi: 1 3
mg/kg (ko qu 250mg), gim 10 50% khi sd BZD, opioid, tin m.
-Ch nh: pthut nh, khi m cho cc thuc m hh
-Chg ch nh: bnh porphyrin, thuc qua g` nhau thaithn trg
b) Thuc khc:
PROPOFOL (bd: DIPRIVAN)
- L thuc m f bin nht M
- Nh tng trong du d b nhim khun dng ngay
- u im: khi m & hi fc nhanh xut vin nhanh, chg nn thch
hp trog bun nn, nn ma; an ton cho PNCT, tr s sinh
- Nhc im: c th gy ngg th, suy h hp, h HA, tg nhp tim, fng
thch Histamin, sc fn v (t l rt thp nhg xy ra rt kh x l)
- Ch nh: pthut ngn, pthut di dg liu duy tr, an thn trog csc bit
- Thn trg: ng kinh, RLCH lipid, sn khoa.
ETOMIDAT: (bd: HIPNOMIDATE) thuc khg acid
- u im: khi m nhanh, t a?h? n nhp tim, HA & cug lg tim rt
thch hp cho i tng c nguy c b h HA; ko gy kta khi fi hp vs cc
thuc tin m
-Nhc: ko c t.d gim au, c th gy co git fi hp BZD ko dg duy
tr m,gy au ni chch,c ch tuyn TT RL in gii,h HA,tiu niu
-cn fi hp thm Opioid hay BZD chg co git
KETAMIN (Bd: Ketalar)
- u im: khi m nhanh, thch hp cho i tng c nguy c h HA, co
tht f qun, COPD, nhi; BN cao tui: shock tim, shock nhim khun

-Nhc: gy mt nh hng, o gic, c mng hu fu sd thm thuc

tin m atropine, diazepam; tg p lc ni s CC: tg p lc ni s u
trog no hay xut huyt no, chn thg vg u, thiu mu no
-chng C: tg HA, tin s t qu, RL tm thn
B- Thuc m g` h hp:
Khong an ton hp (LD50/ED50) = 2 4 (liu gy c/liu gy m)
TDP cao
c tnh dc ng:
N kh m/hn hp kh th t l p sut rig fn;
Khi gy m: kh f nag mu no;
H s pb mu/kh (tnh tan/mu):
N2O: t tan/mu nhah chg tg p sut rig fn/M CBg nhanh
vs no khi ft nhanh gy m nhanh
Halothan: tan/mu ttchm tg p sut rig fn/M khi ft chm
HALOTHAN (FLUOTHAN)
- 1 fn halothan antibody hoi t gan bc ft
- TDP:
Tim mch: h HA M, gin mch mu da, no, chm nhp xoag nh
H hp: t ft nhah &ng, gim thg kh f nag
Thn inh: tg p lc ni s
Thn gan: tiu niu, vim gan
ISOFLURANE:
- Ko p vs CO2 dtr tt
- TDP: Gn ging halothan
ENFLURANE, DESFLURANE
THUC T
1) N: l thuc c tc dng: c ch ngn dy TK cgic lm mt cgic tm thi khi
txc, ko nh hng n thc, ko nh hng n cc hg khc
2) Cc ngtc gy t:
Gy t b mt: xt, nh, bi da, nim mc
Gy t xuyn thm: tim m c tn cg TK cgic
Gy t dn tr`: tim gn dy TK mt cgic vg c nhnh TK lan ta
Gy t mng cng: tim ngoi mg cg mt cgic kv di ni tim
Gy t ty sng: tim vo ty sng
3) Cu trc ha hc tg qut:
- Nhn thm (thn du)
- Ni amid hay ester
- Chui trug gian (HC)
- Nhm amin (thn nc
Mt acid dg ion ha cng cao tan trog nc kh thm vo TBTK
gim hiu lc thuc
L cc base yu dg ko ion ha tan trog lipid d thm vo TB TK
hthu thuc tt

4) C ch tc ng:
- Thuc t fong b knh Na+ trn MTB TK i vo trog mng
5) Phn loi nhm thuc t:
- Nhm amid: Lidocain, Bupivacain, Mepivacain, Ropivacain, Levo Bupivacain,
Prilocain, Etidocain.
- Nhm ester: Cocain (ko sd), Tetracain, Procain, Benzocain, Chloroprocain
Chuyn ha, p qu mn, chch cng gn vtr dy TK ch cng tt, ko tim
tr.tip vo dy TK gy tn thg dy TK.
6) Tc g dc l:
Trn TKTW:
Gim dn tr` TK
Gim tg s lng dy TK b kthch
Gim lng Na+, Ca2+ vo MTB TK c ch dn tr`
Qua HRMN.
N thp: tg ngng co git/chg co git
N cao: gy co git
N rt cao: c ch TKTW, hn m
Liu cao c ch c h TK c ch ln h TK kthch c ch TKW & ngng h hp
Trn TK ngoi bin:
c ch hot tnh TK ngoi bin
Lidocain c ch px ho
Liu c gy c ch TK c
COCAIN: gy t b mt rt mnh
PROCAIN (NOVOCAIN) :
Gy t mnh, ngn
Ko gy t b mt
Thy fn thnh PABA (Para amino benzoid acid) c ch sulfamid c cht
tg hp ADN of VK
LIDOCAIN:
Hiu lc gy t mnh
Dng tim, dng ngoi da, dng dn ngoi da
Tgian gy t ko di nhg hiu lc, c gy t vn gi nguyn
c tnh: tai, hoa mt, chg mt, liu cao gy g kinh, hn m,ngg hh
BUPIVACAIN LEVOBUPIVACAIN (gy t ngoi mng cng)
Gim au hu fu hoc Gy t trog sinh
TETRACAIN:
- Tc ng di gy t ty sng
Cc thuc ng tim chch khc : ARTICAIN, ROPIVACAIN, PRILOCAIN
(hiu lc tt, gy m ngoi mg cng) yu hn Procain
Thuc t sd gy t b mt:
Kch ng mt
Gim nga hu mn, bfn sdc

 PARAMOXIN: PARAMOCAIN : dng kem, lotion, xt, gel

QUINISOCAIN: dng kem, lotion, xt, gel
BENZOCAIN: gy t b mt tt
Thuc t sd gy t trong nhn khoa:
PROPARACAIN 0,5% & TETRACAIN 0,5%
Bt buc: t gy kch ng mt, t gy d ng ktra px mi mt
Nh tng git 1 hiu qu gy t
Sd lu chm lnh, r, trc TB biu m gic mc
THUC NG
NG: l tnh trg v thc, no p ng kthch ni ti >ngoi ti, c ck, c hi fc
Do cc k hon cnh, tm l, bnh l hay thuc m mt ng.
1) Sinh l gic ng:
Non REM
G 1 (m mg): nhanh
G 2 (v thc): nhanh nhg bin cao hn, chim 20% gic ng
G 3 (ng su) + G 4 (ng rt su): gic ng delta: ti to TB, c th tr em
ptrin. Su: tnh to, nng: mt
REM: ging G1, mu dn v no nhiu hn, cc c bp ko c g c.
Gic ng ngon: tri qua 4 ck mi m
Sng : lc ngh ngi, : tr.thi hg, : m mng, : ng su
2) Thuc ng:
Mt ng :
- u gic: kh bu gic ng
- Gia gic: kh duy tr gic ng
- Cui gic: thc gic sm
Mt ng thag qua: mt, tm l
Mt ng mn tnh ( >3tun): stress, bnh tt, tm l
3) Mc tiu tr mt ng: gip d ng, dtr gic ng, sg khoi khi thc
4) Hn ch sd thuc ng (<2-3 tun)
5) tr mt ng ko dg thuc: to mt thch hp,thi quen ng thc g h,luyn tp
6) Cc nhm thuc ng
A) Benzodiazepin:
TD ngn (<6h)
TD TB (6 24h)
TD di (>24h)
- Triazolam
- Estazolam, Temazepam,
Flurazepam, Quazepam,
Lorazepam, Alprazolam,
Diazepam, Clorazepam,
Nitrazepam
Chlordiazepoxid,
Clonazepam
Mt ng u gic
Duy tr gic ng
Mt ng cui gic, gii lo u
(ban ngy)
a) C ch tc dg:
GABA: cht c ch TK, tfn bo dtr hg bth of no b, gim bt s hg noron
- BZD gn vo GABA tg hot tnh of GABA trn rct GABAA tg dn Cl- Khg trc tip m knh Cl-

- Flumazenil: cht i khg c hiu

- c ch: Vg di i, hi hi m, nhn en, v no, v tiu no, ct sg.
b) Tc dng dc l:
- Gii lo u, an thn, gy ng,gin c,chg co git, c ch h hp,tim mch
- Trn gic ng: rt ngn tgian khi ft ng, gim s ln thc gic, gim G
1,3,4; tng G 2, rt ngn tgian REM nhg tg s ck REM, tg tg tgian ng
c) Dung np: p ng/lp li liu. C th do chuyn ha, BZD rct
d) L thuc: Hi chg cai thuc (lo u, mt ng, kthch)
e) Ch nh lm sg:
Gii lo u, chng s ch g ng, mt ng, an thn trc/trog cc qtrnh y hc/pthut,
tr co git, g kinh, thfn trog gy m IV, ksot hi chg cai ru, thuc ng, gin
c (RL TK-c), chn on
f) S dng lm sng:
- Diazepam (Valium),Clorazepat (Tranxene): tr ng kinh
- Clodiazepoxid (Librium): Cai ru
- Clonazepam (Klonopin): ng kinh, thao cung.
g) c tnh, tc dng bt li:
Cc tg ko mong mun:
Cmax: nhc u, u oi, gim fi hp vg, tinh thn
Gy chng quyn thun chiu
Trnh ng hay li xe, vn hnh my
Cc tc g i nghch:
Flurazepam: c mng/tun u
BZP (benzodiazepam): ni nh`, bn chn, mt ng, o gic, hoag tng
Cc tg bt li: Flurazepam, Triazolam c tnh trn gan, huyt hc
B) Nhm Barbiturate:
TD rt ngn
TD TB
TD di
Thiopental, Methohexital Amobarbital, Secobarbital, Phenobarbital,
Pentobarbital, Butabarbital Mephobarbital
Khi m, dtr m
Mt ng, tin m, g kinh ng kinh, an thn/ban ngy
C) 1 s thuc ng khc
Thuc
c tnh
Ch nh
Zolpidem, Zaleplon Tg t BZD, t gy l thuc v
Mt ng u gic
(Nhm thuc Z)
suy h hp
Busipron
Serotonin rct agonist
Gii lo u, ko an thn, ng
Diphenhydramin
Thuc khg Histamin H1
Gy ng nh
Melatonin (tit nh` Hormon tuyn tng, ha chu k
Ri lon chu k gic ng
gic ng
ko tnh to)
Mt ng u gic
Melatonin MT1,2 rct agonist
Ramelteol
(agonist)
THUC GIM AU

Thuc tr: thuc gim au loi opioid, thuc gim au hng TK, thuc gim au loi
NSAID, Paracetamol, thuc gy t ti ch.
1) au: l cgic kh chu v kinh nghim cxc i km vs tn thg m thc s hay tim
tg c cng t v
2) C ch dn truyn cgic au:
Dn truyn qua 3 G:
Cm nhn cgic au qua cc rct nhn cm au (nociceptor) - G ngoi bin
Chuyn thg tin v cgic au ngoi bin n ct sg fng thch glutamate
Chuyn t.tin cgic au ct sng n i th, v no
3) C ch hot ha, tng cm au qua NOCICEPTOR
Kthch: c hc, nhit , ha hc
Tn thg lp PL kp PL phospholipase A a.arachidonic COX PGE2,I2
gn ln nociceptor tng cm A
Cht ni sinh trg cth:Bradykinin, histamine, PG, serotonin, ATP, acid lactic, K +
kthch C hay A
Dy TK dn truyn:
A: to, bao bc = myelin, nhanh (15m/s), au but, nh r v tr
C: nh, ko myelin, chm (1m/s), au m , kh nh r v tr
4) C ch dn truyn au r lng CT SNG
Rct do acid, tn thg, nhit truyn cgic au v ct sng gn ln cc
nociceptor fg thch glutamate gn ln NMDA, AMPA (rct of glutamate)
Clonidin gn ln 2 rct c ch fng thch glutamate gim au.
5) Cc nhm thuc gim au
A- Thuc gim au loi OPIOID:(thuc gim au gy ng)
Opioid: bt c cht no c tng tng t morphin
Opium: nha thuc phin, trch t cy thuc phin
Opiate: morphin, c trog nha thuc phin, chit xut t opium
a) Phn loi:
- Ngun gc tnhin: morphin, heroin, codein, nalorphin, levallorphan
-Tg hp ko lquan ctrc vs morphin: phenylpiperidin, methadone,
benzomorphan, thebain
-Opiod ni sinh: -Endorphin, Leu-enkephalin, met-enkephalin, Dynorphin
- Thuc khg morphin: nalorphin, naloxone, naltrexone.
b) Opioid receptor: MOPr, DOPr, KOPr, NOPr
: RCT chnh, chu tc cc p ng ca morphin & opioid
-Endorphin, Leu-enkephalin, Met-enkephalin: gn nh` trn &,gn t trn
Dynorphin: gn nh` trn ,gn t trn &
Orphanin FQ/nociception : gn trn NOPr
c) C ch tc ng ca Opioid r lng CT SNG
Morphin gn vo cc rct ,, c ch Ca2+ i vo ko fg thch dc
glutamate gim au (rt mnh)
Trn ct sng cn c rct c ch cgic au.
- c ch AC

- Tng m knh K+
- Gim m knh Ca2+
c ch dn truyn cm gic au
d) Tc ng dc l:
Tc ng gim au: ( & )c hiu, ko gy mt thc, ko xo trn cgim
khc.
SD trong : au cp, mn tnh, hiu qu yu trn au TK
Tc ng gy sng kha: () khoan khoi, ph du thot tc
Suy h hp: ( & ) c ch t.tm hh r no, gim /ng vs CO2 thiu ht O2
c ch ho: c ch t.tm ho hnh no
Gy bun nn & nn ma
Co tht ng t
Gim nhu ng d dy rut tr tiu chy
Gy dung np & l thuc thuc: sau 2- 3 tun
Ngng dg thuc hi chg cai thuc
Tng thn nhit, gin g t, i ma, tiu chy, ri lon h hp t vog
e) S dg lm sng:
Gim au
Ph phi cp: morphin
au tht ngc nng km ph fi cp: morphin
Ho: Codein, dextromethorphan
Tiu chy: Loperamid
Lnh run: Meperidine (thuc m)
Gy m: Fentanyl
f) c tnh ca 1 s opiate opioid chnh:
Morphin: T1/2 = 3 4h
Hydromorphin: gim au = 10 ln morphin
Bupremorphin: duy tr nghin. T1/2 ~ 12h, khi ft chm. Mnh = 20 ln morphin
Methadon: duy tr nghin. T1/2 ~ 24h
Pethidin: au cp (si, sn khoa)
Sufentanil, Fentanyl: thuc dng dn da q 3d ( 3 ngy thay 1 ln)
Thuc gim au bc 2 (t gy nghin):
Dextropropoxyphen, Nalbuphin, Pentazocin, Tramadol, Codein
1 s thuc khc:
Ketamin (NMDA rct antagonist): thuc m gim au tt
Ziconotid (chn knh Ca2+ )
Boltulinum toxin: botox
g) Chg ch nh thn trng:
S dng 1 thuc i khng ton fn v 1 thuc i khng 1 fn:
Morphin + Pentazocin gim t/d gim au, gy h/c ngg thuc
Bnh nhn tn thg vg u: CO2 tch ly do suy hh gin mch no
Ph n c thai: l thuc thuc trc sinh, hi chng ngng thuc sau sinh
Suy gim cn fi: suy hh cp
BN suy gan, thn: gim liu thch hp
BN mc bnh ni tit: Addison suy gip (Thiu glucocorticoid): t/d opioid tg
h) 1 s thuc i khng vs opioid:

Naloxon, Naltrexon, Nalorphin, Pentazocin, Nalbuphin

- tr cc triu chng ng c cp, qu liu opioid
- Cp cu, chn on nghin
B- Thuc gim au hng tm thn :
a) Ch nh: bnh TK do i tho ng, au sau zona, au u, RL tm l
b) SD: tr liu c /ng sau 2- 4 tun, duy tr 4-6 thg cho n khi ht triu chng
Amitryptylin, Fluoxetin, Mirtazapin, Sertraline
C- Thuc gim au, h st, khng vim NHM NSAIDs:
a) n: hiu lc gim au nh - TB, gim st, khg vim
b) P vim: /ng t v of cth /v tc nhn gy bnh. C tnh bv qu mc
s gy c hi. Gy gin mch, tg tnh thm, tch t bcu. gii fg cc cht
trug gian: PG, Histamin, Leucotrien, PAF, Bradykinin, Cytokin...
Leucotrien B4 gy hen nhng c t/d chg li virus gy bnh
c) P au trong vim
d) St: cn st khi ft bi cc yu t sinh nhit ngoi lai trn cth bcu tit
yu t sinh nhit ni sinh (IL-1) ln i th tg tg hp PG
e) Cc thuc NSAIDs:
Dxut ca acid salicylic
- Acid acetylsalicylic (Aspirin)
Tc ng dc l: gim cn au nh, TB. Gim thn nhit khi st. C tg
khg vim. Ngn s kt tp tiu cu chg g mu.
c tnh: kch ng tiu ha, gy xut huyt d dy, hi chng salicylat tai,
hoa mt, bun nn, nn ma. hi chng Reye( RL c/n gan +bnh no) xy
ra tr em. RLCB huyt hc, a-b, in gii, suy hh
CC: lot d dy, t trg. Cc bnh xut huyt. ph n c thai 3 thg cui
Thn trg: lm tg tg wafarin (cht chg g mu)
- Acid salicylic: dung ngoi ko kch ng da mnh
- Salicylat Na: tg gim dau, h st yu hn aspirin
- Salicylat methyl: ch dg ngoi (salonpas)
Dn cht ca a. propionic:
- Naproxen: khng vim mnh, gim au, h st
- Ibuprofen: sd trog au bg kinh, thuc chn la u tin trog tr vim khp
- Ketoprofen: gel bi, dug np tt
Dn cht of acid acetic:
Diclofenac c ch COX rt mnh hqu khg vim cao. TDP: nhc u,
chg mt, kch g, RL g` tieu ha
Dn cht fenamat
Dn cht oxicam:
Piroxicam, Tenoxicam: vn c ch COX-1
Meloxicam: c ch COX mnh hiu qu khng vim cao. c ch chn
lc COX-2t TDP, ko kch g d dy, ni mn. Liu cao vn c ch COX-1.
Cc Coxib:
- Rofecoxib, Valdecoxib b cm sd
- Etoricoxib,

- Parecoxib tim vo khp

- Celecoxib c ch chuyn bit COX-2 t gy lot d dy t trg
- CC: suy thn, suy gan, suy tim. Tng HA
D- Nhm thuc gim dau:
Dxut aniline:
Paracetamol
- C ch: c ch COX-1, 2 yu
- c tnh: ko gy kch ng d dy,him gp Met-Hb, liu cao gy hoi t TB gan
Acetanilid: tin cht paracetamol. c tnh cao, Met-Hb
THUC TR NG KINH
ng kinh: Cn cc b (cn ton th ha th pht),Cn ton th ha (kinh th >, <)
1) Thuc tr ng kinh:
- Chn knh Na+: Valproate, Phenytoin
- Chn knh Ca2+: Ethosuximid
Gim th hot ng.
- Barbiturat: Phenobarbital
- Benzodiazepin: Clonazepam, diazepam, lorazepam
- GABA-like agent: Gabapentin
Tng hot tnh GABA
2) c tnh ca cc thuc tr g kinh:
- Carbamazepin, Phenytoin: (Na+ ) cc cn g kinh ngoi tr cn nh
- Valproat (Na+, Ca2+, c ch GABA-T): hu ht cc cn kinh
- Ethosuximid (Ca2+): cn nh, c th lm nng them cn ln
- Phenobarbital (GABAA): cc cn kinh ngoi tr kinh cn nh
- BZD (GABAA): hu ht cc cn kinh. Lorazepam IV: kinh cn ln ltc
- Gabapentin, Pregabalin (Ca2+): ng kinh nng
3) Chng ch nh:
- Topiramat, Lamotrigin, Gabapentin, Pregabalin: mn cm
- Phenytoin: chm nhp xoang, nghn nh tht
- Carbamazepin: bnh gan, suy ty, nghn nh tht, iMAO
- Barbiturat: RL chuyn ha porphyrin
- Valproat: suy gan, c thai
THUC TR LON THN (TM THN PHN LIT)
Thuc tr tm thn fn lit. tr.thi thao cug, hoag tng, RL hnh vi, cm xc
1) C ch c bn:
- Dopamin rct antagonist
- 5 HT (Serotonin) rct antagonist
- Muscarin antagonist
2) C ch bnh sinh (Gthit v Dopamin):
- Khi ft sm (20t) mt tr sm
- Mi trng + di truyn
- Cn lon thn: tng hot tnh h dopaminergic qua rct D2
- Lon ngn ng: bin dng no tht

3) Triu chg kthch:

o tng (hoag tng), o gic (kch g), RL suy ngh (c tn, v l), hnh vi bt
thng (mt nh hng, gy hn), cng trng lc, RL tm l
4) Triu chng c ch:
Cch ly vs mt, xh, tr v mt cxc, mt khoi cm
5) Thuc tr lon thn: Dopamin D2 antagonist:
- Nhm c in (th h 1): Chlorpromazin, Haloperidol, Fluphenazin, Flupenxitol,
Clopenxitol. Nhiu TDP
- Nhm mi (th h 2): Clozapin, Risperidon, Sertidol, Quetiapin. t TDP > nhm1
- T/dg di (Depot-lu tr): Flupentixol, Haloperidol, Fluphenazin, Risperidon,
Aripiprazol, Ziprasidon . Dd tim trog du, tg tg gn 3 thng BN thao cug
Bi 1:
Ca2+& Mg2+ rt qtrng /v c th, chng i lp vs nhau
- Ca2+ td kthch gfng cht TGTK
- Ca2+ vo TB c ch tg c ch of troponin trn tg tc actin & myosin gy co c
MgSO4: cnhtranh vi Ca, c th c ch fng thch cht TGTK xynap TK c
- Ch nh: h Mg2+ huyt, dng trog THp nui qua ng thng.
- Ch nh ko chnh thng: tr tin sn git
CaCl2:
gii phng cht dn truyn thn kinh, co c, bo ton mng v lm ng mu.
kch ng ng tiu ha v gy hoi t m, do vy khng bao gi c tim vo cc m
hoc bp tht.
- Ch nh: Co git do h calci huyt tr s sinh, co tht thanh qun do h calci
huyt, thiu nng cn gip trng,do thiu vitamin D, nhim kim. Sau truyn mu
khi lng ln cha calci citrat gy gim Ca++ mu.Trng hp tng Mg huyt,
calci clorid cng c s dng nhm mc ch iu tr cc tc ng gy c ch
h TKTW khi dng qu liu MgSO4.Qu liu do thuc chn calci, ng c do
ethylen glycol.
- Chng ch nh:Rung tht trong hi sc tim; tng calci mu,qu liu do vitamin D;
si thn v suy thn nng;
- Tc dng khng mong mun (ADR): Thng gp:Tun hon: H huyt p
(chng mt), gin mch ngoi vi. Tiu ha: To bn, y hi, bun nn, nn. Da:
da, au hoc rt bng ni tim. t gp:Thn kinh: V m hi. Tun hon:
Lon nhp, RL chc nng tim cp. Him gp: Mu: Huyt khi.
Bi 2:
- Clopromazin (thuc tr RL tm thn): c ch dopamine, rct histamine H1
Ch nh: tr lon thn ko thuc dg trm cm, tt c cc th tm thn fn lit,
G hng cm ca ri lon lng cc.Bun nn, nn.An thn trc fu thut.
Chng ch nh Ngi bnh ng c cc barbiturat, cc opiat v ru. Ngi
bnh c tin s gim bch cu ht, ri lon mu, nhc c.
TDP: Mt mi, chng mt, h huyt p, nhp tim nhanh,hi chng Parkinson, RL
ngoi thp, RL kinh nguyt,Chng v to n ng, tng tit sa,kh ming
- Phenobarbital:Loi thuc: Chng co git v an thn, gy ng.
Tng cng c ch fng xung TK
Tng hot tnh c ch TK ca GABA.
Phenobarbital c ch h TKTW mi mc , t an thn n gy m.

Ch nh : ng kinh, Phng co git,fg tg bilirubin huyt, Vng da s sinh

Phenobarbital c knag cm ng men gan tg chuyn ha men gan tg
bilirubin tr vg da
Chng ch nh: suy h hp nng, suy gan nng
Thn trng: Ngi bnh c tin s nghin ma ty, nghin ru. suy thn, cao
tui. Khng c ngng thuc t ngt ngi bnh mc ng kinh. Dng lu
ngyl thuc thuc. B trm cm, pn c thai(do thuc bi tit qua sa)
TDP: bun ng,Ni mn do d ng, hcu to trog mu ngoi vi, ci xg, au khp
Tng tc thuc:Phenobarbital c th lm mt td of thuc trnh thai theo PO,
khi c dng ng thi, do lm tng chuyn ha gan.
Phenobarbital v cc thuc trm cm khc, thuc khng H1, BZD, clonidin, dxut
ca morphin, cc thuc an thn, thuc gii lo...: lm tng td c ch h TKTW.
- Cafein : kthch TKTW, h hp, tim mch, li tiu. hn ch dg cho tr em <12t
Tng hot nng tr tu, gim cgic mt mi, bn ng. liu cao: kthch, lo lg, mt
ng. liu cao hn: co git. tr chng ngt th tr so sinh, suy hh bi morphin
Tng nhp tim, sc co bp c tim, lu lng tim, tiu th oxy tg
Gin c trn, co c vn, tng tit acid & pepsin dch v
Li tiu: tng lu lng mu thn, tg s lc qun cu thn, gim THT Na +
C ch:fng thch Ca2+ ni bo hoc c ch men phosphodiesterase tg
AMPvtg glu mu, tg p/hy lipid, gin c trn, tg co bp tim
Bi 3:
Barbiturat: chng co git, gy m ngn hn
Lm thun li v ko di tc ng c ch ca GABA v glycin Barbiturat khng gn vo
receptor BZD hay receptor GABA. Lm tng thi gian m knh Cl- qua trung gian GABA.
- Qu liu: c ch hh, gy hn m
- TDP: gy quen thuc, nhim c barbiturate, ko c cht i khg c hiu
BZD: tr lo u, co git, mt ng
- tr mt ng: gim tgian khi ft gic ng, ko di, tgian ng fa Non-REM (mc 2
gin c, no b ngh ngi), gim tgian fa REM, tg tg tgian ng hn 30-60
- tr co git: tgian bn thi hi di: lorazepam, diazepam
- C ch: BZD gn vo GABA trn GABAA rct tg tnh dn Cl- tg tn s m
knh Cl-. BZD ko trc tip lm m knh Cl- Thn trng: tr em, ng gi <75t, ng b chng ngg th khi ng, ngy nh` ngy to
- TDP: mt mi, bun ng, gim ha hg (nn dg liu thp), hin tng quen
thuc BZD (SD 3-4 tun ltc) ngng thuc gy kh ng, lo u tr li. nu
ngng t ngt s gy au u, bc rc nn ngg t t
Nhm thuc Z (Non BZD):chn lc hn, t gy quen thuc hn, ch c t/d gy ng, ko
cn t.d gin c, ko chng co git
- Thuc t.ng cc ngn (T1/2<1h): Zaleplon
- Thuc tg ngn (<6h): Triazolam, Zolpidem, Eszopiclon
- TB (6-24h): Estazolam, Temazepam
- Di (>24h): Diazepam, Quazepam, Flurazepam
- Chng co git: Nitrazepam, Lorazepam, Diazepam
- Gin c: Clonazepam

Cht ch vn Metalonyl (Ramelteon): thuc an thn cho ph n mang thai, gy gim

tgian khi ft gic ng, rt t gy t/d ri lon hg, tg tit Prolactin
Barbiturate
Benzodiazepin
- Khng c tnh chn lc
- C tnh chn lc
- Ko c cht i khng
- C cht i khng gii c: flumazenil
& nhm thuc Z
- /v cht gy ng l GABA, c t/d gy
- /v cht gy ng l GABA, ch c t/d l
ng
h tr
- T m knh Cl .
- Ko tr.tip m knh Cl- Qu liu barbiturate vn ng dc
- Qu liu BZD ko ng c
- Tng tgian m knh
- Tng s ln m knh
Niketamid: kthch mnh TK, tuy nhin yu & ko chuyn bit
- Kthch trung khu hh & vn mch hnh no. Tng bin & nhp hh, tg nhp & sc co
bp tim
- Liu c: kthch TKTW co git
- Sd tr liu: Suy hh cp, ngt th tr s sinh, sc v nhim c
Bi 4:
HTKTV: bo ~ c/n sng cn of CT thn nhit, h 2, t/hon, tiu ha & ha 1 cch t g
Si tin hch tit ACh, Si hu hch tit NE
Tuyn thng thn : hch GC ln, ch c si tin hch. tit Catecholamine
- HGC:khi kthch 1 hch tr.tm khuch i ln nh` CQ /ng tnh hug cp bch
- HGC: hg, tiu ha, ngh ngi cxc, hiu qu
Insulin m knh dn glu vo TB. Thiu insulin: ko m knh glu cn trog mu.
- Cht ch vn: chia lm 3 nhm
Nhm tc ng trc tip: chia lm 2 loi
C chn lc: phenylephrine (1 co mch), Clonidin (1 co mch h HA)
, Dobutamin (1 c th tg co bp tim), Terbutalin (2 c th co f qun)
Ko chn lc: Oxymetazolin (1,2 ), Isoprenalin (1, 2)
Nhm tc ng gin tip: fng thch 1 cht dn truyn t khe xynap ln th th
tm thi c th chuyn ha = MAO, COMT hoc ti hp thu. Phn loi
Tng phng thch CTGTK ra ngoi xynap: Amphetamin
c ch THT: Cocain
c ch enzyme MAO: Selegiline
c ch enzyme COMT: Entacapone
Nhm tc ng hn hp
- Cht i vn:
i vn : chn ko chn lc, chn chn lc 1, 2
i vn : th h 1,2 ,3
Cc thuc sd trog tim mch
- Nhm thuc kthch 2: Clonidine, methyldopa, guanabenz, guanfacin
SD tr liu: cao HA
TDP: bun ng, kh ming, mt tp trug
Clonidine: ngng thuc t ngt p hi ng tg HA t ngt

c ch no b gim sinh GC; c ch cc cht GC fng thch

Methyldopa: tng HA pn c thai
Kthch 2, co mch tng HA
- Nhm thuc chn 1: Prazosin, Terazosin, Doxazosin
SD tr lieu: ph i tuyn tin lit lnh tnh
TDP: nhc u, mt mi, h HA t th
Chn 1 gin mch, gin c trn gin g` tiu ra thg thag tr tiu
lc nhc
- Nhm thuc chn :
Th h 1 - chn ko chn lc: Propanolol, Naldolol, Penbutolol
Th h 2 chn chn lc 1: Atenolol, Bisopralol, Esmolol
Th h 3 chn chn lc hoc ko chn lc + hot tnh ni ti
SD tr liu: tng HA,au tht ngc, lon nhp tim
au tht ngc do c tim b thiu NL (hp mch vnh) ch? qua sd cht khc
tg a.lactic trog tim, cht gy c khc c tim thiu O2 au
Gim co bp, gim nhp tim, gim nhu cu NL of tim au tht ngc
TDP:
Lm nng suy tim, nhi mu c tim cp, ph i tim.
Chm nhp tim v gy block nh tht
Lnh u chi (Raynaud)
C knng co tht f qun (do c ch 2 lin tc b ng hen suyn)
Che giu h glu/mu
Chng C: hen suyn, nghn dn tr`, suy tim r rt
Cc thuc tr hen suyn:
- SABA (cht ch bn 2 tng ngn): Salbutamol, Terbutalin, Fenoterol.
- LABA (cht ch bn 2 tng di): Salmeterol, Formoterol.
Salbutamol (SD trog hen, d fng sinh non (gin c, ko gy co tht))
- TDP: ch yu trn tim mch
Tng nhp tim
Run: hay gp nn bt u = liu thp
Cc tdp ny gim ng k /v thuc dng kh dung
Trn c tim cn 2 gy co mach, tng nhp tim
Thuc c tnh chn lc tng i: tng nhp tim
Hen suyn chn th h 3: c t/d f duy nht l gy co tht c trn ph qun
Adrenalin (Epinephrin):thuc tdng tr.tip ging GC, kthch c th th v , nhng ln
th th mnh hn th th .
Ch nh: Hi sc tim phi. Cp cu chong phn v v Sc phn v (c gin mch h
thng v cung lng tim thp). Cn hen c tnh (phi hp vi cc thuc khc nh
glucocorticoid, salbutamol). Glcm gc m tin pht.
Bi 5:

Thuc ktn mnh hn qua knh

Acid yu: pH = pKa + logA-/HA
Diclofenac:
Huyt tng: logA-/HA= pH pKa = 7,4 4,15 = 3,25 A-/HA= 1778,3
D dy: logA-/HA= pH pKa = 1,4 4,15 = -2,75 A-/HA=1,8/1000
D dy c dg pt nh` hn d hthu hn
Thuc dg pt ktn t d dy huyt tng (gn nh 1 chiu)
Base yu: pH = pKa + logB/BH+
Strychnin:cht c, chit xut t ht cy m tin
Huyt tng: logB/BH+ = pH pKa = 7,4 8,25 = -0,85 B/BH+ = 7/50
D dy: logB/BH+ = pH pKa = 1,4 8,25 = -6,85 B/BH+= 7/50.000.000
Rut non:logB/BH+ = pH pKa = 8 8,25 = -0,25 B/BH+= 0,56
kh hthu ti d dy, d hthu ti RN
C ch: kthch tt c cc fn of TKTW, bit trn ty sg do chn chn lc 1 s
knh, gy ra co git kiu tetani (sd BZD ct cn co git)
Hthu: = PO, tim
T/dng: kthch px, tg hg c, kthch s trao i cht, kthch tiu ha, tg tit
dch v, tg tit dch tiu ha n ngon
Ch nh: tr suy nhc & vim dy TK, au TK
Liu c:
kthch ty sng tg px & gy co git kiu tetani suy h hp do nh
hng n cc CQ hh thiu O2 cht bi c ch hh
du hiu bit trc: au c, lo u, co cng
cn co git xy ra khi c tnh px, khi b tg vs tc nhn bn ngoi
Bi 6:
Vim l 1 /ng of HMD chg li tc nhn gy hi ni hoc ngoi sinh
- Triu chng: sng, nng, , au, suy gim c/n
- P vim c to ra fc hi c/n of cth
- P gn nh din ra ngay lp tc, tng lu lng mu n ch vim, tng tnh
thm mao mch, c s thm nhim bcu.
Bth mmch lin: hcu, bcu ko ra ngoi c. Vim bcu, tiu cu, kth ra ch b
tn thng tiu dit VK mu n nh` lm mao mch n ra
Cyclooxygenase (COX) enzyme to cc cht gy vim.
- COX 1: pb khp c th. SX PG:
Thn: ksot ti mu
Tiu ha: bv nim mc
Thc y kt tp tiu cu
- COX 2: pb trog TB, bcu, TB mng hot dch. SX PG trog vim
- PG l cc cht TGHH c tng hp t acid arachidonic
Td trog p vim: gin mch, tg tnh thm thnh mch, tng nhy cm ca
th th au, gy st
PG tg hp bi COX 2 : xhin trog qt vim tit qu mc vim qu mc
PG tg hp bi COX 1: c t.d trog qt g mu, tng lu lng mu n d
dy, tg tit cht nhy bv nim mc d dy

Thuc gim au, h st, khng vim: c hiu lc gim au nh & TB, c tnh khu tr
nh au u, au rang, au dy TK. Cn c td h st, khng vim.
Thuc c ch sx COX -2 gim sx PG gim au, gim vim, gim st
- Ibuprofen, ketoprofen, naproxen, fenoprofen a. arylpropionic thng sd
- Nhm oxicams
- Thuc c ch chn lc COX-2: tr vim l tng nhg c TDP
PL theo dc lc: Ibuprofen & Naproxenl tt nht
- Thuc c ch COX 1 nhiu TDP v COX-1 bv c th
- Thuc c ch COX 2 qu nh` tg g mu, t, qu, nhi mu c tim
- au d dy: ung thuc lch v COX-1 lot d dy do c ch COX-1
au tim:ung thuc lch v COX-2 au tim ng hn do c ch COX-2
NSAIDs (Nonsteroid anti inflammatory drugs): thuc khng vim
- Ch nh:
H st, gim au nh - TB
Fng nga huyt khi (aspirin)
Khng vim: thoi ha khp, vim khp, gout, vim cp
- TDP:
H tiu ha: au thng v , nn, tiu chy, lot, xut huyt
Tiu cu: c ch hot ha , tg nguy c chy mu
Thn: PG ha dng mu n thnthuc lm co M thn nn gi mui
nc, gy f/suy thn, suy tim xung huyt, tg kali huyt, i khg li tiu
Tim mch: tg nguy c t qu, nhi mu c tim, huyt khi TDP of
thuc u tin c ch COX-2
TKTW: au u, bun ng
T cung: ko di thai k, chm sinh
P qu mn: hen suyn, ng
Trn no c t.tm ksot mc nhit bth khi st, PG kthch t.tm CT co li
gi nhit. Thuc c ch PG thn nhit v li bth
Thn nhit tg ksot VK nn st va l tt.
u fng cha a.arachidonic khi n vo lm tng ng.liu tng hp PG
Para gim au, h st nhg ko khng vim.
au bng inh do t cung tit ra qu nh` PG
au nh sd para 325mg nu ko hiu qu th sd Ibuprofen Naproxen
Metoxicam, Diclofenac nghing v COX-2 nn b tim mch nn trnh
au d dy dng Naproxen km thuc au d dy. Nu c nguy c tim mch & d dy
u tin nguy c tim mch SD thuc c ch COX-1 vi thuc chg au d dy
Dng thuc khng vim c tgian bn thi di khi b vim mn tnh.
Ko sd NSAIDs 3 thg cui thai k, bit l 7 ngy trc khi sinh v gy xut huyt sau sinh
Aspirin fg nga huyt khi v Aspirin ti ctrc of COX cn thuc khc th ko
DICLOFENAC:l 1 cht c ch mnh hot tnh ca COX, do lm gim ng k
s to thnh prostaglandin, prostacyclin v thromboxan l nhng cht trung gian ca qu
trnh vim. Diclofenac cng iu ha con ng lipoxygenase v s kt t tiu cu.
Ch nh: tr di ngy vim khp mn, thoi ha khp. Thng kinh nguyn pht.
au cp (vim sau chn thg, sng n) v au mn. Vim a khp dng thp thiu nin.

Tc dng ph:
Nhc u, bn chn. au vng thng v, bun nn, nn, a chy, trng bng,
chn n, kh tiu. Gan: Tng cc transaminase. Tai: tai. Ph, d ng (c bit co tht
ph qun ngi bnhhen), chong phn v k c tt huyt p, vim mi, my ay. Tiu
ha: au bng, chy mu ng tiu ha. H thn kinh: Bun ng, trm cm, mt ng, lo
u, kh chu, d b kch thch. Da: My ay. H hp: Co tht ph qun.
Phn loi: tgian bn thi, TCHH, T/d u tin trn COX