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MORPHIN
1.Cng thc: C17H19O3N
Morphin l hot cht chnh ca thuc phin, l mt opiat in hnh. Trong nha kh
ca qu cy thuc phin c khong 25 alcaloid th morphin chim 10%. Trong cng thc
cu to, morphin c cha nhn piperridin-phenanthren.
Trong y hc, morphin thng dng di dng cc mui nh morphin hydroclorid,
morphin sulfat
2.Tnh cht:
Tinh th hnh kim nh, mm, mu trng hay ng thnh khi vung, d b bin mu
do b oxy ha, thng hoa ngoi khng kh kh.
Khng mi, v ng, d tan trong nc, kh tan trong Ethanol, khng tan trong
Cloroform, tan trong dung dch kim.
3.nh tnh:
To ta vi thuc th chung ca alcaloid.
Do c nhm OH phenolic nn c tnh acid, cho mu tm vi dung dch st III
clorid, tc dng vi cc mui diazoni trong mi trng kim cho mu .
5 ml dung dch ch phm 0,1% + 1 ml dung dch nc oxy gi long + 1ml dung
dch amoniac long + 0,05 ml dung dch ng sulfat 4,0% s xut hin mu .
B oxy ha.
Gii phng iod t kali iodat.
un nng vi accid v c nh HCl, H 3PO4 c ri sau thm HNO 3 c s c
mu .
Ph t ngoi.
4. nh lng:
Bng acid perclorid 0,1N trong mi trng acid acetic khan, ch th tm tinh th
(cn thm dung dch thy ngn II acetat).
5. Dc ng hc:
Hp thu: ng ung km hn tim, phi sau 30 - 60 pht mi t nng ti a.
Phn b: vo cc t chc, qua c hng ro mu no, nhau thai.
Chuyn ha: ch yu gan, mt t thn.
Thi tr: qua thn ( 90 % ), mt t qua mt, phn, m hi, sa, nc bt.
6. Tc dng:
Morphin l mt thuc c tc dng gim au, gy nghin in hnh. Thuc tc dng
ln h thn kinh v c trn. N kch thch mt s trung tm dn n gy bun nn v nn,
lm co ng t, lm tng trng lc c, c bit l c vng gia rut vi d dy v
ng mt.
- Trn h thn kinh trung ng
Tc ng thay i ty theo liu dng:
Liu thp 1 3 mg: gy khoan khoi, gia tng tr tng tng, cho cm gic ph du
thot tc, lm kh ng, nn ma.
Liu iu tr 1 3 cg: Gim au v gy bun ng.
Liu cao hn: Gy ng v c th lm hn m.
- Trn h h hp
Liu thp: lm tng nhp h hp.
Liu cao hn: Suy h hp, lm trung tm h hp gim nhy cm vi CO2.
Liu c: c ch hon ton trung tm h hp.
8. Ch nh:
Dng trong cc trng hp au nhiu nh au qun do si thn, si mt, au do
chn thng, do ung th, au sau phu thut.
Morphin cn c tc dng gy ng nn c dng khi mt ng do au.
Chng a chy do morphin c tc dng lm gim nhu ng rut.
Dng gy m, gim au, gim lo lng trong phu thut.
Ri lon thn kinh: vt v, m sng...
Liu dng:
Liu gim au: 1 3 cg ty b nh nhn.
Liu ti a: ung, tim di da 0.02g /ln, 0.05 g/24 gi.
Liu thm d khi u: 5 10 mg/ln, cch qung 4 gi.
Ngi trn 60 tui v suy gan dng liu nh hn v cch qung xa hn.
i vi b n h nhn au nhiu nh au do ung th khi dng morphin ho c cc thuc
gim au thc th khc rt t nguy c gy c ch h hp (do tc ng au lm gim
qu trnh c ch). Liu dng cn c vo p ng ca b nh nhn, c th dng liu cao so
vi liu thng dng. Khng c gii hn ti a.
11. Bo qun: Trnh nh sng. Bo qun nhit trong phng v ni kh ro (vin nn
v nang).
12. Nhim c morphin:
12.1. c tnh cp:
Giai on u kch thch ngn: nhc u, chng mt, nng ran, ming kh, mch
nhanh, nn. Giai on sau bnh nhn ng su, co ng t, khng phn ng vi nh sng,
th Cheyne-Stokes. Giai on cui: ngt th, v m hi lnh, gin ng t, try tim
mch, ri cht.
iu tr: m bo thng kh cho bnh nhn, dung thuc naloxon (thuc i khng vi
morphin).
12.2. c tnh mn:
Quen thuc:
Quen thuc ph thuc vo liu dng v s dng lp li. Khi dng morphin hoc
opioid lp i lp li nhiu ln vi liu iu tr, th hiu qu s gim dn, i hi phi dng
tng liu mi gi c hiu qu nh ban u...
Ngi quen thuc c th dng liu cao gp 10 - 20 ln so vi bnh thng. Hin
tng ny gi l quen thuc. Nu dng liu cao vi khong cch ngn, quen thuc s
xut hin nhanh. lm gim thiu s quen thuc, phi dng liu thp v khong cch
gia cc ln dng thuc di hn.
C ch: morphin kch thch receptor, c ch gii phng mt s cht trung gian ha
hc, c ch enzym adenylcyclase, lm gim sn xut AMPc (cyclic adenosin
monophosphate) - cht truyn tin th hai.
Khi dng thuc lp i lp li, c th phn ng bng cch tng tng hp AMPc, gim
cn bng sn xut adenylcyclase, v vy liu morphin sau i hi phi cao hn liu trc
receptor p ng mnh nh c, dn n hin tng quen thuc.
Nghin thuc:
Khi dng morphin ngoi sinh ko di s dn ti 2 hu qu:
Receptor gim p ng vi morphin.
C th gim sn xut morphin ni sinh.
S thiu ht morphin ni sinh lm cho ngi dng phi l thuc vo morphin ngoi lai,
l nghin thuc.
Ngi nghin lun luni morphin, khi thi thuc t ngt, morphin ni sinh
khng , cc receptor morphin ang trong tnh trng chng li s tc ng thng xuyn
ca morphin b ri vo trng thi mt thng bng, xut hin hi chng nghin thuc: chy
nc mi, nc mt, tng thn nhi t, dn ng t, i ma, tiu chy, yu c, run, ri lon
tun hon - h hp v c th dn n t vong.
iu tr:
Ngi nghin cn c cch ly, kt hp lao ng chn tay v tm l liu php, dng
mt s thuc.
Dng thuc loi morphin: dng methadon, mt loi thuc opioid c tc dng ko di.
Ngoi ra c th dng cc thuc i khng vi morphin nh naloxon, naltrexon...
CODEIN
Bit dc: Codicept, Rami, Pentuss.
1.Cng thc: C18H21NO3.H2O
Thng gp: au u, chng mt, kht v c cm gic khc l, bun nn, nn, to bn, b
i, i t, mch nhanh, mch chm, hi hp, yu mt, h huyt p th ng.
Him gp: phn ng phn v, o gic, mt phng hng, ri lon th gic, co git, suy
tun hon, mt, tot m hi, mt mi.
Nghin thuc: dng codein thi gian di vi liu t 240-540 mg/ngy c th gy nghin
thuc. Cc biu hin thng gp khi thiu thuc l bn chn, run, co git c, tot m hi,
chy nc mi. C th gy l thuc thuc v tm l, v thn th v gy quen thuc.
8. Ch nh:
- Ho khan .
- au nh v va.
9.Chng ch nh:
- Mn cm vi cc thnh phn ca thuc
- Tr di 1 tui
- Bnh gan h hp.
10.Dng dng v liu dng:
10.1 Dng dng:
- Codein c tm thy trong nhiu sn phm dc trn ton th gii, n c tm
thy trong nhiu hnh thc bao vin nn vin nang, xirovv. Cc mui phosphate v
suphate c s dng thng xuyn trong y hc.
au nh v va:
Ung: mi ln 30mg cch 4h nu cn thit: liu thng thng dao ng t 15-60
mg, ti a l 240mg/ ngy. Tr em 1-12 tui: 3 mg/kg/ngy, chia thnh liu nh (6 liu)
Tim bp: mi ln 30-60 mg, cch 4h nu cn thit.
Ho khan:
10-20 mg/ln, 3-4 ln/ngy (dng dng thuc nc 15mg/ 5ml) khng vt qu
120 mg/ngy.
Tr em 1-5 tui dng mi ln 3mg, 3-4 ln/ngy (dng dng thuc nc 5mg/5ml)
khng vt qu 12 mg/ngy, 5-12 tui dng mi ln 5-10 mg, chia 3-4 ln trong ngy,
khng vt qu 60 mg/ngy.
Qu liu:
Triu chng suy h hp. L m dn n trng thi dn hn m, mm c, da lnh v
m, i khi mch chm v h huyt p. Trong trng hp nng ngng th try tim mch
X tr: h tr h hp c kim sot dng ngay naloxon bng ng tim tnh mch trong
trng hp nng.
11.Bo qun:
Bo qun thuc nhit phng, bao b kn.
Bo qun codein phosphat tim trnh nh sng nhit di 400C.
12.Tng tc thuc:
Tc dng gim au ca Codein tng khi phi hp vi aspirin v paracetamol, nhng gim
hoc mt tc dng bi quinidin.
Codein lm gim chuyn ha cyclosporin do c ch men cytochrom P450.
Khng c kt hp Codein vi cc dd cha aminophylin, amoni clorid, natri
amobarbital, natri pentobarbital, natri phenobarbital, natrimethicillin, natri nitrofurantoin,
natri clorothiazid, natri bicarbonat, natri iodid, natri thiopental, natri heparin.
NALORPHIN HYDROCLORID
Tn khc: N allylnormorphin.
Bit dc: Lethidrone, Norfin.
1.Cng thc:
2.Tnh cht
Bt kt tinh c nhit nng chy t 260 0C n 2630C (phn hy). Nng sut quay
cc t -1200 n -1250 (dung dch 2% trong H2O).
Tnh cht ha hc v l ha tng t nh morphin hydroclorid.
3.nh tnh:
o ph hng ngoi, ph t ngoi, phn ng ca ion clorid.
4.nh tnh:
o ph t ngoi 285 nm (mi trng nc).
5.C ch tc dng:
Nalorphine mt cht c tc ng hn hp, hot ng ti hai th th opioid, ti th
th n c tc dng i khng v c tc ng ch vn ti th th k.
6.Dc ng hc:
Nalorphine hp thu km khi a qua ng ming. S ng ng tim hiu qu
hn khi ung, c l v bin i sinh hc nhanh chng trong gan ( ch yu l thng qua s
1.Cng thc:
2.Tc dng:
Butorphanol c tc dng iu tr cc cn au t va n nng, bao gm au sau
phu thut, au c, au u v au na u. Butorphanol l mt thuc gim au c cht
gy nghin tng t nh morphine.
Butorphanol cng c th ngn chn tc dng ca cc thuc gim au gy nghin
v c th gy ra cc triu chng ngng thuc nhng ngi ph thuc vo thuc gim
au gy nghin.
3.Chng ch nh:
D ng vi butorphanol hoc bt c thnh phn no ca thuc
C tin s: co git, chn thng no, suy h hp, tng p lc ni s, suy tim, cao
huyt p, lon nhp tim, nhi mu c tim cp tnh, hen ph qun, suy gan/thn.
Ngi nghin ma ty
ang dng cc loi thuc: thuc chng trm cm; thuc khng histamin;
barbiturates; erythromycin; nhm thuc IMAO; thuc xt mi nh oxymetazolin (Afrin,
Dristan); thuc an thn; thuc ng.
4.Tc dng ph:
Cc tc dng ph thng gp nht ca thuc ny l bun ng (xy ra khong
43% cc trng hp), chng mt (thy trong 19% bnh nhn), bun nn v/hoc nn (c
trng bi 13% s bnh nhn).
Ngoi ra cn gp mt s phn ng bt li nh:
H thng tim mch: Cc triu chng ca gin mch, gim huyt p, ngt xu,
nhp tim chm.
H thng thn kinh: nhc u, lo u, mt ng, gic m bt thng, cm gic
nng, dysphoria, th ch, o gic, kch ng, d cm, run, lo lng, l ln, hng phn, mt
mi, th , hi chng cai nghin.
H thng tiu ha: to bn, chn n, au vng thng v, kh nim mc ming
i vi da: nga, tng tit m hi, pht ban, ni m ay.
Cc gic quan: au mt, m mt, tai.
5.Dng dng v liu lng:
Dng dng ham lng:
Dung dch, thuc tim, dng mui tartrate: 1 mg/ml (1 ml); 2 mg/mL (1 ml, 2
ml, 10 ml).
Dung dch, thuc tim, dng mui tartrate (khng cht bo qun): 1 mg/ml (1
ml); 2 mg/mL (1 ml).
Dung dch, thuc xt m, dng mui tartrate: 10 g/ml (2,5 ml).
Liu dng:
Thuc tim:
Liu dng thng thng cho ngi ln gy m
Trc phu thut: liu khi u: 2 mg tim bp 60-90 pht trc khi phu
thut.
Cn bng qu trnh gy m: liu khi u: 2 mg tim tnh mch ngay trc qu
trnh gy m v / hoc gia tng 0,5 mg n 1 mg trong khi gy m.
Liu dng thng thng cho ngi ln khi sinh con:
S dng khi ang trong qu trnh chuyn d: liu khi u: 1 hoc 2 mg tim tnh
mch hoc tim bp mt ln. Liu ny c th c lp li mi 4 gi nu cn thit.
NALOXON HYDROCLORID
Bit dc: Nalonee, Narcanti.
2.Tnh cht:
Naloxon hydroclorid dng bt trng, nhit nng chy khong 200-2050C.
D tan trong nc , trong ethanol, thc t khng tan trong toluen.
3.nh tnh:
- o ph hng ngoi, phi ph hp vi ph cht chun.
- Bng sc k lp mng.
- Lm phn ng ca ion clorid.
4.nh lng:
Ha ch phm vo etanol, thm dung dch HCl 0,01M vo v chun bng dung
dch NaOH 0,1M trong ethanol. Xc nh im kt thc bng o th, c th tch gi 2
im un.
5.Dc ng hc:
Mc d c hp thu d qua ng tiu ha nhng naloxon b chuyn ha
gan trc khi vo vng tun hon nn liu ung phi ln hn nhiu so vi liu tim.
Thuc c tc dng nhanh (1 - 2 pht sau khi tim tnh mch) thi gian tc dng ph thuc
vo liu v ng dng. Sau khi tim, naloxon phn b nhanh vo cc m v dch c th.
Thi gian bn thi l 60 - 90 pht.
6.Tc dng:
Khc vi levallorphan hoc nalorphin, naloxon t hoc khng c hot tnh ch
vn. ngi dng liu ln opioid, naloxon i khng phn ln nhng tc dng khng
mong mun ca opioid nh c ch h hp, an thn, gy ng...
Naloxon khng gy nhn thuc hoc khng gy nghin v mt th cht hoc tm
l. Khi dng, naloxon c th gy ra hi chng thiu thuc sm ngi nghin opioid, tuy
vy dng liu cao s ngn chn c triu chng suy h hp trong hi chng ny
7.Tc dng ph:
H thn kinh trung ng: Mt ng, d b kch thch, lo u, triu chng cai nghin i vi
opiat.
Da: Ban.
D dy - rut: Bun nn, nn.
Mt: Nhn m.
Khc: V m hi.
8.Ch nh:
Khi b c ch do ch phm opiat v khi dng ch phm opiat qu liu cp tnh.
Naloxon hydroclorid c dng iu tr c ch h hp do cc opiat t nhin v tng
hp nh anileridin, codein, diphenoxylat, fentanyl citrat, heroin, methadon, morphin,
alcaloid hydroclorid ca thuc phin m c v propoxyphen.
Thuc cng iu tr c hiu qu c ch h hp do nhng thuc ch vn tng phn ca
opiat gm butorphanol, nalbuphin, pentazocin, v cyclazocin.
C th dng naloxon cho tr s sinh iu tr chng ngt do dng opiat cho ngi m
trong thi gian chuyn d v .
Naloxon cn c dng chn on ngi nghin opiat v iu tr nghin opiat.
9.Chng ch nh:
Chng ch nh vi ngi bnh mn cm vi thuc.
Khng c trn ln thuc tim naloxon hydroclorid vi nhng ch phm cha bisulfit,
metabisulfit, nhng anion c mch di hoc trng lng phn t cao, hoc bt c dung
dch no c pH kim.
Khng c cho thm cc thuc hoc cc cht ha hc vo dung dch naloxon
hydroclorid tr khi xc nh c tc dng ca chng trn n nh ha hc v vt
l ca dng dch naloxon.
10.Dng dng v liu lng:
Dng dng:
Thuc vin: vin nn, vin nang.
Dung dch tim: 0.4mg/ml. ng gi: Hp 10 ng/1 ml.
Liu lng: ngi ln: 0,4- 2 mg, tim tnh mch, 2 -3 pht tim nhc li nu cn.
Tng liu 10 mg.
V thi gian tc dng ca naloxon rt ngn (60 - 90 pht) nn cn truyn lin tc
naloxone khi bnh nhn ng c opioid nng.
11.Bo qun:
Thuc tim naloxon hydroclorid 15 - 30oC, v trnh nh sng. Thuc tim n nh
pH 2,5 - 5. Sau khi pha long trong dung dch tim dextrose 5% hoc natri clorid 0,9%
ti nng 0,004 mg/ml (4 microgam/ml), dung dch naloxon hydroclorid n nh trong
24 gi; sau 24 gi, phi loi b bt c dung dch thuc no khng dng n.