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PARACETAMOL

1. Tng quan v paracetamol.


1.1. Gii thiu
- Paracetamol hay Acetaminophen, l mt thuc c tc dng h st, gim au
thuc nhm NSAID (non-steroidal anti-inflammatory drug)
- Tn gi Paracetamol v Acetaminophen c ly t tn ca hp cht: para
acetyaminophenol.
- 1878, Harmon Northrop Morse ln u tin tng hp c paracetamol.
- 1955, sn phm paracetamol ln u c bn ra vi tn Tylenol Childrens
Elixir.
1.2. Cng thc ha hc, tnh cht l ha.
1.2.1 Cng thc ha hc:

1.2.2 Tnh cht vt l:


- Bt kt tinh trng, khng mi, v ng nh, nng chy 170oC
- Tnh tan: hi tan trong nc, tan nhiu hn trong nc si, tan trong ethanol v
dung dch kim, rt kh tan trong chloroform, ether.
1.2.3 Tnh cht ha hc:
- Mang tnh cht ca nhm OH phenolic, nhm chc acetamid v nhn thm.
1.2.4. Tng hp:
T nguyn liu ban u l phenol, paracetamol c th tng hp c theo cch
sau:
2

2. Tc ng dc l.
2.1 C ch gy au, gy st
2.1.1 C ch gy au.

T bo Th cm th
Chn thng
b tn thng (Da, c, khp, rng, ty sng, ni tng)

Sn xut Truyn tn hiu

Prostaglandins (H2)
No

Gim ngng
au

au
3

2.1.2 C ch gy st.
Cht gy st ngoi lai (vi khun , c t, nm...) xm nhp vo c th s kch thch
bch cu sn xut cc cht gy st ni ti (cc cytokin, interferon, TNF...). Cht
ny hot ha prostaglandin synthetase, lm tng tng hp Prostaglandin(PG, c
bit l PGE1,PGE2) t acid Arachidonic ca vng di i, lm tng qu trnh to
nhit (rung c, tng h hp, tng chuyn ha) v gim qu trnh mt nhit (co mch
da) t gy st.
* Prostaglandin (PG) l cc acid bo khng bo ha cc m, c vai tr nh mt cht
trung gian ha hc ca qu trnh vim v nhn cm au, ngoi ra cn c cc tc dng sinh
l cc m ring bit. PGE2 c gii phng do kch thch c hc, ha hc, nhit, vi
khun c tc dng lm gin mch, tng tnh thm thnh mch gy vim
* Cyclooxygenase (COX) hay Prostaglandin H2 synthetase(PGHS) l mt loi
enzyme hnh thnh prostanoids - prostaglandins, prostacyclins, v thromboxanes. Tt c
u chu trch nhim cho phn ng vim. COX tng hp PG (nht l PGE1 v PGE2 ), c
hai v tr tc ng l COX v POX( peroxidase). Trong COX chuyn acid arachidonic
thnh hydroperoxit trung gian khng n nh l PGG2, sau v tr POX chuyn PGG2
thnh PGH2 l dng hot tnh.
* COX-1 (PGH2 synthetase-1): tham gia trong qu trnh sn xut cc PG c tc dng
iu ha cc chc phn sinh l, n nh ni mi, bo v t bo. C mt hu ht cc m:
thn, d dy, ni mc mch mu, tiu cu
*- COX-2 (PGH2 synthetase-2): tham gia tng hp cc PG thc y qu trnh vim. C
mt hu ht cc m vi nng nh. Thng thy cc im vim vi nng ln.

Cht gy st ngoi lai

2.2 C ch gim au h st ca paracetamol.


Bch cu

Cht gy st ni sinh
Tng qu trnh to nhit Gim qu trnh thi nhit
(RungAcid
c, tng h Prostaglandin
hp, tng Prostaglandin (Co mch)
arachidonic
chuyn ha) synthetase St
(E1,E2)
4

- Paracetamol c xem l cht c ch yu trong tng hp prostaglandin (PG).


Thuc c tc dng c ch sinh tng hp PG do c ch enzyme COX lm gim tng
hp PG bng cch cnh tranh vo v tr POX ca enzyme COX.
- Tc dng c ch ny c lin quan n nng peroxid cc t chc khc nhau.
i vi cc t bo nguyn vn, nng arachidonic thp, tc dng c ch ca
paracetamol th hin mnh. cc t bo b tn thng, nng hydroperoxide cao,
tc dng ca paracetamol yu. iu ny gii thch kh nng hot ng khc nhau
ca paracetamol cc t chc khc nhau nh no vi nng peroxide thp v
im vim nng peroxide cao.
- Trong c ch gy st, thng qua c ch tng hp PG, paracetamol tc ng lm
gim cc qu trnh sinh nhit ng thi tng qu trnh thi nhit t h st.

Cht gy st ngoi lai

Bch cu

Cht gy st ni sinh

Prostaglandin synthetase

c ch
Paracetamol
Prostaglandin
(E1,E2)

Tng qu trnh to nhit Gim qu trnh thi nhit


(Rung c, tng h hp, tng (Co mch)
chuyn ha)

St
5

- Tng t tc dng c ch tng hp PG ca paracetamol cng tc dng lm gim


s nhy cm ca cc receptor tip nhn cm gic au t tng ngng au gip
gim au.
Th cm th
(Da, c, khp, rng, ty sng, ni
tng)

T bo
b tn thng

Chn thng

Acid
arachidonic

Paracetamol c ch Sn xut Truyn tn hiu

Prostaglandins (H2) No

Gim
ngng au
au
3. Dc ng hc.
- Hp thu: Paracetamol c hp thu nhanh chng v hon ton qua ng tiu
ha.
6

- Phn b: Paracetamol c phn b nhanh v ng u trong phn ln cc m


trong c th. Khong 25% paracetamol trong mu kt hp vi protein huyt tng.
- Chuyn ha: Paracetamol chuyn ha bi cytocrom P450 gan to N acetyl
imin (NAPQI) l cht trung gian, cht ny tip tc ln kt vi nhm sulfydryl ca
glutathione to thnh cht khng c hot tnh.
- Thi tr: Thuc thi tr qua nc tiu ch yu dng chuyn ha, thanh thi
l 19,3 l/h. Thi gian bn thi khong 2,5h.
- Pracetamol liu cao (>10 g/ngy), s to ra nhiu N acetyl benzoquinonimin
(NAPQI) lm cn kit glutathione gan, khi NAPQI s phn ng vi sulfydrid
ca protein gan gy tn thng gan, hoi t gan, c th gy cht ngi nu khng
cp cu kp thi.

4. Ch nh.
- Paracetamol c dng rng ri trong iu tr cc chng au v st t nh n va
- au:
+ Paracetamol c lm gim au tm thi trong cc chng au nh v va: au
u, au rang, au bng kinh Thuc c hiu qu nht l gim au cng thp
c ngun gc khng phi ni tng.
+ Paracetamol khng c tc dng tr thp khp
+ Paracetamol l thuc thay th salicylic (c a thch ngi bnh chng ch
nh hoc khng dung np salicylic) gim au nh hoc h st.
- St: Paracetamol thng c dng gim thn nhit ngi bnh st, khi st
c th c hi hoc khi h st ni chung khng c hiu, khng nh hng n tin
trnh ca bnh c bn v c th che lp tnh trng bnh ca ngi bnh.

5. Cch dng Liu dng:


5.1. Cch dng:
- Thng dng ung.
- i vi ngi bnh khng ung c: dng dng thuc n t trc trng v thng
c liu cao hn liu ung.
- c k hng dn s dng trc khi dng thuc.
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5.2 Liu dng:


- Liu ung: + Ngi ln: 325 -1000mg/ngy (khng c qu 4000mg/ngy).
+ Tr em: 10mg/kg/ln x 3 4 ln ngy.
- Thuc n: a vo trc trng c 4-6h mt ln.
- Dng tim: Paracetamol dch tim truyn 10mg/ml (Perfalgan). Dng chng au trong
trng hp cp cu hay trong phu thut.

6. Tc dng ph, c tnh.


6.1 Tc dng ph:
-Thng l ban hoc my ay, nhng i khi nng hn v c th km theo st
do thuc v thng tn nim mc.
- t gp: bun nn, nn, lon to mu (gim bch cu trung tnh, gim tiu cu v
gim ton th huyt cu), c tnh thn khi lm dng di ngy.
6.2 c tnh:
- Liu iu tr: rt him, khng gy Met Hb.
- Liu cao, s dng ko di: gy hoi t t bo gan rt nguy him.
+ Thuc iu tr: Acetylcystein v methionin ( ch dng cho trng hp liu
cao)

7. Chng ch inh.
- Ngi bnh nhiu ln thiu mu hoc c bnh tim, phi, thn hoc gan.
- Ngi bnh qu mn vi paracetamol.
- Ngi bnh thiu ht glucose 6 phosphat dehydrogenase.

8. Tng tc thuc:
8.1. Tng tc thuc
- Ung paracetamol liu cao di ngy c th lm tng nh tc dng chng ng ca
coumarin v dn cht indandion.
- Dng ng thi isoniazid vi paracetamol cng c th dn n tng nguy c c tnh
vi gan.
8

- Cc thuc chng git (nh phenytoin, barbiturat, carbamazepin...) gy cm


ng enzyme microsom th gan, c th lm tng tnh c hi cho gan ca paracetamol.
- Cn phi ch n kh nng gy h st nghim trng ngi bnh dng ng thi
phenothiazin v liu php h nhit bng paracetamol.
- Phi hp paracetamol 1000mg v codein 60mg lm tng tc dng gim au i vi
sau phu thut, au trong vim thoi ha khp hng.
8.2. Thn trng khi dng:
Thuc t c tnh v hu nh khng c tc dng ph, tuy nhin khi s dng cn
ch mt s trng hp sau y, c bit khi dng cc ch phm kt hp vi cc
dc cht khc.
- Cc ch phm kt hp vi Codein khng dng cho tr em, ph n c thai, ph n cho
con b v ngi suy h hp.
- Cc ch phm kt hp vi Chlorpheniramin maleate gy bun ng, khng dng cho
nhng ngi m yu cu cn tp trung cao trong cng vic hoc sinh hot.
- Khng hoc hn ch s dng ru.
- Ch dng Paraetamol cho ph n c thai khi tht cn thit.

9. Bo qun
Bo qun thuc di 40C, tt nht l 15 30 C, trnh ng lnh dung dch,
dch treo ung.

10. Cc dng bo ch v ch phm trn th trng.


10.1. Dng ung: Dng s dng ph bin nht.
10.1.1Vin nn bao phim:
a s ch phm paracetamol trn th trng sn xut theo dng vin nn bao phim
theo c ch phng thch chm.
- u im:

- Tc ng 2 pha: Pha phng thch nhanh nhm gim nhanh triu chng
gim au, pha phng thch chm nhm duy tr lng thuc ti thiu gy hiu qu.
- Thi gian s dng thuc ko di, gim s ln s dng thuc
- Gim nguy c gy ng c cho gan.
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- Tin dng, d bo qun.


- Nhc im: Kh s dng cho bnh nhn kh nut nh tr em v ngi cao tui.

- i tng s dng: Ngi ln, tr em trn 3 tui, ph n c thai phi s dng


theo ch nh ca bc s.

- Liu dng:

- Ngi ln v tr em trn 12 tui: ung 1 2 vin 500mg/ln, ngy 3 ln.


Khng qu 6 vin/ngy.
- Tr em trn 6 12 tui: ung 1/2 1 vin 500mg/ln, ngy 2 4 ln. Khng
qu 4 vin/ngy.
- Tr em t 3 6 tui: ung 1/2 vin 500mg/ln, ngy 2 4 ln. Khng qu 2
vin/ngy.
- Hoc dng theo ch dn ca bc s.
Khong cch gia cc ln dng thuc ti thiu l 4 gi
- Ch phm trn th trng:

Tn thng mi: Panadol Tn thng mi: Panadol Extra


Thnh phn: Paracetamol 500mg
Thnh phn: Paracetamol
Cafein 65mg
500mg
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Tn thng mi: HAPACOL Blue Tn thng mi: HAPACOL Codein


Thnh phn: Paracetamol 500mg
Thnh phn: Paracetamol 500mg Codein 8mg

10.1.2 Vin nang mm


- u im:

- D nut do hnh dng thun, mm, b mt trn bng. Tin dng v d bo


qun v c phn liu ng gi ging vin nn.
- Sinh kh dng cao do cng thc bo ch thng n gin t t dc, v t
tc ng ca k thut bo ch so vi vin nn, v nang thng d tan r
gii phng dc cht.
- Nhc im: D tp trung dc cht khi gii phng gy kch ng.

- i tng s dng: Ngi ln v tr em.

- Liu dng:

- Ngi ln v tr em trn 12 tui: Mi ln ung 1 - 2 vin 500mg, ngy


ung 2 - 3 ln, khng qu 8 vin/ngy.
- Tr em 7 - 12 tui: Mi ln ung 1 vin, ngy ung 2 - 3 ln 500mg, khng
qu 4 vin/ngy.
- Ch phm trn th trng:
11

10.1.3.Vin si
- u im:

- D s dng, trong cc trng hp kh hoc khng nut c vin thuc


c bit l tr em, ngi cao tui. C thm t dc che giu mi v
gip d chu hn khi ung.
- Hp thu nhanh v gy tc dng nhanh hn, v vy ngi bnh s gim
nhanh cc triu chng (au, h nhit), bnh phc nhanh hn (au xng
khp, au u).
- Nhc im:

- D b lm dng, d gy qu liu.
- Kh bo qun.
- i tng s dng: Thch hp cho nhiu i tng.

- Liu dng v cch dng: Ha tan vin thuc trong lng nc tu thch n khi
ht si bt. Khong cch gia 2 ln ung phi hn 4 gi v khng ung qu 8 vin/
ngy.
- Ngi ln v tr em > 12 tui: ung 1 vin 500mg/ ln.
- au nhiu: ngi ln c th ung 2 vin/ ln.
- Trng hp bnh nhn suy thn nng ( thanh thi creatinin < 10 ml /pht),
khong cch gia cc liu ung phi t nht l 8 gi. Hoc theo ch dn ca Thy
thuc.
Lu : Liu ti a/ 24 gi: khng qu 4 g, khong cch gia 2 ln ung thuc phi
hn 4 gi.
- Ch phm trn th trng:
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10.1.4. Thuc bt si bt
- u im: Thch hp s dng cho tr em. C thm t dc to v ngt, thm d
ung.

- Nhc im:

- D b lm dng, gy qu liu.

- Kh bo qun.

- Liu dng v cch dng:


Ha tan thuc vo lng nc (thch hp cho b) n khi si ht bt.
Cch mi 6 gi ung mt ln, khng qu 5 ln/ ngy.
Liu ung: trung bnh t 10 - 15 mg/ kg th trng/ ln.
Tng liu ti a khng qu 60 mg/ kg th trng/ 24 gi.
- Ch phm trn th trng:
13

10.2. t hu mn: Vin n


- u im: Khong 50-70% thuc c hp th vo h tun hon m khng tri
qua giai on chuyn ha ti gan. Tc dng h st, gim au nhanh.

- Nhc im:

- Kh bo qun.

- Cch dng bt tin.

- i tng s dng: Tr em khng s dng c dng ung, bnh nhn hn m.

Liu dng: Vin n 80mg: Tr t 4-6 kg


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Vin n 150mg: Tr t 8-12kg


Vin n 300mg: Tr t 15-24kg
- Ch phm trn th trng:

10.3. Tim truyn:


- u im: Sinh kh dng cao, gy tc dng gim au h st nhanh.
- Nhc im:
- Gi thnh cao.
- Kh s dng.
- Kh bo qun.
10.3.1.Thuc tim
- Cch dng: Tim bp

- Liu dng:
15

- Ngi ln: 0,15g n 0,3g/ ngy tim 1 ln vo bui sng trong trng hp
au ngn ngy, au ko di khng qu 3 ngy.
- Tr em: liu 5mg/kg/ngy, tim 1 ln vo bui sng

10.3.2 Dung dch truyn tnh mch


- Cch dng: Truyn tnh mch

- Liu dng:

PARACOL 1 g/100ml:
Ch dng cho ngi ln v tr em c th trng > 33 kg.
Ngi ln v tr em trn 13 tui c th trng > 50 kg: 1 g/ln (= 1 chai
100 ml), c th truyn 4 ln/ngy. Liu ti a 4 g/ngy.
Tr em c th trng > 33 kg v ngi ln c th trng < 50 kg: 15
mg/kg/ln (= 1,5 ml dung dch cho 1 kg th trng). Liu ti a 60
mg/kg/ngy.
PARACOL 0,5 g/50ml:
Dng cho tr s sinh (di 10 ngy tui) v tr em c th trng 33 kg.
Tr em c th trng 33 kg:15 mg/kg/ln (= 1,5 ml dung dch cho 1 kg
th trng), c th truyn 4 ln/ngy. Liu ti a 60 mg/kg/ngy.
Tr s sinh (di 10 ngy tui): 7,5 mg/kg/ln, khng qu 4 ln/ngy.
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Dng Dng bo u im Nhc im i tng Ch phm trn


dng ch s dng th trng

Vin nn - Tc dng ko Kh s dng Ngi ln, - Panadol


bao phim di. cho bnh nhn tr trn 3 - Panadol Extra
Dng - Gim tn sut kh nut. tui. - Hapacol Blue
ung dng thuc. - Hapacol Codein
- Gim nguy c (tr em, ngi
c gan cao tui)
- Tin dng, d
bo qun.
Vin nang - D nut. C th gy Ngi ln, - Paracetamol
mm - Tin dng, d kch ng. tr em. Codein
bo qun. - Paralmax
- Sinh kh dng
cao.
Vin si - D s dng. - D b lm Nhiu i - Hapacol si
- Hp thu nhanh, dng, d gy tng. - Efferalgan
tc dng nhanh. qu liu.
- Kh bo
qun.

Thuc bt - D s dng. - D b lm Tr em - Hapacol 80mg


si bt - Hp thu nhanh, dng, d gy - Hapacol 150mg
tc dng nhanh. qu liu. - Hapacol 250mg
- Kh bo
qun.
t hu Vin n - 50-70% thuc - Kh bo - Tr em - Efferalgan
mn c hp th vo qun. khng 80mg
tun hon m - Cch dng dng dn - Efferalgan
khng tri qua bt tin. ung. 150mg
chuyn ha ti - Bnh - Efferalgan
gan. nhn hn 300mg
- Tc dng m.
nhanh.
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Tim Thuc - Sinh kh dng - Kh s dng. - Paracetamol


truyn tim cao. - Gi thnh injection
- Tc dng cao.
nhanh. - Kh bo qun
Dung dch - Paracetamol
truyn tnh Bivid.
mch - Rifaxon.

* Ti liu tham kho:


1. Gio trnh Dc l hc tp 1, nh xut bn i hc Y- Dc H Ni.
2. Dc th Vit Nam.
3. http://www.nidqc.org.vn/duocthu/category/cac-chuyen-luan-thuoc/muc-04-
thuoc-giai-doc-va-cac-thuoc-dung-trong-nhiem-doc/4-2-thuoc-giai-doc-dac-hieu/4-
2-1-thuoc-giai-doc-paracetamol
4. https://vi.wikipedia.org/wiki/Paracetamol#T.C6.B0.C6.A1ng_t.C3.A1c
5. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8171ecb8-fc2e-
4980-8d43-2f03cf972ac8 )
6. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=488899c6-9f7d-42d0-
825f-1ee1fa03d1a9
7. https://123doc.org/document/1755125-cac-thuoc-chong-viem-khong-steroid-
docx.htm
8. https://123doc.org/document/992515-tai-lieu-cac-thuoc-chong-viem-non-steroid-
ppt.htm
9. https://www.slideshare.net/OPEXL/1-thuoc-giam-dau-ha-sot-khang-viem
10. https://www.ncbi.nlm.nih.gov/pubmed/15662292
11. https://www.thuocbietduoc.com.vn/thuoc-goc-898/paracetamol.aspx
12. https://www.quora.com/What-is-the-mechanism-of-absorption-of-paracetamol
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Contents
1. Tng quan v paracetamol. .............................................................................................. 1
1.1. Gii thiu .................................................................................................................. 1
1.2. Cng thc ha hc, tnh cht l ha. ........................................................................ 1
1.2.1 Cng thc ha hc: ............................................................................................. 1
1.2.2 Tnh cht vt l: .................................................................................................. 1
1.2.3 Tnh cht ha hc: .............................................................................................. 1
1.2.4. Tng hp:........................................................................................................... 1
2. Tc ng dc l. ............................................................................................................ 2
2.1 C ch gy au, gy st ............................................................................................. 2
2.1.1 C ch gy au. .................................................................................................. 2
2.1.2 C ch gy st. ................................................................................................... 3
2.2 C ch gim au h st ca paracetamol. ................................................................. 3
3. Dc ng hc. ............................................................................................................... 5
4. Ch nh. .......................................................................................................................... 6
5. Cch dng Liu dng:................................................................................................... 6
5.1. Cch dng: ................................................................................................................ 6
5.2 Liu dng: .................................................................................................................. 7
6. Tc dng ph, c tnh. ................................................................................................... 7
6.1 Tc dng ph: ............................................................................................................ 7
6.2 c tnh: .................................................................................................................... 7
7. Chng ch inh................................................................................................................. 7
8. Tng tc thuc: .............................................................................................................. 7
8.1. Tng tc thuc ........................................................................................................ 7
8.2. Thn trng khi dng: ................................................................................................ 8
9. Bo qun .......................................................................................................................... 8
10. Cc dng bo ch v ch phm trn th trng. ............................................................ 8
10.1. Dng ung: Dng s dng ph bin nht. .............................................................. 8
20

10.1.1Vin nn bao phim: ........................................................................................... 8


10.1.2 Vin nang mm............................................................................................... 10
10.1.3.Vin si ........................................................................................................... 11
10.1.4. Thuc bt si bt ........................................................................................... 12
10.2. t hu mn: Vin n ......................................................................................... 13
10.3. Tim truyn: ......................................................................................................... 14
10.3.1.Thuc tim ...................................................................................................... 14
10.3.2 Dung dch truyn tnh mch ........................................................................... 15
* Ti liu tham kho: ......................................................................................................... 18

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