{"id":18705,"date":"2019-08-01T18:45:53","date_gmt":"2019-08-01T11:45:53","guid":{"rendered":"https:\/\/www.vnras.com\/drug\/?p=18705"},"modified":"2019-08-01T18:45:53","modified_gmt":"2019-08-01T11:45:53","slug":"thuoc-khang-histamin-h1","status":"publish","type":"post","link":"https:\/\/vnras.com\/drug\/thuoc-khang-histamin-h1\/","title":{"rendered":"Thu\u1ed1c kh\u00e1ng histamin H1"},"content":{"rendered":"

L\u1ecbch s\u1eed nghi\u00ean c\u1ee9u v\u00e0 ph\u00e1t tri\u1ec3n<\/h2>\n
Thu\u1ed1c kh\u00e1ng histamin H1 l\u00e0 thu\u1ed1c ng\u0103n ch\u1eb7n ho\u1ea1t \u0111\u1ed9ng c\u1ee7a histamin \u1edf th\u1ee5 th\u1ec3 H1. H\u1ea7u h\u1ebft c\u00e1c thu\u1ed1c kh\u00e1ng histamin H1 \u0111\u1ec1u l\u00e0 ch\u1ea5t ch\u1ee7 v\u1eadn ng\u01b0\u1ee3c H1-receptor ch\u1ee9 kh\u00f4ng ph\u1ea3i l\u00e0 ch\u1ea5t \u0111\u1ed1i kh\u00e1ng.<\/p>\n
\u0110\u1ec3 hi\u1ec3u v\u1ec1 thu\u1ed1c kh\u00e1ng histamin H1, c\u1ea7n \u0111\u00e1nh gi\u00e1 t\u00ecnh tr\u1ea1ng khoa h\u1ecdc v\u00e0o nh\u1eefng n\u0103m 1930. B\u1eb1ng quan s\u00e1t trong c\u00f4ng vi\u1ec7c c\u1ee7a m\u00ecnh, Daniel Bovet \u0111\u00e3 vi\u1ebft ra \u201cBa lo\u1ea1i amin t\u1ef1 nhi\u00ean: acetylcholin, epinephrin v\u00e0 histamin c\u00f3 th\u1ec3 x\u1ebfp v\u00e0o m\u1ed9t nh\u00f3m v\u00ec s\u1ef1 t\u01b0\u01a1ng \u0111\u1ed3ng trong c\u1ea5u tr\u00fac h\u00f3a h\u1ecdc, \u0111\u1ec1u c\u00f3 trong d\u1ecbch c\u01a1 th\u1ec3 v\u00e0 c\u00f3 c\u00e1c ho\u1ea1t t\u00ednh d\u01b0\u1ee3c l\u00ed \u0111\u1eb7c tr\u01b0ng m\u1ea1nh m\u1ebd. C\u00f3 m\u1ed9t s\u1ed1 alkaloid c\u1ea3n tr\u1edf ho\u1ea1t \u0111\u1ed9ng c\u1ee7a acetylcholin. T\u01b0\u01a1ng t\u1ef1, c\u00f3 m\u1ed9t s\u1ed1 ch\u1ea5t trung h\u00f2a ho\u1eb7c \u0111\u1ea3o ng\u01b0\u1ee3c t\u00e1c d\u1ee5ng c\u1ee7a epinephrin. Do \u0111\u00f3, d\u01b0\u1eddng nh\u01b0 c\u00f3 th\u1ec3 t\u1ed3n t\u1ea1i m\u1ed9t s\u1ed1 ch\u1ea5t c\u00f3 t\u00e1c d\u1ee5ng \u0111\u1ed1i kh\u00e1ng c\u1ee5 th\u1ec3 v\u1edbi histamin.\u201d Bovet, khi \u0111ang t\u00ecm ki\u1ebfm ch\u1ea5t \u0111\u1ed1i kh\u00e1ng acetylcholin, \u0111\u00e3 y\u00eau c\u1ea7u h\u1ecdc tr\u00f2 c\u1ee7a m\u00ecnh l\u00e0 Anne-Marie Staub ki\u1ec3m tra t\u00e1c d\u1ee5ng \u0111\u1ed1i kh\u00e1ng histamin c\u1ee7a m\u1ed9t v\u00e0i h\u1ee3p ch\u1ea5t trong n\u00e0y. \u0110i\u1ec1u n\u00e0y d\u1eabn \u0111\u1ebfn vi\u1ec7c ph\u00e1t hi\u1ec7n ra thu\u1ed1c kh\u00e1ng histamin \u0111\u1ea7u ti\u00ean v\u00e0o n\u0103m 1937. M\u1eb7c d\u00f9 h\u1ee3p ch\u1ea5t n\u00e0y qu\u00e1 \u0111\u1ed9c \u0111\u1ec3 s\u1eed d\u1ee5ng tr\u00ean ng\u01b0\u1eddi, nh\u01b0ng n\u00f3 \u0111\u00e3 m\u1edf ra c\u01a1 h\u1ed9i gi\u1edbi thi\u1ec7u tr\u00ean l\u00e2m s\u00e0ng c\u1ee7a antergan n\u0103m 1942, sau \u0111\u00f3 l\u00e0 diphenhydramine n\u0103m 1945, chlorpheniramine, brompheniramine v\u00e0 promethazine sau \u0111\u00f3 trong c\u00f9ng th\u1eadp k\u1ec9. C\u00e1c thu\u1ed1c n\u00e0y g\u1ecdi l\u00e0 thu\u1ed1c kh\u00e1ng histamin H1 th\u1ebf h\u1ec7 m\u1ed9t. Ch\u00fang \u0111\u1eb7c tr\u01b0ng b\u1edfi s\u1ef1 kh\u00e1ng muscarinic, kh\u00e1ng \u03b1-adrenergic v\u00e0 kh\u00e1ng serotonin. Nh\u01b0\u1ee3c \u0111i\u1ec3m l\u1edbn nh\u1ea5t c\u1ee7a ch\u00fang l\u00e0 \u0111i qua h\u00e0ng r\u00e0o m\u00e1u n\u00e3o v\u00e0 kh\u00e1ng histaminergic th\u1ea7n kinh trung \u01b0\u01a1ng. \u0110i\u1ec1u n\u00e0y c\u0169ng l\u00ed gi\u1ea3i cho c\u00e1c t\u00e1c d\u1ee5ng ph\u1ee5 tr\u00ean th\u1ea5n kinh trung \u01b0\u01a1ng c\u1ee7a c\u00e1c thu\u1ed1c th\u1ebf h\u1ec7 m\u1ed9t.<\/p>\n
$\"L\u1ecbch$
\u1ea2nh: L\u1ecbch s\u1eed thu\u1ed1c kh\u00e1ng histamin H1.<\/figcaption><\/figure>\n
N\u0103m 1980 \u0111\u00e3 ch\u1ee9ng ki\u1ebfn s\u1ef1 ti\u1ebfn b\u1ed9 l\u1edbn trong ph\u00e1t tri\u1ec3n c\u00e1c thu\u1ed1c kh\u00e1ng histamin. C\u00e1c thu\u1ed1c kh\u00e1ng histamin H1 th\u1ebf h\u1ec7 th\u1ee9 hai ra \u0111\u1eddi, v\u1edbi kh\u1ea3 n\u0103ng \u0111i qua h\u00e0ng r\u00e0o m\u00e1u n\u00e3o th\u1ea5p h\u01a1n nhi\u1ec1u th\u1ebf h\u1ec7 th\u1ee9 nh\u1ea5t. C\u00e1c thu\u1ed1c n\u00e0y c\u00f3 t\u00ednh ch\u1ecdn l\u1ecdc cao v\u1edbi th\u1ee5 th\u1ec3 histamin H1 v\u00e0 kh\u00f4ng c\u00f3 t\u00e1c d\u1ee5ng kh\u00e1ng cholinergic. C\u00e1c h\u01b0\u1edbng d\u1eabn m\u1edbi nh\u1ea5t c\u1ee7a EAACI\/GA LEN\/EDF\/WAO trong qu\u1ea3n l\u00ed n\u1ed5i m\u00e0y \u0111ay khuy\u1ebfn c\u00e1o ph\u01b0\u01a1ng ph\u00e1p \u0111i\u1ec1u tr\u1ecb \u0111\u1ea7u tay n\u00ean l\u00e0 c\u00e1c thu\u1ed1c kh\u00e1ng histamin H1 th\u1ebf h\u1ec7 hai \u2013 lo\u1ea1i kh\u00f4ng g\u00e2y bu\u1ed3n ng\u1ee7.<\/p>\n
M\u1ed9t s\u1ed1 thu\u1ed1c \u0111\u01b0\u1ee3c coi l\u00e0 thu\u1ed1c kh\u00e1ng histamin H1 th\u1ebf h\u1ec7 ba th\u1ef1c ch\u1ea5t l\u00e0 c\u00e1c \u0111\u1ed3ng ph\u00e2n quang h\u1ecdc ho\u1eb7c ch\u1ea5t chuy\u1ec3n h\u00f3a c\u1ee7a th\u1ebf h\u1ec7 hai \u0111\u01b0\u1ee3c cho l\u00e0 l\u00e0m t\u0103ng t\u00e1c d\u1ee5ng v\u00e0 gi\u1ea3m c\u00e1c ph\u1ea3n \u1ee9ng b\u1ea5t l\u1ee3i (v\u00ed d\u1ee5: levocetirizine, desloratadine, fexofenadine). V\u1eabn c\u00f2n nh\u1eefng tranh c\u00e3i xung quanh vi\u1ec7c c\u00f3 n\u00ean g\u1ecdi c\u00e1c thu\u1ed1c n\u00e0y l\u00e0 th\u1ebf h\u1ec7 ba hay kh\u00f4ng.<\/p>\n
D\u01b0\u1ee3c l\u1ef1c h\u1ecdc<\/h2>\n
C\u00e1c th\u1ee5 th\u1ec3 histamin H1 thu\u1ed9c si\u00eau h\u1ecd th\u1ee5 th\u1ec3 c\u1eb7p \u0111\u00f4i protein G (GPCRs) (H\u00ecnh a). GPCRs c\u00f3 th\u1ec3 \u0111\u01b0\u1ee3c xem \u0111i nh\u01b0 \u201cb\u1ed9 ng\u1eaft m\u1ea1ch t\u1ebf b\u00e0o\u201d, t\u1ed3n t\u1ea1i c\u00e2n b\u1eb1ng gi\u1eefa tr\u1ea1ng th\u00e1i kh\u00f4ng ho\u1ea1t \u0111\u1ed9ng (\u201coff\u201d) v\u00e0 ho\u1ea1t \u0111\u1ed9ng (\u201con\u201d). Trong tr\u01b0\u1eddng h\u1ee3p c\u1ee7a th\u1ee5 th\u1ec3 histamin H1, histamin li\u00ean k\u1ebft ch\u00e9o v\u1edbi c\u00e1c domain xuy\u00ean m\u00e0ng III v\u00e0 V, \u1ed5n \u0111\u1ecbnh th\u1ee5 th\u1ec3 trong c\u1ea5u tr\u00fac ho\u1ea1t \u0111\u1ed9ng c\u1ee7a n\u00f3, l\u00e0m cho tr\u1ea1ng th\u00e1i c\u00e2n b\u1eb1ng chuy\u1ec3n sang v\u1ecb tr\u00ed \u201con\u201d (h\u00ecnh b). Thu\u1ed1c kh\u00e1ng histamin H1 kh\u00f4ng c\u00f3 c\u1ea5u tr\u00fac t\u01b0\u01a1ng t\u1ef1 histamin, kh\u00f4ng \u0111\u1ed1i kh\u00e1ng s\u1ef1 g\u1eafn k\u1ebft c\u1ee7a histamin m\u00e0 li\u00ean k\u1ebft v\u1edbi c\u00e1c v\u1ecb tr\u00ed kh\u00e1c nhau tr\u00ean th\u1ee5 th\u1ec3 t\u1ea1o ra t\u00e1c d\u1ee5ng ng\u01b0\u1ee3c. Vi d\u1ee5, cetirizine li\u00ean k\u1ebft ch\u00e9o v\u1edbi c\u00e1c v\u1ecb tr\u00ed tr\u00ean domain xuy\u00ean m\u00e0ng IV v\u00e0 VI \u1ed5n \u0111\u1ecbnh th\u1ee5 th\u1ec3 \u1edf tr\u1ea1ng th\u00e1i kh\u00f4ng ho\u1ea1t \u0111\u1ed9ng v\u00e0 chuy\u1ec3n tr\u1ea1ng th\u00e1i c\u00e2n b\u1eb1ng sang v\u1ecb tr\u00ed \u201coff\u201d (h\u00ecnh c). Nh\u01b0 v\u1eady thu\u1ed1c kh\u00e1ng histamin kh\u00f4ng ph\u1ea3i l\u00e0 ch\u1ea5t \u0111\u1ed1i kh\u00e1ng th\u1ee5 th\u1ec3, m\u00e0 l\u00e0 ch\u1ea5t ch\u1ee7 v\u1eadn ng\u01b0\u1ee3c do ch\u00fang t\u1ea1o ra t\u00e1c d\u1ee5ng ng\u01b0\u1ee3c l\u1ea1i tr\u00ean th\u1ee5 th\u1ec3 histamin. Do \u0111\u00f3 ng\u01b0\u1eddi ta s\u1eed d\u1ee5ng thu\u1eadt ng\u1eef \u201cH1-antihistamines\u201d \u00a0thay v\u00ec \u201chistamine antagonists\u201d.<\/p>\n
T\u00f3m l\u1ea1i, c\u00e1c thu\u1ed1c kh\u00e1ng histamin H1 c\u00f3 t\u00e1c d\u1ee5ng ng\u01b0\u1ee3c l\u1ea1i v\u1edbi histamin tr\u00ean th\u1ee5 th\u1ec3 H1, th\u1ee5 th\u1ec3 n\u00e0y xu\u1ea5t hi\u1ec7n \u1edf c\u01a1 tr\u01a1n h\u00f4 h\u1ea5p, c\u01a1 tr\u01a1n m\u1ea1ch m\u00e1u… \u0111\u1eb7c\u00a0 bi\u1ec7t l\u00e0 \u1edf t\u1ebf b\u00e0o mast (d\u01b0\u1ee1ng b\u00e0o) v\u00e0 khi li\u00ean k\u1ebft v\u1edbi histamin, ch\u00fang \u0111\u00f3ng vai tr\u00f2 quan tr\u1ecdng trong h\u00ecnh th\u00e0nh c\u00e1c ph\u1ea3n \u1ee9ng d\u1ecb \u1ee9ng: ng\u1ee9a, gi\u00e3n m\u1ea1ch, h\u1ea1 huy\u1ebft \u00e1p, t\u0103ng t\u00ednh th\u1ea5m th\u00e0nh m\u1ea1ch v\u00e0 co th\u1eaft ph\u1ebf qu\u1ea3n. Do v\u1eady thu\u1ed1c kh\u00e1ng histamin H1 gi\u00fap gi\u1ea3m tri\u1ec7u ch\u1ee9ng ng\u1ee9a, gi\u1ea3m ph\u1ea3n \u1ee9ng d\u1ecb \u1ee9ng, m\u00e0y \u0111ay… do gi\u1ea3i ph\u00f3ng qu\u00e1 nhi\u1ec1u histamin.<\/p>\n
$\"S\u01a1$
\u1ea2nh: S\u01a1 \u0111\u1ed3 m\u1ed9t th\u1ee5 th\u1ec3 histamin H1 cho th\u1ea5y 7 domain xuy\u00ean m\u00e0ng. Histamin k\u00edch th\u00edch th\u1ee5 th\u1ec3 sau khi x\u00e2m nh\u1eadp v\u00e0o l\u00f5i trung t\u00e2m. (b) Histamin li\u00ean k\u1ebft v\u1edbi domain III v\u00e0 V. (c) cetirizine li\u00ean k\u1ebft v\u1edbi domain IV v\u00e0 VI.<\/figcaption><\/figure>\n
L\u01b0u \u00fd r\u1eb1ng thu\u1ed1c kh\u00e1ng histamin H1\u00a0th\u1ebf h\u1ec7 \u0111\u1ea7u ti\u00ean c\u00f3 chung\u00a0ngu\u1ed3n g\u1ed1c h\u00f3a h\u1ecdc m\u00e0 t\u1eeb \u0111\u00f3 c\u00e1c ch\u1ea5t \u0111\u1ed1i kh\u00e1ng muscarinic cholinergic, thu\u1ed1c an th\u1ea7n, thu\u1ed1c ch\u1ed1ng lo\u1ea1n th\u1ea7n v\u00e0 thu\u1ed1c ch\u1ed1ng t\u0103ng huy\u1ebft \u00e1p c\u0169ng \u0111\u01b0\u1ee3c ph\u00e1t tri\u1ec3n, n\u00ean kh\u00f4ng ng\u1ea1c nhi\u00ean khi ch\u00fang c\u00f3 kh\u1ea3 n\u0103ng ch\u1ecdn l\u1ecdc th\u1ee5 th\u1ec3 k\u00e9m v\u00e0 th\u01b0\u1eddng t\u01b0\u01a1ng t\u00e1c v\u1edbi c\u00e1c th\u1ee5 th\u1ec3 kh\u00e1c. Thu\u1ed1c g\u00e2y ra t\u00e1c d\u1ee5ng antimuscarinic, kh\u00e1ng \u03b1-adrenergic v\u00e0 antiserotonin.\u00a0Khi \u0111i qua h\u00e0ng r\u00e0o m\u00e1u n\u00e3o, ch\u00fang c\u1ea3n tr\u1edf ch\u1ee9c n\u0103ng c\u1ee7a histamin trong th\u1ea7n kinh trung \u01b0\u01a1ng. Histamin l\u00e0 m\u1ed9t ch\u1ea5t k\u00edch th\u00edch th\u1ea7n kinh quan tr\u1ecdng trong n\u00e3o ng\u01b0\u1eddi (c\u00f3 t\u1edbi 64,000 neuron s\u1ea3n xu\u1ea5t histamin), b\u1eaft ngu\u1ed3n t\u1eeb nh\u00e2n tuberomammillary. K\u00edch th\u00edch th\u1ee5 th\u1ec3 H1 trong t\u1ea5t c\u1ea3 c\u00e1c ph\u1ea7n ch\u00ednh c\u1ee7a n\u00e3o, ti\u1ec3u n\u00e3o, th\u00f9y sau tuy\u1ebfn y\u00ean v\u00e0 c\u1ed9t s\u1ed1ng l\u00e0m t\u0103ng t\u1ec9nh th\u1ee9c trong chu k\u00ec th\u1ee9c\/ng\u1ee7 nh\u1ecbp sinh h\u1ecdc, c\u1ee7ng c\u1ed1 tr\u00ed nh\u1edb v\u00e0 kh\u1ea3 n\u0103ng h\u1ecdc t\u1eadp, \u0111\u00f3ng vai tr\u00f2 trong c\u00e2n b\u1eb1ng ch\u1ea5t l\u1ecfng trong c\u01a1 th\u1ec3, \u1ee9c ch\u1ebf th\u00e8m \u0103n, ki\u1ec3m so\u00e1t nhi\u1ec7t \u0111\u1ed9 c\u01a1 th\u1ec3, ki\u1ec3m so\u00e1t h\u1ec7 th\u1ed1ng tim m\u1ea1ch v\u00e0 can thi\u1ec7p v\u00e0o s\u1ef1 gi\u1ea3i ph\u00f3ng hormon h\u01b0\u1edbng v\u1ecf th\u01b0\u1ee3ng th\u1eadn (ACTH) v\u00e0 b-endorphin t\u1eeb tuy\u1ebfn y\u00ean. Kh\u00f4ng c\u00f3 g\u00ec ng\u1ea1c nhi\u00ean khi c\u00e1c thu\u1ed1c kh\u00e1ng histamin th\u1ebf h\u1ec7 \u0111\u1ea7u \u0111i qua h\u00e0ng r\u00e0o m\u00e1u n\u00e3o can thi\u1ec7p v\u00e0o t\u1ea5t c\u1ea3 c\u00e1c qu\u00e1 tr\u00ecnh n\u00e0y.<\/p>\n
Khi \u0111\u01b0\u1ee3c s\u1eed d\u1ee5ng v\u00e0o ban ng\u00e0y, c\u00e1c thu\u1ed1c kh\u00e1ng histamin\u00a0th\u1ebf h\u1ec7 \u0111\u1ea7u ti\u00ean, ngay c\u1ea3 \u1edf li\u1ec1u khuy\u1ebfn c\u00e1o c\u1ee7a nh\u00e0 s\u1ea3n xu\u1ea5t, th\u01b0\u1eddng g\u00e2y\u00a0 an th\u1ea7n, bu\u1ed3n ng\u1ee7, m\u1ec7t m\u1ecfi, gi\u1ea3m kh\u1ea3 n\u0103ng t\u1eadp trung v\u00e0 tr\u00ed nh\u1edb.\u00a0C\u00e1c thu\u1ed1c n\u00e0y l\u00e0m t\u0103ng \u0111\u1ed9 tr\u1ec5 kh\u1edfi \u0111\u1ea7u c\u1ee7a gi\u1ea5c ng\u1ee7 REM (gi\u1ea5c ng\u1ee7 m\u1eaft chuy\u1ec3n \u0111\u1ed9ng nhanh) v\u00e0 gi\u1ea3m th\u1eddi gian gi\u1ea5c ng\u1ee7 REM. \u0110\u1eb7c bi\u1ec7t v\u1edbi c\u00e1c thu\u1ed1c c\u00f3 th\u1eddi gian b\u00e1n h\u1ee7y d\u00e0i th\u00ec c\u00e1c t\u00e1c d\u1ee5ng ph\u1ee5 c\u00f2n k\u00e9o d\u00e0i \u0111\u1ebfn s\u00e1ng h\u00f4m sau.<\/p>\n
Trong m\u1ed9t s\u1ed1 tr\u01b0\u1eddng h\u1ee3p ng\u01b0\u1eddi ta c\u0169ng l\u1ee3i d\u1ee5ng t\u00e1c d\u1ee5ng kh\u00f4ng mong mu\u1ed1n c\u1ee7a thu\u1ed1c \u0111\u1ec3 s\u1eed d\u1ee5ng cho nh\u1eefng m\u1ee5c \u0111\u00edch kh\u00e1c nh\u01b0: l\u00e0m thu\u1ed1c ch\u1ed1ng n\u00f4n, thu\u1ed1c ch\u1ed1ng lo\u1ea1n th\u1ea7n, thu\u1ed1c ch\u1ed1ng say t\u00e0u xe, thu\u1ed1c ti\u1ec1n m\u00ea…<\/p>\n
M\u1ed9t s\u1ed1 th\u1eed nghi\u1ec7m l\u00e2m s\u00e0ng<\/h2>\n
M\u1ed9t nghi\u00ean c\u1ee9u t\u1ea1i Ba Lan theo nh\u00f3m ng\u1eabu nhi\u00ean, song song, m\u00f9 \u0111\u00f4i so s\u00e1nh hi\u1ec7u qu\u1ea3 v\u00e0 an to\u00e0n c\u1ee7a bilastine 20 mg so v\u1edbi cetirizine 10 mg v\u00e0 gi\u1ea3 d\u01b0\u1ee3c trong \u0111i\u1ec1u tr\u1ecb vi\u00eam m\u0169i d\u1ecb \u1ee9ng theo m\u00f9a (h\u00ecnh d\u01b0\u1edbi). C\u00e1c th\u00f4ng s\u1ed1 th\u1ec3 hi\u1ec7n tr\u00ean \u1ea3nh. C\u00e1c t\u00e1c gi\u1ea3: Kuna P, Bachert C, Nowacki Z, van Cauwenberge P, Agache I, Fouquert L, Roger A, Sologuren A v\u00e0 Valiente R.<\/p>\n
$\"So$
\u1ea2nh: So s\u00e1nh hi\u1ec7u qu\u1ea3 v\u00e0 an to\u00e0n c\u1ee7a bilastine 20 mg so v\u1edbi cetirizine 10 mg v\u00e0 gi\u1ea3 d\u01b0\u1ee3c tr\u00ean t\u00e1c d\u1ee5ng ph\u1ee5 bu\u1ed3n ng\u1ee7 trong \u0111i\u1ec1u tr\u1ecb vi\u00eam m\u0169i d\u1ecb \u1ee9ng theo m\u00f9a.<\/figcaption><\/figure>\n
K\u1ebft qu\u1ea3 cho th\u1ea5y vai tr\u00f2 c\u1ee7a bilastine trong vi\u1ec7c qu\u1ea3n l\u00fd vi\u00eam m\u0169i d\u1ecb \u1ee9ng v\u00e0 n\u1ed5i m\u00e0y \u0111ay nh\u01b0 m\u1ed9t lo\u1ea1i thu\u1ed1c kh\u00e1ng histamin H1 th\u1ebf h\u1ec7 th\u1ee9 hai kh\u00f4ng an th\u1ea7n. Bilastine c\u00f3 m\u1ed9t h\u1ed3 s\u01a1 an to\u00e0n c\u1ef1c k\u1ef3 thu\u1eadn l\u1ee3i, kh\u00f4ng \u1ea3nh h\u01b0\u1edfng \u0111\u1ebfn kh\u1ea3 n\u0103ng l\u00e1i xe v\u00e0 v\u1eadn h\u00e0nh m\u00e1y m\u00f3c, kh\u00f4ng c\u00f3 b\u1ea5t k\u1ef3 t\u01b0\u01a1ng t\u00e1c v\u1edbi c\u00e1c lo\u1ea1i thu\u1ed1c kh\u00e1c ho\u1eb7c r\u01b0\u1ee3u (v\u00ec n\u00f3 kh\u00f4ng chuy\u1ec3n h\u00f3a \u1edf gan), v\u00e0 l\u00e0m gi\u1ea3m bu\u1ed3n ng\u1ee7 (\u1edf b\u1ec7nh nh\u00e2n d\u1ecb \u1ee9ng) ngay c\u1ea3 khi so s\u00e1nh v\u1edbi gi\u1ea3 d\u01b0\u1ee3c. Hi\u1ec7u qu\u1ea3 c\u1ee7a bilastine t\u01b0\u01a1ng \u0111\u01b0\u01a1ng v\u1edbi hi\u1ec7u qu\u1ea3 c\u1ee7a cetirizine, desloratadine v\u00e0 fexofenadine trong vi\u1ec7c l\u00e0m gi\u1ea3m c\u00e1c tri\u1ec7u ch\u1ee9ng vi\u00eam m\u0169i d\u1ecb \u1ee9ng.\u00a0Bilastine c\u1ea3i thi\u1ec7n \u0111\u00e1ng k\u1ec3 ch\u1ea5t l\u01b0\u1ee3ng cu\u1ed9c s\u1ed1ng c\u1ee7a b\u1ec7nh nh\u00e2n vi\u00eam m\u0169i d\u1ecb \u1ee9ng.<\/p>\n
$\"So$
\u1ea2nh: So s\u00e1nh hi\u1ec7u qu\u1ea3 v\u00e0 an to\u00e0n c\u1ee7a bilastine 20 mg so v\u1edbi cetirizine 10 mg v\u00e0 gi\u1ea3 d\u01b0\u1ee3c tr\u00ean t\u00e1c d\u1ee5ng ph\u1ee5 m\u1ec7t m\u1ecfi trong \u0111i\u1ec1u tr\u1ecb vi\u00eam m\u0169i d\u1ecb \u1ee9ng theo m\u00f9a.<\/figcaption><\/figure>\n
\u0110\u1ec3 t\u00ecm hi\u1ec3u th\u00eam v\u1ec1 c\u00e1c th\u1eed nghi\u1ec7m l\u00e2m s\u00e0ng kh\u00e1c, b\u1ea1n \u0111\u1ecdc xem ph\u1ea7n T\u00e0i li\u1ec7u tham kh\u1ea3o<\/em>.<\/p>\n
D\u01b0\u1ee3c \u0111\u1ed9ng h\u1ecdc<\/h2>\n
H\u1ea5p thu:<\/em> Thu\u1ed1c h\u1ea5p thu t\u1ed1t qua \u0111\u01b0\u1eddng ti\u00eau h\u00f3a v\u1edbi sinh kh\u1ea3 d\u1ee5ng thay \u0111\u1ed5i t\u00f9y thu\u1ed1c. V\u1edbi thu\u1ed1c c\u00f3 chuy\u1ec3n h\u00f3a b\u01b0\u1edbc 1 qua gan th\u00ec sinh kh\u1ea3 d\u1ee5ng F th\u01b0\u1eddng th\u1ea5p (v\u00ed d\u1ee5: chlorpromazine F = 20%, diphenhydramine F = 42-62%). Th\u1eddi gian \u0111\u1ea1t n\u1ed3ng \u0111\u1ed9 \u0111\u1ec9nh trong huy\u1ebft t\u01b0\u01a1ng (T_{max<\/sub>) th\u01b0\u1eddng nhanh, d\u01b0\u1edbi 3 gi\u1edd. M\u1ed9t s\u1ed1 thu\u1ed1c d\u01b0\u1edbi 1 gi\u1edd.<\/p>\n}
Ph\u00e2n b\u1ed1:<\/em> T\u1ec9 l\u1ec7 thu\u1ed1c g\u1eafn v\u1edbi protein huy\u1ebft t\u01b0\u01a1ng thay \u0111\u1ed5i nh\u01b0ng nh\u00ecn chung th\u01b0\u1eddng cao tr\u00ean 90%. Th\u1ebf t\u00edch ph\u00e2n b\u1ed1 V\u00ad_{d<\/sub> \u0111a s\u1ed1 thay \u0111\u1ed5i, c\u00f3 th\u1ec3 dao \u0111\u1ed9ng t\u1eeb 0.4 L\/kg \u0111\u1ebfn 22 L\/kg.<\/p>\n}
Chuy\u1ec3n h\u00f3a:<\/em> Ph\u1ea7n l\u1edbn c\u00e1c thu\u1ed1c \u0111\u01b0\u1ee3c chuy\u1ec3n h\u00f3a t\u1ea1i gan b\u1eb1ng nhi\u1ec1u ki\u1ec3u ph\u1ea3n \u1ee9ng kh\u00e1c nhau: oxy h\u00f3a \u2013 kh\u1eed, li\u00ean h\u1ee3p, O-dealkylation h\u00f3a… H\u1ec7 enzyme chuy\u1ec3n h\u00f3a l\u00e0 CYP450, ch\u1ee7 y\u1ebfu l\u00e0 CYP3A4 v\u00e0 m\u1ed9t s\u1ed1 \u0111\u1ed3ng d\u1ea1ng c\u1ee7a n\u00f3.<\/p>\n
Th\u1ea3i tr\u1eeb: <\/em>Th\u1eddi gian b\u00e1n th\u1ea3i c\u1ee7a c\u00e1c thu\u1ed1c thay \u0111\u1ed5i nhi\u1ec1u (h\u00ecnh d\u01b0\u1edbi). Th\u00f4ng th\u01b0\u1eddng th\u1eddi gian t\u00e1c d\u1ee5ng c\u1ee7a c\u00e1c thu\u1ed1c th\u1ebf h\u1ec7 hai l\u00e2u h\u01a1n th\u1ebf h\u1ec7 m\u1ed9t (th\u01b0\u1eddng k\u00e9o d\u00e0i c\u1ea3 ng\u00e0y). Thu\u1ed1c \u0111\u01b0\u1ee3c b\u00e0i xu\u1ea5t theo hai \u0111\u01b0\u1eddng ch\u00ednh l\u00e0 n\u01b0\u1edbc ti\u1ec3u v\u00e0 ph\u00e2n, trong \u0111\u00f3 \u0111\u01b0\u1eddng n\u01b0\u1edbc ti\u1ec3u th\u01b0\u1eddng chi\u1ebfm \u01b0u th\u1ebf.<\/p>\n
$\"Th\u1eddi$
\u1ea2nh: Th\u1eddi gian b\u00e1n th\u1ea3i m\u1ed9t s\u1ed1 thu\u1ed1c kh\u00e1ng histamin H1.<\/figcaption><\/figure>\n
Ch\u1ec9 \u0111\u1ecbnh<\/h2>\n
Thu\u1ed1c \u0111\u01b0\u1ee3c ch\u1ec9 \u0111\u1ecbnh trong c\u00e1c tr\u01b0\u1eddng h\u1ee3p:<\/p>\n
\n
M\u00e0y \u0111ay.<\/li>\n
Vi\u00eam m\u0169i d\u1ecb \u1ee9ng.<\/li>\n
Vi\u00eam k\u1ebft m\u1ea1c d\u1ecb \u1ee9ng.<\/li>\n
Vi\u00eam da ti\u1ebfp x\u00fac.<\/li>\n
Ng\u1eeba do vi\u00eam da d\u1ecb \u1ee9ng, do c\u00f4n tr\u00f9ng c\u1eafn.<\/li>\n
Ph\u00f9 m\u1ea1ch.<\/li>\n
Bu\u1ed3n n\u00f4n.<\/li>\n
Lo\u1ea1n th\u1ea7n \u0111i\u1ec3n h\u00ecnh.<\/li>\n
Ti\u1ec1n m\u00ea.<\/li>\n
Say t\u00e0u xe.<\/li>\n
Ho (ph\u1ed1i h\u1ee3p v\u1edbi thu\u1ed1c gi\u1ea3m ho trung \u01b0\u01a1ng).<\/li>\n
G\u00e2y t\u00ea t\u1ea1i ch\u1ed7.<\/li>\n<\/ul>\n
Li\u1ec1u d\u00f9ng c\u1ee5 th\u1ec3 t\u00f9y thu\u1ed1c v\u00e0 ch\u1ec9 \u0111\u1ecbnh.<\/p>\n
T\u00e1c d\u1ee5ng ph\u1ee5<\/h2>\n
Th\u1ebf h\u1ec7 m\u1ed9t:<\/em> Thu\u1ed1c th\u1ebf h\u1ec7 \u0111\u1ea7u ti\u00ean c\u00f3 nhi\u1ec1u t\u00e1c d\u1ee5ng ph\u1ee5 do k\u00e9m ch\u1ecdn l\u1ecdc tr\u00ean th\u1ee5 th\u1ec3 H1 v\u00e0 c\u00f3 th\u1ec3 qua \u0111\u01b0\u1ee3c h\u00e0ng r\u00e0o m\u00e1u n\u00e3o. T\u00e1c d\u1ee5ng ph\u1ee5 th\u01b0\u1eddng g\u1eb7p nh\u1ea5t l\u00e0 an th\u1ea7n, g\u00e2y bu\u1ed3n ng\u1ee7 \u1edf b\u1ec7nh nh\u00e2n. C\u00e1c t\u00e1c d\u1ee5ng ph\u1ee5 kh\u00e1c c\u00f2n c\u00f3 nh\u1ee9c \u0111\u1ea7u, ch\u00f3ng m\u1eb7t, \u00f9 tai, kh\u00f4 mi\u1ec7ng, nh\u00ecn m\u1edd, t\u00e1o b\u00f3n, ti\u00eau ch\u1ea3y, b\u00ed ti\u1ec3u, m\u1ea5t \u0111i\u1ec1u h\u00f2a, lo l\u1eafng, t\u0103ng c\u00e2n (do t\u0103ng c\u1ea3m gi\u00e1c ngon mi\u1ec7ng), \u0111\u00e1nh tr\u1ed1ng ng\u1ef1c, h\u1ea1 huy\u1ebft \u00e1p t\u01b0 th\u1ebf, nh\u1ecbp tim nhanh ph\u1ea3n x\u1ea1, \u1ea3o gi\u00e1c, r\u1ed1i lo\u1ea1n t\u00e2m th\u1ea7n…<\/p>\n
Th\u1ebf h\u1ec7 hai:<\/em> Thu\u1ed1c th\u1ebf h\u1ec7 n\u00e0y ch\u1ecdn l\u1ecdc tr\u00ean th\u1ee5 th\u1ec3 H1 h\u01a1n v\u00e0 \u00edt qua h\u00e0ng r\u00e0o m\u00e1u n\u00e3o h\u01a1n n\u00ean \u00edt g\u00e2y bu\u1ed3n ng\u1ee7 h\u01a1n th\u1ebf h\u1ec7 m\u1ed9t. C\u00e1c t\u00e1c d\u1ee5ng ph\u1ee5 c\u00f3 th\u1ec3 g\u1eb7p l\u00e0 bu\u1ed3n ng\u1ee7, nh\u1ee9c \u0111\u1ea7u, kh\u00f4 mi\u1ec7ng, bu\u1ed3n n\u00f4n.<\/p>\n
\u0110\u1ed9c t\u00ednh tr\u00ean tim m\u1ea1ch: astemizole v\u00e0 terfenadine c\u00f3 th\u1ec3 g\u00e2y k\u00e9o d\u00e0i kho\u1ea3ng QT, c\u00f3 kh\u1ea3 n\u0103ng g\u00e2y r\u1ed1i lo\u1ea1n nh\u1ecbp th\u1ea5t nghi\u00eam tr\u1ecdng nh\u01b0 xo\u1eafn \u0111\u1ec9nh. Hai thu\u1ed1c n\u00e0y \u0111\u00e3 kh\u00f4ng c\u00f2n \u0111\u01b0\u1ee3c ch\u1ea5p thu\u1eadn \u1edf h\u1ea7u h\u1ebft c\u00e1c n\u01b0\u1edbc. M\u1ed9t s\u1ed1 thu\u1ed1c th\u1ebf h\u1ec7 \u0111\u1ea7u nh\u01b0 promethazine, brompheniramine v\u00e0 diphenhydramine c\u0169ng c\u00f3 li\u00ean quan \u0111\u1ebfn QT k\u00e9o d\u00e0i ho\u1eb7c lo\u1ea1n nh\u1ecbp tim khi d\u00f9ng li\u1ec1u l\u1edbn ho\u1eb7c qu\u00e1 li\u1ec1u. C\u00e1c thu\u1ed1c sau kh\u00f4ng c\u00f3 t\u00e1c d\u1ee5ng \u0111\u00e1ng k\u1ec3 tr\u00ean tim tr\u00ean l\u00e2m s\u00e0ng: loratadine, fexofenadine, mizolastine, ebastine, azelastine, cetirizine, desloratadine v\u00e0 levocetirizine.<\/p>\n
L\u01b0u \u00fd v\u00e0 th\u1eadn tr\u1ecdng<\/h2>\n
Th\u1eadn tr\u1ecdng v\u1edbi ph\u1ee5 n\u1eef c\u00f3 thai v\u00e0 cho con b\u00fa, m\u1ed9t s\u1ed1 thu\u1ed1c c\u00f3 th\u1ec3 g\u00e2y qu\u00e1i thai nh\u01b0 cyclizin v\u00e0 d\u1eabn xu\u1ea5t.<\/p>\n
Th\u1eadn tr\u1ecdng v\u1edbi b\u1ec7nh nh\u00e2n suy gan, th\u1eadn.<\/p>\n
Th\u1eadn tr\u1ecdng v\u1edbi t\u00e1c d\u1ee5ng ph\u1ee5 tr\u00ean th\u1ea7n kinh trung \u01b0\u01a1ng c\u1ee7a thu\u1ed1c, \u0111\u1eb7c bi\u1ec7t l\u00e0 th\u1ebf h\u1ec7 m\u1ed9t: th\u1eadn tr\u1ecdng khi d\u00f9ng cho ng\u01b0\u1eddi ph\u1ea3i l\u00e1i xe ho\u1eb7c v\u1eadn h\u00e0nh m\u00e1y m\u00f3c, ng\u01b0\u1eddi c\u1ea7n t\u1eadp trung cao \u0111\u1ed9, h\u1ecdc sinh, sinh vi\u00ean trong giai \u0111o\u1ea1n thi c\u1eed…<\/p>\n
Th\u1eadn tr\u1ecdng v\u1edbi b\u1ec7nh nh\u00e2n t\u0103ng nh\u00e3n \u00e1p, t\u1eafc ngh\u1ebdn \u0111\u01b0\u1eddng ni\u1ec7u, ph\u00ec \u0111\u1ea1i ti\u1ec1n li\u1ec7t tuy\u1ebfn, lo\u00e9t d\u1ea1 d\u00e0y, t\u1eafc ngh\u1ebdn m\u00f4n v\u1ecb… v\u1edbi thu\u1ed1c th\u1ebf h\u1ec7 m\u1ed9t.<\/p>\n
Nguy c\u01a1 tri\u1ec7u ch\u1ee9ng ngo\u1ea1i th\u00e1p v\u1edbi c\u00e1c thu\u1ed1c th\u1ebf h\u1ec7 m\u1ed9t.<\/p>\n
Th\u1eadn tr\u1ecdng v\u1edbi thu\u1ed1c c\u00f3 th\u1ec3 g\u00e2y k\u00e9o d\u00e0i kho\u1ea3ng QT, r\u1ed1i lo\u1ea1n nh\u1ecbp tim (\u0111\u00e3 n\u00eau \u1edf tr\u00ean).<\/p>\n
T\u00e1c d\u1ee5ng ch\u1ed1ng n\u00f4n c\u1ee7a thu\u1ed1c th\u1ebf h\u1ec7 m\u1ed9t c\u00f3 th\u1ec3 l\u00e0m m\u1edd \u0111\u1ed9c t\u00ednh c\u1ee7a thu\u1ed1c h\u00f3a tr\u1ecb li\u1ec7u ung th\u01b0.<\/p>\n
Tr\u00e1nh s\u1eed d\u1ee5ng chlorpromazine \u1edf tr\u1ebb em nghi ng\u1edd m\u1eafc h\u1ed9i ch\u1ee9ng Reye.<\/p>\n
M\u1ed9t s\u1ed1 thu\u1ed1c nh\u01b0 diphenhydramine l\u00e0m t\u0103ng nguy c\u01a1 t\u00e9 ng\u00e3 \u1edf ng\u01b0\u1eddi cao tu\u1ed5i.<\/p>\n
T\u01b0\u01a1ng t\u00e1c thu\u1ed1c<\/h2>\n
D\u00f9ng c\u00f9ng r\u01b0\u1ee3u, thu\u1ed1c \u1ee9c ch\u1ebf th\u1ea7n kinh trung \u01b0\u01a1ng (benzodiazepin, barbiturat, opioid…): t\u0103ng t\u00e1c d\u1ee5ng an th\u1ea7n c\u1ee7a thu\u1ed1c kh\u00e1ng histamin H1, \u0111\u1eb7c bi\u1ec7t l\u00e0 th\u1ebf h\u1ec7 m\u1ed9t.<\/p>\n
D\u00f9ng c\u00f9ng thu\u1ed1c k\u00edch th\u00edch th\u1ea7n kinh trung \u01b0\u01a1ng (cafein, camphor…): \u0111\u1ed1i kh\u00e1ng t\u00e1c d\u1ee5ng \u1ee9c ch\u1ebf th\u1ea7n kinh trung \u01b0\u01a1ng c\u1ee7a thu\u1ed1c kh\u00e1ng histamin H1, \u0111\u1eb7c bi\u1ec7t l\u00e0 th\u1ebf h\u1ec7 1.<\/p>\n
D\u00f9ng c\u00f9ng thu\u1ed1c kh\u00e1ng cholinergic (atropin, scopolamin, thu\u1ed1c ch\u1ed1ng tr\u1ea7m c\u1ea3m ba v\u00f2ng TCA, IMAO, thu\u1ed1c \u0111i\u1ec1u tr\u1ecb Parkinson…): t\u0103ng t\u00e1c d\u1ee5ng kh\u00e1ng cholinergic c\u1ee7a thu\u1ed1c kh\u00e1ng histamin H1 (th\u1ebf h\u1ec7 m\u1ed9t).<\/p>\n
D\u00f9ng c\u00f9ng thu\u1ed1c c\u01b0\u1eddng ph\u00f3 giao c\u1ea3m (pilocarpin, neostigmin…): \u0111\u1ed1i kh\u00e1ng t\u00e1c d\u1ee5ng kh\u00e1ng cholinergic c\u1ee7a thu\u1ed1c kh\u00e1ng histamin H1 (th\u1ebf h\u1ec7 m\u1ed9t).<\/p>\n
D\u00f9ng c\u00f9ng thu\u1ed1c h\u1ea1 huy\u1ebft \u00e1p: nguy c\u01a1 g\u00e2y h\u1ea1 huy\u1ebft \u00e1p qu\u00e1 m\u1ee9c (th\u1ebf h\u1ec7 m\u1ed9t).<\/p>\n
Loratadine d\u00f9ng c\u00f9ng r\u01b0\u1ee3u benzyl: c\u00f3 th\u1ec3 g\u00e2y h\u1ed9i ch\u1ee9ng th\u1edf g\u1ea5p, nguy c\u01a1 g\u00e2y t\u1eed vong.<\/p>\n
Ch\u1ed1ng ch\u1ec9 \u0111\u1ecbnh<\/h2>\n
Qu\u00e1 m\u1eabn c\u1ea3m v\u1edbi b\u1ea5t c\u1ee9 th\u00e0nh ph\u1ea7n n\u00e0o c\u1ee7a thu\u1ed1c.<\/p>\n
Ng\u1ed9 \u0111\u1ed9c thu\u1ed1c \u1ee9c ch\u1ebf th\u1ea7n kinh trung \u01b0\u01a1ng (thu\u1ed1c m\u00ea…).<\/p>\n
\u0110ang d\u00f9ng thu\u1ed1c IMAO ho\u1eb7c ng\u1eebng s\u1eed d\u1ee5ng IMAO ch\u01b0a \u0111\u01b0\u1ee3c 14 ng\u00e0y.<\/p>\n
Cyclizin v\u00e0 d\u1eabn xu\u1ea5t b\u1ecb ch\u1ed1ng ch\u1ec9 \u0111\u1ecbnh cho ph\u1ee5 n\u1eef c\u00f3 thai.<\/p>\n
<\/p>\n
T\u00e0i li\u1ec7u tham kh\u1ea3o:<\/em><\/p>\n
https:\/\/www.ncbi.nlm.nih.gov\/pmc\/articles\/PMC5183790\/<\/a><\/p>\n
https:\/\/www.ncbi.nlm.nih.gov\/pmc\/articles\/PMC3667286\/<\/a><\/p>\n
\u00a0<\/em><\/p>\n","protected":false},"excerpt":{"rendered":"
L\u1ecbch s\u1eed nghi\u00ean c\u1ee9u v\u00e0 ph\u00e1t tri\u1ec3n Thu\u1ed1c kh\u00e1ng histamin H1 l\u00e0 thu\u1ed1c ng\u0103n ch\u1eb7n ho\u1ea1t \u0111\u1ed9ng c\u1ee7a histamin \u1edf th\u1ee5 th\u1ec3 H1. H\u1ea7u h\u1ebft c\u00e1c thu\u1ed1c kh\u00e1ng histamin H1 \u0111\u1ec1u l\u00e0 ch\u1ea5t ch\u1ee7 v\u1eadn ng\u01b0\u1ee3c H1-receptor ch\u1ee9 kh\u00f4ng ph\u1ea3i l\u00e0 ch\u1ea5t \u0111\u1ed1i kh\u00e1ng. \u0110\u1ec3 hi\u1ec3u v\u1ec1 thu\u1ed1c kh\u00e1ng histamin H1, c\u1ea7n \u0111\u00e1nh gi\u00e1 t\u00ecnh […]\n","protected":false},"author":1,"featured_media":18715,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[1],"tags":[],"class_list":["post-18705","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-y-te-suc-khoe"],"acf":[],"_links":{"self":[{"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/posts\/18705","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/comments?post=18705"}],"version-history":[{"count":0,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/posts\/18705\/revisions"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/media\/18715"}],"wp:attachment":[{"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/media?parent=18705"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/categories?post=18705"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/vnras.com\/drug\/wp-json\/wp\/v2\/tags?post=18705"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}