Halofantrine
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| Names | |
|---|---|
| Trade names | Halfan |
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| Clinical data | |
| Routes of use | Oral |
| External links | |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a603030 |
| Pharmacokinetics | |
| Protein binding | 60–70% |
| Metabolism | Hepatic (CYP3A4-mediated) |
| Elimination half-life | 6–10 days |
| Identifiers | |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| ATC code | |
| Chemical and physical data | |
| Formula | C26H30Cl2F3NO |
| Molar mass | Templeeti:Val g·mol−1 |
| 3D model (JSmol) | |
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| Ihe ọmụma gbasara ahụike | |
|---|---|
| Aha azụmahịa | Halfan |
| AHFS/Drugs.com | Ihe ọmụma Ọgwụ Ndị Ahịa |
| MedlinePlus | a6030 |
| Ụzọ nchịkwa |
Okwu |
| Koodu ATC |
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| Ihe omuma pharmacokinetic | |
| Njikọ protein | 60–70% |
| Metabolism | Ọrịa imeju (CYP3A4-mediated) |
| <span class="nowrap">ọkara ndụ</span> e wepụrụ | Ụbọchị 6-10 |
| Ihe ndị na-eme ka a mata ya | |
Aha IUPAC
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| Nọmba CAS | |
| [./PubChem#<span style= <abbr title="<nowiki>Compound ID</nowiki>">CID" rel="mw:WikiLink" title="PubChem">PubChem] CID | |
| Ụlọ Akụ̀ Ọgwụ | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| CompTox Dashboard (<abbr title="<nowiki>U.S. Environmental Protection Agency</nowiki>">EPA) | |
| <span title="echa.europa.eu">ECHA InfoCard</span> | 100.067.346 |
| Ihe omuma kemịkal na nke anụ ahụ | |
| Nhazi | C26H30Cl2F3NO |
| Ọkpụkpụ nke ọkpụkpụ | 500.43 g·mol-1 −1 |
| Ihe nlereanya 3D (JSmol) | |
Udo
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InChI
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| (Nnyocha) | |
Halofantrine ọgwụ a na-eji agwọ ịba. Ọdịdị Halofantrine nwere phenanthrene e dochiri anya ya, o nwekwara njikọ ya na ọgwụ mgbochi ịba ahụ bụ quinine na lumefantrine. A na-ere ya dị ka Halfan, a naghị eji halofantrine egbochi ịba n'ụzọ ọbụla, a maghịkwa otu o si arụ ọrụ, ọ bụ ezie na nyocha crystallographic gosiri na ọ na-ejikọta na hematin in vitro, na-atụ aro usoro o nwere ike i si na-arụ ọrụ ya.[1] E gosikwala na Halofantrine na-ejikọta ya na plasmepsin, enzyme na-emebi haemoglobin nke dị iche dịịrị nje ịba.[2]
E mepụtara Halofantrine na SRI International maka Walter Reed Army Institute of Research site site na 1965 ruo 1975 site n'aka otu nke onye na-ahụ maka ọgwụ William Colwell duziri.[3]
Mmeghachi omume ọjọọ Ọ Na-Emeghachi N'ahụ
[dezie | dezie ebe o si]Halofantrine nwere ike ịkpata mgbu afọ, afọ ọsịsa, ịgbọ agbọ, ihe itokasị mmadụ n'ahụ, isi ọwụwa, ọkọ ịkọkasị mmadụ n'ahụ na enzymes imeju dị elu.
Enwere ike ijikọta ya na ọrịa obi.[4] Mmetụta ya kachasị ize ndụ bụ arrhythmias nke obi: halofantrine na-akpata mgbatị QT , a na-ahụkwa mmetụta ọjọọ ya ọbụna na mgbe a ṅụrụ ya otu o kwesịrị.[5] Ya mere, ekwesighi inye ya ndị ọrịa nwere ọrịa obi, ekwesighikwa ijikọta ya na mefloquine. Nnyocha sitere na 2009 na-atụ aro na ọgwụ ahụ dị mma mgbe a na-enye ya n'ụzọ ziri ezi.[6]
Mmeghachi omume ọjọọ ndị ọzọ
[dezie | dezie ebe o si]Iri mkpụrụ osisi grapefruit mgbe a nụrụ ọgwụ ụfọdụ nwere ike ịkpata mmetụta siri ike, ọbụnakwa ọnwụ. Halofantrine e jikọtara ya na mkpụrụ osisi a ma ọ bụ mmiri grapefruit dị ize ndụ. Usoro ịrụ ọrụ ya bụ igbochi CYP3A4, nke dị mkpa iji gbarie ọgwụ ahụ ma wepụ ya n'ahụ. Na-enweghị CYP3A4, ọkwa nke ọgwụ ahụ ga-aghọ ihe na-egbu egbu n'ime ahụ.
Ọmụmụ Ọgwụ a
[dezie | dezie ebe o si]A maghị usoro ọrụ nke halofantrine. Mmikọrọ nke halofantrine n'ahụ na-agbanwe agbanwe, mana ọ na-abawanye mgbe a na-aṅụ ya na nri nwere abụba. N'ihi egwu nke nsị n'ihi mmụba nke halofantrine n'ọbara, e kwesịrị ị na-aṅụ halofantrine n'afọ efu.
Ogo Plasma na-arị elu na awa iri na isii na ọkara ndụ nke ọgwụ ahụ bụ ihe dịka ụbọchị anọ.
Ojiji Ya
[dezie | dezie ebe o si]A na-eji Halofantrine agwọ ịba naanị. A naghị eji ya egbochi ịba (prophylaxis) n'ihi ihe ize ndụ nke nsị na mmịkọrọ ya n'ahụ nke a na-apụghị ịdabere na ya.
Otu A Ga-Esi na-aṅụ Ya
[dezie | dezie ebe o si]Ndị okenye: ịṅụ 500mg ugboro atọ nke ọbụla n'ime ha ma awa isii gachaa. A ga-aṅụ Halofantrine n'afọ efu.
Ozi mmepụta na ọdịdị Ya
[dezie | dezie ebe o si]Halfan (GlaxoSmithKline) dị dịka mbadamba mkpụrụ ọgwụ 250 mg. Usoro ọgwụgwọ zuru oke (mbadamba mkpụrụ ọgwụ isii) na-efu US $ 1.40 na mba ndị na-emepe emepe. Halofantrine adịghị na UK ma ọ bụ US.
Edensibịa
[dezie | dezie ebe o si]- ↑ "The crystal structure of halofantrine-ferriprotoporphyrin IX and the mechanism of action of arylmethanol antimalarials". J. Inorg. Biochem. 102 (8): 1660–7. 2008. doi:10.1016/j.jinorgbio.2008.04.001. PMID 18508124.
- ↑ "Discovery of plasmepsin inhibitors by fragment-based docking and consensus scoring" (PDF). ChemMedChem. 4 (8): 1317–26. 2009. doi:10.1002/cmdc.200900078. PMID 19472268. Retrieved 2019-04-08.
- ↑ Nielson, Donald (2006). A Heritage of Innovation: SRI's First Half Century. Menlo Park, California: SRI International. pp. 10Templeeti:Hyphen3–10Templeeti:Hyphen5. ISBN 978-0974520810.
- ↑ "Mechanism of cardiotoxicity of halofantrine". Clin. Pharmacol. Ther. 67 (5): 521–9. May 2000. doi:10.1067/mcp.2000.106127. PMID 10824631.
- ↑ "Block of wild-type and inactivation-deficient human ether-a-go-go-related gene K+ channels by halofantrine". Naunyn-Schmiedeberg's Arch. Pharmacol. 370 (6): 484–91. 2004. doi:10.1007/s00210-004-0995-5. PMID 15558243.
- ↑ "Fatal cardiotoxicity related to halofantrine: a review based on a worldwide safety data base". Malaria Journal. 8. 2009. doi:10.1186/1475-2875-8-289. PMID 20003315.
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