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Mefloquine
drug data and news
Mefloquine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Mefloquine | ||
| Brand Names/Synonyms | CHEMBANK1387; Lariam; Mefloquine; Mefloquine Hcl; Mefloquinone | ||
| Indication | For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible Plasmodium falciparum strains | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Mefloquine is an antimalarial agent which acts as a blood schizonticide. Mefloquine is active against the erythrocytic stages of Plasmodium species. However, the drug has no effect against the exoerythrocytic (hepatic) stages of the parasite. Mefloquine is effective against malaria parasites resistant to chloroquine. | ||
| Mechanism Of Action | Mefloquine interferes with transportation of haemoglobin products and other substances from the host cell to the parasite’s food vacuole. Mefloquine specifically has been found to produce swelling of the P. falciparum food vacuoles. It may therefore act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components. | ||
| Mefloquine News (When available) |
Pending issues on policy change Mar 1, 2006 The New Malaria Drug Policy Feb 28, 2006 Feb. 27 - MIP Seminar: ‘Drug Discovery for Malaria, a Novel ... Feb 22, 2006 Health bureau states medical claim limits for Taiwanese tourists Feb 3, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Antimalarials; ATC:P01BC02 | ||
| Absorption | Well absorbed from gastrointestinal tract. Bioavailability is about 85% | ||
| Interactions | Interactions for Mefloquine: Drug-drug interactions with Mefloquine have not been explored in detail. There is one report of cardiopulmonary arrest, with full recovery, in a patient who was taking a beta blocker (propranolol). The effects of Mefloquineuine on the compromised cardiovascular system have not been evaluated. The benefits of Mefloquine therapy should be weighed against the possibility of adverse effects in patients with cardiac disease. Because of the danger of a potentially fatal prolongation of the QTc interval, halofantrine must not be given simultaneously with or subsequent to Mefloquine. Concomitant administration of Mefloquine and other related compounds (eg, quinine, quinidine and chloroquine) may produce electrocardiographic abnormalities and increase the risk of convulsions. If these drugs are to be used in the initial treatment of severe malaria, Mefloquine administration should be delayed at least 12 hours after the last dose. There is evidence that the use of halofantrine after Mefloquineuine causes a significant lengthening of the QTc interval. Clinically significant QTc prolongation has not been found with Mefloquineuine alone. This appears to be the only clinically relevant interaction of this kind with Mefloquine, although theoretically, coadministration of other drugs known to alter cardiac conduction (eg, anti-arrhythmic or beta-adrenergic blocking agents, calcium channel blockers, antihistamines or H1-blocking agents, tricyclic antidepressants and phenothiazines) might also contribute to a prolongation of the QTc interval. There are no data that conclusively establish whether the concomitant administration of Mefloquineuine and the above listed agents has an effect on cardiac function. In patients taking an anticonvulsant (eg, valproic acid, carbamazepine, phenobarbital or phenytoin), the concomitant use of Mefloquine may reduce seizure control by lowering the plasma levels of the anticonvulsant. Therefore, patients concurrently taking antiseizure medication and Mefloquine should have the blood level of their antiseizure medication monitored and the dosage adjusted appropriately. When Mefloquine is taken concurrently with oral live typhoid vaccines, attenuation of immunization cannot be excluded. Vaccinations with attenuated live bacteria should therefore be completed at least 3 days before the first dose of Mefloquine. No other drug interactions are known. Nevertheless, the effects of Mefloquine on travelers receiving comedication, particularly diabetics or patients using anticoagulants, should be checked before departure. In clinical trials, the concomitant administration of sulfadoxine and pyrimethamine did not alter the adverse reaction profile. | ||
| Toxicity | It is known to cause severe depression, anxiety, paranoia, nightmares, vestibular (balance) damage and CNS problems. LD50 = 880 mg/kg (oral, rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | ||
| Chemical Formula | C17H16F6N2O | ||
| Molecular Weight | 378.312 g/mol | ||
| Smiles String | C1CCNC(C1)C(C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O | ||
| Melting Point | Not Available | ||
| Water Solubility | 5 mg/mL (HCl salt) | ||
| State | Solid | ||
| LogP/Hphobicity | 3.811 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic (partial); metabolized primarily to the carboxylic acid metabolite | ||
| Half Life | 2 and 4 weeks | ||
| Protein Binding [%] | 98% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Mefloquine.html http://www.rxlist.com/cgi/generic2/mefloq.htm http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00300 | ||
| CAS Registry Number | 53230-10-7 | ||
| KEGG Compound ID | C07633 | ||
| PubChem ID | SID:9835 | ||
| PharmGKB ID | PA450348 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2244366 |
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