Malar J. Population pharmacokinetics and pharmacodynamic considerations of amodiaquine and desethylamodiaquine in Kenyan adults with uncomplicated malaria receiving artesunate—amodiaquine combination therapy.
Effects of amodiaquine and artesunate on sulphadoxine—pyrimethamine pharmacokinetic parameters in children under five in Mali.
The disposition of oral amodiaquine in Papua New Guinean children with falciparum malaria. Population pharmacokinetic and pharmacodynamic modeling of amodiaquine and desethylamodiaquine in women with Plasmodium vivax malaria during and after pregnancy.
Anti-malarial drug safety information obtained through routine monitoring in a rural district of south-western Senegal. Safety of artemisinin-based combination therapies in Nigeria: a cohort event monitoring study. Drug Saf. Eur J Drug Metab Pharmacokinet. A randomized comparison of dihydroartemisinin—piperaquine and artesunate—amodiaquine combined with primaquine for radical treatment of vivax malaria in Sumatera, Indonesia. J Infect Dis. Frequency of severe neutropenia associated with amodiaquine prophylaxis against malaria.
Reversible binocular visual loss in temporal association with artesunate—amodiaquine treatment in a child on mefloquine chemoprophylaxis.
Ghana Med J. High risk of neutropenia in HIV-infected children following treatment with artesunate plus amodiaquine for uncomplicated malaria in Uganda. Clin Infect Dis. Guevart E, Aguemon A. Deux hepatites fulminantes survenues au cours d'un traitement curatif par l'association artesunate—amodiaquine. Med Mal Infect. Electrocardiographic study in Ghanaian children with uncomplicated malaria, treated with artesunate—amodiaquine or artemether—lumefantrine. McEwen J. Artesunate- and amodiaquine-associated extrapyramidal reactions: a series of 49 cases in VigiBase.
PLoS One. Intermittent preventive treatment of malaria provides substantial protection against malaria in children already protected by an insecticide-treated bednet in Mali: a randomised, double-blind, placebo-controlled trial.
PLoS Med. Intermittent preventive treatment of malaria provides substantial protection against malaria in children already protected by an insecticide-treated bednet in Burkina Faso: a randomised, double-blind, placebo-controlled trial.
A trial of the efficacy, safety and impact on drug resistance of four drug regimens for seasonal intermittent preventive treatment for malaria in Senegalese children. Use of weight-for-age-data to optimize tablet strength and dosing regimens for a new fixed-dose artesunate—amodiaquine combination for treating falciparum malaria.
Bull World Health Organ. Although artemether was superior to quinine in the treatment of severe malaria in adults but not in children , its absorption is unpredictable, which may affect treatment responses in the most severely ill patients. Artemether is an alternative for pre-referral treatment of severe malaria in adults when parenteral artesunate is not available and in children when neither parenteral nor rectal artesunate is available.
Artemether is also used in a fixed-dose oral combination with lumefantrine see A5. Pharmacokinetics Table A5. Figure A5. Safety Adverse effects Artemether is generally very well tolerated after both oral and intramuscular administration.
Contraindications Artemether is contraindicated in patients with known hypersensitivity to any artemisinin derivative.
Cautions A marked increase in the concentration of artemether in the cerebrospinal fluid of patients with meningitis was observed, prompting researchers to advise caution in treating patients with signs of meningitis 2 , 10 , Drug interactions See Table A5. Current perspectives on the mechanism of action of artemisinins. Int J Parasitol. Comparative pharmacokinetics of intramuscular artesunate and artemether in patients with severe falciparum malaria.
The disposition of intramuscular artemether in children with cerebral malaria; a preliminary study. Pharmacokinetics and bioavailability of oral and intramuscular artemether. Pharmacokinetics of intramuscular artemether in patients with severe falciparum malaria with or without acute renal failure.
Artesunate suppositories versus intramuscular artemether for treatment of severe malaria in children in Papua New Guinea. Dose-finding and efficacy study for i. Population pharmacokinetics of artemether and dihydroartemisinin following single intramuscular dosing of artemether in African children with severe falciparum malaria. Artemether bioavailability after oral or intramuscular administration in uncomplicated falciparum malaria. Meningeal inflammation increases artemether concentrations in cerebrospinal fluid in Papua New Guinean children treated with intramuscular artemether.
Severe allergic reactions to oral artesunate: a report of two cases. Artemether-lumefantrine may also be used as follow-on, but not initial, treatment in severe malaria when the patient is well enough to take oral medication. Structure and mechanism of action For artemether: See A5.
Pharmacokinetics The pharmacokinetic parameters of artemether—lumefantrine are presented in Table A5. Safety Adverse events Artemether—lumefantrine has a wide therapeutic index and is generally well tolerated, with reported side-effects such as nausea, dizziness and headache that are not easily distinguishable from symptoms of acute malaria 13 , 28 , 32 — Contraindications Artemether—lumefantrine should not to be administered to patients with known hypersensitivity to either artemether or lumefantrine.
Dosage recommendations Formulations currently available: Dispersible or standard tablets containing 20 mg of artemether and mg of lumefantrine in a fixed-dose combination formulation. Clinical pharmacology of artemisinin-based combination therapies.
Clin Pharmacokin. Clinical pharmacokinetics and pharmacodynamics and pharmacodynamics of artemether—lumefantrine. How much fat is necessary to optimize lumefantrine oral bioavailability? Trop Med Int Health. Comparable lumefantrine oral bioavailability when co-administered with oil-fortified maize porridge or milk in healthy volunteers. Basic Clin Pharmacol Toxicol. Pharmacokinetic study of artemether—lumefantrine given once daily for the treatment of uncomplicated multidrug-resistant falciparum malaria.
The effect of food consumption on lumefantrine bioavailability in African children receiving artemether—lumefantrine crushed or dispersible tablets Coartem for acute uncomplicated Plasmodium falciparum malaria.
Supervised versus unsupervised antimalarial treatment with six-dose artemether—lumefantrine: pharmacokinetic and dosage-related findings from a clinical trial in Uganda. Pharmacokinetic and pharmacodynamic characteristics of a new pediatric formulation of artemether—lumefantrine in African children with uncomplicated Plasmodium falciparum malaria. Pharmacokinetics and pharmacodynamics of lumefantrine benflumetol in acute falciparum malaria.
Population pharmacokinetics and pharmacodynamics of artemether and lumefantrine during combination treatment in children with uncomplicated falciparum malaria in Tanzania. A clinical and pharmacokinetic trial of six doses of artemether—lumefantrine for multidrug-resistant Plasmodium falciparum malaria in Thailand. Am J Trop Med Hyg. Comparison of bioavailability between the most available generic tablet formulation containing artemether and lumefantrine on the Tanzanian market and the innovator's product.
Pharmacokinetics of benflumetol given as a fixed combination artemether—benflumetol CGP in Thai patients with uncomplicated falciparum malaria. Int J Clin Pharmacol Res. Population pharmacokinetics of artemether, lumefantrine, and their respective metabolites in Papua New Guinean children with uncomplicated malaria. Effect of single nucleotide polymorphisms in cytochrome P isoenzyme and N-acetyltransferase 2 genes on the metabolism of artemisinin-based combination therapies in malaria patients from Cambodia and Tanzania.
Population pharmacokinetics of mefloquine, piperaquine and artemether—lumefantrine in Cambodian and Tanzanian malaria patients. Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria. Int J Antimicrob Agents. The pharmacokinetics of artemether and lumefantrine in pregnant women with uncomplicated falciparum malaria. A randomised controlled trial of artemether—lumefantrine versus artesunate for uncomplicated plasmodium falciparum treatment in pregnancy.
Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda. Population pharmacokinetics of artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda. Population pharmacokinetics of lumefantrine in pregnant women treated with artemether—lumefantrine for uncomplicated Plasmodium falciparum malaria. Molecular and pharmacological determinants of the therapeutic response to artemether—lumefantrine in multidrug-resistant Plasmodium falciparum malaria.
Efficacy of artemether—lumefantrine in area of high malaria endemicity in India and its correlation with blood concentration of lumefantrine. Treatment of acute uncomplicated falciparum malaria with artemether—lumefantrine in nonimmune populations: a safety, efficacy, and pharmacokinetic study. Population pharmacokinetics of lumefantrine in pregnant and nonpregnant women with uncomplicated Plasmodium falciparum malaria in Uganda.
Update on the efficacy, effectiveness and safety of artemether—lumefantrine combination therapy for treatment of uncomplicated malaria. Ther Clin Risk Manage. Desbutyl—lumefantrine is a metabolite of lumefantrine with potent in vitro antimalarial activity that may influence artemether—lumefantrine treatment outcome. Therapeutic efficacy of artemether—lumefantrine and artesunate—mefloquine for treatment of uncomplicated Plasmodium falciparum malaria in Luang Namtha Province, Lao People's Democratic Republic.
Similar efficacy and tolerability of double-dose chloroquine and artemether—lumefantrine for treatment of Plasmodium falciparum infection in Guinea-Bissau: a randomized trial. Efficacy and safety of artemether—lumefantrine dispersible tablets compared with crushed commercial tablets in African infants and children with uncomplicated malaria: a randomised, single-blind, multicentre trial. Comparison of the cardiac effects of the antimalarials co-artemether and halofantrine in healthy participants.
Coartem product information. Artesunate—amodiaquine, artesunate—mefloquine or artesunate—SP are indicated for the treatment of acute uncomplicated P. Structure and mechanism of action Artesunate is a hemisuccinate derivative of dihydroartemisinin, which is obtained by the reduction of artemisinin, a sesquiterpene lactone endoperoxide 1.
Pharmacokinetics The pharmacokinetic parameters of intravenous, intramuscular, rectal and oral artesunate are presented in Table 5. Safety Pregnancy In experimental animals, dose-dependent fetal toxicity was observed after administration of artesunate in the first trimester and was more likely to occur with increased duration of treatment 1. Adverse events Artesunate is generally well-tolerated and has a better safety profile than quinine in severe malaria 34 — Contraindications Artesunate is contraindicated in patients with known hypersensitivity to artesunate or artemisinin derivatives.
Cautions As lower plasma concentrations of artesunate and dihydroartemisinin are reported in young children with severe anaemia , it is important to monitor their response to treatment closely. Guilin Pharmaceuticals. Injectable Artesun Product Information. A pharmacokinetic and pharmacodynamic study of artesunate for vivax malaria. A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria.
Eur J Drug Metab Pharmacokin. Oral bioavailability of dihydroartemisinin in Vietnamese volunteers and in patients with falciparum malaria. Pharmacokinetics and pharmacodynamics of intravenous artesunate during severe malaria treatment in Ugandan adults.
Pharmacokinetics and pharmacodynamics of intravenous artesunate in severe falciparum malaria. Plasma levels of artesunate and dihydroartemisinin in children with Plasmodium falciparum malaria in Gabon after administration of milligram artesunate suppositories. Population pharmacokinetics of intramuscular artesunate in African children with severe malaria: implications for a practical dosing regimen.
Clin Pharmacol Ther. The pharmacokinetic properties of intramuscular artesunate and rectal dihydroartemisinin in uncomplicated falciparum malaria.
Effects of alpha-thalassemia on pharmacokinetics of the antimalarial agent artesunate. Disposition of artesunate and dihydroartemisinin after administration of artesunate suppositories in children from Papua New Guinea with uncomplicated malaria.
Bioavailability and preliminary clinical efficacy of intrarectal artesunate in Ghanaian children with moderate malaria. Pharmacokinetic profiles of artesunate after single intravenous doses at 0. Does artesunate prolong the electrocardiograph QT interval in patients with severe malaria? Intramuscular bioavailability and clinical efficacy of artesunate in Gabonese children with severe malaria.
The pharmacokinetics of intravenous artesunate in adults with severe falciparum malaria. Life-saving rectal artesunate for complicated malaria in children. Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients. Ann Trop Paediatrics.
Investigation of bioavailability, pharmacokinetics and safety of new pediatric formulations of artesunate and mefloquine. Assessment of the effect of mefloquine on artesunate pharmacokinetics in healthy male volunteers. New fixed-dose artesunate—mefloquine formulation against multidrug-resistant Plasmodium falciparum in adults: a comparative phase IIb safety and pharmacokinetic study with standard-dose nonfixed artesunate plus mefloquine.
Pharmacokinetics of two paediatric artesunate mefloquine drug formulations in the treatment of uncomplicated falciparum malaria in Gabon. J Antimicrob Chemother. Population parmacokinetic and pharmacodynamic modelling of artemisinin and mefloquine enantiomers in patients with falciparum malaria.
Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria. Pharmacokinetics and pharmacodynamics of artesunate and dihydroartemisinin following oral treatment in pregnant women with asymptomatic Plasmodium falciparum infections in Kinshasa DRC. Intravenous artesunate for the treatment of severe malaria. Ann Pharmacother. Clinical experience with intravenous quinine, intramuscular artemether and intravenous artesunate for the treatment of severe malaria in Thailand.
Artesunate versus quinine for treatment of severe falciparum malaria: a randomised trial. Efficacy of rectal artesunate compared with parenteral quinine in initial treatment of moderately severe malaria in African children and adults: a randomised study. Artesunate versus quinine in the treatment of severe imported malaria: comparative analysis of adverse events focussing on delayed haemolysis.
Dose-dependent risk of neutropenia after 7-day courses of artesunate monotherapy in Cambodian patients with acute Plasmodium falciparum malaria. Neuropathological assessment of artemether-treated severe malaria. Clinical and neurophysiological study of the effects of multiple doses of artemisinin on brain-stem function in Vietnamese patients.
Nwanjo H, Oze G. Acute hepatotocixity following administration of artesunate in guinea pigs. Internet J Toxicol. Atovaquone—proguanil may also be considered for the treatment of uncomplicated malaria in travellers outside malaria-endemic areas and for use in combination with artesunate and primaquine as an alternative treatment for uncomplicated malaria, where WHO recommmended treatments are not available or not effective.
Safety Pregnancy Atovaquone—proguanil is regarded as safe in pregnancy, as no evidence of adverse effects associated with its use was found in studies in pregnant humans or experimental animals 2 , 7 , 8 , Adverse effects Generally atovaquone—proguanil is well tolerated.
Contraindications Atovaquone—proguanil is contraindicated in patients with known serious hypersensitivity reactions to atovaquone or proguanil. Caution In the elderly, doses should be selected cautiously, taking into account the greater frequency of decreased hepatic, renal or cardiac function, higher systemic exposure to cycloguanil and a greater frequency of concomitant disease or other drug therapy Antiparasitic agent atovaquone.
Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Prolonged protection provided by a single dose of atovaquone—proguanil for the chemoprophylaxis of Plasmodium falciparum malaria in a human challenge model.
Population pharmacokinetics of proguanil in patients with acute P. The pharmacokinetics of atovaquone and proguanil in pregnant women with acute falciparum malaria.
The pharmacokinetics and pharmacodynamics of atovaquone and proguanil for the treatment of uncomplicated falciparum malaria in third-trimester pregnant women. Efficacy and pharmacokinetics of atovaquone and proguanil in children with multidrug-resistant Plasmodium falciparum malaria. Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil Malarone when taken as chemoprophylaxis.
AIDS London. Absence of an interaction between artesunate and atovaquone—proguanil. Malarone tablets and paediatric tablets drug information. Pancytopenia due to proguanil toxicity in a returning traveller with fever. Chloroquine is no longer recommended for prophylaxis against P. Safety Pregnancy At the doses used for treatment or prophylaxis of P.
Adverse effects Chloroquine is generally well tolerated at therapeutic doses. Contraindications Chloroquine is contraindicated in patients with known hypersensitivity to chloroquine or any aminoquinoline compounds. Caution Use with caution in patients with psoriasis, neurological e. From methylene blue to chloroquine: a brief review of the development of an antimalarial therapy.
Parasitol Res. Titus EO. Recent developments in the understanding of the pharmacokinetics and mechanism of action of chloroquine. Ther Drug Monit. Access to hematin: the basis of chloroquine resistance.
Mol Pharmacol. Pharmacokinetics of sequential and simultaneous treatment with the combination chloroquine and sulfadoxine—pyrimethamine in acute uncomplicated Plasmodium falciparum malaria in the Philippines.
The pharmacokinetics and electrocardiographic effects of chloroquine in healthy subjects. Trop Med Parasitol. Pharmacokinetics of chloroquine: saliva and plasma levels relationship.
Krishna S, White NJ. Pharmacokinetics of quinine, chloroquine and amodiaquine. Clinical implications. The pharmacokinetics of chloroquine in healthy Thai subjects and patients with Plasmodium vivax malaria.
The pharmacokinetics of three multiple dose regimens of chloroquine: implications for malaria chemoprophylaxis. Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria.
Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. Population pharmacokinetics of chloroquine and sulfadoxine and treatment response in children with malaria: suggestions for an improved dose regimen.
Effect of chlorpheniramine on the pharmacokinetics of and response to chloroquine of Nigerian children with falciparum malaria. The effect of aspirin, paracetamol and analgin on pharmacokinetics of chloroquine.
Indian J Physiol Pharmacol. Pharmacokinetics of chloroquine in renal insufficiency. Afr J Med Med Sci. Ducharme J, Farinotti R. Clinical pharmacokinetics and metabolism of chloroquine. Focus on recent advancements. Arch Pharmacol Res. The effects of quinine and chloroquine antimalarial treatments in the first trimester of pregnancy.
Pregnancy outcome following first trimester exposure to chloroquine. Am J Perinatol. Chloroquine pharmacokinetics in pregnant and nonpregnant women with vivax malaria. Chloroquine blood concentrations and malaria prophylaxis in Tanzanian women during the second and third trimesters of pregnancy. Pharmacokinetics The pharmacokinetic parameters reported for clindamycin are summarized in Table A5. Safety Studies of reproductive toxicity with clindamycin in experimental animals revealed no evidence of impaired fertility or harm to the fetus.
Adverse events Clindamycin is generally well tolerated after oral administration. Contraindications Clindamycin is contraindicated in patients with known hypersensitivity to clindamycin or lincomycin. Cautions Clindamycin should be used with caution in patients with gastrointestinal diseases as they may be at greater risk for pseudomembranous colitis.
The mechanism of action of macrolides, lincosamides and streptogramin B reveals the nascent peptide exit path in the ribosome. J Mol Biol. Dalacin C product information. Placental transfer of clindamycin and gentamicin in term pregnancy. Am J Obstet Gynecol.
Pharmacokinetics of clindamycin phosphate in the first year of life. J Pediatrics. Pharmacokinetics of intravenous clindamycin in newborn infants. Pediatric Pharmacol New York. Evaluation of gender in the oral pharmacokinetics of clindamycin in humans.
Biopharm Drug Dispos. Population pharmacokinetics of clindamycin orally and intravenously administered in patients with osteomyelitis. Comparative pharmacokinetics and serum inhibitory activity of clindamycin in different dosing regimens. Comparative study of bioavailabilities and pharmacokinetics of clindamycin in healthy volunteers and patients with AIDS. Pharmacokinetics of clindamycin in pregnant women in the peripartum period. Assessment of the pharmacokinetics and dynamics of two combination regimens of fosmidomycin—clindamycin in patients with acute uncomplicated falciparum malaria.
Protein binding of clindamycin in sera of patients with AIDS. Pharmacokinetic parameters Dihydroartemisinin—piperaquine is readily absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 1—3 h for dihydroartemisinin and 3—6 h for piperaquine. Safety Adverse events Overall, dihydroartemisinin—piperaquine was well tolerated in large randomized controlled trials.
Contraindications Dihydroartemisinin—piperaquine should not be administered to patients with known hypersensitivity to either dihydroartemisinin or piperaquine 2. Drug interactions See Table 5. European Medicines Agency. Keating GM. Tarning J. Piperaquine bioanalysis, drug metabolism and pharmacokinetics. Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt , pfmdr1 , pfmrp , and pfnhe genes in Plasmodium falciparum.
Basco LK, Ringwald P. In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon.
Population pharmacokinetics and pharmacodynamics of piperaquine in children with uncomplicated falciparum malaria. Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and non-pregnant women with uncomplicated malaria. Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin—piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan. Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin—piperaquine in patients with Plasmodium falciparum malaria in Thailand. Clinical and pharmacological determinants of the therapeutic response to dihydroartemisinin—piperaquine for drug-resistant malaria.
Population pharmacokinetics of piperaquine in adults and children with uncomplicated falciparum or vivax malaria. Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated falciparum malaria.
Pharmacokinetics of piperaquine in pregnant women in Sudan with uncomplicated Plasmodium falciparum malaria. A small amount of fat does not affect piperaquine exposure in patients with malaria. Population pharmacokinetic assessment of the effect of food on piperaquine bioavailability in patients with uncomplicated malaria.
Pharmacokinetic comparison of two piperaquine-containing artemisinin combination therapies in Papua New Guinean children with uncomplicated malaria. Efficacy and safety of dihydroartemisinin—piperaquine Artekin in Cambodian children and adults with uncomplicated falciparum malaria. Therapeutic efficacy and safety of dihydroartemisinin—piperaquine versus artesunate—mefloquine in uncomplicated Plasmodium falciparum malaria in India.
A randomized open study to assess the efficacy and tolerability of dihydroartemisinin—piperaquine for the treatment of uncomplicated falciparum malaria in Cambodia.
A phase III, randomized, non-inferiority trial to assess the efficacy and safety of dihydroartemisinin—piperaquine in comparison with artesunate—mefloquine in patients with uncomplicated Plasmodium falciparum malaria in southern Laos.
Comparative study of the efficacy and tolerability of dihydroartemisinin—piperaquine—trimethoprim versus artemether—lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Cameroon, Ivory Coast and Senegal. Safety and efficacy of dihydroartemisinin—piperaquine versus artemether—lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children. Efficacy and safety of artemisinin—naphthoquine versus dihydroartemisinin—piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia.
Multicentric assessment of the efficacy and tolerability of dihydroartemisinin—piperaquine compared to artemether—lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in sub-Saharan Africa. Dihydroartemisinin—piperaquine and artemether—lumefantrine for treating uncomplicated malaria in African children: a randomised, non-inferiority trial.
An open-label, randomised study of dihydroartemisinin—piperaquine versus artesunate—mefloquine for falciparum malaria in Asia. Understanding dosing: children are small adults, neonates are immature children. Arch Dis Child. The effect of dosing regimens on the antimalarial efficacy of dihydroartemisinin—piperaquine: a pooled analysis of individual patient data.
Population pharmacokinetics of piperaquine in young Ugandan children treated with dihydroartemisinin-piperaquine for uncomplicated malaria.
Pharmacokinetics The reported pharmacokinetic parameters of doxycycline are summarized in Table A5. Safety Adverse effects Doxycycline has side-effects similar to those of other tetracyclines 4. Contraindications Doxycycline is contraindicated in individuals with known hypersensitivity to tetracyclines. Caution Doxycycline should be used with caution in patients with gastric or intestinal diseases such as colitis, who may be at greater risk for pseudomembranous colitis.
Tetracyclines specifically target the apicoplast of the malaria parasite Plasmodium falciparum. Doxycycline for malaria chemoprophylaxis and treatment: report from the CDC expert meeting on malaria chemoprophylaxis.
Bioavailability of tetracycline and doxycycline in fasted and nonfasted subjects. Influence of milk on the bioavailability of doxycycline—new aspects. Pharmacokinetics of doxycycline in adults with cystic fibrosis. Sex affects the steady-state pharmacokinetics of primaquine but not doxycycline in healthy subjects. Serum level, half-life and apparent volume of distribution of doxycycline in geriatric patients.
Pharmacokinetics of quinine and doxycycline in patients with acute falciparum malaria: a study in Africa. The effect of rifampicin on the pharmacokinetics of doxycycline. Pharmacokinetics and bioequivalence study of doxycycline capsules in healthy male subjects. The effects of chronic renal insufficiency on the pharmacokinetics of doxycycline in man.
Antipyrine and doxycycline pharmacokinetics in patients with thyroid disorders. J Postgrad Med. Pharmacokinetics of oral doxycycline during combination treatment of severe falciparum malaria. Raghuram TC, Krishnaswamy K. Pharmacokinetics and plasma steady state levels of doxycycline in undernutrition. Bioavailability of doxycycline from dissolved doxycycline hydrochloride tablets—comparison to solid form hydrochloride tablets and dissolved monohydrate tablets. Saivin S, Houin G. Clinical pharmacokinetics of doxycycline and minocycline.
Pharmacokinetics of doxycycline polyphosphate after oral multiple dosing in humans. Failure of doxycycline as a causal prophylactic agent against Plasmodium falciparum malaria in healthy nonimmune volunteers. Ann Intern Med.
Modification of the pharmacokinetics of doxycycline in man by ferrous sulphate or charcoal. Doxycycline pharmacokinetics in the absence of renal function. Kidney Int. Tetracycline-associated fatty liver of pregnancy, including possible pregnancy risk after chronic dermatologic use of tetracycline. J Reprod Med. Pharmacokinetics The pharmacokinetic parameters of mefloquine used with artesunate for the treatment of uncomplicated malaria and for chemoprophylaxis in healthy subjects 3 — 23 are summarised in Table A5.
Safety Adverse events Although mefloquine is associated with higher incidences of central nervous system and gastrointestinal adverse effects than other ACTs, it is generally well tolerated when given in combination with artesunate for the treatment of uncomplicated malaria. Contraindications Mefloquine is contraindicated in patients with known hypersensitivity to mefloquine or related compounds e.
Caution Given the lack of evidence on the safety of mefloquine in severe hepatic impairment, such patients should be monitored carefully because of a potential increase in the risk for adverse events. Mefloquine derivatives: synthesis, mechanisms of action, antimicrobial activities. Synopsis : Antimalarial Agents written by Graham L.
Patrick, published by Elsevier which was released on 30 May Download Antimalarial Agents Books now! ADQ besides being used as an effec- the high incidence of co-administration of P-gp substrate tive antimalarial especially in chloroquine-resistant malaria is drugs with antimalarials.
Thus, this study is anticipated to also known to possess potent anti-inflammatory and anti- provide useful information that will lead to more effective pyretic properties. Therefore, there is the potential of several treatment policies for malaria. However, further in vivo inves- DDIs occurring. In addition, ART which has a moderate tigations are recommended to confirm the in vitro findings.
Accepted for publication March 31, Thus, co-administration of antima- 1. WHO, Therefore, there. Accessed April 28, In addition, Urbanization, malaria transmission and disease burden in colchicine, a drug used to treat gout and a well-known P-gp Africa. Nat Rev Microbiol 3: 81— Challenges in the con- CQ, which can also be used to treat gout. Colchicine is noto- current management of malaria and HIV in pregnancy in sub- rious for its narrow therapeutic index, and hence DDIs with Saharan Africa.
Lancet Infect Dis 6: — Drug interactions in the treatment and che- induced toxicity. This potentially clinically relevant DDI may moprophylaxis of malaria in HIV infected individuals in sub also require dose adjustments. Curr Drug Metab 51— Previous studies have shown that some antimalarial drugs 6. Nat Rev Drug Reungpatthanaphong P, Mankhetkorn S, Modulation of Discov 9: — Giacomini K, Sugiyama Y, Biol drug response. New York: Predicting McGraw-Hill, 41— AAPS J 8.
Tanigawara Y, Role of P-glycoprotein in drug disposition. Ther Drug Monit — The drug transporter P-glycoprotein Sugiyama Y, Extrapolation of in vitro metabolic and limits oral absorption and brain entry of HIV-1 protease inhib- P-glycoprotein-mediated transport data to in vivo by modeling itors.
J Clin Invest — New York: Springer, — Biochem Pharmacol — Clin Toxicol Xenobiotica — Rostami-Hodjegan A, Tucker G, In silico simulations to Drug Discov Today Technol 1: — Antimicrob Agents Chemother — Establishment of in vitro P- F, Gimenez F, Interactions of racemic mefloquine and its glycoprotein inhibition assay and its exclusion criteria to assess enantiomers with P-glycoprotein in an immortalised rat brain the risk of drug—drug interaction at the drug discovery stage.
Transport and epithelial Br J Pharmacol — Biochem Lin JH, Transporter-mediated drug interactions: clinical Biophys Res Commun — Expert Opin Drug Metab Guidelines for the Treatment of Malaria.
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