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At least 19 recordsLinked to original sources
PubMed1975

Amodiaquin accumulation by mouse erythrocytes infected with Plasmodium berghei.

[14C]amodiaquin accumulation by washed erythrocyte preparations was characterized to permit comparisons with chloroquine accumulation. Erythrocytes infected with Plasmodium berghei CS (chloroquine-susceptible) accumulate amodiaquin by a saturable process that has an apparent dissociation constant for amodiaquin of 7.6 X 10(-8) M and is competitively inhibited by chloroquine, quinine and quinacrine, as is the process of chloroquine accumulation. Within experimental error, the K1 of 8 X 10(-7) M estimated for chloroquine is the same regardless of whether the drug being accumulated is [14C]amodiaquin or [14C]chloroquine. Likewise, the K1 for amodiaquin is the same regardless of which drug is being accumulated. In addition, glucose stimulates and hydrogen ion, cold or interruption of glycolysis inhibits amodiaquin as well as chloroquine accumulation. These findings are evidence that a single process serves to accumulate both drugs. In the absence of substrate, erythrocytes infected with P. berghei CR (chloroquine-resistant) accumulate twice as much amodiaquin as chloroquine, and they accumulate more amodiaquin than do erythrocytes infected with P. berghei CS. These differences occur because P. berghei CR infects polychromatophilic erythrocytes possessing a high-affinity, substrate-independent process of accumulation to which amodiaquin has greater access than chloroquine. In the presence of glucose, amodiaquin accumulation by erythrocytes infected with P. berghei CR, when plotted as a function of amodiaquin concentration in the medium, describes a sigmoid curve.

Amodiaquine↗
PubMed1979

Preliminary screening of antifilarial activity of levamisole and amodiaquine on Wuchereria bancrofti.

A single dose of levamisole of 3 mg/kg had a marked microfilaricidal effect in some persons harbouring Wuchereria bancrofti, but there was considerable variation in the response. In some cases blood examinations for microfilariae remained negative or at a low level for several months. Persons with high pretreatment microfilaraemias responded less to therapy than did those with low counts. The main side-reaction to levamisole was fever, which began six to eight hours after treatment. Combined DEC-levamisole therapy appears to have no advantage over the use of DEC alone. Amodiaquine in a total dose of 40 mg/kg appears to be macrofilaricidal, but because of the slight possibility of blood dyscrasias, mass chemotherapy with this dosage could not be recommended. Some amodiaquine congeners shown to be effective in experimental infections against adult filarial worms may prove to have a higher chemotherapeutic index than amodiaquine against W. bancrofti in man.

Adolescent↗
PubMed1977

Amodiaquine agranulocytosis.

A case of profound neutropenia and severe infection after the administration of amodiaquine is presented. The recommended dose for malaria prophylaxis was administered.

Adult↗
PubMed1978

Field evaluation of primaquine in the control of Plasmodium vivax.

Two regimens of primaquine in combination with amodiaquine have been compared with amodiaquine alone in known cases of Plasmodium vivax in an endemic area of El Salvador, C.A. A 5-day regimen of primaquine, with dosages based on an adult dose of 15 mg per day, produced a substantial reduction in the numbers of patients experiencing renewed parasite activity and in the number of parasitemias experienced by the group during 9 mo of posttreatment observation, when compared with patients treated only with amodiaquine. A single dose regimen, based on an adult dose of 45 mg, similarly reduced the number of patients with renewed parasite activity and the number of parasitemias in the group. Those patients who experienced malaria attacks subsequent to treatment with either primaquine regimen experienced fewer such attacks than did those receiving amodiaquine alone. It is concluded that such primaquine regimens, which are more practicable for field use than the full 14-days curative regimen, are of value to both the patient and the community through the reduction of parasite episodes and the reduction of the source of mosquito infection for continuation of transmission.

Adolescent↗
PubMed1977

Activities of various 4-aminoquinolines against infections with chloroquine-resistant strains of Plasmodium falciparum.

The studies reported here stemmed from a personal report by Geiman on the capacity of the 4-aminoquinoline amodiaquin to inhibit in vitro maturation of ring stages of the chloroquine-resistant Monterey strain of Plasmodium falciparum. This observation, confirmed in owl monkeys infected with this strain, led to a comparison of the activities of chloroquine, amodiaquin, amopyroquin, and dichlorquinazine (12,278 RP) against infections with various chloroquine-susceptible and chloroquine-resistant strains. The results showed that: (i) these 4-aminoquinolines were essentially equally active against infections with chloroquine-susceptible strains and (ii) the activities of amodiaquin, amopyroquin, and dichlorquinazine were reduced significantly in the face of chloroquine resistance, but (iii) well-tolerated doses of these compounds would cure infections with strains that fully resisted treatment with maximally tolerated doses of chloroquine. Two other 4-aminoquinolines, SN-8137 and SN-9584, which also exhibited activity against chloroquine-resistant parasites in vitro, displayed curative activity in monkeys infected with a chloroquine-resistant strain. These observations show that there is cross-resistance among the 4-aminoquinolines, confirming earlier findings, but indicate that the dimensions of this phenomenon are sufficiently limited so that some derivatives are therapeutically effective against infections refractory to maximally tolerated doses of chloroquine.

Aminoquinolines↗
PubMed1979

Drug-related transient dyskinesias.

The ability of some antimalarials, especially chloroquine and amodiaquine, to provoke alarming but transient extrapyramidal movement disorders has been reported. The basis of the reported extrapyramidal symptoms has been the cause of some speculation. This paper reviews case reports and presents some data of the regional uptake of chloroquine in mammalian brain as a factor to consider, along with other factors that could influence the action of chloroquine on the extrapyramidal system. A neuropharmacologic mechanism for the transient extrapyramidal disturbances has been formulated.

Amodiaquine↗
PubMed1979

A pocket of controlled malaria in a holoendemic region of West Africa.

Yekepa, a mining town in northern Liberia, has been built entirely since 1960 and now has a population of 16 000 inhabitants including 1500 expatriates. Although situated in a holoendemic region with constant human movements in and out of the town, the mining company has succeeded in controlling malaria in Yekepa. Furthermore, there is a constant threat of the vector in the close surroundings to the town. Control is maintained by regular residual insecticide sprayings with DDT, regular larviciding with fuel oil and fortnightly issue of amodiaquine chemoprophylactic to all workers. A Malariometric survey showed that the spleen and parasite rates were 11% and 13% respectively in the controlled areas and 95% and 67% respectively in surrounding regions not subjected to control measures. The dominant malaria parasite in the area was Plasmodium falciparum. No adult vectors were found in the town. In the surrounding villages the average room density of adult vectors was 3.8 and the sporozoite rate in a village very close to the town was 9.2%. The dominant vector of the area was Anopheles gambiae with A. Funestusalso being present. The annual per capita cost, including all control activities, is about 4--5 US dollars.

Amodiaquine↗
PubMed2025

Strategies for mitigating emerging artemisinin-based antimalarial drug resistance in Rwanda: a promising approach for managing therapies in malaria-endemic countries.

Malaria treatment failures associated with reduced efficacy of chloroquine (CQ) and amodiaquine (AQ) antimalarial drugs emerged in Rwanda during the 1980s, prompting the policy shift towards adopting artemisinin-based combination therapies in 2006 as an alternative. However, recent findings from malaria surveillance and therapeutic efficacy studies have revealed a countrywide increase in antimalarial drug resistance. Particularly, artemether-lumefantrine (AL) efficacy has significantly decreased, probably due to the emergence of Plasmodium falciparum (Pf) genomic mutations. To mitigate the current drug resistance, Rwanda has adopted targeted multiple first-line therapies. Through the national malaria control program, antimalarial drugs were deployed in accordance with the reported resistance profile. A significant rise in Pfkelch13 mutations, particularly A675V associated with AL resistance, was mainly reported in the western region; therefore, artesunate-pyronaridine was recommended. Dihydroartemisinin-piperaquine was considered in eastern and central regions, where R561H mutations were predominant. On the contrary, AL was maintained in the southern region, where the prevalence of the R561H mutation was low. Insights from this data-driven model will inform its extension to other malaria-endemic countries facing emerging Pf genetic diversity.

Antimalarials↗
PubMed1977

Behavioral toxicity and equivocal suicide associated with chloroquine and its derivatives.

Although the antimalarial agents chloroquine, hydroxychloroquine, and amodiaquine are widely used to treat a variety of medical conditions, their behavioral toxicity and lethality are not generally recognized. Therapeutic doses sometimes cause psychosis, delirium, personality change, and depression. Since moderately low overdoses of chloroquine can result in rapid death, such behavioral effects could lead to accidental or state-dependent overdosage and death.

Adult↗
PubMedDate not supplied

The effect of antihistamine drugs on the neuroleptic-induced catalepsy.

The effect of atropine on the spiperone- or reserpine-induced catalepsy was compared with the effect pure antihistamines (chlorcyclizine, diphenhydramine, mepyramine) and antiserotonin -- antihistamine drugs (cyproheptadine, danitracen). All the drugs were used in equipotent doses in respect of their central cholinolytic action, assassed previously on the basis of the tremorine test. The potency of the antiserotonin action of chlorcyclizine, diphenhydramine and mepyramine was estimated by assessing the ID50 values of these compounds in the test based on antagonism to L-5-hydroxytryptophan action in the mouse. The spiperone-induced catelepsy, was most effectively inhibited by classical histaminolytics and less by drugs of a combined antiserotonin and antihistamine action. For the reserpine-induced catalepsy, differences in action of the two groups of drugs were less distinct. In both cases atropine produced the weakest anticataleptic effect. Amodiaquine, an inhibitor of histamine degradation, enhanced the catalepsy induced by either neuroleptic (the reserpine-induced catalepsy in a statistically significant menner). A possibility that the anticataleptic action of chlorcyclizine, cyproheptadine, diphenhydramine, mepyrymine and danitracen depends on the blockade of the histamine receptors in the brain is discussed.

5-Hydroxytryptophan↗
PubMedDate not supplied

Influence of some inhibitors of histamine metabolism on the gastric secretion.

Influence of some inhibitors of histamine metabolism on the gastric secretion. Acta Physiol. Pol., 1977, 28 (6): 515-520. The influence of inhibitors of histamine metabolism on histamine (H) and Nalpha Nalpha-dimethylhistamine (NDMH) stimulated gastric secretion was studied in guinea-pigs and cats. Inhibitors of monoamine oxidase (MAO) and diamine oxidase (DAO): N-oxide diacetylaminopyridine (AAP) and N-oxide 2 aminopyridine (AP) increased HCI secretion in the gastric juice after H and NDMH. Inhibitors of N-methyl transferase: amodiaquine (A) and quinacrine (Q) increased HC1 secretion in the gastric juice after H but not after NDMH. The lack of action of A and Q on NDMH-stimulated gastric secretion suggests, that in guinea-pig and cat NDMH is not methylated additionally at the imidazole ring and therefore, it is a stronger gastric secretagogue than histamine itself.

Amodiaquine↗
PubMed1976

Chloroquine-resistant falciparum malaria from Irian Jaya (Indonesian New Guinea).

A strain of Plasmodium falciparum, transmitted in Irian Jaya (Indonesian New Guinea) was isolated in 1974 and sent to the University of Maryland for characterization in nonimmune volunteers. At Maryland the Indonesia (Whit.) strain, as it has been designated, was transmitted to colonized Anopheles stephensi. Prophylactically, it was not suppressed by proguanil hydrochloride 100 mg. daily. Curatively, parasitaemia was not cleared by treatment with 1-5 g. (base) in three days of chloroquine or amodiaquine (RII responses), nor by treatment with 150 mg. of pyrimethamine in three days (RIII), and some resistance was also shown to quinine. A single dose of 1-5 g. of mefloquine (WR 142,490) produced radical cure in the two patients treated with this new 4-quinolinemethanol compound.

Amodiaquine↗
PubMed1976

[Chemotherapy and chemoprophylaxis of malaria (author's transl)].

Chloroquine and amodiaquine are demonstrably still the most reliable drugs for the treatment of malaria, except in the south east Asia area, and in parts of south and central America where an altered sensitivity of falciparum plasmodia has been confirmed. The present position of malaria prophylaxis is, unfortunately, anything but satisfactory. But there are already some good preparations which, if correctly used with consideration of all available information, contribute considerably to the prevention of an infection.

Adult↗
PubMed1977

Direct or indirect action of histamine on dopamine metabolism in the rat striatum?

Intraventricular administration of 500 microgram of 2-pyridylethylamine, an agonist of the histamine (Hi) H1-receptor, produced a 20% increase of striatal HVA in the rat while the Hi H2-receptor agonist 4-methylhistamine had no influence on HVA and DOPAC levels. L-Histidine (1.5 g/kg) or amodiaquine (60 mg/kg) given i.p. increased HVA and DOPAC levels to the same extent as did pyridylethylamine. Histidine combined with tremorine had an additive effect with respect to the increase of DA acidic metabolites while mepyramine slightly attenuated the tremorine-induced rise of HVA.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1977

Endogenous histamine in rabbit thoracic aorta.

A sensitive automated assay was developed for the determination of histamine. The endogenous histamine content of intact rabbit thoracic aorta, and of its separated adventitial and medial layers was determined. The histamine content of the intact aorta was found to be only partially sensitive to compound 48/80. The isolated aorta accumulated labelled histamine against a concentration gradient. The uptake was abolished by cooling to 1 degree, but was unaffected by oxygen lack. The uptake process was sensitive to a variety of agents including extraneuronal catecholamine uptake inhibitors (deoxycorticosterone acetate, normetanephrine) as well as inhibitors of catecholamine and histamine metabolism (tranylcypromine, hydrallazine). The uptake was not affected by amodiaquin, a histamine N-methyl-transferase inhibitor, by the metabolites 1,4-methylhistamine or imidazole acetic acid, by compound 48/80 or by the basic amino acid arginine.

Animals↗