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PubMed1987

A preliminary pharmacokinetic study of the antimalarial drugs, proguanil and chlorproguanil.

Pharmacokinetic parameters for cycloguanil and chlorcycloguanil, the active metabolites of proguanil (Paludrine] and chlorproguanil (Lapudrine) have been measured in a bioassay which assesses the in-vitro growth inhibition of a cycloguanil- and chlorcycloguanil-sensitive strain of Plasmodium falciparum produced by dilutions of plasma collected after oral administration of the pro-drugs. A single compartment model is applicable for cycloguanil with mean rate constants of elimination of 0.0624 h-1 and availability of 0.2398 h-1. The elimination profile for chlorcycloguanil indicates partition of drug into more than one compartment. In 2 of 10 subjects dosed with proguanil and 1 of 11 subjects dosed with chlorproguanil, the active metabolite levels were significantly lower than the mean for the other subjects. Abnormally low cycloguanil or chlorcycloguanil plasma levels may be of importance in relation to effective prophylaxis against malaria.

Adult↗
PubMed1988

Steady-state kinetics of proguanil and its active metabolite, cycloguanil, in man.

The pharmacokinetics of proguanil and its active metabolite, cycloguanil, were determined at steady-state in 6 healthy male volunteers after daily administration of 2 Paludrine tablets (200 mg proguanil hydrochloride). A maximum plasma proguanil concentration of 130.3 +/- 16.0 ng/ml (mean +/- SD) was reached at 3.8 +/- 1.3 h while a maximum cycloguanil concentration of 52.0 +/- 15.2 ng/ml was obtained at 5.3 +/- 1.0 h after dosing. The elimination half-lives of proguanil and cycloguanil were 14.5 +/- 3.0 h and 11.7 +/- 3.1 h, respectively. The plasma clearance of proguanil was 1.43 +/- 0.33 l/h/kg and the apparent volume of distribution was 30.7 +/- 12.3 l/kg. Renal clearance of proguanil (0.33 +/- 0.19 l/h/kg) was about 23% of the plasma clearance and 35.6 +/- 9.6% of the oral dose was recovered as proguanil and cycloguanil.

Administration, Oral↗
PubMed1991

The effect of prophylaxis with chloroquine and proguanil on delayed-type hypersensitivity and antibody production following vaccination with diphtheria, tetanus, polio, and pneumococcal vaccines.

In vitro studies have shown that anti-malarial drugs suppress immunity. In this study, the effects of chloroquine and proguanil (Paludrine) on the cellular and humoral immune system were measured by two in vivo methods: 1) cell-mediated immunity (delayed cutaneous hypersensitivity) i.e., skin tests with seven delayed-type common antigens (Multitest) and 2) humoral immunity by measurement of specific antibody response to vaccination. Sixty healthy young individuals were randomized into four groups and given 1) no treatment (controls), 2) chloroquine diphosphate (500 mg/week), 3) chloroquine diphosphate (1,000 mg/week), or 4) proguanil hydrochloride (200 mg/day) for six weeks. Skin testing was performed on days 0 and 28. Vaccinations with diphtheria, tetanus, polio, and pneumococcal polysaccharide antigen vaccines were performed on day 28, and the presence of specific antibodies was determined on days 0, 28, and 42. The skin tests induced a significant increase in skin reactive areas from day 0 to day 28 in all groups. Furthermore, the skin test induced an increase in the level of specific IgG for diphtheria and tetanus, but had no effect on antibodies to antigens not included in the skin test. The results showed that there were no significant differences among the four groups regarding skin test areas and increases in antibody titers following vaccination. Therefore, it is concluded that in healthy persons, six weeks intake of chloroquine, even in double doses, or proguanil in chemoprophylactic dosages, does not induce any detectable suppression of delayed-type hypersensitivity or vaccination responses to diphtheria, tetanus, polio, or pneumococcal polysaccharide antigens.

Adult↗
PubMed2001

Development of new drugs for chemoprophylaxis of malaria.

When U.S. troops first encountered drug resistant malaria during the Vietnam war, the United States Army responded by establishing a malaria drug research program. In 1988, the Walter Reed Army Institute of Research developed mefloquine (WR 149240) and halofantrine (WR 171669). Actually, in association with SmithKline Beecham, the WRAIR is developing tafenoquine (WR 238605), an analog of primaquine, which is expected to be effective in both preventing and treating malaria in deployed military personnel. Final phase III studies leading to U.S. Food and Drug Administration approval are planned for 2000. Applied research is also carried out with the association atovaquone-proguanil (Malarone) or with azithromycin, but also with primaquine, the associations paludrine-dapsone or lapudrine-dapsone, analogs of floxacrine (WR 243251), and a guanylhydrazone (WR 182393). The future scientific directions must focus on basic and applied research for a better understanding of the modes of action and mechanisms of resistance to standard and developmental drugs. Using new techniques, the design and synthesis of new drugs would hopefully result in the development of drugs that circumvent the malaria parasites elusive mechanisms of drug resistance.

Antimalarials↗
PubMed2001

Development of new drugs for chemoprophylaxis of malaria.

When U.S. troops first encountered drug resistant malaria during the Vietnam war, the United States Army responded by establishing a malaria drug research program. In 1988, the Walter Reed Army Institute of Research developed mefloquine (WR 149240) and halofantrine (WR 171669). Actually in association with SmithKline Beecham, the WRAIR is developing tafenoquine (WR 238605), an analogue of primaquine, which is expected to be effective in both preventing and treating malaria in deployed military personnel. Final phase III studies leading to U.S. Food and Drug Administration approval are planned for 2000. Applied research is also carried out with the association atovaquone-proguanil (Malarone) or with azithromycin, but also with primaquine, the associations paludrine-dapsone or lapudrine-dapsone, analogues of floxacrine (WR 243251), and a guanylhydrazone (WR 182393). The future scientific directions must focus on basic and applied research for a better understanding of the modes of action and mechanisms of resistance to standard and developmental drugs. Using new techniques, the design and synthesis of new drugs would hopefully result in the development of drugs that circumvent the malaria parasites elusive mechanisms of drug resistance.

Antimalarials↗
PubMed2006

[A patient with fever following a visit to the tropics: tick-borne relapsing fever discovered in a thick blood smear preparation].

A 26-year-old woman presented with a 2-day history of fever peaking to 39 degrees C and cold shivers that developed after a 2-weeks trip to Guatemala and Belize. Prior to the fever the patient had felt symptoms of a common cold and general malaise. Moreover, she complained of generalised myalgia and nausea. She had taken paludrine as a prophylactic against malaria. Borrelia spirochaetes, the pathogen of relapsing fever, were detected in a thick blood smear preparation. On the basis of the anamnesis, geography and specific exposure, the patient had a form of relapsing fever that is transmitted by ticks and not by lice: tick-borne relapsing fever. She was treated with doxycycline, 100 mg b.i.d. for 7 days. She could be discharged home in good condition after 2 days.

Adult↗
PubMed1991

Proguanil daily or chlorproguanil twice weekly are efficacious against falciparum malaria in a holoendemic area of Tanzania.

The prophylactic efficacy of proguanil 100 mg (Paludrine) daily was compared to that of chlorproguanil 20 mg (Lapudrine) twice weekly in school children from Nyamisathi village, in a coastal area of Tanzania, 160 km south of Dar es Salaam. A total of 80 children were randomly allocated to three groups after radical treatment with a curative dose of mefloquine (Lariam). Seventy-six children were then followed up with daily prophylaxis and/or placebo for 13 weeks. All children in the group taking placebo prophylaxis were reinfected within 10 weeks whereas no parasites were detected in the children taking proguanil or chlorproguanil for prophylaxis. We conclude that both regimens were efficacious and that chlorproguanil represents an important alternative for chemoprophylaxis if taken at least twice weekly instead of the recommended once weekly regimen.

Adolescent↗
PubMedDate not supplied

[A current problem: the prevention of malaria].

The A.A. weight present criteria of choice in order to set right a correct and effective anti-malarial prophylaxis. In the last ten years, a progressive increase of tropical diseases has been observed. This is due to the considerable growth of intercontinental traffic and of the number of persons moving to or from tropical areas where such diseases are endemic. Among these, malaria represent the most alarming problem, both because of the incidence cases and the difficulties related to the efficacy of pharmacological remedies for the chemoprophylaxis. In particular, three are now various pharmacological possibilities for malarial prophylaxis. Undoubtedly Chloroquine is the most efficacious even if there are many Plasmodium falciparum species resistant to Chloroquine and to other available medicines (multi-resistance). Most authors recommend to associate Chloroquine to others pharmacological substances to avoid pharmaco-resistance phenomena. Among the most famous pharmacological products used elsewhere are Fansidar, Maloprim, Paludrine and Lapudrine, not all are available in Italy. In China, for the therapy of resistant forms of malaria, the Qinghaosu a "schizont-killer" acting on multiresistant plasmodium falciparum has been utilizing for years. The Qinghaosu is not responsible for the crossing-reactions with other anti-malarial medicines. Various substances with Ca-antagonist action (Verapamil) are being experimented. It is supposed that Verapamil associated with Chloroquine can stop the flow of chlorine from plasmodium cells. The same mechanism is expected to be valid also for Desipramine, an experimental tricyclic anti-depressive when associated to Chloroquine. To the people moving to endemic areas, the A.A., at the end, suggest a series of practical norms to prevent infection and, therefore, the incidence of imported cases, still increasing at the moment, due to the absence of efficacious vaccine.

Antimalarials↗
PubMed1977

[Hydatid cyst of the heart. Apropos of 9 cases].

The authors report 9 cases of hydatic cyst of the heart which they have encountered over an 8 year period. They illustrate the variable nature of this parastic illness, which may stimulate almost and cardiovascular disorder. The various clinical presentations and the methods of diagnosis and treatment are presented: the clinical picture is of little help in establishing the diagnosis. This is made at three levels: the history (country of origin where the disease is endemic, or other associated cyst), the presence of Xray of a swelling of the heart which is later calcified, and the presence on the electrocardiograph of ischaemic changes, which may be severe enough for necrosis. They emphasise the importance of serological tests to make a formal diagnosis of the condition, and a repetition of such tests as part of the postoperative follow-up. Surgical treatment (usually by an open heart technique) is the rule. It may be coupled with medical treatment with anti-malarials (paludrin of flavoquin).

Adolescent↗
PubMedDate not supplied

Iron studies in patients with sickle cell disease.

The prevalence of iron deficiency anaemia during the first three decades of life was investigated in eighty-five patients with SS and SC haemoglobins. The parameters used were the haematocrit, serum iron, total iron binding capacity (TIBC), percentage saturation of transferrin and availability of iron in the bone marrow. The mean haematocrit values were similar throughout the three decades, but increased with age (r = 0.41). The mean serum iron was significantly lower (P less than 0.01) in the first decade than in the second or third decade. Females had lower serum iron in the first and second decades and higher values in the third decade than their male counterparts. The transferrin saturation was significantly lower (P less than 0.01) in the first decade than in the third decade. No haemosiderin was found in the marrow aspirates at a transferrin saturation of less than or equal to 15%. Of the eighty-five bone marrow aspirates studied for stainable iron, fifty-eight (68.2%) had nil iron. The data presented show that iron deficiency anaemia is a common finding in patients with haemoglobinopathies. The need to incorporate oral iron with folic acid and paludrine in the treatment of sickle cell disease is suggested.

Adolescent↗