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Amodiaquine, sold under the trade name Camoquin, is a medication used to treat malaria and as an anti-inflammatory agent.[1]

Common side effects include cause, diarrhoea, and itching. [2] Its use has also been linked with liver damage and effects on the heart including low blood pressure. [2][3]

It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.[4] In 2012, the World Health Organization recommended Seasonal Malaria Chemoprevention treatment for children under 5, which required amodiaquine plus sulfadoxine-pyrimethamine treatment for a month in order to reduce malaria infections. [5]

Medical uses[edit]

Amodiaquine is an important medication in the combination therapy for malaria treatment in Africa.[6] It is often used in combination with artensunate as a by mouth artemisinin-based combination therapy (ACT) for uncomplicated P. falciparum malaria.[7] Amodiaquine has also been found to work against chloroquine-resistant P. falciparum strains of malaria. [1]

Pregnancy and breastfeeding[edit]

There is limited data on the safety of amodiaquine in pregnant women, although its use has not indicated any associated cases of birth defects in the baby.[8][9] Prescribers should assess the risks and benefits of therapy. Its use during breast-feeding is generally safe, as the amount found in breast milk is small.[9]

Contraindications[edit]

Amodiaquine should not be used in people with liver problems or for prevention of malaria.[8] It should also be used with caution in people with alcoholism. [1]

Adverse effects[edit]

Amodiaquine has adverse effect similar to that of chloroquine, including nausea, vomiting, abdominal pain, itchiness, and diarrhea.[8] Amodiaquine may cause less itchiness than chloroquine. When used for prevention, amodiaquine has a much greater risk of a low white blood cell count and higher risk of liver toxicty.[7][8] Due to reports of fatal cases of sudden liver inflammation, amodiaquine is currently only recommended for malaria treatment and not prevention.[2] When amodiaquine is used for treatment of malaria, the severity of these risks are unknown.[7]

Overdose[edit]

High doses of amodiaquine may cause syncope, convulsions, muscle spasms, and involuntary movements.[7][8] Patients may also experience shock, due to reduced blood circulation, and a reduced heart rate.[3]

Interactions[edit]

There have been reports of increased liver toxicity in people with HIV/AIDS on zidovudine or efavirenz when treated with amodiaquine-containing ACT regimens, therefore it is recommended that these people avoid amodiaquine.[7]

Pharmacology[edit]

Mechanism of action[edit]

Amodiaquine is a 4-aminoquinoline that has active antimalarial effects on P. flaciparum, P. vivax, P. ovale, and P. malaria by destroying their presence in the blood. Its mode of action is not completely understood, yet it is believed that it penetrates red blood cells and prevents the parasites from digesting heme, causing death of the parasites.[9]

Pharmacokinetics[edit]

Once amodiaquine is taken by mouth, it is quickly absorbed in the gastrointestinal tract and transformed into its active metabolite, N-desethylamodiaquine. Bioavailability is unknown. Its estimated volume of distribution is 20-40 L/kg. Metabolism of amodiaquine is primarily via CYP2C8, oxidation, and glucuronidation. An estimated 2% of amodiaquine is excreted unchanged in the urine, however its active metabolite has a slower elimination with a half-life of 9-18 days.[9]

http://apps.who.int/iris/bitstream/10665/162441/1/9789241549127_eng.pdf?ua=1&ua=1

References[edit]

  1. ^ a b c Pubchem. "amodiaquine | C20H22ClN3O - PubChem". pubchem.ncbi.nlm.nih.gov. Retrieved 2016-10-19.
  2. ^ a b c "Amodiaquine". livertox.nlm.nih.gov. Retrieved 10 October 2016.
  3. ^ a b "amodiaquine". PharmGKB. Retrieved 2016-10-19.
  4. ^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
  5. ^ "Fact sheet about Malaria". World Health Organization. Retrieved 2016-10-20.
  6. ^ Kerb, Reinhold; Fux; Morike; Kremsner; Gil; Gleiter; Schwab (2009). "Pharmacogenetics of antimalarial drugs: effect on metabolism and transport". Lancet Infectious Disease. 9 (12): 760–774. doi:10.1016/S1473-3099(09)70320-2. PMID 19926036.
  7. ^ a b c d e Guidelines for the Treatment of Malaria - 2nd Edition. World Health Organization. 2010. p. 33. ISBN 9789241547925.
  8. ^ a b c d e "Overseas Refugee Health Guidelines: Malaria". Immigrant and Refugee Health. Centers for Disease Control and Prevention. 3 July 2012. Retrieved 9 October 2016.
  9. ^ a b c d "Summary of Product Characteristics" (PDF). Artensunate/Amodiaquine tablets. World Health Organization. September 2010. Retrieved 9 October 2016.