Friday, March 20, 2009

Evolution of Antimalarial Drugs

The effectiveness of the antimalarial drugs may differ with the species and stage of parasite and the parasite load in the liver and blood circulation. The malaria is an intracellular protozoan infection, endemic in tropical and subtropical countries. Four species of the protozoal parasite Plasmodium cause all infections in human beings and these are: Plasmodium vivax, Plasmodium malariae, Plasmodium ovale and Plasmodium falciparum. The parasites are inoculated into the human host by blood sucking female anopheline mosquitoes. The sporozoites from the infected mosquito reach the liver and develop into tissue schizonts. These tissue schizonts then rupture, form free merozoites and invade erythrocytes or red blood cells (RBCs) and develop as erythrocytic schizonts and lead to rupture of RBCs. Antimalarial drugs have undergone a great deal of evolution and at present there are many classifications of antimalarial drugs depending on the stages of malarial parasites in the liver and erythrocytes, on the bases of chemical groups or clinical effectiveness of the drugs.


If we look at the chemical groups of antimalarial drugs the Cinchona alkaloid or Quinine and Quinidine were the very first drugs and there after 4-aminoquinoline (Chloroquine and Amodiaquine), 8-aminoquinoline (Primaquine and Bulaquine), Quinoline-Methanol (Mefloquine) and Biguanides (Proguanil and Chlorproguanil) were developed. Diaminopyrimidines (Pyrimethamine), Sulfonamides (Sulfadoxine and Dapsone), Tetracyclines (Tetracycline and Doxycycline) and Aminoalcohols (Halofantrine and Lumefantrine) are other effective antimalarial drugs. Chloroquine has been used extensively for the treatment and prevention of malaria. It has considerable efficacy for the treatment of Plasmodium vivax, Plasmodium malariae and Plasmodium ovale infections, however, widespread resistance has been seen against Plasmodium falciparum infection. Artemisinin, Artemether, Artemotil and Atovaquone could be called newer antimalarial drugs. Artemisinin or Qinghaosu is a sesquiterpene lactone extracted from the leaves of Artemisia annua known as Sweet Wormwood in China. The extract of the leaves of Artemisia annua or Sweet Wormwood has been used in China for over a thousand years for the treatment of fever. Antifolate combinations like sulfadoxine pyrimethamine and sulfalene pyrimethamine are more safe drugs but are known to have longer elimination half life.


In terms of clinical effect on various stages of malarial parasites, the effectiveness of antimalarial drugs is contested for prophylaxis and anti-parasite activity. Effective suppressive prophylaxis has been documented with chloroquine, mefloquine, proguanil and doxycycline as these are schizonticidal drugs. Proguanil and primaquine are best known for causal prophylaxis as these drugs effectively kill the hepatic stages of the parasite. Quinine, chloroquine, primaquine and artemisnins are established gametocidal drugs also. Sulfonamides (sulfadoxine and dapsone) and aminoalcohols (halofantrine and lumefantrine) are also used in the treatment of malaria but are more toxic drugs. The drug toxicity may lead to acute hemolytic anemia in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency. Consult your physician for the diagnosis and treatment of malaria.

Wednesday, March 18, 2009

What Could Lead to Drug Addiction ?

Experimentation with psychotropic drugs for fun and elated feelings could activate certain receptors of our brain to such an extent that one would feel depressed without taking a particular drug. When a person starts taking a psychotropic drug, he/she enjoys the drug's euphoric effects. Repeated desire for elevated mood and a kick makes one addict for ever. The drug addiction is mostly unintentional as a person who begins with casual use of a drug does not know that the substance could become his/her daily desire. The drug associated altered neurophysiology leads to drug dependence. The drug related release of neurotransmitters may alter the ultrastructural architecture of neurons at a later stage. Some drugs may lock into some neurons and act like a pump and extensively stimulate the neurons to release more and more neurotransmitters. There exists a natural balance of neurotransmitters under the normal conditions of neurophysiology, but certain drugs may block reabsorption or reuptake of neurotransmitters, leading to behavioral changes altered physiology. The drug adiction is a complex brain disease. Despite the fact that the high effects of a drug are short term phenomenon, one finds it difficult to quit the habit. The compulsive and uncontrollable craving for a psychotropic drug leads to such a behavioral change that one would ignore all the moral values of the life and society to acquire a drug. The habitual use of a neurostimulator or psychotropic drug severely affects the neurophysiology and leads to drug addiction.

Effect of Drugs on Brain

The neurostimulators or psychotropic drugs bind to the receptors in the brain and start an unnatural chain of reactions causing electrical changes and stimulate neurons to release large amounts of drug associated neurotransmitters. Some drugs may lock into the neuron and act like pump. The locked in psychotropic drugs extensively stimulate the neurons to release more and more neurotransmitters. There exists a natural biobalance of neurotransmitters under the normal conditions of neurophysiology, but certain drugs may block reabsorption or reuptake of neurotransmitters, leading to behavioral changes. The drug addiction is a complex brain disease. There could be compulsive and uncontrollable craving for drugs. The compulsive desire for drugs may lead to such a behavioral change when one ignores all the moral values of the life and society to acquire a drug. The habitual use of a drug severely affects the neurophysiology and leads to addiction.