side effects of malaria drugs #all drugs in details


malarial drugs

Malaria is a protozoal infection that caused by the 4 species of protozoal parasite like plasmodium vivax, plasmodium malariae, plasmodium ovale and plasmodium falciparum. 

This is drugs are used for treatment and prevention of malarial. But, the side effects of malaria drugs are various with their own function.

Day by day malarial infection is increasing worldwide. In India, plasmodium falciparum and plasmodium vivax are both parasites are common. 

In worldwide, it is one of the major health problems. Estimated actually in India 40,000 malarial death occurs annually. (This report by WHO IN 2011). So, various drugs are used in malaria.

various types of medication used in malarial disease. various medication produced their own side effect or adverse effect. here, I will discuss side effect of malarial drugs via categorized. do not all side effect produce in patients when it's take this medication. but, it's depend various factors like age, disease history, immunity etc. 

Let's start anti-malarial drugs side effect.  


side effects of malaria drugs


4 – aminoquinoline


example of 4- aminoquinoline

chloroquine (Aralen)
amodiaquine (basoquine)
piperaquine (Eurartesim)

Chloroquine

Chloroquine is a 4 – aminoquinoline. Its inhibit the conversion of haeme to hemozoin. Produce the drugs haeme complex. This drugs haeme complex is very toxic and kills the parasite infection.

 

Side effects of malaria drugs (chloroquine)

➞ Chloroquine toxicity is low but, it produces some side an effect like nausea, vomiting, skin rashes, itching and headache.

 If chloroquine is administered through parenteral produce some side effect like hypotension, cardiac arrhythmia, confusion and cardiac arrest.

 In rheumatoid arthritis, given chloroquine in a large amount that cause ototoxicity, reversible retinopathy and loss of vision due to the retinal damage.

 In the case of long term use chloroquine. It produces some side effect include photoallergy, loss of hearing and mental disturbance.

 Its also cause cardiomyopathy, neuropathy and myopathy. Rarely produce some psychiatric disturbance.

 Chloroquine is not given in epileptic condition. and contraindicate with the mefloquine, amiodarone and antiarrhythmics.

 Chloroquine is used in during pregnancy. That not produce any teratogenic effect.


Amodiaquine

It is same as chloroquine but, less bitter than chloroquine. It is a congener of chloroquine. Mechanism of action is similar to the chloroquine. In chloroquine resistance falciparum malaria it used combination with artesunate.


Side effects of malaria drugs (amodiaquine)

 amodiaquine are produced similar side effect to chloroquine.

 When it's given children and HIV patient that receives the antiretroviral therapy (what is antiretroviral) it produces neutropenia.

 Amodiaquine is not used for prophylaxis of malaria. Produce some toxicity like- agranulocytosis and hepatotoxicity.

 

8 – aminoquinoline

example of 8aminoquinoline

primaquine
tafenoquine (krintafel)

 
primaquine

Primaquine is a synthetic 8 – aminoquinoline. It is a poor erythrocytic schizontocide. It is more active against the pre-erythrocytic stage of Plasmodium falciparum than Plasmodium vivax.

Primaquine is highly active against hypnozoites and gametocytes. The exact mechanism of action of primaquine is not known.

 

Side effects of malaria drugs (primaquine)

 The common dose of primaquine produce some side effect like GI upset, abdominal pain, weakness. It can be minimized with by the drugs taking with meals.

 In a higher dose of primaquine leucopenia produced.

  Also, a CNS and cardiovascular symptoms are produced infrequently.

 The important toxic potential is dose-related methaemoglobinaemia, haemolysis, tachypnoea and cyanosis.

 In rheumatoid arthritis patients, primaquine produces some side effect like leucopenia and haemolysis.

 Primaquine is contraindicated in pregnancy.


Quinoline methanol

example of quinoline methanol

mefloquine (Lariam)


Mefloquine

Mefloquine are introduced in 1963. It's effective against chloroquine resistance plasmodium falcifarum. It's effective in erythrocytic schizontocide. It does not any effect produce on hepatic form and has no any gametocidal activity produced. 

Mechanism of action of mefloquine is similar to quinine drugs.

Its administered in orally, but when given through parental it produces a local irritation of action. It is well absorbed, widely distributed and highly bound to the plasma proteins. And excreted with faeces.

 

Side effects of malaria drugs (mefloquine)

 Mefloquine is producing a bitter test. Some common side effect produce include nausea, vomiting, dizziness and diarrhoea and abdominal pain.

 Neuropsychiatric symptoms are some seizures are produced. (anxiety, hallucination, ataxia, disturbance sense of the balance, error in operatory machinery etc)

 Mefloquine is also producing haematological, hepatic and cutaneous toxicity.

 Generally, it's safe during the pregnancy but, avoid in first trimester.

 Also, it's safe for use in younger children

 Mefloquine is contraindicated with patients depression, anxiety and psychosis.

 

Cinchona Alkaloids

example of cinchona alkaloids

quinine (Qualaquin)

quinidine (Cardioquin, Quinora)


Quinine & Quinidine

Quinine and quinidine are derived from the cinchona bark. Generally, cinchona bark contains various alkaloid but, quine and quinidine are most important alkaloid. 

Quinine is used in all species of plasmodium as a erythrocytic schizontocide. But, quinine are less effective and more active than chloroquine. Further, no activity on hepatic form. But, It also produces a gametocidal activity against the plasmodium vivax.

Mechanism of action of quinine is similar to the chloroquine. Its directly depresse the contraction of skeletal muscle. Also depress the myocardium and cause hypotension. Also, a mild analgesic and antipyretic effect produce.

 

Side effects of malaria drugs (quinine and quinidine)

 Quinine are produce some side effect like, hypotension, hypoglycaemia and cinchonism. It also cause a dose dependent toxicities.

 When stope this therapy produce some adverse effect include blurred vision, colour defect, headache, nausea and vomiting.

 If quinine is given through i.v its produce hypoglycaemia because release of insulin.

 Also, hypotension produce when it given through intravenous.

 It is more cardiotoxic effect produce than quinine.

 Both drugs not given with mefloquine drugs because it produce a serious risk of cardiac toxicity.

 Also, sometimes produce a ‘black liver disease’ and hypersensitivity reaction.

 Quinine and quinidine both are safely used during pregnancy.

 

Antifolates      

example of antifolates

pyrimethamine (Daraprim)
dapsone (Aczone)
sulphadoxine (Fansidar)
proguanil (Malarone)

pyrimethamine & proguanil

Both of drugs are actually a folate reductase. Plasmodium are utllize the para amino benzoic acid (PABA) for the synthesis of folic acid.  Further folic acid are necessary to DNA synthesis.


PABA   dihydrofolate   tetrahydrofolate   folic acid   DNA synthesis in plasmodium


Pyrimethamine are inhibit the folate reductase. That also inhibit the conversion of dihydrofolate to tetrahydrofolate. Further, prevent the formation of folic acid in plasmodium. 

Same as, dapsone and sulphadoxime are prevent the formation of PABA to dihydrofolate. Then, further, block the folic acid synthesis and DNA synthesis in plasmodium.

 

Side effects of malaria drugs (pyrimethamine and proguanil)

 Pyrimethamine are produced occasional side effect like nausea and skin rashes.

 High dose of pyrimethamine produce some side effect include megaloblastic anaemia and granulocytopenia.

 It is not taken during pregnancy because produce a teratogenic effect.

 Proguanil are produce some side effect include skin rashes, nausea, vomiting, diarrhoea, abdominal pain and haematuria.  


Antibiotics

example of antibiotics

tetracyclin 

doxycyclin

clindamycin


Tetracyclin, doxycyclin & clindamycin 

This all antibiotics are slow-acting on all Plasmodium species. That is weak erythrocytic schizontocidal effect produce.

But, these antibiotics do not affect the hepatic stages.

Used with artemisinin and quinine. Tetracyclin are never used to alone a treat the malarial infection.

Doxycycline is alone used against the multidrug-resistant the strain of malaria. But, clindamycin is safely in such cases.


side effect of malarial drugs (antibiotics)

 heart-burn

 stomach upset

 sun-burn & trush

 Tetracycline is not used during pregnancy because produce a teratogenic effect.


Artemisinins derivatives

example of artemisinins derivatives

artesunate

artemether

arteether


Artemisinin derivatives are derived from the artemisia annua. Some of the drugs are semisynthetic artemisinin include artesunate, artemether, arteether, dihydroartemisinin. Arterolane is synthetic artemisimin drugs.

 

Mechanism of artemisinin derivatives like this,

Haeme iron through breakdown the endoperoxide bridge artemisinin compounds  generate a free radical   that free radical are damage the lipid peroxide and protein   finally death of parasite.

 

Artemisinin derivatives are rapid-acting, highly potent and produce a faster clinical cure than other antimalarial drugs. produce a gametocidal action. But, no effect on hepatic stage. They reduce the transmission of the malarial parasite.

 

Side effects of malaria drugs (artemisinin derivatives)

 It produces some gastric disturbance include nausea, vomiting, epigastric pain, itching and abdominal pain.

 Also produce some adverse effect like headache, tinnitus, dizziness and bleeding a dark urine.

 When patient improved or drug therapy stopped produce some a rare side effect like leukopenia and transient reticulopenia, S – T segment changes and QT prolongation.

 Parenteral artesunate is much safe than parenteral quinine. And faster parasite clearance than parenteral quinine.

 When given a combination with astemizole, antiarrhythmics, tricyclic antidepression and phenothiazines increase the risk of the cardiac defects.

 The half-life of artemisinin are short and not used for chemoprophylaxis. Also, a not used in monotherapy.

 

Some other drugs like halofantrine and atovaquone are used in malarial infection. But, generally, these drugs not used in the world wide like these drugs used in the USA and other country but not used in India these drugs are not approved.

 

CONCLUSION:

The various side effect of malaria drugs produce based on their mechanism of action and site of action. Here, I will discuss all classes mechanism of action side effect and such details. if you like it comment out.

 

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