Download Antiameobic drugs

Anti-aembic and anti-malarial
drugs
By
Dr.Mohamed Abd AlMoneim Attia
Classifications
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1-Tissue amoebicidial:
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Metronidazole(Flagyl)
Chloroquine
Emetine and Dihydroemetine
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2-Luminal amebicidal;
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Diloxinade & etofamide
Iodoquinol & clioquinol
Paromomycin & Tetracycline
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Mechanism of action:
Ferrodoxine oxidoreductase enzyme
5-nitroimidazole
Free radical
Electron ransfer
Multiple DNA breaks
No replication
No transcription
No repair
Metronidazole
Indications:
 Tissue amoebicidal:
( intestinal,hepatic,pulmonary)
 Giardiasis
 Trichominasis
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Anaerobic infection:e.g
- serious infection caused by bacteroid fragilis
-enterocolitis cause by cl.difficil
-acute ulcerative vaginitis
-decubitus lesion
-to reduce postoperative infection following abdominal
surgery
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Side effects:
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GIT: bad taste in mouth,angular stomatitis,dry mouth
Dark red urine
CNS: headache,insomnia,parathesia
Blood:leucopenia & thrombocytopenia
Disulfiram like reaction in alcoholism
Phlebitis if given IV
Mutagenesis and carcinogenesis in mammalian
cell culture
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Contraindication & Cautions
Be caution if prescribe drugs to:
Patients with hepatic,brain,or blood disorders.
 Don't give it to pregnant , lactating or young
age.
 It increases the effects of oral anticoagulant
by decreasing its metabolism.
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Chloroquine
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Reach high concentration in liver so it is effective in hepatic
amoebiasis with little or no effect on intestinal or lumenal
one.
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Indication:
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Prevention of amoebic liver abscess during ttt of
intestinal amoebiasis
treatment of amoebic liver abscess in case of failure
or contraindication to flagyl
Following metronidazole for ttt of amoebic hepatitis
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Side effects: see antimalarial
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Emetine & dihydroemetine:
They inhibit protein synthesis by
preventing translocation
 Indication:
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Alternate therapy to metronidazole in treatment of
intestinal or hepatic amoebiasis
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Side effects:
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Cardiotoxic: hypotension and ECG changes
Pain at site of injection
Muscular ache, tenderness,stiffness & weakness
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Diloxanide Furoate
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-luminal amoebicidial
-not absorbed from GIT
-used to eradicate amoebae present in
intestinal lumen
-flatulence, dryness of mouth and vomiting
are infrequent side effects
-the drug is contraindicated in pregnancy and
in children below 2years of age
Iodoquinol
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-luminal amoebicidial
-used to eradicate amoebae present in intestinal
lumen
-Side effects:
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Thyroid enlargement due to high iodine content of the drug
N/V and diarrhea
-Contraindication:
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Thyroid, renal or hepatic disease
Shouldn't be used for prophylaxis or ttt of travelers or non
specific diarrhea
Stop it if persistent diarrhea or iodine reaction occur
Anti Malaria
PATHOPHYSIOLOGY and life cycle:
Anopheles mosquito inoculates sporozoites to human .
Sporozoites invade liver cells ( primary tissue phase).
Merozoites released from liver & invade erythrocytes .
Merozoites multiply, red cell enlarges ( blood schizont).
blood schizont ruptures, merozoites invade more RBCs.
Repeated cycles cause clinical illness, fever, etc.
In P. vivax & P. ovale some merozoite invade liver cells (
secondary tissue phase) & become dormant ( hypnozoites )
hypnozoites may develop again and cause relapse.
In P. falciparum & P. malariae no second liver phase.
Some merozoite -- gametocytes-- mosquito -- sporozoites
Life cycle of malaria
Anti- malarial drugs
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Classifications;
1-clinical cure: drugs used to treat the acute
attack of malaria by acting on the erythrocyte stage
of the parasite
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1-chloroquine-sensitive malaria:chloroquine
2-chloroquine-resistance malaria:
-Quinie
-mefloquine
-pyremethamine & proguanil
-sulphadoxine
-combination:
Fansidar = sulphadoxine + pyremethamine
Fansimaf = sulphadoxine + pyremethamine + mefloquine
II-chemoprophylaxis:
1-clinical prophylaxis: suppress the clinical
manifestation of malaria by killing parasite as soon as
they reach the RBCs .chloroquine, proguanil, fansidar
2-antirelapse therapy in P.vivax and ovale only by
killing the dormant stage in liver. Primaquine
3-prevent transmission by killing the gametocytes:
primaquine ,progunail ,pyremethamine
Chloroquine, hydroxy-chloroquine, amodiaquine.
CHLOROQUINE:
Mechanism and anti-malarial action:
Chloroquine ,accumulates in acid pH of RBCs & food
vacuoles of plasmodia, ↓ polymerization of heme to
hemozoin (food of malarial parasites).
Heme accumulates & cuases death of plasmodia.
Blood schizonticidal of all types of plasmodium.
Not effective against liver stages.
Uses:
 Treatment : Drug of choice for acute attack of P. vivax, ovale,
malariae, & non-resistant falciparum.
• (P. falciparum is becoming resistant)
 Prophylaxis: Effective in P. vivax & ovale regions. Also for P.
falciparum in non-resistant regions.
 Other uses: Hepatic amoebiasis & some autoimmune
diseases ( like, rheumatoid arthritis & SLE ).
Adverse effects:
Neurological: headache, anorexia, malaise, optic
neuritis & rarely seizures.
CVS: Cardiac depression, vasodilation & fall of
blood pressure.
Give slow IV infusion & monitor cardiac functions.
Heamatologic: Heamatolysis in G6PD deficiency.
Cautions/ Contraindications:
☻Visual defects, epilepsy, heart failure.
HYDROXY-CHLOROQUINE:
- Less likely to cause optic neuritis.
-Used in rheumatoid artharitis.
AMODIAQUINE:
- Can cause agranulocytosis.
- Recommended for chloroquine resistant malaria.
Quinine
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Therapeutic uses:
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Treatment of acute attack of chloroquine resistant P.falciparum
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Side effects:
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Cinnchonism : sweeting,nausea,vomiting,diarrhea,ringing in
ear,blurring of vision
Hypoglycemia
Hypotension and arrhythmias
Black water fever due to excessive haemolysis of RBCs in the
form of fever, acute renal failure and jaundice
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Mefloquine:
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Therapeutic uses:
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Treatment of acute attack of chloroquine
resistant P.falciparum especially mild and
moderate cases
chemoprophylaxis
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side effects:
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headache vertigo and visual disturbance
psychosis ,hallucination and confusion
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Antifolate;(pyremethamine,progunail,sulph
onamides):
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Therapeutic uses:
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Treatment of acute attack of chloroquine
resistant P.falciparum in combination with
Quinine
Chemoprophylaxis in chloroquine resistant
P.falciparum
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Side effects: see antimicrobials
Primaquine:
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Therapeutic uses:
The only drug that used in prevention of relapse in
P.vivax and ovale because it affects the dormant
liver stage
It has no effect on erythrocytic stage (not used in
acute attack)
Prevent transmission of infection from human to
mosquito by killing the gametocytes
Side effects:
Haemolysis in G6PD deficiency
Purities
methaemoglobinemia manifested by cyanosis
‫بسم هللا الرحمن الرحيم‬
‫‪‬‬
‫(اليكلف هللا نفسا إال وسعها لها ما كسبت و عليها ما‬
‫اكتسبت‬
‫ربنا ال تؤاخذنا إن نسينا أو أخطأنا‬
‫ربنا و ال تحمل علينا إصرا كما حملته على اللذين من قبلنا‬
‫ربنا و ال تحملنا ما ال طاقة لنا به و اعف عنا واغفر لنا و‬
‫ارحمنا أنت موالنا فانصرنا على القوم الكافرين)‬
‫صدق هللا العظيم‬
‫‪‬‬
‫‪‬‬
‫‪‬هذا و ما كان من توفيق فمن‬
‫هللا و ما كان من خطا أو‬
‫سهو أو نسيان فمني و من‬
‫الشيطان‪.‬‬
‫سبحانك اللهم و بحمدك نستغفرك و نتوب اليك‬
‫‪URTI:Throat infections‬‬