ddt 23

Question 1

whats an ideal anti malarial drug:

Answer 1

• not expsenive
• rapid speed of action
• works for exoerthycotic rather than just for the rbc
• potent activity against all plasmodium species
• very strong and safe for children and preggos

Question 2

— is an alkaloid from species cinchona

Answer 2

quinine
and its a 4-quinloin methanol

Question 3

quinine is a —- and the side effects are – but is still used for severe malaria although parenteral artesunate superior

Answer 3

• 4-quinloin methanol
• vasodilation , hemolytic anemia , mycorcardial deoresson , curare effect

Question 4

4-aminoquilonines and dertaives are developed from the prototype — and the deratives are:

Answer 4

• quinine e
  as:
  1- chlorquine
  2- hydroxychlorquin
  3- mefloquine
  -amadiaquin
• halofantrin ( a 9-phananthrenemathonal )

Question 5

for 4-aminoquinlines the — is not important and nitrogen must be a — and the best subsutiuent for R1 is — and the X chain length is

Answer 5

• chirality is not important
• trisubutuited usually ethyl
• Cl
  -c2-c5

Question 6

the mode of action for 40aminoquilines is — hypothesis and it states that:
plasmodium digest the hosts —
—- is the waste product and it contains ——
the free FPIX is — so its normally —
the drug-FBIX complex contains the toxicity which leads to —-

Answer 6

• FPIX
• hemoglobin
• hemozoin
• contains ferriprotoporphyivn IX ( FPIX)
• toxic , bound
• cell death

Question 7

— inhibits plasmodial dihydrofloate reductase

Answer 7

pyrimethamine

Question 8

– inhibits the dihydropterotate synthase

Answer 8

sulfadoxine

Question 9

— and — developed for prevention and treatment of chlorine resistant malaria and sometimes is used for intermitted preventative treatment ( IPT) for infarcts and pregnant women in regions with moderate to high or stable transmission

Answer 9

• prymithemaine and sulfadoxine

Question 10

—- is a 8-aminoquilones

Answer 10

pamaquine ( paraquine was marked later )
- its active against tissue ad heptatic stages

Question 11

— is often given with chloroquine to eradicate all stages of malaria

Answer 11

paraquine , and its not given long term to avoid toxity and resistance

Question 12

the mechanism of action of 8-aminoqulone is –

Answer 12

interference with the cell redox system and causes oxidative stress and eventually cell death ( produces : quinoneimine which are very reactive species )

Question 13

the structure of 8-aminoquinolines

Answer 13

• the second OCH3 on C4 or C5 increases the activity and the a second substuint increases the activity
• X can vary from C2 to C6

Question 14

tafenoquine is a —-
and it aims to provide —–
its highly affective for —-
and — dose for vivax

Answer 14

• 8-aminoquilines
• longer acting and more potent and less toxic agent than primaquine
• radical cure of relapsing malaria and caudal prophylaxis of p.vivax
• single dose

Question 15

—–is isolated from TCM and is template for synthetic dertaives and have reactive —- moity by ——

Answer 15

• artimisem
• endiperoxide
• free radical mechanism and oxidative damage to parasite membrane
• active in resistant and cerebral malaria
• cornerstone of ACT

Question 16

— is a cornerstone of ACT

Answer 16

artimsiem

Question 17

mechanism of artimisem

Answer 17

artimisem –> dihydroartominsm ( active metabolite ) which produces ethers where r= ch3 aka arthmether and esters which is sodium artesunate

Question 18

recommendation of malaria treatment :

Answer 18

• 3 days treatment with ACT that is short and sharp treatment
• all artimisem containtaing dertaives are partnered with other drug even though artimism is fast but alone is not a good drug so the effect will go away fast , that’s why we give it with another drug so it can be long lasting and more effective so fewer chance of resistance

Question 19

— is a newer derative of halofantrine and has an aryl amino alcohol and lipophilic substiunet

Answer 19

lumefantrine which is used in combination with artemther in falciparum malaria and acts over a longer period than rapidly acting artemther to eliminate the residual parasite than remain after artemether is cleared from the body and thus minimise the risk of recrudescence

Question 20

the risk of pregnancy areas of low transmission has — than non pregnanct adults
and areas of high and stable malaria trasmission most woman have —-
— supplemts is important
drug treatment includes —-
for prophlyxix —-

Answer 20

• 2-3 folds higher risk
• enough immunity so infection doesn’t usually result in clinical symptoms
• Fe supplements
• quinine I , clindamycin , artimesim II , III
• mefloquine

Question 21

malaria prophylaxis ( prevention ) can be — or —
and most common regimens are —-

Answer 21

• casual or suppressive
  (travels need covers , expert advice essential , generally 1 week before and up to 4 after , protection against bites is vital and post travel illness must mean consideration of possible malaria )
  -malarone ( atavoquone-pronguil )
• doxycylin
• maflaquine

Question 22

atovaquine is a — hydroxynaphthoquine and inhibits —– and impairs — and is synergistic with —–

Answer 22

• lipophilic
• electron transport in mitochondria
• pyrimidine sytheis
• pronguil ( malarone)

Question 23

common drug prescribed for travellers is doxycycline and it works for inhibiting —— and is used in malaria prophylaxis and especially if there’s mefloquine intolerance

Answer 23

• inhibition of prokaryote-like RNA
• its fat soluble and good tissue distribution

Question 24

some antibiotics are effective in malaria due to the presence of plasmid like organelle called

Answer 24

apicoplast

Question 25

tetracycline are active but are

Answer 25

slow acting

Question 26

avoidance and preventing mosquito bites :

Answer 26

Wear trousers, socks, and long sleeved shirts when outside between dusk and dawn
Apply insect repellents to exposed skin
30-50% diethyltoluamide (DEET)
pregnancy
children >2 months

Use bed nets (ITN) impregnated with insecticide
Tuck in under mattress
Re-treat with pyrethroids every 6 months
Resistance to pyrethroids reported in 41 countries

Question 27

the need for new therapy

Answer 27

2012: Pyronaridine, fixed-dose combination with artesunate
Once daily, 3-day treatment of acute, uncomplicated P. falciparum and blood-stage P. vivax malaria in adults and children over 20kg
Pyramax® will be registered in areas of low malaria transmission where there is reported artemisinin resistance and diminished efficacy of other ACTs

Question 28

vaccines and malaria :

Answer 28

RTS,S (Mosquirix)

Directed against sporozoites
50.4% effective vs. falciparum malaria in 6000 African children aged 5-17 months
45.1% effective vs. severe malaria
As only partially protective, will not obliterate need for antimalarial drugs
( VACCINES ARE ONLY PARTIALLY PROTECTIVE)