1 t
-C 1
I1
pr 1 ry I 1 •
1 1 l •1 '
1 • J • 1 •
I le I o 1n 1 •
r ' rte t. cl ng 11 1
I.I lur , h ort, d br ln 1 r
do 1 t:h•n 100 ,/1<9 ).
A h.1 sto11 Lt lo !col ll 1 li t l
froo tu y c,f ll'll oc;J WIii r 1 l
ln•tl t:ul or Roli e1ch (W Al ) 1n l • • • 1
n1cro .opic vx, in •inn o 1 l • 1 •
11v r, •,•lClln, th) roJ I, thy
I I1)1
Il rt.
I Ibon Dl'LOW 41\d ye. Th 0 n111lr t •
I•
100�, Jl('r k.1logr weight p r J�y ) - li;J
ed r t et 111 r t or 1n 0."'I yo l or do -r l l
colloi d pl at1 ,,n .1n thci rot thyroid t "50 flnll 10.00.::g/
-82-OTIIE'!l Aln'l'tlALAHI,1L DRUGS ( CONCISE ACCOUH'l')
Through tm generations, variouu attempta have been �ode
to troat •malaria fcvcrr. with whatever r:intcriala r ight be r,iodil)' at h nd. Cnc or the inter •11tin9 method• was th,., wearing of choL11::
nnd or:.ul to. Thia boc:o er. more intriguing con:.idcring the .fact
that o�c modern inveatigatoaa hove placed rlngc, banda, or cpiralc of vorlouo metal� on chicka infected with!• gRl11nac�1n
and Cound ao:nc protective c!fccto.
Var iouo and •,\1ndry inorganic material ::i hnve been <:Kh!bitcd for treatment of nolor1a. The uac of anti:iony, arsenic and ino�gllllic compound:. or these clemPnti: had little influence on actunl
therapy of rnnlat·io. llowcvt>r, it ia not. po:;slbl to mc-nt1on all the num.,rou.s r.ub1tarces tr at were <?ver Cl'lployed 11t one tine or
the other for the trcal1nent of m11l11r10. So.-�c of the noteworthy on�.i;
are hereby dlscu11aed.
QUllll.NC I Qu�ine remain• the corncri:tonc of invc.-otioationo of anti m�lorials, the best known of the ulkalo1ds ?rc.-.i;ent in tt.c cinchona tree. The recorded history of cinchona olkaloidc dotes to 1630, when cinchona bQck was u&ed to t.eat on intermittent
fever of or,�· Don Juan Cope� de Cannizzarce While be w;is in 3outh Anl•rico. The no�c cinchona �ao given the tree many yeor$ lotcr by o Swedish botuni11t Linn�. Cinchona bark woe introduced
into Europe about 1640. ror a long tll!le, Quinine, remained the
•
UNIVERSITY OF IBADAN LIBRARY
-83- ...
-only th�raprut1c agent !or olario until after the first World War. Many exploration progrllZll!les would not hove
boon poaeiblc �lthout th� lntroduct1on of Quinine, for instance th cola.:l:.ntion o! the .. �h!.rd 1.orld. Quinine olon!J
with chloroquino .uid �-J!o�,in3 or cloancd oo blood sch12.ontoci,Jc. It ?11111 no 11ctio1, on the pr1::iory or
cocondory exo-orythrocyc ic ticc.uc fonis of the parasite�
and therofore cannot bring olbout o radical cur� of Dolorin cour.ed by P. mnl cir: P. vivax or P. ov11l . It 1e not -
-effectively ,oTietociiul or aporontoeidol to P. falci�riru.
-Though quinine cannot pt-o\·cnt infection , it con r.upprc c lhc ayr.iptooi. of r.,.1lnrla ond bring II out r;,pid control of on cute at trick. It hac long be n ';no�'TI c a practic l <1;1ent for •
the tt otmenl oi clincic:111 rittacr of malarin. It ha bcon found to be lcnc effective: lhnn · hlcroqu1ne i,nll l:"opocrinc Qulnin<' hall rcgnln•d &1 !, nlflcl'lnce in the management of
chlor�_uinc-rcaistanl falcip�rw,, �nl arla . It 1o odmini� orocl by int:rav�noua drip to nan-ic"",unes r.uf.fcrin9 fro.a on ocut:o attack "
of folciporurn mnlarin in ar�a wh�rc chloroquine - rcnlstont stroin5 o: P. folcipoL-um ore known to - e,,ict, In the
t:r�at�cnt of relopolng vlvox m�lorio, a combination of chloroquine and pri;naquinc or!.' now in v09ue for II rodicol
cure, Quinine actions on the cordiova�cular ayalcr., ore
quallt,,ti•,cly i;i.'ldlor to those of l'jUinldine. though lcs!: pot�nt UNIVERSITY OF IBADAN LIBRARY
-oii-It haa a �light effect on Drnooth muocle other thon a litt�o oxytocic nction on the gravid utorua, e£pccially during the
third tr1moc:tcr of pre,rH1cy. In 11koletol mur.clo, il hoa a Curare-like effect on the motor-end plate and cau11eD a
lengthening of the tcf'roctory period. Quinine ciay dUiini:ih tetanic controctionu aocociated with various conditio.,o
and it haa been employed to lcri£cn the controctioni; of' lll)'otonin congP-nito and to provide a diagnoatic to11t for myaalhenia
gravia by aggravat�ng the oympto=s. Hany advarao affect• arc attibuted to 1 ·1nc adrniniotra�ion. Ona of Duch in Cinchonii:::i which dovolopn when the pla£ma lcv l of quinine exccedc 10-121:19/
litre. Sympto�s include flushed and sweaty Dkin, diz:inoa, nn uuca, vomiting and diarrhoea. Quinine irritate:, tho ga£tric mucoca,
cauaing nausea and pain.
There 111 hao�olyoia and in severe cas� 1� o to b��c� wator fov�r.
AIIODI,\OUINE: Thi a ia 7-chloro-4-( 3-dicthylM1no111ethyl--!
Hydroxy4nilino) quinolinc. Chloroquine Jrtd Amodiaquino are both 4-llJllinoquinolinos and ahnre similar pharmacological propertiob.
Allodiaquino 1s ftlao affective agoinat tho orythrocytic atogco of malaria end cannot cure tho relapsing fevers of!!.· v1vax,
P. 1111,1 ,ri.i and P. ovaln; plasi:iod1a rcsiatc11 t lo chloroquine is
, olao resi•tont to 11111odiaquine. Amodioquinc follows quilc much the
-UNIVERSITY OF IBADAN LIBRARY
-8S-Yellow pigmentation of face, nails, handH and palate hove been dcmonotratcd with amodlaquine only.
HEPACR!tlE I Al :-.o known o:i Atel>r inc and Qui nacrine was the 1st effective nyntnetic ontimolJrinl of low toxicity. The
standard { 100�9) malaria nupprceeivc oral do�e is readily nbaorbcd rrom the intestinal tr"ct �nd peak pla:imo lovels
arc reached within 8 hourc like Quinine and the 4-��ino quinolincu. Quinacrinc 1s a blood achizontcx:idc. With
contioous therapy all 4 types of human malaria can bo
ouppresscd.Malaria due to!• ovale, !!_.vlvax 1 f• malarinc will relapco a few weeks after discontinuing the drug because
quinac: rinc hos no effect. on exo-crythroc:ytic achi.:onta.
Crone resist.mcc occurs br.�wcen c:hl roquine nnd �cpoc:rine.
H�pac:rine is also one of the drug or choic: in the treat�ent of Tacniosis. In low doses as on Gntinolari 1, quinacrinc
produces ycllo11 staining Md SOMe infrequent .inc:idenc:c of minor psychotic reactions. Hopac:rine potent! 1tea tho toxic effect of the 8-C111inoquinolino.
Dihydro-tolntf! 1·educ:l se inhibitor •
Chloroguanide ( Pcogu .nil), Pyri1111ttham1no end Trimothoprir.l.
The Briti$h �or time ccseorchbr a COl!lplotely non Loxic:
anti-malocial for 11111aa chemoprophylaxia rcr.ul tcd in 119·\6 in
chloroquanide. UNIVERSITY OF IBADAN LIBRARY
•
• -55_
In 1948 Pyri.rnathar.1inc wao tantcd and round to be " h1.<;hly
offcctivc ont.1malnriol. Trir.lott,oprim � .. n ,1oitj.nll�· ,!Sc•lel.o;>ctl ao All l\ntil>actcriol (•nt, it oo not until 1760 o.ncl 1969 th.it
il:' • r.1alori"l octJ::ity ·�ab tuc.tt'J orul pro·.rod.
,\ll threo druc;in h11v11 been found to be stron9l y
sporontoci ol. Pyrimr lhaminc, the mo:.t j>otent of the three
hos bcon calculated to bo 2000 ticH:G oo to:r.ic to lhc onlnrin parasite co to the hor:t. They c,n prtvf'nC i.porogon}· in the
mosquito gul:. The threo dru�u con provide malaria chc-,oprOj!h ylaxii; provided they arc continued for at least 10 wcol:r: �f'' ....
lost infected mosquito bite and that there �re no ro 1•t11nt strain:. in lhc aroa. 'I'hey ar<' not u .cd for t:rcotnont ot ncutc attacks alone since their bloo ochitontocillal action 1:. very slow, Cbl.or09\\anide 1:: mctol:!oliscd to an oct!vc fo.cm
-trioz1nu r.ict:wolit • Th• plao od1c1dal effects o! the>:1c 3
ont.iJnaloriols aro clue to o del'ici .. ncy or tc!:'.e�k,drtlP.,lntc thllt reaul ts in inh1bi tion o! cell divioion c111d :.chizouony. Thie
inlcrfercnco �ith Col 1c ocid r.otabol 1:;m �xplains the ,,,ll.t:kcd
•
UNIVERSITY OF IBADAN LIBRARY
-s --
-blocl d of folic ac1d ��n�· cic t 2 dir. r nt cta;c long the I t,-wolic p thwoy. Pyr1n thc.'lino plurs qu1n1n c, o.."ld
Pyi:1 1 l hom!..-,c plu 1,ul 1 h n • C'.111 h doxin r �vocet :I unJ hovo boon off et.iv , bul, l ria ciatnncc to lh�co n 1
c0111b1n t1cnn of� n :lev lo;,, Pyr11 th ::iinc in c binati n :!.th
toxopln •
In document
Diseño de un dispositivo experimental de maquinado para aleaciones de aluminio silicio.
(página 43-49)