Escolar Documentos
Profissional Documentos
Cultura Documentos
Cyclophosphamide/
ifosfamide
Cisplatin
Carboplatin
MOA
Metabolically activated by
liver to Phosphoramide
mustard which forms
DNA cross links between
(interstrand cross-linkages)
and within (intrastrand
cross-linkages) DNA strands
at guanine N-7 positions.
This leads to cell death.
ci-SPLAT-IN == splatsound
made when vomiting, goes
IN dna to bind
Methotrexate
Use/Treatment of
ANTINEOPLASTICS
Alkylating Agents
Breast cancer
Lymphoma
Acrolein, a cytotoxic
metabolite causes
hemorraghic cystitis
(blood in urine)
chemotherapy-induced
nausea and vomiting
(CINV), bone marrow
suppression, stomach
ache, diarrhea, darkening
of the skin/nails, alopecia
(hair loss) or thinning of
hair, changes in color and
texture of the hair, and
lethargy
Notes/PK
6-Mecaptopurine
Converted to metabolite
(6-thioinosinic acid) that
inhibits purine biosynthesis
at several steps. S phase
specific
Nausea
Vomiting
Renal failure
Highly teratogenic
(pregnant women should
not take)
competitive inhibitor
Given IV, Intrathecal, OP
Renal Clearance
5-Fluorouracil
Actinomycin D
(Dactinomycin)
Bleomycin
Bleo-Mycin blows my DNA
to bits
Doxorubicin
Metabolised to FdUMP
which inhibits thymidylate
synthesis. Falsely
incorporated into DNA/
RNA
Metabolised to araCTP which inhibits DNA
polymerase, thus blocking
synthesis and repair.
Also falsely incorporated
into DNA leading to
interference in chain
elongation and defective
ligation of DNA fragments
Cytotoxic
Intercalate btwn strands to
block RNA/DNA synthesis
Cause DNA strand scission
Superoxide (free radical)
generation causing DNA
strand scission (blowing
DNA to bits)
Inhibits topoisomerase II
Cause DNA strand scission
Colorectal cancer
Acute inflammatory breast
cancer
Pancreatic cancer
myelosuppression,
mucositis, dermatitis,
diarrhea and cardiac
toxicity
Given IV
T1/2 = 10 minutes
Fever
Pulmonary fibrosis
Pulmonary toxicity
Allergies
Cardiotoxicity (caused
by oxygen radicalmediated damage to the
membranes)
Given IV
Given IV
Cytarabine given in conjunc
Vincristine
Vinblastine
Vindesine
Etoposide
Teniposide
eTOPoside action,
indications, side effect
Action: inhibits
TOPoisomerase Two (II)
Inhibits topoisomerase II
And so blocks cell division
in late S-G2 phase of the
cell cycle
eToposide & Teniposide
inhibit Topoisomerase Two
neuroblastoma,
Ewings sarcoma,
osteosarcoma,
rhabdomyosarcoma
Hematologic
malignancies multiple
myeloma, Hodgkins
and non-Hodgkins
lymphomas
Natural Products
Hodgkins disease
Lymphomas
Vinblastin (also breast cancer,
germ cell cancer)
Vincristine (also Ewings
sarcoma, Wilms tumor)
Nausea
Vomiting
Bone marrow suppression
Nephrotoxicity
Alopecia
Vinca alkaloids
Derived from Madagascar
periwinkle plant (Vinca rosea)
Vincristine - neurotoxicity
Alopecia
Indications: Testicular
Inhibits topoisomerase I
which is responsible for
cutting a ligating single
DNA strands DNA
damage
Inhibits microtubule
disassembly
Prednisone
Testosterone
Oestradiol
Megestrol
Goserelin
Leuprolide
Tamoxifen
Campothecin
Derived from Campotheca
acuminata
Campothecins affect
topoisomerse I, as opposed
to your podophyllotoxins
Taxanes
Given IV
Cushings Syndrome
Masculinisation
Gynaecomastia
Glucocorticoid
Androgen
Estrogen
Fluid Retention
Progestin
GnRH analogues
Nausea
Hot flushes
Amenorrhoea
Anti-estrogen
Active metabolite produced
(monohydroxytamoxifen)
Given orally
Highly protein-bound
Flutamide
Nilutamide
Finasteride (Proscar)
Competitive antagonist at
androgen receptor
5--reductase enzyme
inhibitor
Interleukin-2
Interferon-
Trastuzumab (Herceptin)
Immunotherapy
Prostate cancer
Prostate cancer
Benign prostatic hyperplasia
Androgenetic alopecia (male
pattern baldness)
Gynaecomastia
Fluid retention
Impotence
Abnormal ejaculation
Decreased ejaculatory
volume
Abnormal sexual function
Gynecomastia
Rectile dysfunction
Ejaculation disorder
Testicular pain
Anti-androgen
Cardiac dysfunction
Anti-androgen
(5-alpha reductase,
the enzyme that
converts testosterone to
dihydrotestosterone (DHT)
Miscellaneous
Bevacizumab (Avastin)
Use of monoclonal
antibodies
Binds to the domain
IV of the extracellular
segment of the HER2/neu
receptor. Cells treated
with trastuzumab undergo
arrest during the G1 phase
of the cell cycle so there is
reduced proliferation
Binds to and prevents
VEGF-A from interacting
with the target VEGF
receptor, thus inhibiting
a major factor in tumor
Breast cancer
Hypertension
Increased incidence of
arterial thromboembolic
events (angina, MI, stroke,
transient ischemia attack)
L-asparaginase
Hydroxyurea
Inhibits
deoxyribonucelotides via
inhibition of the enzyme
ribonucleotide reductase
polycythemia vera
Wound healing
complications
GI perforations
Proteinuria (excess protein
in urine)
Heptatotoxicity
L asparaginase affects the
LIVER (hepatotocity)
Myelosuppression
and oxaplatin-based
chemotherapy in the
treatment of metastatic
colorectal cancer
Given OP
essential thrombocytosis
Sickle-cell disease
AIDS
Psoriasis
Mitoxantrone
Procarbazine
Topoisomerase II inhibitor
Systemic Mastocytosis
metastatic breast cancer, acute
myeloid leukemia, and nonHodgkin's lymphoma
also used to treat multiple
sclerosis (MS)
Hodgkins lymphoma
Gliobastoma multiforme
Mild nausea
Vomiting
Alopecia
Somatitis
Leucopenia
Cardiotoxicity
D/I with alcohol
causes a disulfiramlike reaction in some
patients (unpleasant
hypersensitivity to
alcohol)
It also inhibits the liver's
Alkylating agent
One of the MVPP drugs
(mechlorethamine,
vincristine, procarbazine,
prednisone) for HL
One of the PCV drugs
CYP450 microsomal
system, which leads
to an increased effect
of barbiturates,
phenothiazenes, and
narcotics normally
metabolized by the
CYP450 enzymes.
Diphenhydramine
Mepyramine
Chlorpheniramine
Cyclizine
Meclizine
Chlorcycline
Promethazine
Promethazine is the most
POTENT sedative
1. Ethanolamines eg.
Diphenhydramine,
Dimenhydrinate
2. Ethylenediamines eg.
mepyramine
3. Alkylamines eg.
chlorpheniramine
(procarbazine, lomustine/
CCNU, vincristine) for
malignant gliomas
Ethanolamine
Ethylamine
Long duration of action
Alkylamine
Piperazines
Phenothiazine
Generally H1 antagonists
block H1 receptors,
but may also block 5HT
receptors (cyproheptadine),
1-adrenoceptors
(promethazine) and
muscarinic receptors
(diphenhydramine), but
have higher affinity for
H1 receptors (this is
resp. for a lot of the side
effects associated with
antihistamines)
PiperidinesTerfenadine Astemizole,
Loratadine (claritin)
PiperazinesCetirizine
Phenothiazines-mequitazine
Nizatidine
Cimetidine
Famotidine
Ranitidine
Nausea
Vomiting
Muscle pains
Diarrhoea
Gynecomastia
Decrease in sexual
function
Bradykinin
No specific drugs
In smooth muscle:
ASTHMA
DIARRHOEA
Causes release of cytokines
such as TNF
Causes bronchioconstriction,
increases fluid secretion
TRIGGERS ABORTION
Sumatriptan
Ketanserin
Cyproheptadine
Pizotifen
Ergot alkaloids :
(methysergide and
dihydroergotamine )
Pizotifen
Ketotifen
Extrinsic asthma
More selective
Ondansetron
Tropisetron
Granisetron
Gimeprost
Misoprostol
Dinoprostone (PGE2),
Dinoprost (PGF2) or
Misoprostol
PGE1 analogues
Given intravaginally
Dinoprostone Given
intravaginally as gel or
tablets, or extra-amniotically
as solution
Carboprost (15-methyl
PGF2)
Postpartum haemorrhage
(haemorraghing following
labour)
Given IM
Alprostadil (PGE1)
Impotence
Misoprostol
Epoprostenol (PGE2)
fluid secretion in
intestines, relaxes GIT
smooth muscles
Inhibits platelet
Haemodialysis
aggregation (replaces
heparin where it is
contraindicated)
Zafirlukast
Antagonists of the
leukotriene receptorsCysLT receptor antagonists
Montelukast
Antagonists of the
leukotriene receptorsCysLT receptor antagonists
Iralukast
Antagonists of the
leukotriene receptorsCysLT receptor antagonists
Asthma
In preclinical stages of
development
Zileuton
Piripost
Sulphonamides
-Sulfamethoxazole
-Sulfadoxine
-Sulfacetamide
Competitively inhibits
dihydropterate synthetase,
thus inhibiting folic acid
formation
-Sulfamethoxazole:
Absorbed and excreted
rapidly, t1/2 = 11 hours
Bacteriostatic
Anti-inflammatory agents
Anti-asthmatics
ANTI BACTERIAL
Antimetabolites
Antibacterial
Antimalarial
Broad spectrum:
-Streptococci spp
-Haemophilus spp
-Nocardia spp
-Actinomyces spp
-Chlamydia spp
-E. coli
-Sulfadoxine:
Absorbed and excreted
slowly (longer lasting), t1/2
= 100-230 hours
Hypersensitivity rxns
-uticarial rashes
-exfoliative dermatitis
-erythema multiforme
-Steven-Johnson
syndrome
Photosensitivity
sunburn
Urine stone formation
Opportunistic infections
due to broad spectrum
-Sulfacetamide:
Poorly absorbed, only used
topically (eye drops)
Trimethoprim
Cotrimoxazole
Antibacterial
Antimalarial
Broad spectrum:
-Streptococci spp
-Haemophilus spp
-Nocardia spp
-Actinomyces spp
-Chlamydia spp
-E. coli
UTIs
RTIs
Otits media
Pneumocystsis carinii (fungi)
Toxoplasmosis (protozoa)
Penicillins
Benzylpenicillin & its long
acting parenteral forms
BENZYLPENICILLIN (PEN G),
BENZATHINE PENICILLIN,
PROCAINE PENICILLIN
Inhibits peptidoglycan
cross-linking by binding to
transpeptidase (penicillin
binding proteins) thus
inhibiting cell wall
formation
UTIs
Syphilis
Typhoid fever
Rheumatoid fever
Bacterial endocarditis
Generally safe
Allergic rxns :
rashes, pruritus (intense
itching), anaphylaxis, S-J
syndrome , appx 10% of
patients
Bacteriocidal
Orally absorbed penicillins
resembling PEN G:
PHENOXYMETHYLPENICILLIN
(PEN V)
broad spectrum
agents associated with
superinfections.
CNS concentrations>
10mg/l = drowsiness,
convulsions, death
Penicillins resistant to
staphylococcal Betalactamase:
CLOXACILLIN, METHICILLIN,
NAFCILLIN, OXACILLIN
Extended spectrum
penicillin:
AMPICILLIN, AMOXYCILLIN,
MECILLINAM
Penicillins active against
Pseudomonas:
CARBENICILLIN, TICARCILLIN,
AZLOCILLIN
1st gen cephalosporins
Cephalothin (Keflin)
Cephalexin
Cefazolin (Ancef)
Cephapirin
Cephradine
Inhibits peptidoglycan
cross-linking by binding to
transpeptidase (penicillin
binding proteins) thus
inhibiting cell wall
formation
Cefadroxil(Duricef)
Bacteriocidal
RTIs
Otitis media
Acute sinusitis
Prophylaxis in abdominal
surgery
spleen.
Accumulation in
CSF greatest with
3rd generation increased with
inflammation
Readily distributed
info body fluids and
cross placenta
Excreted mainly
unchanged- via
tubular secretion,
Some undergo
excretion by bile
Meningitis
Otitis media
Most do not cover
Pseudomonas
Pseudomonas aeruginosa
Stapylococci
Carbapenems
Imipenem (Primaxin )
Meropenems (Merrem)
Spectrum: broad
(Beta-lactamases are
produced by the bacteria
and make them resistant to
bacteria)
Monobactams
Aztreonam (Azactam)
Moxolactam
Vancomycin
Binds to d-alanyl-d-alanyl
terminal subunits through
hydrogen bonding and
therefore terminates crosslinking to form cell wall
layers
Immediately Bacteriocidal
Polymycin B
Binds to
lipopolysaccharides in the
cell membranes-disrupting
integrity of both inner and
outer lipid membranes of
gram negative organisms
Isoniazid
= leaky membranes
Pro-drug , only activated
by bacterial catalase
to form isoniazid- NADH
Inhibition of mycolic acid
synthesis
Tuberculosis
Bacteriocidal
Aminoglycosides
-STREPTOMYCIN
-GENTAMICIN
-PAROROMYCIN
-KANAMYCIN
-AMIKACIN
-TOBRAMYCIN
Binds to receptor on
30s ribosomal sub-unit
irreversibly to:
Prevent translocation of
peptidyl-tRNA from A site
to P- site
Blocks initiation of protein
synthesis
Causes misreading of the
Low TI
Pain at injection site
Nephrotoxic after one
week administration
(reversible with
discontinuation)=tubular
cell degeration and
mRNA codon
In-cooperation of
Incorrect AA cause
premature termination of
protein synthesis
infections
Mycobacterial infections
Staphylococcal
infections
Bacteriostatic and
bacteriocidal
sloughing
Not absorbed O
Ototoxic (degeneration of
auditory fibres, tinnitus,
deafness)-irreversible
NMJ blockage-decrease
Ach release
Allergic Rxn- rashes and
fever
Given parenterally
Do not penetrate cells,
tissues
However, concentrate
into renal cortical tissue,
endolymph and perilymph.
Low PPB
Tetracyclines
CHLORTETRACYCLINE
TETRACYCLINE
DEMECLOCYCLINE
MINOCYCLINE
OXYTETRACYCLINE
METHACYCLINE
DOXYCYCLINE
Genital infections
Acne (Propionibacterium)
TETRACYCLINE is
the semi-synthetic
derivative of
Chlortetracycline.
MINOCYCLINE,
DOXYCYCLINE &
METHACYCLINE
are semi-synthetic
Hepatoxoticity in
pregnancy (fatal)
Superinfections
diarrhea, thrush, vaginal
candidiasis.
Do not give babies and
pregnant women in the
first tri-mester: Ca probs
derivatives of
Demeclocycline.
Chloramphenicol
Bacteriostatic
Macrolides
Spectrum: Gram-positive,
AZITHROMYCIN
CLARITHROMYCIN
ERYTHROMYCIN
Bacteriostatic
Nucleic Acid Inhibitors
Metronidazole
Pyruvate dehydrogenase
(PD) acts as electron
donor to form reduced
metronidazole:
PD used by
anaerobic bacteria
and protazoaorganisms without
mitochondria
Reduced form
binds to DNA
(and proteins)=
destruction
Quinolones
First Generation
Nalidixic acid (NegGram)
Cinoxacin (Cinobac)
Second Generation
Class I:
Norfloxacin (Norflox)
Lomefloxacin (Maxaquin)
Enoxacin (Penetrex)
UTI
Gonorrhea
Chlamydia trachomatis
Respiratory infections
Metallic taste
Nausea
Headache
Epi-gastric pain
Paresthesia
Aldehyde dehydrogenase
inhibition
PRO-DRUG
Well absorbed O; peak 1-2
hrs.
t1/2 = 8 hrs
Eliminated renally
Pass into CSF, placenta, saliva
and breast milk
convulsions
4- quinolones with a
carboxylic acid moiety.
Class II :
Ciprofloxacin (Ciproxina)
Ofloxacin (Floxin)
inhibitors of
cyp450 (cyp3A4)
Third Generation
Levofloxacin (Levaquin)
Moxifloxacin (Avelox)
Sparfloxacin (Zagam)
Gatifloxacin (Tequin)
Fourth Generation
Trovafloxacin (Trovan)
WITHDRAWN
Isoniazid
(See notes in Antibacterials:
Cell Wall Inhibitors)
Rifampin
Inhibits DNA-dependent
RNA polymerase by
forming a stable drugenzyme complex.
Thus inhibiting RNA
synthesis
At higher doses inhibit
mammalian mitochondrial
RNA synthesis
ANTI TB DRUGS
bacteriocidal
Antidote: Pyridoxine
Rashes, Jaundice,
Vomiting
Flu-like syndrome = Fever,
Chills,
Thrombocytopenia
Nausea,anemia
Cholestatic jaundice
Hepatitis
Pyrizinamide
Ethambutol
Streptomycin
Pro-drug -Inactive at
neutral pH
Requires pH 5.5 for
activation-inside host cells
Destroys organism
intracellular only
Converted in mycobacteria
pyrazinoic acid-ACTIVE
FORM
Bacteriocidal mechanism
unknown
Selective drug
Inhibits arabinoside
transferase, disrupting cell
wall formation
The disruption increases
the lipophilicity of the wall,
increasing the entry of
other drugs eg. rifampin
Aminogylcoside
Tuberculosis
Tuberculosis
INDUCES CYTP450
(CYP34A)
INDUCES P-Glycoprotein
Toxic dose= 40-50mg/
kg daily causes severe
liver damage = Jaundice,
hepatic necrosis, death.
Tuberculosis
Activity directed at
extracelluar organism-does
not enter cells
Amantidine
ANTI VIRALS
Influenza A (H3N2,
H2N2 and H1N1)
Parkinsonism
nervousness, confusion,
hallucinations, seizures,
coma
C/I in patients with
epilepsy, pregnant and
nursing mothers.
Acyclovir
Idoxuridine
Vidarabine
Nausea
Vomiting
Headache
With topical
administration:
Local irritation, edema,
itching and corneal
clouding
Nausea, vomiting,
Zidovudine (AZT)
diarrhoea, contra
indicated in pregnancy
Anaemia, nausea fever
and headache, bone
marrow depression,
insomnia, abnormal
liver function. (DNA
polymerase in the host cell
is sensitive to AZT action
and may be the reason for
its toxic effect.)
Saquinavir
Ritonavir
Nelfinavir
Indinavir
Protease inhibitors
HIV-1 encodes aspartate
protease
This enzyme is required for
cleavage of polypeptide
precursor
This generates the
structural proteins and
enzymes of the viruses
which includes reverse
transcriptase
Protease inhibitors block
viral maturation and are
therefore active in acute
and chronically infected
cells.
HIV infection
Hyperglycaemia
Hepatoxicity
Gastrointestinal disorders
Metabolic abnormalities
and redistribution of fat.
Drug interaction with
other drugs metabolized
by the cytochrome p450
system.
Thymidine analog
Given orally or intravenously.
T1/2 = 1 hr, bioavailability =
60-80%.
Enters mammalian cell
by passive transport. AZT
enters CSF and brain tissues.
Metabolized in the liver
glucoronidation.
Probenecid inhibits liver
inactivation and renal
clearance. Tribovirine
antagonizes it.
20% is excreted unchanged in
the urine
Given orally, saquinavir
undergoes extensive 1st pass
metabolism.
Resistance develops in
treated patients over a
period of months and limits
their use.
Some protease inhibitors
may show reduced activity
due to high protein binding.
They inhibit the cytochrome
p450 system.
Actively reduced by
Interferon , and
Fever
Bone marrow depression
Hepatitis B and C
Rashes
Prevent the spread of herpes
zoster in cancer
Prevent the reactivation of
herpes simplex
Broad spectrum: DNA (HSV1/
2, HPV, VZV, HBV), RNA
(influenza, HCV)
Alopecia
Headache
Disturbances in thyroid,
cardiovascular and hepatic
function
Beta produced by
connective tissue
fibroblasts
Gamma produced
by T-lymphocytes
Binds to ergosterol-causes
pore formation; interfering
with membrane integrity
Fungicidal
ANTI FUNGALS
Broad spectrum
Nyastin
Binds to ergosterol-causes
pore formation; interfering
with membrane integrity
Hypokalemia
Nephrotoxicity (up to
80% ) Reversible (may
permanently reduce GFR)
Broad spectrum Fungicidal, only Nausea
for Superficial infections
Diarrhoea
Clotrimazole
Terbenafine
Inhibits ergosterol
formation by inhibiting
P450 cytochrome (Prevents
conversion of dimethyl
lanosterol to ergosterol)
Fungicidal
Fluconazole
Broad spectrum
Fungistatic
CRYPTOCOCCUS MENINGITIS
(drug of choice)
GIT upset
Nausea
Hepatitis (rare)
Steven-Johnson
Syndrome(rare)
Negligible inhibition of
p450 system of human
cells (unlike ketoconazole)
Pruritis, urticaria
INHIBITOR of
CYP450, neutrapenia,
epoxide (prevents
conversion on squalene to
squalene epoxide)
Flucytosine
Ketoconazole
Griseofulvin
dermatophytes
lymphocytopenia, hepatic
failure- Contra-indicated
in patients with hepatic
failure
Uracil analogue
Pro-drug
Athletes foot
Ring worm
Candidiasis (yeast infection)
Prostate cancer (anti-androgen)
Specific for dermatophytes as
it selectively accumulates in
newly synthesized keratinized
tissue
Inhibition of p450
Rashes
Pruritis
Inhibits mitosis by
interfering with the fungal
mitotic spindle. Fungistatic.
Once fungus enters these
keratinized-griseofulvin
cells, griseofulvin binds
to microtubules of fungus
and inhibits mitosis.
No effect on mature
infected cells.
IMMUNOSUPRESSANTS (used in transplants)
Cyclosporin
Tacrolimus
SELECTIVE
Suppresses cell mediated
reponses by:
Diffuses into the T cell
Binds to cyclophilin
cyclophilin-cyclosporine
complex binds to and
inhibits calcineurin
receptors inhibits
activation of transcription
factors neccesary for IL-2
synthesis
SELECTIVE
Suppresses cell mediated
responses by:
Diffuses into the T cell
Binds to cyclophilin
cyclophilin-cyclosporine
complex binds to and
inhibits FKBP receptors
inhibits activation of
transcription factors
neccesary for IL-2 synthesis
Hirsutism
Nephrotoxicity
Neurotoxicity
hepatotoxicity
Hypertension
Hyperkalemia
BUT NO BONE MARROW
DEPRESSION
Autoimmune disorders
24 hrs
Macrolide antibiotic
Nephrotoxicity
Given with
GLUCOCORTICOID
Neurotoxicity
Hepatotoxicity
Hypertension
Op (orally), iv
Hyperglycemia
Hepatic Cp450
Thrombocytopenia
7 hrs
Corticosteroids
Prednisolone
Dexamethasone
NON-SELECTIVE
Decrease IL-8, adhesion
molecules, GM-CSF
generation
Inhibit iNOS, leukotriene
synthesis, histamine
Prednisone used in
autoimmune diseases:
RA
SLE
MG (myastenia
gravis) paralyze
No Hirsutism
Cushings Syndrome
(buffalo hump,
hypertension, thin
skin, thin limbs, muscle
wasting, benign
intracranial hypertension,
Non-selective and so
suppresses the whole
immune system
Hepatic metabolism
release
PGE2 inhibition reduced
cox 2 expression
Reduce IgG production
Reduce complement
proteins
Cyclophosphamide
parasympathetic
nervous system (affects
muscles)
and suppressing
allograft (transfer of an
organ from one human
to a next) rejection
Extremely potent
immunosuppressive
Used to ablate lymphoid
elements in prospective bone
marrow transplant patients
Autoimmune disorders:
SLE, Hemolytic anemias,
Wegeners granulomatosis
Used in combination
with prednisolone & antilymphocyte globulin
Inactive until metabolised to
Acrolein and phosphoramide
Hepatic Cp450
Op, iv, im
3-12 hrs iv
Methotrexate
Folate antagonists-
Inhibits dihydrofolate
reductase and hence DNA
synthesis
Psoriasis(skin conditon)
refractory to other drugs
Hepatic fibrosis
Cirrhosis
Severe active RA
Pneumonitis
GIT epithelial damage
Basiliximab/Daclizumab
Moromonab CD3
Anti Lymphocyte Globulin
ANTI HELMINTHS
Benzimidazole
Piperazine
Bind to B-tubulin
& microtubule
polymerization; interfering
with membrane integrity
Blocks nicotinic receptors
Hypersensitivity
Anaphylactoid reactions
Aplastic anaemia
insomnia
Ataxia
Prodrug of 6-mecaptopurine
Diethylcarbamazine
Ivermectin
Pyrantel
Praziquantel
Niclosamide
ANTI MALARIALS
Chloroquine
Pyrimethamine
Increases pH of food
vacuole of plasmodium;
affecting its haemoglobin
digestion
Enters plasmodium, bks
peroxide bond, releasing
free radicals causing
cellular destruction
Co enzyme Q action
inhibition
DHFR inhibition
B-Artermether
Prevents a relapse
ANTI AMOEBALS
Diloxanide
Emetine/Dehydroemetine
unknown
Blocks protein synthesis
Artemisimine
Primaquine
anorexia
Cysticerosis
With Albendizole
Gametocidal; except to
P.falciparum
Cardiotoxicity, oxotoxicity
and peripheral
neuropathy
gametocidal
Haemolysis
CARDIOTOXIC
Chloroquine
Chlorotetracycline &
paramomycin
Metronidazole(Flagyl)
Pregnancy: teratogenic
effects