PHARMACOLOGY LECTURE

NOTES 2
P.BANDA
 1. ANTIVIRALS

• Viral infections are usually self-

limiting and resolve on their own and
do not require specific therapy. In
this discussion the focus is on drug
that are used in
• Herpes simplex and varicella zoster
infections
• Cytomegalovirus
• N.B: drugs used in HIV will be
discussed separately at a later stage.
• Herpes simplex and varicella zoster
infections
 Acyclovir

• Action: the drug belongs to

Nucleoside Analogue DNA
Polymerase Inhibitors that inhibit the
synthesis of viral DNA.
• It is activated by conversion to
monophosphate following
phosphorylation of the drug by
herpes thymidine kinase.
• The monophosphate is then
converted to a triphosphate
derivative by other intracellular
enzymes.
• The triphosphate derivatives are
potent inhibitors of viral DNA
polymerase and results into
termination of DNA synthesis and
thus inhibit viral replication.
• Presentation: tablet containing
200mg, 400mg, 800mg. Infusion vial
containing 250mg and 500mg.
• Sugar free suspension containing
200mg/5ml, 400mg/5ml.
• Cream containing 5% in 2g and10g
tube. An eye ointment containing 3%
4.5g tube.
• Indications: Herpes simplex and
varicella zoster.
• Dose: oral
• Herpes simplex 200mg (400mg in
immune compromised or impaired
absorption 5 times daily for 5 days,
child under 2 years half adult dose).
Prevention of recurrence 200mg 4 times
daily or 400mg b.d and interrupted
every 6-12 days. For Prophylaxis in
immune compromised 200mg-400mg 4
times daily.
• Varicella and herpes zoster treatment
800mg 5 times daily for 7 days, child
20mg/Kg 4 times daily for 5 days.
• For IV infusion give over an hour in
herpes simplex and varicella zoster
5mg/Kg every 8 hours.
Side effects:
• Rashes, GIT disturbances, rise in
bilirubin and liver enzymes, increase
in blood urea and creatinine,
decreases in haematological indices,
neurological reactions such as
dizziness, convulsions and psychosis.
• Caution: maintain hydration, renal
impairment, pregnancy and breast-feeding.

• Other drugs in this group include

Valacyclovir and Idoxuridine.

• Cytomegalovirus infection
• Gancyclovir: the drug is related to
acyclovir but more active against
CMV and is also more toxic and
therefore it is only to be given when
benefit outweighs risk.
• Presentation: capsule containing
250mg and IV infusion powder
containing 500mg.
• Indication: life and sight
threatening CMV infections in the
immune compromised individuals.
• Dose: by IV over an hour induction
5mg/Kg every 12 hours for 14-21
days. 7-14 days for prevention,
maintenance of 6mg/Kg for 5 days
per week
• Side effects: leucopenia,
thrombocytopenia, less frequent
anaemia, fever, rash, infections, GIT
haemorrhage, dizziness.
• Caution: monitor closely blood
counts, history of cytopenia.
 2. ANTIFUNGALS

• These are drugs which are used in

the treatment of fungal infections.
Fungi are pathogenic microorganisms
that possess a rigid chitnous
(polysaccharide that is principle
component of the exoskeleton of
fungi bodies) cell wall.
• Treatment of fungal infections is
generally more difficult and
problematic compared to treatment
of bacterial infections because of the
complex method of reproduction,
their structure and metabolism.
• Action: antifungals act by increasing
cell membrane permeability in
susceptible organisms by decreasing
potassium, sodium and nutrients in
the cell.
• The nature of treatment depends on
two important factors these been
 a. Type of fungus

• A mould- is a fungus that grows in the

form of multicellular filaments called
hyphae. Moulds are a large.
• Yeast- any of various small, single-
celled fungi of the phylum Ascomycota
that reproduce by fission or budding, the
daughter cells often remaining attached
• Dimorphic- fungi which can exist as
mould filamentous form or as yeast.
b. The location of the infection-
nails, hair, skin or systemic fungal
infection which is an indication of
serious immunologic compromise.
• In treatment of superficial fungal
infections, it is generally
recommended that oral medication
should be supplemented with topical
antifungal cream or ointment in
order to achieve better results and
treatment to minimum of four to six
weeks.
 Antifungals are classified as

1. Polyene
2. Imidazole
3. Triazole
4. Penicillin derived
5. Fluorinated pyrimidine derivatives
6. Others
 Polyene antifungals
• this includes Nystatin and Amphotericin
B
Nystatin
• Presentation: sugar coated tablets
containing 500, 000 units, suspension
containing 100, 000 units/ml, vaginal
pessaries containing 100, 000 i.u.
• Indications: oral and vaginal candidiasis
• Dose: oral intestinal candidiasis 500,
000 units qid doubled in severe
infections. Child 100, 000 units’ qid,
neonates 100, 000 units as a single
dose.
• In vaginal candidiasis insert 1-2
pessaries at night for at least 14
nights.
 Side effects:
• nausea, vomiting, diarrhoea at high
doses, local irritation, sensitization,
rash
• Contraindications: history of
hypersensitivity.
 Amphotericin B
• Presentation tablet containing
100mg, IV infusion containing 50mg.
• Indications: intestinal candidiasis,
systemic fungal infections
(cryptococcal meningitis)
• Dose: oral 100-200mg qid. By IV
infusion in systemic fungal infections
(0.25mg/Kg) or 250mcg/Kg body
weight daily gradually increased if
tolerated to 1mg/Kg daily. Maximum
dose for severe infection is 1.5mg/Kg
or on alternate days.
• Side effects: anorexia, nausea,
vomiting, diarrhoea, epigastric pain,
febrile reactions, renal toxicity, blood
disorders, neurological disorders
including hearing loss, abnormal liver
function (discontinue treatment).
• Caution: toxicity, pregnancy,
breastfeeding.
 Nursing Implication/considerations

• Monitor vital signs every 15-30

minutes during first infusion and
note changes in pulse and blood
pressure.
• Monitor blood studies Hb, Hct, K, Na
Ca, and Mg every two weeks.
• Monitor weight of the patient weekly,
as oedema is likely to ensue
• Monitor for renal toxicity; increase in
BUN and creatinine and if BUN is
>40mg/dl or if creatinine is >3mg/dl
drug may be stopped or reduce dosage.
• Monitor for Hepatoxicity; increasing
AST/ASL alkaline phosphatase and
bilirubin
• Monitor for allergic reactions; dermatitis,
rash, drug should be discontinued.
 Imidazole antifungals
• This group includes clotrimazole,
econazole. Isoconazole, ketaconzole
and tioconazole. They have active
against a wide range of fungi and
yeasts. Their major indication is in
the treatment of vaginal candidiasis
and dermatophyte infections.
 Clotrimazole

• Presentation: Pessaries containing

100mg, 500mg. Lozenges 1%,
Cream 1%, topical 505, vaginal
cream 1%, lotions 1% and solutions
1%.
• Indications: vaginal and vulval
candidiasis
• Dose: insert 2 pessaries at night for
3 nights, oral pessaries for 6 nights.
For oral drops after meals 3 times
and for fungal dermatosis apply
twice daily.
• Side effects: occasional local
irritation.
• Caution: antibiotic therapy, oral
contraceptives, pregnancy, diabetes
mellitus may affect the clinical
effectiveness of clotrimazole.
• Contraindications: hypersensitivity.
 Ketoconazole

• Presentation: tablet containing

200mg, suspension containing
100mg/5mls.
• Indications: Systemic mycosis,
serious chronic resistant
mucocutanous candidiasis, serious
GIT mycosis, resident dermatophyte
of the skin and finger nails (not for
toes).
• Dose: adult 200mg o.d daily with
food usually for 14 days. If response
is poor after 14 days continue until at
least 1 week after symptoms have
cleared and culture becomes negative.
Maximum dose 400mg daily.
• Child: 3mg/Kg body weight. In chronic
vaginal candidiasis 400mg daily with
food for 5 days.
• Side effects: nausea, vomiting,
abdominal pain, rashes, urticarial,
thrombocytopenia rarely,
gynaescomatia, fatal liver damage if
given more than 14 days.
• Caution: monitor LFT’s, avoid in
porphyria and pregnancy
• Contraindications: Liver impairment.
• Nursing Implications
• Assess for signs and symptoms of infection;
drainage, sore throat, urinary pain, haematuria
and fever.
• Obtain cultures for sensitivity tests before
beginning treatment.
• Monitor for Hepatoxicity; increased AST, ALT,
alkaline phosphatase, bilirubin, drug is
discontinued if hepatotoxicity occurs.
• Triazole antifungals- this group includes
fluconazole and itraconazole which are
absorbed by mouth. They are indicated for the
treatment of local and systemic candidiasis
and cryptococcal infections, also indicated in
the treatment of aspergillosis and
histoplasmosis.
• Fluconazole
• Presentation: capsules containing 50mg,
150mg and 200mg. Suspension containing
50mg/5mls, 200mg/5mls. IV infusion
containing 2mg/ml.
• Indications: acute and recurrent vaginal
candidiasis, tinea pedis, mucosal candidiasis,
corporis cruris and dermal candidiasis,
systemic candidiasis, cryptococcal infections
including meningitis.
• Used also in the prevention of cryptococcal
meningitis in AIDS, in immune-compromised
patients after cytotoxic treatment or
radiotherapy.
• Dose: vaiginal candidiasis single dose 150mg,
mucosal candidiasis 50-100mg for 7-14 days.
Tinea pedis, corporis cruris and dermal
candidiasis oral 50mg for 2-4 weeks. In
systemic candidiasis infusion 400mg initially
then 200mg daily and continued according to
patient response. In cryptococcal meningitis
800mg daily.
• Child over 1 year oral or IV 2mg/Kg body
weight. Systemic and life threatening
infections 3-6mg/Kg body weight and can be
increased up to 12mg/Kg body weight in child
aged 5-13 years.
• Caution: renal impairment, pregnancy,
breastfeeding, children (only if no alternative),
raised liver enzymes.
• Side effects: vestibular and auditory damage,
nephrotoxicity, antibiotic associated colitis,
nausea, vomiting, rash.
• Contraindications: child under 1 year.
• Nursing Implications
• Assess for signs and symptoms of infection:
clearing of CSF culture during treatment,
obtain culture and sensitivity baseline and
during treatment.
• Monitor for hepatotoxicity; increased AST and
ALT, alkaline phosphatase, bilirubin, drug may
be discontinued if toxicity occurs.
• Penicillin derived antifungals- in this group is
Griseofulvin and other drugs are selectively
concentrated on keratinized tissue. This makes
Griseofulvin to be the drug of choice for
widespread or intractable dermatophyte
infection. It is well absorbed by mouth but
inactive when applied topically.
• Griseofulvin
• Presentation: tablet containing 125mg,
500mg. Suspension containing 125mg/5mls.
• Indications: treatment of ringworm infections
of the skin, hair, nails namely tinea corporis,
tinea pedis, tinea cruris, tinea barbae, and
tinea capitis.
• Dose: adult 500mg daily in divided doses or as
a single dose. Child 19mg/KG body weight in
divided doses or as a single dose.
• Side effects: headache, nausea, vomiting,
rashes, photosensitivity, dizziness, fatigue,
agranulocytosis, leucopenia, lupus
erythematous, toxic epidermal necrolysis,
peripheral neuropathy, confusion and
impaired coordination.
• Caution: in breastfeeding, enhances the
effects of alcohol and may impair performance
of skilled tasks e.g. driving.
• Contraindications: hypersensitivity,
hepatocellular failure, lupus erythematosis,
and in pregnancy.
• Nursing Implications
• Administer the drug with high fat meal.
• Monitor INR Warfarin effectiveness may be
compromised.
• Fluorinated Pyrimidine Derivative Antifungals-
these include flucytosine. This is a synthetic
drug which is only active against yeast and has
been used for the treatment of systemic
candidiasis, crptococcosis and toruplopsosis.
• Flucytosine
• Presentation:
• Indications: systemic yeast and fungal
infections and as an adjunct to amphotericin,
cryptococcal meningitis.
• Dose: by IV oner 20-40 minutes adult and
child 200mg/Kg daily in 4 divided doses
usually for not more 7 days. In extremely
sensitive organism100-150mg/Kg daily and
treat for at least 4 months in cryptococcal
meningitis.
• Side effects: rare but may have nausea,
vomiting, diarrhoea, rashes, less frequently
confusion, hallucinations, convulsions,
headache, sedation, vertigo, altered liver
function tests, blood disorders including
thrombocytopenia and aplastic anaemia.
• Caution: renal impairment, elderly, blood
disorders, pregnancy and breastfeeding.
• Nursing implications
• Evaluate haematologic profiles before each
dose.
• Do not crush tablet.
• Inform patient to fall pregnant while taking
the drug.
ANTIMALARIAL DRUGS
• Artemether-Lumefantrine (coartem)
• Presentation: tablet containing 20mg
artemether and 120mg lumefantrine
• Action: the drug interfers with conversion of
haem, a toxic intermediate produced during
haemoglobin breakdown to non-toxic
haemozoin malarial pigment.
• Lumefantrine interferes with the
polymerisation process while artemether
generates reactive metabolites as a result of
interaction between its peroxide bridge and
haem-iron.
• Both drug elements inhibit nucleic acid and
protein synthesis with the malarial parasite. In
short the drug is a blood schizonticide.
• Indications: malaria caused by plasmodium
falciparum
 Dose:

WEIGHT IMMEDIATE AFTER 8 HOURS DOSE NEXT DAY DOSE DAY 2 TOTAL TABLETS

>35Kg 4 4 4 BD 4 BD 24

25-24Kg 3 3 3BD 3 BD 18

15-24Kg 2 2 2 BD 2 BD 12

10-14Kg 1 1 1 BD 1 BD 6
• Side effects: anorexia, sleep disorders,
headache, dizziness, palpitations, cough,
vomiting, diarrhoea, rash, arthralgia,
increased LFTs, and hypersensitivity.
• Caution: not to be used in cerebral malaria,
malaria prophylaxis, and other types of
malaria
• Contraindication: hypersensitivity, severe
malaria, first trimester of pregnancy, those
taking drugs that affect the QT wave,
disturbed electrolyte balance.
• Nursing implications
• Give drug with fatty foods
• For those unable to swallow tablets (infants,
children), tablets may be crushed and mixed with a
small amount of water.
• If vomiting occurs within 1–2 hr after
administration, a repeat dose should be taken. If the
repeat dose is vomited, give the client an alternative
anti-malarial drug.
• Store tablets from 15–30°C (59–86°F).
• Fansider (Sulfadoxine-Pyrimethamine (SP)
• Presentation: tablet containing 500mg sulfadoxine
and 25mg pyrimethamine.
• Action: inhibits folic acid metabolism in the
parasite, and prevents transmission by stopping
growth of the fertilized gametes. It is a
schizonticide.
• Indication: used in prevention of malaria
antenatally (Intermittent Presumptive Treatment
(IPT).
• Dose: 3 tablets after 16 weeks of gestation, 3
tablets after 4 weeks and finally 3 tablets after
another 4 weeks in the second and third
trimester respectively.
• Side effects: cutaneous reactions (Stevenson
Johnson Syndrome), toxic epidermal
necrolysis, nausea, vomiting, and stomatitis.
• Caution: blood dyscrasias, seizures, disorders,
G6PD, hepatic, renal diseases
• Contraindications: hypersensitivity, and
hepatic dysfunction
• Nursing interventions
• Monitor serum uric acid which may be
elevated and cause gout symptoms.
• Monitor liver function weekly- AST, ALT,
decreased appetite, hepatic status etc.
• Monitor renal before therapy and month after
month.
• Monitor mental status- affect, mood and
behavioural changes.
• Quinine
• Presentation: tablet (coated) containing 200
and 300mg, injection containing 150mg,
300mg/2mls.
• Action: inhibits parasite replications
transcription of DNA to RNA by forming
complexes with DNA of parasite. Ultimate
effect schizonticide.
• Indications: plasmodium falciparum malaria
• Dose: adult 600mg every 8 hours for 5-7 days.
IM 10mg/Kg diluted in saline or water for
injection repeated after 4 hours then 8 hourly.
IV loading dose 20mg/Kg body weight adult
dose over 4 hours in half litre dextrose 5%
with resting period of 4 hours then 10mg/Kg 8
hourly in half litre Dextrose 5% over 4 hours.
• Children 10mg/Kg body weight diluted in
saline or water for injection.
• Side effects: tinnitus, headache, hot and
flushed skin, nausea, abdominal pains, rashes,
visual disturbance, confusion, hypersensitivity,
thrombocytopenia, intravascular coagulation,
acute renal failure, hypoglycaemia.
• Caution: atrial fibrillation, conduction defects,
heart block, G6PD deficiency.
• Contraindications: hypersensitivity to quinine,
G6PD deficiency, optic neuritis,
thrombocytopenic purpura, tinnitus
• Nursing interventions
• Monitor BP, pulse and watch for hypotension
and tachycardia.
• Assess liver function weekly AST, ALT, bilirubin.
• Blood studies need to be done
• Assess for cinchonism: nausea, blurred vision,
vomiting, tinnitus, headache etc.
• Educate the patient on visual changes that
may occur as he/she is medication.
• Teach patient to insect repellents and ITNs.
Amodiaquine

• Presentation: tablet containing 200mg

and 600mg and 600mg amodiaquine
base as HCL or 153.1mg base as
chlorohydrate. Suspension containing
10mg/ml base.
• Indication: treatment of uncomplicated
malaria.
• Dose: 25-35mg base/Kg body weight
over 3 days for both children and adults.
• Side effects: leucopenia,
agranulocytosis, nausea, vomiting,
abdominal pains, diarrhoea, itching.
• Contraindications: hepatic
disorders, hypersensitivity. Not
recommended for prophylaxis.
Proguanil

• Action: inhibits plasmodial dihydrofoliate

reductase mainly through its active
metabolite. This inhibits folate production
in both pre-erythrocytic and erythrocytic
parasites. Usually given in combination
with Chloroquine as prophylaxis
• Presentation: tablet containing 100mg
• Indication: chemoprophylaxis of malaria
• Dose: 200mg once daily
• Side effects: mouth ulcer, epigastric
discomfort,, stomatitis, skin
reactions and hair loss.
• Caution: renal impairment,
pregnancy and foliate deficiency
• Contraindications: hypersensitivity
 Primaquine

• Action: its intermediate act as

oxidants that are responsible for
schizonticidal action as well as for
haemolysis and
methemoglobinaemia encountered as
toxicities.
• Presentation: tablet containing
26.2mg primaquine phosphate
(1.5mg primaquine base).
• Indications: adjunct in the Rx to
eliminate the liver stages of
infestation of Plasmodium vivax and
ovale.
• Dose: adult 15mg daily for 14-21
days; child 0.25mg/Kg body weight
daily for 12-21 days. Given after
treatment with other antimalarials.
• Side effects: nausea, vomiting,
abdominal pain, haemolytic anaemia
especially in G6PD deficiency.
• Caution: G6PD deficiency, pregnancy,
breastfeeding.
• Contraindications: patients undergoing
quinacrine therapy, acutely ill patients
with systemic diseases that present with
agranulocytopenia (rheumatoid arthritis,
lupus erythema).
DRUGS USED IN SCHISTOSOMIASIS (Schitosomicides)
 Mode of action

• These are known to interfere with

Calcium homeostasis in the parasite
causing muscular paralysis and
increasing cell membrane permeability
or they increase the cell permeability to
calcium in Schistosomes, causing strong
contractions and paralysis of worm
musculature leading to detachment of
suckers from the blood vessel walls and
to dislodgment.
 Praziquantel (Biltricide)

• Presentation: tablet containing

600mg
• Indications: schistosoma
japonicum, haematobium and
mansoni
• Dose: S. haematobium and mansoni
adult 40mg/Kg body weight.
S.japonicum 60mg/Kg body weight
• Side effects: malaise, headache,
dizziness, abdominal discomfort with
nausea, rarely urticarial.
• Caution: safety in children under 4
not established.
• Contraindications: hypersensitivitry.
• Nursing implications
• Tablets can be halved or quartered
 Oxaminiquine (vansil)

• Presentation: capsule containing

250mg.
• Indications: All stages of
Schistosoma mansoni infection,
including acute and chronic phases
with hepatosplenic involvement.
• Dose: oral 15mg/Kg in adults and
10-15mg/Kg in children
 Side effects
• CNS: Transitory dizziness,
drowsiness, headache; persistent
fever (in patients being treated in
Egypt); EEG abnormalities,
convulsions (rare).
• GIT: Anorexia, nausea, vomiting,
abdominal pain, elevated liver
enzyme concentrations.
• Hematologic: Increased erythrocyte
sedimentation rate, reticulocyte
count, and increased or decreased
leukocyte count. Skin: Urticaria.
• Urogenital: Red-orange urine.
• Contraindications: safe use during
pregnancy (category C), lactation, or
in children is not established.
• Caution Use: history of convulsions.
 Nursing Implications

• Supervise ambulation and use other

safety precautions because >30% of
patients experience dizziness or
drowsiness.
• If patient has a history of seizures,
the possibility of seizures is
increased because of drug action
(occurs within hours of drug
administration).
• Use caution while driving or
performing other tasks requiring
alertness because drug can cause
dizziness or drowsiness.
• Be aware that drug may change the
normal urine colour to a harmless
orange-red.
• Do not breast feed while taking this
drug without consulting physician.
 Metrifonate (Bilarcil)

• Action: the drug is an

organophosphorus cholinesterase
inhibitor that results into
schistosomicide action.
• Indication: S. haematobium
• Dose: 7.5-10mg/kg once after a 2
week interval in 3 does
• Side effects: mild Git disturbance,
abdominal pain, diarrhoea,
flatulence, nausea, leg cramps and
slight decrease in heart rate and
vertigo.
• Contraindications: GIT, heart and
glaucoma disorders
• Overdosage (antidote): Atropine
sulfate (for adults, 1 mg every 6
hours) may be used as a specific
antidote to relieve symptoms of
cholinergic activity. This does not
impair the antiparasitic action.
Nursing implications
• Metrifonate tablets should be kept in
tightly closed containers and stored at
a temperature not exceeding 25 °C,
preferably in a refrigerator.
• Discoloured tablets should be
discarded.
• Avoid drug in pregnancy as the drug
is teratogenic or embryotoxic
• Not to given to breastfeeding mother
as drug is excreted in breast milk.
• Other drugs in this group include
Hycanthone, Lucanthone Niridazole
and Sodium Stibocanptate
DRUGS IN WORMS (Anthelmintics)

BENZIMIDAZOLES
• Mode of action
• These drugs are generally called
benzimidazoles. They act by binding to
tubulin, preventing its polymerisation
into cytoskeletal microtubules. The
effect is selective for parasitic tubulin
and the drugs are active against the
adults, larvae and eggs.
 Mebendazole (vermox)

• Presentation: tablet containing

100mg and suspension 500mg/5ml
• Indications: in trichuris trichura
(whipworm), enterobius vermicularis
(pinworm), threadworms, ascaris
lumbricoides (roundworm), and
ancylostoma duodenal (common
hookworm).
• Dose: threadworm adult and child
over 2 years 100mg single dose,
whipworm adult and child over 2
years 100mg twice daily for 3 days
or 500mg single dose, roundworm
adult and child 100mg twice daily for
3 days, hookworm adult 100mg daily
for 3 days.
• Side effects: abdominal pain,
diarrhoea, hypersensitivity reactions-
erythema, rash, urticarial and
angioedema
• Caution: pregnancy especially in
first trimester, breastfeeding, safety
in children less than 2 years not
established.
• Contraindications: hypersensitivity.
Nursing Implications
• Initiate second course of treatment if
cure does not occur within 3 week.
• Examine and treat all family
members simultaneously because
pinworms are readily transmitted
from person to person.
•
 Albendazole

• Presentation: 200 mg tablets

• Actions: Albendazole is a broad-
spectrum oral anthelmintic agent. It
is the only anthelmintic drug active
against all stages of the helminth life
cycle (ova, larvae, and adult worms).
• Its mechanism of action is unclear,
but it appears to cause selective
degeneration of cytoplasmic
microtubules in the intestinal cells of
the helminths and larvae. In general
Albendazole ultimately causes
decreased ATP production in the
helminths, resulting in energy
depletion, which kills the worms.
• Indications: Treatment of
neurocysticercosis caused by the larval
form of pork tapeworm (Taenia solium),
hydatid disease caused by the larval form of
dog tapeworm (Echinococcus granulosus).
• Contraindications: Hypersensitivity to the
benzimidazole class of compounds or any
components of albendazole; pregnancy
(category C).
• Caution: Retinal lesions, lactation.
 DOSE
Neurocysticercosis
Adult/Child: PO >6 y, weight <60 kg, 15 mg/kg/d divided b.i.d. for 8–30 d cycle (max: 800
mg/d); weight 60 kg, 400 mg b.i.d. for 8–30 d cycle

Hydatid Disease
Adult/Child: PO >6 y, weight <60 kg, 15 mg/kg/d divided b.i.d. (max: 800 mg/d); weight 60
kg, 400 mg b.i.d. for 28 d cycle (then 14 d without drug & repeat regimen for 3 cycles)
• Side Effects
• Body as a Whole: Hypersensitivity
reactions.
• CNS: Headache, dizziness, vertigo,
increased intracranial pressure,
meningeal signs, alopecia
(reversible), fever.
• GI: Abnormal liver function tests,
abdominal pain, nausea, vomiting.
Hematologic: (Rare) Reversible
leukopenia, granulocytopenia,
pancytopenia, agranulocytosis.
• Skin: Rash, urticaria.
• Drug interaction: Cimetidine,
dexamethasone, praziquantel increase
albendazole levels.
• Nursing Implications
• Lab tests: Monitor WBC count, absolute
neutrophil count, and liver function tests at
start of each 28-d cycle and q2wk during
cycle.
• Withhold drug and notify physician if WBC
count falls below normal or liver enzymes are
elevated.
• Note: Patients should be concurrently
treated with appropriate steroid and
anticonvulsant therapy.
• Give with meals. Absorption is
significantly increased with a fatty
meal.
• Do not exceed maximum total daily
dose of 800 mg.
• Store at 20°–25° C (68°–77° F).
 PIPERAZINE

• Mode of action
• The drug competitively inhibits the
effect of acetylcholine on the smooth
muscle of worm, producing a
reversible flaccid paralysis.
• The only Piperazine treatment
available is Pripsen Powder Sachets
which is Piperazine combined with a
mild laxative (senna). Piperazine
works by paralysing the worms
which are then evacuated by the
laxative action of the senna.
• A second dose of Piperazine is given
after 14 days to ensure that any
worms that were unhatched at the
time of the first dose will be cleared
from the system. Pripsen Powders
are the only drug treatment for
threadworms which can be given to
children under the age of two years
old (from 3 months of age).
• Presentation: syrup 750mg/5mls, oral
powder 4g
• Indications: threadworm and roundworm
• Dose: threadworms stirred in milk/water
adult and child 6years and above content
of 1 sachet as a single dose at bed time
repeated after 14 days. In roundworms
same dose as for threadworms and
repeated at monthly intervals for 3 months.
• NB: Read on Combantrin as individual drug
study assignment (other name, action,
indications, dose, side effects, cautions,
contraindications and nursing implications).
DRUGS USED IN TRYPANOSOMIASIS (Trypanocides)
 Melarsoprol

• Action: the drug reacts with

sulfhydryl groups of various
substance including enzymes in both
organism and host. The parasites
are more sensitive than host
enzymes as the drug has poor
penetrating power.
• Presentation: injection containing
3.6% melarsoprol
• Indications: meningo encephalitic
stage of African trypansomiasis.
Effective in both Gambian and
Rhodesian strains and is effective in
the early stages of the disease.
• Dose: IV slowly through a fine
needle and avoid leakage to tissue.
Adult 50mg or more; 3.5mg/Kg for
3-4 days and repeated after 7 days
and third same dose can be given if
needed after 10-21 days. In children
reduce dose accordingly and
underweight patients
• Side effects: pyrexia, reactive
encephalopathy, haemorrhagic
encephalopathy, hypersensitivity
reaction, hepatic damage, vomiting,
agranulocytosis and dermatitis.
• Caution: leprosy patients
• Contraindications: G6PD deficiency
and hypersensitivity
• Nursing Implications
• Ensure the patient is taking his
meals.
• Watch for convulsions and record
• Observe for level of consciousness as
the drug causes loss of
consciousness
 Suramin

• Presentation: injection containing 1g

suramin powder
• Indications: treatment of early
stages of both Gambian and
Rhodesian strains of trypanosomiasis.
Used as prophylaxis of the same. Also
used in treatment of late stages of the
disease involving CNS, it should be
given in combination with Melarsoprol.
• Dose: give initial test dose due to
toxicity between 100-200mg.
• Early stage A. trypanosomiasis
5mg/Kg body weight on day 1
• 10mg/Kg body weight on day 3
• 20mg/Kg body weight on days, 5,
11, 17, 23 and 30.
• Side effects: nausea, vomiting, loss of
consciousness are most common side
effects. Colic and acute urticarial are
some of the immediate side effects.
• Later popular eruptions, paraesthesia,
photophobia, hyperaesthesia of palms
and soles of feet,, albuminuria,
haematuria and crystaluria after
prolonged use.
• Caution: renal insufficiency, palmer-
planter hyperaesthesia as this
indicate peripheral neuritis
• Contraindications:known
hypersensitivity.
 Eflornithine
• (α-difluoromethylornithine or DFMO)
is a drug found to be effective in the
treatment of African trypanosomiasis
(sleeping sickness). The form of
Eflornithine is available for treatment
of sleeping sickness.
• Mode of action: Eflornithine
appears to kill trypanosomes by
acting as a suicide inhibitor of the
enzyme ornithine decarboxylase This
enzyme regulates cell division by
catalysing the first step in
polyamine biosynthesis.
• As the inhibitor has a low half-life in
humans, it is broken down rapidly
while the parasite cannot metabolise
it quickly enough. This means that it
preferentially or selectively harms
the parasite.
• Indications: Sleeping sickness
treatment
• Dose: Sleeping sickness is treated with
pentamidine or suramin (depending on
subspecies of parasite) delivered by
intramuscular injection in the first phase
of the disease, and with melarsoprol
and eflornithine in intravenous injection
(50 mg/kg every six hours for 14 days
in the second phase of the disease
 Pentamidine
• (formulated as a salt, pentamidine di
sethionate or dimesilate) is an
antimicrobial medication given for
prevention and treatment of
Pneumocystis pneumonia (PCP) caused
by Pneumocystis jirovecii (formerly
known as Pneumocystis carinii), a
severe interstitial type of pneumonia
often seen in patients with HIV
infection.
• The drug is also the mainstay of
treatment for stage I infection with
Trypanosoma brucei gambiense
(West African Trypanosomiasis).
• Action: The mechanism is not well
characterized, but there is some
evidence that it may involve
mitochondrial function. The drug
binds to parasite DNA and interfers
in the synthesis of RNA, DNA
phospholipids and protein of the
parasite.
• Indications: Treatment of
Trypanosoma brucei gambiense, also
used as prophylaxis in PCP patients
receiving chemotherapy,
leishmaniasis, and yeast infections
caused by the organism Candida
albicans. Pentamidine is also used as
a prophylactic antibiotic for children
undergoing treatment for leukemia.
Side effects
• Pentamidine can cause allergic and
toxic side effects, most commonly
having effects on the pancreas,
which in part depend on the daily
and/or cumulative dose:
• Blood: Pentamidine frequently
causes leukopenia and less often
thrombopenia, which may cause
symptomatic bleeding. Some cases
of anemia, possibly related to
folic acid deficiency, have been
described.
• Cardiovascular: Hypotension, which may be
severe, severe or fatal arrhythmias and
heart failure are quite frequent.
• Gastrointestinal: Nausea, vomiting,
gastrointestinal discomfort, diarrhea, unpleasant
taste.
• Kidney: 25 percent develop signs of
nephrotoxicity ranging from mild,
asymptomatic azotemia (increased
serum creatinine and urea) to
irreversible renal failure. Ample fluids
or intravenous hydration may
prevent some nephrotoxicity.
• Liver: Elevated liver enzymes are
associated with intravenous use of
pentamidine. Hepatomegaly and
hepatitis have been encountered
with long term prophylactic use of
pentamidine inhalation.
• Neurological: Dizziness, drowsiness,
neuralgia, confusion, hallucinations,
seizures and other central side
effects are reported.
• Pancreas: Hypoglycemia that
requires symptomatic treatment is
frequently seen. On the other hand,
pentamidine may cause or worsen
diabetes mellitus.[5]
• Respiratory: Cough and
bronchospasm, most frequently seen
with inhalation.
• Skin: Severe local reactions after
extravasculation of intravenous
solutions or following intramuscular
injection treatment have been seen.
• Pentamidine itself may cause rash, or
rarely Stevens–Johnson syndrome or
Lyell syndrome.
• Contraindications: severe allergy.