Immunomodulators & Antineoplasts

Front 1

Methotrexate
folic acid antagonist with cytotoxic,
immunosuppressive and anti-inflammatory action

Back 1

D; Antineoplast,
individual protocols
Arthritis/Psoriasis,
5 – 25 mg ONCE WEEKLY
15-25mg weekly chrons disease
I: Treatment and palliation of
solid tumours, lymphoma
and leukaemia
Severe disabling psoriasis
Rheumatoid arthritis

SE: Myelosuppression
(neutropenia,
thrombocytopenia)
GI side effects (mucositis,
ulceration, n, v)
Pulmonary toxicity
Hepatotoxicity
Rash, urticaria, itch
Photosensitivity
ADEC Cat X

Hint 1

5, 8, 10a, 20, 21
! Take tablets strictly as directed.
They should be taken ONE A
WEEK on the same day each
week; they must not be taken
every day.
! Tell your doctor if you have a
cough, difficulty breathing or signs
of infection.
! Avoid excessive or prolonged
sun exposure, wear protective
clothing and use sunscreen.
! Use of some medications
together with methotrexate may
lead to toxicity; tell your doctor and
pharmacist that you are taking this
drug.
! You may need to attend regular
blood tests and medical
consultations while being treated
with this medication.
! Take a folic acid (5 mg) tablet
on every other day than that of the
methotrexate to reduce GI side
effects.

MONITOR:
FBC, RF, LFT every 2-3weeks for the first 3 months
TDM- MTX [ ]
Sx of pneumonitis

Front 2

Cyclosporin

Back 2

Organ transplantation
8 – 15 mg/kg daily in 2 divided
doses
Rheumatoid arthritis, psoriasis
2 – 5 mg/kg daily

SE: gingival hyperplasia
hirsutism
nephrotoxicity
neurotoxicity (seizures)
hypertension
hyperkalaemia (care with
other drugs that cause this)`
hypercholesterolaemia
hyperglycaemia, increased
insulin requirements,
diabetes
opportunistic infections
myopathy, muscle weakness

Hint 2

5, 8, 18
! Clean your teeth and gums
regularly.
! Swallow capsules whole and at
the same times each day.
! If you forget to take a dose at
the usual time take it as soon as
you remember. If it is almost time
for your next dose, skip the dose
you missed. Take your next dose
(normal amount) at the usual time.
note: can be used with diltiazem to
increase its t& and decrease dose
required

MONITOR:
QT intervals
Blood conc.
RF
LFTs
Glucose
Cholestrol levels
BP

Front 3

Aromatase Inhibitors
Aromatase enzymes (in fat, liver, muscle and breast tissue in postmenopausal women) convert
circulating androstenedione and testosterone to oestriol and oestradiol. Aromatase inhibitors reduce tissue oestrogen concentration.

Back 3

I: breast cancer (hormone receptive)

SE: hot flushes
headache
n/v
vaginal dryness
(anastrozole)
vaginal bleeding and
spotting (letrozole,
exemestane)
musculoskeletal pain
fractures
hair thinning

Hint 3

MONITOR:
BMD
Ca/VitD
VTE
Liver enzymes

Front 4

Anastrozole

Back 4

1 mg daily

vaginal dryness

Front 5

Letrozole

Back 5

2.5mg

vaginal bleeding and
spotting (letrozole,
exemestane)

Front 6

Exemestane

Back 6

25 mg daily

vaginal bleeding and
spotting (letrozole,
exemestane)

Hint 6

Exemestane best absorbed if taken
with food.

Front 7

Tamoxifen
Compete with oestrogen for receptor sites in breast tissue (antioestrogenic effect) inhibiting tumour growth. Also have estrogen agonist activity on endometrium, bone and lipids

Back 7

20-40mg daily
I: Hormone receptor-positive
advanced breast cancer
SE:
hot flushes, nausea, fluid
retention, headache, vaginal
discharge, menstrual
irregularity
musculoskeletal pain,
increased bone and tumour
pain
deep vein thrombosis,
pulmonary embolism

Hint 7

12+
If abnormal vaginal bleeding or
discharge, pain or pressure in the
pelvic region, blurred vision, or bone pain occur, seek medical advice.
- can cause endometrial cancer

MONITOR
plasma Ca

Front 8

Azathioprine;
metabolised to MERCAPTOPURINE which impairs cellular immunity, depresses cell proliferation and
inhibits cellular inflammatory
response through alterations of purine synthesis

Back 8

D: 1 mg/kg daily to a maximum of
2.5 mg/kg daily (5 mg/kg daily
for organ transplant). Monitor
haematologic response
(especially leucocyte count) as
a guide to dosing. Bone
marrow suppression limits dose

I: Prevention of organ
transplant rejection
Immunosuppression in
severe RA, SLE, IBD

SE: bone marrow suppression -
leucopenia,
thrombocytopenia, anaemia
immunosuppression #
infection
alopecia
GI upset (diarrhoea,
anorexia, nausea and
vomiting, mouth ulceration
and oesophagitis)
hepatitis

Hint 8

8, 21, A, B
! Tell your doctor immediately if
you have bleeding, increasedbruising or infection.
! Tell your doctor immediately if
you have bleeding, increased
bruising or infection.

Allopurinol reduces metabolism of
azathioprine, increasing the risk of
severe bone marrow toxicity. Reduce azathioprine dose to one-quarter to onethird of normal or consider an alternative drug (eg mycophenolate).

MONITOR:
WBC
LFTs

Front 9

CS

Back 9

Immunosuppression in
autoimmune disease and
transplantation.
Anti-inflammatory (IBD,
asthma, allergy and skin
conditions).
Chemotherapy-induced
nausea and vomiting.
Replacement therapy in
adrenal insufficiency

Hint 9

9, B
! Take with food
! Do not stop abruptly
! Take in the morning if once
daily dosing as may cause
insomnia if taken close to bedtime
! If you become ill, or have close
contact with someone with an
infection, chickenpox or shingles,
see your doctor
! This medication may affect your
mood, if affected speak to your
doctor

MONITOR:
BP
BGL
BMD
Electrolytes

Front 10

Glucocorticoid SE

Back 10

Glucocorticoid
GI effects (dyspepsia, peptic
ulceration, gastric bleeding)
Metabolic effects
(hyperglycaemia, diabetes)
Increased appetite, weight
gain
Insomnia
Psychological disturbances
(psychosis, euphoria,
depression)
Immunosuppression and
increase risk of infection
Myopathy, muscle weakness
Osteoporosis (long-term)

Front 11

Mineralocorticoid SE

Back 11

Mineralocorticoid
Salt retention
Oedema
Hypertension
ADEC Cat A

Front 12

Prednisolone

Back 12

Adult, 5 – 60 (0.5-1mg/kg) mg daily in
divided doses
Children
Asthma, 1-2 mg/kg once daily (for 3-5 days)

Front 13

Prednisone

Back 13

Prednisone is converted to prednisolone in the liver.

Front 14

Dexamethasone

Back 14

500mcg-4mg d in 2-4 doses

Hint 14

is potent glucocortical steroid with no mineralocorticoid activity.

Front 15

Fludrocortisone

Back 15

50 – 200 mcg daily

Hint 15

has predominantly mineralocorticoid activity and is thus used for Mineralocorticoid replacement in adrenal insufficiency, with a glucocorticoid.