Akram Hussein
21/8/11 & 5/10/11
PHAR3823
Muskoskeletal Tute 1
Mr Elric
(Age: 66, CrCl = 35.33, High urea and urate levels , Diagnosis: HF, Gout, POA glaucoma, Depression )
Scenario 1
a) Questions for patient specific facts
a. Have you had this kind of rash before?
b. How long has this rash been?
c. Do you have any other symptoms?
d. Do you have any allergies?
e. What other medications are you taking?
f. What did the doctor tell you about these 2 medications?
b) Issues with prescribed medicines
a. Previous and current medications:
Medication
Celebrex
(celecoxib)
COX-2 inhibition,
resulting antiinflammatory and
analgesic action
Indication
-Rheumatoid
arthritis,
-Osteoarthritis,
-Acute gout
Dose
100 mg BD
Zyloprim
(allopurinol)
Reduces uric acid
production by inhibiting
xanthine oxidase, and
lowers plasma and
urinary urate
concentrations.
Allopurinol is
metabolised to
oxypurinol, which also
inhibits xanthine
oxidase.
-Gout, long-term
treatment
-Urate
nephrolithiasis or
acute uric acid
nephropathy
-Hyperuricaemia
secondary to
disease
(chemo/radioTP)
Gout, long term:
Initially, 100 mg
once daily,
increase by 100
mg daily each
month according
to response.
Usual
maintenance,
100–300 mg D
Astrix
(aspirin)
Inhibits platelet
Secondary
aggregation by
prevention in
irreversibly inhibiting
ischaemic heart
cyclo-oxygenase,
disease
reducing the synthesis
of thromboxane A2 (an
inducer of platelet
aggregation) for the life
of the platelet.
TCAs inhibit reuptake -Major depression
of noradrenaline and
-Nocturnal enuresis
serotonin into
presynaptic terminals.
Although unrelated to
the therapeutic effects
of the TCAs, they also
block cholinergic,
histaminergic, alpha1adrenergic and
serotonergic receptors.
Endep
(amitriptyline)
MOA
Long term, up
to 150 mg D
(low dose
aspirin)
Adult, 25–75 mg
daily, increasing
by 25–50 mg
every 2–3 days to
75–150 mg
daily. Maximum
300 mg daily
Counselling points
-Risk of cardiovascular adverse events
is dose-related; do not use >200 mg
daily long term
-Contraindicated in heart failure
-Celecoxib should be discontinued at
the first appearance of skin rash,
- Take after food (possible stomach
upset)
- Drink a lot of fluids to prevent
kidney stones
- May make you dizzy/drowsy
- Consider using low dose colchicine or
a low dose NSAID to prevent attacks
during the first 3–6 months of
allopurinol treatment (longer
preventive treatment may be needed if
attacks continue or if large tophi are
present)
- Check serum uric acid concentration
after 4 weeks and adjust dose; aim for
uric acid concentration <0.36 mmol/L
(failure to achieve normal uric acid
concentrations may indicate poor
compliance)
Common SE: GI irritation, increased
bleeding time
-You may get side effects such as
blurred vision, drowsiness and dry
mouth. They may be troublesome but
may lessen or disappear after about 7
days. Try taking this medicine at night
to reduce daytime drowsiness. Discuss
any problems with your doctor or
pharmacist.
Avapro
(ibersartan)
Dilatrend
(carvedilol)
Competitively block
binding of angiotensin
II to type 1 angiotensin
(AT1) receptors. They
reduce angiotensininduced
vasoconstriction,
sodium reabsorption
and aldosterone release.
Competitively block
beta receptors in heart,
peripheral vasculature,
bronchi, pancreas,
uterus, kidney, brain and
liver.
Antihypertensive effect due
to reduction in cardiac output
without reflex increase in
peripheral vascular resistance;
CNS effect and reduced renin
secretion may also contribute.
Antianginal effect due to
reduction in left ventricular
work and oxygen use,
resulting from decrease in
heart rate and contractility.
-Hypertension
-Heart failure in
patients unable to
tolerate ACE
inhibitors
-usually 150 mg
once daily;
increase if
necessary to
300 mg D
-Before starting a sartan stop
potassium supplements and
potassium-sparing diuretics; check
renal function and electrolytes and
review regularly
-Hypertension
-Stable mild-tosevere heart
failure, as an
adjunct to
conventional
treatments (eg
diuretics, digoxin,
ACE inhibitors
and vasodilators)
-Initially 3.125
mg twice daily
for 2 weeks;
increase at
intervals of at
least 2 weeks to
6.25 mg twice
daily, then 12.5
mg twice daily,
then 25 mg
twice D
-You may feel dizzy on standing when
taking this medicine. Get up gradually
from sitting or lying to minimise this
effect; sit or lie down if you become
dizzy
- Initially 20–40
mg once or twice
daily, adjusted
according to
clinical response
to maintenance
dose of 20–400
mg D.
Maximum dose 1
g daily.
75–150 mg
daily in 2 or 3
doses.
Maximum 200
mg daily
Gout—may be aggravated by diureticinduced Hyperuricaemia
Lasix
(frusemide)
Inhibit reabsorption of
sodium and chloride in
the ascending limb of
the loop of Henle. This
site accounts for
retention of
approximately 20% of
filtered sodium;
therefore, these are
potent diuretics.
-Oedema associated
with heart failure,
hepatic cirrhosis,
renal impairment
and nephrotic
syndrome
Voltaren
(diclofenac)
Have analgesic,
antipyretic and antiinflammatory actions.
They inhibit synthesis of
prostaglandins by
inhibiting cyclooxygenase (COX)
present as COX-1 and
COX-2:
ACE inhibitors block
conversion of
angiotensin I to
angiotensin II and also
inhibit the breakdown
of bradykinin.
-Reduce intraocular
pressure by increasing
uveoscleral outflow of
aqueous humour.
-Pain, especially due
to inflammatio
-Artificial tear
supplement providing
lubrication.
Coversyl
(perindopril)
Xalatan
(latanaprost)
Refresh tears
plus
(carmellose
0.5%)
Lipitor
(atorvastatin)
-Heart failure
Initially 5 mg D.
Max 10 mg D.
-Glaucoma
-Ocular
hypertension
1 drop once
daily, preferably
at night.
- Dry eye syndrome
- Relief of mild
ocular irritation
1 drop every 1–
12 hours prn
-HMG-CoA reductase - Hypertensive
(a rate-limiting enzyme
patients with
in cholesterol synthesis) additional risk
10–80 mg once
daily
Common SE: nausea, dyspepsia, GI
ulceration or bleeding
- Common SE: hypotension, cough,
hyperkalaemia, headache, dizziness,
fatigue, nausea, renal impairment
-These eye drops may slowly change
the colour of your eye making the iris
appear darker. This change is
permanent and may be more
noticeable when only one eye is being
treated.
- a paradoxical increase in intraocular
pressure may occur if 2 ocular
prostaglandin analogues are used
together; avoid combination
- The frequency of ocular irritation
differs slightly with the preservative
used
-Avoid grapefruit juice as it may
increase the amount of atorvastatin in
your bloodstream and could increase
inhibitor. Increase hepatic
cholesterol uptake from
blood, reduce concentrations
of total cholesterol, LDL and
triglyceride (modest), and
produce a small increase in
HDL concentrations.
the chances of side effects occurring.
factors for heart
disease
b. New script:
i. Phenergan (promethazine)
ii. Hydrocortison cream 1%
iii. Colgout
Phenergan
(promethazine)
OTC
Hydrocortison
cream 1%
(Dermaid,
Sigmacort,
Cortic-DS)
OTC
Colgout
(colchicine)
-Antagonise the action -Allergic conditions,
of histamine at H1
eg rhinitis,
receptors, reducing
conjunctivitis,
histamine-related
urticaria, contact
vasodilation and
dermatitis
increased capillary
permeability.
-Anti-inflammatory,
-Inflammatory skin
immunosuppressive and conditions (rash)
antimitotic activity
against cutaneous
fibroblasts and
epidermal cells. They
are also
vasoconstrictive.
Inhibits neutrophil
-Relief of pain in
migration, chemotaxis,
acute gout
adhesion and
phagocytosis in the
inflamed area; reduces
the inflammatory
reaction to urate crystals
but has no effect on uric
acid production or
excretion.
5–75 mg D, or
10–25 mg 2–3
times daily
Script:
25 mg nocte prn
-Apply to
affected areas 1
or 2 times a day.
Script:
Apply to rash bd
prn
Preventative:
0.5 mg D or
BD
(if CrCl < 50,
halve dose; may alt
days)
Scritp:
1 mg stat
followed by 0.5
mg q6h mdu
-This medication may make you
sleepy; don’t drive or operate
machinery if this happens.
Avoid alcohol and other medication
which may cause sedation.
- Avoid tolerance by applying
corticosteroid on alternate days or
using medication-free periods (eg 5
days on then 2 days off) during
treatment of chronic dermatoses
- Avoid grapefruit juice
- Stop taking this medicine, and tell
your doctor if you develop severe
diarrhoea or vomiting; muscle pain,
tenderness or weakness; numbness or
tingling in your fingers or toes;
unusual bleeding or bruising or an
infection.
- Colchicine may be used instead of
NSAIDs in heart failure as it does not
cause fluid retention
colchicine is used to prevent attacks
during the first 3–6 months of uratelowering treatment (longer treatment
may be needed if attacks continue or
if large tophi are present)
- Measure complete blood count
before using colchicine for prevention
of attacks; repeat after 1 and 6
months, then annually
c) Grades and Associated symptoms of an allergy
a. Mild Allergy Symptoms
i. Rash
ii. Itchy, watery eyes
iii. Congestion
iv. Mild allergic reactions do not spread to other parts of the body.
b. Moderate Allergy Symptoms
i. Itchiness
ii. Can spread to other parts of the body
iii. Difficulty breathing
c. Severe Allergy Symptoms (Anaphylaxis)
i. Anaphylaxis is a rare, life-threatening emergency in which the body's response to the allergen is
sudden and affects the whole body. Allergy symptoms may begin with sudden itching of the eyes
or face and within minutes progress to more serious symptoms, including:
ii. Varying degrees of swellings that can make breathing and swallowing difficult
iii.
iv.
v.
vi.
vii.
Abdominal pain
Cramps
Vomiting
Diarrhoea
Mental confusion or dizziness
d) Difference between immediate hypersensitivity reactions and delayed hypersensitivity reactions
a. Type I reactions (ie, immediate hypersensitivity reactions, anaphylaxis, asthma) involve
immunoglobulin E (IgE)–mediated release of histamine and other mediators from mast cells and
basophils.
b. Type II reactions (ie, cytotoxic hypersensitivity reactions, thrombocytopenia) involve IgG or IgM
antibodies bound to cell surface antigens, with subsequent complement fixation.
c. Type III reactions (ie, immune-complex reactions, RA) involve circulating antigen-antibody immune
complexes that deposit in postcapillary venules, with subsequent complement fixation. IgG and Comp
d. Type IV reactions (ie, delayed hypersensitivity reactions, cell-mediated immunity, contact dermatitis,
multiple sclerosis) are mediated by T cells rather than by antibodies
e. Which is more common? Immediate?
e) Should Mr Elric avoid any other medications in the future?
a. The rash experienced from Celebrex is possibly an allergic reaction to
sulphonamide group in the structure or celecoxib.
b. Although there’s not enough evidence to suggest the cross-reactivity between antibiotic sulphonamide
drus and non-antibiotic sulphonamide drug
f)
What is the most appropriate treatment for Mr Elric’s allergy?
a. Corticosteroids
g) What is the function of COX1 and COX2?
a. COX-1 is constitutive, maintaining normal cell function within the mucosa of many organs
b. COX-2 is an inducible enzyme, it is responsible for inflammation, pain and fever responses, but also a
have constitutive function like the protection of renal function
h) What are the clinical and molecular differences between a non-selective and selective COX2 inhibitor?
a. Selective COX-2 inhibitors are more bulky and can’t fit in COX-2. COX-2 has a side pocket which
provides extra room for these selective inhibitors to bind.
b. COX-2 inhibitors don’t affect the housekeeping PGs thus less GI side effects.
i)
Risk factors for gout:
a. Hyperuricaemia
b. High purine diet
c. Alcohol
d. Surgery
e. Joint trauma
f. Physical stress/strenuous exercise
g. Tight shoes, hiking (big toe)
h. Dieting
j)
Medications that are recommended for an acute gout attack:
a. NSAIDs
b. Colchicine
c. Corticosteroids
k) Which medications can be used in renal impairment?
a. Corticosteroids (eg. Prednisone)
l)
What medications should be avoided during an acute gout attack?
a. Diuretics
b. Aspirin?
m) What medications are recommended for maintenance gout?
a. Allopurinol
n) What will you tell Mr Elric about Colgout?
a. Take no more than 3 tablets for a course and don’t repeat it in less than 3 days.
b. Avoid alcohol
c. It is a short term treatment to relief the pain.
Scenario 2
i)
What does OD, OS and OU stand for?
a. OD = oculus dexter = right eye
b. OS = oculus sinister = left eye
c. OU = oculus uterque = both eyes
ii) What should be used in pharmacy instead of OD, OS and OU?
a. Right eye, Left eye, Both eyes
iii) What other medications beside Tenopt could be added to lower Mr Elric’s IOP
a. Carbonic anhydrase inhibitors
i. Brinzolamide (Azopt)
iv) How do these medications lower IOP?
a. Carbonic anhydrase inhibitors
i. Reduces HCO3- level  recudes Na+  stops the production of aqueous humour
b. B-blockers
i. Reduces aqueous humour production, probably by blockade of beta receptors on the ciliary
epithelium.
v) Is Tenopt the most appropriate glaucoma medication to give Mr Elric?
a. No, he’s on blood pressure lowering medication. Timolol is a β blocker, and due to its minor systemic
absorption, it might cause hypotension and bradycardia.
vi) Can carbonic anhydrase inhibitors be dispensed to a patient with an allergy to a sulphonamide medication?
a. Not recommended
vii) What does the product information for Azopt say regarding sulphonamide allergies?
a. Allergy to sulfonamides—may increase risk of allergy to carbonic anhydrase inhibitors.
viii) What are common side effects with brimonidine?
a. ocular irritation, ocular allergic reaction, conjunctival blanching, lid retraction, blepharitis, dry mouth and
nose, taste disturbance, fatigue, headache, drowsiness, dizziness
ix) How do you minimise side-effects from eye drops?
a. DOT technique
i. Don’t Open the Eyelids Technique
ii. Digital Occlusion of the Tear duct (3 mins)
x) What are possible causes for Mr Elric’s conjunctivitis?
a. Using expired eye drop – might have contaminated, either due to poor storage or wearing off of the
preservatives.
xi) How can you minimise microbial contamination when using eye drops?
a. Correct storage – store at room temperature
b. Light protection – opaque bottle, put in shades or dark cabinet.
xii) What will you tell Mr Elric about his new eye drops?
a. Review his technique
b. Tell him the importance of adherence to his medication
c. Emphasis the need to use the eye drops within their expiry date.