Diclofenac to happen much faster as the drug avoids

Diclofenac sodium can also be administered as
suppositories; this formulation will enter the body through the rectum and is
used for treating conditions such as pain and inflammation in rheumatic disease
including juvenile idiopathic arthritis, pain and inflammation in musculoskeletal
disorders, acute gout and postoperative pain (BNF, 2017). This formulation
allows the drug to dissolve and spread over the lining of the lower bowel; the
drug can then be absorbed into the blood where it is transported around the
body for systemic effect. This dosage form is a suitable way of administering
diclofenac as it allows absorption to happen much faster as the drug avoids the
first-pass metabolism and plentiful supply of blood into the rectum area. It
can also provide an alternative route to oral formulation; this is useful for
patients who have difficulties swallowing or feeling sick (Netdoctor, 2015).

Another dosage form of diclofenac sodium is tablets. These
type of medication are administered orally through the mouth of the patient.
This type of diclofenac sodium can be used for relieving pain and inflammation
in rheumatic disease including juvenile idiopathic arthritis, pain and inflammation
in musculoskeletal disorders, acute gout and postoperative pain (BNF, 2017). Diclofenac
sodium can be administered in two types of tablets; gastro-resistant and
modified-release tablets. Gastro-resistant tablets have an enteric coating,
which allows it to be absorbed in the intestine rather than in the stomach;
this type is suitable as it provides its beneficial effects and also reduces
the chance of stomach related side effects. modified-release tablets, this
means the drug has been modified to provide slow release of the drug, this is a
useful formulation for many reasons: The tablets are taken less often due to
the slow release meaning there is less chance of missing a dose, and due to the
slow release the concentration of drug in the body increases slowly and not
likely to go very high therefore reducing the possibility of unwanted side
effects (SwallowingDifficulties, no date).

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The gel (Voltarol ® Emulgel) is one dosage form of diclofenac
which is administered by applying the medication directly to the skin. This
type of diclofenac can be used by patients for musculoskeletal pain relief;
used for topical treatments, mostly for knee and hand osteoarthritis (BNF,
2017). Voltarol ® Emulgel provides topical treatment; this means that it works
by applying a thin layer of the gel to the skin over the affected area. The
drug is then absorbed from the surface of the skin into the underlying tissues targeting
inflammations at their source to relieve pain, decrease swells, reduce pain and
provide support for healing. This formulation can also lead to faster pain
relief as it can bypass first-pass metabolism and instead get absorbed much
faster through the skin, both these properties make topical treatments useful
for conditions such as pain in knee and hand osteoarthritis (Voltarol, 2017).

c)    Diclofenac
sodium is available as a gel (Voltarol® Emulgel), tablets and suppositories.
Using your BNF, identify an indication for each of these medicines, and justify
why this route of administration might be suitable for that condition. (50 %
marks)

 

As stated in answer 3.a. Gastro-resistant Diclofenac sodium
tablets are designed to go past the stomach unchanged and get broken down and
absorbed further down in the intestine to help reduce the gastrointestinal side
effects of the diclofenac sodium. Reducing the gastrointestinal side effects
are a fundamental property of this formulation of diclofenac sodium. Therefore,
the cautionary labels state that the diclofenac sodium gastro-resistant tablets
should never be crushed or chewed before swallowing; if the drug is chewed or
crushed the enteric coating of the drug is damaged and destroyed, thus the drug
is absorbed in the stomach, and the stomach related side effects of diclofenac
sodium can be suffered by the patient. Furthermore, another statement on the
cautionary label is that diclofenac sodium gastro-resistant tablets should not
be used while on indigestion medicines such as proton pump inhibitors
(antacids). This statement is due to the effect of antacids on stomach acidity;
antacids increase PH in the stomach making the conditions less acidic, as
answered in question 3.a. gastro-resistant drugs are designed to resist
stomachs acidic condition and break down and absorbed in areas of lower acidity
such as the intestine. Therefore, lowering the acidity in the stomach means
that diclofenac sodium gastro-resistant tablets can be broken down and absorbed
in the stomach, this means that the drug is released and absorbed too soon;
this would increase the chance of side effects concerning the stomach such as
stomach ulcers.

b)    Discuss the
reasons for the cautionary labels on gastro-resistant Diclofenac sodium. (40 %
marks)

 

Diclofenac sodium is present as gastro-resistant tablets to
help with three things. Protect the drug from the stomach and break it down
further down the gastrointestinal tract after the stomach, this is useful as it
allows diclofenac to resist breaking down in the acidic stomach and instead
break down to get absorbed and show their effects further down, e.g. in the
intestine. Lastly, it protects the stomach from the drug; this is significant
in reducing diclofenac’s gastrointestinal side effects such as stomach ulcers
and heartburn (SwallowingDifficulties, no date).

Gastro-resistant tablets are drugs that have an enteric
coating; this enteric coating protects the drug from dissolving in the stomach
acid and instead to dissolve further down the gastrointestinal tract, e.g. in
the intestine. Therefore, gastro-resistant tablets are said to be designed to
temporary withstand attacks by the stomach acid (Collins dictionary, 2018).

a)    Explain why
diclofenac sodium is formulated into gastro-resistant tablets. (10 % marks)

Diclofenac sodium is a non-steroidal anti-inflammatory drug
available as gastro-resistant (enteric) tablets. The cautionary labels state
that this medicine should not be chewed or crushed before swallowing and that
indigestion medicines (e.g. proton-pump inhibitors) should be avoided
beforehand.

Question 2.

 

 

 

 

 

 

 

 

 

 

As part of the counselling, I would provide for Mr B; I
would provide him information on direction of use for the medicine provided,
for example, when the medications should be taken. I will provide information
on the side effects caused by the medication he will be taking; give him
information on how to reduce the chance of suffering these unwanted side
effects and which rare side effects would require him to stop taking the
medications and ask for medical attention. I would also ensure that he is not
suffering from kidney disease, liver disease, heart failure, high blood
pressure or ulcers and if he is the general practitioner is informed about this
condition and has taken the precautionary actions such as regular blood tests
and check-ups. I would also ensure that he is not allergic to NSAIDs and not on
any other medications that interact with the provided NSAIDs such as blood
thinners. Finally, I will inform him about any precautionary and auxiliary
information he needs to be informed of (BootsWebMD, 2017).

Other general guides for reducing NSAIDs related side
effects would be to take one NSAIDs medication at a time, using simple
analgesics instead of NSAIDs if possible (SpinalHealthcare, 2018).

Reducing side effects caused by COX-2 specific drugs such
as celecoxib would be taking one NSAIDs medication at a time, not using the
drug for longer than required and using the lowest possible dosage effective
for the person. Taking oral doses of this medication with or after food, using
antacids while on these treatments; both these methods help to reduce side effects
such as heartburns (SpinalHealthcare, 2018).

To minimise and reduce the gastrointestinal side effects
caused by NSAIDs, which inhibit both COX-1 and COX-2 enzymes e.g. Diclofenac,
healthcare professionals look at who the patient is and if they have any
medical conditions that increase the risk of NSAID related side effects. For
example, patients over the age of 75, have history of ulcers, require high dose
of NSAIDs, use more than one NSAIDs or have a severe disease such as Kidney
disease, liver disease, history of heart failure, stroke or heart attack and
high blood pressure would be at a higher risk of suffering from NSAIDs related
gastrointestinal ulcers. Therefore, NSAIDs would be provided with greater
precautions and more regular check-ups. Healthcare professionals also need to
decide which Method and time of administration of NSAIDs is most useful for a
specific patient to reduce the side effects caused by NSAIDs, for example,
using gastro-protective agents, e.g. Omeprazole (antacid) while on NSAIDs
treatment, this helps to reduce the risk of side effects related to the
intestine and the stomach. Other methods would be to take oral dosage forms
with or after food or with milk to help reduce the stomach and intestine
related side effects, avoid drinking alcohol as alcohol can cause irritations
for the stomach, drinking lots of water and fluids in order to replace the
water lost if suffering from diarrhoea due the NSAIDs related side effects, and
also avoiding diets with high-calorie intake (SpinalHealthcare, 2018).

Most frequent side effects that can be caused by NSAIDs are
stomach and intestinal problems (pain, indigestion, constipation, diarrhoea,
stomach ulcers, nausea and heartburn), problems with kidney function and
anaemia. If the named side effects continue for a few days, the patient should
contact the healthcare provider, and the NSAIDs treatment may be stopped. Occasional
side effects caused by NSAIDs are dizziness, vertigo (problems with balance),
mild headache and increase in blood pressure. Again if these symptoms continue
for more than a few days, the patient should stop taking the NSAID and contact
their healthcare provider for more instructions. Some side effects are rare,
but if these are present in the patients, they must contact their healthcare
provider immediately. Few examples of these side effects are severe pain
(stomach, chest, back and head), rapid heartbeat, bloody or black stools,
bloody or cloudy urine and blood in vomit (ClevelandClinic, 2016).

Like any other drug, NSAIDs also have many side effects,
which can affect people who are using them. Side effects are more likely to
take place if the patient is using NSAIDs at a high dose and also if the
patient has been taking NSAIDs for a long time. Some side effects are mild and
can be minimised, but some are serious and could require medical attention.

c)    Describe the
side effects caused by non-steroidal anti-inflammatory drugs (NSAIDs) and how
these side effects can be kept to a minimum. 
Refer more than one NSAID to illustrate your answer and mention any
counselling you would provide to Mr B. (60% of marks)

 

Diclofenac and Celecoxib are both NSAIDs and show the same
analgesic, antipyretic and anti-inflammatory properties effects. The difference
between their actions are that Diclofenac inhibits both COX-1 and COX-2 enzymes
but Celecoxib is a COX-2 specific inhibitor and has no inhibitory effect on the
COX-1 enzyme.

COX-2 is said to be an inducible enzyme; this enzyme is
activated and used in site of injury in a large variety of tissues, an example
of these tissues are vascular endothelium and rheumatoid synovial endothelial
cells causing inflammation, pain, pyrexia and cancerous responses. Increase in
the COX-2 enzyme due to an injury or an inflammatory process will trigger the
hyper synthesis of pro-inflammatory prostaglandins, these prostaglandin
synthesised by COX-2 are responsible for inflammation and pain during an
injury. Even though COX-2 is mostly regarded as an inducible enzyme studies
show that it has some constitutive (regulatory) roles such as reproduction, resorption
and neurotransmission (Osafo et al, 2017).

COX-1 is said to be a constitutively in the majority of the
mammalian cells and tissues, for example, endothelium, seminal vesicles and
platelets. While at rest COX-1 performs continuous regulatory processes called
‘housekeeping duties’. Prostaglandins synthesised by COX-1 enzymes are
responsible for the production of platelets, mucus production and therefore
protection of stomach, intestine and renal lining by mucus. Molecular studies
show us that mRNA and protein expression of COX-1 does not change during an
inflammatory condition; this confirms that COX-1 does not have a significant
role in inflammation (Osafo et al, 2017).

Most evidence available on non-steroidal anti-inflammatory
drugs (NSAIDs) suggests that the primary mechanism of action for NSAIDs is
inhibition of cyclooxygenase (COX) enzymes, these enzymes are also known as
prostaglandin endoperoxide H synthase (PGHS) and exist in two isoforms (PGHS-1/
COX-1) or (PGHS-2/ COX-2); the two isoforms are significantly distinct in
regards to their structure as they are coded for by different genes, but the
two isoforms are membrane bound glycol proteins (a protein attached to a
carbohydrate) that can catalyse conversion of arachidonic acid to prostanoid.
Therefore, inhibition of COX enzymes also inhibits synthesis of eicosanoids
such as prostaglandin and thromboxane giving NSAIDs their analgesic,
antipyretic and anti-inflammatory properties (Osafo et al, 2017).

b)    Describe the
mode of action of non-steroidal anti-inflammatory drugs (NSAIDs) explaining the
difference between the action of Diclofenac and Celecoxib.  (30% of marks)

 

Most drugs are designed in a way to bring in their effect
by interaction with specific targets such as proteins; an example of these
target proteins are enzymes (Biological catalysts which increase the rate of
conversion of a specific substrate to a product), drugs use enzymes as their
target due to their importance of their role in human body; such as catalysing
important biological reactions. When drugs bind to enzymes, they can create their
effect by changing the way an enzyme works; an example of this would be a drug
inhibiting an enzyme, this means that the substrate is not able to bind to the
enzyme and products are not synthesised. Therefore, we can say that enzymes are
the targets in drug actions and a drug can release its effects by binding to
enzymes (Silverman and Holladay, 2015).

a)    Explain what is
meant by enzyme targets in drug action. (10% of marks)   

Clinical scenario: For the last 6 months, Mr B (age 52)
has been taking prescribed Diclofenac tablets 50mg twice a day to help relieve
the pain caused by his osteoarthritis.  He
started to experience mild indigestion, so the prescriber has changed his medication
to Celecoxib 200mg daily.  Mr B is
concerned about the side effects of these drugs

Question
1.

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I'm Jamie!

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