2229604902 - Plag, Plag PHARMACEUTICS_ASSIGNMENT
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PHARMACEUTICS ASSIGNMENT
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PART 1
Fig 1: Chemical Formula of Diclofenac
Source: (
Shirasaka 2022).
Diclofenac is a popular pharmaceutical used to treat pain, decrease inflammation, and
manage a wide range of medical disorders since it is a nonsteroidal anti-inflammatory
drug (NSAID). It may be obtained either with a doctor's prescription or without. In this
article, we will cover the fundamentals of diclofenac:
What is Diclofenac?
Diclofenac is an NSAID that belongs to a family of pharmaceuticals known as
nonsteroidal anti-inflammatory drugs. Brand names like Voltaren and Cataflam
demonstrate its widespread availability.
What is it used for?
Diclofenac's primary function is to alleviate the pain and inflammation caused by a wide
range of medical disorders, such as:
Arthritis:
It is commonly prescribed for osteoarthritis and rheumatoid arthritis.
Pain Management:
Diclofenac is used to relieve pain from injuries, dental
procedures, and other sources (
Shirasaka 2022).
Menstrual Pain:
It can help alleviate menstrual cramps.
Migraines:
Diclofenac may be used for the treatment of migraine headaches.
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Ankylosing Spondylitis:
It is sometimes prescribed for this inflammatory
condition affecting the spine.
How does it work?
Diclofenac is effective because it reduces the formation of prostaglandins, which are
involved in inflammation and pain. Diclofenac helps relieve pain and inflammation by
decreasing levels of prostaglandins (
Heimbach 2023).
What chemical forms is it used as?
Diclofenac comes in many different chemical forms, such as sodium, potassium, and
epolamine. Each of these types may have somewhat different characteristics and
release rates (
Shirasaka 2022).
What dosage forms is it available in?
Diclofenac can be found in several dosage forms, including:
Tablets and Capsules:
These are the most common forms, taken orally with
water.
Topical Gels and Creams:
Diclofenac gel can be applied directly to the skin
over the affected area.
Topical Patches:
These adhesive patches are applied to the skin and provide a
slow release of the medication (
Chang 2023).
Injections:
Diclofenac can be administered as an injection, typically in a clinical
setting.
Because of the possibility of adverse effects and drug interactions, diclofenac should
only be used as prescribed by a doctor. Patients should carefully follow the dosage
directions stated in the package insert (
Cardot 2023).
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PART 2: Pharmacokinetics of Oral Diclofenac Administration
Fig 2: Pharmacokinetics of Oral Diclofenac
Source:
(Chang 2023).
Diclofenac passes through a range of pharmacokinetic processes as it makes its way
through the digestive system after being taken orally in the form of tablets, capsules, or
liquid. The drug's absorption and distribution in the body may be understood by learning
about these mechanisms (
Shirasaka 2022).
Oral Dosage Forms and Administration:
Because of how well it works when
taken orally, diclofenac is often used in this fashion. Drug release and absorption
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are both affected by the dose form (tablet, capsule, or liquid) used (
Ouyang
2022).
Oral Absorption:
Diclofenac enters the stomach after being taken orally. The
medicine may be affected by the stomach's acidic environment. Diclofenac has a
relatively low pKa of around 4, making it a mildly acidic medication. The non-
ionized, lipophilic version of diclofenac is more easily absorbed in the stomach
because of the acidic environment (pH 1-3). Absorption is facilitated by its pH
partition behaviour.
Stomach Acid Interaction:
Diclofenac is better absorbed through the gastric
mucosa because it is largely converted to its non-ionized, lipophilic form by the
acidic conditions in the stomach. This step is crucial for the effective absorption
of drugs (
Shirasaka 2022).
Absorption Site:
The small intestine is the main site of absorption for diclofenac.
After leaving the stomach, it travels via the duodenum and jejunum, where the
pH is more neutral, between 4 and 6. Diclofenac is readily absorbed through the
intestinal lining in this pH range because it is mostly in its non-ionized form.
Distribution:
Diclofenac, once ingested, is carried by the bloodstream to all parts
of the body. Its distribution is regulated by variables such as its lipid solubility
(Log P) and protein binding. Diclofenac is able to cross cell membranes and
reach its target tissues since it is somewhat lipid solubile (
Cardot 2023).
Metabolism:
The liver is the primary site for diclofenac metabolism, where it
undergoes oxidation and glucuronidation, among other routes. Metabolism leads
in the creation of numerous metabolites, including 4'-hydroxydiclofenac and 5-
hydroxydiclofenac. Both beneficial and harmful effects of the medicine may be
influenced by these metabolites.
Elimination:
The kidneys are responsible for the bulk of diclofenac and its
metabolite elimination. They are eliminated in the urine as conjugated
glucuronide and sulphate metabolites. Enterohepatic circulation, in which some
of the medication is reabsorbed by the intestines and carried back to the liver,
may occur in very low doses.
In summary, when diclofenac is administered orally and swallowed:
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It meets the acidic environment of the stomach, where it partly changes to its
non-ionized, lipophilic form, boosting absorption.
The small intestine has a more optimal pH for medication absorption, so that's
where most of it goes.
The liver's metabolism and the solubility of lipids in the body both have a role in
its circulation and removal (
Shirasaka 2022).
Healthcare providers may better manage patients' dosages and avoid harmful
medication interactions if they have a firm grasp on these pharmacokinetic processes.
Effective treatment results for patients taking diclofenac are reliant on both correct
delivery and selection of oral dose forms.
PART 3:
Depending on the patient's condition and the intended therapeutic impact, diclofenac
may be given via a variety of methods outside the oral route. Diclofenac also comes in
the following formulations and administration methods:
Topical Diclofenac Gel and Creams:
Diclofenac comes in both oral and topical
forms, the latter of which is applied topically to the skin over the afflicted region.
In situations of osteoarthritis or sports injuries, when pain and inflammation are
localised, these medications are often prescribed. The potential for
gastrointestinal adverse effects is reduced because to the localised action of
topical treatment (
Shirasaka 2022).
Transdermal Patches:
Transdermal patches containing diclofenac deliver the
medication into the bloodstream over time. They release diclofenac gradually
over a long period of time. Patients who endure stomach distress while taking
oral drugs or who have a personal preference for transdermal patches would
appreciate their convenience (
Heimbach 2023).
Intramuscular Injections:
In a medical environment, intramuscular injections of
diclofenac are possible. Patients who need immediate pain relief or who cannot
take oral drugs owing to nausea or vomiting often choose via this approach.
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Diclofenac intramuscular injections are very helpful for postoperative pain
management and the treatment of acute musculoskeletal disorders.
Intravenous (IV) Administration:
Intravenous administration of diclofenac is
possible in some circumstances, such as for the treatment of postoperative pain
at a medical facility. The quick onset of effect and precise dose control that IV
diclofenac provides make it an excellent choice for treating severe pain and
inflammation (
Prasad 2023).
Suppositories:
Suppositories containing diclofenac are intended for rectal use.
Patients who have gastrointestinal complications, such as bleeding or ulcers,
may benefit from these alternatives to oral medicine administration. Haemorrhoid
sufferers may get systemic pain relief via suppositories while also receiving
localised therapy (
Shirasaka 2022).
Eye Drops:
Inflammation and discomfort in the eye, including postoperative
ocular inflammation, may be treated with diclofenac eye drops. They are not
intended for consumption or application to any other area of the body save the
eyes.
Intradermal Injections:
For localised pain relief from disorders like tendinitis,
diclofenac may be injected intradermally directly into the afflicted joint or tissue
(
Cardot 2023).
The method and formulation used for a given patient will vary according on the nature
and severity of their medical condition, the intensity of their symptoms, and their
personal preferences and tolerances. Targeted relief, quick start of action, and less
systemic adverse effects are just a few of the benefits that may be realised by using a
variety of formulations and administration modalities. These considerations are taken
into account by healthcare providers when deciding how to effectively give diclofenac
for the patient's therapeutic benefit.
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References
Ahire, D.S., Heyward, S. and Prasad, B. (2023). Intestinal metabolism of diclofenac by
polymorphic UGT2B17 correlates with its highly variable pharmacokinetics and safety
across
populations.
Clinical
Pharmacology
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https://doi.org/10.1002/cpt.2907
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Eleftheria Tsakalozou, Mohamed, M.F., Polak, S. and Heimbach, T. (2023). Applications
of Modeling and Simulation Approaches in Support of Drug Product Development of
Oral Dosage Forms and Locally Acting Drug Products: a Symposium Summary.
The
AAPS Journal
, 25(6). doi:
https://doi.org/10.1208/s12248-023-00862-x
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Kambayashi, A. and Shirasaka, Y. (2022). Food effects on gastrointestinal physiology
and drug absorption.
Drug Metabolism and Pharmacokinetics
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Kiyota, T., Atsushi Kambayashi, Takagi, T. and Yamashita, S. (2022). Importance of
Gastric Secretion and the Rapid Gastric Emptying of Ingested Water along the Lesser
Curvature (‘Magenstraße’) in Predicting the In Vivo Performance of Liquid Oral Dosage
Forms in the Fed State Using a Modeling and Simulation.
Molecular Pharmaceutics
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19(2), pp.642–653. doi:
https://doi.org/10.1021/acs.molpharmaceut.1c00778
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Perlik, V., Kulasekaran, A., Coutinho, G., Votava, M. and Cardot, J.-M. (2023).
Relationship between Pharmacokinetic Profile and Clinical Efficacy Data of Three
Different Forms of Locally Applied Flurbiprofen in the Mouth/Throat.
Pharmaceutics
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Wang, W. and Ouyang, D. (2022). Opportunities and challenges of physiologically
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Drug Discovery Today
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