Kidney Stones drugs (Ibuprofen and Tamsulosin)

Question 1

What is ibuprofen?

Answer 1

Ibuprofen is an NSAID and non-selective COX inhibitor used to treat mild-moderate pain, fever, and inflammation.

Question 2

Why is ibuprofen considered to be a non selective inhibitor/antagonist?

Answer 2

It inhibits all types of COX enzyme including both COX-1 AND COX-2. Ibuprofen doesn’t just work on a SINGLE SPECIFIC type of COX enzyme, but works on ALL types of them.

Question 3

What is COX?

Answer 3

Cyclooxygenase (an enzyme)

Question 4

What do COX-1 enzymes do?

Answer 4

Synthesises thromboxane (TxA2) which stimulates platelet aggregation and vasoconstriction.

Question 5

What do COX-2 enzymes do?

Answer 5

Produces prostaglandins which play a role in natural bodily processes such as allowing us to feel pain and inflammation.

Question 6

How might ibuprofen help with kidney stones? [FULL]

Answer 6

Ibuprofen inhibits COX-1 and COX-2 enzymes. This decreases the synthesis of prostaglandins (which are involved in mediating pain and fever), which thereby relieves pain caused by the kidney stones. This also decreases the synthesis of thromboxane, preventing vasoconstriction, causing vasodilation instead, causing the ureter to widen, allowing the kidney stone to more easily pass through the ureter, into the bladder, and be expelled along with urine.

Question 7

What does ibuprofen inhibit?

Answer 7

inhibits COX-1 and COX-2 enzymes

Question 8

What does NSAID stand for?

Answer 8

Non-steroidal anti-inflammatory drugs (NSAIDs)

Question 9

What is an NSAID?

Answer 9

They’re medicines that are widely used to relieve pain, reduce inflammation, and bring down a high temperature. They’re often used to relieve symptoms of: headaches, painful periods, sprains and strains.

Question 10

What are the side effects of ibuprofen?

Answer 10

nausea or vomiting
constipation or diarrhoea
indigestion (dyspepsia) or abdominal pain
headache or dizziness
bloating (fluid retention)
raised blood pressure
inflammation of the stomach (gastritis)
a stomach ulcer
allergic reactions – such as a rash
worsening of asthma symptoms by causing narrowing of the airways (bronchospasm)
kidney failure
black stools and blood in your vomit – this can indicate bleeding in your stomach

Question 11

Why can ibuprofen cause side effects such as a stomach ulcer?

Answer 11

inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration

Question 12

Whats the best website?

Answer 12

This:
https://go.drugbank.com/drugs/DB01050

Question 13

How is ibuprofen administered?

Answer 13

Either a tablet or suspension (liquid), both to be taken by mouth.

Question 14

Advantages of oral tablet administration?

Answer 14

• Convenient, so people are more likely to adhere
• Easy to take, so people are more likely to adhere.
• Relatively cheap, not expensive
• Not invasive - no need for surgery - safe method of administration - money saved by NHS

Question 15

Disadvantages of oral tablet administration?

Answer 15

• People who are nil by mouth or have phobia of tablets wont adhere (in this case, other methods of administration would have to be considered).
• Difficult to administer to children
• Potentially easy to forget to take the medication.
• Takes longer for effects to start than drugs given intravenously

Question 16

Advantages of oral suspension liquid administration?

Answer 16

• Easier to give to children or elderly because the liquid can have a flavour, so it doesn’t taste bad, so the recipient is more likely to take it.
• Convenient, so people are more likely to adhere
• Easy to take, so people are more likely to adhere.
• Not invasive - no need for surgery - safe method of administration - money saved by NHS

Question 17

Disadvantages of oral suspension liquid administration?

Answer 17

• Potentially easy to forget to take the medication.
• People who are nil by mouth wont adhere (in this case, other methods of administration would have to be considered).

Question 18

What is Tamsulosin?

Answer 18

A selective alpha-1a, alpha-1b and alpha-1d adrenoceptor antagonist used to treat benign prostatic hyperplasia, kidney stones, and female voiding dysfunction

Question 19

What kind of drug is tamsulosin?

Answer 19

a selective alpha-1A, alpha-1B, and alpha-1D adrenergic receptor antagonist

Question 20

What receptors does Tamsulosin work on?

Answer 20

alpha-1A, alpha-1B, and alpha-1D adrenergic receptors

Question 21

Where does tamsulosin exert its greatest effect?

Answer 21

in the prostate and bladder, where alpha adrenergic receptors are most commonly found

Question 22

Why does tamsulosin work so well in the prostate and bladder?

Answer 22

Because this is where alpha-1A, alpha-1B, and alpha-1D adrenergic receptors are most commonly found.

Question 23

What happens when Tamsulosin inhibits the alpha-1A, alpha-1B, and alpha-1D adrenergic receptors/adrenoceptors?

Answer 23

By blocking these adrenoceptors in the bladder and prostate, smooth muscle in the prostate is relaxed and urinary flow is improved. The blocking of alpha-1D adrenoceptors relaxes the detrusor muscles of the bladder which prevents storage symptoms.

Question 24

What are adrenergic receptors?

Answer 24

Adrenergic receptors (or Adrenoceptors) mediate the diverse effects of the neurotransmitters of the sympathetic nervous system, norepinephrine and epinephrine.

Question 25

What are the two types of adrenergic receptor?

Answer 25

alpha and beta

Question 26

What is an adrenoceptor also referred to as?

Answer 26

adrenoceptor = adrenergic receptor

Question 27

Why is tamsulosin considered to be a selective drug?

Answer 27

It only targets alpha1 adrenoceptors, such as alpha1-A, alpha1-B and alpha1-D adrenoceptors. Doesn’t target any others such as beta adrenoceptors.

Question 28

How does tamsulosin help kidney stones? [FULL]

Answer 28

By blocking the alpha1 adrenoceptors such as alpha1-A, alpha1-B and alpha1-D, smooth muscle in the bladder, and prostate relaxes, causing the ureter and urethra to widen, thereby improving urine flow. For example, when alpha1-D receptors are inhibited, the detrusor muscles of the bladder relax. This allows the kidney stone(s) to pass and be expelled more easily through the ureter, out of the bladder and through the urethra along with urine.

Question 29

What happens when alpha1-d adrenoceptors are inhibited?

Answer 29

detrusor muscles of the bladder relax.

Question 30

Where are detrusor muscles found?

Answer 30

in the bladder.

Question 31

What is the detrusor muscle?

Answer 31

The detrusor muscle is a collection of smooth muscle fibres which are oriented in many different directions. These allow the bladder to stretch in response to the presence of urine. During urination, the detrusor muscle contracts to push urine out of the bladder and into the urethra, before it is expelled.

Question 32

Why does the bladder need the ability to stretch?

Answer 32

For maximal storage of urine.

Question 33

Whats the half life of tamsulosin?

Answer 33

15 hours

Question 34

Where is tamsulosin metabolised?

Answer 34

Metabolised in liver by P450

Question 35

What are Cytochrome P450 Enzymes?

Answer 35

A family of proteins that play a key role in the metabolism of drugs.

Question 36

Define metabolism (in regard to drugs)?

Answer 36

the metabolic breakdown of drugs by living organisms

Question 37

How is tamsulosin administered?

Answer 37

oral

Question 38

best website?

Answer 38

https://go.drugbank.com/drugs/DB00706

Question 39

What are some side effects of tamsulosin?

Answer 39

sleepiness.
nausea.
difficulty falling asleep or staying asleep.
weakness.
back pain.
diarrhea.
runny or stuffy nose.
pain or pressure in the face.
sore throat, cough, fever, chills, or other signs of infection.