Kidney Stones drugs (Ibuprofen and Tamsulosin) Flashcards
What is ibuprofen?
Ibuprofen is an NSAID and non-selective COX inhibitor used to treat mild-moderate pain, fever, and inflammation.
Why is ibuprofen considered to be a non selective inhibitor/antagonist?
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.
What is COX?
Cyclooxygenase (an enzyme)
What do COX-1 enzymes do?
Synthesises thromboxane (TxA2) which stimulates platelet aggregation and vasoconstriction.
What do COX-2 enzymes do?
Produces prostaglandins which play a role in natural bodily processes such as allowing us to feel pain and inflammation.
How might ibuprofen help with kidney stones? [FULL]
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.
What does ibuprofen inhibit?
inhibits COX-1 and COX-2 enzymes
What does NSAID stand for?
Non-steroidal anti-inflammatory drugs (NSAIDs)
What is an NSAID?
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.
What are the side effects of ibuprofen?
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
Why can ibuprofen cause side effects such as a stomach ulcer?
inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration
Whats the best website?
This:
https://go.drugbank.com/drugs/DB01050
How is ibuprofen administered?
Either a tablet or suspension (liquid), both to be taken by mouth.
Advantages of oral tablet administration?
- 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
Disadvantages of oral tablet administration?
- 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
Advantages of oral suspension liquid administration?
- 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
Disadvantages of oral suspension liquid administration?
- 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).
What is Tamsulosin?
A selective alpha-1a, alpha-1b and alpha-1d adrenoceptor antagonist used to treat benign prostatic hyperplasia, kidney stones, and female voiding dysfunction
What kind of drug is tamsulosin?
a selective alpha-1A, alpha-1B, and alpha-1D adrenergic receptor antagonist
What receptors does Tamsulosin work on?
alpha-1A, alpha-1B, and alpha-1D adrenergic receptors
Where does tamsulosin exert its greatest effect?
in the prostate and bladder, where alpha adrenergic receptors are most commonly found
Why does tamsulosin work so well in the prostate and bladder?
Because this is where alpha-1A, alpha-1B, and alpha-1D adrenergic receptors are most commonly found.
What happens when Tamsulosin inhibits the alpha-1A, alpha-1B, and alpha-1D adrenergic receptors/adrenoceptors?
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.
What are adrenergic receptors?
Adrenergic receptors (or Adrenoceptors) mediate the diverse effects of the neurotransmitters of the sympathetic nervous system, norepinephrine and epinephrine.
What are the two types of adrenergic receptor?
alpha and beta
What is an adrenoceptor also referred to as?
adrenoceptor = adrenergic receptor
Why is tamsulosin considered to be a selective drug?
It only targets alpha1 adrenoceptors, such as alpha1-A, alpha1-B and alpha1-D adrenoceptors. Doesn’t target any others such as beta adrenoceptors.
How does tamsulosin help kidney stones? [FULL]
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.
What happens when alpha1-d adrenoceptors are inhibited?
detrusor muscles of the bladder relax.
Where are detrusor muscles found?
in the bladder.
What is the detrusor muscle?
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.
Why does the bladder need the ability to stretch?
For maximal storage of urine.
Whats the half life of tamsulosin?
15 hours
Where is tamsulosin metabolised?
Metabolised in liver by P450
What are Cytochrome P450 Enzymes?
A family of proteins that play a key role in the metabolism of drugs.
Define metabolism (in regard to drugs)?
the metabolic breakdown of drugs by living organisms
How is tamsulosin administered?
oral
best website?
https://go.drugbank.com/drugs/DB00706
What are some side effects of tamsulosin?
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.
