Thyroid Pharmacology Flashcards
How many iodines does T3 and T4 have
- T3 : 3
- T4 : 4
Where are thyroid hormones stored
- in the colloid
Why would the treatment of someone with hyperthyroidism not work for the first 3-4 weeks
- the colloid storage units have a lot of thyroid hormones stored
- if the synthesis of TH is cut of the colloid can still release the thyroid hormones they have stored for a couple weeks
When is hypothalamus stimulated to release TRH
- when cold , stressed or due to trauma
MOA of Thyroid hormone (T3 & T4 )
- lipid soluble so they pass through cell membrane and bind to Thyroid Nuclear Receptor TR
- bind to hormone responsive elements in DNA
- change activity of RNA polymerase , gene transcription and translation of mRNA
What is the effect of Thyroid Hormone
- increase metabolic rate
- increase heat
- increase oxygen & caloric consumption
- increase heart rate
- effect GTH and CNS development
Signs of Hyperthyroidism (thyrotoxicosis )
1- nervous / edgy 2- shaky 3- palpitations 4- Heat intolerance 5- increased appetite 6- decreased weight 7 - manic levels of energy 8- tremor 9- sweaty / warm 10 - tachycardia 11- hyper refelxia
List the types of treatment for Hyperthyroidism and the pharmacological options
1- Surgical treatment is there’s tracheal compression , pharmacological if not
2- Drugs options :
- Block TH formation
- block & replace with artificial TH
- radioactive iodine kills thyroid = permanent hypothyroid
3 - symptomatic control
Is goitre a sign indicating hyperthyroidism
- no it does not indicate what type of thyroid problem there is
- blood tests are needed to see thyroid hormone levels
Explain what are block drugs and give examples
- prodrug that inhibits iodination of thyroxine residue in thyroglobulin
- thioureylenes : carbimazole
How are Thioureylenes administered, and how long does it take to work
- orally
- within 12 hours it inhibits 90% of iodination ( half life of 6-15 hours )
What is the block drug regimen for hyperthyroidism
- Carbimazole initially for 4-8 weeks ( 15-40 mg )
- gradually reduce Rx to maintenance level once TSH is normal
- maintenance level is 18 to 24 months
- after discontinue if TSH levels are normal
Adverse effects of Thioureylenes
- usually well tolerated
- common : rash, nausea and less energy
- rare: agranulocytosis ( have to warn the patient to report any infection symptoms once started on Carbimazole)
- lowest effect given to pregnant women as carbimazole can cross placenta
What drug is given during the first 4 weeks while patient on carbimazole due to stored thyroxine still being released and WHY
1- propranolol : non-selective beta blocker
- rapidly reliefs thyrotoxic symptoms
- inhibits T4 to T3 conversion
- improves palpitations , tremors , arrhythmias
What’s the one disadvantage of symptomatic relief drug for hyperthyroidism
- has to be taken orally 3 times a day