FOP resit past paper 2

Formoterol is a bronchodilator- Which receptor does it act on?

B2 adrenoceptor

In drug development, healthy volunteers are recruited to take part in:

Phase 1 trials

True of false, does L-NAME ihnhibit nitric oxoide synthase

True

Which inflammatory mediator has a role to play in maintaining daytime alertness in our circadian rhythm?

Histamine

Ipratropium and tiotropium are bronchodilators. Which receptor do they antagonise to mediate this effect?

M3 receptor

Acetylcholine is rapidly removed from the neuromuscular junction by:

acetylcholinesterase

Stimulation of the β₂ adrenoceptor on airway smooth muscle can be mediated by

formoterol, salbutamol

Parenteral administration includes the following:

intravenous, subcutaneous

Which of the following are true about serotonin receptors?

5-HT₂ receptor activation increases intracellular calcium,5-HT₄ receptor activation increases cAMP

Which of the following drugs block(s) bradykinin receptors?

icatibant

Where are H₁ receptors found?

in the brain, on blood vessel smooth muscle cells

M2 recptors are

Gi coupled, inhibitory and found in the heart

Describe the pros and cons of oral drug administration (first paragraph)

Oral drug administration is convenient and easy to use therefore will increase user compliance. It is safe and does not carry a risk of infection. Drugs can be formulated in many ways to allow the drug to have the desired time scale of effect, for example, drugs can have fast and slow release particles in a matric which will allow for rapid but sustained effects.

Describe the pros and cons of oral drug administration (second paragraph)

Oral drug administration has a slow onset of action (around 20-30 minutes) therefore is not suitable in an emergency situation. Not suitable for drugs which are broken down in the stomach ie peptides such as insulin.  Absorption can be affected by interactions with foods and other medications, blood flow to the GI tract and GI tract motility. Drugs are taken from the GI tract in the hepatic vein to the liver where they are metabolised. This is known as first pass metabolism and can limit the ability of drugs to be give orally.

Explain how nitric oxide (NO) controls blood vessel relaxation. Include how it is made, how it works in smooth muscle (6 marks), and give examples of drugs that affect this pathway (4 marks). first two bullet points

 

• Nitric oxide (NO) is an endothelium-derived relaxing factor. Plays a key role in controlling vascular tone.

• Synthesised in endothelial cells from L-arginine. Enzyme: endothelial nitric oxide synthase (eNOS). 

Explain how nitric oxide (NO) controls blood vessel relaxation. Include how it is made, how it works in smooth muscle (6 marks), and give examples of drugs that affect this pathway (4 marks). second 2 bullet points

• Stimuli: acetylcholine, shear stress.

• NO diffuses from endothelium into smooth muscle cells. Activates soluble guanylyl cyclase (sGC). Increases cyclic GMP (cGMP) levels. cGMP activates protein kinase G (PKG). PKG reduces intracellular calcium and activates myosin light chain phosphatase. Result: smooth muscle relaxation → vasodilation.

Explain how nitric oxide (NO) controls blood vessel relaxation. Include how it is made, how it works in smooth muscle (6 marks), and give examples of drugs that affect this pathway (4 marks). third 2 bullet points

• Stimuli: acetylcholine, shear stress.

• NO diffuses from endothelium into smooth muscle cells. Activates soluble guanylyl cyclase (sGC). Increases cyclic GMP (cGMP) levels. cGMP activates protein kinase G (PKG). PKG reduces intracellular calcium and activates myosin light chain phosphatase. Result: smooth muscle relaxation → vasodilation.

Explain how nitric oxide (NO) controls blood vessel relaxation. Include how it is made, how it works in smooth muscle (6 marks), and give examples of drugs that affect this pathway (4 marks). last bullet point

• NOS inhibitors (e.g., L-NAME) → experimentally reduce NO production → reduce relaxation.