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17 Cards in this Set
- Front
- Back
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Why don't peptides work well as drugs? |
- They're hydrolysed in the intestines - They're difficult to manufacture - They're hydrolysed in plasma - They don't penetrate the blood brain barrier - They may be immunogenic |
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What is the mechanism of action and indication of icatibant? |
Icatibant is a bradykinin B2 antagonist used to treat angioedema |
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Bradykinin is important in the development of a certain side effect of a certain type of drug. Which drug and what is the side effect? |
Accumulation of bradykinin during ACE inhibitor treatment causes dry cough as a side effect. |
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Name two drugs which act on tachykinin receptors and their indications. |
Aprepitant and netupitant are NK1-receptor antagonists and have anti-emetic effect. |
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What are the name and indications of somatostatin analogues? |
Somatostatin analogues like octreotide are used to treat cancers that secrete any of the hormones that are inhibited by somatostatin. They’re also used to treat acromegaly, a condition characterised by too much growth hormone. |
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Name some drugs which act on the purinergic system and which receptors they act on. |
Theophylline, caffeine - antagonizes adenosine receptors Clopidogrel, prasugrel and ticlopidine - antagonize P2Y12 receptors. |
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What are the indications for P2Y12 antagonists? |
Antiplatelet therapy |
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What are the indications for adenosine receptor antagonists?
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Theophylline - COPD, asthma Caffeine - medical students |
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Describe the synthesis of nitric oxide (NO)
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NO is produced by arginine by the enzyme nitric oxide synthase (NOS) Three forms of NOS exist: endothelial NOS, neuronal NOS, inducible NOS |
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What is the function of endothelial NOS? |
Endothelial NO synthase is found in the endothelium and produces NO for use as a vasodilator |
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What is the function of neuronal NOS? |
Neuronal NO synthase (nNOS) is found in neurons and produces NO for use as a neurotransmitter |
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What is the function of inducible NOS? |
Inducible NO synthase (iNOS) is found in immune cells and produces NO in response to inflammation |
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Describe the signal transduction of NO
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NO diffuses across the cell membrane and activates soluble guanylyl cyclase. This increases the level of cGMP. |
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Name some drugs whose mechanism of action are related to NO |
Nitroprusside Organic nitrates Sildenafil Inhaled NO |
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What is the mechanism of action of nitroprusside? |
Nitroprusside is rapidly broken down into NO, which causes peripheral vasodilation. |
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What is the mechanism of action of organic nitrates?
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Organic nitrates are broken down into NO. They vasodilate the arterial circulation, decreasing the afterload of the heart, and they vasodilate the venous circulation, decreasing the preload. |
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What is the mechanism of action of sildenafil? |
Sildenafil is a phosphodiesterase 5 inhibitor. PDE inactivates cGMP, and so sildenafil increases the level of cGMP intracellularly. PDE5 is found on vessels in the corpus cavernosum. |
